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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| Application Number | Title | Priority Date | Filing Date |
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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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| Country | Link |
|---|---|
| US (3) | US8530480B2 (show.php) |
| EP (1) | EP2200436B1 (show.php) |
| JP (2) | JP5611826B2 (show.php) |
| CA (1) | CA2698511C (show.php) |
| ES (1) | ES2535166T3 (show.php) |
| PT (1) | PT2200436E (show.php) |
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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 |
| MX2009009792A (es) * | 2007-03-12 | 2009-09-23 | Cytopia Res Pty Ltd | Compuestos de fenil amino pirimidina y usos de los mismos. |
| AU2016200866B2 (en) * | 2007-03-12 | 2017-06-22 | Glaxosmithkline Llc | Phenyl amino pyrimidine compounds and uses thereof |
| AU2013201306B2 (en) * | 2007-03-12 | 2015-11-12 | Glaxosmithkline Llc | Phenyl Amino Pyrimidine Compounds and Uses Thereof |
| US8507511B2 (en) * | 2007-04-24 | 2013-08-13 | Ingenium Pharmaceuticals Gmbh | Inhibitors of protein kinases |
| CA2698511C (en) | 2007-09-04 | 2016-10-11 | The Scripps Research Institute | Substituted pyrimidinyl-amines as protein kinase inhibitors |
| WO2009087127A1 (en) | 2008-01-11 | 2009-07-16 | F. Hoffmann-La Roche Ag | Modulators for amyloid beta |
| JP5328816B2 (ja) * | 2008-02-22 | 2013-10-30 | エフ.ホフマン−ラ ロシュ アーゲー | アミロイドβの調節薬 |
| MX2011003246A (es) | 2008-10-09 | 2011-04-21 | Hoffmann La Roche | Moduladores de beta amiloide. |
| WO2010052199A1 (en) | 2008-11-10 | 2010-05-14 | F. Hoffmann-La Roche Ag | Heterocyclic gamma secretase modulators |
| NZ599826A (en) * | 2009-10-12 | 2014-08-29 | Myrexis Inc | Amino-pyrimidine compounds as inhibitors of ikk epsilon and/or tbk1 |
| EP2513098B1 (en) | 2009-12-17 | 2016-11-09 | Merck Sharp & Dohme Corp. | Aminopyrimidines as syk inhibitors |
| EP2512246B1 (en) | 2009-12-17 | 2015-09-30 | Merck Sharp & Dohme Corp. | Aminopyrimidines as syk inhibitors |
| US8486967B2 (en) | 2010-02-17 | 2013-07-16 | Hoffmann-La Roche Inc. | Heteroaryl substituted piperidines |
| BR112013000925A2 (pt) | 2010-07-15 | 2020-12-01 | Bayer Intellectual Property Gmbh | compostos heterocíclicos como pesticidas |
| GB201012105D0 (en) * | 2010-07-19 | 2010-09-01 | Domainex Ltd | Novel pyrimidine compounds |
| EP2598661B1 (en) | 2010-07-26 | 2017-09-27 | Biomatrica, INC. | Compositions for stabilizing dna, rna and proteins in saliva and other biological samples during shipping and storage at ambient temperatures |
| CA2806670A1 (en) | 2010-07-26 | 2012-02-09 | Biomatrica, Inc. | Compositions for stabilizing dna, rna and proteins in blood and other biological samples during shipping and storage at ambient temperatures |
| EP2630133A1 (de) | 2010-10-22 | 2013-08-28 | Bayer Intellectual Property GmbH | Neue heterocylische verbindungen als schädlingsbekämpfungsmittel |
| US8754114B2 (en) | 2010-12-22 | 2014-06-17 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3 |
| US9133187B2 (en) | 2011-02-28 | 2015-09-15 | Array Biopharma Inc. | Serine/threonine kinase inhibitors |
| US8703767B2 (en) | 2011-04-01 | 2014-04-22 | University Of Utah Research Foundation | Substituted N-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs as tyrosine receptor kinase BTK inhibitors |
| EP2696683A4 (en) * | 2011-04-12 | 2014-08-13 | Alzheimer S Inst Of America Inc | COMPOSITIONS AND THERAPEUTIC APPLICATIONS OF IKK-MEDIATED KINASE EPSILON AND TANK BINDING KINASE-1 HEMMER |
| ES2613103T3 (es) | 2011-04-19 | 2017-05-22 | Bayer Intellectual Property Gmbh | 4-Aril-n-fenil-1,3,5-triacin-2-aminas sustituidas |
| KR20140028062A (ko) | 2011-05-10 | 2014-03-07 | 머크 샤프 앤드 돔 코포레이션 | Syk 억제제로서의 아미노피리미딘 |
| EP2707357B1 (en) | 2011-05-10 | 2017-01-18 | Merck Sharp & Dohme Corp. | Pyridyl aminopyridines as syk inhibitors |
| US9145391B2 (en) | 2011-05-10 | 2015-09-29 | Merck Sharp & Dohme Corp. | Bipyridylaminopyridines 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 |
| US20130019348A1 (en) * | 2011-07-12 | 2013-01-17 | Dow Agrosciences Llc | Pesticidal compositions and processes related thereto |
| WO2013020062A1 (en) | 2011-08-04 | 2013-02-07 | Array Biopharma Inc. | Quinazoline compounds as serine/threonine kinase inhibitors |
| DE102011112978A1 (de) * | 2011-09-09 | 2013-03-14 | Merck Patent Gmbh | Benzonitrilderivate |
| 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 |
| CA2848616A1 (en) | 2011-09-16 | 2013-03-21 | Bayer Intellectual Property Gmbh | Disubstituted 5-fluoro-pyrimidines |
| DK3321262T3 (da) | 2012-03-01 | 2021-01-25 | Array Biopharma Inc | Serin-/threoninkinasehæmmere |
| PH12019502809B1 (en) | 2012-06-13 | 2024-04-24 | Incyte Holdings Corp | 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 |
| MX369989B (es) | 2012-08-27 | 2019-11-27 | Array Biopharma Inc | Inhibidores de serina/treonina cinasa para el tratamiento de enfermedades hiperproliferativas. |
| EP2903971B1 (en) * | 2012-10-04 | 2019-06-12 | University Of Utah Research Foundation | Substituted n-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs as tyrosine receptor kinase btk inhibitors |
| 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 |
| EP2909183B1 (en) | 2012-10-18 | 2016-08-24 | Bayer Pharma Aktiengesellschaft | 4-(ortho)-fluorophenyl-5-fluoropyrimidin-2-yl amines containing a sulfone group |
| ES2595222T3 (es) | 2012-10-18 | 2016-12-28 | Bayer Pharma Aktiengesellschaft | Derivados de 5-fluoro-N-(piridin-2-il)piridin-2-amina que contienen un grupo sulfona |
| 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 |
| EP3249054A1 (en) | 2012-12-20 | 2017-11-29 | Biomatrica, INC. | Formulations and methods for stabilizing pcr reagents |
| GB201303109D0 (en) * | 2013-02-21 | 2013-04-10 | Domainex Ltd | Novel pyrimidine compounds |
| MY181497A (en) | 2013-04-19 | 2020-12-23 | Incyte Holdings Corp | Bicyclic heterocycles as fgfr inhibitors |
| EP3007556B1 (en) | 2013-06-13 | 2020-05-20 | Biomatrica, INC. | Cell stabilization |
| JP6661554B2 (ja) | 2014-06-10 | 2020-03-11 | バイオマトリカ,インク. | 周囲温度における血小板の安定化 |
| TWI729644B (zh) | 2014-06-12 | 2021-06-01 | 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 |
| CN107207475A (zh) | 2014-10-16 | 2017-09-26 | 拜耳医药股份有限公司 | 含有砜基团的氟化苯并呋喃基‑嘧啶衍生物 |
| 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 |
| PE20171514A1 (es) | 2015-02-20 | 2017-10-20 | Incyte Corp | Heterociclos biciclicos como inhibidores de fgfr |
| WO2016134294A1 (en) | 2015-02-20 | 2016-08-25 | Incyte Corporation | Bicyclic heterocycles as fgfr4 inhibitors |
| 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 |
| CA2980507A1 (en) | 2015-03-24 | 2016-09-29 | Public University Corporation Nagoya City University | Use of 4-(4-fluoro-2-methoxyphenyl)-n-{3-[(s-methylsulfonimidoyl)methyl]phenyl}-1,3,5-triazin-2-amine for treating lymphomas |
| US20180078560A1 (en) | 2015-03-24 | 2018-03-22 | 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 |
| US10421756B2 (en) | 2015-07-06 | 2019-09-24 | Rodin Therapeutics, Inc. | Heterobicyclic N-aminophenyl-amides as inhibitors of histone deacetylase |
| PT3319959T (pt) | 2015-07-06 | 2021-12-06 | Alkermes Inc | Inibidores hetero-halo de histona desacetilase |
| ES2786552T3 (es) | 2015-09-29 | 2020-10-13 | Bayer Pharma AG | Compuestos de sulfondiimina macrocíclicos nuevos |
| ES2819869T3 (es) | 2015-10-08 | 2021-04-19 | Bayer Pharma AG | Nuevos compuestos macrocíclicos modificados |
| 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 |
| CN113588501B (zh) | 2015-12-08 | 2024-12-17 | 生物马特里卡公司 | 降低红细胞沉降速率 |
| WO2018019204A1 (zh) * | 2016-07-26 | 2018-02-01 | 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 |
| EP3509586A4 (en) * | 2016-09-12 | 2020-05-06 | Imago Pharmaceuticals, Inc. | TREATMENT OF FIBROTIC DISORDERS WITH JUN N-TERMINAL KINASE INHIBITORS |
| KR102526032B1 (ko) | 2017-01-11 | 2023-04-25 | 로딘 테라퓨틱스, 인크. | 히스톤 데아세틸라제의 바이시클릭 억제제 |
| US20190381125A1 (en) * | 2017-02-15 | 2019-12-19 | University Of Massachusetts | Methods of Treating Angiogenesis-Related Disorders Using JNK3 Inhibitors |
| GB201702947D0 (en) | 2017-02-23 | 2017-04-12 | Domainex Ltd | Novel compounds |
| CA3057891A1 (en) | 2017-03-28 | 2018-10-04 | Bayer Aktiengesellschaft | Novel ptefb inhibiting macrocyclic compounds |
| CA3057892A1 (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 |
| DK3664802T3 (en) | 2017-08-07 | 2022-05-30 | Alkermes Inc | Bicyclic inhibitors of histone deacetylase |
| EP3697773A1 (en) * | 2017-10-17 | 2020-08-26 | Merck Patent GmbH | PYRIMIDINE TBK/IKKe INHIBITOR COMPOUNDS AND USES THEREOF |
| CA3078579A1 (en) * | 2017-10-17 | 2019-04-25 | Merck Patent Gmbh | Pyrimidine tbk/ikk.epsilon. inhibitor compounds and uses thereof |
| WO2019133810A1 (en) | 2017-12-28 | 2019-07-04 | Tract Pharmaceuticals, Inc. | Stem cell culture systems for columnar epithelial stem cells, and uses related thereto |
| SG11202006470RA (en) | 2018-02-13 | 2020-08-28 | Bayer Ag | Use of 5-fluoro-4-(4-fluoro-2-methoxyphenyl)-n-{4-[(s-methylsulfonimidoyl)methyl]pyridin-2-yl}pyridin-2-amine for treating diffuse large b-cell lymphoma |
| JP7568512B2 (ja) | 2018-05-04 | 2024-10-16 | インサイト・コーポレイション | Fgfr阻害剤の塩 |
| CN112867716B (zh) | 2018-05-04 | 2024-09-13 | 因赛特公司 | Fgfr抑制剂的固体形式和其制备方法 |
| KR20210082454A (ko) * | 2018-09-25 | 2021-07-05 | 카듀리온 파마슈티칼스, 인크. | 아미노피리미딘 화합물 |
| WO2020068846A1 (en) * | 2018-09-25 | 2020-04-02 | Heterocyclic Compound | Heterocyclic compound |
| CA3124324A1 (en) * | 2018-12-21 | 2020-06-25 | Bayer Aktiengesellschaft | 1,3,4-oxadiazoles and their derivatives as new antifungal agents |
| WO2020185532A1 (en) | 2019-03-08 | 2020-09-17 | Incyte Corporation | Methods of treating cancer with an fgfr inhibitor |
| WO2021007269A1 (en) | 2019-07-09 | 2021-01-14 | 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 |
| WO2021067374A1 (en) | 2019-10-01 | 2021-04-08 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| US11607416B2 (en) | 2019-10-14 | 2023-03-21 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| US11566028B2 (en) | 2019-10-16 | 2023-01-31 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| WO2021113462A1 (en) | 2019-12-04 | 2021-06-10 | Incyte Corporation | Derivatives of an fgfr inhibitor |
| US11897891B2 (en) | 2019-12-04 | 2024-02-13 | Incyte Corporation | Tricyclic heterocycles as FGFR inhibitors |
| WO2021146424A1 (en) | 2020-01-15 | 2021-07-22 | 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 |
| CA3215903A1 (en) | 2021-04-12 | 2022-10-20 | Incyte Corporation | Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent |
| US11939331B2 (en) | 2021-06-09 | 2024-03-26 | Incyte Corporation | Tricyclic heterocycles as FGFR inhibitors |
| JP2024522188A (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 |
| US12084453B2 (en) | 2021-12-10 | 2024-09-10 | Incyte Corporation | Bicyclic amines as CDK12 inhibitors |
Family Cites Families (34)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0233461B2 (en) * | 1986-01-13 | 2002-05-29 | American Cyanamid Company | 4,5,6-Substituted-2-pyrimidinamines |
| 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 |
| TW225528B (show.php) * | 1992-04-03 | 1994-06-21 | Ciba Geigy Ag | |
| US5521184A (en) | 1992-04-03 | 1996-05-28 | Ciba-Geigy Corporation | Pyrimidine derivatives and processes for the preparation thereof |
| JP3588116B2 (ja) * | 1993-10-01 | 2004-11-10 | ノバルティス アクチェンゲゼルシャフト | 薬理活性のピリミジンアミン誘導体およびその製造方法 |
| 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 |
| CA2441733A1 (en) * | 2001-03-29 | 2002-10-10 | Vertex Pharmaceuticals Incorporated | Inhibitors of c-jun n-terminal kinases (jnk) and other protein kinases |
| CA2446939C (en) * | 2001-05-16 | 2005-08-02 | Matthias Stein-Gerlach | Pyridylpyrimidine derivatives as effective compounds against prion diseases |
| GB0215676D0 (en) * | 2002-07-05 | 2002-08-14 | Novartis Ag | Organic compounds |
| JP2006512314A (ja) * | 2002-11-01 | 2006-04-13 | バーテックス ファーマシューティカルズ インコーポレイテッド | Jakインヒビターおよび他のプロテインキナーゼインヒビターとしての組成物の使用 |
| WO2004041814A1 (en) | 2002-11-04 | 2004-05-21 | Vertex Pharmaceuticals Incorporated | Heteroaryl-pyramidine derivatives as jak inhibitors |
| US7348335B2 (en) | 2002-11-05 | 2008-03-25 | Vertex Pharmaceuticals Incorporated | Compositions useful as inhibitors of JAK and other protein kinases |
| GB0308466D0 (en) * | 2003-04-11 | 2003-05-21 | Novartis Ag | Organic compounds |
| WO2005012262A1 (en) | 2003-07-30 | 2005-02-10 | 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 |
| GT200500286A (es) * | 2004-10-13 | 2006-06-13 | Analogos de anilino-pirimidina | |
| EP1973408A2 (en) * | 2006-01-04 | 2008-10-01 | Locus Pharmaceuticals, Inc. | Inhibitors of protein kinases |
| KR20080110998A (ko) * | 2006-01-30 | 2008-12-22 | 엑셀리시스, 인코포레이티드 | Jak2 조절자로서 4아릴2아미노피리미딘 또는 4아릴2아미노알킬피리미딘 및 이들을 포함하는 약제학적 조성물 |
| AU2007335921B2 (en) | 2006-12-18 | 2012-08-16 | Visa Cape Town (Pty) Ltd | Transaction system and method |
| KR20090091306A (ko) | 2006-12-22 | 2009-08-27 | 노파르티스 아게 | 암, 염증 및 바이러스 감염 치료용 cdk 억제제로서의 헤테로아릴-헤테로아릴 화합물 |
| AT504205B1 (de) * | 2007-01-02 | 2008-04-15 | Hoermann Richard Dr | Einrichtung zur entkeimung eines fluids |
| BRPI0806811A2 (pt) * | 2007-01-23 | 2011-09-13 | Palau Pharma Sa | derivados de purina |
| MX2009009792A (es) * | 2007-03-12 | 2009-09-23 | Cytopia Res Pty Ltd | Compuestos de fenil amino pirimidina y usos de los mismos. |
| 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 |
| CA2698511C (en) | 2007-09-04 | 2016-10-11 | The Scripps Research Institute | Substituted pyrimidinyl-amines as protein kinase inhibitors |
| CA2715658C (en) * | 2008-02-15 | 2016-07-19 | Rigel Pharmaceuticals, Inc. | Pyrimidine-2-amine compounds and their use as inhibitors of jak kinases |
| JP5328816B2 (ja) * | 2008-02-22 | 2013-10-30 | エフ.ホフマン−ラ ロシュ アーゲー | アミロイドβの調節薬 |
-
2008
- 2008-09-03 CA CA2698511A patent/CA2698511C/en not_active Expired - Fee Related
- 2008-09-03 WO PCT/US2008/075151 patent/WO2009032861A1/en not_active Ceased
- 2008-09-03 EP EP08829943.3A patent/EP2200436B1/en not_active Not-in-force
- 2008-09-03 ES ES08829943.3T patent/ES2535166T3/es active Active
- 2008-09-03 JP JP2010524122A patent/JP5611826B2/ja not_active Expired - Fee Related
- 2008-09-03 US US12/676,411 patent/US8530480B2/en not_active Expired - Fee Related
- 2008-09-03 PT PT88299433T patent/PT2200436E/pt unknown
-
2013
- 2013-02-13 US US13/766,075 patent/US9018205B2/en not_active Expired - Fee Related
-
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 |
|---|---|
| US20150232429A1 (en) | 2015-08-20 |
| EP2200436B1 (en) | 2015-01-21 |
| PT2200436E (pt) | 2015-04-29 |
| JP5611826B2 (ja) | 2014-10-22 |
| CA2698511C (en) | 2016-10-11 |
| CA2698511A1 (en) | 2009-03-12 |
| JP2015007102A (ja) | 2015-01-15 |
| WO2009032861A1 (en) | 2009-03-12 |
| JP5937648B2 (ja) | 2016-06-22 |
| EP2200436A1 (en) | 2010-06-30 |
| JP2010538076A (ja) | 2010-12-09 |
| US9018205B2 (en) | 2015-04-28 |
| US20100298312A1 (en) | 2010-11-25 |
| US20130231336A1 (en) | 2013-09-05 |
| EP2200436A4 (en) | 2011-12-28 |
| US8530480B2 (en) | 2013-09-10 |
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