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    Cyclic depsipeptides and drugs containing the same as the active ingredient
    2.
    发明授权
    Cyclic depsipeptides and drugs containing the same as the active ingredient 失效
    循环利肽和含有与活性成分相同的药物

    公开(公告)号：US06858585B1

    公开(公告)日：2005-02-22

    申请号：US09147434

    申请日：1997-06-25

    申请人： Makoto Yanai ,  Masashi Suzuki ,  Norio Oshida ,  Koji Kawamura ,  Shigeru Hiramoto ,  Orie Yasuda ,  Nobuhiro Kinoshita ,  Akiko Shingai ,  Masako Takasu

    发明人： Makoto Yanai ,  Masashi Suzuki ,  Norio Oshida ,  Koji Kawamura ,  Shigeru Hiramoto ,  Orie Yasuda ,  Nobuhiro Kinoshita ,  Akiko Shingai ,  Masako Takasu

    IPC分类号： A61K38/00 ,  C07K7/06 ,  A61K38/15 ,  C07K7/00

    CPC分类号： C07K7/06 ,  A61K38/00

    摘要： Cyclic depsipeptides represented by the formula wherein: R is a straight or branched alkyl group of 5-20 carbon atoms or a straight or branched alkoxymethyl group of 5-15-carbon atoms; A, B, D, E and F independently each other are alanine, valine, leucine, isoleucine, phenylalanine, etc.; W and Z independently each other are aspartic acid, asparagine, glutamic acid or glutamine; and m and n independently each other is 0 or 1, or pharmacologically acceptable salts thereof. The present compounds are prepared according to a method conventionally used in peptide synthesis. The present compounds are useful as an agent for promoting the production of apolipoprotein E, a therapeutic agent for neurologic damages, a therapeutic agent for dementia, an agent for inhibiting the production of apolipoprotein B, an agent for promoting the production of apolipoprotein A1 or a therapeutic agent for hyperlipemia.

    摘要翻译： 以下式表示的环状缩酚酸酯：R为5-20个碳原子的直链或支链烷基或5-15个碳原子的直链或支链烷氧基甲基; A，B，D，E和F独立地为丙氨酸，缬氨酸，亮氨酸，异亮氨酸，苯丙氨酸等; W和Z独立地是天冬氨酸，天冬酰胺，谷氨酸或谷氨酰胺; m和n彼此独立地为0或1，或其药理学上可接受的盐。 本发明化合物根据肽合成中常规使用的方法制备。 本发明化合物可用作促进载脂蛋白E的产生，神经损伤治疗剂，痴呆治疗剂，抑制载脂蛋白B的制备的试剂，促进载脂蛋白A1的制造的试剂或 高脂血症治疗剂。

    Bicyclic depsipeptides
    3.
    发明授权
    Bicyclic depsipeptides 失效
    双环脱肽

    公开(公告)号：US06211145B1

    公开(公告)日：2001-04-03

    申请号：US09212481

    申请日：1998-12-16

    申请人： Makoto Yanai ,  Masashi Suzuki ,  Norio Oshida ,  Koji Kawamura ,  Shigeru Hiramoto ,  Orie Yasuda ,  Nobuhiro Kinoshita ,  Akiko Shingai ,  Masako Takasu

    发明人： Makoto Yanai ,  Masashi Suzuki ,  Norio Oshida ,  Koji Kawamura ,  Shigeru Hiramoto ,  Orie Yasuda ,  Nobuhiro Kinoshita ,  Akiko Shingai ,  Masako Takasu

    IPC分类号： A61K3808

    CPC分类号： C07K7/06 ,  A61K38/00 ,  C07K7/56 ,  C07K7/64

    摘要： The present invention provides a bicyclic depsipeptide having the formula (1) wherein: R is a straight or branched alkyl group of 5-20 carbon atoms or a straight or branched alkoxymethyl group of 5-15 carbon atoms; A, D, E and J independently are a residue of an amino acid selected from the group of alanine, valine, leucine, etc.; B and F are the same or different and a residue of an amino acid selected from the group consisting of cysteine, aspartic acid, glutamic acid, lysine, hydroxylysine and serine; G is a disulfide bond, an amido bond or an ester bond; W is a residue of an amino acid selected from the group consisting of aspartic acid and glutamic acid; Z is a residue of an amino acid selected from the group consisting of aspartic acid, asparagine, glutamic acid and glutamine; l, m, n, p and q independently are 0 or 1; or a pharmacologically acceptable salt thereof.

    摘要翻译： 本发明提供具有式（1）的双环脱肽酶，其中：R是5-20个碳原子的直链或支链烷基或5-15个碳原子的直链或支链烷氧基甲基; A，D，E和J独立地是选自丙氨酸，缬氨酸，亮氨酸等的氨基酸的残基; B和F相同或不同，并且选自半胱氨酸，天冬氨酸，谷氨酸，赖氨酸，羟赖氨酸和丝氨酸的氨基酸残基; G是二硫键，酰胺键或酯键; W是选自天冬氨酸和谷氨酸的氨基酸残基; Z是选自天冬氨酸，天冬酰胺，谷氨酸和谷氨酰胺的氨基酸的残基; l，m，n，p和q独立地为0或1; 或其药理学上可接受的盐。

    Flash device
    4.
    发明授权
    Flash device 失效
    闪存设备

    公开(公告)号：US4982210A

    公开(公告)日：1991-01-01

    申请号：US349843

    申请日：1989-05-10

    申请人： Takahisa Shimada ,  Togo Teramoto ,  Toshihiko Taniguchi ,  Nobuharu Murashima ,  Makoto Yanai

    发明人： Takahisa Shimada ,  Togo Teramoto ,  Toshihiko Taniguchi ,  Nobuharu Murashima ,  Makoto Yanai

    IPC分类号： G03B15/05 ,  G03B15/03

    CPC分类号： G03B15/05 ,  G03B2215/051

    摘要： A flash device in which a mechanism for shifting a light emitting section up and down and a mechanism for changing over the light distribution angle can be automatically controlled by means of a single motor and which occupies a comparatively small spacing when mounted on a camera. The flash device includes a bidirectional drive motor mounted in a body member, and a shiftable member having the light emitting section thereon. The shiftable member is shifted by rotation of the motor in either direction between a retracted inoperative position and a projected operative position. The light distribution angle of the light emitting section is changed over by continued energization of the motor after the shiftable member is moved from the inoperative to the operative position. A friction mechanism is interposed in a motion transmitting mechanism from the motor to the shiftable member. The motor and the motion transmitting mechanism are disposed at a location within the body member at which they are located, when mounted on a camera, above a spacing sidewardly of a central portion of the camera in which a pentagonal prism is disposed.

    摘要翻译： 其中用于使发光部分上下移动的机构和用于改变配光角度的机构的闪光装置可以通过单个电动机自动控制，并且当安装在照相机上时占据相对较小的间隔。 闪光装置包括安装在主体部件中的双向驱动马达和在其上具有发光部的可移动部件。 可移动构件通过电动机在缩回非操作位置和投影操作位置之间的任一方向上的旋转而移动。 在可移动构件从不工作状态移动到操作位置之后，通过电动机的继续通电来改变发光部分的配光角度。 摩擦机构插入到运动传递机构中，从马达到可移动构件。 当安装在相机上时，马达和运动传递机构设置在它们所位于的主体部件内的位置，在设置有五边形棱镜的照相机的中心部分的一侧的间隔的上方。

    Indole derivatives
    8.
    发明授权
    Indole derivatives 失效
    INDOLE DORIVATIVES

    公开(公告)号：US5124324A

    公开(公告)日：1992-06-23

    申请号：US614219

    申请日：1990-11-16

    申请人： Haruhiko Kikuchi ,  Hiroaki Satoh ,  Makoto Yanai ,  Toshio Suguro ,  Koichiro Hagihara

    发明人： Haruhiko Kikuchi ,  Hiroaki Satoh ,  Makoto Yanai ,  Toshio Suguro ,  Koichiro Hagihara

    IPC分类号： C07D209/42 ,  C07D401/12 ,  C07D403/12 ,  C07D403/14

    CPC分类号： C07D401/12 ,  C07D209/42 ,  C07D403/12 ,  C07D403/14

    摘要： Disclosed are compounds of formula I ##STR1## wherein R.sub.1 is a hydrogen atom, a C.sub.1 -C.sub.6 alkyl group, benzyl or an indolyl carbonyl group, R.sub.2 is a saturated or unsaturated 5- or 8-membered heterocyclic group containing as a hetero atom one or more nitrogen atoms, the heterocyclic group is optionally substituted at an N or C atom by a C.sub.1 -C.sub.6 alkyl or aralkyl group, n is an integer of 1 to 5 and one or more hydrogen atoms, in an alkylene chain --(CH.sub.2).sub.n -- are optionally substituted by a C.sub.1 -C.sub.6 alkyl, phenyl and/or hydroxyl group, physiologically acceptable salts and quaternary ammonium salts thereof. The compounds are selective antagonists of 5-HT.sub.3 receptors and are useful in the treatment of psychotic disorders, neurotic diseases, gastric stasis symptoms, gastrointestinal disorders, nausea and vomiting.