CN104640857B - 作为整合素拮抗剂的β氨基酸衍生物 - Google Patents

作为整合素拮抗剂的β氨基酸衍生物 Download PDF

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CN104640857B
CN104640857B CN201380048418.3A CN201380048418A CN104640857B CN 104640857 B CN104640857 B CN 104640857B CN 201380048418 A CN201380048418 A CN 201380048418A CN 104640857 B CN104640857 B CN 104640857B
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CN104640857A (zh
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P·卢明斯基
D·格里格斯
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St Louis University
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CN201380048418.3A 2012-07-18 2013-07-17 作为整合素拮抗剂的β氨基酸衍生物 Expired - Fee Related CN104640857B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201261673058P 2012-07-18 2012-07-18
US61/673,058 2012-07-18
US201361764443P 2013-02-13 2013-02-13
US61/764,443 2013-02-13
PCT/US2013/050917 WO2014015054A1 (en) 2012-07-18 2013-07-17 Beta amino acid derivatives as integrin antagonists

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US (1) US9085606B2 (https=)
EP (1) EP2875021B1 (https=)
JP (1) JP6215324B2 (https=)
KR (1) KR20150038185A (https=)
CN (1) CN104640857B (https=)
AU (1) AU2013292580B2 (https=)
CA (1) CA2878469A1 (https=)
ES (1) ES2647585T3 (https=)
IL (1) IL236688B (https=)
IN (1) IN2015DN00099A (https=)
MX (1) MX2015000794A (https=)
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WO2015048819A1 (en) 2013-09-30 2015-04-02 The Regents Of The University Of California Anti-alphavbeta1 integrin compounds and methods
CA2981371A1 (en) * 2015-03-10 2016-09-15 The Regents Of The University Of California Anti-alphavbeta1 integrin inhibitors and methods of use
WO2016154369A1 (en) * 2015-03-26 2016-09-29 Merck Sharp & Dohme Corp. Composition and methods for treating chronic kidney disease
BR112018012981A2 (pt) * 2015-12-30 2018-12-04 Saint Louis University derivados do ácido meta-azacíclico amino benzoico como antagonistas de pan integrina com melhores propriedades farmacocinéticas
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
CN110177787A (zh) * 2016-12-29 2019-08-27 圣路易斯大学 整合素拮抗剂
MA52117A (fr) 2017-02-28 2022-04-06 Morphic Therapeutic Inc Inhibiteurs de l'intégrine (alpha-v) (bêta-6)
MA47697A (fr) * 2017-02-28 2020-01-08 Morphic Therapeutic Inc Inhibiteurs de l'(alpha-v)(bêta-6) intégrine
CN109879969B (zh) * 2017-12-06 2024-04-09 天士力生物医药股份有限公司 一种hm-3融合蛋白及其应用
PL3761980T3 (pl) * 2018-03-07 2024-06-10 Pliant Therapeutics, Inc. Związki aminokwasowe i sposoby zastosowania
EP4086254B1 (en) 2018-08-29 2024-12-18 Morphic Therapeutic, Inc. Integrin inhibitors
FI3844162T3 (fi) 2018-08-29 2025-03-27 Morphic Therapeutic Inc Alfa v beeta6 -integriinin estäjiä
WO2020047208A1 (en) 2018-08-29 2020-03-05 Morphic Therapeutic, Inc. Inhibitors of (alpha-v)(beta-6) integrin
US11419869B2 (en) 2019-04-08 2022-08-23 Pliant Therapeutics, Inc. Dosage forms and regimens for amino acid compounds
CN110974938A (zh) * 2019-12-02 2020-04-10 上海长海医院 整合素α1β1抑制剂在制备预防或治疗主动脉疾病药物中的应用
EP4151632A4 (en) * 2020-05-14 2024-04-24 UBE Corporation 1, 4, 5, 6-tetrahydropyrimidine-2-amine derivative
US20250049806A1 (en) * 2021-11-12 2025-02-13 Ube Corporation Pharmaceutical composition for providing treatment for or preventing alport syndrome
WO2024262620A1 (ja) 2023-06-22 2024-12-26 株式会社抗体医学研究所 インテグリン阻害低分子化合物

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1201454A (zh) * 1995-08-30 1998-12-09 G·D·瑟尔公司 间－胍基、脲基、硫脲基或氮杂环氨基苯甲酸衍生物用作整合素拮抗剂
WO2004060376A1 (en) * 2002-12-20 2004-07-22 Pharmacia Corpration The r-isomer of beta amino acid compounds as integrin receptor antagonists derivatives

Family Cites Families (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5639765A (en) 1995-01-17 1997-06-17 G. D. Searle & Co. Guanidinoalkyl glycine β-amino acids useful for inhibiting bone loss
US5602155A (en) 1995-01-17 1997-02-11 G. D. Searle & Co. Platelet aggregation inhibitors
US5681820A (en) 1995-05-16 1997-10-28 G. D. Searle & Co. Guanidinoalkyl glycine β-amino acids useful for inhibiting tumor metastasis
US6013651A (en) 1995-08-30 2000-01-11 G. D. Searle & Co. Meta-azacyclic amino benzoic acid compounds and derivatives thereof
CA2250698A1 (en) 1996-03-29 1997-10-09 G.D. Searle & Co. Para-substituted phenylpropanoic acid derivatives as integrin antagonists
DE69713582T2 (de) 1996-03-29 2003-01-09 G.D. Searle & Co., Chicago Zimtsäurederivate und deren verwendung als integrin-antagonisten
PT889877E (pt) 1996-03-29 2002-02-28 Searle & Co Derivados fenileno meta substituidos e sua utilizacao como antagonitas ou inibidores integrina alfa v beta3
JP2000514809A (ja) 1996-07-12 2000-11-07 ジー．ディー．サール アンド カンパニー キラルβ―アミノ酸の不斉合成
ZA991107B (en) 1998-03-04 2000-02-14 Searle & Co Process for preparing 3-hydroxy-5-[(1,4,5,6-tetrahydro-5-hydroxy-2-pyrimidinyl)amino] benzoic acid.
US6372719B1 (en) 1998-03-04 2002-04-16 Jay Cunningham ανβ3 integrin antagonists in combination with chemotherapeutic agents
ZA994406B (en) 1998-03-04 2000-02-11 Searle & Co Meta-azacyclic amino benzoic acid and derivatives thereof.
ZA991105B (en) 1998-03-04 2000-02-11 Searle & Co Synthesis of chiral beta-amino acids.
CZ20003672A3 (cs) 1998-04-10 2001-08-15 G. D. Searle & Co. Heterocyklické glycyl-beta-alaninové deriváty jako agonisté vitronektinu
BR9916536A (pt) 1998-12-23 2002-01-02 Searle & Co Método para o tratamento ou prevenção de um distúrbio de neoplasia em um mamìfero em necessidade deste tratamento ou prevenção, e, combinação
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
US20020072500A1 (en) * 2000-09-27 2002-06-13 Thomas Rogers Hydroxy acid integrin antagonists
EP1667668B1 (en) 2003-10-01 2008-07-02 MERCK PATENT GmbH Alfavbeta3 and alfavbeta6 integrin antagonists as antifibrotic agents
TWI433839B (zh) 2006-08-11 2014-04-11 Neomed Inst 新穎的苯并咪唑衍生物290
WO2010010184A1 (en) 2008-07-25 2010-01-28 Galapagos Nv [1, 2, 4] triazolo [1, 5-a] pyridines as jak inhibitors
WO2010104933A1 (en) 2009-03-11 2010-09-16 Merck Sharp & Dohme Corp. Inhibitors of akt activity
JO3002B1 (ar) 2009-08-28 2016-09-05 Irm Llc مركبات و تركيبات كمثبطات كيناز بروتين
US8580829B2 (en) 2010-08-26 2013-11-12 Boehringer Ingelheim International Gmbh Oxadiazole inhibitors of leukotriene production

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1201454A (zh) * 1995-08-30 1998-12-09 G·D·瑟尔公司 间－胍基、脲基、硫脲基或氮杂环氨基苯甲酸衍生物用作整合素拮抗剂
WO2004060376A1 (en) * 2002-12-20 2004-07-22 Pharmacia Corpration The r-isomer of beta amino acid compounds as integrin receptor antagonists derivatives

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
Ligands to the integrin receptor αvβ3;Mark E Duggan 等;《Expert Opinion on Therapeutic Patents》;20001231;第10卷(第9期);1367-1383 *
REGISTRY;STN;《STN REGISTRY》;20110325;第1-3页 *
R-Isomers of Arg-Gly-Asp (RGD) mimics as potent avb3 inhibitors;Srinivasan R. Nagarajan等;《Bioorganic & Medicinal Chemistry》;20070315;第15卷;3783–3800 *

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CN104640857A (zh) 2015-05-20
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