主权项 |
1. A compound of Formula I wherein: R1 is azetidinyl, pyrrolyl, pyrazolyl, imidazolyl, triazolyl, thiazolyl, pyridyl, pyridyl N-oxide, pyrazinyl, pyrimidinyl, pyridazyl, piperidinyl, quinazolinyl, cinnolinyl, benzothiazolyl, indazolyl, tetrahydropyranyl, tetrahydrofuranyl, furanyl, phenyl, oxazolyl, isoxazolyl, thiophenyl, benzoxazolyl, benzimidazolyl, indolyl, thiadiazolyl, oxadiazolyl or quinolinyl; wherein said piperidinyl, pyridyl, pyridyl N-oxide, pyrimidinyl, pyridazyl, pyrazinyl, quinazolinyl, cinnolinyl, benzothiazolyl, indazolyl, imidazolyl, phenyl, thiophenyl, benzoxazolyl, benzimidazolyl, indolyl, quinolinyl, and pyrazolyl are optionally substituted with C(O)C(1-4)alkyl, C(O)NH2, C(O)NHC(1-2)alkyl, C(O)N(C(1-2)alkyl)2, NHC(O)C(1-4)alkyl, NHSO2C(1-4)alkyl, C(1-4)alkyl, CF3, CH2CF3, Cl, F, —CN, OC(1-4)alkyl, N(C(1-4)alkyl)2, —(CH2)3OCH3, SC(1-4)alkyl, OH, CO2H, CO2C(1-4)alkyl, C(O)CF3, SO2CF3, OCF3, OCHF2, SO2CH3, SO2NH2, SO2NHC(1-2)alkyl, SO2N(C(1-2)alkyl)2, C(O)NHSO2CH3, or OCH2OCH3; and optionally substituted with up to two additional substituents independently selected from the group consisting of Cl, C(1-2)alkyl, SCH3, OC(1-2)alkyl, CF3, —CN, and F; and wherein said triazolyl, oxazolyl, isoxazolyl, pyrrolyl, and thiazolyl are optionally substituted with up to two substituents independently selected from the group consisting of SO2CH3, SO2NH2, C(O)NH2, —CN, OC(1-2)alkyl, (CH2)(2-3)OCH3, SCH3, CF3, F, Cl, and C(1-2)alkyl; and said thiadiazolyl and oxadiazolyl are optionally substituted with C(1-2)alkyl; and said pyridyl, pyridyl-N-oxide, pyrimidinyl, pyridazyl, and pyrazinyl are optionally substituted with up to three additional substituents independently selected from the group consisting of C(O)NHC(1-2)alkyl, C(O)N(C(1-2)alkyl)2, NHC(O)C(1-4)alkyl, NHSO2C(1-4)alkyl, C(O)CF3, SO2CF3, SO2NHC(1-2)alkyl, SO2N(C(1-2)alkyl)2, C(O)NHSO2CH3, SO2CH3, SO2NH2, C(O)NH2, —CN, OC(1-4)alkyl, (CH2)(2-3)OCH3, SC(1-4)alkyl, CF3, F, Cl, and C(1-4)alkyl; and wherein said azetidinyl is optionally substituted with C(1-3)alkyl, C(O)C(1-2)alkylOH, C(O)NH2, CO2C(CH3)3, SO2CH3, Or C(O)CH3; R2 is C(1-6)alkyl, C(3-6)cycloalkyl, or alkynyl; wherein said C(1-6)alkyl or C(3-6)cycloalkyl is optionally substituted with NH2, NHC(1-2)alkyl, N(C(1-2)alkyl)2, SO2C(1-2)alkyl, SO2NH2, SO2NHC(1-2)alkyl, SO2N(C(1-2)alkyl)2, CF3, COOH, NHC(O)C(1-2)alkyl, N(C(1-2)alkyl)C(O)C(1-2)alkyl, NHSO2C(1-2)alkyl, N(C(1-2)alkyl)SO2C(1-2)alkyl, C(O)NHC(1-2)alkyl, C(O)N(C(1-2)alkyl)2, OH, —CN, OCF3, OCHF2, C(O)NH2, OC(1-4)alkyl, or up to three fluorine atoms; and wherein said alkynyl is optionally substituted with C(1-3)alkyl; R3 is H, OH, OCH3, or NH2; R4 is H, or F; R5 is H, Cl, —CN, CF3, SC(1-4)alkyl, OC(1-4)alkyl, OH, C(1-4)alkyl, N(CH3)OCH3, NH(C(1-4)alkyl), N(C(1-4)alkyl)2, 4-hydroxy-piperidinyl, azetidin-1-yl, or fur-2-yl; provided that R5 may not be H if R7 is OCH3; R6 is pyridyl, pyrimidinyl, pyridazyl, pyrazinyl, thiazolyl, isothiazolyl, furanyl, thiophenyl, oxazolyl, isoxazolyl, imidazolyl, pyrazolyl, pyrrolyl, triazolyl, oxadiazolyl, thiadiazolyl, or phenyl, any of which is optionally substituted with up to two substituents independently selected from the group consisting of piperidinyl, pyrrolidinyl, azetidinyl, pyrazolyl, triazolyl, imidazolyl, —CN, C(1-4)alkyl, OC(1-4)alkyl, C(O)C(1-4)alkyl, CO2H, CO2C(1-4)alkyl, NH2, NHC(1-2)alkyl, N(C(1-2)alkyl)2, SO2NH2, SONH2, SO2NHC(1-2)alkyl, SON(CH3)2, SO2N(C(1-2)alkyl)2, SCH3, OCH2CF3, SO2CH3, CF3, Cl, F, OH, and OCF3; or R6 is —O-phenyl, —NHphenyl, —N(C(1-3)alkyl)phenyl, —N(CO2C(CH3)3)phenyl, N(COCH3)phenyl, —O-pyridyl, —NHpyridyl, —N(C(1-3)alkyl)pyridyl, N(CO2C(CH3)3)pyridyl, N(COCH3)pyridyl, —O-pyrimidinyl, —NHpyrimidinyl, —N(C(1-3)alkyl)pyrimidinyl, N(CO2C(CH3)3)pyrimidinyl, N(COCH3)pyrimidinyl, —O-pyridazyl, —NHpyridazyl, —N(C(1-3)alkyl)pyridazyl, N(CO2C(CH3)3)pyridazyl, N(COCH3)pyridazyl, —O-pyrazinyl, —NHpyrazinyl, —N(C(1-3)alkyl)pyrazinyl, N(CO2C(CH3)3)pyrazinyl, or N(COCH3)pyrazinyl; wherein said pyrimidinyl portions thereof, pyridazyl portions thereof, or pyrazinyl portions thereof are optionally substituted with Cl, F, CH3, SCH3, OC(1-4)alkyl, —CN, CONH2, SO2NH2, or SO2CH3; and wherein said phenyl portions thereof or said pyridyl portions thereof are optionally substituted with up to two substituents independently selected from the group consisting of OCF3, SO2C(1-4)alkyl, CF3, CHF2, pyrazolyl, triazolyl, imidazolyl, tetrazolyl, oxazolyl, thiazolyl, C(1-4)alkyl, C(3-4)cycloalkyl, OC(1-4)alkyl, N(CH3)2, SO2NH2, SO2NHCH3, SO2N(CH3)2, CONH2, CONHCH3, CON(CH3)2, Cl, F, —CN, CO2H, OH, CH2OH, NHCOC(1-2)alkyl, COC(1-2)alkyl, SCH3, CO2C(1-4)alkyl, NH2, NHC(1-2)alkyl, and OCH2CF3; and wherein said pyrazolyl, triazolyl, imidazolyl, tetrazolyl, oxazolyl, and thiazolyl are optionally further substituted with CH3; or R6 is —CH2R6, wherein R6 is pyridyl, phenyl, benzothiophenyl, thiophenyl, pyrimidinyl, pyridazyl, or pyrazinyl; wherein said pyrimidinyl, pyridazyl, or pyrazinyl are optionally substituted with Cl, F, CH3, SCH3, OC(1-4)alkyl, —CN, CONH2, SO2NH2, or SO2CH3; and wherein said pyridyl or phenyl is optionally substituted with up to two substituents independently selected from the group consisting of OCF3, SO2C(1-4)alkyl, CF3, CHF2, pyrazolyl, triazolyl, imidazolyl, tetrazolyl, oxazolyl, thiazolyl, C(1-4)alkyl, C(3-4)cycloalkyl, OC(1-4)alkyl, N(CH3)2, SO2NH2, SO2NHCH3, SO2N(CH3)2, CONH2, CONHCH3, CON(CH3)2, Cl, F, —CN, CO2H, OH, CH2OH, NHCOC(1-2)alkyl, COC(1-2)alkyl, SCH3, CO2C(1-4)alkyl, NH2, NHC(1-2)alkyl, and OCH2CF3; and wherein said pyrazolyl, triazolyl, imidazolyl, tetrazolyl, oxazolyl, and thiazolyl are optionally further substituted with CH3; R7 is H, Cl, —CN, C(1-4)alkyl, OC(1-4)alkylCF3, OCF3, OCHF2, OCH2CH2OC(1-4)alkyl, CF3, SCH3, C(1-4)alkylNA1A2, CH2OC(2-3)alkylNA1A2, NA1A2, C(O)NA1A2, CH2NHC(2-3)alkylNA1A2, CH2N(CH3)C(2-3)alkylNA1A2, NHC(2-3)alkylNA1A2, N(CH3)C(2-4)alkylNA1A2, OC(2-4)alkylNA1A2, OC(1-4)alkyl, OCH2-(1-methyl)-imidazol-2-yl, phenyl, thiophenyl, furyl, pyrazolyl, imidazolyl, pyridyl, pyridazyl, pyrazinyl, pyrimidinyl, indazolyl, phenyl, orwherein said phenyl, thiophenyl, furyl, pyrazolyl, imidazolyl, pyridyl, pyridazyl, pyrazinyl, pyrimidinyl, and indazolyl are optionally substituted with up to three substituents independently selected from the group consisting of F, Cl, CH3, CF3, and OCH3;
A1 is H or C(1-4)alkyl; A2 is H, C(1-4)alkyl, C(1-4)alkylOC(1-4)alkyl, C(1-4)alkylOH, C(O)C(1-4)alkyl, or OC(1-4)alkyl; or A1 and A2 may be taken together with their attached nitrogen to form a ring selected from the group consisting of: Ra is H, OC(1-4)alkyl, CH2OH, NH(CH3), N(CH3)2, NH2, CH3, F, CF3, SO2CH3, or OH; Rb is H, CO2C(CH3)3, C(1-4)alkyl, C(O)C(1-4)alkyl, SO2C(1-4)alkyl, CH2CH2CF3, CH2CF3, CH2-cyclopropyl, phenyl, CH2-phenyl, or C(3-6)cycloalkyl; R8 is H, C(1-3)alkyl, OC(1-3)alkyl, CF3, NH2, NHCH3, —CN, or F; R9 is H, or F;and pharmaceutically acceptable salts thereof. |