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    Phenylglycine derivatives useful for treating disorders of the central nervous system
    4.
    发明授权
    Phenylglycine derivatives useful for treating disorders of the central nervous system 失效
    用于治疗中枢神经系统疾病的苯基甘氨酸衍生物

    公开(公告)号：US5863947A

    公开(公告)日：1999-01-26

    申请号：US853285

    申请日：1997-05-09

    Applicant: Stephen Richard Baker ,  Barry Peter Clark ,  John Goldsworthy ,  John Richard Harris

    Inventor： Stephen Richard Baker ,  Barry Peter Clark ,  John Goldsworthy ,  John Richard Harris

    IPC: C07D295/14 ,  A61K31/195 ,  A61K31/245 ,  A61K31/34 ,  A61K31/341 ,  A61K31/38 ,  A61K31/381 ,  A61K31/40 ,  A61P1/08 ,  A61P25/04 ,  A61P25/18 ,  C07C229/36 ,  C07C229/38 ,  C07C259/10 ,  C07C305/24 ,  C07C309/58 ,  C07C313/02 ,  C07D257/04 ,  C07D295/155 ,  C07D307/54 ,  C07D333/24 ,  C07D521/00 ,  C07F9/09 ,  C07F9/40 ,  C07C321/28

    CPC classification number: C07D295/155 ,  C07C229/36 ,  C07C229/38 ,  C07D307/54 ,  C07D333/24

    Abstract: A pharmaceutical compound of the formula: ##STR1## in which R.sup.1 is hydrogen, hydroxy or C.sub.1-6 alkoxy, R.sup.2 is hydrogen, carboxy, tetrazolyl, --SO.sub.2 H, --SO.sub.3 H, --OSO.sub.3 H, --CONHOH, or --P(OH)OR', --PO(OH)OR', --OP(OH)OR' or --OPO(OH)OR' where R' is hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl or aryl C.sub.1-6 alkyl,R.sup.3 is hydrogen, hydroxy or C.sub.1-4 alkoxy, andR.sup.4 is fluoro, trifluoromethyl, nitro, C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.1-6 alkylthio, heteroaryl, optionally substituted aryl, optionally substituted aryl C.sub.1-6 alkyl, optionally substituted aryl C.sub.2-6 alkenyl, optionally substituted aryl C.sub.2-6 alkynyl, optionally substituted aryloxy, optionally substituted aryl C.sub.1-6 alkoxy, optionally substituted arylthio, optionally substituted aryl C.sub.1-6 alkylthio or --CONR"R'", --SO.sub.2 NR"R"", --NR"R'", --OCONR"R"' or --SONR"R'" where R" and R'" are each hydrogen, C.sub.1-6 alkyl or aryl C.sub.1-6 alkyl, or R" and R'" together form a C.sub.3-7 alkylene ring;provided that (i) R.sup.1, R.sup.2 and R.sup.3 are not all hydrogen,and (ii) when R.sup.2 and R.sup.3 are hydrogen and R.sup.1 is hydroxy, R.sup.4 is not fluoro;or a salt or ester thereof.

    Abstract translation: 下式的药物化合物：其中R 1是氢，羟基或C 1-6烷氧基，R 2是氢，羧基，四唑基，-SO 2 H，-SO 3 H，-OSO 3 H，-CONHOH或-P（ OH）OR'，-PO（OH）OR'，-OP（OH）OR'或-OPO（OH）OR'，其中R'是氢，C 1-6烷基，C 2-6烯基或芳基C 1-6烷基， R3是氢，羟基或C1-4烷氧基，R4是氟，三氟甲基，硝基，C1-6烷基，C3-7环烷基，C2-6烯基，C2-6炔基，C1-6烷硫基，杂芳基，任选取代的芳基 ，任选取代的芳基C 1-6烷基，任选取代的芳基C 2-6烯基，任选取代的芳基C 2-6炔基，任选取代的芳氧基，任选取代的芳基C 1-6烷氧基，任选取代的芳硫基，任选取代的芳基C 1-6烷硫基或 - CONR''R“'，-SO2NR''R”'，-NR''R“'，-OCONR''R”'或-SONR''R“'，其中R”和R“ “各自为氢，C 1-6烷基或芳基C 1-6烷基，或R”和R“”一起形成C 3-7亚烷基环; 条件是（i）R 1，R 2和R 3不全部为氢，和（ii）当R 2和R 3为氢且R 1为羟基时，R 4不为氟; 或其盐或酯。

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