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1.发明申请Process for preparing an o-alkylated rapamycin derivative and o-alkylated rapamycin derivative 有权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
Applicant: Tetsuro Kawanishi , Masashi Isozaki
Inventor： Tetsuro Kawanishi , Masashi Isozaki
IPC: C07D487/14
CPC classification number: C07D498/18 , B01D15/322 , B01D15/325
Abstract: 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.
Abstract translation: 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。
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公开(公告)号：US20050192311A1
公开(公告)日：2005-09-01
申请号：US11067718
申请日：2005-03-01
Applicant: Masashi Isozaki , Tetsuro Kawanishi
Inventor： Masashi Isozaki , Tetsuro Kawanishi
IPC: A61F2/82 , A61K31/436 , A61L31/00 , A61M29/02 , A61P31/10 , A61P35/00 , A61P37/06 , C07D498/18 , A61K31/4745 , C07D491/14
CPC classification number: C07D498/18
Abstract: 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.
Abstract translation: 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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公开(公告)号：US08241663B2
公开(公告)日：2012-08-14
申请号：US10594427
申请日：2005-03-25
Applicant: Masashi Isozaki , Keisuke Yoshino , Kyoko Taguchi , Masayo Kondo
Inventor： Masashi Isozaki , Keisuke Yoshino , Kyoko Taguchi , Masayo Kondo
CPC classification number: A61K9/1271 , A61K9/1272 , A61K31/704
Abstract: 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.
Abstract translation: 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。
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4.发明授权Process for preparing an o-alkylated rapamycin derivative and o-alkylated rapamycin derivative 有权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：US07812155B2
公开(公告)日：2010-10-12
申请号：US11984988
申请日：2007-11-26
Applicant: Tetsuro Kawanishi , Masashi Isozaki
Inventor： Tetsuro Kawanishi , Masashi Isozaki
IPC: C07D498/18
CPC classification number: C07D498/18 , B01D15/322 , B01D15/325
Abstract: 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.
Abstract translation: 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。
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公开(公告)号：US20080069868A1
公开(公告)日：2008-03-20
申请号：US11597435
申请日：2005-05-31
Applicant: Keisuke Yoshino , Shigenori Nozawa , Masashi Isozaki , Seigo Sawada , Ikuo Kato , Takeshi Matsuzaki
Inventor： Keisuke Yoshino , Shigenori Nozawa , Masashi Isozaki , Seigo Sawada , Ikuo Kato , Takeshi Matsuzaki
IPC: A61K31/437 , A61K9/127 , A61P35/00
CPC classification number: A61K9/1271 , A61K31/4745
Abstract: 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.
Abstract translation: 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。
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Patent Agency Ranking
6.发明申请Novel amphiphilic substance, and drug delivery system and molecular imaging system using the same 有权新型两亲物质，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
Applicant: Hitoshi Akitsu , Eiichi Ozeki , Ryoji Fushimi , Shunsaku Kimura , Masashi Isozaki , Shigenori Nozawa
Inventor： Hitoshi Akitsu , Eiichi Ozeki , Ryoji Fushimi , Shunsaku Kimura , Masashi Isozaki , Shigenori Nozawa
CPC classification number: C08G69/10 , A61K49/0034 , A61K49/0043 , A61K49/0052 , A61K49/0093 , B82Y5/00
Abstract: 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.
Abstract translation: 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。
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公开(公告)号：US5189189A
公开(公告)日：1993-02-23
申请号：US689622
申请日：1991-04-23
Applicant: Yoshihisa Misawa , Hisao Kondo , Tetsuya Tsutsumi , Masahiro Hayashi , Daisuke Sugimori , Yorishige Matsuba , Masashi Isozaki , Hiroharu Nishigaki , Kazunaga Yazawa , Kiyosi Kondo
Inventor： Yoshihisa Misawa , Hisao Kondo , Tetsuya Tsutsumi , Masahiro Hayashi , Daisuke Sugimori , Yorishige Matsuba , Masashi Isozaki , Hiroharu Nishigaki , Kazunaga Yazawa , Kiyosi Kondo
IPC: C07C51/487 , C07C67/60
CPC classification number: C07C51/487 , C07C67/60
Abstract: [Object] A fatty acid-related polyunsaturated compound can be selectively purified using an industrially operable successive method under moderate conditions. [Content] A highly purified fatty acid-related polyunsaturated compound is obtained by a process comprising steps of forming a complex with silver on account of the high degree of unsaturation of the fatty acid-related polyunsaturated compound, isolating the complex from other fats on account of the hydrophilicity of the complex and then applying dissociating procedures to the complex to obtain the fatty acid-related polyunsaturated compound as a target substance on account of the hydrophobicity of the fatty acid-related polyunsaturated compound. As to the procedures for dissociation, addition of a dissociating agent and reduction of silver are disclosed. As to the dissociating agent, various compounds which produce insoluble composition with silver other then water are disclosed. Furthermore, an apparatus appropriately used to carry out this method is also disclosed.
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8.发明授权Amphiphilic substance, and drug delivery system and molecular imaging system using the same 有权两亲物质，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
Applicant: Hitoshi Akitsu , Eiichi Ozeki , Ryoji Fushimi , Shunsaku Kimura , Masashi Isozaki , Shigenori Nozawa
Inventor： Hitoshi Akitsu , Eiichi Ozeki , Ryoji Fushimi , Shunsaku Kimura , Masashi Isozaki , Shigenori Nozawa
CPC classification number: C08G69/10 , A61K49/0034 , A61K49/0043 , A61K49/0052 , A61K49/0093 , B82Y5/00
Abstract: 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.
Abstract translation: 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。
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公开(公告)号：US20080279916A1
公开(公告)日：2008-11-13
申请号：US10594427
申请日：2005-03-25
Applicant: Masashi Isozaki , Keisuke Yoshino , Kyoko Taguchi , Masayo Kondo
Inventor： Masashi Isozaki , Keisuke Yoshino , Kyoko Taguchi , Masayo Kondo
CPC classification number: A61K9/1271 , A61K9/1272 , A61K31/704
Abstract: 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.
Abstract translation: 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。
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10.发明授权Thiourea derivatives and antimicrobial agent and antiulcer agent containing the same 失效硫脲衍生物和抗微生物剂和含有其的抗微生物剂
公开(公告)号：US5214053A
公开(公告)日：1993-05-25
申请号：US939692
申请日：1992-09-02
Applicant: Keiichi Nakazawa , Masashi Isozaki , Shingo Koyama
Inventor： Keiichi Nakazawa , Masashi Isozaki , Shingo Koyama
IPC: A61K31/335 , A61K31/357 , A61K31/435 , A61P1/04 , A61P31/00 , A61P31/04 , C07D317/48 , C07D317/58 , C07D317/66 , C07D319/18 , C07D405/12 , C07D405/14
CPC classification number: C07D405/12 , C07D317/66 , C07D319/18
Abstract: 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 and R.sub.2 taken together represent a group having the formula --(CH.sub.2).sub.x --CHR.sub.3 --(CH.sub.2).sub.y -- in which R.sub.3 represents hydrogen or a lower alkyl group and x and y represent an integer of 0 to 2, respectively, A represents the formula --CH.dbd.CH-- or --CH.dbd.N--, 1 is 1 or 2, m represents an integer of 0 to 2 and n represents an integer of 1 to 5.The thiourea derivatives possess an antiulcer activity and an antimicrobial activity against Helicobacter pyroli and are useful as an antiulcer agent and an antimicrobial agent against Helicobacter pyroli.
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