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1. 发明授权

US06133443A Optically active 1,4-dihydropyridine derivatives and process for the preparation thereof 失效
标题翻译：光学活性的1,4-二氢吡啶衍生物及其制备方法
公开(公告)号：US06133443A
公开(公告)日：2000-10-17
申请号：US125608
申请日：1998-08-21
申请人： Takashi Nakashima , Kunio Isshiki , Noriaki Sakata , Naoki Agata , Takeo Yoshioka
发明人： Takashi Nakashima , Kunio Isshiki , Noriaki Sakata , Naoki Agata , Takeo Yoshioka
IPC分类号： C07D211/90 , C07D401/12 , C07D417/12 , C07D521/00 , C07D251/00 , C07D213/79 , C07D401/00 , C07D403/00 , C07D417/00
CPC分类号： C07D231/12 , C07D211/90 , C07D233/56 , C07D249/08 , C07D401/12 , C07D417/12
摘要： Optically active 1,4-dihydropyridine derivatives represented by general formula (I) and anion salts thereof and a production method therefor: ##STR1## (wherein R.sup.1 represents a C.sub.1-6 alkyl group, R.sup.2 represents a nitrogen-containing heterocyclic group forming a quaternary ammonium which may be substituted, and n is an integer of 1, 2 or 3). The optically active 1,4-dihydropyridine derivatives represented by general formula (I) have vasodilating activity and hypotensive activity and are excellent in water solubility so that they are useful as a drug for circulatory system such as a hypotensor or vasodilator.
摘要翻译： PCT No.PCT / JP96 / 03414 Sec。 371日期1998年8月21日 102（e）1998年8月21日PCT PCT 1996年11月21日PCT公布。公开号WO97 / 30987 日本8月28日，通式（I）表示的光学活性的1,4-二氢吡啶衍生物及其阴离子盐及其制造方法：其中，R1表示C1-6烷基，R2表示含氮杂环基，可以被取代的季铵，n是1,2或3的整数）。由通式（I）表示的光学活性的1,4-二氢吡啶衍生物具有血管扩张活性和降血压活性，并且水溶性优异，因此它们可用作循环系统如低血压或血管扩张剂的药物。

2. 发明授权

US5395941A Optically active 1,4-hydropyridine compounds 失效
标题翻译：光学活性的1,4-二氢吡啶化合物
公开(公告)号：US5395941A
公开(公告)日：1995-03-07
申请号：US216216
申请日：1994-03-22
申请人： Kunio Isshiki , Takashi Nakashima , Hiroshi Tanaka , Takeo Yoshioka
发明人： Kunio Isshiki , Takashi Nakashima , Hiroshi Tanaka , Takeo Yoshioka
IPC分类号： A61K31/455 , A61K31/443 , A61K31/4439 , A61K31/444 , A61P9/08 , A61P9/12 , A61P43/00 , C07B53/00 , C07D211/90 , C07D405/12 , C07D405/02
CPC分类号： C07D405/12 , C07D211/90 , Y02P20/55
摘要： Optically active 1,4-dihydropyridine derivatives represented by general formula (I), process for preparing compounds (Ic) (in general formula (I) , R.sup.1 is a lower alkyl group), process for preparing compounds represented by general formula (II) by hydrolyzing the compounds (Ic) under acidic conditions, process for preparing compounds represented by general formula (II) by solvolysis, under basic conditions, of compounds represented by general formula (III); ##STR1## wherein R.sup.1 is H, a lower alkyl group, a cyanoethyl group, a lower alkanoylaminoethyl group, or a lower dialkylaminoethyl group; R.sup.2 is a 2-tetrahydropyranyl group or a lower alkyloxymethyl group; R.sup.3 is a cyano group, a lower dialkylamino group or a lower alkanoylamino group; and R.sup.4 is a lower alkyl group. The compounds of general formula (I) and (II) are intermediate compounds for preparing optically active 1,4-dihydropyridine derivatives which are useful as medicines for circulatory organs. The compounds can be produced efficiently by the process of the present invention.
摘要翻译：通式（I）表示的光学活性的1,4-二氢吡啶衍生物，化合物（Ic）的制备方法（通式（I）中，R 1为低级烷基），由通式（II）表示的化合物的制备方法，通过在酸性条件下水解化合物（Ic），通过在碱性条件下通过通式（III）表示的化合物的溶剂分解来制备由通式（II）表示的化合物的方法; （II）其中R1是H，低级烷基，氰基乙基，低级烷酰基氨基乙基或低级二烷基氨基乙基; R2是2-四氢吡喃基或低级烷氧基甲基; R3是氰基，低级二烷基氨基或低级烷酰氨基; R4为低级烷基。通式（I）和（II）的化合物是制备用作循环器官药物的光学活性1,4-二氢吡啶衍生物的中间体化合物。可以通过本发明的方法有效地制备化合物。

3. 发明授权

US06361987B1 Gene encoding a protein having asymmetric hydrolase activity for 4-substituted 1,4-dihydropyridine derivatives and its expression product 失效
标题翻译：编码具有4-取代的1,4-二氢吡啶衍生物及其表达产物的不对称水解酶活性的蛋白质的基因
公开(公告)号：US06361987B1
公开(公告)日：2002-03-26
申请号：US09514340
申请日：2000-02-28
申请人： Akira Arisawa , Motoko Matsufuji , Takurou Tsuruta , Kazuyuki Dobashi , Takashi Nakashima , Kunio Isshiki , Takeo Yoshioka
发明人： Akira Arisawa , Motoko Matsufuji , Takurou Tsuruta , Kazuyuki Dobashi , Takashi Nakashima , Kunio Isshiki , Takeo Yoshioka
IPC分类号： C12N914
CPC分类号： C07D211/88 , C07D211/90 , C12N9/18 , C12N9/78 , C12P17/12 , C12P41/006
摘要： This invention provides DNA fragments for efficiently preparing a protein having asymmetric hydrolase activity for 4-substituted 1,4-dihydropyridine derivatives, transformants obtained by using such a DNA fragment, and a process for preparing the aforesaid enzyme. Specifically, an isolated gene derived from the chromosome of Streptomyces viridosporus and encoding a protein having asymmetric hydrolase activity for 4-substituted 1,4-dihydropyridine derivatives, plasmids having the aforesaid gene integrated thereinto, transformants obtained by using such a plasmid, and a process for preparing the aforesaid enzyme by using such a transformant are disclosed. A process for the enzymatic conversion of 4-substituted 1,4-dihydropyridine derivatives by using the aforesaid enzyme is also disclosed.
摘要翻译：本发明提供了用于有效制备对4-取代的1,4-二氢吡啶衍生物具有不对称水解酶活性的蛋白质的DNA片段，以及通过使用这样的DNA片段得到的转化体及其制备方法。具体来说，来源于链球菌链球菌的染色体的分离的基因，编码对4-取代的1,4-二氢吡啶衍生物具有不对称的水解酶活性的蛋白质，将上述基因整合到其中的质粒，使用这样的质粒获得的转化体，公开了通过使用这种转化体制备上述酶的方法。还公开了通过使用上述酶酶促转化4-取代的1,4-二氢吡啶衍生物的方法。

4. 发明授权

US6143541A Gene encoding a protein having symmetric hydrolase activity for 4-substituted 1,4-dihydropyridine derivatives and its expression product 失效
标题翻译：编码具有4-取代的1,4-二氢吡啶衍生物的对称水解酶活性的蛋白质的基因及其表达产物
公开(公告)号：US6143541A
公开(公告)日：2000-11-07
申请号：US16
申请日：1998-01-30
申请人： Akira Arisawa , Motoko Matsufuji , Takurou Tsuruta , Kazuyuki Dobashi , Takashi Nakashima , Kunio Isshiki , Takeo Yoshioka
发明人： Akira Arisawa , Motoko Matsufuji , Takurou Tsuruta , Kazuyuki Dobashi , Takashi Nakashima , Kunio Isshiki , Takeo Yoshioka
IPC分类号： C07D211/88 , C07D211/90 , C12N9/18 , C12N9/78 , C12N15/55 , C12P17/12 , C12P41/00 , C12N9/14 , C12N1/20 , C12N9/16 , C12P12/12
CPC分类号： C07D211/88 , C07D211/90 , C12N9/18 , C12N9/78 , C12P17/12 , C12P41/006
摘要： This invention provides DNA fragments for efficiently preparing a protein having asymmetric hydrolase activity for 4-substituted 1,4-dihydropyridine derivatives, transformants obtained by using such a DNA fragment, and a process for preparing the aforesaid enzyme. Specifically, an isolated gene derived from the chromosome of Streptomyces viridosporus and encoding a protein having asymmetric hydrolase activity for 4-substituted 1,4-dihydropyridine derivatives, plasmids having the aforesaid gene integrated thereinto, transformants obtained by using such a plasmid, and a process for preparing the aforesaid enzyme by using such a transformant are disclosed. A process for the enzymatic conversion of 4-substituted 1,4-dihydropyridine derivatives by using the aforesaid enzyme is also disclosed.
摘要翻译： PCT No.PCT / JP96 / 02147 Sec。 371日期1998年1月30日 102（e）1998年1月30日PCT PCT 1996年7月30日PCT公布。公开号WO97 / 05243 日期1997年2月13日本发明提供了用于有效制备对4-取代的1,4-二氢吡啶衍生物具有不对称水解酶活性的蛋白质的DNA片段，以及通过使用该DNA片段得到的转化体及其制备方法。具体来说，来源于链球菌链球菌的染色体的分离的基因，编码对4-取代的1,4-二氢吡啶衍生物具有不对称的水解酶活性的蛋白质，将上述基因整合到其中的质粒，使用这样的质粒获得的转化体，公开了通过使用这种转化体制备上述酶的方法。还公开了通过使用上述酶酶促转化4-取代的1,4-二氢吡啶衍生物的方法。

5. 发明授权

US5760238A 1,4-dihydropyridine derivatives 失效
标题翻译： 1,4-二氢吡啶衍生物
公开(公告)号：US5760238A
公开(公告)日：1998-06-02
申请号：US793283
申请日：1997-02-25
申请人： Kunio Isshiki , Naoki Matsumoto , Takashi Nakashima , Kazuyuki Dobashi , Takurou Tsuruta , Takeo Yoshioka
发明人： Kunio Isshiki , Naoki Matsumoto , Takashi Nakashima , Kazuyuki Dobashi , Takurou Tsuruta , Takeo Yoshioka
IPC分类号： C07D211/90 , C07D401/12 , C07D401/14 , C12P17/12
CPC分类号： C07D401/12 , C07D211/90 , C07D401/14
摘要： Disclosed are 1,4-dihydropyridine derivatives represented by the general formula (I) and salts thereof, as well as optical active 1,4-dihydropyridine derivatives represented by the general formula (II) and salts thereof which are obtained from the derivative by biochemical reactions using microorganisms or enzymes and useful as preventive and therapeutic agents for ischemic heart diseases and hypertension. ##STR1## (wherein x and Y are H, NO.sub.2, CN, halogen; R.sup.1 and R.sup.2 are H, CHO, substituted alkylcarbonyl, crotonyl, cinnamoyl, alkoxycarbonyl, aryloxycarbonyl, benzyloxycarbonyl, carboxybenzoyl, or R.sup.1 and R.sup.2 taken together represent phthaloyl; n is an integer of 1 to 3).
摘要翻译： PCT No.PCT / JP95 / 01606 Sec。 371日期1997年2月25日 102（e）日期1997年2月25日PCT提交1995年8月11日PCT公布。公开号WO96 / 06829 日期：1996年3月7日公开了由通式（I）表示的1,4-二氢吡啶衍生物及其盐，以及由通式（II）表示的光学活性1,4-二氢吡啶衍生物及其盐，通过使用微生物或酶的生物化学反应从衍生物中获得，并且可用作缺血性心脏病和高血压的预防和治疗剂。（Ⅰ）（Ⅰ）（Ⅱ）（其中x和Y是H，NO2，CN，卤素; R1和R2是H，CHO，取代的烷基羰基，巴豆基，肉桂酰，烷氧羰基，芳氧羰基，苄氧基羰基，羧基苯甲酰基或 R1和R2一起代表邻苯二甲酰基; n是1至3的整数）。

6. 发明授权

US5635395A Optically active 1,4-dihydropyridine compounds and the microbial process for the stereoselection thereof 失效
标题翻译：光学活性的1,4-二氢吡啶化合物及其立体选择的微生物过程
公开(公告)号：US5635395A
公开(公告)日：1997-06-03
申请号：US387750
申请日：1995-02-21
申请人： Kunio Isshiki , Takashi Nakashima , Takeo Yoshioka , Hiroshi Tsunekawa , Takashi Adachi , Tomomi Ota
发明人： Kunio Isshiki , Takashi Nakashima , Takeo Yoshioka , Hiroshi Tsunekawa , Takashi Adachi , Tomomi Ota
IPC分类号： C07D211/90 , C12P17/12 , C12P41/00 , A01N43/40 , C07D213/803
CPC分类号： C07D211/90 , C12P17/12 , C12P41/005
摘要： (4R)-3-(Substituted aminoalkyl)oxycarbonyl-1,4-dihydro-2,6-dimethyl-4-(nitrophenyl)pyridine-5-carboxylic acids can be prepared efficiently, by reacting bis(substituted aminoalkyl) 1,4-dihydro-2,6-dimethyl-4-(nitrophenyl)pyridine-3,5-dicarboxylates with a microorganism capable of asymmetric hydrolysis and belonging to the genus Streptomyces, the genus Paecilomyces, the genus Botryodioplodia, the genus Alternaria or the genus Helminthosporium, or a treated product thereof. The compounds are extremely useful as important intermediates for preparation of pharmaceuticals useful for the prevention and treatment of angina pectoris, hypertension, etc.
摘要翻译： PCT No.PCT / JP93 / 01222 Sec。 371日期1995年2月21日 102（e）1995年2月21日PCT PCT 1993年8月31日PCT公布。公开号WO94 / 05637 日期：1994年3月17日（4R）-3-（取代氨基烷基）氧羰基-1,4-二氢-2,6-二甲基-4-（硝基苯基）吡啶-5-羧酸可以通过双取代的氨基烷基）1,4-二氢-2,6-二甲基-4-（硝基苯基）吡啶-3,5-二羧酸盐与能够不对称水解的微生物属于链霉菌属，拟青霉属，Botryodioplodia属，链格孢属或Helminthosporium属，或其处理产物。该化合物作为制备可用于预防和治疗心绞痛，高血压等的药物的重要中间体非常有用。

7. 发明授权

US06426420B1 Process for producing isocoumarines and intermediates for the same 失效
标题翻译：生产异香豆素及其中间体的方法
公开(公告)号：US06426420B1
公开(公告)日：2002-07-30
申请号：US09610362
申请日：2000-07-05
申请人： Toshio Tsuchida , Hazuki Nagai , Takashi Nakashima , Masashi Yoshida , Kaname Konuki , Asako Kuroda , Kunio Isshiki , Tomio Takeuchi
发明人： Toshio Tsuchida , Hazuki Nagai , Takashi Nakashima , Masashi Yoshida , Kaname Konuki , Asako Kuroda , Kunio Isshiki , Tomio Takeuchi
IPC分类号： C07D31176
CPC分类号： C07D311/76 , C07C67/31 , C07C67/343 , C07C67/46 , C07C69/92 , Y02P20/55 , C07C69/88
摘要： Provided is a process for producing an isocoumarin-3-yl-acetic acid derivative, characterized by reacting a homophthalic acid derivative represented by a formula: (wherein Rc, R2 and R are mainly protecting groups) with a malonic acid derivating represented by a formula: (wherein R is an organic group including a lower alkyl group; R3 is a protecting group for a carboxyl group; and X is a halogen atom or a —OM group (wherein M is alkaline metal or alkaline earth metal)). According to the above process, various isocoumarin-3-yl-acetic acid derivatives can efficiently be provided.
摘要翻译：提供了一种制备异香豆素-3-基 - 乙酸衍生物的方法，其特征在于使由式（其中Rc，R2和R主要是保护基团）表示的均苯二甲酸衍生物与由式（其中，R为低级烷基的有机基团，R3为羧基的保护基，X为卤原子或-OM基）（其中，M为碱金属或碱土金属）。根据上述方法，可以有效地提供各种异香豆素-3-基 - 乙酸衍生物。

8. 发明授权

US06548695B2 Process for producing isocoumarins and intermediates for the same 失效
标题翻译：生产异香豆素及其中间体的方法
公开(公告)号：US06548695B2
公开(公告)日：2003-04-15
申请号：US10119734
申请日：2002-04-11
申请人： Toshio Tsuchida , Hazuki Nagai , Takashi Nakashima , Masashi Yoshida , Kaname Konuki , Asako Kuroda , Kunio Isshiki , Tomio Takeuchi
发明人： Toshio Tsuchida , Hazuki Nagai , Takashi Nakashima , Masashi Yoshida , Kaname Konuki , Asako Kuroda , Kunio Isshiki , Tomio Takeuchi
IPC分类号： C07C51493
CPC分类号： C07D311/76 , C07C67/31 , C07C67/343 , C07C67/46 , C07C69/92 , Y02P20/55 , C07C69/88
摘要： Provided is a process for producing an isocoumarin-3-yl-acetic acid derivative, characterized by reacting a homophthalic acid derivative represented by a formula: (wherein Rc, R2 and R are mainly protecting groups) with a malonic acid derivating represented by a formula: (wherein R is an organic group including a lower alkyl group; R3 is a protecting group for a carboxyl group; and X is a halogen atom or a —OM group (wherein M is alkaline metal or alkaline earth metal)). According to the above process, various isocoumarin-3-yl-acetic acid derivatives can efficiently be provided.
摘要翻译：提供了一种制备异香豆素-3-基 - 乙酸衍生物的方法，其特征在于使由式（其中Rc，R2和R主要是保护基团）表示的均苯二甲酸衍生物与由式（其中，R为低级烷基的有机基团，R3为羧基的保护基，X为卤原子或-OM基）（其中，M为碱金属或碱土金属）。根据上述方法，可以有效地提供各种异香豆素-3-基 - 乙酸衍生物。

9. 发明授权

US6030951A Chrysomycin derivative compounds and use as antitumor agents 失效
标题翻译：赤霉素衍生物，用作抗肿瘤剂
公开(公告)号：US6030951A
公开(公告)日：2000-02-29
申请号：US308710
申请日：1999-07-08
申请人： Takashi Nakashima , Tadashi Fujii , Kazuya Sakai , Tomohiro Sameshima , Hiroyuki Kumagai , Takeo Yoshioka
发明人： Takashi Nakashima , Tadashi Fujii , Kazuya Sakai , Tomohiro Sameshima , Hiroyuki Kumagai , Takeo Yoshioka
IPC分类号： C07D311/78 , C07D407/04 , C12P17/06 , A61K31/70 , C07H7/04
CPC分类号： C07D407/04 , C07D311/78 , C12P17/06
摘要： Disclosed are the novel C-glycoside compounds Mer-1020dA, Mer-1020dB, Mer-1020dC and Mer-1020dD which have a chromophore group in common with well-known chrysomycins A and B, but can be distinguished from the chrysomycins and the like in that the novel C-glycoside compounds have a sugar residue having a higher degree of oxidation, as well as the compound Mer-1020dE comprising only the chromophore thereof. Among these compounds, the C-glycoside compounds are antibiotics which have low toxicity and can strongly inhibit the growth of solid cancer cells in particular.
摘要翻译： PCT No.PCT / JP97 / 04007 Sec。 371日期：1999年7月8日 102（e）1999年7月8日PCT PCT 1997年11月4日PCT公布。公开号WO98 / 22612 PCT 日期1998年5月28日公开了具有发色团组的新颖的C-糖苷化合物Mer-1020dA，Mer-1020dB，Mer-1020dC和Mer-1020dD，与着名的科莫昔霉素A和B相同，但可以区别于科莫昔霉素因为新型C-糖苷化合物具有较高氧化度的糖残基以及仅包含其发色团的化合物Mer-1020dE。在这些化合物中，C-糖苷化合物是具有低毒性并特别强烈地抑制固体癌细胞生长的抗生素。

10. 发明授权

US09238258B2 Method for producing double-wall tube with braided wires at its interface 有权
标题翻译：在其界面生产编织线双壁管的方法
公开(公告)号：US09238258B2
公开(公告)日：2016-01-19
申请号：US13878275
申请日：2011-10-17
申请人： Takuya Hanada , Takashi Nakashima , Tetsuo Yokoyama , Kouichi Kuroda , Tatsuya Okui
发明人： Takuya Hanada , Takashi Nakashima , Tetsuo Yokoyama , Kouichi Kuroda , Tatsuya Okui
IPC分类号： B21C1/22 , B21C37/15 , F28F1/00
CPC分类号： B21C1/22 , B21C37/154 , F28F1/003
摘要： Provided is a method for producing a double-wall tube with braided wires at its interface in which the braided wires are interposed between an outer-wall and inner-wall blank tubes and then a drawing process is applied so as for the braided wires to be brought into close contact with the inner surface of the outer-wall tube and the outer surface of the inner-wall tube, the method comprising: polishing the inner surface of the outer-wall blank tube and the outer surface of the inner-wall blank tube so that a surface roughness thereof satisfies Ra
摘要翻译：提供一种在其界面处制造具有编织线的双壁管的方法，其中编织线插入在外壁和内壁空白管之间，然后进行拉丝处理以使编织线为与外壁管的内表面和内壁管的外表面紧密接触，该方法包括：抛光外壁空白管的内表面和内壁空白的外表面使其表面粗糙度满足Ra <1.0μm，然后将编织线插入外壁和内壁空白管之间; 进行下沉拉伸处理，使得所得双壁管的外径相对于模孔直径的差异为0.1mm至0.3mm; 并进行热处理。所生产的双壁管适合用作传热管。

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