Patent ID: 6605595
Filing Date: 2003-08-12
Classification: A61K,A61P,C07H

Abstract:
A compound represented by formula (I) or a salt thereof: wherein â€”X----Yâ€” represents â€”CH&boxH;CHâ€”, â€”CH2â€”C(&boxH;O)â€”, â€”CH2â€”CH2â€”, or â€”CH2â€”CH(R13)â€”;---- between R1 and a carbon atom at the 4â€³-position represents a single or double bond; ---- between R2 and a carbon atom at the 5-position represents a single or double bond, with the provisos that 1) when â€”X----Yâ€” represents â€”CH&boxH;CHâ€” and ---- between R1 and a carbon atom at the 4â€³-position represents a double bond; R1 represents (R11)(R12)C wherein R11 represents a lower alkyl group (optionally substituted with from 1 to 3 members selected from the group consisting of a hydroxyl group, a halogen atom, an amino group, a hydroxyamino group, a mono(lower alkyl)amino group, a mono(lower alkoxy)amino group, an alkanoylamino group, an azide group, a heterocyclic group, a lower alkanoyloxy group, a heterocyclic carbonyloxy group where the heterocyclic moiety may be substituted with a halogen atom or a lower alkoxycarbonyl group, and a heterocyclic oxy group); a formyl group; a lower alkoxycarbonyl group, the alkyl moiety of which is optionally substituted with a heterocyclic group; â€”CH&boxH;Nâ€”OR3 wherein R3 represents a hydrogen atom or a lower alkyl group; a lower alkenyloxycarbonyl group; â€”CH&boxH;Nâ€”NHâ€”CONH2; a cyano group; â€”COR4 wherein R4 represents a hydroxyl group or N(R5)(R6) wherein R5 and R6 form a nitrogen-containing heterocyclic group together with the adjacent nitrogen atom; a vinyl group substituted with a lower alkenyloxycarbonyl group; â€”COâ€”Sâ€”CH2â€”CH2â€”NHâ€”COâ€”Rx wherein Rx represents a lower alkyl group; or â€”CH&boxH;CHâ€”COOH; and R12 represents a hydrogen atom, except that when R11 represents a cyano group, R12 represents a hydrogen atom or a lower alkyl group; when ---- between R2 and a carbon atom at the 5-position represents a single bond, R2 represents a hydroxyl group, a lower alkoxyl group, or a tri(lower alkyl)silyloxy group; and when ---- between R2 and a carbon atom at the 5-position represents a double bond, R2 forms a carbonyl group or a hydroxime group together with the carbon atom at the 5-position; 2) when â€”X----Yâ€” represents â€”CH2â€”C(&boxH;O)â€”, ---- between R1 and a carbon atom at the 4â€³-position represents a double bond; R1 represents (R11a)R12a)C wherein R11a represents a lower alkoxycarbonyl group, the alkyl moiety of which is optionally may be substituted with a heterocyclic group, or â€”COOCH2CH&boxH;CH2; and R12a represents a hydrogen atom; ---- between R2 and a carbon atom at the 5-position represents a single bond; and R2 represents a hydroxyl group, a lower alkoxy group, or a tri(lower alkyl)silyloxy group; 3) when â€”X----Yâ€” represents â€”CH2â€”CH2â€”, R1 represents (R11b)(R12b)C wherein R11b represents a cyano group, a carboxyl group, or a lower alkenyloxycarbonyl group; and R12b represents a hydrogen atom; or when ---- between R1 and a carbon atom at the 4â€³-position represents a single bond, R1 represents a carboxymethyl group or a cyanomethyl group; ---- between R2 and a carbon atom at the 5-position represents a single bond; and R2 represents a hydroxyl group, a lower alkoxy group, or a tri(lower alkyl)silyloxy group; 4) when â€”X----Yâ€” represents â€”CH2â€”CH(R13)â€”, and ---- between R1 and a carbon atom at the 4â€³-position represents a double bond; R1 represents (R11c)(R12c)C wherein R11c represents a cyano group, a carboxyl group, a lower alkoxycarbonyl group or a lower alkenyloxycarbonyl group; and R12c represents a hydrogen atom; R13 represents a hydroxyl group or a lower alkylcarbonyloxy group; ---- between R2 and a carbon atom at the 5-position represents a single bond; and R2 represents a hydroxyl group, a lower alkoxy group or a tri(lower alkyl)silyloxy group.