Patent ID: 6403587
Filing Date: 2002-06-11
Classification: A61P,C07C,C07D

Abstract:
A compound of the formula whereinR1 is quinoxalin-2-yl or quinoxalin-6-yl optionally substituted with one or more substituents independently selected from the group consisting of hydrogen, halo, CN, (C1-C6)alkyl optionally substituted with one or more fluorine atoms, hydroxy, hydroxy-(C1-C6)alkyl, (C1-C6)alkoxy optionally substituted with one or more fluorine atoms, (C1-C6)alkoxy(C1-C6)alkyl, HOâ€”(C&boxH;O)â€”, (C1-C6)alkyl-Oâ€”(C&boxH;O)â€”, HOâ€”(C&boxH;O)â€”(C1-C6)alkyl, (C1-C6)alkyl-Oâ€”(C&boxH;O)â€”(C1-C6)alkyl, (C1-C6)alkyl-(C&boxH;O)â€”Oâ€”, (C1-C6)alkyl-(C&boxH;O)â€”Oâ€”(C1-C6)alkyl, H(O&boxH;C)â€”, H(O&boxH;C)â€”(C1-C6)alkyl, (C1-C6)alkyl(O&boxH;C)â€”, (C1-C6)alkyl(O&boxH;C)â€”(C1-C6)alkyl, NO2, amino, (C1-C6)alkylamino, [(C1-C6)alkyl]2amino, amino(C1-C6)alkyl, (C1-C6)alkylamino(C1-C6)alkyl, [(C1-C6)alkyl]2amino(C1-C6)alkyl, H2Nâ€”(C&boxH;O)â€”, (C1-C6)alkyl-NHâ€”(C&boxH;O)â€”, [(C1-C6)alkyl]2Nâ€”(C&boxH;O)â€”, H2N(C&boxH;O)â€”(C1-C6)alkyl, (C1-C6)alkyl-HN(C&boxH;O)â€”(C1-C6)alkyl, [(C1-C6)alkyl]2Nâ€”(C&boxH;O)â€”(C1-C6)alkyl, H(O&boxH;C)â€”NHâ€”, (C1-C6)alkyl(C&boxH;O)â€”NH, (C1-C6)alkyl(C&boxH;O)â€”[NH](C1-C6)alkyl, (C1-C6)alkyl(C&boxH;O)â€”[N(C1-C6)alkyl](C1-C6)alkyl, (C1-C6)alkyl-Sâ€”, (C1-C6)alkyl-(S&boxH;O)â€”, (C1-C6)alkyl-SO2â€”, (C1-C6)alkyl-SO2â€”NHâ€”, H2Nâ€”SO2â€”, H2Nâ€”SO2â€”(C1-C6)alkyl, (C1-C6)alkyl HNâ€”SO2â€”(C1-C6)alkyl, [(C1-C6)alkyl]2Nâ€”SO2â€”(C1-C6)alkyl, CF3SO3â€”, (C1-C6)alkyl-SO3â€”, phenyl, (C3-C10)cycloalkyl, (C2-C9)heterocycloalkyl, and (C2-C9)heteroaryl; R2 is phenyl-(CH2)mâ€”, naphthyl-(CH2)mâ€”, (C3-C10)cycloalkyl-(CH2)mâ€”, (C1-C6)alkyl or (C2-C9)heteroaryl-(CH2)mâ€”, wherein m is an interger from zero to four; wherein each of said phenyl, naphthyl, (C3-C10)cycloalkyl or (C2-C9)heteroaryl moieties of said phenyl-(CH2)mâ€”, naphthyl-(CH2)mâ€”, (C3-C10)cycloalkyl-(CH2)mâ€” or (C2-C9)heteroaryl-(CH2)mâ€” groups may optionally be substituted with one or more substituents independently selected from hydrogen, halo, CN, (C1-C6)alkyl optionally substituted with one or more fluorine atoms, hydroxy, hydroxy-(C1-C6)alkyl, (C1-C6)alkoxy optionally substituted with one or more fluorine atoms, (C1-C6)alkoxy(C1-C6)alkyl, HOâ€”(C&boxH;O)â€”, (C1-C6)alkyl-Oâ€”(C&boxH;O)â€”, HOâ€”(C&boxH;O)â€”(C1-C6)alkyl, (C1-C6)alkyl-Oâ€”(C&boxH;O)â€”(C1-C6)alkyl, (C1-C6)alkyl-(C&boxH;O)â€”Oâ€”, (C1-C6)alkyl-(C&boxH;O)â€”Oâ€”(C1-C6)alkyl, H(O&boxH;C)â€”, H(O&boxH;C)â€”(C1-C6)alkyl, (C1-C6)alkyl(O&boxH;C)â€”, (C1-C6)alkyl(O&boxH;C)â€”(C1-C6)alkyl, NO2, amino, (C1-C6)alkylamino, [(C1-C6)alkyl]2amino, amino(C1-C6)alkyl, (C1-C6)alkylamino(C1-C6)alkyl, [(C1-C6)alkyl]2amino(C1-C6)alkyl, H2Nâ€”(C&boxH;O)â€”, (C1-C6)alkyl-NHâ€”(C&boxH;O)â€”, [(C1-C6)alkyl]2Nâ€”(C&boxH;O)â€”, H2N(C&boxH;O)â€”(C1-C6)alkyl, (C1-C6)alkyl-HN(C&boxH;O)â€”(C1-C6)alkyl, [(C1-C6)alkyl]2Nâ€”(C&boxH;O)â€”(C1-C6)alkyl, H(O&boxH;C)â€”NHâ€”, (C1-C6)alkyl(C&boxH;O)â€”NH, (C1-C6)alkyl(C&boxH;O)â€”[NH](C1-C6)alkyl, (C1-C6)alkyl(C&boxH;O)â€”[N(C1-C6)alkyl](C1-C6)alkyl, (C1-C6)alkyl-Sâ€”, (C1-C6)alkyl-(S&boxH;O)â€”, (C1-C6)alkyl-SO2â€”, (C1-C6)alkyl-SO2â€”NHâ€”, H2Nâ€”SO2â€”, H2Nâ€”SO2â€”(C1-C6)alkyl, (C1-C6)alkylHNâ€”SO2â€”(C1-C6)alkyl, [(C1-C6)alkyl]2Nâ€”SO2â€”(C1-C6)alkyl, CF3SO3â€”, (C1-C6)alkyl-SO3â€”, phenyl, phenoxy, benzyloxy, (C3-C10)cycloalkyl, (C2-C9)heterocycloalkyl, and (C2-C9)heteroaryl; R3 is hydrogen, (C1-C10)alkyl, (C3-C10)cycloalkyl-(CH2)nâ€”, (C2-C9)heterocycloalkyl-(CH2)nâ€”, (C2-C9)heteroaryl-(CH2)nâ€” or aryl-(CH2)nâ€”; wherein n is an interger from zero to six; wherein said R3 (C1-C10)alkyl group may optionally be substituted with one or more substituents, independently selected from hydrogen, halo, CN, (C1-C6)alkyl optionally substituted with one or more fluorine atoms, hydroxy, hydroxy-(C1-C6)alkyl, (C1-C6)alkoxy, optionally substituted with one or more fluorine atoms, (C1-C6)alkoxy(C1-C6)alkyl, HOâ€”(C&boxH;O)â€”(C1-C6)alkyl-Oâ€”(C&boxH;O)â€”, HOâ€”(C&boxH;O)â€”(C1-C6)alkyl, (C1-C6)alkyl-Oâ€”(C&boxH;O)â€”(C1-C6)alkyl, (C1-C6)alkyl-(C&boxH;O)â€”Oâ€”, (C1-C6)alkyl-(C&boxH;O)â€”Oâ€”(C1-C6)alkyl, H(O&boxH;C)â€”, H(O&boxH;C)â€”(C1-C6)alkyl, (C1-C6)alkyl(O&boxH;C)â€”, (C1-C6)alkyl(O&boxH;C)â€”(C1-C6)alkyl, NO2, amino, (C1-C6)alkylamino, [(C1-C6)alkyl]2amino, amino(C1-C6)alkyl, (C1-C6)alkylamino(C1-C6)alkyl, [(C1-C6)alkyl]2amino(C1-C6)alkyl, H2Nâ€”(C&boxH;O)â€”, (C1-C6)alkyl-NHâ€”(C&boxH;O)â€”, [(C1-C6)alkyl]2Nâ€”(C&boxH;O)â€”, H2N(C&boxH;O)â€”(C1-C6)alkyl, (C1-C6)alkyl-HN(C&boxH;O)â€”(C1-C6)alkyl, [(C1-C6)alkyl]2Nâ€”(C&boxH;O)â€”(C1-C6)alkyl, H(O&boxH;C)â€”NHâ€”, (C1-C6)alkyl(C&boxH;O)â€”NH, (C1-C6)alkyl(C&boxH;O)â€”[NH](C1-C6)alkyl, (C1-C6)alkyl(C&boxH;O)â€”[N(C1-C6)alkyl](C1-C6)alkyl, (C1-C6)alkyl-Sâ€”, (C1-C6)alkyl-(S&boxH;O)â€”, (C1-C6)alkyl-SO2â€”, (C1-C6)alkyl-SO2â€”NHâ€”, H2Nâ€”SO2â€”, H2Nâ€”SO2â€”(C1-C6)alkyl, (C1-C6)alkylHNâ€”SO2â€”(C1-C6)alkyl, [(C1-C6)alkyl]2Nâ€”SO2â€”(C1-C6)alkyl, CF3SO3â€”, (C1-C6)alkyl-SO3â€”, phenyl, (C3-C10)cycloalkyl, (C2-C9)heterocycloalkyl, and (C2-C9)heteroaryl; and wherein any of the carbon-carbon single bonds of said (C1-C10)alkyl may optionally be replaced by a carbon-carbon double bond; wherein the (C3-C10)cycloalkyl moiety of said R3 (C3-C10)cycloalkyl-(CH2)nâ€” group may optionally be substituted by one to three substitutents independently selected from the group consisting of hydrogen, halo, CN, (C1-C6)alkyl optionally substituted with one or more fluorine atoms, hydroxy, hydroxy-(C1-C6)alkyl, (C1-C6)alkoxy optionally substituted with one or more fluorine atoms, (C1-C6)alkoxy(C1-C6)alkyl, HOâ€”(C&boxH;O)â€”, (C1-C6)alkyl-Oâ€”(C&boxH;O)â€”, HOâ€”(C&boxH;O)â€”(C1-C6)alkyl, (C1-C6)alkyl-Oâ€”(C&boxH;O)â€”(C1-C6)alkyl, (C1-C6)alkyl-(C&boxH;O)â€”Oâ€”, (C1-C6)alkyl-(C&boxH;O)â€”Oâ€”(C1-C6)alkyl, H(O&boxH;C)â€”, H(O&boxH;C)â€”(C1-C6)alkyl, (C1-C6)alkyl(O&boxH;C)â€”, (C1-C6)alkyl(O&boxH;C)â€”(C1-C6)alkyl, NO2, amino, (C1-C6)alkylamino, [(C1-C6)alkyl]2amino, amino(C1-C6)alkyl, (C1-C6)alkylamino(C1-C6)alkyl, [(C1-C6)alkyl]2amino(C1-C6)alkyl, H2Nâ€”(C&boxH;O)â€”, (C1-C6)alkyl-NHâ€”(C&boxH;O)â€”, [(C1-C6)alkyl]2Nâ€”(C&boxH;O)â€”, H2N(C&boxH;O)â€”(C1-C6)alkyl, (C1-C6)alkyl-HN(C&boxH;O)â€”(C1-C6)alkyl, [(C1-C6)alkyl]2Nâ€”(C&boxH;O)â€”(C1-C6)alkyl, H(O&boxH;C)â€”NHâ€”, (C1-C6)alkyl(C&boxH;O)â€”NH, (C1-C6)alkyl(C&boxH;O)â€”[NH](C1-C6)alkyl, (C1-C6)alkyl(C&boxH;O)â€”[N(C1-C6)alkyl](C1-C6)alkyl, (C1-C6)alkyl-Sâ€”, (C1-C6)alkyl-(S&boxH;O)â€”, (C1-C6)alkyl-SO2â€”, (C1-C6)alkyl-SO2â€”NHâ€”, H2Nâ€”SO2â€”, H2Nâ€”SO2â€”(C1-C6)alkyl, (C1-C6)alkylHNâ€”SO2â€”(C1-C6)alkyl, [(C1-C6)alkyl]2Nâ€”SO2â€”(C1-C6)alkyl, CF3SO3â€”, (C1-C6)alkyl-SO3â€”, phenyl, (C3-C10)cycloalkyl. (C2-C9)heterocycloalkyl, and (C2-C9)heteroaryl; wherein the (C2-C9)heterocycloalkyl moiety of said R3 (C2-C9)heterocycloalkyl-(CH2)nâ€” group may contain from one to three heteroatoms independently selected from nitrogen, sulfur, oxygen, >S(&boxH;O), >SO2 or >NR6, wherein said (C2-C9)heterocycloalkyl moiety of said (C2-C9)heterocycloalkyl-(CH2)mâ€” group may optionally be substituted on any of the ring carbon atoms capable of forming an additional bond with a substituent independently selected from the group consisting of hydrogen, halo, CN, (C1-C6)alkyl optionally substituted with one or more fluorine atoms, hydroxy, hydroxy-(C1-C6)alkyl, (C1-C6)alkoxy optionally substituted with one or more fluorine atoms, (C1-C6)alkoxy(C1-C6)alkyl, HOâ€”(C&boxH;O)â€”, (C1-C6)alkyl-Oâ€”(C&boxH;O)â€”, HOâ€”(C&boxH;O)â€”(C1-C6)alkyl, (C1-C6)alkyl-Oâ€”(C&boxH;O)â€”(C1-C6)alkyl, (C1-C6)alkyl-(C&boxH;O)â€”Oâ€”, (C1-C6)alkyl-(C&boxH;O)â€”Oâ€”(C1-C6)alkyl, H(O&boxH;C)â€”, H(O&boxH;C)â€”(C1-C6)alkyl, (C1-C6)alkyl(O&boxH;C)â€”, (C1-C6)alkyl(O&boxH;C)â€”(C1-C6)alkyl, NO2, amino, (C1-C6)alkylamino, [(C1-C6)alkyl]2amino, amino(C1-C6)alkyl, (C1-C6)alkylamino(C1-C6)alkyl, [(C1-C6)alkyl]2amino(C1-C6)alkyl, H2Nâ€”(C&boxH;O)â€”, (C1-C6)alkyl-NHâ€”(C&boxH;O)â€”, [(C1-C6)alkyl]2Nâ€”(C&boxH;O)â€”, H2N(C&boxH;O)â€”(C1-C6)alkyl, (C1-C6)alkyl-HN(C&boxH;O)â€”(C1-C6)alkyl, [(C1-C6)alkyl]2Nâ€”(C&boxH;O)â€”(C1-C6)alkyl, H(O&boxH;C)â€”NHâ€”, (C1-C6)alkyl(C&boxH;O)â€”NH, (C1-C6)alkyl(C&boxH;O)â€”[NH](C1-C6)alkyl, (C1-C6)alkyl(C&boxH;O)â€”[N(C1-C6)alkyl](C1-C6)alkyl, (C1-C6)alkyl-Sâ€”, (C1-C6)alkyl-(S&boxH;O)â€”, (C1-C6)alkyl-SO2â€”, (C1-C6)alkyl-SO2â€”NHâ€”, H2Nâ€”SO2â€”, H2Nâ€”SO2â€”(C1-C6)alkyl, (C1-C6)alkylHNâ€”SO2â€”(C1-C6)alkyl, [(C1-C6)alkyl]2Nâ€”SO2â€”(C2-C6)alkyl, CF3SO3â€”, (C1-C6)alkyl-SO3â€”, phenyl, (C3-C10)cycloalkyl, (C2-C9)heterocycloalkyl, and (C2-C9)heteroaryl; wherein the (C2-C9)heteroaryl moiety of said R3 (C2-C9)heteroaryl-(CH2)nâ€” group may contain from one to three heteroatoms independently selected from nitrogen, sulfur or oxygen wherein said (C2-C9)heteroaryl moiety of said (C2-C9)heteroaryl-(CH2)nâ€” group may optionally be substituted on any of the ring carbon atoms capable of forming an additional bond with a substituent selected from the group consisting of hydrogen, halo, CN, (C1-C6)alkyl optionally substituted with one or more fluorine atoms, hydroxy, hydroxy-(C1-C6)alkyl, (C1-C6)alkoxy optionally substituted with one or more fluorine atoms, (C1-C6)alkoxy(C1-C6)alkyl, HOâ€”(C&boxH;O)â€”, (C1-C6)alkyl-Oâ€”(C&boxH;O)â€”, HOâ€”(C&boxH;O)â€”(C1-C6)alkyl, (C1-C6)alkyl-Oâ€”(C&boxH;O)â€”(C1-C6)alkyl, (C1-C6)alkyl-(C&boxH;O)â€”Oâ€”, (C1-C6)alkyl-(C&boxH;O)â€”Oâ€”(C1-C6)alkyl, H(O&boxH;C)â€”, H(O&boxH;C)â€”(C1-C6)alkyl, (C1-C6)alkyl(O&boxH;C)â€”, (C1-C6)alkyl(O&boxH;C)â€”(C1-C6)alkyl, NO2, amino, (C1-C6)alkylamino, [(C1-C6)alkyl]2amino, amino(C1-C6)alkyl, (C1-C6)alkylamino(C1-C6)alkyl, [(C1-C6)alkyl]2amino(C1-C6)alkyl, H2Nâ€”(C&boxH;O)â€”, (C1-C6)alkyl-NHâ€”(C&boxH;O)â€”, [(C1-C6)alkyl]2Nâ€”(C&boxH;O)â€”, H2N(C&boxH;O)â€”(C1-C6)alkyl, (C1-C6)alkyl-HN(C&boxH;O)â€”(C1-C6)alkyl, [(C1-C6)alkyl]2Nâ€”(C&boxH;O)â€”(C1-C6)alkyl, H(O&boxH;C)â€”NHâ€”, (C1-C6)alkyl(C&boxH;O)â€”NH, (C1-C6)alkyl(C&boxH;O)â€”[NH](C1-C6)alkyl, (C1-C6)alkyl(C&boxH;O)â€”[N(C1-C6)alkyl](C1-C6)alkyl, (C1-C6)alkyl-Sâ€”, (C1-C6)alkyl-(S&boxH;O)â€”, (C1-C6)alkyl-SO2â€”, (C1-C6)alkyl-SO2â€”NHâ€”, H2Nâ€”SO2â€”, H2Nâ€”SO2â€”(C1-C6)alkyl, (C1-C6)alkylHNâ€”SO2â€”(C1-C6)alkyl, [(C1-C6)alkyl]2Nâ€”SO2â€”(C1-C6)alkyl, CF3SO3â€”, (C1-C6)alkyl-SO3â€”, phenyl, (C3-C10)cycloalkyl, (C2-C9)heterocycloalkyl, and (C2-C9)heteroaryl; and wherein said aryl moiety of said R3 aryl-(CH2)nâ€” group is optionally substituted phenyl or naphthyl, wherein said phenyl and naphthyl may optionally be substituted with from one to three substituents independently selected from the group consisting of hydrogen, halo, CN, (C1-C6)alkyl optionally substituted with one or more fluorine atoms, hydroxy, hydroxy-(C1-C6)alkyl, (C1-C6)alkoxy optionally substituted with one or more fluorine atoms, (C1-C6)alkoxy(C1-C6)alkyl, HOâ€”(C&boxH;O)â€”, (C1-C6)alkyl-Oâ€”(C&boxH;O)â€”, HOâ€”(C&boxH;O)â€”(C1-C6)alkyl, (C1-C6)alkyl-Oâ€”(C&boxH;O)â€”(C1-C6)alkyl, (C1-C6)alkyl-(C&boxH;O)â€”Oâ€”, (C1-C6)alkyl-(C&boxH;O)â€”Oâ€”(C1-C6)alkyl, H(O&boxH;C)â€”, H(O&boxH;C)â€”(C1-C6)alkyl, (C1-C6)alkyl(O&boxH;C)â€”, (C1-C6)alkyl(O&boxH;C)â€”(C1-C6)alkyl, NO2, amino, (C1-C6)alkylamino, [(C1-C6)alkyl]2amino, amino(C1-C6)alkyl, (C1-C6)alkylamino(C1-C6)alkyl, [(C1-C6)alkyl]2amino(C1-C6)alkyl, H2Nâ€”(C&boxH;O)â€”, (C1-C6)alkkyl-NHâ€”(C&boxH;O)â€”, [(C1-C6)alkyl]2Nâ€”(C&boxH;O)â€”, H2N(C&boxH;O)â€”(C1-C6)alkyl, (C1-C6)alkyl-HN(C&boxH;O)â€”(C1-C6)alkyl, [(C1-C6)alkyl]2Nâ€”(C&boxH;O)â€”(C1-C6)alkyl, H(O&boxH;C)â€”NHâ€”, (C1-C6)alkyl(C&boxH;O)â€”NH, (C1-C6)alkyl(C&boxH;O)â€”[NH](C1-C6)alkyl, (C1-C6)alkyl(C&boxH;O)â€”[N(C1-C6)alkyl](C1-C6)alkyl, (C1-C6)alkyl-Sâ€”, (C1-C6)alkyl-(S&boxH;O)â€”, (C1-C6)alkyl-SO2â€”, (C1-C6)alkyl-SO2â€”NHâ€”, H2Nâ€”SO2â€”, H2Nâ€”SO2â€”(C1-C6)alkyl, (C1-C6)alkylHNâ€”SO2â€”(C1-C6)alkyl, [(C1-C6)alkyl]2Nâ€”SO2â€”(C1-C6)alkyl, CF3SO3â€”, (C1-C6)alkyl-SO3â€”, phenyl, (C3-C10)cycloalkyl, (C2-C9)heterocycloalkyl, and (C2-C9)heteroaryl; or R3 and the carbon to which it is attached form a five to seven membered carbocyclic ring, wherein any of the carbon atoms of said five membered carbocyclic ring may optionally be substituted with a substituent selected from the group consisting of hydrogen, halo, CN, (C1-C6)alkyl optionally substituted with one or more fluorine atoms (preferably one to three fluorine atoms), hydroxy, hydroxy-(C1-C6)alkyl, (C1-C6)alkoxy optionally substituted with one or more fluorine atoms (preferably one to three fluorine atoms), (C1-C6)alkoxy(C1-C6)alkyl, HOâ€”(C&boxH;O)â€”, (C1-C6)alkyl-Oâ€”(C&boxH;O)â€”, HOâ€”(C&boxH;O)â€”(C1-C6)alkyl, (C1-C6)alkyl-Oâ€”(C&boxH;O)â€”(C1-C6)alkyl, (C1-C6)alkyl-(C&boxH;O)â€”Oâ€”, (C1-C6)alkyl-(C&boxH;O)â€”Oâ€”(C1-C6)alkyl, H(O&boxH;C)â€”, H(O&boxH;C)â€”(C1-C6)alkyl, (C1-C6)alkyl(O&boxH;C)â€”, (C1-C6)alkyl(O&boxH;C)â€”(C1-C6)alkyl, NO2, amino, (C1-C6)alkylamino, [(C1-C6)alkyl]2amino, amino(C1-C6)alkyl, (C1-C6)alkylamino(C1-C6)alkyl, [(C1-C6)alkyl]2amino(C1-C6)alkyl, H2Nâ€”(C&boxH;O)â€”, (C1-C6)alkyl-NHâ€”(C&boxH;O)â€”, [(C1-C6)alkyl]2Nâ€”(C&boxH;O)â€”, H2N(C&boxH;O)â€”(C1-C6)alkyl, (C1-C6)alkyl-HN(C&boxH;O)â€”(C1-C6)alkyl, [(C1-C6)alkyl]2Nâ€”(C&boxH;O)â€”(C1-C6)alkyl, H(O&boxH;C)â€”NHâ€”, (C1-C6)alkyl(C&boxH;O)â€”NH, (C1-C6)alkyl(C&boxH;O)â€”[NH](C1-C6)alkyl, (C1-C6)alkyl(C&boxH;O)â€”[N(C1-C6)alkyl](C1-C6)alkyl, (C1-C6)alkyl-Sâ€”, (C1-C6)alkyl-(S&boxH;O)â€”, (C1-C6)alkyl-SO2â€”, (C1-C6)alkyl-SO2â€”NHâ€”, H2Nâ€”SO2â€”, H2Nâ€”SO2â€”(C1-C6)alkyl, (C1-C6)alkylHNâ€”SO2â€”(C1-C6)alkyl, [(C1-C6)alkyl]2Nâ€”SO2â€”(C1-C6)alkyl, CF3SO3â€”, (C1-C6)alkyl-SO3â€”, phenyl, (C3-C10)cycloalkyl, (C2-C9)heterocycloalkyl, and (C2-C9)heteroaryl; wherein one of the carbon-carbon bonds of said five to seven membered carbocyclic ring may optionally be fused to an optionally substituted phenyl ring, wherein said substitutents may be independently selected from hydrogen, halo, CN, (C1-C6)alkyl optionally substituted with one or more fluorine atoms (preferably one to three fluorine atoms), hydroxy, hydroxy-(C1-C6)alkyl, (C1-C6)alkoxy optionally substituted with one or more fluorine atoms (preferably one to three fluorine atoms), (C1-C6)alkoxy(C1-C6)alkyl, HOâ€”(C&boxH;O)â€”, (C1-C6)alkyl-Oâ€”(C&boxH;O)â€”, HOâ€”(C&boxH;O)â€”(C1-C6)alkyl, (C1-C6)alkyl-Oâ€”(C&boxH;O)â€”(C1-C6)alkyl, (C1-C6)alkyl-(C&boxH;O)â€”Oâ€”, (C1-C6)alkyl-(C&boxH;O)â€”Oâ€”(C1-C6)alkyl, H(O&boxH;C)â€”, H(O&boxH;C)â€”(C1-C6)alkyl, (C1-C6)alkyl(O&boxH;C)â€”, (C1-C6)alkyl(O&boxH;C)â€”(C1-C6)alkyl, NO2, amino, (C1-C6)alkylamino, [(C1-C6)alkyl]2amino, amino(C1-C6)alkyl, (C1-C6)alkylamino(C1-C6)alkyl, [(C1-C6)alkyl]2amino(C1-C6)alkyl, H2Nâ€”(C&boxH;O)â€”, (C1-C6)alkyl-NHâ€”(C&boxH;O)â€”, [(C1-C6)alkyl]2Nâ€”(C&boxH;O)â€”, H2N(C&boxH;O)â€”(C1-C6)alkyl, (C1-C6)alkyl-HN(C&boxH;O)â€”(C1-C6)alkyl, [(C1-C6)alkyl]2Nâ€”(C&boxH;O)â€”(C1-C6)alkyl, H(O&boxH;C)â€”NHâ€”, (C1-C6)alkyl(C&boxH;O)â€”NH, (C1-C6)alkyl(C&boxH;O)â€”[NH](C1-C6)alkyl, (C1-C6)alkyl(C&boxH;O)â€”[N(C1-C6)alkyl](C1-C6)alkyl, (C1-C6)alkyl-Sâ€”, (C1-C6)alkyl-(S&boxH;O)â€”, (C1-C6)alkyl-SO2â€”, (C1-C6)alkyl-SO2â€”NHâ€”, H2Nâ€”SO2â€”, H2Nâ€”SO2â€”(C1-C6)alkyl, (C1-C6)alkylHNâ€”SO2â€”(C1-C6)alkyl, [(C1-C6)alkyl]2Nâ€”SO2â€”(C1-C6)alkyl, CF3SO3â€”, (C1-C6)alkyl-Sâ€”O3â€”, phenyl, (C3-C10)cycloalkyl, (C2-C9)heterocycloalkyl, and (C2-C9)heteroaryl; R4 is hydrogen, (C1-C6)alkyl, hydroxy, (C1-C6)alkoxy, hydroxy(C1-C6)alkyl, (C1-C6)alkoxy(C&boxH;O)â€”, (C3-C10)cycloalkyl-(CH2)pâ€”, (C2-C9)heterocycloalkyl-(CH2)pâ€”, (C2-C9)heteroaryl-(CH2)pâ€”, phenyl-(CH2)pâ€”, or naphthyl-(CH2)pâ€”, wherein p is an integer from zero to four; wherein said (C2-C9)heterocycloalkyl, (C2-C9)heteroaryl, phenyl and naphthyl groups of said (C2-C9)heterocycloalkyl-(CH2)pâ€”, (C2-C9)heteroaryl-(CH2)pâ€”, phenyl-(CH2)pâ€”, or naphthyl-(CH2)pâ€” may be optionally substituted on any of the ring atoms capable of supporting an additional bond with a substituent selected from the group consisting of hydrogen, halo, CN, (C1-C6)alkyl optionally substituted with one or more fluorine atoms, hydroxy, hydroxy-(C1-C6)alkyl, (C1-C6)alkoxy optionally substituted with one or more fluorine atoms, (C1-C6)alkoxy(C1-C6)alkyl, HOâ€”(C&boxH;O)â€”, (C1-C6)alkyl-Oâ€”(C&boxH;O)â€”, HOâ€”(C&boxH;O)â€”(C1-C6)alkyl, (C1-C6)alkyl-Oâ€”(C&boxH;O)â€”(C1-C6)alkyl, (C1-C6)alkyl-(C&boxH;O)â€”Oâ€”, (C1-C6)alkyl-(C&boxH;O)â€”Oâ€”(C1-C6)alkyl, H(O&boxH;C)â€”, H(O&boxH;C)â€”(C1-C6)alkyl, (C1-C6) alkyl(O&boxH;C)â€”, (C1-C6)alkyl(O&boxH;C)â€”(C1-C6)alkyl, NO2, amino, (C1-C6)alkylamino, [(C1-C6)alkyl]2 amino, amino(C1-C6)alkyl, (C1-C6)alkylamino (C1-C6)alkyl, [(C1-C6)alkyl]2amino(C1-C6)alkyl, H2Nâ€”, (C&boxH;O)â€”, (C1-C6)alkyl-NHâ€”(C&boxH;O)â€”, [(C1-C6)alkyl]2Nâ€”(C&boxH;O)â€”, H2N(C&boxH;O)â€”(C1-C6)alkyl, (C1-C6)alkyl-HN(C&boxH;O)â€”(C1-C6)alkyl, [(C1-C6)alkyl]2Nâ€”(C&boxH;O)â€”(C1-C6)alkyl, H(O&boxH;C)â€”NHâ€”, (C1-C6)alkyl(C&boxH;O)â€”NH, (C1-C6)alkyl(C&boxH;O)â€”[NH](C1-C6)alkyl, (C1-C6)alkyl(C&boxH;O)â€”[N(C1-C6)alkyl](C1-C6)alkyl, (C1-C6)alkyl-Sâ€”, (C1-C6)alkyl-(S&boxH;O)â€”, (C1-C6)alkyl-SO2â€”, (C1-C6)alkyl-SO2â€”NHâ€”, H2Nâ€”SO2â€”, H2Nâ€”SO2â€”(C1-C6)alkyl, (C1-C6)alkylHNâ€”SO2â€”(C1-C6)alkyl, [(C1-C6)alkyl]2Nâ€”SO2â€”(C1-C6)alkyl, CF3SO3â€”, (C1-C6)alkyl-SO3â€”, phenyl, (C3-C10)cycloalkyl, (C2-C9)heterocycloalkyl, and (C2-C9)heteroaryl; R5 is hydrogen, (C1-C6)alkyl or amino; R6 is hydrogen, (C1-C6)alkyl, (C1-C6)alkoxy-(CH2)gâ€”, (C1-C6)alkoxy(C&boxH;O)â€”(CH2)gâ€”, (C1-C6)alkyl-(SO2)â€”(CH2)gâ€”, (C6-C10)aryloxy-(CH2)gâ€”, (C6-C10)aryloxy(C&boxH;O)â€”(CH2)gâ€”, and (C6-C10)aryl-(SO2)â€”(CH2)gâ€”, wherein g is an integer from 1 to four; with the proviso that when either R4 or R5 is hydrogen, and the other of R4 or R5 is (C1-C6)alkyl, or morpholinoethyl, R2 is (C3-C10)cycloalkyl or isopropyl and R3 is (C3-C5)alkyl, phenyl, methylvinyl, dimethylvinyl, halovinyl, hydroxy(C1-C3)alkyl or amino(C1-C4)alkyl then R1 must be other than indol-5-yl, 6-azaindol-2-yl, 2,3-dichloro-pyrol-5-yl, 4-hydroxyquinolin-3-yl, 2-hydroxyquinoxalin-3-yl, 6-azaindolin-3-yl, or optionally substituted indol-2 or 3-yl; and the pharmaceutically acceptable salts of such compounds.