CN105008352B - 用作溴区结构域抑制剂的咔唑化合物 - Google Patents
用作溴区结构域抑制剂的咔唑化合物 Download PDFInfo
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- CN105008352B CN105008352B CN201480010613.1A CN201480010613A CN105008352B CN 105008352 B CN105008352 B CN 105008352B CN 201480010613 A CN201480010613 A CN 201480010613A CN 105008352 B CN105008352 B CN 105008352B
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- Prior art keywords
- carbazole
- dimethyl
- carboxamide
- oxazol
- carbonyl
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- 0 C[C@](C1)O[C@@](C)CN1C(c(cc1)cc2c1[n](*)c1c2ccc(-c2c(C)[o]nc2C)c1)=[U] Chemical compound C[C@](C1)O[C@@](C)CN1C(c(cc1)cc2c1[n](*)c1c2ccc(-c2c(C)[o]nc2C)c1)=[U] 0.000 description 10
- QADAUDJLDUVNIJ-UHFFFAOYSA-N CC(C(Cc1cc(Br)c2)C(C3CCOCC3)c3ccccc3)c(cc(cc3)C(OC)=O)c3-c1c2C#N Chemical compound CC(C(Cc1cc(Br)c2)C(C3CCOCC3)c3ccccc3)c(cc(cc3)C(OC)=O)c3-c1c2C#N QADAUDJLDUVNIJ-UHFFFAOYSA-N 0.000 description 1
- IDSJIXNNXHYMIR-UHFFFAOYSA-N CC(C)(c(cc1)cc([n](C(CF)c2c(C3)ccc3c2)c2cc(-c3c(C)[o]nc3C)c3)c1c2c3C(N)=O)O Chemical compound CC(C)(c(cc1)cc([n](C(CF)c2c(C3)ccc3c2)c2cc(-c3c(C)[o]nc3C)c3)c1c2c3C(N)=O)O IDSJIXNNXHYMIR-UHFFFAOYSA-N 0.000 description 1
- HGPJZRHXGJMNGI-UHFFFAOYSA-N CC(C)(c(cc1)cc([n](Cc2ccccc2)c2cc(-c3c(C)[o]nc3C)c3)c1c2c3C#N)O Chemical compound CC(C)(c(cc1)cc([n](Cc2ccccc2)c2cc(-c3c(C)[o]nc3C)c3)c1c2c3C#N)O HGPJZRHXGJMNGI-UHFFFAOYSA-N 0.000 description 1
- JPEPWYQWFFGVKX-UHFFFAOYSA-N CCc(cc1)cc([n](C(C2CCOCC2)c(cc2)ccc2F)c2c3)c1c2c(C1OC1N)cc3-c1c(C)[o]nc1C Chemical compound CCc(cc1)cc([n](C(C2CCOCC2)c(cc2)ccc2F)c2c3)c1c2c(C1OC1N)cc3-c1c(C)[o]nc1C JPEPWYQWFFGVKX-UHFFFAOYSA-N 0.000 description 1
- QNZWPJDXSCKNSE-UHFFFAOYSA-N Cc1n[o]c(C)c1-c1cc(C(N)=O)c(c(cc(cc2)N)c2[n]2Cc3ccccc3)c2c1 Chemical compound Cc1n[o]c(C)c1-c1cc(C(N)=O)c(c(cc(cc2)N)c2[n]2Cc3ccccc3)c2c1 QNZWPJDXSCKNSE-UHFFFAOYSA-N 0.000 description 1
- CEGDWRFGPGOTIM-UHFFFAOYSA-N Cc1n[o]c(C)c1-c1cc(N)cc(C(OC)=O)c1 Chemical compound Cc1n[o]c(C)c1-c1cc(N)cc(C(OC)=O)c1 CEGDWRFGPGOTIM-UHFFFAOYSA-N 0.000 description 1
- ZZGYLIUMKKQVCL-UHFFFAOYSA-N Cc1n[o]c(C)c1-c1cc([nH]c(c2c3)ccc3C(N(C3)CC3F)=O)c2c(C(NC)=O)c1 Chemical compound Cc1n[o]c(C)c1-c1cc([nH]c(c2c3)ccc3C(N(C3)CC3F)=O)c2c(C(NC)=O)c1 ZZGYLIUMKKQVCL-UHFFFAOYSA-N 0.000 description 1
- OLMHJFBVMFYZKW-UHFFFAOYSA-N NC(c1c(c2cc(C(N3CCOCC3)=O)ccc2[nH]2)c2cc(Br)c1)=O Chemical compound NC(c1c(c2cc(C(N3CCOCC3)=O)ccc2[nH]2)c2cc(Br)c1)=O OLMHJFBVMFYZKW-UHFFFAOYSA-N 0.000 description 1
Classifications
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- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
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- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
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- A61K31/4192—1,2,3-Triazoles
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- A61K31/42—Oxazoles
- A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
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- A61K31/425—Thiazoles
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- 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
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- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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- 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
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- A61K31/54—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 sulfur as the ring hetero atoms, e.g. sulthiame
- A61K31/541—Non-condensed thiazines containing further heterocyclic rings
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- 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
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- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
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- C—CHEMISTRY; METALLURGY
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
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- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pulmonology (AREA)
- Urology & Nephrology (AREA)
- Dermatology (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Hematology (AREA)
- Physical Education & Sports Medicine (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Indole Compounds (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361769996P | 2013-02-27 | 2013-02-27 | |
| US61/769,996 | 2013-02-27 | ||
| US14/190,477 | 2014-02-26 | ||
| US14/190,477 US9492460B2 (en) | 2013-02-27 | 2014-02-26 | Carbazole compounds useful as bromodomain inhibitors |
| PCT/US2014/018820 WO2014134232A1 (en) | 2013-02-27 | 2014-02-27 | Carbazole compounds useful as bromodomain inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN105008352A CN105008352A (zh) | 2015-10-28 |
| CN105008352B true CN105008352B (zh) | 2018-12-07 |
Family
ID=50382555
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201480010613.1A Active CN105008352B (zh) | 2013-02-27 | 2014-02-27 | 用作溴区结构域抑制剂的咔唑化合物 |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US9492460B2 (enExample) |
| EP (1) | EP2961748B1 (enExample) |
| JP (1) | JP6395731B2 (enExample) |
| CN (1) | CN105008352B (enExample) |
| BR (1) | BR112015020389A8 (enExample) |
| CA (1) | CA2902737A1 (enExample) |
| EA (1) | EA027345B1 (enExample) |
| ES (1) | ES2669189T3 (enExample) |
| MX (1) | MX2015010921A (enExample) |
| WO (1) | WO2014134232A1 (enExample) |
Families Citing this family (48)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2666530C2 (ru) | 2012-01-12 | 2018-09-11 | Йейл Юниверсити | Соединения и способы усиления деградации белков-мишеней и других полипептидов с помощью е3 убиквитин лигазы |
| WO2014080291A2 (en) | 2012-11-21 | 2014-05-30 | Rvx Therapeutics Inc. | Biaryl derivatives as bromodomain inhibitors |
| US9073878B2 (en) | 2012-11-21 | 2015-07-07 | Zenith Epigenetics Corp. | Cyclic amines as bromodomain inhibitors |
| WO2014096965A2 (en) | 2012-12-21 | 2014-06-26 | Rvx Therapeutics Inc. | Novel heterocyclic compounds as bromodomain inhibitors |
| JP6404838B2 (ja) | 2013-02-27 | 2018-10-17 | ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company | ブロモドメイン阻害剤として有用なカルバゾール化合物 |
| EP2970312B1 (en) | 2013-03-11 | 2017-11-15 | The Regents of The University of Michigan | Bet bromodomain inhibitors and therapeutic methods using the same |
| MX366703B (es) | 2013-03-15 | 2019-07-22 | Incyte Holdings Corp | Heterociclos tricíclicos como inhibidores de la proteína bet. |
| WO2015004533A2 (en) | 2013-06-21 | 2015-01-15 | Zenith Epigenetics Corp. | Novel substituted bicyclic compounds as bromodomain inhibitors |
| SG11201510409QA (en) | 2013-06-21 | 2016-01-28 | Zenith Epigenetics Corp | Novel bicyclic bromodomain inhibitors |
| WO2015006193A1 (en) | 2013-07-08 | 2015-01-15 | Incyte Corporation | Tricyclic heterocycles as bet protein inhibitors |
| WO2015015318A2 (en) | 2013-07-31 | 2015-02-05 | Zenith Epigenetics Corp. | Novel quinazolinones as bromodomain inhibitors |
| WO2015081203A1 (en) | 2013-11-26 | 2015-06-04 | Incyte Corporation | Bicyclic heterocycles as bet protein inhibitors |
| US9315501B2 (en) | 2013-11-26 | 2016-04-19 | Incyte Corporation | Bicyclic heterocycles as BET protein inhibitors |
| US9309246B2 (en) | 2013-12-19 | 2016-04-12 | Incyte Corporation | Tricyclic heterocycles as BET protein inhibitors |
| US9458156B2 (en) | 2014-12-23 | 2016-10-04 | Bristol-Myers Squibb Company | Tricyclic compounds as anticancer agents |
| DK3466949T3 (da) * | 2013-12-24 | 2021-03-15 | Bristol Myers Squibb Co | Tricyklisk forbindelse som anticancermidler |
| US9580430B2 (en) | 2014-02-28 | 2017-02-28 | The Regents Of The University Of Michigan | 9H-pyrimido[4,5-B]indoles and related analogs as BET bromodomain inhibitors |
| US20180228907A1 (en) | 2014-04-14 | 2018-08-16 | Arvinas, Inc. | Cereblon ligands and bifunctional compounds comprising the same |
| UA119870C2 (uk) | 2014-04-23 | 2019-08-27 | Інсайт Корпорейшн | 1H-ПІРОЛО[2,3-c]ПІРИДИН-7(6H)-ОНИ ТА ПІРАЗОЛО[3,4-c]ПІРИДИН-7(6H)-ОНИ ЯК ІНГІБІТОРИ БІЛКІВ BET |
| MX2016014574A (es) * | 2014-05-08 | 2017-02-23 | Oncoethix Gmbh | El uso de compuestos de tienotriazolodiazepina para el tratamiento de cancer de mama triple-negativo. |
| ES2855225T3 (es) | 2014-09-15 | 2021-09-23 | Incyte Corp | Heterociclos tricíclicos para su uso como inhibidores de proteínas BET |
| BR112017006342A2 (pt) * | 2014-10-02 | 2017-12-19 | Glaxosmithkline Ip No 2 Ltd | composto de sal de ácido benzenossulfônico, forma em estado sólido cristalino, composição farmacêutica, produto farmacêutico de combinação, método de tratamento de doenças ou condições, uso de um composto de sal de ácido benzenossulfônico, e, processo para preparação de um composto de sal de ácido benzenossulfônico. |
| US10710992B2 (en) | 2014-12-01 | 2020-07-14 | Zenith Epigenetics Ltd. | Substituted pyridinones as bromodomain inhibitors |
| EP3227280B1 (en) | 2014-12-01 | 2019-04-24 | Zenith Epigenetics Ltd. | Substituted pyridines as bromodomain inhibitors |
| JP2017537946A (ja) | 2014-12-11 | 2017-12-21 | ゼニス・エピジェネティクス・リミテッドZenith Epigenetics Ltd. | ブロモドメイン阻害剤としての置換複素環 |
| HK1245247A1 (zh) | 2014-12-17 | 2018-08-24 | 恒翼生物医药科技(上海)有限公司 | 溴结构域的抑制剂 |
| AU2016232705C1 (en) | 2015-03-18 | 2021-06-17 | Arvinas, Inc. | Compounds and methods for the enhanced degradation of targeted proteins |
| GB201504694D0 (en) | 2015-03-19 | 2015-05-06 | Glaxosmithkline Ip Dev Ltd | Covalent conjugates |
| WO2016183114A1 (en) * | 2015-05-11 | 2016-11-17 | Bristol-Myers Squibb Company | Tricyclic compounds as anticancer agents |
| ES2770349T3 (es) | 2015-05-12 | 2020-07-01 | Bristol Myers Squibb Co | Compuestos de 5H-pirido[3,2-b]indol como agentes antineoplásicos |
| US9725449B2 (en) * | 2015-05-12 | 2017-08-08 | Bristol-Myers Squibb Company | Tricyclic compounds as anticancer agents |
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Also Published As
| Publication number | Publication date |
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| CA2902737A1 (en) | 2014-09-04 |
| EA027345B1 (ru) | 2017-07-31 |
| WO2014134232A1 (en) | 2014-09-04 |
| JP6395731B2 (ja) | 2018-09-26 |
| EA201591591A1 (ru) | 2015-12-30 |
| MX2015010921A (es) | 2016-01-12 |
| CN105008352A (zh) | 2015-10-28 |
| EP2961748B1 (en) | 2018-03-28 |
| BR112015020389A8 (pt) | 2019-11-12 |
| US20140256700A1 (en) | 2014-09-11 |
| BR112015020389A2 (pt) | 2017-07-18 |
| JP2016515098A (ja) | 2016-05-26 |
| EP2961748A1 (en) | 2016-01-06 |
| US9492460B2 (en) | 2016-11-15 |
| ES2669189T3 (es) | 2018-05-24 |
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