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1. 发明授权

US07846473B2 Irinotecan preparation 有权
标题翻译：伊立替康制剂
公开(公告)号：US07846473B2
公开(公告)日：2010-12-07
申请号：US11597435
申请日：2005-05-31
申请人： Keisuke Yoshino , Shigenori Nozawa , Masashi Isozaki , Seigo Sawada , Ikuo Kato , Takeshi Matsuzaki
发明人： Keisuke Yoshino , Shigenori Nozawa , Masashi Isozaki , Seigo Sawada , Ikuo Kato , Takeshi Matsuzaki
IPC分类号： A61K9/127
CPC分类号： A61K9/1271 , A61K31/4745
摘要： Provided is an irinotecan formulation capable of supporting irinotecan and/or a salt thereof in a closed vesicle carrier at a high concentration and existing in blood for a long period of time by dramatically improved retentivity in blood compared to a conventionally known irinotecan liposome formulation. That is, an irinotecan formulation including a closed vesicle formed by a lipid membrane, in which irinotecan and/or a salt thereof is encapsulated at a concentration of at least 0.07 mol/mol (drug mol/membrane total lipid mol). There is an ion gradient between an inner aqueous phase and an outer aqueous phase in the irinotecan formulation. The closed vesicle is preferably liposome, in which only the outer surface of the liposome is preferably modified with a surface-modifying agent containing a hydrophilic polymer.
摘要翻译：本发明提供了一种伊立替康制剂，其能够通过显着提高血液中的保留性，与常规已知的伊立替康脂质体制剂相比，可以高密度地在密闭囊泡载体中以高浓度和血液中长时间地支持伊立替康和/或其盐。也就是说，包括由脂质膜形成的封闭囊泡的伊立替康制剂，其中伊立替康和/或其盐以至少0.07mol / mol（药物mol /膜总脂质摩尔）的浓度包封。伊立替康制剂中的内部水相和外部水相之间存在离子梯度。封闭的囊泡优选为脂质体，其中仅脂质体的外表面优选用含有亲水性聚合物的表面改性剂改性。

2. 发明申请

US20080069868A1 Irinotecan Preparation 有权
标题翻译：伊立替康制剂
公开(公告)号：US20080069868A1
公开(公告)日：2008-03-20
申请号：US11597435
申请日：2005-05-31
申请人： Keisuke Yoshino , Shigenori Nozawa , Masashi Isozaki , Seigo Sawada , Ikuo Kato , Takeshi Matsuzaki
发明人： Keisuke Yoshino , Shigenori Nozawa , Masashi Isozaki , Seigo Sawada , Ikuo Kato , Takeshi Matsuzaki
IPC分类号： A61K31/437 , A61K9/127 , A61P35/00
CPC分类号： A61K9/1271 , A61K31/4745
摘要： Provided is an irinotecan formulation capable of supporting irinotecan and/or a salt thereof in a closed vesicle carrier at a high concentration and existing in blood for a long period of time by dramatically improved retentivity in blood compared to a conventionally known irinotecan liposome formulation. That is, an irinotecan formulation including a closed vesicle formed by a lipid membrane, in which irinotecan and/or a salt thereof is encapsulated at a concentration of at least 0.07 mol/mol (drug mol/membrane total lipid mol). There is an ion gradient between an inner aqueous phase and an outer aqueous phase in the irinotecan formulation. The closed vesicle is preferably liposome, in which only the outer surface of the liposome is preferably modified with a surface-modifying agent containing a hydrophilic polymer.
摘要翻译：本发明提供了一种伊立替康制剂，其能够通过显着提高血液中的保留性，与常规已知的伊立替康脂质体制剂相比，可以高密度地在密闭囊泡载体中以高浓度和血液中长时间地支持伊立替康和/或其盐。也就是说，包括由脂质膜形成的封闭囊泡的伊立替康制剂，其中伊立替康和/或其盐以至少0.07mol / mol（药物mol /膜总脂质摩尔）的浓度包封。伊立替康制剂中的内部水相和外部水相之间存在离子梯度。封闭的囊泡优选为脂质体，其中仅脂质体的外表面优选用含有亲水性聚合物的表面改性剂改性。

3. 发明授权

US5190961A Thiourea derivatives and antimicrobial agent and antulcer agent containing the same 失效
标题翻译：硫脲衍生物和抗微生物剂和含有其的抗菌剂
公开(公告)号：US5190961A
公开(公告)日：1993-03-02
申请号：US739437
申请日：1991-08-02
申请人： Hirokazu Hasegawa , Isamu Endo , Shingo Koyama , Masashi Isozaki , Yukari Yoshiyama , Shigenori Nozawa , Norio Arakawa
发明人： Hirokazu Hasegawa , Isamu Endo , Shingo Koyama , Masashi Isozaki , Yukari Yoshiyama , Shigenori Nozawa , Norio Arakawa
IPC分类号： A61K31/17 , A61P1/04 , A61P31/04 , C07C335/08 , C07C335/14 , C07C335/16 , C07D213/75 , C07D295/08 , C07D295/096 , C07D307/52 , C07D333/20
CPC分类号： C07D213/75 , C07C335/08 , C07D295/096 , C07D307/52 , C07D333/20 , C07C2101/14
摘要： Thiourea derivatives represented by the formula (I) ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and each represents a lower alkyl group, or R.sub.1 or R.sub.2 taken together represent a group having the formula --(CH.sub.2).sub.m --in which m is 4 or 5, R.sub.3 represents a lower alkyl group or a cycloalkyl group or a group having the formula--(CH.sub.2).sub.l --R.sub.4 in which R.sub.4 is a phenyl, naphthyl, pyridyl, furyl or thienyl group optionally having 1-3 substituents selected from the group consisting of lower alkyl, lower alkoxy, phenoxy, lower alkylthio, hydroxy, halogen, nitro, cyano and trifluoromethyl, and l represents an integer of 0 to 2 and n represents an integer of 1 to 5 or a physiologically acceptable salt thereof.The compounds of the invention are useful as a therapeutic agent for peptic ulcers which is also effective on prevention of the recurrence after discontinuation of the administration due to the antimicrobial activity against Helicobacter pyroli.
摘要翻译：由式（I）表示的硫脲衍生物其中R 1和R 2相同或不同并且各自表示低级烷基，或者R 1或R 2一起表示具有式 - （CH 2）m - 其中m为4或5，R 3表示低级烷基或环烷基或具有式 - （CH 2）1 -R 4的基团，其中R 4为苯基，萘基，吡啶基，呋喃基或噻吩基， 3个选自低级烷基，低级烷氧基，苯氧基，低级烷硫基，羟基，卤素，硝基，氰基和三氟甲基的取代基，l表示0〜2的整数，n表示1〜5的整数或生理上其可接受的盐。本发明的化合物可用作消化性溃疡的治疗剂，其对于防止由于对幽门螺杆菌的抗微生物活性而在停止施用后的复发也是有效的。

4. 发明授权

US08945526B2 Amphiphilic substance, and drug delivery system and molecular imaging system using the same 有权
标题翻译：两亲物质，药物输送系统和分子成像系统使用相同
公开(公告)号：US08945526B2
公开(公告)日：2015-02-03
申请号：US11812131
申请日：2007-06-15
申请人： Hitoshi Akitsu , Eiichi Ozeki , Ryoji Fushimi , Shunsaku Kimura , Masashi Isozaki , Shigenori Nozawa
发明人： Hitoshi Akitsu , Eiichi Ozeki , Ryoji Fushimi , Shunsaku Kimura , Masashi Isozaki , Shigenori Nozawa
IPC分类号： A61K31/74 , C08G69/10 , A61K49/00 , B82Y5/00
CPC分类号： C08G69/10 , A61K49/0034 , A61K49/0043 , A61K49/0052 , A61K49/0093 , B82Y5/00
摘要： The present invention provides a novel amphiphilic substance, a nanoparticle using the novel amphiphilic substance, which can be used as a nanocarrier having high biocompatibility, a drug delivery system and a probe useful for the system, and, a molecular imaging system and a probe useful for the system. An amphiphilic block polymer comprising a hydrophilic block; and a hydrophobic block, wherein the hydrophilic block is a hydrophilic polypeptide chain having 10 or more sarcosine units, and the hydrophobic block is a hydrophobic molecular chain comprising units selected from the group consisting of amino acid units and hydroxyl acid units as essential structural units, and having 5 or more of the essential structural units.
摘要翻译：本发明提供一种新颖的两亲物质，使用该新型两亲性物质的纳米粒子，其可以用作具有高生物相容性的纳米载体，药物递送系统和可用于该系统的探针，以及分子成像系统和有用的探针为系统。包含亲水嵌段的两亲嵌段聚合物; 和疏水嵌段，其中所述亲水嵌段是具有10个或更多个肌氨酸单元的亲水性多肽链，疏水嵌段是包含选自氨基酸单元和羟基酸单元作为必需结构单元的单元的疏水分子链，并具有5个以上的基本结构单元。

5. 发明申请

US20080019908A1 Novel amphiphilic substance, and drug delivery system and molecular imaging system using the same 有权
标题翻译：新型两亲物质，以及药物输送系统和分子成像系统使用相同
公开(公告)号：US20080019908A1
公开(公告)日：2008-01-24
申请号：US11812131
申请日：2007-06-15
申请人： Hitoshi Akitsu , Eiichi Ozeki , Ryoji Fushimi , Shunsaku Kimura , Masashi Isozaki , Shigenori Nozawa
发明人： Hitoshi Akitsu , Eiichi Ozeki , Ryoji Fushimi , Shunsaku Kimura , Masashi Isozaki , Shigenori Nozawa
IPC分类号： A61K49/00 , A61K38/00 , A61P43/00 , C07K14/00
CPC分类号： C08G69/10 , A61K49/0034 , A61K49/0043 , A61K49/0052 , A61K49/0093 , B82Y5/00
摘要： The present invention provides a novel amphiphilic substance, a nanoparticle using the novel amphiphilic substance, which can be used as a nanocarrier having high biocompatibility, a drug delivery system and a probe useful for the system, and, a molecular imaging system and a probe useful for the system. An amphiphilic block polymer comprising a hydrophilic block; and a hydrophobic block, wherein the hydrophilic block is a hydrophilic polypeptide chain having 10 or more sarcosine units, and the hydrophobic block is a hydrophobic molecular chain comprising units selected from the group consisting of amino acid units and hydroxyl acid units as essential structural units, and having 5 or more of the essential structural units.
摘要翻译：本发明提供一种新颖的两亲物质，使用该新型两亲性物质的纳米粒子，其可以用作具有高生物相容性的纳米载体，药物递送系统和可用于该系统的探针，以及分子成像系统和有用的探针为系统。包含亲水嵌段的两亲嵌段聚合物; 和疏水嵌段，其中所述亲水嵌段是具有10个或更多个肌氨酸单元的亲水性多肽链，疏水嵌段是包含选自氨基酸单元和羟基酸单元作为必需结构单元的单元的疏水分子链，并具有5个以上的基本结构单元。

6. 发明申请

US20080279916A1 Liposome Preparation 有权
标题翻译：脂质体制备
公开(公告)号：US20080279916A1
公开(公告)日：2008-11-13
申请号：US10594427
申请日：2005-03-25
申请人： Masashi Isozaki , Keisuke Yoshino , Kyoko Taguchi , Masayo Kondo
发明人： Masashi Isozaki , Keisuke Yoshino , Kyoko Taguchi , Masayo Kondo
IPC分类号： A61K9/127 , A61P43/00
CPC分类号： A61K9/1271 , A61K9/1272 , A61K31/704
摘要： A liposome preparation is provided. This liposome preparation is capable of stably encapsulating a drug which is unstable under an acidic condition, and such stable encapsulation is realized without detracting the effect realized by the modification of the membrane by a hydrophilic macromolecule such as stability in blood. More specifically, the liposome preparation comprises a unilamellar vesicle formed from a lipid bilayer comprising a phospholipid as its main membrane component, and an interior aqueous phase of the vesicle at a pH of up to 5. The liposome has a drug loaded therein, and the vesicle is modified with a hydrophilic macromolecule only on its exterior surface.
摘要翻译：提供了脂质体制剂。该脂质体制剂能够稳定地包封在酸性条件下不稳定的药物，并且实现这种稳定的包封，而不会降低通过亲水性高分子如血液稳定性改性膜所产生的效果。更具体地说，脂质体制剂包括由包含磷脂作为其主要成分的脂质双层形成的单层囊泡和pH至多为5的囊泡的内部水相。脂质体中装载有药物，并且囊泡仅在其外表面上用亲水性大分子修饰。

7. 发明申请

US20070298094A1 Medicinal Composition, Preparation and Combined Preparation 审中-公开
标题翻译：药用成分，制备及联合制剂
公开(公告)号：US20070298094A1
公开(公告)日：2007-12-27
申请号：US11667954
申请日：2005-11-16
申请人： Keisuke Yoshino , Masashi Isozaki , Katsumi Morimoto , Miyuki Shimizu
发明人： Keisuke Yoshino , Masashi Isozaki , Katsumi Morimoto , Miyuki Shimizu
IPC分类号： A61K9/127 , A61K31/765 , A61P37/00 , A61K47/30
CPC分类号： A61K9/1271
摘要： A medicinal composition and a medicinal preparation which are capable of inhibiting complement activation. The medicinal composition comprises: a medicinal preparation modified with a first hydrophilic polymer; and a second hydrophilic polymer. The medicinal preparation contains as an active ingredient a second hydrophilic polymer which inhibits an immunoreaction caused by a medicinal preparation modified with a first hydrophilic polymer.
摘要翻译：能够抑制补体活化的药物组合物和药物制剂。所述药物组合物包含：用第一亲水性聚合物改性的药物制剂; 和第二亲水性聚合物。药物制剂含有作为活性成分的第二亲水性聚合物，其抑制由用第一亲水性聚合物改性的药物制剂引起的免疫反应。

8. 发明授权

US08241663B2 Liposome preparation 有权
标题翻译：脂质体制备
公开(公告)号：US08241663B2
公开(公告)日：2012-08-14
申请号：US10594427
申请日：2005-03-25
申请人： Masashi Isozaki , Keisuke Yoshino , Kyoko Taguchi , Masayo Kondo
发明人： Masashi Isozaki , Keisuke Yoshino , Kyoko Taguchi , Masayo Kondo
IPC分类号： A61K9/127 , G01N33/53
CPC分类号： A61K9/1271 , A61K9/1272 , A61K31/704
摘要： A liposome preparation is provided. This liposome preparation is capable of stably encapsulating a drug which is unstable under an acidic condition, and such stable encapsulation is realized without detracting the effect realized by the modification of the membrane by a hydrophilic macromolecule such as stability in blood. More specifically, the liposome preparation comprises a unilamellar vesicle formed from a lipid bilayer comprising a phospholipid as its main membrane component, and an interior aqueous phase of the vesicle at a pH of up to 5. The liposome has a drug loaded therein, and the vesicle is modified with a hydrophilic macromolecule only on its exterior surface.
摘要翻译：提供了脂质体制剂。该脂质体制剂能够稳定地包封在酸性条件下不稳定的药物，并且实现这种稳定的包封，而不会降低通过亲水性高分子如血液稳定性改性膜所产生的效果。更具体地说，脂质体制剂包括由包含磷脂作为其主要成分的脂质双层形成的单层囊泡和pH至多为5的囊泡的内部水相。脂质体中装载有药物，并且囊泡仅在其外表面上用亲水性大分子修饰。

9. 发明申请

US20080146796A1 Process for preparing an o-alkylated rapamycin derivative and o-alkylated rapamycin derivative 有权
标题翻译：制备邻烷基化雷帕霉素衍生物和邻烷基化雷帕霉素衍生物的方法
公开(公告)号：US20080146796A1
公开(公告)日：2008-06-19
申请号：US11984988
申请日：2007-11-26
申请人： Tetsuro Kawanishi , Masashi Isozaki
发明人： Tetsuro Kawanishi , Masashi Isozaki
IPC分类号： C07D487/14
CPC分类号： C07D498/18 , B01D15/322 , B01D15/325
摘要： A process for preparing an o-alkylated rapamycin derivative represented by the following general formula (1) is provided. The process includes the steps of reacting rapamycin with an alkyl triflate, purifying the resulting reaction product with a normal phase chromatograph and further purifying a purified product, which has been purified with the normal phase chromatograph, with a reverse phase chromatography wherein R represents an alkyl, arylalkyl, hydroxyalkyl, alkoxyalkyl, acyloxyalkyl, aminoalkyl, alkylaminoalkyl, alkoxycarbonylaminoalkyl, acylaminoalkyl, or aryl.
摘要翻译：提供了制备由以下通式（1）表示的邻烷基化的雷帕霉素衍生物的方法。该方法包括以下步骤：使雷帕霉素与三氟甲磺酸烷基酯反应，用正相色谱法纯化所得反应产物，并进一步纯化已经用正相色谱法纯化的纯化产物，其中R代表烷基，芳基烷基，羟基烷基，烷氧基烷基，酰氧基烷基，氨基烷基，烷基氨基烷基，烷氧基羰基氨基烷基，酰基氨基烷基或芳基。

10. 发明申请

US20050192311A1 Process for production of O-alkylated rapamycin derivatives 有权
标题翻译： O-烷基化雷帕霉素衍生物的制备方法
公开(公告)号：US20050192311A1
公开(公告)日：2005-09-01
申请号：US11067718
申请日：2005-03-01
申请人： Masashi Isozaki , Tetsuro Kawanishi
发明人： Masashi Isozaki , Tetsuro Kawanishi
IPC分类号： A61F2/82 , A61K31/436 , A61L31/00 , A61M29/02 , A61P31/10 , A61P35/00 , A61P37/06 , C07D498/18 , A61K31/4745 , C07D491/14
CPC分类号： C07D498/18
摘要： Disclosed herein is a process for production of an O-alkylrapamycin derivative represented by the general formula (1) below by reaction between rapamycin and alkyl triflate in an organic solvent, characterized in that the reaction is carried out in the presence of trialkylamine. (where R denotes alkyl, arylalkyl, hydroxyalkyl, alkoxyalkyl, acyloxyalkyl, aminoalkyl, alkylaminoalkyl, alkoxycarbonylaminoalkyl, acylaminoalkyl, or aryl.) This process is capable of producing O-alkylrapamycin derivative efficiently owing to improvement in reaction yields for O-alkylation.
摘要翻译：本文公开了通过在有机溶剂中雷帕霉素和三氟甲磺酸烷基酯之间的反应制备由以下通式（1）表示的O-烷基雷帕霉素衍生物的方法，其特征在于反应在三烷基胺存在下进行。（其中R表示烷基，芳基烷基，羟基烷基，烷氧基烷基，酰氧基烷基，氨基烷基，烷基氨基烷基，烷氧基羰基氨基烷基，酰氨基烷基或芳基）。由于O-烷基化的反应产率提高，该方法能够有效地生产O-烷基雷帕霉素衍生物。

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