Patent ID: 6818638
Filing Date: 2004-11-16
Classification: A61P,C07C,C07D

Abstract:
A compound of formula I whereineach of a - - - b and &agr; - - - &bgr; independently, is either a single bond or a double bond; R1 is H, C1-4alkyl or ORa wherein Ra is H, C1-6alkyl optionally substituted by OH or C1-4alkoxy, C2-6alkenyl or aryl-C1-4alkyl;R2 is OH; â€”Oâ€”COâ€”R5 wherein R5 is C1-8alkyl, C3-7cycloalkyl, C3-7cycloalkyl-C1-4alkyl, aryl or aryl-C1-4alkyl; or â€”Oâ€”R6 wherein R6 is the residue of an &agr;-amino-acid attached to O through its carbonyl residue or â€”CHR7â€”COR8 wherein R7 is H, C1-4alkyl, heteroC1-4alkyl, C3-7cycloalkyl, C3-7cycloalkyl-C1-4alkyl, aryl or aryl-C1-4alkyl and R6 is OH, C1-4alkoxy or NR9R10 wherein each of R9 and R10 independently is H, C1-4alkyl or R9 and R10 form together with the nitrogen to which they are bound, a heteroaryl group; R3 is a substituted linear amino alcohol or cyclic carbamate of formula (c2); whereineach of R50, independently is H; C1-8alkyl; C3-7cycloalkyl; aryl; C3-7cycloalkyl-C1-4alkyl; aryl-C1-4alkyl; heteroaryl; heteroaryl-C1-4alkyl; C1-4alkylcarbonyl; aryl-carbonyl; heteroaryl-carbonyl; aryl-C1-4alkyl-carbonyl or heteroaryl-C1-4alkyl-carbonyl, and each of R51, independently is H; C1-4alkyl; hydroxy-C1-4alkyl; amino-C1-4alkyl; C1-4alkoxy-C1-4alkyl; C1-4alkoxy-carbonyl-C1-4alkyl wherein C1-4alkoxy is optionally substituted by amino, C1-4alkyl-amino or di-(C1-4alkyl)amino; HOOCâ€”C1-4alkyl; or R23R24Nâ€”COâ€”C1-4alkyl wherein R23 is H, C1-4alkyl, hydroxy-C1-4alkyl, polyhydroxy-C1-8alkyl, heteroaryl, heteroaryl-C1-4alkyl, amino-C1-4alkyl, C1-4alkylamino-C1-4alkyl, di-(C1-4alkyl)amino-C1-4alkyl or aryl-C1-4alkyl and R24 is H, C1-4alkyl or hydroxy-C1-4alkyl, at least one of R50 and R51 being other than H, each of X and Y is H or X and Y form together â€ƒeach of a - - - b and &agr; - - - &bgr; being a single bond when each of R13 or R14 is OH; and R4 is H or OR19 wherein R19 is C1-6alkyl, hydroxy-C1-6alkyl, C1-4alkoxy-C1-6alkyl, aryl-C1-4alkyl or C1-4alkoxycarbonyl-C1-4alkyl, and wherever â€œarylâ€  appears as is or in the significances of â€œaryl-C1-4alkylâ€  in the above definition, it is â€œphenylâ€  or â€œnaphthylâ€  optionally substituted by halogen, OH, NR11R12, COOH, CF3, C1-4alkoxy, C1-4alkyl, hydroxy-C1-4alkyl, hydroxy-C1alkoxy, C1-4alkoxy-carbonyl, cyano or CONR11R12, each of R11 and R12 independently being H, C1-4alkyl, phenyl, naphthyl, phenyl-C1-4alkyl or naphthyl-C1-4alkyl or R11 and R12 together with the nitrogen to which they are bound forming heteroaryl; and wherever â€œheteroarylâ€  appears, it is a 5- or 6-membered heteroaryl optionally fused to a benzene ring; in free form or in salt form.