| 主权项 |
1. A compound having the structure:or a pharmaceutically acceptable salt or solvate thereof, or an enantiomer or diastereomer thereof, and wherein
R2 is selected from the group consisting of hydrogen, deuterium, C1-C6 linear or branched chain alkyl, C3-C6 cycloalkyl, C6-C10 aryl, monocyclic or bicyclic heteroaryl, comprising 5- and/or 6-membered rings, (aryl)C1-C6 linear or branched chain alkyl, (heteroaryl)C1-C6 linear or branched chain alkyl, (heterocyclic)C1-C6 linear or branched chain alkyl, (C1-C6 linear or branched chain alkyl)aryl, (C1-C6 linear or branched chain alkyl)heteroaryl, (C1-C6 linear or branched chain alkyl)heterocyclic, C1-C6 linear or branched chain perfluoroalkyl, C1-C6 linear or branched chain alkoxy, C1-C6 linear or branched chain perfluoroalkoxy, halogen, cyano, hydroxyl, amino, carboxy, aminocarbonyl, (C1-C6 linear or branched chain alkyl)aminocarbonylamino, (C1-C6 linear or branched chain alkyl)aminocarbonyl, —SOR12, —SO2R12, —NR13SO2R12, —SO2NR13R14, and —NR13SO2NR14R15; where said alkyl, aryl and heteroaryl is independently optionally substituted with one or more substituents selected from the group consisting of halo, hydroxy, methoxy, amino, cyano, alkylamino, dialkylamino, CF3, aminocarbonyl, (C1-C6 linear or branched chain alkyl)aminocarbonyl, and C3-C6 cycloalkyl; R3 is selected from the group consisting of hydrogen, deuterium, C1-C6 linear or branched chain alkyl, C1-C6 linear or branched chain perfluoroalkyl, halogen, and cyano; A is —(CRaRb)q—(CRcRd)r—, wherein Ra, Rb, Rc and Rd are independently selected from hydrogen, C1-C6 linear or branched chain alkyl, C1-C6 linear or branched chain perfluoroalkyl, C6-C10 aryl, monocyclic or bicyclic heteroaryl, comprising 5- and/or 6-membered rings, alkylaryl, (aryl)C1-C6 linear or branched chain alkyl, (heteroaryl)C1-C6 linear or branched chain alkyl, halogen, cyano, hydroxyl, C1-C6 linear or branched chain alkoxy, amino, carboxy, aminocarbonyl, (heterocyclic)C1-C6 linear or branched chain alkyl, (C1-C6 linear or branched chain alkyl)aryl, (C1-C6 linear or branched chain alkyl)heteroaryl, and (C1-C6 linear or branched chain alkyl)heterocyclic, where said alkyl is further optionally substituted with one or more substituents selected from the group consisting of halo, hydroxy, methoxy, amino, alkylamino, dialkylamino, CF3, and C3-C6 cycloalkyl; R0, R1, R4, R5, R6, R7, R8, R9 and R10 are independently selected from hydrogen, C1-C6 linear or branched chain alkyl, C1-C6 linear or branched chain perfluoroalkyl, C6-C10 aryl, monocyclic or bicyclic heteroaryl, comprising 5- and/or 6-membered rings, (aryl)C1-C6 linear or branched chain alkyl, (heteroaryl)C1-C6 linear or branched chain alkyl, heteroaryl, halogen, cyano, hydroxyl, C1-C6 linear or branched chain alkoxy, amino, carboxy, aminocarbonyl, (heterocyclic)C1-C6 linear or branched chain alkyl, (C1-C6 linear or branched chain alkyl)aryl, (C1-C6 linear or branched chain alkyl)heteroaryl, and (C1-C6 linear or branched chain alkyl)heterocyclic, where said alkyl is further optionally substituted with one or more substituents selected from the group consisting of halo, hydroxy, methoxy, amino, alkylamino, dialkylamino, CF3, and C3-C6 cycloalkyl; where, alternatively, R0 or R1, and/or R6 or R7, respectively together with either of R4, R5, Ra, Rb, Rc or Rd, may independently form a bond or a C1-C6 linear alkyl chain; and/or, alternatively, R4 or R5, respectively together with either of Ra, Rb, Rc or Rd, may independently form a bond or a C1-C6 linear alkyl chain; and/or, alternatively, R8 and R9 may together form a 3-6-membered ring optionally containing one or two O or N atoms; R11 is hydrogen or deuterium; R12, R13, R14 and R15 are independently selected from hydrogen, C1-C6 linear or branched chain alkyl, C1-C6 linear or branched chain perfluoroalkyl, C6-C10 aryl, alkylaryl, and (aryl)C1-C6 linear or branched chain alkyl; Y is O or N, where when Y is O, n is 0; one and only one of the dotted bonds to Z and Z′ constitutes a single bond, the other being absent, and either Z is C when the dotted bond to Z is a single bond, and Z′ is N or CR16; or, Z is CR16 or N when the dotted bond to Z′ is a single bond, and Z′ is C; where R16 is C1-C4 alkyl, C6-C10 aryl, monocyclic or bicyclic heteroaryl, comprising 5- and/or 6-membered rings, (aryl)C1-C6 linear or branched chain alkyl, (heteroaryl)C1-C6 linear or branched chain alkyl, (heterocyclic)C1-C6 linear or branched chain alkyl, (C1-C6 linear or branched chain alkyl)aryl, (C1-C6 linear or branched chain alkyl)heteroaryl, or (C1-C6 linear or branched chain alkyl)heterocyclic, where said alkyl is further optionally substituted with one or more substituents selected from the group consisting of halo, hydroxy, methoxy, amino, CF3, and C3-C6 cycloalkyl; X and the dotted bonds thereto may be present or absent, whereby, (a) if X is present, Y is N, and X is O or —(CReRf)s—, where Re and Rf are independently hydrogen, deuterium, halo, hydroxy, C1-C4 alkoxy, amino, CF3, C1-C6 linear or branched chain alkyl, C3-C6 cycloalkyl, C6-C10 aryl, monocyclic or bicyclic heteroaryl, comprising 5- and/or 6-membered rings, (aryl)C1-C6 linear or branched chain alkyl, (C1-C6 linear or branched chain alkyl)heteroaryl, (heteroaryl)C1-C6 linear or branched chain alkyl, or (heterocyclic)C1-C6 linear or branched chain alkyl, and said dotted bonds are present and are single bonds, whereby when n is 0, and X is O, said O is bonded to H, and said dotted bond between X and —(CH2)n— is absent, and when X is —(CReRf)s—, and X is bonded directly to Y; and (b) if X is absent, said dotted bonds are absent and n is 0, whereby when Y is N, either (i) said N atom is substituted by H, (ii) Z is C, Z′ is C or N, the dotted bond to Z is a single bond, the dotted bond to Z′ being absent, or (iii) Z is C or N, Z′ is C, the dotted bond to Z′ is a single bond, the dotted bond to Z being absent, where said Y being an N atom may together with R2 and the atoms intervening therebetween form a 6-membered ring optionally substituted by C1-C6 linear or branched chain alkyl or C3-C6 cycloalkyl; and, n, p, q, r and s are independently 0, 1 or 2. |
