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1. 发明授权

US06436912B1 Drug complexes 失效
标题翻译：药物复合物
公开(公告)号：US06436912B1
公开(公告)日：2002-08-20
申请号：US09147342
申请日：1999-03-25
申请人： Kazuhiro Inoue , Hiroshi Susaki , Masahiro Ikeda , Hiroshi Kuga , Eiji Kumazawa , Akiko Togo
发明人： Kazuhiro Inoue , Hiroshi Susaki , Masahiro Ikeda , Hiroshi Kuga , Eiji Kumazawa , Akiko Togo
IPC分类号： A61K31715
CPC分类号： A61K47/61
摘要： A drug complex characterized in that a residue of a drug compound such as antineoplastic agents and a carboxy(C1-4)alkyldextran polyalcohol obtained by treating a dextran under conditions that enable substantially complete polyalcoholization are bound to each other by means of a spacer comprising an amino acid or a spacer comprising peptide-bonded 2 to 8 amino acids. Said complex is characterized-in that it has excellent selectivity to tumorous sites so as to exhibit high antineoplastic activity and also achieves reduced appearance of toxicity.
摘要翻译：一种药物复合物，其特征在于药物化合物如抗肿瘤剂和通过在能够基本上完全多元醇化的条件下处理葡聚糖而获得的羧基（C 1-4）烷基葡聚糖多元醇的残基通过包含氨基酸或包含肽键合的2至8个氨基酸的间隔子。所述复合物的特征在于其对肿瘤部位具有优异的选择性，从而表现出高的抗肿瘤活性，并且还实现了毒性的降低。

2. 发明授权

US06838450B2 Drug complex 失效
标题翻译：药物复合体
公开(公告)号：US06838450B2
公开(公告)日：2005-01-04
申请号：US10155170
申请日：2002-05-28
申请人： Kazuhiro Inoue , Hiroshi Susaki , Masahiro Ikeda , Hiroshi Kuga , Eiji Kumazawa , Akiko Togo
发明人： Kazuhiro Inoue , Hiroshi Susaki , Masahiro Ikeda , Hiroshi Kuga , Eiji Kumazawa , Akiko Togo
IPC分类号： A61K47/48 , A01N43/04 , A61K31/715 , A61K38/00
CPC分类号： A61K47/61
摘要： A drug complex characterized in that a residue of a drug compound such as antineoplastic agents and a carboxy(C1-4)alkyldextran polyalcohol obtained by treating a dextran under conditions that enable substantially complete polyalcoholization are bound to each other by means of a spacer comprising an amino acid or a spacer comprising peptide-bonded 2 to 8 amino acids. Said complex is characterized in that it has excellent selectivity to tumorous sites so as to exhibit high antineoplastic activity and also achieves reduced appearance of toxicity.
摘要翻译：一种药物复合物，其特征在于药物化合物如抗肿瘤剂和通过在能够基本上完全多元醇化的条件下处理葡聚糖而获得的羧基（C 1-4）烷基葡聚糖多元醇的残基通过包含氨基酸或包含肽键合的2至8个氨基酸的间隔子。所述复合物的特征在于其对肿瘤部位具有优异的选择性，从而表现出高的抗肿瘤活性，并且还实现了毒性的降低。

3. 发明授权

US07041818B2 DDS compound and method for measurement thereof 失效
标题翻译： DDS化合物及其测定方法
公开(公告)号：US07041818B2
公开(公告)日：2006-05-09
申请号：US10822661
申请日：2004-04-13
申请人： Hiroshi Susaki , Kazuhiro Inoue , Hiroshi Kuga , Masahiro Ikeda , Yoshinobu Shiose
发明人： Hiroshi Susaki , Kazuhiro Inoue , Hiroshi Kuga , Masahiro Ikeda , Yoshinobu Shiose
IPC分类号： A61K31/47 , A61K47/26 , A61K47/30 , A61K47/48
CPC分类号： A61K31/4745 , A61K47/61 , A61K47/65 , C08B37/0021
摘要： A DDS compound comprising a carboxy(C1-4)alkyldextran polyalcohol modified with a saccharide compound and a residue of drug compound bound to the carboxy(C1-4)alkyldextran polyalcohol, and a method for measuring a DDS compound in which a polymer carrier and a residue of drug compound are bound to each other by means of a spacer comprising 2 to 8 amino acids linked by peptide bond(s), which comprises the steps of treating the DDS compound with a peptidase, and measuring the resulting hydrolysate.
摘要翻译：包含用糖类化合物改性的羧基（C 1-4烷基）葡聚糖多元醇和与羧基（C 1-4烷基）葡聚糖结合的药物化合物残基的DDS化合物多元醇，以及测定DDS化合物的方法，其中聚合物载体和药物化合物的残基通过包含通过肽键连接的2-8个氨基酸的间隔物彼此结合，所述间隔基包括以下步骤：用肽酶处理DDS化合物，并测量所得的水解产物。

4. 发明授权

US06835807B1 Drug complex and drug delivery system 失效
标题翻译：药物复合物和药物输送系统
公开(公告)号：US06835807B1
公开(公告)日：2004-12-28
申请号：US09674526
申请日：2001-02-13
申请人： Hiroshi Susaki , Kazuhiro Inoue , Hiroshi Kuga
发明人： Hiroshi Susaki , Kazuhiro Inoue , Hiroshi Kuga
IPC分类号： A61K900
CPC分类号： A61K47/62 , A61K47/56 , A61K47/61 , A61K47/65
摘要： A drug complex useful as a DDS compound, which is represented by the following formula: A-R—NH—Y—CH2—O—CO-Q, wherein A is a polymer as a drug carrier; R is a spacer, wherein the spacer is an amino acid or an oligopeptide comprising 2 to 8 amino acids; Y is phenylene group which may be substituted; and Q is a residue of a drug compound such as antineoplastic agents. The complex provides rapid and site-selective release of a drug compound such as antineoplastic or anti-inflammatory agents and surely exhibits expected efficacy.
摘要翻译：用作DDS化合物的药物复合物，其由下式表示：A-R-NH-Y-CH 2 -O-CO-Q，其中A是作为药物载体的聚合物; R是间隔基，其中间隔基是氨基酸或包含2-8个氨基酸的寡肽; Y为可被取代的亚苯基; Q是药物化合物的残留物，例如抗肿瘤剂。该复合物提供药物化合物如抗肿瘤药物或抗炎药物的快速和选择性释放，并且肯定具有预期的疗效。

5. 发明授权

US06291671B1 Process for producing drug complexes 失效
标题翻译：生产药物复合物的方法
公开(公告)号：US06291671B1
公开(公告)日：2001-09-18
申请号：US09147341
申请日：1999-03-22
申请人： Kazuhiro Inoue , Hiroshi Susaki , Masahiro Ikeda
发明人： Kazuhiro Inoue , Hiroshi Susaki , Masahiro Ikeda
IPC分类号： C08B3702
CPC分类号： A61K47/61
摘要： A method for preparing a drug complex in which a polysaccharide derivative having carboxyl groups and a residue of a drug compound are bound to each other by means of a spacer comprising an amino acid or a spacer comprising peptide-bonded 2 to 8 amino acids, or a drug complex in which a polysaccharide derivative having carboxyl groups and a residue of a drug compound are bound to each other without the spacer, characterized in that an organic amine salt of the polysaccharide derivative having carboxyl groups is reacted with the drug compound or the spacer bound to the drug compound in a non-aqueous system. The reaction between the polysaccharide derivative having carboxyl groups and the drug compound bound with the spacer or the like can be carried out in high yields, and when a drug compound having a lactone ring is subjected to the reaction, side reactions can be reduced.
摘要翻译：一种制备药物复合物的方法，其中具有羧基的多糖衍生物和药物化合物的残基通过包含氨基酸或包含肽键合的2-8个氨基酸的间隔子的间隔物彼此结合，或其中具有羧基的多糖衍生物和药物化合物的残基在没有间隔基的情况下彼此结合的药物复合物，其特征在于，具有羧基的多糖衍生物的有机胺盐与药物化合物或间隔基在非水系统中与药物化合物结合。具有羧基的多糖衍生物与与间隔物等结合的药物化合物之间的反应可以高收率地进行，当使具有内酯环的药物化合物进行反应时，可以减少副反应。

6. 发明申请

US20120245152A1 3-(BIARYOXY)PROPIONIC ACID DERIVATIVE 有权
标题翻译： 3-（二羟基）丙酸衍生物
公开(公告)号：US20120245152A1
公开(公告)日：2012-09-27
申请号：US13393018
申请日：2010-08-27
申请人： Tatsuya Nishi , Masashi Hasegawa , Yumi Shinagawa-ku , Yuichi Ochiai , Ryoko Kitazawa , Hiroshi Susaki
发明人： Tatsuya Nishi , Masashi Hasegawa , Yumi Shinagawa-ku , Yuichi Ochiai , Ryoko Kitazawa , Hiroshi Susaki
IPC分类号： A61K31/5365 , C07D471/04 , A61P7/02 , A61K31/542 , C07D498/04 , A61K31/4375 , C07D513/04
CPC分类号： C07D413/04 , C07D401/04 , C07D471/04 , C07D498/04 , C07D513/04
摘要： A compound of the general formula (I): [wherein, R1 represents a halogen atom, or the like, R2 represents a hydrogen atom, or the like, R3 and R4, each independently, represent a hydrogen atom, a C1-4 alkyl group, or the like, R5 represents a hydrogen atom, a halogen atom, or the like, R6 represents a hydrogen atom, a halogen atom, or the like, R7 and R8, each independently, represent a hydrogen atom, a halogen atom, or the like, R9 and R10, each independently, represent a hydrogen atom, a C1-4 alkyl group, R11 and R12, each independently, represent a hydrogen atom, a C1-4 alkyl group, or the like, X represents an oxygen atom, a group —CH2—, or the like, Y represents a nitrogen atom, a group ═CH—, or the like, and Z represents a nitrogen atom, or the like] or a pharmacologically acceptable salt thereof, which has an excellent suppressive action on platelet aggregation, and is useful for prevention and/or treatment of thromboembolism.
摘要翻译：通式（I）的化合物：[其中，R 1表示卤素原子等，R 2表示氢原子等，R 3和R 4各自独立地表示氢原子，C 1-4烷基基团等，R 5表示氢原子，卤素原子等，R 6表示氢原子，卤素原子等，R 7和R 8各自独立地表示氢原子，卤素原子， R 9和R 10各自独立地表示氢原子，C 1-4烷基，R 11和R 12各自独立地表示氢原子，C 1-4烷基等，X表示氧原子，基团-CH 2 - 等，Y表示氮原子，基团-CH-等，Z表示氮原子等]或其药理学上可接受的盐，其具有优异的对血小板聚集的抑制作用，并且可用于预防和/或治疗血栓栓塞。

7. 发明授权

US5583218A Carbapenem derivatives 失效
标题翻译：卡巴培南衍生物
公开(公告)号：US5583218A
公开(公告)日：1996-12-10
申请号：US601142
申请日：1996-02-13
申请人： Makoto Takemura , Toshiyuki Nishi , Hiroshi Susaki , Youhei Ishida , Hiroko Koda , Takeshi Hayano
发明人： Makoto Takemura , Toshiyuki Nishi , Hiroshi Susaki , Youhei Ishida , Hiroko Koda , Takeshi Hayano
IPC分类号： C07D477/20 , C07D519/00 , C07D519/06 , C07D487/01
CPC分类号： C07D477/20
摘要： Carbapenem derivatives of formula (I): ##STR1## wherein (a) R.sub.1 is a hydrogen atom, an alkyl group of from 1 to 6 carbon atoms, a hydroxy-lower alkyl group or a protected hydroxy-lower alkyl group of from 1 to 6 carbon atoms in its alkyl moiety, (b) COOR.sub.2 is a carboxyl group, a carboxylate anion or a protected carboxyl group, (c) R.sub.3 is an alkyl group of from 1 to 6 carbon atoms and (d) R.sub.4 is a substituted or unsubstituted heterobicyclic group of formula (II): ##STR2## in which the partial structure ##STR3## is a 5- or 6-membered, saturated or unsaturated, nitrogen-containing heterocycle containing 1 to 4 hereto atoms each selected from the group consisting of oxygen, sulfur and nitrogen, at least one hetero atom being nitrogen, and is which R.sub.5 and R.sub.6 each is a hydrogen atom or an appropriate substituent, any isomeric form thereof, and pharmacologically acceptable salts thereof are potent and stable antimicrobial agents.
摘要翻译：式（I）的碳青霉烯衍生物：其中（a）R 1是氢原子，1至6个碳原子的烷基，羟基 - 低级烷基或被保护的羟基 - 低级烷基（b）COOR2是羧基，羧酸根阴离子或受保护的羧基，（c）R3是1-6个碳原子的烷基，（d）R4是取代或未取代的式（II）的杂双环基团：其中部分结构“IMAGE”是每个含有1至4个原子的5或6元饱和或不饱和的含氮杂环，选自氧，硫和氮，至少一个杂原子是氮，R5和R6各自是氢原子或适当的取代基，其任何异构形式及其药理学上可接受的盐是有效和稳定的抗菌剂。

8. 发明授权

US08729095B2 3-(biaryloxy)propionic acid derivatives for prevention and/or treatment of thromboembolic diseases 有权
标题翻译： 3-（二芳氧基）丙酸衍生物，用于预防和/或治疗血栓栓塞性疾病
公开(公告)号：US08729095B2
公开(公告)日：2014-05-20
申请号：US13393018
申请日：2010-08-27
申请人： Tatsuya Nishi , Masashi Hasegawa , Yumi Nakamoto , Yuichi Ochiai , Ryoko Kitazawa , Hiroshi Susaki
发明人： Tatsuya Nishi , Masashi Hasegawa , Yumi Nakamoto , Yuichi Ochiai , Ryoko Kitazawa , Hiroshi Susaki
IPC分类号： A61K31/44
CPC分类号： C07D413/04 , C07D401/04 , C07D471/04 , C07D498/04 , C07D513/04
摘要： A compound of the general formula (I): [wherein, R1 represents a halogen atom, or the like, R2 represents a hydrogen atom, or the like, R3 and R4, each independently, represent a hydrogen atom, a C1-4 alkyl group, or the like, R5 represents a hydrogen atom, a halogen atom, or the like, R6 represents a hydrogen atom, a halogen atom, or the like, R7 and R8, each independently, represent a hydrogen atom, a halogen atom, or the like, R9 and R10, each independently, represent a hydrogen atom, a C1-4 alkyl group, R11 and R12, each independently, represent a hydrogen atom, a C1-4 alkyl group, or the like, X represents an oxygen atom, a group —CH2—, or the like, Y represents a nitrogen atom, a group ═CH—, or the like, and Z represents a nitrogen atom, or the like] or a pharmacologically acceptable salt thereof, which has an excellent suppressive action on platelet aggregation, and is useful for prevention and/or treatment of thromboembolism.
摘要翻译：通式（I）的化合物：[其中，R 1表示卤素原子等，R 2表示氢原子等，R 3和R 4各自独立地表示氢原子，C 1-4烷基基团等，R 5表示氢原子，卤素原子等，R 6表示氢原子，卤素原子等，R 7和R 8各自独立地表示氢原子，卤素原子， R 9和R 10各自独立地表示氢原子，C 1-4烷基，R 11和R 12各自独立地表示氢原子，C 1-4烷基等，X表示氧原子，基团-CH 2 - 等，Y表示氮原子，基团-CH-等，Z表示氮原子等]或其药理学上可接受的盐，其具有优异的对血小板聚集的抑制作用，并且可用于预防和/或治疗血栓栓塞。

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