HK1051539A1 - Benzamides and related inhibitors of factor xa - Google Patents

Benzamides and related inhibitors of factor xa

Info

Publication number
HK1051539A1
HK1051539A1 HK03103788A HK03103788A HK1051539A1 HK 1051539 A1 HK1051539 A1 HK 1051539A1 HK 03103788 A HK03103788 A HK 03103788A HK 03103788 A HK03103788 A HK 03103788A HK 1051539 A1 HK1051539 A1 HK 1051539A1
Authority
HK
Hong Kong
Prior art keywords
factor
benzamides
compounds
related inhibitors
compositions
Prior art date
Application number
HK03103788A
Other languages
English (en)
Inventor
Bing-Yan Zhu
Penglie Zhang
Lingyan Wang
Wenrong Huang
Erick Goldman
Wenhao Li
Jingmei Zuckett
Yonghong Song
Robert Scarborough
Original Assignee
Millennium Pharm 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=26881428&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=HK1051539(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Priority claimed from US09/663,420 external-priority patent/US6844367B1/en
Application filed by Millennium Pharm Inc filed Critical Millennium Pharm Inc
Publication of HK1051539A1 publication Critical patent/HK1051539A1/xx

Links

Classifications

    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • 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
    • A61K31/60—Salicylic acid; Derivatives thereof
    • A61K31/612—Salicylic acid; Derivatives thereof having the hydroxy group in position 2 esterified, e.g. salicylsulfuric acid
    • A61K31/616—Salicylic acid; Derivatives thereof having the hydroxy group in position 2 esterified, e.g. salicylsulfuric acid by carboxylic acids, e.g. acetylsalicylic acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4858—Organic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4866—Organic macromolecular compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/28—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton
    • C07C237/42—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00—Carboxylic acid nitriles
    • C07C255/49—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C255/58—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton
    • C07C255/60—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton at least one of the singly-bound nitrogen atoms being acylated
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C257/00—Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines
    • C07C257/10—Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. amidines
    • C07C257/18—Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. amidines having carbon atoms of amidino groups bound to carbon atoms of six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C259/00—Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups
    • C07C259/12—Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. N-hydroxyamidines
    • C07C259/18—Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. N-hydroxyamidines having carbon atoms of hydroxamidine groups bound to carbon atoms of six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/15—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C311/16—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/30—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/45—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups at least one of the singly-bound nitrogen atoms being part of any of the groups, X being a hetero atom, Y being any atom, e.g. N-acylaminosulfonamides
    • C07C311/46—Y being a hydrogen or a carbon atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C317/00—Sulfones; Sulfoxides
    • C07C317/26—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton
    • C07C317/32—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
    • C07C317/34—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton having sulfone or sulfoxide groups and amino groups bound to carbon atoms of six-membered aromatic rings being part of the same non-condensed ring or of a condensed ring system containing that ring
    • C07C317/38—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton having sulfone or sulfoxide groups and amino groups bound to carbon atoms of six-membered aromatic rings being part of the same non-condensed ring or of a condensed ring system containing that ring with the nitrogen atom of at least one amino group being part of any of the groups, X being a hetero atom, Y being any atom, e.g. N-acylaminosulfones
    • C07C317/40—Y being a hydrogen or a carbon atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C317/00—Sulfones; Sulfoxides
    • C07C317/44—Sulfones; Sulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen 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
    • C07D213/72—Nitrogen atoms
    • C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
    • C07D213/82—Amides; Imides in position 3
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems 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 carbon atoms of the nitrogen-containing ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/64—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • 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
    • C07D295/12—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 singly or doubly bound nitrogen atoms
    • C07D295/125—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 singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur 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
    • C07D333/38—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • 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
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur 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
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Hydrogenated Pyridines (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pyridine Compounds (AREA)
HK03103788A 2000-02-29 2003-05-27 Benzamides and related inhibitors of factor xa HK1051539A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US18574600P 2000-02-29 2000-02-29
US09/663,420 US6844367B1 (en) 1999-09-17 2000-09-15 Benzamides and related inhibitors of factor Xa
PCT/US2001/006255 WO2001064643A2 (en) 2000-02-29 2001-02-28 BENZAMIDES AND RELATED INHIBITORS OF FACTOR Xa

Publications (1)

Publication Number Publication Date
HK1051539A1 true HK1051539A1 (en) 2003-08-08

Family

ID=26881428

Family Applications (1)

Application Number Title Priority Date Filing Date
HK03103788A HK1051539A1 (en) 2000-02-29 2003-05-27 Benzamides and related inhibitors of factor xa

Country Status (10)

Country Link
US (13) US6376515B2 (da)
EP (1) EP1259485B1 (da)
AT (1) ATE311366T1 (da)
AU (2) AU2001245353A1 (da)
CA (1) CA2401778C (da)
DE (1) DE60115394T2 (da)
DK (1) DK1259485T3 (da)
ES (1) ES2254385T3 (da)
HK (1) HK1051539A1 (da)
WO (2) WO2001064642A2 (da)

Families Citing this family (224)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6822267B1 (en) * 1997-08-20 2004-11-23 Advantest Corporation Signal transmission circuit, CMOS semiconductor device, and circuit board
DK1259485T3 (da) * 2000-02-29 2006-04-10 Millennium Pharm Inc Benzamider og beslægtede inhibitorer for faktor Xa
AU776053B2 (en) 2000-03-31 2004-08-26 Astellas Pharma Inc. Diazepan derivatives or salts thereof
TWI288745B (en) 2000-04-05 2007-10-21 Daiichi Seiyaku Co Ethylenediamine derivatives
ES2292607T3 (es) 2000-07-27 2008-03-16 Eli Lilly And Company Amidas heterociclicas sustituidas.
AU2002224064B2 (en) 2000-11-22 2005-12-08 Astellas Pharma Inc. Substituted benzene derivatives or salts thereof
EP1379506A2 (en) 2000-11-28 2004-01-14 Eli Lilly And Company Substituted carboxamides
US7067539B2 (en) 2001-02-08 2006-06-27 Schering Corporation Cannabinoid receptor ligands
US7507767B2 (en) 2001-02-08 2009-03-24 Schering Corporation Cannabinoid receptor ligands
US7312235B2 (en) * 2001-03-30 2007-12-25 Millennium Pharmaceuticals, Inc. Benzamide inhibitors of factor Xa
WO2003000657A1 (fr) 2001-06-20 2003-01-03 Daiichi Pharmaceutical Co., Ltd. Derives de diamine
SE0102764D0 (sv) * 2001-08-17 2001-08-17 Astrazeneca Ab Compounds
AUPR738301A0 (en) * 2001-08-30 2001-09-20 Starpharma Limited Chemotherapeutic agents
KR20100107509A (ko) 2001-09-14 2010-10-05 9222-9129 퀘벡 인코포레이티드 히스톤 데아세틸라아제의 억제제
US7868204B2 (en) 2001-09-14 2011-01-11 Methylgene Inc. Inhibitors of histone deacetylase
US6897220B2 (en) * 2001-09-14 2005-05-24 Methylgene, Inc. Inhibitors of histone deacetylase
NZ532291A (en) 2001-11-14 2005-11-25 Schering Corp Cannabinoid receptor ligands
EP1314733A1 (en) 2001-11-22 2003-05-28 Aventis Pharma Deutschland GmbH Indole-2-carboxamides as factor Xa inhibitors
US7030141B2 (en) 2001-11-29 2006-04-18 Christopher Franklin Bigge Inhibitors of factor Xa and other serine proteases involved in the coagulation cascade
WO2003050088A1 (en) 2001-12-07 2003-06-19 Eli Lilly And Company Substituted heterocyclic carboxamides with antithrombotic activity
US20050026929A1 (en) * 2002-04-23 2005-02-03 Axys Pharmaceuticals, Inc. Novel phenyl derivatives as inducers of apoptosis
MXPA04012704A (es) 2002-06-19 2005-03-23 Schering Corp Agonistas de los receptores canabinoides.
TW200409637A (en) 2002-06-26 2004-06-16 Glaxo Group Ltd Compounds
GB0215293D0 (en) * 2002-07-03 2002-08-14 Rega Foundation Viral inhibitors
US7307088B2 (en) * 2002-07-09 2007-12-11 Amgen Inc. Substituted anthranilic amide derivatives and methods of use
WO2004035047A1 (en) 2002-10-18 2004-04-29 F. Hoffmann-La Roche Ag 4-piperazinyl benzenesulfonyl indoles with 5-ht6 receptor affinity
GB0226930D0 (en) 2002-11-19 2002-12-24 Astrazeneca Ab Chemical compounds
SI1569912T1 (sl) 2002-12-03 2015-09-30 Pharmacyclics Llc Derivati 2-(2-hidroksibifenil-3-il)-1h-benzoimidazol-5-karboksamidina kot inhibitorji faktorja viia
US7696225B2 (en) 2003-01-06 2010-04-13 Osi Pharmaceuticals, Inc. (2-carboxamido)(3-Amino) thiophene compounds
TWI299664B (en) 2003-01-06 2008-08-11 Osi Pharm Inc (2-carboxamido)(3-amino)thiophene compounds
KR20050096956A (ko) 2003-02-07 2005-10-06 다이이찌 세이야꾸 가부시기가이샤 피라졸 유도체
TW200505902A (en) 2003-03-20 2005-02-16 Schering Corp Cannabinoid receptor ligands
EP1720844B1 (de) * 2003-04-03 2009-04-29 MERCK PATENT GmbH Pyrrolidin-1,2-dicarbonsäure-1-(phenylamid)-2-(4-(3-oxo-morpholin-4-yl)-phenylamid) derivate und verwandte verbindungen als inhibitoren des koagulationsfaktors xa zur behandlung von thromboembolischen erkrankungen
KR20050109617A (ko) * 2003-04-03 2005-11-21 메르크 파텐트 게엠베하 혈전증 치료용 응집 인자 ｘａ 저해제로서의피라졸리딘-１,２-디카르복실디페닐아미드 유도체
TWI372050B (en) 2003-07-03 2012-09-11 Astex Therapeutics Ltd (morpholin-4-ylmethyl-1h-benzimidazol-2-yl)-1h-pyrazoles
NZ544756A (en) 2003-07-22 2009-09-25 Astex Therapeutics Ltd 3,4-Disubstituted 1H-pyrazole compounds and their use as cyclin dependent kinases (CDK) and glycogen synthase kinase-3 (GSK-3) modulators
ATE352550T1 (de) 2003-09-19 2007-02-15 Astrazeneca Ab Chinazolinderivate
KR101153335B1 (ko) * 2003-09-24 2012-07-05 메틸진 인코포레이티드 히스톤 데아세틸라제의 억제제
SE0302573D0 (sv) * 2003-09-26 2003-09-26 Astrazeneca Ab Benzimidazole derivatives, compositions containing them, preparation thereof and uses thereof
WO2005049604A2 (en) * 2003-09-30 2005-06-02 Eli Lilly And Company Antithrombotic aromatic ethers
TW200526631A (en) 2003-10-07 2005-08-16 Renovis Inc Amide derivatives as ion-channel ligands and pharmaceutical compositions and methods of using the same
JP2007508308A (ja) 2003-10-09 2007-04-05 ミレニアム ファーマシューティカルズ インク． 第Ｘａ因子の阻害剤としてのチオエーテル置換されたベンズアミド誘導体
CA2549606C (en) 2003-12-22 2015-10-06 K.U. Leuven Research & Development Imidazo[4,5-c]pyridine compounds and methods of antiviral treatment
KR101164258B1 (ko) 2003-12-23 2012-07-11 아스텍스 테라퓨틱스 리미티드 단백질 키나아제 조절제로서의 피라졸 유도체
WO2005073193A1 (en) * 2004-01-23 2005-08-11 Amgen Inc. Vanilloid receptor ligands and their use in treatments
US20080280872A1 (en) * 2004-02-18 2008-11-13 Craig Johnstone Benzamide Derivatives and Their Use as Glucokinase Activating Agents
AU2005214137B2 (en) * 2004-02-18 2008-05-29 Astrazeneca Ab Compounds
US7253204B2 (en) * 2004-03-26 2007-08-07 Methylgene Inc. Inhibitors of histone deacetylase
US7166738B2 (en) 2004-04-23 2007-01-23 Roche Palo Alto Llc Non-nucleoside reverse transcriptase inhibitors
US7625949B2 (en) 2004-04-23 2009-12-01 Roche Palo Alto Llc Methods for treating retroviral infections
TW200600086A (en) * 2004-06-05 2006-01-01 Astrazeneca Ab Chemical compound
US7696352B2 (en) * 2004-06-18 2010-04-13 Millennium Pharmaceuticals, Inc. Factor Xa inhibitors
EP1893572B1 (en) * 2004-06-18 2016-12-14 Millennium Pharmaceuticals, Inc. Factor xa inhibitors
PA8640701A1 (es) 2004-08-03 2006-09-08 Wyeth Corp Indazoles utiles para tratamiento de enfermedades cardiovascular
MX2007003105A (es) * 2004-09-24 2007-06-07 Aztrazeneca Ab Derivados de bencimidazol, composiciones que los contienen, sus preparaciones y sus usos i.
GB0422556D0 (en) * 2004-10-11 2004-11-10 Syngenta Participations Ag Novel insecticides
GB0423044D0 (en) * 2004-10-16 2004-11-17 Astrazeneca Ab Compounds
KR20070085371A (ko) 2004-10-16 2007-08-27 아스트라제네카 아베 페녹시 벤즈아미드 화합물의 제조 방법
GB0423043D0 (en) * 2004-10-16 2004-11-17 Astrazeneca Ab Compounds
US7582673B2 (en) 2004-10-21 2009-09-01 High Point Pharmaceuticals, Llc Bissulfonamide compounds as agonists of GalR1, compositions, and methods of use
RU2007120685A (ru) 2004-11-03 2008-12-10 Ф.Хоффманн-Ля Рош Аг (Ch) ДИКАРБОКСАМИДНЫЕ ПРОИЗВОДНЫЕ И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ ИНГИБИТОРОВ ФАКТОРА Ха
ATE457302T1 (de) 2004-11-24 2010-02-15 Lilly Co Eli Aromatische etherderivate als thrombin-hemmer
US7666866B2 (en) * 2004-11-29 2010-02-23 Eli Lilly And Company Antithrombotic diamides
JP2008524246A (ja) 2004-12-16 2008-07-10 タケダ サン ディエゴ インコーポレイテッド ヒストンデアセチラーゼ阻害剤
PL1841765T3 (pl) * 2004-12-21 2009-08-31 Gilead Sciences Inc Związek imidazo[4,5-c]pirydyny i sposób leczenia przeciwwirusowego
EP1833819A1 (en) 2004-12-30 2007-09-19 Astex Therapeutics Limited Pyrazole compounds that modulate the activity of cdk, gsk and aurora kinases
BRPI0606476A2 (pt) 2005-01-07 2009-06-30 Synta Pharmaceuticals Corp compostos para inflamação e usos imuno-relacionados e suas composições farmacêuticas
AU2006207321B2 (en) 2005-01-21 2012-09-06 Astex Therapeutics Limited Pharmaceutical compounds
MX2007008781A (es) 2005-01-21 2007-09-11 Astex Therapeutics Ltd Compuestos farmaceuticos.
US8404718B2 (en) 2005-01-21 2013-03-26 Astex Therapeutics Limited Combinations of pyrazole kinase inhibitors
AR054425A1 (es) 2005-01-21 2007-06-27 Astex Therapeutics Ltd Sales de adicion de piperidin 4-il- amida de acido 4-(2,6-dicloro-benzoilamino) 1h-pirazol-3-carboxilico.
EP1847527A4 (en) * 2005-02-02 2009-04-08 Ajinomoto Kk NEW BENZAMIDINE DERIVATIVE
US7576099B2 (en) 2005-02-28 2009-08-18 Renovis, Inc. Amide derivatives as ion-channel ligands and pharmaceutical compositions and methods of using the same
US7264402B2 (en) * 2005-03-10 2007-09-04 Corning Cable Systems Llc Multi-fiber optic receptacle and plug assembly
DE602006009231D1 (de) 2005-03-10 2009-10-29 Pfizer Substituierte n-sulfonylaminophenylethyl-2-phenoxyacetamidverbindungen
JP2008540574A (ja) 2005-05-11 2008-11-20 タケダ サン ディエゴ インコーポレイテッド ヒストンデアセチラーゼ阻害剤
US20110059941A1 (en) * 2005-05-24 2011-03-10 Peter William Rodney Caulkett 2-phenyl substituted imidazol [4,5b] pyridine/pyrazine and purine derivatives as glucokinase modulators
TW200714597A (en) * 2005-05-27 2007-04-16 Astrazeneca Ab Chemical compounds
JP2008546751A (ja) 2005-06-22 2008-12-25 アステックス・セラピューティクス・リミテッド 医薬組成物
WO2006136837A2 (en) 2005-06-23 2006-12-28 Astex Therapeutics Limited Pharmaceutical combinations comprising pyrazole derivatives as protein kinase modulators
NZ575512A (en) * 2005-07-09 2009-11-27 Astrazeneca Ab Heteroaryl benzamide derivatives for use as GLK activators in the treatment of diabetes
EP2027113A1 (en) * 2005-07-09 2009-02-25 AstraZeneca AB Heteroaryl benzamide derivatives for use as glk activators in the treatment of diabetes
JP2009500442A (ja) * 2005-07-09 2009-01-08 アストラゼネカ アクチボラグ ２型糖尿病を処置するためのグルコキナーゼのモジュレーターとしての２−ヘテロシクリルオキシベンゾイルアミノヘテロシクリル化合物
JP2009501236A (ja) * 2005-07-14 2009-01-15 タケダ サン ディエゴ インコーポレイテッド ヒストンデアセチラーゼ阻害剤
US9202182B2 (en) * 2005-08-11 2015-12-01 International Business Machines Corporation Method and system for analyzing business architecture
ATE478044T1 (de) 2005-09-16 2010-09-15 Arrow Therapeutics Ltd Biphenylderivate und ihre verwendung bei der behandlung von hepatitis c
BRPI0617720A2 (pt) 2005-10-19 2011-08-02 Hoffmann La Roche compostos inibidores de nnrt de fenil-acetamida, usos dos referidos compostos e composição farmacêutica que os contém
NZ592533A (en) * 2005-11-08 2012-08-31 Millennium Pharm Inc METHOD FOR THE PREPARATION OF N-(5-CHLORO-2-PYRIDINYL)-2-[[4-[(DIMETHYLAMINO) IMINOMETHYL] BENZOYL] AMINO]-5-METHOXY-BENZAMIDE, A FACTOR Xa INHIBITOR
TW200738621A (en) 2005-11-28 2007-10-16 Astrazeneca Ab Chemical process
EP1968579A1 (en) 2005-12-30 2008-09-17 Astex Therapeutics Limited Pharmaceutical compounds
JP2009525955A (ja) * 2006-01-13 2009-07-16 タケダ サン ディエゴ インコーポレイテッド ヒストンデアセチラーゼ阻害剤
EP1991226B1 (en) 2006-02-28 2013-03-20 Merck Sharp & Dohme Corp. Inhibitors of histone deacetylase
TW200745049A (en) * 2006-03-23 2007-12-16 Astrazeneca Ab New crystalline forms
WO2007112367A2 (en) * 2006-03-27 2007-10-04 Portola Pharmaceuticals, Inc. Potassium channel modulators and platelet procoagulant activity
JP2009531385A (ja) 2006-03-31 2009-09-03 グラクソ グループ リミテッド 成長ホルモン分泌促進物質（ｇｈｓ）受容体アゴニストとしてのピペラジン誘導体
CN101466670B (zh) * 2006-04-07 2013-04-17 梅特希尔基因公司 组蛋白脱乙酰酶抑制剂
TW200808769A (en) * 2006-04-18 2008-02-16 Astrazeneca Ab Therapeutic compounds
CN101490036B (zh) * 2006-05-05 2013-07-17 米伦纽姆医药公司 Xa因子抑制剂
WO2008001101A2 (en) * 2006-06-29 2008-01-03 Astex Therapeutics Limited Pharmaceutical combinations
US8435970B2 (en) 2006-06-29 2013-05-07 Astex Therapeutics Limited Pharmaceutical combinations of 1-cyclopropyl-3-[3-(5-morpholin-4-ylmethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-urea
AR061969A1 (es) * 2006-07-07 2008-08-10 Gilead Sciences Inc Derivados halogenados de imidazo-piridino, metodo de preparacion, composiciones farmaceuticas que los contienen y usos como agentes anti vhc
TW200825063A (en) * 2006-10-23 2008-06-16 Astrazeneca Ab Chemical compounds
SA07280576B1 (ar) * 2006-10-26 2011-06-22 استرازينيكا ايه بي مركبات بنزويل أمينو سيكليل غير متجانسة بأعتبارها عوامل منشطة للجلوكوكيناز
PT2404906E (pt) 2006-11-02 2015-11-02 Millennium Pharm Inc Métodos de sintetizar sais farmacêuticos de um inibidor de fator xa
AU2007320906A1 (en) * 2006-11-13 2008-05-22 Pfizer Products Inc. Diaryl, dipyridinyl and aryl-pyridinyl derivatives and uses thereof
EP2101760B1 (en) * 2006-12-08 2013-02-27 Millennium Pharmaceuticals, Inc. Unit dose formulations and methods of treating thrombosis with an oral factor xa inhibitor
CN101595104A (zh) * 2006-12-21 2009-12-02 阿斯利康(瑞典)有限公司 作为glk活化剂的新的晶态化合物
EP2114930A2 (en) * 2007-01-05 2009-11-11 Millennium Pharmaceuticals, Inc. Factor xa inhibitors
UY30892A1 (es) * 2007-02-07 2008-09-02 Smithkline Beckman Corp Inhibidores de la actividad akt
WO2008112941A1 (en) * 2007-03-13 2008-09-18 Board Of Regents The University Of Texas System Composition and method for the treatment of diseases affected by a peptide receptor
GB0704932D0 (en) 2007-03-14 2007-04-25 Astex Therapeutics Ltd Pharmaceutical compounds
AU2008239659B2 (en) * 2007-04-13 2013-09-05 Millennium Pharmaceuticals, Inc. Combination anticoagulant therapy with a compound that acts as a factor Xa inhibitor
NZ599556A (en) * 2007-05-02 2013-10-25 Portola Pharm Inc Combination therapy with a compound acting as a platelet adp receptor inhibitor
UA99466C2 (en) 2007-07-06 2012-08-27 Гилиад Сайенсиз, Инк. Crystalline pyridazine compound
LT2193196T (lt) * 2007-09-28 2016-12-12 Portola Pharmaceuticals, Inc. Faktoriaus xa inhibitoriu antidotai ir jų panaudojimo būdai
US8268783B2 (en) 2007-09-28 2012-09-18 Portola Pharmaceuticals, Inc. Antidotes for factor Xa inhibitors and methods of using the same
UA103319C2 (en) 2008-05-06 2013-10-10 Глаксосмитклайн Ллк Thiazole- and oxazole-benzene sulfonamide compounds
EA201100097A1 (ru) 2008-08-04 2011-10-31 Астразенека Аб Производные пиразоло[3,4]пиримидин-4-ила и их применения для лечения диабета и ожирения
EP2364165B1 (en) 2008-11-14 2018-01-03 Portola Pharmaceuticals, Inc. Antidotes for factor xa inhibitors and methods of using the same in combination with blood coagulating agents
US20110288142A1 (en) * 2009-01-30 2011-11-24 Chen Pingyun Y CRYSTALLINE N--5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecarboxamide hydrochloride
GB0902406D0 (en) * 2009-02-13 2009-04-01 Astrazeneca Ab Crystalline polymorphic form
GB0902434D0 (en) * 2009-02-13 2009-04-01 Astrazeneca Ab Chemical process
EP2406389B1 (en) 2009-03-13 2019-05-08 Agios Pharmaceuticals, Inc. Methods and compositions for cell-proliferation-related disorders
JP5756457B2 (ja) 2009-04-06 2015-07-29 アジオス ファーマシューティカルズ， インコーポレイテッド ピルビン酸キナーゼｍ２調節剤、治療組成物および関連する使用方法
WO2010116177A1 (en) 2009-04-09 2010-10-14 Astrazeneca Ab A pyrazolo [4,5-e] pyrimidine derivative and its use to treat diabetes and obesity
AR076221A1 (es) * 2009-04-09 2011-05-26 Astrazeneca Ab Derivado de pirazol [4,5-e] pirimidina y su uso para tratar diabetes y obesidad
PT2448582T (pt) 2009-06-29 2017-07-10 Agios Pharmaceuticals Inc Compostos e composições terapêuticas
PT2453910T (pt) 2009-07-15 2016-12-07 Portola Pharm Inc Formulação de dose unitária de antídoto contra inibidores de fator xa para uso na prevenção de sangramento
US20110086853A1 (en) * 2009-10-08 2011-04-14 William Brown Therapeutic Compounds
EP2491145B1 (en) 2009-10-21 2016-03-09 Agios Pharmaceuticals, Inc. Methods and compositions for cell-proliferation-related disorders
CA2784921A1 (en) 2009-12-17 2011-07-14 Millennium Pharmaceuticals, Inc. Salts and crystalline forms of a factor xa inhibitor
US8394964B2 (en) 2009-12-17 2013-03-12 Millennium Pharmaceuticals, Inc. Methods of synthesizing factor Xa inhibitors
US8742120B2 (en) 2009-12-17 2014-06-03 Millennium Pharmaceuticals, Inc. Methods of preparing factor xa inhibitors and salts thereof
EA015918B1 (ru) * 2010-03-03 2011-12-30 Дмитрий Геннадьевич ТОВБИН УРЕТАНЫ, МОЧЕВИНЫ, АМИДЫ И РОДСТВЕННЫЕ ИНГИБИТОРЫ ФАКТОРА Xa
EP2575453B1 (en) 2010-05-28 2018-08-01 The Board of Regents of the University of Texas System Oligo-benzamide compounds and their use
WO2012054110A2 (en) 2010-07-07 2012-04-26 Ardelyx, Inc. Compounds and methods for inhibiting phosphate transport
EP2590965B1 (en) 2010-07-07 2016-04-20 Ardelyx, Inc. Compounds and methods for inhibiting phosphate transport
JP5827326B2 (ja) 2010-07-07 2015-12-02 アーデリクス，インコーポレーテッド リン酸輸送を阻害する化合物及び方法
WO2012006477A1 (en) 2010-07-07 2012-01-12 Ardelyx, Inc. Compounds and methods for inhibiting phosphate transport
AR082803A1 (es) 2010-09-01 2013-01-09 Portola Pharm Inc Metodos y formulaciones para el tratamiento de la trombosis con betrixaban y un inhibidor de la glicoproteina p
AR082804A1 (es) 2010-09-01 2013-01-09 Portola Pharm Inc Formas cristalinas de un inhibidor del factor xa
JP5837091B2 (ja) 2010-12-17 2015-12-24 アジオス ファーマシューティカルズ， インコーポレイテッド ピルビン酸キナーゼｍ２（ｐｋｍ２）調節剤としての新規ｎ−（４−（アゼチジン−１−カルボニル）フェニル）−（ヘテロ−）アリールスルホンアミド誘導体
US9328077B2 (en) 2010-12-21 2016-05-03 Agios Pharmaceuticals, Inc Bicyclic PKM2 activators
TWI549947B (zh) 2010-12-29 2016-09-21 阿吉歐斯製藥公司 治療化合物及組成物
JP2014506448A (ja) 2011-01-19 2014-03-17 バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツング 凝固因子の阻害剤に対する結合タンパク質
GB201104267D0 (en) 2011-03-14 2011-04-27 Cancer Rec Tech Ltd Pyrrolopyridineamino derivatives
CA2834602C (en) 2011-05-03 2020-10-06 Agios Pharmaceuticals, Inc. Pyruvate kinase activators for use in therapy
ES2746558T3 (es) 2011-05-03 2020-03-06 Agios Pharmaceuticals Inc Activadores de piruvato cinasa R para uso en terapia
JP5934782B2 (ja) 2011-05-04 2016-06-15 メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． アミノ−ピリジン含有脾臓チロシンキナーゼ（Ｓｙｋ）阻害薬
CN102827170A (zh) 2011-06-17 2012-12-19 安吉奥斯医药品有限公司 治疗活性组合物和它们的使用方法
CN102827073A (zh) 2011-06-17 2012-12-19 安吉奥斯医药品有限公司 治疗活性组合物和它们的使用方法
US20150224091A1 (en) 2011-08-31 2015-08-13 Portola Pharmaceuticals, Inc. Prevention and treatment of thrombosis in medically ill patients
EP2578582A1 (en) 2011-10-03 2013-04-10 Respivert Limited 1-Pyrazolyl-3-(4-((2-anilinopyrimidin-4-yl)oxy)napththalen-1-yl)ureas as p38 MAP kinase inhibitors
ES2583853T3 (es) 2011-10-03 2016-09-22 Respivert Limited 1-Pirazolil-3-(4-((2-anilinopirimidin-4-il)oxi)naftalen-1-il)ureas como inhibidores de p38 MAP cinasa
US8754124B2 (en) 2011-11-23 2014-06-17 Board Of Regents, The University Of Texas System Oligo-benzamide compounds and their use in treating cancers
US8835493B2 (en) 2011-11-23 2014-09-16 Board Of Regents, The University Of Texas System Oligo-benzamide compounds for use in treating cancers
US9474779B2 (en) 2012-01-19 2016-10-25 Agios Pharmaceuticals, Inc. Therapeutically active compositions and their methods of use
ES2860299T3 (es) 2012-04-24 2021-10-04 Vertex Pharma Inhibidores de DNA-PK
GB201214750D0 (en) 2012-08-17 2012-10-03 Respivert Ltd Compounds
GB201215357D0 (en) 2012-08-29 2012-10-10 Respivert Ltd Compounds
GB201216018D0 (en) 2012-09-07 2012-10-24 Cancer Rec Tech Ltd Pharmacologically active compounds
JP2015531395A (ja) 2012-10-04 2015-11-02 ファイザー・リミテッドＰｆｉｚｅｒ Ｌｉｍｉｔｅｄ ピロロ［３，２−ｃ］ピリジントロポミオシン関連キナーゼ阻害剤
US20140346397A1 (en) 2012-12-27 2014-11-27 Portola Pharmaceuticals, Inc. Compounds and methods for purification of serine proteases
US9200268B2 (en) 2012-12-27 2015-12-01 Portola Pharmaceuticals, Inc. Compounds and methods for purification of serine proteases
FR3000895B1 (fr) 2013-01-11 2017-02-24 Laboratoire Francais Du Fractionnement Et Des Biotechnologies Sa Utilisation d'antidotes d'inhibiteurs de la coagulation indiques dans la prevention ou le traitement de pathologies thromboemboliques
ES2711839T3 (es) 2013-03-12 2019-05-07 Vertex Pharma Inhibidores de DNA-PK
US20160016934A1 (en) 2013-03-14 2016-01-21 Respivert Limited Kinase inhibitors
WO2015003355A2 (en) 2013-07-11 2015-01-15 Agios Pharmaceuticals, Inc. Therapeutically active compounds and their methods of use
WO2015003360A2 (en) 2013-07-11 2015-01-15 Agios Pharmaceuticals, Inc. Therapeutically active compounds and their methods of use
US9579324B2 (en) 2013-07-11 2017-02-28 Agios Pharmaceuticals, Inc Therapeutically active compounds and their methods of use
JP6529492B2 (ja) 2013-07-11 2019-06-12 アジオス ファーマシューティカルズ， インコーポレイテッド 癌の処置のためのｉｄｈ２突然変異体阻害剤としての２，４−または４，６−ジアミノピリミジン化合物
US20150031627A1 (en) 2013-07-25 2015-01-29 Agios Pharmaceuticals, Inc Therapeutically active compounds and their methods of use
EA201300843A1 (ru) * 2013-08-01 2015-04-30 Арсений Валерьевич Айбушев Карбамоилфенильные производные для остановки, предотвращения и профилактики кровотечений или усиления системы гемостаза
GB201314452D0 (en) 2013-08-13 2013-09-25 Ostara Biomedical Ltd Embryo implantation
DK3054936T5 (da) 2013-10-10 2024-03-18 Eastern Virginia Medical School 4-((2-hydroxy-3-methoxybenzyl)amino) benzensulfonamid derivater som 12-lipoxygenase inhibitorer
RS57969B1 (sr) 2013-10-17 2019-01-31 Vertex Pharma Kokristali (s)-n-metil-8-(1-((2'-metil-[4,5'-bipirimidin]-6-il)amino)propan-2-il) hinolin-4-karboksamid i njihovi deuterisani derivati kao inhibitori dnk-pk
US9636298B2 (en) 2014-01-17 2017-05-02 Methylgene Inc. Prodrugs of compounds that enhance antifungal activity and compositions of said prodrugs
MX371353B (es) 2014-02-14 2020-01-27 Respivert Ltd Compuestos heterociclicos aromaticos como compuestos antiinflamatorios.
KR20240010105A (ko) 2014-03-14 2024-01-23 아지오스 파마슈티컬스 아이엔씨. 치료적으로 활성인 화합물의 약제학적 조성물
DE102014108210A1 (de) 2014-06-11 2015-12-17 Dietrich Gulba Rodentizid
EP3182993B1 (en) 2014-08-20 2020-07-01 Portola Pharmaceuticals, Inc. Lyophilized formulations for factor xa antidote
GB201501302D0 (en) 2015-01-27 2015-03-11 Ostara Biomedical Ltd Embryo implantation
AU2016276951B2 (en) 2015-06-11 2020-10-08 Agios Pharmaceuticals, Inc. Methods of using pyruvate kinase activators
CN106349228B (zh) 2015-07-17 2019-07-09 广东东阳光药业有限公司 取代的喹唑啉酮类化合物及其制备方法和用途
GB201514021D0 (en) 2015-08-07 2015-09-23 Arner Elias Set Jeno Novel Pyridines and their use in the treatment of cancer
GB201517523D0 (en) 2015-10-05 2015-11-18 Ostara Biomedical Ltd Methods and compositions for managing reproduction
EP3362066B1 (en) 2015-10-15 2021-10-06 Les Laboratoires Servier SAS Combination therapy for treating malignancies
SG10202111439SA (en) 2015-10-15 2021-11-29 Les Laboratoires Servier Sas Combination therapy for treating malignancies
WO2017091757A1 (en) 2015-11-24 2017-06-01 Portola Pharmaceuticals, Inc. Isotopically enriched betrixaban
ES2776658T3 (es) 2016-01-22 2020-07-31 Janssen Pharmaceutica Nv Nuevos derivados de cianoindolina con sustituyente heteroaromático de 6 miembros como inhibidores de NIK
CA3011880A1 (en) 2016-01-22 2017-07-27 Janssen Pharmaceutica Nv Substituted cyanoindoline derivatives as nik inhibitors
EP3419650B1 (en) 2016-02-24 2021-06-02 Alexion Pharmaceuticals, Inc. Lyophilized formulations for factor xa antidote
RU2698202C2 (ru) * 2016-06-01 2019-08-23 Закрытое акционерное общество "ФАРМА ВАМ" СПОСОБ ПОЛУЧЕНИЯ ПРЯМОГО ИНГИБИТОРА ФАКТОРА Ха
AU2017283720C1 (en) 2016-06-17 2024-07-25 Alexion Pharmaceuticals, Inc. Preparation of factor Xa derivatives
EP3478675B1 (en) 2016-06-30 2020-04-22 Janssen Pharmaceutica NV Heteroaromatic derivatives as nik inhibitors
EP3478673B1 (en) 2016-06-30 2020-09-16 Janssen Pharmaceutica NV Cyanoindoline derivatives as nik inhibitors
ES2957159T3 (es) 2016-09-02 2024-01-12 Cyclerion Therapeutics Inc Estimuladores de SGC fusionados bicíclicos
MX2019003317A (es) 2016-09-27 2019-08-05 Vertex Pharma Metodo para tratar cancer usando una combinacion de agentes que dañan adn e inhibidores de proteina cinasa dependiente de adn (adn-pk).
WO2018069936A1 (en) 2016-10-13 2018-04-19 Mylan Laboratories Limited Polymorphs and solid dispersion of betrixaban and methods for the preparation thereof
AU2018218521C1 (en) 2017-02-07 2022-06-09 Oblique Therapeutics Ab Heterocyclylsulfonyl-substituted pyridines and their use in the treatment of cancer
WO2018146469A1 (en) 2017-02-07 2018-08-16 Oblique Therapeutics Ab Heteroarylsulfonyl-substituted pyridines and their use in the treatment of cancer
MA47450A (fr) 2017-02-07 2019-12-18 Oblique Therapeutics Ab Sulfinylpyridines et leur utilisation dans le traitement du cancer
KR20190115014A (ko) 2017-02-07 2019-10-10 오블리크 세러퓨틱스 에이비 하이드로카르빌설포닐-치환된 피리딘 및 암의 치료에서 이의 용도
WO2018229796A2 (en) 2017-06-14 2018-12-20 Mylan Laboratories Limited A process for betrixaban hydrochloride and betrixaban maleate salt
SG11202000230VA (en) 2017-07-11 2020-02-27 Vertex Pharma Carboxamides as modulators of sodium channels
BR112020003725A2 (pt) 2017-10-06 2020-11-03 Forma Therapeutics, Inc. inibição da peptidase 30 específica de ubiquitina
EP3700902B8 (en) 2017-10-27 2023-08-02 Boehringer Ingelheim International GmbH Pyridine carbonyl derivatives and therapeutic uses thereof as trpc6 inhibitors
MA52360A (fr) 2018-04-26 2021-03-03 Pfizer Dérivés de 2-amino-pyridine ou de 2-amino-pyrimidine utilisés en tant qu'inhibiteurs de kinases dépendantes des cyclines
GB201807014D0 (en) 2018-04-30 2018-06-13 Univ Leeds Innovations Ltd Factor xlla inhibitors
WO2019222468A1 (en) 2018-05-17 2019-11-21 Forma Therapeutics, Inc. Fused bicyclic compounds useful as ubiquitin-specific peptidase 30 inhibitors
US10980788B2 (en) 2018-06-08 2021-04-20 Agios Pharmaceuticals, Inc. Therapy for treating malignancies
GB201810581D0 (en) 2018-06-28 2018-08-15 Ctxt Pty Ltd Compounds
RS64321B1 (sr) 2018-10-05 2023-08-31 Forma Therapeutics Inc Fuzionisani pirolini koji se ponašaju kao inhibitori ubikvitin specifične proteaze 30 (usp30)
PE20220808A1 (es) 2019-06-18 2022-05-20 Pfizer Derivados de benzisoxazol sulfonamida
PE20230300A1 (es) 2019-12-06 2023-02-13 Vertex Pharma Tetrahidrofuranos sustituidos como moduladores de canales de sodio
TW202322824A (zh) 2020-02-18 2023-06-16 美商基利科學股份有限公司 抗病毒化合物
JP7429799B2 (ja) 2020-02-18 2024-02-08 ギリアード サイエンシーズ， インコーポレイテッド 抗ウイルス化合物
TWI775313B (zh) 2020-02-18 2022-08-21 美商基利科學股份有限公司 抗病毒化合物
WO2022211680A1 (ru) * 2021-03-30 2022-10-06 Общество С Ограниченной Ответственностью "Фармадиол" Способ получения антикоагулянта n-(5-хлорпиридин-2-ил)-2-({4-[этан-имидоил(метил)амино]бензоил}амино)-5-метилбензамид гидрохлорида
EP4070658A1 (de) 2021-04-06 2022-10-12 BIORoxx GmbH Verwendung von blutgerinnungshemmenden verbindungen als rodentizide
WO2022221514A1 (en) 2021-04-16 2022-10-20 Gilead Sciences, Inc. Methods of preparing carbanucleosides using amides
GB202107722D0 (en) 2021-05-28 2021-07-14 Lunac Therapeutics Ltd Factor XIIA Inhibitors
KR20240031300A (ko) 2021-06-04 2024-03-07 버텍스 파마슈티칼스 인코포레이티드 나트륨 채널 조절제로서의 n-(하이드록시알킬 (헤테로)아릴) 테트라하이드로푸란 카르복스아미드
JP2024532166A (ja) 2021-08-18 2024-09-05 ギリアード サイエンシーズ， インコーポレイテッド リン脂質化合物並びにその製造方法及び使用方法

Family Cites Families (64)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2095619A (en) * 1937-10-12 Aryl oxides
CH428747A (de) * 1961-09-11 1967-01-31 Wander Ag Dr A Verfahren zur Herstellung neuer Harnstoff- und Thioharnstoffderivate
GB1047245A (da) * 1963-02-15
JPS6033389B2 (ja) * 1979-02-22 1985-08-02 日産化学工業株式会社 複素環エ−テル系フェノシキ脂肪酸誘導体、その製造法および該誘導体を含有する除草剤
DE3207033C2 (de) 1981-02-27 1984-09-13 Torii & Co., Ltd., Tokyo Amidinverbindungen, Verfahren zu ihrer Herstellung und diese Verbindungen enthaltende pharmazeutische Mittel
US4500714A (en) * 1981-10-15 1985-02-19 Chugai Seiyaku Kabushiki Kaisha 3-Substituted-ureido-N-pyridyl benzamides
US4588587A (en) 1983-03-01 1986-05-13 Pennsylvania Hospital Method of treatment to inhibit metastasis
JPS59181257A (ja) 1983-03-31 1984-10-15 Chugai Pharmaceut Co Ltd ウレイドベンズアミド誘導体
JPS648675A (en) 1987-06-30 1989-01-12 Mitsubishi Electric Corp Formation of schottky gate
JP2668231B2 (ja) 1987-12-29 1997-10-27 大日精化工業株式会社 電子写真感光体
AU606808B2 (en) * 1988-06-29 1991-02-14 Otsuka Pharmaceutical Factory, Inc. Arylcarboxamide substituted by alkylphosphonates, process for preparing the same and a pharmaceutical composition containing the same
JPH0418675A (ja) 1990-05-11 1992-01-22 Ricoh Co Ltd 回路図入力装置
GB9816837D0 (en) * 1998-08-04 1998-09-30 Zeneca Ltd Amide derivatives
ZA928276B (en) 1991-10-31 1993-05-06 Daiichi Seiyaku Co Aromatic amidine derivates and salts thereof.
US5612360A (en) 1992-06-03 1997-03-18 Eli Lilly And Company Angiotensin II antagonists
EP0675899B1 (en) 1992-12-15 1999-03-17 Corvas International, Inc. NOVEL INHIBITORS OF FACTOR Xa
US5610335A (en) 1993-05-26 1997-03-11 Cornell Research Foundation Microelectromechanical lateral accelerometer
WO1996016940A1 (fr) 1994-12-02 1996-06-06 Yamanouchi Pharmaceutical Co., Ltd. Nouveau derive d'amidinonaphtyle ou sel de celui-ci
AU707323B2 (en) 1995-03-10 1999-07-08 Berlex Laboratories, Inc. Benzamidine derivatives and their use as anti-coagulants
EP0742208A1 (en) 1995-05-05 1996-11-13 Grelan Pharmaceutical Co., Ltd. 2-Ureido-benzamide derivatives
US5849759A (en) 1995-12-08 1998-12-15 Berlex Laboratories, Inc. Naphthyl-substituted benzimidazole derivatives as anti-coagulants
US5994375A (en) 1996-02-12 1999-11-30 Berlex Laboratories, Inc. Benzamidine derivatives substituted by amino acid and hydroxy acid derivatives and their use as anti-coagulants
DE69718194T2 (de) 1996-08-16 2003-10-16 Bristol-Myers Squibb Pharma Co., Wilmington Amidinophenyl-pyrrolidine, -pyrroline und -isoxazolidine und ihre derivate
WO1998009630A1 (en) 1996-09-09 1998-03-12 Smithkline Beecham Corporation Compounds and methods
WO1998028282A2 (en) 1996-12-23 1998-07-02 Du Pont Pharmaceuticals Company OXYGEN OR SULFUR CONTAINING 5-MEMBERED HETEROAROMATICS AS FACTOR Xa INHIBITORS
EA003056B1 (ru) * 1996-12-23 2002-12-26 Дюпон Фармасьютикалз Компани АЗОТСОДЕРЖАЩИЕ ГЕТЕРОАРОМАТИЧЕСКИЕ СОЕДИНЕНИЯ В КАЧЕСТВЕ ИНГИБИТОРОВ ФАКТОРА Ха, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ И СПОСОБ ЛЕЧЕНИЯ
WO1998057934A1 (en) * 1997-06-19 1998-12-23 The Du Pont Merck Pharmaceutical Company (AMIDINO)6-MEMBERED AROMATICS AS FACTOR Xa INHIBITORS
JP2002506462A (ja) 1997-06-26 2002-02-26 イーライ・リリー・アンド・カンパニー 抗血栓物質
IL133623A0 (en) 1997-06-26 2001-04-30 Lilly Co Eli Antithrombotic agents
AU8270898A (en) 1997-06-26 1999-01-19 Eli Lilly And Company Antithrombotic agents
JP2002510313A (ja) 1997-06-26 2002-04-02 イーライ・リリー・アンド・カンパニー 抗血栓物質
CA2295620A1 (en) 1997-08-11 1999-02-18 Boehringer Ingelheim Pharmaceuticals, Inc. 5,6-heteroaryl-dipyrido¬2,3-b:3',2'-f|azepines and their use in the prevention or treatment of hiv infection
AU8747598A (en) 1997-08-27 1999-03-16 Kissei Pharmaceutical Co. Ltd. 3-amidinoaniline derivatives, activated blood coagulation factor x inhibitors, and intermediates for producing both
US6140351A (en) 1997-12-19 2000-10-31 Berlex Laboratories, Inc. Ortho-anthranilamide derivatives as anti-coagulants
HUP0101172A3 (en) 1997-12-19 2002-12-28 Schering Ag Ortho-anthranilamide derivatives and their use as anti-coagulants
EP0937711A1 (de) * 1998-02-18 1999-08-25 Roche Diagnostics GmbH Neue Thiobenzamide, Verfahren zu ihrer Herstellung sowie diese enthaltende Arzneimittel
JPH11302177A (ja) 1998-04-27 1999-11-02 Otsuka Pharmaceut Factory Inc 腎炎治療剤
CA2350996A1 (en) 1998-12-09 2000-06-15 Bryan Mark O'hara Thiourea inhibitors of herpes viruses
IL143182A0 (en) 1998-12-09 2002-04-21 American Home Prod Heterocyclic carboxamide-containing thiourea inhibitors of herpes viruses containing phenylenediamine group
CA2350899A1 (en) 1998-12-09 2000-06-15 Stanley Albert Lang Acetamide and substituted acetamide-containing thiourea inhibitors of herpes viruses
ATE272052T1 (de) 1998-12-09 2004-08-15 Wyeth Corp Thioharnstoff-inhibitoren von herpes-virus
WO2000034269A1 (en) 1998-12-09 2000-06-15 American Home Products Corporation Thiourea inhibitors of herpes viruses
WO2000034260A2 (en) 1998-12-09 2000-06-15 American Home Products Corporation Alpha-methylbenzyl-containing thiourea inhibitors of herpes viruses containing a phenylenediamine group
CA2351690A1 (en) 1998-12-09 2000-06-15 Adma Antonia Ross Heterocyclic carboxamide-containing thiourea inhibitors of herpes viruses containing a substituted phenylenediamine group
EP1140903B1 (en) 1998-12-23 2004-08-04 Eli Lilly And Company Aromatic amides
US6632815B2 (en) 1999-09-17 2003-10-14 Millennium Pharmaceuticals, Inc. Inhibitors of factor Xa
US6844367B1 (en) * 1999-09-17 2005-01-18 Millennium Pharmaceuticals, Inc. Benzamides and related inhibitors of factor Xa
US6720317B1 (en) 1999-09-17 2004-04-13 Millennium Pharmaceuticals, Inc. Inhibitors of factor Xa
BR0014076A (pt) 1999-09-17 2002-10-15 Millennium Pharm Inc Benzamidas e inibidores correlatos do fator xa
DK1259485T3 (da) 2000-02-29 2006-04-10 Millennium Pharm Inc Benzamider og beslægtede inhibitorer for faktor Xa
AU776053B2 (en) * 2000-03-31 2004-08-26 Astellas Pharma Inc. Diazepan derivatives or salts thereof
US6373515B1 (en) * 2000-08-09 2002-04-16 Hewlett-Packard Company Variable resolution transition placement device
US7312235B2 (en) 2001-03-30 2007-12-25 Millennium Pharmaceuticals, Inc. Benzamide inhibitors of factor Xa
KR20040055774A (ko) * 2001-07-31 2004-06-26 웨인 스테이트 유니버시티 퀴놀린 유도체 및 항종양제로서 그의 용도
JP2007508308A (ja) * 2003-10-09 2007-04-05 ミレニアム ファーマシューティカルズ インク． 第Ｘａ因子の阻害剤としてのチオエーテル置換されたベンズアミド誘導体
US7696352B2 (en) * 2004-06-18 2010-04-13 Millennium Pharmaceuticals, Inc. Factor Xa inhibitors
EP1893572B1 (en) * 2004-06-18 2016-12-14 Millennium Pharmaceuticals, Inc. Factor xa inhibitors
NZ592533A (en) * 2005-11-08 2012-08-31 Millennium Pharm Inc METHOD FOR THE PREPARATION OF N-(5-CHLORO-2-PYRIDINYL)-2-[[4-[(DIMETHYLAMINO) IMINOMETHYL] BENZOYL] AMINO]-5-METHOXY-BENZAMIDE, A FACTOR Xa INHIBITOR
WO2007112367A2 (en) * 2006-03-27 2007-10-04 Portola Pharmaceuticals, Inc. Potassium channel modulators and platelet procoagulant activity
CN101490036B (zh) * 2006-05-05 2013-07-17 米伦纽姆医药公司 Xa因子抑制剂
EP2101760B1 (en) * 2006-12-08 2013-02-27 Millennium Pharmaceuticals, Inc. Unit dose formulations and methods of treating thrombosis with an oral factor xa inhibitor
EP2114930A2 (en) * 2007-01-05 2009-11-11 Millennium Pharmaceuticals, Inc. Factor xa inhibitors
AU2008239659B2 (en) * 2007-04-13 2013-09-05 Millennium Pharmaceuticals, Inc. Combination anticoagulant therapy with a compound that acts as a factor Xa inhibitor
NZ599556A (en) * 2007-05-02 2013-10-25 Portola Pharm Inc Combination therapy with a compound acting as a platelet adp receptor inhibitor

Also Published As

Publication number Publication date
US7727982B2 (en) 2010-06-01
US9108922B2 (en) 2015-08-18
US20130172310A1 (en) 2013-07-04
US9629831B2 (en) 2017-04-25
CA2401778A1 (en) 2001-09-07
US20060241153A1 (en) 2006-10-26
US20180036296A1 (en) 2018-02-08
AU2001250783A1 (en) 2001-09-12
US20090131411A1 (en) 2009-05-21
US6835739B2 (en) 2004-12-28
CA2401778C (en) 2010-12-21
US20020002183A1 (en) 2002-01-03
EP1259485B1 (en) 2005-11-30
WO2001064643A2 (en) 2001-09-07
US8691847B2 (en) 2014-04-08
WO2001064643A3 (en) 2002-04-04
DK1259485T3 (da) 2006-04-10
WO2001064642A3 (en) 2002-05-02
US20030162690A1 (en) 2003-08-28
US20050261346A1 (en) 2005-11-24
ATE311366T1 (de) 2005-12-15
US7314874B2 (en) 2008-01-01
US7727981B2 (en) 2010-06-01
US20070021472A1 (en) 2007-01-25
US10179124B2 (en) 2019-01-15
US8518977B2 (en) 2013-08-27
ES2254385T3 (es) 2006-06-16
US8063036B2 (en) 2011-11-22
US20120083602A1 (en) 2012-04-05
US20100298284A1 (en) 2010-11-25
AU2001245353A1 (en) 2001-09-12
US20140377247A1 (en) 2014-12-25
WO2001064642A2 (en) 2001-09-07
US7342013B2 (en) 2008-03-11
US20160317511A1 (en) 2016-11-03
DE60115394D1 (de) 2006-01-05
US6376515B2 (en) 2002-04-23
DE60115394T2 (de) 2006-10-19
US20040097561A1 (en) 2004-05-20
EP1259485A2 (en) 2002-11-27

Similar Documents

Publication Publication Date Title
HK1051539A1 (en) Benzamides and related inhibitors of factor xa
WO2001056989A3 (en) Inhibitors of factor xa
WO2002026712A3 (en) Quaternary amines and related inhibitors of factor xa
NZ511927A (en) Phenylglycine derivatives
WO2000071507A3 (en) INHIBITORS OF FACTOR Xa
BG106013A (en) New compounds and compositions as protease inhibitors
BG106586A (en) Pyrazolopyramidines as therapeutic agents
WO2000071515A3 (en) INHIBITORS OF FACTOR Xa
BRPI0014076B8 (pt) benzamidas e inibidores correlatos do fator xa
BR0014078A (pt) Inibidores de fator xa
PL362834A1 (en) Phenyl derivatives
EP1248612A4 (en) NEW SUBSTANCES AND COMPOUNDS AS PROTEASE INHIBITORS
WO2001072708A3 (en) OXINDOLE INHIBITORS OF FACTOR Xa
WO2001057021A3 (en) 2-[1H]-QUINOLONE AND 2-[1H]-QUINOXALONE INHIBITORS OF FACTOR Xa
MY133897A (en) N-(4-carb-amimidophenyl) glycineamide derivatives
MXPA03008215A (es) Inhibidores de integrina alfa v beta 6.
DE60221505D1 (de) FAKTOR Xa BENZAMIDIN INHIBITOREN
WO2002026720A3 (en) PIPERAZINE BASED INHIBITORS OF FACTOR Xa
MX9709910A (es) Compuestos que contienen arginina e imitaciones de arginina, su uso y composiciones que los contienen.
SE0302756D0 (sv) Novel Compounds
WO2002006280A3 (en) INHIBITORS OF FACTOR Xa
ATE211482T1 (de) Selektive inhibitoren des faktors x, eine azepinonstruktur enthaltend
WO2002026718A3 (en) Bicyclic pyrimidin-4-one based inhibitors of factor xa
WO2002026731A3 (en) Quaternary amidino based inhibitors of factor xa
SE9902387D0 (sv) New pharmaceutically active compounds

Legal Events

Date Code Title Description
PE Patent expired

Effective date: 20210227