ES2589801T3 - Derivados de dihidroquinolina como inhibidores de bromodominio - Google Patents

Derivados de dihidroquinolina como inhibidores de bromodominio Download PDF

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Publication number
ES2589801T3
ES2589801T3 ES12718651.8T ES12718651T ES2589801T3 ES 2589801 T3 ES2589801 T3 ES 2589801T3 ES 12718651 T ES12718651 T ES 12718651T ES 2589801 T3 ES2589801 T3 ES 2589801T3
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Spain
Prior art keywords
compound
methyl
mmol
formula
salt
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ES12718651.8T
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English (en)
Spanish (es)
Inventor
Dominique AMANS
Emmanuel Hubert Demont
Katherine Louise Jones
Jonathan Thomas Seal
Ann Louise Walker
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GlaxoSmithKline LLC
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GlaxoSmithKline LLC
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    • 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
    • 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
    • A61K31/47064-Aminoquinolines; 8-Aminoquinolines, e.g. chloroquine, primaquine
    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • C07D401/02Heterocyclic 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
    • C07D401/10Heterocyclic 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
    • 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

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Transplantation (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
ES12718651.8T 2011-05-04 2012-05-02 Derivados de dihidroquinolina como inhibidores de bromodominio Active ES2589801T3 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB201107325 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 (1)

Publication Number Publication Date
ES2589801T3 true ES2589801T3 (es) 2016-11-16

Family

ID=44203063

Family Applications (1)

Application Number Title Priority Date Filing Date
ES12718651.8T Active ES2589801T3 (es) 2011-05-04 2012-05-02 Derivados de dihidroquinolina como inhibidores de bromodominio

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
US9271978B2 (en) 2012-12-21 2016-03-01 Zenith Epigenetics Corp. Heterocyclic compounds as bromodomain inhibitors
US9115054B2 (en) * 2013-02-21 2015-08-25 Bristol-Myers Squibb Company Tetrahydronaphthalenyl compounds useful as sipi agonists
EP2970285B1 (en) 2013-03-11 2019-04-17 AbbVie Inc. Fused tetracyclic bromodomain inhibitors
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
ES2704048T3 (es) 2013-03-14 2019-03-14 Glaxosmithkline Ip No 2 Ltd Derivados de 1-acil-4-amino-1,2,3,4-tetrahidroquinolina-2,3-disustituida y su uso como inhibidores de bromodominio
US9227985B2 (en) 2013-03-15 2016-01-05 Incyte Corporation Tricyclic heterocycles as bet protein inhibitors
EP2792355A1 (en) 2013-04-17 2014-10-22 Albert-Ludwigs-Universität Freiburg Compounds for use as bromodomain inhibitors
SG11201510409QA (en) 2013-06-21 2016-01-28 Zenith Epigenetics Corp Novel bicyclic bromodomain inhibitors
WO2015004533A2 (en) 2013-06-21 2015-01-15 Zenith Epigenetics Corp. Novel substituted bicyclic compounds as bromodomain inhibitors
EP3019502B1 (en) 2013-07-08 2017-05-17 Incyte Holdings Corporation Tricyclic heterocycles as bet protein inhibitors
AU2014298051B2 (en) 2013-07-31 2018-11-15 Zenith Epigenetics Ltd. Novel quinazolinones as bromodomain inhibitors
DK3290407T3 (da) 2013-10-18 2020-03-23 Celgene Quanticel Res Inc Bromodomæneinhibitorer
WO2015074081A1 (en) 2013-11-18 2015-05-21 Bair Kenneth W Benzopiperazine compositions as bet bromodomain inhibitors
PT3071203T (pt) 2013-11-18 2021-03-11 Forma Therapeutics Inc Composições de tetra-hidroquinolina como inibidores de bromodomínio bet
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
WO2015081189A1 (en) 2013-11-26 2015-06-04 Incyte Corporation Bicyclic heterocycles as bet protein inhibitors
US9309246B2 (en) 2013-12-19 2016-04-12 Incyte Corporation Tricyclic heterocycles as BET protein inhibitors
JP6480944B2 (ja) * 2014-01-09 2019-03-13 オリオン コーポレーション ブロモドメイン阻害剤としての二環式複素環誘導体
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
TR201820050T4 (tr) 2014-09-12 2019-01-21 Glaxosmithkline Ip No 2 Ltd Bromodomain inhibitörleri olarak tetrahidrokinolin türevleri.
US9527864B2 (en) 2014-09-15 2016-12-27 Incyte Corporation Tricyclic heterocycles as BET protein inhibitors
WO2016087942A1 (en) 2014-12-01 2016-06-09 Zenith Epigenetics Corp. Substituted pyridines as bromodomain inhibitors
CN107207474B (zh) 2014-12-11 2021-05-07 恒翼生物医药科技(上海)有限公司 被取代的杂环作为溴结构域抑制剂
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
WO2017075377A1 (en) 2015-10-29 2017-05-04 Incyte Corporation Amorphous solid form of a bet protein inhibitor
KR102643344B1 (ko) 2016-06-20 2024-03-07 인사이트 코포레이션 Bet 저해제의 결정질 고체 형태
WO2018022802A1 (en) 2016-07-26 2018-02-01 University Of Southern California Selective bromodomain inhibition of fungal bdf1
WO2018111805A1 (en) 2016-12-13 2018-06-21 St. Jude Children's Research Hospital Tetrahydroquinoline-based bromodomain inhibitors
TWI825085B (zh) * 2018-03-30 2023-12-11 日商協和麒麟股份有限公司 具有抗癌活性之化合物
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
CN1901958B (zh) 2003-11-03 2011-03-09 葛兰素集团有限公司 流体分配装置
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
US8476260B2 (en) 2007-12-28 2013-07-02 Mitsubishi Tanabe Pharma Corporation Antitumor agent
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
US9315487B2 (en) 2016-04-19
JP5926793B2 (ja) 2016-05-25
WO2012150234A1 (en) 2012-11-08
JP2014513110A (ja) 2014-05-29
EP2705032B1 (en) 2016-06-15
GB201107325D0 (en) 2011-06-15
US20140066459A1 (en) 2014-03-06

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