HK1222646A1 - 作為溴結構域抑制劑的苯並咪唑衍生物 - Google Patents

作為溴結構域抑制劑的苯並咪唑衍生物

Info

Publication number
HK1222646A1
HK1222646A1 HK16110539.9A HK16110539A HK1222646A1 HK 1222646 A1 HK1222646 A1 HK 1222646A1 HK 16110539 A HK16110539 A HK 16110539A HK 1222646 A1 HK1222646 A1 HK 1222646A1
Authority
HK
Hong Kong
Prior art keywords
benzimidazole derivatives
bromodomain inhibitors
bromodomain
inhibitors
benzimidazole
Prior art date
Application number
HK16110539.9A
Other languages
English (en)
Inventor
Evangelos Aktoudianakis
Gregory Chin
Britton Kenneth Corkey
Jinfa Du
Kristyna Elbel
Robert H Jiang
Tetsuya Kobayashi
Rick Lee
Ruben Martinez
Samuel E Metobo
Michael Mish
Manuel Munoz
Sophie Shevick
David Sperandio
Hai Yang
Jeff Zablocki
Original Assignee
Gilead Sciences Inc
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 Gilead Sciences Inc filed Critical Gilead Sciences Inc
Publication of HK1222646A1 publication Critical patent/HK1222646A1/zh

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/04Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D453/00Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
    • C07D453/02Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Epidemiology (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
HK16110539.9A 2013-05-09 2016-09-05 作為溴結構域抑制劑的苯並咪唑衍生物 HK1222646A1 (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201361821612P 2013-05-09 2013-05-09
US201361826912P 2013-05-23 2013-05-23
US201361860229P 2013-07-30 2013-07-30
US201461951347P 2014-03-11 2014-03-11
PCT/US2014/037344 WO2014182929A1 (en) 2013-05-09 2014-05-08 Benzimidazole derivatives as bromodomain inhibitors

Publications (1)

Publication Number Publication Date
HK1222646A1 true HK1222646A1 (zh) 2017-07-07

Family

ID=50897952

Family Applications (2)

Application Number Title Priority Date Filing Date
HK16107380.5A HK1219278A1 (zh) 2013-05-09 2016-06-24 作為溴結構域抑制劑的苯並咪唑衍生物
HK16110539.9A HK1222646A1 (zh) 2013-05-09 2016-09-05 作為溴結構域抑制劑的苯並咪唑衍生物

Family Applications Before (1)

Application Number Title Priority Date Filing Date
HK16107380.5A HK1219278A1 (zh) 2013-05-09 2016-06-24 作為溴結構域抑制劑的苯並咪唑衍生物

Country Status (26)

Country Link
US (4) US20160075695A1 (zh)
EP (1) EP2994469B1 (zh)
JP (1) JP6049942B2 (zh)
KR (1) KR101761049B1 (zh)
CN (1) CN105324379B (zh)
AP (1) AP2015008869A0 (zh)
AR (1) AR096246A1 (zh)
AU (1) AU2014262622B2 (zh)
BR (1) BR112015028017A2 (zh)
CA (1) CA2911408C (zh)
CL (1) CL2015003280A1 (zh)
CR (1) CR20150639A (zh)
EA (1) EA029091B1 (zh)
ES (1) ES2710120T3 (zh)
HK (2) HK1219278A1 (zh)
MD (1) MD4592B1 (zh)
MX (1) MX2015015478A (zh)
NZ (1) NZ713718A (zh)
PE (1) PE20160029A1 (zh)
PH (1) PH12015502534A1 (zh)
PT (1) PT2994469T (zh)
SG (1) SG11201509220XA (zh)
TW (1) TWI527811B (zh)
UA (1) UA112618C2 (zh)
UY (1) UY35559A (zh)
WO (1) WO2014182929A1 (zh)

Families Citing this family (63)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014080290A2 (en) 2012-11-21 2014-05-30 Rvx Therapeutics Inc. Cyclic amines as bromodomain inhibitors
WO2014080291A2 (en) 2012-11-21 2014-05-30 Rvx Therapeutics Inc. Biaryl derivatives as bromodomain inhibitors
CA2895905A1 (en) 2012-12-21 2014-06-26 Zenith Epigenetics Corp. Novel heterocyclic compounds as bromodomain inhibitors
SG10201707487VA (en) 2013-03-15 2017-10-30 Incyte Corp Tricyclic heterocycles as bet protein inhibitors
JP6461118B2 (ja) * 2013-06-21 2019-01-30 ゼニス・エピジェネティクス・リミテッドZenith Epigenetics Ltd. ブロモドメイン阻害剤としての新規の置換された二環式化合物
NZ714669A (en) 2013-06-21 2021-07-30 Zenith Epigenetics Ltd Novel bicyclic bromodomain inhibitors
WO2015006193A1 (en) 2013-07-08 2015-01-15 Incyte Corporation Tricyclic heterocycles as bet protein inhibitors
EA201690087A1 (ru) 2013-07-31 2016-08-31 Зенит Эпидженетикс Корп. Новые квиназолиноны как ингибиторы бромодомена
US9315501B2 (en) 2013-11-26 2016-04-19 Incyte Corporation Bicyclic heterocycles as BET protein inhibitors
WO2015081203A1 (en) 2013-11-26 2015-06-04 Incyte Corporation Bicyclic heterocycles as bet protein inhibitors
WO2015095492A1 (en) 2013-12-19 2015-06-25 Incyte Corporation Tricyclic heterocycles as bet protein inhibitors
SG11201608843TA (en) 2014-04-23 2016-11-29 Incyte Corp 1H-PYRROLO[2,3-c]PYRIDIN-7(6H)-ONES AND PYRAZOLO[3,4-c]PYRIDIN-7(6H)-ONES AS INHIBITORS OF BET PROTEINS
JP2017523214A (ja) * 2014-08-05 2017-08-17 ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company ヘテロ環キナーゼ阻害剤
WO2016044130A1 (en) * 2014-09-15 2016-03-24 Incyte Corporation Tricyclic heterocycles for use as bet protein inhibitors
CA2966303A1 (en) 2014-12-01 2016-06-09 Zenith Epigenetics Ltd. Substituted pyridines as bromodomain inhibitors
WO2016087936A1 (en) 2014-12-01 2016-06-09 Zenith Epigenetics Corp. Substituted pyridinones as bromodomain inhibitors
CA2966449A1 (en) 2014-12-11 2016-06-16 Zenith Epigenetics Ltd. Substituted heterocycles as bromodomain inhibitors
CN107406438B (zh) * 2014-12-17 2021-05-14 恒翼生物医药科技(上海)有限公司 溴结构域的抑制剂
US20190055235A1 (en) * 2014-12-17 2019-02-21 Zenith Epigenetics Ltd. Substituted bicyclic compounds as bromodomain inhibitors
GB201504689D0 (en) * 2015-03-19 2015-05-06 Glaxosmithkline Ip Dev Ltd Chemical compounds
CN104788441A (zh) * 2015-04-02 2015-07-22 湖南华腾制药有限公司 一种多取代苯并恶唑衍生物的制备方法
GB201506658D0 (en) * 2015-04-20 2015-06-03 Cellcentric Ltd Pharmaceutical compounds
WO2016186967A1 (en) * 2015-05-15 2016-11-24 Gilead Sciences, Inc. Benzimidazole and imadazopyridine carboximidamide compounds having activity as inhibitors of indoleamine 2,3-dioxygenase
EP3298005B1 (en) * 2015-05-21 2024-01-24 The Regents of The University of California Anti-cancer compounds
SG10201912386RA (en) 2015-09-21 2020-02-27 Plexxikon Inc Heterocyclic compounds and uses thereof
US20170121347A1 (en) 2015-10-29 2017-05-04 Incyte Corporation Amorphous solid form of a bet protein inhibitor
CN108689945A (zh) * 2015-12-01 2018-10-23 江苏理工学院 一种苯并咪唑衍生物的制备方法
CA3006772A1 (en) 2015-12-17 2017-06-22 Gilead Sciences, Inc. Tank-binding kinase inhibitor compounds
WO2017106568A1 (en) 2015-12-17 2017-06-22 Gilead Sciences, Inc. Combination of a jak inhibitor and a bromodomain inhibitor for treating cancer
EA201891514A1 (ru) * 2015-12-24 2019-01-31 Селджен Квонтисел Рисёрч, Инк. Комбинированная терапия ингибитором бромодомена и экстратерминального белка
IL263824B2 (en) 2016-06-20 2023-10-01 Incyte Corp Crystals in solid form in the presence of an inhibitor
CA3029004A1 (en) 2016-06-24 2017-12-28 The Regents Of The University Of California Phthalazine derivatives as inhibitors of parp1, parp2 and/or tubulin useful for the treatment of cancer
GB201614939D0 (en) * 2016-09-02 2016-10-19 Glaxosmithkline Ip Dev Ltd Crystalline hydrate
GB201617630D0 (en) * 2016-10-18 2016-11-30 Cellcentric Ltd Pharmaceutical compounds
GB201617627D0 (en) * 2016-10-18 2016-11-30 Cellcentric Ltd Pharmaceutical compounds
KR102587839B1 (ko) 2016-10-27 2023-10-11 셀젠 콴티셀 리서치, 인크. 브로모도메인 및 엑스트라-말단 단백질 억제제 병용 치료요법
US20180133212A1 (en) 2016-11-03 2018-05-17 Gilead Sciences, Inc. Combination of a bcl-2 inhibitor and a bromodomain inhibitor for treating cancer
US20180141939A1 (en) 2016-11-22 2018-05-24 Gilead Sciences, Inc. Solid forms of a bet inhibitor
WO2018097976A1 (en) 2016-11-22 2018-05-31 Gilead Sciences, Inc. Synthesis of a compound that modulates the activity of bromodomain-containing proteins
US20180153867A1 (en) * 2016-12-06 2018-06-07 Gilead Sciences, Inc. Treatment of prostate cancer by concomitant administration of a bromodomain inhibitor and a second agent
US20180153868A1 (en) * 2016-12-06 2018-06-07 Gilead Sciences, Inc. Treatment of breast cancer by concomitant administration of a bromodomain inhibitor and a second agent
AU2017378398B2 (en) * 2016-12-14 2023-02-02 Biora Therapeutics, Inc. Treatment of a disease of the gastrointestinal tract with a JAK inhibitor and devices
CN108314680A (zh) * 2017-01-16 2018-07-24 凯惠科技发展(上海)有限公司 一种含芳环化合物、其制备方法、药物组合物及应用
JOP20180040A1 (ar) 2017-04-20 2019-01-30 Gilead Sciences Inc مثبطات pd-1/pd-l1
EP3625355A4 (en) * 2017-05-19 2021-02-24 Epicypher, Inc. ANALYZES FOR A NUCLEOSOME REMODELING ACTIVITY
MA50250A (fr) 2017-09-15 2020-07-22 Forma Therapeutics Inc Compositions de tétrahydroimidazo quinoléine utilisées en tant qu'inhibiteurs de cbp/p300
SG11202005793SA (en) * 2017-12-20 2020-07-29 Betta Pharmaceuticals Co Ltd Compound functioning as bromodomain protein inhibitor, and composition
AU2019222644B2 (en) 2018-02-13 2021-04-01 Gilead Sciences, Inc. PD-1/PD-L1 inhibitors
GB201806320D0 (en) * 2018-04-18 2018-05-30 Cellcentric Ltd Process
CN112041311B (zh) 2018-04-19 2023-10-03 吉利德科学公司 Pd-1/pd-l1抑制剂
CN114145817A (zh) * 2018-05-08 2022-03-08 贝利斯医疗公司 在穿刺线上制造至少一个位置标记物的方法
PL3793565T3 (pl) 2018-05-14 2022-05-02 Gilead Sciences, Inc. Inhibitory MCL-1
SG11202012767UA (en) 2018-06-29 2021-01-28 Forma Therapeutics Inc Inhibiting creb binding protein (cbp)
EP4234030A3 (en) 2018-07-13 2023-10-18 Gilead Sciences, Inc. Pd-1/pd-l1 inhibitors
WO2020086556A1 (en) 2018-10-24 2020-04-30 Gilead Sciences, Inc. Pd-1/pd-l1 inhibitors
CN109912584B (zh) * 2019-03-22 2021-08-13 中国药科大学 一种具有抗肿瘤活性的brd4蛋白抑制剂及其制备方法和应用
CN113544129B (zh) * 2019-04-04 2024-07-23 上海华汇拓医药科技有限公司 三环类化合物制备方法及其在医药领域的应用
CN112625036A (zh) * 2019-10-08 2021-04-09 上海海和药物研究开发股份有限公司 一类具有brd4抑制活性的化合物、其制备方法及用途
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
US11801243B2 (en) 2020-09-23 2023-10-31 Forma Therapeutics, Inc. Bromodomain inhibitors for androgen receptor-driven cancers
US11795168B2 (en) 2020-09-23 2023-10-24 Forma Therapeutics, Inc. Inhibiting cyclic amp-responsive element-binding protein (CREB) binding protein (CBP)
EP4074317A1 (en) 2021-04-14 2022-10-19 Bayer AG Phosphorus derivatives as novel sos1 inhibitors
WO2024211696A1 (en) * 2023-04-07 2024-10-10 Biogen Ma Inc. 1h-pyrrolo[2,3-b]pyridin-4-yl]-2-oxopyrrolidine-3-carbonitrile derivatives as tyrosine kinase 2 (tyk2) inhibitors for the treatment of inflammatory diseases

Family Cites Families (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3845770A (en) 1972-06-05 1974-11-05 Alza Corp Osmatic dispensing device for releasing beneficial agent
US4326525A (en) 1980-10-14 1982-04-27 Alza Corporation Osmotic device that improves delivery properties of agent in situ
US5364620A (en) 1983-12-22 1994-11-15 Elan Corporation, Plc Controlled absorption diltiazem formulation for once daily administration
US5023252A (en) 1985-12-04 1991-06-11 Conrex Pharmaceutical Corporation Transdermal and trans-membrane delivery of drugs
US4992445A (en) 1987-06-12 1991-02-12 American Cyanamid Co. Transdermal delivery of pharmaceuticals
US5001139A (en) 1987-06-12 1991-03-19 American Cyanamid Company Enchancers for the transdermal flux of nivadipine
US4902514A (en) 1988-07-21 1990-02-20 Alza Corporation Dosage form for administering nilvadipine for treating cardiovascular symptoms
US6162804A (en) 1997-09-26 2000-12-19 Merck & Co., Inc. Tyrosine kinase inhibitors
EP1620413A2 (en) 2003-04-30 2006-02-01 Cytokinetics, Inc. Compounds, compositions, and methods
GB0420719D0 (en) 2004-09-17 2004-10-20 Addex Pharmaceuticals Sa Novel allosteric modulators
US8486941B2 (en) 2007-03-12 2013-07-16 Ym Biosciences Australia Pty Ltd Phenyl amino pyrimidine compounds and uses thereof
US20090176778A1 (en) 2007-08-10 2009-07-09 Franz Ulrich Schmitz Certain nitrogen containing bicyclic chemical entities for treating viral infections
US20100204265A1 (en) 2009-02-09 2010-08-12 Genelabs Technologies, Inc. Certain Nitrogen Containing Bicyclic Chemical Entities for Treating Viral Infections
GB0919423D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
AR084070A1 (es) * 2010-12-02 2013-04-17 Constellation Pharmaceuticals Inc Inhibidores del bromodominio y usos de los mismos
EP2681200A4 (en) 2011-03-03 2015-05-27 Zalicus Pharmaceuticals Ltd INHIBITORS OF BENZIMIDAZOLE TYPE OF SODIUM CHANNEL
GB201106799D0 (en) * 2011-04-21 2011-06-01 Glaxosmithkline Llc Novel compounds
EP2765860B1 (en) * 2011-10-13 2016-08-17 Merck Sharp & Dohme Corp. Mineralocorticoid receptor antagonists
WO2013097052A1 (en) * 2011-12-30 2013-07-04 Abbott Laboratories Bromodomain inhibitors

Also Published As

Publication number Publication date
AU2014262622B2 (en) 2016-08-11
US9458145B2 (en) 2016-10-04
US20140336190A1 (en) 2014-11-13
EA029091B1 (ru) 2018-02-28
UY35559A (es) 2014-11-28
EP2994469A1 (en) 2016-03-16
MD20150121A2 (ro) 2016-05-31
SG11201509220XA (en) 2015-12-30
CN105324379B (zh) 2018-12-04
JP6049942B2 (ja) 2016-12-27
TW201506022A (zh) 2015-02-16
ES2710120T3 (es) 2019-04-23
PT2994469T (pt) 2019-03-18
CL2015003280A1 (es) 2016-06-24
CR20150639A (es) 2016-01-29
MD4592B1 (ro) 2018-09-30
EA201591965A1 (ru) 2016-08-31
CN105324379A (zh) 2016-02-10
AR096246A1 (es) 2015-12-16
KR101761049B1 (ko) 2017-07-24
US20160376261A1 (en) 2016-12-29
AP2015008869A0 (en) 2015-11-30
BR112015028017A2 (pt) 2017-07-25
KR20160008232A (ko) 2016-01-21
EP2994469B1 (en) 2018-12-19
US20180282316A1 (en) 2018-10-04
CA2911408C (en) 2017-10-24
NZ713718A (en) 2016-12-23
AU2014262622A1 (en) 2015-11-12
PE20160029A1 (es) 2016-02-14
PH12015502534A1 (en) 2016-02-22
US10017501B2 (en) 2018-07-10
US20160075695A1 (en) 2016-03-17
TWI527811B (zh) 2016-04-01
WO2014182929A1 (en) 2014-11-13
UA112618C2 (uk) 2016-09-26
MX2015015478A (es) 2016-06-14
HK1219278A1 (zh) 2017-03-31
CA2911408A1 (en) 2014-11-13
JP2016520062A (ja) 2016-07-11

Similar Documents

Publication Publication Date Title
HK1222646A1 (zh) 作為溴結構域抑制劑的苯並咪唑衍生物
HK1220692A1 (zh) 作為布羅莫結構域抑制劑的苯並咪唑酮衍生物
IL256946B (en) Bromodomain inhibitors
HK1224297A1 (zh) 布羅莫結構域抑制劑
IL241123A0 (en) Dihydro-pyrrolopyridinones as inhibitors of bromo sites
HK1213885A1 (zh) 作為 抑制劑的咪唑並-三嗪衍生物
EP2968324A4 (en) SUBSTITUTED PYRIDONE DERIVATIVES AS PDE10 INHIBITORS