CN109071562B - 作为bet溴结构域抑制剂的稠合1,4-氧氮杂䓬和相关类似物 - Google Patents
作为bet溴结构域抑制剂的稠合1,4-氧氮杂䓬和相关类似物 Download PDFInfo
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- CN109071562B CN109071562B CN201780023735.8A CN201780023735A CN109071562B CN 109071562 B CN109071562 B CN 109071562B CN 201780023735 A CN201780023735 A CN 201780023735A CN 109071562 B CN109071562 B CN 109071562B
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- triazolo
- oxazazem
- methyl
- thieno
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D495/14—Ortho-condensed systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D498/14—Ortho-condensed systems
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Oncology (AREA)
- Immunology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Communicable Diseases (AREA)
- Epidemiology (AREA)
- Hematology (AREA)
- Transplantation (AREA)
- Virology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662295271P | 2016-02-15 | 2016-02-15 | |
| US62/295,271 | 2016-02-15 | ||
| US201662393897P | 2016-09-13 | 2016-09-13 | |
| US62/393,897 | 2016-09-13 | ||
| PCT/US2017/017848 WO2017142881A1 (en) | 2016-02-15 | 2017-02-15 | Fused 1,4-oxazepines and related analogs as bet bromodomain inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN109071562A CN109071562A (zh) | 2018-12-21 |
| CN109071562B true CN109071562B (zh) | 2022-03-22 |
Family
ID=58191613
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201780023735.8A Expired - Fee Related CN109071562B (zh) | 2016-02-15 | 2017-02-15 | 作为bet溴结构域抑制剂的稠合1,4-氧氮杂䓬和相关类似物 |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US11548899B2 (https=) |
| EP (1) | EP3416969B1 (https=) |
| JP (1) | JP6967522B2 (https=) |
| CN (1) | CN109071562B (https=) |
| AU (1) | AU2017219627B2 (https=) |
| CA (1) | CA3014644A1 (https=) |
| ES (1) | ES2882066T3 (https=) |
| WO (1) | WO2017142881A1 (https=) |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3512855B1 (en) * | 2016-09-13 | 2022-07-27 | The Regents of the University of Michigan | Fused 1,4-oxazepines as bet protein degraders |
| WO2019055444A1 (en) * | 2017-09-13 | 2019-03-21 | The Regents Of The University Of Michigan | DEGRADATION AGENTS OF BROMODOMAIN BET PROTEIN WITH CLEAR BINDERS |
| CN115466315A (zh) * | 2021-06-10 | 2022-12-13 | 首都医科大学 | 抑制侵袭的1-咪唑-β-咔啉-3-甲酰-RGDS及制备,抗癌转移作用和应用 |
| CN116410205B (zh) * | 2021-12-29 | 2024-07-05 | 上海皓元生物医药科技有限公司 | 一种3-取代-9-甲基-噻吩并三唑并噁嗪类化合物的制备方法 |
| AU2024265078A1 (en) | 2023-05-04 | 2025-12-11 | Revolution Medicines, Inc. | Combination therapy for a ras related disease or disorder |
| IL326136A (en) | 2023-08-07 | 2026-03-01 | Revolution Medicines Inc | RMC-6291 for use in the treatment of a disease or disorder associated with the RAS protein |
| US20250154171A1 (en) | 2023-10-12 | 2025-05-15 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025240847A1 (en) | 2024-05-17 | 2025-11-20 | Revolution Medicines, Inc. | Ras inhibitors |
| US20250375445A1 (en) | 2024-06-07 | 2025-12-11 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| WO2025265060A1 (en) | 2024-06-21 | 2025-12-26 | Revolution Medicines, Inc. | Therapeutic compositions and methods for managing treatment-related effects |
| WO2026006747A1 (en) | 2024-06-28 | 2026-01-02 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026015825A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Use of ras inhibitor for treating pancreatic cancer |
| WO2026015796A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015801A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015790A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026050446A1 (en) | 2024-08-29 | 2026-03-05 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026072904A2 (en) | 2024-09-26 | 2026-04-02 | Revolution Medicines, Inc. | Compositions and methods for treating lung cancer |
Citations (5)
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| WO2010011653A1 (en) * | 2008-07-23 | 2010-01-28 | Schering Corporation | Tricyclic heterocycle derivatives as histamine h3 antagonists |
| CN101925586A (zh) * | 2008-01-24 | 2010-12-22 | 万能药生物有限公司 | 新的杂环化合物 |
| CN103037865A (zh) * | 2010-05-14 | 2013-04-10 | 达那-法伯癌症研究所 | 用于治疗瘤形成、炎性疾病和其他失调的组合物和方法 |
| WO2013064231A1 (en) * | 2011-10-31 | 2013-05-10 | Phenex Pharmaceuticals Ag | SEVEN-MEMBERED SULFONAMIDES AS MODULATORS OF RAR-RELATED ORPHAN RECEPTOR-GAMMA (RORγ, NR1F3) |
| CN105164135A (zh) * | 2013-02-22 | 2015-12-16 | 拜耳医药股份有限公司 | 4-取代的吡咯并二氮杂卓和吡唑并二氮杂卓 |
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| 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 |
| 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 |
| RS54645B1 (sr) | 2009-11-05 | 2016-08-31 | Glaxosmithkline Llc | Benzodiazepin kao inhibitor bromodomena |
| GB0919423D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| JP5715241B2 (ja) * | 2010-05-14 | 2015-05-07 | ダナ−ファーバー キャンサー インスティテュート, インコーポレイテッド | 新生物、炎症性疾患、およびその他の障害を治療するための組成物および方法 |
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| EP2970312B1 (en) | 2013-03-11 | 2017-11-15 | The Regents of The University of Michigan | Bet bromodomain inhibitors and therapeutic methods using the same |
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-
2017
- 2017-02-15 EP EP17708046.2A patent/EP3416969B1/en active Active
- 2017-02-15 US US16/077,844 patent/US11548899B2/en active Active
- 2017-02-15 AU AU2017219627A patent/AU2017219627B2/en not_active Ceased
- 2017-02-15 ES ES17708046T patent/ES2882066T3/es active Active
- 2017-02-15 WO PCT/US2017/017848 patent/WO2017142881A1/en not_active Ceased
- 2017-02-15 CN CN201780023735.8A patent/CN109071562B/zh not_active Expired - Fee Related
- 2017-02-15 CA CA3014644A patent/CA3014644A1/en active Pending
- 2017-02-15 JP JP2018543139A patent/JP6967522B2/ja not_active Expired - Fee Related
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101925586A (zh) * | 2008-01-24 | 2010-12-22 | 万能药生物有限公司 | 新的杂环化合物 |
| WO2010011653A1 (en) * | 2008-07-23 | 2010-01-28 | Schering Corporation | Tricyclic heterocycle derivatives as histamine h3 antagonists |
| CN103037865A (zh) * | 2010-05-14 | 2013-04-10 | 达那-法伯癌症研究所 | 用于治疗瘤形成、炎性疾病和其他失调的组合物和方法 |
| WO2013064231A1 (en) * | 2011-10-31 | 2013-05-10 | Phenex Pharmaceuticals Ag | SEVEN-MEMBERED SULFONAMIDES AS MODULATORS OF RAR-RELATED ORPHAN RECEPTOR-GAMMA (RORγ, NR1F3) |
| CN105164135A (zh) * | 2013-02-22 | 2015-12-16 | 拜耳医药股份有限公司 | 4-取代的吡咯并二氮杂卓和吡唑并二氮杂卓 |
Non-Patent Citations (1)
| Title |
|---|
| Bicyclic and tricyclic heterocycle derivatives as histamine H3 receptor antagonists for the treatment of obesity;Manuel de Lera Ruiz et al.;《Bioorganic & Medicinal Chemistry Letters》;20130819;第23卷;第6006页Table 1 * |
Also Published As
| Publication number | Publication date |
|---|---|
| JP6967522B2 (ja) | 2021-11-17 |
| ES2882066T3 (es) | 2021-12-01 |
| EP3416969B1 (en) | 2021-05-05 |
| JP2019507143A (ja) | 2019-03-14 |
| CN109071562A (zh) | 2018-12-21 |
| US20210188870A1 (en) | 2021-06-24 |
| AU2017219627B2 (en) | 2021-08-05 |
| AU2017219627A1 (en) | 2018-09-20 |
| EP3416969A1 (en) | 2018-12-26 |
| WO2017142881A1 (en) | 2017-08-24 |
| US11548899B2 (en) | 2023-01-10 |
| CA3014644A1 (en) | 2017-08-24 |
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