申请人:Hodson Harold Francis
公开号:US20080161301A1
公开(公告)日:2008-07-03
The use of a compound comprising formula (I):
or a salt, ester, amide or prodrug thereof in the inhibition of an enzyme whose preferred mode of action is to catalyse the hydrolysis of an ester functionality, e.g. in the control and inhibition of unwanted enzymes in products and processes. The compounds are also useful in medicine e.g. in the treatment of obesity and related conditions. The invention also relates to novel compounds within formula (I), to processes for preparing them and pharmaceutical compositions containing them.
In formula (I) A is a 6-membered aromatic or heteroaromatic ring; and
R
1
is a branched or unbranched alkyl (optionally interrupted by one or more oxygen atoms), alkenyl, alkynyl, cycloalkyl, cycloalkenyl, aryl, arylalkyl, reduced arylalkyl, arylalkenyl, heteroaryl, heteroarylalkyl, heteroarylalkenyl, reduced aryl, reduced heteroaryl, reduced heteroarylalkyl or a substituted derivative of any of the foregoing groups.
使用式(I)的化合物或其盐、酯、酰胺或前药在抑制一种首选模式为催化酯官能团水解的酶方面具有应用,例如在产品和过程中控制和抑制不需要的酶。该化合物也在医学上有用,例如在肥胖和相关疾病的治疗中。该发明还涉及式(I)内的新化合物,以及制备它们的过程和含有它们的药物组成物。
在式(I)中,A是6元芳香或杂芳香环;而R1是支链或非支链烷基(可选地被一个或多个氧原子打断)、烯基、炔基、环烷基、环烯基、芳基、芳基烷基、还原芳基烷基、芳基烯基、杂芳基、杂芳基烷基、杂芳基烯基、还原芳基、还原杂芳基、还原杂芳基烷基或上述任何基团的取代衍生物。