主权项 |
1. A compound of formula (I) wherein R1 is selected from the group consisting of hydrogen and hydroxy;is selected from the group consisting of phenyl, furyl, thienyl, thiazolyl, benzothiazolyl and benzo[d][1,3]dioxolyl;
wherein the phenyl, furyl, thienyl, 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 and NRARB; wherein RA and RB are each independently selected from the group consisting of hydrogen and C1-4alkyl; provided that each substituent is bound to a carbon atom of the ring;is selected from the group consisting of phenyl, furyl, thienyl, thiazolyl, benzothiazolyl and benzo[d][1,3]dioxolyl;
wherein the phenyl, furyl, thienyl, 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 and NRCRD; wherein RC and RD are each independently selected from the group consisting of hydrogen and C1-4alkyl; provided that each substituent is bound to a carbon atom of the ring; a is an integer from 0 to 1; L1 is selected from the group consisting of —N(R2)—, —N(R2)—CH2— and —N(R2)—CH2CH2—; wherein R2 is selected from the group consisting of hydrogen and C1-2alkyl; and wherein the L1 is bound to the cinnoline core through a nitrogen atom;is selected from the group consisting of(wherein X is selected from the group consisting of C and N);
provided that whenis selected from the group consisting ofthen a is 0 or a is 1 and L1 is other than —N(R2) and —N(R2)—CH2—;
wherein R3 is selected from the group consisting of hydrogen, halogen, hydroxy, cyano, C1-4alkyl, halogenated C1-4alkyl, hydroxy substituted C1-4alkyl, C1-4alkoxy, halogenated C1-4alkoxy, —CO2H, —C(O)O—(C1-4alkyl), —(C1-4alkyl)-CO2H, —(C1-4alkyl)-C(O)O—(C1-4alkyl), —SO2—(C1-4alkyl) and —SO2-(halogenated C1-4alkyl); c is an integer from 0 to 2; each R4 is independently selected from the group consisting of halogen, C1-4alkyl, halogenated C1-2alkyl, C1-4alkoxy and halogenated C1-2alkoxy; wherein R5 is selected from the group consisting of —C(O)—(C1-4alkyl), —C(O)O—(C1-4alkyl), —SO2—(C1-4alkyl) and —SO2-(halogenated C1-4alkyl); and wherein R6 is selected from the group consisting of C1-4alkyl, halogenated C1-4alkyl, —C(O)—NRE1RF, —NRE—C(O)—(C1-4alkyl), —NRE—SO2—(C1-4alkyl), andwherein RE and RF are each independently selected from the group consisting of hydrogen, methyl and ethyl;
b is an integer from 0 to 1; L2 is selected from the group consisting of —CH2—, —CH2CH2—, —NH—, —N(CH3)—, —C(O)— and —SO2—; provided that whenis selected from the group consisting ofthen b is 0 or b is 1 and L2 is other than —NH— or —N(CH3)—;is selected from the group consisting of phenyl, furan-2-yl, thien-2-yl;
wherein the phenyl is optionally substituted with a substituent selected from the group consisting of halogen, hydroxy, cyano, C1-4alkyl, halogenated C1-4alkyl, hydroxy substituted C1-4alkyl, C1-4alkoxy, halogenated C1-4alkoxy, —CO2H, —C(O)O—(C1-4alkyl), —(C1-4alkyl)-CO2H, —(C1-4alkyl)-C(O)O—(C1-4alkyl), —SO2—(C1-4alkyl) and —SO2-(halogenated C1-4alkyl); and wherein the phenyl is further optionally substituted with one to two additional substituents independently selected from the group consisting of halogen, C1-4alkyl, halogenated C1-2alkyl, C1-4alkoxy and halogenated C1-2alkoxy; and wherein the furan-2-yl or thien-2-yl is optionally substituted with a substituent selected from the group consisting of halogen, C1-4alkyl, halogenated C1-4alkyl, C1-4alkoxy, halogenated C1-4alkoxy, —CO2H, —C(O)O—(C1-4alkyl) and —C(O)—NRGRH; wherein RG and RH are each independently selected from the group consisting of hydrogen, methyl and ethyl; or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof. |