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1. 发明授权

US06252041B1 Depsipeptides containing non-natural amino acids 失效
标题翻译：含有非天然氨基酸的脱脂肽
公开(公告)号：US06252041B1
公开(公告)日：2001-06-26
申请号：US09235479
申请日：1999-01-22
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： C07K508
CPC分类号： C07K5/06043 , A61K38/00 , C07C237/10 , C07K5/06052 , C07K5/101 , Y02P20/55
摘要： A depsipeptide containing a non-natural amino acid(s) having the formula (1) wherein R1 represents a C5-C20 alkyl group and others; R2 represents —O—CO—CH(R5)—X—CH(R6)—NH— (wherein X represents N(R7)—CO, CH2—CO, CH2—CH2 and others, R5, R6, and R7 represent a hydrogen atom or a C1-C6 alkyl group); R3 represents and wherein the remaining substituent variables are as defined herein. The above depsipeptides have a promoting activity on the production of apolipoprotein E, and are useful as a therapeutic agent for neurologic damages, especially dementia, and hyperlipemia.
摘要翻译：含有具有式（1）的非天然氨基酸的前肽，其中R1表示C5-C20烷基等; R2表示-O-CO-CH（R5）-X-CH（R6）-NH-（其中X表示N（R7）-CO，CH2-CO，CH2-CH2等，R5，R6和R7表示氢原子或C1-C6烷基）; R3代表并且其中剩余的取代基变量如本文所定义。上述脱肽对载脂蛋白E的产生具有促进活性，并且可用作神经损伤，特别是痴呆和高脂血症的治疗剂。

2. 发明授权

US06222050B1 Optically active 1,4-benzodioxine-2-carboxylic acid derivatives and process for producing the same 失效
标题翻译：光活性1,4-苯并二恶英-2-羧酸衍生物及其制备方法
公开(公告)号：US06222050B1
公开(公告)日：2001-04-24
申请号：US09509200
申请日：2000-03-23
申请人： Koji Kawamura , Masahiro Ueno , Masashi Suzuki , Makoto Yanai , Toshihiro Takahashi , Koichi Itoh
发明人： Koji Kawamura , Masahiro Ueno , Masashi Suzuki , Makoto Yanai , Toshihiro Takahashi , Koichi Itoh
IPC分类号： C07D31920
CPC分类号： C07D319/20 , C12P17/06 , C12P41/004
摘要： Disclosed are optically active alcohols having formula (1) and (2) wherein R is (R)-1-phenylethylamino or (S)-1-phenylethylamino. The active alcohols can be prepared by acylating a racemate of formula (3) in the presence of a hydrolase, followed by alcoholysis or hydrolysis. R in formula (3) is the same as that defined for formula (1) and (2).
摘要翻译：公开了具有式（1）和（2）的光学活性醇，其中R是（R）-1-苯乙基氨基或（S）-1-苯乙基氨基。活性醇可以通过在水解酶的存在下酰化式（3）的外消旋化物，然后进行醇解或水解来制备。式（3）中的R与式（1）和（2）所定义的相同。

3. 发明授权

US5256656A Azabicyclo derivatives 失效
标题翻译：氮杂双环衍生物
公开(公告)号：US5256656A
公开(公告)日：1993-10-26
申请号：US853521
申请日：1992-05-12
申请人： Haruhiko Kikuchi , Hiroaki Satoh , Nobuhiro Yahata , Kiochiro Hagihara , Toru Hayakawa , Setsuko Mino , Makoto Yanai
发明人： Haruhiko Kikuchi , Hiroaki Satoh , Nobuhiro Yahata , Kiochiro Hagihara , Toru Hayakawa , Setsuko Mino , Makoto Yanai
IPC分类号： C07D471/08 , C07D498/08 , C07D513/08 , A61K31/54 , A61K31/535 , C07D265/36 , C07D498/02
CPC分类号： C07D471/08 , C07D513/08
摘要： Azabicyclo derivatives of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein A is a group of formula (a), (b) or (c): ##STR2## wherein R.sub.1 is hydrogen, C.sub.1 -C.sub.10 alkyl, aralkyl or di(C.sub.1 -C.sub.4) alkylamino(C.sub.1 -C.sub.6)alkyl;R.sub.2, R.sub.3 and R.sub.4 may be the same or different and each is hydrogen, amino, halogen, C.sub.1 -C.sub.4 alkoxy or phthalimide;X is O or NH;R is C.sub.1 -C.sub.4 alkyl; andY is NR, O or S;having 5-HT.sub.3 receptor antagonist activity.
摘要翻译：（I）的叠氮杂双环衍生物及其药学上可接受的盐：其中A是式（a），（b）或（c）的基团：（a）（c）其中R1是氢，C1-C10烷基，芳烷基或二（C1-C4）烷基氨基（C1-C6）烷基; R2，R3和R4可以相同或不同，各自为氢，氨基，卤素，C1-C4烷氧基或邻苯二甲酰亚胺; X是O或NH; R是C 1 -C 4烷基; Y为NR，O或S; 具有5-HT 3受体拮抗剂活性。

4. 发明授权

US5124324A Indole derivatives 失效
标题翻译： 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.

5. 发明授权

US06858585B1 Cyclic depsipeptides and drugs containing the same as the active ingredient 失效
标题翻译：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。

6. 发明授权

US06211145B1 Bicyclic depsipeptides 失效
标题翻译：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。

7. 发明授权

US4982210A Flash device 失效
标题翻译：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。

8. 发明授权

US07022732B2 Propanolamine derivative having 1, 4-benzodioxane ring 失效
标题翻译：具有1,4-苯并二恶烷环的丙醇胺衍生物
公开(公告)号：US07022732B2
公开(公告)日：2006-04-04
申请号：US10489332
申请日：2001-09-13
申请人： Masahiro Ueno , Koji Kawamura , Makoto Yanai , Toshihiro Takahashi , Nobuhiro Kinoshita , Koichi Katsuyama , Satoko Fuchizawa , Shigeru Hiramoto
发明人： Masahiro Ueno , Koji Kawamura , Makoto Yanai , Toshihiro Takahashi , Nobuhiro Kinoshita , Koichi Katsuyama , Satoko Fuchizawa , Shigeru Hiramoto
IPC分类号： A61K31/36 , C07D319/20
CPC分类号： C07D405/12 , A61K31/357 , A61K31/404 , A61K31/4433 , A61K31/506 , C07D319/20
摘要： This invention relates to a medicament containing as an active ingredient, a novel propanolamine having a 1,4-benzodioxane ring or a pharmaceutically acceptable salt thereof: The present compound is represented by the above formula wherein R1-3 may be the same or different and each represents a hydrogen atom, a halogen atom, a hydroxy group, a (C1–C6)alkyl group, a (C1–C6)alkoxy group, a (C1–C6)alkylsulfonamido group, or a phenyl group; R4-5 each represents a hydrogen atom or a (C1–C6)alkyl group; and A represents any of a benzene ring, a pyridine ring and a pyrimidine ring.This compound is useful as a prophylactic or therapeutic agent for diabetes, obesity, hyperlipemia, depression, a respiratory disease, or a gastrointestinal disease.
摘要翻译：本发明涉及含有作为活性成分的具有1,4-苯并二恶烷环的新型丙醇胺或其药学上可接受的盐的药物：本发明化合物由上式表示，其中R 1〜3 3 可以相同或不同，各自表示氢原子，卤素原子，羟基，（C 1 -C 6）烷基，（C 1 -C 6 -C 6）烷基，（C 1 -C 6 -C 6烷基磺酰氨基）或苯基（C 1 -C 6）组; R 4-5各自表示氢原子或（C 1 -C 6 -C 6）烷基; A表示苯环，吡啶环和嘧啶环中的任一个。该化合物可用作糖尿病，肥胖症，高脂血症，抑郁症，呼吸系统疾病或胃肠道疾病的预防或治疗剂。

9. 外观设计

USD513026S1 Binoculars 失效
公开(公告)号：USD513026S1
公开(公告)日：2005-12-20
申请号：US29200457
申请日：2004-03-01
申请人： Makoto Yanai , Takashi Kishigami , Eiji Takenaka , Nobuo Hashimoto
设计人： Makoto Yanai , Takashi Kishigami , Eiji Takenaka , Nobuo Hashimoto

10. 发明授权

US06329533B2 Optically active 1,4-benzodioxin-2-carboxylic acid derivatives and process for producing the same 失效
标题翻译：光活性1,4-苯并二恶英-2-羧酸衍生物及其制备方法
公开(公告)号：US06329533B2
公开(公告)日：2001-12-11
申请号：US09765424
申请日：2001-01-22
申请人： Koji Kawamura , Masahiro Ueno , Masashi Suzuki , Makoto Yanai , Toshihiro Takahashi , Koichi Itoh
发明人： Koji Kawamura , Masahiro Ueno , Masashi Suzuki , Makoto Yanai , Toshihiro Takahashi , Koichi Itoh
IPC分类号： C07D31920
CPC分类号： C07D319/20 , C12P17/06 , C12P41/004
摘要： Disclosed are optically active alcohols having formula (1) and (2) wherein R is (R)-1-phenylethylamino or (S)-1-phenylethylamino
摘要翻译：公开了具有式（1）和（2）的光学活性醇，其中R是（R）-1-苯基乙基氨基或（S）-1-苯乙基氨基

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