RU2009104340A - Производные [4,5']бипиримидинил-6,4'-диамина в качестве ингибиторов протеинкиназы - Google Patents
Производные [4,5']бипиримидинил-6,4'-диамина в качестве ингибиторов протеинкиназы Download PDFInfo
- Publication number
- RU2009104340A RU2009104340A RU2009104340/04A RU2009104340A RU2009104340A RU 2009104340 A RU2009104340 A RU 2009104340A RU 2009104340/04 A RU2009104340/04 A RU 2009104340/04A RU 2009104340 A RU2009104340 A RU 2009104340A RU 2009104340 A RU2009104340 A RU 2009104340A
- Authority
- RU
- Russia
- Prior art keywords
- bipyrimidinyl
- group
- ylamino
- pyridin
- dichloro
- Prior art date
Links
- 229940045988 antineoplastic drug protein kinase inhibitors Drugs 0.000 title 1
- 239000003909 protein kinase inhibitor Substances 0.000 title 1
- -1 pyrrolidino, piperidino, piperazino Chemical group 0.000 claims abstract 169
- 229910052739 hydrogen Inorganic materials 0.000 claims abstract 48
- 239000001257 hydrogen Substances 0.000 claims abstract 45
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims abstract 26
- 229910052799 carbon Inorganic materials 0.000 claims abstract 26
- 125000002950 monocyclic group Chemical group 0.000 claims abstract 23
- 150000001875 compounds Chemical class 0.000 claims abstract 21
- 229910052757 nitrogen Inorganic materials 0.000 claims abstract 19
- 150000002431 hydrogen Chemical group 0.000 claims abstract 18
- 125000004429 atom Chemical group 0.000 claims abstract 16
- 229910052760 oxygen Inorganic materials 0.000 claims abstract 16
- 229910052717 sulfur Inorganic materials 0.000 claims abstract 16
- 125000002619 bicyclic group Chemical group 0.000 claims abstract 14
- 125000001424 substituent group Chemical group 0.000 claims abstract 14
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims abstract 12
- 229920006395 saturated elastomer Polymers 0.000 claims abstract 12
- 229910052736 halogen Inorganic materials 0.000 claims abstract 11
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims abstract 10
- 239000000126 substance Substances 0.000 claims abstract 10
- 150000002367 halogens Chemical group 0.000 claims abstract 8
- 125000003118 aryl group Chemical group 0.000 claims abstract 5
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 claims 20
- KXDAEFPNCMNJSK-UHFFFAOYSA-N Benzamide Chemical compound NC(=O)C1=CC=CC=C1 KXDAEFPNCMNJSK-UHFFFAOYSA-N 0.000 claims 15
- 201000010099 disease Diseases 0.000 claims 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 6
- 239000000203 mixture Substances 0.000 claims 6
- SYSQUGFVNFXIIT-UHFFFAOYSA-N n-[4-(1,3-benzoxazol-2-yl)phenyl]-4-nitrobenzenesulfonamide Chemical class C1=CC([N+](=O)[O-])=CC=C1S(=O)(=O)NC1=CC=C(C=2OC3=CC=CC=C3N=2)C=C1 SYSQUGFVNFXIIT-UHFFFAOYSA-N 0.000 claims 6
- 150000003839 salts Chemical class 0.000 claims 6
- 150000001204 N-oxides Chemical class 0.000 claims 5
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 5
- 125000001064 morpholinomethyl group Chemical group [H]C([H])(*)N1C([H])([H])C([H])([H])OC([H])([H])C1([H])[H] 0.000 claims 5
- 239000012453 solvate Substances 0.000 claims 5
- 108091000080 Phosphotransferase Proteins 0.000 claims 4
- 238000000034 method Methods 0.000 claims 4
- 125000006203 morpholinoethyl group Chemical group [H]C([H])(*)C([H])([H])N1C([H])([H])C([H])([H])OC([H])([H])C1([H])[H] 0.000 claims 4
- 102000020233 phosphotransferase Human genes 0.000 claims 4
- 241001465754 Metazoa Species 0.000 claims 3
- 150000001412 amines Chemical class 0.000 claims 3
- 125000004093 cyano group Chemical group *C#N 0.000 claims 3
- 125000000753 cycloalkyl group Chemical group 0.000 claims 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 3
- 125000004307 pyrazin-2-yl group Chemical group [H]C1=C([H])N=C(*)C([H])=N1 0.000 claims 3
- 125000004527 pyrimidin-4-yl group Chemical group N1=CN=C(C=C1)* 0.000 claims 3
- 125000004066 1-hydroxyethyl group Chemical group [H]OC([H])([*])C([H])([H])[H] 0.000 claims 2
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 claims 2
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N EtOH Substances CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 2
- 101710182396 Fibroblast growth factor receptor 3 Proteins 0.000 claims 2
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 2
- ZCQWOFVYLHDMMC-UHFFFAOYSA-N Oxazole Chemical compound C1=COC=N1 ZCQWOFVYLHDMMC-UHFFFAOYSA-N 0.000 claims 2
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 claims 2
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 claims 2
- 229910052794 bromium Inorganic materials 0.000 claims 2
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 2
- 229910052801 chlorine Inorganic materials 0.000 claims 2
- 239000000460 chlorine Substances 0.000 claims 2
- 125000006264 diethylaminomethyl group Chemical group [H]C([H])([H])C([H])([H])N(C([H])([H])*)C([H])([H])C([H])([H])[H] 0.000 claims 2
- 125000006222 dimethylaminomethyl group Chemical group [H]C([H])([H])N(C([H])([H])[H])C([H])([H])* 0.000 claims 2
- 229910052731 fluorine Inorganic materials 0.000 claims 2
- 239000011737 fluorine Substances 0.000 claims 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 2
- 150000004702 methyl esters Chemical class 0.000 claims 2
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims 2
- 125000004076 pyridyl group Chemical group 0.000 claims 2
- 208000024891 symptom Diseases 0.000 claims 2
- TYOCSGNRWAHCPK-UHFFFAOYSA-N 1-[3-[[6-[4-(2,6-dichloro-3,5-dimethoxyanilino)pyrimidin-5-yl]pyrimidin-4-yl]amino]phenyl]ethanol Chemical compound COC1=CC(OC)=C(Cl)C(NC=2C(=CN=CN=2)C=2N=CN=C(NC=3C=C(C=CC=3)C(C)O)C=2)=C1Cl TYOCSGNRWAHCPK-UHFFFAOYSA-N 0.000 claims 1
- WIGBPFMLSVEBSH-UHFFFAOYSA-N 1-[3-[[6-[4-(2,6-difluoro-3,5-dimethoxyanilino)pyrimidin-5-yl]pyrimidin-4-yl]amino]phenyl]ethanol Chemical compound COC1=CC(OC)=C(F)C(NC=2C(=CN=CN=2)C=2N=CN=C(NC=3C=C(C=CC=3)C(C)O)C=2)=C1F WIGBPFMLSVEBSH-UHFFFAOYSA-N 0.000 claims 1
- FIJKNTZDZYOAGB-UHFFFAOYSA-N 1-[4-[[6-[[6-[4-(2,6-dichloro-3,5-dimethoxyanilino)pyrimidin-5-yl]pyrimidin-4-yl]amino]pyridin-3-yl]methyl]piperazin-1-yl]-2-hydroxyethanone Chemical compound COC1=CC(OC)=C(Cl)C(NC=2C(=CN=CN=2)C=2N=CN=C(NC=3N=CC(CN4CCN(CC4)C(=O)CO)=CC=3)C=2)=C1Cl FIJKNTZDZYOAGB-UHFFFAOYSA-N 0.000 claims 1
- NMMBKQUZGJYFKU-UHFFFAOYSA-N 1-[4-[[6-[[6-[4-(2,6-dichloro-3,5-dimethoxyanilino)pyrimidin-5-yl]pyrimidin-4-yl]amino]pyridin-3-yl]methyl]piperazin-1-yl]ethanone Chemical compound COC1=CC(OC)=C(Cl)C(NC=2C(=CN=CN=2)C=2N=CN=C(NC=3N=CC(CN4CCN(CC4)C(C)=O)=CC=3)C=2)=C1Cl NMMBKQUZGJYFKU-UHFFFAOYSA-N 0.000 claims 1
- PNCFUDLLXJUXSH-UHFFFAOYSA-N 1-[4-[[6-[[6-[4-(2,6-difluoro-3,5-dimethoxyanilino)pyrimidin-5-yl]pyrimidin-4-yl]amino]pyridin-3-yl]methyl]piperazin-1-yl]ethanone Chemical compound COC1=CC(OC)=C(F)C(NC=2C(=CN=CN=2)C=2N=CN=C(NC=3N=CC(CN4CCN(CC4)C(C)=O)=CC=3)C=2)=C1F PNCFUDLLXJUXSH-UHFFFAOYSA-N 0.000 claims 1
- AYJYBVQKLXRDQJ-UHFFFAOYSA-N 1-[4-[[6-[[6-[4-(2-chloro-6-fluoro-3,5-dimethoxyanilino)pyrimidin-5-yl]pyrimidin-4-yl]amino]pyridin-3-yl]methyl]piperazin-1-yl]-2-hydroxyethanone Chemical compound COC1=CC(OC)=C(Cl)C(NC=2C(=CN=CN=2)C=2N=CN=C(NC=3N=CC(CN4CCN(CC4)C(=O)CO)=CC=3)C=2)=C1F AYJYBVQKLXRDQJ-UHFFFAOYSA-N 0.000 claims 1
- GSQTWFXIKOAEQF-UHFFFAOYSA-N 1-[4-[[6-[[6-[4-(2-chloro-6-fluoro-3,5-dimethoxyanilino)pyrimidin-5-yl]pyrimidin-4-yl]amino]pyridin-3-yl]methyl]piperazin-1-yl]ethanone Chemical compound COC1=CC(OC)=C(Cl)C(NC=2C(=CN=CN=2)C=2N=CN=C(NC=3N=CC(CN4CCN(CC4)C(C)=O)=CC=3)C=2)=C1F GSQTWFXIKOAEQF-UHFFFAOYSA-N 0.000 claims 1
- LFWDKYXONJPXLV-UHFFFAOYSA-N 1-[6-[[6-[4-(2,6-dichloro-3,5-dimethoxyanilino)pyrimidin-5-yl]pyrimidin-4-yl]amino]pyridin-3-yl]ethanol Chemical compound COC1=CC(OC)=C(Cl)C(NC=2C(=CN=CN=2)C=2N=CN=C(NC=3N=CC(=CC=3)C(C)O)C=2)=C1Cl LFWDKYXONJPXLV-UHFFFAOYSA-N 0.000 claims 1
- YWENEVBVNPLSKO-UHFFFAOYSA-N 1-[6-[[6-[4-(2,6-difluoro-3,5-dimethoxyanilino)pyrimidin-5-yl]pyrimidin-4-yl]amino]pyridin-3-yl]ethanol Chemical compound COC1=CC(OC)=C(F)C(NC=2C(=CN=CN=2)C=2N=CN=C(NC=3N=CC(=CC=3)C(C)O)C=2)=C1F YWENEVBVNPLSKO-UHFFFAOYSA-N 0.000 claims 1
- STNPCJBTHDGVDG-UHFFFAOYSA-N 1-[6-[[6-[4-(2-chloro-3,5-dimethoxy-6-methylanilino)pyrimidin-5-yl]pyrimidin-4-yl]amino]pyridin-3-yl]ethanol Chemical compound COC1=CC(OC)=C(Cl)C(NC=2C(=CN=CN=2)C=2N=CN=C(NC=3N=CC(=CC=3)C(C)O)C=2)=C1C STNPCJBTHDGVDG-UHFFFAOYSA-N 0.000 claims 1
- WXASKJZNTGILEK-UHFFFAOYSA-N 1-[6-[[6-[4-(2-chloro-6-fluoro-3,5-dimethoxyanilino)pyrimidin-5-yl]pyrimidin-4-yl]amino]pyridin-3-yl]ethanol Chemical compound COC1=CC(OC)=C(Cl)C(NC=2C(=CN=CN=2)C=2N=CN=C(NC=3N=CC(=CC=3)C(C)O)C=2)=C1F WXASKJZNTGILEK-UHFFFAOYSA-N 0.000 claims 1
- MWXFVCCQBSSGDD-UHFFFAOYSA-N 2-[4-[[6-[[6-[4-(2,6-dichloro-3,5-dimethoxyanilino)pyrimidin-5-yl]pyrimidin-4-yl]amino]pyridin-3-yl]methyl]piperazin-1-yl]ethanol Chemical compound COC1=CC(OC)=C(Cl)C(NC=2C(=CN=CN=2)C=2N=CN=C(NC=3N=CC(CN4CCN(CCO)CC4)=CC=3)C=2)=C1Cl MWXFVCCQBSSGDD-UHFFFAOYSA-N 0.000 claims 1
- HBJDUPZNFBWSNF-UHFFFAOYSA-N 2-[4-[[6-[[6-[4-(2,6-difluoro-3,5-dimethoxyanilino)pyrimidin-5-yl]pyrimidin-4-yl]amino]pyridin-3-yl]methyl]piperazin-1-yl]ethanol Chemical compound COC1=CC(OC)=C(F)C(NC=2C(=CN=CN=2)C=2N=CN=C(NC=3N=CC(CN4CCN(CCO)CC4)=CC=3)C=2)=C1F HBJDUPZNFBWSNF-UHFFFAOYSA-N 0.000 claims 1
- XUPGEWMUHRNEHO-UHFFFAOYSA-N 2-[4-[[6-[[6-[4-(2-chloro-3,5-dimethoxy-6-methylanilino)pyrimidin-5-yl]pyrimidin-4-yl]amino]pyridin-3-yl]methyl]piperazin-1-yl]ethanol Chemical compound COC1=CC(OC)=C(Cl)C(NC=2C(=CN=CN=2)C=2N=CN=C(NC=3N=CC(CN4CCN(CCO)CC4)=CC=3)C=2)=C1C XUPGEWMUHRNEHO-UHFFFAOYSA-N 0.000 claims 1
- SWQLRHRBOQUCSW-UHFFFAOYSA-N 2-[4-[[6-[[6-[4-(2-chloro-6-fluoro-3,5-dimethoxyanilino)pyrimidin-5-yl]pyrimidin-4-yl]amino]pyridin-3-yl]methyl]piperazin-1-yl]ethanol Chemical compound COC1=CC(OC)=C(Cl)C(NC=2C(=CN=CN=2)C=2N=CN=C(NC=3N=CC(CN4CCN(CCO)CC4)=CC=3)C=2)=C1F SWQLRHRBOQUCSW-UHFFFAOYSA-N 0.000 claims 1
- XYIBIKYKRKQRGW-UHFFFAOYSA-N 2-[4-[[6-[[6-[4-(2-fluoro-3,5-dimethoxyanilino)pyrimidin-5-yl]pyrimidin-4-yl]amino]pyridin-3-yl]methyl]piperazin-1-yl]ethanol Chemical compound COC1=CC(OC)=CC(NC=2C(=CN=CN=2)C=2N=CN=C(NC=3N=CC(CN4CCN(CCO)CC4)=CC=3)C=2)=C1F XYIBIKYKRKQRGW-UHFFFAOYSA-N 0.000 claims 1
- 125000000872 2-diethylaminoethoxy group Chemical group [H]C([H])([H])C([H])([H])N(C([H])([H])C([H])([H])[H])C([H])([H])C([H])([H])O* 0.000 claims 1
- YUCPGZSYMDFVJE-UHFFFAOYSA-N 3-(6-aminopyrimidin-4-yl)-n-(2,6-dichlorophenyl)pyrazin-2-amine Chemical compound C1=NC(N)=CC(C=2C(=NC=CN=2)NC=2C(=CC=CC=2Cl)Cl)=N1 YUCPGZSYMDFVJE-UHFFFAOYSA-N 0.000 claims 1
- ZZGSXDHMSPQHBF-UHFFFAOYSA-N 4-[[6-[[6-[4-(2,6-dichloro-3,5-dimethoxyanilino)pyrimidin-5-yl]pyrimidin-4-yl]amino]pyridin-3-yl]methyl]piperazine-1-carboxylic acid Chemical compound ClC1=C(C(=C(C=C1OC)OC)Cl)NC1=NC=NC=C1C1=NC=NC(=C1)NC1=CC=C(C=N1)CN1CCN(CC1)C(=O)O ZZGSXDHMSPQHBF-UHFFFAOYSA-N 0.000 claims 1
- 125000004195 4-methylpiperazin-1-yl group Chemical group [H]C([H])([H])N1C([H])([H])C([H])([H])N(*)C([H])([H])C1([H])[H] 0.000 claims 1
- VHTOEAQTTZXCOA-UHFFFAOYSA-N 6-[4-(2-chloro-3,5-dimethoxy-6-methylanilino)pyrimidin-5-yl]-n-[5-(morpholin-4-ylmethyl)pyridin-2-yl]pyrimidin-4-amine Chemical compound COC1=CC(OC)=C(Cl)C(NC=2C(=CN=CN=2)C=2N=CN=C(NC=3N=CC(CN4CCOCC4)=CC=3)C=2)=C1C VHTOEAQTTZXCOA-UHFFFAOYSA-N 0.000 claims 1
- 239000005711 Benzoic acid Substances 0.000 claims 1
- 206010005003 Bladder cancer Diseases 0.000 claims 1
- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- 102100027842 Fibroblast growth factor receptor 3 Human genes 0.000 claims 1
- 208000034578 Multiple myelomas Diseases 0.000 claims 1
- 241001425800 Pipa Species 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 1
- 150000001408 amides Chemical class 0.000 claims 1
- 125000002490 anilino group Chemical group [H]N(*)C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 claims 1
- 235000010233 benzoic acid Nutrition 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- CXTQRJIXPYUUSY-UHFFFAOYSA-N n-(2,6-dichlorophenyl)-3-[6-[4-[2-(diethylamino)ethoxy]anilino]pyrimidin-4-yl]pyrazin-2-amine Chemical compound C1=CC(OCCN(CC)CC)=CC=C1NC1=CC(C=2C(=NC=CN=2)NC=2C(=CC=CC=2Cl)Cl)=NC=N1 CXTQRJIXPYUUSY-UHFFFAOYSA-N 0.000 claims 1
- RWKOJOJGEWDVNF-UHFFFAOYSA-N n-(2,6-dichlorophenyl)-3-[6-[[5-(2-morpholin-4-ylethyl)pyridin-2-yl]amino]pyrimidin-4-yl]pyrazin-2-amine Chemical compound ClC1=CC=CC(Cl)=C1NC1=NC=CN=C1C1=CC(NC=2N=CC(CCN3CCOCC3)=CC=2)=NC=N1 RWKOJOJGEWDVNF-UHFFFAOYSA-N 0.000 claims 1
- 230000007170 pathology Effects 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- OYRRZWATULMEPF-UHFFFAOYSA-N pyrimidin-4-amine Chemical compound NC1=CC=NC=N1 OYRRZWATULMEPF-UHFFFAOYSA-N 0.000 claims 1
- 125000002112 pyrrolidino group Chemical group [*]N1C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 1
- 108091008598 receptor tyrosine kinases Proteins 0.000 claims 1
- 102000027426 receptor tyrosine kinases Human genes 0.000 claims 1
- 201000005112 urinary bladder cancer Diseases 0.000 claims 1
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 0 CN(*)c1ncnc(C2=C(Nc3c(*)c(*)cc(*)c3*)N=C(*)**2)c1 Chemical compound CN(*)c1ncnc(C2=C(Nc3c(*)c(*)cc(*)c3*)N=C(*)**2)c1 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- 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
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US83049206P | 2006-07-12 | 2006-07-12 | |
| US60/830,492 | 2006-07-12 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| RU2009104340A true RU2009104340A (ru) | 2010-08-20 |
Family
ID=38617203
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
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| RU2009104340/04A RU2009104340A (ru) | 2006-07-12 | 2007-07-10 | Производные [4,5']бипиримидинил-6,4'-диамина в качестве ингибиторов протеинкиназы |
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| EP (1) | EP2044036B1 (enExample) |
| JP (1) | JP2009543798A (enExample) |
| KR (1) | KR20090029832A (enExample) |
| CN (1) | CN101511798B (enExample) |
| AR (1) | AR061867A1 (enExample) |
| AT (1) | ATE508119T1 (enExample) |
| AU (1) | AU2007272646A1 (enExample) |
| BR (1) | BRPI0714291A2 (enExample) |
| CA (1) | CA2657381A1 (enExample) |
| CL (1) | CL2007002017A1 (enExample) |
| DE (1) | DE602007014374D1 (enExample) |
| ES (1) | ES2367666T3 (enExample) |
| MX (1) | MX2009000429A (enExample) |
| PE (1) | PE20080548A1 (enExample) |
| PL (1) | PL2044036T3 (enExample) |
| PT (1) | PT2044036E (enExample) |
| RU (1) | RU2009104340A (enExample) |
| TW (1) | TW200811134A (enExample) |
| UY (1) | UY30477A1 (enExample) |
| WO (1) | WO2008008747A1 (enExample) |
Families Citing this family (49)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8131527B1 (en) | 2006-12-22 | 2012-03-06 | Astex Therapeutics Ltd. | FGFR pharmacophore compounds |
| CN101679409B (zh) | 2006-12-22 | 2014-11-26 | Astex治疗学有限公司 | 双环杂环衍生化合物、其医药组合物和其用途 |
| AU2007337886C1 (en) | 2006-12-22 | 2014-10-16 | Astex Therapeutics Limited | Bicyclic heterocyclic compounds as FGFR inhibitors |
| GB0720041D0 (en) | 2007-10-12 | 2007-11-21 | Astex Therapeutics Ltd | New Compounds |
| GB0720038D0 (en) | 2007-10-12 | 2007-11-21 | Astex Therapeutics Ltd | New compounds |
| GB0810902D0 (en) | 2008-06-13 | 2008-07-23 | Astex Therapeutics Ltd | New compounds |
| GB0906470D0 (en) | 2009-04-15 | 2009-05-20 | Astex Therapeutics Ltd | New compounds |
| GB0906472D0 (en) | 2009-04-15 | 2009-05-20 | Astex Therapeutics Ltd | New compounds |
| EP2308866A1 (de) | 2009-10-09 | 2011-04-13 | Bayer CropScience AG | Phenylpyri(mi)dinylpyrazole und ihre Verwendung als Fungizide |
| CN102762551A (zh) | 2009-12-21 | 2012-10-31 | 拜尔农作物科学股份公司 | 噻吩基吡(嘧)啶基吡唑及其用于防治植物致病菌的用途 |
| WO2012088266A2 (en) | 2010-12-22 | 2012-06-28 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3 |
| AR086992A1 (es) | 2011-06-20 | 2014-02-05 | Bayer Ip Gmbh | Tienilpiri(mi)dinilpirazoles |
| EP2763987B1 (en) | 2011-10-06 | 2018-07-18 | Bayer CropScience AG | Heterocyclylpyri(mi)dinylpyrazole as fungicidals |
| PL2763993T3 (pl) | 2011-10-06 | 2017-09-29 | Bayer Intellectual Property Gmbh | Heterocyklilopiry(mi)dynylopirazol |
| IN2014KN02601A (enExample) | 2012-04-24 | 2015-05-08 | Vertex Pharma | |
| SI2861595T1 (sl) | 2012-06-13 | 2017-04-26 | Incyte Holdings Corporation | Substituirane triciklične spojine kot inhibitorji fgfr |
| US9388185B2 (en) | 2012-08-10 | 2016-07-12 | Incyte Holdings Corporation | Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors |
| EP2902489B9 (en) * | 2012-09-27 | 2018-02-07 | Chugai Seiyaku Kabushiki Kaisha | Fgfr3 fusion gene and pharmaceutical drug targeting same |
| US9266892B2 (en) | 2012-12-19 | 2016-02-23 | Incyte Holdings Corporation | Fused pyrazoles as FGFR inhibitors |
| AR094812A1 (es) | 2013-02-20 | 2015-08-26 | Eisai R&D Man Co Ltd | Derivado de piridina monocíclico como inhibidor del fgfr |
| SMT201900107T1 (it) | 2013-03-12 | 2019-02-28 | Vertex Pharma | Inibitori della dna-pk |
| LT2986610T (lt) | 2013-04-19 | 2018-04-10 | Incyte Holdings Corporation | Bicikliniai heterociklai, kaip fgfr inhibitoriai |
| PL3424920T3 (pl) | 2013-10-17 | 2020-11-16 | Vertex Pharmaceuticals Incorporated | Kokryształy (S)-N-metylo-8-(1-((2'-metylo-4’,6'-dideutero-[4,5'-bipirymidyn]-6-ylo)amino)propan-2-ylo)chinolino-4-karboksyamidu i ich deuterowane pochodne jako inhibitory DNA-PK |
| MX369646B (es) | 2014-08-18 | 2019-11-15 | Eisai R&D Man Co Ltd | Sal de derivado de piridina monociclico y su cristal. |
| US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| SG10201913036RA (en) | 2015-02-20 | 2020-02-27 | Incyte Corp | Bicyclic heterocycles as fgfr 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 |
| WO2016152907A1 (ja) | 2015-03-25 | 2016-09-29 | 国立研究開発法人国立がん研究センター | 胆管癌治療剤 |
| CN108367000A (zh) | 2015-12-17 | 2018-08-03 | 卫材R&D管理有限公司 | 用于乳腺癌的治疗剂 |
| MX394860B (es) | 2016-09-27 | 2025-03-24 | Vertex Pharma | Metodo para tratar cancer usando una combinacion de agentes que dañan adn e inhibidores de proteina cinasa dependiente de adn (adn-pk). |
| AR111960A1 (es) | 2017-05-26 | 2019-09-04 | Incyte Corp | Formas cristalinas de un inhibidor de fgfr y procesos para su preparación |
| KR102613433B1 (ko) * | 2017-10-11 | 2023-12-13 | 주식회사 대웅제약 | 신규한 페닐피리딘 유도체 및 이를 포함하는 약학 조성물 |
| WO2019189241A1 (ja) | 2018-03-28 | 2019-10-03 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | 肝細胞癌治療剤 |
| KR20210018264A (ko) | 2018-05-04 | 2021-02-17 | 인사이트 코포레이션 | Fgfr 억제제의 염 |
| PL3788047T3 (pl) | 2018-05-04 | 2025-04-14 | Incyte Corporation | Stałe postacie inhibitora fgfr i sposoby ich otrzymywania |
| WO2020185532A1 (en) | 2019-03-08 | 2020-09-17 | Incyte Corporation | Methods of treating cancer with an fgfr inhibitor |
| KR102133595B1 (ko) | 2019-05-31 | 2020-07-13 | 에이치케이이노엔 주식회사 | 단백질 키나제 억제제로서의 헤테로고리 화합물 |
| US11591329B2 (en) | 2019-07-09 | 2023-02-28 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| KR102112336B1 (ko) | 2019-08-12 | 2020-05-18 | 에이치케이이노엔 주식회사 | 단백질 키나제 억제제로서의 헤테로고리 화합물 |
| WO2021067374A1 (en) | 2019-10-01 | 2021-04-08 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| CR20220169A (es) | 2019-10-14 | 2022-10-27 | Incyte Corp | Heterociclos bicíclicos como inhibidores de fgfr |
| US11566028B2 (en) | 2019-10-16 | 2023-01-31 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| JP7720840B2 (ja) | 2019-12-04 | 2025-08-08 | インサイト・コーポレイション | Ｆｇｆｒ阻害剤としての三環式複素環 |
| AU2020395185A1 (en) | 2019-12-04 | 2022-06-02 | Incyte Corporation | Derivatives of an FGFR inhibitor |
| WO2021146424A1 (en) | 2020-01-15 | 2021-07-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| 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 |
| EP4352060A1 (en) | 2021-06-09 | 2024-04-17 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| US11939331B2 (en) | 2021-06-09 | 2024-03-26 | Incyte Corporation | Tricyclic heterocycles as FGFR inhibitors |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9924862D0 (en) | 1999-10-20 | 1999-12-22 | Celltech Therapeutics Ltd | Chemical compounds |
| MXPA05012281A (es) | 2003-05-14 | 2006-05-19 | Torreypines Therapeutics Inc | Compuestos y uso de los mismos en la modulacion beta amiloide. |
| EP1670771A4 (en) | 2003-09-30 | 2010-09-01 | Irm Llc | COMPOUNDS AND COMPOSITIONS INHIBITING PROTEIN-KINASES |
| CA2564355C (en) | 2004-05-07 | 2012-07-03 | Amgen Inc. | Protein kinase modulators and method of use |
| WO2007092531A2 (en) | 2006-02-06 | 2007-08-16 | Irm Llc | Compounds and compositions as protein kinase inhibitors |
-
2007
- 2007-07-04 TW TW096124311A patent/TW200811134A/zh unknown
- 2007-07-10 RU RU2009104340/04A patent/RU2009104340A/ru not_active Application Discontinuation
- 2007-07-10 KR KR1020097002815A patent/KR20090029832A/ko not_active Withdrawn
- 2007-07-10 EP EP07812739A patent/EP2044036B1/en not_active Not-in-force
- 2007-07-10 DE DE602007014374T patent/DE602007014374D1/de active Active
- 2007-07-10 CA CA002657381A patent/CA2657381A1/en not_active Abandoned
- 2007-07-10 AU AU2007272646A patent/AU2007272646A1/en not_active Abandoned
- 2007-07-10 MX MX2009000429A patent/MX2009000429A/es not_active Application Discontinuation
- 2007-07-10 PT PT07812739T patent/PT2044036E/pt unknown
- 2007-07-10 PE PE2007000885A patent/PE20080548A1/es not_active Application Discontinuation
- 2007-07-10 AR ARP070103061A patent/AR061867A1/es unknown
- 2007-07-10 BR BRPI0714291-9A2A patent/BRPI0714291A2/pt not_active Application Discontinuation
- 2007-07-10 WO PCT/US2007/073111 patent/WO2008008747A1/en not_active Ceased
- 2007-07-10 PL PL07812739T patent/PL2044036T3/pl unknown
- 2007-07-10 JP JP2009519623A patent/JP2009543798A/ja active Pending
- 2007-07-10 US US12/373,441 patent/US8026243B2/en not_active Expired - Fee Related
- 2007-07-10 ES ES07812739T patent/ES2367666T3/es active Active
- 2007-07-10 AT AT07812739T patent/ATE508119T1/de active
- 2007-07-10 CN CN2007800337140A patent/CN101511798B/zh not_active Expired - Fee Related
- 2007-07-11 UY UY30477A patent/UY30477A1/es not_active Application Discontinuation
- 2007-07-11 CL CL200702017A patent/CL2007002017A1/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CN101511798A (zh) | 2009-08-19 |
| PL2044036T3 (pl) | 2011-09-30 |
| TW200811134A (en) | 2008-03-01 |
| EP2044036A1 (en) | 2009-04-08 |
| UY30477A1 (es) | 2009-04-30 |
| BRPI0714291A2 (pt) | 2014-10-21 |
| JP2009543798A (ja) | 2009-12-10 |
| ATE508119T1 (de) | 2011-05-15 |
| EP2044036B1 (en) | 2011-05-04 |
| PE20080548A1 (es) | 2008-06-24 |
| CN101511798B (zh) | 2011-11-02 |
| CA2657381A1 (en) | 2008-01-17 |
| PT2044036E (pt) | 2011-08-23 |
| ES2367666T3 (es) | 2011-11-07 |
| AR061867A1 (es) | 2008-09-24 |
| KR20090029832A (ko) | 2009-03-23 |
| DE602007014374D1 (de) | 2011-06-16 |
| MX2009000429A (es) | 2009-01-29 |
| AU2007272646A1 (en) | 2008-01-17 |
| WO2008008747A1 (en) | 2008-01-17 |
| CL2007002017A1 (es) | 2008-06-13 |
| US8026243B2 (en) | 2011-09-27 |
| US20100234376A1 (en) | 2010-09-16 |
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| Date | Code | Title | Description |
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| FA93 | Acknowledgement of application withdrawn (no request for examination) |
Effective date: 20110301 |