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9 条记录 (耗时 0.021 秒)

    Epoxysuccinic acid derivatives, their production and use
    1.
    发明授权
    Epoxysuccinic acid derivatives, their production and use 失效
    环氧琥珀酸衍生物，其生产和使用

    公开(公告)号：US5679708A

    公开(公告)日：1997-10-21

    申请号：US513895

    申请日：1995-09-05

    申请人： Shigetoshi Tsubotani ,  Masayuki Takizawa ,  Junji Mizoguchi

    发明人： Shigetoshi Tsubotani ,  Masayuki Takizawa ,  Junji Mizoguchi

    IPC分类号： C07D303/48 ,  A61K31/335 ,  C07D405/12

    CPC分类号： C07D303/48

    摘要： The present invention relates to a compound of the formula: ##STR1## wherein R.sub.1 stands for an optionally esterified or amidated carboxyl group, X stands for an optionally substituted divalent hydrocarbon residue, R.sub.2 stands for hydrogen or an optionally substituted hydrocarbon residue, R.sub.3 stands for an alkyl group which is substituted with a group bonded through O or S(O).sub.n wherein n is 0, 1 or 2, with a proviso that when the partial structural formula: --NH--X--CO-- is leucine residue, R.sub.3 is not 3-hydroxy-3-methylbutyl group nor 4-hydroxy-3-methylbutyl group, or a salt thereof, which is useful as prophylactic and therapeutic agents of bone diseases and as inhibitory agents of thiol protease.

    摘要翻译： PCT No.PCT / JP95 / 01004 Sec。 371 1995年9月5日第 102（e）1995年9月5日PCT PCT 1995年5月25日PCT公布。 出版物WO95 / 32954 日期：1994年12月7日本发明涉及下式化合物：其中R1代表任意酯化或酰胺化的羧基，X代表任意取代的二价烃残基，R2代表氢或 任选取代的烃基，R3代表被O或S（O）n键合的基团取代的烷基，其中n为0,1或2，条件是当部分结构式为：-NH-X- CO-是亮氨酸残基，R3不是3-羟基-3-甲基丁基也不是4-羟基-3-甲基丁基，或其盐，其可用作骨疾病的预防和治疗剂，并且作为硫醇蛋白酶的抑制剂 。

    Lactol derivatives, their production and use
    8.
    发明授权
    Lactol derivatives, their production and use 失效
    乳糖衍生物，其生产和使用

    公开(公告)号：US5496834A

    公开(公告)日：1996-03-05

    申请号：US300738

    申请日：1994-09-02

    申请人： Takashi Sohda ,  Yukio Fujisawa ,  Satoru Oi ,  Junji Mizoguchi

    发明人： Takashi Sohda ,  Yukio Fujisawa ,  Satoru Oi ,  Junji Mizoguchi

    IPC分类号： A61K38/00 ,  C07K5/06 ,  C07K5/078 ,  A61K31/44 ,  A61K31/35 ,  A61K31/40

    CPC分类号： C07K5/06139 ,  C07K5/06043 ,  A61K38/00

    摘要： The present invention provides novel compound of the formulas (Ia) or (I): ##STR1## wherein Q is one or two amino acid residues which may be substituted; R.sup.3 is a carboxyl group which may be esterified or an acyl group; A is an alkylene group; B is hydrogen or an alkyl group which may be substituted or an acyl group; or a salt thereof; ##STR2## wherein R.sup.1 and R.sup.2 may be the same or different and each is hydrogen or a hydrocarbon residue which may be substituted; R.sup.3, A and B have the same definitions as those shown above; m and n each is 0 or 1; provided that where both m and n are both equal to 0, R.sup.3 is a carboxyl group which may be esterified or an acyl group having not less than 7 carbon atoms; or a salt thereof.The compound (Ia) or (I) shows cathepsin L inhibitory and bone resorption inhibitory activities and are useful as a prophylactic/therapeutic agent for osteoporosis.

    摘要翻译： 本发明提供新的式（Ia）或（I）化合物：其中Q是一个或两个可被取代的氨基酸残基; R3是可被酯化的羧基或酰基; A是亚烷基; B是氢或可以被取代的烷基或酰基; 或其盐; （I）其中R 1和R 2可以相同或不同，各自为氢或可被取代的烃残基; R3，A和B具有与上述相同的定义; m和n各自为0或1; 条件是当m和n都等于0时，R 3是可被酯化的羧基或具有不少于7个碳原子的酰基; 或其盐。 化合物（Ia）或（I）表示组织蛋白酶L抑制和骨吸收抑制活性，可用作骨质疏松症的预防/治疗剂。

    Condensed thiadiazole derivative, method of its production, and use thereof
    9.
    发明授权
    Condensed thiadiazole derivative, method of its production, and use thereof 失效
    缩合噻二唑衍生物，其制备方法及其用途

    公开(公告)号：US5550138A

    公开(公告)日：1996-08-27

    申请号：US039579

    申请日：1993-03-23

    申请人： Takashi Sohda ,  Zen-ichi Terashita ,  Yu Momose ,  Yukio Fujisawa ,  Junji Mizoguchi

    发明人： Takashi Sohda ,  Zen-ichi Terashita ,  Yu Momose ,  Yukio Fujisawa ,  Junji Mizoguchi

    IPC分类号： C07D513/04 ,  A61K31/435

    CPC分类号： C07D513/04

    摘要： (1) a compound represented by the following formula (I): ##STR1## wherein R represents a hydrocarbon group or heterocyclic group which may be substituted; the ring A represents a pyridine ring having a substituent or a thiazole ring which may be substituted; or a pharmaceutically acceptable salt thereof, and a method of its production, and(2) an endothelin receptor antagonist, an cathepsin B inhibitor or a bone resorption suppressor having as an active ingredient a compound represented by the following formula (I'): ##STR2## wherein R has the same definition as in term (1); the ring A' represents a pyridine ring or thiazole ring which may be substituted; or a pharmaceutically acceptable salt thereof.

    摘要翻译： （1）由下式（I）表示的化合物：其中R表示可被取代的烃基或杂环基; 环A表示具有取代基的吡啶环或可被取代的噻唑环; 或其药学上可接受的盐及其制备方法，和（2）作为活性成分的下式（I'）表示的化合物的内皮素受体拮抗剂，组织蛋白酶B抑制剂或骨吸收抑制剂： （I'）其中R与术语（1）具有相同的定义; 环A'表示可被取代的吡啶环或噻唑环; 或其药学上可接受的盐。