CA3014644A1 - Fused 1,4-oxazepines and related analogs as bet bromodomain inhibitors - Google Patents
Fused 1,4-oxazepines and related analogs as bet bromodomain inhibitors Download PDFInfo
- Publication number
- CA3014644A1 CA3014644A1 CA3014644A CA3014644A CA3014644A1 CA 3014644 A1 CA3014644 A1 CA 3014644A1 CA 3014644 A CA3014644 A CA 3014644A CA 3014644 A CA3014644 A CA 3014644A CA 3014644 A1 CA3014644 A1 CA 3014644A1
- Authority
- CA
- Canada
- Prior art keywords
- cancer
- triazolo
- oxazepine
- cell
- thieno
- 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
Classifications
-
- 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
-
- 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
- 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
-
- 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
- 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
-
- 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
Landscapes
- 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 (1)
| Publication Number | Publication Date |
|---|---|
| CA3014644A1 true CA3014644A1 (en) | 2017-08-24 |
Family
ID=58191613
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA3014644A Pending CA3014644A1 (en) | 2016-02-15 | 2017-02-15 | Fused 1,4-oxazepines and related analogs as bet bromodomain inhibitors |
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=) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
Families Citing this family (17)
| 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 |
| 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 |
Family Cites Families (45)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| EA018612B1 (ru) * | 2008-01-24 | 2013-09-30 | Панацеа Биотек Лимитед | Новые гетероциклические соединения |
| KR101629356B1 (ko) | 2008-06-26 | 2016-06-13 | 리스버로직스 코퍼레이션 | 퀴나졸리논 유도체의 제조방법 |
| US20110136790A1 (en) * | 2008-07-23 | 2011-06-09 | De Lera Ruiz Manuel | Tricyclic Heterocyclic Derivatives and Methods of Use |
| 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 |
| PL2902030T3 (pl) * | 2010-05-14 | 2017-07-31 | Dana-Farber Cancer Institute, Inc. | Związki tienotriazolodiazepinowe do leczenia nowotworu |
| MX354217B (es) | 2010-05-14 | 2018-02-19 | Dana Farber Cancer Inst Inc | Composiciones y metodos para el tratamiento de leucemia. |
| WO2011143651A1 (en) | 2010-05-14 | 2011-11-17 | Dana-Farber Cancer Institute, Inc. | Compositions and methods for modulating metabolism |
| US9085582B2 (en) | 2010-06-22 | 2015-07-21 | Glaxosmithkline Llc | Benzotriazolodiazepine compounds inhibitors of bromodomains |
| 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 |
| EP2677865A4 (en) | 2011-02-23 | 2015-04-22 | Icahn School Med Mount Sinai | BROMODOMAIN INHIBITORS AS MODULATORS OF GENE EXPRESSION |
| WO2012151512A2 (en) | 2011-05-04 | 2012-11-08 | Constellation Pharmaceuticals, Inc. | Bromodomain inhibitors and uses thereof |
| EP2721031B1 (en) | 2011-06-17 | 2016-01-20 | 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 |
| WO2013064231A1 (en) * | 2011-10-31 | 2013-05-10 | Phenex Pharmaceuticals Ag | SEVEN-MEMBERED SULFONAMIDES AS MODULATORS OF RAR-RELATED ORPHAN RECEPTOR-GAMMA (RORγ, NR1F3) |
| WO2013097052A1 (en) | 2011-12-30 | 2013-07-04 | Abbott Laboratories | Bromodomain inhibitors |
| US20130281399A1 (en) | 2012-04-19 | 2013-10-24 | Rvx Therapeutics Inc. | Treatment of diseases by epigenetic regulation |
| EP2838881B1 (en) | 2012-04-20 | 2018-08-08 | AbbVie Inc. | Isoindolone derivatives |
| JP6215315B2 (ja) | 2012-06-12 | 2017-10-18 | アッヴィ・インコーポレイテッド | ピリジノンおよびピリダジノン誘導体 |
| EP2958923A1 (de) * | 2013-02-22 | 2015-12-30 | Bayer Pharma Aktiengesellschaft | 4-substituierte pyrrolo- und pyrazolo-diazepine |
| EP2970312B1 (en) | 2013-03-11 | 2017-11-15 | The Regents of The University of Michigan | Bet bromodomain inhibitors and therapeutic methods using the same |
| AU2015247817C1 (en) | 2014-04-14 | 2022-02-10 | Arvinas Operations, Inc. | Imide-based modulators of proteolysis and associated methods of use |
| GB201504314D0 (en) | 2015-03-13 | 2015-04-29 | Univ Dundee | Small molecules |
| EP3454862B1 (en) | 2016-05-10 | 2024-09-11 | C4 Therapeutics, Inc. | Spirocyclic degronimers for target protein degradation |
| EP3700901A1 (en) | 2017-10-24 | 2020-09-02 | Genentech, Inc. | (4-hydroxypyrrolidin-2-yl)-heterocyclic compounds and methods of use thereof |
| WO2019246430A1 (en) | 2018-06-21 | 2019-12-26 | Foghorn Therapeutics Inc. | Methods of treating disorders |
| EP3813834B1 (en) | 2018-06-29 | 2025-03-26 | Dana-Farber Cancer Institute, Inc. | New crbn modulators |
| US12060366B2 (en) | 2018-06-29 | 2024-08-13 | Dana-Farber Cancer Institute, Inc. | Bispecific degraders |
| TW202019946A (zh) | 2018-07-04 | 2020-06-01 | 日商田邊三菱製藥股份有限公司 | 具有bet蛋白質分解誘導作用的醯胺化合物及其作為醫藥的用途 |
| CA3102996A1 (en) | 2018-07-20 | 2020-01-23 | Dana-Farber Cancer Institute, Inc. | Degraders that target proteins via keap1 |
-
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
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
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 |
| CN109071562B (zh) | 2022-03-22 |
| WO2017142881A1 (en) | 2017-08-24 |
| US11548899B2 (en) | 2023-01-10 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| EEER | Examination request |
Effective date: 20220208 |