Oral GSNOR inhibitor and pharmaceutical use thereof

    公开(公告)号:US11667616B2

    公开(公告)日:2023-06-06

    申请号:US17628904

    申请日:2021-04-25

    摘要: Disclosed are a thiazolone derivative of N6022 and a pharmaceutical use thereof. The characteristic structure of the thiazolone derivative of N6022 is:




    Compared to N6022, the compound of the present disclosure has good oral bioavailability and a longer half-life period. In in-vitro experiments, administering the compound of the present disclosure can improve migration ability, tube formation ability and, the permeability of human umbilical vein endothelial cells caused by high glucose, and administering the compound of the present disclosure at an animal level can obviously promote the angiogenesis and blood flow recovery of ischemic lateral limbs of diabetic mice. Overall, it suggests that the compound of the present disclosure can be used for treating diseases related to diabetic vascular complications.

    Fungicidal N-[2-(Haloalkoxy)Phenyl]Heteroarylcarboxamides
    9.
    发明申请
    Fungicidal N-[2-(Haloalkoxy)Phenyl]Heteroarylcarboxamides 审中-公开
    杀真菌剂N- [2-(卤代烷氧基)苯基]杂芳基甲酰胺

    公开(公告)号:US20100222217A1

    公开(公告)日:2010-09-02

    申请号:US11989973

    申请日:2006-08-02

    摘要: N-[2-(Haloalkoxy)phenyl]heteroarylcarboxamides of the formula I, where n=0 or 1, Hal=halogen, X=C2-C4-haloalkyl, Het=a pyrazole, thiazole or pyridine radical (a), (b) or (c), where R1=C1-C4-alkyl or C1-C4-haloalkyl, R2=hydrogen or halogen, R3=C1-C4-alkyl or C1-C4-haloalkyl and R5=halogen, C1-C4-alkyl or C1-C4-haloalkyl; except for N-[2-(1,1,2,2-tetrafluoroethoxy)phenyl]-1,3-dimethylpyrazol-4-yl-carboxamide, N-[2-(1,1,2,2-tetrafluoroethoxy)phenyl]-3-trifluoromethyl-1-methylpyrazol-4-yl-carboxamide and N-[2-(2,2,2-trifluorethoxy)phenyl]-3-trifluormethyl-1-methylpyrazol-4-yl-carboxamide. A fungicidal composition comprising at least one compound I, the use of the compounds I for preparing a composition suitable for controlling harmful fungi, a method for controlling harmful fungi using the compounds I and also seed comprising at least one compound I.

    摘要翻译: 式I的N- [2-(卤代烷氧基)苯基]杂芳基甲酰胺,其中n = 0或1,Hal =卤素,X = C 2 -C 4 - 卤代烷基,Het =吡唑,噻唑或吡啶基(a),(b )或(c)中,其中R 1 = C 1 -C 4 - 烷基或C 1 -C 4 - 卤代烷基,R 2 =氢或卤素,R 3 = C 1 -C 4 - 烷基或C 1 -C 4卤代烷基,R 5 =卤素,C 1 -C 4 - 烷基 或C 1 -C 4 - 卤代烷基; 除了N- [2-(1,1,2,2-四氟乙氧基)苯基] -1,3-二甲基吡唑-4-基 - 甲酰胺,N- [2-(1,1,2,2-四氟乙氧基)苯基 ] -3-三氟甲基-1-甲基吡唑-4-基甲酰胺和N- [2-(2,2,2-三氟乙氧基)苯基] -3-三氟甲基-1-甲基吡唑-4-基 - 甲酰胺。 包含至少一种化合物I的杀真菌组合物,使用化合物I制备适于控制有害真菌的组合物,使用化合物I控制有害真菌的方法,还包含至少一种化合物I的种子。