Thyromimetic antiobesity agents

A - Human Necessities – 61 – K

Patent

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Details

A61K 31/21 (2006.01) A61K 31/195 (2006.01) A61K 31/198 (2006.01) A61K 31/215 (2006.01) A61K 31/216 (2006.01) A61P 3/04 (2006.01)

Patent

CA 2299972

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 Image 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 Image wherein R8 is hydrogen, lower alkyl, aryl, cycloalkyl, aryl-lower alkyl or cycloalkyl- lower alkyl; R9 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.

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