ES2882066T3 - 1,4-oxazepinas fusionadas y análogos relacionados como inhibidores de bromodominio BET - Google Patents
1,4-oxazepinas fusionadas y análogos relacionados como inhibidores de bromodominio BET Download PDFInfo
- Publication number
- ES2882066T3 ES2882066T3 ES17708046T ES17708046T ES2882066T3 ES 2882066 T3 ES2882066 T3 ES 2882066T3 ES 17708046 T ES17708046 T ES 17708046T ES 17708046 T ES17708046 T ES 17708046T ES 2882066 T3 ES2882066 T3 ES 2882066T3
- Authority
- ES
- Spain
- Prior art keywords
- triazolo
- oxazepine
- methyl
- thieno
- dimethyl
- 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.)
- Active
Links
- 0 CC(*)(*C(*)(*)c1nnc(*)[n]1-1)c2c-1[s]c(*)c2* Chemical compound CC(*)(*C(*)(*)c1nnc(*)[n]1-1)c2c-1[s]c(*)c2* 0.000 description 16
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- TXIOGJHPPVXTOY-UHFFFAOYSA-N CCN1CCN(C)CC1 Chemical compound CCN1CCN(C)CC1 TXIOGJHPPVXTOY-UHFFFAOYSA-N 0.000 description 1
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- WKOOCBNYIUQIKN-JTQLQIEISA-N C[C@@H](c1nnc(C)[n]1-1)OCc2c-1[s]c(Br)c2Cc1ccccc1 Chemical compound C[C@@H](c1nnc(C)[n]1-1)OCc2c-1[s]c(Br)c2Cc1ccccc1 WKOOCBNYIUQIKN-JTQLQIEISA-N 0.000 description 1
- IFVRGYHCCBLUKD-AWEZNQCLSA-N C[C@@H](c1nnc(C)[n]1-1)OCc2c-1[s]c(C#CCCO)c2Cc1ccccc1 Chemical compound C[C@@H](c1nnc(C)[n]1-1)OCc2c-1[s]c(C#CCCO)c2Cc1ccccc1 IFVRGYHCCBLUKD-AWEZNQCLSA-N 0.000 description 1
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- RACKOVAPLUVOJA-UHFFFAOYSA-N C[n]1ncc(C#C)c1 Chemical compound C[n]1ncc(C#C)c1 RACKOVAPLUVOJA-UHFFFAOYSA-N 0.000 description 1
- BKNUEFIETPVROC-UHFFFAOYSA-N Cc([s]c-1c2COCc3nnc(C)[n]-13)c2C1=CCCc2c1ccc(F)c2 Chemical compound Cc([s]c-1c2COCc3nnc(C)[n]-13)c2C1=CCCc2c1ccc(F)c2 BKNUEFIETPVROC-UHFFFAOYSA-N 0.000 description 1
- WYQUIEODMZMDBL-UHFFFAOYSA-N Cc1c(Cc(cccc2)c2F)c(COCc2nnc(C)[n]2-2)c-2[s]1 Chemical compound Cc1c(Cc(cccc2)c2F)c(COCc2nnc(C)[n]2-2)c-2[s]1 WYQUIEODMZMDBL-UHFFFAOYSA-N 0.000 description 1
- XRPHQQVHMCFFOH-UHFFFAOYSA-N Cc1c(Cc2ccccc2)c(CN(C)Cc2nnc(C)[n]2-2)c-2[s]1 Chemical compound Cc1c(Cc2ccccc2)c(CN(C)Cc2nnc(C)[n]2-2)c-2[s]1 XRPHQQVHMCFFOH-UHFFFAOYSA-N 0.000 description 1
- IDSWMFYTNLOBAO-UHFFFAOYSA-N Cc1c(Cc2ccccc2)c(CNCc2nnc(C)[n]2-2)c-2[s]1 Chemical compound Cc1c(Cc2ccccc2)c(CNCc2nnc(C)[n]2-2)c-2[s]1 IDSWMFYTNLOBAO-UHFFFAOYSA-N 0.000 description 1
- IIJBTVGDUHWUAA-UHFFFAOYSA-N Cc1c2N(C)CCOc2ccc1 Chemical compound Cc1c2N(C)CCOc2ccc1 IIJBTVGDUHWUAA-UHFFFAOYSA-N 0.000 description 1
- PLLLBSPBFALBFB-UHFFFAOYSA-N Cc1c[s]c(N)c1C(OC)=O Chemical compound Cc1c[s]c(N)c1C(OC)=O PLLLBSPBFALBFB-UHFFFAOYSA-N 0.000 description 1
- OWLHUJGVZQUUQP-UHFFFAOYSA-N Cc1cc(CO)c(NC(CCl)=O)[s]1 Chemical compound Cc1cc(CO)c(NC(CCl)=O)[s]1 OWLHUJGVZQUUQP-UHFFFAOYSA-N 0.000 description 1
- HRSALGWDVBUUBJ-UHFFFAOYSA-N Cc1cc(COCC(N2)=O)c2[s]1 Chemical compound Cc1cc(COCC(N2)=O)c2[s]1 HRSALGWDVBUUBJ-UHFFFAOYSA-N 0.000 description 1
- XGWXDMJKXOJAPJ-UHFFFAOYSA-N Cc1nnc(COC2)[n]1-c([s]1)c2c(Cc2ccccc2)c1Br Chemical compound Cc1nnc(COC2)[n]1-c([s]1)c2c(Cc2ccccc2)c1Br XGWXDMJKXOJAPJ-UHFFFAOYSA-N 0.000 description 1
- XTICQJWUZPDKAF-UHFFFAOYSA-N Cc1nnc(COC2)[n]1-c(cc1)c2c(CN)c1Cl Chemical compound Cc1nnc(COC2)[n]1-c(cc1)c2c(CN)c1Cl XTICQJWUZPDKAF-UHFFFAOYSA-N 0.000 description 1
- APOVNXBBFLSURM-UHFFFAOYSA-N Cc1nnc(COC2)[n]1-c1c2c(C(CO)(c2ccccc2)O)ccc1 Chemical compound Cc1nnc(COC2)[n]1-c1c2c(C(CO)(c2ccccc2)O)ccc1 APOVNXBBFLSURM-UHFFFAOYSA-N 0.000 description 1
- KGZGFVYBBYRGGW-UHFFFAOYSA-N Cc1nnc(COC2)[n]1-c1c2c(C(c2ccccc2)=C)ccc1 Chemical compound Cc1nnc(COC2)[n]1-c1c2c(C(c2ccccc2)=C)ccc1 KGZGFVYBBYRGGW-UHFFFAOYSA-N 0.000 description 1
- JGKOYBJMDMVWOL-UHFFFAOYSA-N Cc1nnc(COC2)[n]1-c1c2c(Cc2ccccc2)c(C#N)[s]1 Chemical compound Cc1nnc(COC2)[n]1-c1c2c(Cc2ccccc2)c(C#N)[s]1 JGKOYBJMDMVWOL-UHFFFAOYSA-N 0.000 description 1
- VINVQQFDCLOPMA-UHFFFAOYSA-N Cc1nnc(COC2)[n]1-c1c2c(Sc2ccccc2)ccc1 Chemical compound Cc1nnc(COC2)[n]1-c1c2c(Sc2ccccc2)ccc1 VINVQQFDCLOPMA-UHFFFAOYSA-N 0.000 description 1
- VJEAHPCNDKMPEB-UHFFFAOYSA-N Cc1nnc(COC2)[n]1C1=C2C(Cc2ccccc2)CS1 Chemical compound Cc1nnc(COC2)[n]1C1=C2C(Cc2ccccc2)CS1 VJEAHPCNDKMPEB-UHFFFAOYSA-N 0.000 description 1
- WJSIHBNDVHSGNQ-UHFFFAOYSA-N Cc1nnc2[n]1-c1cccc(S(c3ccccc3)(=O)=O)c1COC2 Chemical compound Cc1nnc2[n]1-c1cccc(S(c3ccccc3)(=O)=O)c1COC2 WJSIHBNDVHSGNQ-UHFFFAOYSA-N 0.000 description 1
- VRGHJEFRBREWMJ-UHFFFAOYSA-N Cc1nnc2[n]1-c1cccc([S-](c3ccccc3)[O-])c1COC2 Chemical compound Cc1nnc2[n]1-c1cccc([S-](c3ccccc3)[O-])c1COC2 VRGHJEFRBREWMJ-UHFFFAOYSA-N 0.000 description 1
- HZTMYTXWFHBHDC-UHFFFAOYSA-N Ic1ccc2OCCOc2c1 Chemical compound Ic1ccc2OCCOc2c1 HZTMYTXWFHBHDC-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- 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
- C07D498/12—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
- 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)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Oncology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Communicable Diseases (AREA)
- Epidemiology (AREA)
- Transplantation (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Virology (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662295271P | 2016-02-15 | 2016-02-15 | |
| US201662393897P | 2016-09-13 | 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 |
|---|---|
| ES2882066T3 true ES2882066T3 (es) | 2021-12-01 |
Family
ID=58191613
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES17708046T Active ES2882066T3 (es) | 2016-02-15 | 2017-02-15 | 1,4-oxazepinas fusionadas y análogos relacionados como inhibidores de bromodominio BET |
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 |
|---|---|---|---|---|
| CA3036834A1 (en) * | 2016-09-13 | 2018-03-22 | 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 |
| TW202508595A (zh) | 2023-05-04 | 2025-03-01 | 美商銳新醫藥公司 | 用於ｒａｓ相關疾病或病症之組合療法 |
| US20250049810A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| AU2024360465A1 (en) | 2023-10-12 | 2026-04-09 | Revolution Medicines, Inc. | Macrocyclic ras inhibitors |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| TW202547461A (zh) | 2024-05-17 | 2025-12-16 | 美商銳新醫藥公司 | Ｒａｓ抑制劑 |
| WO2025255438A1 (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 |
| WO2026015801A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015796A1 (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 |
| WO2026015825A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Use of ras inhibitor for treating pancreatic cancer |
| 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 |
| CN1109037C (zh) | 1996-09-13 | 2003-05-21 | 三菱制药株式会社 | 噻吩并－三唑并二氮杂䓬化合物及其医药用途 |
| WO2006129623A1 (ja) | 2005-05-30 | 2006-12-07 | Mitsubishi Tanabe Pharma Corporation | チエノトリアゾロジアゼピン化合物及びその医薬としての用途 |
| PT2118074E (pt) | 2007-02-01 | 2014-03-20 | Resverlogix Corp | Compostos para a prevenção e tratamento de doenças cardiovasculares |
| KR101600634B1 (ko) | 2007-12-28 | 2016-03-07 | 미쓰비시 타나베 파마 코퍼레이션 | 항암제 |
| US8455479B2 (en) * | 2008-01-24 | 2013-06-04 | Panacea Biotec Limited | Heterocyclic compounds |
| SI2346837T1 (sl) | 2008-06-26 | 2015-05-29 | Resverlogix Corporation | Postopki pripravljanja kinazolinonskih derivatov |
| US20110136790A1 (en) * | 2008-07-23 | 2011-06-09 | De Lera Ruiz Manuel | Tricyclic Heterocyclic Derivatives and Methods of Use |
| US9757368B2 (en) | 2009-04-22 | 2017-09-12 | Resverlogix Corp. | Anti-inflammatory agents |
| DE102009051823A1 (de) | 2009-11-04 | 2011-05-05 | Fraunhofer-Gesellschaft zur Förderung der angewandten Forschung e.V. | Einkristallines Schweißen von direktional verfestigten Werkstoffen |
| GB0919423D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| GB0919432D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Use |
| EP3050885B1 (en) | 2009-11-05 | 2017-10-18 | GlaxoSmithKline LLC | Benzodiazepine bromodomain inhibitor |
| GB0919434D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| GB0919426D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| CN103119160B (zh) | 2010-05-14 | 2016-06-01 | 达那-法伯癌症研究所 | 用于调节代谢的组合物和方法 |
| 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 |
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2017
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- 2017-02-15 WO PCT/US2017/017848 patent/WO2017142881A1/en not_active Ceased
- 2017-02-15 AU AU2017219627A patent/AU2017219627B2/en not_active Ceased
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- 2017-02-15 JP JP2018543139A patent/JP6967522B2/ja not_active Expired - Fee Related
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| US11548899B2 (en) | 2023-01-10 |
| CN109071562B (zh) | 2022-03-22 |
| WO2017142881A1 (en) | 2017-08-24 |
| US20210188870A1 (en) | 2021-06-24 |
| JP2019507143A (ja) | 2019-03-14 |
| CA3014644A1 (en) | 2017-08-24 |
| JP6967522B2 (ja) | 2021-11-17 |
| EP3416969A1 (en) | 2018-12-26 |
| AU2017219627A1 (en) | 2018-09-20 |
| EP3416969B1 (en) | 2021-05-05 |
| CN109071562A (zh) | 2018-12-21 |
| AU2017219627B2 (en) | 2021-08-05 |
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