Treatment for atherosclerosis and other cardiovascular and inflammatory diseases
First Claim
Patent Images
1. A method for the treatment of a cardiovascular disease in humans comprising administering an effective amount of a dithiocarbamate of the formula A--SC(S)--B;
- wherein A is selected from the group consisting of hydrogen a pharmaceutically acceptable cation, and a physiologically cleavable leaving group;
and B is selected form the group consisting of alkyl, alkenyl, alkynyl, alkaryl aralkyl, haloalkyl, haloalkenyl, haloalkynyl, aryl, alkaryl, hydrogen, C1-6 alkoxy-C1-10 alkyl, C1-6 alkylthio-C1 alkyl, NR2 R3, heterocyclic, alkylheterocyclic --(CHOH)n CH2 OH, wherein n is 0, 1, 2, 3, 4, 5, or 6, --(CH2)n CO2 R1, hydroxy (C1-6) alkyl-, --(CH2)n CO2 R4 alkyl(CO2 H) alkenyl(CO2 H), alkynyl(CO2 H) wherein R1 is hydrogen or a pharmaceutically acceptable cation, R4 is alkyl, aryl, alkaryl, or aralkyl and R2 and R3 are independently C1-10 linear, branched, or cyclic alkyl, --(CHOH)n (CH2)OH, wherein n is 0, 1, 2, 3, 4, 5, or 6, or R2 and R3 together constitute a bridge, in association with a lipid lowering agent.
0 Assignments
0 Petitions
Accused Products
Abstract
Dithiocarboxylates, and in particular, dithiocarbamates, block the induced expression of the endothelial cell surface adhesion molecule VCAM-1, and are therefor useful in the treatment of cardiovascular disease, including atherosclerosis, post-angioplasty restenosis, coronary artery diseases, and angina, as well as noncardiovascular inflammatory diseases that are mediated by VCAM-1.
43 Citations
16 Claims
-
1. A method for the treatment of a cardiovascular disease in humans comprising administering an effective amount of a dithiocarbamate of the formula A--SC(S)--B;
-
wherein A is selected from the group consisting of hydrogen a pharmaceutically acceptable cation, and a physiologically cleavable leaving group; and B is selected form the group consisting of alkyl, alkenyl, alkynyl, alkaryl aralkyl, haloalkyl, haloalkenyl, haloalkynyl, aryl, alkaryl, hydrogen, C1-6 alkoxy-C1-10 alkyl, C1-6 alkylthio-C1 alkyl, NR2 R3, heterocyclic, alkylheterocyclic --(CHOH)n CH2 OH, wherein n is 0, 1, 2, 3, 4, 5, or 6, --(CH2)n CO2 R1, hydroxy (C1-6) alkyl-, --(CH2)n CO2 R4 alkyl(CO2 H) alkenyl(CO2 H), alkynyl(CO2 H) wherein R1 is hydrogen or a pharmaceutically acceptable cation, R4 is alkyl, aryl, alkaryl, or aralkyl and R2 and R3 are independently C1-10 linear, branched, or cyclic alkyl, --(CHOH)n (CH2)OH, wherein n is 0, 1, 2, 3, 4, 5, or 6, or R2 and R3 together constitute a bridge, in association with a lipid lowering agent. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15)
-
- 16. A method for the treatment of a cardiovascular disease in humans comprising administering an effective amount of a dithiocarbamate of the formula
- space="preserve" listing-type="equation">B--C(S)S--SC(S)--B
wherein B is selected form the group consisting of alkyl, alkenyl, alkynyl, alkaryl, aralkyl, haloalkyl, haloalkenyl, haloalkynyl, aryl, alkaryl, hydrogen, C1-6 alkoxy-C1-10 alkyl, C1-6 alkylthio-C1-10 alkyl, NR2 R3, --(CHOH)n CH2 OH, wherein n is 0, 1, 2, 3, 4, 5, or 6, --(CH2)n CO2 R1, alkylacetyl, alkylpropionyl, alkylbutyryl, hydroxy (C1-6) alkyl-, --(CH2)n CO2 R4, wherein n is 0, 1, 2, 3, 4, 5, or 6, alkyl(CO2 H), alkenyl (CO2 H), alkynyl(CO2 H) wherein R1 is hydrogen or a pharmaceutically acceptable cation, and R2 and R3 are independently propyl, isopropyl, butyl, isobutyl, t-butyl, pentyl, cyclopentyl, isopentyl, neopentyl, hexyl, isohexyl, cyclohexyl, 3-methylpentyl, 2,2-dimethylbutyl, and 2,3-dimethylbutyl or R2 and R3 together constitute a bridge, in association with a lipid lowering agent.
Specification