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1. 发明授权

US5166397A Process for producing optically active cyclobutylamines 失效
标题翻译：光学活性环丁胺的制备方法
公开(公告)号：US5166397A
公开(公告)日：1992-11-24
申请号：US757312
申请日：1991-09-10
申请人： Kazuhisa Narita , Masashi Nagai , Hideo Sugimura , Yukihiro Sagawa , Akira Shiozawa
发明人： Kazuhisa Narita , Masashi Nagai , Hideo Sugimura , Yukihiro Sagawa , Akira Shiozawa
IPC分类号： C07C213/10 , C07C215/42 , C07D473/00
CPC分类号： C07D473/00 , C07C213/10 , C07C215/42 , C07C2101/04 , Y02P20/55
摘要： This invention relates to a process for producing an optically active cyclobutylamine which comprises reacting a racemic modification of cyclobuthylamine represented by the following general formula [I]: ##STR1## wherein R.sup.1 and R.sup.2 represent each a hydrogen atom or a protecting group; with an optically active N-acylphenylglycine to thereby give two corresponding diastereomeric salts, crystallizing the more difficultly soluble diastereomeric salt and isolating the corresponding optically active cyclobutylamine from the diastereomeric salt thus crystallized. The optically active substances of the compound of the above general formula [I] are useful as, for example, an intermediate in the synthesis of 9-[(1R, 2R, 3S)-2,3-bis(hydroxymethyl)-1-cyclobutyl]guanine which is expected as an antiviral agent.
摘要翻译：本发明涉及一种光学活性环丁胺的制备方法，其包括使由以下通式[I]表示的环丁胺的外消旋体：其中R 1和R 2各自表示氢原子或保护基; 与光学活性的N-酰基苯基甘氨酸反应，从而得到两个相应的非对映异构体盐，使难溶于水的非对映异构体盐结晶，并从如此结晶的非对映体盐中分离相应的光学活性环丁基胺。上述通式[I]的化合物的光学活性物质可用作例如合成9 - [（1R，2R，3S）-2,3-双（羟甲基）-1- 环丁基]鸟嘌呤，其被预期作为抗病毒剂。

2. 发明授权

US06384063B1 Compound having effect of promoting neuron differentiation 失效
标题翻译：具有促进神经元分化作用的化合物
公开(公告)号：US06384063B1
公开(公告)日：2002-05-07
申请号：US09463354
申请日：2000-03-31
申请人： Seiichi Saito , Masashi Nagai , Tomio Morino , Tsugio Tomiyoshi , Takaaki Nishikiori , Atsushi Kuwahara , Takamichi Sato , Takashi Harada
发明人： Seiichi Saito , Masashi Nagai , Tomio Morino , Tsugio Tomiyoshi , Takaaki Nishikiori , Atsushi Kuwahara , Takamichi Sato , Takashi Harada
IPC分类号： A61K3144
CPC分类号： C07D295/185 , C07C229/04 , C07C229/34 , C07C323/41 , C07C323/60 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07D205/04 , C07D207/16 , C07D213/32 , C07D213/50 , C07D213/55 , C07D295/145 , C07D295/155 , C07D295/192 , C07D307/54
摘要： A novel cystacycline derivative which has an excellent effect of promoting the differentiation of neurons and is useful as a remedy for central nervous system disorders, a remedy for peripheral nerve disorders, etc.
摘要翻译：一种新颖的胱天蛋白衍生物，其具有促进神经元分化的优异效果，并且可用作中枢神经系统疾病的补救剂，对于周围神经障碍的治疗等。

3. 发明授权

US4214704A Reciprocator 失效
标题翻译：往复者
公开(公告)号：US4214704A
公开(公告)日：1980-07-29
申请号：US903959
申请日：1978-05-08
申请人： Masashi Nagai
发明人： Masashi Nagai
IPC分类号： B21C1/00 , B05B13/04 , B05B15/08 , B05B15/10 , B21J3/00 , B22C23/02 , B22D17/20 , B05B3/18 , F16N25/00
CPC分类号： B05B15/08 , B22D17/2007
摘要： Apparatus for moving a reciprocating fluid-emission head automatically through successive, variable-speed, variable-function operating cycles that include linear extension and retraction to and from a space within which predetermined operations are to be sequentially performed. The apparatus has an elongated fixed frame, an intermediate carriage on the frame and a head carriage on the intermediate carriage, the head carriage being adapted to support the fluid emission head. The carriages are moved simultaneously between a retracted position coextensive with the frame and an extended position by chain and sprocket drive, the maximum extension of the fluid emission head being about twice the length of the frame due to the double extension achieved by extending both carriages simultaneously. A plurality of fluids to be sprayed (including, e.g. liquid lubricant) are transmitted from a manifold block on the fixed frame to the reciprocating emission head by a plurality of inflexible, extensible fluid conduits. The operation of the apparatus is controlled by means of pulses generated in response to motion of the chain and sprocket drive for the carriages and by a pulse counter adapted to count the pulses being generated and to count a plurality of preset position representative totals.
摘要翻译：用于通过连续，可变速度的可变功能操作循环自动移动往复式流体排放头的装置，其包括到要从其中顺序执行预定操作的空间的线性延伸和缩回。该装置具有细长的固定框架，框架上的中间托架和中间托架上的头托架，头托架适于支撑流体排放头。托架同时在与框架延伸的缩回位置和通过链条和链轮驱动器延伸的位置之间移动，由于通过同时延伸两个托架实现的双重延伸，流体排放头的最大延伸大约是框架长度的两倍。要喷射的多种流体（包括例如液体润滑剂）通过多个不弯曲的可延展流体导管从固定框架上的歧管块传递到往复式排放头。该装置的操作是通过响应于链条和用于支架的链轮驱动器的运动而产生的脉冲和通过脉冲计数器来控制的，所述脉冲计数器适于对所产生的脉冲进行计数并计数多个预设位置代表总数。

4. 发明授权

US07348318B2 α-Amino-N-(diaminophosphinyl)lactam derivatives 失效
标题翻译： α-氨基-N-（二氨基氧膦基）内酰胺衍生物
公开(公告)号：US07348318B2
公开(公告)日：2008-03-25
申请号：US10508573
申请日：2003-03-24
申请人： Masatoshi Abe , Masashi Nagai , Keiichirou Yamamoto , Chihiro Nishimura
发明人： Masatoshi Abe , Masashi Nagai , Keiichirou Yamamoto , Chihiro Nishimura
IPC分类号： A61K31/675 , A61K31/45 , C07D211/92 , C07F9/06
CPC分类号： A61K31/675 , C07F9/5532 , C07F9/568 , C07F9/572 , C07F9/59
摘要： There are disclosed a novel α-amino-N-(diaminophosphinyl)lactam derivative represented by general formula (1): wherein, for example, A is a hydrogen atom or a substituent such as a lower alkyl group or the like; W, X, Y and Z are independently a hydrogen atom or a substituent such as a lower alkyl group, aryl group, arylacyl group, arylaminocarbonyl group or the like; and Q is —(CH2)n— wherein n is 0 to 3, or its salt, and a therapeutic agent and a prophylactic agent for myelosuppression, a therapeutic agent for infectious diseases, an agent for increasing the number of leukocytes and a dipeptidyl peptidase IV inhibitor which comprise the above-mentioned derivative or salt thereof as an active ingredient.
摘要翻译：公开了通式（1）表示的新型α-氨基-N-（二氨基膦氧基）内酰胺衍生物：其中，例如，A为氢原子或低级烷基等取代基; W，X，Y和Z独立地为氢原子或低级烷基，芳基，芳基酰基，芳基氨基羰基等取代基。和Q为 - （CH 2）n - n - 其中n为0至3，或其盐，治疗剂和骨髓抑制预防剂，治疗剂感染性疾病，增加白细胞数量的药剂和包含上述衍生物或其盐作为活性成分的二肽基肽酶IV抑制剂。

5. 发明授权

US4760961A Modular sprayhead assembly 失效
标题翻译：模块化喷头总成
公开(公告)号：US4760961A
公开(公告)日：1988-08-02
申请号：US14832
申请日：1987-02-13
申请人： Masashi Nagai
发明人： Masashi Nagai
IPC分类号： B05B1/30 , B05B7/12 , B05B13/02 , B22D17/20 , B05B1/20
CPC分类号： B05B13/0278 , B05B7/1272 , B22D17/2007 , B05B1/306 , Y10S239/01
摘要： A modular spraying assembly particularly adapted for use with automatic molding or dye casting machines which is characterized by a plurality of identical sprayhead modules which can be mounted in linear relationship to one another to form variable vertical and horizontal columns accomodating the particular design of a mold or dye which may be sprayed. A support hanger and manifold blocks are provided to communicate a source of air pressure and liquid mold release compound or lubricant to each linear column of spray head modules. Each sprayhead module is mounted in communication with the sprayhead modules forming a given linear column via a plurality of parallel bores which form air and liquid supply passages common to all sprayheads in the linear column and through which tie rods extend to provide a convenient connecting means for any given number of sprayhead modules in the linear array.
摘要翻译：特别适用于自动模制或染色铸造机的模块化喷涂组件，其特征在于具有多个相同的喷头模块，其可以彼此成线性关系安装，以形成可变的垂直和水平柱，以适应模具的特定设计或可喷涂的染料。提供支撑悬挂器和歧管块以将气压源和液体脱模剂或润滑剂传送到喷雾头模块的每个直线柱。每个喷头模块安装成与喷头组件连通，所述喷头组件通过多个平行孔形成给定的直线柱，所述多个平行孔形成通向所述线性柱中的所有喷头的空气和液体供应通道，并且所述拉杆延伸通过所述连接装置提供方便的连接装置线性阵列中任意数量的喷头组件。

6. 发明授权

US4795124A Extractor apparatus for removing articles from article forming machines 失效
标题翻译：用于从制品成型机中去除物品的抽出装置
公开(公告)号：US4795124A
公开(公告)日：1989-01-03
申请号：US908792
申请日：1986-09-18
申请人： Masashi Nagai
发明人： Masashi Nagai
IPC分类号： B29C37/00 , B29C45/42 , B29C39/36 , B29C43/50
CPC分类号： B29C45/42 , B29C37/0007
摘要： An article extracting means which is mounted on a carriage means which in turn is slidably mounted on the side of an article forming machine having two members movable relative to one another to form an article between them. A pivoted extractor arm in mounted on the carriage means to pivot in a vertical plane toward and away from the forming machine. An upper portion of the extractor arm carries an independently pivoted arm which may move in the same vertical plane as the extractor arm between at least two 180 degree opposed positions related to positioning gripping members carried thereby between an article gripping and an article release positions. The gripping members feature a construction wherein opposing jaw members are moved in a parallel direction toward and away from one another. One jaw member is actuated in a linear direction which via a rack and pinion arrangement cause the other jaw to move in parallel, but opposing direction. A quick manual release connection is also provided to permit the carriage means carrying the extractor arm to a position providing unobstructed and safe access to the casting die or mold for maintenance personnel.
摘要翻译：一种物品提取装置，其安装在托架装置上，托架装置依次可滑动地安装在具有可相对于彼此移动的两个构件的物品成型机的侧面上，以在它们之间形成物品。枢转抽出臂安装在滑架装置上，以便在垂直平面中朝向和远离成型机转动。提取器臂的上部承载独立的枢转臂，该臂独立地枢转臂，该臂可以在提取器臂在与定位夹持构件相关联的至少两个180度相对位置之间在相同的垂直平面内移动，定位夹持构件由物品夹持和物品释放位置之间承载。夹持构件具有这样的结构，其中相对的夹爪构件沿彼此平行的方向并且彼此远离地移动。一个钳口构件在线性方向上致动，通过齿条和小齿轮装置使得另一个钳口平行移动但是相反的方向。还提供了快速的手动释放连接，以允许将提取臂支撑在一个提供维护人员的铸模或模具的通畅且安全的位置的托架装置。

7. 发明授权

US07531657B2 Method for preparing sulphostin and analogue thereof or preparation intermediate thereof 失效
标题翻译：磺普钠及其类似物的制备方法或其制备方法
公开(公告)号：US07531657B2
公开(公告)日：2009-05-12
申请号：US10498272
申请日：2002-12-16
申请人： Masashi Nagai , Hiroko Yamazaki , Keiichirou Yamamoto , Masatoshi Abe
发明人： Masashi Nagai , Hiroko Yamazaki , Keiichirou Yamamoto , Masatoshi Abe
IPC分类号： C07F9/00 , C07F9/02 , C07D205/08 , C07D223/12
CPC分类号： C07C215/30 , C07B2200/07 , C07F9/5532 , C07F9/568 , C07F9/572 , C07F9/59 , Y02P20/55
摘要： A method for preparing a compound represented by the following general formula (5) where, n is an integer of 0 to 3; and Y represents a protecting group for an amino group, the method including the steps of reacting a compound represented by the following general formula (3) where n and Y are as described above, with a silylating agent, and subsequently reacting it with P (═O) T3, where T represents a halogen atom, and further with ammonia. A method for preparing an optically active intermediate of sulphostin or an analogue thereof, which is an optically active amine salt of an optically active compound represented by the following general formula (8) where n is integer of 0 to 3; Y represents protecting group for the amino group; and each configuration at C* and P* may be the same or different and indicates S or R, the method including reacting a compound represented by the following general formula (7) where n and Y are as described above; and the configuration of C* indicates either of S or R, with an optically active amine, and resolving the formed diastereomeric salt by fractional crystallization.
摘要翻译：一种制备由以下通式（5）表示的化合物的方法，其中n为0-3的整数; Y表示氨基的保护基，该方法包括使下述通式（3）表示的化合物（其中n和Y如上所述）与甲硅烷基化剂反应，然后使其与P（ -O）T3，其中T表示卤素原子，并且还含有氨。一种制备光学活性中间体磺酸钠或其类似物的方法，它是由以下通式（8）表示的光学活性化合物的光学活性胺盐，其中n为0-3的整数; Y表示氨基的保护基; 并且C *和P *的每个构型可以相同或不同，表示S或R，该方法包括使由以下通式（7）表示的化合物，其中n和Y如上所述; 并且C *的构型表示S或R中的任一个与光学活性胺，并且通过分级结晶拆分形成的非对映体盐。

8. 发明申请

US20050164989A1 Novel $g(a)-amino-n-(diaminophosphinyl) lactam derivative 失效
标题翻译：新型$ g（a） - 氨基 - （（二氨基氧膦基））内酰胺衍生物
公开(公告)号：US20050164989A1
公开(公告)日：2005-07-28
申请号：US10508573
申请日：2003-03-24
申请人： Masatoshi Abe , Masashi Nagai , Keiichirou Yamamoto , Chihiro Nishimura
发明人： Masatoshi Abe , Masashi Nagai , Keiichirou Yamamoto , Chihiro Nishimura
IPC分类号： A61K31/675 , A61P3/10 , A61P5/00 , A61P7/00 , A61P7/06 , A61P29/00 , A61P31/00 , A61P31/18 , A61P37/02 , A61P37/08 , A61P43/00 , C07F9/553 , C07F9/568 , C07F9/572 , C07F9/59
CPC分类号： A61K31/675 , C07F9/5532 , C07F9/568 , C07F9/572 , C07F9/59
摘要： There are disclosed a novel α-amino-N-(diaminophosphinyl)lactam derivative represented by general formula (1): wherein, for example, A is a hydrogen atom or a substituent such as a lower alkyl group or the like; W, X, Y and Z are independently a hydrogen atom or a substituent such as a lower alkyl group, aryl group, arylacyl group, arylaminocarbonyl group or the like; and Q is —(CH2)n— wherein n is 0 to 3, or its salt, and a therapeutic agent and a prophylactic agent for myelosuppression, a therapeutic agent for infectious diseases, an agent for increasing the number of leukocytes and a dipeptidyl peptidase IV inhibitor which comprise the above-mentioned derivative or salt thereof as an active ingredient.
摘要翻译：公开了通式（1）表示的新型α-氨基-N-（二氨基膦氧基）内酰胺衍生物：其中，例如，A为氢原子或低级烷基等取代基; W，X，Y和Z独立地为氢原子或低级烷基，芳基，芳基酰基，芳基氨基羰基等取代基。和Q为 - （CH 2）n - n - 其中n为0至3，或其盐，治疗剂和骨髓抑制预防剂，治疗剂感染性疾病，增加白细胞数量的药剂和包含上述衍生物或其盐作为活性成分的二肽基肽酶IV抑制剂。

9. 发明申请

US20050020834A1 Method for preparation of sulphostin and its analogue or intermediates thereof 失效
标题翻译：磺普钠及其类似物或其中间体的制备方法
公开(公告)号：US20050020834A1
公开(公告)日：2005-01-27
申请号：US10498272
申请日：2002-12-16
申请人： Masashi Nagai , Hiroko Yamazaki , Keichirou Yamamoto , Masatoshi Abe
发明人： Masashi Nagai , Hiroko Yamazaki , Keichirou Yamamoto , Masatoshi Abe
IPC分类号： C07C215/30 , C07F9/553 , C07F9/568 , C07F9/572 , C07F9/59 , C07F9/547
CPC分类号： C07C215/30 , C07B2200/07 , C07F9/5532 , C07F9/568 , C07F9/572 , C07F9/59 , Y02P20/55
摘要： A method for preparing a compound represented by the following general formula (5) where, n is an integer of 0 to 3; and Y represents a protecting group for an amino group, the method including the steps of reacting a compound represented by the following general formula (3) where n and Y are as described above, with a silylating agent, and subsequently reacting it with P (═O) T3, where T represents a halogen atom, and further with ammonia. A method for preparing an optically active intermediate of sulphostin or an analogue thereof, which is an optically active amine salt of an optically active compound represented by the following general formula (8) where n is an integer of 0 to 3; Y represents a protecting group for the amino group; and each configuration at C* and P* may be the same or different and indicates S or R, the method including reacting a compound represented by the following general formula (7) where n and Y are as described above; and the configuration of C* indicates either of S or R, with an optically active amine, and resolving the formed diastereomeric salt by fractional crystallization.
摘要翻译：一种制备由以下通式（5）表示的化合物的方法，其中n为0-3的整数; Y表示氨基的保护基，该方法包括使下述通式（3）表示的化合物（其中n和Y如上所述）与甲硅烷基化剂反应，然后使其与P（ = O）T3，其中T表示卤素原子，并且还含有氨。一种制备磺普钠或其类似物的光学活性中间体的方法，其为由以下通式（8）表示的光学活性化合物的光学活性胺盐，其中n为0-3的整数; Y表示氨基的保护基; 并且C *和P *的每个构型可以相同或不同，表示S或R，该方法包括使由以下通式（7）表示的化合物，其中n和Y如上所述; 并且C *的构型表示S或R中的任一个与光学活性胺，并且通过分级结晶拆分形成的非对映体盐。

10. 发明授权

US06433174B1 Process for producing novel naphthyridine derivatives 失效
标题翻译：制备新型萘啶衍生物的方法
公开(公告)号：US06433174B1
公开(公告)日：2002-08-13
申请号：US09831860
申请日：2001-05-15
申请人： Yoshitaka Satoh , Makoto Tsuda , Masashi Nagai , Hiroko Yamazaki
发明人： Yoshitaka Satoh , Makoto Tsuda , Masashi Nagai , Hiroko Yamazaki
IPC分类号： C07D47104
CPC分类号： C07D471/04 , C07B2200/07 , C07C67/343 , C07C67/60 , C07C69/65
摘要： A novel naphthyridine derivative showing high activity as a tachykinin receptor antagonist can be produced at high efficiency by reacting an acylating agent such as a carboxylic acid derivative with a compound represented by the formula (1): wherein R1, R2 and R3 represent independently a hydrogen atom, a lower alkyl group, a lower alkoxyl group, an aryl group, a heteroaryl group, an amino group, etc., and X1 and X2 represent respectively a halogen atom.
摘要翻译：通过使酰化剂如羧酸衍生物与式（1）表示的化合物反应，可以高效率地制备显示高活性作为速激肽受体拮抗剂的新型萘啶衍生物：其中R1，R2和R3独立地表示氢原子，低级烷基，低级烷氧基，芳基，杂芳基，氨基等，X1和X2分别表示卤素原子。

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