JP6395731B2 - 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 - Google Patents
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 Download PDFInfo
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- JP6395731B2 JP6395731B2 JP2015560285A JP2015560285A JP6395731B2 JP 6395731 B2 JP6395731 B2 JP 6395731B2 JP 2015560285 A JP2015560285 A JP 2015560285A JP 2015560285 A JP2015560285 A JP 2015560285A JP 6395731 B2 JP6395731 B2 JP 6395731B2
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- Prior art keywords
- carbazole
- dimethyl
- carboxamide
- oxazol
- carbonyl
- 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.)
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- 0 CCCC(*)(*C)N Chemical compound CCCC(*)(*C)N 0.000 description 6
- ZMRXQYKYQMJHGL-MXBHVSOOSA-N B[I](C)[C@@H](C)CC(C1)OCCC1C(c(cc1)ccc1F)[n](c1cc(-c2c(C)[o]nc2C)c2)c(c(F)c(C(C)(C)O)cc3)c3c1c2C(N)=O Chemical compound B[I](C)[C@@H](C)CC(C1)OCCC1C(c(cc1)ccc1F)[n](c1cc(-c2c(C)[o]nc2C)c2)c(c(F)c(C(C)(C)O)cc3)c3c1c2C(N)=O ZMRXQYKYQMJHGL-MXBHVSOOSA-N 0.000 description 1
- AVAQRUMMAQGPFV-UHFFFAOYSA-N CC(C)(c1ccc(c(c(C(N)=O)cc(-c2c(C)[o]nc2I)c2)c2[n]2C(C(CC3)CCC3(F)F)c3ccccc3)c2c1F)O Chemical compound CC(C)(c1ccc(c(c(C(N)=O)cc(-c2c(C)[o]nc2I)c2)c2[n]2C(C(CC3)CCC3(F)F)c3ccccc3)c2c1F)O AVAQRUMMAQGPFV-UHFFFAOYSA-N 0.000 description 1
- PTXYHIKUWBROMP-UHFFFAOYSA-N CC(c1ccccc1)[n]1c2cc(-c3c(C)[o]nc3C)cc(C(N)=O)c2c2c1ccc(OC)c2 Chemical compound CC(c1ccccc1)[n]1c2cc(-c3c(C)[o]nc3C)cc(C(N)=O)c2c2c1ccc(OC)c2 PTXYHIKUWBROMP-UHFFFAOYSA-N 0.000 description 1
- GUTMCWTWQHGARP-UHFFFAOYSA-N CC(c1ccccc1)[n]1c2cc(-c3c(C)[o]nc3C)cc(C(NC)=O)c2c2c1ccc(C(N(C1)CC1(F)F)=O)c2 Chemical compound CC(c1ccccc1)[n]1c2cc(-c3c(C)[o]nc3C)cc(C(NC)=O)c2c2c1ccc(C(N(C1)CC1(F)F)=O)c2 GUTMCWTWQHGARP-UHFFFAOYSA-N 0.000 description 1
- CKJBOELSUHMBOJ-UHFFFAOYSA-N CCNC(c1c(c(cc(cc2)N(CCCO3)C3=O)c2[nH]2)c2cc(Br)c1)=O Chemical compound CCNC(c1c(c(cc(cc2)N(CCCO3)C3=O)c2[nH]2)c2cc(Br)c1)=O CKJBOELSUHMBOJ-UHFFFAOYSA-N 0.000 description 1
- XLSJOKIOSULYMW-UHFFFAOYSA-N CCNC(c1c(c(cc(cc2)N(CCCO3)C3=O)c2[n]2Cc(cc3)ccc3F)c2cc(-c2c(C)[o]nc2C)c1)=O Chemical compound CCNC(c1c(c(cc(cc2)N(CCCO3)C3=O)c2[n]2Cc(cc3)ccc3F)c2cc(-c2c(C)[o]nc2C)c1)=O XLSJOKIOSULYMW-UHFFFAOYSA-N 0.000 description 1
- CNZLWYRCMIBGIC-UHFFFAOYSA-N COC(c(cc1)cc([N+]([O-])=O)c1-c(ccc(Br)c1)c1C#N)=O Chemical compound COC(c(cc1)cc([N+]([O-])=O)c1-c(ccc(Br)c1)c1C#N)=O CNZLWYRCMIBGIC-UHFFFAOYSA-N 0.000 description 1
- IIHYRGUHXVSSTK-UHFFFAOYSA-N COC(c1ccc2c(c(C#N)cc(Br)c3)c3[n](Cc3ccccc3)c2c1)=O Chemical compound COC(c1ccc2c(c(C#N)cc(Br)c3)c3[n](Cc3ccccc3)c2c1)=O IIHYRGUHXVSSTK-UHFFFAOYSA-N 0.000 description 1
- WGAKEWCXPMTYNX-HDICACEKSA-N C[C@H](C1)O[C@@H](C)CN1C(c(cc1)cc2c1[n](C(c1ccccc1)=O)c1cc(-c3c(C)[o]nc3C)cc(C(N)=O)c21)=O Chemical compound C[C@H](C1)O[C@@H](C)CN1C(c(cc1)cc2c1[n](C(c1ccccc1)=O)c1cc(-c3c(C)[o]nc3C)cc(C(N)=O)c21)=O WGAKEWCXPMTYNX-HDICACEKSA-N 0.000 description 1
- ISSDVGGKCURKBO-UHFFFAOYSA-N Cc1n[o]c(C)c1-c1cc(C#N)c(c(ccc(C(N(C)C)=O)c2)c2[n]2C(c3ccccc3)c3ccccc3)c2c1 Chemical compound Cc1n[o]c(C)c1-c1cc(C#N)c(c(ccc(C(N(C)C)=O)c2)c2[n]2C(c3ccccc3)c3ccccc3)c2c1 ISSDVGGKCURKBO-UHFFFAOYSA-N 0.000 description 1
- FHCKTQREELEKJA-UHFFFAOYSA-N Cc1n[o]c(C)c1-c1cc(C(N)=O)c(c(cc(cc2)C(N3CCOCC3)=O)c2[n]2Cc3ccccc3)c2c1 Chemical compound Cc1n[o]c(C)c1-c1cc(C(N)=O)c(c(cc(cc2)C(N3CCOCC3)=O)c2[n]2Cc3ccccc3)c2c1 FHCKTQREELEKJA-UHFFFAOYSA-N 0.000 description 1
- GAWGFAKARWGUIF-UHFFFAOYSA-N Cc1n[o]c(C)c1-c1cc(C(N)=O)c(c(cc(cc2)O)c2[n]2Cc3ccccc3)c2c1 Chemical compound Cc1n[o]c(C)c1-c1cc(C(N)=O)c(c(cc(cc2)O)c2[n]2Cc3ccccc3)c2c1 GAWGFAKARWGUIF-UHFFFAOYSA-N 0.000 description 1
- MUXWSGPORBEBNB-UHFFFAOYSA-N Cc1n[o]c(C)c1-c1cc(C(N)=O)c(c(cc(cc2)OC)c2[n]2Cc3ccccc3)c2c1 Chemical compound Cc1n[o]c(C)c1-c1cc(C(N)=O)c(c(cc(cc2)OC)c2[n]2Cc3ccccc3)c2c1 MUXWSGPORBEBNB-UHFFFAOYSA-N 0.000 description 1
- DVYNFYBBONTKLE-UHFFFAOYSA-N Cc1n[o]c(C)c1-c1cc(C(N)=O)c(c(ccc(C(OC)=O)c2)c2[n]2Cc3ccccc3)c2c1 Chemical compound Cc1n[o]c(C)c1-c1cc(C(N)=O)c(c(ccc(C(OC)=O)c2)c2[n]2Cc3ccccc3)c2c1 DVYNFYBBONTKLE-UHFFFAOYSA-N 0.000 description 1
- ATKPAWJXHKUPJS-UHFFFAOYSA-N Cc1n[o]c(C)c1-c1cc(C(NC)=O)c(c(cc(cc2)C(N(C3)CC3(F)F)=O)c2[n]2Cc(cc3)ccc3Cl)c2c1 Chemical compound Cc1n[o]c(C)c1-c1cc(C(NC)=O)c(c(cc(cc2)C(N(C3)CC3(F)F)=O)c2[n]2Cc(cc3)ccc3Cl)c2c1 ATKPAWJXHKUPJS-UHFFFAOYSA-N 0.000 description 1
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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
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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
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- C07D—HETEROCYCLIC COMPOUNDS
- 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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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- 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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- C07—ORGANIC CHEMISTRY
- 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)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Endocrinology (AREA)
- Physical Education & Sports Medicine (AREA)
- Urology & Nephrology (AREA)
- Dermatology (AREA)
- Oncology (AREA)
- Reproductive Health (AREA)
- Pulmonology (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (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 (3)
| Publication Number | Publication Date |
|---|---|
| JP2016515098A JP2016515098A (ja) | 2016-05-26 |
| JP2016515098A5 JP2016515098A5 (enExample) | 2017-03-30 |
| JP6395731B2 true JP6395731B2 (ja) | 2018-09-26 |
Family
ID=50382555
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015560285A Active JP6395731B2 (ja) | 2013-02-27 | 2014-02-27 | 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 |
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 |
| JP2018526430A (ja) | 2015-07-10 | 2018-09-13 | アルヴィナス・インコーポレイテッド | タンパク質分解のmdm2系修飾因子および関連の使用方法 |
| WO2017030814A1 (en) | 2015-08-19 | 2017-02-23 | Arvinas, Inc. | Compounds and methods for the targeted degradation of bromodomain-containing proteins |
| TW201722966A (zh) | 2015-10-29 | 2017-07-01 | 英塞特公司 | Bet蛋白質抑制劑之非晶固體形式 |
| WO2017165139A1 (en) | 2016-03-25 | 2017-09-28 | St. Jude Children's Research Hospital | 1,4,5-substituted 1,2,3-triazole analogues as antagonists of the pregnane x receptor |
| WO2017172914A1 (en) | 2016-03-30 | 2017-10-05 | Wisconsin Alumni Research Foundation | Methods and compositions for modulating frataxin expression |
| US20170281784A1 (en) | 2016-04-05 | 2017-10-05 | Arvinas, Inc. | Protein-protein interaction inducing technology |
| AU2017281286B2 (en) | 2016-06-20 | 2021-05-20 | Incyte Corporation | Crystalline solid forms of a bet inhibitor |
| JP2020506922A (ja) | 2017-01-31 | 2020-03-05 | アルビナス・オペレーションズ・インコーポレイテッドArvinas Operations, Inc. | セレブロンリガンド、およびセレブロンリガンドを含有する二官能性化合物 |
| WO2018183679A1 (en) | 2017-03-29 | 2018-10-04 | Wisconsin Alumni Research Foundation | Methods and compositions for modulating gene expression |
| WO2019148055A1 (en) | 2018-01-26 | 2019-08-01 | Yale University | Imide-based modulators of proteolysis and methods of use |
| PE20221582A1 (es) | 2019-12-19 | 2022-10-06 | Arvinas Operations Inc | Compuestos y metodos para la degradacion dirigida de receptor de androgenos |
| US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
| CN111809182B (zh) * | 2020-07-08 | 2025-04-18 | 江苏和达电子科技有限公司 | 一种用于铜/钼(铌)/igzo膜层的刻蚀液及其制备方法和应用 |
| US12016847B2 (en) | 2021-03-12 | 2024-06-25 | Bristol-Myers Squibb Company | Methods of treating prostate cancer |
| CA3255952A1 (en) * | 2022-05-20 | 2023-11-23 | University Of Puerto Rico | 1,2,3-Triazoles 1,4,5-Trisubstitutes and their uses |
| WO2025049555A1 (en) | 2023-08-31 | 2025-03-06 | Oerth Bio Llc | Compositions and methods for targeted inhibition and degradation of proteins in an insect cell |
| US12516051B1 (en) | 2024-09-30 | 2026-01-06 | St. Jude Children's Research Hospital, Inc. | Small molecule degraders and fluorescent probes of PXR |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9310635D0 (en) * | 1993-05-21 | 1993-07-07 | Glaxo Group Ltd | Chemical compounds |
| US6177440B1 (en) | 1996-10-30 | 2001-01-23 | Eli Lilly And Company | Substituted tricyclics |
| WO2002000255A1 (en) * | 2000-06-29 | 2002-01-03 | Shionogi & Co., Ltd. | Remedies for cancer |
| ATE353876T1 (de) * | 2001-03-28 | 2007-03-15 | Lilly Co Eli | Substituierte carbazole als inhibitoren von spla2 |
| US6602619B2 (en) | 2001-10-19 | 2003-08-05 | Lightronik Technology Inc. | Organic EL device |
| WO2005039569A1 (en) | 2003-10-18 | 2005-05-06 | Bayer Healthcare Ag | 5-substituted 2-(phenylmethyl) thio-4-phenyl-4h-1,2,4-triazole derivatives and related compounds as gaba-agonists for the treatment of urinary incontinence and related diseases |
| WO2006012310A2 (en) * | 2004-06-25 | 2006-02-02 | Genzyme Corporation | Carbazole derivatives for treating polycystic kidney disease |
| CN102325752B (zh) * | 2008-12-19 | 2015-02-04 | 百时美施贵宝公司 | 咔唑和咔啉激酶抑制剂 |
| MY160456A (en) * | 2009-11-05 | 2017-03-15 | Glaxosmithkline Llc | Benzodiazepine bromodomain inhibitor |
| EP2566858A2 (en) | 2010-05-04 | 2013-03-13 | Pfizer Inc. | Heterocyclic derivatives as alk inhibitors |
| JP5623996B2 (ja) | 2010-09-21 | 2014-11-12 | 株式会社半導体エネルギー研究所 | カルバゾール誘導体 |
| JP5842630B2 (ja) | 2011-03-16 | 2016-01-13 | 株式会社リコー | カルバゾール誘導体、及び半導体ナノ結晶 |
| EP2694619A4 (en) * | 2011-05-03 | 2014-10-22 | Rohm & Haas Elect Mat | NEW ORGANIC ELECTROLUMINESCENSE COMPOUNDS AND ORGANIC ELECTROLUMINESCENCE DEVICE THEREWITH |
| UA115576C2 (uk) * | 2012-12-06 | 2017-11-27 | Байєр Фарма Акцієнгезелльшафт | Похідні бензимідазолу як антагоністи ер4 |
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| CN105008352A (zh) | 2015-10-28 |
| EP2961748B1 (en) | 2018-03-28 |
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| CN105008352B (zh) | 2018-12-07 |
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| 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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