Patent ID: 6545041
Filing Date: 2003-04-08
Classification: A61K,A61P,Y02A

Abstract:
A method for treating a patient who exhibits the symptoms associated with cachexia due to acquired immune deficiency syndrome, neoplasia, trauma or other wasting diseases, which method comprises administering to the patient a pharmaceutical composition in order to prevent production of or block the action of tumor necrosis factor in the patient, wherein the pharmaceutical composition comprises a therapeutically effective amount of a compound of the formula (I): having the (3S,4S) configuration and being essentially free of the (3R,4R) enantiomer, whereinA - - - B indicates an optional 1(2) or 6(1) double bond, R is (a) â€”Q wherein Q is a heterocyclic moiety having a labile hydrogen atom so that said moiety acts as a carboxylic acid analogue, (b) â€”Râ€²X wherein Râ€² is C1-C5 alkyl and X is halogen, â€”ORâ€³ wherein Râ€³ is hydrogen, C1-C5 alkyl, or â€”OC(O)Râ€²â€³ wherein Râ€²â€³ is hydrogen or C1-C5 alkyl, (c) â€”Râ€²N(Râ€³)2 wherein Râ€² is C1-C5 alkyl and each Râ€³, which may be the same or different, is hydrogen or C1-C5 alkyl optionally containing a terminal â€”ORâ€²â€³ or â€”OC(O)Râ€²â€³ moiety wherein Râ€²â€³ is hydrogen or C1-C5 alkyl, (d) â€”Râ€² wherein Râ€² is C1-C5 alkyl, (e) â€”Râ€²ORâ€²â€³ wherein Râ€² is C1-C5 alkyl and Râ€²â€³ is hydrogen or C1-C5 alkyl, or, (f) â€”Râ€²â€”C(O)â€”ORâ€²â€³, wherein Râ€² may be absent and Râ€² and Râ€²â€³ are as defined above; G is (a) halogen, (b) C1-C5 alkyl, or (c) â€”OR1 wherein R1 is (aâ€²) â€”Râ€³, wherein Râ€³ is hydrogen or C1-C5 alkyl optionally containing a terminal â€”ORâ€²â€³ or â€”OC(O)Râ€²â€³ moiety wherein Râ€²â€³ is hydrogen or C1-C5 alkyl, or (bâ€²) â€”C(O)Râ€²â€³ wherein Râ€²â€³ is as previously defined; and R2 is (a) C1-C12 alkyl, (b) â€”ORâ€³â€³, in which Râ€³â€³ is a straight chain or branched C2-C9 alkyl which may be substituted at the terminal carbon atom by a phenyl group, or (c) â€”(CH2)nORâ€²â€³ wherein n is an integer of 1 to 7 and Râ€²â€³ is hydrogen or C1-C5 alkyl.