公开(公告)号：US06344481B1

公开(公告)日：2002-02-05

申请号：US09488110

申请日：2000-01-20

申请人： Peter Cornelius ,  Diane M. Hargrove ,  Bradley P. Morgan ,  Andrew G. Swick

发明人： Peter Cornelius ,  Diane M. Hargrove ,  Bradley P. Morgan ,  Andrew G. Swick

IPC分类号： A61K3124

CPC分类号： A61K31/216 ,  A61K31/195 ,  A61K31/198 ,  A61K31/215 ,  A61K2300/00 ,  A61K31/00

摘要： The invention relates to pharmaceutical compositions and methods useful in the treatment of obesity which methods comprise administering to animal, including a human or companion animal, in need of such treatment an effective amount of a compound of the structural formula or a pharmaceutically acceptable salt, racemate or enantiomer thereof, wherein R is hydroxy, esterified hydroxy or etherified hydroxy; R1 and R2 are, independently, halogen, trifluoromethyl or lower alkyl; R3 is halogen, trifluoromethyl, lower alkyl, aryl, aryl-lower alkyl, cycloalkyl or cycloalkyl-lower alkyl, carbocyclic arylmethyl, carbocyclic aroyl, carbocyclic arylhydroxymethyl; or R3 is the radical wherein R8 is hydrogen, lower alkyl, aryl, cycloalkyl, aryl-lower alkyl or cycloalkyl-lower alkyl; R6 is hydroxy or acyloxy; R10 is hydrogen or lower alkyl; or R9 and R10, taken together with the carbon atom to which they are attached, form a carbonyl group; R4 is hydrogen, halogen, trifluoromethyl or lower alkyl; R5 and R6 are, independently, hydrogen or lower alkyl or R5 and R6, taken together with the carbon atom to which they are attached, form a carbonyl group; X is O, S or —NR7; R7 is hydrogen or lower alkyl; W is O or S; and Z is carboxyl or carboxyl derivatized as a pharmaceutically acceptable ester or amide. The invention further provides for pharmaceutical compositions and methods of using the compounds of structural formula (I), or the pharmaceutically acceptable salts, racemates and enantiomers thereof, in combination with an anorectic agent, in treating obesity.

摘要翻译： 本发明涉及可用于治疗肥胖症的药物组合物和方法，该方法包括向需要这种治疗的动物，包括人或伴侣动物施用有效量的结构式化合物或其药学上可接受的盐，外消旋体或 其中R是羟基，酯化的羟基或醚化羟基; R 1和R 2独立地是卤素，三氟甲基或低级烷基; R 3是卤素，三氟甲基，低级烷基，芳基，芳基 - 低级烷基，环烷基或环烷基 - 低级烷基， 碳环芳基甲基，碳环芳酰基，碳环芳基羟甲基; 或R 3是其中R 8是氢，低级烷基，芳基，环烷基，芳基 - 低级烷基或环烷基 - 低级烷基的基团; R 6是羟基或酰氧基; R 10是氢或低级烷基; 或R 9和R 10与它们所连接的碳原子一起形成羰基; R 4是氢，卤素，三氟甲基或低级烷基; R 5和R 6独立地是氢或低级烷基或R 5和R 6，取代 与它们所连接的碳原子一起形成羰基; X是O，S或-NR 7; R 7是氢或低级烷基; W是O或S; 并且Z是作为药学上可接受的酯或酰胺衍生的羧基或羧基。本发明还提供了药物组合物和使用结构式（I）化合物或其药学上可接受的盐，外消旋体和对映异构体与厌食症 代理，治疗肥胖。