JP2016513137A5 - - Google Patents
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- Publication number
- JP2016513137A5 JP2016513137A5 JP2015560300A JP2015560300A JP2016513137A5 JP 2016513137 A5 JP2016513137 A5 JP 2016513137A5 JP 2015560300 A JP2015560300 A JP 2015560300A JP 2015560300 A JP2015560300 A JP 2015560300A JP 2016513137 A5 JP2016513137 A5 JP 2016513137A5
- Authority
- JP
- Japan
- Prior art keywords
- optionally substituted
- alkyl
- substituted
- cycloalkyl
- heteroaryl
- 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
Links
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 111
- 125000001072 heteroaryl group Chemical group 0.000 claims 77
- 229910052739 hydrogen Inorganic materials 0.000 claims 69
- 239000001257 hydrogen Substances 0.000 claims 69
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 47
- 150000002431 hydrogen Chemical group 0.000 claims 43
- 125000000623 heterocyclic group Chemical group 0.000 claims 39
- 125000004093 cyano group Chemical group *C#N 0.000 claims 31
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 27
- 229910052736 halogen Inorganic materials 0.000 claims 27
- 150000002367 halogens Chemical class 0.000 claims 27
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 26
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 26
- 125000003107 substituted aryl group Chemical group 0.000 claims 24
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 22
- 229920001577 copolymer Chemical group 0.000 claims 21
- 125000000217 alkyl group Chemical group 0.000 claims 16
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 16
- 150000003839 salts Chemical class 0.000 claims 15
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 14
- 150000001875 compounds Chemical class 0.000 claims 9
- 239000008194 pharmaceutical composition Substances 0.000 claims 9
- 125000003118 aryl group Chemical group 0.000 claims 8
- 229910052757 nitrogen Inorganic materials 0.000 claims 8
- 125000001424 substituent group Chemical group 0.000 claims 7
- 125000005842 heteroatom Chemical group 0.000 claims 6
- 238000006467 substitution reaction Methods 0.000 claims 6
- 201000010099 disease Diseases 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 206010028980 Neoplasm Diseases 0.000 claims 3
- 201000011510 cancer Diseases 0.000 claims 3
- 102000001805 Bromodomains Human genes 0.000 claims 2
- 108050009021 Bromodomains Proteins 0.000 claims 2
- 229940125763 bromodomain inhibitor Drugs 0.000 claims 2
- 239000003085 diluting agent Substances 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims 2
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 1
- 208000034578 Multiple myelomas Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 206010041067 Small cell lung cancer Diseases 0.000 claims 1
- 208000029052 T-cell acute lymphoblastic leukemia Diseases 0.000 claims 1
- 201000011176 T-cell adult acute lymphocytic leukemia Diseases 0.000 claims 1
- 208000003721 Triple Negative Breast Neoplasms Diseases 0.000 claims 1
- 239000013543 active substance Substances 0.000 claims 1
- 238000003556 assay Methods 0.000 claims 1
- 239000013066 combination product Substances 0.000 claims 1
- 229940127555 combination product Drugs 0.000 claims 1
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 1
- 238000002866 fluorescence resonance energy transfer Methods 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 208000000587 small cell lung carcinoma Diseases 0.000 claims 1
- 208000022679 triple-negative breast carcinoma Diseases 0.000 claims 1
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 1
- 0 C[C@]1C(*)=CC(c2c(*)cccc2*2)=C2C(*)=C1 Chemical compound C[C@]1C(*)=CC(c2c(*)cccc2*2)=C2C(*)=C1 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361770021P | 2013-02-27 | 2013-02-27 | |
| US61/770,021 | 2013-02-27 | ||
| PCT/US2014/018914 WO2014134267A1 (en) | 2013-02-27 | 2014-02-27 | Carbazole compounds useful as bromodomain inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016513137A JP2016513137A (ja) | 2016-05-12 |
| JP2016513137A5 true JP2016513137A5 (https=) | 2017-03-30 |
| JP6404838B2 JP6404838B2 (ja) | 2018-10-17 |
Family
ID=50272771
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015560300A Active JP6404838B2 (ja) | 2013-02-27 | 2014-02-27 | ブロモドメイン阻害剤として有用なカルバゾール化合物 |
Country Status (5)
| Country | Link |
|---|---|
| US (2) | US10053454B2 (https=) |
| EP (1) | EP2961747B1 (https=) |
| JP (1) | JP6404838B2 (https=) |
| CN (1) | CN105189488B (https=) |
| WO (1) | WO2014134267A1 (https=) |
Families Citing this family (35)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9073878B2 (en) | 2012-11-21 | 2015-07-07 | Zenith Epigenetics Corp. | Cyclic amines as bromodomain inhibitors |
| US9765039B2 (en) | 2012-11-21 | 2017-09-19 | Zenith Epigenetics Ltd. | Biaryl derivatives as bromodomain inhibitors |
| JP2016507496A (ja) | 2012-12-21 | 2016-03-10 | ゼニス・エピジェネティクス・コーポレイションＺｅｎｉｔｈ Ｅｐｉｇｅｎｅｔｉｃｓ Ｃｏｒｐ． | ブロモドメイン阻害剤としての新規複素環式化合物 |
| EP2970312B1 (en) * | 2013-03-11 | 2017-11-15 | The Regents of The University of Michigan | Bet bromodomain inhibitors and therapeutic methods using the same |
| SG11201506924YA (en) | 2013-03-15 | 2015-09-29 | Incyte Corp | Tricyclic heterocycles as bet protein inhibitors |
| SI3010503T1 (sl) | 2013-06-21 | 2020-07-31 | Zenith Epigenetics Ltd. | Novi biciklični inhibitorji bromodomene |
| JP6461118B2 (ja) | 2013-06-21 | 2019-01-30 | ゼニス・エピジェネティクス・リミテッドＺｅｎｉｔｈ Ｅｐｉｇｅｎｅｔｉｃｓ Ｌｔｄ． | ブロモドメイン阻害剤としての新規の置換された二環式化合物 |
| EP3019502B1 (en) | 2013-07-08 | 2017-05-17 | Incyte Holdings Corporation | Tricyclic heterocycles as bet protein inhibitors |
| JP6542212B2 (ja) | 2013-07-31 | 2019-07-10 | ゼニス・エピジェネティクス・リミテッドＺｅｎｉｔｈ Ｅｐｉｇｅｎｅｔｉｃｓ Ｌｔｄ． | ブロモドメイン阻害剤としての新規キナゾリノン |
| US9399640B2 (en) | 2013-11-26 | 2016-07-26 | Incyte Corporation | Substituted pyrrolo[2,3-c]pyridines and pyrazolo[3,4-c]pyridines as BET protein inhibitors |
| WO2015081189A1 (en) | 2013-11-26 | 2015-06-04 | Incyte Corporation | Bicyclic heterocycles as bet protein inhibitors |
| WO2015095492A1 (en) | 2013-12-19 | 2015-06-25 | Incyte Corporation | Tricyclic heterocycles as bet protein inhibitors |
| KR102457145B1 (ko) * | 2013-12-24 | 2022-10-19 | 브리스톨-마이어스 스큅 컴퍼니 | 항암제로서의 트리시클릭 화합물 |
| US9458156B2 (en) | 2014-12-23 | 2016-10-04 | Bristol-Myers Squibb Company | Tricyclic compounds as anticancer agents |
| WO2015131005A1 (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 |
| PL3134403T3 (pl) | 2014-04-23 | 2020-07-13 | Incyte Corporation | 1H-pirolo[2,3-c]pirydyn-7(6H)-ony i pirazolo[3,4-c]pirydyn-7(6H)-ony jako inhibitory białek BET |
| JP6599979B2 (ja) | 2014-09-15 | 2019-10-30 | インサイト・コーポレイション | Ｂｅｔタンパク質阻害剤として用いるための三環式複素環化合物 |
| US10710992B2 (en) | 2014-12-01 | 2020-07-14 | Zenith Epigenetics Ltd. | Substituted pyridinones as bromodomain inhibitors |
| US10179125B2 (en) | 2014-12-01 | 2019-01-15 | Zenith Epigenetics Ltd. | Substituted pyridines as bromodomain inhibitors |
| WO2016092375A1 (en) | 2014-12-11 | 2016-06-16 | Zenith Epigenetics Corp. | Substituted heterocycles as bromodomain inhibitors |
| CA2966450A1 (en) | 2014-12-17 | 2016-06-23 | Olesya KHARENKO | Inhibitors of bromodomains |
| GB201504694D0 (en) | 2015-03-19 | 2015-05-06 | Glaxosmithkline Ip Dev Ltd | Covalent conjugates |
| US10683290B2 (en) | 2015-05-11 | 2020-06-16 | Bristol-Myers Squibb Company | Tricyclic compounds as anticancer agents |
| US9725449B2 (en) | 2015-05-12 | 2017-08-08 | Bristol-Myers Squibb Company | Tricyclic compounds as anticancer agents |
| ES2770349T3 (es) | 2015-05-12 | 2020-07-01 | Bristol Myers Squibb Co | Compuestos de 5H-pirido[3,2-b]indol como agentes antineoplásicos |
| WO2017075377A1 (en) | 2015-10-29 | 2017-05-04 | Incyte Corporation | Amorphous solid form of a bet protein inhibitor |
| CA3028689A1 (en) | 2016-06-20 | 2017-12-28 | Incyte Corporation | Crystalline solid forms of a bet inhibitor |
| KR102625861B1 (ko) * | 2016-06-28 | 2024-01-17 | 삼성디스플레이 주식회사 | 헤테로시클릭 화합물 및 이를 포함한 유기 발광 소자 |
| US11192900B2 (en) | 2018-10-30 | 2021-12-07 | Nuvation Bio Inc. | Substituted 1,6-dihydropyridinones and 1,2-dihydroisoquinolinones as bet inhibitors |
| 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 |
| KR102677015B1 (ko) | 2019-07-02 | 2024-06-19 | 누베이션 바이오 인크. | Bet 억제제로서의 헤테로시클릭 화합물 |
| US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
| US12016847B2 (en) | 2021-03-12 | 2024-06-25 | Bristol-Myers Squibb Company | Methods of treating prostate cancer |
| JP2025533301A (ja) * | 2022-10-15 | 2025-10-03 | ピライ ユニバーサル エルエルシー | 新規の治療用分子 |
| CN118993985A (zh) * | 2023-05-17 | 2024-11-22 | 中国医学科学院药物研究所 | 一种具有抗肿瘤活性的化合物，其制备方法及制药用途 |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS545433A (en) | 1977-06-14 | 1979-01-16 | Ricoh Co Ltd | Photoreceptor for electrophotography |
| JPH0812430B2 (ja) * | 1986-07-07 | 1996-02-07 | キヤノン株式会社 | 電子写真感光体 |
| US6602619B2 (en) * | 2001-10-19 | 2003-08-05 | Lightronik Technology Inc. | Organic EL device |
| US7955716B2 (en) * | 2003-06-09 | 2011-06-07 | Hitachi Chemical Co., Ltd. | Metal coordination compound, polymer composition, and organic electroluminescent device employing same |
| UY30892A1 (es) | 2007-02-07 | 2008-09-02 | Smithkline Beckman Corp | Inhibidores de la actividad akt |
| EP2370407B1 (en) * | 2008-12-19 | 2014-06-18 | Bristol-Myers Squibb Company | Carbazole and carboline kinase inhibitors |
| JP5623996B2 (ja) * | 2010-09-21 | 2014-11-12 | 株式会社半導体エネルギー研究所 | カルバゾール誘導体 |
| CN102167913B (zh) | 2011-02-25 | 2013-09-25 | 中国科学院上海有机化学研究所 | 含多联咔唑的有机染料及其制备方法和应用 |
| JP5842630B2 (ja) * | 2011-03-16 | 2016-01-13 | 株式会社リコー | カルバゾール誘導体、及び半導体ナノ結晶 |
| 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 |
| KR102457145B1 (ko) | 2013-12-24 | 2022-10-19 | 브리스톨-마이어스 스큅 컴퍼니 | 항암제로서의 트리시클릭 화합물 |
-
2014
- 2014-02-27 EP EP14709856.0A patent/EP2961747B1/en active Active
- 2014-02-27 US US14/770,230 patent/US10053454B2/en active Active
- 2014-02-27 JP JP2015560300A patent/JP6404838B2/ja active Active
- 2014-02-27 CN CN201480023597.XA patent/CN105189488B/zh active Active
- 2014-02-27 WO PCT/US2014/018914 patent/WO2014134267A1/en not_active Ceased
-
2017
- 2017-02-13 US US15/430,883 patent/US10196387B2/en active Active
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