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23 条记录 (耗时 0.03 秒)

    Phosphinic acid derivatives
    21.
    发明授权
    Phosphinic acid derivatives 失效
    次膦酸衍生物

    公开(公告)号：US4988681A

    公开(公告)日：1991-01-29

    申请号：US370190

    申请日：1989-06-22

    申请人： Kiyofumi Ishikawa ,  Takehiro Fukami ,  Hiroshi Naganuma ,  Kyoko Nakamichi

    发明人： Kiyofumi Ishikawa ,  Takehiro Fukami ,  Hiroshi Naganuma ,  Kyoko Nakamichi

    IPC分类号： C07F9/30 ,  C07F9/32 ,  C07F9/58 ,  C07F9/6506 ,  C07F9/6518

    CPC分类号： C07F9/65182 ,  C07F9/302 ,  C07F9/303 ,  C07F9/3217 ,  C07F9/3223 ,  C07F9/582 ,  C07F9/65062

    摘要： A phosphinic acid derivative represented by the general formula [I], or a pharmaceutically acceptable salt thereof, ##STR1## wherein R.sup.1 represents an alkyl, cycloalkyl or aralkyl group which may be substituted; R.sup.2 and R.sup.5 may be identical or different, and each represents a hydrogen atom, or an ester residue capable of forming a non-toxic ester hydrolyzable in vivo; and A represents a group of the formula ##STR2## wherein R.sup.3 represents an alkyl group, a group of the formula ##STR3## wherein R.sup.30 represents a halogen atom, a carboxyl group, a hydroxyl group, a cycloalkyl group which may be substituted, an aryl group which may be substituted, an arylthio group, a heteroarylthio group which may be substituted, an alkylthio group which may be substituted, an amino group which may be substituted, or a lower alkoxycarbonyl group; R.sup.31 represents a hydrogen atom or a lower alkyl group; and n represents an integer of 0 to 6, a cycloalkyl group which may be substituted or an aryl group which may be substituted; and the double bond at A has a Z-configuration, or a group of the formula ##STR4## wherein R.sup.4 represents a cycloalkyl group which may be substituted. Said phosphinic acid derivative is useful for reducing renal toxicity induced by a carbapenem or penem antibiotic and for inhibiting dipeptidase.

    Process for producing halogenated heteroaryl compounds
    22.
    发明授权
    Process for producing halogenated heteroaryl compounds 失效
    卤化杂芳基化合物的制备方法

    公开(公告)号：US6114524A

    公开(公告)日：2000-09-05

    申请号：US319642

    申请日：1999-06-08

    申请人： Shigemitsu Okada ,  Ryosuke Ushijima ,  Kiyofumi Ishikawa

    发明人： Shigemitsu Okada ,  Ryosuke Ushijima ,  Kiyofumi Ishikawa

    IPC分类号： C07D213/61 ,  C07D213/79 ,  C07D213/85 ,  C07D215/48 ,  C07D241/44 ,  C07D213/02 ,  C07D215/18 ,  C07D215/20 ,  C07D237/12 ,  C07D237/14

    CPC分类号： C07D213/79 ,  C07D213/61 ,  C07D213/85 ,  C07D215/48 ,  C07D241/44

    摘要： The present invention relates to a process for producing a compound represented by the formula (II): ##STR1## wherein X is a halogen atom, each of A.sup.1, A.sup.2 and A.sup.3 are the same or different and are selected from a carbon atom or a nitrogen atom, provided that at least A.sup.1, A.sup.2, or A.sup.3 is a nitrogen atom. Each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same or different and are selected from a hydrogen atom, a lower alkyl group, a cyano group, a carboxyl group, a lower alkoxycarbonyl group, a halogen atom, and a nitro group. It is also provided that where R.sup.1 and R.sup.2 are adjacent to each other, R.sup.1 and R.sup.2 may be combined with each other to form a 5- or 6-membered ring which may carry on the ring thereof one substituent selected from the group consisting of a lower alkyl group, a nitrile group, a carboxyl group, a lower alkoxycarbonyl group, a carbamoyl group, a halogen atom, a nitro group, and an amino-(lower alkyl) group. The compound is prepared by reacting a compound represented by the formula (I): ##STR2## with a quaternary ammonium halide in the presence of phosphorus pentoxide.

    摘要翻译： PCT No.PCT / JP97 / 04508 Sec。 371 1999年6月8日第 102（e）日期1999年6月8日PCT 1997年12月9日PCT公布。 第WO98 / 25906号公报 日期：1998年6月18日本发明涉及式（II）表示的化合物的制造方法：其中，X为卤素原子，A1，A2和A3各自相同或不同，选自碳原子数 或氮原子，条件是至少A1，A2或A3为氮原子。 R 1，R 2，R 3和R 4各自相同或不同，选自氢原子，低级烷基，氰基，羧基，低级烷氧基羰基，卤素原子和硝基。 还提供其中R 1和R 2彼此相邻，R 1和R 2可以彼此组合以形成5-或6-元环，其可以在其环上带有一个选自以下的取代基： 低级烷基，腈基，羧基，低级烷氧基羰基，氨基甲酰基，卤素原子，硝基和氨基 - （低级烷基）基。 该化合物通过在五氧化二磷存在下使式（I）表示的化合物与季铵卤化物反应来制备。