CN107207474B - 被取代的杂环作为溴结构域抑制剂 - Google Patents

被取代的杂环作为溴结构域抑制剂 Download PDF

Info

Publication number
CN107207474B
CN107207474B CN201580066758.8A CN201580066758A CN107207474B CN 107207474 B CN107207474 B CN 107207474B CN 201580066758 A CN201580066758 A CN 201580066758A CN 107207474 B CN107207474 B CN 107207474B
Authority
CN
China
Prior art keywords
cancer
triazol
imidazol
cyclopropyl
phenyl
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.)
Active
Application number
CN201580066758.8A
Other languages
English (en)
Chinese (zh)
Other versions
CN107207474A (zh
Inventor
S·D·布朗
C·A·科伯恩
O·哈伦科
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Hengyi Biomedicine Shanghai Co ltd
Original Assignee
Hengyi Biomedical Technology Shanghai Co Ltd
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Hengyi Biomedical Technology Shanghai Co Ltd filed Critical Hengyi Biomedical Technology Shanghai Co Ltd
Publication of CN107207474A publication Critical patent/CN107207474A/zh
Application granted granted Critical
Publication of CN107207474B publication Critical patent/CN107207474B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • 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
    • A61K31/44—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
    • 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
    • A61K31/44—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
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/495—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
    • A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61K31/495—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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • 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
    • 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
    • A61K31/495—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
    • 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
    • A61K31/535—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
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C—CHEMISTRY; METALLURGY
    • 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
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN201580066758.8A 2014-12-11 2015-12-11 被取代的杂环作为溴结构域抑制剂 Active CN107207474B (zh)

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
CN107207474A CN107207474A (zh) 2017-09-26
CN107207474B true CN107207474B (zh) 2021-05-07

Family

ID=56106790

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201580066758.8A Active CN107207474B (zh) 2014-12-11 2015-12-11 被取代的杂环作为溴结构域抑制剂

Country Status (7)

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

Families Citing this family (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2935253B1 (en) 2012-12-21 2018-08-01 Zenith Epigenetics Ltd. Novel heterocyclic compounds as bromodomain inhibitors
WO2015004533A2 (en) 2013-06-21 2015-01-15 Zenith Epigenetics Corp. Novel substituted bicyclic compounds as bromodomain inhibitors
WO2015002754A2 (en) 2013-06-21 2015-01-08 Zenith Epigenetics Corp. Novel bicyclic bromodomain inhibitors
WO2015015318A2 (en) 2013-07-31 2015-02-05 Zenith Epigenetics Corp. Novel quinazolinones as bromodomain inhibitors
WO2016087942A1 (en) 2014-12-01 2016-06-09 Zenith Epigenetics Corp. Substituted pyridines as bromodomain inhibitors
WO2016087936A1 (en) 2014-12-01 2016-06-09 Zenith Epigenetics Corp. Substituted pyridinones as bromodomain inhibitors
US10292968B2 (en) 2014-12-11 2019-05-21 Zenith Epigenetics Ltd. Substituted heterocycles as bromodomain inhibitors
US10231953B2 (en) 2014-12-17 2019-03-19 Zenith Epigenetics Ltd. 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
JP7300394B2 (ja) 2017-01-17 2023-06-29 ヘパリジェニックス ゲーエムベーハー 肝再生の促進又は肝細胞死の低減もしくは予防のためのプロテインキナーゼ阻害
AU2018302178A1 (en) 2017-07-18 2020-02-13 Nuvation Bio Inc. 1,8-naphthyridinone compounds and uses thereof
SG11202000418XA (en) 2017-07-18 2020-02-27 Nuvation Bio Inc Heterocyclic compounds as adenosine antagonists
KR20190110740A (ko) 2018-03-21 2019-10-01 주식회사유한양행 신규의 아릴 또는 헤테로아릴 트라이아졸론 유도체 또는 이의 염 및 이를 포함하는 약학 조성물
KR20190110736A (ko) * 2018-03-21 2019-10-01 주식회사유한양행 신규의 트라이아졸론 유도체 또는 이의 염 및 이를 포함하는 약학 조성물
AU2019372121A1 (en) 2018-10-30 2021-05-27 Nuvation Bio Inc. Heterocyclic compounds as BET inhibitors
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
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
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
AU2020207951A1 (en) 2019-01-18 2021-08-26 Nuvation Bio Inc. 1,8-naphthyridinone compounds and uses thereof
EP3911323A4 (en) 2019-01-18 2022-11-16 Nuvation Bio Inc. HETEROCYCLIC COMPOUNDS AS ADENOSINE ANTAGONISTS
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

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006038734A1 (en) * 2004-10-08 2006-04-13 Astellas Pharma Inc. Pyridazinone derivatives cytokines inhibitors
WO2014096965A2 (en) * 2012-12-21 2014-06-26 Rvx Therapeutics Inc. Novel heterocyclic compounds as bromodomain inhibitors
WO2014191894A1 (en) * 2013-05-27 2014-12-04 Novartis Ag Imidazopyrrolidinone derivatives and their use in the treatment of disease

Family Cites Families (175)

* 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
DE4023369A1 (de) 1990-07-23 1992-01-30 Thomae Gmbh Dr K Benzimidazole, diese verbindungen enthaltende arzneimittel und verfahren zu ihrer herstellung
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
DE4225756A1 (de) 1992-01-22 1994-03-10 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
DE4224752A1 (de) 1992-04-11 1994-02-03 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
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
WO1996004274A1 (en) 1994-08-02 1996-02-15 Merck Sharp & Dohme Limited Azetidine, pyrrolidine and piperidine derivatives
DE69617665T2 (de) 1995-04-21 2002-05-08 Neurosearch A/S, Ballerup Benzmidazolverbindungen und ihre verwendung als modulatoren des gabaa-rezeptor-komplexes
JP2000072675A (ja) 1998-08-26 2000-03-07 Tanabe Seiyaku Co Ltd 医薬組成物
CN1177831C (zh) 1998-12-04 2004-12-01 神经研究公司 作为离子通道调节剂的新的苯并咪唑啉酮一、苯并噁唑酮一或苯并噻唑啉酮衍生物
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
EP1263754A1 (en) 2000-02-01 2002-12-11 Millennium Pharmaceuticals, Inc. INDALONE AND BENZIMIDAZOLONE INHIBITORS OF FACTOR Xa
US20120028912A1 (en) 2000-02-22 2012-02-02 J.David Gladstone Institute Methods of modulating bromodomains
MXPA03004672A (es) 2000-10-27 2004-04-20 Dow Agrosciences Llc 4,5-dihidro-1,2,4-triazin-6-onas sustituidas, 1,2,4-triazin-6-onas sustituidas, y su uso como fungicidas e insecticidas.
MXPA03004717A (es) 2000-12-01 2004-06-30 Osi Pharm Inc Compuestos especificos para el receptor a1, a2 y a3 de adenosina y usos de los mismos.
PL365027A1 (en) 2001-03-01 2004-12-27 Shionogi & Co, Ltd. Nitrogen-containing heteroaryl compounds having hiv integrase inhibitory activity
MXPA03008142A (es) 2001-03-09 2003-12-12 Pfizer Prod Inc Nuevos compuestos antiinflamatorios de bencimidazol.
CA2437785C (en) 2001-03-15 2009-05-12 Janssen Pharmaceutica N.V. Hiv inhibiting pyrazinone derivatives
EP1370553B1 (en) 2001-03-23 2006-05-10 Bayer Corporation Rho-kinase inhibitors
HUP0400323A2 (hu) 2001-03-28 2005-11-28 Bristol-Myers Squibb Company Tirozin-kináz inhibitorok és a vegyületeket tartalmazó gyógyszerkészítmények
US7081454B2 (en) 2001-03-28 2006-07-25 Bristol-Myers Squibb Co. Tyrosine kinase inhibitors
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
WO2004098494A2 (en) 2003-04-30 2004-11-18 Cytokinetics, Inc. Compounds, compositions, and methods
AU2003902860A0 (en) 2003-06-06 2003-06-26 Daicel Chemical Industries, Ltd Benzimidazole compounds
CA2533990A1 (en) 2003-08-08 2005-02-17 Avanir Pharmaceuticals Selective pharmacologic inhibition of protein trafficking and related methods of treating human diseases
NL1026826C2 (nl) 2003-08-13 2007-01-04 Pharmacia Corp Gesubstitueerde pyridinonen.
WO2005080380A1 (en) 2004-02-03 2005-09-01 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
JP4627315B2 (ja) 2004-03-23 2011-02-09 エフ．ホフマン−ラ ロシュ アーゲー 非ヌクレオシド逆転写酵素阻害剤としてのベンジルピリダジノン誘導体
EP1734820A4 (en) 2004-04-16 2008-01-23 Neurogen Corp Imidazopyrrazine, imidazopyridine, and imidazo-pyrimidine as CRF1 receptor ligands
EP1750706B1 (en) 2004-06-01 2016-10-05 University Of Virginia Patent Foundation Dual small molecule inhibitors of cancer and angiogenesis
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
MX2007001986A (es) 2004-08-26 2007-05-10 Pfizer Compuestos de aminoheteroarilo como inhibidores de proteina quinasa.
GB0420722D0 (en) 2004-09-17 2004-10-20 Addex Pharmaceuticals Sa Novel allosteric modulators
GB0420719D0 (en) 2004-09-17 2004-10-20 Addex Pharmaceuticals Sa Novel allosteric modulators
WO2006045096A2 (en) 2004-10-20 2006-04-27 Resverlogix Corp. Flavanoids and isoflavanoids for the prevention and treatment of cardiovascular diseases
CA2596424C (en) 2005-02-04 2016-03-29 Millennium Pharmaceuticals, Inc. Inhibitors of e1 activating enzymes
US7893267B2 (en) 2005-03-14 2011-02-22 High Point Pharmaceuticals, Llc Benzazole derivatives, compositions, and methods of use as β-secretase inhibitors
KR20080013990A (ko) 2005-05-03 2008-02-13 다우 아그로사이언시즈 엘엘씨 치환된 4,5-디하이드로-1,2,4-트리아진-6-온,1,2,4-트리아진-6-온 및 살진균제로서의 이의 용도
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
JP5119924B2 (ja) 2005-10-03 2013-01-16 小野薬品工業株式会社 含窒素複素環化合物およびその医薬用途
US20070197532A1 (en) 2005-11-18 2007-08-23 Cao Sheldon X Glucokinase activators
CN101321525B (zh) 2005-12-01 2013-01-30 霍夫曼-拉罗奇有限公司 作为l-cpt1抑制剂的杂芳基取代的哌啶衍生物
JP2009528989A (ja) 2006-02-17 2009-08-13 ファイザー・リミテッド Ｔｌｒ７変調剤としての３−デアザプリン誘導体
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
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
EP2007750B1 (en) 2006-04-03 2013-08-21 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
US7998995B2 (en) * 2006-12-08 2011-08-16 Exelixis Patent Company Llc LXR and FXR modulators
WO2008072784A1 (en) 2006-12-14 2008-06-19 Astellas Pharma Inc. Polycyclic acid compounds useful as crth2 antagonists and antiallergic agents
SG144809A1 (en) 2007-01-11 2008-08-28 Millipore U K Ltd Benzimidazole compounds and their use as chromatographic ligands
JP5236664B2 (ja) 2007-02-01 2013-07-17 レスバーロジックス コーポレイション 心血管疾患を予防および治療するための化合物
WO2008153701A1 (en) 2007-05-24 2008-12-18 Schering Corporation Compounds for inhibiting ksp kinesin activity
CN101687815A (zh) 2007-06-26 2010-03-31 塞诺菲-安万特股份有限公司 苯并咪唑和氮杂苯并咪唑的区域选择性铜催化合成
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
KR101600634B1 (ko) 2007-12-28 2016-03-07 미쓰비시 타나베 파마 코퍼레이션 항암제
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
US9540322B2 (en) 2008-08-18 2017-01-10 Yale University MIF modulators
EP2326631A4 (en) 2008-08-18 2012-03-21 Univ Yale MIF MODULATORS
ES2554375T3 (es) 2008-11-25 2015-12-18 University Of Rochester Inhibidores de las MLK y métodos de uso
PL2370413T3 (pl) 2008-12-08 2016-01-29 Arena Pharm Inc Modulatory receptora prostacykliny (PGI2) użyteczne w leczeniu zaburzeń z nimi związanych
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
US20120202793A1 (en) 2009-03-09 2012-08-09 Paul Sweetnam Rho kinase inhibitors
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
MX392179B (es) 2009-03-18 2025-03-21 Resverlogix Corp Nuevos agentes anti-inflamatorios.
AU2010239266B2 (en) 2009-04-22 2015-01-22 Resverlogix Corp. Novel anti-inflammatory agents
AU2010244553A1 (en) 2009-05-05 2011-12-01 F. Hoffmann-La Roche Ag Isoxazole-pyridine derivatives
GB0919431D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB0919432D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Use
GB0919423D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
DK2496582T3 (en) 2009-11-05 2016-03-21 Glaxosmithkline Llc Benzodiazepine-BROMDOMAeNEINHIBITOR.
GB0919434D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
PH12012500894A1 (en) 2009-11-05 2022-03-09 Glaxosmithkline Llc Benzodiazepine bromodomain inhibitor
WO2011062437A2 (ko) 2009-11-20 2011-05-26 에스케이케미칼주식회사 고나도트로핀 방출 호르몬 수용체 길항제, 이의 제조방법 및 이를 함유하는 약제학적 조성물
US20130085133A1 (en) 2010-02-08 2013-04-04 Sourthern Research Institute Office of Commercialization and Intellectual Prop. Anti-viral treatment and assay to screenfor anti-viral agent
KR101165996B1 (ko) 2010-04-23 2012-07-18 주식회사 녹십자 프탈라지논 유도체, 이의 제조방법 및 이를 함유하는 약학적 조성물
PL2571503T3 (pl) 2010-05-14 2015-06-30 Dana Farber Cancer Inst Inc Kompozycje i sposoby leczenia nowotworu, choroby zapalnej i innych zaburzeń
WO2011156626A1 (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
US20130165426A1 (en) 2010-07-06 2013-06-27 Université de Montréal Imidazopyridine, imidazopyrimidine and imidazopyrazine derivatives as melanocortin-4 receptor modulators
WO2012021382A1 (en) 2010-08-12 2012-02-16 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
WO2012075456A1 (en) 2010-12-02 2012-06-07 Constellation Pharmaceuticals Bromodomain inhibitors and uses thereof
AR084070A1 (es) 2010-12-02 2013-04-17 Constellation Pharmaceuticals Inc Inhibidores del bromodominio y usos de los mismos
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
GB201106799D0 (en) 2011-04-21 2011-06-01 Glaxosmithkline Llc Novel compounds
GB201106750D0 (en) 2011-04-21 2011-06-01 Glaxosmithkline Llc Novel compounds
GB201106743D0 (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
PT2773354T (pt) 2011-11-01 2019-07-17 Resverlogix Corp Formulações orais de libertação imediata para quinazolinonas substituídas
AU2012345779B2 (en) 2011-12-01 2017-04-06 Chemocentryx, Inc. Substituted benzimidazoles and benzopyrazoles as CCR(4) antagonists
WO2013097052A1 (en) 2011-12-30 2013-07-04 Abbott Laboratories Bromodomain inhibitors
US20130281396A1 (en) 2012-04-19 2013-10-24 Rvx Therapeutics Inc. Treatment of diseases by epigenetic regulation
US20130281397A1 (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
US20130281398A1 (en) 2012-04-19 2013-10-24 Rvx Therapeutics Inc. Treatment of diseases by epigenetic regulation
CA2870931A1 (en) 2012-04-20 2013-10-24 Abbvie Inc. Isoindolone derivatives
WO2013184878A1 (en) 2012-06-06 2013-12-12 Constellation Pharmaceuticals, Inc. Benzo [b] isoxazoloazepine bromodomain inhibitors and uses thereof
TR201807207T4 (tr) 2012-06-11 2018-06-21 Ucb Biopharma Sprl Tnf-alfa modüle edici benzimidazol bileşikleri.
EP2888256A4 (en) 2012-08-24 2016-02-17 Univ Texas HETEROCYCLIC HIF ACTIVITY MODULATORS FOR THE TREATMENT OF DISEASES
BR112015004858A2 (pt) 2012-09-05 2017-07-04 Bayer Cropscience Ag uso de 2-amidobenzimidazóis, 2-amidobenzoxazóis e 2-amidobenzotiazóis substituídos ou sais dos mesmos como substâncias ativas contra estresse abiótico em plantas
WO2014043246A1 (en) 2012-09-11 2014-03-20 The Board Of Trustees Of The University Of Illinois 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
WO2014080290A2 (en) 2012-11-21 2014-05-30 Rvx Therapeutics Inc. Cyclic amines as bromodomain inhibitors
US9765039B2 (en) 2012-11-21 2017-09-19 Zenith Epigenetics Ltd. Biaryl derivatives as bromodomain inhibitors
JP2016509576A (ja) 2012-12-20 2016-03-31 バイエル ファーマ アクチエンゲゼルシャフト Ｂｅｔタンパク質阻害性ジヒドロキノキザリノン類
WO2014128111A1 (de) 2013-02-22 2014-08-28 Bayer Pharma Aktiengesellschaft 4-substituierte pyrrolo- und pyrazolo-diazepine
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
WO2014128655A1 (en) 2013-02-25 2014-08-28 Aurigene Discovery Technologies Limited Substituted imidazo[4,5-c]quinoline derivatives as bromodomain inhibitors
US9492460B2 (en) 2013-02-27 2016-11-15 Bristol-Myers Squibb Company Carbazole compounds useful as bromodomain inhibitors
EP2961747B1 (en) 2013-02-27 2017-11-15 Bristol-Myers Squibb Company Carbazole compounds useful as bromodomain inhibitors
US9675697B2 (en) 2013-03-11 2017-06-13 The Regents Of The University Of Michigan BET bromodomain inhibitors and therapeutic methods using the same
JP2016512524A (ja) 2013-03-11 2016-04-28 アッヴィ・インコーポレイテッド ブロモドメイン阻害剤
EP2970285B1 (en) 2013-03-11 2019-04-17 AbbVie Inc. Fused tetracyclic bromodomain inhibitors
SG11201507383WA (en) 2013-03-12 2015-10-29 Abbvie Inc Dihydro-pyrrolopyridinone bromodomain inhibitors
CN105164113B (zh) 2013-03-12 2018-03-02 艾伯维公司 吡咯酰胺抑制剂
SG11201506245QA (en) 2013-03-14 2015-09-29 Glaxosmithkline Ip No 2 Ltd 2,3-disubstituted 1 -acyl-4-amino-1,2,3,4-tetrahydroquinoline derivatives and their use as bromodomain inhibitors
KR20150135359A (ko) 2013-03-14 2015-12-02 컨버진 엘엘씨 브로모도메인-함유 단백질의 억제를 위한 방법 및 조성물
JP6280573B2 (ja) 2013-03-14 2018-02-14 グラクソスミスクライン、インテレクチュアル、プロパティー、（ナンバー２）、リミテッドＧｌａｘｏｓｍｉｔｈｋｌｉｎｅ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ （Ｎｏ．２） Ｌｉｍｉｔｅｄ ブロモドメイン阻害薬としてのフロピリジン
US20140303121A1 (en) 2013-03-15 2014-10-09 Plexxikon Inc. Heterocyclic compounds and uses thereof
WO2014152029A2 (en) 2013-03-15 2014-09-25 Epigenetix, Inc. Oxazolo[5,4-c]quinolin-2-one compounds as bromodomain inhibitors
DK2970265T3 (en) 2013-03-15 2018-10-01 Plexxikon Inc HETEROCYCLIC COMPOUNDS AND APPLICATIONS THEREOF
ES2909778T3 (es) 2013-03-15 2022-05-10 Incyte Holdings Corp Heterociclos tricíclicos como inhibidores de proteína BET para su uso en el tratamiento de una enfermedad proliferativa en combinación con un inhibidor de Janus quinasas
EP2978758B1 (en) 2013-03-27 2017-02-08 Boehringer Ingelheim International GmbH Dihydroquinazolinone analogues as brd4 inhibitors
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
US10435364B2 (en) 2013-04-17 2019-10-08 Albert Ludwigs Universität Freiburg Compounds for use as bromodomain inhibitors
EP2792355A1 (en) 2013-04-17 2014-10-22 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
JP2016521722A (ja) 2013-06-17 2016-07-25 バイエル ファーマ アクチエンゲゼルシャフト 置換フェニル−２，３−ベンゾジアゼピン
WO2015004533A2 (en) 2013-06-21 2015-01-15 Zenith Epigenetics Corp. Novel 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
ES2635560T3 (es) 2013-07-08 2017-10-04 Incyte Holdings Corporation Heterociclos tricíclicos como inhibidores de la proteína NET
CN105555786A (zh) 2013-07-23 2016-05-04 拜耳制药股份公司 作为BET蛋白和极体样激酶的双重抑制剂的取代的二氢吡啶并[3,4-b]吡嗪酮
MX2016001037A (es) 2013-07-25 2016-11-10 Dana Farber Cancer Inst Inc Inhibidores de factores de transcripción y usos.
WO2015015318A2 (en) 2013-07-31 2015-02-05 Zenith Epigenetics Corp. Novel quinazolinones as bromodomain inhibitors
US20150051208A1 (en) 2013-08-14 2015-02-19 Boehringer Ingelheim International Gmbh Pyridinones
US9422281B2 (en) 2013-11-18 2016-08-23 Forma Therapeutics, Inc. Benzopiperazine compositions as BET bromodomain inhibitors
SMT202100125T1 (it) 2013-11-18 2021-05-07 Forma Therapeutics Inc Composizioni di tetraidrochinolina come inibitori di bromodomini bet
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
WO2016087942A1 (en) 2014-12-01 2016-06-09 Zenith Epigenetics Corp. Substituted pyridines as bromodomain inhibitors
WO2016087936A1 (en) 2014-12-01 2016-06-09 Zenith Epigenetics Corp. Substituted pyridinones as bromodomain inhibitors
US10292968B2 (en) 2014-12-11 2019-05-21 Zenith Epigenetics Ltd. Substituted heterocycles as bromodomain inhibitors
US10231953B2 (en) 2014-12-17 2019-03-19 Zenith Epigenetics Ltd. 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

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006038734A1 (en) * 2004-10-08 2006-04-13 Astellas Pharma Inc. Pyridazinone derivatives cytokines inhibitors
WO2014096965A2 (en) * 2012-12-21 2014-06-26 Rvx Therapeutics Inc. Novel heterocyclic compounds as bromodomain inhibitors
WO2014191894A1 (en) * 2013-05-27 2014-12-04 Novartis Ag Imidazopyrrolidinone derivatives and their use in the treatment of disease

Also Published As

Publication number Publication date
HK1245248B (en) 2020-05-15
WO2016092375A1 (en) 2016-06-16
CA2966449A1 (en) 2016-06-16
JP2017537946A (ja) 2017-12-21
CN107207474A (zh) 2017-09-26
EP3230277A1 (en) 2017-10-18
EP3230277A4 (en) 2018-04-25
US20170360756A1 (en) 2017-12-21
US10292968B2 (en) 2019-05-21
EP3230277B1 (en) 2019-09-18

Similar Documents

Publication Publication Date Title
CN107207474B (zh) 被取代的杂环作为溴结构域抑制剂
US11026926B2 (en) Substituted bicyclic compounds as bromodomain inhibitors
US10500209B2 (en) Quinazolinones as bromodomain inhibitors
CN107406438B (zh) 溴结构域的抑制剂
US9278940B2 (en) Cyclic amines as bromodomain inhibitors
US9765039B2 (en) Biaryl derivatives as bromodomain inhibitors
EP3227280B1 (en) Substituted pyridines as bromodomain inhibitors
CN108602821B (zh) 1h-咪唑并[4,5-b]吡啶基bet溴结构域抑制剂
CN109939113B (zh) 双环溴结构域抑制剂
HK1245248A1 (en) Substituted heterocycles as bromodomain inhibitors
US20190055235A1 (en) Substituted bicyclic compounds as bromodomain inhibitors
HK1246273A1 (en) Substituted pyridines as bromodomain inhibitors
HK40010367A (en) Bicyclic bromodomain inhibitors
HK1224659B (en) Novel substituted bicyclic compounds as bromodomain inhibitors
HK1224659A1 (en) Novel substituted bicyclic compounds as bromodomain inhibitors
HK1218547B (en) Novel quinazolinones as bromodomain inhibitors

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
TA01 Transfer of patent application right
TA01 Transfer of patent application right

Effective date of registration: 20200702

Address after: Room 413, building 3, No. 1690, Cailun Road, China (Shanghai) pilot Free Trade Zone, Pudong New Area, Shanghai

Applicant after: Hengyi biomedical technology (Shanghai) Co.,Ltd.

Address before: Alberta, Canada

Applicant before: ZENITH EPIGENETICS Corp.

GR01 Patent grant
GR01 Patent grant
CP03 Change of name, title or address
CP03 Change of name, title or address

Address after: 201203 building 10, No. 860, Xinyang Road, Lingang xinpian District, China (Shanghai) pilot Free Trade Zone, Pudong New Area, Shanghai

Patentee after: Hengyi biomedicine (Shanghai) Co.,Ltd.

Address before: Room 413, building 3, 1690 Cailun Road, China (Shanghai) pilot Free Trade Zone, Pudong New Area, Shanghai, 201203

Patentee before: Hengyi biomedical technology (Shanghai) Co.,Ltd.