CN107074851B - 作为αvβ6整联蛋白拮抗剂用于治疗例如纤维变性疾病的萘啶衍生物 - Google Patents

作为αvβ6整联蛋白拮抗剂用于治疗例如纤维变性疾病的萘啶衍生物 Download PDF

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Publication number
CN107074851B
CN107074851B CN201580052204.2A CN201580052204A CN107074851B CN 107074851 B CN107074851 B CN 107074851B CN 201580052204 A CN201580052204 A CN 201580052204A CN 107074851 B CN107074851 B CN 107074851B
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methyl
ethyl
pyrazol
phenyl
pharmaceutically acceptable
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Expired - Fee Related
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Chinese (zh)
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CN107074851A (zh
Inventor
N.A.安德森
I.B.坎贝尔
M.H.J.坎贝尔-克劳福德
A.P.汉考克
S.莱马
S.J.F.麦克唐纳
J.M.普里查德
P.A.普罗科皮欧
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GlaxoSmithKline Intellectual Property Development Ltd
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GlaxoSmithKline Intellectual Property Development Ltd
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    • 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
    • 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
    • A61K31/4375Heterocyclic 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 six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • 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
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/002Heterocyclic compounds
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05Isotopically modified compounds, e.g. labelled

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CN201580052204.2A 2014-09-26 2015-09-22 作为αvβ6整联蛋白拮抗剂用于治疗例如纤维变性疾病的萘啶衍生物 Expired - Fee Related CN107074851B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB1417094.8 2014-09-26
GBGB1417094.8A GB201417094D0 (en) 2014-09-26 2014-09-26 Novel compounds
PCT/EP2015/071782 WO2016046230A1 (en) 2014-09-26 2015-09-22 Naphthyridine derivatives as alpha v beta 6 integrin antagonists for the treatment of e.g. fibrotic diseases

Publications (2)

Publication Number Publication Date
CN107074851A CN107074851A (zh) 2017-08-18
CN107074851B true CN107074851B (zh) 2020-01-10

Family

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CN201580052204.2A Expired - Fee Related CN107074851B (zh) 2014-09-26 2015-09-22 作为αvβ6整联蛋白拮抗剂用于治疗例如纤维变性疾病的萘啶衍生物

Country Status (12)

Country Link
US (2) US10144733B2 (https=)
EP (1) EP3197894B1 (https=)
JP (1) JP6657196B2 (https=)
KR (1) KR20170053638A (https=)
CN (1) CN107074851B (https=)
AU (1) AU2015320863B2 (https=)
BR (1) BR112017006242A2 (https=)
CA (1) CA2962321A1 (https=)
ES (1) ES2811119T3 (https=)
GB (1) GB201417094D0 (https=)
RU (1) RU2692775C2 (https=)
WO (1) WO2016046230A1 (https=)

Families Citing this family (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB201305668D0 (en) 2013-03-28 2013-05-15 Glaxosmithkline Ip Dev Ltd Avs6 Integrin Antagonists
GB201417018D0 (en) 2014-09-26 2014-11-12 Glaxosmithkline Ip Dev Ltd Novel compounds
GB201417002D0 (en) 2014-09-26 2014-11-12 Glaxosmithkline Ip Dev Ltd Novel compound
GB201417011D0 (en) 2014-09-26 2014-11-12 Glaxosmithkline Ip Dev Ltd Novel compounds
GB201417094D0 (en) * 2014-09-26 2014-11-12 Glaxosmithkline Ip Dev Ltd Novel compounds
US20190144547A1 (en) * 2015-11-23 2019-05-16 Merck Patent Gmbh Anti-alpha-v integrin antibody for the treatment of fibrosis and/or fibrotic disorders
KR20180125960A (ko) 2016-03-15 2018-11-26 바이엘 크롭사이언스 악티엔게젤샤프트 동물 해충을 방제하기 위한 치환된 술포닐 아미드
GB201604680D0 (en) 2016-03-21 2016-05-04 Glaxosmithkline Ip Dev Ltd Chemical Compounds
SI3538528T1 (sl) 2016-11-08 2021-03-31 Bristol-Myers Squibb Company Pirol amidi kot alfa v integrin inhibitorji
AU2017359025A1 (en) 2016-11-08 2019-06-20 Bristol-Myers Squibb Company Cyclobutane- and azetidine-containing mono and spirocyclic compounds as alpha V integrin inhibitors
MX2019005234A (es) 2016-11-08 2019-08-12 Squibb Bristol Myers Co Amidas y aminas de azol como inhibidores de integrina alfa v.
WO2018089353A1 (en) 2016-11-08 2018-05-17 Bristol-Myers Squibb Company 3-substituted propionic acids as alpha v integrin inhibitors
KR102506327B1 (ko) 2016-11-08 2023-03-03 브리스톨-마이어스 스큅 컴퍼니 αV 인테그린 길항제로서의 인다졸 유도체
USRE50554E1 (en) 2016-12-23 2025-08-26 Pliant Therapeutics, Inc. Amino acid compounds and methods of use
MA47697A (fr) 2017-02-28 2020-01-08 Morphic Therapeutic Inc Inhibiteurs de l'(alpha-v)(bêta-6) intégrine
MA52117A (fr) 2017-02-28 2022-04-06 Morphic Therapeutic Inc Inhibiteurs de l'intégrine (alpha-v) (bêta-6)
ES2904645T3 (es) 2017-11-07 2022-04-05 Bristol Myers Squibb Co Derivados de pirrolopirazina como inhibidores de integrina alfa v
FI3844162T3 (fi) * 2018-08-29 2025-03-27 Morphic Therapeutic Inc Alfa v beeta6 -integriinin estäjiä
EP4086254B1 (en) 2018-08-29 2024-12-18 Morphic Therapeutic, Inc. Integrin inhibitors
WO2020047208A1 (en) 2018-08-29 2020-03-05 Morphic Therapeutic, Inc. Inhibitors of (alpha-v)(beta-6) integrin
GB202010626D0 (en) 2020-07-10 2020-08-26 Univ Nottingham Compound
CN119173446A (zh) 2022-03-08 2024-12-20 赤盾医疗有限公司 机器人药物制备系统中的流体转移站
CN120731091A (zh) 2022-12-14 2025-09-30 阿尔尼拉姆医药品有限公司 用于肝外递送的α-Vβ-6(αvβ6)整合素配体
WO2025259743A1 (en) 2024-06-12 2025-12-18 Alnylam Pharmaceuticals, Inc. Dual conjugate compounds for extrahepatic delivery
WO2025259747A2 (en) 2024-06-12 2025-12-18 Alnylam Pharmaceuticals, Inc. Dystrophy myotonic protein kinase (dmpk) irna compositions and methods of use thereof

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001024797A1 (en) * 1999-10-04 2001-04-12 Merck & Co., Inc. Integrin receptor antagonists
WO2005082889A1 (en) * 2004-02-18 2005-09-09 Janssen Pharmaceutica N.V. Piperidinyl targeting compounds that selectively bind integrins
WO2014154725A1 (en) * 2013-03-28 2014-10-02 Glaxosmithkline Intellectual Property Development Limited Naphthyridine derivatives useful as alpha-v-beta-6 integrin antagonists

Family Cites Families (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2241192T3 (es) 1997-12-17 2005-10-16 MERCK & CO., INC. (A NEW JERSEY CORP.) Antagonistas del receptor de integrina.
WO1999030709A1 (en) 1997-12-17 1999-06-24 Merck & Co., Inc. Integrin receptor antagonists
PT1187592E (pt) 1999-06-02 2007-10-19 Merck & Co Inc Antagonistas dos receptores de integrina alfa v
JP2003502373A (ja) 1999-06-23 2003-01-21 メルク エンド カムパニー インコーポレーテッド インテグリン受容体アンタゴニスト
CZ20021508A3 (cs) 1999-11-08 2002-10-16 Merck & Co., Inc. Způsob výroby imidazolidinonových derivátů
JP2004511434A (ja) * 2000-06-15 2004-04-15 ファルマシア・コーポレーション インテグリン受容体アンタゴニストとしてのヘテロアリールアルカン酸
DE60126496T2 (de) 2000-07-26 2007-11-15 Merck & Co., Inc. Alpha v integrin-rezeptor-antagonisten
AU2001290772A1 (en) 2000-09-14 2002-03-26 Merck And Co., Inc. Alpha v integrin receptor antagonists
JP2004517853A (ja) 2001-01-03 2004-06-17 メルク エンド カムパニー インコーポレーテッド 歯周病の治療方法及び治療用組成物
DE10112771A1 (de) 2001-03-16 2002-09-26 Merck Patent Gmbh Inhibitoren des Integrins alpha¶v¶beta¶6¶
AR037517A1 (es) * 2001-11-05 2004-11-17 Novartis Ag Derivados de naftiridinas, un proceso para su preparacion, composicion farmaceutica y el uso de los mismos para la preparacion de un medicamento para el tratamiento de una enfermedad inflamatoria
BR0317600A (pt) 2002-12-20 2005-11-29 Pharmacia Corp ácidos heteroarilalcanóicos como derivados de antagonistas de receptor de integrina
US6932865B2 (en) 2003-04-11 2005-08-23 Lockheed Martin Corporation System and method of making single-crystal structures through free-form fabrication techniques
RS53151B (sr) 2007-03-23 2014-06-30 Amgen Inc. 3-supstituisani derivati hinolina ili hinoksalina i njihova upotreba kao inhibitora fosfatidilinozitol 3-kinaze (pi3k)
US8563566B2 (en) 2007-08-01 2013-10-22 Valeant Pharmaceuticals International Naphthyridine derivatives as potassium channel modulators
US20100311736A1 (en) 2007-10-22 2010-12-09 Glaxosmithkline Llc Pyridosulfonamide derivatives as p13 kinase inhibitors
WO2011111880A1 (ko) 2010-03-08 2011-09-15 주식회사 메디젠텍 세포핵에서 세포질로의 gsk3의 이동을 억제하는 화합물을 함유하는 세포핵에서 세포질로의 gsk3 이동에 의해 발생되는 질환의 치료 또는 예방용 약학적 조성물
WO2015048819A1 (en) 2013-09-30 2015-04-02 The Regents Of The University Of California Anti-alphavbeta1 integrin compounds and methods
GB201417094D0 (en) * 2014-09-26 2014-11-12 Glaxosmithkline Ip Dev Ltd Novel compounds
GB201417011D0 (en) 2014-09-26 2014-11-12 Glaxosmithkline Ip Dev Ltd Novel compounds
GB201417002D0 (en) 2014-09-26 2014-11-12 Glaxosmithkline Ip Dev Ltd Novel compound
GB201417018D0 (en) 2014-09-26 2014-11-12 Glaxosmithkline Ip Dev Ltd Novel compounds
KR102647026B1 (ko) 2015-02-19 2024-03-12 사이플루어 라이프 사이언시즈, 인크 플루오르화 테트라히드로나프티리디닐 노난산 유도체 및 이의 용도
CA2981371A1 (en) 2015-03-10 2016-09-15 The Regents Of The University Of California Anti-alphavbeta1 integrin inhibitors and methods of use
GB201604589D0 (en) 2016-03-18 2016-05-04 Glaxosmithkline Ip Dev Ltd Chemical compound
GB201604680D0 (en) 2016-03-21 2016-05-04 Glaxosmithkline Ip Dev Ltd Chemical Compounds
GB201604681D0 (en) 2016-03-21 2016-05-04 Glaxosmithkline Ip Dev Ltd Chemical Compounds

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001024797A1 (en) * 1999-10-04 2001-04-12 Merck & Co., Inc. Integrin receptor antagonists
WO2005082889A1 (en) * 2004-02-18 2005-09-09 Janssen Pharmaceutica N.V. Piperidinyl targeting compounds that selectively bind integrins
WO2014154725A1 (en) * 2013-03-28 2014-10-02 Glaxosmithkline Intellectual Property Development Limited Naphthyridine derivatives useful as alpha-v-beta-6 integrin antagonists

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US10513517B2 (en) 2019-12-24
WO2016046230A1 (en) 2016-03-31
JP6657196B2 (ja) 2020-03-04
RU2017114355A3 (https=) 2019-01-14
RU2692775C2 (ru) 2019-06-27
JP2017528504A (ja) 2017-09-28
BR112017006242A2 (pt) 2017-12-12
CN107074851A (zh) 2017-08-18
US20190048005A1 (en) 2019-02-14
KR20170053638A (ko) 2017-05-16
ES2811119T3 (es) 2021-03-10
EP3197894A1 (en) 2017-08-02
AU2015320863A1 (en) 2017-03-09
US20170291899A1 (en) 2017-10-12
EP3197894B1 (en) 2020-06-03
US10144733B2 (en) 2018-12-04
GB201417094D0 (en) 2014-11-12
RU2017114355A (ru) 2018-10-29
AU2015320863B2 (en) 2018-09-06
CA2962321A1 (en) 2016-03-31

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