发明公开
EP0127848A2 5-Thiaalkanoic acid derivatives having antihypercholesterolemic activity
失效
具有抗高胆固醇血症活性的5-硫杂链烷酸衍生物
- 专利标题： 5-Thiaalkanoic acid derivatives having antihypercholesterolemic activity
- 专利标题（中）： 具有抗高胆固醇血症活性的5-硫杂链烷酸衍生物
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申请号： EP84105921.5申请日： 1984-05-24
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公开(公告)号： EP0127848A2公开(公告)日： 1984-12-12
- 发明人: Prugh, John D.
- 申请人： Merck & Co., Inc.
- 申请人地址： 126, East Lincoln Avenue P.O. Box 2000 Rahway New Jersey 07065-0900 US
- 专利权人： Merck & Co., Inc.
- 当前专利权人： Merck & Co., Inc.
- 当前专利权人地址： 126, East Lincoln Avenue P.O. Box 2000 Rahway New Jersey 07065-0900 US
- 代理机构： Abitz, Walter, Dr.-Ing.
- 优先权： US500606 19830602
- 主分类号： C07C149/00
- IPC分类号： C07C149/00 ; C07C147/14 ; C07C147/00 ; A61K31/19
摘要：
Derivatives of 3-hydroxy-5-thia-ω-aryl-alkanoic acids are disclosed having the structural formula:
wherein Z is:
n is 0, 1 or 2;
E is -CH 2 - -CH 2 -CH 2 -, -CH 2 -CH 2 -CH 2 -, -CH=CH-CH 2 -: or -CH 2 -CH=CH-;
R,, R 2 and R 3 are, e.g.. hydrogen, chloro, bromo, fluoro, C 1-4 alkyl, phenyl, substituted phenyl or OR 7 in which R 7 is, e.g., hydrogen,
C 2-8 alkanoyl, benzoyl, phenyl,
substituted phenyl, C 1-9 alkyl,
annamyl, C 1-4 haloalkyl, allyl,
cycloalkyl-C 1-3 -alkyl, adamantyl-C 1-3 -atkyl.
or phenyl Ci-3 alkyl;
R 4 , R 5 and R 6 are gydrogen, chloro, bromo, fluoro or C 1-3 alkyl; and
X is, e.g., hydrogen, C 1-3 alkyl, a cation derived from an alkali metal, or is ammonium.
Those compounds have antihypercholesterolemic activity by virtue of their ability to inhibit 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase and antifungal acticity.
wherein Z is:
n is 0, 1 or 2;
E is -CH 2 - -CH 2 -CH 2 -, -CH 2 -CH 2 -CH 2 -, -CH=CH-CH 2 -: or -CH 2 -CH=CH-;
R,, R 2 and R 3 are, e.g.. hydrogen, chloro, bromo, fluoro, C 1-4 alkyl, phenyl, substituted phenyl or OR 7 in which R 7 is, e.g., hydrogen,
C 2-8 alkanoyl, benzoyl, phenyl,
substituted phenyl, C 1-9 alkyl,
annamyl, C 1-4 haloalkyl, allyl,
cycloalkyl-C 1-3 -alkyl, adamantyl-C 1-3 -atkyl.
or phenyl Ci-3 alkyl;
R 4 , R 5 and R 6 are gydrogen, chloro, bromo, fluoro or C 1-3 alkyl; and
X is, e.g., hydrogen, C 1-3 alkyl, a cation derived from an alkali metal, or is ammonium.
Those compounds have antihypercholesterolemic activity by virtue of their ability to inhibit 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase and antifungal acticity.
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