Patent ID: 6525059
Filing Date: 2003-02-25
Classification: A61P,C07D

Abstract:
A compound of Formula IB: whereinR1 is selected from the group consisting of hydrogen, hydroxy, alkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, cycloalkylalkylene, cycloalkenylalkylene, haloalkyl, haloalkenyl, haloalkynyl, hydroxyalkyl, hydroxyalkenyl, hydroxyalkynyl, aralkyl, aralkenyl, aralkynyl, carboxy, carboxyalkyl, alkoxyalkyl, alkenoxyalkyl, alkynoxyalkyl, aryloxyalkyl, alkoxyaryl, alkoxyalkoxy, mercaptoalkyl, alkylthioalkylene, alkenylthioalkylene, alkylthioalkenylene, amino, aminoalkyl, alkylamino, alkenylamino, alkynylamino, arylamino, alkylsulfinyl, alkenylsulfinyl, alkynylsulfinyl, arylsulfinyl, alkylsulfonyl, alkenylsulfonyl, alkynylsulfonyl, arylsulfonyl, alkylaminoalkylene, alkylsulfonylalkylene, acyl, acyloxycarbonyl, alkoxycarbonylalkylene, aryloxycarbonylalkylene, alkoxycarbonylarylene, aryloxycarbonylarylene, alkylcarbonylalkylene, arylcarbonylalkylene, alkylcarbonylarylene, arylcarbonylarylene, alkylcarbonyloxyalkylene, arylcarbonyloxyalkylene, alkylcarbonyloxyarylene, and arylcarbonyloxyarylene; or R1 has the formula wherein:i is an integer from 0 to 9; R25 is selected from the group consisting of hydrogen, alkyl, aralkyl, alkoxyalkylene, aryloxyalkylene, aminoalkyl, alkylaminoalkyl, arylaminoalkyl, alkylcarbonylalkylene, and arylcarbonylalkylene; and R26 is selected from the group consisting of hydrogen, alkyl, alkenyl, alkynyl, cycloalkylalkylene, aralkyl, alkoxycarbonylalkylene, and alkylaminoalkyl; and R27 is selected from the group consisting of alkyl, cycloalkyl, alkynyl, aryl, aralkyl, cycloalkylalkylene, cycloalkenylalkylene, cycloalkylarylene, cycloalkylcycloalkyl, alkylarylene, alkylaralkyl, aralkylarylene, alkoxyalkylene, alkoxyarylene, alkoxyaralkyl, alkoxyalkoxyarylene, aryloxyarylene, aralkoxyarylene, aryloxyalkoxyarylene, alkoxycarbonylalkylene, aminoalkyl, alkylaminoalkylene, arylaminocarbonylalkylene, alkoxyarylaminocarbonylalkylene, aminocarbonylalkylene, arylaminocarbonylalkylene, alkylaminocarbonylalkylene, arylcarbonylalkylene, alkoxycarbonylarylene, aryloxycarbonylarylene, alkylaryloxycarbonylarylene, arylcarbonylarylene, alkylarylcarbonylarylene, alkoxycarbonylalkoxylarylene, alkylthioalkylene, cycloalkylthioalkylene, alkylthioarylene, aralkylthioarylene, arylthioalklylarylene, arylsulfonylaminoalkylene, alkylsulfonylarylene, and alkylaminosulfonylarylene; wherein said alkyl, cycloalkyl, aryl, aralkyl, alkoxyarylene, aryloxyarylene, arylaminocarbonylalkylene, aryloxycarbonylarylene, arylcarbonylarylene, alkylthioarylene, arylthioalklylarylene, and alkylsulfonylarylene groups may be optionally substituted with one or more substituents independently selected from the group consisting of alkyl, halo, haloalkyl, alkoxy, keto, amino, nitro, and cyano; or R27 is â€”CHR28R29 wherein R28 is alkoxycarbonyl, and R29 is selected from the group consisting of aralkyl, aralkoxyalkylene, alkoxycarbonylalkylene, alkylthioalkylene, and aralkylthioalkylene; wherein said aralkyl group may be optionally substituted with one or more substituents independently selected from the group consisting of alkyl and nitro; and R2 is piperidinyl substituted with one or more substituents selected from the group consisting of hydroxyalkyl, hydroxyalkenyl, hydroxyalkynyl, alkoxyalkylene, alkoxyalkenylene, alkoxyalkynylene, and hydroxyacyl, wherein said hydroxyalkyl, hydroxyalkenyl, hydroxyalkynyl, alkoxyalkylene, alkoxyalkenylene, alkoxyalkynylene, and hydroxyacyl substitutents may be optionally substituted with one or more substituents selected from the group consisting of cycloalkyl, alkyl, aryl, arylalkyl, and haloalkyl, wherein said cycloalkyl, alkyl, aryl, arylalkyl, and haloalkyl substituents may be optionally substituted with one or more substituents selected from the group consisting of alkylene, alkynylene, hydroxy, halo, haloalkyl, alkoxy, keto, amino, nitro, cyano, alkylsulfonyl, alkylsulfinyl, alkylthio, alkoxyalkyl, and aryloxy; or R2 is piperidinyl substituted with one or more substituents selected from the group consisting of hydroxycycloalkyl and alkoxycycloalkyl, and wherein said hydroxycycloalkyl and alkoxycycloalkyl substitutents may be optionally substituted with one or more substituents selected from the group consisting of cycloalkyl, alkyl, aryl, arylalkyl, and haloalkyl, wherein said cycloalkyl, alkyl, aryl, arylalkyl, and haloalkyl substituents may be optionally substituted with one or more substituents selected from the group consisting of alkylene, alkynylene, hydroxy, halo, haloalkyl, alkoxy, keto, amino, nitro, cyano, alkylsulfonyl, alkylsulfinyl, alkylthio, alkoxyalkyl, and aryloxy; and R3 is pyrimidinyl, wherein said pyrimidinyl may be optionally substituted with one or more substituents independently selected from the group consisting of hydrogen, aryl, alkylamino, alkylthio, alkyloxy, aryloxy, arylamino, arylthio, and aralkoxy, wherein said aryl, alkylamino, alkylthio, alkyloxy, aryloxy, arylamino, arylthio, and aralkoxy substituents may be optionally substituted with one or more substituents selected from the group consisting of alkylene, alkenylene, hydroxy, halo, haloalkyl, alkoxy, keto, amino, nitro, cyano, alkylsulfonyl, alkylsulfinyl, alkylthio, alkoxyalkyl, and aryloxy; and R4 is phenyl, wherein said phenyl may be optionally substituted with one or more substituents independently selected from the group consisting of halo, haloalkyl, haloalkoxy, alkoxy, cyano, hydroxy, alkyl, alkenyl, and alkynyl, wherein said haloalkyl, haloalkoxy, alkoxy, cyano, hydroxy, alkyl, alkenyl, and alkynyl substituents may be optionally substituted with one or more substituents selected from the group consisting of alkylene, alkenylene, alkynylene, hydroxy, halo, haloalkyl, alkoxy, keto, amino, nitro, cyano, alkylsulfonyl, alkylsulfinyl, alkylthio, alkoxyalkyl, and aryloxy; or a pharmaceutically-acceptable salt or tautomer thereof.