发明名称 Cyclosporin A analogs
摘要 The present invention relates to novel cyclosporin analogs, processes for preparing them, pharmaceutical compositions containing them, and methods for using these analogs and the compositions containing them for the treatment of medical conditions, including but not limited to ocular conditions such as dry eye.
申请公布号 US9266927(B2) 申请公布日期 2016.02.23
申请号 US201313905491 申请日期 2013.05.30
申请人 Allergan, Inc. 发明人 Pettit Simon N.;Jones Andrew D.;Frydrych Catherine Simone V.;Carling William R.;Garst Michael E.
分类号 A61K38/13;C07K7/64;A61K38/00 主分类号 A61K38/13
代理机构 代理人 Potts Barbara C.
主权项 1. A compound having Formula I: or a pharmaceutically acceptable salt thereof, wherein: R1 is —H, —C1-6alkyl, —OC1-6alkyl, —CH2F, —CH2OCH3, —SC1-6alkyl, —R13R14, R2 is —CH3, —CH2CH3 or —CH2CH2CH3; R3 is —CH2CH(CH3)2, —CH(CH3)2, —CH2C(CH3)2(OH), —CH(CH3)(CH2CH3) or —CH2CH(R7)(CH2CH3); R4 is —CH3 or —CH2OH; R5 is —R8(CH2)n(C═O)m—; R6 is —CH2CH3, —CH(CH3)(OH), —CH(CH3)2 or —CH2CH2CH3; R7 is OC1-5 alkyl; R8 is O, S, CH2O, CH2S or CH2; R9, R10, R11, and the N to which R9 and R10 are attached, together form a monocyclic or polycyclic non-aromatic heterocycle, wherein said heterocycle is optionally interrupted by a C═O, and the S and N atoms are optionally oxidized, and wherein said heterocycle is optionally substituted with halogen, nitro, cyano, —OC1-6 alkyl, —SC1-6 alkyl, —C1-6 alkyl, —C2-6 alkenyl, —C2-6 alkynyl, carboxylic acid, ester, ketone, aldehyde, amide, amine, sulfonamide, C3-8 cycloalkyl, hydroxyl or haloalkyl; R13 is O, S, CH2O, CH2S, CH2SO or CH2SO2; R14 is H, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C3-8cycloalkyl, CH2CH2N(CH2CH3)2, CH2CH2NH(CH2CH3), heterocycle or aryl; n is 0, 1, 2, 3 or 4; m is 0 or 1; and p is 1; wherein R14 is optionally substituted with one or more groups independently selected from the group consisting of H, C1-6alkyl, halogen, hydroxyl, ester, sulfonamide, ketone, aldehyde, cycloalkyl, heterocycle, aryl, amine, heterocycle, amide and guanidinyl; and wherein “- - - - - -” is a single bond.
地址 Irvine CA US