CN110636843A - 作为共价多发性内分泌腺瘤蛋白抑制剂的哌啶 - Google Patents
作为共价多发性内分泌腺瘤蛋白抑制剂的哌啶 Download PDFInfo
- Publication number
- CN110636843A CN110636843A CN201880032488.2A CN201880032488A CN110636843A CN 110636843 A CN110636843 A CN 110636843A CN 201880032488 A CN201880032488 A CN 201880032488A CN 110636843 A CN110636843 A CN 110636843A
- Authority
- CN
- China
- Prior art keywords
- compound
- pharmaceutically acceptable
- solvate
- acceptable salt
- cancer
- 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.)
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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)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (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)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicinal Preparation (AREA)
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 (1)
| Publication Number | Publication Date |
|---|---|
| CN110636843A true CN110636843A (zh) | 2019-12-31 |
Family
ID=63677047
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201880032488.2A Pending CN110636843A (zh) | 2017-03-31 | 2018-03-30 | 作为共价多发性内分泌腺瘤蛋白抑制剂的哌啶 |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US11045448B2 (https=) |
| EP (1) | EP3600313A4 (https=) |
| JP (1) | JP2020515571A (https=) |
| KR (1) | KR20190133224A (https=) |
| CN (1) | CN110636843A (https=) |
| AU (1) | AU2018243586A1 (https=) |
| BR (1) | BR112019020130A2 (https=) |
| CA (1) | CA3058448A1 (https=) |
| EA (1) | EA201992320A1 (https=) |
| IL (1) | IL269542A (https=) |
| MX (1) | MX2019011412A (https=) |
| PH (1) | PH12019502263A1 (https=) |
| SG (1) | SG11201909083UA (https=) |
| WO (1) | WO2018183857A1 (https=) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN113166059A (zh) * | 2018-10-03 | 2021-07-23 | 密歇根大学董事会 | 小分子menin抑制剂 |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2017192543A1 (en) | 2016-05-02 | 2017-11-09 | Regents Of The University Of Michigan | Piperidines as menin inhibitors |
| JP2021519785A (ja) * | 2018-03-30 | 2021-08-12 | ザ リージェンツ オブ ザ ユニヴァシティ オブ ミシガン | 共有結合性メニン阻害剤としてのピペリジン化合物 |
| EP3906026A4 (en) * | 2018-12-31 | 2022-10-19 | Biomea Fusion, LLC | IRREVERSIBLE INHIBITORS OF MENIN-MLL INTERACTION |
| 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 |
| TW202126636A (zh) | 2019-09-30 | 2021-07-16 | 美商阿吉歐斯製藥公司 | 作為ｍｅｎｉｎ抑制劑之六氫吡啶化合物 |
| 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 |
| US20240124467A1 (en) * | 2020-12-16 | 2024-04-18 | Biomea Fusion, Inc. | Fused pyrimidine compounds as inhibitors of menin-mll interaction |
| AU2022325861A1 (en) | 2021-08-11 | 2024-02-29 | Biomea Fusion, Inc. | Covalent inhibitors of menin-mll interaction for diabetes mellitus |
| IL310717A (en) | 2021-08-20 | 2024-04-01 | Biomea Fusion Inc | Crystalline form of N-[4-[4-(4-morpholinyl)-7H-PYRROLO[2,3-D]PYRIMIDIN-6-YL]PHENYL]-4-[[3(R)-[(1-OXO ] -2-PROPEN-1-YL)AMINO]-1-PIPERIDINYL]METHYL]-2-PYRIDINECARBOXAMIDE, IRREVERSIBLE MENIN-MLL INHIBITOR FOR CANCER TREATMENT |
| WO2023056589A1 (en) | 2021-10-08 | 2023-04-13 | Servier Pharmaceuticals Llc | Menin inhibitors and methods of use for treating cancer |
| SE546936C2 (en) | 2021-10-15 | 2025-03-11 | Skechers Usa Inc Ii | A shoe comprising a heel cup attached to an interior compressible layer |
| CN120529900A (zh) | 2022-11-24 | 2025-08-22 | 奥莱松基因组股份有限公司 | 用于治疗癌症的LSD1抑制剂和Menin抑制剂的组合 |
| WO2024155710A1 (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 covalent inhibitor of menin-mll interaction |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103874686A (zh) * | 2011-05-09 | 2014-06-18 | 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 |
| US20140371239A1 (en) * | 2013-06-12 | 2014-12-18 | 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 |
Family Cites Families (24)
| 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 |
| US8242078B2 (en) | 2006-10-19 | 2012-08-14 | The University Of Chicago | Therapeutics to inhibit MLL-menin interaction for treating leukemia |
| EP2473054B1 (en) | 2009-09-04 | 2017-06-14 | 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 |
| AU2012324015A1 (en) | 2011-12-01 | 2013-06-20 | Purdue Pharma L.P. | Azetidine-substituted quinoxaline-type piperidine compounds and uses thererof |
| KR20150130389A (ko) | 2013-03-13 | 2015-11-23 | 더 리젠츠 오브 더 유니버시티 오브 미시간 | 티에노피리미딘 및 티에노피리딘 화합물을 포함하는 조성물 및 이의 사용 방법 |
| WO2014200479A1 (en) | 2013-06-12 | 2014-12-18 | The Regents Of The University Of Michigan | Menin-mll inhibitors and methods of use thereof |
| WO2016197027A1 (en) | 2015-06-04 | 2016-12-08 | Kura Oncology, Inc. | Methods and compositions for inhibiting the interaction of menin with mll proteins |
| AR104020A1 (es) | 2015-06-04 | 2017-06-21 | Kura Oncology Inc | Métodos y composiciones para inhibir la interacción de menina con proteínas mill |
| AU2016378579A1 (en) | 2015-12-22 | 2018-06-14 | Vitae Pharmaceuticals, Inc. | Inhibitors of the menin-MLL interaction |
| CN109152784B (zh) | 2016-03-16 | 2021-12-28 | 库拉肿瘤学公司 | 经取代的menin-mll抑制剂及使用方法 |
| CN109640987B (zh) | 2016-03-16 | 2022-12-02 | 库拉肿瘤学公司 | Menin-mll的桥联双环抑制剂及使用方法 |
| WO2017192543A1 (en) | 2016-05-02 | 2017-11-09 | Regents Of The University Of Michigan | Piperidines as menin inhibitors |
| EP3805215A1 (en) | 2016-06-10 | 2021-04-14 | Vitae Pharmaceuticals, LLC | Inhibitors of the menin-mll interaction |
| US10899758B2 (en) | 2016-09-16 | 2021-01-26 | Vitae Pharmaceuticals, Llc | Inhibitors of the menin-MLL interaction |
| WO2018106818A1 (en) | 2016-12-07 | 2018-06-14 | Kura Oncology, Inc. | Methods of promoting beta cell proliferation |
| CN110691779B (zh) | 2017-03-24 | 2023-10-10 | 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 |
| US11542248B2 (en) | 2017-06-08 | 2023-01-03 | Kura Oncology, Inc. | Methods and compositions for inhibiting the interaction of menin with MLL proteins |
| US11649251B2 (en) | 2017-09-20 | 2023-05-16 | Kura Oncology, Inc. | Substituted inhibitors of menin-MLL and methods of use |
| US11325921B2 (en) | 2018-03-30 | 2022-05-10 | Sumitomo Dainippon Pharma Co., Ltd. | Optically active crosslinked cyclic secondary amine derivative |
| EP3856173A4 (en) | 2018-09-26 | 2022-07-06 | Kura Oncology, Inc. | TREATMENT OF HEMATOLOGICAL MALIGNITIES WITH MENIN INHIBITORS |
| EP3906026A4 (en) | 2018-12-31 | 2022-10-19 | Biomea Fusion, LLC | IRREVERSIBLE INHIBITORS OF MENIN-MLL INTERACTION |
| 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 CA CA3058448A patent/CA3058448A1/en active Pending
- 2018-03-30 AU AU2018243586A patent/AU2018243586A1/en not_active Abandoned
- 2018-03-30 WO PCT/US2018/025417 patent/WO2018183857A1/en not_active Ceased
- 2018-03-30 EA EA201992320A patent/EA201992320A1/ru unknown
- 2018-03-30 US US16/497,856 patent/US11045448B2/en not_active Expired - Fee Related
- 2018-03-30 SG SG11201909083U patent/SG11201909083UA/en unknown
- 2018-03-30 CN CN201880032488.2A patent/CN110636843A/zh active Pending
- 2018-03-30 BR BR112019020130A patent/BR112019020130A2/pt not_active Application Discontinuation
- 2018-03-30 MX MX2019011412A patent/MX2019011412A/es unknown
- 2018-03-30 EP EP18776755.3A patent/EP3600313A4/en not_active Withdrawn
- 2018-03-30 KR KR1020197031798A patent/KR20190133224A/ko not_active Ceased
- 2018-03-30 PH PH1/2019/502263A patent/PH12019502263A1/en unknown
- 2018-03-30 JP JP2019553080A patent/JP2020515571A/ja active Pending
-
2019
- 2019-09-23 IL IL26954219A patent/IL269542A/en unknown
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103874686A (zh) * | 2011-05-09 | 2014-06-18 | 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 |
| US20140371239A1 (en) * | 2013-06-12 | 2014-12-18 | 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 |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN113166059A (zh) * | 2018-10-03 | 2021-07-23 | 密歇根大学董事会 | 小分子menin抑制剂 |
Also Published As
| Publication number | Publication date |
|---|---|
| IL269542A (en) | 2019-11-28 |
| EP3600313A1 (en) | 2020-02-05 |
| SG11201909083UA (en) | 2019-10-30 |
| US20200022953A1 (en) | 2020-01-23 |
| MX2019011412A (es) | 2020-02-07 |
| CA3058448A1 (en) | 2018-10-04 |
| EP3600313A4 (en) | 2020-09-23 |
| WO2018183857A1 (en) | 2018-10-04 |
| BR112019020130A2 (pt) | 2020-04-22 |
| EA201992320A1 (ru) | 2020-04-22 |
| US11045448B2 (en) | 2021-06-29 |
| JP2020515571A (ja) | 2020-05-28 |
| AU2018243586A1 (en) | 2019-10-17 |
| PH12019502263A1 (en) | 2020-10-26 |
| KR20190133224A (ko) | 2019-12-02 |
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| Date | Code | Title | Description |
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| PB01 | Publication | ||
| PB01 | Publication | ||
| SE01 | Entry into force of request for substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| WD01 | Invention patent application deemed withdrawn after publication | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20191231 |