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    Tripeptide derivatives
    4.
    发明授权
    Tripeptide derivatives 失效

    公开(公告)号：US4826814A

    公开(公告)日：1989-05-02

    申请号：US046189

    申请日：1987-05-05

    申请人： Tadahiro Sawayama ,  Masatoshi Tsukamoto ,  Takashi Sasagawa ,  Kazuya Nishimura ,  Kanoo Hosoki ,  Kunihiko Takeyama

    发明人： Tadahiro Sawayama ,  Masatoshi Tsukamoto ,  Takashi Sasagawa ,  Kazuya Nishimura ,  Kanoo Hosoki ,  Kunihiko Takeyama

    IPC分类号： A61K38/00 ,  A61K38/05 ,  A61K38/06 ,  A61K38/55 ,  A61P9/00 ,  A61P9/12 ,  A61P43/00 ,  C07K1/02 ,  C07K1/113 ,  C07K5/02 ,  C07K5/06 ,  C07K5/068 ,  C07K5/08 ,  C07K14/81 ,  A61K37/43

    CPC分类号： C07K5/06086 ,  C07K5/0215 ,  A61K38/00

    摘要： There are provided tripeptide compounds represented by the following formula ##STR1## wherein R.sub.1 represents a C.sub.1-10 alkyl group, a C.sub.4-7 cycloalkyl or C.sub.5-7 cycloalkyl-lower alkyl group, a phenyl or phenyl-lower alkyl group in which the benzene ring may optionally be substituted by a substituent selected from halogen, lower alkyl, lower alkoxy, phenyl, methylenedioxy, ethylenedioxy, amino, di(lower alkyl)amino and hydroxy, a naphthyl or naphthyl-lower alkyl group in which the naphthalene ring may optionally be substituted by a substituent selected from halogen, lower alkyl, lower alkoxy and hydroxy, a heterocyclic or heterocyclic-lower alkyl group in which the heterocycle is a saturated or unsaturated 5- or 6-membered ring containing a nitrogen, oxygen or sulfur atom as the hetero atom, and may optionally be substituted by a substituent selected from halogen, lower alkyl, lower alkoxy, amino, di(lower alkyl)amino, hydroxy, oxo and saturated 5- or 6-membered nitrogen-containing heterocyclic group, and further may optionally be fused to a benzene ring, or an imidazolylvinyl group; R.sub.2 represents a hydrogen atom, a C.sub.1-10 alkyl group or a benzyl group; R.sub.3 represents a group of the formula ##STR2## represents a benzene, cyclopentane or cyclohexane ring, R.sub.4 represents a hydrogen atom, a C.sub.1-10 alkyl group or a benzyl group, p is 0 or 1, q is 1, 2, or 3, and X represents a phenyl group which may optionally be substituted by a substituent selected from halogen, lower alkoxy and hydroxy, a C.sub.4-8 cycloalkyl group, or a C.sub.5-7 cycloalkyl group which is fused to a benzene, and Y represents a hydrogen atom or a lower alkyl group, or X and Y, together with the nitrogen and carbon atoms to which they are bonded, forms a 5- or 6-membered heterocycle which may contain a nitrogen, oxygen or sulfur atom,W represents a single bond, --O-- or --NH--, T represents a single bond, ##STR3## and m is 2 or 3, or salts thereof and processes for production thereof. The compounds are useful as antihypertensive agents.

    Optically active N-substituted phenylalaninols and use thereof
    5.
    发明授权
    Optically active N-substituted phenylalaninols and use thereof 失效
    光学活性N-取代苯丙氨醇及其用途

    公开(公告)号：US4536601A

    公开(公告)日：1985-08-20

    申请号：US535284

    申请日：1983-09-23

    申请人： Masatoshi Tukamoto ,  Tadahiro Sawayama

    发明人： Masatoshi Tukamoto ,  Tadahiro Sawayama

    IPC分类号： C07B57/00 ,  C07C327/22 ,  C07D317/58 ,  C07C91/02 ,  C07D317/44

    CPC分类号： C07D317/58 ,  C07C327/00

    摘要： Optically active N-substituted phenylalaninols of the formula (I): ##STR1## wherein R is isopropyl, 1-ethylpropyl, cyclopentyl, cyclohexyl, cycloheptyl, 4-methylbenzyl, 4-methoxybenzyl, or 3,4-methylenedioxybenzyl; and acid addition salts thereof which are useful as a resolving agent, and a process for preparing D-3-acetylthio-2-methylpropionic acid which comprises reacting DL-3-acetylthio-2-methylpropionic acid with an optically active N-substituted phenylalaninol of the formula (I) to form diastereomeric salts, subjecting the formed diastereomeric salts to a fractional crystallization from a solvent to separate the D-acid salt from the L-acid salt, and then decomposing the D-acid salt with a mineral acid to give D-3-acetylthio-2-methylpropionic acid.

    摘要翻译： 式（I）的光学活性N-取代苯丙氨醇：其中R是异丙基，1-乙基丙基，环戊基，环己基，环庚基，4-甲基苄基，4-甲氧基苄基或3,4-亚甲二氧基苄基; 可用作拆分剂的其酸加成盐，以及制备D-3-乙酰硫基-2-甲基丙酸的方法，其包括将DL-3-乙酰硫基-2-甲基丙酸与光学活性N-取代苯丙氨醇 式（I）形成非对映异构盐，使形成的非对映体盐从溶剂中分级结晶，从D-酸盐与L-酸盐分离，然后用无机酸分解D-酸盐，得到 D-3-乙酰硫基-2-甲基丙酸。