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
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compound
fluoro
mmol
formula
acid
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JP2017516365A
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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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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—Ortho-condensed 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4375—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 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
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (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)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pyrrole Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (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
GB1417011.2 2014-09-26
GBGB1417011.2A GB201417011D0 (en) 2014-09-26 2014-09-26 Novel compounds
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 (27)

* 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
BR112019009245A2 (pt) 2016-11-08 2019-07-16 Bristol-Myers Squibb Company azol amidas e aminas como inibidores de alfav integrina
CA3042710A1 (en) 2016-11-08 2018-05-17 Bristol-Myers Squibb Company Cyclobutane- and azetidine-containing mono and spirocyclic compounds as .alpha.v integrin inhibitors
WO2018089353A1 (en) 2016-11-08 2018-05-17 Bristol-Myers Squibb Company 3-substituted propionic acids as alpha v integrin inhibitors
EA201991123A1 (ru) 2016-11-08 2019-11-29 ИНДАЗОЛОВЫЕ ПРОИЗВОДНЫЕ В КАЧЕСТВЕ АНТАГОНИСТОВ ИНТЕГРИНА αV
PL3538528T3 (pl) * 2016-11-08 2021-05-31 Bristol-Myers Squibb Company Amidy pirolu jako inhibitory integryny alfa v
EP3558303A4 (en) 2016-12-23 2020-07-29 Pliant Therapeutics, Inc. AMINO ACID COMPOUNDS AND PROCESSES FOR USE
IL316954A (en) 2017-02-28 2025-01-01 Morphic Therapeutic Inc (Alpha-V)(beta-6)integrin inhibitors
EP3760202A1 (en) 2017-02-28 2021-01-06 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
BR112020008893A2 (pt) 2017-11-07 2020-10-13 Bristol-Myers Squibb Company derivados de pirrolopirazina como inibidores de alfa v integrina
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
UY38352A (es) * 2018-08-29 2020-03-31 Morphic Therapeutic Inc Inhibidores de integrina alfavbeta6
UY38353A (es) 2018-08-29 2020-03-31 Morphic Therapeutic Inc Inhibición de integrina alfavbeta6
WO2020047208A1 (en) 2018-08-29 2020-03-05 Morphic Therapeutic, Inc. Inhibitors of (alpha-v)(beta-6) integrin
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
JP2022512648A (ja) * 2018-10-09 2022-02-07 アンスティチュ ナショナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシュ メディカル 心筋線維化の処置のためのαＶ－インテグリン（ＣＤ５１）阻害剤の使用
MX2021006544A (es) * 2018-12-04 2021-07-07 Sumitomo Pharma Oncology Inc Inhibidores de cinasa dependiente de ciclina 9 (cdk9) y polimorfos de los mismos para uso como agentes para el tratamiento de cancer.
EP4525866A1 (en) * 2022-05-18 2025-03-26 Pliant Therapeutics, Inc. Stabilization of integrin inhibitors
WO2024129931A1 (en) 2022-12-14 2024-06-20 Alnylam Pharmaceuticals, Inc. ALPHA-V BETA-6(ανβ6) INTEGRIN LIGANDS 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
WO2025259743A1 (en) 2024-06-12 2025-12-18 Alnylam Pharmaceuticals, Inc. Dual conjugate compounds for extrahepatic delivery

Family Cites Families (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1047425A4 (en) 1997-12-17 2009-04-22 Merck & Co Inc INTEGRIN RECEPTOR ANTAGONISTS
BR9813769A (pt) 1997-12-17 2000-10-10 Merck & Co Inc Composto, composição farmacêutica, e, processos para fabricar a mesma, para evocar um efeito antagonizante do receptor da integrina em um mamìfero em necessidade deste, para tratar ou prevenir uma condição mediada pelo antagonismo de um receptor da integrina em um mamìfero em necessidade deste, para inibir a reabsorção óssea em um mamìfero em necessidade deste, e para tratar o desenvolvimento tumoral em um mamìfero em necessidade deste.
DZ3263A1 (fr) 1999-06-02 2000-12-07 Merck & Co Inc Antagonistes du recepteur de l'alpha v integrine
AU748949B2 (en) 1999-06-23 2002-06-13 Merck & Co., Inc. Integrin receptor antagonists
WO2001024797A1 (en) * 1999-10-04 2001-04-12 Merck & Co., Inc. Integrin receptor antagonists
CN1414966A (zh) 1999-11-08 2003-04-30 麦克公司 用于制备咪唑烷酮αu蛋白拮抗剂的方法和中间体
US7119098B2 (en) 2000-06-15 2006-10-10 Pharmacia Corporation Heteroarylakanoic acids as intergrin receptor antagonists
US7056909B2 (en) 2000-07-26 2006-06-06 Merck & Co., Inc. Alpha v integrin receptor antagonists
WO2002022616A2 (en) 2000-09-14 2002-03-21 Merck & Co., Inc. Alpha v integrin receptor antagonists
EP1349548A4 (en) 2001-01-03 2004-06-02 Merck & Co Inc METHOD AND COMPOSITIONS FOR TREATING PERIODONTOSIS
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
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
US7705018B2 (en) 2007-03-23 2010-04-27 Amgen Inc. Substituted quinolines and their uses in treatment of inflammatory and related conditions
EP2211615A4 (en) 2007-10-22 2010-10-13 Glaxosmithkline Llc PYRIDOSULFONAMIDE DERIVATIVES AS PI3 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
GB201305668D0 (en) * 2013-03-28 2013-05-15 Glaxosmithkline Ip Dev Ltd Avs6 Integrin Antagonists
WO2015048819A1 (en) 2013-09-30 2015-04-02 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
EP3925959A1 (en) 2015-02-19 2021-12-22 OcuTerra Therapeutics, 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
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

Also Published As

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

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