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US 5,317,031 AGranted
Cholesterol lowering compounds
AssigneeMerck & Co., Inc.
InventorsJohn G. MacConnell, Byron H. Arison, George A. Doss, Richard L. Monaghan
Life of this patent
Estimating the term…
Abstract
Cholesterol lowering compounds and compositions are formed from the photochemical treatment of the Zaragozic Acids followed by esterification. These compounds and compositions are active squalene synthetase inhibitors useful in the treatment of hypercholesterolemia.
Claims13
A composition comprising a compound of formula (I) and formula (II) and formula (III):
- ##STR25## wherein R is selected from
- a) ##STR26## b) ##STR27## or c) ##STR28## and R.sub.1 is selected from
- a) ##STR29## b) ##STR30## or c) ##STR31## R.sub.2 is selected from a) H and
- b) ##STR32## R.sub.3 is C.sub.1-5 alkyl;
- Z is selected from
- (i) H;
- (ii) C.sub.1-5 alkyl;
- (iii) C.sub.1-5 alkyl substituted with
- a) C.sub.1-5 alkylcarbonyloxy;
- b) arylcarbonyloxy;
- c) C.sub.1-5 alkoxycarbonyloxy;
- d) aryloxycarbonyloxy;
- e) ##STR33## f) ##STR34## g) or the groups a) through d) form a 5 to 10 membered mono or bicyclic ring with C.sub.1-5 alkyl;
- (iv) C.sub.3-6 cycloalkyl;
- or a pharmaceutically acceptable salt thereof,
- provided that when R is ##STR35## then R.sub.1 is ##STR36## and when R is ##STR37## then R.sub.1 is ##STR38## and when R is ##STR39## then R.sub.1 is ##STR40##
13 more elements
A composition comprising a compound of formula (I) or formula (II) or formula (III):
- ##STR41## wherein R is selected from
- a) ##STR42## b) ##STR43## or c) ##STR44## and R.sub.1 is selected from
- a) ##STR45## b) ##STR46## or c) ##STR47## R.sub.2 is selected from a) H and
- b) ##STR48## R.sub.3 is C.sub.1-5 alkyl;
- Z is selected from
- (i) H;
- (ii) C.sub.1-5 alkyl;
- (iii) C.sub.1-5 alkyl substituted with
- a) C.sub.1-5 alkylcarbonyloxy;
- b) arylcarbonyloxy;
- c) C.sub.1-5 alkoxycarbonyloxy;
- d) aryloxycarbonyloxy;
- e) ##STR49## f) ##STR50## g) or the groups a) through d) form a 5 to 10 membered mono or bicyclic ring with C.sub.1-5 alkyl;
- (iv) C.sub.3-6 cycloalkyl;
- or a pharmaceutically acceptable salt thereof,
- provided that when R is ##STR51## then R.sub.1 is ##STR52## and when R is ##STR53## then R.sub.1 is ##STR54## and when R is ##STR55## then R.sub.1 is ##STR56##
13 more elements
Dependencies are inferred from the claim text.