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公开(公告)号：US08633163B2
公开(公告)日：2014-01-21
申请号：US12524862
申请日：2007-01-29
申请人： Daniel Obrecht , Frank Gombert , Steve J. Demarco , Christian Ludin , Alexander Lederer , Christian Bisang , Odile Sellier-Kessler , Francoise Jung , Reshmi Mukherjee , Heiko Henze , Barbara Romagnoli
发明人： Daniel Obrecht , Frank Gombert , Steve J. Demarco , Christian Ludin , Alexander Lederer , Christian Bisang , Odile Sellier-Kessler , Francoise Jung , Reshmi Mukherjee , Heiko Henze , Barbara Romagnoli
IPC分类号： A61K38/00 , C07K14/72 , C07K14/705 , A61K38/04 , C07K5/00 , C07K7/00 , C07K16/00 , C07K17/00
CPC分类号： C07K7/64 , A61K38/00 , C07K5/02 , C07K5/101 , C07K5/1013 , C07K5/1016 , C07K5/1021 , C07K5/1024 , C07K7/06 , C07K7/08
摘要： Template-fixed β-hairpin peptidomimetics of the general formula (I) wherein Z is a template-fixed chain of 4 α-amino acid residues which, depending on their positions in the chain (counted starting from the N-terminal amino acid) are Gly, or of certain types which, as the remaining symbols in the above formula, are defined in the description and the claims, and salts thereof, have the property to agonize or to antagonize GPCR receptors such as CXCR3, urotensin and CCR10. They can be used as medicaments to treat or prevent diseases such as cardiovascular disorders, dermatological disorders, endocrine system and hormone disorders, metabolic diseases, inflammatory diseases, neurological diseases, respiratory diseases, haematological diseases and cancer. These β-hairpin peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.
摘要翻译： 通式（I）的模板固定的β-发夹肽模拟物，其中Z是4个α-氨基酸残基的模板固定链，其取决于其在链中的位置（从N-末端氨基酸开始计数）为 Gly或某些类型，其作为上述式中的其余符号在说明书和权利要求及其盐中定义，具有激动或拮抗GPCR受体如CXCR3，尿素调节素和CCR10的性质。 它们可以用作治疗或预防心血管疾病，皮肤病，内分泌系统和激素失调，代谢疾病，炎性疾病，神经疾病，呼吸系统疾病，血液病和癌症等疾病的药物。 这些β-发夹肽模拟物可以通过基于混合固相和溶液相合成策略的方法制备。
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公开(公告)号：US20100093644A1
公开(公告)日：2010-04-15
申请号：US12524862
申请日：2007-01-29
申请人： Daniel Obrecht , Frank Gombert , Steve J. Demarco , Christian Ludin , Alexander Lederer , Christian Bisang , Odile Sellier-Kessler , Francoise Jung , Reshmi Mukherjee , Heiko Henze , Barbara Romagnoli
发明人： Daniel Obrecht , Frank Gombert , Steve J. Demarco , Christian Ludin , Alexander Lederer , Christian Bisang , Odile Sellier-Kessler , Francoise Jung , Reshmi Mukherjee , Heiko Henze , Barbara Romagnoli
CPC分类号： C07K7/64 , A61K38/00 , C07K5/02 , C07K5/101 , C07K5/1013 , C07K5/1016 , C07K5/1021 , C07K5/1024 , C07K7/06 , C07K7/08
摘要： Template-fixed β-hairpin peptidomimetics of the general formula (I) wherein Z is a template-fixed chain of 4 α-amino acid residues which, depending on their positions in the chain (counted starting from the N-terminal amino acid) are Gly, or of certain types which, as the remaining symbols in the above formula, are defined in the description and the claims, and salts thereof, have the property to agonize or to antagonize GPCR receptors such as CXCR3, urotensin and CCR10. They can be used as medicaments to treat or prevent diseases such as cardiovascular disorders, dermatological disorders, endocrine system and hormone disorders, metabolic diseases, inflammatory diseases, neurological diseases, respiratory diseases, haematological diseases and cancer. These β-hairpin peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.
摘要翻译： 通式（I）的模板固定和半乳糖肽模拟物，其中Z是4个α-氨基酸残基的模板固定链，其取决于其在链中的位置（从N-末端氨基酸开始计数） 是Gly，或某些类型，其作为上述式中的其余符号在说明书和权利要求书及其盐中定义，具有激动或拮抗GPCR受体如CXCR3，尿素调节素和CCR10的性质。 它们可以用作治疗或预防心血管疾病，皮肤病，内分泌系统和激素失调，代谢疾病，炎性疾病，神经疾病，呼吸系统疾病，血液病和癌症等疾病的药物。 这些可以通过基于混合固相和溶液相合成策略的方法制造。
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公开(公告)号：US20110230426A1
公开(公告)日：2011-09-22
申请号：US13057932
申请日：2008-08-08
申请人： Daniel Obrecht , Frank Gombert , Markus Seitz , Ludovic T. Maillard , Roba Mounme , Kerstin Moehle , John Anthony Robinson , Odile Sellier-Kessler , Heiko Henze , Christian Bisang , Alexander Lederer
发明人： Daniel Obrecht , Frank Gombert , Markus Seitz , Ludovic T. Maillard , Roba Mounme , Kerstin Moehle , John Anthony Robinson , Odile Sellier-Kessler , Heiko Henze , Christian Bisang , Alexander Lederer
IPC分类号： A61K38/12 , C07K7/64 , C07K1/00 , A61P3/10 , A61P29/00 , A61P13/12 , A61P9/00 , A61P11/06 , A61P11/02 , A61P11/00
摘要： Template-fixed β-hairpin peptidomimetics of the general formula wherein Z is a template-fixed chain of 8 α-amino acid residues which, depending on their positions in the chain (counted starting from the N-terminal amino acid), are Gly or Pro or of certain types which, as the remaining symbols in the above formula, are defined in the description and the claims, and salts thereof, have agonizing or antagonizing activity against urotensin II or show inhibition of the STAT6/NCoA-1 interaction and can be used for preventing or treating diseases or disorders related to urotensin II, STAT6 and NCoA-1.These β-hairpin peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.
摘要翻译： 模板固定和通用拟肽模拟物，其中Z是8个α-氨基酸残基的模板固定链，取决于它们在链中的位置（从N-末端氨基酸开始计数）是Gly 或Pro或某些类型，其作为上述公式中的其余符号在说明书和权利要求书及其权利要求书中定义及其盐具有对泌尿生长因子II的激动或拮抗作用或显示STAT6 / NCoA-1相互作用的抑制， 可用于预防或治疗与泌尿前列腺素II，STAT6和NCoA-1相关的疾病或病症。 这些可以通过基于混合固相和溶液相合成策略的方法制造。
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