JP2020515571A5 - - Google Patents
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- JP2020515571A5 JP2020515571A5 JP2019553080A JP2019553080A JP2020515571A5 JP 2020515571 A5 JP2020515571 A5 JP 2020515571A5 JP 2019553080 A JP2019553080 A JP 2019553080A JP 2019553080 A JP2019553080 A JP 2019553080A JP 2020515571 A5 JP2020515571 A5 JP 2020515571A5
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- Prior art keywords
- cancer
- tumor
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- leukemia
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Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762479520P | 2017-03-31 | 2017-03-31 | |
| US62/479,520 | 2017-03-31 | ||
| PCT/US2018/025417 WO2018183857A1 (en) | 2017-03-31 | 2018-03-30 | Piperidines as covalent menin inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2020515571A JP2020515571A (ja) | 2020-05-28 |
| JP2020515571A5 true JP2020515571A5 (enExample) | 2021-04-30 |
Family
ID=63677047
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019553080A Pending JP2020515571A (ja) | 2017-03-31 | 2018-03-30 | 共有結合性メニン阻害剤としてのピペリジン |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US11045448B2 (enExample) |
| EP (1) | EP3600313A4 (enExample) |
| JP (1) | JP2020515571A (enExample) |
| KR (1) | KR20190133224A (enExample) |
| CN (1) | CN110636843A (enExample) |
| AU (1) | AU2018243586A1 (enExample) |
| BR (1) | BR112019020130A2 (enExample) |
| CA (1) | CA3058448A1 (enExample) |
| EA (1) | EA201992320A1 (enExample) |
| IL (1) | IL269542A (enExample) |
| MX (1) | MX2019011412A (enExample) |
| PH (1) | PH12019502263A1 (enExample) |
| SG (1) | SG11201909083UA (enExample) |
| WO (1) | WO2018183857A1 (enExample) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX384087B (es) | 2016-05-02 | 2025-03-14 | Univ Michigan Regents | Piperidinas como inhibidores de menina. |
| TW202003465A (zh) * | 2018-03-30 | 2020-01-16 | 美國密西根州立大學 | 作為共價menin抑制劑之六氫吡啶化合物 |
| CA3112340A1 (en) * | 2018-10-03 | 2020-04-09 | The Regents Of The University Of Michigan | Small molecule menin inhibitors |
| TW202043205A (zh) | 2018-12-31 | 2020-12-01 | 美商拜歐米富士恩有限公司 | Menin-mll相互作用之抑制劑 |
| MX2021007925A (es) | 2018-12-31 | 2021-10-26 | Biomea Fusion Llc | Inhibidores irreversibles de la interaccion menina-mll. |
| WO2021067215A1 (en) | 2019-09-30 | 2021-04-08 | Agios Pharmaceuticals, Inc. | Piperidine compounds as menin inhibitors |
| WO2021207310A1 (en) | 2020-04-08 | 2021-10-14 | Agios Pharmaceuticals, Inc. | Menin inhibitors and methods of use for treating cancer |
| TW202204333A (zh) | 2020-04-08 | 2022-02-01 | 美商阿吉歐斯製藥公司 | Menin抑制劑及治療癌症之使用方法 |
| EP4263542A1 (en) * | 2020-12-16 | 2023-10-25 | Biomea Fusion, Inc. | Fused pyrimidine compounds as inhibitors of menin-mll interaction |
| CA3228627A1 (en) | 2021-08-11 | 2023-02-16 | Thomas Butler | Covalent inhibitors of menin-mll interaction for diabetes mellitus |
| CN119816500A (zh) | 2021-08-20 | 2025-04-11 | 拜欧米富士恩公司 | 用于治疗癌症的不可逆menin-MLL抑制剂N-[4-[4-(4-吗啉基)-7H-吡咯并[2,3-d]嘧啶-6-基]苯基]-4-[[3(R)-[(1-氧代-2-丙烯-1-基)氨基]-1-哌啶基]甲基]-2-吡啶甲酰胺的结晶形式 |
| WO2023056589A1 (en) | 2021-10-08 | 2023-04-13 | Servier Pharmaceuticals Llc | Menin inhibitors and methods of use for treating cancer |
| AU2023385514A1 (en) | 2022-11-24 | 2025-07-10 | Oryzon Genomics, S.A. | Combinations of lsd1 inhibitors and menin inhibitors for treating cancer |
| WO2024155719A1 (en) | 2023-01-18 | 2024-07-25 | Biomea Fusion, Inc. | Crystalline forms of n-[4-[4-(4-morpholinyl)-7h-pyrrolo[2,3-d]pyrimidin-6-yl]phenyl]-4-[[3(r)-[(l-oxo-2-propen-l-yl)amino]-l-piperidinyl]methyl]-2- pyridinecarboxamide as a covalentinhibitor of menin-mll interaction |
Family Cites Families (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1998054167A1 (en) | 1997-05-28 | 1998-12-03 | Mitsubishi-Tokyo Pharmaceuticals, Inc. | Indole compounds |
| US7576082B2 (en) | 2005-06-24 | 2009-08-18 | Hoffman-La Roche Inc. | Oxindole derivatives |
| WO2008070303A2 (en) | 2006-10-19 | 2008-06-12 | The University Of Chicago | Therapeutics to inhibit mll-menin interaction for treating leukemia |
| WO2011029054A1 (en) | 2009-09-04 | 2011-03-10 | The Regents Of The University Of Michigan | Compositions and methods for treatment of leukemia |
| WO2011060321A1 (en) | 2009-11-16 | 2011-05-19 | Chdi, Inc. | Transglutaminase tg2 inhibitors, pharmaceutical compositions, and methods of use thereof |
| CN103874686B (zh) | 2011-05-09 | 2016-08-17 | 福马Tm有限责任公司 | 用于抑制烟酰胺磷酸核糖基转移酶(nampt)的哌啶衍生物和组合物 |
| ES2583146T3 (es) | 2011-12-01 | 2016-09-19 | Purdue Pharma L.P. | Compuestos de piperidina de tipo quinoxalina sustituidos con azetidina y usos de éstos |
| EP2968342B1 (en) | 2013-03-13 | 2018-10-03 | The Regents of the University of Michigan | Compositions comprising thienopyrimidine and thienopyridine compounds and methods of use thereof |
| WO2014200479A1 (en) | 2013-06-12 | 2014-12-18 | The Regents Of The University Of Michigan | Menin-mll inhibitors and methods of use thereof |
| US9212180B2 (en) * | 2013-06-12 | 2015-12-15 | The Regents Of The University Of Michigan | Menin-MLL inhibitors and methods of use thereof |
| WO2016040330A1 (en) * | 2014-09-09 | 2016-03-17 | The Regents Of The University Of Michigan | Thienopyrimidine and thienopyridine compounds and methods of use thereof |
| AR104020A1 (es) | 2015-06-04 | 2017-06-21 | Kura Oncology Inc | Métodos y composiciones para inhibir la interacción de menina con proteínas mill |
| US10588907B2 (en) | 2015-06-04 | 2020-03-17 | Kura Oncology, Inc. | Methods and compositions for inhibiting the interaction of menin with MLL proteins |
| RU2018126774A (ru) | 2015-12-22 | 2020-01-23 | Витэ Фармасьютикалз, Инк. | Ингибиторы менин-mll взаимодействия |
| KR102419524B1 (ko) | 2016-03-16 | 2022-07-08 | 쿠라 온콜로지, 인크. | 메닌-mll의 가교된 이환식 억제제 및 사용 방법 |
| BR112018068703B1 (pt) | 2016-03-16 | 2024-02-06 | Kura Oncology, Inc. | Inibidores substituídos de menin-mll e métodos de uso |
| MX384087B (es) | 2016-05-02 | 2025-03-14 | Univ Michigan Regents | Piperidinas como inhibidores de menina. |
| PT3468966T (pt) | 2016-06-10 | 2020-11-10 | Vitae Pharmaceuticals Llc | Inibidores da interação menina-mll |
| AR109658A1 (es) | 2016-09-16 | 2019-01-09 | Vitae Pharmaceuticals Inc | Inhibidores de la interacción de menina-mll |
| WO2018106818A1 (en) | 2016-12-07 | 2018-06-14 | Kura Oncology, Inc. | Methods of promoting beta cell proliferation |
| CN117298275A (zh) | 2017-03-24 | 2023-12-29 | 库拉肿瘤学公司 | 治疗血液系统恶性肿瘤和尤因肉瘤的方法 |
| WO2018226976A1 (en) | 2017-06-08 | 2018-12-13 | Kura Oncology, Inc. | Methods and compositions for inhibiting the interaction of menin with mll proteins |
| TW201920170A (zh) | 2017-09-20 | 2019-06-01 | 美商庫拉腫瘤技術股份有限公司 | 經取代之menin-mll 抑制劑及使用方法 |
| US11325921B2 (en) | 2018-03-30 | 2022-05-10 | Sumitomo Dainippon Pharma Co., Ltd. | Optically active crosslinked cyclic secondary amine derivative |
| CN113164443A (zh) | 2018-09-26 | 2021-07-23 | 库拉肿瘤学公司 | 用多发性内分泌抑癌蛋白抑制剂治疗血液系统恶性肿瘤 |
| MX2021007925A (es) | 2018-12-31 | 2021-10-26 | Biomea Fusion Llc | Inhibidores irreversibles de la interaccion menina-mll. |
| TW202043205A (zh) | 2018-12-31 | 2020-12-01 | 美商拜歐米富士恩有限公司 | Menin-mll相互作用之抑制劑 |
-
2018
- 2018-03-30 SG SG11201909083U patent/SG11201909083UA/en unknown
- 2018-03-30 JP JP2019553080A patent/JP2020515571A/ja active Pending
- 2018-03-30 BR BR112019020130A patent/BR112019020130A2/pt not_active Application Discontinuation
- 2018-03-30 AU AU2018243586A patent/AU2018243586A1/en not_active Abandoned
- 2018-03-30 EA EA201992320A patent/EA201992320A1/ru unknown
- 2018-03-30 CN CN201880032488.2A patent/CN110636843A/zh active Pending
- 2018-03-30 US US16/497,856 patent/US11045448B2/en not_active Expired - Fee Related
- 2018-03-30 CA CA3058448A patent/CA3058448A1/en active Pending
- 2018-03-30 EP EP18776755.3A patent/EP3600313A4/en not_active Withdrawn
- 2018-03-30 WO PCT/US2018/025417 patent/WO2018183857A1/en not_active Ceased
- 2018-03-30 PH PH1/2019/502263A patent/PH12019502263A1/en unknown
- 2018-03-30 MX MX2019011412A patent/MX2019011412A/es unknown
- 2018-03-30 KR KR1020197031798A patent/KR20190133224A/ko not_active Ceased
-
2019
- 2019-09-23 IL IL26954219A patent/IL269542A/en unknown
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