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US 9,102,656 B2Granted
Use of rosuvastatin lactols as medicaments
AssigneeRedx Pharma PLC
InventorsDerek Lindsay, Peter Jackson
Life of this patent
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Abstract
This invention relates to the discovery of novel rosuvastatin analogs. More specifically, the invention relates to novel rosuvastatin analogs which have utility in treating conditions treatable by the inhibition of HMG-CoA reductase.
Claims26
A method of treating a condition comprising:
- administering an effective amount of a compound of Formula I
- or pharmaceutically acceptable salts or solvates thereof to inhibit the enzyme 3-hydroxy-3-methylglutaryl-coenzyme A reductase (HMG-CoA reductase),
- wherein the condition is selected from the group consisting of:
- hypercholesterolemia, atherosclerosis, hyperlipidemia, coronary heart disease, myocardial infarction, stroke, and peripheral artery disease,
- further wherein:
- R1 and R4 are independently selected from the group consisting of:
- hydrogen, halo, C1-6 alkyl, C2-6 alkenyl, C3-6 cycloalkyl, aryl, C1-4 alkyl aryl, heterocyclyl, and C1-4 alkyl heteroaryl;
- R2 is —S(O)2R9 wherein R9 is C1-6 alkyl, C3-6 cycloalkyl, C1-6 alkyl aryl or aryl;
- R3 is hydrogen, C1-6 alkyl, C2-6 alkenyl, C3-6 cycloalkyl or aryl;
- R5 and R6 are independently selected from the group consisting of:
- hydrogen, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C3-6 cycloalkyl, aryl, C1-6 alkyl aryl, C1-6 alkanoyl aryl, heteroaryl, C1-6 alkanoyl heteroaryl and C1-6 alkyl heteroaryl;
- provided always that both R5 and R6 are not hydrogen;
- R7 and R8 are independently selected from the group consisting of:
- H, C1-4 alkyl and halo;
- X is —(CRaRb)m(CRa═CRb)n(CRaRb)o where Ra and Rb are independently selected from the group consisting of:
- H, methyl, ethyl and halo and m, n, and o are independently 0, 1, 2, or 3 provided that m+n+o is not more than 3;
- and wherein each of the above groups R1 to R9 may, where chemically possible, be independently optionally substituted by from 1 to 5 groups chosen independently at each occurrence from the group consisting of:
- halo, C1-3 alkyl, halo C1-3 alkyl, C1-3 alkoxy, C1-3 haloalkoxy, hydroxy, and cyano.
15 more elements
Dependencies are inferred from the claim text.