CR20150639A - Derivados de benzimidazol como inhbidores de bromodominio - Google Patents

Derivados de benzimidazol como inhbidores de bromodominio

Info

Publication number
CR20150639A
CR20150639A CR20150639A CR20150639A CR20150639A CR 20150639 A CR20150639 A CR 20150639A CR 20150639 A CR20150639 A CR 20150639A CR 20150639 A CR20150639 A CR 20150639A CR 20150639 A CR20150639 A CR 20150639A
Authority
CR
Costa Rica
Prior art keywords
inhabitors
bromodominum
benzimidazol derivatives
compounds
bromodomain
Prior art date
Application number
CR20150639A
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 CR20150639A publication Critical patent/CR20150639A/es

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)

Abstract

Esta solicitud se relaciona con compuestos químicos que pueden actuar como in-hibidores, o modular de alguna otra forma, la actividad de una proteína que con-tiene bromodominio, incluyendo la proteína 4 que contiene bromodominio (BRD4) y con composiciones y formulaciones que contienen dichos compuestos, así como métodos para usar y realizar dichos compuestos.
CR20150639A 2013-05-09 2015-12-04 Derivados de benzimidazol como inhbidores de bromodominio CR20150639A (es)

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
CR20150639A true CR20150639A (es) 2016-01-29

Family

ID=50897952

Family Applications (1)

Application Number Title Priority Date Filing Date
CR20150639A CR20150639A (es) 2013-05-09 2015-12-04 Derivados de benzimidazol como inhbidores de bromodominio

Country Status (26)

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

Families Citing this family (62)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9765039B2 (en) 2012-11-21 2017-09-19 Zenith Epigenetics Ltd. Biaryl derivatives as bromodomain inhibitors
WO2014080290A2 (en) 2012-11-21 2014-05-30 Rvx Therapeutics Inc. Cyclic amines as bromodomain inhibitors
KR20150096794A (ko) 2012-12-21 2015-08-25 제니쓰 에피제네틱스 코포레이션 브로모도메인 저해제로서의 신규한 헤테로사이클릭 화합물
EP2970282B1 (en) 2013-03-15 2019-08-21 Incyte Holdings Corporation Tricyclic heterocycles as bet protein inhibitors
CN109939113B (zh) 2013-06-21 2022-02-15 恒翼生物医药科技(上海)有限公司 双环溴结构域抑制剂
US9636328B2 (en) * 2013-06-21 2017-05-02 Zenith Epigenetics Ltd. Substituted bicyclic compounds as bromodomain inhibitors
EP3019502B1 (en) 2013-07-08 2017-05-17 Incyte Holdings Corporation Tricyclic heterocycles as bet protein inhibitors
CA2919948C (en) 2013-07-31 2020-07-21 Zenith Epigenetics Corp. Novel quinazolinones as bromodomain inhibitors
WO2015081189A1 (en) 2013-11-26 2015-06-04 Incyte Corporation Bicyclic heterocycles as bet protein inhibitors
US9399640B2 (en) 2013-11-26 2016-07-26 Incyte Corporation Substituted pyrrolo[2,3-c]pyridines and pyrazolo[3,4-c]pyridines as BET protein inhibitors
US9309246B2 (en) 2013-12-19 2016-04-12 Incyte Corporation Tricyclic heterocycles as BET protein inhibitors
MY180775A (en) 2014-04-23 2020-12-09 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
JP6599979B2 (ja) * 2014-09-15 2019-10-30 インサイト・コーポレイション Betタンパク質阻害剤として用いるための三環式複素環化合物
WO2016087936A1 (en) 2014-12-01 2016-06-09 Zenith Epigenetics Corp. Substituted pyridinones as bromodomain inhibitors
EP3227280B1 (en) 2014-12-01 2019-04-24 Zenith Epigenetics Ltd. Substituted pyridines as bromodomain inhibitors
CA2966449A1 (en) 2014-12-11 2016-06-16 Zenith Epigenetics Ltd. Substituted heterocycles as bromodomain inhibitors
EP3233846A4 (en) * 2014-12-17 2018-07-18 Zenith Epigenetics Ltd. Inhibitors of bromodomains
CA2966452A1 (en) * 2014-12-17 2016-06-23 Samuel David Brown 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
CA2985642A1 (en) * 2015-05-15 2016-11-24 Gilead Sciences, Inc. Benzimidazole and imadazopyridine carboximidamide compounds having activity as inhibitors of indoleamine 2,3-dioxygenase
WO2016187620A2 (en) 2015-05-21 2016-11-24 The Regents Of The University Of California Anti-cancer compounds
NZ741112A (en) * 2015-09-21 2021-07-30 Plexxikon Inc Heterocyclic compounds and uses thereof
TW201722966A (zh) 2015-10-29 2017-07-01 英塞特公司 Bet蛋白質抑制劑之非晶固體形式
CN105399683B (zh) * 2015-12-01 2018-07-20 江苏理工学院 苯并咪唑衍生物及其制备方法
WO2017106568A1 (en) 2015-12-17 2017-06-22 Gilead Sciences, Inc. Combination of a jak inhibitor and a bromodomain inhibitor for treating cancer
AU2016370916A1 (en) 2015-12-17 2018-06-07 Gilead Sciences, Inc. Tank-binding kinase inhibitor compounds
SG11201805385QA (en) * 2015-12-24 2018-07-30 Celgene Quanticel Research Inc Bromodomain and extra-terminal protein inhibitor combination therapy
EP4234554A3 (en) 2016-06-20 2023-12-27 Incyte Corporation Crystalline solid forms of a bet inhibitor
EP3475272B1 (en) 2016-06-24 2023-09-13 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
GB201617627D0 (en) 2016-10-18 2016-11-30 Cellcentric Ltd Pharmaceutical compounds
GB201617630D0 (en) * 2016-10-18 2016-11-30 Cellcentric Ltd Pharmaceutical compounds
PL3532059T3 (pl) * 2016-10-27 2022-05-09 Celgene Quanticel Research, Inc. Terapia skojarzona z zastosowaniem inhibitora białka bet
WO2018085069A1 (en) 2016-11-03 2018-05-11 Gilead Sciences, Inc. Combination of a bcl-2 inhibitor and a bromodomain inhibitor for treating cancer
WO2018097977A1 (en) 2016-11-22 2018-05-31 Gilead Sciences, Inc. Crystalline forms of a phosphate complex 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
WO2018106433A1 (en) * 2016-12-06 2018-06-14 Gilead Sciences, Inc. Treatment of prostate cancer by concomitant administration of a bromodomain inhibitor and a second agent
WO2018106444A1 (en) * 2016-12-06 2018-06-14 Gilead Sciences, Inc. Treatment of breast cancer by concomitant administration of a bromodomain inhibitor and a second agent
CN116869457A (zh) * 2016-12-14 2023-10-13 比奥拉治疗股份有限公司 使用jak抑制剂治疗胃肠道疾病及装置
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
WO2018213719A1 (en) * 2017-05-19 2018-11-22 Epicypher, Inc. Assays for nucleosome remodeling activity
EP3681885B1 (en) 2017-09-15 2024-02-28 Forma Therapeutics, Inc. Tetrahydro-imidazo quinoline compositions as cbp/p300 inhibitors
JP2021506903A (ja) 2017-12-20 2021-02-22 貝達薬業股▲ふん▼有限公司Betta Pharmaceuticals Co.,Ltd ブロモドメインタンパク質阻害剤である化合物、および組成物
CR20200347A (es) 2018-02-13 2020-09-23 Gilead Sciences Inc Inhibidores pd-1/pd-l1
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
CA3099451A1 (en) * 2018-05-08 2019-11-14 Baylis Medical Company Inc. Methods and devices for puncturing tissue
CN112118845B (zh) 2018-05-14 2023-06-13 吉利德科学公司 Mcl-1抑制剂
MX2023013508A (es) 2018-06-29 2023-12-13 Forma Therapeutics Inc Inhibicion de la proteina de union a creb (cbp).
KR20230159715A (ko) 2018-07-13 2023-11-21 길리애드 사이언시즈, 인코포레이티드 Pd-1/pd-l1 억제제
AU2019366355B2 (en) 2018-10-24 2022-10-13 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
CN113544129A (zh) * 2019-04-04 2021-10-22 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
US11795168B2 (en) 2020-09-23 2023-10-24 Forma Therapeutics, Inc. Inhibiting cyclic amp-responsive element-binding protein (CREB) binding protein (CBP)
US11801243B2 (en) 2020-09-23 2023-10-31 Forma Therapeutics, Inc. Bromodomain inhibitors for androgen receptor-driven cancers
EP4074317A1 (en) 2021-04-14 2022-10-19 Bayer AG Phosphorus derivatives as novel sos1 inhibitors

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
US5001139A (en) 1987-06-12 1991-03-19 American Cyanamid Company Enchancers for the transdermal flux of nivadipine
US4992445A (en) 1987-06-12 1991-02-12 American Cyanamid Co. Transdermal delivery of pharmaceuticals
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
CN104030990B (zh) 2007-03-12 2017-01-04 Ym生物科学澳大利亚私人有限公司 苯基氨基嘧啶化合物及其用途
JP2010535773A (ja) 2007-08-10 2010-11-25 グラクソスミスクライン エルエルシー ウイルス感染を治療するための窒素含有二環式化学物質
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
WO2012116440A1 (en) 2011-03-03 2012-09-07 Zalicus Pharmaceuticals Ltd. Benzimidazole inhibitors of the 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
NZ713718A (en) 2016-12-23
HK1222646A1 (zh) 2017-07-07
US20160376261A1 (en) 2016-12-29
CN105324379B (zh) 2018-12-04
JP6049942B2 (ja) 2016-12-27
PT2994469T (pt) 2019-03-18
EP2994469A1 (en) 2016-03-16
AU2014262622A1 (en) 2015-11-12
US20160075695A1 (en) 2016-03-17
MX2015015478A (es) 2016-06-14
PH12015502534A1 (en) 2016-02-22
MD20150121A2 (ro) 2016-05-31
KR20160008232A (ko) 2016-01-21
CA2911408A1 (en) 2014-11-13
CA2911408C (en) 2017-10-24
US20180282316A1 (en) 2018-10-04
EA029091B1 (ru) 2018-02-28
US20140336190A1 (en) 2014-11-13
PE20160029A1 (es) 2016-02-14
UA112618C2 (uk) 2016-09-26
CN105324379A (zh) 2016-02-10
ES2710120T3 (es) 2019-04-23
EA201591965A1 (ru) 2016-08-31
BR112015028017A2 (pt) 2017-07-25
WO2014182929A1 (en) 2014-11-13
AP2015008869A0 (en) 2015-11-30
CL2015003280A1 (es) 2016-06-24
MD4592B1 (ro) 2018-09-30
AU2014262622B2 (en) 2016-08-11
US10017501B2 (en) 2018-07-10
TW201506022A (zh) 2015-02-16
JP2016520062A (ja) 2016-07-11
SG11201509220XA (en) 2015-12-30
HK1219278A1 (zh) 2017-03-31
TWI527811B (zh) 2016-04-01
AR096246A1 (es) 2015-12-16
KR101761049B1 (ko) 2017-07-24
EP2994469B1 (en) 2018-12-19
UY35559A (es) 2014-11-28
US9458145B2 (en) 2016-10-04

Similar Documents

Publication Publication Date Title
CR20150639A (es) Derivados de benzimidazol como inhbidores de bromodominio
CR20150515A (es) Derivados de bencimidazolona como inhibidores del bromodominio
CL2016000508A1 (es) Compuestos derivados de (2-metil-3-fenilfenil)metoxi sustituidos, inhibidores de la interacción pd-1/proteína pd-l1/proteína; composición farmacéutica que los comprende; y su uso para tratar una enfermedad infecciosa o cáncer.
CO2017001994A2 (es) Compuestos activos hacia bromodominios
CL2018002334A1 (es) Moduladores de complementos factor b (divisional solicitud 201600606)
CL2016001604A1 (es) “compuestos derivados de pirazolo[1,5-a]piridina, inhibidores de quinasas axl y c-met; composición farmacéutica que los comprende; y su uso en el tratamiento del cáncer”. pct
CL2015002658A1 (es) Derivados de 2, 3 - disustituto 1- acil -4 amino - 1,2,3,4 tetrahidroquinilina y su uso como inhibidores de bromodominio
CR20150066A (es) 2,3-benzodiacepinas
CO2018000631A2 (es) Compuestos bicíclicos como inhibidores de atx
CL2016000241A1 (es) Formulación de inhibidores de la syk.
CO6761389A2 (es) Inhibidores de nampt y rock
EA201391285A1 (ru) Производные тетрагидрохинолина, полезные в качестве ингибиторов бромодомена
CR20180057A (es) Nuevos compuestos biciclicos como inhibidores duales de atx/ca.
BR112015023417A2 (pt) compostos heterocíclicos e seus usos
UY33917A (es) ?composiciones para recubrimiento que comprenden submicropartículas que comprenden carbonato de calcio, proceso para prepararlas, y uso de las submicropartículas?.
EA201591591A1 (ru) Соединения карбазола, применяемые в качестве ингибиторов бромодомена
PE20151894A1 (es) Composiciones y metodos de variantes de inhibidor tisular de la metaloproteinasa tipo tres (timp 3)
CO7461129A2 (es) Beta-glucosidasa de magnaporthe grisea
UY34636A (es) Composiciones tópicas que comprenden fipronilo y permetrina y sus métodos de uso
BR112015017241A8 (pt) composto, composição farmacêutica, uso do composto e da composição farmacêutica e kit
CL2015002060A1 (es) Compuestos.
DOP2016000007A (es) Pirazolpiridinas sustituidas
UY34842A (es) Formulaciones estabilizadas que contienen anticuerpos anti-dll4
CL2017000587A1 (es) Derivados de tetrahidroquinolina como inhibidores de bromodominio
ECSP16058769A (es) Composicion para la administracion oral de agente bioactivos