JP2015532295A5 - - Google Patents
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- JP2015532295A5 JP2015532295A5 JP2015534985A JP2015534985A JP2015532295A5 JP 2015532295 A5 JP2015532295 A5 JP 2015532295A5 JP 2015534985 A JP2015534985 A JP 2015534985A JP 2015534985 A JP2015534985 A JP 2015534985A JP 2015532295 A5 JP2015532295 A5 JP 2015532295A5
- Authority
- JP
- Japan
- Prior art keywords
- cycloalkyl
- alkyl
- aryl
- heteroaryl
- heterocyclyl
- 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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- 125000000217 alkyl group Chemical group 0.000 claims description 82
- 125000003342 alkenyl group Chemical group 0.000 claims description 53
- 125000000304 alkynyl group Chemical group 0.000 claims description 53
- 125000003118 aryl group Chemical group 0.000 claims description 53
- 125000001072 heteroaryl group Chemical group 0.000 claims description 52
- 125000000623 heterocyclic group Chemical group 0.000 claims description 52
- 125000002853 C1-C4 hydroxyalkyl group Chemical group 0.000 claims description 40
- 125000003709 fluoroalkyl group Chemical group 0.000 claims description 40
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 claims description 38
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 30
- 150000001875 compounds Chemical class 0.000 claims description 28
- 125000003545 alkoxy group Chemical group 0.000 claims description 19
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 18
- 229910052736 halogen Inorganic materials 0.000 claims description 14
- 150000002367 halogens Chemical class 0.000 claims description 14
- -1 —N (R 1 ′ ) 2 Chemical group 0.000 claims description 14
- 150000003839 salts Chemical class 0.000 claims description 13
- 239000012453 solvate Substances 0.000 claims description 12
- 125000002947 alkylene group Chemical group 0.000 claims description 10
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims description 10
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims description 9
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims description 9
- 125000004104 aryloxy group Chemical group 0.000 claims description 9
- 125000002993 cycloalkylene group Chemical group 0.000 claims description 9
- 201000010099 disease Diseases 0.000 claims description 9
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 9
- 125000005553 heteroaryloxy group Chemical group 0.000 claims description 9
- 239000000203 mixture Substances 0.000 claims description 9
- 230000001419 dependent effect Effects 0.000 claims description 8
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 5
- 239000008194 pharmaceutical composition Substances 0.000 claims description 5
- 239000003814 drug Substances 0.000 claims description 3
- 238000006467 substitution reaction Methods 0.000 claims description 3
- 239000013543 active substance Substances 0.000 claims description 2
- 239000000969 carrier Substances 0.000 claims description 2
- 239000003085 diluting agent Substances 0.000 claims description 2
- 229940079593 drug Drugs 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 2
- 241000257303 Hymenoptera Species 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 description 9
- 125000004450 alkenylene group Chemical group 0.000 description 8
- 125000004419 alkynylene group Chemical group 0.000 description 8
- 125000000732 arylene group Chemical group 0.000 description 8
- 125000005549 heteroarylene group Chemical group 0.000 description 8
- 125000004122 cyclic group Chemical group 0.000 description 5
- 125000006586 (C3-C10) cycloalkylene group Chemical group 0.000 description 4
- 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 description 4
- 125000005010 perfluoroalkyl group Chemical group 0.000 description 4
- 229940002612 prodrug Drugs 0.000 description 4
- 239000000651 prodrug Substances 0.000 description 4
- 206010028980 Neoplasm Diseases 0.000 description 2
- 201000011510 cancer Diseases 0.000 description 2
- 230000002401 inhibitory effect Effects 0.000 description 2
- 238000000034 method Methods 0.000 description 2
- YGYGASJNJTYNOL-CQSZACIVSA-N 3-[(4r)-2,2-dimethyl-1,1-dioxothian-4-yl]-5-(4-fluorophenyl)-1h-indole-7-carboxamide Chemical compound C1CS(=O)(=O)C(C)(C)C[C@@H]1C1=CNC2=C(C(N)=O)C=C(C=3C=CC(F)=CC=3)C=C12 YGYGASJNJTYNOL-CQSZACIVSA-N 0.000 description 1
- 230000001028 anti-proliverative effect Effects 0.000 description 1
- 230000000259 anti-tumor effect Effects 0.000 description 1
- 239000000824 cytostatic agent Substances 0.000 description 1
- 230000001085 cytostatic effect Effects 0.000 description 1
- 125000002768 hydroxyalkyl group Chemical group 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
- 230000002062 proliferating effect Effects 0.000 description 1
Applications Claiming Priority (9)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261708806P | 2012-10-02 | 2012-10-02 | |
| DKPA201200599 | 2012-10-02 | ||
| DKPA201200599 | 2012-10-02 | ||
| US61/708,806 | 2012-10-02 | ||
| US201361770050P | 2013-02-27 | 2013-02-27 | |
| DKPA201370112 | 2013-02-27 | ||
| US61/770,050 | 2013-02-27 | ||
| DKPA201370112 | 2013-02-27 | ||
| PCT/EP2013/070457 WO2014053491A1 (en) | 2012-10-02 | 2013-10-01 | Inhibitors of histone demethylases |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017214526A Division JP2018016661A (ja) | 2012-10-02 | 2017-11-07 | ヒストン脱メチル化酵素の阻害剤 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015532295A JP2015532295A (ja) | 2015-11-09 |
| JP2015532295A5 true JP2015532295A5 (OSRAM) | 2018-10-04 |
| JP6530313B2 JP6530313B2 (ja) | 2019-06-12 |
Family
ID=52781382
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015534985A Active JP6530313B2 (ja) | 2012-10-02 | 2013-10-01 | ヒストン脱メチル化酵素の阻害剤 |
| JP2017214526A Pending JP2018016661A (ja) | 2012-10-02 | 2017-11-07 | ヒストン脱メチル化酵素の阻害剤 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017214526A Pending JP2018016661A (ja) | 2012-10-02 | 2017-11-07 | ヒストン脱メチル化酵素の阻害剤 |
Country Status (33)
| Country | Link |
|---|---|
| US (3) | US20150203453A1 (OSRAM) |
| EP (3) | EP3023415B1 (OSRAM) |
| JP (2) | JP6530313B2 (OSRAM) |
| KR (1) | KR102160320B1 (OSRAM) |
| CN (2) | CN107434803B (OSRAM) |
| AP (1) | AP2015008389A0 (OSRAM) |
| AU (1) | AU2018200876C1 (OSRAM) |
| BR (1) | BR112015007083A2 (OSRAM) |
| CA (2) | CA3095019C (OSRAM) |
| CL (1) | CL2015000829A1 (OSRAM) |
| CR (1) | CR20150217A (OSRAM) |
| CY (1) | CY1118695T1 (OSRAM) |
| DK (1) | DK2903968T3 (OSRAM) |
| EA (1) | EA030698B1 (OSRAM) |
| ES (2) | ES2654143T3 (OSRAM) |
| HK (1) | HK1215710A1 (OSRAM) |
| HR (1) | HRP20170358T1 (OSRAM) |
| HU (1) | HUE033380T2 (OSRAM) |
| IL (2) | IL237831A (OSRAM) |
| LT (1) | LT2903968T (OSRAM) |
| MD (1) | MD20150043A2 (OSRAM) |
| ME (1) | ME02597B (OSRAM) |
| MX (1) | MX2015003959A (OSRAM) |
| NZ (1) | NZ706635A (OSRAM) |
| PE (1) | PE20150998A1 (OSRAM) |
| PH (2) | PH12015500730A1 (OSRAM) |
| PL (2) | PL3023415T3 (OSRAM) |
| PT (2) | PT2903968T (OSRAM) |
| RS (1) | RS55764B1 (OSRAM) |
| SG (2) | SG10201703682YA (OSRAM) |
| SI (2) | SI2903968T1 (OSRAM) |
| SM (2) | SMT201700109T1 (OSRAM) |
| WO (1) | WO2014053491A1 (OSRAM) |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| PE20150998A1 (es) | 2012-10-02 | 2015-06-29 | Epitherapeutics Aps | Inhibidores de histona demetilasas |
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| AR099890A1 (es) * | 2014-03-31 | 2016-08-24 | Epitherapeutics Aps | Inhibidores de histona demetilasas |
| MA40470A (fr) | 2014-08-27 | 2016-03-03 | Gilead Sciences Inc | Composés et procédés d'inhibition des histones déméthylases |
| JP6723663B2 (ja) * | 2014-09-17 | 2020-07-15 | セルジーン クオンティセル リサーチ，インク． | ヒストンデメチラーゼ阻害剤 |
| EP3453710B1 (en) | 2014-09-17 | 2022-09-21 | Celgene Quanticel Research, Inc. | Histone demethylase inhibitors |
| US10030017B2 (en) | 2014-09-17 | 2018-07-24 | Celgene Quanticel Research, Inc. | Histone demethylase inhibitors |
| MX2017005346A (es) | 2014-10-29 | 2017-08-02 | Dong A St Co Ltd | Nuevos compuestos de piridopirimidinona para modular la actividad catalitica de histona lisina desmetilasas (kdm). |
| US20190100769A1 (en) * | 2014-10-31 | 2019-04-04 | Massachusetts Institute Of Technology | Massively parallel combinatorial genetics for crispr |
| AU2016250099A1 (en) * | 2015-04-14 | 2017-10-12 | Gilead Sciences, Inc. | Methods of treating hepatitis B virus |
| US10206930B2 (en) * | 2015-08-14 | 2019-02-19 | New York University | Methods for treating T-cell acute lymphoblastic leukemia |
| WO2017099829A1 (en) | 2015-12-11 | 2017-06-15 | The General Hospital Corporation | Compositions and methods for treating drug-tolerant glioblastoma |
| JP6883913B2 (ja) | 2015-12-28 | 2021-06-09 | セルジーン クオンティセル リサーチ，インク． | ヒストンデメチラーゼ阻害剤 |
| JP6970681B2 (ja) * | 2016-03-15 | 2021-11-24 | セルジーン クオンティセル リサーチ，インク． | ヒストンデメチラーゼ阻害剤 |
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| ES2826748T3 (es) | 2016-09-02 | 2021-05-19 | Gilead Sciences Inc | Derivados de 4,6-diamino-pirido[3,2-d]pirimidina como moduladores de receptores de tipo Toll |
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