申请人:American Home Products Corporation
公开号:US05968975A1
公开(公告)日:1999-10-19
This invention relates to the treatment of atherosclerosis via raising the level of HDL cholesterol by administration of a compound of the formula ##STR1## wherein: R.sup.1, R.sup.2, and R.sup.3 are independently hydrogen, C.sub.1 -C.sub.6 alkyl or --(CH.sub.2).sub.0-6 Ph where Ph is phenyl optionally substituted by halogen, cyano, nitro, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, trifluoromethyl, C.sub.1 -C.sub.6 alkoxycarbonyl, --CO.sub.2 H or OH; R.sup.4 and R.sup.5 are independently hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.8 cycloalkyl, or --(CH.sub.2).sub.0-6 Ar.sup.1 where Ar.sup.1 is phenyl, naphthyl, furanyl, pyridinyl or thienyl and Ar.sup.1 can be optionally substituted by halogen, cyano, nitro, C.sub.1 -C.sub.6 alkyl, phenyl, C.sub.1 -C.sub.6 alkoxy, phenoxy, trifluoromethyl, C.sub.1 -C.sub.6 alkoxycarbonyl, --CO.sub.2 H or OH; and Ar is phenyl, naphthyl, furanyl, pyridinyl or thienyl or Ar is optionally substituted by halogen, cyano, nitro, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl, phenyl, C.sub.1 -C.sub.6 alkoxy, phenoxy, trifluoromethyl, C.sub.1 -C.sub.6 alkoxycarbonyl, --CO.sub.2 H or OH.
本发明涉及通过给予一个公式为##STR1##的化合物来提高HDL胆固醇水平从而治疗动脉粥样硬化,其中:R.sup.1、R.sup.2和R.sup.3独立地是氢、C.sub.1 -C.sub.6烷基或--(CH.sub.2).sub.0-6苯基,其中Ph是苯基,可以选择性地被卤素、氰基、硝基、C.sub.1 -C.sub.6烷基、C.sub.1 -C.sub.6烷氧基、三氟甲基、C.sub.1 -C.sub.6烷氧羰基、--CO.sub.2 H或OH取代;R.sup.4和R.sup.5独立地是氢、C.sub.1 -C.sub.6烷基、C.sub.3 -C.sub.8环烷基,或--(CH.sub.2).sub.0-6 Ar.sup.1,其中Ar.sup.1是苯基、萘基、呋喃基、吡啶基或噻吩基,Ar.sup.1可以选择性地被卤素、氰基、硝基、C.sub.1 -C.sub.6烷基、苯基、C.sub.1 -C.sub.6烷氧基、苯氧基、三氟甲基、C.sub.1 -C.sub.6烷氧羰基、--CO.sub.2 H或OH取代;Ar是苯基、萘基、呋喃基、吡啶基或噻吩基,或Ar可以选择性地被卤素、氰基、硝基、C.sub.1 -C.sub.6烷基、C.sub.3 -C.sub.6环烷基、苯基、C.sub.1 -C.sub.6烷氧基、苯氧基、三氟甲基、C.sub.1 -C.sub.6烷氧羰基、--CO.sub.2 H或OH取代。