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

Inhibitori proteinske kinaze c i metode za njihovu primjenu Download PDF

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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
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amino
pyridin
carboxamide
pyrazine
trifluoromethyl
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Michael Joseph Luzzio
Julien Papillon
Michael Scott Visser
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Novartis Ag
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic 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
    • C07D495/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

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  • Health & Medical Sciences (AREA)
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  • 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)

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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
RU2018108804A (ru) * 2015-08-14 2019-09-16 Новартис Аг Фармацевтические комбинации и их применение
SG11201900090TA (en) 2016-07-14 2019-02-27 Mingsight Pharmaceuticals Inc Treatment of cancer
US11413284B2 (en) * 2017-09-12 2022-08-16 Novartis Ag Protein kinase C inhibitors for treatment of uveal melanoma
LT3762368T (lt) 2018-03-08 2022-06-10 Incyte Corporation Aminopirazindiolio junginiai, kaip pi3k-γ inhibitoriai
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
WO2020010003A1 (en) 2018-07-02 2020-01-09 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
KR102405055B1 (ko) * 2019-01-16 2022-06-07 상하이 잉리 파마슈티컬 컴퍼니 리미티드 모르폴리노퀴나졸린 화합물의 제조방법 및 이의 중간체
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
US20220401440A1 (en) * 2019-11-18 2022-12-22 Ideaya Biosciences, Inc. Dosing regimens for a protein kinase c inhibitor
BR112022024071A2 (pt) 2020-05-27 2022-12-20 Axial Therapeutics Inc Compostos moduladores de tlr2, composições farmacêuticas e usos dos mesmos
PL243663B1 (pl) * 2020-06-29 2023-09-25 Univ Medyczny Im Piastow Slaskich We Wroclawiu Zastosowanie wanikozydów
IL300952A (en) * 2020-09-08 2023-04-01 Ideaya Biosciences Inc Drug combination and tumor treatment
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
US4231938A (en) 1979-06-15 1980-11-04 Merck & Co., Inc. Hypocholesteremic fermentation products and process of preparation
US4319039A (en) 1979-06-15 1982-03-09 Merck & Co., Inc. Preparation of ammonium salt of hypocholesteremic fermentation product
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
WO1984002131A1 (en) 1982-11-22 1984-06-07 Sandoz Ag Analogs of mevalolactone and derivatives thereof, processes for their production, pharmaceutical compositions containing them and their use as pharmaceuticals
US5354772A (en) 1982-11-22 1994-10-11 Sandoz Pharm. Corp. Indole analogs of mevalonolactone and derivatives thereof
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
US4885314A (en) 1987-06-29 1989-12-05 Merck & Co., Inc. Novel HMG-CoA reductase inhibitors
US4782084A (en) 1987-06-29 1988-11-01 Merck & Co., Inc. 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
US5030447A (en) 1988-03-31 1991-07-09 E. R. Squibb & Sons, Inc. Pharmaceutical compositions having good stability
US5180589A (en) 1988-03-31 1993-01-19 E. R. Squibb & Sons, Inc. Pravastatin pharmaceuatical 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
CA2297592A1 (en) 1993-01-15 1994-07-21 G.D. Searle & Co. 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
WO1994026723A2 (en) 1993-05-14 1994-11-24 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
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
US5474995A (en) 1993-06-24 1995-12-12 Merck Frosst Canada, Inc. Phenyl heterocycles as cox-2 inhibitors
WO1995008542A1 (fr) 1993-09-22 1995-03-30 Kyowa Hakko Kogyo Co., Ltd. Inhibiteur de la farnesyl-transferase
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
TW308594B (hr) 1993-10-15 1997-06-21 Schering Corp
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
JP2875392B2 (ja) 1993-10-15 1999-03-31 シェーリング コーポレイション Ｇ−タンパク質機能の阻害および増殖性疾患の治療に有用な三環式スルホンアミド化合物
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
NZ275037A (en) 1993-10-25 1998-01-26 Parke Davis & Co Substituted tetra- and pentapeptide inhibitors of protein as farnesyl transferase inhibitors
US5344991A (en) 1993-10-29 1994-09-06 G.D. Searle & Co. 1,2 diarylcyclopentenyl compounds for the treatment of inflammation
ES2130452T3 (es) 1993-11-04 1999-07-01 Abbott Lab Derivados de ciclobutano utilizados como inhibidores de la escualeno-sintetasa y de la farnesiltransferasa proteica.
US5783593A (en) 1993-11-04 1998-07-21 Abbott Laboratories Inhibitors of squalene synthetase and protein farnesyltransferase
HUT75308A (en) 1993-11-05 1997-05-28 Warner Lambert Co Substituted di- and tripeptide inhibitors of protein:farnesyl transferase
US5466823A (en) 1993-11-30 1995-11-14 G.D. Searle & Co. Substituted pyrazolyl benzenesulfonamides
PT657458E (pt) 1993-12-07 2002-02-28 Lilly Co Eli Inibidores de proteina cinase c
US5484799A (en) 1993-12-09 1996-01-16 Abbott Laboratories Antifungal dorrigocin derivatives
ATE456367T1 (de) 1993-12-23 2010-02-15 Lilly Co Eli Proteinkinase c inhibitoren
US5545636A (en) 1993-12-23 1996-08-13 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
CA2185441A1 (en) 1994-03-15 1995-09-21 Michael D. Lewis Isoprenyl transferase inhibitors
AU1615895A (en) 1994-03-31 1995-10-12 Bristol-Myers Squibb Company Imidazole-containing inhibitors of farnesyl protein transferase
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
PL317580A1 (en) 1994-06-10 1997-04-14 Rhone Poulenc Rorer Sa Novel inhibitors of farnesil transferase, method of obtaining them and pharmaceutic compositions containing such inhibitors
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
AU3192395A (en) 1994-08-11 1996-03-07 Banyu Pharmaceutical Co., Ltd. Substituted amide derivative
CA2155448A1 (en) 1994-08-11 1996-02-12 Katerina Leftheris Inhibitors of farnesyl protein transferase
WO1996005169A1 (fr) 1994-08-12 1996-02-22 Banyu Pharmaceutical Co., Ltd. Derive d'acide amique n,n-bisubstitue
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
KR100389754B1 (ko) 1994-11-22 2003-10-17 코닌클리즈케 필립스 일렉트로닉스 엔.브이. 반도체장치
AU3971295A (en) 1994-12-09 1996-06-26 Warner-Lambert Company Substituted tetra- and pentapeptide inhibitors of protein:farnesyl transferase
EA000164B1 (ru) 1995-01-09 1998-10-29 Магла Интернэшнл Лтд. Состав для печати изображения на поверхности изделия из каучукового латекса, способ печати изображения и изделия из каучукового латекса
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
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
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
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
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
AU5432696A (en) 1995-04-07 1996-10-23 Pharmacopeia, Inc. Carbonyl-piperazinyl and piperidinil compounds which inhibit farnesyl protein transferase
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
AU6034296A (en) 1995-06-16 1997-01-15 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
DE69627377T2 (de) 1995-11-06 2004-02-05 University Of Pittsburgh Inhibitoren der protein-isoprenyl-transferase
ES2218328T5 (es) 1995-11-17 2011-11-11 GESELLSCHAFT FüR BIOTECHNOLOGISCHE FORSCHUNG MBH (GBF) Derivados de epotilón, su preparación y utilización.
CN1093759C (zh) 1995-11-20 2002-11-06 伊莱利利公司 蛋白激酶c抑制剂
WO1997018813A1 (en) 1995-11-22 1997-05-29 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
CZ293296B6 (cs) 1995-12-08 2004-03-17 Janssen Pharmaceutica N.V. (Imidazol-5-yl)methyl-2-chinolinonové deriváty inhibující farnesyl protein transferázu
TW350844B (en) 1995-12-22 1999-01-21 Schering Corp Tricyclic amides useful to 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
CA2249601A1 (en) 1996-04-03 1997-10-23 Thorsten E. Fisher Inhibitors of farnesyl-protein transferase
CA2249009C (en) 1996-04-12 2003-09-16 G.D. Searle & Co. Substituted benzenesulfonamide derivatives as prodrugs of cox-2 inhibitors
WO1997044350A1 (en) 1996-05-22 1997-11-27 Warner-Lambert Company Inhibitors of protein farnesyl transferase
WO1998002436A1 (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
EP1386922B1 (en) 1996-12-03 2012-04-11 Sloan-Kettering Institute For Cancer Research Synthesis of epothilones, intermediates thereof, analogues and uses thereof
CA2276081A1 (en) 1996-12-30 1998-07-09 Lekhanh O. Tran Inhibitors of farnesyl-protein transferase
AU5719598A (en) 1996-12-30 1998-07-31 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
IL144578A0 (en) 1999-01-29 2002-05-23 Imclone Systems Inc Antibodies specific to kdr and uses thereof
GB9904387D0 (en) 1999-02-25 1999-04-21 Pharmacia & Upjohn Spa Antitumour synergistic composition
WO2000061186A1 (en) 1999-04-08 2000-10-19 Arch Development Corporation Use of anti-vegf antibody to enhance radiation in cancer therapy
EP1686120A3 (en) 1999-10-27 2007-05-30 Cytokinetics, Inc. Methods and compositions utilizing quinazolinones
US6545004B1 (en) 1999-10-27 2003-04-08 Cytokinetics, Inc. Methods and compositions utilizing quinazolinones
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
US6645970B2 (en) 2000-11-07 2003-11-11 Novartis Ag Indolylmaleimide derivatives
IL155618A0 (en) 2000-11-07 2003-11-23 Novartis Ag Indolylmaleimide derivatives as protein kinase c inhibitors
EP1379251B1 (en) 2001-04-10 2008-07-09 Merck & Co., Inc. Inhibitors of akt activity
EP1379250A2 (en) 2001-04-10 2004-01-14 Merck & Co., Inc. A method of treating cancer
WO2002083140A1 (en) 2001-04-10 2002-10-24 Merck & Co., Inc. Inhibitors of akt activity
WO2002083139A1 (en) 2001-04-10 2002-10-24 Merck & Co., Inc. Inhibitors of akt activity
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
US7060705B2 (en) 2001-11-07 2006-06-13 Merck & Co., Inc. Mitotic kinesin inhibitors
CA2468156A1 (en) 2001-12-06 2003-06-19 Merck & Co., Inc. Azolopyrimidinone compounds and their use
EP1458726B1 (en) 2001-12-06 2009-07-15 Merck & Co., Inc. Mitotic kinesin inhibitors
ES2291543T3 (es) 2001-12-06 2008-03-01 MERCK & CO., INC. Inhibicion de kinesina mitotica.
US7244723B2 (en) 2001-12-06 2007-07-17 Merck & Co., Inc. Substituted furopyrimidinones as a mitotic kinesin inhibitors
EP1551812B1 (en) 2001-12-06 2009-03-04 Merck & Co., Inc. 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
WO2004096795A2 (en) 2003-04-25 2004-11-11 3-Dimensional Pharmaceuticals, Inc. C-fms kinase inhibitors
CA2555402A1 (en) 2004-02-12 2005-09-01 Celine Bonnefous 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
EP1838296B1 (en) 2004-10-20 2012-08-08 Resverlogix Corp. Flavanoids and isoflavanoids for the prevention and treatment of cardiovascular diseases
WO2006048771A1 (en) 2004-11-04 2006-05-11 Addex Pharmaceuticals Sa Novel tetrazole derivatives as positive allosteric modulators of metabotropic glutamate receptors
KR20080023732A (ko) 2005-07-11 2008-03-14 노파르티스 아게 인돌릴말레이미드 유도체
TW200815426A (en) 2006-06-28 2008-04-01 Astrazeneca Ab New pyridine analogues II 333
KR20090113325A (ko) * 2007-02-08 2009-10-29 더 리젠츠 오브 더 유니버시티 오브 캘리포니아 흑색종에서의 ｇｎａｑ 돌연변이
MX2009009304A (es) * 2007-03-01 2009-11-18 Novartis Ag Inhibidores de cinasa pim y metodos para su uso.
EP2178861B1 (en) 2007-07-19 2014-08-20 Merck Sharp & Dohme Corp. Heterocyclic amide compounds as protein kinase inhibitors
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
WO2009115477A2 (en) 2008-03-18 2009-09-24 Novartis Ag Coating process for ophthalmic lenses
GEP20135849B (en) 2008-09-02 2013-06-10 Novartis Ag Picolinamide derivatives as kinase inhibitors
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
KR101755216B1 (ko) 2008-12-19 2017-07-07 버텍스 파마슈티칼스 인코포레이티드 Ａｔｒ 키나제의 억제제로서 유용한 피라진 유도체
EP2367823A1 (en) 2008-12-23 2011-09-28 Abbott Laboratories Anti-viral compounds
AU2010259009A1 (en) 2009-06-08 2012-01-12 Nantbioscience, Inc. Triazine derivatives and their therapeutical applications
US8415381B2 (en) 2009-07-30 2013-04-09 Novartis Ag Heteroaryl compounds and their uses
CN102482265A (zh) * 2009-09-04 2012-05-30 诺瓦提斯公司 用于治疗增殖性疾病的吡嗪基吡啶化合物
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
EP2552428A1 (en) * 2010-03-30 2013-02-06 Novartis AG Pkc inhibitors for the treatment of b-cell lymphoma having chronic active b-cell-receptor signalling
JP2013530199A (ja) * 2010-07-06 2013-07-25 ノバルティス アーゲー キナーゼ阻害剤として有用な環状エーテル化合物
EP2651404B1 (en) 2010-12-14 2015-10-14 Electrophoretics Limited Casein kinase 1delta (ck1delta) inhibitors
WO2012101064A1 (en) 2011-01-28 2012-08-02 Novartis Ag N-acyl pyrimidine biaryl compounds as protein kinase inhibitors
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
UY33930A (es) 2011-03-04 2012-10-31 Novartis Ag Inhibidores novedosos de quinasas
WO2012129562A2 (en) 2011-03-24 2012-09-27 The Scripps Research Institute Compounds and methods for inducing chondrogenesis
ME02382B (me) 2011-07-27 2016-06-20 Astrazeneca Ab 2-(2,4,5-supstituisani-anilino) piramidisnki derivati kao egfr modulatori korisni za tretman raka
US9173883B2 (en) * 2012-05-21 2015-11-03 Novartis Ag Ring-substituted N-pyridinyl amides as kinase inhibitors
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
US11413284B2 (en) * 2017-09-12 2022-08-16 Novartis Ag Protein kinase C inhibitors for treatment of uveal melanoma

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