JP2017511801A5 - - Google Patents
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- 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 |
|---|---|---|---|---|
| JP6401773B2 (ja) | 2013-03-11 | 2018-10-10 | 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およびこれを用いる治療方法 |
| BR112015022942B1 (pt) | 2013-03-15 | 2022-02-22 | Incyte Holdings Corporation | Compostos heterocíciclos tricíclicos, método para inibir proteína bet in vitro e composição farmacêutica compreendendo os referidos compostos |
| WO2015095492A1 (en) | 2013-12-19 | 2015-06-25 | Incyte Corporation | Tricyclic heterocycles as bet protein inhibitors |
| EP3110818B1 (en) * | 2014-02-28 | 2019-10-23 | The Regents of The University of Michigan | 9h-pyrimido[4,5-b]indoles and related analogs as bet bromodomain inhibitors |
| NZ725930A (en) | 2014-04-23 | 2023-04-28 | Incyte Holdings Corp | 1h-pyrrolo[2,3-c]pyridin-7(6h)-ones and pyrazolo[3,4-c]pyridin-7(6h)-ones as inhibitors of bet proteins |
| ES2855225T3 (es) | 2014-09-15 | 2021-09-23 | Incyte Corp | Heterociclos tricíclicos para su uso como inhibidores de proteínas BET |
| US10307407B2 (en) | 2015-02-27 | 2019-06-04 | 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 |
| AR106520A1 (es) | 2015-10-29 | 2018-01-24 | Incyte Corp | Forma sólida amorfa de un inhibidor de proteína bet |
| US11214565B2 (en) | 2015-11-20 | 2022-01-04 | Denali Therapeutics Inc. | Compound, compositions, and methods |
| US20190040063A1 (en) * | 2016-02-05 | 2019-02-07 | Chia Tai Tianqing Pharmaceutical Group Co., Ltd. | Tricyclic compound for bromodomain-containing protein inhibitor and preparation pharmaceutical composition, and application thereof |
| US11028080B2 (en) | 2016-03-11 | 2021-06-08 | Denali Therapeutics Inc. | Substituted pyrimidines as LRKK2 inhibitors |
| CN113788818A (zh) * | 2016-04-06 | 2021-12-14 | 密执安大学评议会 | Mdm2蛋白质降解剂 |
| AU2017246453A1 (en) | 2016-04-06 | 2018-11-08 | The Regents Of The University Of Michigan | Monofunctional intermediates for ligand-dependent target protein degradation |
| UA123168C2 (uk) | 2016-04-12 | 2021-02-24 | Дзе Ріджентс Оф Дзе Юніверсіті Оф Мічіган | Деструктори білка вет |
| JOP20180113B1 (ar) | 2016-06-16 | 2022-03-14 | Denali Therapeutics Inc | مركبات بيريميدين -2-يل امينو -h1- بيرازول كمثبطات lrrk2 للاستخدام في علاج اضطرابات تنكسية عصبية |
| EP3472157B1 (en) | 2016-06-20 | 2023-04-12 | Incyte Corporation | Crystalline solid forms of a bet inhibitor |
| WO2018052945A1 (en) | 2016-09-13 | 2018-03-22 | The Regents Of The University Of Michigan | Fused 1,4-oxazepines as bet protein degraders |
| ES2857743T3 (es) | 2016-09-13 | 2021-09-29 | Univ Michigan Regents | 1,4-diazepinas fusionadas como degradadores de proteína BET |
| JP2020527593A (ja) | 2017-07-18 | 2020-09-10 | ニューベイション・バイオ・インコーポレイテッドＮｕｖａｔｉｏｎ Ｂｉｏ Ｉｎｃ． | １，８−ナフチリジノン化合物およびその使用 |
| JP2020527588A (ja) | 2017-07-18 | 2020-09-10 | ニューベイション・バイオ・インコーポレイテッドＮｕｖａｔｉｏｎ Ｂｉｏ Ｉｎｃ． | アデノシンアンタゴニストとしてのヘテロ環式化合物 |
| 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 |
| WO2020020288A1 (zh) | 2018-07-25 | 2020-01-30 | 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 |
| JP2022509534A (ja) | 2018-10-30 | 2022-01-20 | 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 |
| 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 |
| SG11202107810WA (en) | 2019-01-18 | 2021-08-30 | 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 |
| US11584756B2 (en) | 2019-07-02 | 2023-02-21 | Nuvation Bio Inc. | Heterocyclic compounds as BET inhibitors |
| JP7340100B2 (ja) | 2019-10-28 | 2023-09-06 | メルク・シャープ・アンド・ドーム・エルエルシー | Ｋｒａｓ ｇ１２ｃ変異型の小分子阻害薬 |
| 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 |
| WO2021106230A1 (ja) | 2019-11-29 | 2021-06-03 | 大鵬薬品工業株式会社 | 新規なフェノール化合物又はその塩 |
| 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 |
| MX2022007278A (es) * | 2019-12-18 | 2022-09-19 | Univ Montreal | Moduladores del adaptador kbtbd4 de cullin 3 como compuestos anti-cáncer. |
| 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 |
| US12466840B2 (en) | 2023-10-20 | 2025-11-11 | 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)
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|---|---|---|---|---|
| US5093330A (en) | 1987-06-15 | 1992-03-03 | Ciba-Geigy Corporation | Staurosporine derivatives substituted at methylamino nitrogen |
| WO1998011111A1 (en) | 1996-09-13 | 1998-03-19 | Yoshitomi Pharmaceutical Industries, Ltd. | Thienotriazolodiazepine compounds and medicinal uses thereof |
| US8044042B2 (en) | 2005-05-30 | 2011-10-25 | Mitsubishi Tanabe Pharma Corporation | Thienotriazolodiazepine compound and medicinal use thereof |
| NZ579355A (en) | 2007-02-01 | 2012-03-30 | Resverlogix Corp | 2-(Aryl)-4-oxo-quinazoline derivatives |
| US8431569B2 (en) * | 2007-12-13 | 2013-04-30 | Merck Sharp & Dohme Corp. | 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 |
| SI2346837T1 (sl) | 2008-06-26 | 2015-05-29 | Resverlogix Corporation | Postopki pripravljanja kinazolinonskih derivatov |
| JP5813626B2 (ja) | 2009-04-22 | 2015-11-17 | レスバーロジックス コーポレイション | 新規抗炎症剤 |
| 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 |
| GB0919423D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| GB0919432D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Use |
| WO2011054845A1 (en) | 2009-11-05 | 2011-05-12 | Glaxosmithkline Llc | Benzodiazepine bromodomain inhibitor |
| GB0919426D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| DE102009053235A1 (de) * | 2009-11-06 | 2011-05-19 | Gottwald Port Technology Gmbh | Umschlagsystem für ISO-Container mit einer Containerbrücke |
| CA2799403C (en) | 2010-05-14 | 2020-01-21 | Dana-Farber Cancer Institute, Inc. | Compositions and methods for treating leukemia |
| US20130252331A1 (en) | 2010-05-14 | 2013-09-26 | James Elliott Bradner | Compositions and methods for modulating metabolism |
| BR112012029005A2 (pt) | 2010-05-14 | 2016-07-26 | Dana Farber Cancer Inst Inc | composições e métodos de tratamento de neoplasia, doença inflamatória e outros distúrbios |
| EP2585465B1 (en) | 2010-06-22 | 2014-11-12 | GlaxoSmithKline LLC | Benzotriazolodiazepine compounds inhibitors of bromodomains |
| EP2590972B1 (en) | 2010-07-09 | 2015-01-21 | Pfizer Limited | N-sulfonylbenzamides as inhibitors of voltage-gated sodium channels |
| 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 |
| US20140066410A1 (en) | 2011-02-23 | 2014-03-06 | 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 |
| WO2012174487A2 (en) | 2011-06-17 | 2012-12-20 | 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 |
| US9409906B2 (en) * | 2012-01-27 | 2016-08-09 | Universite De Montreal | Pyrimido[4,5-B]indole derivatives and use thereof in the expansion of hematopoietic stem cells |
| US20130281399A1 (en) | 2012-04-19 | 2013-10-24 | Rvx Therapeutics Inc. | Treatment of diseases by epigenetic regulation |
| MX2014012635A (es) | 2012-04-20 | 2015-05-15 | Abbvie Inc | Derivados de isoindolona. |
| BR112014031068A2 (pt) | 2012-06-12 | 2017-06-27 | Abbvie Inc | derivados piridinona e piridazinona |
| 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 |
| JP6401773B2 (ja) | 2013-03-11 | 2018-10-10 | 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およびこれを用いる治療方法 |
| SI3466949T1 (sl) * | 2013-12-24 | 2021-03-31 | Bristol-Myers Squibb Company | Triciklična spojina kot sredstvo proti raku |
| EP3110818B1 (en) * | 2014-02-28 | 2019-10-23 | The Regents of The University of Michigan | 9h-pyrimido[4,5-b]indoles and related analogs as bet bromodomain inhibitors |
-
2015
- 2015-02-27 EP EP15711599.9A patent/EP3110818B1/en active Active
- 2015-02-27 CN CN201580023829.6A patent/CN107074861A/zh active Pending
- 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 WO PCT/US2015/017908 patent/WO2015131005A1/en not_active Ceased
- 2015-02-27 CA CA2940554A patent/CA2940554A1/en not_active Abandoned
- 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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