Patent ID: 6506912
Filing Date: 2003-01-14
Classification: A61K,A61P,C07C

Abstract:
A compound having the formula: where R1 and R2 are each independently selected from the group consisting of hydrogen, alkyl, hydroxyalkyl, aminoalkyl, halogenalkyl, alkoxyalkyl, aryloxyalkyl, aryl, halogen, hydroxyl, protected hydroxy, alkoxyl, aryloxyl, acyl, an amino group, an amino group substituted with alkyl or aryl substituents and where R1 and R2, taken together, represent an oxo group, or a group â€”CH2)mâ€” where m is an integer having a value of from 2 to 5, and wherein n is an integer having a value of from 1 to 4, and wherein any of the groups CR1R2â€” in the formula (CR1R2)n may be replaced by an oxygen, sulfur or nitrogen atom, and R is represented by the structure below where the stereochemical center at carbon 20 may have the R or S configuration, and where Z is selected from Y, â€”OY, â€”CH2OY, â€”Câ‰¡CY and â€”CH&boxH;CHY, where the double bond may have the cis or trans geometry, and where Y is selected from hydrogen, methyl, â€”COR10 and a radical of the structure: where x and y, independently, represent the integers from 0 to 5, where R6 is selected from hydrogen, deuterium, hydroxy, protected hydroxy, fluoro, trifluoromethyl, and C1-5-alkyl, which may be straight chain or branched and, optionally, bear a hydroxy or protected-hydroxy substituent, and where each of R7, R8, and R9, independently, is selected from deuterium, deuteroalkyl, hydrogen, fluoro, trifluoromethyl and C1-5 alkyl, which may be straight-chain or branched, and optionally, bear a hydroxy or protected-hydroxy substituent, and where R6 and R7, taken together, represent an oxo group, or an alkylidene group, &boxH;CR7R8, or the group â€”(CH2)pâ€”, where p is an integer from 2 to 5, and where R8 and R9, taken together, represent an oxo group, or the group â€”(CH2)qâ€”, where q is an integer from 2 to 5, and where R10 represents hydrogen, hydroxy, protected hydroxy, or C1-5 alkyl and wherein any of the CHâ€” groups at positions 20, 22, or 23 in the side chain may be replaced by a nitrogen atom, or where any of the groups â€”CH(CH3)â€”, â€”(CH2)x, â€”(CR6R7)â€” or â€”(CH2)yâ€” at positions 20, 22; and 23, respectively, may be replaced by an oxygen or sulfur atom.