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1. 发明授权

US08940332B2 High-molecular weight conjugate of podophyllotoxins 有权
标题翻译：鬼臼毒素的高分子量结合物
公开(公告)号：US08940332B2
公开(公告)日：2015-01-27
申请号：US12226962
申请日：2007-05-16
申请人： Masayuki Kitagawa , Keizou Ishikawa , Keiichirou Yamamoto , Kazutoshi Takashio , Masao Shibata
发明人： Masayuki Kitagawa , Keizou Ishikawa , Keiichirou Yamamoto , Kazutoshi Takashio , Masao Shibata
IPC分类号： A61K9/14 , A61K31/7048 , A61K9/00 , A61K31/365 , A61K47/48 , C08G65/331 , C08G65/332 , C08G73/10 , C08G83/00 , C08L71/02 , A61K47/26 , C08L77/00
CPC分类号： A61K31/7048 , A61K9/0019 , A61K31/365 , A61K47/26 , A61K47/60 , C08G65/331 , C08G65/3314 , C08G65/3324 , C08G73/1092 , C08G83/00 , C08L71/02 , C08L77/00 , C08L2203/02 , C08L2205/05 , C08L2666/20
摘要： A novel podophyllotoxin derivative, which is capable of releasing a drug without depending on biological enzymes and can be expected to have an effective therapeutic effect and is soluble in water has been demanded. A polymer having a polyethyleneglycol structural unit and two or more succinic monoamide structural units, particularly a polymer conjugate of a podophyllotoxin in which a carboxylic acid group of polyethyleneglycol/polyaspartic acid copolymer and a hydroxyl group of podophyllotoxin and linked via an ester bond is provided.
摘要翻译：已经要求一种新颖的鬼臼毒素衍生物，其能够释放药物而不依赖于生物酶，并且可以预期其具有有效的治疗效果并且可溶于水。具有聚乙二醇结构单元和两种或更多种琥珀酸单酰胺结构单元的聚合物，特别是鬼臼毒素的聚合物缀合物，其中聚乙二醇/聚天冬氨酸共聚物的羧酸基和鬼臼毒酚羟基并通过酯键连接。

2. 发明申请

US20090162313A1 High-Molecular Weight Conjugate of Podophyllotoxins 有权
标题翻译：鬼臼毒素的高分子量偶联物
公开(公告)号：US20090162313A1
公开(公告)日：2009-06-25
申请号：US12226962
申请日：2007-05-16
申请人： Masayuki Kitagawa , Keizou Ishikawa , Keiichirou Yamamoto , Kazutoshi Takashio , Masao Shibata
发明人： Masayuki Kitagawa , Keizou Ishikawa , Keiichirou Yamamoto , Kazutoshi Takashio , Masao Shibata
IPC分类号： A61K31/765 , A61P35/00
CPC分类号： A61K31/7048 , A61K9/0019 , A61K31/365 , A61K47/26 , A61K47/60 , C08G65/331 , C08G65/3314 , C08G65/3324 , C08G73/1092 , C08G83/00 , C08L71/02 , C08L77/00 , C08L2203/02 , C08L2205/05 , C08L2666/20
摘要： [PROBLEMS] A novel podophyllotoxin derivative, which is capable of releasing a drug without depending on biological enzymes and can be expected to have an effective therapeutic effect and is soluble in water has been demanded.[MEANS FOR SOLVING PROBLEMS] A polymer having a polyethyleneglycol structural unit and two or more succinic monoamide structural units, particularly a polymer conjugate of a podophyllotoxin in which a carboxylic acid group of polyethyleneglycol/polyaspartic acid copolymer and a hydroxyl group of podophyllotoxin and linked via an ester bond is provided.
摘要翻译： [问题]需要能够释放药物而不依赖于生物酶并且可以预期具有有效治疗效果并且可溶于水的新型鬼臼毒素衍生物。用于解决问题的方法具有聚乙二醇结构单元和两种或更多种琥珀酸单酰胺结构单元的聚合物，特别是鬼臼毒素的聚合物缀合物，其中聚乙二醇/聚天冬氨酸共聚物的羧酸基和鬼臼毒素的羟基和连接的通孔提供酯键。

3. 发明授权

US07700709B2 Polymeric derivative of cytidine metabolic antagonist 有权
标题翻译：胞苷代谢拮抗剂的聚合衍生物
公开(公告)号：US07700709B2
公开(公告)日：2010-04-20
申请号：US11919912
申请日：2006-04-27
申请人： Akira Masuda , Takeshi Onda , Hiroko Mashiba , Keiichirou Yamamoto , Kazutoshi Takashio
发明人： Akira Masuda , Takeshi Onda , Hiroko Mashiba , Keiichirou Yamamoto , Kazutoshi Takashio
IPC分类号： C08G61/12
CPC分类号： C08G73/0233 , A61K47/60 , A61K47/645 , C08G65/329 , C08G65/3332 , C08G73/028
摘要： A derivative of a cytidine metabolic antagonist which can exert a high therapeutic effect at a low dose. A polymeric derivative of a cytidine metabolic antagonist which comprises a polymeric compound having a polyethylene glycol moiety and a polymer moiety having a carboxyl group in a side chain and a cytidine metabolic antagonist, which has such a structure that the carboxyl group in the side chain of the polymeric compound and an amino group in the cytidine metabolic antagonist are bound together to form an amide bond.
摘要翻译：胞苷代谢拮抗剂的衍生物，其可以在低剂量下发挥高治疗效果。胞苷代谢拮抗剂的聚合衍生物，其包含具有聚乙二醇部分的聚合化合物和在侧链具有羧基的聚合物部分和胞苷代谢拮抗剂，其具有以下结构：侧链中的羧基胞苷代谢拮抗剂中的高分子化合物和氨基结合在一起形成酰胺键。

4. 发明申请

US20090012252A1 Polymeric Derivative of Cytidine Metabolic Antagonist 有权
标题翻译：胞苷代谢拮抗剂的聚合衍生物
公开(公告)号：US20090012252A1
公开(公告)日：2009-01-08
申请号：US11919912
申请日：2006-04-27
申请人： Akira Masuda , Takeshi Onda , Hiroko Mashiba , Keiichirou Yamamoto , Kazutoshi Takashio
发明人： Akira Masuda , Takeshi Onda , Hiroko Mashiba , Keiichirou Yamamoto , Kazutoshi Takashio
IPC分类号： C08G83/00
CPC分类号： C08G73/0233 , A61K47/60 , A61K47/645 , C08G65/329 , C08G65/3332 , C08G73/028
摘要： [PROBLEMS] To provide a derivative of a cytidine metabolic antagonist which can exert a high therapeutic effect at a low dose.[MEANS FOR SOLVING PROBLEMS] A polymeric derivative of a cytidine metabolic antagonist which comprises a polymeric compound having a polyethylene glycol moiety and a polymer moiety having a carboxyl group in a side chain and a cytidine metabolic antagonist, which has such a structure that the carboxyl group in the side chain of the polymeric compound and an amino group in the cytidine metabolic antagonist are bound together to form an amide bond.
摘要翻译： [问题]提供可以以低剂量发挥高治疗效果的胞苷代谢拮抗剂的衍生物。解决问题的手段胞苷代谢拮抗剂的聚合衍生物包含具有聚乙二醇部分和侧链中具有羧基的聚合物部分和胞苷代谢拮抗剂的聚合物，其具有以下结构：羧基聚合化合物的侧链基团和胞苷代谢拮抗剂中的氨基结合在一起形成酰胺键。

5. 发明授权

US09346923B2 Method for manufacturing block copolymer 有权
标题翻译：制备嵌段共聚物的方法
公开(公告)号：US09346923B2
公开(公告)日：2016-05-24
申请号：US14241924
申请日：2012-08-31
申请人： Keiichirou Yamamoto , Masayuki Kitagawa
发明人： Keiichirou Yamamoto , Masayuki Kitagawa
IPC分类号： C08G65/333 , C08G73/10 , C08G81/00 , C08G69/10 , C08G69/40 , C08G73/14
CPC分类号： C08G81/00 , C08G65/3315 , C08G65/333 , C08G65/33334 , C08G69/10 , C08G69/40 , C08G73/14
摘要： Providing a method for producing a compound represented by formula (1) from a compound represented by formula (2), by which the additive amount of an aryl (C1-C8) alkyl alcohol which may have a substituent and the amount of residual carboxyl groups of pAsp (polyaspartic acid) are controlled.A production method including obtaining a compound represented by formula (1) by allowing a compound represented by formula (2) to react with an aryl (C1-C8) alkyl alcohol which may have a substituent, and a carbodiimide-based compound in an amount of 2(x+y) equivalents or more relative to the amount of carboxyl groups in formula (2) (sum of x and y), in a solvent at 15° C. to 30° C. for 2 hours to 48 hours, is used.
摘要翻译：提供由式（2）表示的化合物制备由式（1）表示的化合物的方法，其中可以具有取代基的芳基（C1-C8）烷基醇的添加量和残留的羧基的量的pAsp（聚天冬氨酸）被控制。一种制备方法，包括通过使式（2）表示的化合物与可以具有取代基的芳基（C1-C8）烷基醇反应得到式（1）表示的化合物和碳二亚胺类化合物相对于式（2）中的羧基量（x和y的总和）为2（x + y）当量或更多，在15℃至30℃的溶剂中2小时至48小时，用来。

6. 发明申请

US20140288244A1 Method For Manufacturing Block Copolymer 有权
标题翻译：制备嵌段共聚物的方法
公开(公告)号：US20140288244A1
公开(公告)日：2014-09-25
申请号：US14241924
申请日：2012-08-31
申请人： Keiichirou Yamamoto , Masayuki Kitagawa
发明人： Keiichirou Yamamoto , Masayuki Kitagawa
IPC分类号： C08G81/00
CPC分类号： C08G81/00 , C08G65/3315 , C08G65/333 , C08G65/33334 , C08G69/10 , C08G69/40 , C08G73/14
摘要： Providing a method for producing a compound represented by formula (1) from a compound represented by formula (2), by which the additive amount of an aryl (C1-C8) alkyl alcohol which may have a substituent and the amount of residual carboxyl groups of pAsp (polyaspartic acid) are controlled.A production method including obtaining a compound represented by formula (1) by allowing a compound represented by formula (2) to react with an aryl (C1-C8) alkyl alcohol which may have a substituent, and a carbodiimide-based compound in an amount of 2(x+y) equivalents or more relative to the amount of carboxyl groups in formula (2) (sum of x and y), in a solvent at 15° C. to 30° C. for 2 hours to 48 hours, is used.
摘要翻译：提供由式（2）表示的化合物制备由式（1）表示的化合物的方法，其中可以具有取代基的芳基（C1-C8）烷基醇的添加量和残留的羧基的量的pAsp（聚天冬氨酸）被控制。一种制备方法，包括通过使式（2）表示的化合物与可以具有取代基的芳基（C1-C8）烷基醇反应得到式（1）表示的化合物和碳二亚胺类化合物相对于式（2）中的羧基量（x和y的总和）为2（x + y）当量或更多，在15℃至30℃的溶剂中2小时至48小时，用来。

7. 发明申请

US20090239782A1 High-molecular weight conjugate of resorcinol derivatives 审中-公开
标题翻译：间苯二酚衍生物的高分子量缀合物
公开(公告)号：US20090239782A1
公开(公告)日：2009-09-24
申请号：US12311086
申请日：2007-09-27
申请人： Masaharu Nakamura , Masayuki Kitagawa , Keiichirou Yamamoto , Chieko Seno
发明人： Masaharu Nakamura , Masayuki Kitagawa , Keiichirou Yamamoto , Chieko Seno
IPC分类号： A61K38/02 , C07K2/00 , A61P35/00
CPC分类号： A61K31/787 , C08G69/10 , C08G73/1092 , C08G81/00 , C08G2650/38
摘要： Provided is a high-molecular weight conjugate of resorcinol derivatives which is excellent in water solubility and stability and has high antitumor activity even when used in a smaller total drug amount than the resorcinol derivatives. The high-molecular weight conjugate of resorcinol derivatives comprises a structure in which a carboxyl group of polymer moiety having a carboxyl group in the side chain and polyethylene glycol moiety is linked to a hydroxyl group of resorcinol derivatives via an ester bond.
摘要翻译：提供了间苯二酚衍生物的高分子量缀合物，其水溶性和稳定性优异，并且即使以比间苯二酚衍生物更小的总药物量使用也具有高抗肿瘤活性。间苯二酚衍生物的高分子量缀合物包括其侧链中具有羧基的聚合物部分的羧基和聚乙二醇部分通过酯键与间苯二酚衍生物的羟基连接的结构。

8. 发明授权

US07348318B2 α-Amino-N-(diaminophosphinyl)lactam derivatives 失效
标题翻译： α-氨基-N-（二氨基氧膦基）内酰胺衍生物
公开(公告)号：US07348318B2
公开(公告)日：2008-03-25
申请号：US10508573
申请日：2003-03-24
申请人： Masatoshi Abe , Masashi Nagai , Keiichirou Yamamoto , Chihiro Nishimura
发明人： Masatoshi Abe , Masashi Nagai , Keiichirou Yamamoto , Chihiro Nishimura
IPC分类号： A61K31/675 , A61K31/45 , C07D211/92 , C07F9/06
CPC分类号： A61K31/675 , C07F9/5532 , C07F9/568 , C07F9/572 , C07F9/59
摘要： There are disclosed a novel α-amino-N-(diaminophosphinyl)lactam derivative represented by general formula (1): wherein, for example, A is a hydrogen atom or a substituent such as a lower alkyl group or the like; W, X, Y and Z are independently a hydrogen atom or a substituent such as a lower alkyl group, aryl group, arylacyl group, arylaminocarbonyl group or the like; and Q is —(CH2)n— wherein n is 0 to 3, or its salt, and a therapeutic agent and a prophylactic agent for myelosuppression, a therapeutic agent for infectious diseases, an agent for increasing the number of leukocytes and a dipeptidyl peptidase IV inhibitor which comprise the above-mentioned derivative or salt thereof as an active ingredient.
摘要翻译：公开了通式（1）表示的新型α-氨基-N-（二氨基膦氧基）内酰胺衍生物：其中，例如，A为氢原子或低级烷基等取代基; W，X，Y和Z独立地为氢原子或低级烷基，芳基，芳基酰基，芳基氨基羰基等取代基。和Q为 - （CH 2）n - n - 其中n为0至3，或其盐，治疗剂和骨髓抑制预防剂，治疗剂感染性疾病，增加白细胞数量的药剂和包含上述衍生物或其盐作为活性成分的二肽基肽酶IV抑制剂。

9. 发明授权

US07531657B2 Method for preparing sulphostin and analogue thereof or preparation intermediate thereof 失效
标题翻译：磺普钠及其类似物的制备方法或其制备方法
公开(公告)号：US07531657B2
公开(公告)日：2009-05-12
申请号：US10498272
申请日：2002-12-16
申请人： Masashi Nagai , Hiroko Yamazaki , Keiichirou Yamamoto , Masatoshi Abe
发明人： Masashi Nagai , Hiroko Yamazaki , Keiichirou Yamamoto , Masatoshi Abe
IPC分类号： C07F9/00 , C07F9/02 , C07D205/08 , C07D223/12
CPC分类号： C07C215/30 , C07B2200/07 , C07F9/5532 , C07F9/568 , C07F9/572 , C07F9/59 , Y02P20/55
摘要： A method for preparing a compound represented by the following general formula (5) where, n is an integer of 0 to 3; and Y represents a protecting group for an amino group, the method including the steps of reacting a compound represented by the following general formula (3) where n and Y are as described above, with a silylating agent, and subsequently reacting it with P (═O) T3, where T represents a halogen atom, and further with ammonia. A method for preparing an optically active intermediate of sulphostin or an analogue thereof, which is an optically active amine salt of an optically active compound represented by the following general formula (8) where n is integer of 0 to 3; Y represents protecting group for the amino group; and each configuration at C* and P* may be the same or different and indicates S or R, the method including reacting a compound represented by the following general formula (7) where n and Y are as described above; and the configuration of C* indicates either of S or R, with an optically active amine, and resolving the formed diastereomeric salt by fractional crystallization.
摘要翻译：一种制备由以下通式（5）表示的化合物的方法，其中n为0-3的整数; Y表示氨基的保护基，该方法包括使下述通式（3）表示的化合物（其中n和Y如上所述）与甲硅烷基化剂反应，然后使其与P（ -O）T3，其中T表示卤素原子，并且还含有氨。一种制备光学活性中间体磺酸钠或其类似物的方法，它是由以下通式（8）表示的光学活性化合物的光学活性胺盐，其中n为0-3的整数; Y表示氨基的保护基; 并且C *和P *的每个构型可以相同或不同，表示S或R，该方法包括使由以下通式（7）表示的化合物，其中n和Y如上所述; 并且C *的构型表示S或R中的任一个与光学活性胺，并且通过分级结晶拆分形成的非对映体盐。

10. 发明申请

US20050164989A1 Novel $g(a)-amino-n-(diaminophosphinyl) lactam derivative 失效
标题翻译：新型$ g（a） - 氨基 - （（二氨基氧膦基））内酰胺衍生物
公开(公告)号：US20050164989A1
公开(公告)日：2005-07-28
申请号：US10508573
申请日：2003-03-24
申请人： Masatoshi Abe , Masashi Nagai , Keiichirou Yamamoto , Chihiro Nishimura
发明人： Masatoshi Abe , Masashi Nagai , Keiichirou Yamamoto , Chihiro Nishimura
IPC分类号： A61K31/675 , A61P3/10 , A61P5/00 , A61P7/00 , A61P7/06 , A61P29/00 , A61P31/00 , A61P31/18 , A61P37/02 , A61P37/08 , A61P43/00 , C07F9/553 , C07F9/568 , C07F9/572 , C07F9/59
CPC分类号： A61K31/675 , C07F9/5532 , C07F9/568 , C07F9/572 , C07F9/59
摘要： There are disclosed a novel α-amino-N-(diaminophosphinyl)lactam derivative represented by general formula (1): wherein, for example, A is a hydrogen atom or a substituent such as a lower alkyl group or the like; W, X, Y and Z are independently a hydrogen atom or a substituent such as a lower alkyl group, aryl group, arylacyl group, arylaminocarbonyl group or the like; and Q is —(CH2)n— wherein n is 0 to 3, or its salt, and a therapeutic agent and a prophylactic agent for myelosuppression, a therapeutic agent for infectious diseases, an agent for increasing the number of leukocytes and a dipeptidyl peptidase IV inhibitor which comprise the above-mentioned derivative or salt thereof as an active ingredient.
摘要翻译：公开了通式（1）表示的新型α-氨基-N-（二氨基膦氧基）内酰胺衍生物：其中，例如，A为氢原子或低级烷基等取代基; W，X，Y和Z独立地为氢原子或低级烷基，芳基，芳基酰基，芳基氨基羰基等取代基。和Q为 - （CH 2）n - n - 其中n为0至3，或其盐，治疗剂和骨髓抑制预防剂，治疗剂感染性疾病，增加白细胞数量的药剂和包含上述衍生物或其盐作为活性成分的二肽基肽酶IV抑制剂。

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