CA2982588A1 - Bromodomain inhibitors - Google Patents

Bromodomain inhibitors Download PDF

Info

Publication number
CA2982588A1
CA2982588A1 CA2982588A CA2982588A CA2982588A1 CA 2982588 A1 CA2982588 A1 CA 2982588A1 CA 2982588 A CA2982588 A CA 2982588A CA 2982588 A CA2982588 A CA 2982588A CA 2982588 A1 CA2982588 A1 CA 2982588A1
Authority
CA
Canada
Prior art keywords
alkyl
compound
hydrogen
pharmaceutically acceptable
acceptable salt
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.)
Pending
Application number
CA2982588A
Other languages
English (en)
French (fr)
Inventor
Michael John Bennett
Juan Manuel Betancort
Amogh Boloor
Stephen W. Kaldor
Jeffrey Alan Stafford
James Marvin Veal
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.)
Celgene Quanticel Research Inc
Original Assignee
Celgene Quanticel Research 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 Celgene Quanticel Research Inc filed Critical Celgene Quanticel Research Inc
Publication of CA2982588A1 publication Critical patent/CA2982588A1/en
Pending legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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 two hetero rings
    • C07D401/04Heterocyclic 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 two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D473/00Heterocyclic compounds containing purine ring systems
    • C07D473/26Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/32Nitrogen atom
    • C07D473/34Nitrogen atom attached in position 6, e.g. adenine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/425Thiazoles
    • A61K31/428Thiazoles condensed with carbocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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
    • A61K31/437Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/472Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • 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
    • C07D417/02Heterocyclic 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 two hetero rings
    • C07D417/04Heterocyclic 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 two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • 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
    • C07D471/06Peri-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
CA2982588A 2015-04-15 2016-04-15 Bromodomain inhibitors Pending CA2982588A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201562148098P 2015-04-15 2015-04-15
US62/148,098 2015-04-15
PCT/US2016/027874 WO2016168682A2 (en) 2015-04-15 2016-04-15 Bromodomain inhibitor

Publications (1)

Publication Number Publication Date
CA2982588A1 true CA2982588A1 (en) 2016-10-20

Family

ID=57126317

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2982588A Pending CA2982588A1 (en) 2015-04-15 2016-04-15 Bromodomain inhibitors

Country Status (21)

Country Link
US (3) US9908885B2 (enExample)
EP (2) EP3831383A1 (enExample)
JP (1) JP6856543B2 (enExample)
KR (1) KR20170135938A (enExample)
CN (1) CN107635558A (enExample)
AR (1) AR104259A1 (enExample)
AU (1) AU2016249273B2 (enExample)
CA (1) CA2982588A1 (enExample)
CL (1) CL2017002606A1 (enExample)
CO (1) CO2017011484A2 (enExample)
EA (1) EA201792229A1 (enExample)
EC (1) ECSP17070706A (enExample)
ES (1) ES2868355T3 (enExample)
HK (1) HK1243326A1 (enExample)
IL (1) IL255006A0 (enExample)
MX (1) MX2017013207A (enExample)
PE (1) PE20180258A1 (enExample)
PH (1) PH12017501888A1 (enExample)
SG (1) SG11201708470SA (enExample)
TW (1) TW201643153A (enExample)
WO (1) WO2016168682A2 (enExample)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11981657B2 (en) 2015-08-12 2024-05-14 Epigenetix, Inc. Substituted benzimidazoles, their preparation and their use as pharmaceuticals

Families Citing this family (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR104259A1 (es) * 2015-04-15 2017-07-05 Celgene Quanticel Res Inc Inhibidores de bromodominio
EP3334717B1 (en) 2015-08-11 2020-07-01 Neomed Institute Aryl-substituted dihydroquinolinones, their preparation and their use as pharmaceuticals
WO2017024406A1 (en) 2015-08-11 2017-02-16 Neomed Institute N-substituted bicyclic lactams, their preparation and their use as pharmaceuticals
WO2017066876A1 (en) 2015-10-21 2017-04-27 Neomed Institute Substituted imidazopyridines, their preparation and their use as pharmaceuticals
WO2017127930A1 (en) 2016-01-28 2017-08-03 Neomed Institute Substituted [1,2,4]triazolo[4,3-a]pyridines, their preparation and their use as pharmaceuticals
US10150754B2 (en) 2016-04-19 2018-12-11 Celgene Quanticel Research, Inc. Histone demethylase inhibitors
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
WO2018195155A1 (en) 2017-04-18 2018-10-25 Celgene Quanticel Research, Inc. Therapeutic compounds
CN107098844B (zh) * 2017-05-17 2019-07-30 许昌学院 一种c-5位硝基取代的酰基吲哚啉类化合物的合成方法
KR20200101434A (ko) * 2017-12-20 2020-08-27 베타 파머수티컬 컴퍼니 리미티드 브로모도메인 단백질 억제제로서 작동하는 화합물 및 조성물
EP3746135A4 (en) 2018-01-30 2022-03-09 Foghorn Therapeutics Inc. METHODS AND COMPOUNDS FOR TREATMENT OF DISEASE
CN108516973A (zh) * 2018-03-30 2018-09-11 广西师范大学 3-苯并噻唑-1-(3-二甲氨基)丙基喹啉-4-酮衍生物及其制备方法和应用
EA202190170A1 (ru) * 2018-07-23 2021-08-13 Селджен Квонтисел Рисёрч, Инк. Способ получения ингибитора бромодомена
PT3860998T (pt) 2018-10-05 2024-04-02 Annapurna Bio Inc Compostos e composições para o tratamento de condições associadas à atividade do recetor apj
AU2019372121A1 (en) 2018-10-30 2021-05-27 Nuvation Bio Inc. Heterocyclic compounds as BET inhibitors
WO2020160198A1 (en) 2019-01-29 2020-08-06 Foghorn Therapeutics Inc. Compounds and uses thereof
WO2020160196A1 (en) * 2019-01-29 2020-08-06 Foghorn Therapeutics Inc. Compounds and uses thereof
CN113874016A (zh) 2019-01-29 2021-12-31 福宏治疗公司 化合物及其用途
US20230065463A1 (en) * 2019-01-29 2023-03-02 Foghorn Therapeutics Inc. Compounds and uses thereof
JP2022053557A (ja) * 2019-02-08 2022-04-06 マルホ株式会社 ピリドン誘導体
EP3958867B1 (en) * 2019-04-24 2024-06-26 Convergene Llc Small molecule bromodomain inhibitors and uses thereof
AU2020299592A1 (en) 2019-07-02 2022-02-17 Nuvation Bio Inc. Heterocyclic compounds as BET inhibitors
CN112174945B (zh) * 2019-07-02 2022-06-07 四川大学 具有抗癌作用的吲唑类化合物及其制备方法和用途
WO2021022163A2 (en) * 2019-07-31 2021-02-04 Foghorn Therapeutics Inc. Compounds and uses thereof
US12528825B2 (en) 2020-01-29 2026-01-20 Foghorn Therapeutics Inc. Compounds and uses thereof
KR20220133259A (ko) 2020-01-29 2022-10-04 포그혼 쎄라퓨틱스 인크. 화합물 및 이의 용도
JP2023536139A (ja) * 2020-07-29 2023-08-23 フォグホーン セラピューティクス インコーポレイテッド 化合物及びその使用
US11787800B2 (en) 2020-07-29 2023-10-17 Foghorn Therapeutics Inc. BRD9 degraders and uses thereof
US12527741B2 (en) 2021-06-17 2026-01-20 Wisconsin Alumni Research Foundation Modular dendron micelles for treatment of pulmonary diseases related to fibrosis and viral infection including COVID-19
WO2023283263A1 (en) 2021-07-06 2023-01-12 Foghorn Therapeutics Inc. Citrate salt, pharmaceutical compositions, and methods of making and using the same
CN114014842B (zh) * 2021-11-04 2024-03-01 中国药科大学 一种杂环酮类化合物与其组合物及其制备方法和应用
WO2023090859A1 (ko) * 2021-11-17 2023-05-25 일동제약(주) 아이속사졸 유도체의 제조 방법 및 그의 신규한 중간체
GB202213163D0 (en) 2022-09-08 2022-10-26 Cambridge Entpr Ltd Novel compounds, compositions and therapeutic uses thereof

Family Cites Families (68)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US1349418A (en) * 1919-08-05 1920-08-10 George F Flynn Motor-support
US3590036A (en) * 1968-11-18 1971-06-29 George Y Lesher Naphthyridine-3-carboxylic acids,their derivatives and preparation thereof
DE2011970A1 (en) 1970-03-13 1971-11-18 CH. Boehringer Sohn, 6507 Ingelheim Imidazo-(1, 2-a)- pyrimidines prepn
US3635667A (en) 1970-07-23 1972-01-18 Fmc Corp Drycleaning with hydrogen peroxide
GB1322318A (en) * 1971-05-19 1973-07-04 Sterling Drug Inc 1-alkyl-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acids and esters
BE786028A (fr) 1971-07-08 1973-01-08 Boehringer Sohn Ingelheim 2,3-dihydro-oxo-imidazo(1,2-a)-pyrimidines, leurs sels d'addition avec des acides et procedes pour les fabriquer
DE2356005A1 (de) 1973-11-09 1975-05-22 Boehringer Sohn Ingelheim Neue 7-amino-imidazo eckige klammer auf 1,2-a eckige klammer zu pyrimidine, diese enthaltende arzneimittel sowie verfahren zu deren herstellung
AU577105B2 (en) 1985-04-02 1988-09-15 T.P.O. :Pharmachim: Acylaminic penicillin derivatives
US6117940A (en) 1997-10-17 2000-09-12 Mjalli; Adnan M. M. Amino-ketone solid support templates
PT1300396E (pt) * 2000-06-12 2009-04-20 Eisai R&D Man Co Ltd Compostos de 1,2-di-hidropiridina, processos para a sua preparação e sua utilização
GB0129260D0 (en) * 2001-12-06 2002-01-23 Eisai London Res Lab Ltd Pharmaceutical compositions and their uses
BR0314759A (pt) 2002-09-26 2005-07-26 Pfizer Derivados de pirazol
JP2005089352A (ja) 2003-09-16 2005-04-07 Kissei Pharmaceut Co Ltd 新規なイミダゾ[1,5−a]ピラジン誘導体、それを含有する医薬組成物およびそれらの用途
JP4718467B2 (ja) 2003-09-23 2011-07-06 メルク・シャープ・エンド・ドーム・コーポレイション イソキノリノンカリウムチャネル阻害剤
US7763614B2 (en) * 2003-09-23 2010-07-27 Merck Sharp & Dohme Corp. Isoquinoline potassium channel inhibitors
KR100703068B1 (ko) 2003-12-30 2007-04-05 에스케이케미칼주식회사 피리딘 유도체와 이의 제조방법, 및 이를 포함하는약제조성물
TW200536830A (en) * 2004-02-06 2005-11-16 Chugai Pharmaceutical Co Ltd 1-(2H)-isoquinolone derivative
KR20070008674A (ko) 2004-04-01 2007-01-17 아스테라스 세이야쿠 가부시키가이샤 피라진 유도체, 및 아데노신 길항제로서의 이의 약학적용도
GB0420722D0 (en) 2004-09-17 2004-10-20 Addex Pharmaceuticals Sa Novel allosteric modulators
KR100781704B1 (ko) 2005-04-20 2007-12-03 에스케이케미칼주식회사 피리딘 유도체와 이의 제조방법, 및 이를 포함하는약제조성물
US7452892B2 (en) 2005-06-17 2008-11-18 Bristol-Myers Squibb Company Triazolopyrimidine cannabinoid receptor 1 antagonists
SI1912949T1 (sl) 2005-07-26 2011-12-30 Sanofi Sa Cikloheksilamin izokinolonski derivati kot inhibitorji Rho-kinaze
PT1910333E (pt) 2005-07-26 2013-08-01 Sanofi Sa Derivados de isoquinolona substituída com piperidinilo como inibidores da rho-cinase
US20070099911A1 (en) 2005-10-28 2007-05-03 Wyeth Pyrroloquinolinone derivatives as 5-hydroxytryptamine-6 ligands
JP2009531314A (ja) 2006-03-10 2009-09-03 ニューロジェン・コーポレーション ピペラジニルオキソアルキルテトラヒドロイソキノリン類および関連類似物
GB0612428D0 (en) * 2006-06-22 2006-08-02 Prolysis Ltd Antibacterial agents
RU2457203C2 (ru) 2006-12-27 2012-07-27 Санофи-Авентис Замещенные циклоалкиламином производные изохинолона
PT2102164E (pt) 2006-12-27 2011-01-21 Sanofi Aventis Derivados de isoquinolina e de isoquinolinona substituída com cicloalquilamina
JP5421783B2 (ja) 2006-12-27 2014-02-19 サノフイ Rhoキナーゼ阻害剤としての置換イソキノロン及びイソキノリノン誘導体
WO2009029214A1 (en) * 2007-08-23 2009-03-05 Amgen Inc. Isoquinolone derivatives as phosphodiesterase 10 inhibitors
EP2250176B1 (en) 2008-01-30 2012-08-01 Cephalon, Inc. Substituted spirocyclic piperidine derivatives as histamine-3 (h3) receptor ligands
ES2389478T3 (es) 2008-06-25 2012-10-26 Bristol-Myers Squibb Company Derivados de dicetopiperidina como inhibidores de la fijación del VIH
WO2010039186A2 (en) * 2008-09-23 2010-04-08 Renovis, Inc. Compounds useful as faah modulators and uses thereof
EP2196465A1 (en) 2008-12-15 2010-06-16 Almirall, S.A. (3-oxo)pyridazin-4-ylurea derivatives as PDE4 inhibitors
EP2379564A1 (en) * 2008-12-19 2011-10-26 Schering Corporation Bicyclic heterocyclic derivatives and methods of use thereof
AU2010303567B2 (en) 2009-10-06 2016-06-09 Millennium Pharmaceuticals, Inc Heterocyclic compounds useful as PDK1 inhibitors
CA2784710A1 (en) * 2009-12-15 2011-06-23 Shionogi & Co., Ltd. Oxadiazole derivative having endothelial lipase inhibitory activity
CN102958930B (zh) 2010-06-28 2018-04-27 默克专利有限公司 作为用于对抗癌症的激酶抑制剂的2,4-二芳基取代的[1,8]二氮杂萘化合物
JPWO2012086735A1 (ja) * 2010-12-22 2014-06-05 大正製薬株式会社 縮合複素環化合物
AU2012258977A1 (en) 2011-05-23 2014-01-16 Imago Pharmaceuticals, Inc. Inhibitors of LRRK2 kinase activity
RU2477723C2 (ru) * 2011-06-16 2013-03-20 Общество С Ограниченной Ответственностью "Фьюжн Фарма" Ингибиторы протеинкиназ (варианты), их применение для лечения онкологических заболеваний и фармацевтическая композиция на их основе
CN102827073A (zh) 2011-06-17 2012-12-19 安吉奥斯医药品有限公司 治疗活性组合物和它们的使用方法
JP6014155B2 (ja) 2011-10-31 2016-10-25 ゼノン・ファーマシューティカルズ・インコーポレイテッドXenon Pharmaceuticals Inc. ビアリールエーテルスルホンアミドおよび治療剤としてのそれらの使用
CN103183675A (zh) 2011-12-27 2013-07-03 山东轩竹医药科技有限公司 磷酸二酯酶-4抑制剂
US9434743B2 (en) * 2012-03-02 2016-09-06 Takeda Pharmaceutical Company Limited Indazole derivatives
CA2874303C (en) 2012-06-11 2020-10-13 Ucb Biopharma Sprl Tnf -alpha modulating benz imidazoles
JP2014024838A (ja) * 2012-06-21 2014-02-06 Taisho Pharmaceutical Co Ltd 縮合複素環化合物を有効成分として含有する血糖低下作用薬
WO2014015088A1 (en) * 2012-07-19 2014-01-23 Bristol-Myers Squibb Company Amide, urea or sulfone amide linked benzothiazole inhibitors of endothelial lipase
WO2014080291A2 (en) * 2012-11-21 2014-05-30 Rvx Therapeutics Inc. Biaryl derivatives as bromodomain inhibitors
WO2014109414A1 (ja) * 2013-01-11 2014-07-17 富士フイルム株式会社 含窒素複素環化合物またはその塩
JP6401773B2 (ja) * 2013-03-11 2018-10-10 ザ リージェンツ オブ ザ ユニヴァシティ オブ ミシガン Betブロモドメイン阻害剤およびこれを用いる治療方法
HRP20181392T1 (hr) * 2013-03-15 2018-10-19 Plexxikon Inc. Heterociklični spojevi i njihova uporaba
CA2913697A1 (en) * 2013-05-27 2014-12-04 Novartis Ag Imidazopyrrolidinone derivatives and their use in the treatment of disease
WO2015004533A2 (en) * 2013-06-21 2015-01-15 Zenith Epigenetics Corp. Novel substituted bicyclic compounds as bromodomain inhibitors
WO2014205594A1 (en) * 2013-06-24 2014-12-31 Merck Sharp & Dohme Corp. Substituted benzofuran compounds and methods of use thereof for treatment of viral diseases
EP3483167A1 (en) * 2013-06-26 2019-05-15 AbbVie Inc. Primary carboxamides as btk inhibitors
DK3290407T3 (da) * 2013-10-18 2020-03-23 Celgene Quanticel Res Inc Bromodomæneinhibitorer
WO2015081189A1 (en) * 2013-11-26 2015-06-04 Incyte Corporation Bicyclic heterocycles as bet protein inhibitors
WO2015086519A1 (en) 2013-12-09 2015-06-18 Ucb Biopharma Sprl Imidazopyridine derivatives as modulators of tnf activity
US10173991B2 (en) * 2014-01-07 2019-01-08 Bristol-Myers Squibb Company Sulfone amide linked benzothiazole inhibitors of endothelial lipase
CA2936551A1 (en) 2014-01-24 2015-07-30 Confluence Life Sciences, Inc. Substituted pyrrolopyridines and pyrrolopyrazines for treating cancer or inflammatory diseases
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
MA40940A (fr) * 2014-11-10 2017-09-19 Constellation Pharmaceuticals Inc Pyrrolopyridines substituées utilisées en tant qu'inhibiteurs de bromodomaines
MA40943A (fr) * 2014-11-10 2017-09-19 Constellation Pharmaceuticals Inc Pyrrolopyridines substituées utilisées en tant qu'inhibiteurs de bromodomaines
WO2016086200A1 (en) * 2014-11-27 2016-06-02 Genentech, Inc. 4,5,6,7-tetrahydro-1 h-pyrazolo[4,3-c]pyridin-3-amine compounds as cbp and/or ep300 inhibitors
US11319318B2 (en) * 2015-03-05 2022-05-03 Boehringer Ingelheim International Gmbh Pyridinones and isoquinolinones as inhibitors of the bromodomain BRD9
AR104259A1 (es) * 2015-04-15 2017-07-05 Celgene Quanticel Res Inc Inhibidores de bromodominio
TW201642860A (zh) * 2015-04-22 2016-12-16 塞爾基因定量細胞研究公司 布羅莫結構域抑制劑

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11981657B2 (en) 2015-08-12 2024-05-14 Epigenetix, Inc. Substituted benzimidazoles, their preparation and their use as pharmaceuticals

Also Published As

Publication number Publication date
EP3831383A1 (en) 2021-06-09
TW201643153A (zh) 2016-12-16
EP3283077A4 (en) 2019-01-23
CO2017011484A2 (es) 2018-01-31
EP3283077B1 (en) 2021-03-10
ES2868355T3 (es) 2021-10-21
AU2016249273A1 (en) 2017-11-09
WO2016168682A3 (en) 2016-12-08
US20200071332A1 (en) 2020-03-05
CL2017002606A1 (es) 2018-05-18
US10494371B2 (en) 2019-12-03
CN107635558A (zh) 2018-01-26
HK1243326A1 (zh) 2018-07-13
PE20180258A1 (es) 2018-02-05
SG11201708470SA (en) 2017-11-29
US10807982B2 (en) 2020-10-20
JP2018511626A (ja) 2018-04-26
MX2017013207A (es) 2018-02-19
EA201792229A1 (ru) 2018-05-31
IL255006A0 (en) 2017-12-31
AR104259A1 (es) 2017-07-05
PH12017501888A1 (en) 2018-03-05
ECSP17070706A (es) 2017-12-01
KR20170135938A (ko) 2017-12-08
WO2016168682A2 (en) 2016-10-20
AU2016249273B2 (en) 2020-07-09
US20180134710A1 (en) 2018-05-17
JP6856543B2 (ja) 2021-04-07
US9908885B2 (en) 2018-03-06
EP3283077A2 (en) 2018-02-21
US20170050968A1 (en) 2017-02-23

Similar Documents

Publication Publication Date Title
US10807982B2 (en) Bromodomain inhibitors
US11884680B2 (en) Bromodomain inhibitors
JP6768857B2 (ja) リジン特異的なデメチラーゼ−1の阻害剤
CA2915561A1 (en) Novel substituted bicyclic compounds as bromodomain inhibitors
HK40080347A (en) Bromodomain inhibitors
HK40017640A (en) Bromodomain inhibitors
HK1226316B (en) Bromodomain inhibitors
HK1226316A1 (en) Bromodomain inhibitors

Legal Events

Date Code Title Description
EEER Examination request

Effective date: 20210331