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    Acetamidine derivatives and their use as inhibitors for the nitric oxide synthase
    7.
    再颁专利
    Acetamidine derivatives and their use as inhibitors for the nitric oxide synthase 有权
    乙酰脒衍生物及其作为一氧化氮合酶抑制剂的用途

    公开(公告)号：USRE37438E1

    公开(公告)日：2001-11-06

    申请号：US09304947

    申请日：1999-05-04

    申请人： Jeffrey Alan Oplinger ,  Edward Patrick Garvey ,  Eric Steven Furfine ,  Barry George Shearer ,  Jon Loren Collins

    发明人： Jeffrey Alan Oplinger ,  Edward Patrick Garvey ,  Eric Steven Furfine ,  Barry George Shearer ,  Jon Loren Collins

    IPC分类号： A61K31155

    CPC分类号： C07D249/08 ,  A61K31/155 ,  A61K31/416 ,  C07C257/14 ,  C07C257/18 ,  C07C311/46 ,  C07C323/41 ,  C07C323/60 ,  C07C335/36 ,  C07C2602/08 ,  C07D213/74 ,  C07D217/04 ,  C07D217/22 ,  C07D231/12 ,  C07D231/56 ,  C07D233/56 ,  C07D277/40 ,  C07D333/20

    摘要： A class of acetamidine derivatives of general formula (I) wherein R1 is hydrogen, C1-6 hydrocarbyl group optionally substituted by halo, halo, nitro, cyano or a group XR3 wherein X is oxygen, C(O)m wherein m is 1 or 2, S(O)n wherein n is 0, 1 or 2, or a group NR4 wherein R4 is hydrogen or C1-6 alkyl; and R3 is hydrogen, C1-6 alkyl, or a group NR5R6 wherein R5 and R6 are independently hydrogen or C1-6 alkyl, provided that R3 is not NR5R6 when X is oxygen or S(O)n; R1a and R1b are independently selected from hydrogen and halo; R2 is a C1-14 hydrocarbyl group which may optionally contain one or two heteroatoms, the group R2 being optionally substituted by one or more groups independently selected from halo; N3; nitro; CF3; ZR7 wherein Z is oxygen, C(O)m′ wherein m′ is 1 or 2, S(O)n′ wherein n′ is 0, 1 or 2, or a group NR8 wherein R8 is hydrogen or C1-6 alkyl and R7 is hydrogen, C1-6 alkyl or a group NR9R10 wherein R9 and R10 are independently hydrogen or C1-6 alkyl; or R2is substituted by a group (a) wherein R11 has a definition the same as for R1; with the proviso that when R1 is a C1-6 alkyl group and R2 is a C1-14 hydrocarbyl substituted by two groups ZR7 wherein one group ZR7 is CO2H, the other group ZR7 is not NH2; and salts thereof, methods for the manufacture thereof, and therapies, particularly inhibtion of nitric oxide synthase, is disclosed.

    摘要翻译： 一类通式（I）的脒基衍生物，其中R 1是氢，任选被卤素，卤素，硝基，氰基取代的C 1-6烃基或XR 3基团，其中X是氧，C（O）m，其中m是1或 2，S（O）n，其中n是0,1或2，或者NR4，其中R4是氢或C1-6烷基; 并且R 3是氢，C 1-6烷基或NR 5 R 6基团，其中R 5和R 6独立地是氢或C 1-6烷基，条件是当X是氧或S（O）n时，R 3不是NR 5 R 6; R1a和R1b独立地选自氢和卤素; R2是可以任选地含有一个或两个杂原子的C1-14烃基，基团R2任选地被一个或多个独立地选自卤素的基团取代; N3; 硝基 CF3; ZR7，其中Z是氧，C（O）m'，其中m'是1或2，S（O）n'，其中n'是0,1或2，或NR8，其中R8是氢或C1-6烷基， R 7是氢，C 1-6烷基或NR 9 R 10基团，其中R 9和R 10独立地是氢或C 1-6烷基; 或其中R a被基团（a）取代，其中R 11具有与R 1相同的定义;条件是当R 1为C 1-6烷基且R 2为被两个ZR 7基团取代的C 1-14烃基时，其中一个基团ZR 7 是CO 2 H，另一组ZR 7不是NH 2;其盐，其制备方法和治疗，特别是一氧化氮合酶的抑制。