Patent ID: 6506917
Filing Date: 2003-01-14
Classification: A61K,C07K,C12P

Abstract:
A pharmaceutically acceptable formulation consisting essentially of a pharmaceutically acceptable carrier and at least one compound having the structure: wherein:unsaturation between carbon atoms C9 and C10 has a cis configuration, and one or both sites of unsaturation between carbon atoms C11 through C14 optionally have a cis configuration; â€œRingâ€  is a an optionally substituted cyclic moiety selected from the group consisting of cyclopentane, cyclopentene, cyclohexane, cyclohex-2-ene, cyclohex-3-ene, cyclohex-4-ene, cyclohex-5-ene, 2,4-cyclohexadiene, 2,5-cyclohexadiene, 3,5-cyclohexadiene, dihydropyran, tetrahydropyran, dihydrothiopyran, tetrahydrothiopyran, piperidine, pyrrolidine, phenyl, tolyl, xylyl, mesityl, benzyl, and pyridyl, wherein if Ring is phenyl, none of the optional substituents is halogen; Z is selected from the group consisting of carboxyl (â€”COOH), carboxaldehyde (â€”COH), hydroxyalkyl (â€”(CRâ€²2)nâ€”OH, wherein each Râ€² is independently selected from hydrogen or a lower alkyl and n falls in the range of 1 up to about 4), thioalkyl (â€”(CRâ€²2)nâ€”SH, wherein Râ€² and n are as defined above), hydroxyalkyl phosphate (â€”(CRâ€²2)nâ€”OP(OM)3, wherein Râ€² and n are as defined above and M is hydrogen, lower alkyl, or a cationic species), alkyl ether of a hydroxyalkyl group (â€”(CRâ€²2)nâ€”ORâ€², wherein Râ€² and n are as defined above), alkyl thioether of a thioalkyl group (â€”(CRâ€²2)nâ€”SRâ€², wherein Râ€² and n are as defined above), esters of hydroxyalkyl groups (â€”(CRâ€²2)nâ€”Oâ€”COâ€”Râ€², wherein Râ€² and n are as defined above), thioesters of hydroxyalkyl groups (â€”(CRâ€²2)nâ€”Oâ€”CSâ€”Râ€², wherein Râ€² and n are as defined above), esters of thioalkyl groups (â€”(CRâ€²2)nâ€”Sâ€”COâ€”Râ€², wherein Râ€² and n are as defined above), thioesters of thioalkyl groups (â€”(CRâ€²2)nâ€”Sâ€”CSâ€”Râ€², wherein Râ€² and n are as defined above), aminoalkyl (â€”(CRâ€²2)nâ€”NRâ€²2, wherein Râ€² and n are as defined above), N-acyl aminoalkyl (â€”(CRâ€²2)nâ€”NRâ€²â€”COâ€”Râ€³, wherein Râ€² and n are as defined above and Râ€³ is a lower alkyl or benzyl), carbamate (CRâ€²2)nâ€”NRâ€²â€”COâ€”ORâ€² or â€”(CRâ€²2)nâ€”Oâ€”COâ€”NRâ€²2, wherein Râ€² and n are as defined above); and each R is independently selected from H, halogen, alkyl, aryl, hydroxy, thiol, alkoxy, thioalkoxy, amino, keto, or any of the Z substituents, wherein said compound is not 9-cis-retinoic acid.