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12 条记录 (耗时 0.02 秒)

    Carboxycyclopropylglycine and process for producing the same
    1.
    发明授权
    Carboxycyclopropylglycine and process for producing the same 失效
    羧基环丙基甘氨酸及其制备方法

    公开(公告)号：US4959493A

    公开(公告)日：1990-09-25

    申请号：US184920

    申请日：1988-04-22

    申请人： Yasufumi Ohfume ,  Keiko Shimamoto ,  Haruhiko Shinozaki

    发明人： Yasufumi Ohfume ,  Keiko Shimamoto ,  Haruhiko Shinozaki

    IPC分类号： C07C227/32 ,  C07C229/46

    CPC分类号： C07C229/46 ,  C07C227/32 ,  C07C2101/02

    摘要： A novel compound (2S,3R,4S)-carboxycyclopropylglycine represented by the formula (1): ##STR1## has proved to be the most potent agonist for the N-methyl-D-aspartate (NMDA) receptor which is one of the glutamate receptor sub-types in the mammalian central nervous system. This compound provides useful tools to open a road to the development of glutamic acid receptor antagonists that may have thereapeutic value in epilepsy, neuronal disorders such as Huntington's chorea and Parkinsonism, as well as various acute and chronic neurodegerative disorders.Also disclosed is a process for producing this compound, as well as a process for individually synthesizing four carboxycyclopropylglycine steroisomers including those of the following formulas (1a, 1b, 1c): ##STR2## and the formula (1).

    摘要翻译： 由式（1）表示的新型化合物（2S，3R，4S） - 羧基环丙基甘氨酸：已被证明是N-甲基-D-天冬氨酸（NMDA）受体最有效的激动剂，它是一种 的哺乳动物中枢神经系统中的谷氨酸受体亚型。 该化合物提供了有用的工具，以开辟可能具有癫痫治疗价值的谷氨酸受体拮抗剂，亨廷顿舞蹈病和帕金森综合征等神经元疾病以及各种急性和慢性神经变性疾病的发展之路。 还公开了制备该化合物的方法，以及用于单独合成包括下式（1a，1b，1c）的四种羧基环丙基甘氨酸立体异构体的方法：（1a）图像（1b）图像 （1c）和式（1）。

    2-(2,3-dicarboxycyclopropyl) glycine and method for producing the same
    2.
    发明授权
    2-(2,3-dicarboxycyclopropyl) glycine and method for producing the same 失效
    2-（2,3-二羧基环丙基）甘氨酸及其制备方法

    公开(公告)号：US5334757A

    公开(公告)日：1994-08-02

    申请号：US53693

    申请日：1993-04-29

    申请人： Yasufumi Ohfune ,  Keiko Shimamoto ,  Haruhiko Shinozaki ,  Michiko Ishida

    发明人： Yasufumi Ohfune ,  Keiko Shimamoto ,  Haruhiko Shinozaki ,  Michiko Ishida

    IPC分类号： A61K31/195 ,  A61P25/00 ,  A61P25/08 ,  C07C227/18 ,  C07C229/46

    CPC分类号： C07C229/46 ,  C07C2101/02

    摘要： (2S,1'R,2'R,3'R)-2-(2,3-dicarboxycyclopropyl)-glycine (DCG-I) and (2S,1'S,2'S,3'S)-2-(2,3-dicarboxycyclopropyl)glycine (DCG-II), as well as methods for synthesizing these compounds are provided. Studies on L-glutamate receptors with the use of DCG-I and DCG-II, which are agonists for NMDA receptors, contribute to the development of remedies for various nervous disorders. Further, DCG-I and DCG-II selectively inhibit monosynaptic reflex even at a low concentration, which makes them useful as a remedy for spastic palsy, an anesthetic and an analgesic.

    摘要翻译： （2S，1'R，2'R，3'R）-2-（2,3-二羧基环丙基） - 甘氨酸（DCG-1）和（2S，1'S，2'S，3'S） 二羧基环丙基）甘氨酸（DCG-II），以及合成这些化合物的方法。 使用作为NMDA受体激动剂的DCG-1和DCG-II对L-谷氨酸受体的研究有助于各种神经障碍的治疗的发展。 此外，即使在低浓度下，DCG-I和DCG-II选择性地抑制单突触反射，这使得它们可用作痉挛性麻痹，麻醉剂和止痛剂的补救剂。

    Alkylenediamine derivatives
    5.
    发明授权
    Alkylenediamine derivatives 失效
    烷二胺衍生物

    公开(公告)号：US5310902A

    公开(公告)日：1994-05-10

    申请号：US741590

    申请日：1991-08-07

    申请人： Mitsuo Masaki ,  Masaru Satoh ,  Naoya Moritoh ,  Koichi Hashimoto ,  Toshiro Kamishiro ,  Haruhiko Shinozaki

    发明人： Mitsuo Masaki ,  Masaru Satoh ,  Naoya Moritoh ,  Koichi Hashimoto ,  Toshiro Kamishiro ,  Haruhiko Shinozaki

    IPC分类号： C07D295/13 ,  C07D223/00 ,  C07D211/26

    CPC分类号： C07D295/13

    摘要： Novel alkylenediamine derivatives effectively employable glutamate blockers have the formula (I) or (II): ##STR1## wherein each of R.sup.1 and R.sup.6 is an aliphatic hydrocarbon group, an alicyclic hydrocarbon group, an aryl group, or an aralkyl group; each of R.sup.2 and R.sup.7 is an aliphatic hydrocarbon group, an alkoxy group, an aliphatic hydrocarbon group containing an ester bonding, an aliphatic hydrocarbon group containing an ether bonding, or an aryloxy group; each of R.sup.3, R.sup.4, R.sup.5 R.sup.8, R.sup.9 and R.sup.10 is hydrogen, an alkyl group, an alkoxy group, an acyloxy group, an aryl group, an aralkyl group, hydroxyl, a hydroxylalkyl group, halogen, nitrile, nitro, amino, carbamoyl or alkoxycarbonyl; and each of m and n is an integer of 0-3 (m+n does not exceed 3); k is an integer of 1-4; each of p and i is an integer of 2-13; and each of q and j is an integer of 4-7.

    摘要翻译： 新型亚烷基二胺衍生物有效地可用的谷氨酸盐阻滞剂具有式（I）或（II）：其中R 1和R 6各自为脂族烃基，脂环族烃基，芳基 ，或芳烷基; R 2和R 7各自为脂族烃基，烷氧基，含酯键的脂族烃基，含有醚键的脂族烃基或芳氧基; R 3，R 4，R 5，R 9和R 10各自为氢，烷基，烷氧基，酰氧基，芳基，芳烷基，羟基，羟基烷基，卤素，腈，硝基，氨基，氨基甲酰基 或烷氧基羰基; 并且m和n分别为0-3的整数（m + n不超过3）; k是1-4的整数; p和i中的每一个是2-13的整数; 并且q和j中的每一个是4-7的整数。

    Cyclopropylglycine derivatives and agonists for metabotronic L-glutamate receptors
    6.
    发明授权
    Cyclopropylglycine derivatives and agonists for metabotronic L-glutamate receptors 失效
    代谢异丁酸L-谷氨酸受体的环丙基甘氨酸衍生物和激动剂

    公开(公告)号：US06245919B1

    公开(公告)日：2001-06-12

    申请号：US09221916

    申请日：1998-12-28

    申请人： Haruhiko Shinozaki ,  Takeo Taguchi ,  Michiko Ishida

    发明人： Haruhiko Shinozaki ,  Takeo Taguchi ,  Michiko Ishida

    IPC分类号： C07D20932

    CPC分类号： C07C229/46 ,  C07B2200/07 ,  C07C2601/02

    摘要： A cyclopropylglycine derivative having the following formula: and an intermediate compound for the synthesis of the cyclopropylglycine derivative are novel compounds. The cyclopropylglycine derivative shows a selectivity higher than that of the known agonists to metabotropic L-glutamate receptors, and therefore is a metabotropic type agonist to L-glutamate which has excellent characteristics.

    摘要翻译： 具有下式的环丙基甘氨酸衍生物和用于合成环丙基甘氨酸衍生物的中间体化合物是新化合物。 环丙基甘氨酸衍生物显示比已知的代谢型L-谷氨酸受体的激动剂更高的选择性，因此是具有优异特征的代谢型激动剂L-谷氨酸。

    Alkylenediamine derivatives
    9.
    发明授权
    Alkylenediamine derivatives 失效
    烷二胺衍生物

    公开(公告)号：US5070196A

    公开(公告)日：1991-12-03

    申请号：US562422

    申请日：1990-08-01

    申请人： Mitsuo Masaki ,  Masaru Satoh ,  Naoya Moritoh ,  Koichi Hashimoto ,  Toshiro Kamishiro ,  Haruhiko Shinozaki

    发明人： Mitsuo Masaki ,  Masaru Satoh ,  Naoya Moritoh ,  Koichi Hashimoto ,  Toshiro Kamishiro ,  Haruhiko Shinozaki

    IPC分类号： C07D295/13

    CPC分类号： C07D295/13

    摘要： Novel alkylenediamine derivatives effectively employable as glutamate blockers have the formula (I) or (II): ##STR1## wherein each of R.sup.1 and R.sup.6 is an aliphatic hydrocarbon group, an alicyclic hydrocarbon group, an aryl group, or an aralkyl group; each of R.sup.2 and R.sup.7 is an aliphatic hydrocarbon group, an alkoxy group, an aliphatic hydrocarbon group containing an ester bonding, an aliphatic hydrocarbon group containing an ether bonding, or an aryloxy group; each of R.sup.3, R.sup.4, R.sup.5, R.sup.8, R.sup.9 and R.sup.10 is hydrogen, an alkyl group, an alkoxy group, an acyloxy group, an aryl group, an aralkyl group, hydroxyl, a hydroxylalkyl group, halogen, nitrile, nitro, amino, carbamoyl or alkoxycarbonyl; and each of m and n is an integer of 0-3 (m+n does not exceed 3); k is an integer of 1-4; each of p and i is an integer of 2-13; and each of q and j is an integer of 4-7.

    摘要翻译： 作为谷氨酸盐阻滞剂有效利用的新型亚烷基二胺衍生物具有式（I）或（II）：其中R 1和R 6各自为脂族烃基，脂环族烃基，芳基 基团或芳烷基; R 2和R 7各自为脂族烃基，烷氧基，含酯键的脂族烃基，含有醚键的脂族烃基或芳氧基; R 3，R 4，R 5，R 8，R 9和R 10各自为氢，烷基，烷氧基，酰氧基，芳基，芳烷基，羟基，羟烷基，卤素，腈，硝基，氨基， 氨基甲酰基或烷氧基羰基; 并且m和n分别为0-3的整数（m + n不超过3）; k是1-4的整数; p和i中的每一个是2-13的整数; 并且q和j中的每一个是4-7的整数。

    Amino-alcohol derivatives and processes for their preparation
    10.
    发明授权
    Amino-alcohol derivatives and processes for their preparation 失效
    氨基醇衍生物及其制备方法

    公开(公告)号：US5250546A

    公开(公告)日：1993-10-05

    申请号：US551037

    申请日：1990-07-11

    申请人： Mitsuo Masaki ,  Haruhiko Shinozaki ,  Masaru Satoh ,  Naoya Moritoh ,  Koichi Hashimoto ,  Toshiro Kamishiro

    发明人： Mitsuo Masaki ,  Haruhiko Shinozaki ,  Masaru Satoh ,  Naoya Moritoh ,  Koichi Hashimoto ,  Toshiro Kamishiro

    IPC分类号： C07D295/13 ,  A61K31/445

    CPC分类号： C07D295/13

    摘要： Amino-alcohol derivatives of the formula, ##STR1## where R.sub.1 is a straight or branched alkyl group having 3 to 8 carbon atoms, R.sub.2 and R.sub.3 are each a lower alkyl group, or R.sub.2 and R.sub.3 form a 5- to 7-membered ring together with the adjacent nitrogen atom which may have an oxygen atom attached thereto, R.sub.4 is a hydrogen atom or a lower alkyl group, R.sub.5 is a hydrogen atom or a lower alkyl group, X is a hydrogen or halogen atom or a lower alkyl or lower alkoxy group, and n is an integer of 2 or 3, and acid addition salts thereof, are effectively useful as medicines and agricultural chemicals. Processes are also disclosed for preparing such compounds.

    摘要翻译： 其中R1是具有3至8个碳原子的直链或支链烷基，R2和R3各自为低级烷基，或R2和R3形成5-至7-元环的下式的氨基醇衍生物， 与可能具有氧原子的相邻氮原子一起，R4是氢原子或低级烷基，R5是氢原子或低级烷基，X是氢或卤素原子或低级烷基或低级烷基 烷氧基，n为2或3的整数，其酸加成盐可有效用作药物和农药。 还公开了制备这些化合物的方法。