JP6967522B2 - Betブロモドメイン阻害剤としての融合1,4−オキサゼピンおよび関連類似体 - Google Patents
Betブロモドメイン阻害剤としての融合1,4−オキサゼピンおよび関連類似体 Download PDFInfo
- Publication number
- JP6967522B2 JP6967522B2 JP2018543139A JP2018543139A JP6967522B2 JP 6967522 B2 JP6967522 B2 JP 6967522B2 JP 2018543139 A JP2018543139 A JP 2018543139A JP 2018543139 A JP2018543139 A JP 2018543139A JP 6967522 B2 JP6967522 B2 JP 6967522B2
- Authority
- JP
- Japan
- Prior art keywords
- triazolo
- cancer
- oxazepine
- thieno
- methyl
- 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.)
- Expired - Fee Related
Links
- 0 Cc1c(*)c(C*Cc2nnc(C)[n]2-2)c-2[s]1 Chemical compound Cc1c(*)c(C*Cc2nnc(C)[n]2-2)c-2[s]1 0.000 description 22
- BQTFTZBVKPCCCE-UHFFFAOYSA-N Cc([s]c-1c2COCc3nnc(C)[n]-13)c2Br Chemical compound Cc([s]c-1c2COCc3nnc(C)[n]-13)c2Br BQTFTZBVKPCCCE-UHFFFAOYSA-N 0.000 description 2
- RUCPUEYQKXFLEJ-UHFFFAOYSA-N Cc1nnc(COC2)[n]1-c(cc1)c2c(Cc2ccccc2)c1Cl Chemical compound Cc1nnc(COC2)[n]1-c(cc1)c2c(Cc2ccccc2)c1Cl RUCPUEYQKXFLEJ-UHFFFAOYSA-N 0.000 description 2
- IJUOAFGWSRMEHU-VMHBGOFLSA-N Bc1c(C)[s]c(N/C(/C)=N\NC(C)[C@@H]2C(OC)=O)c1CN2C(OCc1ccccc1)=O Chemical compound Bc1c(C)[s]c(N/C(/C)=N\NC(C)[C@@H]2C(OC)=O)c1CN2C(OCc1ccccc1)=O IJUOAFGWSRMEHU-VMHBGOFLSA-N 0.000 description 1
- DCPYNZLLYWMEER-MDZDMXLPSA-N CC(C)(C)OC(N/C(/S)=C(/C=C(C)C)\C=O)=O Chemical compound CC(C)(C)OC(N/C(/S)=C(/C=C(C)C)\C=O)=O DCPYNZLLYWMEER-MDZDMXLPSA-N 0.000 description 1
- LMQZHWPJZZGRPW-UHFFFAOYSA-N CC(C)(C)OC(Nc1c(C=O)cc(C)[s]1)=O Chemical compound CC(C)(C)OC(Nc1c(C=O)cc(C)[s]1)=O LMQZHWPJZZGRPW-UHFFFAOYSA-N 0.000 description 1
- MEGCSBNSADCMCH-UHFFFAOYSA-N CCc1cccc-2c1COCc1nnc(C)[n]-21 Chemical compound CCc1cccc-2c1COCc1nnc(C)[n]-21 MEGCSBNSADCMCH-UHFFFAOYSA-N 0.000 description 1
- UOMHCXCDHSRTML-PIJUOJQZSA-N C[C@@H](C1N2C(C)=NN1C)OCc1c2[s]cc1Cc(cc1)ccc1F Chemical compound C[C@@H](C1N2C(C)=NN1C)OCc1c2[s]cc1Cc(cc1)ccc1F UOMHCXCDHSRTML-PIJUOJQZSA-N 0.000 description 1
- 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
- XELZBALYGDKAGE-AWEZNQCLSA-N C[C@@H](c1nnc(C)[n]1-1)OCc2c-1[s]c(C#CCOC)c2Cc1ccccc1 Chemical compound C[C@@H](c1nnc(C)[n]1-1)OCc2c-1[s]c(C#CCOC)c2Cc1ccccc1 XELZBALYGDKAGE-AWEZNQCLSA-N 0.000 description 1
- VSJGDQUMYFYEFZ-LLVKDONJSA-N C[C@H](c1nnc(C)[n]1-1)NCc2c-1[s]c(C)c2Cc1ccccc1 Chemical compound C[C@H](c1nnc(C)[n]1-1)NCc2c-1[s]c(C)c2Cc1ccccc1 VSJGDQUMYFYEFZ-LLVKDONJSA-N 0.000 description 1
- RYGOBSYXIIUFOR-UHFFFAOYSA-N C[n]1[n]cc(B(O)O)c1 Chemical compound C[n]1[n]cc(B(O)O)c1 RYGOBSYXIIUFOR-UHFFFAOYSA-N 0.000 description 1
- MEFBEANVNDSZQJ-UHFFFAOYSA-N Cc([s]c(N1)c2COCC1=O)c2Br Chemical compound Cc([s]c(N1)c2COCC1=O)c2Br MEFBEANVNDSZQJ-UHFFFAOYSA-N 0.000 description 1
- BKNUEFIETPVROC-UHFFFAOYSA-N Cc([s]c-1c2COCc3nnc(C)[n]-13)c2C1=CCCc2cc(F)ccc12 Chemical compound Cc([s]c-1c2COCc3nnc(C)[n]-13)c2C1=CCCc2cc(F)ccc12 BKNUEFIETPVROC-UHFFFAOYSA-N 0.000 description 1
- JTVUZEQBJXPHBH-UHFFFAOYSA-N Cc([s]c-1c2COCc3nnc(C)[n]-13)c2C1=CCc2c1cccc2 Chemical compound Cc([s]c-1c2COCc3nnc(C)[n]-13)c2C1=CCc2c1cccc2 JTVUZEQBJXPHBH-UHFFFAOYSA-N 0.000 description 1
- DUOGROUHRZVOIW-UHFFFAOYSA-N Cc1c(C)[s]c-2c1COCc1nnc(C)[n]-21 Chemical compound Cc1c(C)[s]c-2c1COCc1nnc(C)[n]-21 DUOGROUHRZVOIW-UHFFFAOYSA-N 0.000 description 1
- VXJLICQTVXWPGK-UHFFFAOYSA-N Cc1c(CC2=CCCC=C2)c(CN=C(C)c2nnc(C)[n]2-2)c-2[s]1 Chemical compound Cc1c(CC2=CCCC=C2)c(CN=C(C)c2nnc(C)[n]2-2)c-2[s]1 VXJLICQTVXWPGK-UHFFFAOYSA-N 0.000 description 1
- BWZMCVSVYSYHCI-HSZRJFAPSA-N Cc1c(Cc2ccccc2)c(CN([C@@H](C(OC)=O)c2nnc(C)[n]2-2)C(OCc3ccccc3)=O)c-2[s]1 Chemical compound Cc1c(Cc2ccccc2)c(CN([C@@H](C(OC)=O)c2nnc(C)[n]2-2)C(OCc3ccccc3)=O)c-2[s]1 BWZMCVSVYSYHCI-HSZRJFAPSA-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
- GUUBZDPNXUTFQX-UHFFFAOYSA-N Cc1nnc(C2(CC2)OC2)[n]1-c([s]1)c2cc1Br Chemical compound Cc1nnc(C2(CC2)OC2)[n]1-c([s]1)c2cc1Br GUUBZDPNXUTFQX-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
- UZWMJCIFRXXGCP-UHFFFAOYSA-N Cc1nnc(COC2)[n]1-c(cc1)c2c(Cc2ccccc2)c1-c1c[n](C)nc1 Chemical compound Cc1nnc(COC2)[n]1-c(cc1)c2c(Cc2ccccc2)c1-c1c[n](C)nc1 UZWMJCIFRXXGCP-UHFFFAOYSA-N 0.000 description 1
- UEGYNCIEBZCNHJ-UHFFFAOYSA-N Cc1nnc(COC2)[n]1-c(cc1)c2c(Cc2ccccc2)c1-c1c[o]cc1 Chemical compound Cc1nnc(COC2)[n]1-c(cc1)c2c(Cc2ccccc2)c1-c1c[o]cc1 UEGYNCIEBZCNHJ-UHFFFAOYSA-N 0.000 description 1
- MIDZBDABQBLNCQ-UHFFFAOYSA-N Cc1nnc(COC2)[n]1-c1c2c(Br)ccc1 Chemical compound Cc1nnc(COC2)[n]1-c1c2c(Br)ccc1 MIDZBDABQBLNCQ-UHFFFAOYSA-N 0.000 description 1
- DKMLZMDUQKTFAV-UHFFFAOYSA-N Cc1nnc(COC2)[n]1-c1c2c(Cc2ccccc2)c(-c2c[nH]nc2)[s]1 Chemical compound Cc1nnc(COC2)[n]1-c1c2c(Cc2ccccc2)c(-c2c[nH]nc2)[s]1 DKMLZMDUQKTFAV-UHFFFAOYSA-N 0.000 description 1
- HXOJXTBMYNYBBU-UHFFFAOYSA-N Cc1nnc(COC2)[n]1-c1c2c(Cc2ccccc2)c(-c2c[n](C)nc2)[s]1 Chemical compound Cc1nnc(COC2)[n]1-c1c2c(Cc2ccccc2)c(-c2c[n](C)nc2)[s]1 HXOJXTBMYNYBBU-UHFFFAOYSA-N 0.000 description 1
- KHDSTVQDUUSMAQ-UHFFFAOYSA-N Cc1nnc(COC2)[n]1-c1c2c(Cc2ccccc2)c(C#Cc2cnccc2)[s]1 Chemical compound Cc1nnc(COC2)[n]1-c1c2c(Cc2ccccc2)c(C#Cc2cnccc2)[s]1 KHDSTVQDUUSMAQ-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
- CFIXBDKOLHMIBK-UHFFFAOYSA-N OB(C1=C=Cc2ccccc12)O Chemical compound OB(C1=C=Cc2ccccc12)O CFIXBDKOLHMIBK-UHFFFAOYSA-N 0.000 description 1
- CYEFKCRAAGLNHW-UHFFFAOYSA-N OB(c1c[o]cc1)O Chemical compound OB(c1c[o]cc1)O CYEFKCRAAGLNHW-UHFFFAOYSA-N 0.000 description 1
Images
Classifications
-
- 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
-
- 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
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)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (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 (3)
| Publication Number | Publication Date |
|---|---|
| JP2019507143A JP2019507143A (ja) | 2019-03-14 |
| JP2019507143A5 JP2019507143A5 (enExample) | 2020-03-26 |
| JP6967522B2 true JP6967522B2 (ja) | 2021-11-17 |
Family
ID=58191613
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018543139A Expired - Fee Related JP6967522B2 (ja) | 2016-02-15 | 2017-02-15 | Betブロモドメイン阻害剤としての融合1,4−オキサゼピンおよび関連類似体 |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US11548899B2 (enExample) |
| EP (1) | EP3416969B1 (enExample) |
| JP (1) | JP6967522B2 (enExample) |
| CN (1) | CN109071562B (enExample) |
| AU (1) | AU2017219627B2 (enExample) |
| CA (1) | CA3014644A1 (enExample) |
| ES (1) | ES2882066T3 (enExample) |
| WO (1) | WO2017142881A1 (enExample) |
Families Citing this family (26)
| 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 |
| US11267822B2 (en) | 2017-09-13 | 2022-03-08 | The Regents Of The University Of Michigan | BET bromodomain protein degraders with cleavable linkers |
| 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 |
| KR20260019479A (ko) | 2023-05-04 | 2026-02-10 | 레볼루션 메디슨즈, 인크. | Ras 관련 질환 또는 장애를 위한 병용 요법 |
| CN121889155A (zh) | 2023-08-07 | 2026-04-17 | 锐新医药公司 | 用于治疗ras蛋白相关疾病或病症的rmc-6291 |
| 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 |
| 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 |
| WO2026015801A1 (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 |
| WO2026015790A1 (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 |
| 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 |
| WO2026090116A2 (en) | 2024-10-21 | 2026-04-30 | Revolution Medicines, Inc. | Ras inhibitors |
| US20260108528A1 (en) | 2024-10-22 | 2026-04-23 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| WO2026090245A1 (en) | 2024-10-22 | 2026-04-30 | Revolution Medicines, Inc. | Use of ras inhibitors for treating cancer |
| WO2026106912A1 (en) | 2024-11-12 | 2026-05-21 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026112260A1 (en) | 2024-11-21 | 2026-05-28 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026122764A2 (en) | 2024-12-06 | 2026-06-11 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026128688A2 (en) | 2024-12-13 | 2026-06-18 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026161839A1 (en) | 2025-01-27 | 2026-07-30 | Revolution Medicines, Inc. | Ras inhibitors |
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 |
| WO1998011111A1 (en) | 1996-09-13 | 1998-03-19 | Yoshitomi Pharmaceutical Industries, Ltd. | Thienotriazolodiazepine compounds and medicinal uses thereof |
| 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 |
| CN101910182B (zh) | 2007-12-28 | 2013-07-17 | 田边三菱制药株式会社 | 抗癌剂 |
| JP5640208B2 (ja) * | 2008-01-24 | 2014-12-17 | パナセア バイオテック リミテッド | 新規複素環化合物 |
| US8114995B2 (en) | 2008-06-26 | 2012-02-14 | Resverlogix Corp. | Methods of preparing quinazolinone derivatives |
| 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 |
| GB0919434D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| GB0919426D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| GB0919432D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Use |
| AU2010317096B2 (en) | 2009-11-05 | 2015-03-26 | Glaxosmithkline Llc | Benzodiazepine bromodomain inhibitor |
| GB0919423D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| CN103154246B (zh) | 2010-05-14 | 2015-11-25 | 达那-法伯癌症研究所 | 用于治疗白血病的组合物和方法 |
| ES2606958T3 (es) | 2010-05-14 | 2017-03-28 | Dana-Farber Cancer Institute, Inc. | Compuestos de tienotriazolodiazepina para tratar una neoplasia |
| 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 |
| WO2011143651A1 (en) | 2010-05-14 | 2011-11-17 | Dana-Farber Cancer Institute, Inc. | Compositions and methods for modulating metabolism |
| EP2585465B1 (en) | 2010-06-22 | 2014-11-12 | GlaxoSmithKline LLC | Benzotriazolodiazepine compounds inhibitors of bromodomains |
| WO2012075456A1 (en) | 2010-12-02 | 2012-06-07 | Constellation Pharmaceuticals | Bromodomain inhibitors and uses thereof |
| AR084070A1 (es) | 2010-12-02 | 2013-04-17 | Constellation Pharmaceuticals Inc | Inhibidores del bromodominio y usos de los mismos |
| 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 |
| WO2012174487A2 (en) | 2011-06-17 | 2012-12-20 | 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 |
| WO2013033268A2 (en) | 2011-08-29 | 2013-03-07 | Coferon, Inc. | Bivalent bromodomain ligands, 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 |
| WO2013155695A1 (en) | 2012-04-20 | 2013-10-24 | Abbott Laboratories | Isoindolone derivatives |
| HK1208681A1 (en) | 2012-06-12 | 2016-03-11 | Abbvie Inc. | Pyridinone and pyridazinone derivatives |
| CA2901805A1 (en) * | 2013-02-22 | 2014-08-28 | Bayer Pharma Aktiengesellschaft | 4-substituted pyrrolo- and pyrazolo-diazepines |
| EP2970312B1 (en) | 2013-03-11 | 2017-11-15 | The Regents of The University of Michigan | Bet bromodomain inhibitors and therapeutic methods using the same |
| EP4649963A3 (en) | 2014-04-14 | 2026-05-13 | 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 |
| CN109562113A (zh) | 2016-05-10 | 2019-04-02 | C4医药公司 | 用于靶蛋白降解的螺环降解决定子体 |
| WO2019084026A1 (en) | 2017-10-24 | 2019-05-02 | Genentech, Inc. | (4-HYDROXYPYRROLIDIN-2-YL) -HETEROCYCLIC COMPOUNDS AND METHODS OF USE |
| WO2019246430A1 (en) | 2018-06-21 | 2019-12-26 | Foghorn Therapeutics Inc. | Methods of treating disorders |
| EP3814380A4 (en) | 2018-06-29 | 2022-06-15 | Dana Farber Cancer Institute, Inc. | BISPECIFIC DEGRADATION PRODUCTS |
| US12030892B2 (en) | 2018-06-29 | 2024-07-09 | Dana-Farber Cancer Institute, Inc. | CRBN modulators |
| US11542273B2 (en) | 2018-07-04 | 2023-01-03 | Mitsubishi Tanabe Pharma Corporation | Amide compound having bet proteolysis-inducing action and medicinal application thereof |
| WO2020018788A1 (en) | 2018-07-20 | 2020-01-23 | Dana-Farber Cancer Institute, Inc. | Degraders that target proteins via keap1 |
-
2017
- 2017-02-15 CA CA3014644A patent/CA3014644A1/en active Pending
- 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 WO PCT/US2017/017848 patent/WO2017142881A1/en not_active Ceased
- 2017-02-15 JP JP2018543139A patent/JP6967522B2/ja not_active Expired - Fee Related
- 2017-02-15 EP EP17708046.2A patent/EP3416969B1/en active Active
- 2017-02-15 CN CN201780023735.8A patent/CN109071562B/zh not_active Expired - Fee Related
- 2017-02-15 ES ES17708046T patent/ES2882066T3/es active Active
Also Published As
| Publication number | Publication date |
|---|---|
| ES2882066T3 (es) | 2021-12-01 |
| CA3014644A1 (en) | 2017-08-24 |
| AU2017219627B2 (en) | 2021-08-05 |
| JP2019507143A (ja) | 2019-03-14 |
| WO2017142881A1 (en) | 2017-08-24 |
| CN109071562A (zh) | 2018-12-21 |
| AU2017219627A1 (en) | 2018-09-20 |
| CN109071562B (zh) | 2022-03-22 |
| US11548899B2 (en) | 2023-01-10 |
| EP3416969B1 (en) | 2021-05-05 |
| US20210188870A1 (en) | 2021-06-24 |
| EP3416969A1 (en) | 2018-12-26 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN109071562B (zh) | 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 | |
| JP6961684B2 (ja) | Betタンパク質分解物質としての縮合1,4−オキサゼピン | |
| TWI760685B (zh) | 作為mcl-1抑制劑的大環稠合的吡唑 | |
| JP7035027B2 (ja) | Betタンパク質分解物質としての縮合1,4-ジアゼピン | |
| JP7072519B2 (ja) | Betタンパク質分解剤 | |
| TWI749404B (zh) | 作為mcl-1抑制劑的大環吲哚 | |
| TWI602820B (zh) | 溴域抑制劑及其用途 | |
| CN110914265B (zh) | 作为lsd-1抑制剂的吡咯并[2,3-c]吡啶和相关类似物 | |
| US11045448B2 (en) | Piperidines as covalent menin inhibitors | |
| JP2017511801A (ja) | BETブロモドメイン阻害剤としての9H−ピリミド[4,5−b]インドールおよび関連類似体 | |
| US10307407B2 (en) | 9H-pyrimido [4,5-B] indoles as BET bromodomain inhibitors | |
| KR20130125378A (ko) | 브로모도메인 억제제 및 이의 용도 | |
| CN112119080B (zh) | 作为lsd-1抑制剂的咪唑并[4,5-c]吡啶化合物 | |
| CN107406414B (zh) | 作为用于治疗癌症的组蛋白脱甲基酶kdm2b的抑制剂的(哌啶-3-基)(萘-2-基)甲酮衍生物 | |
| US11046709B2 (en) | Fused 1,4-diazepines as BET bromodomain inhibitors | |
| AU2024277290A1 (en) | Compounds, compositions and methods of treating disorders | |
| HK40041770B (en) | Imidazo[4,5-c]pyridine compounds as lsd-1 inhibitors | |
| HK40041770A (en) | Imidazo[4,5-c]pyridine compounds as lsd-1 inhibitors | |
| HK40022861B (en) | Pyrrolo[2,3-c]pyridines and related analogs as lsd-1 inhibitors |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20200214 |
|
| A621 | Written request for application examination |
Free format text: JAPANESE INTERMEDIATE CODE: A621 Effective date: 20200214 |
|
| A977 | Report on retrieval |
Free format text: JAPANESE INTERMEDIATE CODE: A971007 Effective date: 20210121 |
|
| A131 | Notification of reasons for refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A131 Effective date: 20210203 |
|
| RD04 | Notification of resignation of power of attorney |
Free format text: JAPANESE INTERMEDIATE CODE: A7424 Effective date: 20210219 |
|
| A601 | Written request for extension of time |
Free format text: JAPANESE INTERMEDIATE CODE: A601 Effective date: 20210428 |
|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20210729 |
|
| TRDD | Decision of grant or rejection written | ||
| A01 | Written decision to grant a patent or to grant a registration (utility model) |
Free format text: JAPANESE INTERMEDIATE CODE: A01 Effective date: 20211011 |
|
| A61 | First payment of annual fees (during grant procedure) |
Free format text: JAPANESE INTERMEDIATE CODE: A61 Effective date: 20211025 |
|
| R150 | Certificate of patent or registration of utility model |
Ref document number: 6967522 Country of ref document: JP Free format text: JAPANESE INTERMEDIATE CODE: R150 |
|
| LAPS | Cancellation because of no payment of annual fees |