发明名称 Carbamoylphosphonates as inhibitors and uses thereof
摘要 The present invention relates to novel metalloproteinase inhibitors having an aryloxybenzenesulfonamide moiety and a carbamoylphosphonic acid moiety, to pharmaceutical compositions comprising them, and to their uses in the prevention and/or treatment of disease or disorder associated with MMP.
申请公布号 US8993544(B2) 申请公布日期 2015.03.31
申请号 US201013148421 申请日期 2010.02.09
申请人 Yissum Research Development Company of the Hebrew University of Jerusalem, Ltd. 发明人 Breuer Eli;Reich Reuven;Frant Julia;Hoffman Amnon;Ainelly Veerendhar
分类号 A61K31/662;C07F9/44;C07F9/38;C07F9/40 主分类号 A61K31/662
代理机构 Browdy and Neimark, PLLC 代理人 Browdy and Neimark, PLLC
主权项 1. A compound defined by formula (II):wherein L is a C1-C10-alkylene, being optionally substituted with A; X1 is at least one substituent selected from —H; halo; —C1-C6-alkyl; —C2-C6-alkenyl; —C2-C6-alkynyl; —C3-C6-cycloalkyl; —C6-C10-aryl; —CF3; —OH; —O—C1-C6-alkyl; —NO2; —NHC(O)R3; and —NR′R″, each of said R′ and R″ independently of each other is selected from —H and —C1-C6-alkyl; each of R1 and R2, independently of each other, is selected from —H, —C1-C6-alkyl, —CR4R5—O—(O)C—C1-C6-alkyl and a cation; R3 is selected from —C1-C6-alkyl; —C2-C6-alkenyl; —C2-C6-alkynyl; —C3-C6-carbocyclic rings; —O—C1-C6-alkyl; —CF3; and —C6-C10-aryl; each of R4 and R5, independently of each other, is selected from —H and C1-C6-alkylene; and A is selected from —H; halo; C1-C6-alkyl; —C2-C6-alkenyl; —C2-C6-alkynyl; —C3-C6-cycloalkyl; —CF3; —C6-C10-aryl; OH; —O—C1-C6-alkyl; —NO2; —N3, and —NR′R″, wherein each of said R′ and R″ independently of each other is selected from —H, —C1-C6-alkyl and —C(O)O-t-Bu.
地址 Jerusalem IL