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    Substituted kynurenines and process for their preparation
    1.
    发明授权
    Substituted kynurenines and process for their preparation 失效
    替代的犬尿苷及其制备方法

    公开(公告)号：US5786508A

    公开(公告)日：1998-07-28

    申请号：US411656

    申请日：1995-04-06

    申请人： Robert Schwarcz ,  Mario Varasi ,  Arturo Della Torre ,  Carmela Speciale ,  Alberto Bianchetti

    发明人： Robert Schwarcz ,  Mario Varasi ,  Arturo Della Torre ,  Carmela Speciale ,  Alberto Bianchetti

    IPC分类号： C07C229/36 ,  A61K31/195 ,  C07C239/36

    CPC分类号： C07C229/36 ,  C07C2101/14

    摘要： The present invention relates to the use in the treatment of cognitive disorders associated with the aging processes of the brain and perinatal brain disorders of compounds which act as inhibitors of the enzyme kynurenine aminotransferase (KAT). The present invention also provides, as novel compounds, a selected class of KAT inhibitors which are the compounds of formula (IA) ##STR1## wherein R is halogen, C.sub.1 -C.sub.6 alkyl, C.sub.5 -C.sub.7 cycloalkyl, phenyl-C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.6 -C.sub.10 aryloxy, phenyl-C.sub.1 -C.sub.4 alkoxy or trifluoromethyl, and R.sub.1 is hydroxy, C.sub.1 -C.sub.6 alkoxy, amino, mono-C.sub.1 -C.sub.6 alkylamino, di-C.sub.1 -C.sub.6 alkylamino, hydroxylamino, C.sub.1 -C.sub.4 alkoxyamino or benzyloxyamino, with the provisos that: (i) when R.sub.1 is hydroxy and, at the same time, R is halogen, then this halogen is not fluorine; and (ii) when R.sub.1 is hydroxy and, at the same time, R is C.sub.1 -C.sub.6 alkyl, then this C.sub.1 -C.sub.6 alkyl is not methyl, either as a single isomer or as a mixture of isomers, and the pharmaceutically acceptable salts thereof.

    摘要翻译： PCT No.PCT / US94 / 07804 Sec。 371日期：1995年4月6日 102（e）日期1995年4月6日PCT 1994年7月15日PCT公布。 公开号WO95 / 04714 日期1995年2月16日本发明涉及用作治疗与作为犬尿氨酸转氨酶（KAT）酶抑制剂的化合物的脑老化过程和围产期脑疾病相关的认知障碍的用途。 本发明还提供作为新化合物的选择类别的作为式（IA）化合物的KAT抑制剂，其中R是卤素，C 1 -C 6烷基，C 5 -C 7环烷基，苯基-C 1 -C 4烷基， C 1 -C 6烷氧基，C 6 -C 10芳氧基，苯基-C 1 -C 4烷氧基或三氟甲基，R 1是羟基，C 1 -C 6烷氧基，氨基，单-C 1 -C 6烷基氨基，二-C 1 -C 6烷基氨基，羟基氨基，C 1 -C 4 烷氧基氨基或苄氧基氨基，条件是：（ⅰ）当R 1为羟基，同时R为卤素时，该卤素不为氟; 和（ii）当R 1是羟基，并且同时R是C 1 -C 6烷基时，则该C 1 -C 6烷基不是甲基，作为单一异构体或作为异构体的混合物，以及其药学上可接受的盐 。

    Substituted kynurenines and process for their preparation
    3.
    发明授权
    Substituted kynurenines and process for their preparation 失效
    替代的犬尿苷及其制备方法

    公开(公告)号：US5519055A

    公开(公告)日：1996-05-21

    申请号：US102843

    申请日：1993-08-06

    申请人： Robert Schwarcz ,  Mario Varasi ,  Arturo Della Torre ,  Carmela Speciale ,  Alberto Bianchetti

    发明人： Robert Schwarcz ,  Mario Varasi ,  Arturo Della Torre ,  Carmela Speciale ,  Alberto Bianchetti

    IPC分类号： A61K31/00 ,  A61K31/165 ,  A61K31/195 ,  A61K31/198 ,  A61K31/215 ,  A61K31/216 ,  C07C229/36 ,  C07C233/43 ,  C07C233/44 ,  C07C235/10 ,  A61K31/24 ,  C07C229/00

    CPC分类号： C07C229/36 ,  A61K31/00 ,  A61K31/165 ,  A61K31/195 ,  A61K31/198 ,  A61K31/215 ,  A61K31/216 ,  C07C2101/08

    摘要： The present invention relates to the use in the treatment of cognitive disorders associated with the aging processes of the brain and perinatal brain disorders of compounds which act as inhibitors of the enzyme kynurenine aminotransferase (KAT).The present invention also provides, as novel compounds, a selected class of KAT inhibitors which are the compounds of formula (IA) ##STR1## wherein R is halogen, C.sub.1 -C.sub.6 alkyl, C.sub.5 -C.sub.7 cycloalkyl, phenyl-C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.6 -C.sub.10 aryloxy, phenyl-C.sub.1 -C.sub.4 alkoxy or trifluoromethyl, andR.sub.1 is hydroxy, C.sub.1 -C.sub.6 alkoxy, amino, mono-C.sub.1 -C.sub.6 alkylamino, di-C.sub.1 -C.sub.6 alkylamino, hydroxylamino, C.sub.1 -C.sub.4 alkoxyamino or benzyloxyamino; with the provisos that(i) when R.sub.1 is hydroxy and, at the same time, R is halogen, then this halogen is not fluorine; and(ii) when R.sub.1 is hydroxy and, at the same time, R is C.sub.1 -C.sub.6 alkyl, then this C.sub.1 -C.sub.6 alkyl is not methyl, and the pharmaceutically acceptable salts thereof.

    摘要翻译： 本发明涉及用于治疗与脑衰老过程相关的认知障碍和围产期脑疾病的化合物的用途，所述化合物作为犬尿氨酸转氨酶（KAT）酶的抑制剂。 本发明还提供作为新化合物的选定类别的KAT抑制剂，其是式（IA）化合物其中R是卤素，C 1 -C 6烷基，C 5 -C 7环烷基，苯基-C 1 -C 6烷基， C4烷基，C1-C6烷氧基，C6-C10芳氧基，苯基-C1-C4烷氧基或三氟甲基，R1为羟基，C1-C6烷氧基，氨基，单C1-C6烷基氨基，二C1-C6烷基氨基， C1-C4烷氧基氨基或苄氧基氨基; 条件是（i）当R 1是羟基，同时R是卤素时，该卤素不是氟; 和（ii）当R 1是羟基，并且同时R是C 1 -C 6烷基时，则该C 1 -C 6烷基不是甲基，及其药学上可接受的盐。