Abstract:
The invention relates to a novel cyclic hexapeptide having antifungal and antipneumocystic activity as well as pharmaceutical compositions comprising, methods of treating using, and a process for preparing the claimed compounds.
Abstract:
The present invention relates to compounds of formula (I), wherein R 1 is selected from the group consisting of hydrogen, cycloalkyl, alkyl and haloalkyl; Y is selected from the group consisting of -(CR 4a R- 4b ) m -, -C(O)-, -O-, -N(H)-, -N(alkyl)- and -S-; wherein m is 1, 2 or 3; Ar 3 is phenyl or monocyclic heteroaryl; wherein Ar 3 is substituted with 1, 2 or 3 or 4 substituents. Ar 1 is selected from the group consisting of phenyl and a monocyclic, five or six- membered heteroaryl; Ar 2 is a monocyclic five membered heteroaryl, wherein each Ar 2 is independently unsubstituted or substituted with 1 or 2 substituents selected from the group consisting of alkyl, alkenyl, halogen, -CN, -NO 2 , hydroxy, alkoxy, -NH 2 , -N(H)(alkyl), -N(alkyl) 2 . -C(O)OH, -C(O)Oalkyl, -C(O)H, -C(O)alkyl, and haloalkyl; Z is selected from the group consisting of -OR 9a , -alkylenyl-OR 9a , -NR 6 R9 9b ; and -alkylenyl-NR 6 R 9b ; which inhibit acetyl-CoA carboxylase (ACC) and are useful for the prevention or treatment of metabolic syndrome, type U diabetes, obesity, atherosclerosis and cardiovascular diseases in humans.
Abstract translation:本发明涉及式(I)化合物,其中R 1选自氢,环烷基,烷基和卤代烷基; Y选自 - (CR 4a),-S(O) - , - C(O) - , - ,-N(H) - , - N(烷基) - 和-S-; 其中m为1,2或3; Ar 3是苯基或单环杂芳基; 其中Ar 3 3被1,2或3或4个取代基取代。 Ar 1选自苯基和单环,五或六元杂芳基; Ar 2是单环五元杂芳基,其中每个Ar 2 2独立地是未取代的或被1或2个选自烷基,烯基,卤素, CN,-NO 2,羟基,烷氧基,-NH 2,-N(H)(烷基), - N(烷基) 。 -C(O)OH,-C(O)O烷基,-C(O)H,-C(O)烷基和卤代烷基; Z选自-OR 9a, - 亚烷基-OR 9a,-NR 6 R 9 9b,/ N >; 和 - 亚烷基-NR 6 R 9b; 其抑制乙酰辅酶A羧化酶(ACC),并且可用于预防或治疗人类的代谢综合征,U型糖尿病,肥胖症,动脉粥样硬化和心血管疾病。
Abstract:
The present invention relates to compounds of formula (I); Pharmaceutical compositions and methods that are useful in the treatment or prevention of metabolic diseases or conditions are also provided.
Abstract:
Compounds of formula (I) or a pharmaceutically acceptable salt or prodrug thereof, wherein R is selected from the group consisting of hydrogen, methyl, ethyl, propyl, and isolpropyl; and one of R or R is 3,4,5-trimethoyxphenyl, and the other is phenyl substituted with one, two, or three substitutents independently selected from the group consisting of alkoxy, halo, and -NR R , wherein R and R are independently selected from the group consisting of hydrogen and alkyl, inhibit celluar proliferation. Processes for the preparation of the compounds, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds are disclosed.