JP2017505762A5 - - Google Patents
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- JP2017505762A5 JP2017505762A5 JP2016542692A JP2016542692A JP2017505762A5 JP 2017505762 A5 JP2017505762 A5 JP 2017505762A5 JP 2016542692 A JP2016542692 A JP 2016542692A JP 2016542692 A JP2016542692 A JP 2016542692A JP 2017505762 A5 JP2017505762 A5 JP 2017505762A5
- Authority
- JP
- Japan
- Prior art keywords
- optionally substituted
- alkyl
- methyl
- substituted
- cycloalkyl
- 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.)
- Granted
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- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 99
- 229910052739 hydrogen Inorganic materials 0.000 claims 59
- 239000001257 hydrogen Substances 0.000 claims 59
- 150000002431 hydrogen Chemical class 0.000 claims 52
- 125000001072 heteroaryl group Chemical group 0.000 claims 42
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 37
- 125000000623 heterocyclic group Chemical group 0.000 claims 30
- 229910052736 halogen Inorganic materials 0.000 claims 29
- 150000002367 halogens Chemical class 0.000 claims 29
- -1 CD 3 Chemical class 0.000 claims 28
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 27
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 25
- 125000003107 substituted aryl group Chemical group 0.000 claims 18
- 150000003839 salts Chemical class 0.000 claims 17
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 16
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 16
- 125000004093 cyano group Chemical group *C#N 0.000 claims 14
- 150000001875 compounds Chemical class 0.000 claims 12
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 10
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 7
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 7
- 238000006243 chemical reaction Methods 0.000 claims 7
- 125000000753 cycloalkyl group Chemical group 0.000 claims 7
- 229910052757 nitrogen Inorganic materials 0.000 claims 7
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 7
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 6
- 125000001188 haloalkyl group Chemical group 0.000 claims 6
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 6
- 206010028980 Neoplasm Diseases 0.000 claims 5
- 125000003118 aryl group Chemical group 0.000 claims 5
- 201000010099 disease Diseases 0.000 claims 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 5
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- 125000000217 alkyl group Chemical group 0.000 claims 4
- 201000011510 cancer Diseases 0.000 claims 4
- 108091005625 BRD4 Proteins 0.000 claims 3
- 102100029895 Bromodomain-containing protein 4 Human genes 0.000 claims 3
- 238000003556 assay Methods 0.000 claims 3
- 229940125763 bromodomain inhibitor Drugs 0.000 claims 3
- 238000002866 fluorescence resonance energy transfer Methods 0.000 claims 3
- 125000001424 substituent group Chemical group 0.000 claims 3
- 125000004198 2-fluorophenyl group Chemical group [H]C1=C([H])C(F)=C(*)C([H])=C1[H] 0.000 claims 2
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 claims 2
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 2
- 102000001805 Bromodomains Human genes 0.000 claims 2
- 108050009021 Bromodomains Proteins 0.000 claims 2
- 206010009944 Colon cancer Diseases 0.000 claims 2
- 208000034578 Multiple myelomas Diseases 0.000 claims 2
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 2
- 206010041067 Small cell lung cancer Diseases 0.000 claims 2
- 208000029742 colonic neoplasm Diseases 0.000 claims 2
- 125000000814 indol-3-yl group Chemical group [H]C1=C([H])C([H])=C2N([H])C([H])=C([*])C2=C1[H] 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 2
- 208000000587 small cell lung carcinoma Diseases 0.000 claims 2
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 2
- BPCOFZMFXLWUCE-XDFJSJKPSA-N (1R)-1-cyclopropyl-1-[3-(3,5-dimethyltriazol-4-yl)-6-fluoro-5-[(S)-(2-fluorophenyl)-(oxan-4-yl)methyl]pyrido[3,2-b]indol-7-yl]ethanol Chemical compound C1(CC1)[C@@](C)(O)C=1C=CC=2C3=C(N(C=2C=1F)[C@@H](C1CCOCC1)C1=C(C=CC=C1)F)C=C(C=N3)C1=C(N=NN1C)C BPCOFZMFXLWUCE-XDFJSJKPSA-N 0.000 claims 1
- MSEKYFJKNKKJIR-QMGDAUJMSA-N (1R)-1-cyclopropyl-1-[6-fluoro-3-[3-methyl-5-(trideuteriomethyl)triazol-4-yl]-5-[(S)-oxan-4-yl(phenyl)methyl]pyrido[3,2-b]indol-7-yl]ethanol Chemical compound C1(CC1)[C@@](C)(O)C=1C=CC=2C3=C(N(C=2C=1F)[C@H](C1=CC=CC=C1)C1CCOCC1)C=C(C=N3)C1=C(N=NN1C)C([2H])([2H])[2H] MSEKYFJKNKKJIR-QMGDAUJMSA-N 0.000 claims 1
- BPCOFZMFXLWUCE-MDSYIZKJSA-N (1R)-1-cyclopropyl-1-[6-fluoro-5-[(S)-(2-fluorophenyl)-(oxan-4-yl)methyl]-3-[3-methyl-5-(trideuteriomethyl)triazol-4-yl]pyrido[3,2-b]indol-7-yl]ethanol Chemical compound C1(CC1)[C@@](C)(O)C=1C=CC=2C3=C(N(C=2C=1F)[C@@H](C1CCOCC1)C1=C(C=CC=C1)F)C=C(C=N3)C1=C(N=NN1C)C([2H])([2H])[2H] BPCOFZMFXLWUCE-MDSYIZKJSA-N 0.000 claims 1
- MSEKYFJKNKKJIR-CEKGIIEHSA-N (1S)-1-cyclopropyl-1-[6-fluoro-3-[3-methyl-5-(trideuteriomethyl)triazol-4-yl]-5-[(S)-oxan-4-yl(phenyl)methyl]pyrido[3,2-b]indol-7-yl]ethanol Chemical compound C1(CC1)[C@](C)(O)C=1C=CC=2C3=C(N(C=2C=1F)[C@H](C1=CC=CC=C1)C1CCOCC1)C=C(C=N3)C1=C(N=NN1C)C([2H])([2H])[2H] MSEKYFJKNKKJIR-CEKGIIEHSA-N 0.000 claims 1
- SSJXIUAHEKJCMH-WDSKDSINSA-N (1s,2s)-cyclohexane-1,2-diamine Chemical compound N[C@H]1CCCC[C@@H]1N SSJXIUAHEKJCMH-WDSKDSINSA-N 0.000 claims 1
- JZTHYZIZUIOGKF-SSEXGKCCSA-N 2-[3-(3,5-dimethyl-1,2-oxazol-4-yl)-5-[(S)-(4-fluorophenyl)-(oxan-4-yl)methyl]pyrido[3,2-b]indol-7-yl]propan-2-ol Chemical compound CC1=C(C(=NO1)C)C1=CC=2N(C=3C=C(C=CC=3C=2N=C1)C(C)(C)O)[C@@H](C1CCOCC1)C1=CC=C(C=C1)F JZTHYZIZUIOGKF-SSEXGKCCSA-N 0.000 claims 1
- LZAPXWCSDTYFNB-SSEXGKCCSA-N 2-[3-(3,5-dimethyl-1,2-oxazol-4-yl)-5-[(S)-oxan-4-yl(phenyl)methyl]pyrido[3,2-b]indol-7-yl]propan-2-ol Chemical compound CC1=C(C(=NO1)C)C1=CC=2N(C=3C=C(C=CC=3C=2N=C1)C(C)(C)O)[C@H](C1=CC=CC=C1)C1CCOCC1 LZAPXWCSDTYFNB-SSEXGKCCSA-N 0.000 claims 1
- BTZFFGCZYGLTFW-UHFFFAOYSA-N 2-[3-(3,5-dimethyltriazol-4-yl)-5-(1,1,1,7,7,7-hexafluoroheptan-4-yl)pyrido[3,2-b]indol-7-yl]propan-2-ol Chemical compound CC=1N=NN(C=1C1=CC=2N(C=3C=C(C=CC=3C=2N=C1)C(C)(C)O)C(CCC(F)(F)F)CCC(F)(F)F)C BTZFFGCZYGLTFW-UHFFFAOYSA-N 0.000 claims 1
- RURNTLSPMSYZJR-QFIPXVFZSA-N 2-[3-(3,5-dimethyltriazol-4-yl)-5-[(1S)-4,4,4-trifluoro-1-phenylbutyl]pyrido[3,2-b]indol-7-yl]propan-2-ol Chemical compound CC=1N=NN(C=1C1=CC=2N(C=3C=C(C=CC=3C=2N=C1)C(C)(C)O)[C@@H](CCC(F)(F)F)C1=CC=CC=C1)C RURNTLSPMSYZJR-QFIPXVFZSA-N 0.000 claims 1
- KGERZPVQIRYWRK-GDLZYMKVSA-N 2-[3-(3,5-dimethyltriazol-4-yl)-5-[(S)-oxan-4-yl(phenyl)methyl]pyrido[3,2-b]indol-7-yl]propan-2-ol Chemical compound CC=1N=NN(C=1C1=CC=2N(C=3C=C(C=CC=3C=2N=C1)C(C)(C)O)[C@H](C1=CC=CC=C1)C1CCOCC1)C KGERZPVQIRYWRK-GDLZYMKVSA-N 0.000 claims 1
- UWIXBDZWGJDKJL-MUUNZHRXSA-N 2-[3-(3,5-dimethyltriazol-4-yl)-6-fluoro-5-[(S)-oxan-4-yl(phenyl)methyl]pyrido[3,2-b]indol-7-yl]propan-2-amine Chemical compound CC=1N=NN(C=1C1=CC=2N(C=3C(=C(C=CC=3C=2N=C1)C(C)(C)N)F)[C@H](C1=CC=CC=C1)C1CCOCC1)C UWIXBDZWGJDKJL-MUUNZHRXSA-N 0.000 claims 1
- OYOOOLZFBKNGEJ-MUUNZHRXSA-N 2-[3-(3,5-dimethyltriazol-4-yl)-6-fluoro-5-[(S)-oxan-4-yl(phenyl)methyl]pyrido[3,2-b]indol-7-yl]propan-2-ol Chemical compound CC=1N=NN(C=1C1=CC=2N(C=3C(=C(C=CC=3C=2N=C1)C(C)(C)O)F)[C@H](C1=CC=CC=C1)C1CCOCC1)C OYOOOLZFBKNGEJ-MUUNZHRXSA-N 0.000 claims 1
- FUDZXYQEMRWJGN-HHHXNRCGSA-N 2-[3-(5-methoxy-3-methyltriazol-4-yl)-5-[(S)-oxan-4-yl(phenyl)methyl]pyrido[3,2-b]indol-7-yl]propan-2-ol Chemical compound COC=1N=NN(C=1C1=CC=2N(C=3C=C(C=CC=3C=2N=C1)C(C)(C)O)[C@H](C1=CC=CC=C1)C1CCOCC1)C FUDZXYQEMRWJGN-HHHXNRCGSA-N 0.000 claims 1
- KGERZPVQIRYWRK-GNUZTRDVSA-N 2-[3-[3-methyl-5-(trideuteriomethyl)triazol-4-yl]-5-[(S)-oxan-4-yl(phenyl)methyl]pyrido[3,2-b]indol-7-yl]propan-2-ol Chemical compound C(C=1N=NN(C=1C1=CC=2N(C=3C=C(C=CC=3C=2N=C1)C(C)(C)O)[C@H](C1=CC=CC=C1)C1CCOCC1)C)([2H])([2H])[2H] KGERZPVQIRYWRK-GNUZTRDVSA-N 0.000 claims 1
- RMQALCZQOUJTEN-MUUNZHRXSA-N 2-[3-[5-(hydroxymethyl)-3-methyltriazol-4-yl]-5-[(S)-oxan-4-yl(phenyl)methyl]pyrido[3,2-b]indol-7-yl]propan-2-ol Chemical compound OCC=1N=NN(C=1C1=CC=2N(C=3C=C(C=CC=3C=2N=C1)C(C)(C)O)[C@H](C1=CC=CC=C1)C1CCOCC1)C RMQALCZQOUJTEN-MUUNZHRXSA-N 0.000 claims 1
- DVGOMSURZGWXJT-GNUZTRDVSA-N 2-[5-[(S)-(4,4-difluorocyclohexyl)-phenylmethyl]-3-[3-methyl-5-(trideuteriomethyl)triazol-4-yl]pyrido[3,2-b]indol-7-yl]propan-2-ol Chemical compound FC1(CCC(CC1)[C@H](N1C2=C(C=3C=CC(=CC1=3)C(C)(C)O)N=CC(=C2)C1=C(N=NN1C)C([2H])([2H])[2H])C1=CC=CC=C1)F DVGOMSURZGWXJT-GNUZTRDVSA-N 0.000 claims 1
- PUHMOBALEOWSMA-HHHXNRCGSA-N 3-(3,5-dimethyltriazol-4-yl)-6-methylsulfonyl-5-[(S)-oxan-4-yl(phenyl)methyl]pyrido[3,2-b]indole Chemical compound CS(=O)(=O)C1=CC=CC=2C3=C(N(C1=2)[C@H](C1=CC=CC=C1)C1CCOCC1)C=C(C=N3)C1=C(N=NN1C)C PUHMOBALEOWSMA-HHHXNRCGSA-N 0.000 claims 1
- WMGCUONRPGLRCM-GDLZYMKVSA-N 3-(3,5-dimethyltriazol-4-yl)-7-(methylsulfonylmethyl)-5-[(S)-oxan-4-yl(phenyl)methyl]pyrido[3,2-b]indole Chemical compound Cc1nnn(C)c1-c1cnc2c(c1)n([C@@H](C1CCOCC1)c1ccccc1)c1cc(CS(C)(=O)=O)ccc21 WMGCUONRPGLRCM-GDLZYMKVSA-N 0.000 claims 1
- NWGRIRJJSNFTFM-MUUNZHRXSA-N 3-(3,5-dimethyltriazol-4-yl)-9-methoxy-6-methylsulfonyl-5-[(S)-oxan-4-yl(phenyl)methyl]pyrido[3,2-b]indole Chemical compound CS(=O)(=O)C1=CC=C(C=2C3=C(N(C1=2)[C@H](C1=CC=CC=C1)C1CCOCC1)C=C(C=N3)C1=C(N=NN1C)C)OC NWGRIRJJSNFTFM-MUUNZHRXSA-N 0.000 claims 1
- HQGZYVXIERSSDA-MUUNZHRXSA-N 3-(3,5-dimethyltriazol-4-yl)-9-methylsulfonyl-5-[(S)-oxan-4-yl(phenyl)methyl]pyrido[3,2-b]indole Chemical compound CS(=O)(=O)C=1C=2C3=C(N(C=2C=CC=1)[C@H](C1=CC=CC=C1)C1CCOCC1)C=C(C=N3)C1=C(N=NN1C)C HQGZYVXIERSSDA-MUUNZHRXSA-N 0.000 claims 1
- RLXUBJLRVMWJTK-AREMUKBSSA-N 3-(5-methoxy-3-methyltriazol-4-yl)-7-methylsulfonyl-5-[(S)-oxan-4-yl(phenyl)methyl]pyrido[3,2-b]indole Chemical compound CS(=O)(=O)C=1C=CC=2C3=C(N(C=2C=1)[C@H](C1=CC=CC=C1)C1CCOCC1)C=C(C=N3)C1=C(N=NN1C)OC RLXUBJLRVMWJTK-AREMUKBSSA-N 0.000 claims 1
- YJMAADZMFJXYOJ-MZHKYADFSA-N 5-[(R)-(4,4-difluorocyclohexyl)-(3-fluoropyridin-2-yl)methyl]-9-fluoro-7-methylsulfonyl-3-[3-methyl-5-(trideuteriomethyl)triazol-4-yl]pyrido[3,2-b]indole Chemical compound FC1(CCC(CC1)[C@H](C1=NC=CC=C1F)N1C2=C(C=3C(=CC(=CC1=3)S(=O)(=O)C)F)N=CC(=C2)C1=C(N=NN1C)C([2H])([2H])[2H])F YJMAADZMFJXYOJ-MZHKYADFSA-N 0.000 claims 1
- UJSHFOHIUINCFM-MLBVKCQFSA-N 5-[(S)-(4-fluorophenyl)-(oxan-4-yl)methyl]-7-methylsulfonyl-3-[3-methyl-5-(trideuteriomethyl)triazol-4-yl]pyrido[3,2-b]indole Chemical compound FC1=CC=C(C=C1)[C@@H](N1C2=C(C=3C=CC(=CC1=3)S(=O)(=O)C)N=CC(=C2)C1=C(N=NN1C)C([2H])([2H])[2H])C1CCOCC1 UJSHFOHIUINCFM-MLBVKCQFSA-N 0.000 claims 1
- GGUNMQZRJAUVAP-MLBVKCQFSA-N 9-fluoro-7-methylsulfonyl-3-[3-methyl-5-(trideuteriomethyl)triazol-4-yl]-5-[(S)-oxan-4-yl(phenyl)methyl]pyrido[3,2-b]indole Chemical compound [2H]C([2H])([2H])C1=C(N(C)N=N1)C1=CC2=C(N=C1)C1=C(F)C=C(C=C1N2[C@@H](C1CCOCC1)C1=CC=CC=C1)S(C)(=O)=O GGUNMQZRJAUVAP-MLBVKCQFSA-N 0.000 claims 1
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims 1
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 1
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 claims 1
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 1
- VPTJTZKWJIHVPF-SSEXGKCCSA-N N-[2-[3-(3,5-dimethyltriazol-4-yl)-6-fluoro-5-[(S)-oxan-4-yl(phenyl)methyl]pyrido[3,2-b]indol-7-yl]propan-2-yl]acetamide Chemical compound CC=1N=NN(C=1C1=CC=2N(C=3C(=C(C=CC=3C=2N=C1)C(C)(C)NC(C)=O)F)[C@H](C1=CC=CC=C1)C1CCOCC1)C VPTJTZKWJIHVPF-SSEXGKCCSA-N 0.000 claims 1
- UIWQTEYTWQYNMF-GDLZYMKVSA-N N-[2-[3-(3,5-dimethyltriazol-4-yl)-6-fluoro-5-[(S)-oxan-4-yl(phenyl)methyl]pyrido[3,2-b]indol-7-yl]propan-2-yl]methanesulfonamide Chemical compound CC=1N=NN(C=1C1=CC=2N(C=3C(=C(C=CC=3C=2N=C1)C(C)(C)NS(=O)(=O)C)F)[C@H](C1=CC=CC=C1)C1CCOCC1)C UIWQTEYTWQYNMF-GDLZYMKVSA-N 0.000 claims 1
- UBWXNTKYRHDOQL-SSEXGKCCSA-N N-[3-(3,5-dimethyltriazol-4-yl)-6-methylsulfonyl-5-[(S)-oxan-4-yl(phenyl)methyl]pyrido[3,2-b]indol-9-yl]cyclopropanesulfonamide Chemical compound CC=1N=NN(C=1C1=CC=2N(C=3C(=CC=C(C=3C=2N=C1)NS(=O)(=O)C1CC1)S(=O)(=O)C)[C@H](C1=CC=CC=C1)C1CCOCC1)C UBWXNTKYRHDOQL-SSEXGKCCSA-N 0.000 claims 1
- 206010029260 Neuroblastoma Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 239000013543 active substance Substances 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 201000005787 hematologic cancer Diseases 0.000 claims 1
- 208000024200 hematopoietic and lymphoid system neoplasm Diseases 0.000 claims 1
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 1
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 201000007270 liver cancer Diseases 0.000 claims 1
- 208000014018 liver neoplasm Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- WDHSXBMZTHNROU-GDLZYMKVSA-N methyl N-[2-[3-(3,5-dimethyltriazol-4-yl)-6-fluoro-5-[(S)-oxan-4-yl(phenyl)methyl]pyrido[3,2-b]indol-7-yl]propan-2-yl]carbamate Chemical compound CC=1N=NN(C=1C1=CC=2N(C=3C(=C(C=CC=3C=2N=C1)C(C)(C)NC(OC)=O)F)[C@H](C1=CC=CC=C1)C1CCOCC1)C WDHSXBMZTHNROU-GDLZYMKVSA-N 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 229940127557 pharmaceutical product Drugs 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 0 *c1c[n](*)nc1 Chemical compound *c1c[n](*)nc1 0.000 description 16
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361920500P | 2013-12-24 | 2013-12-24 | |
| US61/920,500 | 2013-12-24 | ||
| PCT/US2014/072031 WO2015100282A1 (en) | 2013-12-24 | 2014-12-23 | Tricyclic compounds as anticancer agents |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019002078A Division JP6675501B2 (ja) | 2013-12-24 | 2019-01-09 | 抗がん剤としての三環式化合物 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017505762A JP2017505762A (ja) | 2017-02-23 |
| JP2017505762A5 true JP2017505762A5 (OSRAM) | 2017-12-21 |
| JP6466456B2 JP6466456B2 (ja) | 2019-02-06 |
Family
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Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016542692A Active JP6466456B2 (ja) | 2013-12-24 | 2014-12-23 | 抗がん剤としての三環式化合物 |
| JP2019002078A Active JP6675501B2 (ja) | 2013-12-24 | 2019-01-09 | 抗がん剤としての三環式化合物 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019002078A Active JP6675501B2 (ja) | 2013-12-24 | 2019-01-09 | 抗がん剤としての三環式化合物 |
Country Status (34)
| Country | Link |
|---|---|
| US (1) | US20160318928A1 (OSRAM) |
| EP (2) | EP3087071B1 (OSRAM) |
| JP (2) | JP6466456B2 (OSRAM) |
| KR (1) | KR102457145B1 (OSRAM) |
| CN (2) | CN108558871B (OSRAM) |
| AR (2) | AR099379A1 (OSRAM) |
| AU (1) | AU2014369982B2 (OSRAM) |
| BR (1) | BR112016013744B1 (OSRAM) |
| CA (1) | CA2934953C (OSRAM) |
| CL (1) | CL2016001629A1 (OSRAM) |
| CY (2) | CY1121076T1 (OSRAM) |
| DK (2) | DK3466949T3 (OSRAM) |
| EA (2) | EA032469B1 (OSRAM) |
| ES (2) | ES2857848T3 (OSRAM) |
| HR (2) | HRP20181849T1 (OSRAM) |
| HU (2) | HUE054183T2 (OSRAM) |
| IL (1) | IL246359B (OSRAM) |
| LT (2) | LT3087071T (OSRAM) |
| MA (1) | MA39211B1 (OSRAM) |
| MX (1) | MX369491B (OSRAM) |
| MY (1) | MY176489A (OSRAM) |
| NZ (1) | NZ722326A (OSRAM) |
| PE (1) | PE20160844A1 (OSRAM) |
| PH (1) | PH12016500953A1 (OSRAM) |
| PL (2) | PL3087071T3 (OSRAM) |
| PT (2) | PT3466949T (OSRAM) |
| RS (2) | RS61479B1 (OSRAM) |
| SG (1) | SG11201605097SA (OSRAM) |
| SI (2) | SI3087071T1 (OSRAM) |
| SM (2) | SMT201800643T1 (OSRAM) |
| TN (1) | TN2016000238A1 (OSRAM) |
| TW (2) | TWI726544B (OSRAM) |
| UY (1) | UY35916A (OSRAM) |
| WO (1) | WO2015100282A1 (OSRAM) |
Families Citing this family (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10053454B2 (en) | 2013-02-27 | 2018-08-21 | Bristol-Myers Squibb Company | Carbazole compounds useful as bromodomain inhibitors |
| EP3066101B1 (en) | 2013-11-08 | 2020-07-29 | Dana-Farber Cancer Institute, Inc. | Combination therapy for cancer using bromodomain and extra-terminal (bet) protein inhibitors |
| US9458156B2 (en) | 2014-12-23 | 2016-10-04 | Bristol-Myers Squibb Company | Tricyclic compounds as anticancer agents |
| SMT201800643T1 (it) * | 2013-12-24 | 2019-01-11 | Bristol Myers Squibb Co | Composti triciclici come agenti anticancro |
| CA2940554A1 (en) * | 2014-02-28 | 2015-09-03 | The Regents Of The University Of Michigan | 9h-pyrimido[4,5-b]indoles and related analogs as bet bromodomain inhibitors |
| US9725449B2 (en) | 2015-05-12 | 2017-08-08 | Bristol-Myers Squibb Company | Tricyclic compounds as anticancer agents |
| US10174024B2 (en) | 2015-05-12 | 2019-01-08 | Bristol-Myers Squibb Company | 5H-pyrido[3,2-B]indole compounds as anticancer agents |
| NZ739503A (en) * | 2015-07-16 | 2023-06-30 | Bioxcel Therapeutics Inc | A novel approach for treatment of cancer using immunomodulation |
| MA43037A (fr) * | 2015-10-02 | 2018-08-08 | Dana Farber Cancer Inst Inc | Polythérapie par inhibiteurs de bromodomaine et blocage de point de contrôle |
| WO2017124934A1 (zh) * | 2016-01-20 | 2017-07-27 | 宁波文达医药科技有限公司 | 作为布罗莫区结构域抑制剂的含膦咔啉衍生物 |
| CN108137589B (zh) * | 2016-01-20 | 2021-03-26 | 宁波文达医药科技有限公司 | 作为布罗莫区结构域抑制剂的咔啉衍生物 |
| WO2017133681A1 (zh) * | 2016-02-05 | 2017-08-10 | 正大天晴药业集团股份有限公司 | 溴区结构域蛋白抑制剂的三环类化合物及其制备、药物组合物和用途 |
| SG11201807421TA (en) | 2016-03-01 | 2018-09-27 | Corcept Therapeutics Inc | The use of glucocorticoid receptor modulators to potentiate checkpoint inhibitors |
| US10150754B2 (en) * | 2016-04-19 | 2018-12-11 | Celgene Quanticel Research, Inc. | Histone demethylase inhibitors |
| EP3539960A4 (en) | 2016-11-10 | 2020-03-18 | Luoxin Pharmaceutical (Shanghai) Co., Ltd. | NITROGEN MACROCYCLIC COMPOUND, ITS PREPARATION METHOD, ITS PHARMACEUTICAL COMPOSITION AND ITS APPLICATION |
| CN109824693B (zh) * | 2017-04-18 | 2020-12-08 | 四川大学 | Brd4抑制剂及其在肿瘤治疗药物中的应用 |
| WO2019080941A1 (en) * | 2017-10-27 | 2019-05-02 | Jacobio-Beta Pharmaceuticals Co., Ltd. | NEW TRICYCLIC COMPOUNDS |
| CN112513041B (zh) * | 2018-06-25 | 2022-05-10 | 北京加科思新药研发有限公司 | 三环化合物 |
| CN108840868B (zh) * | 2018-08-01 | 2019-10-18 | 上海山的实业有限公司 | 具有抗肿瘤活性的吲哚并吡啶酮类化合物的制备方法及应用 |
| WO2020132046A1 (en) | 2018-12-19 | 2020-06-25 | Corcept Therapeutics Incorporated | Methods of treating cancer comprising administration of a glucocorticoid receptor modulator and a cancer chemotherapy agent |
| US11234971B2 (en) | 2018-12-19 | 2022-02-01 | Corcept Therapeutics Incorporated | Methods of treating cancer comprising administration of a glucocorticoid receptor modulator and a cancer chemotherapy agent |
| CN113544129B (zh) * | 2019-04-04 | 2024-07-23 | 上海华汇拓医药科技有限公司 | 三环类化合物制备方法及其在医药领域的应用 |
| CN110003204B (zh) * | 2019-04-30 | 2020-08-11 | 上海勋和医药科技有限公司 | 一种bet蛋白抑制剂、其制备方法及用途 |
| US10947253B2 (en) | 2019-08-05 | 2021-03-16 | Ankh Life Sciences Limited | Fused polycyclic dimers |
| EP4039333A4 (en) | 2019-09-30 | 2024-02-14 | Kyowa Kirin Co., Ltd. | BET DEGRADATION AGENT |
| US12129265B2 (en) | 2020-07-21 | 2024-10-29 | Ankh Life Sciences Limited | Therapeutic agents and uses thereof |
| JP2024506260A (ja) * | 2021-01-22 | 2024-02-13 | ジンルイ バイオファーマ カンパニー リミテッド | 抗がん剤としての三環式化合物 |
| CA3206708A1 (en) * | 2021-02-25 | 2022-09-01 | Ida ARONCHIK | Use of a bet inhibitor alone or in combination with fedratinib or ruxolitinib for treating a hematological malignancy such as myelofibrosis |
| EP4334286A4 (en) * | 2021-05-06 | 2025-03-19 | Raziel Therapeutics Ltd. | CRYSTALLINE CARBAZOLE DERIVATIVE |
| WO2024099441A1 (en) * | 2022-11-11 | 2024-05-16 | Jingrui Biopharma (Shandong) Co., Ltd. | Bromodomain and extra-terminal (bet) protein degrader |
Family Cites Families (49)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU3427093A (en) * | 1992-01-15 | 1993-08-03 | E.I. Du Pont De Nemours And Company | Bridged heterocyclic fungicides |
| EP1677786A1 (en) | 2003-10-18 | 2006-07-12 | Bayer HealthCare AG | 5-substituted 2-(phenylmethyl)thio-4-phenyl-4h-1,2,4-triazole derivatives and related compounds as gaba-agonists for the treatment of urinary incontinence and related diseases |
| WO2005051318A2 (en) * | 2003-11-24 | 2005-06-09 | Viropharma Incorporated | Compounds, compositions and methods for treatment and prophylaxis of hepatitis c viral infections and associated diseases |
| TWI309240B (en) | 2004-09-17 | 2009-05-01 | Hoffmann La Roche | Anti-ox40l antibodies |
| EP1866339B8 (en) | 2005-03-25 | 2021-12-01 | GITR, Inc. | Gitr binding molecules and uses therefor |
| GB0507298D0 (en) | 2005-04-11 | 2005-05-18 | Novartis Ag | Organic compounds |
| ME02461B (me) | 2005-05-10 | 2017-02-20 | Incyte Holdings Corp | Modulatori indoleamina 2,3-dioksigenaze i metode za upotrebu istih |
| KR101607288B1 (ko) | 2005-07-01 | 2016-04-05 | 이. 알. 스퀴부 앤드 선즈, 엘.엘.씨. | 예정 사멸 리간드 1 (피디-엘1)에 대한 인간 모노클로날 항체 |
| EP1971583B1 (en) | 2005-12-20 | 2015-03-25 | Incyte Corporation | N-hydroxyamidinoheterocycles as modulators of indoleamine 2,3-dioxygenase |
| US7696166B2 (en) | 2006-03-28 | 2010-04-13 | Albany Molecular Research, Inc. | Use of cyclosporin alkyne/alkene analogues for preventing or treating viral-induced disorders |
| US20080125470A1 (en) | 2006-09-19 | 2008-05-29 | Incyte Corporation | N-hydroxyamidinoheterocycles as modulators of indoleamine 2,3-dioxygenase |
| CL2007002650A1 (es) | 2006-09-19 | 2008-02-08 | Incyte Corp | Compuestos derivados de heterociclo n-hidroxiamino; composicion farmaceutica, util para tratar cancer, infecciones virales y desordenes neurodegenerativos entre otras. |
| UY30892A1 (es) | 2007-02-07 | 2008-09-02 | Smithkline Beckman Corp | Inhibidores de la actividad akt |
| EP1987839A1 (en) | 2007-04-30 | 2008-11-05 | I.N.S.E.R.M. Institut National de la Sante et de la Recherche Medicale | Cytotoxic anti-LAG-3 monoclonal antibody and its use in the treatment or prevention of organ transplant rejection and autoimmune disease |
| EP2175884B8 (en) | 2007-07-12 | 2017-02-22 | GITR, Inc. | Combination therapies employing gitr binding molecules |
| EP2044949A1 (en) | 2007-10-05 | 2009-04-08 | Immutep | Use of recombinant lag-3 or the derivatives thereof for eliciting monocyte immune response |
| EP2227233B1 (en) | 2007-11-30 | 2013-02-13 | Newlink Genetics | Ido inhibitors |
| FR2927330B1 (fr) | 2008-02-07 | 2010-02-19 | Sanofi Aventis | Derives de 5,6-bisaryl-2-pyridine-carboxamide, leur preparation et leur application en therapeutique comme antagonistes des recepteurs a l'urotensine ii |
| AR072999A1 (es) | 2008-08-11 | 2010-10-06 | Medarex Inc | Anticuerpos humanos que se unen al gen 3 de activacion linfocitaria (lag-3) y los usos de estos |
| TWI729512B (zh) | 2008-12-09 | 2021-06-01 | 美商建南德克公司 | 抗pd-l1抗體及其於增進t細胞功能之用途 |
| CN102325752B (zh) * | 2008-12-19 | 2015-02-04 | 百时美施贵宝公司 | 咔唑和咔啉激酶抑制剂 |
| CN102574924A (zh) | 2009-09-03 | 2012-07-11 | 先灵公司 | 抗-gitr抗体 |
| EP2493862B1 (en) | 2009-10-28 | 2016-10-05 | Newlink Genetics Corporation | Imidazole derivatives as ido inhibitors |
| PT2949670T (pt) | 2009-12-10 | 2019-05-20 | Hoffmann La Roche | Anticorpos que se ligam preferencialmente ao domínio extracelular 4 do csf1r e respetiva utilização |
| MX2012009735A (es) | 2010-02-26 | 2012-09-12 | Boehringer Ingelheim Int | 4-[cicloalquiloxi (hetero) arilamino] tieno [2,3-d] pirimidinas que tienen actividad inhibitoria de mnk1/mnk2 para composiciones farmaceuticas. |
| NZ705128A (en) | 2010-03-04 | 2015-04-24 | Macrogenics Inc | Antibodies reactive with b7-h3, immunologically active fragments thereof and uses thereof |
| WO2011107553A1 (en) | 2010-03-05 | 2011-09-09 | F. Hoffmann-La Roche Ag | Antibodies against human csf-1r and uses thereof |
| CA2789071C (en) | 2010-03-05 | 2018-03-27 | F. Hoffmann-La Roche Ag | Antibodies against human csf-1r and uses thereof |
| TWI503323B (zh) * | 2010-03-29 | 2015-10-11 | Oncotherapy Science Inc | 三環化合物以及含此化合物之ｐｂｋ抑制劑 |
| CN107011438B (zh) | 2010-05-04 | 2020-11-20 | 戊瑞治疗有限公司 | 结合csf1r的抗体 |
| EP2582698B1 (en) | 2010-06-16 | 2016-09-14 | Vitae Pharmaceuticals, Inc. | Substituted 5-,6- and 7-membered heterocycles, medicaments containing such compounds, and their use |
| SG10201912092VA (en) | 2010-09-09 | 2020-02-27 | Pfizer | 4-1bb binding molecules |
| MX2013006858A (es) * | 2010-12-16 | 2013-07-29 | Hoffmann La Roche | Compuesto triciclicos inhibidores de la pi3k y metodos de uso. |
| US8580399B2 (en) * | 2011-04-08 | 2013-11-12 | Universal Display Corporation | Substituted oligoazacarbazoles for light emitting diodes |
| NO2694640T3 (OSRAM) | 2011-04-15 | 2018-03-17 | ||
| DK2699264T3 (en) | 2011-04-20 | 2018-06-25 | Medimmune Llc | ANTIBODIES AND OTHER MOLECULES BINDING B7-H1 AND PD-1 |
| EP2762477A1 (en) * | 2011-09-28 | 2014-08-06 | Idemitsu Kosan Co., Ltd | Material for organic electroluminescent element, and organic electroluminescent element produced using same |
| KR101981873B1 (ko) | 2011-11-28 | 2019-05-23 | 메르크 파텐트 게엠베하 | 항-ｐｄ-ｌ1 항체 및 그의 용도 |
| RU2658603C2 (ru) | 2011-12-15 | 2018-06-21 | Ф.Хоффманн-Ля Рош Аг | Антитела против человеческого csf-1r и их применения |
| CA2861122A1 (en) | 2012-02-06 | 2013-08-15 | Genentech, Inc. | Compositions and methods for using csf1r inhibitors |
| AR090263A1 (es) | 2012-03-08 | 2014-10-29 | Hoffmann La Roche | Terapia combinada de anticuerpos contra el csf-1r humano y las utilizaciones de la misma |
| AU2012374617B2 (en) | 2012-05-11 | 2015-09-17 | Five Prime Therapeutics, Inc. | Methods of treating conditions with antibodies that bind colony stimulating factor 1 receptor (CSF1R) |
| UY34887A (es) | 2012-07-02 | 2013-12-31 | Bristol Myers Squibb Company Una Corporacion Del Estado De Delaware | Optimización de anticuerpos que se fijan al gen de activación de linfocitos 3 (lag-3) y sus usos |
| SG10201906328RA (en) | 2012-08-31 | 2019-08-27 | Five Prime Therapeutics Inc | Methods of treating conditions with antibodies that bind colony stimulating factor 1 receptor (csf1r) |
| UA115576C2 (uk) * | 2012-12-06 | 2017-11-27 | Байєр Фарма Акцієнгезелльшафт | Похідні бензимідазолу як антагоністи ер4 |
| US10053454B2 (en) * | 2013-02-27 | 2018-08-21 | Bristol-Myers Squibb Company | Carbazole compounds useful as bromodomain inhibitors |
| US9492460B2 (en) * | 2013-02-27 | 2016-11-15 | Bristol-Myers Squibb Company | Carbazole compounds useful as bromodomain inhibitors |
| AU2014249192B2 (en) * | 2013-03-11 | 2017-12-21 | The Regents Of The University Of Michigan | BET bromodomain inhibitors and therapeutic methods using the same |
| SMT201800643T1 (it) * | 2013-12-24 | 2019-01-11 | Bristol Myers Squibb Co | Composti triciclici come agenti anticancro |
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