| 主权项 |
1. A compound represented by Formula I: including all stereoisomers, geometric isomers, and tautomers; or a pharmaceutically acceptable salt or solvate of any of the foregoing; wherein: A1 is one of the following:
(i) phenyl or a six-membered heteroaryl, each of which is optionally substituted with 1, 2, or 3 substituents independently selected from the group consisting of halogen, haloalkyl, alkyl, cycloalkyl, heterocycloalkyl, hydroxyl, C1-C6alkoxy, cyano, —CO2R4, —C(O)R5, —S(O)R5, —SO2R5, —SO2N(R6)(R7), —C(O)N(R6)(R7), —N(R6)(R7), and —N(R4)C(O)(R5); or(ii) that is optionally substituted with 1 or 2 substituents independently selected from the group consisting of halogen, haloalkyl, alkyl, cycloalkyl, heterocycloalkyl, hydroxyl, and C1-C6alkoxy; wherein B1 is a 5-membered or 6-membered heterocycle; A2 is wherein B2 is a 6-membered heteroaromatic group; R1 and R2 each represent independently hydrogen or alkyl; R3 is one of the following:
(i) alkyl optionally substituted with 1 or 2 substituents independently selected from the group consisting of hydroxyl, alkoxyl, —O—(C(R4)2)m-alkoxyl, —O—(C(R4)2)m—OH, —N(R6)(R7), cycloalkyl, heterocycloalkyl, —N(R6)C(O)R8, —C(O)N(R6)(R7), —N(R6)C(O)N(R6)(R7), halogen, haloalkyl, and cyano;(ii) cycloalkyl optionally substituted with 1, 2, or 3 substituents independently selected from the group consisting of halogen, haloalkyl, hydroxyl, cycloalkyl, hydroxyalkyl, alkoxy, —O—(C(R4)2)m-alkoxyl, —O—(C(R4)2)m—OH, and cyano; or(iii) heterocycloalkyl optionally substituted with 1, 2, or 3 substituents independently selected from the group consisting of halogen, haloalkyl, hydroxyl, alkyl, cycloalkyl, hydroxyalkyl, alkoxy, —O—(C(R4)2)m-alkoxyl, —O—(C(R4)2)m—OH, and cyano; R4 represents independently for each occurrence hydrogen, alkyl, or cycloalkyl; or two occurrences of R4 attached to the same carbon atom are taken together with said carbon atom to form a saturated carbocylic ring; R5 represents independently for each occurrence alkyl or cycloalkyl; R6 and R7 each represent independently for each occurrence hydrogen, alkyl, or cycloalkyl; or R6 and R7 are taken together with the nitrogen atom to which they are attached to form a 3 to 7 membered heterocyclic ring optionally substituted with 1, 2, or 3 substituents independently selected from the group consisting of halogen, haloalkyl, hydroxyl, alkyl, cycloalkyl, and C1-C6alkoxy; R8 is hydrogen, or R8 is alkyl substituted by hydroxyl, —N(H)(R6), heterocycloalkyl, —N(H)C(O)R10, —C(O)N(H)(R6), or —N(H)C(O)N(R6)(R7); R9 represents independently for each occurrence halogen, haloalkyl, alkyl, cycloalkyl, heterocycloalkyl, hydroxyl, C1-C6alkoxy, or cyano; R10 is alkyl, cycloalkyl, aryl, or aralkyl; and n is 0, 1, 2, 3, or 4; and m is 1, 2, 3, 4, or 5. |
