Patent ID: 6492367
Filing Date: 2002-12-10
Classification: A61P,C07D,Y02P

Abstract:
A compound or a pharmaceutically acceptable salt thereof, wherein:the compound corresponds in structure to the following formula: â€ƒas to R1 and R2: R1 and R2, taken together with the carbon to which they are bonded, form a heterocyclo or cycloalkyl, wherein: the heterocyclo or cycloalkyl optionally is substituted with up to 3 independently selected Rx substituents, or R1 and R2 are independently selected from the group consisting of hydrogen, alkyl, alkoxyalkyl, alkylthioalkyl, alkenyl, alkynyl, aryl, arylalkyl, arylalkoxyalkyl, aryloxyalkyl, arylthioalkyl, arylalkylthioalkyl, cycloalkyl, bicycloalkyl, cycloalkenyl, cycloalkylalkyl, bicycloalkylalkyl, cycloalkyloxyalkyl, bicycloalkyloxyalkyl, cycloalkylalkoxyalkyl, bicycloalkyloxyalkyl, cycloalkylthioalkyl, bicycloalkylthioalkyl, cycloalkylalkylthioalkyl, bicycloalkylalkylthioalkyl, heterocyclo, heterocycloalkyl, heteroaryl, biarylalkyl, arylalkenyl, arylalkynyl, heterocycloalkylthio, heterocycloalkyloxyalkyl, heteroarylalkenyl, and heteroarylalkoxyalkyl, wherein: any such substituent (other than hydrogen) optionally is substituted with up to 3 independently selected Rx substituents; each Rx is independently selected from the group consisting of aryl, heteroaryl, heterocyclo, arylcarbonyl, alkylcarbonyl, heteroarylcarbonyl, halogen, cyano, aldehydo, hydroxy, RcRd-amino, RcRd-aminoalkyl, nitro, nitroso, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, alkoxy, aryloxy, heteroaryloxy, alkenyloxy, alkynyloxy, alkoxyaryl, alkoxyheteroaryl, alkoxyalkyl, Rc-oxyalkyl, alkylenedioxy, aryloxyalkyl, perfluoroalkyl, trifluoroalkyl, alkylthio, arylthio, alkoxycarbonyl, alkoxycarbonyloxy, aryloxycarbonyl, arylalkoxycarbonyl, alkoxycarbonyl-Rc-amino, arylalkoxycarbonyl-Rc-amino, aryloxycarbonyloxy, carboxy, RcRd-aminocarbonyloxy, RcRd-aminocarbonyl, RcRd-aminoalkylcarbonyl, hydroxy-Rc-aminocarbonyl, RcRd-aminosulfonyl, arylsulfonyl(Rc)amino, RcRd-aminoalkoxy, RcRd-aminocarbonyl(Rc)amino, trifluoromethylsulfonyl(Rc)amino, heteroarylsulfonyl-(Rc)amino, alkylsulfonyl, arylsulfonyl(Rc)amino, arylsulfonyl(Rc)aminocarbonyl, alkylsulfonyl-(Rc)amino, arylcarbonyl(Rc)-aminosulfonyl, and alkylsulfonyl(Rc)aminocarbonyl; each Rc and Rd is independently selected from the group consisting of hydrogen, alkylcarbonyl, arylalkyl, arylcarbonyl, bisalkoxyalkyl, alkyl, haloalkyl, perfluoroalkyl, trifluoromethylalkyl, perfluoroalkoxyalkyl, alkoxyalkyl, cycloalkyl, heterocycloalkyl, heterocycloalkylcarbonyl, aryl, heterocyclo, heteroaryl, cycloalkylalkyl, aryloxyalkyl, heteroaryloxyalkyl, heteroarylalkoxyalkyl, heteroarylthioalkyl, arylsulfonyl, alkylsulfonyl, heteroarylsulfonyl, carboxyalkyl, alkoxycarbonylalkyl, aminocarbonyl, alkyliminocarbonyl, aryliminocarbonyl, heterocycloiminocarbonyl, arylthioalkyl, alkylthioalkyl, arylthioalkenyl, alkylthioalkenyl, heteroarylalkyl, haloalkylcarbonyl, hydroxyalkylcarbonyl, thiolalkylcarbonyl, alkenyl, alkynyl, alkoxycarbonyl, aryloxycarbonyl, aminoalkylcarbonyl, hydroxyalkyl, aminoalkyl, aminoalkylsulfonyl, and aminosulfonyl, wherein: any amino nitrogen of Rc or Rd optionally is substituted with up to 2 independently selected RY substituents, and any amino nitrogen of Rc or Rd optionally is substituted with 2 substituents such that the 2 substituents, taken together with the amino nitrogen, form: a saturated or partially unsaturated heterocyclo group optionally substituted with up to 3 independently selected Rw substituents, or a heteroaryl group optionally substituted with up to 3 independently selected Rv substituents; each Ry is independently selected from the group consisting of arylalkyl, aryl, heteroaryl, heterocyclo, alkyl, alkynyl, alkenyl, alkoxyalkyl, substituted aminoalkyl, unsubstituted aminoalkyl, alkoxycarbonyl, arylalkoxycarbonyl, carboxyalkyl, haloalkyl, alkylcarbonyl, arylcarbonyl, substituted aminoalkylcarbonyl, unsubstituted aminoalkylcarbonyl, haloalkylcarbonyl, and hydroxyalkyl, wherein: any such substituent optionally is substituted by up to 2 independently selected Ru substituents, and the amino nitrogen of the substituted aminoalkyl or substituted aminoalkylcarbonyl is substituted with 1 or 2 independently selected Ru substituents; each Rv is independently selected from the group consisting of aryl, heteroaryl, heterocyclo, arylcarbonyl, alkylcarbonyl, heteroarylcarbonyl, halogen, cyano, aldehydo, hydroxy, amino, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, alkoxy, aryloxy, heteroaryloxy, alkenyloxy, alkynyloxy, alkoxyaryl, alkoxyheteroaryl, RyRz-amino, alkoxyalkyl, alkylenedioxy, aryloxyalkyl, perfluoroalkyl, trifluoroalkyl, alkylthio, arylthio, alkoxycarbonyl, alkoxycarbonyloxy, aryloxycarbonyl, arylalkoxycarbonyl, arylalkoxycarbonylamino, aryloxycarbonyloxy, carboxy, RyRz-aminocarbonyloxy, RyRz-aminocarbonyl, RyRz-aminoalkylcarbonyl, hydroxyaminocarbonyl, RyRz-aminosulfonyl, RyRz-aminocarbonyl(Ry)amino, trifluoromethylsulfonyl(Ry)amino, heteroarylsulfonyl-(Ry)amino, arylsulfonyl(Ry)amino, arylsulfonyl(Ry)-aminocarbonyl, alkylsulfonyl(Ry)amino, arylcarbonyl-(Ry)aminosulfonyl, and alkylsulfonyl(Ry)-aminocarbonyl; each Rw is independently selected from the group consisting of hydrogen, aryl, heteroaryl, heterocyclo, arylcarbonyl, alkylcarbonyl, heteroarylcarbonyl, halogen, cyano, aldehydo, hydroxy, amino, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, alkoxy, aryloxy, heteroaryloxy, alkenyloxy, alkynyloxy, alkoxyaryl, alkoxyheteroaryl, RyRz-amino, alkoxyalkyl, alkylenedioxy, aryloxyalkyl, perfluoroalkyl, trifluoroalkyl, alkylthio, arylthio, alkoxycarbonyl, alkoxycarbonyloxy, aryloxycarbonyl, arylalkoxycarbonyl, arylalkoxycarbonylamino, aryloxycarbonyloxy, carboxy, RyRz-aminocarbonyloxy, RyRz-aminocarbonyl, RyRz-aminoalkylcarbonyl, hydroxyaminocarbonyl, RyRz-aminosulfonyl, RyRz-aminocarbonyl(Ry)amino, trifluoromethylsulfonyl(Ry)amino, heteroarylsulfonyl-(Ry)amino, arylsulfonyl(Ry)amino, arylsulfonyl(Ry)-aminocarbonyl, alkylsulfonyl(Ry)amino, arylcarbonyl-(Ry)aminosulfonyl, and alkylsulfonyl(Ry)-aminocarbonyl; each Rz is independently selected from the group consisting of arylalkyl, aryl, heteroaryl, heterocyclo, alkyl, alkynyl, alkenyl, alkoxyalkyl, alkoxyalkyl, substituted aminoalkyl, unsubstituted aminoalkyl, alkoxycarbonyl, arylalkoxycarbonyl, carboxyalkyl, haloalkyl, alkylcarbonyl, arylcarbonyl, substituted aminoalkylcarbonyl, unsubstituted aminoalkylcarbonyl, haloalkylcarbonyl, and hydroxyalkyl, wherein: each such substituent optionally is substituted by up to 2 independently selected Ru substituents, and the amino nitrogen of the substituted aminoalkyl or substituted aminoalkylcarbonyl is substituted with 1 or 2 independently selected Ru substituents; each Ru is independently selected from the group consisting of arylalkyl, aryl, heteroaryl, heterocyclo, alkyl, alkynyl, alkenyl, alkoxyalkyl, substituted aminoalkyl, unsubstituted aminoalkyl, alkoxycarbonyl, arylalkoxycarbonyl, carboxyalkyl, haloalkyl, alkylcarbonyl, arylcarbonyl, substituted aminoalkylcarbonyl, unsubstituted aminoalkylcarbonyl, haloalkylcarbonyl, and hydroxyalkyl, wherein: the amino nitrogen of the substituted aminoalkyl or substituted aminoalkylcarbonyl is substituted with 1 or 2 substituents independently selected from the group consisting of alkyl, alkenyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, aryloxycarbonyl, and alkoxycarbonyl; R is selected from the group consisting of alkyl, alkoxyalkyl, aryl, heteroaryl, cycloalkyl, heterocycloalkyl, aralkyl, heteroaralkyl, heterocycloalkyl, cycloalkylalkyl, cycloalkyloxyalkyl, heterocycloalkyloxyalkyl, aryloxyalkyl, heteroaryloxyalkyl, arylthioalkyl, heteroarylthioalkyl, cycloalkylthioalkyl, and heterocycloalkylthioalkyl, wherein: the aryl, heteroaryl, cycloalkyl, or heterocycloalkyl optionally is substituted with up to 2 substituents (in addition to -EY2) independently selected from the group consisting of halogen, alkyl, perfluoroalkyl, perfluoroalkoxy, perfluoroalkylthio, trifluoromethylalkyl, amino, alkoxycarbonylalkyl, alkoxy, C1-C2-alkylene-dioxy, hydroxycarbonylalkyl, hydroxycarbonylalkylamino, nitro, hydroxy, hydroxyalkyl, alkylcarbonylamino, and alkoxycarbonyl; E is selected from the group consisting of: (1) â€”CO(Rw)â€”, (2) â€”(Rw)COâ€”, (3) â€”CONHâ€”, (4) â€”HNCOâ€”, (5) â€”COâ€”, (6) â€”SO2Rw, (7) â€”RwSO2, (8) â€”SO2â€”, (9) â€”NHâ€”SO2â€”, (10) â€”SO2â€”NHâ€”, and (11) a bond; Y2 is selected from the group consisting of hydrogen, alkyl, alkoxy, haloalkyl, haloalkoxy, aryl, arylalkyl, cycloalkyl, heteroaryl, hydroxy, aryloxy, arylalkoxy, heteroaryloxy, heteroarylalkyl, haloalkylthio, alkenyl, heterocycloalkyl, alkoxycarbonyl, and aminoalkyl, wherein: the aryl, heteroaryl, or heterocycloalkyl optionally is substituted with up to 2 substituents independently selected from the group consisting of alkylcarbonyl, halogen, nitro, nitrile, alkyl, haloalkyl, arylalkyl, aryl, alkoxy, and amino, wherein: the amino nitrogen optionally is substituted with up to 2 substituents independently selected from the group consisting of alkyl and arylalkyl; R20 is selected from the group consisting of â€”Oâ€”R21, â€”NHâ€”Oâ€”R22, and â€”NHâ€”Oâ€”R14; R21 is selected from the group consisting of hydrogen, C1-C6-alkyl, aryl, and aryl-C1-C6-alkyl; R22 is a selectively removable protecting group; R14 is selected from the group consisting of hydrogen and C(W)R15; R15 is selected from the group consisting of C1-C6-alkyl, aryl, C1-C6-alkoxy, heteroaryl-C1-C6-alkyl, C3-C8-cycloalkyl-C1-C6-alkyl, aryloxy, aryl-C1-C6-alkoxy, aryl-C1-C6-alkyl, heteroaryl, and amino-C1-C6-alkyl, wherein: the amino-C1-C6-alkyl nitrogen optionally is substituted with up to 2 substituents independently selected from the group consisting of C1-C6-alkyl, aryl, aryl-C1-C6-alkyl, C3-C8-cycloalkyl-C1-C6-alkyl, aryl-C1-C6-alkoxycarbonyl, C1-C6-alkoxycarbonyl, and C1-C6-alkylcarbonyl, or the amino-C1-C6-alkyl nitrogen optionally is substituted with 2 substituents such that the 2 substituents, together with the nitrogen, form a 5- to 8-membered heterocyclo or heteroaryl ring; W is selected from the group consisting of O and S; and in addition to any other possible substitutions, any heterocyclo or heteroaryl substituent optionally is substituted: on any carbon ring atom with up to 2 substituents independently selected from the group consisting of halogen, alkyl, alkoxy, and oxo, on any sulfur ring atom with up to 2 oxo, and on any secondary nitrogen ring atom with a substituent independently selected from the group consisting of alkyl, arylalkoxycarbonyl, alkylcarbonyl, aryl, and arylalkyl.