JP2017505762A5 - - Google Patents

Download PDF

Info

Publication number: JP2017505762A5
Authority: JP; Japan
Prior art keywords: optionally substituted; alkyl; methyl; substituted; cycloalkyl
Prior art date: 2014-12-23
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

Application number

JP2016542692A

Other languages

English (en)

Japanese (ja)

Other versions

JP6466456B2 (ja

JP2017505762A (ja

Filing date

2014-12-23

Publication date

2017-12-21

2014-12-23 Application filed filed Critical

2014-12-23 Priority claimed from PCT/US2014/072031 external-priority patent/WO2015100282A1/en

2017-02-23 Publication of JP2017505762A publication Critical patent/JP2017505762A/ja

2017-12-21 Publication of JP2017505762A5 publication Critical patent/JP2017505762A5/ja

2019-02-06 Application granted granted Critical

2019-02-06 Publication of JP6466456B2 publication Critical patent/JP6466456B2/ja

Status Active legal-status Critical Current

2034-12-23 Anticipated expiration legal-status Critical

Links

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

JP2016542692A 2013-12-24 2014-12-23 抗がん剤としての三環式化合物 Active JP6466456B2 (ja)

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 (2)	2017-12-21
JP6466456B2 JP6466456B2 (ja)	2019-02-06

Family

ID=52293305

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 (2)
EP (2)	EP3466949B1 (2)
JP (2)	JP6466456B2 (2)
KR (1)	KR102457145B1 (2)
CN (2)	CN108558871B (2)
AR (2)	AR099379A1 (2)
AU (1)	AU2014369982B2 (2)
BR (1)	BR112016013744B1 (2)
CA (1)	CA2934953C (2)
CL (1)	CL2016001629A1 (2)
CY (2)	CY1121076T1 (2)
DK (2)	DK3087071T3 (2)
EA (2)	EA201990240A1 (2)
ES (2)	ES2857848T3 (2)
HR (2)	HRP20181849T1 (2)
HU (2)	HUE041719T2 (2)
IL (1)	IL246359B (2)
LT (2)	LT3466949T (2)
MA (1)	MA39211B1 (2)
MX (1)	MX369491B (2)
MY (1)	MY176489A (2)
NZ (1)	NZ722326A (2)
PE (1)	PE20160844A1 (2)
PH (1)	PH12016500953A1 (2)
PL (2)	PL3087071T3 (2)
PT (2)	PT3087071T (2)
RS (2)	RS61479B1 (2)
SG (1)	SG11201605097SA (2)
SI (2)	SI3466949T1 (2)
SM (2)	SMT202100165T1 (2)
TN (1)	TN2016000238A1 (2)
TW (2)	TWI726544B (2)
UY (1)	UY35916A (2)
WO (1)	WO2015100282A1 (2)

Families Citing this family (31)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
CN105189488B (zh)	2013-02-27	2018-07-24	百时美施贵宝公司	用作溴区结构域抑制剂的咔唑化合物
CA2929652A1 (en)	2013-11-08	2015-05-14	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
ES2857848T3 (es) *	2013-12-24	2021-09-29	Bristol Myers Squibb Co	Compuestos tricíclicos como agentes antineoplásicos
US9580430B2 (en) *	2014-02-28	2017-02-28	The Regents Of The University Of Michigan	9H-pyrimido[4,5-B]indoles and related analogs as BET bromodomain inhibitors
EP3307740B1 (en)	2015-05-12	2019-12-18	Bristol-Myers Squibb Company	5h-pyrido[3,2-b]indole compounds as anticancer agents
US9725449B2 (en)	2015-05-12	2017-08-08	Bristol-Myers Squibb Company	Tricyclic compounds as anticancer agents
CN116059219A (zh)	2015-07-16	2023-05-05	比奥克斯塞尔医疗股份有限公司	一种使用免疫调节治疗癌症的新颖方法
BR112018006689A2 (pt) *	2015-10-02	2018-10-09	Dana Farber Cancer Inst Inc	terapia de combinação de inibidores de bromodomínio e bloqueio de ponto de controle
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
KR102238012B1 (ko) *	2016-01-20	2021-04-09	닝보 웬다 파르마 테크놀로지 엘티디	브로모도메인 억제제인 카르볼린 유도체
CN108770356A (zh) *	2016-02-05	2018-11-06	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
WO2017151613A1 (en) *	2016-03-01	2017-09-08	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
CA3045855A1 (en)	2016-11-10	2018-05-17	Shandong Luoxin Pharmaceutical Group Stock Co., Ltd.	Nitrogenous macrocyclic compound, preparation method therefor, pharmaceutical composition and application thereof
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
CN111356695B (zh) *	2017-10-27	2022-12-30	北京加科思新药研发有限公司	新的三环化合物
SG11202012819YA (en)	2018-06-25	2021-01-28	Jacobio Pharmaceuticals Co Ltd	Tricyclic compounds
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
US11389432B2 (en)	2018-12-19	2022-07-19	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
WO2020200284A1 (zh) *	2019-04-04	2020-10-08	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
TW202126638A (zh)	2019-09-30	2021-07-16	日商協和麒麟股份有限公司	Bet分解劑
US12129265B2 (en)	2020-07-21	2024-10-29	Ankh Life Sciences Limited	Therapeutic agents and uses thereof
CA3206066A1 (en) *	2021-01-22	2022-07-28	Jingrui Biopharma Co., Ltd.	Tricyclic compounds as anticancer agents
MX2023009858A (es) *	2021-02-25	2023-09-12	Impact Biomedicines Inc	Uso de inhibidores de proteina de bromodominio y motivo extraterminal (bet) solo o en combinacion con fedratinib o ruxolitinib como tratamiento para una malignidad hematologica tal como la mielofibrosis.
US12016847B2 (en) *	2021-03-12	2024-06-25	Bristol-Myers Squibb Company	Methods of treating prostate cancer
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)

* Cited by examiner, † Cited by third party
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
CA2542682A1 (en)	2003-10-18	2005-05-06	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
AU2006230099B2 (en)	2005-03-25	2012-04-19	Gitr, Inc.	GITR binding molecules and uses therefor
GB0507298D0 (en)	2005-04-11	2005-05-18	Novartis Ag	Organic compounds
PL1879573T3 (pl)	2005-05-10	2013-05-31	Incyte Holdings Corp	Modulatory 2,3-dioksygenazy indoloaminy i sposoby ich zastosowania
CN104356236B (zh)	2005-07-01	2020-07-03	E.R.施贵宝&圣斯有限责任公司	抗程序性死亡配体1(pd-l1)的人单克隆抗体
CA2634198C (en)	2005-12-20	2014-06-03	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
ES2444574T3 (es)	2006-09-19	2014-02-25	Incyte Corporation	N-hidroxiamidinoheterociclos como moduladores de la indolamina 2,3-dioxigenasa
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
ES2776406T3 (es)	2007-07-12	2020-07-30	Gitr Inc	Terapias de combinación que emplean moléculas de enlazamiento a GITR
EP2044949A1 (en)	2007-10-05	2009-04-08	Immutep	Use of recombinant lag-3 or the derivatives thereof for eliciting monocyte immune response
JP5583592B2 (ja)	2007-11-30	2014-09-03	ニューリンクジェネティクスコーポレイション	Ｉｄｏ阻害剤
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
AU2009333580B2 (en)	2008-12-09	2016-07-07	Genentech, Inc.	Anti-PD-L1 antibodies and their use to enhance T-cell function
US8815840B2 (en) *	2008-12-19	2014-08-26	Bristol-Myers Squibb Company	Carbazole and carboline kinase inhibitors
EP2473531A4 (en)	2009-09-03	2013-05-01	Merck Sharp & Dohme	Anti-gitr antibodies
US8722720B2 (en)	2009-10-28	2014-05-13	Newlink Genetics Corporation	Imidazole derivatives as IDO inhibitors
PH12012500881A1 (en)	2009-12-10	2017-07-26	Hoffmann La Roche	Antibodies binding preferentially human csf1r extracellular domain 4 and their use
UY33246A (es)	2010-02-26	2011-09-30	Boehringer Ingelheim Int	Tienopirimidinas que contienen cicloalquilo para composiciones farmacéuticas
JP5998060B2 (ja)	2010-03-04	2016-09-28	マクロジェニクス，インコーポレーテッド	Ｂ７−ｈ３と反応性のある抗体、その免疫学的に活性なフラグメントおよびその使用
CA2789076C (en)	2010-03-05	2017-11-21	F. Hoffmann-La Roche Ag	Antibodies against human colony stimulating factor-1 receptor and uses thereof
CN102918061B (zh)	2010-03-05	2016-06-08	霍夫曼-拉罗奇有限公司	针对人csf-1r的抗体及其用途
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
MX378336B (es)	2010-05-04	2025-03-10	Five Prime Therapeutics Inc	Anticuerpos que se unen a factor estimulante de colonias 1 (csf1r).
US8933072B2 (en)	2010-06-16	2015-01-13	Vitae Pharmaceuticals, Inc.	Substituted 5-,6- and 7-membered heterocycles, medicaments containing such compounds, and their use
PT2614082T (pt)	2010-09-09	2018-12-03	Pfizer	Moléculas de ligação a 4-1bb
CN103313989B (zh) *	2010-12-16	2016-05-04	霍夫曼-拉罗奇有限公司	三环pi3k抑制剂化合物和使用方法
US8580399B2 (en) *	2011-04-08	2013-11-12	Universal Display Corporation	Substituted oligoazacarbazoles for light emitting diodes
NO2694640T3 (2)	2011-04-15	2018-03-17
KR101970025B1 (ko)	2011-04-20	2019-04-17	메디뮨 엘엘씨	Ｂ7-ｈ1 및 ｐｄ-1과 결합하는 항체 및 다른 분자들
JP6012611B2 (ja) *	2011-09-28	2016-10-25	出光興産株式会社	有機エレクトロルミネッセンス素子用材料及びそれを用いた有機エレクトロルミネッセンス素子
HRP20201595T1 (hr)	2011-11-28	2020-12-11	Merck Patent Gmbh	Anti-pd-l1 protutijela i njihova uporaba
BR112014012624A2 (pt)	2011-12-15	2018-10-09	F Hoffmann-La Roche Ag	anticorpos, composição farmacêutica, ácido nucleico, vetores de expressão, célula hospedeira, método para a produção de um anticorpo recombinante e uso do anticorpo
RU2014136332A (ru)	2012-02-06	2016-03-27	Дженентек, Инк.	Композиции и способы применения ингибиторов csf1r
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
EP2847220A1 (en)	2012-05-11	2015-03-18	Five Prime Therapeutics, Inc.	Methods of treating conditions with antibodies that bind colony stimulating factor 1 receptor (csf1r)
AR091649A1 (es)	2012-07-02	2015-02-18	Bristol Myers Squibb Co	Optimizacion de anticuerpos que se fijan al gen de activacion de linfocitos 3 (lag-3) y sus usos
CN107759690A (zh)	2012-08-31	2018-03-06	戊瑞治疗有限公司	用结合群落刺激因子1受体(csf1r)的抗体治疗病状的方法
UA115576C2 (uk) *	2012-12-06	2017-11-27	Байєр Фарма Акцієнгезелльшафт	Похідні бензимідазолу як антагоністи ер4
US9492460B2 (en) *	2013-02-27	2016-11-15	Bristol-Myers Squibb Company	Carbazole compounds useful as bromodomain inhibitors
CN105189488B (zh) *	2013-02-27	2018-07-24	百时美施贵宝公司	用作溴区结构域抑制剂的咔唑化合物
EP2970312B1 (en) *	2013-03-11	2017-11-15	The Regents of The University of Michigan	Bet bromodomain inhibitors and therapeutic methods using the same
ES2857848T3 (es) *	2013-12-24	2021-09-29	Bristol Myers Squibb Co	Compuestos tricíclicos como agentes antineoplásicos

2014
- 2014-12-23 ES ES18192207T patent/ES2857848T3/es active Active
- 2014-12-23 PL PL14824743T patent/PL3087071T3/pl unknown
- 2014-12-23 SI SI201431748T patent/SI3466949T1/sl unknown
- 2014-12-23 DK DK14824743.0T patent/DK3087071T3/da active
- 2014-12-23 JP JP2016542692A patent/JP6466456B2/ja active Active
- 2014-12-23 ES ES14824743T patent/ES2698998T3/es active Active
- 2014-12-23 BR BR112016013744-2A patent/BR112016013744B1/pt active IP Right Grant
- 2014-12-23 SI SI201430891T patent/SI3087071T1/sl unknown
- 2014-12-23 LT LTEP18192207.1T patent/LT3466949T/lt unknown
- 2014-12-23 TW TW108146502A patent/TWI726544B/zh not_active IP Right Cessation
- 2014-12-23 PT PT14824743T patent/PT3087071T/pt unknown
- 2014-12-23 UY UY0001035916A patent/UY35916A/es unknown
- 2014-12-23 HR HRP20181849TT patent/HRP20181849T1/hr unknown
- 2014-12-23 EA EA201990240A patent/EA201990240A1/ru unknown
- 2014-12-23 CN CN201810460901.7A patent/CN108558871B/zh active Active
- 2014-12-23 LT LTEP14824743.0T patent/LT3087071T/lt unknown
- 2014-12-23 EA EA201691070A patent/EA032469B1/ru not_active IP Right Cessation
- 2014-12-23 MA MA39211A patent/MA39211B1/fr unknown
- 2014-12-23 WO PCT/US2014/072031 patent/WO2015100282A1/en not_active Ceased
- 2014-12-23 RS RS20210158A patent/RS61479B1/sr unknown
- 2014-12-23 AU AU2014369982A patent/AU2014369982B2/en active Active
- 2014-12-23 TW TW103145061A patent/TWI736517B/zh active
- 2014-12-23 TN TN2016000238A patent/TN2016000238A1/en unknown
- 2014-12-23 HU HUE14824743A patent/HUE041719T2/hu unknown
- 2014-12-23 PL PL18192207T patent/PL3466949T3/pl unknown
- 2014-12-23 CA CA2934953A patent/CA2934953C/en active Active
- 2014-12-23 SM SM20210165T patent/SMT202100165T1/it unknown
- 2014-12-23 PT PT181922071T patent/PT3466949T/pt unknown
- 2014-12-23 MY MYPI2016702341A patent/MY176489A/en unknown
- 2014-12-23 AR ARP140104912A patent/AR099379A1/es active IP Right Grant
- 2014-12-23 DK DK18192207.1T patent/DK3466949T3/da active
- 2014-12-23 KR KR1020167019782A patent/KR102457145B1/ko active Active
- 2014-12-23 CN CN201480076189.0A patent/CN106029663B/zh active Active
- 2014-12-23 SM SM20180643T patent/SMT201800643T1/it unknown
- 2014-12-23 EP EP18192207.1A patent/EP3466949B1/en active Active
- 2014-12-23 RS RS20181319A patent/RS58014B1/sr unknown
- 2014-12-23 SG SG11201605097SA patent/SG11201605097SA/en unknown
- 2014-12-23 EP EP14824743.0A patent/EP3087071B1/en active Active
- 2014-12-23 PE PE2016000945A patent/PE20160844A1/es unknown
- 2014-12-23 NZ NZ72232614A patent/NZ722326A/en not_active IP Right Cessation
- 2014-12-23 US US15/107,652 patent/US20160318928A1/en not_active Abandoned
- 2014-12-23 MX MX2016007928A patent/MX369491B/es active IP Right Grant
- 2014-12-23 HU HUE18192207A patent/HUE054183T2/hu unknown
2016
- 2016-05-24 PH PH12016500953A patent/PH12016500953A1/en unknown
- 2016-06-20 IL IL246359A patent/IL246359B/en active IP Right Grant
- 2016-06-23 CL CL2016001629A patent/CL2016001629A1/es unknown
2018
- 2018-12-04 CY CY181101293T patent/CY1121076T1/el unknown
2019
- 2019-01-09 JP JP2019002078A patent/JP6675501B2/ja active Active
2021
- 2021-02-08 HR HRP20210212TT patent/HRP20210212T8/hr unknown
- 2021-03-17 CY CY20211100226T patent/CY1124061T1/el unknown
- 2021-11-03 AR ARP210103062A patent/AR123996A2/es unknown

Publication	Publication Date	Title
JP2017505762A5 (2)	2017-12-21
JP2018515525A5 (2)	2019-06-13
RU2485114C2 (ru)	2013-06-20	Карбоксамидные соединения и их применение в качестве ингибиторов кальпаинов
JP2020516671A5 (2)	2020-12-17
JP2009534386A5 (2)	2013-09-12
JP2012532931A5 (2)	2014-10-09
RU2019132212A (ru)	2021-05-14	Селективные ингибиторы hdac6
JP2016164184A5 (2)	2016-11-10
RU2020112759A (ru)	2021-10-22	Гетероциклические соединения в качестве ингибиторов PAD
RU2019132155A (ru)	2021-05-13	Ингибиторные соединения
RU2012134306A (ru)	2014-02-27	Азотосодержащие производные гетероарилов
JP2018080173A5 (2)	2019-02-14
JP2016516043A5 (2)	2017-04-13
JP2010533158A5 (2)	2012-08-30
IL263511A (en)	2019-01-31	1h-pyrazolo[4,3-b]pyridines as pde1 inhibitors
JP2016515098A5 (2)	2017-03-30
JP2017008079A5 (2)	2017-03-16
WO2015002754A2 (en)	2015-01-08	Novel bicyclic bromodomain inhibitors
RU2010125121A (ru)	2011-12-27	Биарилзамещенные производные азабициклических алканов
JP2016525075A5 (2)	2017-07-20
RU2017121044A (ru)	2018-12-17	Производные амидотиадиазола в качестве ингибиторов надфн-оксидазы
JP2018524338A5 (2)	2019-07-25
JP2019504901A5 (2)	2020-03-26
JP2019512535A5 (2)	2020-04-23
JP2021500332A5 (2)	2021-10-28