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    • 2. 发明申请
    • Novel pharmaceuticals
    • 新药
    • US20050075392A1
    • 2005-04-07
    • US10739425
    • 2003-12-18
    • Kevin DackRobert Maguire
    • Kevin DackRobert Maguire
    • C07D213/30C07D295/185A61K31/215
    • C07D213/30C07D295/185
    • The invention relates to NEP inhibitors for treating cardiovascular disorders. Preferred NEP inhibitors are compounds of formula (I) wherein R1 is C1-C6alkyl, C1-C6alkoxyC1-C3alkyl or C1-C6alkoxyC1-C6alkoxyC1-C3alkyl; R2 is hydrogen or C1-C6alkyl; L is a three atom linkage selected from —CH2—X—CH2— and —CH2—CH2—X— where the right hand side of the linkage is attached to R3 and where X is oxygen, sulfur or methylene; R3 is phenyl or aromatic heterocyclyl, either of which may be independently substituted by one or more groups selected from: C1-C6alkyl, halo, haloC1-C6alkyl, C1-C6alkoxy, haloC1-C6alkoxy, C1-C6alkylthio, haloC1-C6alkylthio and nitrile; and R4 and R5 are either both hydrogen, or one of R4 and R5 is hydrogen and the other is a biolabile ester-forming group that in the body of a patient is replaced by hydrogen.
    • 本发明涉及用于治疗心血管疾病的NEP抑制剂。 优选的NEP抑制剂是式(I)的化合物,其中R 1是C 1 -C 6烷基,C 1 -C 6烷氧基C 1 -C 3烷基或C 1 -C 6烷氧基C 1 -C 6烷氧基C 1 -C 3烷基; R 2是氢或C 1 -C 6烷基; L是选自-CH 2 -X-CH 2 - 和-CH 2 -CH 2 -X-的三原子键,其中键的右手侧连接到R 3,其中X是氧,硫或亚甲基; R 3是苯基或芳族杂环基,其中任一个可以独立地被一个或多个选自以下的基团取代:C 1 -C 6烷基,卤素,卤代C 1 -C 6烷基,C 1 -C 6烷氧基,卤代C 1 -C 6烷氧基,C 1 -C 6烷硫基,卤代C 1 -C 6烷硫基 和腈; R 4和R 5都是氢,R 4和R 5中的一个是氢,另一个是生物不稳定酯形成基团,在患者体内被氢替代 。