| 主权项 |
1. A compound of formula (I): or a pharmaceutically acceptable salt thereof, wherein: X1 is selected from the group consisting of CH2, C(═O), C(═NH), and NHC(═O); R1 is selected from the group consisting of optionally substituted arylalkyl, wherein the aryl substituents are cyano, halogen, hydroxyl, nitro, trifluoromethyl, alkyl, alkylthio, alkoxy, amino, alkylamino, dialkylamino, alkanoyl, amido, N-alkylamido, N,N-dialkylamino, sulfonamido, aryl, or heteroaryl, and optionally substituted heteroarylalkyl, wherein the heteroaryl substituents are alkyl, cycloalkyl, —O—C(halogen)3, biaryl, carbocyclic aryl, heteroalicyclic, heteroaryl, acyl, amidino, amido, amino, alkyoxyamino, carbamoyl, carboxy, cyano, ether, hydroxyl, imino, halo, nitro, sulphamoyl, sulfonyl, sulphinyl, sulphenyl, sulfonamido or urea, or when positioned adjacent to each other, may combine to form cycloalkyl or heteroalicyclic ring systems; R2 is selected from the group consisting of optionally substituted alkyl, wherein the alkyl substituents are cyano, halogen, hydroxyl, alkylamino, dialkylamino, amido, alkylamido, dialkylamido, alkanoyl, alkoxy, sulfonamido, nitro, aryl, or heteroaryl, optionally substituted aryl, wherein the aryl substituents are cyano, halogen, hydroxyl, nitro, trifluoromethyl, alkyl, alkylthio, alkoxy, amino, alkylamino, dialkylamino, alkanoyl, amido, N-alkylamido, N,N-dialkylamino, sulfonamido, aryl, or heteroaryl, optionally substituted heteroaryl, wherein the heteroaryl substituents are alkyl, cycloalkyl, —O—C(halogen)3, biaryl, carbocyclic aryl, heteroalicyclic, heteroaryl, acyl, amidino, amido, amino, alkyoxyamino, carbamoyl, carboxy, cyano, ether, hydroxyl, imino, halo, nitro, sulphamoyl, sulfonyl, sulphinyl, sulphenyl, sulfonamido or urea, or when positioned adjacent to each other, may combine to form cycloalkyl or heteroalicyclic ring systems, and NR24R25; R3 is selected from the group consisting of hydrogen, halogen, hydroxy, alkoxy, aryloxy, optionally substituted alkyl, wherein the alkyl substituents are cyano, halogen, hydroxyl, alkylamino, dialkylamino, amido, alkylamido, dialkylamido, alkanoyl, alkoxy, sulfonamido, nitro, aryl, or heteroaryl, amino, amino sulfonyl, and cyano; R4 and R5 together with the N to which they are attached form a saturated or partially saturated 4-7 membered ring with the general formula (II): wherein: X2 is C(═O), CH2 or CH(R6) or C(R6)(R6); wherein each R6 independently is amino, amino carbonyl, hydroxy, acyl, optionally substituted alkoxy, wherein the alkyl substituents are cyano, halogen, hydroxyl, alkylamino, dialkylamino, amido, alkylamido, dialkylamido, alkanoyl, alkoxy, sulfonamido, nitro, aryl, or heteroaryl, optionally substituted aryloxy, wherein the aryl substituents are cyano, halogen, hydroxyl, nitro, trifluoromethyl, alkyl, alkylthio, alkoxy, amino, alkylamino, dialkylamino, alkanoyl, amido, N-alkylamido, N,N-dialkylamino, sulfonamido, aryl, or heteroaryl, optionally substituted alkyl, wherein the alkyl substituents are cyano, halogen, hydroxyl, alkylamino, dialkylamino, amido, alkylamido, dialkylamido, alkanoyl, alkoxy, sulfonamido, nitro, aryl, or heteroaryl, optionally substituted cycloalkyl, wherein the cycloalkyl substituents are alkyl, cycloalkyl, —O—C(halogen)3, biaryl, carbocyclic aryl, heteroalicyclic, heteroaryl, acyl, amidino, amido, amino, alkyoxyamino, carbamoyl, carboxy, cyano, ether, hydroxyl, imino, halo, nitro, sulphamoyl, sulfonyl, sulphinyl, sulphenyl, sulfonamido or urea, or one or more ring carbons may be bonded via a double bond to a group selected from NH, S and O, optionally substituted arylalkyl, wherein the aryl substituents are cyano, halogen, hydroxyl, nitro, trifluoromethyl, alkyl, alkylthio, alkoxy, amino, alkylamino, dialkylamino, alkanoyl, amido, N-alkylamido, N,N-dialkylamino, sulfonamido, aryl, or heteroaryl, optionally substituted aryl wherein the aryl substituents are cyano, halogen, hydroxyl, nitro, trifluoromethyl, alkyl, alkylthio, alkoxy, amino, alkylamino, dialkylamino, alkanoyl, amido, N-alkylamido, sulfonamido, aryl, or heteroaryl, or optionally substituted heteroaryl, wherein the heteroaryl substituents are alkyl, cycloalkyl, —O—C(halogen)3, biaryl, carbocyclic aryl, heteroalicyclic, heteroaryl, acyl, amidino, amido, amino, alkyoxyamino, carbamoyl, carboxy, cyano, ether, hydroxyl, imino, halo, nitro, sulphamoyl, sulfonyl, sulphinyl, sulphenyl, sulfonamido or urea, or when positioned adjacent to each other, may combine to form cycloalkyl or heteroalicyclic ring systems; X3 is CH2, CH(R7), C(R7)(R7), NH, N(R8), O or S; wherein each R7 independently is amino, amino carbonyl, hydroxy, acyl, optionally substituted alkoxy, wherein the alkyl substituents are cyano, halogen, hydroxyl, alkylamino, dialkylamino, amido, alkylamido, dialkylamido, alkanoyl, alkoxy, sulfonamido, nitro, aryl, or heteroaryl, optionally substituted aryloxy, wherein the aryl substituents are cyano, halogen, hydroxyl, nitro, trifluoromethyl, alkyl, alkylthio, alkoxy, amino, alkylamino, dialkylamino, alkanoyl, amido, N-alkylamido, N,N-dialkylamino, sulfonamido, aryl, or heteroaryl, optionally substituted alkyl, wherein the alkyl substituents are cyano, halogen, hydroxyl, alkylamino, dialkylamino, amido, alkylamido, dialkylamido, alkanoyl, alkoxy, sulfonamido, nitro, aryl, or heteroaryl, optionally substituted cycloalkyl, wherein the cycloalkyl substituents are alkyl, cycloalkyl, —O—C(halogen)3, biaryl, carbocyclic aryl, heteroalicyclic, heteroaryl, acyl, amidino, amido, amino, alkyoxyamino, carbamoyl, carboxy, cyano, ether, hydroxyl, imino, halo, nitro, sulphamoyl, sulfonyl, sulphinyl, sulphenyl, sulfonamido or urea, or one or more ring carbons may be bonded via a double bond to a group selected from NH, S and O, optionally substituted arylalkyl, wherein the aryl substituents are cyano, halogen, hydroxyl, nitro, trifluoromethyl, alkyl, alkylthio, alkoxy, amino, alkylamino, dialkylamino, alkanoyl, amido, N-alkylamido, N,N-dialkylamino, sulfonamido, aryl, or heteroaryl, optionally substituted aryl wherein the aryl substituents are cyano, halogen, hydroxyl, nitro, trifluoromethyl, alkyl, alkylthio, alkoxy, amino, alkylamino, dialkylamino, alkanoyl, amido, N-alkylamido, NN-dialkylamino, sulfonamido, aryl, or heteroaryl, or optionally substituted heteroaryl, wherein the heteroaryl substituents are alkyl, cycloalkyl, —O—C(halogen)3, biaryl, carbocyclic aryl, heteroalicyclic, heteroaryl, acyl, amidino, amido, amino, alkyoxyamino, carbamoyl, carboxy, cyano, ether, hydroxyl, imino, halo, nitro, sulphamoyl, sulfonyl, sulphinyl, sulphenyl, sulfonamido or urea, or when positioned adjacent to each other, may combine to form cycloalkyl or heteroalicyclic ring systems; R8 is acyl, optionally substituted alkyl, wherein the alkyl substituents are cyano, halogen, hydroxyl, alkylamino, dialkylamino, amido, alkylamido, dialkylamido, alkanoyl, alkoxy, sulfonamido, nitro, aryl, or heteroaryl, optionally substituted cycloalkyl, wherein the cycloalkyl substituents are alkyl, cycloalkyl, —O—C(halogen)3, biaryl, carbocyclic aryl, heteroalicyclic, heteroaryl, acyl, amidino, amido, amino, alkyoxyamino, carbamoyl, carboxy, cyano, ether, hydroxyl, imino, halo, nitro, sulphamoyl, sulfonyl, sulphinyl, sulphenyl, sulfonamido or urea, or one or more ring carbons may be bonded via a double bond to a group selected from NH, S and O, optionally substituted arylalkyl, wherein the aryl substituents are cyano, halogen, hydroxyl, nitro, trifluoromethyl, alkyl, alkylthio, alkoxy, amino, alkylamino, dialkylamino, alkanoyl, amido, N-alkylamido, N,N-dialkylamino, sulfonamido, aryl, or heteroaryl, optionally substituted aryl, wherein aryl the substituents are cyano, halogen, hydroxyl, nitro, trifluoromethyl, alkyl, alkylthio, alkoxy, amino, alkylamino, dialkylamino, alkanoyl, amido, N-alkylamido, N,N-dialkylamino, sulfonamido, aryl, or heteroaryl, or optionally substituted heteroaryl, wherein aryl the substituents are cyano, halogen, hydroxyl, nitro, trifluoromethyl, alkyl, alkylthio, alkoxy, amino, alkylamino, dialkylamino, alkanoyl, amido, N-alkylamido, NN-dialkylamino, sulfonamido, aryl, or heteroaryl; R24 and R25 are the same or different and each is hydrogen, optionally substituted alkyl, wherein the alkyl substituents are cyano, halogen, hydroxyl, alkylamino, dialkylamino, amido, alkylamido, dialkylamido, alkanoyl, alkoxy, sulfonamido, nitro, aryl, or heteroaryl, optionally substituted cycloalkyl, wherein the cycloalkyl substituents are alkyl, cycloalkyl, —O—C(halogen)3, biaryl, carbocyclic aryl, heteroalicyclic, heteroaryl, acyl, amidino, amido, amino, alkyoxyamino, carbamoyl, carboxy, cyano, ether, hydroxyl, imino, halo, nitro, sulphamoyl, sulfonyl, sulphinyl, sulphenyl, sulfonamido or urea, or one or more ring carbons may be bonded via a double bond to a group selected from NH, S and O, optionally substituted arylalkyl, wherein the cycloalkyl substituents are alkyl, cycloalkyl, —O—C(halogen)3, biaryl, carbocyclic aryl, heteroalicyclic, heteroaryl, acyl, amidino, amido, amino, alkyoxyamino, carbamoyl, carboxy, cyano, ether, hydroxyl, imino, halo, nitro, sulphamoyl, sulfonyl, sulphinyl, sulphenyl, sulfonamido or urea, or one or more ring carbons may be bonded via a double bond to a group selected from NH, S and O, optionally substituted aryl, wherein the aryl substituents are cyano, halogen, hydroxyl, nitro, trifluoromethyl, alkyl, alkylthio, alkoxy, amino, alkylamino, dialkylamino, alkanoyl, amido, N-alkylamido, N,N-dialkylamino, sulfonamido, aryl, or heteroaryl, or optionally substituted heteroaryl, wherein the heteroaryl substituents are alkyl, cycloalkyl, —O—C(halogen)3, biaryl, carbocyclic aryl, heteroalicyclic, heteroaryl, acyl, amidino, amido, amino, alkyoxyamino, carbamoyl, carboxy, cyano, ether, hydroxyl, imino, halo, nitro, sulphamoyl, sulfonyl, sulphinyl, sulphenyl, sulfonamido or urea, or when positioned adjacent to each other, may combine to form cycloalkyl or heteroalicyclic ring systems; n=1 or 2; and m=1, 2 or 3. |
