JP2017511801A5 - - Google Patents
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- Publication number
- JP2017511801A5 JP2017511801A5 JP2016554607A JP2016554607A JP2017511801A5 JP 2017511801 A5 JP2017511801 A5 JP 2017511801A5 JP 2016554607 A JP2016554607 A JP 2016554607A JP 2016554607 A JP2016554607 A JP 2016554607A JP 2017511801 A5 JP2017511801 A5 JP 2017511801A5
- Authority
- JP
- Japan
- Prior art keywords
- methyl
- methoxy
- dimethylisoxazol
- pyrimido
- amine
- 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.)
- Pending
Links
- 0 CC1=C(*)*N=C1* Chemical compound CC1=C(*)*N=C1* 0.000 description 2
Applications Claiming Priority (9)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201461946501P | 2014-02-28 | 2014-02-28 | |
| US61/946,501 | 2014-02-28 | ||
| US201461950406P | 2014-03-10 | 2014-03-10 | |
| US61/950,406 | 2014-03-10 | ||
| US201462031640P | 2014-07-31 | 2014-07-31 | |
| US62/031,640 | 2014-07-31 | ||
| US201462048388P | 2014-09-10 | 2014-09-10 | |
| US62/048,388 | 2014-09-10 | ||
| PCT/US2015/017908 WO2015131005A1 (en) | 2014-02-28 | 2015-02-27 | 9h-pyrimido[4,5-b]indoles and related analogs as bet bromodomain inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2017511801A JP2017511801A (ja) | 2017-04-27 |
| JP2017511801A5 true JP2017511801A5 (enExample) | 2018-04-05 |
Family
ID=52706277
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016554607A Pending JP2017511801A (ja) | 2014-02-28 | 2015-02-27 | 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 |
Country Status (7)
| Country | Link |
|---|---|
| US (2) | US9580430B2 (enExample) |
| EP (1) | EP3110818B1 (enExample) |
| JP (1) | JP2017511801A (enExample) |
| CN (1) | CN107074861A (enExample) |
| AU (1) | AU2015222887B2 (enExample) |
| CA (1) | CA2940554A1 (enExample) |
| WO (1) | WO2015131005A1 (enExample) |
Families Citing this family (47)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2017156493A1 (en) | 2016-03-11 | 2017-09-14 | Denali Therapeutics Inc. | Compounds, compositions, and methods |
| CN105377851B (zh) * | 2013-03-11 | 2018-07-20 | 密执安州立大学董事会 | Bet布罗莫结构域抑制剂和使用这些抑制剂的治疗方法 |
| TWI719464B (zh) | 2013-03-15 | 2021-02-21 | 美商英塞特控股公司 | 作為bet蛋白抑制劑之三環雜環 |
| US9309246B2 (en) | 2013-12-19 | 2016-04-12 | Incyte Corporation | Tricyclic heterocycles as BET protein inhibitors |
| 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 |
| KR20240134245A (ko) | 2014-04-23 | 2024-09-06 | 인사이트 홀딩스 코포레이션 | BET 단백질의 저해제로서의 1H-피롤로[2,3-c]피리딘-7(6H)-온 및 피라졸로[3,4-c]피리딘-7(6H)-온 |
| US9527864B2 (en) | 2014-09-15 | 2016-12-27 | Incyte Corporation | Tricyclic heterocycles as BET protein inhibitors |
| EP3262045A1 (en) * | 2015-02-27 | 2018-01-03 | The Regents of The University of Michigan | 9h-pyrimido [4,5-b]indoles as bet bromodomain inhibitors |
| US9725449B2 (en) * | 2015-05-12 | 2017-08-08 | Bristol-Myers Squibb Company | Tricyclic compounds as anticancer agents |
| US20170121347A1 (en) | 2015-10-29 | 2017-05-04 | Incyte Corporation | Amorphous solid form of a bet protein inhibitor |
| WO2017087905A1 (en) | 2015-11-20 | 2017-05-26 | Denali Therapeutics Inc. | Compound, compositions, and methods |
| EP3412669A4 (en) * | 2016-02-05 | 2019-09-04 | Chia Tai Tianqing Pharmaceutical Group Co.,Ltd | TRICYCLIC COMPOUND FOR PROTEIN INHIBITOR CONTAINING BROMODOMAINE AND PREPARATION, PHARMACEUTICAL COMPOSITION AND USE THEREOF |
| KR102387316B1 (ko) | 2016-04-06 | 2022-04-15 | 더 리젠츠 오브 더 유니버시티 오브 미시간 | Mdm2 단백질 분해제 |
| WO2017176958A1 (en) | 2016-04-06 | 2017-10-12 | The Regents Of The University Of Michigan | Monofunctional intermediates for ligand-dependent target protein degradation |
| RU2752677C2 (ru) | 2016-04-12 | 2021-07-29 | Дзе Риджентс Оф Дзе Юниверсити Оф Мичиган | Деструкторы белка вет |
| PE20190395A1 (es) | 2016-06-16 | 2019-03-13 | Denali Therapeutics Inc | Pirimidin-2-ilamino-1h-pirazoles como inhibidores de lrrk2 para el uso en el tratamiento de trastornos neurodegenerativos |
| EP4234554A3 (en) | 2016-06-20 | 2023-12-27 | Incyte Corporation | Crystalline solid forms of a bet inhibitor |
| JP6961684B2 (ja) | 2016-09-13 | 2021-11-05 | ザ リージェンツ オブ ザ ユニヴァシティ オブ ミシガン | Ｂｅｔタンパク質分解物質としての縮合１，４−オキサゼピン |
| ES2857743T3 (es) | 2016-09-13 | 2021-09-29 | Univ Michigan Regents | 1,4-diazepinas fusionadas como degradadores de proteína BET |
| AU2018302178A1 (en) | 2017-07-18 | 2020-02-13 | Nuvation Bio Inc. | 1,8-naphthyridinone compounds and uses thereof |
| WO2019018584A1 (en) | 2017-07-18 | 2019-01-24 | GiraFpharma LLC | HETEROCYCLIC COMPOUNDS AS ADENOSINE ANTAGONISTS |
| US11267822B2 (en) | 2017-09-13 | 2022-03-08 | The Regents Of The University Of Michigan | BET bromodomain protein degraders with cleavable linkers |
| CN109223792A (zh) * | 2018-04-24 | 2019-01-18 | 李明霞 | 一种治疗骨关节炎的药物组合物及其制备方法 |
| KR20210038921A (ko) | 2018-07-25 | 2021-04-08 | 치아타이 티안큉 파마수티컬 그룹 주식회사 | 브로모도메인 단백질 억제제로서의 설폭시민 화합물과 약학적 조성물 및 이의 의학적 용도 |
| WO2020092638A1 (en) | 2018-10-30 | 2020-05-07 | Nuvation Bio Inc. | Heterocyclic compounds as bet inhibitors |
| US20220002816A1 (en) * | 2018-11-13 | 2022-01-06 | Center For Cancer Research & Therapeutic Development, Clark Atlanta University | Identification of jund target genes for inhibition of prostate cancer cell growth |
| WO2020106059A1 (ko) * | 2018-11-21 | 2020-05-28 | 한국화학연구원 | Irak4 저해제로서 신규의 삼중고리 화합물 |
| KR102329235B1 (ko) | 2018-11-21 | 2021-11-22 | 한국화학연구원 | Irak4 저해제로서 신규의 삼중고리 화합물 |
| US11254670B2 (en) | 2019-01-18 | 2022-02-22 | Nuvation Bio Inc. | 1,8-naphthyridinone compounds and uses thereof |
| KR20210116550A (ko) | 2019-01-18 | 2021-09-27 | 누베이션 바이오 인크. | 아데노신 길항제로서의 헤테로시클릭 화합물 |
| 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 |
| WO2020243519A1 (en) * | 2019-05-29 | 2020-12-03 | Ifm Due, Inc. | Compounds and compositions for treating conditions associated with sting activity |
| CA3145827A1 (en) | 2019-07-02 | 2021-01-07 | Nuvation Bio Inc. | Heterocyclic compounds as bet inhibitors |
| UA129778C2 (uk) | 2019-10-28 | 2025-07-30 | Мерк Шарп Енд Доум Елелсі | Низькомолекулярні інгібітори g12c-мутантного kras |
| CN112851678B (zh) * | 2019-11-28 | 2022-04-19 | 广东医科大学 | 2，4，7-三取代嘧啶并吲哚化合物抗肿瘤转移作用 |
| CN112851679B (zh) * | 2019-11-28 | 2022-03-25 | 广东医科大学 | 2，4，7-三取代嘧啶并吲哚化合物抗肿瘤作用 |
| US12479834B2 (en) | 2019-11-29 | 2025-11-25 | Taiho Pharmaceutical Co., Ltd. | Phenol compound or salt thereof |
| CN113018301A (zh) * | 2019-12-09 | 2021-06-25 | 中国科学院大连化学物理研究所 | JQ1与Erlotinib组合物在制备治疗肝癌药物中应用和治疗肝癌药物 |
| WO2021119834A1 (en) * | 2019-12-18 | 2021-06-24 | Universite De Montreal | Modulators of cullin 3 adaptor kbtbd4 as anti-cancer compounds |
| US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
| US11814388B1 (en) | 2020-08-28 | 2023-11-14 | Ferris State University | Substituted pyrrolo[2,3-d]pyrimidines and pyrazolo[3,4-d]pyrimidines as inhibitors for multi-resistant cancers |
| CN114044754A (zh) * | 2021-11-23 | 2022-02-15 | 贵州大学 | 一类5-三氟甲基-4-吡唑衍生物的制备方法及其在抑制肿瘤细胞上的应用 |
| CN115057859B (zh) * | 2022-05-10 | 2023-07-21 | 中国人民解放军海军军医大学 | 一类具有抗肿瘤抗真菌活性的化合物及其应用 |
| WO2024099441A1 (en) * | 2022-11-11 | 2024-05-16 | Jingrui Biopharma (Shandong) Co., Ltd. | Bromodomain and extra-terminal (bet) protein degrader |
| WO2024233776A1 (en) * | 2023-05-09 | 2024-11-14 | Merck Sharp & Dohme Llc | Small molecule inhibitors of kras g12d mutant |
| TW202535891A (zh) | 2023-10-20 | 2025-09-16 | 美商默沙東有限責任公司 | Ｋｒａｓ蛋白之小分子抑制劑 |
| WO2025230961A1 (en) * | 2024-04-29 | 2025-11-06 | Merck Sharp & Dohme Llc | Small molecule inhibitors of kras proteins |
Family Cites Families (40)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5093330A (en) | 1987-06-15 | 1992-03-03 | Ciba-Geigy Corporation | Staurosporine derivatives substituted at methylamino nitrogen |
| DE69717160T2 (de) | 1996-09-13 | 2003-05-08 | Mitsubishi Pharma Corp., Osaka | Thienotriazolodiazepinverbindungen und ihre medizinischen anwendungen |
| WO2006129623A1 (ja) | 2005-05-30 | 2006-12-07 | Mitsubishi Tanabe Pharma Corporation | チエノトリアゾロジアゼピン化合物及びその医薬としての用途 |
| DK2118074T3 (en) | 2007-02-01 | 2014-03-10 | Resverlogix Corp | Compounds for the prevention and treatment of cardiovascular diseases |
| EP2231143B1 (en) * | 2007-12-13 | 2013-07-03 | Merck Sharp & Dohme Corp. | 5H-pyrido[4,3-b]indoles as INHIBITORS OF JANUS KINASES |
| CN101910182B (zh) | 2007-12-28 | 2013-07-17 | 田边三菱制药株式会社 | 抗癌剂 |
| ES2532402T3 (es) | 2008-06-26 | 2015-03-26 | Resverlogix Corporation | Métodos de preparación de derivados de quinazolinona |
| CN107252429B (zh) | 2009-04-22 | 2023-06-16 | 雷斯韦洛吉克斯公司 | 新抗炎剂 |
| DE102009051823A1 (de) | 2009-11-04 | 2011-05-05 | Fraunhofer-Gesellschaft zur Förderung der angewandten Forschung e.V. | Einkristallines Schweißen von direktional verfestigten Werkstoffen |
| GB0919423D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| GB0919434D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| GB0919432D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Use |
| GB0919426D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| EP3050885B1 (en) | 2009-11-05 | 2017-10-18 | GlaxoSmithKline LLC | Benzodiazepine bromodomain inhibitor |
| DE102009053235A1 (de) | 2009-11-06 | 2011-05-19 | Gottwald Port Technology Gmbh | Umschlagsystem für ISO-Container mit einer Containerbrücke |
| HUE031073T2 (en) | 2010-05-14 | 2017-06-28 | Dana Farber Cancer Inst Inc | Thieno triazolo-diazepine compounds for the treatment of neoplasia |
| CA2799403C (en) | 2010-05-14 | 2020-01-21 | Dana-Farber Cancer Institute, Inc. | Compositions and methods for treating leukemia |
| CN103119160B (zh) | 2010-05-14 | 2016-06-01 | 达那-法伯癌症研究所 | 用于调节代谢的组合物和方法 |
| WO2011161031A1 (en) | 2010-06-22 | 2011-12-29 | Glaxosmithkline Llc | Benzotriazolodiazepine compounds inhibitors of bromodomains |
| US9145407B2 (en) | 2010-07-09 | 2015-09-29 | Pfizer Limited | Sulfonamide compounds |
| WO2012075456A1 (en) | 2010-12-02 | 2012-06-07 | Constellation Pharmaceuticals | Bromodomain inhibitors and uses thereof |
| AR084070A1 (es) | 2010-12-02 | 2013-04-17 | Constellation Pharmaceuticals Inc | Inhibidores del bromodominio y usos de los mismos |
| AU2012220620A1 (en) | 2011-02-23 | 2013-10-03 | Icahn School Of Medicine At Mount Sinai | Inhibitors of bromodomains as modulators of gene expression |
| EP2705039B1 (en) | 2011-05-04 | 2017-07-26 | 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 |
| WO2013027168A1 (en) | 2011-08-22 | 2013-02-28 | Pfizer Inc. | Novel heterocyclic compounds as bromodomain inhibitors |
| WO2013033270A2 (en) | 2011-08-29 | 2013-03-07 | Coferon, Inc. | Bromodomain ligands capable of dimerizing in an aqueous solution, and methods of using same |
| DE102011082013A1 (de) | 2011-09-01 | 2013-03-07 | Bayer Pharma AG | 6H-Thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine |
| WO2013097052A1 (en) | 2011-12-30 | 2013-07-04 | Abbott Laboratories | Bromodomain inhibitors |
| SI2807165T1 (sl) | 2012-01-27 | 2019-08-30 | Universite De Montreal | Pirimido(4,5-B)indol derivati in njihova uporaba pri ekspanziji hematopoetskih matičnih celic |
| US20130281399A1 (en) | 2012-04-19 | 2013-10-24 | Rvx Therapeutics Inc. | Treatment of diseases by epigenetic regulation |
| HK1206744A1 (en) | 2012-04-20 | 2016-01-15 | Abbvie Inc. | Isoindolone derivatives |
| MX2014015156A (es) | 2012-06-12 | 2015-08-06 | Abbvie Inc | Derivados de piridinona y piridazinona. |
| WO2014080290A2 (en) | 2012-11-21 | 2014-05-30 | Rvx Therapeutics Inc. | Cyclic amines as bromodomain inhibitors |
| 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 |
| CN105377851B (zh) | 2013-03-11 | 2018-07-20 | 密执安州立大学董事会 | Bet布罗莫结构域抑制剂和使用这些抑制剂的治疗方法 |
| MA39211B1 (fr) * | 2013-12-24 | 2019-01-31 | Bristol Myers Squibb Co | Composés tricycliques comme agents anti-cancers |
| 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 |
-
2015
- 2015-02-27 WO PCT/US2015/017908 patent/WO2015131005A1/en not_active Ceased
- 2015-02-27 CA CA2940554A patent/CA2940554A1/en not_active Abandoned
- 2015-02-27 CN CN201580023829.6A patent/CN107074861A/zh active Pending
- 2015-02-27 EP EP15711599.9A patent/EP3110818B1/en active Active
- 2015-02-27 AU AU2015222887A patent/AU2015222887B2/en not_active Ceased
- 2015-02-27 US US14/633,360 patent/US9580430B2/en not_active Expired - Fee Related
- 2015-02-27 JP JP2016554607A patent/JP2017511801A/ja active Pending
-
2017
- 2017-02-27 US US15/443,336 patent/US10253044B2/en not_active Expired - Fee Related
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