| 主权项 |
1. A compound of formula (I) wherein R0 is selected from the group consisting of hydrogen and hydroxy;is selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl, furyl, thienyl, pyridyl, thiazolyl, benzothiazolyl and benzo[d][1,3]dioxolyl,
wherein the phenyl, furyl, thienyl, pyridyl, thiazolyl, benzothiazolyl or benzo[d][1,3]dioxolyl is optionally substituted with one or more substituents independently selected from the group consisting of halogen, hydroxy, 4alkyl, fluorinated C1-4alkyl, C1-4alkoxy, fluorinated C1-4alkoxy, cyano, —C(O)OH, C(O)O—C1-4alkyl, —C(O)NRARB and NRARB; wherein RA and RB are each independently selected from the group consisting of hydrogen, C1-4alkyl, hydroxy substituted C1-2alkyl and carboxy substituted C1-2alkyl, provided that each substituent is bound to a carbon atom of the ring;is selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl, furyl, thienyl, pyridyl, thiazolyl, benzothiazolyl and benzo[d][1,3]dioxolyl,
wherein the phenyl, furyl, thienyl, pyridyl, thiazolyl, benzothiazolyl or benzo[d][1,3]dioxolyl is optionally substituted with one or more substituents independently selected from the group consisting of halogen, hydroxy, C1-4alkyl, fluorinated C1-4alkyl, C1-4alkoxy, fluorinated C1-4alkoxy, cyano, —C(O)OH, C(O)O—C1-4alkyl, —C(O)NRCRD and NRCRD, wherein RC and RD are each independently selected from the group consisting of hydrogen, C1-4alkyl, hydroxy substituted C1-2alkyl and carboxy substituted C1-2alkyl, provided that each substituent is bound to a carbon atom of the ring;is selected from the group consisting of
(a)wherein R1 is selected from the group consisting of hydrogen, C1-4alkyl, hydroxy substituted C1-4alkyl, —C(O)—(C1-4alkyl), —(C1-2alkyl)-C(O)OH, —(C1-2alkyl)-C(O)—O—(C1-4alkyl), —(C1-2alkyl)-O—(C1-2alkyl)-C(O)OH, —(C1-2alkyl)-C(O)—NRERF, —SO2-(fluorinated C3-6cycloalkyl and benzyl;
wherein the benzyl is optionally substituted with one substituent selected from the group consisting of —C(O)OH, —C(O)O—(C1-4alkyl) and —C(O)—NRERF, and wherein RE and RF are each independently selected from the group consisting of hydrogen and C1-2alkyl, and (b)wherein R2 is selected from the group consisting of C3-6cycloalkyl and C1-4alkyl,
a is an integer from 0 to 1; b is an integer from 0 to 1; c is an integer from 0 to 1; X is selected from the group consisting of CH and N; provided that when one or both of b or c is 0, then X is CH; such thatis selected from the group consisting of piperazin-1,4-diyl, piperidin-1,4-diyl, pyrroldin-1,3-diyl and azetidin-1,3-diyl,
R3 is selected from the group consisting of C1-4alkyl, halogenated C1-4alkyl, —C(O)-(fluorinated C1-2alkyl), —C(O)-(hydroxy substituted C1-4alkyl), —C(O)—(C1-2alkyl)-C(O)OH, —C(O)—(C1-2alkyl)-C(O)O—(C1-4alkyl), —C(O)—(C1-4alkyl)-C(O)—NRGRH, —C(O)O—(C1-4alkyl), —C(O)O—(C3-6cycloalkyl), —C(O)—NRGRH, —SO2—(C1-4alkyl), —SO2-(halogenated C1-4alkyl), —SO2—(C1-2alkyl)-C(O)OH, —SO2—(C1-2alkyl)-C(O)O—(C1-4alkyl), —SO2—NRGRH, —SO2—(C1-2alkyl)-C(O)—NRGRH, phenyl, pyridyl (provided that the pyridyl is bound through a carbon atom) and -L1-R4; wherein phenyl or pyridyl is optionally substituted with one or more (preferably one to two) substituents independently selected from the group consisting of halogen, C1-4alkyl, halogenated C1-2alkyl, C1-4alkoxy, —(C1-2alkyl)-C(O)OH, —(C1-2alkyl)-C(O)O—(C1-4alkyl), —(C1-2alkyl)-C(O)—NRJRK, —O—(C1-2alkyl)-C(O)OH, —O—(C1-2alkyl)-C(O)O—(C1-4alkyl), —O—(C1-2alkyl)-C(O)—NRJRK, —C(O)OH, —C(O)O—(C1-4alkyl) and —C(O)—NRJRK, wherein RG and RH are each independently selected from the group consisting of hydrogen and C1-4alkyl, and wherein RJ and RK are each independently selected from the group consisting of hydrogen and C1-2alkyl, L1 is selected from the group consisting of —CH2—, CH2CH2—, —CH(CH3)—, —C(O)—, —C(O)—CH2—, —C(O)O—, —C(O)O—CH2—, —C(O)—NH—, —C(O)—NH—CH2— and —SO2—; R4 is selected from the group consisting of C3-6cycloalkyl, phenyl, furanyl, thienyl, pyridyl, pyrazolyl, triazolyl, and tetrazolyl; wherein the phenyl, furanyl, thienyl, pyridyl, pyrazolyl and triazolyl is optionally substituted with one or more substituents independently selected from the group consisting of halogen, hydroxy, C1-4alkyl, halogenated C1-4alkyl, C1-4alkoxy, halogenated C1-4alkoxy, —C(O)OH, —C(O)O—(C1-4alkyl), NRLRM and —SO2—NRLRM, wherein RL and RM are each independently selected from the group consisting of hydrogen and C1-2alkyl, or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof. |
