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US 5,210,228 AGranted
Decaline based HMC-COA reductase inhibitors with two C-6 substituents
AssigneeBritish Bio-Technology Limited
InventorsRichard S. Todd, Christopher N. Lewis, Alan H. Davidson, Alan H. Drummond
Life of this patent
Estimating the term…
Abstract
Compounds of either of general formulae I and II: ##STR1## wherein: R.sup.1, R.sup.2, R.sup.3, R.sup.5, R.sup.6, a, b, c, and d are variables. These compounds are useful in the treatment of hypercholesterolaemia in general and arteriosclerosis, familial hypercholesterolaemia or hyperlipidaemia in particular.
Claims6
A compound selected from the group consisting of general formulae I and II:
- ##STR14## wherein:
- R.sup.1 represents a C.sub.1-8 alkyl, C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkyl(C.sub.1-8)alkyl, C.sub.2-8 alkenyl, or C.sub.1-6 alkyl substituted phenyl group;
- R.sup.2 represents C.sub.2-5 alkenyl or C.sub.2-5 alkenyl substituted with substituted phenyl group;
- R.sup.3 represents a hydrogen atom or R.sup.4 or M;
- R.sup.4 represents a C.sub.1-5 alkyl group, or a C.sub.1-5 alkyl group substituted with a group chosen from substituted phenyl, dimethylamino and acetylamino;
- R.sup.5 represents a hydrogen atom or a methyl or ethyl group;
- R.sup.6 represents a C.sub.1-8 alkyl, C.sub.2-8 alkenyl or a C.sub.2-8 alkynyl group or a C.sub.1-5 alkyl, C.sub.2-5 alkenyl or a C.sub.2-5 alkynyl group substituted with a substituted phenyl group;
- wherein the term "substituted", as applied to the phenyl group, means substituted with up to four substituents each of which independently may be C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxy, thiol, amino, halo (including fluoro, chloro, bromo, and iodo), trifluoromethyl or mitro;
- M represents a cation capable of forming a pharmaceutically acceptable salt;
- Q represents C.dbd.O or CHOH;
- and
- each of a, b, c, and d is independently a single or double bond except that when a and c are double bonds then b is a single bond.
9 more elements
A compound selected from the group consisting of:
- (A) (1S,2S,4aR,6S,8S,8aS,4'R,6'R)-6'-{2-(1,2,4a,5, 6,7,8,8a-octahydro-2,6-dimethyl-8-[(2",2"-dimethyl-1"-oxobutyl)oxy]-6-[(E) -prop-1-enyl]-1-naphthalenyl)ethyl}-tetra-hydro-4'-hydroxy-2H-pyran-2'-one,
- (B) Sodium (1S,2S,4aR,6S,8S,8aS,3'R,5'R)-7'-(1,2, 4a,5,6,7,8,8a-octahydro-2,6-dimethyl-8-[(2",2""-dimethyl-1"-oxobutyl)oxy]- 6-[(E)-prop-1-enyl]-1-naphthalenyl)-3',5'-dihydroxyheptanoate,
- (C) Methyl (1S,2S,4aR,6S,8S,8aS,3'R,5'R)-7'-(1,2, 4a,5,6,7,8,8a-octahydro-2,6-dimethyl-8-[(2",2"-dimethyl-1"-oxobutyl)oxy]-6 -[(E)-prop-1-enyl]-1-naphthalenyl)-3',5'-dihydroxyheptanoate, and
- (D) Methyl (1S,2S,4aR,6S,8S,8aS,3'R)-7'-(1,2,4a,5, 6,7,8,8a-octahydro-2,6-dimethyl-8-[(2",2"-dimethyl-1"-oxobutyl)oxy]-6-[(E) -prop-1-enyl]-1-naphthalenyl)-3'-hydroxy-5'-oxoheptanoate.
1 more element
Dependencies are inferred from the claim text.