| 摘要 |
The present application relates to amorfrutin analogs and uses as PPAR modulators for the treatment of metabolic syndrome, obesity, hyperlipidemia, elevated fasting blood glucose, elevated blood pressure, low HDL cholesterol, type 2 diabetes, cardiovascular disease, a neurodegenerative disease, malaria or irritable bowel syndrome. |
| 主权项 |
1. A compound of the Formula (Ia)whereinRing A is
(i) optionally substituted phenyl, or (ii) optionally substituted (C5-C6)-heteroaryl,in which the optional substituents are selected from one to four of halo, OH, O—(C1-C6)-alkyl, (C1-C6)-alkyl, —C(O)OH, —OC(O)—(C1-C6)-alkyl or —C(O)O—(C1-C6)-alkyl;X is
(i) R′, (ii) —OR′, (iii) —C(O)O—R′, (iv) —C(O)—R′, or (v) —C(O)—NR′R″;R′ and R″ are each independently or simultaneously
(i) H, (ii) (C1-C8)-alkyl optionally substituted by (C6-C10)aryl, or (iii) (C6-C10)-aryl optionally substituted by (C1-C8)alkyl or (C6-C10)aryl,W is (C2-C6)-alkylene, wherein
(ii.a) at least one carbon atom of the (C2-C6)-alkylene group is substituted with R1 and/or R2; and (ii.b) at least one carbon atom of the (C2-C6)-alkylene group is replaced with an oxygen atom;R1 is
(i) H, (ii) (C1-C8)-alkyl, or (iii) (C3-C8)-cycloalkyl,R2 is
(i) H, (ii) (C1-C8)-alkyl, or (iii) (C3-C8)-cycloalkyl, orR1 and R2 taken together form a (C3-C8)-cycloalkyl ring,R is H or (C1-C8)-alkyl, andn is 6, 7, 8, 9, or 10,or a pharmaceutically acceptable salt, solvate, prodrug and/or stereoisomer thereof. |
