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42 条记录 (耗时 0.046 秒)

    Aminophosponic acid derivative
    8.
    发明授权
    Aminophosponic acid derivative 失效
    氨基磷酸衍生物

    公开(公告)号：US5380921A

    公开(公告)日：1995-01-10

    申请号：US55872

    申请日：1993-05-04

    申请人： Kiyofumi Ishikawa ,  Takehiro Fukami ,  Takashi Hayama ,  Kenji Matsuyama ,  Kazuhito Noguchi ,  Mitsuo Yano

    发明人： Kiyofumi Ishikawa ,  Takehiro Fukami ,  Takashi Hayama ,  Kenji Matsuyama ,  Kazuhito Noguchi ,  Mitsuo Yano

    IPC分类号： A61K31/66 ,  A61K31/675 ,  A61K38/00 ,  A61P9/08 ,  A61P9/12 ,  A61P11/08 ,  A61P13/02 ,  A61P15/00 ,  C07F9/38 ,  C07F9/40 ,  C07K5/06 ,  C12N9/99 ,  C07F9/08

    CPC分类号： C07K5/06191 ,  C07F9/3808 ,  A61K38/00

    摘要： There are provided novel aminophosphonic acid derivatives of the general formula [I]: ##STR1## wherein n is an integer of 2 or 3; R.sup.1 is a phenyl, naphthyl, indolyl, benzothienyl, benzofuryl or benzoxazolyl group which may have 1 to 3 substituents selected from the group consisting of hydroxyl and lower alkyloxy groups, or a hydrogen atom; R.sup.2 is a lower alkyl group, a benzyl group, a 4-hydroxybenzyl group, a 3-indolylmethyl group or a .beta.-phenethyl group; and A is an optional residue of an amino acid selected from the group consisting of tryptophane, tyrosine, phenylalanine, homophenylalanine, naphthylalanine or N.sup..omega. -nitroarginine, and their pharmaceutically acceptable salts. The compounds according to the present invention and their pharmaceutically acceptable salts exhibit an inhibitory activity against endothelin-converting enzyme, and are expected to be useful as a drug treating various diseases with which endothelin is concerned.

    摘要翻译： 提供了通式[I]的新型氨基膦酸衍生物：其中n为2或3的整数; R1是可以具有1至3个选自羟基和低级烷氧基或氢原子的取代基的苯基，萘基，吲哚基，苯并噻吩基，苯并呋喃基或苯并恶唑基; R2是低级烷基，苄基，4-羟基苄基，3-吲哚基甲基或β-苯乙基; A是任选的氨基酸残基，其选自色氨酸，酪氨酸，苯丙氨酸，高苯丙氨酸，萘丙氨酸或N，ω-硝基精氨酸，及其药学上可接受的盐。 根据本发明的化合物及其药学上可接受的盐表现出对内皮素转化酶的抑制活性，并且预期可用作治疗涉及内皮素的各种疾病的药物。

    Phosphinic acid derivatives
    10.
    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.