CN108290866B - 作为溴结构域抑制剂的2-氧代-1,2-二氢吡啶-3,5-二甲酰胺化合物 - Google Patents

作为溴结构域抑制剂的2-氧代-1,2-二氢吡啶-3,5-二甲酰胺化合物 Download PDF

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Publication number
CN108290866B
CN108290866B CN201680071214.5A CN201680071214A CN108290866B CN 108290866 B CN108290866 B CN 108290866B CN 201680071214 A CN201680071214 A CN 201680071214A CN 108290866 B CN108290866 B CN 108290866B
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China
Prior art keywords
methyl
oxo
dihydropyridine
dicarboxamide
benzyl
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Expired - Fee Related
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CN201680071214.5A
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English (en)
Chinese (zh)
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CN108290866A (zh
Inventor
S.J.阿特金森
E.H.德蒙特
L.A.哈里森
T.G.C.海霍夫
M.J.林登
A.G.普雷斯顿
J.T.西尔
I.D.沃尔
R.J.沃森
J.M.伍尔文
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GlaxoSmithKline Intellectual Property No 2 Ltd
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GlaxoSmithKline Intellectual Property No 2 Ltd
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Publication of CN108290866A publication Critical patent/CN108290866A/zh
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Expired - Fee Related legal-status Critical Current
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
    • C07D213/82—Amides; Imides in position 3
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4412—Non condensed pyridines; Hydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • 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
    • 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
    • C07D401/12—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 chain containing hetero atoms as chain links
    • 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)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Immunology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Transplantation (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
CN201680071214.5A 2015-10-05 2016-10-03 作为溴结构域抑制剂的2-氧代-1,2-二氢吡啶-3,5-二甲酰胺化合物 Expired - Fee Related CN108290866B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201562237002P 2015-10-05 2015-10-05
US62/237002 2015-10-05
PCT/EP2016/073532 WO2017060180A1 (en) 2015-10-05 2016-10-03 2-oxo-1,2-dihydropyridine-3,5-dicarboxamide compounds as bromodomain inhibitors

Publications (2)

Publication Number Publication Date
CN108290866A CN108290866A (zh) 2018-07-17
CN108290866B true CN108290866B (zh) 2020-12-18

Family

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CN201680071214.5A Expired - Fee Related CN108290866B (zh) 2015-10-05 2016-10-03 作为溴结构域抑制剂的2-氧代-1,2-二氢吡啶-3,5-二甲酰胺化合物

Country Status (11)

Country Link
US (1) US10471050B2 (https=)
EP (1) EP3359531B1 (https=)
JP (1) JP6832923B2 (https=)
KR (1) KR20180059551A (https=)
CN (1) CN108290866B (https=)
AU (1) AU2016334637A1 (https=)
BR (1) BR112018006545A2 (https=)
CA (1) CA2999379A1 (https=)
ES (1) ES2831322T3 (https=)
RU (1) RU2018114705A (https=)
WO (1) WO2017060180A1 (https=)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HK1249504A1 (zh) 2015-09-02 2018-11-02 Glaxosmithkline Intellectual Property (No. 2) Limited 用作溴结构域抑制剂的吡啶酮二甲酰胺
US10370356B2 (en) 2015-09-22 2019-08-06 Glaxosmithkline Intellectual Property (No. 2) Limited Pyridinone dicarboxamide for use as bromodomain inhibitors
KR20180059551A (ko) 2015-10-05 2018-06-04 글락소스미스클라인 인털렉츄얼 프로퍼티 (넘버 2) 리미티드 브로모도메인 억제제로서 2-옥소-1,2-디하이드로피리딘-3,5-디카복스아미드 화합물
BR112018070536A2 (pt) 2016-04-07 2019-02-12 Glaxosmithkline Intellectual Property (No. composto, composição farmacêutica, combinação, uso de um composto ou um sal farmaceuticamente aceitável do mesmo, e, método de tratamento de uma doença ou condição
CA3023765A1 (en) 2016-05-24 2017-11-30 Glaxosmithkline Intellectual Property (No. 2) Limited Pyridine dicarboxamide derivatives as bromodomain inhibitors
GB201703282D0 (en) * 2017-03-01 2017-04-12 Glaxosmithkline Intellectual Property (No 2) Ltd Compounds
JOP20190192A1 (ar) 2017-03-01 2019-08-08 Glaxosmithkline Ip No 2 Ltd مشتقات بيرازول بوصفها مثبطات برومودومين
GB201814167D0 (en) 2018-08-31 2018-10-17 Glaxosmithkline Ip No 2 Ltd Compounds

Citations (2)

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Publication number Priority date Publication date Assignee Title
EP1477186A1 (en) * 2002-02-19 2004-11-17 Shionogi & Co., Ltd. Antipruritics
WO2014096965A2 (en) * 2012-12-21 2014-06-26 Rvx Therapeutics Inc. Novel heterocyclic compounds as bromodomain inhibitors

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ES2330719T3 (es) * 2000-12-28 2009-12-15 SHIONOGI & CO., LTD. Derivados de 2-piridona con afinidad para el receptor cannabinoide de tipo 2.
AU2003273675A1 (en) 2002-10-09 2004-05-04 Wayne R. Danter Protein tyrosine kinase inhibitors
EP1433788A1 (en) 2002-12-23 2004-06-30 Aventis Pharma Deutschland GmbH Pyrazole-derivatives as factor Xa inhibitors
GB0919434D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
KR20150079963A (ko) 2012-11-08 2015-07-08 브리스톨-마이어스 스큅 컴퍼니 키나제 조절제로서 유용한 헤테로아릴 치환된 피리딜 화합물
JP6542212B2 (ja) 2013-07-31 2019-07-10 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キナゾリノン
HK1249504A1 (zh) 2015-09-02 2018-11-02 Glaxosmithkline Intellectual Property (No. 2) Limited 用作溴结构域抑制剂的吡啶酮二甲酰胺
KR20180059551A (ko) 2015-10-05 2018-06-04 글락소스미스클라인 인털렉츄얼 프로퍼티 (넘버 2) 리미티드 브로모도메인 억제제로서 2-옥소-1,2-디하이드로피리딘-3,5-디카복스아미드 화합물
BR112018070536A2 (pt) 2016-04-07 2019-02-12 Glaxosmithkline Intellectual Property (No. composto, composição farmacêutica, combinação, uso de um composto ou um sal farmaceuticamente aceitável do mesmo, e, método de tratamento de uma doença ou condição
CA3023765A1 (en) 2016-05-24 2017-11-30 Glaxosmithkline Intellectual Property (No. 2) Limited Pyridine dicarboxamide derivatives as bromodomain inhibitors

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1477186A1 (en) * 2002-02-19 2004-11-17 Shionogi & Co., Ltd. Antipruritics
WO2014096965A2 (en) * 2012-12-21 2014-06-26 Rvx Therapeutics Inc. Novel heterocyclic compounds as bromodomain inhibitors

Non-Patent Citations (2)

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Title
BET bromodomain inhibitors: a patent review;Jean-Marc Garnier et al;《Expert Opinion on Therapeutic Patents》;20131122;第24卷(第2期);185-199 *
Bromodomains and Their Pharmacological Inhibitors;Daniel Gallenkamp et al;《CHEMMEDCHEM》;20140204;第9卷(第3期);438-464 *

Also Published As

Publication number Publication date
ES2831322T3 (es) 2021-06-08
AU2016334637A1 (en) 2018-04-12
US20180280368A1 (en) 2018-10-04
US10471050B2 (en) 2019-11-12
BR112018006545A2 (pt) 2018-10-16
RU2018114705A (ru) 2019-11-07
JP2018529737A (ja) 2018-10-11
EP3359531A1 (en) 2018-08-15
KR20180059551A (ko) 2018-06-04
EP3359531B1 (en) 2020-08-19
CA2999379A1 (en) 2017-04-13
WO2017060180A1 (en) 2017-04-13
JP6832923B2 (ja) 2021-02-24
CN108290866A (zh) 2018-07-17

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Granted publication date: 20201218