JP7092784B2 - αｖβ６インテグリン阻害剤 - Google Patents

αｖβ６インテグリン阻害剤 Download PDF

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JP7092784B2
JP7092784B2 JP2019547426A JP2019547426A JP7092784B2 JP 7092784 B2 JP7092784 B2 JP 7092784B2 JP 2019547426 A JP2019547426 A JP 2019547426A JP 2019547426 A JP2019547426 A JP 2019547426A JP 7092784 B2 JP7092784 B2 JP 7092784B2
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mmol
compound
naphthylidine
tetrahydro
esi
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JP2020510664A5 (enExample
JP2020510664A (ja
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ブルワー，マーク
バーサヴィッチ，マシュー，グレゴリー
ゲラシュト，アレクセイ，イゴレヴィッチ
ハーン，クリストファー，ニール
ハリソン，ブライス，アルデン
コンゼ，カイル，デイヴィッド
リン，フー－ヤン
リッパ，ブレイズ，スコット
ルゴフスコイ，アレクセイ，アレクサンドロヴィッチ
ロジャース，ブルース，ニールセン
スベンソン，マッツ，オーケ
トロースト，ダウン，マリー
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モーフィック セラピューティック，インコーポレイテッド
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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
    • A61K31/435—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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/16—Antivirals for RNA viruses for influenza or rhinoviruses
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • 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
    • 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
    • C07D471/08—Bridged systems
    • 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
    • C07D471/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (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)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Urology & Nephrology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Virology (AREA)
  • Diabetes (AREA)
  • Pain & Pain Management (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Emergency Medicine (AREA)
  • Obesity (AREA)
  • Transplantation (AREA)
  • Endocrinology (AREA)
  • Molecular Biology (AREA)
  • Communicable Diseases (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
JP2019547426A 2017-02-28 2018-02-27 αｖβ６インテグリン阻害剤 Active JP7092784B2 (ja)

Priority Applications (1)

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JP2022097012A JP7443425B2 (ja) 2017-02-28 2022-06-16 αｖβ６インテグリン阻害剤

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US201762464693P 2017-02-28 2017-02-28
US62/464,693 2017-02-28
PCT/US2018/019838 WO2018160521A2 (en) 2017-02-28 2018-02-27 Inhibitors of (alpha-v)(beta-6) integrin

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JP2020510664A5 JP2020510664A5 (enExample) 2021-04-01
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US (5) US20180244648A1 (enExample)
EP (2) EP4159727A1 (enExample)
JP (2) JP7092784B2 (enExample)
KR (2) KR102605460B1 (enExample)
CN (2) CN110573499B (enExample)
AR (2) AR111009A1 (enExample)
AU (3) AU2018229275B2 (enExample)
BR (1) BR112019017929A2 (enExample)
CA (1) CA3054604A1 (enExample)
IL (3) IL297530B2 (enExample)
MA (1) MA47697A (enExample)
MX (2) MX394210B (enExample)
RU (2) RU2022108080A (enExample)
SG (1) SG11201907820SA (enExample)
TW (2) TWI834321B (enExample)
WO (1) WO2018160521A2 (enExample)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2021535141A (ja) * 2018-08-29 2021-12-16 モーフィック セラピューティック，インコーポレイテッド αｖβ６インテグリンの阻害

Families Citing this family (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN109996541A (zh) 2016-09-07 2019-07-09 普利安特治疗公司 N-酰基氨基酸化合物及其使用方法
USRE50554E1 (en) 2016-12-23 2025-08-26 Pliant Therapeutics, Inc. Amino acid compounds and methods of use
KR102605460B1 (ko) * 2017-02-28 2023-11-22 모픽 테라퓨틱, 인코포레이티드 αvβ6 인테그린 억제제
MA52117A (fr) 2017-02-28 2022-04-06 Morphic Therapeutic Inc Inhibiteurs de l'intégrine (alpha-v) (bêta-6)
EP4328230A3 (en) 2018-03-07 2024-04-24 Pliant Therapeutics, Inc. Amino acid compounds and methods of use
TWI841573B (zh) 2018-06-27 2024-05-11 美商普萊恩醫療公司 具有未分支連接子之胺基酸化合物及使用方法
EP3843728B1 (en) * 2018-08-29 2025-04-30 Morphic Therapeutic, Inc. Inhibitors of (alpha-v)(beta-6) integrin
WO2020047208A1 (en) * 2018-08-29 2020-03-05 Morphic Therapeutic, Inc. Inhibitors of (alpha-v)(beta-6) integrin
RS66733B1 (sr) * 2018-08-29 2025-05-30 Morphic Therapeutic Inc Inhibitori alfa v beta6 integrina
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
CN119462635A (zh) 2018-10-30 2025-02-18 吉利德科学公司 作为α4β7整合素抑制剂的喹啉衍生物
WO2020092394A1 (en) 2018-10-30 2020-05-07 Gilead Sciences, Inc. Imidazopyridine derivatives as alpha4beta7 integrin inhibitors
JP7189368B2 (ja) 2018-10-30 2022-12-13 ギリアード サイエンシーズ， インコーポレイテッド アルファ４ベータ７インテグリンの阻害のための化合物
JP7189369B2 (ja) 2018-10-30 2022-12-13 ギリアード サイエンシーズ， インコーポレイテッド アルファ４β７インテグリンの阻害のための化合物
EP3952902A4 (en) 2019-04-08 2022-12-21 Pliant Therapeutics, Inc. DOSAGE FORMS AND THERAPY SCHEMES FOR AMINO ACID COMPOUNDS
KR20220047323A (ko) 2019-08-14 2022-04-15 길리애드 사이언시즈, 인코포레이티드 알파 4 베타 7 인테그린의 저해용 화합물
WO2021076902A1 (en) * 2019-10-16 2021-04-22 Morphic Therapeutic, Inc. INHIBITING HUMAN INTEGRIN α 4 β 7
CN111718250B (zh) * 2020-06-28 2022-04-22 万华化学集团股份有限公司 一种制备r-香茅醛的方法
CN116710169A (zh) 2020-11-19 2023-09-05 普利安特治疗公司 整合素抑制剂及其用途
EP4665458A1 (en) * 2023-02-14 2025-12-24 Morphic Therapeutic, Inc. Inhibiting alpha v beta8 integrin
EP4665339A1 (en) * 2023-02-14 2025-12-24 Morphic Therapeutic, Inc. Inhibiting alpha v beta 8 integrin
WO2025106644A1 (en) * 2023-11-15 2025-05-22 Morphic Therapeutic, Inc. Heterocyclic compounds as inhibitors of alpha-v beta-1 integrin

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2001503060A (ja) 1996-10-30 2001-03-06 メルク エンド カンパニー インコーポレーテッド インテグリン拮抗薬
JP2015524412A (ja) 2012-07-18 2015-08-24 セントルイス ユニバーシティ インテグリンアンタゴニストとしてのβアミノ酸誘導体

Family Cites Families (95)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4522811A (en) 1982-07-08 1985-06-11 Syntex (U.S.A.) Inc. Serial injection of muramyldipeptides and liposomes enhances the anti-infective activity of muramyldipeptides
DE4134467A1 (de) 1991-10-18 1993-04-22 Thomae Gmbh Dr K Heterobiarylderivate, diese verbindungen enthaltende arzneimittel und verfahren zu ihrer herstellung
AU2915892A (en) * 1991-11-14 1993-06-15 Glaxo Group Limited Piperidine acetic acid derivatives as inhibitors of fibrinogen-dependent blood platelet aggregation
WO1993014077A1 (en) 1992-01-21 1993-07-22 Glaxo Group Limited Piperidineacetic acid derivatives as inhibitors of fibrinogen-dependent blood platelet aggregation
DK0623615T3 (da) 1993-05-01 1999-12-13 Merck Patent Gmbh Adhæsionsreceptor-antagonister
US6069143A (en) 1994-12-20 2000-05-30 Smithkline Beecham Corporation Fibrinogen receptor antagonists
TR199801255T2 (xx) * 1995-12-29 1998-10-21 Smithkline Beecham Corporation Vitronektin resept�r antagonistleri.
AU1295597A (en) * 1995-12-29 1997-07-28 Smithkline Beecham Corporation Vitronectin receptor antagonists
US20010034445A1 (en) * 1995-12-29 2001-10-25 Smithkline Beecham Corporation Vitronectin receptor antagonists
WO1997026250A1 (en) 1996-01-16 1997-07-24 Merck & Co., Inc. Integrin receptor antagonists
PT796855E (pt) 1996-03-20 2002-07-31 Hoechst Ag Inibicao da reabsorcao nos ossos e antagonistas de vitronectina
JP3455229B2 (ja) * 1996-03-29 2003-10-14 ファイザー インク． ６―フェニルピリジル―２―アミン誘導体
WO1998008840A1 (en) * 1996-08-29 1998-03-05 Merck & Co., Inc. Integrin antagonists
US5952341A (en) 1996-10-30 1999-09-14 Merck & Co., Inc. Integrin antagonists
JP2001524079A (ja) 1997-04-07 2001-11-27 メルク エンド カンパニー インコーポレーテッド ガンの治療方法
AU7105498A (en) 1997-04-14 1998-11-11 Merck & Co., Inc. Combination therapy for the prevention and treatment of osteoporosis
JP2001524481A (ja) 1997-11-26 2001-12-04 デュポン ファーマシューティカルズ カンパニー αＶβ３アンタゴニストとしての１，３，４−チアジアゾール類および１，３，４−オキサジアゾール類
AU736026B2 (en) 1997-12-17 2001-07-26 Merck & Co., Inc. Integrin receptor antagonists
JP3585839B2 (ja) 1997-12-17 2004-11-04 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拮抗薬
AU738452B2 (en) 1997-12-17 2001-09-20 Merck & Co., Inc. Integrin receptor antagonists
US6048861A (en) 1997-12-17 2000-04-11 Merck & Co., Inc. Integrin receptor antagonists
US6017926A (en) 1997-12-17 2000-01-25 Merck & Co., Inc. Integrin receptor antagonists
ATE298338T1 (de) 1997-12-17 2005-07-15 Merck & Co Inc Integrin-rezeptor-antagonisten
US6329372B1 (en) 1998-01-27 2001-12-11 Celltech Therapeutics Limited Phenylalanine derivatives
WO2000006169A1 (en) 1998-07-29 2000-02-10 Merck & Co., Inc. Integrin receptor antagonists
GB9825652D0 (en) 1998-11-23 1999-01-13 Celltech Therapeutics Ltd Chemical compounds
CZ20012212A3 (cs) 1998-12-19 2001-09-12 Merck Patent Gmbh Peptidická sloučenina, její použití a farmaceutický prostředek, který ji obsahuje
EP1150965A4 (en) 1999-02-03 2002-05-15 Merck & Co Inc BENZAZEPINE DERIVATIVES AS ALPHA-V INTGRIN RECEPTOR ANTAGONISTS
US6723711B2 (en) 1999-05-07 2004-04-20 Texas Biotechnology Corporation Propanoic acid derivatives that inhibit the binding of integrins to their receptors
US6518283B1 (en) 1999-05-28 2003-02-11 Celltech R&D Limited Squaric acid derivatives
AU749351B2 (en) 1999-06-02 2002-06-27 Merck & Co., Inc. Alpha V integrin receptor antagonists
CA2376077A1 (en) 1999-06-23 2000-12-28 Merck & Co., Inc. Integrin receptor antagonists
DE19933173A1 (de) 1999-07-15 2001-01-18 Merck Patent Gmbh Cyclische Peptidderivate als Inhibitoren des Integrins alpha¶v¶beta¶6¶
US6514964B1 (en) 1999-09-27 2003-02-04 Amgen Inc. Fused cycloheptane and fused azacycloheptane compounds and their methods of use
GB9929988D0 (en) 1999-12-17 2000-02-09 Celltech Therapeutics Ltd Chemical compounds
WO2001053297A1 (en) 2000-01-20 2001-07-26 Merck & Co., Inc. Alpha v integrin receptor antagonists
EP1254116A4 (en) 2000-01-24 2003-04-23 Merck & Co Inc ALPHA V INTEGRIN RECEPTOR ANTAGONISTS
WO2001096334A2 (en) 2000-06-15 2001-12-20 Pharmacia Corporation Heteroarylalkanoic acids as integrin receptor antagonists
DE10041423A1 (de) 2000-08-23 2002-03-07 Merck Patent Gmbh Biphenylderivate
CA2421652A1 (en) 2000-09-14 2002-03-21 Merck And Co., Inc. Alpha v integrin receptor antagonists
WO2002022616A2 (en) 2000-09-14 2002-03-21 Merck & Co., Inc. Alpha v integrin receptor antagonists
WO2002022124A1 (en) 2000-09-18 2002-03-21 Merck & Co., Inc. Treatment of inflammation with a combination of a cyclooxygenase-2 inhibitor and an integrin alpha-v antagonist
US6855722B2 (en) 2001-01-29 2005-02-15 Dimensional Pharmaceuticals, Inc. Substituted indoles and their use as integrin antagonists
DE10112771A1 (de) 2001-03-16 2002-09-26 Merck Patent Gmbh Inhibitoren des Integrins alpha¶v¶beta¶6¶
WO2002090325A2 (en) 2001-05-03 2002-11-14 Merck & Co., Inc. Benzazepinone alpha v integrin receptor antagonists
US20040043988A1 (en) 2001-06-15 2004-03-04 Khanna Ish Kurmar Cycloalkyl alkanoic acids as intergrin receptor antagonists
DE10204789A1 (de) 2002-02-06 2003-08-14 Merck Patent Gmbh Inhibitoren des Integrins alpha¶v¶beta6
AU2003259891A1 (en) 2002-08-16 2004-03-19 Janssen Pharmaceutica N.V. Piperidinyl compounds that selectively bind integrins
FI20041129A0 (fi) 2004-08-30 2004-08-30 Ctt Cancer Targeting Tech Oy Tioksotiatsolidinoniyhdisteitä lääkkeinä käytettäviksi
AR059224A1 (es) 2006-01-31 2008-03-19 Jerini Ag Compuestos para la inhibicion de integrinas y uso de estas
EP2049490A1 (en) 2006-06-09 2009-04-22 Astra Zeneca AB N-(benzoyl)-o- [2- (pyridin- 2 -ylamino) ethyl]-l-tyrosine derivatives and related compounds as a5b1 antagonists for the treatment of solid tumors
CL2008001724A1 (es) 2007-06-13 2008-08-08 Bristol Myers Squibb Co Compuestos derivados de analogos dipeptidos, inhibidores del factor de coagulacion; composicion farmaceutica que comprende a dicho compuesto; y uso del compuesto para el tratamiento de un trastorno tromboembolico, infarto de miocardio, trombosis, ate
KR101588469B1 (ko) * 2007-11-16 2016-01-25 우베 고산 가부시키가이샤 벤즈아제피논 화합물
US20120289481A1 (en) 2011-05-13 2012-11-15 O'neil Jennifer Compositions and methods for treating cancer
US8716226B2 (en) 2012-07-18 2014-05-06 Saint Louis University 3,5 phenyl-substituted beta amino acid derivatives as integrin antagonists
EP2784511A1 (en) 2013-03-27 2014-10-01 Universität Zürich Integrin alpha-v-beta6 for diagnosis/prognosis of colorectal carcinoma
GB201305668D0 (en) * 2013-03-28 2013-05-15 Glaxosmithkline Ip Dev Ltd Avs6 Integrin Antagonists
US10533044B2 (en) 2014-01-06 2020-01-14 The General Hospital Corporation Integrin Antagonists
MA39823A (fr) * 2014-04-03 2018-01-09 Janssen Pharmaceutica Nv Dérivés de pyridine macrocyclique
WO2015179823A2 (en) 2014-05-23 2015-11-26 The California Institute For Biomedical Research Lung localized inhibitors of alpha(v)beta 6
WO2016022851A1 (en) 2014-08-06 2016-02-11 Children's Medical Center Corporation Modified integrin polypeptides, modified integrin polypeptide dimers, and uses thereof
GB201417018D0 (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
GB201417094D0 (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
WO2016134223A2 (en) 2015-02-19 2016-08-25 Scifluor Life Sciences, Inc. Fluorinated tetrahydronaphthyridinyl nonanoic acid derivatives and uses thereof
RS62165B1 (sr) 2015-03-25 2021-08-31 Fujifilm Corp Postupak za proizvodnju novog jedinjenja koje sadrži azot, ili njegove soli, i njegov proizvodni intermedijer
JP2018514568A (ja) 2015-04-30 2018-06-07 サイフルーア ライフ サイエンシズ インコーポレイテッド テトラヒドロナフチリジニルプロピオン酸誘導体およびその使用法
JP2019500355A (ja) 2015-12-30 2019-01-10 セントルイス ユニバーシティ 汎インテグリンアンタゴニストとしてのメタ−アザ環式アミノ安息香酸誘導体
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
EP3481814B1 (en) 2016-07-05 2022-04-27 The Rockefeller University Tetrahydronaphthyridinepentanamide integrin antagonists
CN109996541A (zh) 2016-09-07 2019-07-09 普利安特治疗公司 N-酰基氨基酸化合物及其使用方法
JP7291624B2 (ja) 2016-11-01 2023-06-15 アローヘッド ファーマシューティカルズ インコーポレイテッド アルファ－ｖベータ－６インテグリンリガンド及びその使用
WO2018085578A1 (en) 2016-11-02 2018-05-11 Saint Louis University Integrin inhibitors in combination with an agent which interacts with a chemokine receptor
WO2018085552A1 (en) 2016-11-02 2018-05-11 Saint Louis University Integrin antagonists
RS61453B1 (sr) 2016-11-08 2021-03-31 Bristol Myers Squibb Co Amidi pirola kao inhibitori alfa v integrina
US10851098B2 (en) 2016-11-08 2020-12-01 Bristol-Myers Squibb Company Azole amides and amines as alpha v integrin inhibitors
CN110167935B (zh) 2016-11-08 2022-05-27 百时美施贵宝公司 作为αV整合素抑制剂的3-经取代的丙酸
KR102506327B1 (ko) 2016-11-08 2023-03-03 브리스톨-마이어스 스큅 컴퍼니 αV 인테그린 길항제로서의 인다졸 유도체
BR112019009129A2 (pt) 2016-11-08 2019-07-16 Bristol-Myers Squibb Company compostos mono e espirocíclicos contendo ciclobutano e azetidina como inibidores de alfa v integrina
USRE50554E1 (en) 2016-12-23 2025-08-26 Pliant Therapeutics, Inc. Amino acid compounds and methods of use
CN110177787A (zh) 2016-12-29 2019-08-27 圣路易斯大学 整合素拮抗剂
KR102605460B1 (ko) 2017-02-28 2023-11-22 모픽 테라퓨틱, 인코포레이티드 αvβ6 인테그린 억제제
MA52117A (fr) 2017-02-28 2022-04-06 Morphic Therapeutic Inc Inhibiteurs de l'intégrine (alpha-v) (bêta-6)
EP4328230A3 (en) 2018-03-07 2024-04-24 Pliant Therapeutics, Inc. Amino acid compounds and methods of use
TWI841573B (zh) 2018-06-27 2024-05-11 美商普萊恩醫療公司 具有未分支連接子之胺基酸化合物及使用方法
WO2020009889A1 (en) 2018-07-03 2020-01-09 Saint Louis University ALPHAvBETA1 INTEGRIN ANTAGONISTS
WO2020047208A1 (en) 2018-08-29 2020-03-05 Morphic Therapeutic, Inc. Inhibitors of (alpha-v)(beta-6) integrin
RS66733B1 (sr) 2018-08-29 2025-05-30 Morphic Therapeutic Inc Inhibitori alfa v beta6 integrina
EP3843728B1 (en) 2018-08-29 2025-04-30 Morphic Therapeutic, Inc. Inhibitors of (alpha-v)(beta-6) integrin
CN112805001B (zh) 2018-08-29 2024-07-23 莫菲克医疗股份有限公司 抑制αvβ6整联蛋白
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
EP3952902A4 (en) 2019-04-08 2022-12-21 Pliant Therapeutics, Inc. DOSAGE FORMS AND THERAPY SCHEMES FOR AMINO ACID COMPOUNDS

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2001503060A (ja) 1996-10-30 2001-03-06 メルク エンド カンパニー インコーポレーテッド インテグリン拮抗薬
JP2015524412A (ja) 2012-07-18 2015-08-24 セントルイス ユニバーシティ インテグリンアンタゴニストとしてのβアミノ酸誘導体

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2021535141A (ja) * 2018-08-29 2021-12-16 モーフィック セラピューティック，インコーポレイテッド αｖβ６インテグリンの阻害
JP7540998B2 (ja) 2018-08-29 2024-08-27 モーフィック セラピューティック，インコーポレイテッド αｖβ６インテグリンの阻害

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