CETP inhibitors
View Patent ↗Compounds having the structures of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis: In the compounds of Formula I, B or R 2 is a phenyl group which has an ortho aryl, heterocyclic, benzoheterocyclic or benzocycloalkyl substituent, and one other position on the 5-membered ring has an aromatic, heterocyclic, cycloalkyl, benzoheterocyclic or benzocycloalkyl substituent connected directly to the ring or attached to the ring through a —CH 2 —.
1. A method of treating atherosclerosis in a patient in need of treatment comprising the administration of a therapeutically effective amount of a compound of Formula Ii, or a pharmaceutically acceptable salt thereof, wherein:
R 7 is selected from the group consisting of Cl and —CF 3 ;
Each R b is independently selected from the group consisting of —C 1 -C 3 alkyl, —OCH 3 , and F;
R 1 is selected from the group consisting of H and —C 1 -C 2 alkyl;
R c is selected from the group consisting of halogen,—CH 3 , —CF 3 , and —CN;
q is 2 or 3; and
t is an integer from 0-2.
2. The method of claim 1 wherein the compound is selected from the group consisting of the following compounds, or a pharmaceutically acceptable salt thereof:
3. The method of claim 1 wherein the compound is selected from the group consisting of the following compounds, or a pharmaceutically acceptable salt thereof:
wherein R is selected from the group consisting of
4. A method of treating atherosclerosis in a patient in need of treatment comprising the administration of a therapeutically effective amount of a compound having the structure:
or a pharmaceutically acceptable salt thereof.
5. A method of treating atherosclerosis in a patient in need of treatment comprising the administration of a therapeutically effective amount of a compound having the structure:
6. The method of claim 5 comprising the administration of a therapeutically effective amount of the compound having the structure:
and an HMG-CoA reductase inhibitor.
7. The method of claim 6 , wherein the HMG-CoA reductase inhibitor is a statin selected from the group consisting of simvastatin, lovastatin, rosuvastatin, pravastatin, fluvastatin, atorvastatin, rivastatin, and itavastatin.
8. The method of claim 7 , further comprising a cholesterol absorption inhibitor.
9. The method of claim 8 , wherein the cholesterol absorption inhibitor is ezetimibe.