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 (https=) | 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 (https=) |
| EP (1) | EP3110818B1 (https=) |
| JP (1) | JP2017511801A (https=) |
| CN (1) | CN107074861A (https=) |
| AU (1) | AU2015222887B2 (https=) |
| CA (1) | CA2940554A1 (https=) |
| WO (1) | WO2015131005A1 (https=) |
Families Citing this family (48)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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. |
| WO2015095492A1 (en) | 2013-12-19 | 2015-06-25 | 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 |
| EA034972B1 (ru) | 2014-04-23 | 2020-04-13 | Инсайт Корпорейшн | 1h-пирроло[2,3-c]пиридин-7(6h)-оны в качестве ингибиторов белков bet |
| 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 |
| 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 |
| CN108770356A (zh) * | 2016-02-05 | 2018-11-06 | 正大天晴药业集团股份有限公司 | 溴区结构域蛋白抑制剂的三环类化合物及其制备、药物组合物和用途 |
| US11028080B2 (en) | 2016-03-11 | 2021-06-08 | Denali Therapeutics Inc. | Substituted pyrimidines as LRKK2 inhibitors |
| AU2017246452C1 (en) | 2016-04-06 | 2021-06-03 | The Regents Of The University Of Michigan | MDM2 protein degraders |
| WO2017176958A1 (en) | 2016-04-06 | 2017-10-12 | The Regents Of The University Of Michigan | Monofunctional intermediates for ligand-dependent target protein degradation |
| MX384905B (es) * | 2016-04-12 | 2025-03-14 | Univ Michigan Regents | Degradadores de proteínas de bromodominio y dominioextraterminal (bet). |
| MD3472153T2 (ro) | 2016-06-16 | 2022-03-31 | Denali Therapeutics Inc | Pirimidin-2-ilamino-1H-pirazoli în calitate de inhibitori L RRK2 pentru utilizare în tratamentul tulburărilor neurodegenerative |
| KR102643344B1 (ko) | 2016-06-20 | 2024-03-07 | 인사이트 코포레이션 | Bet 저해제의 결정질 고체 형태 |
| CA3036841A1 (en) | 2016-09-13 | 2018-03-22 | The Regents Of The University Of Michigan | Fused 1,4-diazepines as bet protein degraders |
| EP3512855B1 (en) | 2016-09-13 | 2022-07-27 | The Regents of the University of Michigan | Fused 1,4-oxazepines as bet protein degraders |
| EP3654982A4 (en) | 2017-07-18 | 2021-04-14 | Nuvation Bio Inc. | 1,8-NAPHTHYRIDINONE COMPOUNDS AND THEIR USES |
| WO2019018584A1 (en) | 2017-07-18 | 2019-01-24 | GiraFpharma LLC | 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 |
| CN115716827A (zh) | 2018-07-25 | 2023-02-28 | 正大天晴药业集团股份有限公司 | 作为溴区结构域蛋白抑制剂的亚氨基砜类化合物、药物组合物及其医药用途 |
| 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 |
| 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 |
| EP3911323A4 (en) | 2019-01-18 | 2022-11-16 | Nuvation Bio Inc. | HETEROCYCLIC COMPOUNDS AS ADENOSINE ANTAGONISTS |
| EP3911324A4 (en) | 2019-01-18 | 2022-08-17 | Nuvation Bio Inc. | 1,8-NAPHTHYRIDINONE COMPOUNDS AND THEIR USES |
| 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 |
| US20220227760A1 (en) * | 2019-05-29 | 2022-07-21 | Ifm Due, Inc. | Compounds and compositions for treating conditions associated with sting activity |
| EP3997070A4 (en) | 2019-07-02 | 2023-07-26 | Nuvation Bio Inc. | HETEROCYCLIC COMPOUNDS AS BET INHIBITORS |
| CN114867726B (zh) | 2019-10-28 | 2023-11-28 | 默沙东有限责任公司 | Kras g12c突变体的小分子抑制剂 |
| 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 |
| AU2020409437A1 (en) * | 2019-12-18 | 2022-07-14 | 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 |
| WO2025085748A1 (en) | 2023-10-20 | 2025-04-24 | Merck Sharp & Dohme Llc | Small molecule inhibitors of kras proteins |
| 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 |
| EP1887008B1 (en) | 2005-05-30 | 2021-04-21 | Mitsubishi Tanabe Pharma Corporation | Thienotriazolodiazepine compound and a medicinal use thereof |
| WO2008092231A1 (en) | 2007-02-01 | 2008-08-07 | Resverlogix Corp. | Compounds for the prevention and treatment of cardiovascular diseases |
| CA2707491A1 (en) * | 2007-12-13 | 2009-06-18 | Merck Sharp & Dohme Corp. | Inhibitors of janus kinases |
| WO2009084693A1 (ja) | 2007-12-28 | 2009-07-09 | Mitsubishi Tanabe Pharma Corporation | 抗癌剤 |
| KR101629356B1 (ko) | 2008-06-26 | 2016-06-13 | 리스버로직스 코퍼레이션 | 퀴나졸리논 유도체의 제조방법 |
| KR20190091564A (ko) | 2009-04-22 | 2019-08-06 | 리스버로직스 코퍼레이션 | 신규한 소염제 |
| DE102009051823A1 (de) | 2009-11-04 | 2011-05-05 | Fraunhofer-Gesellschaft zur Förderung der angewandten Forschung e.V. | Einkristallines Schweißen von direktional verfestigten Werkstoffen |
| GB0919432D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Use |
| GB0919426D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| GB0919434D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| GB0919423D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| RS54645B1 (sr) | 2009-11-05 | 2016-08-31 | Glaxosmithkline Llc | Benzodiazepin kao inhibitor bromodomena |
| DE102009053235A1 (de) * | 2009-11-06 | 2011-05-19 | Gottwald Port Technology Gmbh | Umschlagsystem für ISO-Container mit einer Containerbrücke |
| WO2011143651A1 (en) | 2010-05-14 | 2011-11-17 | Dana-Farber Cancer Institute, Inc. | Compositions and methods for modulating metabolism |
| PL2902030T3 (pl) | 2010-05-14 | 2017-07-31 | Dana-Farber Cancer Institute, Inc. | Związki tienotriazolodiazepinowe do leczenia nowotworu |
| MX354217B (es) | 2010-05-14 | 2018-02-19 | Dana Farber Cancer Inst Inc | Composiciones y metodos para el tratamiento de leucemia. |
| US9085582B2 (en) | 2010-06-22 | 2015-07-21 | Glaxosmithkline Llc | Benzotriazolodiazepine compounds inhibitors of bromodomains |
| JP5872552B2 (ja) | 2010-07-09 | 2016-03-01 | ファイザー・リミテッドＰｆｉｚｅｒ Ｌｉｍｉｔｅｄ | 化学化合物 |
| 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 |
| 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 |
| PT2807165T (pt) | 2012-01-27 | 2019-07-12 | Univ Montreal | Derivados de pirimido[4,5-b]indole e sua utilização na expansão de células estaminais hematopoiéticas |
| US20130281399A1 (en) | 2012-04-19 | 2013-10-24 | Rvx Therapeutics Inc. | Treatment of diseases by epigenetic regulation |
| EP2838881B1 (en) | 2012-04-20 | 2018-08-08 | AbbVie Inc. | Isoindolone derivatives |
| JP6215315B2 (ja) | 2012-06-12 | 2017-10-18 | アッヴィ・インコーポレイテッド | ピリジノンおよびピリダジノン誘導体 |
| US9073878B2 (en) | 2012-11-21 | 2015-07-07 | Zenith Epigenetics Corp. | Cyclic amines 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 |
| 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 |
| ES2857848T3 (es) * | 2013-12-24 | 2021-09-29 | Bristol Myers Squibb Co | Compuestos tricíclicos como agentes antineoplásicos |
| 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 JP JP2016554607A patent/JP2017511801A/ja active Pending
- 2015-02-27 CA CA2940554A patent/CA2940554A1/en not_active Abandoned
- 2015-02-27 WO PCT/US2015/017908 patent/WO2015131005A1/en not_active Ceased
- 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
-
2017
- 2017-02-27 US US15/443,336 patent/US10253044B2/en not_active Expired - Fee Related
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