JP5850944B2 - ブロモドメイン阻害剤およびその使用 - Google Patents
ブロモドメイン阻害剤およびその使用 Download PDFInfo
- Publication number
- JP5850944B2 JP5850944B2 JP2013542202A JP2013542202A JP5850944B2 JP 5850944 B2 JP5850944 B2 JP 5850944B2 JP 2013542202 A JP2013542202 A JP 2013542202A JP 2013542202 A JP2013542202 A JP 2013542202A JP 5850944 B2 JP5850944 B2 JP 5850944B2
- Authority
- JP
- Japan
- Prior art keywords
- cancer
- optionally substituted
- mmol
- compound
- chlorophenyl
- 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 CC1(C2)CCC2*1 Chemical compound CC1(C2)CCC2*1 0.000 description 9
- JAKIVGRJNOFNPM-LBPRGKRZSA-N CC(C)(C)OC(C[C@@H](c([o]nc1C)c1-c1c(CO)c(F)ncc1)N)=O Chemical compound CC(C)(C)OC(C[C@@H](c([o]nc1C)c1-c1c(CO)c(F)ncc1)N)=O JAKIVGRJNOFNPM-LBPRGKRZSA-N 0.000 description 1
- BQLVDCXTOQDCDE-UHFFFAOYSA-N CC(NC1NC(c(cc2)ccc2C#N)c2ccccc2-c2c1[o]nc2C)=O Chemical compound CC(NC1NC(c(cc2)ccc2C#N)c2ccccc2-c2c1[o]nc2C)=O BQLVDCXTOQDCDE-UHFFFAOYSA-N 0.000 description 1
- COENEHMWVJZOPJ-OTYXRUKQSA-N C[C@H]([C@@H](c([o]nc1C)c1-c1c2c(C)c(C)[s]1)NC2=O)C(OC(C)(C)C)=O Chemical compound C[C@H]([C@@H](c([o]nc1C)c1-c1c2c(C)c(C)[s]1)NC2=O)C(OC(C)(C)C)=O COENEHMWVJZOPJ-OTYXRUKQSA-N 0.000 description 1
- KNBHDYYLEZIUIU-UHFFFAOYSA-N Cc([o]nc12)c1-c(cccc1)c1C(c(cc1)ccc1Cl)=NC2N Chemical compound Cc([o]nc12)c1-c(cccc1)c1C(c(cc1)ccc1Cl)=NC2N KNBHDYYLEZIUIU-UHFFFAOYSA-N 0.000 description 1
- IRLLRSUQPTZEGC-SNAWJCMRSA-N Cc1c(C)[s]c-2c1C(Cl)=NC(/C=C/C(O)=O)c1c-2c(C)n[o]1 Chemical compound Cc1c(C)[s]c-2c1C(Cl)=NC(/C=C/C(O)=O)c1c-2c(C)n[o]1 IRLLRSUQPTZEGC-SNAWJCMRSA-N 0.000 description 1
- DAEHEDUISSQHKV-UHFFFAOYSA-N Cc1n[o]c(CO)c1-c(nc(cc1)OC)c1C(OC)=O Chemical compound Cc1n[o]c(CO)c1-c(nc(cc1)OC)c1C(OC)=O DAEHEDUISSQHKV-UHFFFAOYSA-N 0.000 description 1
- GCWIQUVXWZWCLE-INIZCTEOSA-N Cc1n[o]c2c1-c(cccc1)c1C(c(cc1)ccc1Cl)=N[C@H]2CC(N)=O Chemical compound Cc1n[o]c2c1-c(cccc1)c1C(c(cc1)ccc1Cl)=N[C@H]2CC(N)=O GCWIQUVXWZWCLE-INIZCTEOSA-N 0.000 description 1
- WEINDEABQFLLTO-AWEZNQCLSA-N Cc1n[o]c2c1-c(ccnc1NC)c1C(c(cc1)ccc1Cl)=N[C@H]2CC(N)=O Chemical compound Cc1n[o]c2c1-c(ccnc1NC)c1C(c(cc1)ccc1Cl)=N[C@H]2CC(N)=O WEINDEABQFLLTO-AWEZNQCLSA-N 0.000 description 1
- HKEPQFZZMOWRMH-UHFFFAOYSA-N Cc1n[o]c2c1-c1nc(N)ccc1C(c(cc1)ccc1Cl)=NC2 Chemical compound Cc1n[o]c2c1-c1nc(N)ccc1C(c(cc1)ccc1Cl)=NC2 HKEPQFZZMOWRMH-UHFFFAOYSA-N 0.000 description 1
- COFJNXFLCSMYQC-UHFFFAOYSA-N O=Cc1n[o]c(I)c1C(CCC=CC1)=C1C(C1C=CC(Cl)=CC1)=O Chemical compound O=Cc1n[o]c(I)c1C(CCC=CC1)=C1C(C1C=CC(Cl)=CC1)=O COFJNXFLCSMYQC-UHFFFAOYSA-N 0.000 description 1
- VDBRDPFSSFHZMI-UHFFFAOYSA-N OC(c(cc1)ccc1Cl)c(c(I)ccn1)c1F Chemical compound OC(c(cc1)ccc1Cl)c(c(I)ccn1)c1F VDBRDPFSSFHZMI-UHFFFAOYSA-N 0.000 description 1
- WVRWYFPFESGNPQ-UHFFFAOYSA-N OCc1n[o]c2c1-c1ccccc1C(c(cc1)ccc1Cl)O2 Chemical compound OCc1n[o]c2c1-c1ccccc1C(c(cc1)ccc1Cl)O2 WVRWYFPFESGNPQ-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- 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
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/42—Oxazoles
- A61K31/424—Oxazoles condensed with heterocyclic ring systems, e.g. clavulanic acid
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- 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
- 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
- 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
- C07D498/12—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
-
- 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
- C07D498/20—Spiro-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
- C07D498/22—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 four or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- C07K14/46—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates
- C07K14/47—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates from mammals
- C07K14/4701—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates from mammals not used
- C07K14/4702—Regulators; Modulating activity
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Genetics & Genomics (AREA)
- Biophysics (AREA)
- Toxicology (AREA)
- Zoology (AREA)
- Gastroenterology & Hepatology (AREA)
- Rheumatology (AREA)
- Dermatology (AREA)
- Pain & Pain Management (AREA)
- Physical Education & Sports Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Hematology (AREA)
- Virology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (11)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US41911910P | 2010-12-02 | 2010-12-02 | |
| US61/419,119 | 2010-12-02 | ||
| US201161451332P | 2011-03-10 | 2011-03-10 | |
| US61/451,322 | 2011-03-10 | ||
| US201161482473P | 2011-05-04 | 2011-05-04 | |
| US61/482,473 | 2011-05-04 | ||
| US201161540788P | 2011-09-29 | 2011-09-29 | |
| US201161540725P | 2011-09-29 | 2011-09-29 | |
| US61/540,788 | 2011-09-29 | ||
| US61/540,725 | 2011-09-29 | ||
| PCT/US2011/063046 WO2012075383A2 (en) | 2010-12-02 | 2011-12-02 | Bromodomain inhibitors and uses thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013544847A JP2013544847A (ja) | 2013-12-19 |
| JP2013544847A5 JP2013544847A5 (enExample) | 2015-01-22 |
| JP5850944B2 true JP5850944B2 (ja) | 2016-02-03 |
Family
ID=46235164
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013542202A Active JP5850944B2 (ja) | 2010-12-02 | 2011-12-02 | ブロモドメイン阻害剤およびその使用 |
Country Status (26)
| Country | Link |
|---|---|
| US (2) | US8796261B2 (enExample) |
| EP (1) | EP2646446B1 (enExample) |
| JP (1) | JP5850944B2 (enExample) |
| KR (1) | KR101871013B1 (enExample) |
| CN (1) | CN103415525B (enExample) |
| AR (1) | AR084070A1 (enExample) |
| AU (1) | AU2011336417B2 (enExample) |
| BR (1) | BR112013013167B1 (enExample) |
| CA (1) | CA2818187C (enExample) |
| CY (1) | CY1116578T1 (enExample) |
| DK (1) | DK2646446T3 (enExample) |
| EA (1) | EA022645B1 (enExample) |
| ES (1) | ES2545117T3 (enExample) |
| HR (1) | HRP20150858T1 (enExample) |
| HU (1) | HUE025321T2 (enExample) |
| IL (1) | IL226331A (enExample) |
| MX (1) | MX2013006214A (enExample) |
| NZ (1) | NZ611964A (enExample) |
| PL (1) | PL2646446T3 (enExample) |
| PT (1) | PT2646446E (enExample) |
| RS (1) | RS54175B1 (enExample) |
| SG (1) | SG190739A1 (enExample) |
| SI (1) | SI2646446T1 (enExample) |
| TW (1) | TWI572607B (enExample) |
| WO (1) | WO2012075383A2 (enExample) |
| ZA (1) | ZA201303776B (enExample) |
Families Citing this family (150)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK2118074T3 (en) | 2007-02-01 | 2014-03-10 | Resverlogix Corp | Compounds for the prevention and treatment of cardiovascular diseases |
| KR101709492B1 (ko) | 2009-03-18 | 2017-02-23 | 리스버로직스 코퍼레이션 | 신규한 소염제 |
| MX373121B (es) | 2010-05-14 | 2020-04-30 | Dana Farber Cancer Inst Inc | Composiciones y metodos para el tratamiento de leucemia. |
| US9301962B2 (en) | 2010-05-14 | 2016-04-05 | Baylor College Of Medicine | Male contraceptive compositions and methods of use |
| MX384074B (es) | 2010-05-14 | 2025-03-12 | Dana Farber Cancer Inst Inc | Composiciones y métodos para tratar neoplasias, enfermedades inflamatorias y otros trastornos. |
| AR084070A1 (es) | 2010-12-02 | 2013-04-17 | Constellation Pharmaceuticals Inc | Inhibidores del bromodominio y usos de los mismos |
| US9249161B2 (en) | 2010-12-02 | 2016-02-02 | Constellation Pharmaceuticals, Inc. | Bromodomain inhibitors and uses thereof |
| US8912221B2 (en) * | 2010-12-27 | 2014-12-16 | Hoffmann-La Roche Inc. | Biaryl amide derivatives |
| EP2705039B1 (en) | 2011-05-04 | 2017-07-26 | Constellation Pharmaceuticals, Inc. | Bromodomain inhibitors and uses thereof |
| US9328117B2 (en) | 2011-06-17 | 2016-05-03 | Constellation Pharmaceuticals, Inc. | Bromodomain inhibitors and uses thereof |
| WO2013027168A1 (en) | 2011-08-22 | 2013-02-28 | Pfizer Inc. | Novel heterocyclic compounds as bromodomain inhibitors |
| WO2013033269A1 (en) | 2011-08-29 | 2013-03-07 | Coferon, Inc. | Bioorthogonal monomers capable of dimerizing and targeting bromodomains and methods of using same |
| WO2013033270A2 (en) | 2011-08-29 | 2013-03-07 | Coferon, Inc. | Bromodomain ligands capable of dimerizing in an aqueous solution, and methods of using same |
| RU2640115C2 (ru) | 2011-11-01 | 2017-12-26 | Ресверлоджикс Корп. | Фармацевтические композиции замещенных хиназолинонов |
| JP2015508414A (ja) | 2012-01-12 | 2015-03-19 | イエール ユニバーシティ | E3ユビキチンリガーゼによる標的タンパク質および他のポリペプチドの分解増強のための化合物および方法 |
| TWI602820B (zh) * | 2012-06-06 | 2017-10-21 | 星宿藥物公司 | 溴域抑制劑及其用途 |
| US9624244B2 (en) | 2012-06-06 | 2017-04-18 | Constellation Pharmaceuticals, Inc. | Benzo [B] isoxazoloazepine bromodomain inhibitors and uses thereof |
| WO2013185284A1 (en) * | 2012-06-12 | 2013-12-19 | Abbott Laboratories | Pyridinone and pyridazinone derivatives |
| PE20150729A1 (es) * | 2012-08-16 | 2015-06-14 | Bayer Pharma AG | 2,3-benzodiazepines |
| HK1208448A1 (en) | 2012-09-28 | 2016-03-04 | Bayer Pharma Aktiengesellschaft | Bet protein-inhibiting 5-aryl triazole azepines |
| 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 |
| US9271978B2 (en) | 2012-12-21 | 2016-03-01 | Zenith Epigenetics Corp. | Heterocyclic compounds as bromodomain inhibitors |
| CA2901352A1 (en) | 2013-02-19 | 2014-08-28 | Bayer Pharma Aktiengesellschaft | Bicyclo 2,3-benzodiazepines and spirocyclically substituted 2,3-benzodiazepines |
| HK1212345A1 (en) | 2013-02-22 | 2016-06-10 | Bayer Pharma Aktiengesellschaft | 4-substituted pyrrolo- and pyrazolo-diazepines |
| JP2016513117A (ja) | 2013-02-22 | 2016-05-12 | バイエル ファーマ アクチエンゲゼルシャフト | 過剰増殖性疾患を治療するためのbetタンパク質阻害剤としてのピロロ−およびピラゾロ−トリアゾロジアゼピン類 |
| AU2014223990A1 (en) * | 2013-02-28 | 2015-09-10 | Washington University | Methods of treatment of human cytomegalovirus infection and diseases with bromodomain inhibitors |
| EP2970285B1 (en) * | 2013-03-11 | 2019-04-17 | AbbVie Inc. | Fused tetracyclic bromodomain inhibitors |
| JP6401773B2 (ja) | 2013-03-11 | 2018-10-10 | ザ リージェンツ オブ ザ ユニヴァシティ オブ ミシガン | Betブロモドメイン阻害剤およびこれを用いる治療方法 |
| CN105026403B (zh) * | 2013-03-12 | 2018-05-18 | 艾伯维公司 | 四环布罗莫结构域抑制剂 |
| WO2014159837A1 (en) * | 2013-03-14 | 2014-10-02 | Convergene Llc | Methods and compositions for inhibition of bromodomain-containing proteins |
| US9714946B2 (en) | 2013-03-14 | 2017-07-25 | Dana-Farber Cancer Institute, Inc. | Bromodomain binding reagents and uses thereof |
| US9227985B2 (en) | 2013-03-15 | 2016-01-05 | Incyte Corporation | Tricyclic heterocycles as bet protein inhibitors |
| WO2014173241A1 (en) | 2013-04-26 | 2014-10-30 | Beigene, Ltd. | Substituted5-(3,5-dimethylisoxazol-4-yl)indoline-2-ones |
| TWI527811B (zh) | 2013-05-09 | 2016-04-01 | 吉李德科學股份有限公司 | 作爲溴結構域抑制劑的苯並咪唑衍生物 |
| US8975417B2 (en) * | 2013-05-27 | 2015-03-10 | Novartis Ag | Pyrazolopyrrolidine derivatives and their use in the treatment of disease |
| CA2912986A1 (en) * | 2013-05-28 | 2014-12-04 | Novartis Ag | Pyrazolo-pyrrolidin-4-one derivatives as bet inhibitors and their use in the treatment of disease |
| WO2014193951A1 (en) * | 2013-05-28 | 2014-12-04 | Dana-Farber Cancer Institute, Inc. | Bet inhibition therapy for heart disease |
| 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 |
| GB201311888D0 (en) | 2013-07-03 | 2013-08-14 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| GB201311891D0 (en) | 2013-07-03 | 2013-08-14 | Glaxosmithkline Ip Dev Ltd | Novel compound |
| EP3019502B1 (en) | 2013-07-08 | 2017-05-17 | Incyte Holdings Corporation | Tricyclic heterocycles as bet protein inhibitors |
| WO2015013635A2 (en) | 2013-07-25 | 2015-01-29 | Dana-Farber Cancer Institute, Inc. | Inhibitors of transcription factors and uses thereof |
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