JP5702396B2 - ベンゾジアゼピンブロモドメイン阻害剤 - Google Patents
ベンゾジアゼピンブロモドメイン阻害剤 Download PDFInfo
- Publication number
- JP5702396B2 JP5702396B2 JP2012537381A JP2012537381A JP5702396B2 JP 5702396 B2 JP5702396 B2 JP 5702396B2 JP 2012537381 A JP2012537381 A JP 2012537381A JP 2012537381 A JP2012537381 A JP 2012537381A JP 5702396 B2 JP5702396 B2 JP 5702396B2
- Authority
- JP
- Japan
- Prior art keywords
- methyl
- alkyl
- compound
- chlorophenyl
- methyloxy
- 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 **1C=CC(C2=NC(CC(O)=O)c3nnc(*)[n]3C3=C2C=*=CC=C3)=CC=C1 Chemical compound **1C=CC(C2=NC(CC(O)=O)c3nnc(*)[n]3C3=C2C=*=CC=C3)=CC=C1 0.000 description 5
- AAAQFGUYHFJNHI-SFHVURJKSA-N CCNC(C[C@@H]1N=C(c(cc2)ccc2Cl)c2cc(OC)ccc2-[n]2c1nnc2C)=O Chemical compound CCNC(C[C@@H]1N=C(c(cc2)ccc2Cl)c2cc(OC)ccc2-[n]2c1nnc2C)=O AAAQFGUYHFJNHI-SFHVURJKSA-N 0.000 description 1
- ZYGCCMVLUKBILH-HNNXBMFYSA-N Cc1nnc2[n]1-c(ccc(O)c1)c1C(c(cc1)ccc1Cl)=N[C@H]2CC(O)=O Chemical compound Cc1nnc2[n]1-c(ccc(O)c1)c1C(c(cc1)ccc1Cl)=N[C@H]2CC(O)=O ZYGCCMVLUKBILH-HNNXBMFYSA-N 0.000 description 1
- JHOGIKRGOZKSOX-UHFFFAOYSA-N Cc1nnc2[n]1-c(ccc(OC)c1)c1C(c(cc1)ccc1Cl)=NC2CC(NCCNC)=O Chemical compound Cc1nnc2[n]1-c(ccc(OC)c1)c1C(c(cc1)ccc1Cl)=NC2CC(NCCNC)=O JHOGIKRGOZKSOX-UHFFFAOYSA-N 0.000 description 1
- VEIZLTSJCDOIBH-INIZCTEOSA-N Cc1nnc2[n]1-c(ccc(OC)c1)c1C(c(cc1)ccc1Cl)=N[C@H]2CC(O)=O Chemical compound Cc1nnc2[n]1-c(ccc(OC)c1)c1C(c(cc1)ccc1Cl)=N[C@H]2CC(O)=O VEIZLTSJCDOIBH-INIZCTEOSA-N 0.000 description 1
- DTQVDTLACAAQTR-UHFFFAOYSA-N OC(C(F)(F)F)=O Chemical compound OC(C(F)(F)F)=O DTQVDTLACAAQTR-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- 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
- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
- A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
- A61K31/5517—1,4-Benzodiazepines, e.g. diazepam or clozapine condensed with five-membered rings having nitrogen as a ring hetero atom, e.g. imidazobenzodiazepines, triazolam
-
- 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- 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
- A61P35/00—Antineoplastic agents
-
- 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
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Immunology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Rheumatology (AREA)
- Dermatology (AREA)
- Pain & Pain Management (AREA)
- Physical Education & Sports Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Transplantation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (9)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB0919433.3 | 2009-11-05 | ||
| GB0919433A GB0919433D0 (en) | 2009-11-05 | 2009-11-05 | Novel compounds |
| GBGB1010509.6A GB201010509D0 (en) | 2010-06-22 | 2010-06-22 | Novel compounds |
| GB1010509.6 | 2010-06-22 | ||
| PCT/EP2010/061518 WO2011054553A1 (en) | 2009-11-05 | 2010-08-06 | Benzodiazepine bromodomain inhibitor |
| EPPCT/EP2010/061518 | 2010-08-06 | ||
| GBGB1014231.3A GB201014231D0 (en) | 2010-08-25 | 2010-08-25 | Novel compounds |
| GB1014231.3 | 2010-08-25 | ||
| PCT/EP2010/066697 WO2011054845A1 (en) | 2009-11-05 | 2010-11-03 | Benzodiazepine bromodomain inhibitor |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015030132A Division JP2015143232A (ja) | 2009-11-05 | 2015-02-19 | ベンゾジアゼピンブロモドメイン阻害剤 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013510123A JP2013510123A (ja) | 2013-03-21 |
| JP2013510123A5 JP2013510123A5 (enExample) | 2013-11-21 |
| JP5702396B2 true JP5702396B2 (ja) | 2015-04-15 |
Family
ID=43969589
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012537381A Expired - Fee Related JP5702396B2 (ja) | 2009-11-05 | 2010-11-03 | ベンゾジアゼピンブロモドメイン阻害剤 |
| JP2015030132A Pending JP2015143232A (ja) | 2009-11-05 | 2015-02-19 | ベンゾジアゼピンブロモドメイン阻害剤 |
| JP2016185487A Pending JP2017039738A (ja) | 2009-11-05 | 2016-09-23 | ベンゾジアゼピンブロモドメイン阻害剤 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015030132A Pending JP2015143232A (ja) | 2009-11-05 | 2015-02-19 | ベンゾジアゼピンブロモドメイン阻害剤 |
| JP2016185487A Pending JP2017039738A (ja) | 2009-11-05 | 2016-09-23 | ベンゾジアゼピンブロモドメイン阻害剤 |
Country Status (23)
| Country | Link |
|---|---|
| US (3) | US9102677B2 (enExample) |
| EP (2) | EP3050885B1 (enExample) |
| JP (3) | JP5702396B2 (enExample) |
| KR (1) | KR20120097508A (enExample) |
| CN (1) | CN102781943B (enExample) |
| AU (1) | AU2010317096B2 (enExample) |
| BR (1) | BR112012010705A2 (enExample) |
| CA (1) | CA2779423C (enExample) |
| CY (1) | CY1117424T1 (enExample) |
| DK (1) | DK2496582T3 (enExample) |
| EA (1) | EA023441B1 (enExample) |
| ES (2) | ES2564318T3 (enExample) |
| HK (1) | HK1221221A1 (enExample) |
| HR (1) | HRP20160253T1 (enExample) |
| HU (1) | HUE026967T2 (enExample) |
| IL (2) | IL219253A (enExample) |
| ME (1) | ME02356B (enExample) |
| MX (1) | MX341212B (enExample) |
| PL (1) | PL2496582T3 (enExample) |
| RS (1) | RS54645B1 (enExample) |
| SI (1) | SI2496582T1 (enExample) |
| SM (1) | SMT201600104B (enExample) |
| WO (1) | WO2011054845A1 (enExample) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2015143232A (ja) * | 2009-11-05 | 2015-08-06 | グラクソスミスクライン エルエルシー | ベンゾジアゼピンブロモドメイン阻害剤 |
Families Citing this family (139)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2008007071A1 (en) | 2006-07-10 | 2008-01-17 | Cenes Limited | Short-acting benzodiazepine salts and their polymorphic forms |
| WO2011143657A1 (en) | 2010-05-14 | 2011-11-17 | Dana-Farber Cancer Institute, Inc. | Male contraceptive compositions and methods of use |
| DK2571503T3 (en) | 2010-05-14 | 2015-04-20 | Dana Farber Cancer Inst Inc | COMPOSITIONS AND THEIR USE IN THE TREATMENT OF NEOPLASIA, INFLAMMATORY DISEASE AND OTHER DISORDERS |
| 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 |
| WO2011143660A2 (en) | 2010-05-14 | 2011-11-17 | Dana-Farber Cancer Institute, Inc. | Compositions and methods for treating leukemia |
| EP2450039A1 (en) | 2010-11-08 | 2012-05-09 | PAION UK Ltd. | Dosing regimen for sedation with CNS 7056 (Remimazolam) |
| AR084070A1 (es) | 2010-12-02 | 2013-04-17 | Constellation Pharmaceuticals Inc | Inhibidores del bromodominio y usos de los mismos |
| WO2012075456A1 (en) | 2010-12-02 | 2012-06-07 | Constellation Pharmaceuticals | Bromodomain inhibitors and uses thereof |
| EP2705039B1 (en) | 2011-05-04 | 2017-07-26 | 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 |
| WO2013097052A1 (en) | 2011-12-30 | 2013-07-04 | Abbott Laboratories | Bromodomain inhibitors |
| WO2013155695A1 (en) | 2012-04-20 | 2013-10-24 | Abbott Laboratories | Isoindolone derivatives |
| BR112014029108B1 (pt) * | 2012-05-22 | 2022-02-08 | Paion Uk Limited | Composições que compreendem benzodiazepinas de curta ação, uso de uma mistura de pelo menos um dissacarídeo e pelo menos uma dextrana e método de preparação de uma composição farmacêutica |
| TWI602820B (zh) | 2012-06-06 | 2017-10-21 | 星宿藥物公司 | 溴域抑制劑及其用途 |
| WO2013184878A1 (en) | 2012-06-06 | 2013-12-12 | Constellation Pharmaceuticals, Inc. | Benzo [b] isoxazoloazepine bromodomain inhibitors and uses thereof |
| RU2632915C2 (ru) | 2012-06-12 | 2017-10-11 | Эббви Инк. | Производные пиридинона и пиридазинона |
| ES2628005T3 (es) | 2012-08-16 | 2017-08-01 | Bayer Pharma Aktiengesellschaft | 2,3-Benzodiazepinas |
| AU2013302766B2 (en) * | 2012-08-16 | 2016-10-20 | Glaxosmithkline Llc | Benzodiazepines for treating small cell lung cancer |
| JP6276277B2 (ja) * | 2012-09-28 | 2018-02-07 | バイエル ファーマ アクチエンゲゼルシャフト | Betタンパク質阻害性の5−アリールトリアゾロアゼピン |
| CN105073744B (zh) | 2012-12-21 | 2019-11-08 | 齐尼思表观遗传学有限公司 | 作为溴结构域抑制剂的新型杂环化合物 |
| AR094963A1 (es) | 2013-03-04 | 2015-09-09 | Ono Pharmaceutical Co | Reacción de oxidación excelente en el índice de conversión |
| AU2014249192B2 (en) | 2013-03-11 | 2017-12-21 | The Regents Of The University Of Michigan | BET bromodomain inhibitors and therapeutic methods using the same |
| JP2016516701A (ja) * | 2013-03-11 | 2016-06-09 | アッヴィ・インコーポレイテッド | 縮合四環系ブロモドメイン阻害剤 |
| CN108440528A (zh) * | 2013-03-12 | 2018-08-24 | 艾伯维公司 | 四环布罗莫结构域抑制剂 |
| WO2014159392A1 (en) | 2013-03-14 | 2014-10-02 | Dana-Farber Cancer Institute, Inc. | Bromodomain binding reagents and uses thereof |
| KR20150135359A (ko) * | 2013-03-14 | 2015-12-02 | 컨버진 엘엘씨 | 브로모도메인-함유 단백질의 억제를 위한 방법 및 조성물 |
| EA038494B1 (ru) | 2013-03-15 | 2021-09-07 | Инсайт Холдингс Корпорейшн | Трициклические гетероциклы как ингибиторы белков бэт |
| EA027139B1 (ru) | 2013-04-26 | 2017-06-30 | Бейджин, Лтд. | Замещенные 5-(3,5-диметилизоксазол-4-ил)индолин-2-оны |
| CN103202815B (zh) * | 2013-05-05 | 2014-09-24 | 李友香 | 治疗精神疾病的注射剂 |
| CN104146970A (zh) * | 2013-05-05 | 2014-11-19 | 王元青 | 治疗精神疾病的冻干粉针剂 |
| WO2015002754A2 (en) | 2013-06-21 | 2015-01-08 | Zenith Epigenetics Corp. | Novel bicyclic bromodomain inhibitors |
| US9662311B2 (en) | 2013-06-21 | 2017-05-30 | Zenith Epigenetics Ltd. | Substituted bicyclic compounds as bromodomain inhibitors |
| US9290514B2 (en) | 2013-07-08 | 2016-03-22 | Incyte Holdings Corporation | Tricyclic heterocycles as BET protein inhibitors |
| KR20160034379A (ko) | 2013-07-25 | 2016-03-29 | 다나-파버 캔서 인스티튜트 인크. | 전사 인자의 억제제 및 그의 용도 |
| CA2919948C (en) | 2013-07-31 | 2020-07-21 | Zenith Epigenetics Corp. | Novel quinazolinones as bromodomain inhibitors |
| KR20160072261A (ko) | 2013-11-08 | 2016-06-22 | 다나-파버 캔서 인스티튜트 인크. | 브로모도메인 및 엑스트라-말단 (bet) 단백질 저해제를 이용한 암 치료를 위한 조합 요법 |
| US9315501B2 (en) | 2013-11-26 | 2016-04-19 | Incyte Corporation | Bicyclic heterocycles as BET protein inhibitors |
| WO2015081203A1 (en) | 2013-11-26 | 2015-06-04 | Incyte Corporation | Bicyclic heterocycles as bet protein inhibitors |
| GB201320994D0 (en) * | 2013-11-28 | 2014-01-15 | Univ Dundee | Enzyme function probes |
| WO2015095492A1 (en) | 2013-12-19 | 2015-06-25 | Incyte Corporation | Tricyclic heterocycles as bet protein inhibitors |
| CA2936256A1 (en) | 2014-01-31 | 2015-08-06 | Dana-Farber Cancer Institute, Inc. | Diazepane derivatives and uses thereof |
| KR20160115953A (ko) | 2014-01-31 | 2016-10-06 | 다나-파버 캔서 인스티튜트 인크. | 디아미노피리미딘 벤젠술폰 유도체 및 그의 용도 |
| EP3099693A4 (en) | 2014-01-31 | 2017-08-16 | Dana-Farber Cancer Institute, Inc. | Uses of diazepane derivatives |
| JP6526060B2 (ja) | 2014-02-10 | 2019-06-05 | コンサート ファーマシューティカルズ インコーポレイテッド | 置換トリアゾロベンゾジアゼピン |
| WO2015131113A1 (en) | 2014-02-28 | 2015-09-03 | Tensha Therapeutics, Inc. | Treatment of conditions associated with hyperinsulinaemia |
| CN107074861A (zh) | 2014-02-28 | 2017-08-18 | 密执安大学评议会 | 作为bet溴结构域抑制剂的9h嘧啶并[4,5‑b]吲哚和相关类似物 |
| PL3129378T3 (pl) | 2014-04-09 | 2020-03-31 | Kainos Medicine, Inc. | Związki hamujące bromodomenę i zawierająca je kompozycja farmaceutyczna do zapobiegania lub leczenia nowotworu |
| HRP20200564T1 (hr) | 2014-04-23 | 2020-06-26 | Incyte Corporation | 1h-pirolo[2,3-c]piridin-7(6h)-oni i pirazolo[3,4-c]piridin-7(6h)-oni kao inhibitori bet proteina |
| CA2952526A1 (en) * | 2014-06-18 | 2015-12-23 | Bayer Pharma Aktiengesellschaft | Bet-protein inhibiting 3,4-dihydropyrido[2,3-b]pyrazinones with meta-substituted aromatic amino- or ether groups |
| LT3157928T (lt) | 2014-06-20 | 2019-05-27 | Constellation Pharmaceuticals, Inc. | 2-((4s)-6-(4-chlorfenil)-1-metil-4h-benzo[c]iizoksazolo[4,5-e]azepin-4-il)acetamido kristalinės formos |
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| BR112017002190A2 (pt) | 2014-08-08 | 2017-11-21 | Dana Farber Cancer Inst Inc | derivados de di-hidropteridinona e usos dos mesmos |
| WO2016044130A1 (en) | 2014-09-15 | 2016-03-24 | Incyte Corporation | Tricyclic heterocycles for use as bet protein inhibitors |
| CA2960090A1 (en) * | 2014-10-02 | 2016-04-07 | Glaxosmithkline Intellectual Property (No.2) Limited | Compound |
| CN107635979A (zh) | 2014-10-27 | 2018-01-26 | 腾沙治疗公司 | 溴结构域抑制剂 |
| US10208081B2 (en) | 2014-11-26 | 2019-02-19 | Enanta Pharmaceuticals, Inc. | Bile acid derivatives as FXR/TGR5 agonists and methods of use thereof |
| US10179125B2 (en) | 2014-12-01 | 2019-01-15 | Zenith Epigenetics Ltd. | Substituted pyridines as bromodomain inhibitors |
| WO2016087936A1 (en) | 2014-12-01 | 2016-06-09 | Zenith Epigenetics Corp. | Substituted pyridinones as bromodomain inhibitors |
| WO2016092375A1 (en) | 2014-12-11 | 2016-06-16 | Zenith Epigenetics Corp. | Substituted heterocycles as bromodomain inhibitors |
| WO2016097863A1 (en) | 2014-12-17 | 2016-06-23 | Zenith Epigenetics Corp. | Inhibitors of bromodomains |
| EP3262045A1 (en) | 2015-02-27 | 2018-01-03 | The Regents of The University of Michigan | 9h-pyrimido [4,5-b]indoles as bet bromodomain inhibitors |
| GB201504694D0 (en) | 2015-03-19 | 2015-05-06 | Glaxosmithkline Ip Dev Ltd | Covalent conjugates |
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| JP2015143232A (ja) * | 2009-11-05 | 2015-08-06 | グラクソスミスクライン エルエルシー | ベンゾジアゼピンブロモドメイン阻害剤 |
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