发明名称 |
ALKYL-4-SILYL-PHENOLS AND ESTERS THEREOF AS ANTIATHEROSCLEROTIC AGENTS |
摘要 |
This invention relates to compounds of formula (1), wherein R1 and R6 are each independently C1-C6 alkyl; R2, R3 and R4 are each independently hydrogen or C1-C6 alkyl; R is hydrogen or -C(O)-(CH2)m-Q wherein Q is hydrogen or -COOH and m is an integer 1, 2, 3 or 4; Z is a thio, oxy or methylene group; A is a C1-C4 alkylene group; R5 and R7 are each independently a C1-C6 alkyl or -(CH2)n-(Ar) wherein n is an integer 0, 1, 2 or 3; and Ar is phenyl or naphthyl unsubstituted or substituted with one to three substituents selected from the group consisting of hydroxy, methoxy, ethoxy, halogen, trifluoromethyl, C1-C6 alkyl, or -NR8R9, wherein R8 and R9 are each independently hydrogen or C1-C6 alkyl; with the proviso that when R2 and at least one of R5 or R7 is C1-C6 alkyl, and Ar is not substituted with trifluoromethyl or -NR8R9, then R is -C(O)-(CH2)m-Q; or a pharmaceutically acceptable salt thereof; useful for the treatment of atherosclerosis and chronic inflammatory disorders; for inhibiting cytokine-induced expression of VCAM-1 and/or ICAM-1; for inhibiting the peroxidation of LDL lipid; for lowering plasma cholesterol; and as antioxidant chemical additives useful for preventing oxidative deterioration in organic materials. |
申请公布号 |
WO9741129(A1) |
申请公布日期 |
1997.11.06 |
申请号 |
WO1997US03335 |
申请日期 |
1997.03.03 |
申请人 |
HOECHST MARION ROUSSEL, INC. |
发明人 |
BUSCH, STEVEN, J.;CHEN, KIM, S.;EDWARDS, MICHAEL, J.;MATT, JAMES, E., JR.;PARKER, ROGER, A.;VAAL, MARK, J.;WRIGHT, PAUL, S.;YATES, MARK, T. |
分类号 |
A61K31/695;A61P3/06;A61P11/06;A61P19/02;A61P29/00;A61P37/00;A61P43/00;C07F7/08;C07F7/10;C07F7/12 |
主分类号 |
A61K31/695 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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