ATE520403T1 - N-ä3-fluoro-4-(ä6-(methyloxy)-7-ä(3-morpholin-4 ylpropyl)oxyüquinolin-4-ylüoxy)phenylü-n'-(4- fluorophenyl)cyclopropane-1,1-dicarboxamid zur behandlung von krebs - Google Patents

N-ä3-fluoro-4-(ä6-(methyloxy)-7-ä(3-morpholin-4 ylpropyl)oxyüquinolin-4-ylüoxy)phenylü-n'-(4- fluorophenyl)cyclopropane-1,1-dicarboxamid zur behandlung von krebs

Info

Publication number
ATE520403T1
ATE520403T1 AT10160517T AT10160517T ATE520403T1 AT E520403 T1 ATE520403 T1 AT E520403T1 AT 10160517 T AT10160517 T AT 10160517T AT 10160517 T AT10160517 T AT 10160517T AT E520403 T1 ATE520403 T1 AT E520403T1
Authority
AT
Austria
Prior art keywords
compounds
ylüoxy
phenylü
oxyüquinolin
ylpropyl
Prior art date
Application number
AT10160517T
Other languages
English (en)
Inventor
Lynne Canne Bannen
Diva Sze-Ming Chan
Jeff Chen
Lisa Esther Dalrymple
Timothy Patrick Forsyth
Tai Phat Huynh
Vasu Jammalamadaka
Richard George Khoury
James William Leahy
Morrison B Mac
Grace Mann
Larry W Mann
John M Nuss
Jason Jevious Parks
Craig Stacy Takeuchi
Yong Wang
Wei Xu
Original Assignee
Exelixis Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=34397024&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=ATE520403(T1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Exelixis Inc filed Critical Exelixis Inc
Application granted granted Critical
Publication of ATE520403T1 publication Critical patent/ATE520403T1/de

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/20—Oxygen atoms
    • C07D215/22—Oxygen atoms attached in position 2 or 4
    • C07D215/233—Oxygen atoms attached in position 2 or 4 only one oxygen atom which is attached in position 4
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/20—Oxygen atoms
    • C07D215/22—Oxygen atoms attached in position 2 or 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/36—Sulfur atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/38—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/38—Nitrogen atoms
    • C07D215/42—Nitrogen atoms attached in position 4
    • C07D215/46—Nitrogen atoms attached in position 4 with hydrocarbon radicals, substituted by nitrogen atoms, attached to said nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/88—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/94—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/14—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D295/145—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C07D295/15—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
    • C12Q1/00—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
    • C12Q1/48—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving transferase
    • C12Q1/485—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving transferase involving kinase
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2500/00—Screening for compounds of potential therapeutic value
    • G01N2500/04—Screening involving studying the effect of compounds C directly on molecule A (e.g. C are potential ligands for a receptor A, or potential substrates for an enzyme A)
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Zoology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Wood Science & Technology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Microbiology (AREA)
  • Biotechnology (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Analytical Chemistry (AREA)
  • Physics & Mathematics (AREA)
  • General Engineering & Computer Science (AREA)
  • Genetics & Genomics (AREA)
  • Ophthalmology & Optometry (AREA)
  • Urology & Nephrology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
AT10160517T 2003-09-26 2004-09-24 N-ä3-fluoro-4-(ä6-(methyloxy)-7-ä(3-morpholin-4 ylpropyl)oxyüquinolin-4-ylüoxy)phenylü-n'-(4- fluorophenyl)cyclopropane-1,1-dicarboxamid zur behandlung von krebs ATE520403T1 (de)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US50618103P 2003-09-26 2003-09-26
US53537704P 2004-01-09 2004-01-09
US57738404P 2004-06-04 2004-06-04

Publications (1)

Publication Number Publication Date
ATE520403T1 true ATE520403T1 (de) 2011-09-15

Family

ID=34397024

Family Applications (3)

Application Number Title Priority Date Filing Date
AT10160517T ATE520403T1 (de) 2003-09-26 2004-09-24 N-ä3-fluoro-4-(ä6-(methyloxy)-7-ä(3-morpholin-4 ylpropyl)oxyüquinolin-4-ylüoxy)phenylü-n'-(4- fluorophenyl)cyclopropane-1,1-dicarboxamid zur behandlung von krebs
AT04789057T ATE532782T1 (de) 2003-09-26 2004-09-24 C-met-modulatoren und anwendungsverfahren
AT10160518T ATE517091T1 (de) 2003-09-26 2004-09-24 C-met-modulatoren und verwendungsverfahren

Family Applications After (2)

Application Number Title Priority Date Filing Date
AT04789057T ATE532782T1 (de) 2003-09-26 2004-09-24 C-met-modulatoren und anwendungsverfahren
AT10160518T ATE517091T1 (de) 2003-09-26 2004-09-24 C-met-modulatoren und verwendungsverfahren

Country Status (20)

Country Link
US (14) US9174947B2 (de)
EP (9) EP1673085B1 (de)
JP (14) JP4638436B2 (de)
AT (3) ATE520403T1 (de)
AU (3) AU2004275842B2 (de)
BE (1) BE2014C055I2 (de)
CA (2) CA2537812C (de)
CY (3) CY1111956T1 (de)
DK (4) DK2213661T3 (de)
ES (6) ES2651730T3 (de)
FR (1) FR14C0067I2 (de)
HK (5) HK1141799A1 (de)
HR (4) HRP20110707T1 (de)
HU (1) HUS1400052I1 (de)
LU (1) LU92508I2 (de)
NL (1) NL300678I2 (de)
PL (3) PL2210607T3 (de)
PT (2) PT2213661E (de)
SI (4) SI2392564T1 (de)
WO (1) WO2005030140A2 (de)

Families Citing this family (263)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU9598601A (en) 2000-10-20 2002-04-29 Eisai Co Ltd Nitrogenous aromatic ring compounds
JPWO2004080462A1 (ja) 2003-03-10 2006-06-08 エーザイ株式会社 ｃ−Ｋｉｔキナーゼ阻害剤
ES2279441T3 (es) 2003-09-19 2007-08-16 Astrazeneca Ab Derivados de quinazolina.
EP1673085B1 (de) * 2003-09-26 2011-11-09 Exelixis, Inc. C-met-modulatoren und anwendungsverfahren
JP4303726B2 (ja) 2003-11-11 2009-07-29 エーザイ・アール・アンド・ディー・マネジメント株式会社 ウレア誘導体およびその製造方法
US7767670B2 (en) * 2003-11-13 2010-08-03 Ambit Biosciences Corporation Substituted 3-carboxamido isoxazoles as kinase modulators
JP2007518823A (ja) * 2004-01-23 2007-07-12 アムゲン インコーポレイテッド キノリン、キナゾリン、ピリジン、及びピリミジン化合物と炎症、血管新生、及び癌に対する治療におけるそれら化合物の用途
KR100799535B1 (ko) 2004-02-27 2008-01-31 에자이 알앤드디 매니지먼트 가부시키가이샤 신규 피리딘 유도체 및 피리미딘 유도체(2)
NZ588139A (en) 2004-04-08 2012-02-24 Targegen Inc 7-Aryl-3-arylamino-benzo[1,2,4]triazine derivatives
PL382308A1 (pl) 2004-08-25 2007-08-20 Targegen, Inc. Związki heterocykliczne i sposoby stosowania
WO2006030826A1 (ja) 2004-09-17 2006-03-23 Eisai R & D Management Co., Ltd. 医薬組成物
MX2007003318A (es) 2004-09-20 2007-05-18 Xenon Pharmaceuticals Inc Derivados heterociclicos y su uso como agentes terapeuticos.
WO2006034440A2 (en) 2004-09-20 2006-03-30 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as stearoyl-coa desaturase inhibitors
AR051093A1 (es) 2004-09-20 2006-12-20 Xenon Pharmaceuticals Inc Derivados heterociclicos y su uso como inhibidores de estearoil-coa desaturasa
WO2006034441A1 (en) 2004-09-20 2006-03-30 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as stearoyl-coa desaturase inhibitors
JP5043668B2 (ja) 2004-09-20 2012-10-10 ゼノン・ファーマシューティカルズ・インコーポレイテッド 複素環誘導体および治療薬としてのそれらの使用
TW200626155A (en) 2004-09-20 2006-08-01 Xenon Pharmaceuticals Inc Heterocyclic derivatives and their use as therapeutic agents
TW200626572A (en) 2004-09-20 2006-08-01 Xenon Pharmaceuticals Inc Heterocyclic derivatives and their use as therapeutic agents
CN101072758B (zh) 2004-10-12 2013-07-31 阿斯利康(瑞典)有限公司 喹唑啉衍生物
US7652009B2 (en) 2004-11-30 2010-01-26 Amgem Inc. Substituted heterocycles and methods of use
EP1674466A1 (de) * 2004-12-27 2006-06-28 4Sc Ag 2,5- und 2-6-disubstituierte Benzazol-Derivate zur Verwendung als Protein Kinase Inhibitoren
US7576090B2 (en) * 2004-12-27 2009-08-18 4Sc Ag Benzazole analogues and uses thereof
JO2787B1 (en) 2005-04-27 2014-03-15 امجين إنك, Alternative amide derivatives and methods of use
US8093264B2 (en) * 2005-05-20 2012-01-10 Methylgene Inc. Fused heterocycles as inhibitors of VEGF receptor and HGF receptor signaling
KR20080026562A (ko) * 2005-06-02 2008-03-25 갤럭시 바이오테크, 엘엘씨 항체를 이용한 뇌종양 치료 방법
MX2007015216A (es) 2005-06-03 2008-02-22 Xenon Pharmaceuticals Inc Derivados de aminotiazol y sus usos como agentes terapeuticos.
JP4989476B2 (ja) 2005-08-02 2012-08-01 エーザイ・アール・アンド・ディー・マネジメント株式会社 血管新生阻害物質の効果を検定する方法
WO2007023768A1 (ja) 2005-08-24 2007-03-01 Eisai R & D Management Co., Ltd. 新規ピリジン誘導体およびピリミジン誘導体（３）
TW200804345A (en) 2005-08-30 2008-01-16 Novartis Ag Substituted benzimidazoles and methods of preparation
WO2007033196A1 (en) 2005-09-14 2007-03-22 Bristol-Myers Squibb Company Met kinase inhibitors
WO2007061127A1 (ja) * 2005-11-22 2007-05-31 Eisai R & D Management Co., Ltd. 多発性骨髄腫に対する抗腫瘍剤
CA2636242A1 (en) * 2006-01-30 2008-05-29 Array Biopharma, Inc. Heterobicyclic thiophene compounds and methods of use
UY30183A1 (es) 2006-03-02 2007-10-31 Astrazeneca Ab Derivados de quinolina
AU2007224020A1 (en) 2006-03-07 2007-09-13 Array Biopharma Inc. Heterobicyclic pyrazole compounds and methods of use
AR059922A1 (es) * 2006-04-01 2008-05-07 Galaxy Biotech Llc Anticuerpos monoclonales humanizados para el factor de crecimiento de hepatocitos
US7553854B2 (en) * 2006-04-19 2009-06-30 Novartis Vaccines And Diagnostics, Inc. 6-O-substituted benzoxazole and benzothiazole compounds and methods of inhibiting CSF-1R signaling
RU2448708C3 (ru) 2006-05-18 2017-09-28 Эйсай Ар Энд Ди Менеджмент Ко., Лтд. Противоопухолевое средство против рака щитовидной железы
UA92083C2 (ru) 2006-05-19 2010-09-27 Эбботт Леборетриз Азабициклические алкановые производные, замещенные конденсированным бициклогетероциклом
WO2008035209A2 (en) * 2006-05-30 2008-03-27 Methylgene Inc. Inhibitors of protein tyrosine kinase activity
JP2009539878A (ja) * 2006-06-08 2009-11-19 アレイ バイオファーマ、インコーポレイテッド キノリン化合物および使用方法
US7683060B2 (en) 2006-08-07 2010-03-23 Incyte Corporation Triazolotriazines as kinase inhibitors
CA2661333C (en) 2006-08-23 2014-08-05 Eisai R&D Management Co., Ltd. Salt of phenoxypyridine derivative or crystal thereof and process for producing the same
EP2065372B1 (de) 2006-08-28 2012-11-28 Eisai R&D Management Co., Ltd. Antitumormittel gegen undifferenzierten magenkrebs
US7790885B2 (en) 2006-08-31 2010-09-07 Eisai R&D Management Co., Ltd. Process for preparing phenoxypyridine derivatives
ES2555803T3 (es) 2006-10-23 2016-01-08 Cephalon, Inc. Fusión de derivados bicíclicos 2,4-diaminopirimidina como utilizar inhibidores ALK y c-Met
WO2008049855A2 (en) * 2006-10-27 2008-05-02 Glaxo Group Limited 7-azaindole derivatives as c-met kinase inhibitors
CN101641093B (zh) 2006-11-22 2013-05-29 因塞特公司 作为激酶抑制剂的咪唑并三嗪和咪唑并嘧啶
CA2672438A1 (en) * 2006-12-20 2008-07-03 Amgen Inc. Substituted heterocycles and methods of use
AU2007338795B2 (en) * 2006-12-20 2012-07-19 Amgen Inc. Substituted heterocycles and methods of use
CA2675755C (en) * 2007-01-19 2015-10-06 Xcovery, Inc. Pyridine and pyridazine derivatives as kinase inhibitors
WO2008093855A1 (ja) 2007-01-29 2008-08-07 Eisai R & D Management Co., Ltd. 未分化型胃癌治療用組成物
AU2008254425A1 (en) * 2007-05-21 2008-11-27 Novartis Ag CSF-1R inhibitors, compositions, and methods of use
DE102007026341A1 (de) 2007-06-06 2008-12-11 Merck Patent Gmbh Benzoxazolonderivate
TW200922581A (en) 2007-08-15 2009-06-01 Glaxo Group Ltd Compounds
WO2009026717A1 (en) 2007-08-29 2009-03-05 Methylgene Inc. Inhibitors of protein tyrosine kinase activity
WO2009060945A1 (ja) 2007-11-09 2009-05-14 Eisai R & D Management Co., Ltd. 血管新生阻害物質と抗腫瘍性白金錯体との併用
JP2009132660A (ja) 2007-11-30 2009-06-18 Eisai R & D Management Co Ltd 食道癌治療用組成物
KR101608096B1 (ko) 2008-01-23 2016-03-31 브리스톨-마이어스 스큅 컴퍼니 ４-피리디논 화합물 및 암을 위한 그의 용도
EP2268623B9 (de) 2008-03-17 2018-02-28 Ambit Biosciences Corporation Chinazolinderivate als raf-kinasemodulatoren und verwendungsverfahren
ES2423851T3 (es) 2008-04-10 2013-09-24 Taiho Pharmaceutical Co., Ltd. Compuesto de aciltiourea o sal del mismo y uso del mismo
JP5746015B2 (ja) * 2008-04-16 2015-07-08 マックス プランク ゲゼルシャフト ツゥアー フェデルゥン デル ヴィッセンシャフテン エー フォー Ａｘｌキナーゼ阻害剤としてのキノリン誘導体
UY31800A (es) * 2008-05-05 2009-11-10 Smithkline Beckman Corp Metodo de tratamiento de cancer usando un inhibidor de cmet y axl y un inhibidor de erbb
DK2300455T3 (en) 2008-05-21 2017-10-30 Incyte Holdings Corp SALTS OF 2-FLUORO-N-METHYL-4- [7- (QUINOLIN-6-YL-METHYL) - IMIDAZO [1,2-B] [1,2,4] TRIAZIN-2-YL] BENZAMIDE AND PROCEDURES WITH THE PREPARATION THEREOF
AU2009271003A1 (en) 2008-07-14 2010-01-21 Gilead Sciences, Inc. Imidazolylpyrimidine compounds as HDAC and/or CDK inhibitors
NZ590320A (en) 2008-07-14 2012-12-21 Gilead Sciences Inc Fused heterocyclyc inhibitors of histone deacetylase and/or cyclin-dependent kinases
EP2303841A1 (de) 2008-07-14 2011-04-06 Gilead Sciences, Inc. Oxindolylhemmerverbindungen
EP2149565A1 (de) * 2008-07-24 2010-02-03 Bayer Schering Pharma AG Sulfonsubstituierte Chinazolinderivate als Immunmodulatoren zur Behandlung von enzündlichen und allergischen Erkrankungen
CN102123987A (zh) 2008-07-28 2011-07-13 吉里德科学公司 亚环烷基和亚杂环烷基组蛋白脱乙酰酶抑制剂化合物
UY32142A (es) * 2008-09-26 2010-05-31 Smithkline Beckman Corp Preparación de una quinoliniloxidifenilciclopropanodicarboxamida
AU2009303602B2 (en) * 2008-10-14 2012-06-14 Sunshine Lake Pharma Co., Ltd. Compounds and methods of use
CA2742007C (en) * 2008-10-29 2014-07-08 Deciphera Pharmaceuticals, Llc Cyclopropane amides and analogs exhibiting anti-cancer and anti-proliferative activities
CA2743416A1 (en) * 2008-11-13 2010-05-20 Exelixis Inc. Methods of preparing quinoline derivatives
EP2367795A1 (de) * 2008-12-04 2011-09-28 Exelixis, Inc. Verfahren zur herstellung von chinolinderivaten
DE102009003975A1 (de) 2009-01-07 2010-07-08 Merck Patent Gmbh Benzothiazolonderivate
TWI447108B (zh) 2009-01-16 2014-08-01 Exelixis Inc Ｎ－（４－｛〔６，７雙（甲氧基）喹啉－４－基〕氧基｝苯基）－ｎ’－（４－氟苯基）環丙烷－１，１－二甲醯胺之蘋果酸鹽及其結晶型
EP2210891A1 (de) * 2009-01-26 2010-07-28 Domain Therapeutics Neue Adenosin-Rezeptorliganden und Verwendungen davon
KR20110133048A (ko) * 2009-03-21 2011-12-09 닝 시 아미노 에스테르 유도체, 그의 염 및 이용 방법
GEP20135907B (en) 2009-06-05 2013-08-12 Pfizer L-(piperidin-4-yl)-pyrazole derivatives as gpr 119 modulators
US8258316B2 (en) 2009-06-08 2012-09-04 Gilead Sciences, Inc. Alkanoylamino benzamide aniline HDAC inhibitor compounds
WO2010144378A2 (en) 2009-06-08 2010-12-16 Gilead Colorado, Inc. Cycloalkylcarbamate benzamide aniline hdac inhibitor compounds
EA201200144A1 (ru) 2009-07-17 2012-08-30 Экселиксис, Инк. Кристаллические формы n-[3-фтор-4-({6-(метилокси)-7-[(3-морфолин-4-илпропил)окси]хинолин-4-ил}окси)фенил]-n'-(4-фторфенил)циклопропан-1,1-дикарбоксамида
UA108618C2 (uk) * 2009-08-07 2015-05-25 Застосування c-met-модуляторів в комбінації з темозоломідом та/або променевою терапією для лікування раку
CN102030705B (zh) * 2009-09-30 2012-12-19 上海睿智化学研究有限公司 7-苄氧基-6-甲氧基-4-羟基喹啉的合成方法
EP2311809A1 (de) * 2009-10-16 2011-04-20 Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V. Chinolinyloxyphenylsulfonamide
ES2523465T3 (es) * 2009-11-03 2014-11-26 Glaxosmithkline Llc Compuestos de quinazolina
AU2010322796A1 (en) * 2009-11-27 2012-07-12 Proteologics, Ltd. Quinazolin-4(3A)-one derivatives and methods of use thereof
DE102009056886A1 (de) 2009-12-03 2011-06-09 Bayer Schering Pharma Aktiengesellschaft cMet-Inhibitoren zur Behandlung der Endometriose
CN102086211B (zh) * 2009-12-08 2013-09-11 广东东阳光药业有限公司 作为蛋白激酶抑制剂的芳杂环化合物
KR101870878B1 (ko) 2010-02-03 2018-06-25 인사이트 홀딩스 코포레이션 Ｃ―ＭＥＴ 억제제로서의 이미다조〔１，２―ｂ〕〔１，２，４〕트리아진
US20130143881A1 (en) 2010-03-12 2013-06-06 Exelixis, Inc. Hydrated Crystalline Forms of N-[3-fluoro-4-(oxy)phenyl]-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
EP2553641A4 (de) * 2010-03-26 2015-01-07 EastNets Mobiles computerüberweisungssystem und -verfahren
CN102212062B (zh) * 2010-04-02 2015-04-29 广东东阳光药业有限公司 氨基酯类衍生物及其盐和使用方法
US20120070368A1 (en) * 2010-04-16 2012-03-22 Exelixis, Inc. Methods of Using C-Met Modulators
AR081331A1 (es) 2010-04-23 2012-08-08 Cytokinetics Inc Amino- pirimidinas composiciones de las mismas y metodos para el uso de los mismos
WO2011133920A1 (en) 2010-04-23 2011-10-27 Cytokinetics, Inc. Certain amino-pyridines and amino-triazines, compositions thereof, and methods for their use
AR081626A1 (es) 2010-04-23 2012-10-10 Cytokinetics Inc Compuestos amino-piridazinicos, composiciones farmaceuticas que los contienen y uso de los mismos para tratar trastornos musculares cardiacos y esqueleticos
WO2011139891A1 (en) 2010-04-29 2011-11-10 Deciphera Pharmaceuticals, Llc Pyridone amides and analogs exhibiting anti-cancer and anti-proliferative activites
EP3450432A1 (de) 2010-05-17 2019-03-06 Incozen Therapeutics Pvt. Ltd. Neuartige 3,5-disubstituierte-3h-imidazo[4,5-b]pyridin- und 3,5- disubstituierte-3h-[1,2,3]triazol[4,5-b]pyridin-verbindungen als modulatoren der proteinkinase
EP2586443B1 (de) 2010-06-25 2016-03-16 Eisai R&D Management Co., Ltd. Antitumorwirkstoff mit verbindungen mit kinasehemmungswirkung in kombination
JP2013532627A (ja) 2010-07-01 2013-08-19 武田薬品工業株式会社 ｃＭＥＴ阻害剤とＨＧＦおよび／またはｃＭＥＴに対する抗体との組み合わせ
PT2593090T (pt) 2010-07-16 2021-11-04 Exelixis Inc Composições farmacêuticas moduladoras de c-met
EP2593091A1 (de) 2010-07-16 2013-05-22 Exelixis, Inc. Pharmazeutische c-met-modulator-zusammensetzungen
EP2423208A1 (de) 2010-08-28 2012-02-29 Lead Discovery Center GmbH Pharmazeutisch aktive Zusammensetzungen als Axl-Hemmer
US8664244B2 (en) * 2010-09-12 2014-03-04 Advenchen Pharmaceuticals, LLC Compounds as c-Met kinase inhibitors
SI2621481T2 (sl) 2010-09-27 2023-02-28 Exelixis, Inc., Dvojni inhibitorji MET in VEGF za zdravljenje proti kastraciji odpornega raka prostate in osteoblastnih kostnih metastaz
US20140066444A1 (en) 2010-09-27 2014-03-06 Exelixis, Inc. Method of Treating Cancer
CN103391773A (zh) * 2010-09-27 2013-11-13 埃克塞里艾克西斯公司 用于治疗去势抵抗性前列腺癌和成骨性骨转移的met和vegf的双重抑制剂
WO2012042421A1 (en) 2010-09-29 2012-04-05 Pfizer Inc. Method of treating abnormal cell growth
JP2013543011A (ja) * 2010-11-22 2013-11-28 グラクソスミスクライン、インテレクチュアル、プロパティー、ナンバー２、リミテッド 癌の治療法
CN102093421B (zh) 2011-01-28 2014-07-02 北京康辰药业有限公司 一种含磷取代基的喹啉类化合物及其制备方法、以及含有该化合物的药物组合物及其应用
ES2905571T3 (es) * 2011-02-10 2022-04-11 Exelixis Inc Procedimientos para la preparación de compuestos de quinolina y composiciones farmacéuticas que contienen dichos compuestos
ES2609578T3 (es) 2011-03-04 2017-04-21 Glaxosmithkline Intellectual Property Development Limited Amino-quinolinas como inhibidores de quinasa
US20120252840A1 (en) * 2011-04-04 2012-10-04 Exelixis, Inc. Method of Treating Cancer
WO2012144463A1 (ja) 2011-04-18 2012-10-26 エーザイ・アール・アンド・ディー・マネジメント株式会社 腫瘍治療剤
US8759380B2 (en) 2011-04-22 2014-06-24 Cytokinetics, Inc. Certain heterocycles, compositions thereof, and methods for their use
EA029506B1 (ru) * 2011-05-02 2018-04-30 Экселиксис, Инк. Способ лечения рака и раковой боли в костях
JP6038128B2 (ja) 2011-06-03 2016-12-07 エーザイ・アール・アンド・ディー・マネジメント株式会社 レンバチニブ化合物に対する甲状腺癌対象及び腎臓癌対象の反応性を予測及び評価するためのバイオマーカー
TWI547494B (zh) 2011-08-18 2016-09-01 葛蘭素史克智慧財產發展有限公司 作為激酶抑制劑之胺基喹唑啉類
EP2753176A4 (de) * 2011-09-06 2015-10-21 New York Blood Ct Inc Hiv-inhibitoren
CN102408411B (zh) 2011-09-19 2014-10-22 北京康辰药业股份有限公司 一种含喹啉基的羟肟酸类化合物及其制备方法、以及含有该化合物的药物组合物及其应用
CA2848512A1 (en) 2011-09-22 2013-03-28 Exelixis, Inc. Method for treating osteoporosis
UA116876C2 (uk) 2011-10-20 2018-05-25 Екселіксіс, Інк. Спосіб одержання хінолінових похідних
US8843421B2 (en) 2011-11-01 2014-09-23 Accenture Global Services Limited Identification of entities likely to engage in a behavior
TW201323864A (zh) 2011-11-08 2013-06-16 Exelixis Inc 定量癌症治療之方法
TWI662962B (zh) 2011-11-08 2019-06-21 艾克塞里克斯公司 治療癌症之方法
AR092289A1 (es) 2011-11-14 2015-04-15 Sunshine Lake Pharma Co Ltd Derivados de aminoquinazolina y sus sales y metodos de uso
WO2013091507A1 (zh) * 2011-12-20 2013-06-27 Qian Wei 杂环胺基烷氧基取代的喹唑啉衍生物及其用途
CN102643268B (zh) * 2011-12-30 2014-05-21 沈阳药科大学 喹啉类及噌啉类化合物及其应用
EP2620869B1 (de) 2012-01-27 2017-11-01 Optim Corporation Tragbares Endgerät, Verfahren und Programm zum Ändern einer Benutzeroberfläche
US9358235B2 (en) 2012-03-19 2016-06-07 Plexxikon Inc. Kinase modulation, and indications therefor
AP3908A (en) 2012-03-30 2016-11-24 Rhizen Pharmaceuticals Sa Novel 3,5-disubstituted-3H-imidazo[4,5-B]pyridine and 3,5-disubstituted-3H-[1,2,3]triazolo [4,5-B] pyridine compounds as modulators of C-met protein kinases
WO2013152252A1 (en) 2012-04-06 2013-10-10 OSI Pharmaceuticals, LLC Combination anti-cancer therapy
WO2013166296A1 (en) 2012-05-02 2013-11-07 Exelixis, Inc. A dual met - vegf modulator for treating osteolytic bone metastases
WO2013180128A1 (ja) * 2012-05-28 2013-12-05 協和発酵キリン株式会社 4-[4-(5員環芳香族複素環カルボニルウレイド)フェニルオキシ]キノリン誘導体
CN103509024B (zh) * 2012-06-28 2015-10-28 上海医药工业研究院 嘧啶并苯并氮杂卓类化合物及其作为抗肿瘤药物的应用
CN103626761B (zh) * 2012-08-24 2015-07-29 上海医药工业研究院 苯并吡啶氮杂卓类化合物及其作为抗肿瘤药物的应用
CN103626762B (zh) * 2012-08-24 2015-07-29 上海医药工业研究院 苯并吡啶氮杂卓类化合物及其应用
AR092529A1 (es) 2012-09-13 2015-04-22 Glaxosmithkline Llc Compuesto de aminoquinazolina, composicion farmaceutica que lo comprende y uso de dicho compuesto para la preparacion de un medicamento
TW201425307A (zh) 2012-09-13 2014-07-01 Glaxosmithkline Llc 作為激酶抑制劑之胺基－喹啉類
CN103664776B (zh) * 2012-09-26 2016-05-04 正大天晴药业集团股份有限公司 一种酪氨酸激酶抑制剂及其中间体的制备方法
CN103705521A (zh) * 2012-09-28 2014-04-09 韩冰 一类治疗脑梗塞的化合物及其用途
CN103804382A (zh) * 2012-11-05 2014-05-21 韩文毅 一类治疗湿疹的化合物及其用途
CN103804305A (zh) * 2012-11-05 2014-05-21 韩文毅 一类治疗湿疹的化合物及其用途
CN102977014B (zh) * 2012-11-05 2015-01-07 沈阳药科大学 新的喹啉类化合物及其用途
CN103804381A (zh) * 2012-11-06 2014-05-21 韩冰 一类治疗缺血性脑损伤的化合物及其用途
CN103800328A (zh) * 2012-11-07 2014-05-21 韩冰 一类治疗神经退行性疾病的化合物及其用途
CN103804290A (zh) * 2012-11-07 2014-05-21 韩冰 一类治疗神经退行性疾病的化合物及其用途
CN103804291A (zh) * 2012-11-07 2014-05-21 韩冰 一类治疗神经退行性疾病的化合物及其用途
CN103804361A (zh) * 2012-11-07 2014-05-21 韩冰 一类治疗神经退行性疾病的化合物及其用途
CN103800340A (zh) * 2012-11-09 2014-05-21 韩冰 一类治疗青光眼的化合物及其用途
CN103804298A (zh) * 2012-11-09 2014-05-21 韩冰 一类治疗青光眼的化合物及其用途
CN103804306A (zh) * 2012-11-12 2014-05-21 韩文毅 一类治疗糖尿病的化合物及其用途
CN103804362A (zh) * 2012-11-12 2014-05-21 韩文毅 一类治疗糖尿病的化合物及其用途
CN103804363A (zh) * 2012-11-14 2014-05-21 韩冰 一类具有神经保护作用的化合物及其用途
CN102964308B (zh) * 2012-11-30 2015-03-18 中国药科大学 新型嘧啶类化合物、其制备方法、包含此类化合物的药物组合物及其用途
CN104755463A (zh) 2012-12-21 2015-07-01 卫材R&D管理有限公司 非晶态形式的喹啉衍生物及其生产方法
CN103965104B (zh) * 2013-01-29 2017-09-29 正大天晴药业集团股份有限公司 一种酪氨酸激酶抑制剂及其中间体的制备方法
TWI630203B (zh) 2013-02-21 2018-07-21 葛蘭素史克智慧財產發展有限公司 做為激酶抑制劑的喹唑啉類
WO2014145693A1 (en) * 2013-03-15 2014-09-18 Exelixis, Inc. Metabolites of n-[3-fluoro-4-({ 6-(methyloxy)-7-[(3-morpholin-4-ylpropyl)oxy]quinolin-4-yl}oxy)phenyl]-n'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
BR112015023571A2 (pt) * 2013-03-15 2017-07-18 Hoffmann La Roche derivados de sulfamato e sulfamida de arila como moduladores rorc
EP2970126B1 (de) * 2013-03-15 2019-03-06 Exelixis, Inc. Metaboliten von n-(4-{[6,7-bis(methyloxy)chinolin-4-yl]oxy}phenyl)- n'-(4-fluorophenyl) cyclopropan-1,1-dicarboxamid
AU2014248001A1 (en) 2013-04-04 2015-11-19 Exelixis, Inc. Drug combinations to treat cancer
EP2981263B1 (de) 2013-04-04 2022-06-29 Exelixis, Inc. Cabozantinib dosierungsform und verwendung zur behandlung von krebs
CN104109128B (zh) * 2013-04-19 2016-10-05 连云港润众制药有限公司 卡博替尼苹果酸盐及其制备方法
CN104109124B (zh) * 2013-04-19 2016-08-31 正大天晴药业集团股份有限公司 卡博替尼·0.5苹果酸盐的晶体
MX368099B (es) 2013-05-14 2019-09-19 Eisai R&D Man Co Ltd Biomarcadores para predecir y evaluar el grado de respuesta de sujetos con cancer de endometrio a compuestos de tipo lenvatinib.
CN104370811B (zh) * 2013-08-15 2019-02-12 广东东阳光药业有限公司 一种喹啉化合物的新晶型及其制备方法
PT3039424T (pt) 2013-08-28 2020-09-03 Crown Bioscience Inc Taicang Assinaturas de expressão genética que permitem prever a resposta de um sujeito a um inibidor multiquinase e métodos de utilização do mesmo
CN104628657A (zh) * 2013-11-06 2015-05-20 韩冰 一类治疗缺血性脑损伤的化合物及其用途
EP3105204A1 (de) 2014-02-14 2016-12-21 Exelixis, Inc. Kristalline feste formen von n-{4-[(6,7-dimethoxychinolin-4-yl)oxy]phenyl}-n'-(4-fluorphenyl)-cyclopropan-1, 1-dicarboxamid, verfahren zur herstellung und verfahren zur verwendung davon
US10231965B2 (en) 2014-02-20 2019-03-19 Ignyta, Inc. Molecules for administration to ROS1 mutant cancer cells
WO2015129860A1 (ja) * 2014-02-28 2015-09-03 国立大学法人東北大学 アミド誘導体
EP3119476A1 (de) 2014-03-17 2017-01-25 Exelixis, Inc. Dosierung von cabozantinibformulierungen
MA39776A (fr) 2014-03-24 2017-02-01 Hoffmann La Roche Traitement du cancer avec des antagonistes de c-met et corrélation de ces derniers avec l'expression de hgf
JP6696908B2 (ja) 2014-04-25 2020-05-20 エグゼリクシス， インコーポレイテッド 肺腺癌の治療方法
EP3145913A1 (de) 2014-05-23 2017-03-29 Mylan Laboratories Ltd. Neuartige polymorphe aus cabozantinib-(s)-malat und cabozantinibfreier base
CN104788372B (zh) * 2014-07-25 2018-01-30 上海圣考医药科技有限公司 一种氘代卡博替尼衍生物、其制备方法、应用及其中间体
ES2929888T3 (es) * 2014-07-31 2022-12-02 Exelixis Inc Procedimiento para preparar cabozantinib marcado con flúor 18 y sus análogos
KR102634247B1 (ko) 2014-08-05 2024-02-05 엑셀리시스, 인코포레이티드 다발성 골수종을 치료하기 위한 약물 병용물
US10259791B2 (en) 2014-08-28 2019-04-16 Eisai R&D Management Co., Ltd. High-purity quinoline derivative and method for manufacturing same
US10137107B2 (en) 2014-09-19 2018-11-27 New York Blood Center, Inc. Substituted phenylpyrrolecarboxamides with therapeutic activity in HIV
US10085979B2 (en) 2014-12-02 2018-10-02 Ignyta, Inc. Combinations for the treatment of neuroblastoma
ES2764299T3 (es) 2014-12-09 2020-06-02 Inst Nat Sante Rech Med Anticuerpos monoclonales humanos contra AXL
MX2017010474A (es) 2015-02-25 2017-11-28 Eisai R&D Man Co Ltd Metodo para suprimir el amargor de un derivado de quinoleina.
WO2016135041A1 (en) 2015-02-26 2016-09-01 INSERM (Institut National de la Santé et de la Recherche Médicale) Fusion proteins and antibodies comprising thereof for promoting apoptosis
KR102662228B1 (ko) 2015-03-04 2024-05-02 머크 샤프 앤드 돔 코포레이션 암을 치료하기 위한 pd-1 길항제 및 vegfr/fgfr/ret 티로신 키나제 억제제의 조합
US10053427B2 (en) 2015-03-25 2018-08-21 Sandoz Ag Crystalline forms of cabozantinib phosphate and cabozantinib hydrochloride
CN106279147A (zh) * 2015-05-21 2017-01-04 中国科学院上海药物研究所 一种吡啶并氮杂环化合物及其制备方法和用途
RU2729936C2 (ru) 2015-06-16 2020-08-13 Эйсай Ар Энд Ди Менеджмент Ко., Лтд. Противораковое средство
US20170020856A1 (en) * 2015-06-29 2017-01-26 Ontogenesis, Llc N-Acylalkyl Prodrugs of Multi-Tyrosine Kinase Inhibitors and Methods of Use
CN107646030A (zh) * 2015-08-19 2018-01-30 桑多斯股份公司 丙二酸酯衍生物的不对称双酰胺化
CN105218445B (zh) * 2015-08-25 2018-05-22 江苏中邦制药有限公司 一种酪氨酸激酶抑制剂Foretinib的制备方法
CN106543143B (zh) * 2015-09-22 2019-03-22 合肥中科普瑞昇生物医药科技有限公司 一类新型的flt3激酶抑制剂及其用途
BR112018012255A2 (pt) 2015-12-18 2018-12-04 Ignyta Inc método para tratar câncer
CN105541798B (zh) * 2016-02-03 2018-01-23 中国人民解放军第二军医大学 具有抗肿瘤活性的喹啉类多靶点激酶抑制剂及其制备方法
CN107129465B (zh) * 2016-02-26 2020-06-19 中国科学院上海药物研究所 芳基胍类化合物及其制备方法和用途
WO2017173049A1 (en) * 2016-03-31 2017-10-05 Merck Patent Gmbh Compounds for the inhibition of cyclophilins and uses thereof
EP3442531A1 (de) 2016-04-15 2019-02-20 Exelixis, Inc. Verfahren zur behandlung von nierenzellkarzinomen unter verwendung von n-(4-(6,7-dimethoxychinolin-4-yloxy)phenyl)-n'-(4-fluorpheny)cyclopropan-1,1-dicarboxamid, (2s)-hydroxybutanedioat
CN105906568A (zh) * 2016-04-28 2016-08-31 西安交通大学 一种具有抗肿瘤活性的环丙二酰胺化合物及其制备方法和应用
CN106083715A (zh) * 2016-06-01 2016-11-09 谢阳 一种喹啉、喹唑啉类化合物及其药物组合物和应用
CN106008371A (zh) * 2016-06-24 2016-10-12 谢阳 1-芳基脲基环烷基-1-甲酰胺类化合物及其药物组合物和应用
CN107556238A (zh) * 2016-06-30 2018-01-09 深圳万乐药业有限公司 一种卡博替尼的合成方法
US9957233B1 (en) 2016-08-05 2018-05-01 Calitor Sciences, Llc Process for preparing substituted quinolin-4-ol compounds
CN109922790B (zh) * 2016-09-12 2022-06-14 珠海贝海生物技术有限公司 卡博替尼制剂
CN107235896B (zh) * 2016-09-13 2019-11-05 上海翔锦生物科技有限公司 酪氨酸激酶抑制剂及其应用
AU2017336547A1 (en) 2016-09-27 2019-05-02 The United States Of America, As Represented By The Secretary, Department Of Health & Human Services Method of treating urothelial carcinoma and other genitourinary malignancies using N-(4-(6,7-dimethoxyquinolin-4-yloxy)phenyl)-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
CA3040788C (en) * 2016-10-18 2022-01-11 Beijing Konruns Pharmaceutical Co., Ltd. Quinolyl-substituted carboxylic acid compound or pharmaceutically acceptable salt thereof, pharmaceutical composition of the same, and use of the same
WO2018102455A1 (en) 2016-12-01 2018-06-07 Ignyta, Inc. Methods for the treatment of cancer
CN106632028B (zh) * 2016-12-22 2019-01-22 上海再启生物技术有限公司 一种卡博替尼的制备方法
CN108329298A (zh) * 2017-01-17 2018-07-27 南昌弘益药业有限公司 一类喹啉类新化合物制备方法
AU2018210397B2 (en) 2017-01-20 2024-02-29 Exelixis, Inc. Combinations of cabozantinib and atezolizumab to treat cancer
DK3583943T3 (da) 2017-02-15 2024-10-14 Taiho Pharmaceutical Co Ltd Farmaceutisk sammensætning
CN108503650B (zh) * 2017-02-27 2021-02-12 北京赛特明强医药科技有限公司 二噁烷并喹唑啉类化合物或其药用盐或其水合物及其作为酪氨酸激酶抑制剂的应用
WO2019154133A1 (zh) 2018-02-11 2019-08-15 北京赛特明强医药科技有限公司 二噁烷并喹啉类化合物及其制备方法与应用
CA3059660A1 (en) * 2017-04-27 2018-11-01 Astrazeneca Ab Phenoxyquinazoline compounds and their use in treating cancer
KR102611445B1 (ko) 2017-05-26 2023-12-06 엑셀리시스, 인코포레이티드 N-｛4-[(6,7-디메톡시퀴놀린-4-일)옥시]페닐｝-n′-(4-플루오로페닐) 시클로프로판-1,1-디카르복스아미드의 염의 결정성 고체 형태, 이들을 만들기 위한 제법, 그리고 이들의 이용 방법
UA126402C2 (uk) 2017-06-09 2022-09-28 Екселіксіс, Інк. Рідка лікарська форма для лікування раку
PE20200296A1 (es) 2017-07-14 2020-02-06 Innate Tumor Immunity Inc Moduladores de nlrp3
AU2018302170B2 (en) 2017-07-19 2024-02-29 Ignyta, Inc. Pharmaceutical compositions comprising entrectinib
US10180422B1 (en) 2017-08-22 2019-01-15 Scripps Health Methods of treating a neuroendocrine tumor
TW201920104A (zh) * 2017-08-31 2019-06-01 美商馬愈法瑪公司 外核苷酸焦磷酸酶-磷酸二酯酶1(enpp-1)抑制劑及其用途
CN111225662B (zh) 2017-10-17 2022-11-22 伊尼塔公司 药物组合物和剂型
WO2019079783A1 (en) 2017-10-20 2019-04-25 Vanderbilt University ANTAGONISTS OF THE MUSCARINIC RECEPTOR OF ACETYLCHOLINE M4
US11352344B2 (en) 2017-10-31 2022-06-07 Vanderbilt University Antagonists of the muscarinic acetylcholine receptor M4
CN109824587A (zh) * 2017-11-23 2019-05-31 上海翔锦生物科技有限公司 酪氨酸激酶抑制剂xjf007及其中间体的制备方法
CN109896997A (zh) * 2017-12-08 2019-06-18 中国药科大学 N－酰基苯胺类c－Met激酶抑制剂的制备方法及其用途
CN111511361A (zh) * 2017-12-20 2020-08-07 安杰斯制药公司 作为多激酶抑制剂的胺基碳酸盐及尿素化合物
US20190262330A1 (en) * 2017-12-21 2019-08-29 Exelixis, Inc. Method of Treating Hepatocellular Carcinoma Using N-(4-(6,7-dimethoxyquinolin-4-yloxy)phenyl)-N′-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, (2S)-hydroxybutanedioate
IL276028B1 (en) * 2018-01-26 2024-10-01 Exelixis Inc Compounds for the treatment of kinase-dependent disorders
CA3088198A1 (en) * 2018-01-26 2019-08-01 Exelixis, Inc. Compounds for the treatment of kinase-dependent disorders
CN117402114A (zh) 2018-01-26 2024-01-16 埃克塞里艾克西斯公司 用于治疗激酶依赖性病症的化合物
WO2019152809A1 (en) 2018-02-02 2019-08-08 Vanderbilt University Antagonists of the muscarinic acetylcholine receptor m4
CN108264482A (zh) * 2018-02-05 2018-07-10 南京法恩化学有限公司 一种卡博替尼的制备方法
WO2019180141A1 (en) 2018-03-23 2019-09-26 Bayer Aktiengesellschaft Combinations of rogaratinib
US11498902B2 (en) 2018-06-05 2022-11-15 Natco Pharma Limited Process for the preparation of Cabozantinib and its pharmaceutically acceptable salts thereof
CN112423757A (zh) 2018-06-15 2021-02-26 汉达生技医药责任有限公司 激酶抑制剂的盐类及其组合物
WO2020027723A1 (en) * 2018-08-01 2020-02-06 Agency For Science, Technology And Research Bicyclic compounds as kinase modulators, methods and uses thereof
WO2020042972A1 (zh) * 2018-08-27 2020-03-05 北京赛特明强医药科技有限公司 脲取代的芳环连二噁烷并喹唑啉或喹啉类化合物、组合物及其应用
WO2020075196A1 (en) 2018-10-11 2020-04-16 Cipla Limited Polymorphs of n-(4-(6,7-dimethoxyquinolin-4-yloxy) phenyl)-n'-(4-fluorophenyl)cyclopropane-1, 1-dicarboxamide, (s)- malate, methods of production and pharmaceutical uses thereof
CN111303024B (zh) * 2018-12-12 2023-03-28 安徽中科拓苒药物科学研究有限公司 一种喹啉结构的pan-KIT激酶抑制剂及其用途
AU2019395419A1 (en) 2018-12-13 2021-07-01 Exelixis, Inc. Crystalline forms and salt forms of a kinase inhibitor
TW202038957A (zh) 2018-12-21 2020-11-01 日商第一三共股份有限公司 抗體-藥物結合物與激酶抑制劑之組合
EP3952865A4 (de) * 2019-04-12 2023-05-03 National Health Research Institutes Heterocyclische verbindungen als kinase-inhibitoren für therapeutische verwendungen
CN111825609A (zh) * 2019-04-22 2020-10-27 北京康辰药业股份有限公司 化合物晶型、其制备方法、药物组合物以及应用
SG11202111978VA (en) * 2019-06-03 2021-11-29 Exelixis Inc Crystalline salt forms of a kinase inhibitor
CN110117254B (zh) * 2019-06-20 2022-05-13 江苏君若药业有限公司 卡博替尼的制备方法
CN112778217B (zh) * 2019-11-08 2024-01-26 沈阳化工研究院有限公司 一种喹唑啉类化合物及其应用
CN111393363B (zh) * 2020-04-27 2022-12-20 威海海洋生物医药产业技术研究院有限公司 4-苯氧基喹啉并n-磺酰脒类化合物及其制备方法和用途
CN113577066B (zh) * 2020-04-30 2022-12-16 中国科学院上海药物研究所 芳基胍化合物或其药学上可接受的盐的用途
IT202000027678A1 (it) 2020-11-18 2022-05-18 Indena Spa Dispersioni solide amorfe di cabozantinib-(s)-malato e processi per la loro preparazione
CA3202761A1 (en) 2020-11-25 2022-06-02 Nanocopoeia, Llc Amorphous cabozantinib particles and uses thereof
MX2023007287A (es) * 2020-12-17 2023-07-03 Astrazeneca Ab N-(2-(4-cianotiazolidin-3-il)-2-oxoetil)-quinolin-4-carboxamidas.
KR20240006021A (ko) * 2021-03-24 2024-01-12 바이오콘 리미티드 카보잔티닙의 제조방법
CA3237696A1 (en) 2021-11-08 2023-05-11 Progentos Therapeutics, Inc. Platelet-derived growth factor receptor (pdgfr) alpha inhibitors and uses thereof
WO2023098853A1 (zh) * 2021-12-03 2023-06-08 湖南湘源美东医药科技有限公司 卡博替尼共晶及制备方法以及作为药物或在药物制剂中的应用
CN114605391B (zh) * 2022-02-21 2024-01-26 广州六顺生物科技股份有限公司 喹喔啉类衍生物及其制备方法和应用
WO2023165948A1 (en) 2022-03-01 2023-09-07 Synthon B.V. Cabozantinib salt with l-(+)-tartaric acid and solid forms thereof
WO2023222946A1 (en) 2022-05-18 2023-11-23 Fermion Oy Process for the preparation of cabozantinib
WO2023228095A1 (en) 2022-05-24 2023-11-30 Daiichi Sankyo Company, Limited Dosage regimen of an anti-cdh6 antibody-drug conjugate
WO2024008929A1 (en) 2022-07-08 2024-01-11 Astrazeneca Ab Epidermal growth factor receptor tyrosine kinase inhibitors in combination with hgf-receptor inhibitors for the treatment of cancer
WO2024110606A1 (en) 2022-11-25 2024-05-30 Synthon B.V. A process for preparation of cabozantinib or tivozanib
WO2024114710A1 (zh) * 2022-12-01 2024-06-06 江苏奥赛康药业有限公司 一种制备卡博替尼及其中间体的方法
WO2024163400A1 (en) * 2023-01-31 2024-08-08 Handa Oncology, Llc Improved cabozantinib compositions and methods of use

Family Cites Families (170)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US506181A (en) 1893-10-03 Folding crate
GB2160201B (en) * 1984-06-14 1988-05-11 Wyeth John & Brother Ltd Quinazoline and cinnoline derivatives
US5123951A (en) * 1986-03-31 1992-06-23 Rhone-Poulenc Nederland B.V. Synergistic plant growth regulator compositions
JPS646261A (en) * 1987-03-31 1989-01-10 Nisshin Flour Milling Co 4-thioquinazoline derivative, its production and antiulcer agent containing said derivative as active component
US5143854A (en) * 1989-06-07 1992-09-01 Affymax Technologies N.V. Large scale photolithographic solid phase synthesis of polypeptides and receptor binding screening thereof
US5034393A (en) * 1989-07-27 1991-07-23 Dowelanco Fungicidal use of pyridopyrimidine, pteridine, pyrimidopyrimidine, pyrimidopyridazine, and pyrimido-1,2,4-triazine derivatives
US5238951A (en) * 1991-02-01 1993-08-24 E. R. Squibb & Sons, Inc. Heterocyclic amido prostaglandin analogs
DE4114733A1 (de) * 1991-05-06 1992-11-12 Huels Chemische Werke Ag Verfahren zur herstellung von substituierten malonesteraniliden und malonsaeure-monoaniliden
US5480883A (en) * 1991-05-10 1996-01-02 Rhone-Poulenc Rorer Pharmaceuticals Inc. Bis mono- and bicyclic aryl and heteroaryl compounds which inhibit EGF and/or PDGF receptor tyrosine kinase
US5710158A (en) * 1991-05-10 1998-01-20 Rhone-Poulenc Rorer Pharmaceuticals Inc. Aryl and heteroaryl quinazoline compounds which inhibit EGF and/or PDGF receptor tyrosine kinase
US5358941A (en) 1992-12-02 1994-10-25 Merck & Co., Inc. Dry mix formulation for bisphosphonic acids with lactose
US6498144B1 (en) * 1993-10-18 2002-12-24 North Shore - Long Island Jewish Research Institute Use of scatter factor to enhance angiogenesis
IL112249A (en) 1994-01-25 2001-11-25 Warner Lambert Co Pharmaceutical compositions containing di and tricyclic pyrimidine derivatives for inhibiting tyrosine kinases of the epidermal growth factor receptor family and some new such compounds
GB9510757D0 (en) 1994-09-19 1995-07-19 Wellcome Found Therapeuticaly active compounds
TW321649B (de) 1994-11-12 1997-12-01 Zeneca Ltd
GB9508538D0 (en) * 1995-04-27 1995-06-14 Zeneca Ltd Quinazoline derivatives
US5747498A (en) * 1996-05-28 1998-05-05 Pfizer Inc. Alkynyl and azido-substituted 4-anilinoquinazolines
SI1090642T1 (sl) 1995-06-07 2008-12-31 Glaxosmithkline Biolog Sa Vakcine, ki obsegajo konjugat polisaharidni antigen-nosilni protein in prosti nosilni protein
US5650415A (en) * 1995-06-07 1997-07-22 Sugen, Inc. Quinoline compounds
AU5984296A (en) * 1995-06-07 1996-12-30 Sugen, Inc. Quinazolines and pharmaceutical compositions
GB9514265D0 (en) 1995-07-13 1995-09-13 Wellcome Found Hetrocyclic compounds
WO1997017329A1 (fr) * 1995-11-07 1997-05-15 Kirin Beer Kabushiki Kaisha Derives de quinoline et derives de quinazoline inhibant l'autophosphorylation d'un recepteur de facteur de croissance originaire de plaquettes, et compositions pharmaceutiques les contenant
GB9523675D0 (en) * 1995-11-20 1996-01-24 Celltech Therapeutics Ltd Chemical compounds
GB9624482D0 (en) * 1995-12-18 1997-01-15 Zeneca Phaema S A Chemical compounds
NZ325248A (en) * 1995-12-23 1999-09-29 Pfizer Res & Dev Quinoline and quinazoline compounds useful in therapy
CA2242425C (en) 1996-02-13 2006-07-18 Zeneca Limited Quinazoline derivatives as vegf inhibitors
GB9603095D0 (en) * 1996-02-14 1996-04-10 Zeneca Ltd Quinazoline derivatives
CA2244897C (en) 1996-03-05 2006-04-11 Zeneca Limited 4-anilinoquinazoline derivatives
WO1997034876A1 (en) * 1996-03-15 1997-09-25 Zeneca Limited Cinnoline derivatives and use as medicine
US6107300A (en) * 1996-03-27 2000-08-22 Dupont Pharmaceuticals Arylamino fused pyrimidines
CN100503580C (zh) * 1996-04-12 2009-06-24 沃尼尔·朗伯公司 酪氨酸激酶的不可逆抑制剂
PT912559E (pt) * 1996-07-13 2003-03-31 Glaxo Group Ltd Compostos heterociclicos fundidos como inibidores de proteina tirosina quinase
HRP970371A2 (en) 1996-07-13 1998-08-31 Kathryn Jane Smith Heterocyclic compounds
GB9718972D0 (en) * 1996-09-25 1997-11-12 Zeneca Ltd Chemical compounds
NZ334125A (en) * 1996-09-25 2000-10-27 Zeneca Ltd Quinoline derivatives inhibiting the effect of growth factors such as VEGF
DE69739986D1 (de) * 1996-10-01 2010-10-21 Kyowa Hakko Kogyo Kk Stickstoff enthaltende heterocyclische verbindungen
GB9700504D0 (en) * 1997-01-11 1997-02-26 Pfizer Ltd Pharmaceutical compounds
GB9705361D0 (en) * 1997-03-14 1997-04-30 Celltech Therapeutics Ltd Chemical compounds
UA73073C2 (uk) 1997-04-03 2005-06-15 Уайт Холдінгз Корпорейшн Заміщені 3-ціанохіноліни, спосіб їх одержання та фармацевтична композиція
EP0990647B1 (de) 1997-04-18 2003-07-02 Kirin Beer Kabushiki Kaisha Verfahren zur herstellung von chinolinderivaten
AU7644698A (en) 1997-04-22 1998-11-13 Janssen Pharmaceutica N.V. Crf antagonistic quino- and quinazolines
GB9708917D0 (en) * 1997-05-01 1997-06-25 Pfizer Ltd Compounds useful in therapy
AR012634A1 (es) * 1997-05-02 2000-11-08 Sugen Inc Compuesto basado en quinazolina, composicion famaceutica que lo comprende, metodo para sintetizarlo, su uso, metodos de modulacion de la funcion deserina/treonina proteinaquinasa con dicho compuesto y metodo in vitro para identificar compuestos que modulan dicha funcion
ZA986732B (en) * 1997-07-29 1999-02-02 Warner Lambert Co Irreversible inhibitiors of tyrosine kinases
JP4959049B2 (ja) * 1997-08-22 2012-06-20 アストラゼネカ・ユーケイ・リミテッド 血管新生阻害剤としてのオキシインドリルキナゾリン誘導体
JP4194678B2 (ja) * 1997-11-28 2008-12-10 キリンファーマ株式会社 キノリン誘導体およびそれを含む医薬組成物
RS49779B (sr) * 1998-01-12 2008-06-05 Glaxo Group Limited, Biciklična heteroaromatična jedinjenja kao inhibitori protein tirozin kinaze
AU4317399A (en) * 1998-05-28 1999-12-13 Parker Hughes Institute Quinazolines for treating brain tumor
CN1152031C (zh) * 1998-08-11 2004-06-02 诺瓦提斯公司 具有血管生成抑制活性的异喹啉衍生物
DE69924500T2 (de) 1998-08-21 2006-02-09 Parker Hughes Institute, St. Paul Chinazolinderivate
US6184226B1 (en) * 1998-08-28 2001-02-06 Scios Inc. Quinazoline derivatives as inhibitors of P-38 α
JP5170486B2 (ja) 1998-09-10 2013-03-27 バイオイコール ア−ゲー 局所適用性産物
US6288082B1 (en) * 1998-09-29 2001-09-11 American Cyanamid Company Substituted 3-cyanoquinolines
WO2000018761A1 (en) 1998-09-29 2000-04-06 American Cyanamid Company Substituted 3-cyanoquinolines as protein tyrosine kinases inhibitors
EP1117653B1 (de) * 1998-10-01 2003-02-05 AstraZeneca AB Chinolin- und chinazolin derivate und ihre verwendung als inhibitoren von krankheiten, bei denen cytokine beteiligt wird
JP2002527436A (ja) 1998-10-08 2002-08-27 アストラゼネカ アクチボラグ キナゾリン誘導体
NZ512189A (en) * 1998-11-19 2003-10-31 Warner Lambert Co N-[4-(3-chloro-4-fluoro-phenylamino)-7-(3-morpholin-4- yl-propoxy)-quinazolin-6-yl]-acrylamide useful as an irreversible inhibitor of tyrosine kinases
AU771504B2 (en) * 1999-01-22 2004-03-25 Kyowa Hakko Kirin Co., Ltd. Quinoline derivatives and quinazoline derivatives
MXPA01008182A (es) 1999-02-10 2003-08-20 Astrazeneca Ab Derivados de quinazolina como inhibidores de angiotensina.
GB9904103D0 (en) * 1999-02-24 1999-04-14 Zeneca Ltd Quinoline derivatives
US6080747A (en) * 1999-03-05 2000-06-27 Hughes Institute JAK-3 inhibitors for treating allergic disorders
DE19911509A1 (de) * 1999-03-15 2000-09-21 Boehringer Ingelheim Pharma Bicyclische Heterocyclen, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung
AU3630100A (en) 1999-03-19 2000-10-09 Parker Hughes Institute Quinazoline formulations and therapeutic use thereof
US6258820B1 (en) * 1999-03-19 2001-07-10 Parker Hughes Institute Synthesis and anti-tumor activity of 6,7-dialkoxy-4-phenylamino-quinazolines
RS49836B (sr) * 1999-03-31 2008-08-07 Pfizer Products Inc., Postupci i intermedijeri za dobijanje anti-kancernih jedinjenja
GB9910577D0 (en) 1999-05-08 1999-07-07 Zeneca Ltd Chemical compounds
GB9910580D0 (en) * 1999-05-08 1999-07-07 Zeneca Ltd Chemical compounds
US6126917A (en) * 1999-06-01 2000-10-03 Hadasit Medical Research Services And Development Ltd. Epidermal growth factor receptor binding compounds for positron emission tomography
SK287010B6 (sk) * 1999-06-21 2009-09-07 Boehringer Ingelheim Pharma Gmbh & Co. Kg Bicyklické heterocyklické zlúčeniny, spôsob ich prípravy, farmaceutický prostriedok s ich obsahom a ich použitie
GB9922171D0 (en) 1999-09-21 1999-11-17 Zeneca Ltd Chemical compounds
CA2384291A1 (en) * 1999-09-21 2001-03-29 Astrazeneca Ab Quinazoline derivatives and their use as pharmaceuticals
US6759410B1 (en) * 1999-11-23 2004-07-06 Smithline Beecham Corporation 3,4-dihydro-(1H)-quinazolin-2-ones and their use as CSBP/p38 kinase inhibitors
WO2001045641A2 (en) * 1999-11-30 2001-06-28 Parker Hughes Institute Inhibitors of thrombin induced platelet aggregation
US20020002169A1 (en) * 1999-12-08 2002-01-03 Griffin John H. Protein kinase inhibitors
EP1243582A4 (de) * 1999-12-24 2003-06-04 Kirin Brewery Chinolin- und chinazolinderivate sowie medikamente, die diese enthalten
US6525046B1 (en) * 2000-01-18 2003-02-25 Boehringer Ingelheim Pharmaceuticals, Inc. Aromatic heterocyclic compounds as antiinflammatory agents
WO2001055116A2 (en) * 2000-01-28 2001-08-02 Astrazeneca Ab Quinoline derivatives and their use as aurora 2 kinase inhibitors
US6664390B2 (en) 2000-02-02 2003-12-16 Warner-Lambert Company Llc Method for the simplified production of (3-chloro-4-fluorophenyl)-[7-(3-morpholin-4-yl-propoxy)-6-nitro-quinazoline-4-yl]-amine or (3-chloro-4-fluorophenyl)-[7-(3-morpholin-4-yl-propoxy)-6-amino-quinazoline-4-yl]-amine
CA2398754A1 (en) * 2000-02-07 2001-08-09 Abbott Gmbh & Co. Kg 2-benzothiazolyl urea derivatives and their use as protein kinase inhibitors
EA200200976A1 (ru) 2000-03-13 2003-02-27 Американ Цианамид Компани Способ лечения или ингибирования полипов ободочной кишки
US6608048B2 (en) * 2000-03-28 2003-08-19 Wyeth Holdings Tricyclic protein kinase inhibitors
US6521618B2 (en) * 2000-03-28 2003-02-18 Wyeth 3-cyanoquinolines, 3-cyano-1,6-naphthyridines, and 3-cyano-1,7-naphthyridines as protein kinase inhibitors
US6627634B2 (en) * 2000-04-08 2003-09-30 Boehringer Ingelheim Pharma Kg Bicyclic heterocycles, pharmaceutical compositions containing them, their use, and processes for preparing them
UA73993C2 (uk) 2000-06-06 2005-10-17 Астразенека Аб Хіназолінові похідні для лікування пухлин та фармацевтична композиція
CA2413424C (en) * 2000-06-22 2007-10-02 Pfizer Products Inc. Substituted bicyclic derivatives for the treatment of abnormal cell growth
EP1174118A1 (de) 2000-06-28 2002-01-23 Cognis France S.A. Verwendung von Inulinen und Inulinderivaten
US6919338B2 (en) 2000-06-28 2005-07-19 Astrazeneca Ab Substituted quinazoline derivatives and their use as inhibitors of aurora-2 kinase
FR2811658B1 (fr) 2000-07-17 2004-07-02 Cfpi Nufarm Reacteur biologique a lit fixe immerge et procede de traitement d'effluents liquides
JP2002030083A (ja) * 2000-07-18 2002-01-29 Kirin Brewery Co Ltd Ｎ−（２−クロロ−４−｛［６−メトキシ−７−（３−ピリジルメトキシ）−４−キノリル］オキシ｝フェニル）−ｎ’−プロピルウレアの二塩酸塩
CA2417500C (en) * 2000-07-28 2008-11-18 Georgetown University Medical Center Erbb-2 selective small molecule kinase inhibitors
JP2004506732A (ja) 2000-08-21 2004-03-04 アストラゼネカ　アクチボラグ キナゾリン誘導体
US6653305B2 (en) * 2000-08-26 2003-11-25 Boehringer Ingelheim Pharma Kg Bicyclic heterocycles, pharmaceutical compositions containing them, their use, and processes for preparing them
US6740651B2 (en) * 2000-08-26 2004-05-25 Boehringer Ingelheim Pharma Kg Aminoquinazolines which inhibit signal transduction mediated by tyrosine kinases
US6617329B2 (en) * 2000-08-26 2003-09-09 Boehringer Ingelheim Pharma Kg Aminoquinazolines and their use as medicaments
US6656946B2 (en) 2000-08-26 2003-12-02 Boehringer Ingelheim Pharma Kg Aminoquinazolines which inhibit signal transduction mediated by tyrosine kinases
DE10042058A1 (de) 2000-08-26 2002-03-07 Boehringer Ingelheim Pharma Bicyclische Heterocyclen, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung
US6403580B1 (en) * 2000-08-26 2002-06-11 Boehringer Ingelheim Pharma Kg Quinazolines, pharmaceutical compositions containing these compounds, their use and processes for preparing them
AU2001292137A1 (en) 2000-10-13 2002-04-22 Astrazeneca Ab Quinazoline derivatives
EP1326859A1 (de) 2000-10-13 2003-07-16 AstraZeneca AB Chinazoline derivate mit aktivität gegen tumore
AU9598601A (en) * 2000-10-20 2002-04-29 Eisai Co Ltd Nitrogenous aromatic ring compounds
WO2002034744A1 (en) 2000-10-25 2002-05-02 Astrazeneca Ab Quinazoline derivatives
US7253184B2 (en) 2000-11-02 2007-08-07 Astrazeneca Ab 4-Substituted quinolines as antitumor agents
WO2002044166A1 (en) 2000-11-02 2002-06-06 Astrazeneca Ab Substituted quinolines as antitumor agents
US7220751B2 (en) 2000-11-02 2007-05-22 Nippon Shinyaku Co., Ltd. Quinazoline derivatives and drugs
US7019012B2 (en) * 2000-12-20 2006-03-28 Boehringer Ingelheim International Pharma Gmbh & Co. Kg Quinazoline derivatives and pharmaceutical compositions containing them
US6900220B2 (en) * 2001-01-02 2005-05-31 Syntex (U.S.A.) Llc Quinazolone derivatives as alpha 1A/B adrenergic receptor antagonists
DE60229046D1 (de) 2001-04-19 2008-11-06 Astrazeneca Ab Chinazolin derivate
MXPA03009662A (es) 2001-04-27 2004-12-06 Kirin Brewery Derivados de quinolina y derivados de quinazolina que tienen grupos azolilo.
SE0101675D0 (sv) 2001-05-11 2001-05-11 Astrazeneca Ab Novel composition
WO2002092578A1 (en) 2001-05-14 2002-11-21 Astrazeneca Ab Quinazoline derivatives
WO2002092577A1 (en) 2001-05-14 2002-11-21 Astrazeneca Ab Quinazoline derivatives
WO2002092579A1 (en) 2001-05-14 2002-11-21 Astrazeneca Ab 4-anilinoquinazoline derivatives
US6734303B2 (en) * 2001-05-18 2004-05-11 Pfizer Inc. Process for the production of quinazolines
DE10125432A1 (de) * 2001-05-25 2002-11-28 Bayer Ag Substituierte Benzoylketone
AU2002350105A1 (en) 2001-06-21 2003-01-08 Ariad Pharmaceuticals, Inc. Novel quinazolines and uses thereof
DE60233736D1 (de) * 2001-06-22 2009-10-29 Kirin Pharma K K Chinolinderivat und chinazolinderivat, die die selbstphosphorylierung des hepatocytus-proliferator-rezeptors hemmen, und diese enthaltende medizinische zusammensetzung
KR100397792B1 (ko) * 2001-06-28 2003-09-13 한국과학기술연구원 4-(페닐아미노)-[1,4]디옥사노[2,3-ｇ]퀴나졸린 유도체 및그의 제조방법
GB0118752D0 (en) * 2001-08-01 2001-09-26 Pfizer Ltd Process for the production of quinazolines
US7229774B2 (en) 2001-08-02 2007-06-12 Regents Of The University Of Michigan Expression profile of prostate cancer
US20030066060A1 (en) 2001-09-28 2003-04-03 Ford Richard L. Cross profile guided optimization of program execution
WO2003033472A1 (fr) * 2001-10-17 2003-04-24 Kirin Beer Kabushiki Kaisha Derives de quinoline ou de quinazoline inhibant l'autophosphorylation de recepteurs du facteur de croissance des fibroblastes
AU2002361577A1 (en) 2001-10-30 2003-05-12 Merck And Co., Inc. Tyrosine kinase inhibitors
GB0126433D0 (en) 2001-11-03 2002-01-02 Astrazeneca Ab Compounds
GB0128108D0 (en) 2001-11-23 2002-01-16 Astrazeneca Ab Therapeutic use
TW200300348A (en) * 2001-11-27 2003-06-01 American Cyanamid Co 3-cyanoquinolines as inhibitors of egf-r and her2 kinases
WO2003048159A1 (en) 2001-12-05 2003-06-12 Astrazeneca Ab Quinoline derivatives
WO2003047584A1 (en) 2001-12-05 2003-06-12 Astrazeneca Ab Quinoline derivatives
GB0129099D0 (en) 2001-12-05 2002-01-23 Astrazeneca Ab Chemical compounds
BR0214499A (pt) * 2001-12-12 2005-05-10 Pfizer Prod Inc Derivados de quinazolina para o tratamento do crescimento anormal das células
EA007412B1 (ru) 2001-12-12 2006-10-27 Пфайзер Продактс Инк. Соли е-2-метокси-n-(3-(4-(3-метилпиридин-3-илокси)фениламино)хиназолин-6-ил-аллил)ацетамида, их получение и их применение против рака
TW200301123A (en) 2001-12-21 2003-07-01 Astrazeneca Uk Ltd New use
AU2002361846A1 (en) 2001-12-21 2003-07-15 Bayer Pharmaceuticals Corporation Quinazoline and quinoline derivative compounds as inhibitors of prolylpeptidase, inducers of apoptosis and cancer treatment agents
CN100491372C (zh) 2001-12-24 2009-05-27 阿斯特拉曾尼卡有限公司 作为欧若拉激酶抑制剂的取代喹唑啉衍生物
WO2003064421A1 (en) 2002-01-29 2003-08-07 Glaxo Group Limited Aminopiperidine derivatives
AU2003239302A1 (en) 2002-01-29 2003-09-02 Glaxo Group Limited Aminopiperidine compounds, process for their preparation, and pharmaceutical compositions containing them
EP2292615A1 (de) 2002-02-01 2011-03-09 AstraZeneca AB Chinazoline Verbindungen
DE10204462A1 (de) 2002-02-05 2003-08-07 Boehringer Ingelheim Pharma Verwendung von Tyrosinkinase-Inhibitoren zur Behandlung inflammatorischer Prozesse
WO2003074497A1 (en) * 2002-03-01 2003-09-12 Pintex Pharmaceutical, Inc. Pin1-modulating compounds and methods of use thereof
DE10217689A1 (de) 2002-04-19 2003-11-13 Boehringer Ingelheim Pharma Bicyclische Heterocyclen, diese Verbindungen enthaltende Arzneimittel, ihre Verwendung und Verfahren zu ihrer Herstellung
US7598258B2 (en) * 2002-05-01 2009-10-06 Kirin Beer Kabushiki Kaisha Quinoline derivatives and quinazoline derivatives inhibiting autophosphorylation of macrophage colony stimulating factor receptor
ES2400339T3 (es) 2002-07-15 2013-04-09 Symphony Evolution, Inc. Compuestos, composiciones farmacéuticas de los mismos y su uso en el tratamiento del cáncer
AU2003257666A1 (en) * 2002-08-23 2004-03-11 Kirin Beer Kabushiki Kaisha COMPOUND HAVING TGFss INHIBITORY ACTIVITY AND MEDICINAL COMPOSITION CONTAINING THE SAME
GB0219746D0 (en) 2002-08-23 2002-10-02 Inst Of Ex Botany Ascr Azapurine derivatives
AU2003301430A1 (en) 2002-10-21 2004-05-04 Kirin Beer Kabushiki Kaisha N-{2-chloro-4-((6,7-dimethoxy-4-quinolyl)oxy)phenyl}-n'-(5-methyl-3-isoxazolyl)urea salt in crystalline form
AU2003280599A1 (en) * 2002-10-29 2004-05-25 Kirin Beer Kabushiki Kaisha QUINOLINE DERIVATIVES AND QUINAZOLINE DERIVATIVES INHIBITING AUTOPHOSPHORYLATION OF Flt3 AND MEDICINAL COMPOSITIONS CONTAINING THE SAME
PL215161B1 (pl) 2002-11-04 2013-10-31 Astrazeneca Ab Pochodne chinazoliny, sposób ich wytwarzania, kompozycje farmaceutyczne je zawierajace oraz ich zastosowanie
US20040156869A1 (en) 2002-12-13 2004-08-12 Neurogen Corporation 2-substituted quinazolin-4-ylamine analogues
AU2003303045A1 (en) 2002-12-18 2004-07-09 Pfizer Products Inc. 4-anilino quinazoline derivatives for the treatment of abnormal cell growth
WO2004058267A1 (en) 2002-12-23 2004-07-15 Ariad Pharmaceuticals, Inc. Heterocycles and uses thereof
WO2004060373A1 (ja) * 2002-12-27 2004-07-22 Santen Pharmaceutical Co., Ltd. 滲出型加齢黄斑変性治療剤
US8176532B1 (en) * 2003-03-17 2012-05-08 Sprint Communications Company L.P. Secure access point for scada devices
KR100559180B1 (ko) * 2003-05-20 2006-03-14 김민서 조건부 거래에 따른 전자결제 방법 및 전자결제 서버
WO2005003140A1 (en) 2003-07-02 2005-01-13 Pharmacia & Upjohn Company Llc 4-oxo-4,7-dihydrothieno[2,3-b]pyridine-5-carboxamides as antiviral agents
WO2005005389A2 (en) 2003-07-07 2005-01-20 Merck Patent Gmbh Malonamide derivatives
EP1673085B1 (de) 2003-09-26 2011-11-09 Exelixis, Inc. C-met-modulatoren und anwendungsverfahren
JP2007518823A (ja) 2004-01-23 2007-07-12 アムゲン インコーポレイテッド キノリン、キナゾリン、ピリジン、及びピリミジン化合物と炎症、血管新生、及び癌に対する治療におけるそれら化合物の用途
US20050288290A1 (en) * 2004-06-28 2005-12-29 Borzilleri Robert M Fused heterocyclic kinase inhibitors
WO2006014325A2 (en) * 2004-07-02 2006-02-09 Exelixis, Inc. C-met modulators and method of use
EP1874759A4 (de) * 2005-04-06 2009-07-15 Exelixis Inc C-met-modulatoren und anwendungsverfahren
US7594258B2 (en) * 2005-06-27 2009-09-22 Yahoo! Inc. Access control systems and methods using visibility tokens with automatic propagation
WO2008035209A2 (en) * 2006-05-30 2008-03-27 Methylgene Inc. Inhibitors of protein tyrosine kinase activity
AU2009300328A1 (en) 2008-10-01 2010-04-08 Ludwig Institute For Cancer Research Methods for the treatment of cancer
EP2367795A1 (de) * 2008-12-04 2011-09-28 Exelixis, Inc. Verfahren zur herstellung von chinolinderivaten
TWI447108B (zh) * 2009-01-16 2014-08-01 Exelixis Inc Ｎ－（４－｛〔６，７雙（甲氧基）喹啉－４－基〕氧基｝苯基）－ｎ’－（４－氟苯基）環丙烷－１，１－二甲醯胺之蘋果酸鹽及其結晶型
EA201200144A1 (ru) * 2009-07-17 2012-08-30 Экселиксис, Инк. Кристаллические формы n-[3-фтор-4-({6-(метилокси)-7-[(3-морфолин-4-илпропил)окси]хинолин-4-ил}окси)фенил]-n'-(4-фторфенил)циклопропан-1,1-дикарбоксамида
UA108618C2 (uk) 2009-08-07 2015-05-25 Застосування c-met-модуляторів в комбінації з темозоломідом та/або променевою терапією для лікування раку
WO2011031840A1 (en) 2009-09-09 2011-03-17 Quintiles Transnational Corp. Methods and compositions for the treatment of receptor tyrosine kinase mediated diseases or disorders
JP5461213B2 (ja) 2010-01-29 2014-04-02 三洋電機株式会社 空気調和装置の室外ユニット
US20120070368A1 (en) * 2010-04-16 2012-03-22 Exelixis, Inc. Methods of Using C-Met Modulators
US20120252840A1 (en) * 2011-04-04 2012-10-04 Exelixis, Inc. Method of Treating Cancer

Also Published As

Publication number Publication date
US8476298B2 (en) 2013-07-02
US8067436B2 (en) 2011-11-29
SI2392564T1 (sl) 2014-02-28
JP2010235631A (ja) 2010-10-21
SI2392565T1 (sl) 2014-05-30
SI2213661T1 (sl) 2011-11-30
SI2210607T1 (sl) 2011-11-30
EP2392565A1 (de) 2011-12-07
US20070244116A1 (en) 2007-10-18
JP2010280674A (ja) 2010-12-16
JP5694501B2 (ja) 2015-04-01
EP2609919A3 (de) 2014-02-26
ES2651730T3 (es) 2018-01-29
EP2210607B1 (de) 2011-08-17
BE2014C055I2 (de) 2023-12-14
HK1164313A1 (en) 2012-09-21
AU2010204459A1 (en) 2010-08-19
EP3329918A2 (de) 2018-06-06
PT2210607E (pt) 2012-01-31
US20070054928A1 (en) 2007-03-08
US20160185725A1 (en) 2016-06-30
EP2392565B1 (de) 2014-03-19
HRP20140563T1 (hr) 2014-07-18
EP1673085A2 (de) 2006-06-28
US20140155378A9 (en) 2014-06-05
PL2392565T3 (pl) 2014-08-29
HK1256476A1 (zh) 2019-09-27
US20090105299A1 (en) 2009-04-23
US20210253530A9 (en) 2021-08-19
CY1112056T1 (el) 2015-11-04
EP3329918A3 (de) 2018-08-15
CA2537812A1 (en) 2005-04-07
ATE517091T1 (de) 2011-08-15
US7579473B2 (en) 2009-08-25
EP2210607A1 (de) 2010-07-28
JP5325172B2 (ja) 2013-10-23
US8497284B2 (en) 2013-07-30
AU2004275842B2 (en) 2010-09-02
JP2014055191A (ja) 2014-03-27
JP2014074059A (ja) 2014-04-24
EP2392564B1 (de) 2013-10-23
JP4638436B2 (ja) 2011-02-23
US20150376133A1 (en) 2015-12-31
EP2409704A2 (de) 2012-01-25
CY1111956T1 (el) 2015-11-04
US20130252940A1 (en) 2013-09-26
JP5325173B2 (ja) 2013-10-23
HK1141799A1 (en) 2010-11-19
CA2744997A1 (en) 2005-04-07
US9174947B2 (en) 2015-11-03
JP5185331B2 (ja) 2013-04-17
US20140155396A1 (en) 2014-06-05
JP2019070015A (ja) 2019-05-09
JP2015131859A (ja) 2015-07-23
NL300678I2 (de) 2017-01-31
ES2925655T3 (es) 2022-10-19
DK2213661T3 (da) 2011-09-19
EP1673085A4 (de) 2008-12-10
US20200331860A1 (en) 2020-10-22
ES2466818T3 (es) 2014-06-11
EP2612853A1 (de) 2013-07-10
EP2409704B1 (de) 2017-09-20
ES2371383T3 (es) 2011-12-30
EP2609919A2 (de) 2013-07-03
ES2436888T3 (es) 2014-01-07
EP2392564A1 (de) 2011-12-07
HRP20140012T1 (hr) 2014-02-14
HK1143068A1 (en) 2010-12-24
HRP20110707T1 (hr) 2011-10-31
CY2014037I2 (el) 2019-07-10
LU92508I2 (fr) 2015-11-02
US20170355678A1 (en) 2017-12-14
US11124482B2 (en) 2021-09-21
US20110077233A1 (en) 2011-03-31
US20070225307A1 (en) 2007-09-27
HK1164312A1 (en) 2012-09-21
HRP20110810T1 (hr) 2011-12-31
AU2010204459B2 (en) 2013-06-20
US8178532B2 (en) 2012-05-15
CY2014037I1 (el) 2015-11-04
EP1673085B1 (de) 2011-11-09
AU2010204461A1 (en) 2010-08-19
JP2007506777A (ja) 2007-03-22
JP2021050233A (ja) 2021-04-01
US20090170896A1 (en) 2009-07-02
JP2014055190A (ja) 2014-03-27
WO2005030140A3 (en) 2005-05-19
HUS1400052I1 (hu) 2022-02-28
ATE532782T1 (de) 2011-11-15
JP2011042686A (ja) 2011-03-03
AU2004275842A1 (en) 2005-04-07
PL2213661T3 (pl) 2011-12-30
CA2537812C (en) 2013-01-22
JP2010265302A (ja) 2010-11-25
DK2392565T3 (da) 2014-05-05
WO2005030140A2 (en) 2005-04-07
DK2392564T3 (da) 2014-01-13
EP2213661A1 (de) 2010-08-04
JP2017160270A (ja) 2017-09-14
US20120184523A1 (en) 2012-07-19
FR14C0067I1 (de) 2014-10-17
EP2409704A3 (de) 2013-02-13
EP2213661B1 (de) 2011-07-20
US20120022065A1 (en) 2012-01-26
AU2010204461B2 (en) 2013-06-20
PT2213661E (pt) 2011-12-15
DK2210607T3 (da) 2011-12-12
ES2369652T3 (es) 2011-12-02
PL2210607T3 (pl) 2012-01-31
JP5185332B2 (ja) 2013-04-17
JP2024023447A (ja) 2024-02-21
JP2010235632A (ja) 2010-10-21
FR14C0067I2 (fr) 2015-11-20
EP3329918B1 (de) 2022-05-25

Similar Documents

Publication Publication Date Title
ATE520403T1 (de) N-ä3-fluoro-4-(ä6-(methyloxy)-7-ä(3-morpholin-4 ylpropyl)oxyüquinolin-4-ylüoxy)phenylü-n'-(4- fluorophenyl)cyclopropane-1,1-dicarboxamid zur behandlung von krebs
WO2004006846A3 (en) Receptor-type kinase modulators and methods of use
WO2006014325A3 (en) C-met modulators and method of use
WO2005020921A3 (en) C-kit modulators and methods of use
WO2004092196A3 (en) Tie-2 modulators and methods of use
EA200200473A1 (ru) Ингибиторы тирозинкиназы
WO2004091480A3 (en) Tie-2 modulators and methods of use
DE69520499D1 (de) Histidine und homohistidine derivate zur verwendung als protein farnesyltransferase hemmstoffe
EA201300713A1 (ru) Варианты, происходящие из actriib, и их применение
DE60023926D1 (de) Tyrosin kinase inhibitoren
DE60018782D1 (de) Tyrosin kinase inhibitoren
ATE316088T1 (de) Tyrosin-kinase inhibitoren
WO2005023202A3 (en) Tumor suppressor lkb1 kinase directly activates amp-activated kinase
WO2004083235A3 (en) Tie-2 modulators and methods of use
DE60334289D1 (de) Dithiolopyrrolon-derivate zur behandlung von proliferativen störungen
ATE386748T1 (de) Verwendung von liganden von cd52 antigen zur behandlung von soliden tumoren und von knochenkrebserkrankungen
DE60228056D1 (de) Verfahren und zusammensetzungen zur modulierung der gluconeogenese mit pgc-1
EA201990964A1 (ru) Варианты, происходящие из actriib, и их применение

Legal Events

Date Code Title Description
UEP Publication of translation of european patent specification

Ref document number: 2210607

Country of ref document: EP