ES2535166T3 - Pirimidinil-aminas sustituidas como inhibidores de proteína-quinasas - Google Patents
Pirimidinil-aminas sustituidas como inhibidores de proteína-quinasas Download PDFInfo
- Publication number
- ES2535166T3 ES2535166T3 ES08829943.3T ES08829943T ES2535166T3 ES 2535166 T3 ES2535166 T3 ES 2535166T3 ES 08829943 T ES08829943 T ES 08829943T ES 2535166 T3 ES2535166 T3 ES 2535166T3
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- Prior art keywords
- phenyl
- substituted
- pyrimidin
- ring
- acetamide
- Prior art date
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- -1 pyrimidinyl amines Chemical class 0.000 title abstract description 6
- 229940045988 antineoplastic drug protein kinase inhibitors Drugs 0.000 title 1
- 239000003909 protein kinase inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract description 8
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 abstract description 2
- 125000000623 heterocyclic group Chemical group 0.000 abstract 9
- 229910052760 oxygen Inorganic materials 0.000 abstract 8
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 5
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 5
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 5
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 5
- 241000689227 Cora <basidiomycete fungus> Species 0.000 abstract 4
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 4
- 229910052717 sulfur Inorganic materials 0.000 abstract 4
- 125000002837 carbocyclic group Chemical group 0.000 abstract 3
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 2
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 2
- 229910052799 carbon Inorganic materials 0.000 abstract 2
- 125000004432 carbon atom Chemical group C* 0.000 abstract 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 abstract 2
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 2
- 229910052757 nitrogen Inorganic materials 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- BZSFXOJTWOPMGE-JOCHJYFZSA-N (2r)-n-[4-[2-(1,2,3,4-tetrahydroquinolin-6-ylamino)pyrimidin-4-yl]phenyl]pyrrolidine-2-carboxamide Chemical compound C=1C=C(C=2N=C(NC=3C=C4CCCNC4=CC=3)N=CC=2)C=CC=1NC(=O)[C@H]1CCCN1 BZSFXOJTWOPMGE-JOCHJYFZSA-N 0.000 abstract 1
- LTWXVCJYDNEWDA-OAQYLSRUSA-N (2r)-n-[4-[2-[(6-morpholin-4-ylpyridin-3-yl)amino]pyrimidin-4-yl]phenyl]pyrrolidine-2-carboxamide Chemical compound O=C([C@@H]1NCCC1)NC(C=C1)=CC=C1C(N=1)=CC=NC=1NC(C=N1)=CC=C1N1CCOCC1 LTWXVCJYDNEWDA-OAQYLSRUSA-N 0.000 abstract 1
- 125000006650 (C2-C4) alkynyl group Chemical group 0.000 abstract 1
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 1
- 125000006569 (C5-C6) heterocyclic group Chemical group 0.000 abstract 1
- 125000006091 1,3-dioxolane group Chemical group 0.000 abstract 1
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 abstract 1
- JCXJVPUVTGWSNB-UHFFFAOYSA-N Nitrogen dioxide Chemical compound O=[N]=O JCXJVPUVTGWSNB-UHFFFAOYSA-N 0.000 abstract 1
- MPVDXIMFBOLMNW-UHFFFAOYSA-N chembl1615565 Chemical compound OC1=CC=C2C=C(S(O)(=O)=O)C=C(S(O)(=O)=O)C2=C1N=NC1=CC=CC=C1 MPVDXIMFBOLMNW-UHFFFAOYSA-N 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 1
- KWCRWNXTHBZLFB-UHFFFAOYSA-N n-[3-[[4-(4-acetamidophenyl)pyrimidin-2-yl]amino]cyclohexyl]-2,6-dichlorobenzamide Chemical compound C1=CC(NC(=O)C)=CC=C1C1=CC=NC(NC2CC(CCC2)NC(=O)C=2C(=CC=CC=2Cl)Cl)=N1 KWCRWNXTHBZLFB-UHFFFAOYSA-N 0.000 abstract 1
- JAJXXHHNPOCMMX-UHFFFAOYSA-N n-[4-[2-(1h-indazol-5-ylamino)-5-methylpyrimidin-4-yl]phenyl]acetamide Chemical compound C1=CC(NC(=O)C)=CC=C1C1=NC(NC=2C=C3C=NNC3=CC=2)=NC=C1C JAJXXHHNPOCMMX-UHFFFAOYSA-N 0.000 abstract 1
- MLADDFUCCSVLNA-UHFFFAOYSA-N n-[4-[2-(1h-indazol-6-ylamino)-5-methylpyrimidin-4-yl]phenyl]acetamide Chemical compound C1=CC(NC(=O)C)=CC=C1C1=NC(NC=2C=C3NN=CC3=CC=2)=NC=C1C MLADDFUCCSVLNA-UHFFFAOYSA-N 0.000 abstract 1
- YOODJCZFGYXUCN-UHFFFAOYSA-N n-[4-[2-(1h-indol-5-ylamino)-5-methylpyrimidin-4-yl]phenyl]acetamide Chemical compound C1=CC(NC(=O)C)=CC=C1C1=NC(NC=2C=C3C=CNC3=CC=2)=NC=C1C YOODJCZFGYXUCN-UHFFFAOYSA-N 0.000 abstract 1
- NYHNJXKTKRGCRV-UHFFFAOYSA-N n-[4-[2-(3h-benzimidazol-5-ylamino)-5-methylpyrimidin-4-yl]phenyl]acetamide Chemical compound C1=CC(NC(=O)C)=CC=C1C1=NC(NC=2C=C3NC=NC3=CC=2)=NC=C1C NYHNJXKTKRGCRV-UHFFFAOYSA-N 0.000 abstract 1
- XUFRAXSDLREMKW-UHFFFAOYSA-N n-[4-[2-(piperidin-4-ylamino)pyrimidin-4-yl]phenyl]acetamide Chemical compound C1=CC(NC(=O)C)=CC=C1C1=CC=NC(NC2CCNCC2)=N1 XUFRAXSDLREMKW-UHFFFAOYSA-N 0.000 abstract 1
- NHCQZVLLRICHSK-UHFFFAOYSA-N n-[4-[2-[(6-aminopyridin-2-yl)amino]pyrimidin-4-yl]phenyl]acetamide Chemical compound C1=CC(NC(=O)C)=CC=C1C1=CC=NC(NC=2N=C(N)C=CC=2)=N1 NHCQZVLLRICHSK-UHFFFAOYSA-N 0.000 abstract 1
- POQVDVCNGKTSOU-UHFFFAOYSA-N n-[4-[2-[4-(1,4-dioxa-8-azaspiro[4.5]decan-8-yl)anilino]pyrimidin-4-yl]phenyl]acetamide Chemical compound C1=CC(NC(=O)C)=CC=C1C1=CC=NC(NC=2C=CC(=CC=2)N2CCC3(CC2)OCCO3)=N1 POQVDVCNGKTSOU-UHFFFAOYSA-N 0.000 abstract 1
- RRYULDWOMIUUEE-UHFFFAOYSA-N n-[4-[2-[[1-(2,6-dichlorobenzoyl)piperidin-4-yl]amino]pyrimidin-4-yl]phenyl]acetamide Chemical compound C1=CC(NC(=O)C)=CC=C1C1=CC=NC(NC2CCN(CC2)C(=O)C=2C(=CC=CC=2Cl)Cl)=N1 RRYULDWOMIUUEE-UHFFFAOYSA-N 0.000 abstract 1
- JXYBWWRITKUQLG-UHFFFAOYSA-N n-[6-[[4-(4-acetamidophenyl)pyrimidin-2-yl]amino]pyrimidin-4-yl]-2,6-dichlorobenzamide Chemical compound C1=CC(NC(=O)C)=CC=C1C1=CC=NC(NC=2N=CN=C(NC(=O)C=3C(=CC=CC=3Cl)Cl)C=2)=N1 JXYBWWRITKUQLG-UHFFFAOYSA-N 0.000 abstract 1
- 125000004430 oxygen atom Chemical group O* 0.000 abstract 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 1
- 125000004527 pyrimidin-4-yl group Chemical group N1=CN=C(C=C1)* 0.000 abstract 1
- 238000000034 method Methods 0.000 description 13
- 238000003786 synthesis reaction Methods 0.000 description 8
- 125000006239 protecting group Chemical group 0.000 description 7
- 230000015572 biosynthetic process Effects 0.000 description 4
- IADLVSLZPQYXIF-UHFFFAOYSA-N 3-bromo-5-fluorobenzonitrile Chemical compound FC1=CC(Br)=CC(C#N)=C1 IADLVSLZPQYXIF-UHFFFAOYSA-N 0.000 description 3
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 3
- KDLHZDBZIXYQEI-UHFFFAOYSA-N Palladium Chemical compound [Pd] KDLHZDBZIXYQEI-UHFFFAOYSA-N 0.000 description 3
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 3
- 238000006243 chemical reaction Methods 0.000 description 3
- NXRPIDXQLIHMEJ-UHFFFAOYSA-N n-[4-(3-methyl-1,2,4-triazol-1-yl)phenyl]-4-trimethylstannylpyrimidin-2-amine Chemical compound N1=C(C)N=CN1C(C=C1)=CC=C1NC1=NC=CC([Sn](C)(C)C)=N1 NXRPIDXQLIHMEJ-UHFFFAOYSA-N 0.000 description 3
- KWUBTXODVYERDX-UHFFFAOYSA-N 3-[2-[4-(3-methyl-1,2,4-triazol-1-yl)anilino]pyrimidin-4-yl]-5-(oxan-4-ylamino)benzonitrile Chemical compound N1=C(C)N=CN1C(C=C1)=CC=C1NC1=NC=CC(C=2C=C(C=C(NC3CCOCC3)C=2)C#N)=N1 KWUBTXODVYERDX-UHFFFAOYSA-N 0.000 description 2
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 2
- 125000000524 functional group Chemical group 0.000 description 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 2
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 2
- 230000009466 transformation Effects 0.000 description 2
- 238000000844 transformation Methods 0.000 description 2
- ASUDFOJKTJLAIK-UHFFFAOYSA-N 2-methoxyethanamine Chemical compound COCCN ASUDFOJKTJLAIK-UHFFFAOYSA-N 0.000 description 1
- DGERNRJAWXZTEM-UHFFFAOYSA-N 3-(2-methoxyethylamino)-5-[2-[4-(3-methyl-1,2,4-triazol-1-yl)anilino]pyrimidin-4-yl]benzonitrile Chemical compound COCCNC1=CC(C#N)=CC(C=2N=C(NC=3C=CC(=CC=3)N3N=C(C)N=C3)N=CC=2)=C1 DGERNRJAWXZTEM-UHFFFAOYSA-N 0.000 description 1
- XPOIRRLDFSJOBW-UHFFFAOYSA-N 3-(cyclohexylamino)-5-[2-[4-(3-methyl-1,2,4-triazol-1-yl)anilino]pyrimidin-4-yl]benzonitrile Chemical compound N1=C(C)N=CN1C(C=C1)=CC=C1NC1=NC=CC(C=2C=C(C=C(NC3CCCCC3)C=2)C#N)=N1 XPOIRRLDFSJOBW-UHFFFAOYSA-N 0.000 description 1
- WLRXVMLMVCRTHC-UHFFFAOYSA-N 3-[2-[4-(3-methyl-1,2,4-triazol-1-yl)anilino]pyrimidin-4-yl]-5-(propan-2-ylamino)benzonitrile Chemical compound CC(C)NC1=CC(C#N)=CC(C=2N=C(NC=3C=CC(=CC=3)N3N=C(C)N=C3)N=CC=2)=C1 WLRXVMLMVCRTHC-UHFFFAOYSA-N 0.000 description 1
- HRSZVQXXXHYWNV-UHFFFAOYSA-N 3-bromo-5-(2-methoxyethylamino)benzonitrile Chemical compound COCCNC1=CC(Br)=CC(C#N)=C1 HRSZVQXXXHYWNV-UHFFFAOYSA-N 0.000 description 1
- LODWQHRKTQIXDG-UHFFFAOYSA-N 3-bromo-5-(cyclohexylamino)benzonitrile Chemical compound N#CC1=CC(Br)=CC(NC2CCCCC2)=C1 LODWQHRKTQIXDG-UHFFFAOYSA-N 0.000 description 1
- VMQCLKCFUOBFBL-UHFFFAOYSA-N 3-bromo-5-(oxan-4-ylamino)benzonitrile Chemical compound N#CC1=CC(Br)=CC(NC2CCOCC2)=C1 VMQCLKCFUOBFBL-UHFFFAOYSA-N 0.000 description 1
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 1
- 229920000168 Microcrystalline cellulose Polymers 0.000 description 1
- PAYRUJLWNCNPSJ-UHFFFAOYSA-N N-phenyl amine Natural products NC1=CC=CC=C1 PAYRUJLWNCNPSJ-UHFFFAOYSA-N 0.000 description 1
- ISWSIDIOOBJBQZ-UHFFFAOYSA-N Phenol Chemical compound OC1=CC=CC=C1 ISWSIDIOOBJBQZ-UHFFFAOYSA-N 0.000 description 1
- 239000004480 active ingredient Substances 0.000 description 1
- 239000013543 active substance Substances 0.000 description 1
- 150000001448 anilines Chemical class 0.000 description 1
- 125000001584 benzyloxycarbonyl group Chemical group C(=O)(OCC1=CC=CC=C1)* 0.000 description 1
- 239000002775 capsule Substances 0.000 description 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 description 1
- 239000003054 catalyst Substances 0.000 description 1
- 230000003197 catalytic effect Effects 0.000 description 1
- 239000003153 chemical reaction reagent Substances 0.000 description 1
- PAFZNILMFXTMIY-UHFFFAOYSA-N cyclohexylamine Chemical compound NC1CCCCC1 PAFZNILMFXTMIY-UHFFFAOYSA-N 0.000 description 1
- 239000007903 gelatin capsule Substances 0.000 description 1
- 125000005843 halogen group Chemical group 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- 229940102223 injectable solution Drugs 0.000 description 1
- 239000008101 lactose Substances 0.000 description 1
- 235000019359 magnesium stearate Nutrition 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- 235000019813 microcrystalline cellulose Nutrition 0.000 description 1
- 239000008108 microcrystalline cellulose Substances 0.000 description 1
- 229940016286 microcrystalline cellulose Drugs 0.000 description 1
- 239000000203 mixture Substances 0.000 description 1
- AHVQYHFYQWKUKB-UHFFFAOYSA-N oxan-4-amine Chemical compound NC1CCOCC1 AHVQYHFYQWKUKB-UHFFFAOYSA-N 0.000 description 1
- 229910052763 palladium Inorganic materials 0.000 description 1
- 239000002245 particle Substances 0.000 description 1
- 150000003230 pyrimidines Chemical class 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 125000001424 substituent group Chemical group 0.000 description 1
- 239000000454 talc Substances 0.000 description 1
- 229910052623 talc Inorganic materials 0.000 description 1
- 125000005931 tert-butyloxycarbonyl group Chemical group [H]C([H])([H])C(OC(*)=O)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
Classifications
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- C—CHEMISTRY; METALLURGY
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/32—One oxygen, sulfur or nitrogen atom
- C07D239/42—One nitrogen atom
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- 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
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- 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
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
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- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
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- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/10—Spiro-condensed systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/10—Spiro-condensed systems
- C07D491/113—Spiro-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
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Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
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| US96984907P | 2007-09-04 | 2007-09-04 | |
| US969849P | 2007-09-04 | ||
| PCT/US2008/075151 WO2009032861A1 (en) | 2007-09-04 | 2008-09-03 | Substituted pyrimidinyl-amines as protein kinase inhibitors |
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| ES2535166T3 true ES2535166T3 (es) | 2015-05-06 |
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| ES08829943.3T Active ES2535166T3 (es) | 2007-09-04 | 2008-09-03 | Pirimidinil-aminas sustituidas como inhibidores de proteína-quinasas |
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| EP (1) | EP2200436B1 (cg-RX-API-DMAC7.html) |
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| CA (1) | CA2698511C (cg-RX-API-DMAC7.html) |
| ES (1) | ES2535166T3 (cg-RX-API-DMAC7.html) |
| PT (1) | PT2200436E (cg-RX-API-DMAC7.html) |
| WO (1) | WO2009032861A1 (cg-RX-API-DMAC7.html) |
Families Citing this family (98)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2010513384A (ja) | 2006-12-22 | 2010-04-30 | エフ.ホフマン−ラ ロシュ アーゲー | スピロ−ピペリジン誘導体 |
| AU2016200866B2 (en) * | 2007-03-12 | 2017-06-22 | Glaxosmithkline Llc | Phenyl amino pyrimidine compounds and uses thereof |
| PL2152701T3 (pl) * | 2007-03-12 | 2016-10-31 | Związki fenyloaminopirymidyny i ich zastosowania | |
| AU2013201306B2 (en) * | 2007-03-12 | 2015-11-12 | Glaxosmithkline Llc | Phenyl Amino Pyrimidine Compounds and Uses Thereof |
| EP2137165B1 (en) * | 2007-04-24 | 2013-04-24 | Ingenium Pharmaceuticals GmbH | Inhibitors of protein kinases |
| EP2200436B1 (en) | 2007-09-04 | 2015-01-21 | The Scripps Research Institute | Substituted pyrimidinyl-amines as protein kinase inhibitors |
| BRPI0906799A2 (pt) | 2008-01-11 | 2015-07-14 | Hoffmann La Roche | Moduladores para amiloide beta |
| KR101247840B1 (ko) * | 2008-02-22 | 2013-03-26 | 에프. 호프만-라 로슈 아게 | 아밀로이드 베타 조절제 |
| MX2011003246A (es) | 2008-10-09 | 2011-04-21 | Hoffmann La Roche | Moduladores de beta amiloide. |
| KR101293421B1 (ko) | 2008-11-10 | 2013-08-05 | 에프. 호프만-라 로슈 아게 | 헤테로사이클릭 감마 분비효소 조절제 |
| MX2012004313A (es) * | 2009-10-12 | 2012-07-20 | Myrexis Inc | Compuestos de amino-pirimidina como inhibidores de cinasa 1 de union a tank (tbk1) y/o i-kappa-b-cinasa epsilon (ikk epsilon). |
| WO2011075560A1 (en) | 2009-12-17 | 2011-06-23 | Merck Sharp & Dohme Corp. | Aminopyrimidines as syk inhibitors |
| MA33926B1 (fr) | 2009-12-17 | 2013-01-02 | Merck Sharp & Dohme | Aminopyrimidines en tant qu'inhibiteurs de la syk |
| US8486967B2 (en) | 2010-02-17 | 2013-07-16 | Hoffmann-La Roche Inc. | Heteroaryl substituted piperidines |
| WO2012007500A2 (de) | 2010-07-15 | 2012-01-19 | Bayer Cropscience Ag | Neue heterocyclische verbindungen als schädlingsbekämpfungsmittel |
| GB201012105D0 (en) * | 2010-07-19 | 2010-09-01 | Domainex Ltd | Novel pyrimidine compounds |
| US9376709B2 (en) | 2010-07-26 | 2016-06-28 | Biomatrica, Inc. | Compositions for stabilizing DNA and RNA in blood and other biological samples during shipping and storage at ambient temperatures |
| WO2012018639A2 (en) | 2010-07-26 | 2012-02-09 | Biomatrica, Inc. | Compositions for stabilizing dna, rna and proteins in saliva and other biological samples during shipping and storage at ambient temperatures |
| BR112013009823A2 (pt) * | 2010-10-22 | 2016-07-05 | Bayer Ip Gmbh | novos compostos heterocíclicos como pesticidas |
| US8754114B2 (en) | 2010-12-22 | 2014-06-17 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3 |
| JP6085866B2 (ja) | 2011-02-28 | 2017-03-01 | アレイ バイオファーマ、インコーポレイテッド | セリン/トレオニンキナーゼインヒビター |
| JP6147727B2 (ja) | 2011-04-01 | 2017-06-14 | ユニヴァーシティー オブ ユタ リサーチ ファウンデーション | チロシン受容体キナーゼbtk阻害剤としての置換n−(3−(ピリミジン−4−イル)フェニル)アクリルアミド類似体 |
| WO2012142329A1 (en) * | 2011-04-12 | 2012-10-18 | Myrexis, Inc. | Compositions and therapeutic uses of ikk-related kinase epsilon and tankbinding kinase 1 inhibitors |
| JP5912172B2 (ja) | 2011-04-19 | 2016-04-27 | 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Bayer Intellectual Property GmbH | 置換された4−アリール−n−フェニル−1,3,5−トリアジン−2−アミン |
| JP2014513687A (ja) | 2011-05-10 | 2014-06-05 | メルク・シャープ・アンド・ドーム・コーポレーション | Syk阻害薬としてのピリジルアミノピリジン |
| US9145391B2 (en) | 2011-05-10 | 2015-09-29 | Merck Sharp & Dohme Corp. | Bipyridylaminopyridines as Syk inhibitors |
| WO2012154519A1 (en) | 2011-05-10 | 2012-11-15 | Merck Sharp & Dohme Corp. | Aminopyrimidines as syk inhibitors |
| TWI555737B (zh) | 2011-05-24 | 2016-11-01 | 拜耳知識產權公司 | 含有硫醯亞胺基團之4-芳基-n-苯基-1,3,5-三氮雜苯-2-胺 |
| KR20140045542A (ko) * | 2011-07-12 | 2014-04-16 | 다우 아그로사이언시즈 엘엘씨 | 살충 조성물 및 그에 관한 방법 |
| JP6097289B2 (ja) | 2011-08-04 | 2017-03-15 | アレイ バイオファーマ、インコーポレイテッド | セリン/スレオニンキナーゼインヒビターとしてのキナゾリン化合物 |
| DE102011112978A1 (de) | 2011-09-09 | 2013-03-14 | Merck Patent Gmbh | Benzonitrilderivate |
| ES2587284T3 (es) | 2011-09-16 | 2016-10-21 | Bayer Intellectual Property Gmbh | 5-Fluoro-pirimidinas 2,4-disustituidas como inhibidores selectivos de CDK9 |
| CN103930399B (zh) | 2011-09-16 | 2016-03-16 | 拜耳知识产权有限责任公司 | 包含亚氨基亚磺酰基的二取代的5-氟嘧啶衍生物 |
| DK2820009T3 (en) | 2012-03-01 | 2018-04-16 | Array Biopharma Inc | Serine / threonine kinase inhibitors |
| EP3495367B1 (en) | 2012-06-13 | 2020-09-30 | Incyte Holdings Corporation | Substituted tricyclic compounds as fgfr inhibitors |
| US8809359B2 (en) | 2012-06-29 | 2014-08-19 | Ym Biosciences Australia Pty Ltd | Phenyl amino pyrimidine bicyclic compounds and uses thereof |
| WO2014026125A1 (en) | 2012-08-10 | 2014-02-13 | Incyte Corporation | Pyrazine derivatives as fgfr inhibitors |
| CA2882750A1 (en) | 2012-08-27 | 2014-03-06 | Jim Blake | Serine/threonine kinase inhibitors for the treatment of hyperproliferative|diseases |
| JP6313772B2 (ja) * | 2012-10-04 | 2018-04-18 | ユニヴァーシティー オブ ユタ リサーチ ファウンデーション | チロシン受容体キナーゼbtk阻害剤である置換n−(3−(ピリミジン−4−イル)フェニル)アクリルアミド類似体 |
| CA2887435A1 (en) | 2012-10-04 | 2014-04-10 | University Of Utah Research Foundation | Substituted n-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs as tyrosine receptor kinase btk inhibitors |
| CN104854091B (zh) | 2012-10-18 | 2018-04-03 | 拜耳药业股份公司 | 含砜基团的5‑氟‑n‑(吡啶‑2‑基)吡啶‑2‑胺衍生物 |
| HK1213890A1 (zh) | 2012-10-18 | 2016-07-15 | Bayer Pharma Aktiengesellschaft | 含碸基团的4-(邻)-氟苯基-5-氟嘧啶-2-基胺 |
| TW201418243A (zh) | 2012-11-15 | 2014-05-16 | Bayer Pharma AG | 含有磺醯亞胺基團之n-(吡啶-2-基)嘧啶-4-胺衍生物 |
| US9266892B2 (en) | 2012-12-19 | 2016-02-23 | Incyte Holdings Corporation | Fused pyrazoles as FGFR inhibitors |
| WO2014100755A2 (en) | 2012-12-20 | 2014-06-26 | Biomatrica, Inc. | Formulations and methods for stabilizing pcr reagents |
| GB201303109D0 (en) * | 2013-02-21 | 2013-04-10 | Domainex Ltd | Novel pyrimidine compounds |
| DK2986610T5 (en) | 2013-04-19 | 2018-12-10 | Incyte Holdings Corp | BICYCLIC HETEROCYCLES AS FGFR INHIBITORS |
| EP3632208A1 (en) | 2013-06-13 | 2020-04-08 | Biomatrica, INC. | Cell stabilization |
| EP3154338B1 (en) | 2014-06-10 | 2020-01-29 | Biomatrica, INC. | Stabilization of thrombocytes at ambient temperatures |
| TW202134236A (zh) | 2014-06-12 | 2021-09-16 | 美商西爾拉癌症醫學公司 | N-(氰基甲基)-4-(2-(4-𠰌啉基苯基胺基)嘧啶-4-基)苯甲醯胺 |
| CA2964683A1 (en) | 2014-10-16 | 2016-04-21 | Bayer Pharma Aktiengesellschaft | Fluorinated benzofuranyl-pyrimidine derivatives containing a sulfone group |
| US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
| WO2016134294A1 (en) | 2015-02-20 | 2016-08-25 | Incyte Corporation | Bicyclic heterocycles as fgfr4 inhibitors |
| CR20170390A (es) | 2015-02-20 | 2017-10-23 | Incyte Holdings Corp | Heterociclos biciclicos como inhibidores de fgfr |
| WO2016150902A1 (en) | 2015-03-24 | 2016-09-29 | Bayer Pharma Aktiengesellschaft | Use of 4-(4-fluoro-2-methoxyphenyl)-n-{3-[(s-methylsulfonimidoyl)methyl]phenyl}-1,3,5-triazin-2-amine for treating gastric cancers |
| CN107427520A (zh) | 2015-03-24 | 2017-12-01 | 拜耳医药股份有限公司 | 4‑(4‑氟‑2‑甲氧基苯基)‑n‑{3‑[(s‑甲基磺酰亚氨基)甲基]苯基}‑1,3,5‑三嗪‑2‑胺用于治疗淋巴瘤的用途 |
| WO2016150893A1 (en) | 2015-03-24 | 2016-09-29 | Bayer Pharma Aktiengesellschaft | Use of 4-(4-fluoro-2-methoxyphenyl)-n-{3-[(s-methylsulfonimidoyl)methyl]phenyl}-1,3,5-triazin-2-amine for treating multiple myeloma |
| US20180194769A1 (en) | 2015-07-06 | 2018-07-12 | Rodin Therapeutics, Inc. | Hetero-halo inhibitors of histone deacetylase |
| EP3319968A1 (en) | 2015-07-06 | 2018-05-16 | Rodin Therapeutics, Inc. | Heterobicyclic n-aminophenyl-amides as inhibitors of histone deacetylase |
| EP3356373B1 (en) | 2015-09-29 | 2020-02-19 | Bayer Pharma Aktiengesellschaft | Novel macrocyclic sulfondiimine compounds |
| CN108368129B (zh) | 2015-10-08 | 2021-08-17 | 拜耳医药股份有限公司 | 改性大环化合物 |
| WO2017060322A2 (en) | 2015-10-10 | 2017-04-13 | Bayer Pharma Aktiengesellschaft | Ptefb-inhibitor-adc |
| RU2695133C1 (ru) | 2015-10-12 | 2019-07-22 | Чонг Кун Данг Фармасьютикал Корп. | Производные оксадиазоламина в качестве ингибитора гистондеацетилазы 6 и содержащая их фармацевтическая композиция |
| KR102787387B1 (ko) | 2015-12-08 | 2025-03-26 | 바이오매트리카 인코포레이티드 | 적혈구 침강 속도의 감소 |
| CN110818690B (zh) | 2016-07-26 | 2021-08-10 | 深圳市塔吉瑞生物医药有限公司 | 用于抑制蛋白酪氨酸激酶活性的氨基嘧啶类化合物 |
| US20190231751A1 (en) * | 2016-09-12 | 2019-08-01 | Imago Pharmaceuticals, Inc. | Treatment of fibrotic disorders with jun n-terminal kinase inhibitors |
| JP6756925B2 (ja) | 2017-01-11 | 2020-09-16 | ロダン・セラピューティクス,インコーポレーテッド | ヒストンデアセチラーゼの二環式阻害剤 |
| WO2018152223A1 (en) * | 2017-02-15 | 2018-08-23 | University Of Massachusetts | Methods of treating angiogenesis-related disorders using jnk3 inhibitors |
| GB201702947D0 (en) | 2017-02-23 | 2017-04-12 | Domainex Ltd | Novel compounds |
| US11254690B2 (en) | 2017-03-28 | 2022-02-22 | Bayer Pharma Aktiengesellschaft | PTEFb inhibiting macrocyclic compounds |
| CA3057891A1 (en) | 2017-03-28 | 2018-10-04 | Bayer Aktiengesellschaft | Novel ptefb inhibiting macrocyclic compounds |
| GB201705263D0 (en) * | 2017-03-31 | 2017-05-17 | Probiodrug Ag | Novel inhibitors |
| AR111960A1 (es) | 2017-05-26 | 2019-09-04 | Incyte Corp | Formas cristalinas de un inhibidor de fgfr y procesos para su preparación |
| SMT202200232T1 (it) | 2017-08-07 | 2022-07-21 | Alkermes Inc | Inibitori biciclici di istone deacetilasi |
| TWI802605B (zh) * | 2017-10-17 | 2023-05-21 | 德商默克專利有限公司 | 嘧啶TBK/IKKε抑制劑化合物及其用途 |
| WO2019079373A1 (en) * | 2017-10-17 | 2019-04-25 | Merck Patent Gmbh | PYRIMIDINE TBK / IKKε INHIBITORY COMPOUNDS AND USES THEREOF |
| EP3732285A1 (en) | 2017-12-28 | 2020-11-04 | Tract Pharmaceuticals, Inc. | Stem cell culture systems for columnar epithelial stem cells, and uses related thereto |
| MA51820A (fr) | 2018-02-13 | 2021-05-19 | Bayer Ag | Utilisation de 5-fluoro-4-(4-fluoro-2-méthoxyphényl)-n-(4-[(s-méthylsulfonimidoyl)méthyl]pyridin-2-yl)pyridin-2-amine pour traiter un lymphome diffus à grandes cellules b |
| CN112566912A (zh) | 2018-05-04 | 2021-03-26 | 因赛特公司 | Fgfr抑制剂的盐 |
| US11466004B2 (en) | 2018-05-04 | 2022-10-11 | Incyte Corporation | Solid forms of an FGFR inhibitor and processes for preparing the same |
| WO2020068846A1 (en) * | 2018-09-25 | 2020-04-02 | Heterocyclic Compound | Heterocyclic compound |
| TWI850262B (zh) * | 2018-09-25 | 2024-08-01 | 美商卡都瑞恩醫藥公司 | 胺基嘧啶化合物 |
| AR117487A1 (es) * | 2018-12-21 | 2021-08-11 | Bayer Ag | 1,3,4-oxadiazoles y derivados de éstos como agentes fungicidas |
| WO2020185532A1 (en) | 2019-03-08 | 2020-09-17 | Incyte Corporation | Methods of treating cancer with an fgfr inhibitor |
| US11591329B2 (en) | 2019-07-09 | 2023-02-28 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| WO2021050700A1 (en) * | 2019-09-13 | 2021-03-18 | The Broad Institute, Inc. | Cyclooxygenase-2 inhibitors and uses thereof |
| US12122767B2 (en) | 2019-10-01 | 2024-10-22 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| GEAP202415945A (en) | 2019-10-14 | 2024-04-25 | Incyte Corp | Bicyclic heterocycles as fgfr inhibitors |
| WO2021076728A1 (en) | 2019-10-16 | 2021-04-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| BR112022010664A2 (pt) | 2019-12-04 | 2022-08-16 | Incyte Corp | Derivados de um inibidor de fgfr |
| EP4069696A1 (en) | 2019-12-04 | 2022-10-12 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| US12012409B2 (en) | 2020-01-15 | 2024-06-18 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| JP7587113B2 (ja) * | 2020-09-29 | 2024-11-20 | 日亜化学工業株式会社 | 異方性磁性粉末の製造方法および異方性磁性粉末 |
| TW202304459A (zh) | 2021-04-12 | 2023-02-01 | 美商英塞特公司 | 包含fgfr抑制劑及nectin-4靶向劑之組合療法 |
| JP2024522189A (ja) | 2021-06-09 | 2024-06-11 | インサイト・コーポレイション | Fgfr阻害剤としての三環式ヘテロ環 |
| WO2022261159A1 (en) | 2021-06-09 | 2022-12-15 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| WO2023107705A1 (en) | 2021-12-10 | 2023-06-15 | Incyte Corporation | Bicyclic amines as cdk12 inhibitors |
Family Cites Families (34)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4876252A (en) | 1986-01-13 | 1989-10-24 | American Cyanamid Company | 4,5,6-substituted-N-(substituted-phenyl)-2-pyrimidinamines |
| US4788195A (en) * | 1986-01-13 | 1988-11-29 | American Cyanamid Company | 4,5,6-substituted-N-(substituted-phenyl)-2-pyrimidinamines |
| EP0233461B2 (en) * | 1986-01-13 | 2002-05-29 | American Cyanamid Company | 4,5,6-Substituted-2-pyrimidinamines |
| US5521184A (en) * | 1992-04-03 | 1996-05-28 | Ciba-Geigy Corporation | Pyrimidine derivatives and processes for the preparation thereof |
| TW225528B (cg-RX-API-DMAC7.html) * | 1992-04-03 | 1994-06-21 | Ciba Geigy Ag | |
| DE69434721T2 (de) | 1993-10-01 | 2006-11-09 | Novartis Ag | Pharmacologisch wirksame pyrimidinderivate und verfahren zu deren herstellung |
| GB9523675D0 (en) * | 1995-11-20 | 1996-01-24 | Celltech Therapeutics Ltd | Chemical compounds |
| GB9619284D0 (en) | 1996-09-16 | 1996-10-30 | Celltech Therapeutics Ltd | Chemical compounds |
| GB9914258D0 (en) * | 1999-06-18 | 1999-08-18 | Celltech Therapeutics Ltd | Chemical compounds |
| GB9924862D0 (en) * | 1999-10-20 | 1999-12-22 | Celltech Therapeutics Ltd | Chemical compounds |
| GB0004887D0 (en) | 2000-03-01 | 2000-04-19 | Astrazeneca Uk Ltd | Chemical compounds |
| US7129242B2 (en) * | 2000-12-06 | 2006-10-31 | Signal Pharmaceuticals, Llc | Anilinopyrimidine derivatives as JNK pathway inhibitors and compositions and methods related thereto |
| ES2292753T4 (es) * | 2001-03-29 | 2009-02-16 | Vertex Pharmaceuticals Incorporated | Inhibidores de quinasas n-terminales c-jun (jnk) y otras proteina quinasas. |
| US20030176443A1 (en) * | 2001-05-16 | 2003-09-18 | Matthias Stein-Gerlach | Pyridylpyrimidine derivatives as effective compounds against prion diseases |
| GB0215676D0 (en) | 2002-07-05 | 2002-08-14 | Novartis Ag | Organic compounds |
| EP2172460A1 (en) * | 2002-11-01 | 2010-04-07 | Vertex Pharmaceuticals Incorporated | Compositions useful as inhibitors of JAK and other protein kinases |
| WO2004041814A1 (en) | 2002-11-04 | 2004-05-21 | Vertex Pharmaceuticals Incorporated | Heteroaryl-pyramidine derivatives as jak inhibitors |
| CA2507406A1 (en) * | 2002-11-05 | 2004-05-21 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of jak and other protein kinases |
| GB0308466D0 (en) | 2003-04-11 | 2003-05-21 | Novartis Ag | Organic compounds |
| EP1648875A1 (en) | 2003-07-30 | 2006-04-26 | Cyclacel Limited | 2-aminophenyl-4-phenylpyrimidines as kinase inhibitors |
| JP2008510766A (ja) * | 2004-08-27 | 2008-04-10 | ゲーペーツェー ビオテック アーゲー | ピリミジン誘導体 |
| MX2007004488A (es) * | 2004-10-13 | 2007-09-11 | Wyeth Corp | Analogos de anilino-pirimidina n-bencenosulfonilo sustituidos. |
| US20070185098A1 (en) * | 2006-01-04 | 2007-08-09 | Locus Pharmaceuticals, Inc. | Inhibitors of protein kinases |
| CA2640398A1 (en) * | 2006-01-30 | 2007-08-09 | Exelixis, Inc. | 4-aryl-2-amino-pyrimidines or 4-aryl-2-aminoalkyl-pyrimidines as jak-2 modulators and pharmaceutical compositions containing them |
| AU2007335921B2 (en) | 2006-12-18 | 2012-08-16 | Visa Cape Town (Pty) Ltd | Transaction system and method |
| EA200900799A1 (ru) | 2006-12-22 | 2009-12-30 | Новартис Аг | Гетероарилгетероарильные соединения как ингибиторы cdk, предназначенные для лечения рака, воспаления и борьбы с вирусными инфекциями |
| AT504205B1 (de) * | 2007-01-02 | 2008-04-15 | Hoermann Richard Dr | Einrichtung zur entkeimung eines fluids |
| WO2008090181A1 (en) * | 2007-01-23 | 2008-07-31 | Palau Pharma, S. A. | Purine derivatives |
| PL2152701T3 (pl) | 2007-03-12 | 2016-10-31 | Związki fenyloaminopirymidyny i ich zastosowania | |
| WO2008124085A2 (en) * | 2007-04-03 | 2008-10-16 | Exelixis, Inc. | Methods of using combinations of mek and jak-2 inhibitors |
| WO2009017838A2 (en) * | 2007-08-01 | 2009-02-05 | Exelixis, Inc. | Combinations of jak-2 inhibitors and other agents |
| EP2200436B1 (en) | 2007-09-04 | 2015-01-21 | The Scripps Research Institute | Substituted pyrimidinyl-amines as protein kinase inhibitors |
| CN102007124B (zh) * | 2008-02-15 | 2014-06-18 | 里格尔制药公司 | 嘧啶-2-胺化合物及其作为jak激酶抑制剂的用途 |
| KR101247840B1 (ko) * | 2008-02-22 | 2013-03-26 | 에프. 호프만-라 로슈 아게 | 아밀로이드 베타 조절제 |
-
2008
- 2008-09-03 EP EP08829943.3A patent/EP2200436B1/en not_active Not-in-force
- 2008-09-03 PT PT88299433T patent/PT2200436E/pt unknown
- 2008-09-03 WO PCT/US2008/075151 patent/WO2009032861A1/en not_active Ceased
- 2008-09-03 JP JP2010524122A patent/JP5611826B2/ja not_active Expired - Fee Related
- 2008-09-03 CA CA2698511A patent/CA2698511C/en not_active Expired - Fee Related
- 2008-09-03 US US12/676,411 patent/US8530480B2/en not_active Expired - Fee Related
- 2008-09-03 ES ES08829943.3T patent/ES2535166T3/es active Active
-
2013
- 2013-02-13 US US13/766,075 patent/US9018205B2/en not_active Expired - Fee Related
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2014
- 2014-09-02 JP JP2014177846A patent/JP5937648B2/ja not_active Expired - Fee Related
-
2015
- 2015-04-27 US US14/696,935 patent/US20150232429A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| EP2200436A1 (en) | 2010-06-30 |
| CA2698511C (en) | 2016-10-11 |
| US20130231336A1 (en) | 2013-09-05 |
| JP5611826B2 (ja) | 2014-10-22 |
| EP2200436B1 (en) | 2015-01-21 |
| JP5937648B2 (ja) | 2016-06-22 |
| JP2015007102A (ja) | 2015-01-15 |
| US8530480B2 (en) | 2013-09-10 |
| CA2698511A1 (en) | 2009-03-12 |
| WO2009032861A1 (en) | 2009-03-12 |
| JP2010538076A (ja) | 2010-12-09 |
| PT2200436E (pt) | 2015-04-29 |
| US20150232429A1 (en) | 2015-08-20 |
| US9018205B2 (en) | 2015-04-28 |
| EP2200436A4 (en) | 2011-12-28 |
| US20100298312A1 (en) | 2010-11-25 |
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