JP2011523646A5 - - Google Patents
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- JP2011523646A5 JP2011523646A5 JP2011510716A JP2011510716A JP2011523646A5 JP 2011523646 A5 JP2011523646 A5 JP 2011523646A5 JP 2011510716 A JP2011510716 A JP 2011510716A JP 2011510716 A JP2011510716 A JP 2011510716A JP 2011523646 A5 JP2011523646 A5 JP 2011523646A5
- Authority
- JP
- Japan
- Prior art keywords
- phenyl
- dimethylphosphoryl
- diamine
- pyrimidine
- propan
- 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.)
- Withdrawn
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- YDAVHAXYLYWAID-UHFFFAOYSA-N 2-(4-dimethylphosphoryl-2-methoxyanilino)-9-(2-propan-2-ylsulfonylphenyl)-7h-purin-8-one Chemical compound COC1=CC(P(C)(C)=O)=CC=C1NC1=NC=C(NC(=O)N2C=3C(=CC=CC=3)S(=O)(=O)C(C)C)C2=N1 YDAVHAXYLYWAID-UHFFFAOYSA-N 0.000 claims description 2
- -1 cycloalkynyl Chemical group 0.000 claims 135
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 86
- YAAWASYJIRZXSZ-UHFFFAOYSA-N pyrimidine-2,4-diamine Chemical compound NC1=CC=NC(N)=N1 YAAWASYJIRZXSZ-UHFFFAOYSA-N 0.000 claims 22
- 150000001875 compounds Chemical class 0.000 claims 19
- 125000003118 aryl group Chemical group 0.000 claims 8
- 125000001424 substituent group Chemical group 0.000 claims 8
- 125000001072 heteroaryl group Chemical group 0.000 claims 7
- 229920006395 saturated elastomer Polymers 0.000 claims 7
- 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 6
- 125000000304 alkynyl group Chemical group 0.000 claims 5
- 125000000753 cycloalkyl group Chemical group 0.000 claims 5
- 125000000623 heterocyclic group Chemical group 0.000 claims 5
- 229910052760 oxygen Inorganic materials 0.000 claims 5
- RCACQAFABUTZRJ-UHFFFAOYSA-N pyridazine-3,5-diamine Chemical compound NC1=CN=NC(N)=C1 RCACQAFABUTZRJ-UHFFFAOYSA-N 0.000 claims 5
- 125000003342 alkenyl group Chemical group 0.000 claims 4
- 125000000217 alkyl group Chemical group 0.000 claims 4
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 4
- 229910052736 halogen Inorganic materials 0.000 claims 4
- 150000002367 halogens Chemical class 0.000 claims 4
- 125000005842 heteroatom Chemical group 0.000 claims 4
- 229910052717 sulfur Inorganic materials 0.000 claims 4
- 125000004429 atom Chemical group 0.000 claims 3
- 125000004122 cyclic group Chemical group 0.000 claims 3
- 125000004404 heteroalkyl group Chemical group 0.000 claims 3
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 3
- YGIKNSYRWWYNEM-UHFFFAOYSA-N 2-[2-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl]-1H-pyrimidine-2,4-diamine Chemical compound COC1=CC(N2CCC(CC2)N2CCN(C)CC2)=CC=C1C1(N)NC=CC(N)=N1 YGIKNSYRWWYNEM-UHFFFAOYSA-N 0.000 claims 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 2
- MISVBCMQSJUHMH-UHFFFAOYSA-N pyrimidine-4,6-diamine Chemical compound NC1=CC(N)=NC=N1 MISVBCMQSJUHMH-UHFFFAOYSA-N 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 1
- 125000006656 (C2-C4) alkenyl group Chemical group 0.000 claims 1
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 1
- KZKRRZFCAYOXQE-UHFFFAOYSA-N 1$l^{2}-azinane Chemical compound C1CC[N]CC1 KZKRRZFCAYOXQE-UHFFFAOYSA-N 0.000 claims 1
- IFFLKGMDBKQMAH-UHFFFAOYSA-N 2,4-diaminopyridine Chemical compound NC1=CC=NC(N)=C1 IFFLKGMDBKQMAH-UHFFFAOYSA-N 0.000 claims 1
- YDBJMVUFWQVJEL-UHFFFAOYSA-N 2-(5-dimethylphosphoryl-3-methoxypyrazin-2-yl)-4-(4-phenylpiperazin-1-yl)-5-(trifluoromethyl)pyrimidine Chemical compound COC1=NC(P(C)(C)=O)=CN=C1C1=NC=C(C(F)(F)F)C(N2CCN(CC2)C=2C=CC=CC=2)=N1 YDBJMVUFWQVJEL-UHFFFAOYSA-N 0.000 claims 1
- BGBHYRPFLNTBAO-UHFFFAOYSA-N 2-(5-dimethylphosphoryl-3-methoxypyrazin-2-yl)-n-[2-(1h-indol-3-yl)ethyl]-5-(trifluoromethyl)pyrimidin-4-amine Chemical compound COC1=NC(P(C)(C)=O)=CN=C1C1=NC=C(C(F)(F)F)C(NCCC=2C3=CC=CC=C3NC=2)=N1 BGBHYRPFLNTBAO-UHFFFAOYSA-N 0.000 claims 1
- WRHIFUZIDNNVMH-UHFFFAOYSA-N 2-(5-propan-2-yl-1,3-oxazol-2-yl)-1H-pyrimidine-2,4-diamine Chemical compound CC(C)C1=CN=C(O1)C1(NC=CC(=N1)N)N WRHIFUZIDNNVMH-UHFFFAOYSA-N 0.000 claims 1
- WEISXGQSRWIEMR-UHFFFAOYSA-N 2-(thiophen-2-ylmethyl)-1H-pyrimidine-2,4-diamine Chemical compound S1C(=CC=C1)CC1(NC=CC(=N1)N)N WEISXGQSRWIEMR-UHFFFAOYSA-N 0.000 claims 1
- UUBLRQJKXKPVSH-UHFFFAOYSA-N 2-[(2-morpholin-4-yl-1,3-thiazol-4-yl)methyl]-1H-pyrimidine-2,4-diamine Chemical compound N1(CCOCC1)C=1SC=C(N1)CC1(NC=CC(=N1)N)N UUBLRQJKXKPVSH-UHFFFAOYSA-N 0.000 claims 1
- AURWNYDIEJODIW-UHFFFAOYSA-N 2-n-(3,3a,4,5,6,6a-hexahydro-1h-cyclopenta[c]pyrrol-2-yl)-4-n-(4-dimethylphosphorylphenyl)-1,3,5-triazine-2,4-diamine Chemical compound C1=CC(P(C)(=O)C)=CC=C1NC1=NC=NC(NN2CC3CCCC3C2)=N1 AURWNYDIEJODIW-UHFFFAOYSA-N 0.000 claims 1
- DZZXTFLOJAOWJC-UHFFFAOYSA-N 2-n-(4-dimethylphosphorylphenyl)-4-n-(morpholin-4-ylmethyl)-1,3,5-triazine-2,4-diamine Chemical compound C1=CC(P(C)(=O)C)=CC=C1NC1=NC=NC(NCN2CCOCC2)=N1 DZZXTFLOJAOWJC-UHFFFAOYSA-N 0.000 claims 1
- VHSCAKCTESVCRJ-UHFFFAOYSA-N 2-n-(4-dimethylphosphorylphenyl)-4-n-[2-(1h-indol-3-yl)ethyl]-1,3,5-triazine-2,4-diamine Chemical compound C1=CC(P(C)(=O)C)=CC=C1NC1=NC=NC(NCCC=2C3=CC=CC=C3NC=2)=N1 VHSCAKCTESVCRJ-UHFFFAOYSA-N 0.000 claims 1
- CACQSUQIEIZYKF-UHFFFAOYSA-N 4-[2-[[2-(4-dimethylphosphorylanilino)-5-(trifluoromethyl)pyrimidin-4-yl]amino]ethyl]benzenesulfonamide Chemical compound C1=CC(P(C)(=O)C)=CC=C1NC1=NC=C(C(F)(F)F)C(NCCC=2C=CC(=CC=2)S(N)(=O)=O)=N1 CACQSUQIEIZYKF-UHFFFAOYSA-N 0.000 claims 1
- KKTJDNRADACNKT-UHFFFAOYSA-N 4-[2-[[4-(4-dimethylphosphorylanilino)-1,3,5-triazin-2-yl]amino]ethyl]benzenesulfonamide Chemical compound C1=CC(P(C)(=O)C)=CC=C1NC1=NC=NC(NCCC=2C=CC(=CC=2)S(N)(=O)=O)=N1 KKTJDNRADACNKT-UHFFFAOYSA-N 0.000 claims 1
- XNNVQIKTGVDUSF-UHFFFAOYSA-N 4-[2-[[6-(4-dimethylphosphorylanilino)pyrimidin-4-yl]amino]ethyl]benzenesulfonamide Chemical compound C1=CC(P(C)(=O)C)=CC=C1NC1=CC(NCCC=2C=CC(=CC=2)S(N)(=O)=O)=NC=N1 XNNVQIKTGVDUSF-UHFFFAOYSA-N 0.000 claims 1
- 125000004176 4-fluorobenzyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1F)C([H])([H])* 0.000 claims 1
- RMCDEJJESDZIOW-UHFFFAOYSA-N 4-n-(3,3a,4,5,6,6a-hexahydro-1h-cyclopenta[c]pyrrol-2-yl)-6-n-(4-dimethylphosphorylphenyl)pyrimidine-4,6-diamine Chemical compound C1=CC(P(C)(=O)C)=CC=C1NC1=CC(NN2CC3CCCC3C2)=NC=N1 RMCDEJJESDZIOW-UHFFFAOYSA-N 0.000 claims 1
- JRHYRONVMAWIRB-UHFFFAOYSA-N 4-n-(3,5-dimethylphenyl)-6-n-(4-dimethylphosphorylphenyl)pyrimidine-4,6-diamine Chemical compound CC1=CC(C)=CC(NC=2N=CN=C(NC=3C=CC(=CC=3)P(C)(C)=O)C=2)=C1 JRHYRONVMAWIRB-UHFFFAOYSA-N 0.000 claims 1
- SVZPEWYYMRMFPS-UHFFFAOYSA-N 4-n-(4-dimethylphosphoryl-2-methoxyphenyl)-6-n-(2-propan-2-ylsulfonylphenyl)pyrimidine-4,6-diamine Chemical compound COC1=CC(P(C)(C)=O)=CC=C1NC1=CC(NC=2C(=CC=CC=2)S(=O)(=O)C(C)C)=NC=N1 SVZPEWYYMRMFPS-UHFFFAOYSA-N 0.000 claims 1
- DMENRRRTQGARSY-UHFFFAOYSA-N 4-n-(4-dimethylphosphorylphenyl)-2-n-(4-methylpiperazin-1-yl)-1,3,5-triazine-2,4-diamine Chemical compound C1CN(C)CCN1NC1=NC=NC(NC=2C=CC(=CC=2)P(C)(C)=O)=N1 DMENRRRTQGARSY-UHFFFAOYSA-N 0.000 claims 1
- ACNSRGATKOKXAW-UHFFFAOYSA-N 4-n-(4-dimethylphosphorylphenyl)-2-n-(oxolan-2-yl)-1,3,5-triazine-2,4-diamine Chemical compound C1=CC(P(C)(=O)C)=CC=C1NC1=NC=NC(NC2OCCC2)=N1 ACNSRGATKOKXAW-UHFFFAOYSA-N 0.000 claims 1
- RLYZTKYVVBRBGZ-UHFFFAOYSA-N 4-n-(4-dimethylphosphorylphenyl)-2-n-morpholin-4-yl-1,3,5-triazine-2,4-diamine Chemical compound C1=CC(P(C)(=O)C)=CC=C1NC1=NC=NC(NN2CCOCC2)=N1 RLYZTKYVVBRBGZ-UHFFFAOYSA-N 0.000 claims 1
- ALYOLUKRZAIEKP-UHFFFAOYSA-N 4-n-(4-dimethylphosphorylphenyl)-6-n-(morpholin-4-ylmethyl)pyrimidine-4,6-diamine Chemical compound C1=CC(P(C)(=O)C)=CC=C1NC1=CC(NCN2CCOCC2)=NC=N1 ALYOLUKRZAIEKP-UHFFFAOYSA-N 0.000 claims 1
- TXSHSISKPHJMBD-UHFFFAOYSA-N 4-n-(4-dimethylphosphorylphenyl)-6-n-[2-(1h-indol-3-yl)ethyl]pyrimidine-4,6-diamine Chemical compound C1=CC(P(C)(=O)C)=CC=C1NC1=CC(NCCC=2C3=CC=CC=C3NC=2)=NC=N1 TXSHSISKPHJMBD-UHFFFAOYSA-N 0.000 claims 1
- SYSUPKMNBPBNLM-UHFFFAOYSA-N 4-n-(4-dimethylphosphorylphenyl)-6-n-[[4-(4-methylpiperazin-1-yl)phenyl]methyl]pyrimidine-4,6-diamine Chemical compound C1CN(C)CCN1C(C=C1)=CC=C1CNC1=CC(NC=2C=CC(=CC=2)P(C)(C)=O)=NC=N1 SYSUPKMNBPBNLM-UHFFFAOYSA-N 0.000 claims 1
- VHRWLEQZUWRUIS-UHFFFAOYSA-N 4-n-(5-dimethylphosphoryl-3-methoxypyrazin-2-yl)-6-n-(2-propan-2-ylsulfonylphenyl)pyrimidine-4,6-diamine Chemical compound COC1=NC(P(C)(C)=O)=CN=C1NC1=CC(NC=2C(=CC=CC=2)S(=O)(=O)C(C)C)=NC=N1 VHRWLEQZUWRUIS-UHFFFAOYSA-N 0.000 claims 1
- UJMKWGFPESJWKK-UHFFFAOYSA-N 4-n-(6-dimethylphosphoryl-2-methoxypyridin-3-yl)-6-n-(2-propan-2-ylsulfonylphenyl)pyrimidine-4,6-diamine Chemical compound COC1=NC(P(C)(C)=O)=CC=C1NC1=CC(NC=2C(=CC=CC=2)S(=O)(=O)C(C)C)=NC=N1 UJMKWGFPESJWKK-UHFFFAOYSA-N 0.000 claims 1
- YSXBPUICETXSIN-UHFFFAOYSA-N 4-n-[2-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl]-2-methyl-6-n-(2-propan-2-ylsulfonylphenyl)pyrimidine-4,6-diamine Chemical compound COC1=CC(N2CCC(CC2)N2CCN(C)CC2)=CC=C1NC(N=C(C)N=1)=CC=1NC1=CC=CC=C1S(=O)(=O)C(C)C YSXBPUICETXSIN-UHFFFAOYSA-N 0.000 claims 1
- APPMBZWLLMLIRZ-UHFFFAOYSA-N 5-chloro-n-(6-dimethylphosphoryl-2-methoxypyridin-3-yl)-4-(4-methylpiperazin-1-yl)pyrimidin-2-amine Chemical compound COC1=NC(P(C)(C)=O)=CC=C1NC1=NC=C(Cl)C(N2CCN(C)CC2)=N1 APPMBZWLLMLIRZ-UHFFFAOYSA-N 0.000 claims 1
- GXKHHTFACFLICY-UHFFFAOYSA-N 6-chloro-2-n-(3,5-dimethylphenyl)-4-n-(4-dimethylphosphorylphenyl)-1,3,5-triazine-2,4-diamine Chemical compound CC1=CC(C)=CC(NC=2N=C(NC=3C=CC(=CC=3)P(C)(C)=O)N=C(Cl)N=2)=C1 GXKHHTFACFLICY-UHFFFAOYSA-N 0.000 claims 1
- TZEGVLDYESDWHZ-UHFFFAOYSA-N 6-chloro-2-n-(4-dimethylphosphorylphenyl)-4-n-[[4-(4-methylpiperazin-1-yl)phenyl]methyl]-1,3,5-triazine-2,4-diamine Chemical compound C1CN(C)CCN1C(C=C1)=CC=C1CNC1=NC(Cl)=NC(NC=2C=CC(=CC=2)P(C)(C)=O)=N1 TZEGVLDYESDWHZ-UHFFFAOYSA-N 0.000 claims 1
- ARXUDORRPLTCIG-UHFFFAOYSA-N 6-chloro-n-(4-dimethylphosphoryl-2-methoxyphenyl)-5-[3-fluoro-5-(trifluoromethyl)phenyl]sulfanyl-1,2,4-triazin-3-amine Chemical class COC1=CC(P(C)(C)=O)=CC=C1NC1=NN=C(Cl)C(SC=2C=C(C=C(F)C=2)C(F)(F)F)=N1 ARXUDORRPLTCIG-UHFFFAOYSA-N 0.000 claims 1
- NXEDAGXYLRKKJG-UHFFFAOYSA-N 6-n-(4-dimethylphosphorylphenyl)-4-n-(4-methylpiperazin-1-yl)pyrimidine-4,6-diamine Chemical compound C1CN(C)CCN1NC1=CC(NC=2C=CC(=CC=2)P(C)(C)=O)=NC=N1 NXEDAGXYLRKKJG-UHFFFAOYSA-N 0.000 claims 1
- LAFRLNVCGTZNKL-UHFFFAOYSA-N 6-n-(4-dimethylphosphorylphenyl)-4-n-(oxolan-2-yl)pyrimidine-4,6-diamine Chemical compound C1=CC(P(C)(=O)C)=CC=C1NC1=CC(NC2OCCC2)=NC=N1 LAFRLNVCGTZNKL-UHFFFAOYSA-N 0.000 claims 1
- WWZYCYIMGPENLW-UHFFFAOYSA-N 6-n-(4-dimethylphosphorylphenyl)-4-n-morpholin-4-ylpyrimidine-4,6-diamine Chemical compound C1=CC(P(C)(=O)C)=CC=C1NC1=CC(NN2CCOCC2)=NC=N1 WWZYCYIMGPENLW-UHFFFAOYSA-N 0.000 claims 1
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 1
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 1
- QZUZWADBRGIYGQ-UHFFFAOYSA-N CN1CCN(CC1)C1=NN=C(O1)CC1(NC=CC(=N1)N)N Chemical compound CN1CCN(CC1)C1=NN=C(O1)CC1(NC=CC(=N1)N)N QZUZWADBRGIYGQ-UHFFFAOYSA-N 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- RTZKZFJDLAIYFH-UHFFFAOYSA-N ether Substances CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 125000000814 indol-3-yl group Chemical group [H]C1=C([H])C([H])=C2N([H])C([H])=C([*])C2=C1[H] 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- MGSGCROTQJAWPG-UHFFFAOYSA-N n-(4-dimethylphosphoryl-2-methoxyphenyl)-5-[3-fluoro-5-(trifluoromethyl)phenoxy]pyridazin-3-amine Chemical compound COC1=CC(P(C)(C)=O)=CC=C1NC1=CC(OC=2C=C(C=C(F)C=2)C(F)(F)F)=CN=N1 MGSGCROTQJAWPG-UHFFFAOYSA-N 0.000 claims 1
- MSRYRUDVJJNMCE-UHFFFAOYSA-N n-(4-dimethylphosphorylphenyl)-4-(4-methylpiperazin-1-yl)-1,3,5-triazin-2-amine Chemical compound C1CN(C)CCN1C1=NC=NC(NC=2C=CC(=CC=2)P(C)(C)=O)=N1 MSRYRUDVJJNMCE-UHFFFAOYSA-N 0.000 claims 1
- AFHOWOFMYOOCGZ-UHFFFAOYSA-N n-(4-dimethylphosphorylphenyl)-4-(4-methylpiperazin-1-yl)-5-(trifluoromethyl)pyrimidin-2-amine Chemical compound C1CN(C)CCN1C1=NC(NC=2C=CC(=CC=2)P(C)(C)=O)=NC=C1C(F)(F)F AFHOWOFMYOOCGZ-UHFFFAOYSA-N 0.000 claims 1
- IVNMFNUVKDKMPO-UHFFFAOYSA-N n-(4-dimethylphosphorylphenyl)-4-(4-phenylpiperazin-1-yl)-1,3,5-triazin-2-amine Chemical compound C1=CC(P(C)(=O)C)=CC=C1NC1=NC=NC(N2CCN(CC2)C=2C=CC=CC=2)=N1 IVNMFNUVKDKMPO-UHFFFAOYSA-N 0.000 claims 1
- JGFMDOFRFGNISI-UHFFFAOYSA-N n-(4-dimethylphosphorylphenyl)-4-(4-phenylpiperazin-1-yl)-5-(trifluoromethyl)pyrimidin-2-amine Chemical compound C1=CC(P(C)(=O)C)=CC=C1NC1=NC=C(C(F)(F)F)C(N2CCN(CC2)C=2C=CC=CC=2)=N1 JGFMDOFRFGNISI-UHFFFAOYSA-N 0.000 claims 1
- QSAQYDAITQLRJE-UHFFFAOYSA-N n-(4-dimethylphosphorylphenyl)-6-(4-methylpiperazin-1-yl)pyrimidin-4-amine Chemical compound C1CN(C)CCN1C1=CC(NC=2C=CC(=CC=2)P(C)(C)=O)=NC=N1 QSAQYDAITQLRJE-UHFFFAOYSA-N 0.000 claims 1
- UYZLNVWWINHIOQ-UHFFFAOYSA-N n-(4-dimethylphosphorylphenyl)-6-(4-phenylpiperazin-1-yl)pyrimidin-4-amine Chemical compound C1=CC(P(C)(=O)C)=CC=C1NC1=CC(N2CCN(CC2)C=2C=CC=CC=2)=NC=N1 UYZLNVWWINHIOQ-UHFFFAOYSA-N 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 125000004437 phosphorous atom Chemical group 0.000 claims 1
- 229910052698 phosphorus Inorganic materials 0.000 claims 1
- CSNFMBGHUOSBFU-UHFFFAOYSA-N pyrimidine-2,4,5-triamine Chemical compound NC1=NC=C(N)C(N)=N1 CSNFMBGHUOSBFU-UHFFFAOYSA-N 0.000 claims 1
- 125000006413 ring segment Chemical group 0.000 claims 1
- 229940124530 sulfonamide Drugs 0.000 claims 1
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 1
- 125000004385 trihaloalkyl group Chemical group 0.000 claims 1
- IKYLWDXCBAGPKJ-UHFFFAOYSA-N 2-n-(4-dimethylphosphorylphenyl)-4-n-morpholin-4-yl-5-(trifluoromethyl)pyrimidine-2,4-diamine Chemical compound C1=CC(P(C)(=O)C)=CC=C1NC1=NC=C(C(F)(F)F)C(NN2CCOCC2)=N1 IKYLWDXCBAGPKJ-UHFFFAOYSA-N 0.000 description 1
- CSZBFKKRBBGTRQ-UHFFFAOYSA-N 5-chloro-4-n-(4-dimethylphosphoryl-2-propan-2-ylsulfonylphenyl)-2-n-[5-(4-pyridin-2-ylpiperazin-1-yl)-1,3,4-thiadiazol-2-yl]pyrimidine-2,4-diamine Chemical compound CC(C)S(=O)(=O)C1=CC(P(C)(C)=O)=CC=C1NC1=NC(NC=2SC(=NN=2)N2CCN(CC2)C=2N=CC=CC=2)=NC=C1Cl CSZBFKKRBBGTRQ-UHFFFAOYSA-N 0.000 description 1
- GQJDPRNCUCAFMO-UHFFFAOYSA-N 6-chloro-5-n-(4-dimethylphosphorylphenyl)-3-n-[2-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl]-1,2,4-triazine-3,5-diamine Chemical compound COC1=CC(N2CCC(CC2)N2CCN(C)CC2)=CC=C1NC(N=1)=NN=C(Cl)C=1NC1=CC=C(P(C)(C)=O)C=C1 GQJDPRNCUCAFMO-UHFFFAOYSA-N 0.000 description 1
- XGVXKJKTISMIOW-ZDUSSCGKSA-N simurosertib Chemical compound N1N=CC(C=2SC=3C(=O)NC(=NC=3C=2)[C@H]2N3CCC(CC3)C2)=C1C XGVXKJKTISMIOW-ZDUSSCGKSA-N 0.000 description 1
Applications Claiming Priority (11)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US12831708P | 2008-05-21 | 2008-05-21 | |
| US61/128,317 | 2008-05-21 | ||
| US13749008P | 2008-07-31 | 2008-07-31 | |
| US61/137,490 | 2008-07-31 | ||
| US18879608P | 2008-08-13 | 2008-08-13 | |
| US61/188,796 | 2008-08-13 | ||
| US19293808P | 2008-09-23 | 2008-09-23 | |
| US19296408P | 2008-09-23 | 2008-09-23 | |
| US61/192,964 | 2008-09-23 | ||
| US61/192,938 | 2008-09-23 | ||
| PCT/US2009/044918 WO2009143389A1 (en) | 2008-05-21 | 2009-05-21 | Phosphorous derivatives as kinase inhibitors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015087857A Division JP6190415B2 (ja) | 2008-05-21 | 2015-04-22 | キナーゼ阻害剤としてのリン誘導体 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2011523646A JP2011523646A (ja) | 2011-08-18 |
| JP2011523646A5 true JP2011523646A5 (OSRAM) | 2012-07-05 |
Family
ID=41340562
Family Applications (8)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011510716A Withdrawn JP2011523646A (ja) | 2008-05-21 | 2009-05-21 | キナーゼ阻害剤としてのリン誘導体 |
| JP2015087857A Active JP6190415B2 (ja) | 2008-05-21 | 2015-04-22 | キナーゼ阻害剤としてのリン誘導体 |
| JP2017091616A Active JP6271064B2 (ja) | 2008-05-21 | 2017-05-02 | キナーゼ阻害剤としてのリン誘導体 |
| JP2017248633A Active JP6483233B2 (ja) | 2008-05-21 | 2017-12-26 | キナーゼ阻害剤としてのリン誘導体 |
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Families Citing this family (181)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI389893B (zh) | 2007-07-06 | 2013-03-21 | Astellas Pharma Inc | 二（芳胺基）芳基化合物 |
| US9273077B2 (en) | 2008-05-21 | 2016-03-01 | Ariad Pharmaceuticals, Inc. | Phosphorus derivatives as kinase inhibitors |
| WO2009143389A1 (en) * | 2008-05-21 | 2009-11-26 | Ariad Pharmaceuticals, Inc. | Phosphorous derivatives as kinase inhibitors |
| US11351168B1 (en) | 2008-06-27 | 2022-06-07 | Celgene Car Llc | 2,4-disubstituted pyrimidines useful as kinase inhibitors |
| US8338439B2 (en) | 2008-06-27 | 2012-12-25 | Celgene Avilomics Research, Inc. | 2,4-disubstituted pyrimidines useful as kinase inhibitors |
| US8450335B2 (en) | 2008-06-27 | 2013-05-28 | Celgene Avilomics Research, Inc. | 2,4-disubstituted pyrimidines useful as kinase inhibitors |
| AU2009314631B2 (en) | 2008-11-12 | 2014-07-31 | Takeda Pharmaceutical Company Limited | Pyrazinopyrazines and derivatives as kinase inhibitors |
| WO2010068292A1 (en) | 2008-12-12 | 2010-06-17 | Ariad Pharmaceuticals, Inc. | Azaindole derivatives as kinase inhibitors |
| JP5918693B2 (ja) | 2009-05-05 | 2016-05-18 | ダナ ファーバー キャンサー インスティテュート インコーポレイテッド | Ｅｇｆｒ阻害剤及び疾患の治療方法 |
| KR101614572B1 (ko) | 2009-05-08 | 2016-04-21 | 아스테라스 세이야쿠 가부시키가이샤 | 디아미노 헤테로환 카르복사미드 화합물 |
| TW201100441A (en) | 2009-06-01 | 2011-01-01 | Osi Pharm Inc | Amino pyrimidine anticancer compounds |
| AU2011260323A1 (en) | 2010-06-04 | 2012-11-15 | F. Hoffmann-La Roche Ag | Aminopyrimidine derivatives as LRRK2 modulators |
| JP6068340B2 (ja) | 2010-08-10 | 2017-01-25 | セルジーン アヴィロミクス リサーチ， インコーポレイテッド | Ｂｔｋ阻害剤のベシル酸塩 |
| CN104814970A (zh) * | 2010-10-14 | 2015-08-05 | 阿里亚德医药股份有限公司 | 抑制egfr导致的癌症中细胞增殖的方法 |
| NZ710636A (en) | 2010-11-01 | 2017-02-24 | Celgene Avilomics Res Inc | Heterocyclic compounds and uses thereof |
| ES2635713T3 (es) | 2010-11-01 | 2017-10-04 | Celgene Car Llc | Compuestos de heteroarilo y usos de los mismos |
| JP5957003B2 (ja) | 2010-11-10 | 2016-07-27 | セルジーン アヴィロミクス リサーチ， インコーポレイテッド | 変異体選択的ｅｇｆｒ阻害剤およびその使用 |
| DK2638031T3 (en) | 2010-11-10 | 2017-12-11 | Genentech Inc | PYRAZOLAMINOPYRIMIDINE DERIVATIVES AS LRRK2 MODULATORS |
| US9133224B2 (en) | 2010-11-29 | 2015-09-15 | OSI Pharmaceuticals, LLC | Macrocyclic kinase inhibitors |
| PT2651918T (pt) * | 2010-12-17 | 2017-10-17 | Novartis Ag | Formas cristalinas de 5-cloro-n2-(2-isopropoxi-5-metil-4-piperidin-4-il-fenil)-n4-[2-(propano-2-sulfonil)-fenil]-pirimidin-2,4-diamina |
| ES2691673T3 (es) | 2011-02-17 | 2018-11-28 | Cancer Therapeutics Crc Pty Limited | Inhibidores de Fak |
| DK2675794T3 (da) | 2011-02-17 | 2019-05-06 | Cancer Therapeutics Crc Pty Ltd | Selektive fak-inhibitorer |
| JP5965923B2 (ja) * | 2011-02-24 | 2016-08-10 | ジエンス ハンセン ファーマセウティカル カンパニー リミテッド | プロテインキナーゼ阻害剤としてのリン含有化合物 |
| EP4328223A3 (en) | 2011-04-22 | 2024-11-06 | Signal Pharmaceuticals, LLC | Substituted diaminocarboxamide and diaminocarbonitrile pyrimidines, compositions thereof, and methods of treatment therewith |
| CN103501612B (zh) * | 2011-05-04 | 2017-03-29 | 阿里亚德医药股份有限公司 | 抑制表皮生长因子受体导致的癌症中细胞增殖的化合物 |
| TWI577693B (zh) * | 2011-05-31 | 2017-04-11 | 江蘇康緣藥業股份有限公司 | 聚（ａｄｐ-核糖）聚合酶之三環抑制劑 |
| ES2671748T3 (es) | 2011-07-21 | 2018-06-08 | Tolero Pharmaceuticals, Inc. | Inhibidores heterocíclicos de proteína quinasas |
| US9364476B2 (en) | 2011-10-28 | 2016-06-14 | Celgene Avilomics Research, Inc. | Methods of treating a Bruton's Tyrosine Kinase disease or disorder |
| US9586965B2 (en) | 2012-01-13 | 2017-03-07 | Acea Biosciences Inc. | Pyrrolo[2,3-d]pyrimidine compounds as inhibitors of protein kinases |
| CN104203924B (zh) | 2012-01-13 | 2019-06-11 | 艾森生物科学公司 | 杂环化合物及其作为抗癌药的用途 |
| US9034885B2 (en) | 2012-01-13 | 2015-05-19 | Acea Biosciences Inc. | EGFR modulators and uses thereof |
| US9464089B2 (en) | 2012-01-13 | 2016-10-11 | Acea Biosciences Inc. | Heterocyclic compounds and uses thereof |
| ES2698298T3 (es) | 2012-03-15 | 2019-02-04 | Celgene Car Llc | Sales de un inhibidor de quinasa receptor de factor de crecimiento epidérmico |
| ES2880109T3 (es) | 2012-03-15 | 2021-11-23 | Celgene Car Llc | Formas sólidas de un inhibidor de la cinasa del receptor del factor de crecimiento epidérmico |
| JP6469567B2 (ja) | 2012-05-05 | 2019-02-13 | アリアド・ファーマシューティカルズ・インコーポレイテッド | Ｅｇｆｒ発動性がんの細胞増殖阻害用化合物 |
| CN103420902A (zh) * | 2012-05-18 | 2013-12-04 | 苏州爱斯鹏药物研发有限责任公司 | 一种2-氯-4-碘-5-甲基吡啶的制备方法 |
| JO3300B1 (ar) | 2012-06-06 | 2018-09-16 | Novartis Ag | مركبات وتركيبات لتعديل نشاط egfr |
| RU2509770C2 (ru) * | 2012-06-22 | 2014-03-20 | Общество с ограниченной ответственностью "Молекулярные Технологии" | Новые химические соединения производные 2,4-диамино-1,3,5-триазина для профилактики и лечения заболеваний человека и животных |
| KR101446742B1 (ko) | 2012-08-10 | 2014-10-01 | 한국화학연구원 | Ｎ2,ｎ4-비스(4-(피페라진-1-일)페닐)피리미딘-2,4-디아민 유도체 또는 이의 약학적으로 허용가능한 염 및 이를 유효성분으로 함유하는 암의 예방 또는 치료용 약학적 조성물 |
| KR102156398B1 (ko) * | 2012-11-06 | 2020-09-15 | 상하이 포천 파마슈티컬 씨오 엘티디 | Ａｌｋ 키나아제 억제제 |
| US9126950B2 (en) | 2012-12-21 | 2015-09-08 | Celgene Avilomics Research, Inc. | Heteroaryl compounds and uses thereof |
| PE20151274A1 (es) | 2013-02-08 | 2015-09-12 | Celgene Avilomics Res Inc | Inhibidores de erk y sus usos |
| WO2014164729A1 (en) | 2013-03-12 | 2014-10-09 | Arqule, Inc. | Substituted tricyclic pyrazolo-pyrimidine compounds |
| JP6433974B2 (ja) * | 2013-03-14 | 2018-12-05 | トレロ ファーマシューティカルズ， インコーポレイテッド | Ｊａｋ２およびａｌｋ２阻害剤およびその使用方法 |
| US9611283B1 (en) | 2013-04-10 | 2017-04-04 | Ariad Pharmaceuticals, Inc. | Methods for inhibiting cell proliferation in ALK-driven cancers |
| CN103242341B (zh) * | 2013-04-19 | 2015-12-09 | 中国科学院广州生物医药与健康研究院 | 噻吩并2，4取代嘧啶类化合物及其药物组合物与应用 |
| WO2014183520A1 (zh) * | 2013-05-17 | 2014-11-20 | 上海恒瑞医药有限公司 | 吡啶并嘧啶类衍生物、其制备方法及其在医药上的应用 |
| DK3019496T3 (da) | 2013-07-11 | 2019-12-09 | Acea Therapeutics Inc | Pyrimidinderivater som kinaseinhibitorer |
| US9492471B2 (en) | 2013-08-27 | 2016-11-15 | Celgene Avilomics Research, Inc. | Methods of treating a disease or disorder associated with Bruton'S Tyrosine Kinase |
| ES2738573T3 (es) | 2013-10-16 | 2020-01-23 | Fujifilm Corp | Sal de compuesto heterocíclico que contiene nitrógeno o cristal del mismo, composición farmacéutica e inhibidor de FLT3 |
| US9415049B2 (en) | 2013-12-20 | 2016-08-16 | Celgene Avilomics Research, Inc. | Heteroaryl compounds and uses thereof |
| NZ715903A (en) | 2014-01-30 | 2017-06-30 | Signal Pharm Llc | Solid forms of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide, compositions thereof and methods of their use |
| KR101656382B1 (ko) | 2014-02-28 | 2016-09-09 | 한국화학연구원 | 피리미딘-2,4-디아민 유도체 및 이를 유효성분으로 함유하는 항암용 약학적 조성물 |
| EP3150592B1 (en) * | 2014-05-30 | 2023-08-30 | Shanghai Emerald Wellcares Pharmaceutical Co., LTD | Alk kinase inhibitor, and preparation method and use thereof |
| EP3159338A4 (en) | 2014-06-17 | 2018-01-24 | Korea Research Institute of Chemical Technology | Pyrimidine-2,4-diamine derivative and anticancer pharmaceutical composition comprising same as effective ingredient |
| WO2016004413A2 (en) * | 2014-07-03 | 2016-01-07 | Board Of Regents, University Of Texas System | Gls1 inhibitors for treating disease |
| SI3164394T1 (sl) | 2014-07-03 | 2020-08-31 | Board Of Regents, The University Of Texas System | GLS1 inhibitorji za zdravljenje bolezni |
| CN105330698B (zh) * | 2014-07-04 | 2019-05-28 | 齐鲁制药有限公司 | 螺环芳基磷氧化物和硫化物 |
| EP3165530B1 (en) | 2014-07-04 | 2018-12-05 | Qilu Pharmaceutical Co., Ltd | Spirocyclic aryl phosphorus oxide and aryl phosphorus sulfide |
| CN106661064B (zh) * | 2014-08-07 | 2019-10-15 | 江苏豪森药业集团有限公司 | 一种抗癌化合物的新晶型及其制备方法和用途 |
| CN105330697B (zh) * | 2014-08-07 | 2019-05-28 | 江苏豪森药业集团有限公司 | 一种抗癌化合物的晶型及其制备方法和用途 |
| WO2016019910A1 (zh) * | 2014-08-07 | 2016-02-11 | 江苏豪森药业股份有限公司 | 一种抗癌化合物的晶型及其制备方法和用途 |
| WO2016025561A1 (en) | 2014-08-13 | 2016-02-18 | Celgene Avilomics Research, Inc. | Forms and compositions of an erk inhibitor |
| WO2016027904A1 (ja) | 2014-08-22 | 2016-02-25 | 富士フイルム株式会社 | Ｆｌｔ３変異陽性癌を処置するための医薬組成物、変異型ｆｌｔ３阻害剤およびそれらの応用 |
| KR101633722B1 (ko) | 2014-10-08 | 2016-06-28 | 한국화학연구원 | 4-(1-퍼롤-3,4-디카르복시아미드)피리미딘 유도체, 이의 제조방법 및 이를 유효성분으로 함유하는 암의 예방 또는 치료용 약학적 조성물 |
| PE20171344A1 (es) * | 2014-10-21 | 2017-09-13 | Ariad Pharma Inc | Formas cristalinas de 5-cloro-n4-[2-(dimetilfosforil)fenil]-n2-{2-metoxi-4-[4-(4-metilpiperazin-1-il)piperidin-1-il]pirimidina-2,4-diamina |
| CN107108524A (zh) | 2014-12-16 | 2017-08-29 | 西格诺药品有限公司 | 2‑(叔丁基氨基)‑4‑((1r,3r,4r)‑3‑羟基‑4‑甲基环己基氨基)‑嘧啶‑5‑甲酰胺的配制物 |
| JP6903577B2 (ja) | 2014-12-16 | 2021-07-14 | シグナル ファーマシューティカルズ，エルエルシー | 皮膚におけるｃ−Ｊｕｎ Ｎ末端キナーゼの阻害の測定方法 |
| US20180022710A1 (en) | 2015-01-29 | 2018-01-25 | Signal Pharmaceuticals, Llc | Isotopologues of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide |
| CN105985317B (zh) * | 2015-02-12 | 2018-09-18 | 正大天晴药业集团股份有限公司 | 一种色瑞替尼的制备方法及其中间体 |
| KR101772134B1 (ko) | 2015-04-14 | 2017-08-29 | 한국화학연구원 | N2-(2-메톡시페닐)피리미딘 유도체, 이의 제조 방법 및 이를 유효 성분으로 함유하는 암의 예방 또는 치료용 약학적 조성물 |
| CN106146468B (zh) * | 2015-04-17 | 2020-12-01 | 杭州雷索药业有限公司 | 吡啶酮类蛋白激酶抑制剂 |
| KR101653571B1 (ko) | 2015-04-22 | 2016-09-05 | 한국화학연구원 | 4-(2-아미노-테트라하이드로나프탈렌닐)피리미딘 유도체, 이의 제조 방법 및 이를 유효성분으로 함유하는 암의 예방 또는 치료용 약학적 조성물 |
| CN106188060A (zh) * | 2015-04-29 | 2016-12-07 | 厦门大学 | 嘧啶并吡咯类化合物、其制备方法、药用组合物及其应用 |
| JP6863901B2 (ja) * | 2015-05-13 | 2021-04-28 | アリアド ファーマシューティカルズ， インコーポレイテッド | キナーゼ阻害のためのヘテロアリール化合物 |
| CN104892526A (zh) * | 2015-06-17 | 2015-09-09 | 药源药物化学（上海）有限公司 | 一种2,5-二氯-n-(2-(异丙基磺酰基)苯基)嘧啶-4-胺的制备方法 |
| WO2017004359A1 (en) | 2015-06-30 | 2017-01-05 | Board Of Regents, University Of Texas System | Gls1 inhibitors for treating disease |
| CN106336398A (zh) * | 2015-07-06 | 2017-01-18 | 杭州雷索药业有限公司 | 2‑饱和环基取代的苯胺类蛋白激酶抑制剂 |
| JP6412471B2 (ja) | 2015-07-15 | 2018-10-24 | 富士フイルム株式会社 | 含窒素複素環化合物の製造方法およびその中間体 |
| WO2017009751A1 (en) | 2015-07-15 | 2017-01-19 | Pfizer Inc. | Pyrimidine derivatives |
| WO2017019487A1 (en) | 2015-07-24 | 2017-02-02 | Celgene Corporation | Methods of synthesis of (1r,2r,5r)-5-amino-2-methylcyclohexanol hydrochloride and intermediates useful therein |
| CN105061506B (zh) | 2015-07-27 | 2017-08-29 | 苏州明锐医药科技有限公司 | 抗肿瘤药物ap26113的制备方法 |
| CN106478700B (zh) * | 2015-08-26 | 2020-12-29 | 杭州雷索药业有限公司 | 硼基取代的苯胺类蛋白激酶抑制剂 |
| MX2018004332A (es) | 2015-10-09 | 2019-01-10 | Acea Therapeutics Inc | Sales farmaceuticas, formas fisicas y composiciones de inhibidores de pirrolopirimidina cinasa, y metodos para fabricar las mismas. |
| CN106699810A (zh) * | 2015-11-17 | 2017-05-24 | 清华大学 | 一种含氮杂环化合物及其制备方法与在抑制激酶活性中的应用 |
| RU2606951C1 (ru) * | 2015-11-19 | 2017-01-10 | Закрытое акционерное общество "Р-Фарм" (ЗАО "Р-Фарм") | Дихлорацетаты замещенных N4-[2-(диметилфосфорил)фенил]-N2-(2-метокси-4-пиперидин-1-илфенил)-5-хлорпиримидин-2,4-диаминов в качестве модуляторов ALK и EGFR, предназначенных для лечения рака |
| JP6887430B2 (ja) * | 2015-11-27 | 2021-06-16 | チア タイ ティエンチン ファーマシューティカル グループ カンパニー リミテッドChia Tai Tianqing Pharmaceutical Group Co., Ltd. | 重水素化されたＢｒｉｇａｔｉｎｉｂ誘導体、かかる誘導体を含む薬学的組成物、並びにそれらの使用 |
| CN105294759B (zh) * | 2015-12-02 | 2018-01-19 | 苏州东南药业股份有限公司 | 一种抗肿瘤药物的制备方法 |
| CN113912648A (zh) * | 2015-12-02 | 2022-01-11 | 深圳市塔吉瑞生物医药有限公司 | 一种二氨基嘧啶化合物及包含该化合物的组合物 |
| CN108602782B (zh) | 2015-12-22 | 2022-06-17 | 德克萨斯大学系统董事会 | N-甲基-1h-1,2,3-三唑-4-甲酰胺化合物的盐形式和多晶型物 |
| WO2017133663A1 (en) * | 2016-02-03 | 2017-08-10 | Shanghai Fochon Pharmaceutical Co., Ltd. | Phosphorus containing compounds as protein kinase inhibitors |
| JP6911019B2 (ja) * | 2016-05-17 | 2021-07-28 | 公益財団法人がん研究会 | Ｅｇｆｒ−ｔｋｉ耐性を獲得した肺癌の治療薬 |
| CN106220608B (zh) * | 2016-07-25 | 2018-11-27 | 安润医药科技（苏州）有限公司 | 二苯氨基嘧啶及三嗪化合物、其药用组合物及用途 |
| CN107698603B (zh) * | 2016-08-09 | 2022-04-08 | 南京红云生物科技有限公司 | 噻吩并嘧啶类化合物、其制备方法、药用组合物及其应用 |
| EP3528816A4 (en) | 2016-10-21 | 2020-04-08 | Nimbus Lakshmi, Inc. | TYK2 INHIBITORS AND USES THEREOF |
| CN110036003B (zh) * | 2016-10-25 | 2021-10-29 | 苏州晶云药物科技股份有限公司 | Ap26113的新晶型及其制备方法 |
| EP3548479A1 (en) * | 2016-11-30 | 2019-10-09 | ARIAD Pharmaceuticals, Inc. | Anilinopyrimidines as haematopoietic progenitor kinase 1 (hpk1) inhibitors |
| WO2018108064A1 (zh) * | 2016-12-13 | 2018-06-21 | 南京明德新药研发股份有限公司 | 作为第四代egfr激酶抑制剂的螺环芳基磷氧化合物 |
| WO2018111787A1 (en) * | 2016-12-13 | 2018-06-21 | Bristol-Myers Squibb Company | Phosphine oxide alkyl amide substituted heteroaryl compounds as modulators of il-12, il-23, and/or ifn alpha responses |
| CN110520110A (zh) * | 2017-03-08 | 2019-11-29 | 阿瑞雅德制药公司 | 包含5-氯-n4-[2-(二甲基磷酰基)苯基]-n2-{2-甲氧基-4-[4-(4-甲基哌嗪-1-基)哌啶-1-基]苯基}嘧啶-2,4-二胺的药物制剂 |
| JP2020516682A (ja) | 2017-04-07 | 2020-06-11 | エイシア セラピューティクス， インコーポレイテッド | ピロロピリミジンキナーゼの薬学的な塩、物理的形態および組成物、ならびにその作製方法 |
| JOP20190281A1 (ar) | 2017-06-13 | 2019-12-02 | Korea Res Inst Chemical Tech | مشتق n2، n4 ثنائي فينيل بيريميدين -2، 4- ثنائي أمين، وطريقة لتحضيره، وتركيبة صيدلانية تحتوي على المشتق بوصفه مكون فعال للوقاية من السرطان أو علاجه |
| CN111225903B (zh) | 2017-10-18 | 2024-08-16 | 德州大学系统董事会 | 谷氨酰胺酶抑制剂疗法 |
| WO2019112344A1 (ko) | 2017-12-07 | 2019-06-13 | 주식회사 온코빅스 | 암세포 성장 억제 효과를 나타내는 신규한 피리미딘 유도체 및 그를 포함하는 약제학적 조성물 |
| KR101992621B1 (ko) | 2017-12-07 | 2019-09-27 | 주식회사 온코빅스 | 암세포 성장 억제 효과를 나타내는 신규한 피리미딘 유도체 및 그를 포함하는 약제학적 조성물 |
| WO2019120094A1 (zh) * | 2017-12-21 | 2019-06-27 | 深圳市塔吉瑞生物医药有限公司 | 用于抑制激酶活性的芳基磷氧化物 |
| CN109912655B (zh) | 2017-12-13 | 2021-12-10 | 上海科技大学 | Alk蛋白降解剂及其抗肿瘤应用 |
| WO2019120121A1 (zh) * | 2017-12-21 | 2019-06-27 | 深圳市塔吉瑞生物医药有限公司 | 用于抑制激酶活性的二苯氨基嘧啶类化合物 |
| CA3088526A1 (en) | 2018-01-16 | 2019-07-25 | Syros Pharmaceuticals, Inc. | Inhibitors of cyclin-dependent kinase 7 (cdk7) |
| EP3740206B1 (en) | 2018-01-16 | 2024-03-06 | Syros Pharmaceuticals, Inc. | Inhibitors of cyclin-dependent kinase 7 (cdk7) |
| WO2019148789A1 (zh) * | 2018-02-02 | 2019-08-08 | 苏州科睿思制药有限公司 | 布格替尼的晶型及其制备方法 |
| CN109851638B (zh) * | 2018-02-07 | 2022-05-31 | 深圳市塔吉瑞生物医药有限公司 | 取代的二氨基嘧啶化合物 |
| EP3752132B1 (en) | 2018-02-13 | 2021-12-08 | Sandoz AG | Pharmaceutical composition of brigatinib |
| EP3768275A1 (en) | 2018-03-19 | 2021-01-27 | ARIAD Pharmaceuticals, Inc. | Methods of treating cancer in pediatric patients |
| CN110305161A (zh) * | 2018-03-20 | 2019-10-08 | 暨南大学 | 2-氨基嘧啶类化合物及其应用 |
| WO2019196812A1 (zh) * | 2018-04-09 | 2019-10-17 | 上海科技大学 | 蛋白降解靶向化合物、其抗肿瘤应用、其中间体及中间体应用 |
| WO2019200254A1 (en) | 2018-04-13 | 2019-10-17 | Tolero Pharmaceuticals, Inc. | Pim kinase inhibitors for treatment of myeloproliferative neoplasms and fibrosis associated with cancer |
| CN110467638A (zh) * | 2018-05-09 | 2019-11-19 | 北京赛特明强医药科技有限公司 | 一种含有间氯苯胺类取代基的双氨基氯代嘧啶类化合物、制备方法及其应用 |
| CN110467637B (zh) * | 2018-05-09 | 2022-02-18 | 北京赛特明强医药科技有限公司 | 一种含有氧化膦类取代苯胺的双氨基氯代嘧啶类化合物、制备方法及其应用 |
| CN110526941A (zh) * | 2018-05-24 | 2019-12-03 | 北京赛特明强医药科技有限公司 | 一种含有间氯苯胺类取代基的吡咯并嘧啶类化合物、制备方法及其应用 |
| WO2019223777A1 (zh) * | 2018-05-24 | 2019-11-28 | 北京赛特明强医药科技有限公司 | 一种含有芳胺基取代的吡咯并嘧啶类化合物、制备方法及其应用 |
| AU2019310590A1 (en) | 2018-07-26 | 2021-01-14 | Sumitomo Pharma Oncology, Inc. | Methods for treating diseases associated with abnormal acvr1 expression and acvr1 inhibitors for use in the same |
| CN109053693B (zh) * | 2018-09-20 | 2021-02-05 | 顺毅股份有限公司 | 哒嗪胺类化合物的制备及其应用 |
| WO2020080979A1 (en) * | 2018-10-15 | 2020-04-23 | Gero Discovery Limited Liability Company | Pfkfb3 inhibitors and their uses |
| WO2020088390A1 (zh) * | 2018-10-29 | 2020-05-07 | 江苏先声药业有限公司 | 作为第四代egfr抑制剂的嘧啶吡唑类化合物 |
| JP2022508055A (ja) | 2018-11-01 | 2022-01-19 | サイロス ファーマシューティカルズ， インコーポレイテッド | サイクリン依存性キナーゼ７（ｃｄｋ７）の阻害剤 |
| WO2020099483A1 (en) | 2018-11-15 | 2020-05-22 | Sandoz Ag | Crystalline forms of brigatinib |
| CN113195000A (zh) | 2018-12-21 | 2021-07-30 | 第一三共株式会社 | 抗体-药物缀合物和激酶抑制剂的组合 |
| CA3168211A1 (en) * | 2019-01-18 | 2020-07-23 | Voronoi Co., Ltd. | Pyrrolopyridine derivative and use thereof for preventing or treating protein kinase related disease |
| CA3127502A1 (en) | 2019-02-12 | 2020-08-20 | Sumitomo Dainippon Pharma Oncology, Inc. | Formulations comprising heterocyclic protein kinase inhibitors |
| CN113939518B (zh) * | 2019-03-15 | 2025-02-07 | 杭州英创医药科技有限公司 | 作为激酶抑制剂的稠合三环化合物 |
| JP2022526713A (ja) | 2019-03-21 | 2022-05-26 | オンクセオ | がんの処置のための、キナーゼ阻害剤と組み合わせたＤｂａｉｔ分子 |
| CN111825719A (zh) * | 2019-04-15 | 2020-10-27 | 北京赛特明强医药科技有限公司 | 一种含有芳胺基取代的吡咯并嘧啶类化合物、制备方法及其应用 |
| CN111848677B (zh) * | 2019-04-29 | 2023-03-17 | 浙江同源康医药股份有限公司 | 一种alk激酶抑制剂化合物的晶型、制备方法及应用 |
| WO2020245208A1 (en) | 2019-06-04 | 2020-12-10 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Use of cd9 as a biomarker and as a biotarget in glomerulonephritis or glomerulosclerosis |
| CN112047978A (zh) * | 2019-06-05 | 2020-12-08 | 北京赛思源生物医药技术有限公司 | 5-氯-n4-[2-(二甲基磷酰基)苯基]-n2-{2-甲氧基-4-[4-(4-甲基哌嗪-1-基)哌啶-1-基]苯基}嘧啶-2,4-二胺新晶型 |
| EP3994132A1 (en) | 2019-07-03 | 2022-05-11 | Sumitomo Dainippon Pharma Oncology, Inc. | Tyrosine kinase non-receptor 1 (tnk1) inhibitors and uses thereof |
| US12428395B2 (en) | 2019-08-01 | 2025-09-30 | Sperogenix Therapeutics Limited | Heterocyclic compounds as kinase inhibitor and uses thereof |
| WO2021073498A1 (zh) * | 2019-10-17 | 2021-04-22 | 贝达药业股份有限公司 | Egfr抑制剂、组合物及其制备方法 |
| CN110713497A (zh) * | 2019-10-30 | 2020-01-21 | 成都海杰亚医药科技有限公司 | 一种Brigatinib的中间体2-氨基苯基二甲基氧化膦制备方法 |
| KR102168179B1 (ko) | 2019-10-31 | 2020-10-20 | 주식회사 온코빅스 | 암세포 성장 억제 효과를 나타내는 신규한 헤테로 고리 치환 피리미딘 유도체 및 그를 포함하는 약제학적 조성물 |
| KR20220098759A (ko) | 2019-11-08 | 2022-07-12 | 인쎄름 (엥스띠뛰 나씨오날 드 라 쌍떼 에 드 라 흐쉐르슈 메디깔) | 키나제 억제제에 대해 내성을 획득한 암의 치료 방법 |
| WO2021104441A1 (zh) * | 2019-11-29 | 2021-06-03 | 江苏先声药业有限公司 | 作为egfr激酶抑制剂的多芳基化合物 |
| US20230114177A1 (en) | 2019-12-16 | 2023-04-13 | Oncobix Co., Ltd. | Novel deuterium-substituted pyrimidine derivative and pharmaceutical composition comprising same |
| JP7659560B2 (ja) * | 2019-12-16 | 2025-04-09 | コリア リサーチ インスティチュート オブ ケミカル テクノロジー | 新規なピリミジン誘導体及びその用途 |
| AU2020406824A1 (en) * | 2019-12-16 | 2022-08-11 | Korea Research Institute Of Chemical Technology | Novel pyrimidine derivative and use thereof |
| CN111138492B (zh) * | 2020-01-06 | 2022-08-02 | 沈阳药科大学 | Alk抑制剂布格替尼的制备方法 |
| CN114787154A (zh) * | 2020-01-19 | 2022-07-22 | 苏州科睿思制药有限公司 | 一种Deucravacitinib的晶型及其制备方法和用途 |
| CN111620852B (zh) * | 2020-01-19 | 2023-05-09 | 镇江植生源农业科技有限公司 | 一种5-氯-嘧啶-2,4-二胺类化合物及其制备方法和应用 |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| US20230131025A1 (en) * | 2020-02-14 | 2023-04-27 | Betta Pharmaceuticals Co., Ltd. | Quinolyl phosphine oxide compound, and composition and application thereof |
| US11673879B2 (en) | 2020-03-31 | 2023-06-13 | Theravance Biopharma R&D Ip, Llc | Substituted pyrimidines and methods of use |
| CN114728994B (zh) * | 2020-07-03 | 2023-04-28 | 成都地奥九泓制药厂 | 芳基磷氧类化合物及其用途 |
| CN112225703B (zh) * | 2020-09-28 | 2022-03-11 | 广州智睿医药科技有限公司 | 一种治疗或预防与lrrk2激酶或异常lrrk2突变激酶活性相关疾病的药物 |
| KR20220081631A (ko) | 2020-12-09 | 2022-06-16 | 보로노이 주식회사 | 염증성 질환의 예방 및/또는 치료를 위한 피롤로-피리딘 유도체 화합물의 신규 용도 |
| CA3204383A1 (en) * | 2021-01-07 | 2022-07-14 | Rima AL-AWAR | Thienyl and cycloalkyl aminopyrimidine compounds as inhibitors of nuak kinases, compositions and uses thereof |
| EP4277902A4 (en) * | 2021-01-07 | 2024-12-18 | Ontario Institute for Cancer Research (OICR) | ISOINDOLINONE-AMINOPYRIMIDINE COMPOUNDS AS INHIBITORS OF NUAK KINASES, COMPOSITIONS AND USES THEREOF |
| JP2024508794A (ja) | 2021-02-19 | 2024-02-28 | スドー バイオサイエンシーズ リミテッド | Ｔｙｋ２阻害剤およびその使用 |
| CA3207819A1 (en) | 2021-02-19 | 2022-08-25 | Anjali Pandey | Tyk2 inhibitors and uses thereof |
| WO2022199589A1 (zh) * | 2021-03-23 | 2022-09-29 | 南京明德新药研发有限公司 | 嘧啶衍生物 |
| EP4074317A1 (en) | 2021-04-14 | 2022-10-19 | Bayer AG | Phosphorus derivatives as novel sos1 inhibitors |
| CN117222637A (zh) * | 2021-04-30 | 2023-12-12 | 百济神州有限公司 | Egfr降解剂和相关使用方法 |
| WO2022253081A1 (zh) * | 2021-06-03 | 2022-12-08 | 希格生科（深圳）有限公司 | 氧化膦衍生物及其制备方法和应用 |
| CN117500813A (zh) * | 2021-06-17 | 2024-02-02 | 微境生物医药科技(上海)有限公司 | 芳基氧膦类化合物 |
| US20240376138A1 (en) * | 2021-08-27 | 2024-11-14 | Chengdu Di'ao Jiuhong Pharmaceutical Factory | Crystal Forms, Preparation Method And Application Of Aryl Phosphine Oxide Compound |
| JP2025500871A (ja) * | 2021-12-13 | 2025-01-15 | 希格生科（深▲せん▼）有限公司 | ピリミジン又はピリジン誘導体及びその医薬用途 |
| WO2023204822A1 (en) * | 2022-04-22 | 2023-10-26 | Vivace Therapeutics, Inc. | Phenyl phosphine oxide compounds and methods of use thereof |
| CN115260234A (zh) * | 2022-07-01 | 2022-11-01 | 江苏医药职业学院 | 一种2-氨基-4-氨基芳基磷氧基嘧啶化合物及其制备方法与应用 |
| CN117045664A (zh) * | 2022-08-04 | 2023-11-14 | 中国人民解放军陆军特色医学中心 | 布格替尼作为st3gal4抑制剂的新应用 |
| CN115448906B (zh) * | 2022-09-26 | 2024-04-02 | 深圳大学 | 一种2-苯胺基嘧啶类衍生物及其制备方法与应用 |
| EP4602049A1 (en) | 2022-10-13 | 2025-08-20 | Bayer Aktiengesellschaft | Sos1 inhibitors |
| IL320456A (en) * | 2022-10-27 | 2025-06-01 | Suzhou Genhouse Bio Co Ltd | Phosphorus-containing compound, pharmaceutical composition and use thereof |
| CN120302975A (zh) | 2022-10-31 | 2025-07-11 | 住友制药美国公司 | 治疗骨髓增生性肿瘤的pim1抑制剂 |
| CN115785154B (zh) * | 2022-12-01 | 2025-09-05 | 希格生科（深圳）有限公司 | 杂芳环化合物及其医药用途 |
| CN116768885A (zh) * | 2023-03-14 | 2023-09-19 | 浙江大学 | N2-取代双环-2-氨基嘧啶类衍生物、其制备方法及医药用途 |
| CN119019454A (zh) * | 2023-05-23 | 2024-11-26 | 广州智睿医药科技有限公司 | 一种杂芳基衍生物的制备及用途 |
| WO2024249831A2 (en) * | 2023-06-02 | 2024-12-05 | Unogen Biotech Ltd. | Triple kinase inhibitors |
| TW202515565A (zh) | 2023-06-02 | 2025-04-16 | 美商原子智慧公司 | Ｔｙｋ２之抑制劑 |
| WO2025014773A1 (en) | 2023-07-07 | 2025-01-16 | Viridian Therapeutics, Inc. | Methods of treating chronic thyroid eye disease |
| WO2025073765A1 (en) | 2023-10-03 | 2025-04-10 | Institut National de la Santé et de la Recherche Médicale | Methods of prognosis and treatment of patients suffering from melanoma |
| CN119143806B (zh) * | 2024-11-19 | 2025-03-11 | 四川大学华西医院 | 一种靶向egfr突变的二甲基氧膦取代的苯胺嘧啶衍生物、其制备方法、用途及其制成的药物 |
Family Cites Families (283)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB1129563A (en) | 1966-03-31 | 1968-10-09 | Ici Ltd | Phosphorus-containing pyrimidine derivatives and biologically active compositions containing them |
| US4736866B1 (en) | 1984-06-22 | 1988-04-12 | Transgenic non-human mammals | |
| EP0391451A1 (en) | 1986-04-17 | 1990-10-10 | Imperial Chemical Industries Plc | Fungicides |
| US4966622A (en) | 1988-04-12 | 1990-10-30 | Ciba-Geigy Corporation | N-phenyl-N-pyrimidin-2-ylureas |
| GB8828222D0 (en) | 1988-12-02 | 1989-01-05 | Ici Plc | Reactive dyes |
| GB8903019D0 (en) | 1989-02-10 | 1989-03-30 | Ici Plc | Fungicides |
| US5175383A (en) | 1989-02-17 | 1992-12-29 | President And Fellows Of Harvard College | Animal model for benign prostatic disease |
| GB9016584D0 (en) | 1990-07-27 | 1990-09-12 | Ici Plc | Fungicides |
| EP0472053B1 (en) | 1990-08-20 | 1998-06-17 | Eisai Co., Ltd. | Sulfonamide derivatives |
| GB9220964D0 (en) | 1991-11-15 | 1992-11-18 | Ici Plc | Anionic compounds |
| US5521184A (en) | 1992-04-03 | 1996-05-28 | Ciba-Geigy Corporation | Pyrimidine derivatives and processes for the preparation thereof |
| TW225528B (OSRAM) | 1992-04-03 | 1994-06-21 | Ciba Geigy Ag | |
| EP0672035A1 (en) | 1993-10-01 | 1995-09-20 | Novartis AG | Pyrimidineamine derivatives and processes for the preparation thereof |
| PL313973A1 (en) | 1993-10-12 | 1996-08-05 | Du Pont Merck Pharma | 1 n-alkyl-n-arylopyrimidin amines and their derivatives |
| ES2208737T3 (es) | 1995-03-10 | 2004-06-16 | Berlex Laboratories, Inc. | Derivados de benzamidina, su preparacion y su utilizacion como anticoagulantes. |
| US5728201A (en) | 1995-09-14 | 1998-03-17 | Canon Kabushiki Kaisha | Ink, and ink-jet recording method and instruments using the same |
| GB9519197D0 (en) | 1995-09-20 | 1995-11-22 | Affinity Chromatography Ltd | Novel affinity ligands and their use |
| GB9523675D0 (en) | 1995-11-20 | 1996-01-24 | Celltech Therapeutics Ltd | Chemical compounds |
| WO1997020822A1 (en) | 1995-12-01 | 1997-06-12 | Novartis Ag | Quinazolin-2,4-diazirines as npy receptor antagonist |
| GB9608771D0 (en) | 1996-04-27 | 1996-07-03 | Agrevo Uk Ltd | Pyrimethanil salts |
| JP3106966B2 (ja) | 1996-07-17 | 2000-11-06 | 富士ゼロックス株式会社 | インクジェット記録用インク及びインクジェット記録方法 |
| JPH1060338A (ja) | 1996-08-21 | 1998-03-03 | Fuji Xerox Co Ltd | インクジェット記録用インク及びインクジェット記録方法 |
| US6008234A (en) | 1996-09-12 | 1999-12-28 | Berlex Laboratories, Inc. | Benzamidine derivatives substituted by cyclic amino acid and cyclic hydroxy acid derivatives and their use as anti-coagulants |
| CN1234798A (zh) | 1996-09-12 | 1999-11-10 | 舍林股份公司 | 环状氨基酸和环状羟基羧酸衍生物取代的苄脒衍生物和它们用作抗凝剂的用途 |
| US6004985A (en) | 1996-10-09 | 1999-12-21 | Berlex Laboratories, Inc. | Thio acid derived monocylic N-heterocyclics as anticoagulants |
| CO4940418A1 (es) | 1997-07-18 | 2000-07-24 | Novartis Ag | Modificacion de cristal de un derivado de n-fenil-2- pirimidinamina, procesos para su fabricacion y su uso |
| US6573044B1 (en) | 1997-08-07 | 2003-06-03 | The Regents Of The University Of California | Methods of using chemical libraries to search for new kinase inhibitors |
| JPH1160573A (ja) | 1997-08-22 | 1999-03-02 | Nippon Kayaku Co Ltd | トリアジン誘導体及びテロメラーゼ阻害剤 |
| ATE401312T1 (de) | 1997-12-15 | 2008-08-15 | Astellas Pharma Inc | Pyrimidin-5-carboxamid-derivate |
| US6562833B1 (en) | 1998-06-10 | 2003-05-13 | Basf Aktiengesellschaft | Use of 2-(n-phenylamino)pyrimidines as fungicides, and novel 2-(n-phenylamino) pyrimidines |
| WO2000015645A1 (fr) | 1998-09-11 | 2000-03-23 | Kyorin Pharmaceutical Co., Ltd. | Derives d'esters phosphoniques et leur procede de production |
| HU227453B1 (en) | 1998-11-10 | 2011-06-28 | Janssen Pharmaceutica Nv | Hiv replication inhibiting pyrimidines, and pharmaceutical compositions containing them |
| HUP0104171A3 (en) | 1998-11-17 | 2002-04-29 | Ihara Chemical Ind Co | Pyrimidinylbenzimidazole and triatinylbenzimidazole derivatives, intermediates and use as agricultura/horticultural fungicides |
| US6262088B1 (en) | 1998-11-19 | 2001-07-17 | Berlex Laboratories, Inc. | Polyhydroxylated monocyclic N-heterocyclic derivatives as anti-coagulants |
| US6127376A (en) | 1998-12-04 | 2000-10-03 | Berlex Laboratories, Inc. | Aryl and heterocyclyl substituted pyrimidine derivatives as anti-coagulants |
| CA2362401A1 (en) | 1999-02-04 | 2000-08-10 | Paul Fleming | G-protein coupled heptahelical receptor binding compounds and methods of use thereof |
| GB9910807D0 (en) | 1999-05-10 | 1999-07-07 | Prometic Biosciences Limited | Novel detoxification agents and their use |
| GB9914258D0 (en) | 1999-06-18 | 1999-08-18 | Celltech Therapeutics Ltd | Chemical compounds |
| GB9918035D0 (en) | 1999-07-30 | 1999-09-29 | Novartis Ag | Organic compounds |
| ATE396978T1 (de) | 1999-10-07 | 2008-06-15 | Amgen Inc | Triazin-kinase-hemmer |
| ITMI992711A1 (it) | 1999-12-27 | 2001-06-27 | Novartis Ag | Composti organici |
| JP2003532635A (ja) * | 2000-02-17 | 2003-11-05 | アムジエン・インコーポレーテツド | キナーゼ阻害薬 |
| GB0004887D0 (en) | 2000-03-01 | 2000-04-19 | Astrazeneca Uk Ltd | Chemical compounds |
| GB0004888D0 (en) | 2000-03-01 | 2000-04-19 | Astrazeneca Uk Ltd | Chemical compounds |
| US7087608B2 (en) | 2000-03-03 | 2006-08-08 | Robert Charles Atkins | Use of PDGF receptor tyrosine kinase inhibitors for the treatment of diabetic nephropathy |
| US6525051B2 (en) | 2000-03-27 | 2003-02-25 | Schering Aktiengesellschaft | N-heterocyclic derivatives as NOS inhibitors |
| ES2559273T3 (es) | 2000-05-08 | 2016-02-11 | Janssen Pharmaceutica Nv | Profármacos de pirimidinas que inhiben la replicación del VIH |
| ES2542326T3 (es) | 2000-05-08 | 2015-08-04 | Janssen Pharmaceutica Nv | Inhibidores de la replicación del VIH |
| US7238525B2 (en) | 2000-06-30 | 2007-07-03 | The Regents Of The University Of California | Strategy for leukemia therapy |
| GB0016877D0 (en) | 2000-07-11 | 2000-08-30 | Astrazeneca Ab | Chemical compounds |
| GB0022438D0 (en) | 2000-09-13 | 2000-11-01 | Novartis Ag | Organic Compounds |
| ATE346064T1 (de) | 2000-09-15 | 2006-12-15 | Vertex Pharma | Pyrazolverbindungen als protein-kinasehemmer |
| CA2426541C (en) | 2000-12-05 | 2010-02-23 | Clariant Finance (Bvi) Limited | Trichromatic dyeing process |
| IL156306A0 (en) | 2000-12-21 | 2004-01-04 | Glaxo Group Ltd | Pyrimidineamines as angiogenesis modulators |
| US6881737B2 (en) | 2001-04-11 | 2005-04-19 | Amgen Inc. | Substituted triazinyl acrylamide derivatives and methods of use |
| JP4416501B2 (ja) | 2001-05-30 | 2010-02-17 | ノバルティス アクチエンゲゼルシャフト | ２−｛［ｎ−（２−アミノ−３−（ヘテロアリールまたはアリール）プロピオニル）−アミノアシル］−アミノ｝−アルキルボロン酸誘導体 |
| ATE432929T1 (de) | 2001-06-15 | 2009-06-15 | Vertex Pharma | 5-(2-aminopyrimidin-4-yl)benzisoxazole als proteinkinasehemmer |
| EP1408978A4 (en) * | 2001-06-21 | 2005-07-13 | Ariad Pharma Inc | NOVEL PHENYLAMINO-PYRIMIDINES AND THEIR USE |
| EP1408980A4 (en) | 2001-06-21 | 2004-10-20 | Ariad Pharma Inc | NEW QUINAZOLINES AND THEIR USE |
| GB0115109D0 (en) | 2001-06-21 | 2001-08-15 | Aventis Pharma Ltd | Chemical compounds |
| WO2003023010A2 (en) | 2001-09-07 | 2003-03-20 | Irm Llc | Sensory neuron receptors |
| WO2003030909A1 (en) | 2001-09-25 | 2003-04-17 | Bayer Pharmaceuticals Corporation | 2- and 4-aminopyrimidines n-substtituded by a bicyclic ring for use as kinase inhibitors in the treatment of cancer |
| US20060009642A1 (en) | 2001-10-12 | 2006-01-12 | Irm Llc, A Delaware Limited Liability Company | Methods for the synthesis of substituted purines |
| US6949644B2 (en) | 2001-10-12 | 2005-09-27 | Irm Llc | Methods for the synthesis of substituted purines |
| US7176312B2 (en) | 2001-10-12 | 2007-02-13 | The Scripps Research Institute | Kinase inhibitor scaffolds and methods for their preparation |
| US6770652B2 (en) * | 2001-10-18 | 2004-08-03 | Duquesne University Of The Holy Ghost | Multiple acting anti-angiogenic and cytotoxic compounds and methods for using the same |
| IL161662A0 (en) | 2001-11-01 | 2004-09-27 | Janssen Pharmaceutica Nv | Heteroaryl amines as glycogen synthase kinase 3 beta inhibitors (gsk3 inhibitors) |
| IL162838A0 (en) | 2002-01-04 | 2005-11-20 | Univ Rockefeller | Compositions and methods for prevention and treatment peptide-of amyloid- related disorders |
| CN101717410B (zh) | 2002-02-01 | 2015-04-29 | 阿里亚德医药股份有限公司 | 含磷化合物及其应用 |
| AU2003209077A1 (en) | 2002-02-08 | 2003-09-02 | Smithkline Beecham Corporation | Pyrimidine compounds |
| GB0206215D0 (en) | 2002-03-15 | 2002-05-01 | Novartis Ag | Organic compounds |
| NZ535828A (en) | 2002-04-26 | 2007-10-26 | Gilead Sciences Inc | Cellular accumulation of phosphonate analogs of HIV protease inhibitor compounds and the compounds as such |
| US20050239054A1 (en) | 2002-04-26 | 2005-10-27 | Arimilli Murty N | Method and compositions for identifying anti-HIV therapeutic compounds |
| US7704995B2 (en) | 2002-05-03 | 2010-04-27 | Exelixis, Inc. | Protein kinase modulators and methods of use |
| AU2003231231A1 (en) | 2002-05-06 | 2003-11-11 | Bayer Pharmaceuticals Corporation | Pyridinyl amino pyrimidine derivatives useful for treating hyper-proliferative disorders |
| AR039540A1 (es) | 2002-05-13 | 2005-02-23 | Tibotec Pharm Ltd | Compuestos microbicidas con contenido de pirimidina o triazina |
| JP4372001B2 (ja) | 2002-05-27 | 2009-11-25 | ノバルティス アクチエンゲゼルシャフト | ビス芳香族アルカノール類 |
| GB0217431D0 (en) | 2002-07-27 | 2002-09-04 | Astrazeneca Ab | Novel compounds |
| RS51752B (sr) | 2002-07-29 | 2011-12-31 | Rigel Pharmaceuticals | Metode tretiranja i prevencije autoimunih oboljenja jedinjenjima 2,4-pirimidindiamina |
| WO2004018435A1 (en) | 2002-08-24 | 2004-03-04 | Astrazeneca Ab | Pyrimidine derivatives as modulators of chemokine receptor activity |
| WO2004041789A1 (en) | 2002-11-01 | 2004-05-21 | Vertex Pharmaceuticals Incorporated | Compositions useful as inhibitors of jak and other protein kinases |
| KR20050105190A (ko) | 2003-02-07 | 2005-11-03 | 얀센 파마슈티카 엔.브이. | Ｈｉｖ를 저해하는 1,2,4-트리아진 |
| EP1594508B1 (en) | 2003-02-11 | 2012-08-08 | Irm Llc | Novel bicyclic compounds and compositions |
| US7514446B2 (en) | 2003-02-20 | 2009-04-07 | Smithkline Beecham Corporation | Pyrimidine compounds |
| CL2004000306A1 (es) | 2003-02-20 | 2005-04-08 | Tibotec Pharm Ltd | Compuestos derivados de pirimidina sustituidas con indano; proceso para su preparacion; composicion farmaceutica que lo comprende; combinacion farmaceutica; y su uso para el tratamiento o profilaxis de una enfermedad infecciosa. |
| US7151096B2 (en) | 2003-03-05 | 2006-12-19 | Irm Llc | Cyclic compounds and compositions as protein kinase inhibitors |
| GB0305929D0 (en) * | 2003-03-14 | 2003-04-23 | Novartis Ag | Organic compounds |
| AR043633A1 (es) | 2003-03-20 | 2005-08-03 | Schering Corp | Ligandos de receptores de canabinoides |
| GB2400101A (en) | 2003-03-28 | 2004-10-06 | Biofocus Discovery Ltd | Compounds capable of binding to the active site of protein kinases |
| US20050014753A1 (en) | 2003-04-04 | 2005-01-20 | Irm Llc | Novel compounds and compositions as protein kinase inhibitors |
| US7253166B2 (en) | 2003-04-22 | 2007-08-07 | Irm Llc | 6-phenyl-7H-pyrrolo[2,3-d]pyrimidine compounds that induce neuronal differentiation in embryonic stem cells |
| US7423031B2 (en) | 2003-05-01 | 2008-09-09 | Irm Llc | Compounds and compositions as protein kinase inhibitors |
| US7317027B2 (en) | 2003-05-19 | 2008-01-08 | Sanofi-Aventis Deutschland Gmbh | Azaindole-derivatives as factor Xa inhibitors |
| MY150088A (en) | 2003-05-19 | 2013-11-29 | Irm Llc | Immunosuppressant compounds and compositions |
| CN1860118A (zh) | 2003-07-29 | 2006-11-08 | Irm责任有限公司 | 作为蛋白激酶抑制剂的化合物和组合物 |
| HRP20130602T1 (en) | 2003-07-30 | 2013-07-31 | Rigel Pharmaceuticals, Inc. | 2,4-pyrimidinediamine compounds for use in the treatment or prevention of autoimmune diseases |
| ES2365223T3 (es) | 2003-08-07 | 2011-09-26 | Rigel Pharmaceuticals, Inc. | Compuestos 2,4-pirimidindiamínicos y usos como agentes antiproliferativos. |
| RU2395500C2 (ru) * | 2003-08-15 | 2010-07-27 | Новартис Аг | 2,4-пиримидиндиамины, применяемые в лечении неопластических болезней, воспалительных и иммунных расстройств |
| SG145748A1 (en) | 2003-08-15 | 2008-09-29 | Irm Llc | 6-substituted anilino purines as rtk inhibitors |
| US7338957B2 (en) | 2003-08-28 | 2008-03-04 | Irm Llc | Compounds and compositions as protein kinase inhibitors |
| GB0321710D0 (en) | 2003-09-16 | 2003-10-15 | Novartis Ag | Organic compounds |
| AU2004272288B2 (en) | 2003-09-18 | 2008-11-13 | Novartis Ag | 2,4-di (phenylamino) pyrimidines useful in the treatment of proliferative disorders |
| CN100412066C (zh) | 2003-09-30 | 2008-08-20 | Irm责任有限公司 | 用作蛋白激酶抑制剂的化合物和组合物 |
| AU2004275888B2 (en) | 2003-10-02 | 2008-09-18 | Irm Llc | Compounds and compositions as protein kinase inhibitors |
| CN1863774B (zh) | 2003-10-08 | 2010-12-15 | Irm责任有限公司 | 用作蛋白激酶抑制剂的化合物和组合物 |
| CA2543142A1 (en) | 2003-10-24 | 2005-05-12 | Gilead Sciences, Inc. | Methods and compositions for identifying therapeutic compounds |
| DE10349587A1 (de) | 2003-10-24 | 2005-05-25 | Merck Patent Gmbh | Benzimidazolylderivate |
| CA2545384A1 (en) | 2003-11-10 | 2005-05-26 | Merck Sharp & Dohme Limited | Substituted nitrogen-containing six-membered amino-heterocycles as vanilloid-1 receptor antagonists for treating pain |
| DE502004006439D1 (de) | 2003-12-01 | 2008-04-17 | Tuchenhagen Gmbh | Verfahren zur zeitnahen überwachung, erfassung und übermittlung von prozessdaten |
| CN102127056B (zh) | 2003-12-03 | 2013-08-21 | Ym生物科学澳大利亚私人有限公司 | 微管蛋白抑制剂 |
| MY141255A (en) | 2003-12-11 | 2010-03-31 | Memory Pharm Corp | Phosphodiesterase 4 inhibitors, including n-substituted diarylamine analogs |
| EP1694652A1 (en) | 2003-12-19 | 2006-08-30 | Rigel Pharmaceuticals, Inc. | Stereoisomers and stereoisomeric mixtures of 1-(2,4-pyrimidinediamino)-2-cyclopentanecarboxamide synthetic intermediates |
| CA2553729A1 (en) | 2004-01-16 | 2005-08-04 | Wyeth | Quinoline intermediates of receptor tyrosine kinase inhibitors and the synthesis thereof |
| EP1708571A4 (en) | 2004-01-16 | 2009-07-08 | Merck & Co Inc | NEW CRYSTALLINE SALTS OF A DIPEPTIDYLPEPTIDASE IV HEMMER |
| DK1713806T3 (da) | 2004-02-14 | 2013-08-05 | Irm Llc | Forbindelser og sammensætninger som proteinkinaseinhibitorer |
| EP1751143A1 (en) * | 2004-05-14 | 2007-02-14 | Pfizer Products Incorporated | Pyrimidine derivatives for the treatment of abnormal cell growth |
| WO2005118544A2 (en) | 2004-05-18 | 2005-12-15 | Rigel Pharmaceuticals, Inc. | Cycloalkyl substituted pyrimidinediamine compounds and their uses |
| EP1598343A1 (de) | 2004-05-19 | 2005-11-23 | Boehringer Ingelheim International GmbH | 2-Arylaminopyrimidine als PLK Inhibitoren |
| RU2401265C2 (ru) | 2004-06-10 | 2010-10-10 | Айрм Ллк | Соединения и композиции в качестве ингибиторов протеинкиназы |
| JP2008504281A (ja) | 2004-06-23 | 2008-02-14 | アイアールエム・リミテッド・ライアビリティ・カンパニー | タンパク質キナーゼ阻害剤としての化合物および組成物 |
| GB0512324D0 (en) | 2005-06-16 | 2005-07-27 | Novartis Ag | Organic compounds |
| US7923554B2 (en) | 2004-08-10 | 2011-04-12 | Janssen Pharmaceutica N.V. | HIV inhibiting 1,2,4-triazin-6-one derivatives |
| US7521457B2 (en) | 2004-08-20 | 2009-04-21 | Boehringer Ingelheim International Gmbh | Pyrimidines as PLK inhibitors |
| GB0419161D0 (en) | 2004-08-27 | 2004-09-29 | Novartis Ag | Organic compounds |
| WO2006038594A1 (ja) | 2004-10-04 | 2006-04-13 | Ono Pharmaceutical Co., Ltd. | Ｎ型カルシウムチャネル阻害薬 |
| TW200626559A (en) | 2004-10-13 | 2006-08-01 | Wyeth Corp | Anilino-pyrimidine analogs |
| GT200500321A (es) | 2004-11-09 | 2006-09-04 | Compuestos y composiciones como inhibidores de proteina kinase. | |
| GB2420559B (en) | 2004-11-15 | 2008-08-06 | Rigel Pharmaceuticals Inc | Stereoisomerically enriched 3-aminocarbonyl bicycloheptene pyrimidinediamine compounds and their uses |
| JP5132319B2 (ja) | 2004-12-21 | 2013-01-30 | スミスクライン ビーチャム コーポレーション | ２−ピリミジニルピラゾロピリジンＥｒｂＢキナーゼ阻害剤 |
| US8211929B2 (en) | 2004-12-30 | 2012-07-03 | Exelixis, Inc. | Pyrimidine derivatives as kinase modulators and method of use |
| DE602006010979D1 (de) | 2005-01-19 | 2010-01-21 | Rigel Pharmaceuticals Inc | Prodrugs aus 2,4-pyrimidindiamin-verbindungen und ihre verwendungen |
| CN101106990B (zh) | 2005-01-26 | 2010-12-08 | Irm责任有限公司 | 用作蛋白激酶抑制剂的化合物和组合物 |
| TW200639163A (en) | 2005-02-04 | 2006-11-16 | Genentech Inc | RAF inhibitor compounds and methods |
| CN101500574A (zh) | 2005-03-15 | 2009-08-05 | Irm责任有限公司 | 用作蛋白激酶抑制剂的化合物和组合物 |
| CN101155799A (zh) | 2005-03-16 | 2008-04-02 | 塔格根公司 | 嘧啶化合物和使用方法 |
| DE102005016634A1 (de) | 2005-04-12 | 2006-10-19 | Merck Patent Gmbh | Neuartige Aza-Hetercyclen als Kinase-Inhibitoren |
| WO2006124874A2 (en) | 2005-05-12 | 2006-11-23 | Kalypsys, Inc. | Inhibitors of b-raf kinase |
| AU2006247757B2 (en) | 2005-05-13 | 2009-08-27 | Irm, Llc | Compounds and compositions as protein kinase inhibitors |
| US20080300267A1 (en) | 2005-05-16 | 2008-12-04 | Barun Okram | Compounds and Compositions as Protein Kinase Inhibitors |
| US20090215777A1 (en) | 2005-05-19 | 2009-08-27 | Astex Therapeutics Ltd. | Pyrimidine Derivatives As HSP90 Inhibitors |
| WO2006128129A2 (en) | 2005-05-26 | 2006-11-30 | Synta Pharmaceuticals Corp. | Method for treating cancer |
| US20070032493A1 (en) | 2005-05-26 | 2007-02-08 | Synta Pharmaceuticals Corp. | Method for treating B cell regulated autoimmune disorders |
| WO2006129100A1 (en) | 2005-06-03 | 2006-12-07 | Glaxo Group Limited | Novel compounds |
| US20070203161A1 (en) | 2006-02-24 | 2007-08-30 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the jak pathway |
| CA2608367C (en) | 2005-06-08 | 2014-08-19 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the jak pathway |
| PT1899329E (pt) | 2005-07-01 | 2012-01-13 | Irm Llc | Derivados de benzimidazole substituídos por pirimidina como inibidores de proteína quinase |
| US20070032514A1 (en) | 2005-07-01 | 2007-02-08 | Zahn Stephan K | 2,4-diamino-pyrimidines as aurora inhibitors |
| NZ564872A (en) | 2005-07-11 | 2010-01-29 | Sanofi Aventis | Novel 2,4-dianilinopyrimidine derivatives, the preparation thereof, their use as medicaments, pharmaceutical compositions and, in particular, as ikk inhibitors |
| CN101291927A (zh) | 2005-07-26 | 2008-10-22 | 沃泰克斯药物股份有限公司 | 可用作蛋白激酶抑制剂的苯并咪唑 |
| US20080227783A1 (en) | 2005-08-02 | 2008-09-18 | Irm Llc | 5-Substituted Thiazol-2-Yl Amino Compounds and Compositions as Protein Kinase Inhibitors |
| ES2351939T3 (es) | 2005-08-09 | 2011-02-14 | Irm Llc | Compuestos y composiciones como inhibidores de proteínas cinasas. |
| JP5321061B2 (ja) * | 2005-08-11 | 2013-10-23 | アリアド・ファーマシューティカルズ・インコーポレイテッド | 不飽和複素環誘導体 |
| KR20080035698A (ko) | 2005-08-16 | 2008-04-23 | 아이알엠 엘엘씨 | 단백질 키나제 억제제로서의 화합물 및 조성물 |
| EA200800664A1 (ru) | 2005-10-13 | 2009-02-27 | Глаксо Груп Лимитед | Производные пирролопиримидина в качестве ингибиторов syk |
| US7973060B2 (en) | 2005-10-13 | 2011-07-05 | Crystalgenomics, Inc. | Fab I inhibitor and process for preparing same |
| CA2626742A1 (en) | 2005-10-21 | 2007-04-26 | Exelixis, Inc. | Pyrazolo-pyrimidines as casein kinase ii (ck2) modulators |
| ATE444294T1 (de) | 2005-10-28 | 2009-10-15 | Irm Llc | Verbindungen und zusammensetzungen als proteinkinaseinhibitoren |
| US8604042B2 (en) | 2005-11-01 | 2013-12-10 | Targegen, Inc. | Bi-aryl meta-pyrimidine inhibitors of kinases |
| US8133900B2 (en) | 2005-11-01 | 2012-03-13 | Targegen, Inc. | Use of bi-aryl meta-pyrimidine inhibitors of kinases |
| MX362412B (es) | 2005-11-01 | 2019-01-15 | Targegen Inc | Inhibidores de biaril meta-pirimidina de cinasas. |
| AU2006311910A1 (en) | 2005-11-03 | 2007-05-18 | Irm Llc | Protein kinase inhibitors |
| ES2421450T3 (es) | 2005-12-05 | 2013-09-02 | Glaxosmithkline Llc | 2-Pirimidinil-pirazolopiridinas inhibidoras de la quinasa ErbB |
| WO2007120339A1 (en) | 2005-12-19 | 2007-10-25 | Genentech, Inc. | Pyrimidine kinase inhibitors |
| DE102005062742A1 (de) | 2005-12-22 | 2007-06-28 | Bayer Schering Pharma Ag | Sulfoximin substituierte Pyrimidine, Verfahren zu deren Herstellung und ihre Verwendung als Arzneimittel |
| JO2660B1 (en) | 2006-01-20 | 2012-06-17 | نوفارتيس ايه جي | Pi-3 inhibitors and methods of use |
| TW200736232A (en) | 2006-01-26 | 2007-10-01 | Astrazeneca Ab | Pyrimidine derivatives |
| EA200870217A1 (ru) | 2006-01-30 | 2009-02-27 | Экселиксис, Инк. | 4-арил-2-аминопиримидины или 4-арил-2-аминоалкилпиримидины в качестве модуляторов jak-2 и содержащие их фармацевтические композиции |
| AU2007212345A1 (en) | 2006-02-06 | 2007-08-16 | Irm Llc | Compounds and compositions as protein kinase inhibitors |
| TW200804364A (en) | 2006-02-22 | 2008-01-16 | Boehringer Ingelheim Int | New compounds |
| US20070208164A1 (en) | 2006-02-27 | 2007-09-06 | Wyeth | Methods of synthesizing radiolabeled 3-cyano[14C]quinolines |
| ES2465666T3 (es) | 2006-03-30 | 2014-06-06 | Janssen R&D Ireland | Pirimidinas 5-amido-sustituidas inhibidoras del HIV |
| WO2007113256A1 (en) | 2006-03-30 | 2007-10-11 | Tibotec Pharmaceuticals Ltd. | Hiv inhibiting 5-(hydroxymethylene and aminomethylene) substituted pyrimidines |
| GB0608386D0 (en) | 2006-04-27 | 2006-06-07 | Senexis Ltd | Compounds |
| US7601716B2 (en) | 2006-05-01 | 2009-10-13 | Cephalon, Inc. | Pyridopyrazines and derivatives thereof as ALK and c-Met inhibitors |
| BRPI0711628A2 (pt) | 2006-05-15 | 2011-12-06 | Irm Llc | composto, composição farmacêutica, uso e processo para preparação do composto |
| DE102006027156A1 (de) | 2006-06-08 | 2007-12-13 | Bayer Schering Pharma Ag | Sulfimide als Proteinkinaseinhibitoren |
| US8222256B2 (en) | 2006-07-05 | 2012-07-17 | Exelixis, Inc. | Methods of using IGFIR and ABL kinase modulators |
| WO2008009458A1 (en) | 2006-07-21 | 2008-01-24 | Novartis Ag | 2, 4 -di (arylaminio) -pyrimidine-5-carboxamide compounds as jak kinases inhibitors |
| GB0614579D0 (en) | 2006-07-21 | 2006-08-30 | Black James Foundation | Pyrimidine derivatives |
| DE102006041382A1 (de) | 2006-08-29 | 2008-03-20 | Bayer Schering Pharma Ag | Carbamoyl-Sulfoximide als Proteinkinaseinhibitoren |
| US8314234B2 (en) | 2006-09-25 | 2012-11-20 | Janssen Pharmaceutica N.V. | Bicyclic pyrimidine kinase inhibitors |
| WO2008045978A1 (en) | 2006-10-10 | 2008-04-17 | Rigel Pharmaceuticals, Inc. | Pinane-substituted pyrimidinediamine derivatives useful as axl inhibitors |
| CA2598893C (en) | 2006-10-11 | 2012-04-10 | Astellas Pharma Inc. | Eml4-alk fusion gene |
| CA2673125C (en) | 2006-10-19 | 2015-04-21 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the jak pathway |
| KR20140104060A (ko) | 2006-10-19 | 2014-08-27 | 시그날 파마소티칼 엘엘씨 | 헤테로아릴 화합물, 이들의 조성물 그리고 단백질 키나아제 억제제로서의 이들의 용도 |
| ES2633318T3 (es) | 2006-10-23 | 2017-09-20 | Cephalon, Inc. | Derivados bicíclicos fusionados de 2,4-diaminopirimidina como inhibidores de ALK y c-Met |
| US8236823B2 (en) | 2006-10-27 | 2012-08-07 | Amgen Inc. | Multi-cyclic compounds and methods of use |
| WO2008057994A2 (en) | 2006-11-03 | 2008-05-15 | Bristol-Myers Squibb Company | Pyrrolotriazine kinase inhibitors |
| PT2091918E (pt) | 2006-12-08 | 2014-11-24 | Irm Llc | Compostos e composições como inibidores de proteína cinase |
| EP3012249A1 (en) | 2006-12-08 | 2016-04-27 | Novartis AG | Compounds and composition as protein kinase inhibitors |
| EP2099771A1 (en) | 2006-12-19 | 2009-09-16 | Genentech, Inc. | Pyrimidine kinase inhibitors |
| EP1939185A1 (de) | 2006-12-20 | 2008-07-02 | Bayer Schering Pharma Aktiengesellschaft | Neuartige Hetaryl-Phenylendiamin-Pyrimidine als Proteinkinaseinhibitoren zur Behandlung von Krebs |
| US20100298557A1 (en) | 2006-12-28 | 2010-11-25 | Taisho Pharmaceutical Co., Ltd | Pyrazolopyrimidine compound |
| CA2674178C (en) | 2006-12-29 | 2015-11-10 | Tibotec Pharmaceuticals Ltd. | Hiv inhibiting 6-substituted pyrimidines |
| ES2618057T3 (es) | 2006-12-29 | 2017-06-20 | Janssen Sciences Ireland Uc | Pirimidinas 5,6-sustituidas inhibidoras del VIH |
| FR2911138B1 (fr) * | 2007-01-05 | 2009-02-20 | Sanofi Aventis Sa | Nouveaux derives de n, n'-2,4-dianilinopyrimidines, leur preparation a titre de medicaments, compositions pharmaceutiques et notamment comme inhibiteurs de ikk |
| AR065015A1 (es) | 2007-01-26 | 2009-05-13 | Smithkline Beecham Corp | Derivados de antranilamida, composiciones farmaceuticas que los contienen, y usos para el tratamiento del cancer |
| MX2009007944A (es) * | 2007-01-26 | 2009-08-07 | Irm Llc | Compuestos y composiciones de purina como inhibidores de quinasa para el tratamiento de enfermedades relacionadas con plasmodium. |
| PT2114900T (pt) | 2007-01-31 | 2019-01-17 | Ym Biosciences Australia Pty | Compostos à base de tiopirimidina e as suas utilizações |
| TW200834459A (en) | 2007-02-05 | 2008-08-16 | Huper Lab Co Ltd | Video object segmentation method applied for rainy situations |
| DE102007010801A1 (de) | 2007-03-02 | 2008-09-04 | Bayer Cropscience Ag | Diaminopyrimidine als Fungizide |
| US20100113445A1 (en) | 2007-03-20 | 2010-05-06 | Smithkline Beecham Corporation | Chemical Compounds |
| WO2008115738A1 (en) | 2007-03-20 | 2008-09-25 | Smithkline Beecham Corporation | Chemical compounds |
| WO2008118822A1 (en) | 2007-03-23 | 2008-10-02 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the jak pathway |
| JP5427769B2 (ja) | 2007-03-30 | 2014-02-26 | サノフイ | Ｐｇｄｓ阻害剤としてのピリミジンヒドラジド化合物 |
| EP2152079A4 (en) | 2007-06-04 | 2011-03-09 | Avila Therapeutics Inc | HETEROCYCLIC COMPOUNDS AND USES THEREOF |
| EA201000003A1 (ru) | 2007-06-21 | 2010-06-30 | Айрм Ллк | Ингибиторы протеинкиназ и способы их применения |
| TWI389893B (zh) | 2007-07-06 | 2013-03-21 | Astellas Pharma Inc | 二（芳胺基）芳基化合物 |
| EP2183225A1 (en) | 2007-07-17 | 2010-05-12 | Rigel Pharmaceuticals, Inc. | Cyclic amine substituted pyrimidinediamines as pkc inhibitors |
| WO2009020990A1 (en) | 2007-08-08 | 2009-02-12 | Smithkline Beecham Corporation | 2- [ (2-{phenylamino}-1h-pyrrolo [2, 3-d] pyrimidin-4-yl) amino] benzamide derivatives as igf-1r inhibitors for the treatment of cancer |
| KR101174201B1 (ko) | 2007-08-28 | 2012-08-16 | 아이알엠 엘엘씨 | 키나제 억제제로서의 2-비페닐아미노-4-아미노피리미딘 유도체 |
| AU2008296479A1 (en) | 2007-08-28 | 2009-03-12 | Dana Farber Cancer Institute | Amino substituted pyrimidine, pyrollopyridine and pyrazolopyrimidine derivatives useful as kinase inhibitors and in treating proliferative disorders and diseases associated with angiogenesis |
| US7989465B2 (en) | 2007-10-19 | 2011-08-02 | Avila Therapeutics, Inc. | 4,6-disubstituted pyrimidines useful as kinase inhibitors |
| TWI475996B (zh) | 2007-10-19 | 2015-03-11 | Celgene Avilomics Res Inc | 雜芳基化合物及其用途 |
| CA2707046A1 (en) | 2007-11-28 | 2009-06-11 | Nathanael S. Gray | Small molecule myristate inhibitors of bcr-abl and methods of use |
| JP2011505407A (ja) | 2007-12-03 | 2011-02-24 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 過剰な又は異常な細胞増殖を特徴とする疾患を治療するためのジアミノピリジン |
| EP2234986A2 (en) | 2007-12-20 | 2010-10-06 | Cellzome Limited | Sulfamides as zap-70 inhibitors |
| TW201546079A (zh) | 2007-12-21 | 2015-12-16 | Celgene Avilomics Res Inc | Ｈｃｖ蛋白酶抑制劑及其用途（一） |
| US8309685B2 (en) | 2007-12-21 | 2012-11-13 | Celgene Avilomics Research, Inc. | HCV protease inhibitors and uses thereof |
| WO2009082697A1 (en) | 2007-12-21 | 2009-07-02 | Avila Therapeutics, Inc. | Hcv protease inhibitors and uses thereof |
| US8293705B2 (en) | 2007-12-21 | 2012-10-23 | Avila Therapeutics, Inc. | HCV protease inhibitors and uses thereof |
| AR070127A1 (es) | 2008-01-11 | 2010-03-17 | Novartis Ag | Pirrolo - pirimidinas y pirrolo -piridinas |
| JP2011509931A (ja) | 2008-01-14 | 2011-03-31 | アイアールエム・リミテッド・ライアビリティ・カンパニー | 癌を処置するための組成物および方法 |
| WO2009102446A2 (en) | 2008-02-12 | 2009-08-20 | The Brigham And Women's Hospital, Inc. | Fish assay for eml4 and alk fusion in lung cancer |
| MX2010009743A (es) | 2008-03-05 | 2010-09-28 | Novartis Ag | Uso de derivados de pirimidina para el tratamiento de las enfermedades dependientes de los receptores del factor de crecimiento epidermico (egfr) o de enfermedades que hayan adquirido resistencia a los agentes que se dirigen a los miembros de la fami |
| WO2009112490A1 (en) | 2008-03-11 | 2009-09-17 | Cellzome Limited | Sulfonamides as zap-70 inhibitors |
| CL2009000600A1 (es) | 2008-03-20 | 2010-05-07 | Bayer Cropscience Ag | Uso de compuestos de diaminopirimidina como agentes fitosanitarios; compuestos de diaminopirimidina; su procedimiento de preparacion; agente que los contiene; procedimiento para la preparacion de dicho agente; y procedimiento para combatir plagas de animales y/u hongos dañinos patogenos de plantas. |
| KR101238585B1 (ko) | 2008-04-07 | 2013-02-28 | 노파르티스 아게 | 단백질 키나제 억제제로서의 화합물 및 조성물 |
| EP2271645A1 (en) | 2008-04-07 | 2011-01-12 | Irm Llc | Compounds and compositions as kinase inhibitors |
| WO2009127642A2 (en) | 2008-04-15 | 2009-10-22 | Cellzome Limited | Use of lrrk2 inhibitors for neurodegenerative diseases |
| CN102036952A (zh) | 2008-04-16 | 2011-04-27 | 比奥里波克斯公司 | 用作药物的双芳基化合物 |
| WO2009131687A2 (en) | 2008-04-22 | 2009-10-29 | Portola Pharmaceuticals, Inc. | Inhibitors of protein kinases |
| WO2009143018A2 (en) | 2008-05-19 | 2009-11-26 | Plexxikon, Inc. | Compounds and methods for kinase modulation, and indications therefor |
| US20130225527A1 (en) | 2008-05-21 | 2013-08-29 | Ariad Pharmaceuticals, Inc. | Phosphorus Derivatives as Kinase Inhibitors |
| WO2009143389A1 (en) * | 2008-05-21 | 2009-11-26 | Ariad Pharmaceuticals, Inc. | Phosphorous derivatives as kinase inhibitors |
| US20130225528A1 (en) | 2008-05-21 | 2013-08-29 | Ariad Pharmaceuticals, Inc. | Phosphorus Derivatives as Kinase Inhibitors |
| US9273077B2 (en) | 2008-05-21 | 2016-03-01 | Ariad Pharmaceuticals, Inc. | Phosphorus derivatives as kinase inhibitors |
| CA2726158A1 (en) | 2008-06-11 | 2009-12-17 | Dana Farber Cancer Institute | Compounds and compositions useful for the treatment of malaria |
| US20110294836A1 (en) | 2008-06-20 | 2011-12-01 | Metabolex, Inc. | Aryl gpr119 agonists and uses thereof |
| US8450335B2 (en) | 2008-06-27 | 2013-05-28 | Celgene Avilomics Research, Inc. | 2,4-disubstituted pyrimidines useful as kinase inhibitors |
| US8338439B2 (en) | 2008-06-27 | 2012-12-25 | Celgene Avilomics Research, Inc. | 2,4-disubstituted pyrimidines useful as kinase inhibitors |
| JP5634997B2 (ja) | 2008-09-02 | 2014-12-03 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 新規なベンズアミド、その製造、及び医薬としてのその使用 |
| JP2012501983A (ja) | 2008-09-03 | 2012-01-26 | バイエル・クロップサイエンス・アーゲー | ４−アルキル−置換ジアミノピリミジン類 |
| MX2011002484A (es) | 2008-09-05 | 2011-09-26 | Avila Therapeutics Inc | Algoritmo para diseñar inhibidores irreversibles. |
| WO2010044885A2 (en) | 2008-10-17 | 2010-04-22 | Whitehead Institute For Biomedical Research | Soluble mtor complexes and modulators thereof |
| WO2010048149A2 (en) | 2008-10-20 | 2010-04-29 | Kalypsys, Inc. | Heterocyclic modulators of gpr119 for treatment of disease |
| US8110578B2 (en) | 2008-10-27 | 2012-02-07 | Signal Pharmaceuticals, Llc | Pyrazino[2,3-b]pyrazine mTOR kinase inhibitors for oncology indications and diseases associated with the mTOR/PI3K/Akt pathway |
| CN101723936B (zh) | 2008-10-27 | 2014-01-15 | 上海睿星基因技术有限公司 | 激酶抑制剂及其在药学中的用途 |
| AU2009314631B2 (en) | 2008-11-12 | 2014-07-31 | Takeda Pharmaceutical Company Limited | Pyrazinopyrazines and derivatives as kinase inhibitors |
| WO2010068292A1 (en) | 2008-12-12 | 2010-06-17 | Ariad Pharmaceuticals, Inc. | Azaindole derivatives as kinase inhibitors |
| WO2010072155A1 (zh) | 2008-12-26 | 2010-07-01 | 复旦大学 | 一种嘧啶类衍生物及其制备方法和用途 |
| EP3255047B1 (en) | 2009-01-06 | 2021-06-30 | Dana-Farber Cancer Institute, Inc. | Pyrimido-diazepinone kinase scaffold compounds and uses in treating disorders |
| PL2881402T3 (pl) | 2009-02-12 | 2017-10-31 | Cell Signaling Technology Inc | Ekspresja zmutowanej ROS w ludzkim raku wątroby |
| TW201035088A (en) | 2009-02-27 | 2010-10-01 | Supergen Inc | Cyclopentathiophene/cyclohexathiophene DNA methyltransferase inhibitors |
| US20110071158A1 (en) | 2009-03-18 | 2011-03-24 | Boehringer Ingelheim International Gmbh | New compounds |
| WO2010111406A2 (en) | 2009-03-24 | 2010-09-30 | Myriad Pharmaceuticals, Inc. | Compounds and therapeutic uses thereof |
| ES2423804T3 (es) | 2009-04-03 | 2013-09-24 | Cellzome Gmbh | Métodos para la identificación de moléculas que interaccionan con cinasas y para la purificación de proteínas de cinasa |
| JP5918693B2 (ja) | 2009-05-05 | 2016-05-18 | ダナ ファーバー キャンサー インスティテュート インコーポレイテッド | Ｅｇｆｒ阻害剤及び疾患の治療方法 |
| US8410126B2 (en) | 2009-05-29 | 2013-04-02 | Boehringer Ingelheim International Gmbh | Pyrimidine inhibitors of PKTK2 |
| US20120142667A1 (en) | 2009-06-10 | 2012-06-07 | Nigel Ramsden | Pyrimidine derivatives as zap-70 inhibitors |
| US20120165332A1 (en) | 2009-06-18 | 2012-06-28 | Cellzome Limited | Sulfonamides and sulfamides as zap-70 inhibitors |
| EP3205647B1 (en) | 2009-08-17 | 2020-05-13 | Memorial Sloan-Kettering Cancer Center | 2-(pyrimidin-5-yl)-thiopyrimidine derivatives as hsp70 and hsc70 modulators for the treatment of proliferative disorders |
| CN102625708A (zh) | 2009-09-09 | 2012-08-01 | 阿维拉制药公司 | Pi3激酶抑制剂及其用途 |
| NZ620174A (en) | 2009-09-16 | 2016-08-26 | Celgene Avilomics Res Inc | Protein kinase conjugates and inhibitors |
| MX2012003484A (es) | 2009-09-25 | 2012-04-20 | Vertex Pharma | Metodos para preparar derivados de pirimidina utiles como inhibidores de proteina cinasa. |
| MY177695A (en) | 2009-10-26 | 2020-09-23 | Signal Pharm Llc | Methods of synthesis and purification of heteroaryl compounds |
| WO2011079231A1 (en) | 2009-12-23 | 2011-06-30 | Gatekeeper Pharmaceutical, Inc. | Compounds that modulate egfr activity and methods for treating or preventing conditions therewith |
| EP2519664A4 (en) | 2009-12-30 | 2014-03-12 | Avila Therapeutics Inc | LIGAND-RELATED COVALENTS MODIFYING A PROTEIN |
| EP2536689A1 (en) | 2010-02-17 | 2012-12-26 | Amgen Inc. | Aryl carboxamide derivatives as sodium channel inhibitors for treatment of pain |
| US8383793B2 (en) | 2010-04-15 | 2013-02-26 | St. Jude Children's Research Hospital | Methods and compositions for the diagnosis and treatment of cancer resistant to anaplastic lymphoma kinase (ALK) kinase inhibitors |
| WO2011140338A1 (en) | 2010-05-05 | 2011-11-10 | Gatekeeper Pharmaceuticals, Inc. | Compounds that modulate egfr activity and methods for treating or preventing conditions therewith |
| WO2011143495A1 (en) | 2010-05-13 | 2011-11-17 | Amgen Inc. | Heteroaryloxyheterocyclyl compounds as pde10 inhibitors |
| BR112012033253A2 (pt) | 2010-06-23 | 2016-11-22 | Hanmi Science Co Ltd | novos derivados de pirimidina fundidos para inibição da atividade de tirosina quinase |
| JP6068340B2 (ja) | 2010-08-10 | 2017-01-25 | セルジーン アヴィロミクス リサーチ， インコーポレイテッド | Ｂｔｋ阻害剤のベシル酸塩 |
| WO2012022045A1 (en) | 2010-08-20 | 2012-02-23 | Hutchison Medipharma Limited | Pyrrolopyrimidine compounds and uses thereof |
| CN104814970A (zh) | 2010-10-14 | 2015-08-05 | 阿里亚德医药股份有限公司 | 抑制egfr导致的癌症中细胞增殖的方法 |
| ES2635713T3 (es) | 2010-11-01 | 2017-10-04 | Celgene Car Llc | Compuestos de heteroarilo y usos de los mismos |
| NZ710636A (en) | 2010-11-01 | 2017-02-24 | Celgene Avilomics Res Inc | Heterocyclic compounds and uses thereof |
| JP5957003B2 (ja) | 2010-11-10 | 2016-07-27 | セルジーン アヴィロミクス リサーチ， インコーポレイテッド | 変異体選択的ｅｇｆｒ阻害剤およびその使用 |
| CN103501612B (zh) | 2011-05-04 | 2017-03-29 | 阿里亚德医药股份有限公司 | 抑制表皮生长因子受体导致的癌症中细胞增殖的化合物 |
| ME02887B (me) | 2011-07-27 | 2018-04-20 | Astrazeneca Ab | 2-(2,4,5-supstituisani-anilino) pirimidinski derivati kao egfr modulatori korisni za tretman raka |
| PH12014500638A1 (en) | 2011-09-22 | 2017-08-09 | Pfizer | Pyrrolopyrimidine and purine derivatives |
| JP6469567B2 (ja) | 2012-05-05 | 2019-02-13 | アリアド・ファーマシューティカルズ・インコーポレイテッド | Ｅｇｆｒ発動性がんの細胞増殖阻害用化合物 |
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