Patent ID: 6683077
Filing Date: 2004-01-27
Classification: A61P,C07D

Abstract:
A compound of Formula I wherein R and R2 are independently selected from hydrido, halo, alkyl, wherein R1 is a substituent selected from hydrido, halo, alkoxy, and alkyl; wherein R3 is selected from hydrido, alkyl, alkylaminoalkyl, aralkyl, and heterocyclylalkyl; wherein R4 is selected from hydrido, alkyl, cycloalkyl, cycloalkylalkyl, aryl, heterocyclyl, aralkyl, heterocyclylalkyl, â€ƒor wherein â€”NR3R4 forms a heterocyclic ring of 5 to 7 members; wherein n is 0-6, inclusive; wherein R5 and R6 are independently selected from hydrido, alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, heterocyclyl, heterocyclylalkyl, alkylaminoalkyl, aralkylaminoalkyl, alkoxyalkyl, and aralkoxyalkyl; or wherein â€”NR5R6 forms a heterocyclic ring of 5 to 7 members; wherein R7, R12 and R23 are independently selected from hydrido, alkyl and aralkyl; wherein R8, R9 and R14 are independently selected from hydrido, alkyl, cycloalkyl, cycloalkylalkyl, haloalkyl, aminoalkyl, alkylaminoalkyl, carboxyalkyl, aminocarbonylalkyl, alkylaminocarbonylalkyl, hydroxyalkyl, alkoxyalkyl, aralkoxyalkyl, alkylsulfonylalkyl, alkylsulfinylalkyl, alkylthioalkyl, aryl, aralkyl, aralkenyl, heterocyclyl, and heterocyclylalkyl; or wherein â€”NR8R9 forms a heterocyclic ring of 5 to 7 members; wherein R10 is selected from alkyl, haloalkyl, alkylaminoalkyl, carboxyalkyl, aminocarbonylalkyl, alkylaminocarbonylalkyl, aralkoxyalkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, alkylsulfonylalkyl, alkylsulfinylalkyl, alkylthioalkyl, aryl, aralkyl, heterocyclyl, and heterocyclylalkyl; wherein R11 is alkylene; wherein R13 is selected from amino, alkyl, alkylamino, alkylaminoalkyl and aryl; wherein R15 is selected from hydrido, alkyl, hydroxyalkyl, alkoxyalkyl, aralkoxyalkyl, alkylaminoalkyl and N-aryl-N-alkylaminoalkyl; wherein R16 is selected from hydrido, alkyl, cycloalkyl, cycloalkylalkyl, haloalkyl, guanidinylalkyl, carboxyalkyl, hydroxyalkyl, alkoxyalkyl, aralkoxyalkyl, alkylthioalkyl, alkylsulfinylalkyl, alkylsulfonylalkyl, aryl, heterocyclyl, aralkyl, heterocyclylalkyl, â€ƒor wherein R15 and R16 together form cycloalkyl or heterocyclyl; wherein R17 is selected from hydrido, alkyl, cycloalkyl and aralkyl; wherein R18 and R19 are independently selected from hydrido, alkyl, alkenyl, cycloalkyl, cycloalkylalkyl, aryl, heterocyclyl, aralkyl, heterocyclylalkyl, alkylaminoalkyl, and heterocyclicalkyl; or wherein â€”NR18R19 together forms a heterocyclic ring of 5 to 7 atoms; or wherein R16 and R18 together form a saturated or partially unsaturated ring of 5 to 7 atoms; wherein R20 is alkylene; wherein R21, R22, R25, and R26 are independently selected from hydrido, alkyl, cycloalkyl, cycloalkylalkyl, aminoalkyl, alkylaminoalkyl, hydroxyalkyl, alkoxyalkyl, aralkoxyalkyl, aryl, heterocyclyl, aralkyl, heterocyclylalkyl; or wherein â€”NR21R22 together forms a heterocyclic ring of 5 to 7 atoms; or wherein â€”NR25R26 together forms a heterocyclic ring of 5 to 7 atoms; wherein R24 is selected from alkyl, cycloalkyl, cycloalkylalkyl, alkylaminoalkyl, aralkoxyalkyl, alkoxyalkyl, aryl, aralkyl, heterocyclyl, and heterocyclylalkyl; and wherein R27 is selected from hydrido, alkyl, cycloalkyl, cycloalkylalkyl, alkylaminoalkyl, aminoalkyl, carboxyalkyl, aminocarbonylalkyl, hydroxyalkyl, aralkoxyalkyl, alkoxyalkyl, aryl, aralkyl, heterocyclyl, and heterocyclylalkyl; provided R3 and R4 do not form benzotriazolyl when R2 is hydrido and when R1 is methyl, ethyl, methoxy, or iodo; further provided R, R2 and R1 are not all hydrido; further provided R2 is not methyl, n-butyl, or acetamido when R1 is methyl and when R3 or R4 is benzyl or lower alkyl; further provided R2 is not halo, propyl, trifluoromethyl, or methyl when R1 is hydrido and when R3 or R4 is benzyl, lower alkyl, phenyl, 2-methyl-, or 4-methylphenyl; further provided R4 is not 2-iodophenyl or â€”CH2CONH2 when R2 is hydrido, halo, methoxy or methyl; further provided R is not methyl or dimethylamino when R2 is hydrido or bromo; and further provided R2 is not hydrido when R3 or R4 is lower alkyl, cycloalkyl, D-phenylglycine, valine amide, arginine methyl ester or leucine methyl ester; or a pharmaceutically-acceptable salt or tautomer thereof.