| 主权项 |
1. A compound of formula (I): or a pharmaceutically acceptable salt, ester, amide, or radiolabelled form thereof, wherein: n is 1 or 2; R1 is phenyl or monocyclic heteroaryl, wherein the monocyclic heteroaryl contains one or two ring nitrogens and optionally one ring oxygen or one ring sulfur, wherein the phenyl or monocyclic heteroaryl isoptionally substituted with 1, 2, or 3 substituents selected from the group consisting of C1-C6-alkyl; C1-C6-alkylcarbonylamino; hydroxyC1-C6-alkylcarbonylamino; C1-C6-alkoxyC1-C6alkylcarbonylamino; C1-C6-alkoxy; C1-C6-alkoxyC1-C6-alkoxy; C1-C6-alkoxyC1-C6-alkyl; C1-C6-alkoxycarbonyl; C1-C6-alkoxycarbonylC1-C6-alkyl; aminocarbonyl; C1-C6-alkylaminocarbonyl; hydroxyC1-C6-alkylaminocarbonyl; C1-C6-alkoxyC1-C6-alkylaminocarbonyl; cyano; carboxy; hydroxy; hydroxyC1-C6-alkoxy; hydroxyC1-C6-alkyl; di(hydroxy)C1-C6-alkyl; di(C1-C6alkyl)amino; di(hydroxyC1-C6-alkyl)amino; di(C1-C6-alkoxyC1-C6alkyl)amino; (C1-C6-alkoxyC1-C6-alkyl)(hydroxyC1-C6-alkyl)amino; haloC1-C6-alkyl; and halogen; wherein only 1 substituent can be present on the two atoms adjacent to the atom connected to the amide nitrogen pendant on the furan ring; or R1 is fused-bicyclic heteroaryl, wherein the fused-bicyclic heteroaryl contains 1, 2, 3 or 4 ring nitrogens and optionally one ring oxygen or one ring sulfur, wherein the fused-bicyclic heteroaryl isoptionally substituted with 1, 2, 3, or 4 substituents selected from the group consisting of C1-C6-alkyl; C1-C6-alkylcarbonylamino; hydroxyC1-C6-alkylcarbonylamino; C1-C6-alkoxyC1-C6-alkylcarbonylamino; C1-C6-alkoxy; C1-C6-alkoxyC1-C6-alkoxy; C1-C6alkoxy-C1-C6alkyl; C1-C6-alkoxycarbonyl; C1-C6-alkoxycarbonylC1-C6-alkyl; C3-C7-cycloalkyloxy; M4-M7-heterocycleoxy, wherein the heterocycle of M4-M7-heterocycleoxy isoptionally substituted with C1-C6-alkyl; aminocarbonyl; C1-C6-alkylaminocarbonyl; hydroxyC1-C6-alkylaminocarbonyl; C1-C6-alkoxyC1-C6-alkylamincarbonyl; cyano; hydroxy; hydroxyC1-C6-alkoxy; hydroxyC1-C6-alkyl; di(C1-C6alkyl)amino; di(hydroxyC1-C6-alkyl)amino; di(C1-C6-alkoxyC1-C6-alkyl)amino; (C1-C6-alkoxyC1-C6-alkyl)(hydroxyC1-C6-alkyl)amino; haloC1-C6-alkyl; halogen; C1-C6-alkylsulfonylaminoC2-C6-alkyl; and (i),wherein Ra is selected from the group consisting of a bond, CH2, CHRb, O, S, and N—Rc; wherein only 1 substituent can be present on the two atoms adjacent to the atom connected to the amide nitrogen pendant on the furan ring;
m is 2, 3 or 4 when (i) is attached to a ring nitrogen atom of the bicyclic heteroaryl; or m is 0, 1, 2, 3 or 4 when (i) is attached to a ring carbon atom of the bicyclic heteroaryl; Rb, at each occurrence, is independently selected from the group consisting of hydrogen, C1-C6-alkyl, haloC1-C6-alkyl, C1-C6-alkoxyC1-C6-alkyl, and hydroxyC1-C6-alkyl; Rc is selected from the group consisting of hydrogen, C1-C6-alkyl, C1-C6-alkoxycarbonyl, C1-C6-alkycarbonyl, C1-C6-alkysulfonyl, di(C1-C6-alkyl)aminosulfonyl, heterocyclecarbonyl, C3-C7-cycloalkylcarbonyl, —C(O)NH2, —C(O)NH(alkyl), —C(O)N(alkyl)2 and —C(═NCN)NHCH3; or R1 is (ii), (iii), or (iv);wherein both X1 and X2 are CH, or one of X1 and X2 is N and the other is CH;
X3 is CH or N; L1 is a bond, C(O), or —NHC(O)—; Rd is selected form the group consisting of hydrogen; C1-C6alkoxy; fluoroC1-C6-alkoxy; C1-C6-alkoxyC1-C6-alkoxy; C3-C7-cycloalkyloxy; C3-C7-cycloalkylC1-C6-alkoxy; hydroxyC1-C6-alkoxy; phenylC1-C6-alkoxyC1-C6-alkoxy; M4-M7-heterocycleoxy, wherein the heterocycle of heterocycleoxy isoptionally substituted with C1-C6-alkyl or oxo; and phenoxy, wherein the phenyl of phenoxy isoptionally substituted with hydroxyC1-C6-alkyl, C1-C6-alkoxy, C1-C6-alkoxyC1-C6-alkoxy, or C1-C6-alkoxycarbonyl; Re at each occurrence is independently selected from the group consisting of hydrogen, C1-C6-alkyl, di(C1-C6-alkyl)amino, haloC1-C6-alkyl, C1-C6-alkoxyC1-C6alkyl, and hydroxyC1-C6-alkyl; Rf is selected from the group consisting of a bond, CH2, CHRe, CH2CH2, O, NRg, and CH2NRg; Rg is selected from the group consisting of hydrogen; C1-C6-alkyl; C1-C6-alkoxycarbonyl; C1-C6-alkycarbonyl; C1-C6-alkysulfonyl; di(C1-C6-alkyl)aminosulfonyl; C3-C7-cycloalkylcarbonyl; C1-C6-alkoxyC1-C6-alkylcarbony; hydroxyC2-C6-alkyl; hydroxyC1-C6-alkylcarbonyl; formyl; —C(O)NH2; —C(O)NH(alkyl); —C(O)N(alkyl)2; —C(═NCN)NHCH3; and M4-M7-heterocyclecarbonyl, wherein the heterocycle of heterocyclecarbonyl isoptionally substituted with C1-C6-alkyl; Z1 is NR2 or CR3R4; R2 is selected from the group consisting of hydrogen, C1-C6-alkyl, hydroxyC2-C6-alkyl, di(hydroxy)C2-C6-alkyl, C1-C6-alkoxyC2-C6alkyl, hydroxyC2-C6-alkoxyC2-C6-alkyl, C1-C6-alkylcarbonyloxyC2-C6-alkyl, C1-C6-alkoxycarbonylC1-C6-alkyl, C1-C6-alkylcarbonylC1-C6-alkyl and phenylC1-C6-alkoxyC2-C6alkyl; R3 and R4 are each independently selected from the group consisting of hydrogen, C1-C6-alkyl, hydroxyC1-C6-alkyl, aminoC1-C6-alkyl, and phenyl, wherein phenyl is optionally substituted with 1, 2, 3 or 4 substituents selected from halogen, C1-C6-alkyl, and cyano; or R3 and R4 taken together with the carbon atom to which they are attached form a M4-M7-heterocycle optionally substituted with 1, 2 or 3 halogen, C1-C6-alkyl, cyano or oxo; Z2 is O, NR5, or CR6R7; R5 is selected from the group consisting of hydrogen, C1-C6-alkyl, C1-C6-alkylsulfonyl, C1-C6-alkylcarbonyl, and C1-C6-alkoxycarbonyl; and R6 and R7 are each independently selected from the group consisting of hydrogen, C1-C6-alkyl, C1-C6-alkoxyC1-C6-alkyl, hydroxyC1-C6-alkyl, aminoC1-C6-alkyl, aminocarbonyl, and C1-C6-alkoxycarbonyl; wherein one or more of R3, R4, R6 and R7 is other than hydrogen; or R6 and R7 taken together with the carbon atom to which they are attached form a C3-C6-cycloalkyl or M4-M7-heterocycle, wherein the C3-C6-cycloalkyl or M4-M7-heterocycle are optionally substituted with 1, 2, or 3 substituents selected from C1-C6-alkyl, cyano, aminocarbonyl, halogen, oxo and C1-C6-alkylcarbonyl. |
