EA201992320A1 - Пиперидины в качестве ковалентных ингибиторов менина - Google Patents
Пиперидины в качестве ковалентных ингибиторов менинаInfo
- Publication number
- EA201992320A1 EA201992320A1 EA201992320A EA201992320A EA201992320A1 EA 201992320 A1 EA201992320 A1 EA 201992320A1 EA 201992320 A EA201992320 A EA 201992320A EA 201992320 A EA201992320 A EA 201992320A EA 201992320 A1 EA201992320 A1 EA 201992320A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- piperidines
- covalent
- menin
- menin inhibitors
- formula
- Prior art date
Links
- 102100030550 Menin Human genes 0.000 title abstract 2
- 101710169972 Menin Proteins 0.000 title abstract 2
- 239000003112 inhibitor Substances 0.000 title 1
- 150000003053 piperidines Chemical class 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 2
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 230000005764 inhibitory process Effects 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/397—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D205/00—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
- C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
- C07D205/04—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762479520P | 2017-03-31 | 2017-03-31 | |
| PCT/US2018/025417 WO2018183857A1 (en) | 2017-03-31 | 2018-03-30 | Piperidines as covalent menin inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| EA201992320A1 true EA201992320A1 (ru) | 2020-04-22 |
Family
ID=63677047
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201992320A EA201992320A1 (ru) | 2017-03-31 | 2018-03-30 | Пиперидины в качестве ковалентных ингибиторов менина |
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
Also Published As
| Publication number | Publication date |
|---|---|
| KR20190133224A (ko) | 2019-12-02 |
| EP3600313A4 (en) | 2020-09-23 |
| CN110636843A (zh) | 2019-12-31 |
| US11045448B2 (en) | 2021-06-29 |
| CA3058448A1 (en) | 2018-10-04 |
| MX2019011412A (es) | 2020-02-07 |
| AU2018243586A1 (en) | 2019-10-17 |
| EP3600313A1 (en) | 2020-02-05 |
| WO2018183857A1 (en) | 2018-10-04 |
| BR112019020130A2 (pt) | 2020-04-22 |
| US20200022953A1 (en) | 2020-01-23 |
| IL269542A (en) | 2019-11-28 |
| SG11201909083UA (en) | 2019-10-30 |
| JP2020515571A (ja) | 2020-05-28 |
| PH12019502263A1 (en) | 2020-10-26 |
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