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。

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。

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。

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。

公开(公告)号：US20130315977A1

公开(公告)日：2013-11-28

申请号：US13983366

申请日：2012-02-01

申请人： Hiroo Maeda ,  Kazumitsu Yamamoto ,  Masayasu Tanaka

发明人： Hiroo Maeda ,  Kazumitsu Yamamoto ,  Masayasu Tanaka

IPC分类号： A61K31/496

CPC分类号： A61K31/496 ,  A61K9/7053 ,  A61K9/7061

摘要： The present invention relates to an external preparation for transdermal administration, which remarkably enhances the skin permeability of 2-(4-ethyl-1-piperazinyl)-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydrocycloocta[b]pyridine (compound A). The adhesive preparation of the present invention has an adhesive layer formed on one surface of a support, and the adhesive layer contains (i) compound A or a physiologically acceptable acid addition salt thereof, (ii) an adhesive, (iii) lactic acid, and (iv) an additive containing a particular permeation enhancer, whereby remarkably superior skin permeability is provided.

摘要翻译： 本发明涉及透皮给药的外用制剂，其显着提高了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）。 本发明的粘合剂制剂具有在支撑体的一个表面上形成的粘合剂层，并且粘合剂层含有（i）化合物A或其生理上可接受的酸加成盐，（ii）粘合剂，（iii）乳酸， 和（iv）含有特定渗透促进剂的添加剂，从而提供非常优异的皮肤渗透性。

公开(公告)号：US20090169605A1

公开(公告)日：2009-07-02

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。

公开(公告)号：US06887477B1

公开(公告)日：2005-05-03

申请号：US09762188

申请日：1999-08-04

申请人： Tomokazu Nagano ,  Ikue Kudo ,  Takao Kawamura ,  Mutsuo Taiji ,  Hiroshi Noguchi ,  Shunsuke Tani ,  Hiroo Maeda

发明人： Tomokazu Nagano ,  Ikue Kudo ,  Takao Kawamura ,  Mutsuo Taiji ,  Hiroshi Noguchi ,  Shunsuke Tani ,  Hiroo Maeda

IPC分类号： A61K38/18 ,  A61K38/00 ,  C07K14/00

CPC分类号： A61K38/1833

摘要： Preparations to be administered for treating or preventing ischemic diseases or arterial diseases which contain Hepatocyte growth factor (HGF) as an active ingredient. The preparations provide such effect that HGF concentration in an affected region to which HGF was administered is maintained, a half-life is longer, a dose can be reduced, and other organs except the affected region are less affected in comparison with intravenous administration.

摘要翻译： 用于治疗或预防含有肝细胞生长因子（HGF）作为活性成分的缺血性疾病或动脉疾病的制剂。 所述制剂提供如下效果：维持HGF施用的受影响区域中的HGF浓度，半衰期更长，可以减少剂量，并且与静脉内施用相比，受影响区域以外的其它器官的影响较小。

公开(公告)号：US06756048B1

公开(公告)日：2004-06-29

申请号：US09786746

申请日：2001-04-18

申请人： Akihiko Sano ,  Hiroo Maeda ,  Masako Kajihara ,  Shunsuke Tani ,  Toshihiko Sugie

发明人： Akihiko Sano ,  Hiroo Maeda ,  Masako Kajihara ,  Shunsuke Tani ,  Toshihiko Sugie

IPC分类号： A61F200

CPC分类号： A61K9/0087 ,  A61K31/00 ,  A61K47/30

摘要： The present invention relates to a sustained release preparation of a lipophilic drug, comprising a drug dispersion wherein the lipophilic drug and a water-soluble substance are dispersed, in a solid state at the body temperature of an animal or a human being to which the preparation is to be administered, in a water-impermeable and biocompatible material.

摘要翻译： 本发明涉及亲脂性药物的持续释放制剂，其包含药物分散体，其中所述亲脂性药物和水溶性物质以固体状态分散在动物或人的体温，所述制剂 将在不透水和生物相容的材料中施用。

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。

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.