Patent ID: 6492362
Filing Date: 2002-12-10
Classification: A61P,C07C,C07D

Abstract:
A compound of Formula II: in which:n is 1, 2, 3, 4 or 5; R1 is hydrogen and R2 is cyano, hetero(C5)aryl or (C1-4)alkyl-substituted hetero(C5)aryl or both R1 and R2 are hydrogen, halo, (C1-4)alkyl or â€”X3OR9, wherein X3 and R9 are as defined below, or R1 and R2 together with the carbon atom to which both R1 and R2 are attached form (C3-8)cycloalkylene or (C3-8)heterocycloalkylene; R22 at the first occurrence is selected from a group consisting of nitro, â€”X3NR9R9, â€”X3SR9, â€”X3C(O)NR9R9, â€”X3C(O)OR9, â€”X3S(O)R10, â€”X3S(O)2R10, â€”X3C(O)R10 and â€”X3OR23, wherein X3 is a bond or (C1-2)alkylene, R9 at each occurrence independently is hydrogen, (C1-3)alkyl or halo-substituted (C1-3)alkyl, R10 is (C1-3)alkyl or halo-substituted (C1-3)alkyl and R23 is halo-substituted (C1-3)alkyl and R22 at each other occurrence, independently is selected from a group consisting of (C1-4)alkyl, cyano, halo, halo-substituted (C1-4)alkyl, nitro, â€”X3NR9R9, â€”X3OR9, â€”X3SR9, â€”X3C(O)NR9R9, â€”X3C(O)OR9, â€”X3S(O)R10, â€”X3S(O)2R10 and â€”X3C(O)R10, wherein X3, R9 and R10 are as defined above; and R4 is â€”C(O)X4R11 or â€”S(O)2X4R11, wherein X4 is a bond, â€”Oâ€” or â€”NR12â€”, wherein R12 is hydrogen or (C1-6)alkyl, and R11 is (i) (C1-6)alkyl optionally substituted by â€”OR13, â€”SR13, â€”S(O)R13, â€”S(O)2R13, â€”C(O)R13, â€”C(O)OR13, â€”C(O)R13R14, â€”NR13R14, â€”NR14C(O)R13, â€”NR14C(O)OR13, â€”NR14C(O)NR13R14 or â€”NR14C(NR14)NR13R14, wherein R13 is (C3-12)cycloalkyl(C0-3)alkyl, hetero(C5-12)cycloalkyl(C0-3)alkyl, (C6-12)aryl(C0-3)alkyl hetero(C5-12)aryl(C0-3)alkyl, (C9-12)bicycloaryl(C0-3)alkyl or hetero(C8-12)bicycloaryl(C0-3)alkyl, and R14 at each occurrence independently is hydrogen or (C1-6)alkyl, or (ii)(C3-12)cycloalkyl(C0-3)alkyl, hetero(C5-12)cycloalkyl(C0-3)alkyl, (C6-12)aryl(C0-3)alkyl, hetero(C5-12)aryl(C0-3)alkyl, (C9-12)bicycloaryl(C0-3)alkyl or hetero(C8-12)bicycloaryl(C0-3)alkyl or (iii) (C3-6)cycloalkyl(C0-3)alkyl, hetero(C5-6)cycloalkyl(C0-3)alkyl, phenyl(C0-3)alkyl or hetero(C5-6)aryl(C0-3)alkyl substituted by â€”X5OR15, â€”X5SR15, â€”X5S(O)R15, â€”X5S(O)2R15, â€”X5(O)R15, â€”X5C(O)OR15, â€”X5C(O)NR15R16, â€”X5NR15R16, â€”X5NR16C(O)R15, â€”X5NR16C(O)OR15, â€”X5NR16C(O)NR15R16 OR â€”X5NR16C(NR16)NR15R16, wherein X5 is a bond or methylene, R15 is (C3-6)cycloalkyl(C0-3)alkyl, hetero(C5-6)cycloalkyl(C1-6)alkyl; wherein R4 phenyl(C0-3)alkyl or hetero(C5-6)aryl(C0-3)alkyl and R16 is hydrogen or (C1-6)alkyl; wherein R4 optionally further contains 1 to 5 substituents which when occurring within an alicyclic or aromatic ring system are radicals independently selected from a group consisting of (C1-6)alkyl, (C1-6)alkylidene, cyano, halo, halo-substituted (C1-3)alkyl, nitro, â€”X5NR17R17, â€”X5NR17C(O)OR17, â€”X5NR17C(O)NR17R17, â€”X5NR17C(NR17)NR17R17, â€”X5OR17, â€”X5SR17, â€”X5C(O)OR17, â€”X5C(O)NR17R17, â€”X5S(O)2NR17R17, â€”X5P(O)(OR17)OR17, â€”X5P(O)(OR17)OR17, â€”X5NR17C(O)R17, â€”X5S(O)R18, â€”X5S(O)2R18 and â€”X5C(O)R18 and when occurring within an aliphatic moiety are radicals independently selected from a group consisting of cyano, halo, nitro, â€”NR14R17, â€”NR17C(O)OR17, â€”NR17C(O)NR17R17, â€”NR17C(NR17)NR17R17, â€”OR17, â€”SR17, â€”C(O)OR17, â€”C(O)NR17R17, â€”S(O)2NR17R17, â€”P(O)(OR17)OR17, â€”OP(O)(OR17)OR17, â€”NR17C(O)R18, â€”S(O)R18, â€”S(O)2R18 and â€”C(O)R18, wherein X5 is a bond or (C1-6)alkylene, R17 at each occurrence independently is hydrogen, (C1-6)alkyl or halo-substituted (C1-3)alkyl and R18 is (C1-6)alkyl or halo-substituted (C1-3)alkyl; and the N-oxide derivatives, individual isomers or mixtures of isomers thereof; or the pharmaceutically acceptable salts or solvates of such compounds or the N-oxide derivatives, individual isomers or mixtures of isomers thereof.