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
- Authority
- ES
- Spain
- Prior art keywords
- phenyl
- substituted
- pyrimidin
- ring
- acetamide
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Active
Links
- -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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- 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
-
- 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
- A61P37/02—Immunomodulators
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- 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
-
- 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
- C07D403/02—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
- 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
-
- 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
- C07D403/14—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 three or more hetero rings
-
- 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
- C07D413/02—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
-
- 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
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Diabetes (AREA)
- Obesity (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Immunology (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Hospice & Palliative Care (AREA)
- Urology & Nephrology (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Vascular Medicine (AREA)
- Psychology (AREA)
- Communicable Diseases (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| 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 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2535166T3 true ES2535166T3 (es) | 2015-05-06 |
Family
ID=40429327
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES08829943.3T Active ES2535166T3 (es) | 2007-09-04 | 2008-09-03 | Pirimidinil-aminas sustituidas como inhibidores de proteína-quinasas |
Country Status (7)
| Country | Link |
|---|---|
| US (3) | US8530480B2 (en:Method) |
| EP (1) | EP2200436B1 (en:Method) |
| JP (2) | JP5611826B2 (en:Method) |
| CA (1) | CA2698511C (en:Method) |
| ES (1) | ES2535166T3 (en:Method) |
| PT (1) | PT2200436E (en:Method) |
| WO (1) | WO2009032861A1 (en:Method) |
Families Citing this family (98)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX2009006454A (es) | 2006-12-22 | 2009-06-26 | Hoffmann La Roche | Derivados de espiro-piperidina. |
| AU2016200866B2 (en) * | 2007-03-12 | 2017-06-22 | Glaxosmithkline Llc | Phenyl amino pyrimidine compounds and uses thereof |
| KR101737753B1 (ko) * | 2007-03-12 | 2017-05-18 | 와이엠 바이오사이언시즈 오스트레일리아 피티와이 엘티디 | 페닐 아미노 피리미딘 화합물 및 이의 용도 |
| 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 |
| ES2535166T3 (es) | 2007-09-04 | 2015-05-06 | The Scripps Research Institute | Pirimidinil-aminas sustituidas como inhibidores de proteína-quinasas |
| ATE535515T1 (de) | 2008-01-11 | 2011-12-15 | Hoffmann La Roche | Modulatoren für amyloid beta |
| EP2257541B1 (en) * | 2008-02-22 | 2013-08-14 | F. Hoffmann-La Roche AG | Modulators for amyloid beta |
| MX2011003246A (es) | 2008-10-09 | 2011-04-21 | Hoffmann La Roche | Moduladores de beta amiloide. |
| EP2355817A1 (en) | 2008-11-10 | 2011-08-17 | F. Hoffmann-La Roche AG | Heterocyclic gamma secretase modulators |
| KR20120114224A (ko) * | 2009-10-12 | 2012-10-16 | 마이렉시스 인코포레이티드 | Ｉｋｋ 엡실론 및/또는 ｔｂｋ１의 억제제로서의 아미노-피리미딘 화합물 |
| CN102858767B (zh) | 2009-12-17 | 2015-08-19 | 默沙东公司 | 作为syk抑制剂的氨基嘧啶 |
| WO2011075560A1 (en) | 2009-12-17 | 2011-06-23 | Merck Sharp & Dohme Corp. | Aminopyrimidines as syk inhibitors |
| US8486967B2 (en) | 2010-02-17 | 2013-07-16 | Hoffmann-La Roche Inc. | Heteroaryl substituted piperidines |
| ES2603032T3 (es) | 2010-07-15 | 2017-02-23 | Bayer Intellectual Property Gmbh | Compuestos de 3-piridil-heteroarilcarboxamida como pesticidas |
| GB201012105D0 (en) | 2010-07-19 | 2010-09-01 | Domainex Ltd | Novel pyrimidine compounds |
| EP2598660B1 (en) | 2010-07-26 | 2017-03-15 | Biomatrica, INC. | Compositions for stabilizing dna, rna and proteins in blood and other biological samples during shipping and storage at ambient temperatures |
| CA2806734A1 (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 |
| WO2012052412A1 (de) | 2010-10-22 | 2012-04-26 | Bayer Cropscience Ag | Neue heterocylische verbindungen als schädlingsbekämpfungsmittel |
| WO2012088266A2 (en) | 2010-12-22 | 2012-06-28 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3 |
| CA2828478C (en) | 2011-02-28 | 2019-12-31 | 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 |
| CN103732067A (zh) * | 2011-04-12 | 2014-04-16 | 美国阿尔茨海默病研究所公司 | 化合物，组合物及它们的治疗用途 |
| WO2012143399A1 (en) | 2011-04-19 | 2012-10-26 | Bayer Intellectual Property Gmbh | Substituted 4-aryl-n-phenyl-1,3,5-triazin-2-amines |
| WO2012154518A1 (en) | 2011-05-10 | 2012-11-15 | Merck Sharp & Dohme Corp. | Bipyridylaminopyridines as syk inhibitors |
| KR20140028062A (ko) | 2011-05-10 | 2014-03-07 | 머크 샤프 앤드 돔 코포레이션 | Syk 억제제로서의 아미노피리미딘 |
| WO2012154520A1 (en) | 2011-05-10 | 2012-11-15 | Merck Sharp & Dohme Corp. | Pyridyl aminopyridines 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 |
| BR112014002675A2 (pt) | 2011-08-04 | 2017-02-21 | Array Biopharma Inc | "quinazolina como inibidores de serina/treonina quinase, seus usos, e composição" |
| 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 |
| EP2755948B1 (en) | 2011-09-16 | 2016-05-25 | Bayer Intellectual Property GmbH | Disubstituted 5-fluoro pyrimidine derivatives containing a sulfoximine group |
| ES2857649T3 (es) | 2012-03-01 | 2021-09-29 | Array Biopharma Inc | Inhibidores de serina/treonina cinasa |
| SI2861595T1 (sl) | 2012-06-13 | 2017-04-26 | Incyte Holdings Corporation | Substituirane triciklične spojine kot inhibitorji fgfr |
| US8809359B2 (en) | 2012-06-29 | 2014-08-19 | Ym Biosciences Australia Pty Ltd | Phenyl amino pyrimidine bicyclic compounds and uses thereof |
| US9388185B2 (en) | 2012-08-10 | 2016-07-12 | Incyte Holdings Corporation | Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors |
| JP6378182B2 (ja) | 2012-08-27 | 2018-08-22 | アレイ バイオファーマ、インコーポレイテッド | 過剰増殖性│疾患の処置のためのセリン／スレオニンキナーゼ阻害剤 |
| US9296703B2 (en) | 2012-10-04 | 2016-03-29 | University Of Utah Research Foundation | Substituted N-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs as tyrosine receptor kinase BTK inhibitors |
| US9828376B2 (en) | 2012-10-04 | 2017-11-28 | University Of Utah Research Foundation | Substituted N-(3-pyrimidin-4-yl)phenyl)acrylamide analogs as tyrosine receptor kinase BTK inhibitors |
| CA2888371C (en) | 2012-10-18 | 2021-06-08 | Ulrich Lucking | 5-fluoro-n-(pyridin-2-yl)pyridin-2-amine derivatives containing a sulfone group |
| US20150259300A1 (en) | 2012-10-18 | 2015-09-17 | Bayer Pharma Aktiengesellschaft | 4-(ortho)-fluorophenyl-5-fluoropyrimidin-2-yl amines containing a sulfone group |
| 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 |
| ES2657451T3 (es) | 2013-04-19 | 2018-03-05 | Incyte Holdings Corporation | Heterocíclicos bicíclicos como inhibidores del FGFR |
| US20160135446A1 (en) | 2013-06-13 | 2016-05-19 | Biomatrica, Inc. | Cell stabilization |
| ES2891555T3 (es) | 2014-06-10 | 2022-01-28 | Biomatrica Inc | Estabilización de trombocitos a temperaturas ambiente |
| TWI681954B (zh) | 2014-06-12 | 2020-01-11 | 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 |
| CA2976790C (en) | 2015-02-20 | 2024-02-27 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| WO2016134294A1 (en) | 2015-02-20 | 2016-08-25 | Incyte Corporation | Bicyclic heterocycles as fgfr4 inhibitors |
| 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 |
| CN107428707A (zh) | 2015-03-24 | 2017-12-01 | 拜耳制药股份公司 | 4‑(4‑氟‑2‑甲氧基苯基)‑n‑{3‑[(s‑甲基亚磺酰亚胺基)甲基]苯基}‑1,3,5‑三嗪‑2‑胺用于治疗多发性骨髓瘤的用途 |
| 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 |
| WO2017007756A1 (en) | 2015-07-06 | 2017-01-12 | 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 |
| WO2017055196A1 (en) | 2015-09-29 | 2017-04-06 | Bayer Pharma Aktiengesellschaft | Novel macrocyclic sulfondiimine compounds |
| 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 |
| FI3362445T3 (fi) | 2015-10-12 | 2023-03-21 | Chong Kun Dang Pharmaceutical Corp | Oksadiatsoliamiinijohdannaisyhdisteitä histonideasetylaasi 6:n inhibiittoreina ja niitä käsittävä farmaseuttinen koostumus |
| KR20250047404A (ko) | 2015-12-08 | 2025-04-03 | 바이오매트리카 인코포레이티드 | 적혈구 침강 속도의 감소 |
| 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 |
| WO2018132531A1 (en) | 2017-01-11 | 2018-07-19 | Rodin Therapeutics, Inc. | Bicyclic inhibitors of histone deacetylase |
| 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 |
| WO2018177899A1 (en) | 2017-03-28 | 2018-10-04 | Bayer Aktiengesellschaft | Novel ptefb inhibiting macrocyclic compounds |
| US11242356B2 (en) | 2017-03-28 | 2022-02-08 | Bayer Aktiengesellschaft | 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 |
| CA3071861A1 (en) | 2017-08-07 | 2019-02-14 | Rodin Therapeutics, Inc. | Bicyclic inhibitors of histone deacetylase |
| BR112020007549A2 (pt) * | 2017-10-17 | 2020-09-24 | Merck Patent Gmbh | compostos inibidores de pirimidina tbk/ikképsilon e uso dos mesmos |
| KR20200072519A (ko) * | 2017-10-17 | 2020-06-22 | 메르크 파텐트 게엠베하 | 피리미딘 TBK/IKKε 억제제 화합물 및 이의 용도 |
| JP7416716B2 (ja) | 2017-12-28 | 2024-01-17 | トラクト ファーマシューティカルズ インコーポレイテッド | 円柱上皮幹細胞のための幹細胞培養系およびそれに関連した使用法 |
| CA3090843A1 (en) | 2018-02-13 | 2019-08-22 | Bayer Aktiengesellschaft | 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 |
| KR20210018265A (ko) | 2018-05-04 | 2021-02-17 | 인사이트 코포레이션 | Fgfr 억제제의 고체 형태 및 이의 제조 방법 |
| MX2020011639A (es) | 2018-05-04 | 2021-02-15 | Incyte Corp | Sales de un inhibidor de receptores de factor de crecimiento de fibroblastos (fgfr). |
| WO2020068846A1 (en) * | 2018-09-25 | 2020-04-02 | Heterocyclic Compound | Heterocyclic compound |
| IL281765B2 (en) * | 2018-09-25 | 2024-04-01 | Cardurion Pharmaceuticals Inc | Aminopyrimidine compound |
| CN113473860A (zh) * | 2018-12-21 | 2021-10-01 | 拜耳公司 | 作为新的抗真菌剂的1，3，4-噁二唑及其衍生物 |
| 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 |
| US20220348590A1 (en) * | 2019-09-13 | 2022-11-03 | The Board Institute, Inc. | Cyclooxygenase-2 inhibitors and uses thereof |
| WO2021067374A1 (en) | 2019-10-01 | 2021-04-08 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| JP7675711B2 (ja) | 2019-10-14 | 2025-05-13 | インサイト・コーポレイション | Ｆｇｆｒ阻害剤としての二環式複素環 |
| WO2021076728A1 (en) | 2019-10-16 | 2021-04-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| WO2021113479A1 (en) | 2019-12-04 | 2021-06-10 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| CR20220285A (es) | 2019-12-04 | 2022-10-27 | Incyte Corp | Derivados de un inhibidor de fgfr |
| 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 |
| JP2024513575A (ja) | 2021-04-12 | 2024-03-26 | インサイト・コーポレイション | Ｆｇｆｒ阻害剤及びネクチン－４標的化剤を含む併用療法 |
| AR126102A1 (es) | 2021-06-09 | 2023-09-13 | Incyte Corp | Heterociclos tricíclicos como inhibidores de fgfr |
| EP4352060A1 (en) | 2021-06-09 | 2024-04-17 | 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 |
|---|---|---|---|---|
| US4788195A (en) * | 1986-01-13 | 1988-11-29 | American Cyanamid Company | 4,5,6-substituted-N-(substituted-phenyl)-2-pyrimidinamines |
| US4876252A (en) | 1986-01-13 | 1989-10-24 | 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 |
| TW225528B (en:Method) | 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 |
| AU693114B2 (en) * | 1993-10-01 | 1998-06-25 | Novartis Ag | Pharmacologically active pyrimidineamine derivatives and processes for the preparation thereof |
| 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 |
| WO2002079197A1 (en) * | 2001-03-29 | 2002-10-10 | Vertex Pharmaceuticals Incorporated | Inhibitors of c-jun n-terminal kinases (jnk) and other protein kinases |
| 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 |
| DE60330895D1 (de) * | 2002-11-01 | 2010-02-25 | Vertex Pharma | Verbindungen, die sich als inhibitoren vonjak und anderen proteinkinasen eignen |
| AU2003295396B2 (en) * | 2002-11-04 | 2009-02-26 | Vertex Pharmaceuticals Incorporated | Heteroaryl-pyramidine derivatives as JAK inhibitors |
| JP2006508107A (ja) * | 2002-11-05 | 2006-03-09 | 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および他のプロテインキナーゼのインヒビターとして有用な化合物 |
| GB0308466D0 (en) | 2003-04-11 | 2003-05-21 | Novartis Ag | Organic compounds |
| CA2533474A1 (en) | 2003-07-30 | 2005-02-10 | Shudong Wang | 2-aminophenyl-4-phenylpyrimidines as kinase inhibitors |
| US20080187575A1 (en) | 2004-08-27 | 2008-08-07 | Bert Klebl | Pyrimidine Derivatives |
| JP2008515986A (ja) * | 2004-10-13 | 2008-05-15 | ワイス | Ｎ−ベンゼンスルホニル置換アニリノ−ピリミジン類似物 |
| CA2635888A1 (en) | 2006-01-04 | 2007-07-19 | Locus Pharmaceuticals, Inc. | Inhibitors of protein kinases |
| US8440663B2 (en) * | 2006-01-30 | 2013-05-14 | Exelixis, Inc. | 4-aryl-2-amino-pyrimidines or 4-aryl-2-aminoalkyl-pyrimidines as JAK-2 modulators and methods of use |
| BRPI0720359A2 (pt) | 2006-12-18 | 2013-12-24 | Fundamo Proprietary Ltd | Sistema de transação, e, método para selecionar uma transação alvo a ser conduzida em um sistema de transação. |
| JP2010514689A (ja) * | 2006-12-22 | 2010-05-06 | ノバルティス アーゲー | 癌、炎症およびウイルス感染症の処置のためのｃｄｋ阻害剤としてのヘテロアリール−ヘテロアリール化合物 |
| AT504205B1 (de) * | 2007-01-02 | 2008-04-15 | Hoermann Richard Dr | Einrichtung zur entkeimung eines fluids |
| JP2010526027A (ja) * | 2007-01-23 | 2010-07-29 | パラウ・フアルマ・ソシエダツド・アノニマ | プリン誘導体 |
| KR101737753B1 (ko) | 2007-03-12 | 2017-05-18 | 와이엠 바이오사이언시즈 오스트레일리아 피티와이 엘티디 | 페닐 아미노 피리미딘 화합물 및 이의 용도 |
| 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 |
| ES2535166T3 (es) | 2007-09-04 | 2015-05-06 | The Scripps Research Institute | Pirimidinil-aminas sustituidas como inhibidores de proteína-quinasas |
| CA2715658C (en) * | 2008-02-15 | 2016-07-19 | Rigel Pharmaceuticals, Inc. | Pyrimidine-2-amine compounds and their use as inhibitors of jak kinases |
| EP2257541B1 (en) * | 2008-02-22 | 2013-08-14 | F. Hoffmann-La Roche AG | Modulators for amyloid beta |
-
2008
- 2008-09-03 ES ES08829943.3T patent/ES2535166T3/es active Active
- 2008-09-03 WO PCT/US2008/075151 patent/WO2009032861A1/en not_active Ceased
- 2008-09-03 PT PT88299433T patent/PT2200436E/pt unknown
- 2008-09-03 CA CA2698511A patent/CA2698511C/en not_active Expired - Fee Related
- 2008-09-03 JP JP2010524122A patent/JP5611826B2/ja not_active Expired - Fee Related
- 2008-09-03 EP EP08829943.3A patent/EP2200436B1/en not_active Not-in-force
- 2008-09-03 US US12/676,411 patent/US8530480B2/en not_active Expired - Fee Related
-
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 |
|---|---|
| US8530480B2 (en) | 2013-09-10 |
| EP2200436A1 (en) | 2010-06-30 |
| JP2010538076A (ja) | 2010-12-09 |
| US20130231336A1 (en) | 2013-09-05 |
| EP2200436A4 (en) | 2011-12-28 |
| US9018205B2 (en) | 2015-04-28 |
| WO2009032861A1 (en) | 2009-03-12 |
| JP5937648B2 (ja) | 2016-06-22 |
| US20150232429A1 (en) | 2015-08-20 |
| JP5611826B2 (ja) | 2014-10-22 |
| EP2200436B1 (en) | 2015-01-21 |
| CA2698511C (en) | 2016-10-11 |
| US20100298312A1 (en) | 2010-11-25 |
| JP2015007102A (ja) | 2015-01-15 |
| CA2698511A1 (en) | 2009-03-12 |
| PT2200436E (pt) | 2015-04-29 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| ES2535166T3 (es) | Pirimidinil-aminas sustituidas como inhibidores de proteína-quinasas | |
| KR101671341B1 (ko) | 다이아미노피리미딘 유도체 및 그의 제조방법 | |
| ES2389203T3 (es) | Inhibidores de quinasa selectivos | |
| JP2010538076A5 (en:Method) | ||
| ES2333824T3 (es) | Derivados de piridinilo y pirimidinilo sustituidos como moduladores del metabolismo y el tratamiento de trastornos relacionados con el mismo. | |
| RU2373209C2 (ru) | Пирролотриазиновые соединения как ингибиторы киназ | |
| CN101341138B (zh) | 作为gsk-3抑制剂的环状苯胺基-吡啶并三嗪类 | |
| ES2344484T3 (es) | Derivados de piperazinilo utiles en el tratamiento de enfermedades mediadas por el receptor gpr38. | |
| CN104844566B (zh) | 一种新型结构的激酶抑制剂 | |
| CN101735197B (zh) | 一种伊马替尼的合成方法 | |
| CA2690953A1 (en) | Benzimidazole derivatives | |
| RU2013130925A (ru) | Оксимовые соединения в качестве средств для повышения уровня холестерина высокой плотности | |
| KR20120114355A (ko) | 화합물 및 방법 | |
| IL276946B (en) | Antiproliferative compounds and methods of use | |
| RS56424B1 (sr) | Piridin-2-amidi korisni kao cb2-agonisti | |
| JP2010526056A (ja) | イマチニブの製造方法 | |
| AR073920A1 (es) | Derivados urea de nortropanos sustituidos, medicamentos que contienen dichos compuestos , su uso en el tratamiento de enfermedades mediadas por la inhibicion de la enzima 11beta-hidroxiesteroide deshidrogenasa y proceso para su preparacion. | |
| CN1820001A (zh) | 经取代的杂环二芳基胺类似物 | |
| JP2017530199A5 (en:Method) | ||
| JP2011526913A5 (ja) | キナゾリン化合物及び同化合物を含む治療薬 | |
| JP2007519695A5 (en:Method) | ||
| CN1777591A (zh) | 具有喹唑二酮骨架的苯丙氨酸衍生物的制造方法及制造中间体 | |
| HRP20120069T1 (hr) | Derivati 5,6-bisaril-2-piridinkarboksamida, njihovo dobivanje i njihova upotreba u terapiji kao antagonista receptora urotenzina ii | |
| JP2013505262A (ja) | ｍＧｌｕＲ５ネガティブアロステリックモジュレータとしての置換ヘテロアリールアミンカルボキサミド類似体、ならびに、その形成方法および使用方法 | |
| JP2007527909A5 (en:Method) |