Patent ID: 6525036
Filing Date: 2003-02-25
Classification: A61P,C07C,C07D

Abstract:
The compound of formula I in which:X1 is â€”CR4R5â€” or â€”CHR7â€”; R4 and R5 along with the carbon atom to which they are attached represents â€ƒwherein R31 and R32 independently represent hydrogen or hydroxy, alternatively R31 and R32 can be taken together to represent an oxo (&boxH;O) group; R7 is (C4-8) branched alkyl or â€”CH2-cyclopropyl; R1 is hydrogen; R2 is hydrogen or R2a; alternatively, R1 and R2 together represent â€”CH2â€”CH2â€” or â€”CH2â€”NR8â€”CH2â€”; R2a represents (C2-4) alkyl optionally substituted with a group selected from â€”NR8C(O)OR35, â€”OR35, â€”SR35, â€”S(O)R35, â€”S(O)2R35, â€”C(O)R35, â€”SO2NR8R52 and â€”OP(O)(OR8)OR35; R3 is (C6-10)aryl or hetero(C5-10)aryl, wherein R3 may be substituted further by a radical selected from a group consisting of â€”X3NR8R21, â€”X3NR8C(O)R21, â€”X3NR8C(O)OR21, â€”X3NR8C(O)NR8R21, â€”X3OR21, â€”X3SR21, â€”X3C(O)R21, â€”X3C(O)OR21, â€”X3OC(O)R21, â€”X3C(O)NR8R21, â€”X3OR52, â€”X3CONR8R52 and â€”R21, wherein: X3 is a bond or (C1-6)alkylene, R8 at each occurrence independently is hydrogen or (C1-6)alkyl and R21 is (C1-8)alkyl or â€”X3R22, wherein X3 is as defined above; R22 is selected from a group consisting of hetero(C5-10)cycloalkyl, (C6-10)aryl, hetero(C5-10)aryl and hetero(C8-10)bicycloaryl, wherein R22 may be substituted further by a radical selected from a group consisting of (C1-4)alkyl, â€”X3NR8R23, â€”X3C(O)NR8R52, â€”X3OR23, â€”X3NR8C(O)R23, â€”X3SO2NR8R52, â€”X3C(O)NR8R23, â€”X3SO2NR8R23, â€”X3COR23, â€”X3OR52, â€”X3S(O)2R23, X3N(R8)2 and â€”R23, wherein X3 is a bond or (C1-6)alkylene, R52 represents â€”CH2CH2â€”N(CH2CH2OH)2, â€”CH(CH3)CH2N(CH3)2, â€”CH2CH2OH, â€”CH2CN or â€”CH2CH2N(CH3)2, R8 at each occurrence independently is hydrogen or (C1-6)alkyl and R23 is (C1-8)alkyl or â€”X3R24, wherein X3 is as defined above; R24 is selected from a group consisting of hetero(C5-10)cycloalkyl and hetero(C5-10)aryl, wherein R24 may be substituted further with R25, â€”X3OR52, â€”X3NR8R25, â€”X3COOR25 and â€”X3SO2NR8R52; wherein X3 is a bond or (C1-6)alkylene, R52 represents â€”CH2CH2â€”N(CH2CH2OH)2, â€”CH(CH3)CH2N(CH3)2, â€”CH2CH2OH, â€”CH2CN or â€”CH2CH2N(CH3)2, R8 at each occurrence independently is hydrogen or (C1-6)alkyl and R25 is (C1-8)alkyl or â€”X3R26, wherein X3 is as defined above; R26 is hetero(C5-10)cycloalkyl; and wherein any of the (C3-10)cycloalkyl, hetero(C5-10)cycloalkyl, (C6-10)aryl, hetero(C5-10)aryl, (C9-10)bicycloaryl and hetero(C8-10)bicycloaryl contained within R3, R22, R24 and R26 may be substituted further with up to five substituents selected from a group consisting of (C1-6)alkyl, cyano, halo, nitro, halo-substituted (C1-3)alkyl, â€”X3NR16R16, â€”X3OR52 and â€”X3C(O)R16, wherein: X3 is a bond or (C1-6)alkylene, R52 represents â€”CH2CH2â€”N(CH2CH2OH)2, â€”CH(CH3)CH2N(CH3)2, â€”CH2CH2OH, â€”CH2CH2N(CH3)2 or â€”CH2CN, R16 at each occurrence independently is selected from a group consisting of hydrogen, (C1-3)alkyl or halo-substituted (C1-3)alkyl and R17 is â€”(C1-3)alkyl or halo-substituted (C1-3)alkyl; and the N-oxide compounds, prodrug derivatives, protected derivatives, individual stereo isomers and mixtures of stereo isomers, or pharmaceutically acceptable salts thereof, with the proviso that only one of R3, R22, R24 and R26 represents a fused bicyclic ring structure.