发明名称 Cyclic depsipeptide compounds and their uses
摘要 The present invention relates to novel cycloundecadepsipeptide compounds and their analoges which bind and inhibit cyclophilins, have reduced immunosuppressive activity and improved physicochemical properties including water solubility. The present invention further relates to pharmaceutical compositions containing said depsipeptide compounds and their analoges for use in the treatment or prevention of diseases and pathologies which may be ameliorated by the inhibition of cyclophilin activity.
申请公布号 US9382295(B2) 申请公布日期 2016.07.05
申请号 US201314433327 申请日期 2013.10.02
申请人 Cypralis Limited 发明人 Fliri Hans Georg;Ford Rhonan Lee;Vong Antonio Kuok Keong
分类号 A61K38/12;C07K11/02;C07K7/56;A61K38/00 主分类号 A61K38/12
代理机构 McCarter & English, LLP 代理人 McCarter & English, LLP ;Davis Steven G.;Bai Mei
主权项 1. A compound having the formula (1): or a pharmaceutically acceptable salt, tautomer or N-oxide thereof, wherein L represents a bond or an optionally substituted, optionally partially unsaturated chain of 1-6 carbon atoms with optional additional heteroatoms atoms in the chain, and may be optionally branched and optionally linked to R1 to form a ring structure containing one or more nitrogen atoms, Q represents a primary, secondary or tertiary covalent bond, a carbonyl group and optionally a linking group to R1, R1 and R2 may be absent or independently represent H, alkyl, substituted alkyl, optionally substituted cycloalkyl, optionally substituted aryl, optionally substituted heteroaryl, —COR3, —CO2R3, —OR4, —NR4R5, CONR4R5, —C(═NR6)NR4R5, —C(═NR6)OR3 and optionally R1 and R2 may together with the nitrogen atom to which they are attached form a 4-7 membered aryl, cycloalkyl or heterocyclic ring which may be further fused or optionally substituted, R3 represents alkyl, substituted alkyl, cycloalkyl, optionally substituted aryl, or optionally substituted heteroaryl, R4 and R5 independently represent H, alkyl, substituted alkyl, cycloalkyl, optionally substituted aryl, or optionally substituted heteroaryl and optionally R4 and R5 may together with the nitrogen atom to which they are attached form a 4-7 membered aryl, cycloalkyl or heterocyclic ring which may be further fused or optionally substituted, R6 represents H, alkyl, substituted alkyl, cycloalkyl, optionally substituted aryl, or optionally substituted heteroaryl, X represents H, OH, OC(═O)-alkyl, OC(═O)-substituted alkyl, O-alkyl, O-substituted alkyl, carbonyl (═O) or imine (═N—Y) where Y is —OR4 or —NR4R5, Ra represents hydrogen, alkyl, substituted alkyl, alkoxy, substituted alkoxy, alkylthio, substituted alkylthio or optionally substituted alkylene, and Rb represents hydrogen or is absent.
地址 Ongar, Essex GB