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1. 发明授权

US5214131A Polyethylene glycol derivatives, modified peptides and production thereof 失效
标题翻译：聚乙二醇衍生物，修饰肽及其制备
公开(公告)号：US5214131A
公开(公告)日：1993-05-25
申请号：US798138
申请日：1991-11-26
申请人： Akihiko Sano , Hiroo Maeda , Yoshiyuki Kai , Keiichi Ono
发明人： Akihiko Sano , Hiroo Maeda , Yoshiyuki Kai , Keiichi Ono
IPC分类号： C07K1/06 , C07K1/107 , C08G65/323 , C08G65/329 , C08G65/334
CPC分类号： C07K1/064 , C07K1/1077 , C08G65/323 , C08G65/329 , C08G65/3346
摘要： A polyethylene glycol derivative of the formula ##STR1## wherein R represents a lower alkyl and n represents an optional positive integer which renders the average molecular weight of the polyethylene glycol moiety about 1,000 to 12,000, a peptide modified by said polyethylene glycol derivative and a method for production thereof. The polyethylene glycol derivative (I) is capable of modifying the guanidino groups in peptides. The peptides modified by the polyethylene glycol derivative (I) are extremely stable, are considerably delayed in biological clearance (i.e. the durability is extended) and exhibit their physiological activities effectively over the long period.
摘要翻译：式（I）的聚乙二醇衍生物，其中R表示低级烷基，n表示任选的正整数，其使得聚乙二醇部分的平均分子量为约1,000至12,000，由所述聚乙二醇衍生物修饰的肽及其制造方法。聚乙二醇衍生物（I）能够改变肽中的胍基。由聚乙二醇衍生物（I）改性的肽是非常稳定的，生物清除率（即耐久性延长）显着延迟，并且在长时间内有效地表现出其生理活性。

2. 发明授权

US5342940A Polyethylene glycol derivatives, process for preparing the same 失效
标题翻译：聚乙二醇衍生物，其制备方法
公开(公告)号：US5342940A
公开(公告)日：1994-08-30
申请号：US119821
申请日：1993-09-13
申请人： Keiichi Ono , Yoshiyuki Kai , Hiroo Maeda
发明人： Keiichi Ono , Yoshiyuki Kai , Hiroo Maeda
IPC分类号： A61K38/00 , A61K47/48 , C07D251/26 , C07K1/107 , C08G65/32 , C08G65/329 , C08G65/333 , C12N9/96
CPC分类号： A61K47/48215 , C07D251/26 , C07K1/1077 , C08G65/32 , C08G65/329 , C08G65/333 , C12N9/96 , A61K38/00
摘要： High purity polyethylene glycol derivatives of formula (I) are useful as protein modifiers of interferons, t-PA, EGF, various hormones, etc. The thus modified protein has minimized antigenicity, prolonged plasma half life, or improved transfer to tissue. A novel process for preparing high purity polyethylene glycol derivatives is also disclosed.
摘要翻译：式（I）的高纯度聚乙二醇衍生物可用作干扰素，t-PA，EGF，各种激素等的蛋白质改性剂。由此修饰的蛋白质具有最小的抗原性，延长的血浆半衰期或改善的转移至组织。还公开了一种制备高纯度聚乙二醇衍生物的新方法。

3. 发明授权

US5093531A Polyethylene glycol substituted phenyl glyoxals 失效
标题翻译：聚乙二醇取代苯甲酸
公开(公告)号：US5093531A
公开(公告)日：1992-03-03
申请号：US347902
申请日：1989-05-05
申请人： Akihiko Sano , Hiroo Maeda , Yoshiyuki Kai , Keiichi Ono
发明人： Akihiko Sano , Hiroo Maeda , Yoshiyuki Kai , Keiichi Ono
IPC分类号： C12N9/00 , A61K38/00 , C07K1/02 , C07K1/06 , C07K1/107 , C07K1/113 , C07K7/23 , C07K14/00 , C07K14/52 , C07K14/53 , C07K14/535 , C07K14/575 , C07K14/58 , C07K14/60 , C07K14/65 , C08G65/32 , C08G65/323 , C08G65/329 , C08G65/334 , C08G65/48
CPC分类号： C08G65/323 , C07K1/064 , C07K1/1077 , C08G65/329 , C08G65/3346
摘要： A polyethylene glycol derivative of the formula ##STR1## wherein R represents a lower alkyl and n represents an optional positive integer which renders the average molecular weight of the polyethylene glycol moiety about 1,000 to 12,000, a peptide modified by said polyethylene glycol derivative and a method for production thereof.The polyethylene glycol derivative (I) is capable of modifying the guanidino groups in peptides. The peptides modified by the polyethylene glycol derivative (I) are extremely stable, are considerably delayed in biological clearance (i.e. the durability is extended) and exhibit their physiological activities effectively over the long period.

4. 发明授权

US07601363B2 Sustained-release drug formulations 失效
标题翻译：持续释放药物制剂
公开(公告)号：US07601363B2
公开(公告)日：2009-10-13
申请号：US11688082
申请日：2007-03-19
申请人： Akihiko Sano , Masako Kajihara , Hiroo Maeda
发明人： Akihiko Sano , Masako Kajihara , Hiroo Maeda
IPC分类号： A61K9/14 , A61F2/00 , A61F13/00
CPC分类号： A61K9/0024 , A61K47/02
摘要： The present invention relates to a formulation for implantation having a novel constitution, which accomplishes controlled releases of active ingredients. The formulation comprises one of combinations (a), (b) and (c), as well as a carrier comprising a hydrophobic polymer, wherein the particle combination is dispersed into the carrier: (a) particles comprising an active ingredient, particles comprising a carbonate, and particles comprising a substance which is reacted with the carbonate in an aqueous solution to generate carbon dioxide (substance such as an acid); (b) particles comprising an active ingredient and a carbonate, and particles comprising a substance such as an acid; and (c) particles comprising a carbonate, and particles comprising an active ingredient and a substance such as an acid.
摘要翻译：本发明涉及具有实现活性成分控制释放的新颖结构的植入制剂。制剂包含组合（a），（b）和（c）中的一种，以及包含疏水性聚合物的载体，其中所述颗粒组合分散在载体中：（a）包含活性成分的颗粒，碳酸盐和包含与碳酸盐在水溶液中反应产生二氧化碳（物质如酸）的物质的颗粒; （b）包含活性成分和碳酸酯的颗粒，以及包含物质如酸的颗粒; 和（c）包含碳酸盐的颗粒和包含活性成分和物质如酸的颗粒。

5. 发明申请

US20070254887A1 Pharmaceutical Composition for Transdermal Administration of Perospirone 审中-公开
标题翻译：用于透皮给药螺旋体的药物组合物
公开(公告)号：US20070254887A1
公开(公告)日：2007-11-01
申请号：US11661612
申请日：2005-09-02
申请人： Hiroo Maeda , Naoki Ohara , Yuki Ikeda
发明人： Hiroo Maeda , Naoki Ohara , Yuki Ikeda
IPC分类号： A61K31/495
CPC分类号： A61K31/496 , A61K9/0014
摘要： A pharmaceutical composition for transdermal administration comprising perospirone of the formula (1): or a pharmaceutically acceptable acid addition salt thereof, which can inhibit the generation of metabolites and continuously maintain the blood level of perospirone.
摘要翻译：一种用于透皮给药的药物组合物，其包含式（1）的吐温酮：或其药学上可接受的酸加成盐，其可以抑制代谢物的产生并且持续维持呼吸道虫的血液水平。

6. 发明授权

US6143364A Hot dip plating method and apparatus 失效
标题翻译：热浸镀方法和装置
公开(公告)号：US6143364A
公开(公告)日：2000-11-07
申请号：US113304
申请日：1998-07-10
申请人： Toshio Nakamori , Masashi Yamamoto , Tamotsu Toki , Hirohito Masumoto , Mutsuo Sagara , Hiroo Maeda
发明人： Toshio Nakamori , Masashi Yamamoto , Tamotsu Toki , Hirohito Masumoto , Mutsuo Sagara , Hiroo Maeda
IPC分类号： C23C2/02 , C23C2/06 , C23C2/12 , C23C2/30 , B05D1/18
CPC分类号： C23C2/02
摘要： A batchwise hot dip plating method is performed by dipping a metallic material in a molten metal plating bath, following fluxing by dipping the metallic material in a bath of a fused salt flux (e.g., a mixture of cryolite and one or more alkali metal chlorides and optionally aluminum fluoride) having a melting temperature at least 5.degree. C. higher than the temperature of the molten metal plating bath, which also serves to preheat the metallic material. In the case of hot dip plating with an Al--Zn alloy, particularly a Zn/55% Al/0.5-2% Si alloy, a bare spot-free plated coating having good appearance can be formed by a reduced duration of dipping in the plating bath without post-plating treatment to remove flux residues. The use of a plating tank having a cross section of a round shape such as a semicircular shape or an oblong semielliptic shape, rather than a rectangular box shape, brings about a significantly extended service life of the plating tank.
摘要翻译：通过将金属材料浸入熔融盐助熔剂（例如，冰晶石和一种或多种碱金属氯化物的混合物）和一种或多种碱金属氯化物的混合物中，将金属材料浸入熔融金属镀浴中，任选的氟化铝），其熔融温度比熔融金属电镀浴的温度高至少5℃，这也用于预热金属材料。在使用Al-Zn合金，特别是Zn / 55％Al / 0.5-2％Si合金进行热浸镀的情况下，可以通过减少浸渍时间来形成具有良好外观的裸露点镀覆涂层电镀浴不需要电镀后处理以除去助焊剂残留物。使用具有诸如半圆形或长方形半椭圆形的圆形横截面的电镀槽而不是矩形盒形状，导致电镀槽的使用寿命显着延长。

7. 发明授权

US08354121B2 Tape preparation 失效
标题翻译：磁带准备
公开(公告)号：US08354121B2
公开(公告)日：2013-01-15
申请号：US12308099
申请日：2007-06-07
申请人： Hiroo Maeda , Naoki Ohara
发明人： Hiroo Maeda , Naoki Ohara
IPC分类号： A61F13/02 , A61K31/497
CPC分类号： A61K31/496 , A61K9/7061
摘要： It is intended to provide a preparation for percutaneous administration of 2-(4-ethyl-1-piperazinyl)-4-(4-fluoro-phenyl)-5,6,7,8,9,10-hexahydrocycloocta[b]pyridine (Compound A), which inhibits the generation of a metabolite and is capable of continuously maintaining a blood drug level. Specifically, a tape preparation comprising an adhesive layer formed on one surface of a support, characterized in that the adhesive layer contains (1) Compound A or a physiologically acceptable acid addition salt thereof, and (2) an acrylic adhesive, or (1) Compound A or a physiologically acceptable acid addition salt thereof, (2) an acrylic adhesive, and (3) a permeation enhancer is provided.
摘要翻译：本发明旨在提供经皮给予2-（4-乙基-1-哌嗪基）-4-（4-氟 - 苯基）-5,6,7,8,9,10-六氢环辛[b]吡啶（化合物A），其抑制代谢物的产生并能够连续维持血药浓度。具体而言，包括在载体的一个表面上形成的粘合剂层的胶带制剂，其特征在于，所述粘合剂层包含（1）化合物A或其生理上可接受的酸加成盐，和（2）丙烯酸粘合剂，或（1）化合物A或其生理上可接受的酸加成盐，（2）丙烯酸粘合剂，和（3）渗透促进剂。

8. 发明授权

US07247312B1 Sustained-release drug formulations for implantation 失效
标题翻译：用于植入的持续释放药物制剂
公开(公告)号：US07247312B1
公开(公告)日：2007-07-24
申请号：US10089694
申请日：2000-10-31
申请人： Akihiko Sano , Masako Kajihara , Hiroo Maeda
发明人： Akihiko Sano , Masako Kajihara , Hiroo Maeda
IPC分类号： A61F13/00 , A61F2/00 , A61K9/14
CPC分类号： A61K9/0024 , A61K47/02
摘要： The present invention relates to a formulation for implantation having a novel constitution, which accomplishes controlled releases of active ingredients. The formulation comprises one of combinations (a), (b) and (c), as well as a carrier comprising a hydrophobic polymer, wherein the particle combination is dispersed into the carrier: (a) particles comprising an active ingredient, particles comprising a carbonate, and particles comprising a substance which is reacted with the carbonate in an aqueous solution to generate carbon dioxide (substance such as an acid); (b) particles comprising an active ingredient and a carbonate, and particles comprising a substance such as an acid; and (c) particles comprising a carbonate, and particles comprising an active ingredient and a substance such as an acid.
摘要翻译：本发明涉及具有实现活性成分控制释放的新颖结构的植入制剂。制剂包含组合（a），（b）和（c）中的一种，以及包含疏水性聚合物的载体，其中所述颗粒组合分散在载体中：（a）包含活性成分的颗粒，碳酸盐和包含与碳酸盐在水溶液中反应产生二氧化碳（物质如酸）的物质的颗粒; （b）包含活性成分和碳酸酯的颗粒，以及包含物质如酸的颗粒; 和（c）包含碳酸盐的颗粒和包含活性成分和物质如酸的颗粒。

9. 发明申请

US20070166377A1 SUSTAINED-RELEASE DRUG FORMULATIONS 失效
标题翻译：持续释放药物制剂
公开(公告)号：US20070166377A1
公开(公告)日：2007-07-19
申请号：US11688082
申请日：2007-03-19
申请人： Akihiko Sano , Masako Kajihara , Hiroo Maeda
发明人： Akihiko Sano , Masako Kajihara , Hiroo Maeda
IPC分类号： A61K39/00 , A61K9/46
CPC分类号： A61K9/0024 , A61K47/02
摘要： The present invention relates to a formulation for implantation having a novel constitution, which accomplishes controlled releases of active ingredients. The formulation comprises one of combinations (a), (b) and (c), as well as a carrier comprising a hydrophobic polymer, wherein the particle combination is dispersed into the carrier: (a) particles comprising an active ingredient, particles comprising a carbonate, and particles comprising a substance which is reacted with the carbonate in an aqueous solution to generate carbon dioxide (substance such as an acid); (b) particles comprising an active ingredient and a carbonate, and particles comprising a substance such as an acid; and (c) particles comprising a carbonate, and particles comprising an active ingredient and a substance such as an acid.
摘要翻译：本发明涉及具有实现活性成分控制释放的新颖结构的植入制剂。制剂包含组合（a），（b）和（c）中的一种，以及包含疏水性聚合物的载体，其中所述颗粒组合分散在载体中：（a）包含活性成分的颗粒，碳酸盐和包含与碳酸盐在水溶液中反应产生二氧化碳（物质如酸）的物质的颗粒; （b）包含活性成分和碳酸酯的颗粒，以及包含物质如酸的颗粒; 和（c）包含碳酸盐的颗粒和包含活性成分和物质如酸的颗粒。

10. 发明申请

US20140023695A1 PATCH PREPARATION 审中-公开
标题翻译：配对准备
公开(公告)号：US20140023695A1
公开(公告)日：2014-01-23
申请号：US13983166
申请日：2012-02-01
申请人： Yasuaki Okada , Katsuhiro OKada , Masato Nishimura , Yuji Kawaharada , Hiroo Maeda , Kazumitsu Yamamoto , Masayasu Tanaka
发明人： Yasuaki Okada , Katsuhiro OKada , Masato Nishimura , Yuji Kawaharada , Hiroo Maeda , Kazumitsu Yamamoto , Masayasu Tanaka
IPC分类号： A61K31/496 , A61K9/70
CPC分类号： A61K31/496 , A61K9/7061
摘要： A patch preparation containing a support and an adhesive layer formed on one surface of the support, wherein the adhesive layer contains 2-(4-ethyl-1-piperazinyl)-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydrocycloocta[b]pyridine or a physiologically acceptable acid addition salt thereof, an acrylic polymer, lactic acid, sesame oil and one or more kinds of stabilizers selected from 2-mercaptobenzimidazole, 2,6-di-tert-butyl-4-methylphenol and propyl gallate.A patch preparation containing a support and an adhesive layer containing lactic acid and magnesium aluminometasilicate and formed on at least one surface of the support, which preparation is superior in both skin permeability and adhesiveness in the presence of water.
摘要翻译：一种贴剂，其包含支撑体和形成在支持体的一个表面上的粘合剂层，其中粘合剂层含有2-（4-乙基-1-哌嗪基）-4-（4-氟苯基）-5,6,7,8 ，9,10-六氢环辛[b]吡啶或其生理上可接受的酸加成盐，丙烯酸聚合物，乳酸，芝麻油和一种或多种选自2-巯基苯并咪唑，2,6-二叔丁基 -4-甲基苯酚和没食子酸丙酯。一种贴剂，其含有载体和含有乳酸和硅酸铝镁的粘合剂层，并形成在载体的至少一个表面上，该制剂在水的存在下具有优异的皮肤渗透性和粘合性。

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