发明名称 Use of arylpiperazines as metalloproteinase inhibiting agents (MMP)
摘要 A method of treating a metalloproteinase mediated disease condition such as arthritis or atherosclerosis comprises administering to a non human mammal an arylpiperazine derivative or a pharmaceutically acceptable salt or ester of the formula (I) wherein: Ring A is a optionally substituted 5-7 membered aliphatic ring; Ring B is a monocyclic or bicyclic alkyl, aryl, aralkyl, heteroaryl or heteroalkyl containing one or more heteroatoms of N, S or O or is biphenyl or ring B can be linked to ring A with alkyl or alkoxy chain linking the 2-position of ring B with the carbon atom a to X2; each R3 is H, halogen, NO2, COOR, CN, CF3, alkyl, S-alkyl, SO-alkyl, SO2-alkyl, alkoxy, aryloxy; n1 is 1 to 3; R is H or alkyl; P is -(CH2)n2-, alkene or alkyne chain or when X2 is carbon P may be Het, -(CH[R6])n3-Het, Het-(CH[R6])n3- or Het-(CH[R6])n3-Het; or P is -CON(R6)-, -N(R6)-CO-, -SO2-N(R6)- or -N(R6)-SO2; Het is CO, S, SO, SO2, NR6 or O; n3 is 1 or 2; X1 and X2 are independently nitrogen or carbon; Y is -SO2- or -CO-; Z is -CONHOH, Y is CO and Q is -C(R6)(R7)-, -C(R6)(R7)-CH2, N(R6)- or -N(R6)-CH2- or Z is -CONHOH, Y is SO2 and Q is -C(R6)(R7)- or -C(R6)(R7)-CH2 or Z is -N(OH)-CHO and Q is -C(R6)(R7)-, -C(R6)(R7)-CH2 or -N(R6)-CH2-; R1 is H or optionally substituted alkyl, cycloalkyl, aryl, heteroaryl, aralkyl, heteroarylalkyl or is 2,3,4,5,6-pentafluorophenyl provided that where R1 is substituted by OH, OR4 or -N-Y-R4 Z is not -N(OH)-CHO; R2 is H, alkyl or together with R1 can form a carbocyclic or heterocyclic spiro 5 to 7 membered ring with the heterocyclic ring containing at least one heteroatom of N, S or O; Q can also be linked to either R1 or R2 to form a 5 to 7 membered alkyl or heteroalkyl ring comprising one or more of O, S or N and R4, R6 and R7 are as defined in the specification. (62) Divided out of 509730
申请公布号 NZ524921(A) 申请公布日期 2004.10.29
申请号 NZ19990524921 申请日期 1999.08.25
申请人 ASTRAZENECA AB 发明人 BARLAAM, BERNARD CHRISTOPHE;NEWCOMBE, NICHOLAS JOHN;TUCKER, HOWARD;WATERSON, DAVID
分类号 C07D295/22;A61K;A61K31/44;A61K31/495;A61K31/496;A61K31/505;A61K31/506;A61P9/10;A61P19/02;A61P29/00;A61P43/00;C07D;C07D213/42;C07D213/52;C07D213/74;C07D215/12;C07D239/42;C07D241/12;C07D295/26;C07D333/20;C07D401/12;C07D409/12;C07D417/12;(IPC1-7):A61K31/44 主分类号 C07D295/22
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