Patent ID: 6548520
Filing Date: 2003-04-15
Classification: A61P,C07D,Y02A

Abstract:
A compound of the formula: wherein X is oxygen, carbon, sulfur, or nitrogen, or the moiety Xâ€”R1 is hydrogen; V is CH; R1 is hydrogen, C1-6alkyl, aryl, arylC1-6alkyl, pyrrolidine, piperidine, piperazine, morpholine, imidazolidine, pyrazolidine, pyrrolidine C1-6alkyl, piperidine C1-6alkyl, piperazine C1-6alkyl, morpholine C1-6alkyl, imidazolidine C1-6alkyl, pyrazolidine C1-6alkyl, pyrrole, quinoline, isoquinoline, pyridine, pyrimidine, oxazole, thiazole, thiadiazole, triazole, imidazole, or benzimidazole, pyrrole C1-6alkyl, quinoline C1-6alkyl, isoquinoline C1-6alkyl, pyridine C1-6alkyl, pyrimidine C1-6alkyl, oxazole C1-6alkyl, thiazole C1-6alkyl, thiadiazole C1-6alkyl, triazole C1-6alkyl, imidazole C1-6alkyl, or benzimidazole C1-6alkyl; wherein each of these moieties may be optionally substituted; X1 is hydrogen, XR1, optionally substituted C1-4 alkyl, halogen, hydroxy, optionally substituted C1-4 alkoxy, optionally substituted C1-4 alkylthio, optionally substituted C1-4 alkylsulfinyl, CH2OR12, amino, mono and di-C1-6 alkyl substituted amino, N(R10)C(O)Rb, N(R10)S(O)2Rd, or an N-heterocyclyl ring which ring has from 5 to 7 members and optionally contains an additional heteroatom selected from oxygen, sulfur or NR15; Rb is hydrogen, C1-6 alkyl, C3-7 cycloalkyl, aryl, arylC1-4 alkyl, pyrrolidine, piperidine, piperazine, morpholine, imidazolidine, pyrazolidine, pyrrolidine C1-4alkyl, piperidine C1-4alkyl, piperazine C1-4alkyl, morpholine C1-4alkyl, imidazolidine C1-4alkyl, pyrazolidine C1-4alkyl, pyrrole, quinoline, isoquinoline, pyridine, pyrimidine, oxazole, thiazole, thiadiazole, triazole, imidazole, or benzimidazole, pyrrole C1-4alkyl, quinoline C1-4alkyl, isoquinoline C1-4alkyl, pyridine C1-4alkyl, pyrimidine C1-4alkyl, oxazole C1-64alkyl, thiazole C1-4alkyl, thiadiazole C1-4alkyl, triazole C1-4alkyl, imidazole C1-4alkyl, or benzimidazole C1-4alkyl; Rd is C1-6 alkyl, C3-7 cycloalkyl, aryl, arylC1-4 alkyl, pyrrolidine, piperidine, piperazine, morpholine, imidazolidine, pyrazolidine, pyrrolidine C1-4alkyl, piperidine C1-4alkyl, piperazine C1-4alkyl, morpholine C1-4alkyl, imidazolidine C1-4alkyl, pyrazolidine C1-4alkyl, pyrrole, quinoline, isoquinoline, pyridine, pyrimidine, oxazole, thiazole, thiadiazole, triazole, imidazole, or benzimidazole, pyrrole C1-4alkyl, quinoline C1-4alkyl, isoquinoline C1-4alkyl, pyridine C1-4alkyl, pyrimidine C1-4alkyl, oxazole C1-64alkyl, thiazole C1-4alkyl, thiadiazole C1-4alkyl, triazole C1-4alkyl, imidazole C1-4alkyl, or benzimidazole C1-4alkyl; R2 is independently an optionally substituted C1-4 alkyl, and wherein the two R2 moieties may together form a C3-7 cycloalkyl or C5-7 cycloalkenyl ring which ring may be optionally substituted; Y is a C2-4 alkenyl, hydroxy substituted C1-4alkyl, pyrrolidine, piperidine, piperazine, morpholine, imidazolidine, pyrazolidine or N(R10)C(Z)R3; R3 is C1-6alkyl, aryl, arylC1-6alkyl, pyrrolidine, piperidine, piperazine, morpholine, imidazolidine, pyrazolidine, pyrolidine C1-6alkyl, piperidine C1-6alkyl, piperazine C1-6alkyl, morpholine C1-6alkyl, imidazolidine C1-6alkyl, pyrazolidine C1-6alkyl, pyrrole, quinoline, isoquinoline, pyridine, pyrimidine, oxazole, thiazole, thiadiazole, triazole, imidazole, or benzimidazole, pyrrole C1-6alkyl, quinoline C1-6alkyl, isoquinoline C1-6alkyl, pyridine C1-6alkyl, pyrimidine C1-6alkyl, oxazole C1-6alkyl, thiazole C1-6alkyl, thiadiazole C1-6alkyl, triazole C1-6alkyl, imidazole C1-6alkyl, or benzimidazole C1-6alkyl; wherein each of these moieties may be optionally substituted; Ar is an aryl ring which ring may be optionally substituted; R10 is hydrogen or C1-4alkyl; R12 is hydrogen, C(Z)R13 or optionally substituted C1-4 alkyl, optionally substituted aryl, optionally substituted arylC1-4 alkyl, or S(O)2R25; Z is oxygen or sulfur; R13 is hydrogen, C1-10 alkyl, C3-7 cycloalkyl, pyrrolidine, piperidine, piperazine, morpholine, imidazolidine, pyrazolidine, pyrrolidine C1-10 alkyl, piperidine C1-10 alkyl, piperazine C1-10alkyl, morpholine C1-10alkyl, imidazolidine C1-10alkyl, pyrazolidine C1-10alkyl, pyrrole, quinoline, isoquinoline, pyridine, pyrimidine, oxazole, thiazole, thiadiazole, triazole, imidazole, or benzimidazole, pyrrole C1-10alkyl, quinoline C1-10alkyl, isoquinoline C1-10alkyl, pyridine C1-10alkyl, pyrimidine C1-10alkyl, oxazole C1-10alkyl, thiazole C1-10alkyl, thiadiazole C1-10alkyl, triazole C1-10alkyl, imidazole C1-10alkyl, or benzimidazole C1-10alkyl; wherein all of these moieties may be optionally substituted; R15 is hydrogen, cyano, C1-4 alkyl, C3-7 cycloalkyl or aryl; R25 is C1-10 alkyl, C3-7 cycloalkyl, heterocyclyl, aryl, arylalkyl, pyrrolidine, piperidine, piperazine, morpholine, imidazolidine, pyrazolidine, pyrrolidine C1-10 alkyl, piperidine C1-10 alkyl, piperazine C1-10alkyl, morpholine C1-10alkyl, imidazolidine C1-10alkyl, pyrazolidine C1-10alkyl, pyrrole, quinoline, isoquinoline, pyridine, pyrimidine, oxazole, thiazole, thiadiazole, triazole, imidazole, or benzimidazole, pyrrole C1-10alkyl, quinoline C1-10alkyl, isoquinoline C1-10alkyl, pyridine C1-10alkyl, pyrimidine C1-10alkyl, oxazole C1-10alkyl, thiazole C1-10alkyl, thiadiazole C1-10alkyl, triazole C1-10alkyl, imidazole C1-10alkyl, or benzimidazole C1-10alkyl; or pharmaceutically acceptable salt thereof.