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 (48)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2017156493A1 (en) | 2016-03-11 | 2017-09-14 | Denali Therapeutics Inc. | Compounds, compositions, and methods |
| EP2970312B1 (en) | 2013-03-11 | 2017-11-15 | The Regents of The University of Michigan | Bet bromodomain inhibitors and therapeutic methods using the same |
| MX366703B (es) | 2013-03-15 | 2019-07-22 | Incyte Holdings Corp | Heterociclos tricíclicos como inhibidores de la proteína bet. |
| US9309246B2 (en) | 2013-12-19 | 2016-04-12 | Incyte Corporation | Tricyclic heterocycles as BET protein inhibitors |
| US9580430B2 (en) * | 2014-02-28 | 2017-02-28 | The Regents Of The University Of Michigan | 9H-pyrimido[4,5-B]indoles and related analogs as BET bromodomain inhibitors |
| UA119870C2 (uk) | 2014-04-23 | 2019-08-27 | Інсайт Корпорейшн | 1H-ПІРОЛО[2,3-c]ПІРИДИН-7(6H)-ОНИ ТА ПІРАЗОЛО[3,4-c]ПІРИДИН-7(6H)-ОНИ ЯК ІНГІБІТОРИ БІЛКІВ BET |
| ES2855225T3 (es) | 2014-09-15 | 2021-09-23 | Incyte Corp | Heterociclos tricíclicos para su uso como inhibidores de proteínas BET |
| 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 |
| US9725449B2 (en) * | 2015-05-12 | 2017-08-08 | Bristol-Myers Squibb Company | Tricyclic compounds as anticancer agents |
| 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 |
| US11214565B2 (en) | 2015-11-20 | 2022-01-04 | 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 |
| AU2017246453A1 (en) | 2016-04-06 | 2018-11-08 | The Regents Of The University Of Michigan | Monofunctional intermediates for ligand-dependent target protein degradation |
| CN113788818A (zh) | 2016-04-06 | 2021-12-14 | 密执安大学评议会 | Mdm2蛋白质降解剂 |
| BR112018070859A2 (pt) * | 2016-04-12 | 2019-02-05 | Univ Michigan Regents | degradantes da proteína de bet |
| SI3472153T1 (sl) | 2016-06-16 | 2022-01-31 | Denali Therapeutics Inc. | Pirimidin-2-ilamino-1H-pirazoli kot zaviralci LRRK2 za uporabo pri zdravljenju nevrodegenerativnih motenj |
| AU2017281286B2 (en) | 2016-06-20 | 2021-05-20 | Incyte Corporation | Crystalline solid forms of a bet inhibitor |
| US10975093B2 (en) | 2016-09-13 | 2021-04-13 | The Regents Of The University Of Michigan | Fused 1,4-diazepines as BET protein degraders |
| CN110062759B (zh) | 2016-09-13 | 2022-05-24 | 密执安大学评议会 | 作为bet蛋白降解剂的稠合的1,4-氧氮杂䓬 |
| MX2020000693A (es) | 2017-07-18 | 2020-07-29 | Nuvation Bio Inc | Compuestos de 1,8-naftiridinona, y usos de los mismos. |
| AU2018302179A1 (en) | 2017-07-18 | 2020-02-13 | Nuvation Bio Inc. | Heterocyclic compounds as adenosine antagonists |
| WO2019055444A1 (en) | 2017-09-13 | 2019-03-21 | The Regents Of The University Of Michigan | DEGRADATION AGENTS OF BROMODOMAIN BET PROTEIN WITH CLEAR BINDERS |
| 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 |
| CN113226322A (zh) | 2018-10-30 | 2021-08-06 | 诺维逊生物股份有限公司 | 作为bet抑制剂的杂环化合物 |
| WO2020101909A2 (en) * | 2018-11-13 | 2020-05-22 | Center For Cancer Research & Therapeutic Development, Clark Atlanta University | Identification of jund target genes for inhibition of prostate cancer cell growth |
| KR102329235B1 (ko) | 2018-11-21 | 2021-11-22 | 한국화학연구원 | Irak4 저해제로서 신규의 삼중고리 화합물 |
| WO2020106059A1 (ko) * | 2018-11-21 | 2020-05-28 | 한국화학연구원 | Irak4 저해제로서 신규의 삼중고리 화합물 |
| AU2020208644A1 (en) | 2019-01-18 | 2021-08-26 | Nuvation Bio Inc. | Heterocyclic compounds as adenosine antagonists |
| WO2020150676A1 (en) | 2019-01-18 | 2020-07-23 | Nuvation Bio Inc. | 1,8-naphthyridinone compounds and uses thereof |
| 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 |
| JP2022535743A (ja) * | 2019-05-29 | 2022-08-10 | アイエフエム デュー インコーポレイテッド | Ｓｔｉｎｇ活性に関連する状態を治療するための化合物および組成物 |
| JP7465945B2 (ja) | 2019-07-02 | 2024-04-11 | ニューベイション・バイオ・インコーポレイテッド | Ｂｅｔ阻害剤としてのヘテロ環式化合物 |
| CR20220230A (es) | 2019-10-28 | 2022-06-15 | Merck Sharp & Dohme | Inhibidores de pequeñas moléculas de mutante g12c de kras |
| 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 |
| 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 |
| EP4067343A4 (en) | 2019-11-29 | 2024-01-03 | Taiho Pharmaceutical Co., Ltd. | NEW PHENOLIC 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 |
| CA3164153A1 (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 |
| US12016847B2 (en) * | 2021-03-12 | 2024-06-25 | Bristol-Myers Squibb Company | Methods of treating prostate cancer |
| 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)
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|---|---|---|---|---|
| US5093330A (en) | 1987-06-15 | 1992-03-03 | Ciba-Geigy Corporation | Staurosporine derivatives substituted at methylamino nitrogen |
| PT989131E (pt) | 1996-09-13 | 2003-03-31 | Mitsubishi Pharma Corp | Compostos de trienotriazolodiazepina e suas utilizacoes com fins medicinais |
| EP1887008B1 (en) | 2005-05-30 | 2021-04-21 | Mitsubishi Tanabe Pharma Corporation | Thienotriazolodiazepine compound and a medicinal use thereof |
| MX2009008099A (es) | 2007-02-01 | 2009-12-14 | Resverlogix Corp | Compuestos para la prevencion y tratamiento de enfermedades cardiovasculares. |
| CA2707491A1 (en) * | 2007-12-13 | 2009-06-18 | Merck Sharp & Dohme Corp. | Inhibitors of janus kinases |
| EP2239264A4 (en) | 2007-12-28 | 2012-01-11 | Mitsubishi Tanabe Pharma Corp | ANTITUMORAL MEDIUM |
| KR101629356B1 (ko) | 2008-06-26 | 2016-06-13 | 리스버로직스 코퍼레이션 | 퀴나졸리논 유도체의 제조방법 |
| DK2421533T3 (en) | 2009-04-22 | 2019-01-07 | Resverlogix Corp | Hitherto unknown anti-inflammatory agents |
| DE102009051823A1 (de) | 2009-11-04 | 2011-05-05 | Fraunhofer-Gesellschaft zur Förderung der angewandten Forschung e.V. | Einkristallines Schweißen von direktional verfestigten Werkstoffen |
| GB0919434D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| KR20120097508A (ko) | 2009-11-05 | 2012-09-04 | 글락소스미스클라인 엘엘씨 | 벤조디아제핀 브로모도메인 억제제 |
| GB0919426D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| GB0919423D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| GB0919432D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Use |
| DE102009053235A1 (de) | 2009-11-06 | 2011-05-19 | Gottwald Port Technology Gmbh | Umschlagsystem für ISO-Container mit einer Containerbrücke |
| MX373121B (es) | 2010-05-14 | 2020-04-30 | Dana Farber Cancer Inst Inc | Composiciones y metodos para el tratamiento de leucemia. |
| US8981083B2 (en) | 2010-05-14 | 2015-03-17 | Dana Farber Cancer Institute, Inc. | Compositions and methods for treating neoplasia, inflammatory disease and other disorders |
| JP5913292B2 (ja) | 2010-05-14 | 2016-04-27 | ダナ−ファーバー キャンサー インスティテュート， インコーポレイテッド | 代謝を調節する組成物および方法 |
| US9085582B2 (en) | 2010-06-22 | 2015-07-21 | Glaxosmithkline Llc | Benzotriazolodiazepine compounds inhibitors of bromodomains |
| ES2532356T3 (es) | 2010-07-09 | 2015-03-26 | Pfizer Limited | N-sulfonilbenzamidas como inhibidores de los canales de sodio dependientes de voltaje |
| 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 |
| EP2677865A4 (en) | 2011-02-23 | 2015-04-22 | Icahn School Med Mount Sinai | BROMODOMAIN INHIBITORS AS MODULATORS OF GENE EXPRESSION |
| WO2012151512A2 (en) | 2011-05-04 | 2012-11-08 | Constellation Pharmaceuticals, Inc. | Bromodomain inhibitors and uses thereof |
| US9328117B2 (en) | 2011-06-17 | 2016-05-03 | 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 |
| PL2807165T3 (pl) | 2012-01-27 | 2019-09-30 | Université de Montréal | Pochodne pirymido[4,5-b]indolu i ich zastosowanie do namnażania hematopoetycznych komórek macierzystych |
| US20130281399A1 (en) | 2012-04-19 | 2013-10-24 | Rvx Therapeutics Inc. | Treatment of diseases by epigenetic regulation |
| CA2870931A1 (en) | 2012-04-20 | 2013-10-24 | Abbvie Inc. | Isoindolone derivatives |
| AU2012382373A1 (en) | 2012-06-12 | 2014-12-11 | Abbvie Inc. | Pyridinone and pyridazinone derivatives |
| US9073878B2 (en) | 2012-11-21 | 2015-07-07 | Zenith Epigenetics Corp. | Cyclic amines as bromodomain inhibitors |
| JP6404838B2 (ja) * | 2013-02-27 | 2018-10-17 | ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ | 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 |
| US9492460B2 (en) | 2013-02-27 | 2016-11-15 | Bristol-Myers Squibb Company | Carbazole compounds useful as bromodomain inhibitors |
| EP2970312B1 (en) | 2013-03-11 | 2017-11-15 | The Regents of The University of Michigan | Bet bromodomain inhibitors and therapeutic methods using the same |
| DK3466949T3 (da) * | 2013-12-24 | 2021-03-15 | Bristol Myers Squibb Co | Tricyklisk forbindelse som anticancermidler |
| US9580430B2 (en) * | 2014-02-28 | 2017-02-28 | The Regents Of The University Of Michigan | 9H-pyrimido[4,5-B]indoles and related analogs as BET bromodomain inhibitors |
-
2015
- 2015-02-27 US US14/633,360 patent/US9580430B2/en not_active Expired - Fee Related
- 2015-02-27 EP EP15711599.9A patent/EP3110818B1/en active Active
- 2015-02-27 CA CA2940554A patent/CA2940554A1/en not_active Abandoned
- 2015-02-27 AU AU2015222887A patent/AU2015222887B2/en not_active Ceased
- 2015-02-27 CN CN201580023829.6A patent/CN107074861A/zh active Pending
- 2015-02-27 JP JP2016554607A patent/JP2017511801A/ja active Pending
- 2015-02-27 WO PCT/US2015/017908 patent/WO2015131005A1/en not_active Ceased
-
2017
- 2017-02-27 US US15/443,336 patent/US10253044B2/en not_active Expired - Fee Related
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