JP5926793B2 - ブロモドメイン阻害剤としてのテトラヒドロキノリン誘導体 - Google Patents

ブロモドメイン阻害剤としてのテトラヒドロキノリン誘導体 Download PDF

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JP5926793B2
JP5926793B2 JP2014508771A JP2014508771A JP5926793B2 JP 5926793 B2 JP5926793 B2 JP 5926793B2 JP 2014508771 A JP2014508771 A JP 2014508771A JP 2014508771 A JP2014508771 A JP 2014508771A JP 5926793 B2 JP5926793 B2 JP 5926793B2
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compound
methyl
salt
mmol
amino
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JP2014513110A (ja
JP2014513110A5 (enExample
Inventor
アマン，ドミニク
ドゥモント，エマニュエル，ユベール
ジョーンズ，キャサリン，ルイーズ
シール，ジョナサン，トーマス
ウォーカー，アン，ルイーズ
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グラクソスミスクライン エルエルシー
グラクソスミスクライン エルエルシー
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    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4706—4-Aminoquinolines; 8-Aminoquinolines, e.g. chloroquine, primaquine
    • 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/10—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 two hetero rings linked by a carbon chain containing aromatic rings
    • 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

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2014508771A 2011-05-04 2012-05-02 ブロモドメイン阻害剤としてのテトラヒドロキノリン誘導体 Expired - Fee Related JP5926793B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB1107325.1 2011-05-04
GBGB1107325.1A GB201107325D0 (en) 2011-05-04 2011-05-04 Novel compounds
PCT/EP2012/057978 WO2012150234A1 (en) 2011-05-04 2012-05-02 Dihydroquinoline derivatives as bromodomain inhibitors

Publications (3)

Publication Number Publication Date
JP2014513110A JP2014513110A (ja) 2014-05-29
JP2014513110A5 JP2014513110A5 (enExample) 2015-05-28
JP5926793B2 true JP5926793B2 (ja) 2016-05-25

Family

ID=44203063

Family Applications (1)

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JP2014508771A Expired - Fee Related JP5926793B2 (ja) 2011-05-04 2012-05-02 ブロモドメイン阻害剤としてのテトラヒドロキノリン誘導体

Country Status (6)

Country Link
US (1) US9315487B2 (enExample)
EP (1) EP2705032B1 (enExample)
JP (1) JP5926793B2 (enExample)
ES (1) ES2589801T3 (enExample)
GB (1) GB201107325D0 (enExample)
WO (1) WO2012150234A1 (enExample)

Families Citing this family (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB201106743D0 (en) * 2011-04-21 2011-06-01 Glaxosmithkline Llc Novel compounds
CN105073744B (zh) 2012-12-21 2019-11-08 齐尼思表观遗传学有限公司 作为溴结构域抑制剂的新型杂环化合物
US9115054B2 (en) * 2013-02-21 2015-08-25 Bristol-Myers Squibb Company Tetrahydronaphthalenyl compounds useful as sipi agonists
CA2904049A1 (en) 2013-03-11 2014-10-09 Abbvie Inc. Fused tetracyclic bromodomain inhibitors
US9050346B2 (en) 2013-03-11 2015-06-09 Abbvie Inc. Bromodomain inhibitors
CA2901537C (en) 2013-03-14 2021-09-07 Glaxosmithkline Intellectual Property (No.2) Limited 2,3-disubstituted 1- acyl-4-amino-1 ,2,3,4-tetrahydroquinoline derivatives and their use as bromodomain inhibitors
BR112015022942B1 (pt) 2013-03-15 2022-02-22 Incyte Holdings Corporation Compostos heterocíciclos tricíclicos, método para inibir proteína bet in vitro e composição farmacêutica compreendendo os referidos compostos
EP2792355A1 (en) 2013-04-17 2014-10-22 Albert-Ludwigs-Universität Freiburg Compounds for use as bromodomain inhibitors
SG10201710705UA (en) 2013-06-21 2018-02-27 Zenith Epigenetics Ltd Novel bicyclic bromodomain inhibitors
WO2015004533A2 (en) 2013-06-21 2015-01-15 Zenith Epigenetics Corp. Novel substituted bicyclic compounds as bromodomain inhibitors
ES2635560T3 (es) 2013-07-08 2017-10-04 Incyte Holdings Corporation Heterociclos tricíclicos como inhibidores de la proteína NET
EP3027604B1 (en) 2013-07-31 2019-02-20 Zenith Epigenetics Ltd. Novel quinazolinones as bromodomain inhibitors
SMT202000273T1 (it) 2013-10-18 2020-07-08 Celgene Quanticel Research Inc Inibitori di bromodomini
WO2015074081A1 (en) 2013-11-18 2015-05-21 Bair Kenneth W Benzopiperazine compositions as bet bromodomain inhibitors
MX370535B (es) 2013-11-18 2019-12-17 Forma Therapeutics Inc Compuestos de tetrahidroquinolina como inhibidores del bromodominio extra terminal y bromo (bet) y el uso de los mismos en el tratamiento de cáncer.
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
US9315501B2 (en) 2013-11-26 2016-04-19 Incyte Corporation Bicyclic heterocycles as BET protein inhibitors
WO2015095492A1 (en) 2013-12-19 2015-06-25 Incyte Corporation Tricyclic heterocycles as bet protein inhibitors
DK3092227T3 (en) * 2014-01-09 2018-09-03 Orion Corp BICYCLIC HETEROCYCLIC DERIVATIVES AS BROOM DOMAIN INHIBITORS
NZ725930A (en) 2014-04-23 2023-04-28 Incyte Holdings Corp 1h-pyrrolo[2,3-c]pyridin-7(6h)-ones and pyrazolo[3,4-c]pyridin-7(6h)-ones as inhibitors of bet proteins
BR112017004580A2 (pt) 2014-09-12 2018-01-23 GlaxoSmithKline Intellectual Property composto, composição farmacêutica, produto de combinação, uso de um composto ou sal farmaceuticamente aceitável, e, método de tratamento.
ES2855225T3 (es) 2014-09-15 2021-09-23 Incyte Corp Heterociclos tricíclicos para su uso como inhibidores de proteínas BET
HK1246273B (en) 2014-12-01 2019-12-06 恒翼生物医药(上海)股份有限公司 Substituted pyridines as bromodomain inhibitors
JP2017537946A (ja) 2014-12-11 2017-12-21 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置換複素環
CA2966450A1 (en) 2014-12-17 2016-06-23 Olesya KHARENKO Inhibitors of bromodomains
GB201504694D0 (en) 2015-03-19 2015-05-06 Glaxosmithkline Ip Dev Ltd Covalent conjugates
WO2016203335A1 (en) 2015-06-18 2016-12-22 Pfizer Inc. Novel pyrido[2,3-b]pyrazinones as bet-family bromodomain inhibitors
AR106520A1 (es) 2015-10-29 2018-01-24 Incyte Corp Forma sólida amorfa de un inhibidor de proteína bet
EP3472157B1 (en) 2016-06-20 2023-04-12 Incyte Corporation Crystalline solid forms of a bet inhibitor
ES2937307T3 (es) 2016-07-26 2023-03-27 Univ Southern California Inhibición selectiva del bromodominio del BDF1 fúngico
WO2018111805A1 (en) 2016-12-13 2018-06-21 St. Jude Children's Research Hospital Tetrahydroquinoline-based bromodomain inhibitors
US11629152B2 (en) 2018-03-30 2023-04-18 Kyowa Kirin Co., Ltd. Compound with anticancer activity
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9004781D0 (en) 1990-03-02 1990-04-25 Glaxo Group Ltd Device
EP1435356A1 (en) * 2003-01-06 2004-07-07 Warner-Lambert Company LLC Quinoline derivatives as CRTH2 antagonists
PL1699512T3 (pl) 2003-11-03 2012-11-30 Glaxo Group Ltd Urządzenie do dozowania płynów
WO2006083692A2 (en) * 2005-01-28 2006-08-10 Mount Sinai Schoool Of Medicine Methods of identifying modulators of bromodomains
JP2008156311A (ja) 2006-12-26 2008-07-10 Institute Of Physical & Chemical Research Ｂｒｄ２ブロモドメイン結合剤
CN101910182B (zh) 2007-12-28 2013-07-17 田边三菱制药株式会社 抗癌剂
GB0919431D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB0919434D0 (en) * 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB201106743D0 (en) 2011-04-21 2011-06-01 Glaxosmithkline Llc Novel compounds
GB201106750D0 (en) 2011-04-21 2011-06-01 Glaxosmithkline Llc Novel compounds

Also Published As

Publication number Publication date
EP2705032A1 (en) 2014-03-12
EP2705032B1 (en) 2016-06-15
GB201107325D0 (en) 2011-06-15
JP2014513110A (ja) 2014-05-29
US20140066459A1 (en) 2014-03-06
ES2589801T3 (es) 2016-11-16
WO2012150234A1 (en) 2012-11-08
US9315487B2 (en) 2016-04-19

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