JP2014521735A5 - - Google Patents
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- Publication number
- JP2014521735A5 JP2014521735A5 JP2014525437A JP2014525437A JP2014521735A5 JP 2014521735 A5 JP2014521735 A5 JP 2014521735A5 JP 2014525437 A JP2014525437 A JP 2014525437A JP 2014525437 A JP2014525437 A JP 2014525437A JP 2014521735 A5 JP2014521735 A5 JP 2014521735A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- pharmaceutically acceptable
- acceptable salt
- condition
- disease
- 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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- 150000001875 compounds Chemical class 0.000 claims 11
- 150000003839 salts Chemical class 0.000 claims 9
- 239000011780 sodium chloride Substances 0.000 claims 9
- 201000010099 disease Diseases 0.000 claims 4
- 102000001805 Bromodomains Human genes 0.000 claims 2
- 108050009021 Bromodomains Proteins 0.000 claims 2
- 239000003112 inhibitor Substances 0.000 claims 2
- 230000002401 inhibitory effect Effects 0.000 claims 2
- FICAQKBMCKEFDI-UHFFFAOYSA-N 3,5-dimethyl-1,2-oxazole Chemical compound CC=1C=C(C)ON=1 FICAQKBMCKEFDI-UHFFFAOYSA-N 0.000 claims 1
- HYPXHDJBILNWLI-CQSZACIVSA-N 4-[8-methoxy-1-[(2R)-1-methoxypropan-2-yl]-2-(oxan-4-yl)imidazo[4,5-c]quinolin-7-yl]-3,5-dimethyl-1,2-oxazole Chemical compound COC1=CC2=C3N([C@H](C)COC)C(C4CCOCC4)=NC3=CN=C2C=C1C=1C(C)=NOC=1C HYPXHDJBILNWLI-CQSZACIVSA-N 0.000 claims 1
- HYPXHDJBILNWLI-AWEZNQCLSA-N 4-[8-methoxy-1-[(2S)-1-methoxypropan-2-yl]-2-(oxan-4-yl)imidazo[4,5-c]quinolin-7-yl]-3,5-dimethyl-1,2-oxazole Chemical compound COC1=CC2=C3N([C@@H](C)COC)C(C4CCOCC4)=NC3=CN=C2C=C1C=1C(C)=NOC=1C HYPXHDJBILNWLI-AWEZNQCLSA-N 0.000 claims 1
- -1 8-methoxy-1- (1-methoxypropan-2-yl) -2- (tetrahydro-2H-pyran-4-yl) -1H-imidazo [4,5-c] quinolin-7-yl Chemical group 0.000 claims 1
- 230000001363 autoimmune Effects 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 230000001684 chronic Effects 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
- 230000004968 inflammatory condition Effects 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB1114103.3 | 2011-08-17 | ||
| GBGB1114103.3A GB201114103D0 (en) | 2011-08-17 | 2011-08-17 | Novel compounds |
| PCT/EP2012/065918 WO2013024104A1 (en) | 2011-08-17 | 2012-08-15 | 4-(8-methoxy-1-((1-methoxypropan-2-yl)-2-(tetrahydro-2h-pyran-4-yl)-1 h-imidazo[4,5-c]quinolin-7-yl)-3,5-dimethylisoxazole and its use as bromodomain inhibitor |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014521735A JP2014521735A (ja) | 2014-08-28 |
| JP2014521735A5 true JP2014521735A5 (US07714131-20100511-C00001.png) | 2015-09-10 |
| JP6059723B2 JP6059723B2 (ja) | 2017-01-11 |
Family
ID=44764570
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014525437A Expired - Fee Related JP6059723B2 (ja) | 2011-08-17 | 2012-08-15 | ４−（８−メトキシ−１−（（１−メトキシプロパン−２−イル）−２−（テトラヒドロ−２Ｈ−ピラン−４−イル）−１Ｈ−イミダゾ［４，５−ｃ］キノリン−７−イル）−３，５−ジメチルイソオキサゾールおよびブロモドメイン阻害剤としてのその使用 |
Country Status (37)
Families Citing this family (56)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR084070A1 (es) | 2010-12-02 | 2013-04-17 | Constellation Pharmaceuticals Inc | Inhibidores del bromodominio y usos de los mismos |
| US9249161B2 (en) | 2010-12-02 | 2016-02-02 | Constellation Pharmaceuticals, Inc. | Bromodomain inhibitors and uses thereof |
| US9422292B2 (en) | 2011-05-04 | 2016-08-23 | Constellation Pharmaceuticals, Inc. | Bromodomain inhibitors and uses thereof |
| EP2721031B1 (en) | 2011-06-17 | 2016-01-20 | Constellation Pharmaceuticals, Inc. | Bromodomain inhibitors and uses thereof |
| GB201114103D0 (en) * | 2011-08-17 | 2011-09-28 | Glaxosmithkline Llc | Novel compounds |
| EP2864336B1 (en) | 2012-06-06 | 2016-11-23 | Constellation Pharmaceuticals, Inc. | Benzo[b]isoxazoloazepine bromodomain inhibitors and uses thereof |
| TWI602820B (zh) | 2012-06-06 | 2017-10-21 | 星宿藥物公司 | 溴域抑制劑及其用途 |
| US9765039B2 (en) | 2012-11-21 | 2017-09-19 | Zenith Epigenetics Ltd. | Biaryl derivatives as bromodomain inhibitors |
| WO2014080290A2 (en) | 2012-11-21 | 2014-05-30 | Rvx Therapeutics Inc. | Cyclic amines as bromodomain inhibitors |
| KR20150096794A (ko) | 2012-12-21 | 2015-08-25 | 제니쓰 에피제네틱스 코포레이션 | 브로모도메인 저해제로서의 신규한 헤테로사이클릭 화합물 |
| AU2014249192B2 (en) | 2013-03-11 | 2017-12-21 | The Regents Of The University Of Michigan | BET bromodomain inhibitors and therapeutic methods using the same |
| CA2904048A1 (en) | 2013-03-11 | 2014-10-09 | Abbvie Inc. | Bromodomain inhibitors |
| TW201444843A (zh) | 2013-03-11 | 2014-12-01 | Abbvie Inc | 溴區結構域蛋白抑制劑 |
| EP2970282B1 (en) | 2013-03-15 | 2019-08-21 | Incyte Holdings Corporation | Tricyclic heterocycles as bet protein inhibitors |
| TWI530499B (zh) * | 2013-03-28 | 2016-04-21 | 吉李德科學股份有限公司 | 作為溴結構域（ｂｒｏｍｏｄｏｍａｉｎ）抑制劑之苯並咪唑酮衍生物類 |
| CN109939113B (zh) | 2013-06-21 | 2022-02-15 | 恒翼生物医药科技(上海)有限公司 | 双环溴结构域抑制剂 |
| US9636328B2 (en) | 2013-06-21 | 2017-05-02 | Zenith Epigenetics Ltd. | Substituted bicyclic compounds as bromodomain inhibitors |
| EP3019502B1 (en) | 2013-07-08 | 2017-05-17 | Incyte Holdings Corporation | Tricyclic heterocycles as bet protein inhibitors |
| CA2919948C (en) | 2013-07-31 | 2020-07-21 | Zenith Epigenetics Corp. | Novel quinazolinones as bromodomain inhibitors |
| WO2015049629A1 (en) * | 2013-10-01 | 2015-04-09 | Piramal Enterprises Limited | Imidazoquinoline compounds as bromodomain inhibitors |
| WO2015081189A1 (en) | 2013-11-26 | 2015-06-04 | Incyte Corporation | Bicyclic heterocycles as bet protein inhibitors |
| 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 |
| US9309246B2 (en) | 2013-12-19 | 2016-04-12 | Incyte Corporation | Tricyclic heterocycles as BET protein inhibitors |
| JP2017511801A (ja) | 2014-02-28 | 2017-04-27 | ザ リージェンツ オブ ザ ユニヴァシティ オブ ミシガン | ＢＥＴブロモドメイン阻害剤としての９Ｈ−ピリミド［４，５−ｂ］インドールおよび関連類似体 |
| MY180775A (en) | 2014-04-23 | 2020-12-09 | Incyte Corp | 1h-pyrrolo[2,3-c]pyridin-7(6h)-ones and pyrazolo[3,4-c]pyridin-7(6h)-ones as inhibitors of bet proteins |
| EP3157928B1 (en) | 2014-06-20 | 2019-02-13 | Constellation Pharmaceuticals, Inc. | Crystalline forms of 2-((4s)-6-(4-chlorophenyl)-1-methyl-4h-benzo[c]isoxazolo[4,5-e]azepin-4-yl)acetamide |
| 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 |
| WO2016087936A1 (en) | 2014-12-01 | 2016-06-09 | Zenith Epigenetics Corp. | Substituted pyridinones as bromodomain inhibitors |
| EP3227280B1 (en) | 2014-12-01 | 2019-04-24 | Zenith Epigenetics Ltd. | Substituted pyridines as bromodomain inhibitors |
| CA2966449A1 (en) | 2014-12-11 | 2016-06-16 | Zenith Epigenetics Ltd. | Substituted heterocycles as bromodomain inhibitors |
| EP3233846A4 (en) | 2014-12-17 | 2018-07-18 | Zenith Epigenetics Ltd. | Inhibitors of bromodomains |
| US10259809B2 (en) | 2015-02-03 | 2019-04-16 | Trillium Therapeutics Inc. | Fluorinated imidazo[4,5-C]quinoline derivatives as inhibitors of bromodomain containing proteins |
| WO2016138332A1 (en) | 2015-02-27 | 2016-09-01 | The Regents Of The University Of Michigan | 9h-pyrimido [4,5-b] indoles as bet bromodomain inhibitors |
| GB201504694D0 (en) | 2015-03-19 | 2015-05-06 | Glaxosmithkline Ip Dev Ltd | Covalent conjugates |
| GB201504689D0 (en) * | 2015-03-19 | 2015-05-06 | Glaxosmithkline Ip Dev Ltd | Chemical compounds |
| WO2016186453A1 (en) * | 2015-05-20 | 2016-11-24 | Kainos Medicine, Inc. | Quinoline derivatives as bromodomain inhibitors |
| WO2016196065A1 (en) | 2015-05-29 | 2016-12-08 | Genentech, Inc. | Methods and compositions for assessing responsiveness of cancers to bet inhibitors |
| WO2016199943A1 (en) * | 2015-06-11 | 2016-12-15 | Takeda Pharmaceutical Company Limited | Heterocyclic compounds |
| MX2018001751A (es) | 2015-08-11 | 2018-08-01 | Neomed Inst | Dihidroquinolinonas aril-sustituidas, su preparacion y su uso como farmaceuticos. |
| US10836742B2 (en) | 2015-08-11 | 2020-11-17 | Neomed Institute | N-substituted bicyclic lactams, their preparation and their use as pharmaceuticals |
| AU2016305515A1 (en) | 2015-08-12 | 2018-03-08 | Neomed Institute | Substituted benzimidazoles, their preparation and their use as pharmaceuticals |
| US10501459B2 (en) | 2015-10-21 | 2019-12-10 | Neomed Institute | Substituted imidazo[1,2-a]pyridines as bromodomain inhibitors |
| TW201722966A (zh) | 2015-10-29 | 2017-07-01 | 英塞特公司 | Bet蛋白質抑制劑之非晶固體形式 |
| US10519151B2 (en) | 2016-01-28 | 2019-12-31 | Neomed Institute | Substituted [1,2,4]triazolo[4,3-A]pyridines, their preparation and their use as pharmaceuticals |
| CN109071562B (zh) | 2016-02-15 | 2022-03-22 | 密执安大学评议会 | 作为bet溴结构域抑制剂的稠合1,4-氧氮杂䓬和相关类似物 |
| US10759808B2 (en) | 2016-04-06 | 2020-09-01 | The Regents Of The University Of Michigan | Monofunctional intermediates for ligand-dependent target protein degradation |
| SG11201808728QA (en) | 2016-04-06 | 2018-11-29 | Univ Michigan Regents | Mdm2 protein degraders |
| US10633386B2 (en) | 2016-04-12 | 2020-04-28 | The Regents Of The University Of Michigan | BET protein degraders |
| EP4234554A3 (en) | 2016-06-20 | 2023-12-27 | Incyte Corporation | Crystalline solid forms of a bet inhibitor |
| WO2018052949A1 (en) | 2016-09-13 | 2018-03-22 | The Regents Of The University Of Michigan | Fused 1,4-diazepines as bet protein degraders |
| US11466028B2 (en) | 2016-09-13 | 2022-10-11 | The Regents Of The University Of Michigan | Fused 1,4-oxazepines as BET protein degraders |
| WO2018144789A1 (en) | 2017-02-03 | 2018-08-09 | The Regents Of The University Of Michigan | Fused 1,4-diazepines as bet bromodomain inhibitors |
| WO2019055444A1 (en) | 2017-09-13 | 2019-03-21 | The Regents Of The University Of Michigan | DEGRADATION AGENTS OF BROMODOMAIN BET PROTEIN WITH CLEAR BINDERS |
| CN108033957A (zh) * | 2018-01-09 | 2018-05-15 | 中国药科大学 | 一种喹啉类BET bromodomain抑制剂及其制备方法和用途 |
| US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
| WO2022132049A1 (en) * | 2020-12-17 | 2022-06-23 | National University Of Singapore | Treating cancers using bet inhibitors |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9004781D0 (en) | 1990-03-02 | 1990-04-25 | Glaxo Group Ltd | Device |
| GB0211649D0 (en) | 2002-05-21 | 2002-07-03 | Novartis Ag | Organic compounds |
| AU2003301052A1 (en) | 2002-12-20 | 2004-07-22 | 3M Innovative Properties Company | Aryl / hetaryl substituted imidazoquinolines |
| WO2005044354A1 (en) | 2003-11-03 | 2005-05-19 | Glaxo Group Limited | A fluid dispensing device |
| EP1687305B1 (en) | 2003-11-21 | 2008-07-09 | Novartis AG | 1h-imidazoquinoline derivatives as protein kinase inhibitors |
| CA2597446A1 (en) | 2005-02-11 | 2006-08-31 | Coley Pharmaceutical Group, Inc. | Substituted imidazoquinolines and imidazonaphthyridines |
| KR20080048551A (ko) | 2005-09-23 | 2008-06-02 | 콜레이 파마시티컬 그룹, 인코포레이티드 | 1Ｈ-이미다조[4,5-ｃ]피리딘 및 그의 유사체의 제조법 |
| WO2007075468A1 (en) | 2005-12-16 | 2007-07-05 | Coley Pharmaceutical Group, Inc. | Substituted imidazoquinolines, imidazonaphthyridines, and imidazopyridines, compositions, and methods |
| JP2008156311A (ja) | 2006-12-26 | 2008-07-10 | Institute Of Physical & Chemical Research | Ｂｒｄ２ブロモドメイン結合剤 |
| WO2009084693A1 (ja) * | 2007-12-28 | 2009-07-09 | Mitsubishi Tanabe Pharma Corporation | 抗癌剤 |
| GB0919423D0 (en) * | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| ES2564318T3 (es) * | 2009-11-05 | 2016-03-21 | Glaxosmithkline Llc | Inhibidor de bromodominio de benzodiazepina |
| GB0919432D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Use |
| GB0919434D0 (en) * | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| GB201106799D0 (en) | 2011-04-21 | 2011-06-01 | Glaxosmithkline Llc | Novel compounds |
| GB201114103D0 (en) | 2011-08-17 | 2011-09-28 | Glaxosmithkline Llc | Novel compounds |
-
2011
- 2011-08-17 GB GBGB1114103.3A patent/GB201114103D0/en not_active Ceased
-
2012
- 2012-08-15 KR KR1020147007082A patent/KR20140064878A/ko not_active Application Discontinuation
- 2012-08-15 PE PE2014000167A patent/PE20141406A1/es not_active Application Discontinuation
- 2012-08-15 ME MEP-2016-288A patent/ME02589B/me unknown
- 2012-08-15 EP EP16192662.1A patent/EP3150601A1/en not_active Withdrawn
- 2012-08-15 BR BR112014003681A patent/BR112014003681A8/pt not_active Application Discontinuation
- 2012-08-15 ES ES12748028.3T patent/ES2609857T3/es active Active
- 2012-08-15 CN CN201280040092.5A patent/CN103889984B/zh not_active Expired - Fee Related
- 2012-08-15 MY MYPI2014700328A patent/MY170729A/en unknown
- 2012-08-15 PT PT127480283T patent/PT2744809T/pt unknown
- 2012-08-15 US US14/237,905 patent/US9067936B2/en not_active Expired - Fee Related
- 2012-08-15 AR ARP120102987A patent/AR087545A1/es unknown
- 2012-08-15 DK DK12748028.3T patent/DK2744809T3/en active
- 2012-08-15 UA UAA201400590A patent/UA110838C2/uk unknown
- 2012-08-15 UY UY0001034264A patent/UY34264A/es not_active Application Discontinuation
- 2012-08-15 JP JP2014525437A patent/JP6059723B2/ja not_active Expired - Fee Related
- 2012-08-15 JO JOP/2012/0229A patent/JO3187B1/ar active
- 2012-08-15 RS RS20170014A patent/RS55560B1/sr unknown
- 2012-08-15 PL PL12748028T patent/PL2744809T3/pl unknown
- 2012-08-15 CA CA2843537A patent/CA2843537A1/en not_active Abandoned
- 2012-08-15 TW TW101129613A patent/TWI558704B/zh not_active IP Right Cessation
- 2012-08-15 MX MX2014001834A patent/MX350597B/es active IP Right Grant
- 2012-08-15 IN IN568CHN2014 patent/IN2014CN00568A/en unknown
- 2012-08-15 WO PCT/EP2012/065918 patent/WO2013024104A1/en active Application Filing
- 2012-08-15 EA EA201490200A patent/EA023374B1/ru not_active IP Right Cessation
- 2012-08-15 HU HUE12748028A patent/HUE030106T2/en unknown
- 2012-08-15 LT LTEP12748028.3T patent/LT2744809T/lt unknown
- 2012-08-15 AU AU2012296914A patent/AU2012296914B2/en not_active Ceased
- 2012-08-15 SI SI201230818A patent/SI2744809T1/sl unknown
- 2012-08-15 EP EP12748028.3A patent/EP2744809B1/en active Active
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2014
- 2014-01-16 IL IL230489A patent/IL230489A/en active IP Right Grant
- 2014-01-21 CO CO14011125A patent/CO6862151A2/es not_active Application Discontinuation
- 2014-02-13 CL CL2014000365A patent/CL2014000365A1/es unknown
- 2014-02-17 DO DO2014000031A patent/DOP2014000031A/es unknown
- 2014-02-17 CR CR20140076A patent/CR20140076A/es unknown
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2015
- 2015-05-28 US US14/723,556 patent/US9416130B2/en active Active
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2016
- 2016-07-08 US US15/205,372 patent/US9610284B2/en not_active Expired - Fee Related
- 2016-12-08 HR HRP20161674TT patent/HRP20161674T1/hr unknown
- 2016-12-16 CY CY20161101310T patent/CY1118370T1/el unknown
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2017
- 2017-01-04 SM SM201700005T patent/SMT201700005B/it unknown
- 2017-02-17 US US15/435,697 patent/US9861627B2/en not_active Expired - Fee Related
