HK1245248B - Substituted heterocycles as bromodomain inhibitors - Google Patents

Substituted heterocycles as bromodomain inhibitors Download PDF

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Publication number
HK1245248B
HK1245248B HK18104394.4A HK18104394A HK1245248B HK 1245248 B HK1245248 B HK 1245248B HK 18104394 A HK18104394 A HK 18104394A HK 1245248 B HK1245248 B HK 1245248B
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HK
Hong Kong
Prior art keywords
triazol
imidazol
cancer
cyclopropyl
phenyl
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HK18104394.4A
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German (de)
English (en)
French (fr)
Chinese (zh)
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HK1245248A1 (en
Inventor
Samuel David Brown
Craig Alan Coburn
Olesya KHARENKO
Original Assignee
恒翼生物医药(上海)股份有限公司
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Publication of HK1245248A1 publication Critical patent/HK1245248A1/en
Publication of HK1245248B publication Critical patent/HK1245248B/en

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    • 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
    • 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
    • A61K31/4164—1,3-Diazoles
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • 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
    • A61K31/4196—1,2,4-Triazoles
    • 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
    • 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
    • A61K31/435—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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • 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
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • A—HUMAN NECESSITIES
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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
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
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    • A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring 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
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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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52—Purines, e.g. adenine
    • A—HUMAN NECESSITIES
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    • A61K31/535—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 oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • 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
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
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    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
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    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
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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
    • C07D413/02—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
    • 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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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
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    • C07D473/32—Nitrogen atom
    • C07D473/34—Nitrogen atom attached in position 6, e.g. adenine
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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  • Health & Medical Sciences (AREA)
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  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
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  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
HK18104394.4A 2014-12-11 2015-12-11 Substituted heterocycles as bromodomain inhibitors HK1245248B (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201462090853P 2014-12-11 2014-12-11
US62/090,853 2014-12-11
PCT/IB2015/002479 WO2016092375A1 (en) 2014-12-11 2015-12-11 Substituted heterocycles as bromodomain inhibitors

Publications (2)

Publication Number Publication Date
HK1245248A1 HK1245248A1 (en) 2018-08-24
HK1245248B true HK1245248B (en) 2020-05-15

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HK18104394.4A HK1245248B (en) 2014-12-11 2015-12-11 Substituted heterocycles as bromodomain inhibitors

Country Status (7)

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US (1) US10292968B2 (enExample)
EP (1) EP3230277B1 (enExample)
JP (1) JP2017537946A (enExample)
CN (1) CN107207474B (enExample)
CA (1) CA2966449A1 (enExample)
HK (1) HK1245248B (enExample)
WO (1) WO2016092375A1 (enExample)

Families Citing this family (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
US9662311B2 (en) 2013-06-21 2017-05-30 Zenith Epigenetics Ltd. Substituted bicyclic compounds as bromodomain inhibitors
WO2015002754A2 (en) 2013-06-21 2015-01-08 Zenith Epigenetics Corp. Novel bicyclic bromodomain inhibitors
CA2919948C (en) 2013-07-31 2020-07-21 Zenith Epigenetics Corp. Novel quinazolinones as bromodomain inhibitors
WO2016087936A1 (en) 2014-12-01 2016-06-09 Zenith Epigenetics Corp. Substituted pyridinones as bromodomain inhibitors
US10179125B2 (en) 2014-12-01 2019-01-15 Zenith Epigenetics Ltd. Substituted pyridines 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
CN107349193A (zh) * 2016-05-10 2017-11-17 北京市神经外科研究所 蛋白功能抑制剂dapt在制备治疗内分泌疾病的药物中的用途
MX393780B (es) 2017-01-17 2025-03-24 Heparegenix Gmbh Inhibidores de proteina cinasa para promover la regeneracion hepatica o reducir o prevenir la muerte de hepatocitos
CA3070073A1 (en) 2017-07-18 2019-01-24 Nuvation Bio Inc. 1,8-naphthyridinone compounds and uses thereof
US11028058B2 (en) 2017-07-18 2021-06-08 Nuvation Bio Inc. Heterocyclic compounds as adenosine antagonists
KR20190110736A (ko) * 2018-03-21 2019-10-01 주식회사유한양행 신규의 트라이아졸론 유도체 또는 이의 염 및 이를 포함하는 약학 조성물
KR20190110740A (ko) 2018-03-21 2019-10-01 주식회사유한양행 신규의 아릴 또는 헤테로아릴 트라이아졸론 유도체 또는 이의 염 및 이를 포함하는 약학 조성물
EP3873474A4 (en) 2018-10-30 2022-07-13 Nuvation Bio Inc. HETEROCYCLIC COMPOUNDS USED AS BET INHIBITORS
TW202039486A (zh) 2018-12-14 2020-11-01 南韓商柳韓洋行股份有限公司 三唑并吡啶-3-酮化物或其鹽及包含彼之醫藥組合物
TWI835945B (zh) 2018-12-14 2024-03-21 南韓商柳韓洋行股份有限公司 3,3-二氟烯丙胺化物或其鹽及包含彼的醫藥組合物
CN109350616B (zh) 2018-12-18 2020-04-21 南华大学 I-brd9或其衍生物在制备抗癫痫药物中的应用
AU2020208644A1 (en) 2019-01-18 2021-08-26 Nuvation Bio Inc. Heterocyclic compounds as adenosine antagonists
WO2020150676A1 (en) 2019-01-18 2020-07-23 Nuvation Bio Inc. 1,8-naphthyridinone compounds and uses thereof
GB201905721D0 (en) 2019-04-24 2019-06-05 Univ Dundee Compounds
US11584756B2 (en) 2019-07-02 2023-02-21 Nuvation Bio Inc. Heterocyclic compounds as BET inhibitors
WO2022020114A2 (en) * 2020-07-10 2022-01-27 Ting Therapeutics Llc Methods for the prevention and treatment of hearing loss
EP4558224A1 (en) * 2022-07-21 2025-05-28 Tay Therapeutics Limited Pyrroles and imidazoles as bet protein inhibitors
CN116478141B (zh) * 2023-06-20 2023-10-24 药康众拓(江苏)医药科技有限公司 氘代kras抑制剂药物及用途

Family Cites Families (178)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3508258A1 (de) 1985-03-08 1986-09-18 Bayer Ag, 5090 Leverkusen Ss-lactamantibiotika, verfahren zur herstellung und ihre verwendung als und in arzneimitteln
FR2643903A1 (fr) 1989-03-03 1990-09-07 Union Pharma Scient Appl Nouveaux derives de benzimidazole, leurs procedes de preparation, intermediaires de synthese, compositions pharmaceutiques les contenant, utiles notamment pour le traitement des maladies cardiovasculaires, et des ulceres duodenaux
RU1836357C (ru) 1990-07-23 1993-08-23 Др.Карл Томэ ГмбХ Производные бензимидазола, их изомеры, смеси изомеров, гидраты или их физиологически переносимые соли, обладающие антагонистическими в отношении ангиотензина свойствами
DE4023369A1 (de) 1990-07-23 1992-01-30 Thomae Gmbh Dr K Benzimidazole, diese verbindungen enthaltende arzneimittel und verfahren zu ihrer herstellung
DE4225756A1 (de) 1992-01-22 1994-03-10 Thomae Gmbh Dr K Benzimidazole, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung
SI9210098B (sl) 1991-02-06 2000-06-30 Dr. Karl Thomae Benzimidazoli, zdravila, ki te spojine vsebujejo, in postopek za njihovo pripravo
DE4224752A1 (de) 1992-04-11 1994-02-03 Thomae Gmbh Dr K Benzimidazole, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung
US5614519A (en) 1991-02-06 1997-03-25 Karl Thomae Gmbh (1-(2,3 or 4-N-morpholinoalkyl)-imidazol-4-yl)-benizimidazol-1-yl-methyl]-biphenyls useful as angiotensin-II antagonists
US5125961A (en) 1991-08-12 1992-06-30 Monsanto Company Substituted pyridine compounds
DE4219534A1 (de) 1992-02-19 1993-12-16 Thomae Gmbh Dr K Substituierte Biphenylylderivate, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung
DE4408497A1 (de) 1994-03-14 1995-09-21 Thomae Gmbh Dr K Benzimidazole, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung
JPH10503768A (ja) 1994-08-02 1998-04-07 メルク シヤープ エンド ドーム リミテツド アゼチジン、ピロリジンおよびピペリジン誘導体
CN1072669C (zh) 1995-04-21 2001-10-10 纽罗研究公司 苯并咪唑化合物及其用作gabaa受体复合物调节器的用途
JP2000072675A (ja) 1998-08-26 2000-03-07 Tanabe Seiyaku Co Ltd 医薬組成物
CA2349616A1 (en) 1998-12-04 2000-06-15 Neurosearch A/S New benzimidazolone-, benzoxazolone-, or benzothiazolone derivatives as ion channel modulating agents
US6380235B1 (en) 1999-05-04 2002-04-30 American Home Products Corporation Benzimidazolones and analogues
US6664252B2 (en) 1999-12-02 2003-12-16 Osi Pharmaceuticals, Inc. 4-aminopyrrolo[2,3-d]pyrimidine compounds specific to adenosine A2a receptor and uses thereof
GB0002100D0 (en) 2000-01-28 2000-03-22 Novartis Ag Organic compounds
US20020019395A1 (en) 2000-02-01 2002-02-14 Bing-Yan Zhu Indalone and benzimidazolone inhibitors of factor Xa
US20120028912A1 (en) 2000-02-22 2012-02-02 J.David Gladstone Institute Methods of modulating bromodomains
AU2001297622A1 (en) 2000-10-27 2002-09-12 Dow Agrosciences Llc Substituted 4,5-dihydro-1,2,4-triazin-6-ones, 1,2,4-triazin-6-ones, and their use as fungicides and insecticides
AU2002248151B2 (en) 2000-12-01 2008-02-21 Osi Pharmaceuticals, Inc. Compounds specific to adenosine A1, A2A, and A3 receptor and uses thereof
PL365027A1 (en) 2001-03-01 2004-12-27 Shionogi & Co, Ltd. Nitrogen-containing heteroaryl compounds having hiv integrase inhibitory activity
JP2004526727A (ja) 2001-03-09 2004-09-02 ファイザー・プロダクツ・インク ベンゾイミダゾール抗炎症化合物
DE60221368T2 (de) 2001-03-15 2008-04-17 Janssen Pharmaceutica N.V. Hiv hemmende pyrazinon-derivate
CA2441492C (en) 2001-03-23 2011-08-09 Bayer Corporation Rho-kinase inhibitors
US7081454B2 (en) 2001-03-28 2006-07-25 Bristol-Myers Squibb Co. Tyrosine kinase inhibitors
CN1514833A (zh) 2001-03-28 2004-07-21 ����˹�ж�-����˹˹������˾ 新型酪氨酸激酶抑制剂
EP1475408B1 (en) 2002-02-15 2011-04-06 Bridgestone Corporation Rubber composition and pneumatic tire made therefrom
TWI276631B (en) 2002-09-12 2007-03-21 Avanir Pharmaceuticals Phenyl-aza-benzimidazole compounds for modulating IgE and inhibiting cellular proliferation
WO2004043913A2 (en) 2002-11-08 2004-05-27 Trimeris, Inc. Hetero-substituted benzimidazole compounds and antiviral uses thereof
AR043063A1 (es) 2002-12-13 2005-07-13 Altana Pharma Ag Bencimidazoles 6-sustituidos y su uso como inhibidores de secreciones gastricas
AR042956A1 (es) 2003-01-31 2005-07-13 Vertex Pharma Inhibidores de girasa y usos de los mismos
CL2004000409A1 (es) 2003-03-03 2005-01-07 Vertex Pharma Compuestos derivados de 2-(cilo sustituido)-1-(amino u oxi sustituido)-quinazolina, inhibidores de canales ionicos de sodio y calcio dependientes de voltaje; composicion farmaceutica; y uso del compuesto en el tratamiento de dolor agudo, cronico, neu
EP1620413A2 (en) 2003-04-30 2006-02-01 Cytokinetics, Inc. Compounds, compositions, and methods
AU2003902860A0 (en) 2003-06-06 2003-06-26 Daicel Chemical Industries, Ltd Benzimidazole compounds
EP1651198A2 (en) 2003-08-08 2006-05-03 Avanir Pharmaceuticals Selective pharmacologic inhibition of protein trafficking and related methods of treating human diseases
CL2004002050A1 (es) 2003-08-13 2005-06-03 Pharmacia Corp Sa Organizada B Compuestos derivados de piridinonas sustituidas; su uso en el tratamiento de afecciones causadas o exacerbadas por actividad p38 map kinasa y/o tnf no regulada, tales como inflamaciones, tumores, sida y otros.
EP1720862A1 (en) 2004-02-03 2006-11-15 Eli Lilly And Company Kinase inhibitors
WO2005075432A1 (ja) 2004-02-06 2005-08-18 Chugai Seiyaku Kabushiki Kaisha １−（２ｈ）−イソキノロン誘導体およびその抗ガン剤としての使用
CN1934092A (zh) 2004-03-23 2007-03-21 弗·哈夫曼-拉罗切有限公司 非核苷逆转录酶抑制剂
WO2005115399A2 (en) 2004-04-16 2005-12-08 Neurogen Corporation Imidazopyrazines, imidazopyridines, ans imidazopyrimidines as crf1 receptor ligands
KR101258298B1 (ko) 2004-06-01 2013-04-25 유니버시티 오브 버지니아 페이턴트 파운데이션 암 및 혈관형성의 이중 소분자 억제제
WO2005121132A1 (ja) 2004-06-11 2005-12-22 Shionogi & Co., Ltd. 抗ｈｃｖ作用を有する縮合ヘテロ環化合物
CA2578075A1 (en) 2004-08-26 2006-03-02 Pfizer Inc. Aminoheteroaryl compounds as protein tyrosine kinase inhibitors
GB0420719D0 (en) 2004-09-17 2004-10-20 Addex Pharmaceuticals Sa Novel allosteric modulators
GB0420722D0 (en) 2004-09-17 2004-10-20 Addex Pharmaceuticals Sa Novel allosteric modulators
WO2006038734A1 (en) * 2004-10-08 2006-04-13 Astellas Pharma Inc. Pyridazinone derivatives cytokines inhibitors
US7846915B2 (en) 2004-10-20 2010-12-07 Resverlogix Corporation Stilbenes and chalcones for the prevention and treatment of cardiovascular diseases
DK1848718T3 (da) 2005-02-04 2012-08-27 Millennium Pharm Inc E1 aktiveringsenzymhæmmere
CN101142194B (zh) 2005-03-14 2012-10-10 顶点制药有限责任公司 吲哚衍生物，组合物及用作β-分泌酶抑制剂的方法
WO2006119400A2 (en) 2005-05-03 2006-11-09 Dow Agrosciences Llc Substituted 4,5-dihydro-1,2,4-triazin-6-ones, 1,2,4-trianzin-6-ones, and their use as fungicides
WO2007016525A2 (en) 2005-07-29 2007-02-08 Resverlogix Corp. Pharmaceutical compositions for the prevention and treatment of complex diseases and their delivery by insertable medical devices
RU2008112691A (ru) 2005-10-03 2009-10-10 Оно Фармасьютикал Ко., Лтд. (Jp) Азотсодержащее гетероциклическое соединение и его фармацевтическое применение
WO2007061923A2 (en) 2005-11-18 2007-05-31 Takeda San Diego, Inc. Glucokinase activators
JP4855478B2 (ja) 2005-12-01 2012-01-18 エフ．ホフマン−ラ ロシュ アーゲー Ｌ−ｃｐｔ１阻害剤としてのヘテロアリール置換されたピペリジン誘導体
CN101384593A (zh) 2006-02-17 2009-03-11 辉瑞有限公司 用作tlr7调节剂的3-脱氮嘌呤衍生物
KR20080085232A (ko) 2006-02-17 2008-09-23 화이자 리미티드 Ｔｌｒ7 조절제로서 3-데아자퓨린 유도체
JP5451375B2 (ja) 2006-03-24 2014-03-26 ロレアル 内部カチオン電荷を有するアミノ基を含むチオール／ジスルフィド蛍光着色剤を含有する染色用組成物、および前記着色剤を使用してケラチン物質を明色化する方法
AU2007233715A1 (en) 2006-04-03 2007-10-11 Glaxo Group Limited Azabicyclo [3. 1. 0] hexyl derivatives as modulators of dopamine D3 receptors
WO2008054599A2 (en) 2006-09-27 2008-05-08 Surface Logix, Inc. Rho kinase inhibitors
EP2121621B1 (en) * 2006-12-08 2014-05-07 Exelixis Patent Company LLC Lxr and fxr modulators
CN101636386A (zh) 2006-12-14 2010-01-27 安斯泰来制药有限公司 用作crth2拮抗剂和抗过敏剂的多环酸化合物
SG144809A1 (en) 2007-01-11 2008-08-28 Millipore U K Ltd Benzimidazole compounds and their use as chromatographic ligands
EP2118074B1 (en) 2007-02-01 2014-01-22 Resverlogix Corp. Compounds for the prevention and treatment of cardiovascular diseases
WO2008153701A1 (en) 2007-05-24 2008-12-18 Schering Corporation Compounds for inhibiting ksp kinesin activity
MX2009013753A (es) 2007-06-26 2010-01-26 Sanofi Aventis Una sintesis regioselectiva catalizada por cobre de bencimidazoles y azabencimidazoles.
DE102007032507A1 (de) 2007-07-12 2009-04-02 Merck Patent Gmbh Pyridazinonderivate
DE102007038957A1 (de) 2007-08-17 2009-02-19 Merck Patent Gmbh 6-Thioxo-pyridazinderivate
GB0719235D0 (en) 2007-10-02 2007-11-14 Glaxo Group Ltd Novel compounds
WO2009054790A1 (en) 2007-10-26 2009-04-30 Astrazeneca Ab Amide linked heteroaromatic derivatives as modulators of mglur5
US8084466B2 (en) 2007-12-18 2011-12-27 Janssen Pharmaceutica Nv Bicyclic heteroaryl-substituted imidazoles as modulators of the histamine H4 receptor
CA2710740C (en) 2007-12-28 2016-07-19 Shinji Miyoshi Thienotriazolodiazepine compound as antitumor agent
TW200938542A (en) 2008-02-01 2009-09-16 Irm Llc Compounds and compositions as kinase inhibitors
WO2009158258A1 (en) 2008-06-25 2009-12-30 E. I. Du Pont De Nemours And Company Herbicidal dihydro oxo six-membered azinyl isoxazolines
US20100012745A1 (en) 2008-07-15 2010-01-21 Sturman Digital Systems, Llc Fuel Injectors with Intensified Fuel Storage and Methods of Operating an Engine Therewith
MX2011001872A (es) 2008-08-18 2011-05-23 Univ Yale Moduladores de mif.
US9540322B2 (en) 2008-08-18 2017-01-10 Yale University MIF modulators
CN102264743B (zh) 2008-11-25 2015-02-11 罗彻斯特大学 Mlk抑制剂及其使用方法
WO2010077275A1 (en) 2008-12-08 2010-07-08 Arena Pharmaceuticals, Inc. Modulators of the prostacyclin (pgi2) receptor useful for the treatment of disorders related thereto
EP2196465A1 (en) 2008-12-15 2010-06-16 Almirall, S.A. (3-oxo)pyridazin-4-ylurea derivatives as PDE4 inhibitors
DE102008062826A1 (de) 2008-12-23 2010-07-01 Merck Patent Gmbh Pyridazinonderivate
US8389550B2 (en) 2009-02-25 2013-03-05 Hoffmann-La Roche Inc. Isoxazoles / O-pyridines with ethyl and ethenyl linker
JP2012519732A (ja) 2009-03-09 2012-08-30 サーフェイス ロジックス，インコーポレイティド Ｒｈｏキナーゼ阻害剤
CN105859639A (zh) 2009-03-18 2016-08-17 雷斯韦洛吉克斯公司 新的抗炎剂
CN102448458B (zh) 2009-03-18 2015-07-22 小利兰·斯坦福大学理事会 治疗黄病毒科病毒感染的方法和组合物
CN102458405B (zh) 2009-04-22 2017-06-23 雷斯韦洛吉克斯公司 新抗炎剂
MX2011011489A (es) 2009-05-05 2011-11-18 Hoffmann La Roche Derivados de isoxazol-piridina.
GB0919431D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB0919434D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
ME02360B (me) 2009-11-05 2016-06-20 Glaxosmithkline Llc Inhibitor bromodomena benzodiazepina
SI2496582T1 (sl) 2009-11-05 2016-04-29 Glaxosmithkline Llc Corporation Service Company Benzodiazepinski inhibitor bromodomene
GB0919432D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Use
GB0919423D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
US9034850B2 (en) 2009-11-20 2015-05-19 Sk Chemicals Co., Ltd. Gonadotropin releasing hormone receptor antagonist, preparation method thereof and pharmaceutical composition comprising the same
WO2011097607A1 (en) 2010-02-08 2011-08-11 Southern Research Institute Anti-viral treatment and assay to screen for anti-viral agent
KR101165996B1 (ko) 2010-04-23 2012-07-18 주식회사 녹십자 프탈라지논 유도체, 이의 제조방법 및 이를 함유하는 약학적 조성물
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
CA2810162A1 (en) 2010-06-09 2011-12-15 Rutgers, The State University Of New Jersey Antimicrobial agents
WO2011159926A1 (en) 2010-06-16 2011-12-22 Rutgers, The State University Of New Jersey Antimicrobial agents
CA2803448A1 (en) 2010-07-06 2012-01-12 Universite De Montreal Imidazopyridine, imidazopyrimidine and imidazopyrazine derivatives as melanocortin-4 receptor modulators
EP2603079B1 (en) 2010-08-12 2018-09-19 Merck Sharp & Dohme Corp. Positive allosteric modulators of mglur2
WO2012040499A2 (en) 2010-09-22 2012-03-29 Surface Logix, Inc. Metabolic inhibitors
KR101242572B1 (ko) 2010-10-12 2013-03-19 한국화학연구원 5-환 헤테로 아릴로 치환된 프탈라지논 유도체 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 유효성분으로 포함하는 약학적 조성물
GB201018147D0 (en) 2010-10-27 2010-12-08 Glaxo Group Ltd Method of treatment
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
CN102731409A (zh) 2011-04-08 2012-10-17 中国科学院上海药物研究所 一类哒嗪酮类化合物，其药物组合物、制备方法及用途
GB201106743D0 (en) 2011-04-21 2011-06-01 Glaxosmithkline Llc Novel compounds
GB201106750D0 (en) 2011-04-21 2011-06-01 Glaxosmithkline Llc Novel compounds
GB201106799D0 (en) 2011-04-21 2011-06-01 Glaxosmithkline Llc Novel compounds
GB201107325D0 (en) 2011-05-04 2011-06-15 Glaxosmithkline Llc Novel compounds
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
TR201909777T4 (tr) 2011-11-01 2019-07-22 Resverlogix Corp Sübsti̇tüe ki̇nazoli̇nonlara yöneli̇k oral çabuk salimli formülasyonlar
CA2856831C (en) 2011-12-01 2020-02-18 Chemocentryx, Inc. Substituted benzimidazoles and benzopyrazoles as ccr(4) antagonists
WO2013097052A1 (en) 2011-12-30 2013-07-04 Abbott Laboratories Bromodomain inhibitors
US20130281397A1 (en) 2012-04-19 2013-10-24 Rvx Therapeutics Inc. Treatment of diseases by epigenetic regulation
US20130281398A1 (en) 2012-04-19 2013-10-24 Rvx Therapeutics Inc. Treatment of diseases by epigenetic regulation
US20130281396A1 (en) 2012-04-19 2013-10-24 Rvx Therapeutics Inc. Treatment of diseases by epigenetic regulation
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
WO2013184878A1 (en) 2012-06-06 2013-12-12 Constellation Pharmaceuticals, Inc. Benzo [b] isoxazoloazepine bromodomain inhibitors and uses thereof
WO2013186229A1 (en) 2012-06-11 2013-12-19 Ucb Pharma S.A. Tnf -alpha modulating benzimidazoles
US20140073634A1 (en) 2012-08-24 2014-03-13 Institute For Applied Cancer Science/The University of Texas MD Anderson Cancer Center Heterocyclic modulators of hif activity for treatment of disease
AU2013311826A1 (en) 2012-09-05 2015-03-26 Bayer Cropscience Ag Use of substituted 2-amidobenzimidazoles, 2-amidobenzoxazoles and 2-amidobenzothiazoles or salts thereof as active substances against abiotic plant stress
US20150246888A1 (en) 2012-09-11 2015-09-03 Michael Johnson Enoyl reductase inhibitors with antibacterial activity
US9663533B2 (en) 2012-11-14 2017-05-30 Glaxosmithkline Llc Thieno[3,2-C]pyridin-4(5H)-ones as BET inhibitors
US9765039B2 (en) 2012-11-21 2017-09-19 Zenith Epigenetics Ltd. Biaryl derivatives as bromodomain inhibitors
US9073878B2 (en) 2012-11-21 2015-07-07 Zenith Epigenetics Corp. Cyclic amines as bromodomain inhibitors
WO2014095775A1 (de) 2012-12-20 2014-06-26 Bayer Pharma Aktiengesellschaft Bet-proteininhibitorische dihydrochinoxalinone
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
JP2016513118A (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 ４−置換されたピロロ−およびピラゾロジアゼピン類
CN105189514A (zh) 2013-02-22 2015-12-23 拜耳医药股份有限公司 作为bet-蛋白抑制剂用于治疗过度增殖性疾病的吡咯并-和吡唑并-三唑并二氮杂卓
WO2014128655A1 (en) 2013-02-25 2014-08-28 Aurigene Discovery Technologies Limited Substituted imidazo[4,5-c]quinoline derivatives as bromodomain inhibitors
EP2961747B1 (en) 2013-02-27 2017-11-15 Bristol-Myers Squibb Company Carbazole compounds useful as bromodomain inhibitors
US9492460B2 (en) 2013-02-27 2016-11-15 Bristol-Myers Squibb Company Carbazole compounds useful as bromodomain inhibitors
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
AU2014249192B2 (en) 2013-03-11 2017-12-21 The Regents Of The University Of Michigan BET bromodomain inhibitors and therapeutic methods using the same
CA2904048A1 (en) 2013-03-11 2014-10-09 Abbvie Inc. Bromodomain inhibitors
KR20150126696A (ko) 2013-03-12 2015-11-12 애브비 인코포레이티드 디하이드로-피롤로피리디논 브로모도메인 억제제
JP2016512542A (ja) 2013-03-12 2016-04-28 アッヴィ・インコーポレイテッド ピロールアミド阻害剤
RS58264B1 (sr) 2013-03-14 2019-03-29 Glaxosmithkline Ip No 2 Ltd 2,3-disupstituisani 1-acil-4-amino-1,2,3,4-tetrahidrohinolin derivati i njihova upotreba kao inhibitora bromodomena
KR20150135359A (ko) 2013-03-14 2015-12-02 컨버진 엘엘씨 브로모도메인-함유 단백질의 억제를 위한 방법 및 조성물
BR112015022782A2 (pt) 2013-03-14 2017-07-18 Glaxosmithkline Ip No 2 Ltd composto, composição farmacêutica, combinação, e, uso de um composto
US20140303121A1 (en) 2013-03-15 2014-10-09 Plexxikon Inc. Heterocyclic compounds and uses thereof
CA2904364A1 (en) 2013-03-15 2014-09-25 Epigenetix, Inc. Oxazolo[5,4-c]quinolin-2-one compounds as bromodomain inhibitors
CA2903293C (en) 2013-03-15 2020-10-13 Plexxikon Inc. Heterocyclic compounds and uses thereof
EA038494B1 (ru) 2013-03-15 2021-09-07 Инсайт Холдингс Корпорейшн Трициклические гетероциклы как ингибиторы белков бэт
JP6453845B2 (ja) 2013-03-27 2019-01-16 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Ｂｒｄ４阻害薬としてのジヒドロキナゾリノン類似体
US9102684B2 (en) 2013-03-27 2015-08-11 Boehringer Ingelheim International Gmbh Indolinone analogues
TWI530499B (zh) 2013-03-28 2016-04-21 吉李德科學股份有限公司 作為溴結構域（ｂｒｏｍｏｄｏｍａｉｎ）抑制劑之苯並咪唑酮衍生物類
EP2792355A1 (en) 2013-04-17 2014-10-22 Albert-Ludwigs-Universität Freiburg Compounds for use as bromodomain inhibitors
US10435364B2 (en) 2013-04-17 2019-10-08 Albert Ludwigs Universität Freiburg Compounds for use as bromodomain inhibitors
EA027139B1 (ru) 2013-04-26 2017-06-30 Бейджин, Лтд. Замещенные 5-(3,5-диметилизоксазол-4-ил)индолин-2-оны
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
EA029312B1 (ru) * 2013-05-27 2018-03-30 Новартис Аг Производные имидазопирролидинона и их применение при лечении заболеваний
EP3010909A1 (de) 2013-06-17 2016-04-27 Bayer Pharma Aktiengesellschaft Substituierte phenyl-2,3-benzodiazepine
US9662311B2 (en) 2013-06-21 2017-05-30 Zenith Epigenetics Ltd. Substituted bicyclic compounds as bromodomain inhibitors
WO2015002754A2 (en) 2013-06-21 2015-01-08 Zenith Epigenetics Corp. Novel bicyclic bromodomain inhibitors
AR096758A1 (es) 2013-06-28 2016-02-03 Abbvie Inc Inhibidores cristalinos de bromodominios
US9290514B2 (en) 2013-07-08 2016-03-22 Incyte Holdings Corporation Tricyclic heterocycles as BET protein inhibitors
ES2648876T3 (es) 2013-07-23 2018-01-08 Bayer Pharma Aktiengesellschaft Dihidropirido[3,4-b]pirazinonas sustituidas como inhibidores duales de proteínas BET y quinasas tipo polo
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
US20150051208A1 (en) 2013-08-14 2015-02-19 Boehringer Ingelheim International Gmbh Pyridinones
CN106029076B (zh) 2013-11-18 2019-06-07 福马疗法公司 作为bet溴域抑制剂的苯并哌嗪组合物
RS61519B1 (sr) 2013-11-18 2021-03-31 Forma Therapeutics Inc Sastavi tetrahidrohinolina kao inhibitori bet bromodomena
GB201321739D0 (en) 2013-12-09 2014-01-22 Ucb Pharma Sa Therapeutic agents
US9458156B2 (en) 2014-12-23 2016-10-04 Bristol-Myers Squibb Company Tricyclic compounds as anticancer agents
WO2016087936A1 (en) 2014-12-01 2016-06-09 Zenith Epigenetics Corp. Substituted pyridinones as bromodomain inhibitors
US10179125B2 (en) 2014-12-01 2019-01-15 Zenith Epigenetics Ltd. Substituted pyridines 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
US20190055235A1 (en) 2014-12-17 2019-02-21 Zenith Epigenetics Ltd. Substituted bicyclic compounds as bromodomain inhibitors
CA2915661A1 (en) 2014-12-23 2016-06-23 Husky Oil Operations Limited Multilateral well completions to improve individual branch control

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EP3230277A4 (en) 2018-04-25
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