HRP20192224T1 - Inhibitori proteinske kinaze c i metode za njihovu primjenu - Google Patents

Inhibitori proteinske kinaze c i metode za njihovu primjenu Download PDF

Info

Publication number
HRP20192224T1
HRP20192224T1 HRP20192224TT HRP20192224T HRP20192224T1 HR P20192224 T1 HRP20192224 T1 HR P20192224T1 HR P20192224T T HRP20192224T T HR P20192224TT HR P20192224 T HRP20192224 T HR P20192224T HR P20192224 T1 HRP20192224 T1 HR P20192224T1
Authority
HR
Croatia
Prior art keywords
amino
pyridin
carboxamide
pyrazine
trifluoromethyl
Prior art date
Application number
HRP20192224TT
Other languages
English (en)
Inventor
Michael Joseph Luzzio
Julien Papillon
Michael Scott Visser
Original Assignee
Novartis Ag
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=53836145&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=HRP20192224(T1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of HRP20192224T1 publication Critical patent/HRP20192224T1/hr

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (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)
  • Chemical Kinetics & Catalysis (AREA)
  • Immunology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Transplantation (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)

Claims (15)

1. Spoj formule II ili njegova farmaceutski prihvatljiva sol, naznačeno time, što: X je N ili CR; R, R2, R3 i R4 su svaki zasebno H, 2H, halo, hidroksil (-OH), C1-3 alkoksi, C1-3 haloalkil ili C1-3 alkil, pri čemu je spomenuti C1-3 alkil opcionalno supstituiran s hidroksilom, halo, C1-3 alkoksijem ili C1-3 haloalkoksijem; R5 je zasebno H, 2H, CH3, CH2F, CHF2, CF3, CH2OH, C1-3 alkil, pri čemu je spomenuti C1-3 alkil opcionalno supstituiran s F, OH, C1-3 alkoksijem ili C1-3 haloalkoksijem; R5a i R5b su svaki zasebno H, 2H, C1-3 alkil, pri čemu je spomenuti C1-3 alkil opcionalno supstituiran s F, OH ili C1-3 alkoksijem ili su R5a i R5b spojeni zajedno kako bi formirali metilensku ili etilensku premosnu grupu; R5c i R5d su svaki zasebno H, 2H, F, -OH, C1-3 alkoksi, C1-3 alkil, pri čemu je spomenuti C1-3 alkil opcionalno supstituiran s F, OH ili C1-3 alkoksijem ili su R5c i R5d spojeni zajedno kako bi formirali metilensku, etilensku ili ili –CH2-O- premosnu grupu; R6, R7 i R8 su svaki zasebno odabrani iz H, 2H, halo, C1-3 alkila, C1-3 haloalkila, C1-3 haloalkoksija, C3-7 cikloalkila i heterociklila s 4 do 7 članova koji ima 1 do 3 heteroatoma odabrana iz N, O i S, pri čemu je spomenuti C1-3 alkil opcionalno supstituiran s F, OH, C1-3 alkoksijem ili C1-3 haloalkoksijem; ili naznačeno time, što R6 i R8 opcionalno formira djelomično zasićeni karbobiciklični prsten ili heterobiciklični prsten s heteroarilnim prstenom, pri čemu je spomenuti karbobiciklični prsten ili heterobiciklični prsten opcionalno supstituiran s 1 do 3 grupe odabrane iz: 2H, halo, C1-3 haloalkila, C1-3 alkoksija, C1-3 haloalkoksija, C3-7 cikloalkila i heterociklila s 4 do 7 članova koji ima 1 do 3 heteroatoma odabrana iz N, O i S.
2. Spoj prema patentnom zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeno time, što X je N, a R2, R3 i R4 su svaki zasebno H ili halo.
3. Spoj prema patentnom zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeno time, što X je CR, a R2, R3, R4 i R8 su svaki zasebno H ili halo.
4. Spoj prema patentnom zahtjevu 3 ili njegova farmaceutski prihvatljiva sol, naznačeno time, što su R6 i R7 svaki zasebno odabrani iz H, halo, C1-3 haloalkila, C1-3 haloalkoksija, C3-7 cikloalkila, morfolino, piperidinila i piperazinila.
5. Spoj prema patentnom zahtjevu 4 ili njegova farmaceutski prihvatljiva sol, naznačeno time, što R5 je –H, 2H ili CH3; a R5a i R5b su svaki H, a R5c i R5d su svaki H.
6. Spoj prema patentnom zahtjevu 1 koji je odabran iz sljedećih: 3-amino-N-(3-(4-aminopiperidin-1-il)piridin-2-il)-6-(3-(trifluorometil)piridin-2-il)pirazin-2-karboksamid; 3-amino-N-(3-(4-aminopiperidin-1-il)piridin-2-il)-6-(3-(trifluorometoksi)piridin-2-il)pirazin-2-karboksamid; 3-amino-N-(3-(4-amino-4-(metoksimetil)piperidin-1-il)piridin-2-il)-6-(3-(trifluorometil)piridin-2-il)pirazin-2-karboksamid; 3-amino-N-(3-(4-amino-4-(hidroksimetil)piperidin-1-il)piridin-2-il)-6-(3-(trifluorometil)piridin-2-il)pirazin-2-karboksamid; 3-amino-N-(3-(4-amino-4-(hidroksimetil)piperidin-1-il)piridin-2-il)-6-(3-(trifluorometoksi)piridin-2-il)pirazin-2-karboksamid; 3-amino-N-(3-(4-amino-4-metilpiperidin-1-il)piridin-2-il)-6-(3-(trifluorometil)piridin-2-il)pirazin-2-karboksamid; 3-amino-N-(3-(4-amino-4-metilpiperidin-1-il)piridin-2-il)-6-(3-(trifluorometoksi)piridin-2-il)pirazin-2-karboksamid; 3-amino-N-(3-(4-amino-4-metilpiperidin-1-il)piridin-2-il)-6-(4-metoksi-3-(trifluorometil)piridin-2-il)pirazin-2-karboksamid; 3-amino-N-(3-(4-amino-4-etilpiperidin-1-il)piridin-2-il)-6-(3-(trifluorometil)piridin-2-il)pirazin-2-karboksamid; 3-amino-N-(3-(4-amino-4-metilpiperidin-1-il)piridin-2-il)-6-(3-kloropiridin-2-il)pirazin-2-karboksamid; 3-amino-N-(3-(4-amino-4-metilpiperidin-1-il)piridin-2-il)-6-(3-fluoropiridin-2-il)pirazin-2-karboksamid; 3-amino-N-(3-(4-amino-4-metilpiperidin-1-il)piridin-2-il)-6-(3-fluoro-4-metoksipiridin-2-il)pirazin-2-karboksamid; 3-amino-N-(3-(4-amino-4-(metoksimetil)piperidin-1-il)piridin-2-il)-6-(3-fluoropiridin-2-il)pirazin-2-karboksamid; 3-amino-N-(3-(4-amino-4-etilpiperidin-1-il)piridin-2-il)-6-(3-(trifluorometoksi)piridin-2-il)pirazin-2-karboksamid; 3-amino-N-(3-(4-amino-4-(metoksimetil)piperidin-1-il)piridin-2-il)-6-(3-(trifluorometoksi)piridin-2-il)pirazin-2-karboksamid; 3-amino-N-(3-(4-amino-4-(2-hidroksietil)piperidin-1-il)piridin-2-il)-6-(3-(trifluorometil)piridin-2-il)pirazin-2-karboksamid; 3-amino-N-(3-(4-amino-4-(2-hidroksietil)piperidin-1-il)piridin-2-il)-6-(3-fluoropiridin-2-il)pirazin-2-karboksamid; 3-amino-N-(3-(4-amino-4-(2-metoksietil)piperidin-1-il)piridin-2-il)-6-(3-(trifluorometil)piridin-2-il)pirazin-2-karboksamid; (+)3-amino-N-(3-((cis)-4-amino-3-fluoropiperidin-1-il)piridin-2-il)-6-(3-(trifluorometoksi)piridin-2-il)pirazin-2-karboksamid; 3-amino-N-(3-(4-aminopiperidin-1-il)piridin-2-il)-6-(3-fluoropiridin-2-il)pirazin-2-karboksamid; 3-amino-N-(3-((3S,4R)-4-amino-3-fluoropiperidin-1-il)piridin-2-il)-6-(3-(trifluorometoksi)piridin-2-il)pirazin-2-karboksamid; 3-amino-N-(3-(4-amino-4-etilpiperidin-1-il)piridin-2-il)-6-(3-fluoropiridin-2-il)pirazin-2-karboksamid; 3-amino-N-(3-(4-amino-4-metilpiperidin-1-il)piridin-2-il)-6-(4-etoksi-3-(trifluorometil)piridin-2-il)pirazin-2-karboksamid; 3-amino-N-(3-(4-amino-4-metilpiperidin-1-il)piridin-2-il)-6-(4-kloro-3-(trifluorometil)piridin-2-il)pirazin-2-karboksamid; 3-amino-N-(3-(4-aminopiperidin-1-il)-6-metilpiridin-2-il)-6-(3-(trifluorometoksi)piridin-2-il)pirazin-2-karboksamid; 3-amino-N-(3-(4-aminopiperidin-1-il)-6-metilpiridin-2-il)-6-(3-(trifluorometil)piridin-2-il)pirazin-2-karboksamid; 3-amino-N-(3-(4-amino-3-metoksipiperidin-1-il)piridin-2-il)-6-(3-(trifluorometoksi)piridin-2-il)pirazin-2-karboksamid; 3-amino-N-(3-(4-amino-4-metilpiperidin-1-il)piridin-2-il)-6-(3-fluoro-4-metilpiridin-2-il)pirazin-2-karboksamid; 3-amino-N-(3-(4-amino-4-metilpiperidin-1-il)piridin-2-il)-6-(4-etoksi-3-fluoropiridin-2-il)pirazin-2-karboksamid; 3-amino-N-(3-(4-amino-4-metilpiperidin-1-il)piridin-2-il)-6-(4-(hidroksimetil)-3-(trifluorometil)piridin-2-il)pirazin-2-karboksamid; i 3-amino-N-(3-(4-amino-4-metilpiperidin-1-il)piridin-2-il)-6-(4-(metoksimetil)-3-(trifluorometil)piridin-2-il)pirazin-2-karboksamid; ili njihovih farmaceutski prihvatljivih soli.
7. Spoj prema patentnom zahtjevu 1 koji je odabran iz sljedećih: 3-amino-N-(3-(4-amino-4-(etoksimetil)piperidin-1-il)piridin-2-il)-6-(3-(trifluorometil)piridin-2-il)pirazin-2-karboksamid; 3-amino-N-(3-(4-amino-4-(etoksimetil)piperidin-1-il)piridin-2-il)-6-(3-(trifluorometoksi)piridin-2-il)pirazin-2-karboksamid; 3-amino-N-(3-(4-amino-4-((difluorometoksi)metil)piperidin-1-il)piridin-2-il)-6-(3-(trifluorometil)piridin-2-il)pirazin-2-karboksamid; 3-amino-N-(3-(4-amino-4-metilpiperidin-1-il)piridin-2-il)-6-(4-(trifluorometoksi)piridin-2-il)pirazin-2-karboksamid; 3-amino-N-(3-(4-amino-4-metilpiperidin-1-il)piridin-2-il)-6-(5-metoksi-3-(trifluorometil)piridin-2-il)pirazin-2-karboksamid; 3-amino-N-(3-(4-amino-3-fluoro-4-metilpiperidin-1-il)piridin-2-il)-6-(3-(trifluorometil)piridin-2-il)pirazin-2-karboksamid; 3-amino-N-(3-(4-amino-3-fluoro-4-metilpiperidin-1-il)piridin-2-il)-6-(3-(trifluorometoksi)piridin-2-il)pirazin-2-karboksamid; 3-amino-N-(3-((3S,4R)-4-amino-3-fluoro-4-metilpiperidin-1-il)piridin-2-il)-6-(3-(trifluorometoksi)piridin-2-il)pirazin-2-karboksamid; i 3-amino-N-(3-(4-amino-3-fluoro-4-(2-hidroksietil)piperidin-1-il)piridin-2-il)-6-(3-(trifluorometil)piridin-2-il)pirazin-2-karboksamid; ili njihovih farmaceutski prihvatljivih soli.
8. Spoj prema patentnom zahtjevu 1 koji je odabran iz sljedećih: 3-amino-N-(3-(4-aminopiperidin-1-il)piridin-2-il)-6-(3-(trifluorometil)piridin-2-il)pirazin-2-karboksamid; 3-amino-N-(3-(4-aminopiperidin-1-il)piridin-2-il)-6-(3-(trifluorometoksi)piridin-2-il)pirazin-2-karboksamid; 3-amino-N-(3-(4-amino-4-(metoksimetil)piperidin-1-il)piridin-2-il)-6-(3-(trifluorometil)piridin-2-il)pirazin-2-karboksamid; 3-amino-N-(3-(4-amino-4-(hidroksimetil)piperidin-1-il)piridin-2-il)-6-(3-(trifluorometil)piridin-2-il)pirazin-2-karboksamid; 3-amino-N-(3-(4-amino-4-(hidroksimetil)piperidin-1-il)piridin-2-il)-6-(3-(trifluorometoksi)piridin-2-il)pirazin-2-karboksamid; 3-amino-N-(3-(4-amino-4-metilpiperidin-1-il)piridin-2-il)-6-(3-(trifluorometil)piridin-2-il)pirazin-2-karboksamid; 3-amino-N-(3-(4-amino-4-metilpiperidin-1-il)piridin-2-il)-6-(3-(trifluorometoksi)piridin-2-il)pirazin-2-karboksamid; i 3-amino-N-(3-(4-amino-4-metilpiperidin-1-il)piridin-2-il)-6-(4-metoksi-3-(trifluorometil)piridin-2-il)pirazin-2-karboksamid; ili njihovih farmaceutski prihvatljivih soli.
9. Spoj prema patentnom zahtjevu 8 koji je odabran iz sljedećih: 3-amino-N-(3-(4-aminopiperidin-1-il)piridin-2-il)-6-(3-(trifluorometoksi)piridin-2-il)pirazin-2-karboksamid; 3-amino-N-(3-(4-amino-4-metilpiperidin-1-il)piridin-2-il)-6-(3-(trifluorometil)piridin-2-il)pirazin-2-karboksamid; i 3-amino-N-(3-(4-amino-4-metilpiperidin-1-il)piridin-2-il)-6-(3-(trifluorometoksi)piridin-2-il)pirazin-2-karboksamid, ili njihovih farmaceutski prihvatljivih soli.
10. Spoj prema patentnom zahtjevu 8 koji je 3-amino-N-(3-(4-amino-4-metilpiperidin-1-il)piridin-2-il)-6-(3-(trifluorometil)piridin-2-il)pirazin-2-karboksamid, ili njegova farmaceutski prihvatljiva sol.
11. Farmaceutski pripravak koji sadrži spoj prema bilo kojem patentnom zahtjevu od 1 do 10 ili njegovu farmaceutski prihvatljivu soli farmaceutski prihvatljiv nosač ili ekscipijens.
12. Spoj ili njegova farmaceutski prihvatljiva sol prema bilo kojem patentnom zahtjevu od 1 do 10 za primjenu u liječenju raka.
13. Spoj ili njegova farmaceutski prihvatljiva sol za primjenu prema patentnom zahtjevu 12, naznačeno time, što je rak odabran iz melanoma, uvealnog melanoma, limfoma, difuznog limfoma velikih B stanica i rakova otpornih na ibrutinib.
14. Spoj ili njegova farmaceutski prihvatljiva sol prema bilo kojem patentnom zahtjevu od 1 do 10 za primjenu u liječenju imunoloških poremećaja odabranih iz autoimunih oboljenja, alergijske reakcije i odbacivanja transplantacija tkiva.
15. Spoj ili njegova farmaceutski prihvatljiva sol prema bilo kojem patentnom zahtjevu od 1 do 10 u kombinaciji s drugim sredstvom protiv raka.
HRP20192224TT 2014-08-06 2019-12-11 Inhibitori proteinske kinaze c i metode za njihovu primjenu HRP20192224T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201462033679P 2014-08-06 2014-08-06
EP15750138.8A EP3177608B1 (en) 2014-08-06 2015-08-05 Protein kinase c inhibitors and methods of their use
PCT/IB2015/055951 WO2016020864A1 (en) 2014-08-06 2015-08-05 Protein kinase c inhibitors and methods of their use

Publications (1)

Publication Number Publication Date
HRP20192224T1 true HRP20192224T1 (hr) 2020-03-06

Family

ID=53836145

Family Applications (1)

Application Number Title Priority Date Filing Date
HRP20192224TT HRP20192224T1 (hr) 2014-08-06 2019-12-11 Inhibitori proteinske kinaze c i metode za njihovu primjenu

Country Status (42)

Country Link
US (7) US9452998B2 (hr)
EP (2) EP3177608B1 (hr)
JP (1) JP6644765B2 (hr)
KR (2) KR102518945B1 (hr)
CN (2) CN113214246A (hr)
AP (1) AP2017009729A0 (hr)
AR (1) AR101456A1 (hr)
AU (1) AU2015298364B2 (hr)
BR (1) BR112017002263B1 (hr)
CA (1) CA2956996C (hr)
CL (1) CL2017000290A1 (hr)
CO (1) CO2017001049A2 (hr)
CR (1) CR20170036A (hr)
CU (1) CU24465B1 (hr)
CY (1) CY1122407T1 (hr)
DK (1) DK3177608T3 (hr)
DO (1) DOP2017000035A (hr)
EA (1) EA033361B1 (hr)
EC (1) ECSP17013903A (hr)
ES (1) ES2754248T3 (hr)
GT (1) GT201700025A (hr)
HR (1) HRP20192224T1 (hr)
HU (1) HUE047862T2 (hr)
IL (1) IL250318B (hr)
JO (1) JO3589B1 (hr)
LT (1) LT3177608T (hr)
MX (1) MX2017001640A (hr)
MY (1) MY195488A (hr)
NI (1) NI201700012A (hr)
PE (1) PE20170241A1 (hr)
PH (1) PH12017500215A1 (hr)
PL (1) PL3177608T3 (hr)
PT (1) PT3177608T (hr)
RS (1) RS59692B1 (hr)
SG (1) SG11201700664UA (hr)
SI (1) SI3177608T1 (hr)
SV (1) SV2017005373A (hr)
TN (1) TN2017000032A1 (hr)
TW (1) TWI680968B (hr)
UY (1) UY36258A (hr)
WO (1) WO2016020864A1 (hr)
ZA (1) ZA201700786B (hr)

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JO3589B1 (ar) 2014-08-06 2020-07-05 Novartis Ag مثبطات كيناز البروتين c وطرق استخداماتها
BR112018000496A2 (pt) * 2015-08-14 2018-09-11 Novartis Ag combinações farmacêuticas e seu uso
JP2019524700A (ja) 2016-07-14 2019-09-05 ミングサイト ファーマシューティカルズ,インク. 癌の処置
WO2019053595A1 (en) * 2017-09-12 2019-03-21 Novartis Ag INHIBITORS OF PROTEIN KINASE C FOR THE TREATMENT OF CHOROIDAL MELLANOMA
BR112020018094A2 (pt) 2018-03-08 2020-12-22 Incyte Corporation Compostos de aminopirazina diol como inibidores de pi3k-¿
CN110496223B (zh) * 2018-05-17 2021-09-10 复旦大学附属肿瘤医院 一种治疗非霍奇金氏淋巴瘤的药物组合物
US11046658B2 (en) 2018-07-02 2021-06-29 Incyte Corporation Aminopyrazine derivatives as PI3K-γ inhibitors
WO2020092924A1 (en) * 2018-11-02 2020-05-07 Board Of Regents, The University Of Texas System Combination therapy for the treatment of egfr tyrosine kinase inhibitor resistant cancer
EP3908282A1 (en) * 2019-01-07 2021-11-17 Ideaya Biosciences, Inc. Treatment of cancer having gnaq or gna11 genetic mutations with protein kinase c inhibitors
US11505542B2 (en) * 2019-01-16 2022-11-22 Shanghai Yingli Pharmaceutical Co., Ltd Preparation method for morpholinquinazoline compound and intermediates thereof
WO2020198469A1 (en) * 2019-03-27 2020-10-01 Ideaya Biosciences Inc. Method for treating epidermal growth factor receptor-driven cancers with protein kinase c inhibitors in combination with an egfr-tyrosine kinase inhibitor
CA3161953A1 (en) * 2019-11-18 2021-05-27 Ideaya Biosciences, Inc. Dosing regimens for a protein kinase c inhibitor
JP2023527792A (ja) 2020-05-27 2023-06-30 アキシャル セラピューティクス,インク. Tlr2調節剤化合物、医薬組成物、及びそれらの使用
PL243663B1 (pl) * 2020-06-29 2023-09-25 Univ Medyczny Im Piastow Slaskich We Wroclawiu Zastosowanie wanikozydów
MX2023002757A (es) * 2020-09-08 2023-07-25 Ideaya Biosciences Inc Combinacion farmaceutica y tratamiento antitumoral.
WO2024125543A1 (zh) * 2022-12-16 2024-06-20 苏州科睿思制药有限公司 达洛色替的晶型及其制备方法和用途

Family Cites Families (170)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US15677A (en) * 1856-09-02 Improved cutting device for harvesters
US4319039A (en) 1979-06-15 1982-03-09 Merck & Co., Inc. Preparation of ammonium salt of hypocholesteremic fermentation product
US4231938A (en) 1979-06-15 1980-11-04 Merck & Co., Inc. Hypocholesteremic fermentation products and process of preparation
US4294926A (en) 1979-06-15 1981-10-13 Merck & Co., Inc. Hypocholesteremic fermentation products and process of preparation
US4444784A (en) 1980-08-05 1984-04-24 Merck & Co., Inc. Antihypercholesterolemic compounds
DK149080C (da) 1980-06-06 1986-07-28 Sankyo Co Fremgangsmaade til fremstilling af derivater af ml-236b-carboxylsyre
JPS5889191A (ja) 1981-11-20 1983-05-27 Sankyo Co Ltd 3−ヒドロキシ−ml−236b誘導体の製造法
US5354772A (en) 1982-11-22 1994-10-11 Sandoz Pharm. Corp. Indole analogs of mevalonolactone and derivatives thereof
AU570021B2 (en) 1982-11-22 1988-03-03 Novartis Ag Analogs of mevalolactone
US4911165A (en) 1983-01-12 1990-03-27 Ethicon, Inc. Pliabilized polypropylene surgical filaments
US4681893A (en) 1986-05-30 1987-07-21 Warner-Lambert Company Trans-6-[2-(3- or 4-carboxamido-substituted pyrrol-1-yl)alkyl]-4-hydroxypyran-2-one inhibitors of cholesterol synthesis
US4782084A (en) 1987-06-29 1988-11-01 Merck & Co., Inc. HMG-COA reductase inhibitors
US4885314A (en) 1987-06-29 1989-12-05 Merck & Co., Inc. Novel HMG-CoA reductase inhibitors
US4820850A (en) 1987-07-10 1989-04-11 Merck & Co., Inc. Process for α-C-alkylation of the 8-acyl group on mevinolin and analogs thereof
US5180589A (en) 1988-03-31 1993-01-19 E. R. Squibb & Sons, Inc. Pravastatin pharmaceuatical compositions having good stability
US5030447A (en) 1988-03-31 1991-07-09 E. R. Squibb & Sons, Inc. Pharmaceutical compositions having good stability
US4916239A (en) 1988-07-19 1990-04-10 Merck & Co., Inc. Process for the lactonization of mevinic acids and analogs thereof
US5118853A (en) 1988-10-13 1992-06-02 Sandoz Ltd. Processes for the synthesis of 3-disubstituted aminoacroleins
US5290946A (en) 1988-10-13 1994-03-01 Sandoz Ltd. Processes for the synthesis of 3-(substituted indolyl-2-yl)propenaldehydes
US4929437A (en) 1989-02-02 1990-05-29 Merck & Co., Inc. Coenzyme Q10 with HMG-CoA reductase inhibitors
US5189164A (en) 1989-05-22 1993-02-23 Sandoz Ltd. Processes for the synthesis of syn-(E)-3,5-dihydroxy-7-substituted hept-6-enoic and heptanoic acids and derivatives and intermediates thereof
FI94339C (fi) 1989-07-21 1995-08-25 Warner Lambert Co Menetelmä farmaseuttisesti käyttökelpoisen /R-(R*,R*)/-2-(4-fluorifenyyli)- , -dihydroksi-5-(1-metyylietyyli)-3-fenyyli-4-/(fenyyliamino)karbonyyli/-1H-pyrroli-1-heptaanihapon ja sen farmaseuttisesti hyväksyttävien suolojen valmistamiseksi
PH27357A (en) 1989-09-22 1993-06-21 Fujisawa Pharmaceutical Co Pyrazole derivatives and pharmaceutical compositions comprising the same
US5420245A (en) 1990-04-18 1995-05-30 Board Of Regents, The University Of Texas Tetrapeptide-based inhibitors of farnesyl transferase
US5475085A (en) 1991-02-07 1995-12-12 Molecumetics, Ltd. Conformationally restricted mimetics of beta turns and beta bulges and peptides containing the same
HU217629B (hu) 1991-12-12 2000-03-28 Novartis Ag. Eljárás fluvasztatint tartalmazó stabilizált gyógyszerkészítmények előállítására
US5604260A (en) 1992-12-11 1997-02-18 Merck Frosst Canada Inc. 5-methanesulfonamido-1-indanones as an inhibitor of cyclooxygenase-2
EP0604181A1 (en) 1992-12-21 1994-06-29 Eli Lilly And Company Antitumor compositions and method of treatment
CA2152792C (en) 1993-01-15 2000-02-15 Stephen R. Bertenshaw Novel 3,4-diaryl thiophenes and analogs thereof having use as antiinflammatory agents
WO1994019357A1 (en) 1993-02-23 1994-09-01 Merrell Dow Pharmaceuticals Inc. Farnesyl:protein transferase inhibitors as anticancer agents
US5298627A (en) 1993-03-03 1994-03-29 Warner-Lambert Company Process for trans-6-[2-(substituted-pyrrol-1-yl)alkyl]pyran-2-one inhibitors of cholesterol synthesis
US5409944A (en) 1993-03-12 1995-04-25 Merck Frosst Canada, Inc. Alkanesulfonamido-1-indanone derivatives as inhibitors of cyclooxygenase
CA2118985A1 (en) 1993-04-02 1994-10-03 Dinesh V. Patel Heterocyclic inhibitors of farnesyl protein transferase
US5843941A (en) 1993-05-14 1998-12-01 Genentech, Inc. Ras farnesyl transferase inhibitors
US5602098A (en) 1993-05-18 1997-02-11 University Of Pittsburgh Inhibition of farnesyltransferase
US5380738A (en) 1993-05-21 1995-01-10 Monsanto Company 2-substituted oxazoles further substituted by 4-fluorophenyl and 4-methylsulfonylphenyl as antiinflammatory agents
GB9602877D0 (en) 1996-02-13 1996-04-10 Merck Frosst Canada Inc 3,4-Diaryl-2-hydroxy-2,5- dihydrofurans as prodrugs to cox-2 inhibitors
US5474995A (en) 1993-06-24 1995-12-12 Merck Frosst Canada, Inc. Phenyl heterocycles as cox-2 inhibitors
US5436265A (en) 1993-11-12 1995-07-25 Merck Frosst Canada, Inc. 1-aroyl-3-indolyl alkanoic acids and derivatives thereof useful as anti-inflammatory agents
US5728830A (en) 1993-09-22 1998-03-17 Kyowa Hakko Kogyo Co., Ltd. Farnesyltransferase inhibitor
US5719148A (en) 1993-10-15 1998-02-17 Schering Corporation Tricyclic amide and urea compounds useful for inhibition of g-protein function and for treatment of proliferative diseases
US5661152A (en) 1993-10-15 1997-08-26 Schering Corporation Tricyclic sulfonamide compounds useful for inhibition of G-protein function and for treatment of proliferative diseases
AU699043B2 (en) 1993-10-15 1998-11-19 Schering Corporation Tricyclic carbamate compounds useful for inhibition of G-protein function and for treatment of proliferative diseases
ES2164717T3 (es) 1993-10-15 2002-03-01 Schering Corp Compuestos triciclicos de sulfonamida utiles para inhibir la funcion de la proteina-g y para el tratamiento de enfermedades proliferativas.
US5721236A (en) 1993-10-15 1998-02-24 Schering Corporation Tricyclic carbamate compounds useful for inhibition of G-protein function and for treatment of proliferative diseases
IL111235A (en) 1993-10-15 2001-03-19 Schering Plough Corp Medicinal preparations for inhibiting protein G activity and for the treatment of malignant diseases, containing tricyclic compounds, some such new compounds and a process for the preparation of some of them
KR100378615B1 (ko) 1993-10-25 2003-10-10 파크데이비스앤드캄파니 단백질:파르네실트랜스퍼라제의치환된테트라및펜타펩티드억제제
US5344991A (en) 1993-10-29 1994-09-06 G.D. Searle & Co. 1,2 diarylcyclopentenyl compounds for the treatment of inflammation
US5783593A (en) 1993-11-04 1998-07-21 Abbott Laboratories Inhibitors of squalene synthetase and protein farnesyltransferase
EP0677039B1 (en) 1993-11-04 1999-03-10 Abbott Laboratories Cyclobutane derivatives as inhibitors of squalene synthetase and protein farnesyltransferase
WO1995012612A1 (en) 1993-11-05 1995-05-11 Warner-Lambert Company Substituted di- and tripeptide inhibitors of protein:farnesyl transferase
US5466823A (en) 1993-11-30 1995-11-14 G.D. Searle & Co. Substituted pyrazolyl benzenesulfonamides
PE49195A1 (es) 1993-12-07 1996-01-06 Lilly Co Eli Inhibidor de proteinquinasa
US5484799A (en) 1993-12-09 1996-01-16 Abbott Laboratories Antifungal dorrigocin derivatives
US5545636A (en) 1993-12-23 1996-08-13 Eli Lilly And Company Protein kinase C inhibitors
EP1449529B1 (en) 1993-12-23 2010-01-27 Eli Lilly And Company Protein Kinase C Inhibitors
US5393790A (en) 1994-02-10 1995-02-28 G.D. Searle & Co. Substituted spiro compounds for the treatment of inflammation
WO1995024612A1 (de) 1994-03-07 1995-09-14 International Business Machines Corporation Verfahren und vorrichtung zur schnellen interpolation von zwischenwerten aus periodischen phasenverschobenen signalen und zur erkennung von defekten in einem drehkörper
US5840918A (en) 1994-03-15 1998-11-24 Eisai Co., Ltd. Isoprenyl transferase inhibitors
HUT72440A (en) 1994-03-31 1996-04-29 Bristol Myers Squibb Co Imidazole-containing inhibitors of farnesyl protein transferase and pharmaceutical compositions containing them
US5523430A (en) 1994-04-14 1996-06-04 Bristol-Myers Squibb Company Protein farnesyl transferase inhibitors
US5510510A (en) 1994-05-10 1996-04-23 Bristol-Meyers Squibb Company Inhibitors of farnesyl protein transferase
US5563255A (en) 1994-05-31 1996-10-08 Isis Pharmaceuticals, Inc. Antisense oligonucleotide modulation of raf gene expression
TW365602B (en) 1994-06-10 1999-08-01 Rhone Poulenc Rorer Sa New farnesyl transferase inhibitors, their preparation and the pharmaceutical compositions which contain them
US5571792A (en) 1994-06-30 1996-11-05 Warner-Lambert Company Histidine and homohistidine derivatives as inhibitors of protein farnesyltransferase
WO1996005529A1 (en) 1994-08-09 1996-02-22 Micron Optics, Inc. Temperature compensated fiber fabry-perot filters
EP0776884B1 (en) 1994-08-11 2000-01-05 Banyu Pharmaceutical Co., Ltd. Substituted amide derivative
CA2155448A1 (en) 1994-08-11 1996-02-12 Katerina Leftheris Inhibitors of farnesyl protein transferase
AU3192495A (en) 1994-08-12 1996-03-07 Banyu Pharmaceutical Co., Ltd. N,n-disubstituted amic acid derivative
DE4429506B4 (de) 1994-08-19 2007-09-13 Degussa Gmbh Verfahren zur Extraktion natürlicher Carotinoid-Farbstoffe
DE4429653C2 (de) 1994-08-20 1997-04-03 Anton Dr More Konverter und Verfahren zum Frischen von Metallschmelzen insbesondere von Roheisen zu Stahl
DE69507284T2 (de) 1994-11-22 1999-07-01 Philips Electronics N.V., Eindhoven Halbleiter mit einem träger auf dem ein substrat mit einem halbleiter-element mittels einer klebeschicht und ein leiterbahn-muster befestigt sind
AU3971295A (en) 1994-12-09 1996-06-26 Warner-Lambert Company Substituted tetra- and pentapeptide inhibitors of protein:farnesyl transferase
CN1176652A (zh) 1995-01-09 1998-03-18 马格拉国际有限公司 胶乳表面的耐磨图象印刷
JP3929069B2 (ja) 1995-01-12 2007-06-13 ユニバーシティ オブ ピッツバーグ プレニルトランスフェラーゼの阻害剤
FR2729390A1 (fr) 1995-01-18 1996-07-19 Rhone Poulenc Rorer Sa Nouveaux inhibiteurs de farnesyl transferase, leur preparation et les compositions pharmaceutiques qui les contiennent
FR2730491B1 (fr) 1995-02-09 1997-03-14 Rhone Poulenc Rorer Sa Nouveaux inhibiteurs de farnesyl transferase, leur preparation et les compositions pharmaceutiques qui les contiennent
FR2730492B1 (fr) 1995-02-09 1997-03-14 Rhone Poulenc Rorer Sa Nouveaux inhibiteurs de farnesyl transferase, leur preparation et les compositions pharmaceutiques qui les contiennent
US5633272A (en) 1995-02-13 1997-05-27 Talley; John J. Substituted isoxazoles for the treatment of inflammation
US5684013A (en) 1995-03-24 1997-11-04 Schering Corporation Tricyclic compounds useful for inhibition of g-protein function and for treatment of proliferative diseases
US5700806A (en) 1995-03-24 1997-12-23 Schering Corporation Tricyclic amide and urea compounds useful for inhibition of G-protein function and for treatment of proliferative diseases
IL117580A0 (en) 1995-03-29 1996-07-23 Merck & Co Inc Inhibitors of farnesyl-protein transferase and pharmaceutical compositions containing them
US5891872A (en) 1995-04-07 1999-04-06 Schering Corporation Tricyclic compounds
US5712280A (en) 1995-04-07 1998-01-27 Schering Corporation Tricyclic compounds useful for inhibition of G-protein function and for treatment of proliferative diseases
ES2194986T3 (es) 1995-04-07 2003-12-01 Schering Corp Compuestos de carbonil-piperazinilo y piperidinilo que inhiben la farnesil-protein-transferasa.
IL117798A (en) 1995-04-07 2001-11-25 Schering Plough Corp Tricyclic compounds useful for inhibiting the function of protein - G and for the treatment of malignant diseases, and pharmaceutical preparations containing them
US5831115A (en) 1995-04-21 1998-11-03 Abbott Laboratories Inhibitors of squalene synthase and protein farnesyltransferase
IL118101A0 (en) 1995-05-03 1996-09-12 Abbott Lab Inhibitors of farnesyltransferase
US5919780A (en) 1995-06-16 1999-07-06 Warner Lambert Company Tricyclic inhibitors of protein farnesyltransferase
FR2736641B1 (fr) 1995-07-10 1997-08-22 Rhone Poulenc Rorer Sa Nouveaux inhibiteurs de farnesyl transferase, leur preparation et les compositions pharmaceutiques qui les contiennent
AT402617B (de) 1995-07-11 1997-07-25 Datacon Schweitzer & Zeindl Gm Anlage zum automatisierten, hermetischen anlage zum automatisierten, hermetischen verschliessen von gehäusen verschliessen von gehäusen
FR2736638B1 (fr) 1995-07-12 1997-08-22 Rhone Poulenc Rorer Sa Nouveaux inhibiteurs de farnesyl transferase, leur preparation et les compositions pharmaceutiques qui les contiennent
CH690163A5 (fr) 1995-07-28 2000-05-31 Symphar Sa Dérivés gem-diphosphonates substitués utiles en tant qu'agents anti-cancers.
US6020343A (en) 1995-10-13 2000-02-01 Merck Frosst Canada, Inc. (Methylsulfonyl)phenyl-2-(5H)-furanones as COX-2 inhibitors
CA2235986C (en) 1995-11-06 2006-09-12 University Of Pittsburgh Inhibitors of protein isoprenyl transferases
PT1186606E (pt) 1995-11-17 2004-08-31 Biotechnolog Forschung Mbh Gbf Derivados do epotilone sua preparacao e utilizacao
ATE172199T1 (de) 1995-11-20 1998-10-15 Lilly Co Eli Proteinkinase-c-inhibitor
CA2238081A1 (en) 1995-11-22 1997-05-29 S. Jane Desolms Inhibitors of farnesyl-protein transferase
EE03484B1 (et) 1995-12-08 2001-08-15 Janssen Pharmaceutica N.V. Farnesüülproteiintransferaasi inhibeerivad (5-imidasolüül)metüül-2-kinolinooni derivaadid ja nende kasutamine
EP1019392B1 (en) 1995-12-22 2005-11-09 Schering Corporation Tricyclic amides useful for inhibition of g-protein function and for treatment of proliferative diseases
WO1997026246A1 (en) 1996-01-16 1997-07-24 Warner-Lambert Company Substituted histidine inhibitors of protein farnesyltransferase
US6673927B2 (en) 1996-02-16 2004-01-06 Societe De Conseils De Recherches Et D'applications Scientifiques, S.A.S. Farnesyl transferase inhibitors
WO1997038665A2 (en) 1996-04-03 1997-10-23 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
ES2194195T3 (es) 1996-04-12 2003-11-16 Searle & Co N-((4-(5-metil-3-fenililxazol-4-il)fenil)sulfonilpropanamida y su sal sodica como profarmacos de inhibnidores de cox-2.
JP2000511527A (ja) 1996-05-22 2000-09-05 ワーナー―ランバート・コンパニー タンパク質ファルネシルトランスフェラーゼの阻止
CA2260216A1 (en) 1996-07-15 1998-01-22 Bristol-Myers Squibb Company Thiadioxobenzodiazepine inhibitors of farnesyl protein transferase
US5861419A (en) 1996-07-18 1999-01-19 Merck Frosst Canad, Inc. Substituted pyridines as selective cyclooxygenase-2 inhibitors
EP0977563B1 (en) 1996-12-03 2005-10-12 Sloan-Kettering Institute For Cancer Research Synthesis of epothilones, intermediates thereto, analogues and uses thereof
EP1003374A1 (en) 1996-12-30 2000-05-31 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
JP2001507699A (ja) 1996-12-30 2001-06-12 メルク エンド カンパニー インコーポレーテッド ファルネシル蛋白トランスフェラーゼ阻害薬
EP1151002A4 (en) 1999-01-29 2002-05-02 Imclone Systems Inc KDR-SPECIFIC ANTIBODIES AND USES THEREOF
GB9904387D0 (en) 1999-02-25 1999-04-21 Pharmacia & Upjohn Spa Antitumour synergistic composition
AU4972900A (en) 1999-04-08 2000-11-14 Arch Development Corporation Use of anti-vegf antibody to enhance radiation in cancer therapy
US6545004B1 (en) 1999-10-27 2003-04-08 Cytokinetics, Inc. Methods and compositions utilizing quinazolinones
PL203998B1 (pl) 1999-10-27 2009-11-30 Cytokinetics Inc Nowy związek chinazolinowy, zastosowanie związku chinazolinowego, sposób jego otrzymywania i kompozycja farmaceutyczna zawierająca związek chinazolinowy
AU2001231143A1 (en) 2000-01-27 2001-08-07 Cytovia, Inc. Substituted nicotinamides and analogs as activators of caspases and inducers of apoptosis and the use thereof
US6737957B1 (en) * 2000-02-16 2004-05-18 Verance Corporation Remote control signaling using audio watermarks
ATE445613T1 (de) 2000-11-07 2009-10-15 Novartis Pharma Gmbh Indolylmaleimidderivative als proteinkinase-c- inhibitoren
US6645970B2 (en) 2000-11-07 2003-11-11 Novartis Ag Indolylmaleimide derivatives
WO2002083139A1 (en) 2001-04-10 2002-10-24 Merck & Co., Inc. Inhibitors of akt activity
ATE400274T1 (de) 2001-04-10 2008-07-15 Merck & Co Inc Hemmstoffe der akt aktivität
US6958334B2 (en) 2001-04-10 2005-10-25 Merck & Co., Inc. Inhibitors of Akt activity
WO2002083064A2 (en) 2001-04-10 2002-10-24 Merck & Co., Inc. A method of treating cancer
SE0102439D0 (sv) 2001-07-05 2001-07-05 Astrazeneca Ab New compounds
SE0102438D0 (sv) 2001-07-05 2001-07-05 Astrazeneca Ab New compounds
WO2003013526A1 (en) 2001-08-08 2003-02-20 Merck & Co. Inc. Anticoagulant compounds
AU2002363429B2 (en) 2001-11-07 2008-05-08 Merck & Co., Inc. Mitotic kinesin inhibitors
EP1463733B1 (en) 2001-12-06 2007-09-05 Merck & Co., Inc. Mitotic kinesin inhibitors
DE60234278D1 (de) 2001-12-06 2009-12-17 Merck & Co Inc Mitotische kinesin-hemmer
JP4391825B2 (ja) 2001-12-06 2009-12-24 メルク エンド カムパニー インコーポレーテッド 有糸分裂キネシン阻害剤
JP4464136B2 (ja) 2001-12-06 2010-05-19 メルク・シャープ・エンド・ドーム・コーポレイション 有糸分裂キネシン阻害薬
AU2002364128B2 (en) 2001-12-06 2008-03-06 Merck Sharp & Dohme Corp. Mitotic kinesin inhibitors
TW200918046A (en) 2002-04-03 2009-05-01 Novartis Ag Indolylmaleimide derivatives
SE0203754D0 (sv) 2002-12-17 2002-12-17 Astrazeneca Ab New compounds
CA2536964A1 (en) 2003-04-25 2004-11-11 Ortho-Mcneil Pharmaceutical, Inc. C-fms kinase inhibitors
WO2005079802A1 (en) 2004-02-12 2005-09-01 Merck & Co., Inc. Bipyridyl amides as modulators of metabotropic glutamate receptor-5
DE102004039789A1 (de) 2004-08-16 2006-03-02 Sanofi-Aventis Deutschland Gmbh Arylsubstituierte polycyclische Amine, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
CA2584485C (en) 2004-10-20 2013-12-31 Resverlogix Corp. Stilbenes and chalcones for the prevention and treatment of cardiovascular diseases
EP1809620B1 (en) 2004-11-04 2010-12-29 Addex Pharma SA Novel tetrazole derivatives as positive allosteric modulators of metabotropic glutamate receptors
US7781438B2 (en) 2005-07-11 2010-08-24 Novartis Ag Indolylmaleimide derivatives
TW200815426A (en) 2006-06-28 2008-04-01 Astrazeneca Ab New pyridine analogues II 333
BRPI0807107A2 (pt) * 2007-02-08 2014-05-06 Univ California Mutações gnaq no melanoma
MX2009009304A (es) * 2007-03-01 2009-11-18 Novartis Ag Inhibidores de cinasa pim y metodos para su uso.
BRPI0814441A2 (pt) 2007-07-19 2015-07-14 Schering Corp Compostos de amida heterocíclica como inibidores de proteína cinase
PE20091309A1 (es) 2007-12-21 2009-09-30 Astrazeneca Ab Derivados de ciclohexilo como inhibidores de acetil coenzima a carboxilasa
US8168794B2 (en) 2008-03-03 2012-05-01 Novartis Ag Pim kinase inhibitors and methods of their use
CN101971057B (zh) 2008-03-18 2013-03-27 诺瓦提斯公司 眼用透镜涂覆方法
CN104311480A (zh) * 2008-09-02 2015-01-28 诺华股份有限公司 作为激酶抑制剂的吡啶甲酰胺衍生物
WO2010046780A2 (en) 2008-10-22 2010-04-29 Institut Pasteur Korea Anti viral compounds
US8703962B2 (en) 2008-10-24 2014-04-22 Purdue Pharma L.P. Monocyclic compounds and their use as TRPV1 ligands
KR101958632B1 (ko) 2008-12-19 2019-03-15 버텍스 파마슈티칼스 인코포레이티드 Atr 키나제의 억제제로서 유용한 피라진 유도체
CN102245604A (zh) 2008-12-23 2011-11-16 雅培制药有限公司 抗病毒化合物
JP2012529512A (ja) * 2009-06-08 2012-11-22 アブラクシス バイオサイエンス リミテッド ライアビリティー カンパニー トリアジン誘導体類及びそれらの治療応用
US8415381B2 (en) 2009-07-30 2013-04-09 Novartis Ag Heteroaryl compounds and their uses
AU2010291199A1 (en) * 2009-09-04 2012-03-08 Novartis Ag Pyrazinylpyridines useful for the treatment of proliferative diseases
JP5802677B2 (ja) * 2009-12-01 2015-10-28 ライジェル ファーマシューティカルズ, インコーポレイテッド プロテインキナーゼc阻害剤およびその使用
RU2012146083A (ru) * 2010-03-30 2014-05-10 Новартис Аг Ингибиторы ркс для лечения в-клеточной лимфомы с хроническими активным сигнальным каскадом в-клеточного рецептора
US20130109682A1 (en) 2010-07-06 2013-05-02 Novartis Ag Cyclic ether compounds useful as kinase inhibitors
ES2553610T3 (es) 2010-12-14 2015-12-10 Electrophoretics Limited Inhibidores de la caseína cinasa 1 delta (CK1delta)
WO2012101064A1 (en) 2011-01-28 2012-08-02 Novartis Ag N-acyl pyrimidine biaryl compounds as protein kinase inhibitors
UY33930A (es) * 2011-03-04 2012-10-31 Novartis Ag Inhibidores novedosos de quinasas
CN103429572A (zh) 2011-03-04 2013-12-04 诺瓦提斯公司 作为激酶抑制剂的四取代的环己基化合物
WO2012129562A2 (en) 2011-03-24 2012-09-27 The Scripps Research Institute Compounds and methods for inducing chondrogenesis
CN104109161B (zh) 2011-07-27 2016-08-17 阿斯利康(瑞典)有限公司 2-(2,4,5-取代苯胺)嘧啶衍生物作为egfr调谐子用于治疗癌症
JP6204462B2 (ja) * 2012-05-21 2017-09-27 ノバルティス アーゲー キナーゼ阻害剤としての新規環置換n−ピリジニルアミド
CN103570625A (zh) 2012-07-19 2014-02-12 南京英派药业有限公司 N-(3-杂芳基芳基)-4-芳基芳基甲酰胺和类似物作为Hedgehog通路抑制剂及其应用
US20150336960A1 (en) 2012-12-19 2015-11-26 Novartis Ag Aryl-substituted fused bicyclic pyridazine compounds
WO2014181287A1 (en) 2013-05-09 2014-11-13 Piramal Enterprises Limited Heterocyclyl compounds and uses thereof
JO3589B1 (ar) 2014-08-06 2020-07-05 Novartis Ag مثبطات كيناز البروتين c وطرق استخداماتها
WO2019053595A1 (en) * 2017-09-12 2019-03-21 Novartis Ag INHIBITORS OF PROTEIN KINASE C FOR THE TREATMENT OF CHOROIDAL MELLANOMA

Also Published As

Publication number Publication date
UY36258A (es) 2016-04-01
SI3177608T1 (sl) 2020-01-31
EP3177608A1 (en) 2017-06-14
US9452998B2 (en) 2016-09-27
US9845309B2 (en) 2017-12-19
CN106795151B (zh) 2021-05-07
ECSP17013903A (es) 2019-02-28
CN113214246A (zh) 2021-08-06
TN2017000032A1 (en) 2018-07-04
EP3177608B1 (en) 2019-09-18
US20240308979A1 (en) 2024-09-19
EA033361B1 (ru) 2019-10-31
DK3177608T3 (da) 2019-12-09
AU2015298364B2 (en) 2018-08-16
AP2017009729A0 (en) 2017-02-28
GT201700025A (es) 2019-09-30
JP6644765B2 (ja) 2020-02-12
KR102518945B1 (ko) 2023-04-07
US20190202809A1 (en) 2019-07-04
KR20230051605A (ko) 2023-04-18
NZ728604A (en) 2024-02-23
PE20170241A1 (es) 2017-03-22
US20180179181A1 (en) 2018-06-28
AR101456A1 (es) 2016-12-21
CO2017001049A2 (es) 2017-05-31
BR112017002263B1 (pt) 2022-11-29
SG11201700664UA (en) 2017-02-27
ZA201700786B (en) 2021-05-26
KR102605181B1 (ko) 2023-11-27
PL3177608T3 (pl) 2020-03-31
PH12017500215A1 (en) 2017-07-10
CY1122407T1 (el) 2021-01-27
CU24465B1 (es) 2020-01-03
MX2017001640A (es) 2017-09-01
CR20170036A (es) 2017-05-08
NI201700012A (es) 2017-03-08
MY195488A (en) 2023-01-26
IL250318A0 (en) 2017-03-30
US11505541B2 (en) 2022-11-22
US11059804B2 (en) 2021-07-13
US20210387962A1 (en) 2021-12-16
JP2017523215A (ja) 2017-08-17
US20160046605A1 (en) 2016-02-18
SV2017005373A (es) 2018-05-03
CU20170010A7 (es) 2017-06-05
ES2754248T3 (es) 2020-04-16
US20160347737A1 (en) 2016-12-01
TWI680968B (zh) 2020-01-01
LT3177608T (lt) 2019-10-10
TW201619148A (zh) 2016-06-01
CA2956996A1 (en) 2016-02-11
CN106795151A (zh) 2017-05-31
US10508101B2 (en) 2019-12-17
JO3589B1 (ar) 2020-07-05
RS59692B1 (sr) 2020-01-31
EA201790323A1 (ru) 2017-06-30
CA2956996C (en) 2023-01-03
KR20170033435A (ko) 2017-03-24
BR112017002263A2 (pt) 2017-11-21
IL250318B (en) 2020-05-31
DOP2017000035A (es) 2017-04-30
US20200262814A1 (en) 2020-08-20
CL2017000290A1 (es) 2017-07-14
AU2015298364A1 (en) 2017-02-16
PT3177608T (pt) 2019-12-03
HUE047862T2 (hu) 2020-05-28
WO2016020864A1 (en) 2016-02-11
EP3514151A1 (en) 2019-07-24

Similar Documents

Publication Publication Date Title
HRP20192224T1 (hr) Inhibitori proteinske kinaze c i metode za njihovu primjenu
AR117163A2 (es) Composiciones parasiticidas que comprenden un agente activo de isoxazolina, sus métodos y usos
HRP20171453T1 (hr) Derivati imidazotiadiazola i imidazopirazina kao inhibitori proteazom aktiviranog receptora 4 (par4) za liječenje agregacije trombocita
AR093017A1 (es) MODULARES DE RORgT DE QUINOLINILO UNIDOS POR METILENO
MY187479A (en) 2,3-disubstituted 1-acyl-4-amino-1,2,3,4-tetrahydroquinoline derivatives and their use as bromodomain inhibitors
CY1124085T1 (el) Κρυσταλλικα αλατα (s)-6-((1-ακετυλπιπεριδιν-4-υλ)αμινο)-ν-(3-(3,4-διυδροϊσοκινολιν-2(1η)-υλ)-2-υδροξυπροπυλ)πυριμιδινο-4-καρβοξαμιδιου
EA201301319A1 (ru) Производные пиридин-2(1н)-она, применимые в качестве лекарственных средств для лечения миелопролиферативных нарушений, отторжения трансплантата, иммунологически обусловленных и воспалительных заболеваний
AR092253A1 (es) Inhibidores de serina/treonina cinasa
JP2017523215A5 (hr)
PE20180177A1 (es) Derivados de 1-(het) arilsulfonil-(pirrolidin o piperidin)-2-carboxamida y su uso como antagonistas de trpa1
CR20160548A (es) Nuevos Derivados de Pirazolo Pirimidina y su Uso como Inhibidores de MALT1
AR085324A1 (es) Composiciones de moleculas pesticidas y proceso de aplicacion de dichas composiciones para controlar acaros, insectos y otras plagas
EA201992270A2 (ru) 4-имидазопиридазин-1-ил-бензамиды и 4-имидазотриазин-1-ил-бензамиды в качестве btk-ингибиторов
MA35903B1 (fr) Nouveaux derives d'indolizine, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
MX2015014861A (es) Pirimidinas sustituidas con heterocicloalquilo c-enlazado y sus usos.
EA201400553A1 (ru) Производные 2-(1,2,3-триазол-2-ил)бензамида и 3-(1,2,3-триазол-2-ил)пиколинамида
EA201590748A1 (ru) Противовирусные соединения против rsv
JP2014525420A5 (hr)
AR087355A1 (es) Derivados de piridin-2(1h)-ona como inhibidores de jak
EA201290073A1 (ru) Соединения мочевины, содержащие 5,6-бициклический гетероарил, как ингибиторы киназ
EA201692266A1 (ru) Ингибиторы фосфатидилинозитол-3-киназы
EA201692000A1 (ru) Макроциклические производные пиридина
RS54415B1 (en) BENZAMIDE SUBSTITUTED DERIVATIVES
PE20150774A1 (es) Aminoquinolinas como inhibidores de cinasa
PH12019500497A1 (en) Heteroaryl carboxamide compounds as inhibitors of ripk2