公开(公告)号：US09637520B2

公开(公告)日：2017-05-02

申请号：US14795694

申请日：2015-07-09

申请人： POLYPHOR AG

发明人： Frank Otto Gombert ,  Alexander Lederer ,  Ralf Löwe ,  Daniel Obrecht ,  Barbara Romagnoli ,  Johann Zimmermann ,  Kalpana Patel

IPC分类号： C07K7/64 ,  A61K38/12 ,  C07K14/715 ,  C07K14/705 ,  A61K38/00 ,  A61K38/17

CPC分类号： C07K7/64 ,  A61K38/00 ,  A61K38/17 ,  A61K38/177 ,  A61K38/1793 ,  C07K14/705 ,  C07K14/715 ,  C07K14/7158

摘要： Novel template-fixed β-hairpin peptidomimetics of the general formula (I) wherein the single elements T or P are α-amino acid residues connected from the carbonyl (C═O) point of attachment to the nitrogen (N) of the next element in clockwise direction and wherein said elements, depending on their positions in the chain, are defined in the description and the claims have the property to act on the receptor CXCR7. Thus, these β-hairpin peptidomimetics can be useful in the treatment or prevention of diseases or conditions in the area of dermatological disorders, metabolic diseases, inflammatory diseases, fibrotic diseases, infectious diseases, neurological diseases, cardiovascular diseases, respiratory diseases, gastro-intestinal tract disorders, urological diseases, ophthalmic diseases, stomatological diseases, haematological diseases and cancer; or the mobilization of stem cells.

公开(公告)号：US09284352B2

公开(公告)日：2016-03-15

申请号：US14466709

申请日：2014-08-22

申请人： POLYPHOR AG

发明人： Daniel Obrecht ,  Frank Otto Gombert ,  Alexander Lederer ,  Barbara Romagnoli ,  Christian Bisang

IPC分类号： C07K7/08 ,  C07K7/02 ,  C07K1/06

CPC分类号： C07K7/08 ,  C07K1/061 ,  C07K7/02

摘要： β-Hairpin peptidomimetics of the general formula Cyclo(-Xaa1-Xaa2-Xaa3-Cys4-Xaa5-Xaa6-Xaa7-Xaa8-Arg9-Tyr10-Cys11-Xaa12-Xaa13-Xaa14-Xaa15-Xaa16-), disulfide bond between Cys4 and Cys11, and pharmaceutically acceptable salts thereof, with Xaa1, Xaa2, Xaa3, Xaa5, Xaa6, Xaa7, Xaa8, Xaa12, Xaa13, Xaa14, Xaa15 and Xaa16 being amino acid residues of certain types which are defined in the description and the claims, have CXCR4 antagonizing properties and can be used for preventing HIV infections in healthy individuals or for slowing and halting viral progression in infected patients; or where cancer is mediated or resulting from CXCR4 receptor activity; or where immunological diseases are mediated or resulting from CXCR4 receptor activity; or for treating immunosuppression; or during apheresis collections of peripheral blood stem cells and/or as agents to induce mobilization of stem cells to regulate tissue repair. These peptides can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.

摘要翻译： 通式为（Xaa1-Xaa2-Xaa3-Cys4-Xaa5-Xaa6-Xaa7-Xaa8-Arg9-Tyr10-Cys11-Xaa12-Xaa13-Xaa14-Xaa15-Xaa16-）的通式肽模拟物，Cys4之间的二硫键 和Cys11及其药学上可接受的盐与在说明书和权利要求书中定义的某些类型的氨基酸残基的Xaa1，Xaa2，Xaa3，Xaa5，Xaa6，Xaa7，Xaa8，Xaa12，Xaa13，Xaa14，Xaa15和Xaa16， 具有CXCR4拮抗特性，可用于预防健康个体中的HIV感染，或用于减缓和阻止感染患者的病毒进展; 或由CXCR4受体活性介导或产生癌症; 或其中免疫性疾病介导或由CXCR4受体活性产生; 或用于治疗免疫抑制; 或在外周血干细胞的分离采集期间和/或作为诱导干细胞动员以调节组织修复的试剂。 这些肽可以通过基于混合固相和溶液相合成策略的方法制造。