发明名称 Beta-Arrestin Effectors And Compositions And Methods Of Use Thereof
摘要 This application describes a family of compounds acting as β-arrestin effectors. Such compounds may provide significant therapeutic benefit in the treatment of chronic and acute cardiovascular diseases.
申请公布号 US2015166604(A1) 申请公布日期 2015.06.18
申请号 US201514631461 申请日期 2015.02.25
申请人 Trevena, Inc. 发明人 Yamashita Dennis;Chen Xiao-Tao
分类号 C07K7/06;A61K38/08 主分类号 C07K7/06
代理机构 代理人
主权项 1. A method of treating a cardiovascular disorder in a subject, the method comprising administering to the subject a pharmaceutical composition comprising a peptide, or a pharmaceutically acceptable salt thereof, comprising the sequence of:Xx-Yy-Val-Ww-Zz-Aa-Bb-Cc, wherein Xx is selected from the group consisting of sarcosine, N-methyl-L-alanine, N-methyl-D-alanine, N,N-dimethylglycine, L-aspartic acid, D-aspartic acid, L-glutamic acid, D-glutamic acid, N-methyl-L-aspartic acid, N-methyl-L-glutamic acid, pyrrolid-1-ylacetic acid, and morpholin-4-ylacetic acid; Yy is selected from the group consisting of L-arginine, and L-lysine; Ww is selected from the group consisting of L-isoleucine, glycine, L-tyrosine, O-methyl-L-tyrosine, L-valine, L-phenylalanine, 3-hydroxy-L-tyrosine, 2,6-dimethyl-L-tyrosine, 3-fluoro-L-tyrosine, 4-fluorophenyl-L-analine, 2,6-difluoro-L-tyrosine, 3-nitro-L-tyrosine, 3,5-dinitro-L-tyrosine, 3,5-dibromo-L-tyrosine, 3-chloro-L-tyrosine, O-allyl-L-tyrosine, and 3,5-diiodo-L-tyrosine; Zz is selected from the group consisting of L-isoleucine, L-valine, L-tyrosine, L-glutamic acid, L-phenylalanine, L-histidine, L-lysine, L-arginine, O-methyl-L-threonine, D-alanine, and L-norvaline; Aa is selected from the group consisting of L-histidine, L-histidine-amide, and L-lysine; Bb is selected from the group consisting of L-proline, L-proline-amide, D-proline, and D-proline-amide; and Cc is selected from the group consisting of null, L-isoleucine, L-isoleucine-amide, glycine, glycine-amide, L-alanine, L-alanine-amide, D-alanine, D-phenylalanine, L-norvaline; provided that when Xx is L-Aspartic acid, Cc is not L-phenylalanine; when Xx is sarcosine, Cc is not L-isoleucine; when Ww is glycine, Cc is not glycine; when Xx is sarcosine, and Zz is L-valine, Cc is not L-alanine; and when Xx is sarcosine, Ww is a L-tyrosine, and Zz is L-isoleucine, Cc is not L-alanine.
地址 King of Prussia PA US