知搜-全球专利检索

  1. 登录
  2. 注册

搜索结果

5 条记录 (耗时 0.014 秒)

    Renin-inhibitory oligopeptides, their preparation and use
    4.
    发明授权
    Renin-inhibitory oligopeptides, their preparation and use 失效
    肾素抑制寡肽，其制备和用途

    公开(公告)号：US5364844A

    公开(公告)日：1994-11-15

    申请号：US936883

    申请日：1992-08-27

    申请人： Yasuhiro Morisawa ,  Mitsuru Kataoka ,  Yuichiro Yabe ,  Hiroyuki Koike ,  Yasuteru Iijima ,  Hidekuni Takahagi ,  Tatsuo Kokubu ,  Kunio Hiwada

    发明人： Yasuhiro Morisawa ,  Mitsuru Kataoka ,  Yuichiro Yabe ,  Hiroyuki Koike ,  Yasuteru Iijima ,  Hidekuni Takahagi ,  Tatsuo Kokubu ,  Kunio Hiwada

    IPC分类号： C07K5/02 ,  A61K37/02 ,  C07K5/06 ,  C07K5/08

    CPC分类号： C07K5/0227 ,  C07K5/0207

    摘要： Compounds of formula (I): ##STR1## A is a carbon-carbon bond or C.sub.1 -C.sub.3 alkylene; B is imino group or C.sub.1 -C.sub.2 alkylene; R.sup.1 is C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, heterocyclic or optionally substituted amino; R.sup.2 is optionally substituted phenyl or optionally substituted naphthyl; R.sup.3 is thiazolyl, isoxazolyl or imidazolyl; R.sup.4 is isopropyl or cyclohexyl; R.sup.5 and R.sup.6 are C.sub.1 -C.sub.4 alkyl, or, together with the carbon atom to which they are attached, C.sub.3 -C.sub.7 cycloalkyl; R.sup.7 is hydrogen, optionally substituted C.sub.1 -C.sub.6 alkyl group; and R.sup.8 is hydrogen or C.sub.1 -C.sub.4 alkyl. These compounds have renin-inhibitory and, hence, hypotensive activities. The invention also provides a method for the treatment or prophylaxis of hypertension induced by failures in the renin-angiotensin system.

    摘要翻译： 式（I）的化合物：A是碳 - 碳键或C1-C3亚烷基; B是亚氨基或C 1 -C 2亚烷基; R1是C1-C4烷基，C1-C4烷氧基，杂环或任选取代的氨基; R2是任选取代的苯基或任选取代的萘基; R3是噻唑基，异恶唑基或咪唑基; R4是异丙基或环己基; R 5和R 6是C 1 -C 4烷基，或者与它们所连接的碳原子一起是C 3 -C 7环烷基; R7是氢，任选取代的C 1 -C 6烷基; 并且R 8是氢或C 1 -C 4烷基。 这些化合物具有肾素抑制，因此具有降血压活性。 本发明还提供了用于治疗或预防由肾素 - 血管紧张素系统中的失败引起的高血压的方法。

    New renin-inhibitory peptides and their use
    5.
    发明授权
    New renin-inhibitory peptides and their use 失效
    新的肾素抑制肽及其用途

    公开(公告)号：US4698329A

    公开(公告)日：1987-10-06

    申请号：US696334

    申请日：1985-01-30

    申请人： Rei Matsueda ,  Yuichiro Yabe ,  Mitsuo Yamazaki ,  Tatsuo Kokubu ,  Kunio Hiwada

    发明人： Rei Matsueda ,  Yuichiro Yabe ,  Mitsuo Yamazaki ,  Tatsuo Kokubu ,  Kunio Hiwada

    IPC分类号： C07K14/81 ,  A61K38/00 ,  A61K38/05 ,  A61K38/06 ,  A61K38/55 ,  A61P9/12 ,  A61P43/00 ,  C07F9/30 ,  C07K5/02 ,  C07K5/083 ,  A61K37/64 ,  C07K5/08

    CPC分类号： C07K5/0227 ,  C07F9/301 ,  Y10S530/86

    摘要： Compounds of formulaR.sup.1 CO--NH--CH(R.sup.2)--CONH--CH(R.sup.3)--X[wherein:R.sup.1 represents alkyl having an .alpha.-amino or protected .alpha.-amino substituent and an aryl, heterocyclic or heterocyclic-dithio substituent;R.sup.2 represents a variety of aliphatic and cycloaliphatic hydrocarbon groups, which may be substituted;R.sup.3 represents isobutyl, sec-butyl, benzyl or (C.sub.3 -C.sub.8 cycloalkyl)methyl; andX represents a group of formula --CH(--A--R.sup.4)--Y (in which: A represents a single bond or an alkylene group; R.sup.4 represents a carboxy group; a protected carboxy group, a carbamoyl group, an N-substituted carbamoyl group, a carbazoyl group, an N-substituted carbazoyl group or an acyl group; and Y represents a hydroxy group, a mercapto group or a formyl group), ora group of formula --P(O) (R.sup.5)--OH (in which R.sup.5 represents a substituted alkyl group having at least one substituent selected from carboxy groups, protected carboxy groups, N-substituted carbamoyl groups, carbazoyl groups, N-substituted carbazoyl groups, C.sub.2 -C.sub.7 aliphatic carboxylic acyl groups and aromatic carboxylic acyl groups)];and their salts are renin inhibitors, which may be used in the treatment of angiotensin-induced hypertension.

    摘要翻译： 式R 1 CO-NH-CH（R 2）-CONH-CH（R 3）-X [其中：R 1表示具有α-氨基或被保护的α-氨基取代基和芳基，杂环或杂环二硫基取代基的烷基; R2表示可以被取代的各种脂族和脂环族烃基; R 3表示异丁基，仲丁基，苄基或（C 3 -C 8环烷基）甲基; 并且X表示式-CH（-A-R 4）-Y基团（其中：A表示单键或亚烷基; R 4表示羧基;被保护的羧基，氨基甲酰基，N-取代的 氨基甲酰基，咔唑基，N-取代的咔唑基或酰基; Y表示羟基，巯基或甲酰基）或式-P（O）（R5）-OH（ 其中R 5表示具有至少一个选自羧基，保护的羧基，N-取代的氨基甲酰基，咔唑基，N-取代的咔唑基，C 2 -C 7脂族羧酸酰基和芳族羧酰基的取代基的烷基） ]; 其盐类为肾素抑制剂，可用于治疗血管紧张素诱导的高血压。