JP2016509047A5 - - Google Patents
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- Publication number
- JP2016509047A5 JP2016509047A5 JP2015558495A JP2015558495A JP2016509047A5 JP 2016509047 A5 JP2016509047 A5 JP 2016509047A5 JP 2015558495 A JP2015558495 A JP 2015558495A JP 2015558495 A JP2015558495 A JP 2015558495A JP 2016509047 A5 JP2016509047 A5 JP 2016509047A5
- Authority
- JP
- Japan
- Prior art keywords
- cycloalkyl
- alkyl
- heteroaryl
- aryl
- alkynyl
- 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 225
- 125000000304 alkynyl group Chemical group 0.000 claims description 175
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 171
- 125000003342 alkenyl group Chemical group 0.000 claims description 162
- 125000001072 heteroaryl group Chemical group 0.000 claims description 145
- 125000000623 heterocyclic group Chemical group 0.000 claims description 145
- 125000003118 aryl group Chemical group 0.000 claims description 141
- 229910052799 carbon Inorganic materials 0.000 claims description 95
- 125000003709 fluoroalkyl group Chemical group 0.000 claims description 81
- 229910052739 hydrogen Inorganic materials 0.000 claims description 81
- 125000002853 C1-C4 hydroxyalkyl group Chemical group 0.000 claims description 74
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 claims description 64
- 150000001875 compounds Chemical class 0.000 claims description 56
- 125000003545 alkoxy group Chemical group 0.000 claims description 45
- 125000004043 oxo group Chemical group O=* 0.000 claims description 42
- 229910052736 halogen Inorganic materials 0.000 claims description 36
- 150000002367 halogens Chemical class 0.000 claims description 36
- 239000000203 mixture Substances 0.000 claims description 35
- -1 heterocyclylene Chemical group 0.000 claims description 34
- 125000002947 alkylene group Chemical group 0.000 claims description 29
- 125000004104 aryloxy group Chemical group 0.000 claims description 27
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 27
- 125000005553 heteroaryloxy group Chemical group 0.000 claims description 27
- 239000000651 prodrug Substances 0.000 claims description 25
- 229940002612 prodrug Drugs 0.000 claims description 25
- 150000003839 salts Chemical class 0.000 claims description 25
- 239000012453 solvate Substances 0.000 claims description 25
- 125000002993 cycloalkylene group Chemical group 0.000 claims description 23
- 125000004419 alkynylene group Chemical group 0.000 claims description 22
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 20
- 125000004432 carbon atom Chemical group C* 0.000 claims description 20
- 239000001257 hydrogen Substances 0.000 claims description 20
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 18
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims description 18
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims description 18
- 125000004450 alkenylene group Chemical group 0.000 claims description 18
- 125000000732 arylene group Chemical group 0.000 claims description 18
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims description 18
- 125000005549 heteroarylene group Chemical group 0.000 claims description 18
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 18
- 125000005010 perfluoroalkyl group Chemical group 0.000 claims description 18
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 17
- 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 17
- 125000004122 cyclic group Chemical group 0.000 claims description 16
- 125000000392 cycloalkenyl group Chemical group 0.000 claims description 14
- 125000003003 spiro group Chemical group 0.000 claims description 11
- 125000006374 C2-C10 alkenyl group Chemical group 0.000 claims description 9
- 229910052757 nitrogen Inorganic materials 0.000 claims description 9
- 125000001424 substituent group Chemical group 0.000 claims description 9
- 238000006467 substitution reaction Methods 0.000 claims description 9
- 230000001419 dependent effect Effects 0.000 claims description 7
- 201000010099 disease Diseases 0.000 claims description 7
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 7
- 239000008194 pharmaceutical composition Substances 0.000 claims description 6
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 claims description 4
- 229910052760 oxygen Inorganic materials 0.000 claims description 4
- KRKNYBCHXYNGOX-UHFFFAOYSA-K Citrate Chemical compound [O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O KRKNYBCHXYNGOX-UHFFFAOYSA-K 0.000 claims description 2
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical class OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 claims description 2
- MUBZPKHOEPUJKR-UHFFFAOYSA-N Oxalic acid Chemical compound OC(=O)C(O)=O MUBZPKHOEPUJKR-UHFFFAOYSA-N 0.000 claims description 2
- 239000013543 active substance Substances 0.000 claims description 2
- 229940072107 ascorbate Drugs 0.000 claims description 2
- 235000010323 ascorbic acid Nutrition 0.000 claims description 2
- 239000011668 ascorbic acid Substances 0.000 claims description 2
- 239000000969 carrier Substances 0.000 claims description 2
- 239000003085 diluting agent Substances 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 7
- 125000006586 (C3-C10) cycloalkylene group Chemical group 0.000 claims 4
- 206010028980 Neoplasm Diseases 0.000 description 3
- 239000003814 drug Substances 0.000 description 2
- 0 **N(*)Cc1nccc(*)c1 Chemical compound **N(*)Cc1nccc(*)c1 0.000 description 1
- 201000011510 cancer Diseases 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 238000000034 method Methods 0.000 description 1
Applications Claiming Priority (15)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361770058P | 2013-02-27 | 2013-02-27 | |
| US201361770065P | 2013-02-27 | 2013-02-27 | |
| US201361770067P | 2013-02-27 | 2013-02-27 | |
| DKPA201370114 | 2013-02-27 | ||
| US61/770,058 | 2013-02-27 | ||
| DKPA201370114 | 2013-02-27 | ||
| DKPA201370113 | 2013-02-27 | ||
| US61/770,067 | 2013-02-27 | ||
| US61/770,065 | 2013-02-27 | ||
| DKPA201370115 | 2013-02-27 | ||
| DKPA201370113 | 2013-02-27 | ||
| DKPA201370115 | 2013-02-27 | ||
| US201461931126P | 2014-01-24 | 2014-01-24 | |
| US61/931,126 | 2014-01-24 | ||
| PCT/EP2014/053674 WO2014131777A1 (en) | 2013-02-27 | 2014-02-26 | Inhibitors of histone demethylases |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018082444A Division JP2018127486A (ja) | 2013-02-27 | 2018-04-23 | ヒストン脱メチル化酵素の阻害剤 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016509047A JP2016509047A (ja) | 2016-03-24 |
| JP2016509047A5 true JP2016509047A5 (Direct) | 2017-03-30 |
| JP6514117B2 JP6514117B2 (ja) | 2019-05-15 |
Family
ID=51427545
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015558495A Active JP6514117B2 (ja) | 2013-02-27 | 2014-02-26 | ヒストン脱メチル化酵素の阻害剤 |
| JP2018082444A Withdrawn JP2018127486A (ja) | 2013-02-27 | 2018-04-23 | 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 |
|---|---|---|---|
| JP2018082444A Withdrawn JP2018127486A (ja) | 2013-02-27 | 2018-04-23 | ヒストン脱メチル化酵素の阻害剤 |
Country Status (23)
| Country | Link |
|---|---|
| US (2) | US9650339B2 (Direct) |
| EP (2) | EP2961736B1 (Direct) |
| JP (2) | JP6514117B2 (Direct) |
| KR (1) | KR102229992B1 (Direct) |
| CN (1) | CN105263906B (Direct) |
| AP (1) | AP2015008676A0 (Direct) |
| AU (2) | AU2014222756B2 (Direct) |
| BR (1) | BR112015020650A2 (Direct) |
| CA (1) | CA2901022C (Direct) |
| CL (1) | CL2015002394A1 (Direct) |
| CR (1) | CR20150507A (Direct) |
| EA (1) | EA030451B1 (Direct) |
| ES (1) | ES2670864T3 (Direct) |
| IL (1) | IL240439A0 (Direct) |
| MD (1) | MD20150085A2 (Direct) |
| MX (1) | MX2015011097A (Direct) |
| PE (1) | PE20151667A1 (Direct) |
| PH (1) | PH12015501868A1 (Direct) |
| PL (1) | PL2961736T3 (Direct) |
| SG (2) | SG11201506717UA (Direct) |
| SI (1) | SI2961736T1 (Direct) |
| TR (1) | TR201808599T4 (Direct) |
| WO (1) | WO2014131777A1 (Direct) |
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| TR201808599T4 (tr) | 2013-02-27 | 2018-07-23 | Gilead Sciences Inc | Histon demetilaz inhibitörleri. |
| 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 |
| BR112017008312A2 (pt) | 2014-10-29 | 2017-12-19 | Dong A St Co Ltd | novos compostos de piridopirimidinona para modular a atividade catalítica de histona lisina demetilases (kdms) |
| JP2018511621A (ja) * | 2015-04-14 | 2018-04-26 | ギリアード サイエンシーズ， インコーポレイテッド | Ｂ型肝炎ウイルスを処置する方法 |
| US11998540B2 (en) * | 2015-12-11 | 2024-06-04 | The General Hospital Corporation | Compositions and methods for treating drug-tolerant glioblastoma |
| SG11201809893WA (en) | 2016-05-27 | 2018-12-28 | Gilead Sciences Inc | Methods for treating hepatitis b virus infections using ns5a, ns5b or ns3 inhibitors |
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| EP3630079A4 (en) * | 2017-05-31 | 2021-02-24 | The Children's Medical Center Corporation | TARGETING LYSINE DEMETHYLASE (KDMS) AS A THERAPEUTIC STRATEGY FOR DIFFUSED LARGE B-CELL LYMPHOMA |
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-
2014
- 2014-02-26 TR TR2018/08599T patent/TR201808599T4/tr unknown
- 2014-02-26 PL PL14706607T patent/PL2961736T3/pl unknown
- 2014-02-26 SG SG11201506717UA patent/SG11201506717UA/en unknown
- 2014-02-26 AP AP2015008676A patent/AP2015008676A0/xx unknown
- 2014-02-26 PE PE2015001818A patent/PE20151667A1/es not_active Application Discontinuation
- 2014-02-26 SG SG10201707027SA patent/SG10201707027SA/en unknown
- 2014-02-26 CA CA2901022A patent/CA2901022C/en active Active
- 2014-02-26 JP JP2015558495A patent/JP6514117B2/ja active Active
- 2014-02-26 ES ES14706607.0T patent/ES2670864T3/es active Active
- 2014-02-26 EP EP14706607.0A patent/EP2961736B1/en active Active
- 2014-02-26 AU AU2014222756A patent/AU2014222756B2/en active Active
- 2014-02-26 MD MDA20150085A patent/MD20150085A2/ro not_active Application Discontinuation
- 2014-02-26 BR BR112015020650A patent/BR112015020650A2/pt not_active Application Discontinuation
- 2014-02-26 EP EP16197497.7A patent/EP3170811A1/en not_active Withdrawn
- 2014-02-26 CN CN201480010601.9A patent/CN105263906B/zh active Active
- 2014-02-26 EA EA201591382A patent/EA030451B1/ru not_active IP Right Cessation
- 2014-02-26 KR KR1020157026738A patent/KR102229992B1/ko active Active
- 2014-02-26 US US14/381,556 patent/US9650339B2/en active Active
- 2014-02-26 SI SI201430706T patent/SI2961736T1/en unknown
- 2014-02-26 MX MX2015011097A patent/MX2015011097A/es unknown
- 2014-02-26 WO PCT/EP2014/053674 patent/WO2014131777A1/en not_active Ceased
- 2014-08-28 US US14/472,065 patent/US9221801B2/en active Active
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2015
- 2015-08-09 IL IL240439A patent/IL240439A0/en unknown
- 2015-08-25 PH PH12015501868A patent/PH12015501868A1/en unknown
- 2015-08-26 CL CL2015002394A patent/CL2015002394A1/es unknown
- 2015-09-24 CR CR20150507A patent/CR20150507A/es unknown
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2018
- 2018-04-23 JP JP2018082444A patent/JP2018127486A/ja not_active Withdrawn
- 2018-07-13 AU AU2018205204A patent/AU2018205204A1/en not_active Abandoned
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