CN109071602B - 靶向α4β7整联蛋白的环肽 - Google Patents

靶向α4β7整联蛋白的环肽 Download PDF

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CN109071602B
CN109071602B CN201680079148.6A CN201680079148A CN109071602B CN 109071602 B CN109071602 B CN 109071602B CN 201680079148 A CN201680079148 A CN 201680079148A CN 109071602 B CN109071602 B CN 109071602B
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CN109071602A (zh
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曼努埃尔·佩雷斯·巴斯克斯
M·莫讷祖尔·穆尔希德
珍妮弗·L·希基
阿达姆·保罗·卡法尔
詹姆斯·吉尔拉德
纳伦德拉·帕特尔
赛·库马尔·茶卡
安德鲁·L·拉夫顿
马克-安德·普帕特
杨高强
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Universite de Montreal
Zealand Pharma AS
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CN201680079148.6A 2015-11-11 2016-11-14 靶向α4β7整联蛋白的环肽 Active CN109071602B (zh)

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US201562254003P 2015-11-11 2015-11-11
US62/254,003 2015-11-11
PCT/CA2016/000274 WO2017079820A1 (en) 2015-11-11 2016-11-14 CYCLIC PEPTIDES TARGETING α4β7 INTEGRIN

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CN109071602B true CN109071602B (zh) 2022-09-13

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Families Citing this family (9)

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Publication number Priority date Publication date Assignee Title
CA3004641A1 (en) 2015-11-11 2017-05-18 Encycle Therapeutics, Inc. Cyclic peptides targeting .alpha.4.beta.7 integrin
JP7035044B2 (ja) 2016-11-11 2022-03-14 ジーランド ファーマ エー／エス α４β７インテグリンを標的とする環状ペプチド多量体
EP3621980A4 (en) * 2017-05-10 2021-06-30 Zealand Pharma A/S HOMODETIC CYCLIC PEPTIDES TARGETING INTEGRIN ALPHA4 BETA7
CN110551178B (zh) * 2018-06-01 2020-07-21 深圳翰宇药业股份有限公司 一种含脯氨酸的首尾环肽合成方法
WO2020185999A1 (en) * 2019-03-14 2020-09-17 Genentech, Inc. Cyclic peptide antibiotics
EP4101929A4 (en) * 2019-12-27 2024-05-22 The University of Tokyo BANK CONSTRUCTION METHOD, CYCLIC PEPTIDE, FXIIA BINDER AND IFNGR1 BINDER
JP2021106565A (ja) * 2019-12-27 2021-07-29 国立大学法人 東京大学 ライブラリーの製造方法、環状ペプチド、ＦＸＩＩａ結合剤、及びＩＦＮＧＲ１結合剤
US20230295235A1 (en) 2020-06-29 2023-09-21 Zealand Pharma A/S Compounds targeting alpha4-beta7 integrin
IL313590A (en) 2021-12-20 2024-08-01 Zealand Pharma As Compounds

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3219113A1 (de) * 1982-05-21 1983-11-24 Bayer Ag, 5090 Leverkusen Verwendung von n-substituierten 2,3-diaminocarbonsaeuren in arzneimitteln und ihre herstellung
US5296604A (en) * 1992-05-15 1994-03-22 Miles Inc. Proline derivatives and compositions for their use as inhibitors of HIV protease
WO2009141687A1 (en) * 2008-05-22 2009-11-26 Centre National De La Recherche Scientifique (Cnrs) New optically pure compounds for improved therapeutic efficiency
US20100093612A1 (en) * 2007-02-21 2010-04-15 Giovanni Casiraghi Integrin targeted cyclopeptide ligands, their preparation and use
WO2010107832A1 (en) * 2009-03-17 2010-09-23 Bracco Imaging Spa Lhrh-ii peptide analogs
US20140023700A1 (en) * 2011-02-22 2014-01-23 Leo Pharma A/S Cyclic peptide and conjugate thereof for binding to keratinocytes

Family Cites Families (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU638264B2 (en) 1989-08-10 1993-06-24 Aventis Inc. Cyclic neurokinin a antagonists
US5705481A (en) 1992-11-06 1998-01-06 Merck Patent Gesellschaft Mit Beschrankter Haftung Cyclopeptides
AU681119B2 (en) 1993-05-17 1997-08-21 Fujisawa Pharmaceutical Co., Ltd. New polypeptide compound and a process for preparation thereof
US5693325A (en) 1994-03-15 1997-12-02 Molecumetics, Ltd. Peptide vaccines and methods relating thereto
DE4415310A1 (de) 1994-04-30 1995-11-02 Merck Patent Gmbh Cyclopeptide
GB9524630D0 (en) * 1994-12-24 1996-01-31 Zeneca Ltd Chemical compounds
US5696084A (en) 1996-08-16 1997-12-09 Abbott Laboratories Amino-lipopetide antifungal agents
US6492553B1 (en) 1998-01-29 2002-12-10 Aventis Pharamaceuticals Inc. Methods for preparing N-[(aliphatic or aromatic)carbonyl)]-2-aminoaetamide compounds and for cyclizing such compounds
DE10107707A1 (de) * 2001-02-19 2002-08-29 Wilex Biotechnology Gmbh Antagonisten für alpha¶4¶beta¶7¶-Integrin
US6667407B2 (en) 2002-05-03 2003-12-23 Bayer Polymers Llc Process of making polyaziridines
CA2562411A1 (en) 2004-04-15 2005-11-10 Proteolix, Inc. Compounds for enzyme inhibition
CA2702605C (en) 2006-10-20 2015-03-24 Ryan Hili Unprotected amino aldehydes and applications for same
CN102498124B (zh) 2009-03-16 2015-05-13 多伦多大学管理委员会 环状氨基酸分子及其制备方法
WO2011124998A1 (en) 2010-04-08 2011-10-13 Pfizer Inc. Substituted 3,5- di phenyl - isoxazoline derivatives as insecticides and acaricides
US9273093B2 (en) 2012-10-11 2016-03-01 Protagonist Therapeutics, Inc. α4β7 peptide dimer antagonists
SG11201702553RA (en) 2014-10-01 2017-04-27 Protagonist Therapeutics Inc NOVEL α4β7 PEPTIDE MONOMER AND DIMER ANTAGONISTS
US10301371B2 (en) 2014-10-01 2019-05-28 Protagonist Therapeutics, Inc. Cyclic monomer and dimer peptides having integrin antagonist activity
US10281407B2 (en) 2015-11-02 2019-05-07 Jon A. Petty Multi-fluid strip test
CA3004641A1 (en) 2015-11-11 2017-05-18 Encycle Therapeutics, Inc. Cyclic peptides targeting .alpha.4.beta.7 integrin

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3219113A1 (de) * 1982-05-21 1983-11-24 Bayer Ag, 5090 Leverkusen Verwendung von n-substituierten 2,3-diaminocarbonsaeuren in arzneimitteln und ihre herstellung
US5296604A (en) * 1992-05-15 1994-03-22 Miles Inc. Proline derivatives and compositions for their use as inhibitors of HIV protease
US20100093612A1 (en) * 2007-02-21 2010-04-15 Giovanni Casiraghi Integrin targeted cyclopeptide ligands, their preparation and use
WO2009141687A1 (en) * 2008-05-22 2009-11-26 Centre National De La Recherche Scientifique (Cnrs) New optically pure compounds for improved therapeutic efficiency
WO2010107832A1 (en) * 2009-03-17 2010-09-23 Bracco Imaging Spa Lhrh-ii peptide analogs
US20140023700A1 (en) * 2011-02-22 2014-01-23 Leo Pharma A/S Cyclic peptide and conjugate thereof for binding to keratinocytes

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
A General Method for the Synthesis of (Carbamoylmethylene)amino Pseudopeptides;Suarez-gea, M, et al.;《J. Org. Chem.》;19941231;第59卷(第1期);scheme 1 *
Ce＇dric Couturier,et al..Aziridinium from N,N-Dibenzyl Serine Methyl Ester: Synthesis of Enantiomerically Pure â-Amino and r,â-Diamino Esters.《ORGANIC LETTERS》.2006,第8卷(第10期), *
Convenient Synthesis of 1,2-Diamines from β-Chloro Amines: Precursors of New Substituted Piperazin-2-ones;Soumaya Slama,et al.;《Synthetic Communications》;20131231(第43期);第2286页 *
Second generation, arginine-rich (R–X0–R)4-type cell-penetrating a–x–a-peptides with constrained, chiral x-amino acids (X0) for enhanced cargo delivery into cells;Kiran M. Patil;《Bioorganic & Medicinal Chemistry Letters》;20140719;第4198–4202页 *

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