主权项 |
1. A compound of formula Ib: wherein q is 0 or 1; R1 is selected from the group consisting of hydroxy, alkoxy, substituted alkoxy, acyloxy, cycloalkoxy, substituted cycloalkoxy, aryloxy, substituted aryloxy, mercapto, thioether, amino, substituted amino, and aminoacyl; R2 is selected from the group consisting of hydrogen, deuterium, and methyl; R3 is selected from the group consisting of hydrogen, deuterium, alkyl, and R101; R4 is selected from the group consisting of hydrogen, alkyl, and R101; R5 is selected from the group consisting of hydrogen, halo, alkyl, R101, alkenyl, R111, alkynyl, R113, alkoxy, substituted alkoxy, cycloalkyl, R103, cycloalkoxy, substituted cycloalkoxy, amino, substituted amino, aminoacyl, aryl, R105, aryloxy, substituted aryloxy, furanyl, thienyl, thioether, cyano, and acyl; and R6 and R7 are independently selected from the group consisting of hydrogen, hydroxy, cyano, halo, nitro, acyl, amino, substituted amino, acylamino, sulfonyl, alkyl, R101, alkenyl, R111, alkynyl, R113, alkoxy, substituted alkoxy, aryl, R105, aryloxy, substituted aryloxy, thioether, arylthio, and substituted arylthio; or a pharmaceutically acceptable salt, single stereoisomer, or mixture of stereoisomers thereof, or an ester or amide of the —COOH group on the glycine- or alanine-based substituent of the thienopyridine ring, which ester is selected from —C(O)O-alkyl, —C(O)O—R101, —C(O)O-alkenyl, —C(O)O—R111, —C(O)O-alkynyl, —C(O)O—R113, —C(O)O-aryl, and —C(O)O—R105; and the amide is derived from amines of the formula HNR20R21, where R20 and R21 are independently hydrogen, alkyl, R101, aryl, or R105; and further wherein R101 is substituted alkyl, wherein substituted alkyl is alkyl having from 1 to 5 substituents selected from the group consisting of R200, R201, R202, and R203; R103 is substituted cycloalkyl, wherein substituted cycloalkyl is cycloalkyl having from 3 to 10 carbon atoms having single or multiple cyclic rings and from 1 to 5 substituents selected from the group consisting of oxo (═O), thioxo (═S), alkyl, R101, and R201; R105 is substituted aryl, wherein substituted aryl is aryl having from 1 to 4 substituents selected from the group consisting of R201, alkyl, R101, alkenyl, R111, alkynyl, R113, R202, R203, amidino, aminocarbonyloxy, aminocarbonylamino, aminothiocarbonylamino, cycloalkoxy, substituted cycloalkoxy, thiol, alkylthio, substituted alkylthio, arylthio, substituted arylthio, cycloalkylthio, substituted cycloalkylthio, guanidino, oxycarbonylamino, oxythiocarbonylamino, —S(O)2-alkyl, —S(O)2—R101, —S(O)2-cycloalkyl, —S(O)2—R103, —S(O)2-alkenyl, —S(O)2—R111, —S(O)2-aryl, and —S(O)2—R105; R111 is substituted alkenyl, wherein substituted alkenyl is alkenyl having from 1 to 3 R201; R113 is substituted alkynyl, wherein substituted alkynyl is alkynyl having from 1 to 3 R201; R200 is aminocarbonylamino, aminothiocarbonylamino, aminocarbonyloxy, aryloxyaryl, substituted aryloxyaryl, oxo, thioxo, thiol, alkylthio, substituted alkylthio, arylthio, substituted arylthio, cycloalkylthio, substituted cycloalkylthio, cycloalkoxy, substituted cycloalkoxy, oxycarbonylamino, and oxythiocarbonylamino; R201 is alkoxy, substituted alkoxy, acyl, acylamino, acyloxy, amino, substituted amino, aminoacyl, aryloxy, substituted aryloxy, cyano, halogen, hydroxyl, nitro, carboxyl, carboxyl esters, cycloalkyl, R103, aryl, and R105; R202 is —NR40S(O)2-alkyl, —NR40S(O)2—R101, —NR40S(O)2-aryl, —NR40S(O)2—R105, —NR40S(O)2—NR40-alkyl, —NR40S(O)2—NR40—R101, —NR40S(O)2—NR40-aryl, and —NR40S(O)2—NR40—R105, where each R40 is hydrogen or alkyl; and R203 is —OS(O)2-alkyl, —OS(O)2—R101, —OS(O)2-aryl, —OS(O)2—R105, and —OSO2—NR40R40 where each R40 is hydrogen or alkyl; and further wherein substituted alkoxy is —O—R101; substituted cycloalkoxy is —O—R103; substituted aryloxy is —O—R105; substituted amino is —NR41R41, where each R41 group is independently selected from the group consisting of hydrogen, alkyl, R101, alkenyl, R111, alkynyl, R113, cycloalkyl, R103, aryl, R105, —S(O)2-alkyl, —S(O)2—R101, —S(O)2-cycloalkyl, —S(O)2—R103, —S(O)2-alkenyl, —S(O)2—R111, —S(O)2-aryl, and —S(O)2—R105, provided that both R41 groups are not hydrogen; substituted alkylthio is —S—R101; substituted arylthio is —S—R105; substituted cycloalkylthio is —S—R103; substituted aryloxyaryl is -aryl-O-aryl, wherein each aryl group is substituted on either or both aryl rings with from 1 to 3 substituents selected from the group consisting of R201, alkyl, R101, alkenyl, R111, alkynyl, R113, R202, R203, amidino, aminocarbonyloxy, aminocarbonylamino, aminothiocarbonylamino, cycloalkoxy, substituted cycloalkoxy, thiol, alkylthio, substituted alkylthio, arylthio, substituted arylthio, cycloalkylthio, substituted cycloalkylthio, guanidino, oxycarbonylamino, oxythiocarbonylamino, —S(O)2-alkyl, —S(O)2—R101, —S(O)2-cycloalkyl, —S(O)2—R103, —S(O)2-alkenyl, —S(O)2—R111, —S(O)2-aryl, and —S(O)2—R105; and acyl is H—C(O)—, alkyl-C(O)—, R101—C(O)—, alkenyl-C(O)—, R111-—C(O)—, alkynyl-C(O)—, R113—C(O)—, cycloalkyl-C(O)—, R103—C(O)—, aryl-C(O)—, or R105—C(O)—. |