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15 条记录 (耗时 0.033 秒)

    N-methylphenylserine alkyl ester derivatives and uses thereof
    1.
    发明授权
    N-methylphenylserine alkyl ester derivatives and uses thereof 失效
    N-甲基苯基丝氨酸烷基酯衍生物及其用途

    公开(公告)号：US5288898A

    公开(公告)日：1994-02-22

    申请号：US56619

    申请日：1993-05-04

    申请人： Hamao Umezawa ,  Toshiharu Nagatsu ,  Tomio Takeuchi ,  Hajime Morishima ,  Yoshio Sawasaki ,  Hiroshi Takezawa ,  Fujinori Sasaki

    发明人： Hamao Umezawa ,  Toshiharu Nagatsu ,  Tomio Takeuchi ,  Hajime Morishima ,  Yoshio Sawasaki ,  Hiroshi Takezawa ,  Fujinori Sasaki

    IPC分类号： A61K31/195 ,  C07C229/36 ,  A61K31/24

    CPC分类号： A61K31/195

    摘要： As new compounds are now provided N-methyl-3-(3,4-dihydroxyphenyl)serine alkyl esters which are effective as an .alpha.-adrenergic and .beta.-adrenergic agent to stimulate the .alpha.-adrenergic and .beta.-adrenergic functions of the central nervous system of mammalian animals and are expectable to be useful for therapeutic treatment of disorders as invoked by reduced biological activities or functions of the .alpha.- and/or .beta.-adrenergic neurons. N-methyl-L-threo-3-(3,4-dihydroxyphenyl)serine (C.sub.1 -C.sub.6) alkyl esters are preferred amongst the new compounds of this invention.

    摘要翻译： 由于新化合物现在提供作为（α） - 肾上腺素能和（β） - 肾上腺素能药物有效的N-甲基-3-（3,4-二羟基苯基）丝氨酸烷基酯，以刺激（α） - 肾上腺素能和（β ） - 哺乳动物中枢神经系统的肾上腺素能功能，并且预期可用于通过减少（α） - 和/或（β） - 肾上腺素能神经元的生物活性或功能引起的病症的治疗性治疗。 N-甲基-L-苏式-3-（3,4-二羟基苯基）丝氨酸（C1-C6）烷基酯在本发明的新化合物中是优选的。

    Threo-adrenalinecarboxylic acid, and the production and uses thereof
    2.
    发明授权
    Threo-adrenalinecarboxylic acid, and the production and uses thereof 失效

    公开(公告)号：US4833268A

    公开(公告)日：1989-05-23

    申请号：US80165

    申请日：1987-07-30

    申请人： Hamao Umezawa ,  Toshiharu Nagatsu ,  Hirotaro Narabayashi ,  Tomio Takeuchi ,  Shuichi Iwadare ,  Ikuo Matsumoto ,  Junji Yoshizawa ,  Hajime Morishima ,  Koji Tomimoto

    发明人： Hamao Umezawa ,  Toshiharu Nagatsu ,  Hirotaro Narabayashi ,  Tomio Takeuchi ,  Shuichi Iwadare ,  Ikuo Matsumoto ,  Junji Yoshizawa ,  Hajime Morishima ,  Koji Tomimoto

    IPC分类号： C07C229/36 ,  A61K31/195 ,  A61P25/00 ,  A61P25/24 ,  A61P25/26 ,  C07B57/00

    CPC分类号： C07C229/36 ,  Y02P20/55

    摘要： DL- or L-Threo-3-(3,4-dihydroxyphenyl)-N-methyl-serine which may also be termed as DL- or L-threo-adrenalinecarboxylic acid are now provided, which are new compounds useful for therapeutic treatment of Parkinson's disease and mental depression disease. DL-Adrenalinecarboxylic acid may be produced by a new process comprising reacting glycine with O-protected 3,4-dihydroxybenzaldehyde, hydrolyzing the resultant reaction product under acidic conditions to form O-protected DL-3-(3,4-dihydroxyphenyl)serine, isolating the O-protected DL-3-(3,4-dihydroxyphenyl)serine into the threo isomer and the erythro isomer by recrystallization from a suitable organic solvent, introducing an unsubstituted or substituted benzyl group into the 2-amino group of the resulting O-protected DL-threo-3-(3,4-dihydroxyphenyl)serine, then N-methylating the resulting O-protected DL-threo-3-(3,4-dihydroxyphenyl )-N-benzylserine, and removing the O-protecting groups as well as the unsubstituted or substituted benzyl group at the 2-methylamino group of the N-methylation product.L-Adrenalinecarboxylic acid may be produced by a new process comprising introducing a p-methoxybenzyloxycarbonyl group into the 2-amino group of the O-protected DL-threo-3-(3,4-dihydroxyphenyl)serine obtained as an intermediate product, optically resolving the resultant O-protected DL-threo-3-(3,4-dihydroxyphenyl)-N-p-methoxybenzyloxycarbonyl-serine by reacting the latter with an optically active amine and recrystallizing the resultant amine salt products from a suitable organic solvent, removing the p-methoxy-benzyloxycarbonyl group from the resultant O-protected L-threo-(3,4-dihydroxyphenyl)-N-p-methoxybenzyloxycarbonyl-serine, reacting the resultant O-protected L-threo-(3,4-dihydroxyphenyl)serine with dimethyl sulfate in dry acetone to form an O-protected L- or D-threo-(3,4-dihydroxyphenyl)-N-methylserine methyl ester, saponifying this methyl ester and then removing the O-protecting groups from the saponification product.

    5-substituted amino-4-hydroxy-pentenoic acid derivatives and their use
    8.
    发明授权
    5-substituted amino-4-hydroxy-pentenoic acid derivatives and their use 失效

    公开(公告)号：US4927565A

    公开(公告)日：1990-05-22

    申请号：US133642

    申请日：1987-12-16

    申请人： Seiichi Tanaka ,  Yutaka Koike ,  Masato Nakano ,  Shugo Atsuumi ,  Hajime Morishima ,  Kenji Matsuyama

    发明人： Seiichi Tanaka ,  Yutaka Koike ,  Masato Nakano ,  Shugo Atsuumi ,  Hajime Morishima ,  Kenji Matsuyama

    IPC分类号： A61K38/00 ,  C07K5/02 ,  C07K5/062 ,  C07K5/065

    CPC分类号： C07K5/06026 ,  C07K5/0207 ,  C07K5/06078 ,  A61K38/00 ,  Y10S530/86

    摘要： A 5-substituted amino-4-hydroxy-pentenoic acid or its salt represented by the formula: ##STR1## wherein each of R.sup.1 and R.sup.2 which may be the same or different is a hydrogen atom, a lower alkyl group, an aralkyl group, a lower alkoxycarbonyl group, an aryloxycarbonyl group, an aralkyloxycarbonyl group or a lower alkanoyl group which may be substituted by from one to three substituents selected from the group consisting of an amino group, a hydroxyl group, a carboxyl group, an aryloxy group, an aralkyloxycarbonylamino group, a lower alkoxycarbonylamino group and a ##STR2## group (wherein each of X.sup.1 and X.sup.2 which may be the same or different is a hydrogen atom, a lower alkyl group, an aryl group or an aralkyl group, or X.sup.1 and X.sup.2 form together with the adjacent nitrogen atom a 5- or 6-membered heterocyclic group which may further contain a hetero atom selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom) and which may further contain a double bond in its carbon chain, each of R.sup.3, R.sup.4 and R.sup.6 which may be the same or different is a hydrogen atom, a lower alkyl group, a cycloalkyl group, a cycloalkylalkyl group, an aryl group, an aralkyl group or a residue of an acidic neutral or basic amino acid, R.sup.5 is a hydrogen atom or a lower alkyl group, R.sup.7 is a hydrogen atom, a lower alkyl, cycloalkyl, cycloalkylalkyl or aralkyl group which may be substituted by one or two hydroxyl groups or a residue of an acidic, neutral or basic amino acid, R.sup.8 is a hydroxymethyl group or a --CO--R.sup.9 group (wherein R.sup.9 is a hydroxyl group, a --OY group (wherein Y is a lower alkyl group, an aryl group, an aralkyl group, a lower alkoxyalkyl group, a lower alkanoyloxyalkyl group, a lower alkoxycarbonyloxyalkyl group, or a 1-phthalidyl group) or ##STR3## group (wherein each of Y.sup.1 and Y.sup.2 which may be the same or different is a hydrogen atom, a lower alkyl group, an aryl group, an aralkyl group or a cycloalkyl group, or Y.sup.1 and Y.sup.2 form together with the adjacent nitrogen atom a 5- or 6-membered heterocyclic group which may further contain a hetero atom selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom), and each of n and m which may be the same or different is 0 or 1.

    N-acylamino acid derivatives and their use
    9.
    发明授权
    N-acylamino acid derivatives and their use 失效
    N-酰基氨基酸衍生物及其用途

    公开(公告)号：US5481036A

    公开(公告)日：1996-01-02

    申请号：US179195

    申请日：1994-01-10

    申请人： Hajime Morishima ,  Yutaka Koike ,  Masato Nakano ,  Shugo Atsuumi ,  Seiichi Tanaka ,  Kenji Matsuyama

    发明人： Hajime Morishima ,  Yutaka Koike ,  Masato Nakano ,  Shugo Atsuumi ,  Seiichi Tanaka ,  Kenji Matsuyama

    IPC分类号： A61K31/195 ,  A61K31/535 ,  C07C59/66 ,  C07C317/00 ,  C07C317/44 ,  C07C323/43 ,  C07D207/08 ,  C07D211/14 ,  C07D215/12 ,  C07D233/54 ,  C07D239/38 ,  C07D257/04 ,  C07D265/30 ,  C07D285/12 ,  C07D285/125 ,  C07D295/084 ,  C07D295/12 ,  C07D295/125 ,  C07D295/13 ,  C07D295/24 ,  C07D307/38 ,  C07D319/18 ,  C07D401/12 ,  C07F7/18 ,  C07C321/00

    CPC分类号： C07D207/08 ,  C07C323/00 ,  C07C323/43 ,  C07C59/66 ,  C07D211/14 ,  C07D215/12 ,  C07D233/64 ,  C07D239/38 ,  C07D257/04 ,  C07D285/125 ,  C07D295/084 ,  C07D295/125 ,  C07D295/13 ,  C07D295/24 ,  C07D307/38 ,  C07D319/18 ,  C07D401/12 ,  C07F7/1856

    摘要： An N-acylamino acid derivative of the formula: ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.4 and R.sup.6 is hydrogen lower alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl or a monocyclic or bicyclic heterocyclic group containing from to 4 hetero atoms; each of R.sup.3 and R.sup.5 is hydrogen or lower alkyl; A is --CH(OH)--(CH.sub.2).sub.q R.sup.7 wherein R.sup.7 is hydrogen, lower alkyl, cycloalkyl, cyloalkylalkyl, aryl, aralkyl, a monocyclic or bicyclic heterocyclic group containing from to 4 hereto atoms or --E--R.sup.10 wherein E is --S(O).sub.i -- wherein i is 0, 1 or 2, oxygen, --NR.sup.11 -- wherein R.sup.11 is hydrogen, lower alkyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl, or ##STR2## wherein each of R.sup.12 and R.sup.13 is hydrogen, lower alkyl cycloalkyl, cycloalkylalkyl, aryl or aralkyl, and R.sup.10 is hydrogen, lower alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl or a monocyclic or bicyclic heterocyclic group containing from 1 to 4 hetero atoms provided that when R.sup.10 is hydrogen, i is 0, and a is an integer of from 0 to 5; or --CH.sub.2 --CHR.sup.8 --CO--R.sup.9 wherein R.sup.8 is hydrogen, lower alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl or a monocyclic or bicyclic heterocyclic group containing from 1 to 4 hetero atoms, and R.sup.9 is hydroxyl, --OX wherein X is alkyl, aryl, lower alkoxycarbonyloxyalkyl or 1-phthalidyl, or --N(Y.sup.1) (Y.sup.2) wherein each of Y.sup.1 and Y.sup.2 is hydrogen, lower alkyl, aryl, aralkyl or cycloalkyl, or Y and.sup.1 and Y.sup.2 form together with the adjacent nitrogen atom a 5- or 6-membered heterocyclic group which may contain a further hereto atom; m is 0, 1 or 2; and n is an integer of from 1 to 5, provided that when R.sup.1 is hydrogen, m is 0; or a salt thereof, which is useful as hypotensive drugs.

    摘要翻译： 下式的N-酰基氨基酸衍生物：其中R 1，R 2，R 4和R 6各自为氢低级烷基，环烷基，环烷基烷基，芳基，芳烷基或含有4个杂原子的单环或双环杂环基 原子 R 3和R 5各自为氢或低级烷基; A是-CH（OH） - （CH 2）q R 7，其中R 7是氢，低级烷基，环烷基，环烷基烷基，芳基，芳烷基，含有至4原子的单环或双环杂环基或-E-R 10，其中E是-S （O）i-其中i是0,1或2，氧，-NR 11 - ，其中R 11是氢，低级烷基，环烷基，环烷基烷基，芳基或芳烷基，或者其中R 12和R 13各自是氢， 环烷基，环烷基烷基，芳基或芳烷基，R 10为含有1至4个杂原子的氢，低级烷基，环烷基，环烷基烷基，芳基，芳烷基或单环或双环杂环基，条件是当R 10为氢时，i为0， 是从0到5的整数; 或-CH 2 -CHR 8 -CO-R 9，其中R 8是氢，低级烷基，环烷基，环烷基烷基，芳基，芳烷基或含有1至4个杂原子的单环或双环杂环基，并且R 9是羟基， ，芳基，低级烷氧基羰氧基烷基或1-苯酞基，或-N（Y1）（Y2），其中Y1和Y2各自为氢，低级烷基，芳基，芳烷基或环烷基，或Y和1和Y2与相邻的氮原子一起形成 可含有其它原子的5-或6-元杂环基; m为0,1或2; 且n为1至5的整数，条件是当R 1为氢时，m为0; 或其盐，其可用作降压药物。