JP6665169B2 - 新規化合物αvβ6インテグリンアンタゴニスト - Google Patents

新規化合物αvβ6インテグリンアンタゴニスト Download PDF

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Publication number
JP6665169B2
JP6665169B2 JP2017516365A JP2017516365A JP6665169B2 JP 6665169 B2 JP6665169 B2 JP 6665169B2 JP 2017516365 A JP2017516365 A JP 2017516365A JP 2017516365 A JP2017516365 A JP 2017516365A JP 6665169 B2 JP6665169 B2 JP 6665169B2
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Japan
Prior art keywords
compound
fluoro
mmol
formula
acid
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JP2017516365A
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English (en)
Japanese (ja)
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JP2017528503A5 (enExample
JP2017528503A (ja
Inventor
ニール、アンドリュー、アンダーソン
マシュー、ハワード、ジェームズ、キャンベル−クロフォード
アシュリー、ポール、ハンコック
ジョン、マーティン、プリチャード
ジョアンナ、マリー、レドモンド
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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
    • 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
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61P35/00Antineoplastic agents
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pyrrole Compounds (AREA)
JP2017516365A 2014-09-26 2015-09-22 新規化合物αvβ6インテグリンアンタゴニスト Expired - Fee Related JP6665169B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GBGB1417011.2A GB201417011D0 (en) 2014-09-26 2014-09-26 Novel compounds
GB1417011.2 2014-09-26
PCT/EP2015/071777 WO2016046226A1 (en) 2014-09-26 2015-09-22 Novel compounds

Publications (3)

Publication Number Publication Date
JP2017528503A JP2017528503A (ja) 2017-09-28
JP2017528503A5 JP2017528503A5 (enExample) 2018-11-08
JP6665169B2 true JP6665169B2 (ja) 2020-03-13

Family

ID=51901167

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2017516365A Expired - Fee Related JP6665169B2 (ja) 2014-09-26 2015-09-22 新規化合物αvβ6インテグリンアンタゴニスト

Country Status (15)

Country Link
US (1) US10000489B2 (enExample)
EP (1) EP3197893B1 (enExample)
JP (1) JP6665169B2 (enExample)
KR (1) KR20170063590A (enExample)
CN (1) CN107074849A (enExample)
AR (1) AR101995A1 (enExample)
AU (1) AU2015320859A1 (enExample)
BR (1) BR112017006253A2 (enExample)
CA (1) CA2962326A1 (enExample)
ES (1) ES2704525T3 (enExample)
GB (1) GB201417011D0 (enExample)
RU (1) RU2017114346A (enExample)
TW (1) TW201629057A (enExample)
UY (1) UY36315A (enExample)
WO (1) WO2016046226A1 (enExample)

Families Citing this family (24)

* 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
GB201417094D0 (en) * 2014-09-26 2014-11-12 Glaxosmithkline Ip Dev Ltd Novel compounds
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
AU2017359030A1 (en) * 2016-11-08 2019-06-20 Bristol-Myers Squibb Company Pyrrole amides as alpha v integrin inhibitors
MA46745A (fr) 2016-11-08 2021-03-31 Bristol Myers Squibb Co Dérivés d'indazole en tant qu'antagonistes de l'intégrine alpha v
US10851098B2 (en) 2016-11-08 2020-12-01 Bristol-Myers Squibb Company Azole amides and amines as alpha v integrin inhibitors
WO2018089355A1 (en) 2016-11-08 2018-05-17 Bristol-Myers Squibb Company Cyclobutane- and azetidine-containing mono and spirocyclic compounds as alpha v integrin inhibitors
CA3042707A1 (en) 2016-11-08 2018-05-17 Bristol-Myers Squibb Company 3-substituted propionic acids as .alpha.v integrin inhibitors
US10696672B2 (en) 2016-12-23 2020-06-30 Pliant Therapeutics, Inc. Amino acid compounds and methods of use
TW201835078A (zh) 2017-02-28 2018-10-01 美商萊築理公司 αvβ6整合蛋白之抑制劑
AU2018227417B2 (en) 2017-02-28 2021-12-23 Morphic Therapeutic, Inc. Inhibitors of (alpha-v)(beta-6) integrin
CN107823208A (zh) * 2017-10-25 2018-03-23 南京多宝生物科技有限公司 吗啉类化合物在制备治疗和预防肾纤维化药物中的应用
US11292802B2 (en) 2017-11-07 2022-04-05 Bristol-Myers Squibb Company Substituted tetrahydropyrrolo[1,2-a]pyrazines as alpha v integrin inhibitors
CN108208177A (zh) * 2017-11-28 2018-06-29 上海交通大学医学院附属新华医院 含丁酸类化合物的组合物及其应用
PL3844162T3 (pl) * 2018-08-29 2025-06-09 Morphic Therapeutic, Inc. Inhibitory integryny alfa v beta 6
EP4086254B1 (en) 2018-08-29 2024-12-18 Morphic Therapeutic, Inc. Integrin inhibitors
TW202028179A (zh) * 2018-10-08 2020-08-01 美商普萊恩醫療公司 胺基酸化合物及使用方法
US12351634B2 (en) * 2018-10-09 2025-07-08 INSERM (Institut National de la Santé et de la Recherche Médicale) Use of cilengitide for ameliorating cardiac fibrosis occurring in response to myocardial infarction
JP2022511029A (ja) * 2018-12-04 2022-01-28 スミトモ ダイニッポン ファーマ オンコロジー, インコーポレイテッド がんの処置のための薬剤としての使用のためのcdk9インヒビターおよびその多形
EP4525866A1 (en) * 2022-05-18 2025-03-26 Pliant Therapeutics, Inc. Stabilization of integrin inhibitors
AU2023399039A1 (en) 2022-12-14 2025-05-22 Alnylam Pharmaceuticals, Inc. ALPHA-V BETA-6(ανβ6) INTEGRIN LIGANDS FOR EXTRAHEPATIC DELIVERY

Family Cites Families (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE69829996T2 (de) 1997-12-17 2006-02-23 Merck & Co., Inc. (A New Jersey Corp.) Integrin-rezeptor-antagonisten
WO1999030709A1 (en) 1997-12-17 1999-06-24 Merck & Co., Inc. Integrin receptor antagonists
SK17442001A3 (sk) 1999-06-02 2002-03-05 Merck & Co., Inc. Deriváty kyseliny nonánovej, farmaceutický prostriedok s ich obsahom a ich použitie
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
AU7743400A (en) * 1999-10-04 2001-05-10 Merck & Co., Inc. Integrin receptor antagonists
KR20020048427A (ko) 1999-11-08 2002-06-22 폴락 돈나 엘. 이미다졸리디논 알파 v 인테그린 길항제를 제조하기 위한방법 및 중간체
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
EP1315501B1 (en) 2000-07-26 2007-02-07 Merck & Co., Inc. Alpha v integrin receptor antagonists
AU2001290772A1 (en) 2000-09-14 2002-03-26 Merck And Co., Inc. Alpha v integrin receptor antagonists
AU2002246757B2 (en) 2001-01-03 2006-02-02 Merck & Co., Inc. Methods and compositions for treating periodontal disease
DE10112771A1 (de) 2001-03-16 2002-09-26 Merck Patent Gmbh Inhibitoren des Integrins alpha¶v¶beta¶6¶
US20040224986A1 (en) * 2002-08-16 2004-11-11 Bart De Corte Piperidinyl targeting compounds that selectively bind integrins
JP2006518333A (ja) 2002-12-20 2006-08-10 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
US6932865B2 (en) 2003-04-11 2005-08-23 Lockheed Martin Corporation System and method of making single-crystal structures through free-form fabrication techniques
US7705018B2 (en) 2007-03-23 2010-04-27 Amgen Inc. Substituted quinolines and their uses in treatment of inflammatory and related conditions
JP2011500823A (ja) 2007-10-22 2011-01-06 グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー Pi3キナーゼ阻害物質としてのピリドスルホンアミド誘導体
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
GB201305668D0 (en) * 2013-03-28 2013-05-15 Glaxosmithkline Ip Dev Ltd Avs6 Integrin Antagonists
AU2014324426A1 (en) 2013-09-30 2016-04-21 The Regents Of The University Of California Anti-alphavbeta1 integrin compounds and methods
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
GB201417094D0 (en) 2014-09-26 2014-11-12 Glaxosmithkline Ip Dev Ltd Novel compounds
EP3259271B1 (en) 2015-02-19 2021-05-05 SciFluor Life Sciences, Inc. Fluorinated derivatives of 3-(2-oxo-3-(3-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)propyl)imidazolidin-1-yl)propanoic acid and uses thereof
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
GB201604681D0 (en) 2016-03-21 2016-05-04 Glaxosmithkline Ip Dev Ltd Chemical Compounds
GB201604680D0 (en) 2016-03-21 2016-05-04 Glaxosmithkline Ip Dev Ltd Chemical Compounds

Also Published As

Publication number Publication date
US10000489B2 (en) 2018-06-19
CA2962326A1 (en) 2016-03-31
TW201629057A (zh) 2016-08-16
BR112017006253A2 (pt) 2017-12-12
KR20170063590A (ko) 2017-06-08
ES2704525T3 (es) 2019-03-18
UY36315A (es) 2016-04-29
AR101995A1 (es) 2017-01-25
WO2016046226A1 (en) 2016-03-31
GB201417011D0 (en) 2014-11-12
AU2015320859A1 (en) 2017-03-09
EP3197893A1 (en) 2017-08-02
CN107074849A (zh) 2017-08-18
JP2017528503A (ja) 2017-09-28
EP3197893B1 (en) 2018-10-24
RU2017114346A (ru) 2018-11-02
US20170298063A1 (en) 2017-10-19

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