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 |