| 主权项 |
1. A compound according to structural formula (I): or a salt, hydrate, solvate or N-oxide thereof, wherein: B is wherein R5 and R6 together form a saturated or unsaturated alkylene or saturated or unsaturated heteroalkylene chain of 3 to 4 atoms, optionally substituted with one or more Ra and/or Rb; R2 is selected from the group consisting of a (C6-C20) aryl optionally substituted with one or more R8, a 5-20 membered heteroaryl optionally substituted with one or more R8, a (C7-C28) arylalkyl optionally substituted with one or more R8 and a 6-28 membered heteroarylalkyl optionally substituted with one or more R8; R4 is a saturated or unsaturated, bridged or unbridged cycloalkyl containing a total of from 3 to 16 annular carbon atoms that is substituted with an R7 group, with the proviso that when R4 is an unsaturated unbridged cycloalkyl, or a saturated bridged cycloalkyl, this R7 substituent is optional, wherein R4 is further optionally substituted with one or more Rf R7 is selected from the group consisting of —C(O)ORd, —C(O)NRdRd, —C(O)NRdORd, or —C(O)NRdNRdRd; each R8 group is, independently of the others, selected from the group consisting of a water-solubilizing group, Ra, Rb, C1-C8 alkyl optionally substituted with one or more Ra and/or Rb, C3-C8 cycloalkyl optionally substituted with one or more Ra and/or Rb, heterocycloalkyl containing 3 to 12 annular atoms, optionally substituted with one or more Ra and/or Rb, C1-C8 alkoxy optionally substituted with one or more Ra and/or Rb, and —O—(CH2)x—Rb, where x is 1-6; each Ra is, independently of the others, selected from the group consisting of hydrogen, C1-C8 alkyl, bridged or unbridged C3-C10 cycloalkyl, bridged or unbridged heterocycloalkyl containing 3 to 12 annular atoms, heteroaryl, (C6-C14) aryl, and (C7-C20) arylalkyl, wherein Ra is optionally substituted with one or more Rf; each Rb is, independently of the others, a suitable group selected from the group consisting of ═O, —ORa, (C1-C3) haloalkyloxy, ═S, —SRa, ═NRa, ═NORa, —NRcRc halogen, —C1-C3haloalkyl, —CN, —NC, —OCN, —SCN, —NO, —NO2, ═N2, —N3, —S(O)Ra, —S(O)2Ra, —S(O)2ORa, —S(O)NRcRc, —S(O)2NRcRc, —OS(O)Ra, —OS(O)2Ra, —OS(O)2ORa, —OS(O)2NRcRc, —C(O)Ra, —C(O)ORa, —C(O)NRcRc, —C(O)NRaORa, —C(NH)NRcRc, —C(NRa)NRcRc, —C(NOH)Ra, —C(NOH)NRcRc, —OC(O)Ra, —OC(O)ORa, —OC(O)NRcRc, —OC(NH)NRcRc and —OC(NRa)NRcRc; each Rc is, independently of the others, is Ra or two Rc that are bonded to the same nitrogen atom taken together with the nitrogen atom to which they are both attached form a heterocycloalkyl group containing 5 to 8 annular atoms, which optionally includes from 1 to 3 additional heteroatomic groups selected from the group consisting of —O—, —S—, —N(—(CH2)y—Ra)—, —N(—(CH2)y—C(O)Ra)—, —N(—(CH2)y—C(O)ORa)—, —N(—(CH2)y—S(O)2Ra)—, —N(—(CH2)y—S(O)2ORa)— and —N(—(CH2)y—C(O)NRaRa)—, where y is 0-6, wherein the heterocycloalkyl is optionally substituted with one or more Rf; each Rd is, independently of the others, selected from the group consisting of Ra, Rc and a chiral auxiliary group; and each Rf is independently —C1-C8 alkoxy, —C1-C8 alkyl, —C1-C6 haloalkyl, cyano, nitro, amino, (C1-C8 alkyl)amino, di(C1-C8 alkyl)amino, phenyl, benzyl, oxo, or halogen, or any two Rf bonded to adjacent atoms, taken together with the atoms to which they are each attached, form a fused saturated or unsaturated cycloalkyl or a fused saturated or unsaturated heterocycloalkyl group containing 5 to 8 annular atoms, wherein the formed cycloalkyl and heterocycloalkyl groups are optionally substituted with one or more groups which are each independently selected from halogen, C1-C8 alkyl, and phenyl. |
