发明名称 CYCLOSPORIN ANALOGS
摘要 Disclosed herein are novel analogs of cyclosporin, pharmaceutical compositions containing them, and methods for their use in the treatment of dry eye and other conditions.
申请公布号 US2017029469(A1) 申请公布日期 2017.02.02
申请号 US201615290171 申请日期 2016.10.11
申请人 Allergan, Inc. 发明人 Frydrych Catherine Simone Victoire;Carling William Robert;Garst Michael E.;Stern Michael E.;Schaumburg Christopher S.
分类号 C07K7/64 主分类号 C07K7/64
代理机构 代理人
主权项 1. A compound of formula (I):wherein: A is —CH═CHR, —CH═CH—CH═CHR or —CH2CH2R, wherein R is —CH3; —CH2SH; —CH2-carboxyl; carboxyl; wherein R10 is C1-C6 alkyl; or wherein R11 is C1-C6 alkyl; B is —CH2CH3, 1-hydroxyethyl, isopropyl, or n-propyl; C is isobutyl, 2-hydroxyisobutyl, or 1-methylpropyl; D is —CH3 or —CH2OH; R1 and R2, which are identical or different, each represents hydrogen or C1-C4 alkyl, or together represent C3-C7 cycloalkyl; X is S or —S(O)n, wherein n is 1 or 2; R3 is hydrogen; straight or branched C1-C6 alkyl; straight or branched C2-C6 alkenyl; straight or branched C2-C6 alkynyl; C3-C7 cycloalkyl; C4-C7 heterocyclyl having 1-3 heteroatoms selected from N, O and S; aryl; heteroaryl; and wherein R3 is optionally substituted with one or more groups, which are identical or different, selected from C1-C6 alkyl; halogen; hydroxyl; alkoxycarbonyl; carboxyl; cycloalkyl; saturated or partially unsaturated 5- or 6-member heterocyclyl having 1 to 3 heteroatoms selected from N, O and S, which heterocyclyl is optionally substituted by one or more groups selected from O1—C6 alkyl; aryl; heteroaryl; amino; monoalkylamino; dialkylamino; amidino; guanidine; and urea; or a pharmaceutically acceptable salt thereof.
地址 Irvine CA US