摘要 |
The present disclosure relates to compounds, which are useful for regulating the expression of apolipoprotein A-I (ApoA-I), and their use for treatment and prevention of cardiovascular disease and related disease states, including cholesterol- or lipid-related disorders, such as, for example, atherosclerosis. |
代理机构 |
Finnegan, Henderson, Farabow, Garrett & Dunner, LLP |
代理人 |
Finnegan, Henderson, Farabow, Garrett & Dunner, LLP |
主权项 |
1. A method for increasing expression of ApoA-I in a mammal comprising administering a therapeutically effective amount of a compound of Formula II: wherein: X is N; Y is CO; R1 and R3 are each independently selected from alkoxy, alkyl, amino, halogen, and hydrogen; R2 is selected from alkoxy, alkyl, alkenyl, alkynyl, amide, amino, halogen, and hydrogen; R6 and R8 are each independently selected from alkyl, alkoxy, amino, halogen, and hydrogen; R5 and R9 are each hydrogen; R7 is selected from amino, amide, alkyl, hydroxyl, and alkoxy; R10 is hydrogen; each W is independently selected from C and N, wherein if W is N, then p is 0 or 1, and if W is C, then p is 1; for W—(R10)p, W is N and p is 1; for W—(R7)p, W is C and p is 1; for W—(R4)p, W is C, p is 1 and R4 is H, or W is N and p is 0; Z1 is a double bond, and Z2 and Z3 are each a single bond; with the proviso that if R1 is hydrogen, then R3 is alkoxy; with the proviso that if R3 is hydrogen, then R1 is selected from amino and alkoxy; with the proviso that if R7 is selected from alkyl, hydroxyl, and alkoxy, then at least one of R6 and R8 is independently selected from alkyl, alkoxy, amino, and halogen;or a pharmaceutically acceptable salt thereof. |