JP5566880B2 - プロテインキナーゼの阻害剤としての４，６−二置換アミノピリミジン誘導体 - Google Patents
プロテインキナーゼの阻害剤としての４，６−二置換アミノピリミジン誘導体 Download PDFInfo
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- JP5566880B2 JP5566880B2 JP2010504692A JP2010504692A JP5566880B2 JP 5566880 B2 JP5566880 B2 JP 5566880B2 JP 2010504692 A JP2010504692 A JP 2010504692A JP 2010504692 A JP2010504692 A JP 2010504692A JP 5566880 B2 JP5566880 B2 JP 5566880B2
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- Prior art keywords
- phenyl
- compound
- pyrimidin
- substituted
- methanesulfonamide
- 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.)
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- -1 4,6-disubstituted aminopyrimidine Chemical class 0.000 title claims description 96
- 239000003112 inhibitor Substances 0.000 title description 57
- 102000001253 Protein Kinase Human genes 0.000 title description 7
- 108060006633 protein kinase Proteins 0.000 title description 7
- 150000001875 compounds Chemical class 0.000 claims description 203
- 208000002193 Pain Diseases 0.000 claims description 197
- 230000036407 pain Effects 0.000 claims description 149
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 126
- 239000000203 mixture Substances 0.000 claims description 104
- 201000010099 disease Diseases 0.000 claims description 102
- 125000000217 alkyl group Chemical group 0.000 claims description 101
- 229910052739 hydrogen Inorganic materials 0.000 claims description 91
- 239000001257 hydrogen Substances 0.000 claims description 91
- 208000004296 neuralgia Diseases 0.000 claims description 70
- 208000021722 neuropathic pain Diseases 0.000 claims description 69
- 150000002431 hydrogen Chemical class 0.000 claims description 52
- 239000008194 pharmaceutical composition Substances 0.000 claims description 42
- 208000015181 infectious disease Diseases 0.000 claims description 41
- 208000027866 inflammatory disease Diseases 0.000 claims description 41
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 39
- 125000001072 heteroaryl group Chemical group 0.000 claims description 37
- 230000002062 proliferating effect Effects 0.000 claims description 35
- 206010065390 Inflammatory pain Diseases 0.000 claims description 34
- 208000024172 Cardiovascular disease Diseases 0.000 claims description 32
- 150000003839 salts Chemical class 0.000 claims description 31
- 208000000094 Chronic Pain Diseases 0.000 claims description 29
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims description 29
- 125000000623 heterocyclic group Chemical group 0.000 claims description 28
- 125000003545 alkoxy group Chemical group 0.000 claims description 26
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 26
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 26
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims description 25
- 125000003118 aryl group Chemical group 0.000 claims description 25
- 125000001424 substituent group Chemical group 0.000 claims description 25
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims description 24
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 24
- 208000015122 neurodegenerative disease Diseases 0.000 claims description 23
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 22
- 125000001309 chloro group Chemical group Cl* 0.000 claims description 22
- 230000004770 neurodegeneration Effects 0.000 claims description 21
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims description 19
- 208000026278 immune system disease Diseases 0.000 claims description 19
- 230000002757 inflammatory effect Effects 0.000 claims description 19
- 125000003342 alkenyl group Chemical group 0.000 claims description 17
- 125000005843 halogen group Chemical group 0.000 claims description 16
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 claims description 14
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims description 13
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 13
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 13
- 229910052757 nitrogen Inorganic materials 0.000 claims description 13
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 12
- 238000004519 manufacturing process Methods 0.000 claims description 12
- 150000003857 carboxamides Chemical group 0.000 claims description 11
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 11
- 229910052731 fluorine Inorganic materials 0.000 claims description 11
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 11
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims description 10
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 10
- 239000003937 drug carrier Substances 0.000 claims description 10
- 239000011737 fluorine Substances 0.000 claims description 10
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 10
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 9
- 239000012453 solvate Substances 0.000 claims description 8
- 125000004769 (C1-C4) alkylsulfonyl group Chemical group 0.000 claims description 6
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims description 6
- HEDRZPFGACZZDS-UHFFFAOYSA-N Chloroform Chemical compound ClC(Cl)Cl HEDRZPFGACZZDS-UHFFFAOYSA-N 0.000 claims description 6
- 150000001204 N-oxides Chemical class 0.000 claims description 6
- 125000003302 alkenyloxy group Chemical group 0.000 claims description 6
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 6
- 125000004076 pyridyl group Chemical group 0.000 claims description 6
- 229940124530 sulfonamide Drugs 0.000 claims description 6
- 150000003456 sulfonamides Chemical class 0.000 claims description 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 description 5
- 229910052760 oxygen Inorganic materials 0.000 claims description 5
- YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical compound C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 claims description 4
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims description 4
- 125000005119 alkyl cycloalkyl group Chemical group 0.000 claims description 4
- 125000001589 carboacyl group Chemical group 0.000 claims description 4
- 229940125904 compound 1 Drugs 0.000 claims description 4
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims description 4
- 125000000954 2-hydroxyethyl group Chemical group [H]C([*])([H])C([H])([H])O[H] 0.000 claims description 3
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims description 3
- 229910052799 carbon Inorganic materials 0.000 claims description 3
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims description 3
- 125000003386 piperidinyl group Chemical group 0.000 claims description 3
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims description 3
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims description 3
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims description 3
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 3
- 125000003006 2-dimethylaminoethyl group Chemical group [H]C([H])([H])N(C([H])([H])[H])C([H])([H])C([H])([H])* 0.000 claims description 2
- 125000004200 2-methoxyethyl group Chemical group [H]C([H])([H])OC([H])([H])C([H])([H])* 0.000 claims description 2
- 125000006283 4-chlorobenzyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1Cl)C([H])([H])* 0.000 claims description 2
- CITCBKKAVRLYPK-UHFFFAOYSA-N [3-[[6-(2-ethoxyphenyl)pyrimidin-4-yl]amino]phenyl]methanesulfonamide Chemical compound CCOC1=CC=CC=C1C1=CC(NC=2C=C(CS(N)(=O)=O)C=CC=2)=NC=N1 CITCBKKAVRLYPK-UHFFFAOYSA-N 0.000 claims description 2
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 2
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims description 2
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 2
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 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 description 2
- 125000006222 dimethylaminomethyl group Chemical group [H]C([H])([H])N(C([H])([H])[H])C([H])([H])* 0.000 claims description 2
- 125000001153 fluoro group Chemical group F* 0.000 claims description 2
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims description 2
- 125000004204 2-methoxyphenyl group Chemical group [H]C1=C([H])C(*)=C(OC([H])([H])[H])C([H])=C1[H] 0.000 claims 3
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 claims 3
- GDWVCMUNHLLAQU-UHFFFAOYSA-N 2-[6-[3-(methylsulfonylmethyl)anilino]pyrimidin-4-yl]phenol Chemical compound CS(=O)(=O)CC1=CC=CC(NC=2N=CN=C(C=2)C=2C(=CC=CC=2)O)=C1 GDWVCMUNHLLAQU-UHFFFAOYSA-N 0.000 claims 2
- OJEBBFHEVUJONE-UHFFFAOYSA-N [2-[6-[3-(methylsulfonylmethyl)anilino]pyrimidin-4-yl]phenyl]methanol Chemical compound CS(=O)(=O)CC1=CC=CC(NC=2N=CN=C(C=2)C=2C(=CC=CC=2)CO)=C1 OJEBBFHEVUJONE-UHFFFAOYSA-N 0.000 claims 2
- XTOMHCHXLAXPSD-UHFFFAOYSA-N [3-[[6-(2-ethoxy-5-fluorophenyl)pyrimidin-4-yl]amino]phenyl]methanesulfonamide Chemical compound CCOC1=CC=C(F)C=C1C1=CC(NC=2C=C(CS(N)(=O)=O)C=CC=2)=NC=N1 XTOMHCHXLAXPSD-UHFFFAOYSA-N 0.000 claims 2
- NMZQJJULBWUWIJ-UHFFFAOYSA-N [3-[[6-(3-ethoxyphenyl)pyrimidin-4-yl]amino]phenyl]methanesulfonamide Chemical compound CCOC1=CC=CC(C=2N=CN=C(NC=3C=C(CS(N)(=O)=O)C=CC=3)C=2)=C1 NMZQJJULBWUWIJ-UHFFFAOYSA-N 0.000 claims 2
- FYPVPYOTWMTLIL-UHFFFAOYSA-N [3-[[6-(3-fluorophenyl)pyrimidin-4-yl]amino]phenyl]methanesulfonamide Chemical compound NS(=O)(=O)CC1=CC=CC(NC=2N=CN=C(C=2)C=2C=C(F)C=CC=2)=C1 FYPVPYOTWMTLIL-UHFFFAOYSA-N 0.000 claims 2
- JEKAROVFQXTUPL-UHFFFAOYSA-N [3-[[6-(3-phenylmethoxyphenyl)pyrimidin-4-yl]amino]phenyl]methanesulfonamide Chemical compound NS(=O)(=O)CC1=CC=CC(NC=2N=CN=C(C=2)C=2C=C(OCC=3C=CC=CC=3)C=CC=2)=C1 JEKAROVFQXTUPL-UHFFFAOYSA-N 0.000 claims 2
- SERSRGJYQZHNME-UHFFFAOYSA-N [3-[[6-(4-fluorophenyl)pyrimidin-4-yl]amino]phenyl]methanesulfonamide Chemical compound NS(=O)(=O)CC1=CC=CC(NC=2N=CN=C(C=2)C=2C=CC(F)=CC=2)=C1 SERSRGJYQZHNME-UHFFFAOYSA-N 0.000 claims 2
- LGFYKPSWAJESAR-UHFFFAOYSA-N [3-[[6-[2-(2-methoxyethoxy)phenyl]pyrimidin-4-yl]amino]phenyl]methanesulfonamide Chemical compound COCCOC1=CC=CC=C1C1=CC(NC=2C=C(CS(N)(=O)=O)C=CC=2)=NC=N1 LGFYKPSWAJESAR-UHFFFAOYSA-N 0.000 claims 2
- FNVQNDGVNKTGEI-UHFFFAOYSA-N [3-[[6-[3-(1,2,4-triazol-1-ylmethyl)phenyl]pyrimidin-4-yl]amino]phenyl]methanesulfonamide Chemical compound NS(=O)(=O)CC1=CC=CC(NC=2N=CN=C(C=2)C=2C=C(CN3N=CN=C3)C=CC=2)=C1 FNVQNDGVNKTGEI-UHFFFAOYSA-N 0.000 claims 2
- GBAYTJKMNOIBLH-UHFFFAOYSA-N [3-[[6-[3-(diethylaminomethyl)phenyl]pyrimidin-4-yl]amino]phenyl]methanesulfonamide Chemical compound CCN(CC)CC1=CC=CC(C=2N=CN=C(NC=3C=C(CS(N)(=O)=O)C=CC=3)C=2)=C1 GBAYTJKMNOIBLH-UHFFFAOYSA-N 0.000 claims 2
- ZTGCWIHIQGSMGU-UHFFFAOYSA-N [3-[[6-[3-[(4-methylpiperazin-1-yl)methyl]phenyl]pyrimidin-4-yl]amino]phenyl]methanesulfonamide Chemical compound C1CN(C)CCN1CC1=CC=CC(C=2N=CN=C(NC=3C=C(CS(N)(=O)=O)C=CC=3)C=2)=C1 ZTGCWIHIQGSMGU-UHFFFAOYSA-N 0.000 claims 2
- PLVVQSNGBWUHRU-UHFFFAOYSA-N n-[3-(methylsulfonylmethyl)phenyl]-6-(2-phenylmethoxyphenyl)pyrimidin-4-amine Chemical compound CS(=O)(=O)CC1=CC=CC(NC=2N=CN=C(C=2)C=2C(=CC=CC=2)OCC=2C=CC=CC=2)=C1 PLVVQSNGBWUHRU-UHFFFAOYSA-N 0.000 claims 2
- ASGMFNBUXDJWJJ-JLCFBVMHSA-N (1R,3R)-3-[[3-bromo-1-[4-(5-methyl-1,3,4-thiadiazol-2-yl)phenyl]pyrazolo[3,4-d]pyrimidin-6-yl]amino]-N,1-dimethylcyclopentane-1-carboxamide Chemical compound BrC1=NN(C2=NC(=NC=C21)N[C@H]1C[C@@](CC1)(C(=O)NC)C)C1=CC=C(C=C1)C=1SC(=NN=1)C ASGMFNBUXDJWJJ-JLCFBVMHSA-N 0.000 claims 1
- UAOUIVVJBYDFKD-XKCDOFEDSA-N (1R,9R,10S,11R,12R,15S,18S,21R)-10,11,21-trihydroxy-8,8-dimethyl-14-methylidene-4-(prop-2-enylamino)-20-oxa-5-thia-3-azahexacyclo[9.7.2.112,15.01,9.02,6.012,18]henicosa-2(6),3-dien-13-one Chemical compound C([C@@H]1[C@@H](O)[C@@]23C(C1=C)=O)C[C@H]2[C@]12C(N=C(NCC=C)S4)=C4CC(C)(C)[C@H]1[C@H](O)[C@]3(O)OC2 UAOUIVVJBYDFKD-XKCDOFEDSA-N 0.000 claims 1
- AOSZTAHDEDLTLQ-AZKQZHLXSA-N (1S,2S,4R,8S,9S,11S,12R,13S,19S)-6-[(3-chlorophenyl)methyl]-12,19-difluoro-11-hydroxy-8-(2-hydroxyacetyl)-9,13-dimethyl-6-azapentacyclo[10.8.0.02,9.04,8.013,18]icosa-14,17-dien-16-one Chemical compound C([C@@H]1C[C@H]2[C@H]3[C@]([C@]4(C=CC(=O)C=C4[C@@H](F)C3)C)(F)[C@@H](O)C[C@@]2([C@@]1(C1)C(=O)CO)C)N1CC1=CC=CC(Cl)=C1 AOSZTAHDEDLTLQ-AZKQZHLXSA-N 0.000 claims 1
- ABJSOROVZZKJGI-OCYUSGCXSA-N (1r,2r,4r)-2-(4-bromophenyl)-n-[(4-chlorophenyl)-(2-fluoropyridin-4-yl)methyl]-4-morpholin-4-ylcyclohexane-1-carboxamide Chemical compound C1=NC(F)=CC(C(NC(=O)[C@H]2[C@@H](C[C@@H](CC2)N2CCOCC2)C=2C=CC(Br)=CC=2)C=2C=CC(Cl)=CC=2)=C1 ABJSOROVZZKJGI-OCYUSGCXSA-N 0.000 claims 1
- GLGNXYJARSMNGJ-VKTIVEEGSA-N (1s,2s,3r,4r)-3-[[5-chloro-2-[(1-ethyl-6-methoxy-2-oxo-4,5-dihydro-3h-1-benzazepin-7-yl)amino]pyrimidin-4-yl]amino]bicyclo[2.2.1]hept-5-ene-2-carboxamide Chemical compound CCN1C(=O)CCCC2=C(OC)C(NC=3N=C(C(=CN=3)Cl)N[C@H]3[C@H]([C@@]4([H])C[C@@]3(C=C4)[H])C(N)=O)=CC=C21 GLGNXYJARSMNGJ-VKTIVEEGSA-N 0.000 claims 1
- SZUVGFMDDVSKSI-WIFOCOSTSA-N (1s,2s,3s,5r)-1-(carboxymethyl)-3,5-bis[(4-phenoxyphenyl)methyl-propylcarbamoyl]cyclopentane-1,2-dicarboxylic acid Chemical compound O=C([C@@H]1[C@@H]([C@](CC(O)=O)([C@H](C(=O)N(CCC)CC=2C=CC(OC=3C=CC=CC=3)=CC=2)C1)C(O)=O)C(O)=O)N(CCC)CC(C=C1)=CC=C1OC1=CC=CC=C1 SZUVGFMDDVSKSI-WIFOCOSTSA-N 0.000 claims 1
- GHYOCDFICYLMRF-UTIIJYGPSA-N (2S,3R)-N-[(2S)-3-(cyclopenten-1-yl)-1-[(2R)-2-methyloxiran-2-yl]-1-oxopropan-2-yl]-3-hydroxy-3-(4-methoxyphenyl)-2-[[(2S)-2-[(2-morpholin-4-ylacetyl)amino]propanoyl]amino]propanamide Chemical compound C1(=CCCC1)C[C@@H](C(=O)[C@@]1(OC1)C)NC([C@H]([C@@H](C1=CC=C(C=C1)OC)O)NC([C@H](C)NC(CN1CCOCC1)=O)=O)=O GHYOCDFICYLMRF-UTIIJYGPSA-N 0.000 claims 1
- GCTFTMWXZFLTRR-GFCCVEGCSA-N (2r)-2-amino-n-[3-(difluoromethoxy)-4-(1,3-oxazol-5-yl)phenyl]-4-methylpentanamide Chemical compound FC(F)OC1=CC(NC(=O)[C@H](N)CC(C)C)=CC=C1C1=CN=CO1 GCTFTMWXZFLTRR-GFCCVEGCSA-N 0.000 claims 1
- IUSARDYWEPUTPN-OZBXUNDUSA-N (2r)-n-[(2s,3r)-4-[[(4s)-6-(2,2-dimethylpropyl)spiro[3,4-dihydropyrano[2,3-b]pyridine-2,1'-cyclobutane]-4-yl]amino]-3-hydroxy-1-[3-(1,3-thiazol-2-yl)phenyl]butan-2-yl]-2-methoxypropanamide Chemical compound C([C@H](NC(=O)[C@@H](C)OC)[C@H](O)CN[C@@H]1C2=CC(CC(C)(C)C)=CN=C2OC2(CCC2)C1)C(C=1)=CC=CC=1C1=NC=CS1 IUSARDYWEPUTPN-OZBXUNDUSA-N 0.000 claims 1
- YJLIKUSWRSEPSM-WGQQHEPDSA-N (2r,3r,4s,5r)-2-[6-amino-8-[(4-phenylphenyl)methylamino]purin-9-yl]-5-(hydroxymethyl)oxolane-3,4-diol Chemical compound C=1C=C(C=2C=CC=CC=2)C=CC=1CNC1=NC=2C(N)=NC=NC=2N1[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O YJLIKUSWRSEPSM-WGQQHEPDSA-N 0.000 claims 1
- VIJSPAIQWVPKQZ-BLECARSGSA-N (2s)-2-[[(2s)-2-[[(2s)-2-[[(2s)-2-[[(2s)-2-[[(2s)-2-acetamido-5-(diaminomethylideneamino)pentanoyl]amino]-4-methylpentanoyl]amino]-4,4-dimethylpentanoyl]amino]-4-methylpentanoyl]amino]propanoyl]amino]-5-(diaminomethylideneamino)pentanoic acid Chemical compound NC(=N)NCCC[C@@H](C(O)=O)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(N)=N)NC(C)=O VIJSPAIQWVPKQZ-BLECARSGSA-N 0.000 claims 1
- WWTBZEKOSBFBEM-SPWPXUSOSA-N (2s)-2-[[2-benzyl-3-[hydroxy-[(1r)-2-phenyl-1-(phenylmethoxycarbonylamino)ethyl]phosphoryl]propanoyl]amino]-3-(1h-indol-3-yl)propanoic acid Chemical compound N([C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)O)C(=O)C(CP(O)(=O)[C@H](CC=1C=CC=CC=1)NC(=O)OCC=1C=CC=CC=1)CC1=CC=CC=C1 WWTBZEKOSBFBEM-SPWPXUSOSA-N 0.000 claims 1
- STBLNCCBQMHSRC-BATDWUPUSA-N (2s)-n-[(3s,4s)-5-acetyl-7-cyano-4-methyl-1-[(2-methylnaphthalen-1-yl)methyl]-2-oxo-3,4-dihydro-1,5-benzodiazepin-3-yl]-2-(methylamino)propanamide Chemical compound O=C1[C@@H](NC(=O)[C@H](C)NC)[C@H](C)N(C(C)=O)C2=CC(C#N)=CC=C2N1CC1=C(C)C=CC2=CC=CC=C12 STBLNCCBQMHSRC-BATDWUPUSA-N 0.000 claims 1
- QFLWZFQWSBQYPS-AWRAUJHKSA-N (3S)-3-[[(2S)-2-[[(2S)-2-[5-[(3aS,6aR)-2-oxo-1,3,3a,4,6,6a-hexahydrothieno[3,4-d]imidazol-4-yl]pentanoylamino]-3-methylbutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-[1-bis(4-chlorophenoxy)phosphorylbutylamino]-4-oxobutanoic acid Chemical compound CCCC(NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CCCCC1SC[C@@H]2NC(=O)N[C@H]12)C(C)C)P(=O)(Oc1ccc(Cl)cc1)Oc1ccc(Cl)cc1 QFLWZFQWSBQYPS-AWRAUJHKSA-N 0.000 claims 1
- FNHHVPPSBFQMEL-KQHDFZBMSA-N (3S)-5-N-[(1S,5R)-3-hydroxy-6-bicyclo[3.1.0]hexanyl]-7-N,3-dimethyl-3-phenyl-2H-1-benzofuran-5,7-dicarboxamide Chemical compound CNC(=O)c1cc(cc2c1OC[C@@]2(C)c1ccccc1)C(=O)NC1[C@H]2CC(O)C[C@@H]12 FNHHVPPSBFQMEL-KQHDFZBMSA-N 0.000 claims 1
- IWZSHWBGHQBIML-ZGGLMWTQSA-N (3S,8S,10R,13S,14S,17S)-17-isoquinolin-7-yl-N,N,10,13-tetramethyl-2,3,4,7,8,9,11,12,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-3-amine Chemical compound CN(C)[C@H]1CC[C@]2(C)C3CC[C@@]4(C)[C@@H](CC[C@@H]4c4ccc5ccncc5c4)[C@@H]3CC=C2C1 IWZSHWBGHQBIML-ZGGLMWTQSA-N 0.000 claims 1
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- 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
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
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| AU2011231975B2 (en) * | 2010-03-22 | 2014-07-03 | Bayer Intellectual Property Gmbh | Pharmaceutically active disubstituted triazine derivatives |
| CA2826464C (en) * | 2011-03-02 | 2020-07-28 | Lead Discovery Center Gmbh | Pharmaceutically active disubstituted triazine derivatives |
| WO2012117059A1 (en) | 2011-03-02 | 2012-09-07 | Lead Discovery Center Gmbh | Pharmaceutically active disubstituted pyridine derivatives |
| CN103476759B (zh) * | 2011-04-19 | 2016-03-16 | 拜耳知识产权有限责任公司 | 取代的4-芳基-n-苯基-1,3,5-三嗪-2-胺 |
| TW201636330A (zh) | 2011-05-24 | 2016-10-16 | 拜耳知識產權公司 | 含有硫醯亞胺基團之４－芳基－ｎ－苯基－１，３，５－三氮雜苯－２－胺 |
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| CA2848615C (en) | 2011-09-16 | 2020-02-25 | Bayer Intellectual Property Gmbh | Disubstituted 5-fluoro pyrimidine derivatives containing a sulfoximine group |
| US9108926B2 (en) * | 2011-09-16 | 2015-08-18 | Bayer Intellectual Property Gmbh | Disubstituted 5-fluoro-pyrimidines |
| WO2013059634A1 (en) * | 2011-10-20 | 2013-04-25 | The Regents Of The University Of California | Use of cdk9 inhibitors to reduce cartilage degradation |
| DK2887943T3 (en) * | 2012-08-23 | 2018-03-12 | Virostatics Srl | HIS UNKNOWN 4,6-DISUBSTITUTED AMINOPYRIMIDINE DERIVATIVES |
| CN105283453B (zh) * | 2012-10-18 | 2018-06-22 | 拜耳药业股份公司 | 含砜基的n-(吡啶-2-基)嘧啶-4-胺衍生物 |
| JP6277195B2 (ja) | 2012-10-18 | 2018-02-07 | バイエル ファーマ アクチエンゲゼルシャフト | スルホン基を含んでいる５−フルオロ−ｎ−（ピリジン−２−イル）ピリジン−２−アミン誘導体 |
| ES2597232T3 (es) | 2012-10-18 | 2017-01-17 | Bayer Pharma Aktiengesellschaft | 4-(orto)-fluorofenil-5-fluoropirimidin-2-il aminas que contienen un grupo sulfona |
| TW201418243A (zh) * | 2012-11-15 | 2014-05-16 | Bayer Pharma AG | 含有磺醯亞胺基團之ｎ－（吡啶－２－基）嘧啶－４－胺衍生物 |
| CA2891244C (en) * | 2012-11-15 | 2020-12-01 | Ulrich Lucking | 4-(ortho)-fluorophenyl-5-fluoropyrimidin-2-yl amines containing a sulfoximine group |
| PL2928878T3 (pl) | 2012-11-15 | 2017-04-28 | Bayer Pharma Aktiengesellschaft | Pochodne 5-fluoro-N -(pirydyn-2-ylo)pirydyno-2-aminy zawierające grupę sulfoksyiminową |
| US9770445B2 (en) | 2013-07-04 | 2017-09-26 | Bayer Pharma Aktiengesellschaft | Sulfoximine substituted 5-fluoro-N-(pyridin-2-yl)pyridin-2-amine derivatives and their use as CDK9 kinase inhibitors |
| EP3052102B1 (en) * | 2013-10-04 | 2019-12-04 | Aptose Biosciences Inc. | Compositions for treating cancers |
| AR098394A1 (es) | 2013-11-25 | 2016-05-26 | Lilly Co Eli | Inhibidores de dgat2 (diacilglicerol o-aciltransferasa 2) |
| CN106232596A (zh) | 2014-03-13 | 2016-12-14 | 拜耳医药股份有限公司 | 含有砜基团的5‑氟‑n‑(吡啶‑2‑基)吡啶‑2‑胺衍生物 |
| CA2944251C (en) | 2014-04-01 | 2022-10-18 | Bayer Pharma Aktiengesellschaft | Disubstituted 5-fluoro pyrimidine derivatives containing a sulfondiimine group |
| EP3686290B1 (en) | 2014-04-04 | 2023-08-23 | Memorial Sloan-Kettering Cancer Center | Method and kits for identifying cdk9 inhibitors for the treatment of cancer |
| CA2945237C (en) | 2014-04-11 | 2022-09-06 | Ulrich Lucking | Novel macrocyclic compounds |
| EP3206749B1 (en) | 2014-10-14 | 2021-09-08 | The Regents of the University of California | The cdk9 and brd4 inhibitors flavopiridol and jq1 to inhibit cartilage inflammation |
| CA2964683A1 (en) | 2014-10-16 | 2016-04-21 | Bayer Pharma Aktiengesellschaft | Fluorinated benzofuranyl-pyrimidine derivatives containing a sulfone group |
| EP3207038B1 (en) | 2014-10-16 | 2018-08-22 | Bayer Pharma Aktiengesellschaft | Fluorinated benzofuranyl-pyrimidine derivatives containing a sulfoximine group |
| JP2018509439A (ja) | 2015-03-24 | 2018-04-05 | バイエル ファーマ アクチエンゲゼルシャフト | 多発性骨髄腫を治療するための４−（４−フルオロ−２−メトキシフェニル）−ｎ−｛３−［（ｓ−メチルスルホンイミドイル）メチル］フェニル｝−１，３，５−トリアジン−２−アミンの使用 |
| WO2016150902A1 (en) | 2015-03-24 | 2016-09-29 | Bayer Pharma Aktiengesellschaft | Use of 4-(4-fluoro-2-methoxyphenyl)-n-{3-[(s-methylsulfonimidoyl)methyl]phenyl}-1,3,5-triazin-2-amine for treating gastric cancers |
| US20180050040A1 (en) | 2015-03-24 | 2018-02-22 | Bayer Pharma Aktiengesellschaft | Use of 4-(4-fluoro-2-methoxyphenyl)-n--1,3,5-triazin-2-amine for treating lymphomas |
| EP3539961B1 (en) | 2015-06-29 | 2021-10-06 | Astrazeneca AB | Polycyclic amide derivatives as cdk9 inhibitors |
| US10717749B2 (en) | 2015-09-29 | 2020-07-21 | Bayer Pharma Aktiengesellschaft | Macrocyclic sulfondiimine compounds |
| CN108368129B (zh) | 2015-10-08 | 2021-08-17 | 拜耳医药股份有限公司 | 改性大环化合物 |
| WO2017060322A2 (en) | 2015-10-10 | 2017-04-13 | Bayer Pharma Aktiengesellschaft | Ptefb-inhibitor-adc |
| BR112019000796A2 (pt) | 2016-07-16 | 2019-04-24 | Florida State University Research Foundation, Inc. | compostos e métodos para tratamento e prevenção da infecção flavivirus |
| ES2900199T3 (es) | 2017-03-28 | 2022-03-16 | Bayer Ag | Novedosos compuestos macrocíclicos inhibidores de PTEFB |
| CA3057891A1 (en) | 2017-03-28 | 2018-10-04 | Bayer Aktiengesellschaft | Novel ptefb inhibiting macrocyclic compounds |
| WO2019075011A1 (en) | 2017-10-10 | 2019-04-18 | Florida State University Research Foundation, Inc. | EMETIC COMPOUNDS FOR THE TREATMENT AND PREVENTION OF FLAVIVIRUS INFECTION |
| CN111417395A (zh) | 2017-10-30 | 2020-07-14 | 艾普托斯生物科学公司 | 用于治疗癌症的芳基咪唑 |
| SG11202006470RA (en) | 2018-02-13 | 2020-08-28 | Bayer Ag | Use of 5-fluoro-4-(4-fluoro-2-methoxyphenyl)-n-{4-[(s-methylsulfonimidoyl)methyl]pyridin-2-yl}pyridin-2-amine for treating diffuse large b-cell lymphoma |
| JPWO2020235672A1 (enExample) * | 2019-05-23 | 2020-11-26 | ||
| US12029718B2 (en) | 2021-11-09 | 2024-07-09 | Cct Sciences, Llc | Process for production of essentially pure delta-9-tetrahydrocannabinol |
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| CA2401748A1 (en) | 2000-03-29 | 2001-10-04 | Cyclacel Limited | 2-substituted 4-heteroaryl-pyrimidines and their use in the treatment of proliferative disorders |
| EP1373257B9 (en) | 2001-03-29 | 2008-10-15 | Vertex Pharmaceuticals Incorporated | Inhibitors of c-jun n-terminal kinases (jnk) and other protein kinases |
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| US20040106647A1 (en) | 2002-06-28 | 2004-06-03 | Schneider Michael D. | Modulators of Cdk9 as a therapeutic target in cardiac hypertrophy |
| US7576085B2 (en) | 2002-09-23 | 2009-08-18 | Schering Corporation | Imidazopyrazines as cyclin dependent kinase inhibitors |
| US7419984B2 (en) * | 2002-10-17 | 2008-09-02 | Cell Therapeutics, Inc. | Pyrimidines and uses thereof |
| AU2003285007A1 (en) | 2002-10-30 | 2004-06-07 | Merck & Co., Inc. | Kinase inhibitors |
| JP2006528640A (ja) | 2003-07-22 | 2006-12-21 | ニューロジェン・コーポレーション | 置換ピリジン−２−イルアミン類縁体 |
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| US8084457B2 (en) | 2003-09-15 | 2011-12-27 | Lead Discovery Center Gmbh | Pharmaceutically active 4,6-disubstituted aminopyrimidine derivatives as modulators of protein kinases |
| CA2553513A1 (en) | 2004-01-22 | 2005-08-04 | Altana Pharma Ag | N-4-(6- (heteo) aryl-pyrimidin-4-ylaminophenyl) -bezenesulfonamides as kinase inhibitors |
| TW200614993A (en) | 2004-06-11 | 2006-05-16 | Akzo Nobel Nv | 4-phenyl-pyrimidine-2-carbonitrile derivatives |
| WO2006125616A2 (en) * | 2005-05-25 | 2006-11-30 | Ingenium Pharmaceuticals Ag | Pyrimidine-based cdk inhibitors for treating pain |
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| ES2539518T3 (es) * | 2007-04-24 | 2015-07-01 | Astrazeneca Ab | Inhibidores de proteínas quinasas |
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| WO2008129080A1 (en) | 2008-10-30 |
| EP2137166A1 (en) | 2009-12-30 |
| JP2010525025A (ja) | 2010-07-22 |
| EP2137166B1 (en) | 2012-05-30 |
| US8507498B2 (en) | 2013-08-13 |
| US20130338147A1 (en) | 2013-12-19 |
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