JP6795588B2 - ブロモドメイン阻害薬としての使用のためのピリジノンジカルボキサミド - Google Patents

ブロモドメイン阻害薬としての使用のためのピリジノンジカルボキサミド Download PDF

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Publication number
JP6795588B2
JP6795588B2 JP2018515059A JP2018515059A JP6795588B2 JP 6795588 B2 JP6795588 B2 JP 6795588B2 JP 2018515059 A JP2018515059 A JP 2018515059A JP 2018515059 A JP2018515059 A JP 2018515059A JP 6795588 B2 JP6795588 B2 JP 6795588B2
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JP
Japan
Prior art keywords
oxo
dihydropyridine
methyl
dicarboxamide
benzyl
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Expired - Fee Related
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JP2018515059A
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Japanese (ja)
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JP2018528229A5 (enExample
JP2018528229A (ja
Inventor
ジョン アトキンソン，スティーブン
ジョン アトキンソン，スティーブン
ヒューバート デモント，エマニュエル
ヒューバート デモント，エマニュエル
アンドリュー ハリソン，リー
アンドリュー ハリソン，リー
ジョージ クリストファー ヘイホー，トーマス
ジョージ クリストファー ヘイホー，トーマス
ハウス，デヴィッド
ジェイ リンドン，マシュー
ジェイ リンドン，マシュー
ジー プレストン，アレクサンダー
ジー プレストン，アレクサンダー
トーマス シール，ジョナサン
トーマス シール，ジョナサン
デヴィッド ウォール，イアン
デヴィッド ウォール，イアン
ジェイ ワトソン，ロバート
ジェイ ワトソン，ロバート
マイケル ウールベン，ジェームズ
マイケル ウールベン，ジェームズ
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GlaxoSmithKline Intellectual Property No 2 Ltd
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GlaxoSmithKline Intellectual Property No 2 Ltd
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    • 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
    • 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
    • A61K31/443—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
    • 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
    • A61K31/4433—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
    • 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
    • A61K31/4436—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom
    • 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
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541—Non-condensed thiazines containing further heterocyclic rings
    • 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
    • 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
    • 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
    • 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
    • C07D401/12—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/02—Heterocyclic 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
    • C07D405/12—Heterocyclic 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 linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Transplantation (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)
JP2018515059A 2015-09-22 2016-09-20 ブロモドメイン阻害薬としての使用のためのピリジノンジカルボキサミド Expired - Fee Related JP6795588B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201562221649P 2015-09-22 2015-09-22
US62/221,649 2015-09-22
PCT/EP2016/072216 WO2017050714A1 (en) 2015-09-22 2016-09-20 Pyridinone dicarboxamide for use as bromodomain inhibitors

Publications (3)

Publication Number Publication Date
JP2018528229A JP2018528229A (ja) 2018-09-27
JP2018528229A5 JP2018528229A5 (enExample) 2019-10-17
JP6795588B2 true JP6795588B2 (ja) 2020-12-02

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JP2018515059A Expired - Fee Related JP6795588B2 (ja) 2015-09-22 2016-09-20 ブロモドメイン阻害薬としての使用のためのピリジノンジカルボキサミド

Country Status (9)

Country Link
US (1) US10370356B2 (enExample)
EP (1) EP3353162A1 (enExample)
JP (1) JP6795588B2 (enExample)
KR (1) KR20180052762A (enExample)
CN (1) CN108137541B (enExample)
AU (1) AU2016326864A1 (enExample)
CA (1) CA2998545A1 (enExample)
RU (1) RU2018112312A (enExample)
WO (1) WO2017050714A1 (enExample)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20190006567A (ko) 2016-05-24 2019-01-18 글락소스미스클라인 인털렉츄얼 프로퍼티 (넘버 2) 리미티드 브로모도메인 억제제로서의 피리딘 디카르복사미드 유도체
CA3070073A1 (en) 2017-07-18 2019-01-24 Nuvation Bio Inc. 1,8-naphthyridinone compounds and uses thereof
JP2020527588A (ja) 2017-07-18 2020-09-10 ニューベイション・バイオ・インコーポレイテッドＮｕｖａｔｉｏｎ Ｂｉｏ Ｉｎｃ． アデノシンアンタゴニストとしてのヘテロ環式化合物
GB201716392D0 (en) * 2017-10-06 2017-11-22 Glaxosmithkline Intellectual Property (No 2) Ltd Compounds
GB201716369D0 (en) * 2017-10-06 2017-11-22 Glaxosmithkline Intellectual Property (No 2) Ltd Compounds
EP4389277A3 (en) * 2017-10-18 2024-10-09 Biotage AB Sample clean up device and method of using it
GB201814167D0 (en) 2018-08-31 2018-10-17 Glaxosmithkline Ip No 2 Ltd Compounds
EP3873474A4 (en) 2018-10-30 2022-07-13 Nuvation Bio Inc. HETEROCYCLIC COMPOUNDS USED AS BET INHIBITORS
WO2020150674A1 (en) 2019-01-18 2020-07-23 Nuvation Bio Inc. Heterocyclic compounds as adenosine antagonists
US11254670B2 (en) 2019-01-18 2022-02-22 Nuvation Bio Inc. 1,8-naphthyridinone compounds and uses thereof
JP7465945B2 (ja) 2019-07-02 2024-04-11 ニューベイション・バイオ・インコーポレイテッド Ｂｅｔ阻害剤としてのヘテロ環式化合物

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GB9004781D0 (en) 1990-03-02 1990-04-25 Glaxo Group Ltd Device
DE60139506D1 (de) 2000-12-28 2009-09-17 Shionogi & Co 2-pyridonderivate mit affinität für den cannabinoid-typ-2-rezeptor
WO2003070277A1 (en) * 2002-02-19 2003-08-28 Shionogi & Co., Ltd. Antipruritics
GB0211759D0 (en) 2002-05-22 2002-07-03 Glaxo Group Ltd Novel compounds
CA2542007C (en) 2002-10-09 2010-06-29 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
BRPI0416128B8 (pt) 2003-11-03 2021-06-22 Glaxo Group Ltd dispositivo de dispensação de fluido
GB0919434D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB0919423D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
AU2013341200A1 (en) 2012-11-08 2015-07-02 Bristol-Myers Squibb Company Heteroaryl substituted pyridyl compounds useful as kinase modulators
JP2016507496A (ja) * 2012-12-21 2016-03-10 ゼニス・エピジェネティクス・コーポレイションＺｅｎｉｔｈ Ｅｐｉｇｅｎｅｔｉｃｓ Ｃｏｒｐ． ブロモドメイン阻害剤としての新規複素環式化合物
CN105189461B (zh) 2013-03-14 2018-05-15 葛兰素史克知识产权第二有限公司 2,3-二取代的1-酰基-4-氨基-1,2,3,4-四氢喹啉衍生物和它们作为溴结构域抑制剂的用途
WO2015011252A1 (en) 2013-07-26 2015-01-29 F. Hoffmann-La Roche Ag Pyrimidine-pyridinone serine/threonine kinase inhibitors
CA2919948C (en) 2013-07-31 2020-07-21 Zenith Epigenetics Corp. Novel quinazolinones as bromodomain inhibitors
MA43940A (fr) 2015-09-02 2018-12-12 Glaxosmithkline Ip No 2 Ltd Dicarboxamide de pyridinone utilisé comme inhibiteur de bromodomaine
BR112018006545A2 (pt) 2015-10-05 2018-10-16 Glaxosmithkline Ip No 2 Ltd ?composto, composição farmacêutica, combinação, uso de um composto, e, método para tratamento de uma doença ou condição?
ES2840848T3 (es) 2016-04-07 2021-07-07 Glaxosmithkline Ip No 2 Ltd Derivados de piridilo como inhibidores de bromodominio
KR20190006567A (ko) 2016-05-24 2019-01-18 글락소스미스클라인 인털렉츄얼 프로퍼티 (넘버 2) 리미티드 브로모도메인 억제제로서의 피리딘 디카르복사미드 유도체

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US20180282301A1 (en) 2018-10-04
CN108137541B (zh) 2021-07-06
KR20180052762A (ko) 2018-05-18
RU2018112312A (ru) 2019-10-23
US10370356B2 (en) 2019-08-06
CN108137541A (zh) 2018-06-08
WO2017050714A1 (en) 2017-03-30
EP3353162A1 (en) 2018-08-01
JP2018528229A (ja) 2018-09-27
AU2016326864A1 (en) 2018-03-22
CA2998545A1 (en) 2017-03-30

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