Patent ID: 6528535
Filing Date: 2003-03-04
Classification: A61P,C07D

Abstract:
A compound having the Formula I wherein Q is O, â€”NOR, â€”Nâ€”NRR, â€”NOCH2CO2Ra, L is hydrogen, each Ra or Rb is independently hydrogen, C1-C6 alkyl, C2C6 alkenyl, phenyl, or substituted phenyl, or Ra and Rb along with the carbon atom to which they are bonded form a C3-C6 cycloalkyl ring; each R is independently hydrogen, C1-C6 alkyl, C3-C6 cycloalkyl, benzyl, C2-C6 alkenyl, phenyl, or substituted phenyl; Each - - - is a bond or absent; X is CH2O, CH2S, CH2SO, CH2SO2, or CH2NR; Z is hydrogen when L is â€ƒand Z is â€”NRR, â€”R, â€”OR, â€”SR, (CH2)nE, â€”O(CH2)nE, â€”NR(CH2)nE, â€”S(CH2)nE, â€”N1-piperidinyl, â€”N1-piperazinyl[N4â€”R], â€”N-pyrrolidinyl, â€”N-morpholino, â€”N-thiomorpholino, â€”N-hexahydroazepine, or an amino acid having the structure when L is where A is a side chain of the amino acid glycine, alanine, valine, leucine, isoleucine, phenylalanine, proline, serine, threonine, tyrosine, asparagine, glutamine, lysine, arginine, tryptophan, histidine, cysteine, methionine, aspartic acid, or glutamic acid; E is hydrogen, halogen, â€”CO2R, â€”CONRR, â€”CN, â€”NO2, C1-C6 perfluoroalkyl, C1-C6 perfluoroalkoxy, acetyl, â€”OR, â€”SR, â€”NRR, â€”N1-piperidinyl, â€”N1-piperazinyl[N4â€”R], â€”N-pyrrolidinyl, â€”N-morpholino, â€”N-thiomorpholino, â€”N-hexahydroazepine, aryl, heteroaryl, substituted aryl, or substituted heteroaryl; each Eâ€² is independently hydrogen, halogen, â€”NO2, â€”NRR, â€”R, â€”OR, each n is independently 0 to 5 inclusive; each &agr; is independently 0, 1, or 2; each m is independently 0, 2, 3, 4, or 5; Y is CH2, NR, O, SO, SO2, or S; Aâ€² is aryl, heteroaryl, substituted aryl, substituted heteroaryl, C1-C6 alkyl, C1-C6 substituted alkyl, â€ƒC3-C6 cycloalkyl or C3-C6 substituted cycloalkyl, provided any substituents are not â€”NO2; B is pyrrolyl, substituted pyrrolyl, imidazolyl, substituted imidazolyl, oxazolyl, substituted oxazolyl, thiazolyl, substituted thiazolyl, â€”NR1â€”(CH2)nâ€”(CHX3)â€”(CH2)nâ€”SR1, â€”Sâ€”(CH2)nâ€”(CHX3)â€”(CH2)nâ€”SR1, or â€”(CH2)nâ€”(CHX3)â€”(CH2)nâ€”SR1; X1 is S or NR1; X2 is NR1 or CH2; R1 is hydrogen or C1-C6 alkyl; X3 is hydrogen â€”NR1R1 or â€”C1-C6 alkyl, and the pharmaceutically acceptable salts, esters, amides, and prodrugs thereof, provided that the compound is not 5-(2-imidazole-1-yl-ethoxy)-indan-1-one.