| 主权项 |
1. A compound of formula I and pharmaceutically acceptable salts and solvates thereof R1 is CONRa(C1-2)alkyl-, a heteroarylene selected from isoxazoldiyl, pyrazoldiyl, imidazoldiyl, oxazoldiyl, thiazoldiyl, pyridindiyl, pyradizindiyl, and pyrimidindiyl; R2, R3, and R6 are each independently selected from hydrogen, hydroxy, and C1-6allyl; X is selected from —COOR, —PO(R′)OR, —PO(OR)2, —PO(NRR)2, —SO3R, —PO(C1-10alkyl)OR, PO(C3-10cycloalkyl)OR, PO(H)OR, and PO(NHCR′R″COOR)2 R is independently selected from hydrogen, C1-10 alkyl, —C1-5 alkylaryl, —CR′R′—OCO—C1-10 alkyl, and CR′R′—OCO—OC1-10 alkyl; R′ and R″ are independently selected from hydrogen and C1-10 alkyl; L is selected from CONR6—, and NR6CO—; D is selected from hydrogen, aryl and heteroaryl; Ra, R4, and R5 are each independently selected from
hydrogen,halogen,carboxyl C0-10 alkyl,C1-10 alkyl,C2-10 alkenyl,C2-10 alkynyl,C1-10 alkenylamino,C1-10 alkyl(oxy)0-1 carbonylC1-10 alkyl,aryl C0-10 alkyl(oxy)0-1 carbonylC1-10 alkyl,C3-8 cycloalkyl C0-10 alkyl(oxy)0-1carbonyl C1-10 alkyl,(C3-8)heterocyclyl C0-10 alkyl(oxy)0-1carbonyl C1-10 alkyl,(C3-8)heterocycloalkyl C0-10 alkyl(oxy)0-1 carbonyl C1-10 alkyl,arylC0-10 alkyl,C3-8 cycloalkyl C0-10 alkyl,C3-8 heterocyclyl C0-10 alkyl,C3-8 heterocycloalkyl C0-10 alkyl,C1-10 alkoxyl, andhydroxy C0-10alkyl; wherein, R1, Ra, R4, R5, and D are optionally substituted with 1, 2, or 3 substituent R7, selected from:
halogen,(carbonyl)0-1C1-10 alkyl,(carbonyl)0-1C2-10 alkenyl,(carbonyl)0-1C2-10 alkynyl,C1-10 alkylcarbonyl,C2-10 alkenylcarbonyl,C2-10 alkynylcarbonyl,aryl C0-10 alkyl,(C3-8)heterocyclyl C0-10 alkyl,C3-8 cycloalkyl C0-10 alkyl,(C3-8)heterocycloalkyl C0-10 alkyl,C1-4acylamino C0-10 alkyl,C0-10 alkylamino C0-10 alkyl,arylC0-10 alkylamino C0-10 alkyl,C3-8 cycloalkyl C0-10 alkylamino C0-10 alkyl,C3-8 heterocyclyl C0-10 alkylamino C0-10 alkyl,C3-8 heterocycloalkyl C0-10 alkylamino C0-10 alkyl,C1-10alkyloxy C0-10alkyl,(C1-10 alkyl)2aminocarbonyloxy,hydroxy C0-10alkyl,C1-10 alkylsulfonyl,C1-10 alkylsulfonylamino,aryl C1-10 alkylsulfonylamino,C3-8 heterocyclyl C1-10 alkylsulfonylamino,C3-8 heterocycloalkyl C1-10 alkylsulfonylamino,C3-8 cycloalkyl C1-10 alkylsulfonylamino,cyano,nitro,perfluoroC1-6alkyl, andperfluoroC1-6alkoxy; wherein R7 is optionally substituted with 1, 2, or 3 substituents selected from hydrogen, hydroxy, (C1-6)alkoxyl, halogen, CO2H, CN, O(C═O)C1-C6 alkyl, NO2, trifluoromethoxy, trifluoroethoxy, —O(0-1)(C1-10)perfluoroalkyl, and NH2; and provided that when R1 is a heteroarylene, then X is other than —COOR. |
