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1. 发明授权

US4086417A Cytidine nucleotide derivatives 失效
标题翻译：胞苷核苷酸衍生物
公开(公告)号：US4086417A
公开(公告)日：1978-04-25
申请号：US622794
申请日：1975-10-15
申请人： Torao Ishida , Minoru Akiyama , Yoshio Sakurai , Shigeru Tsukagoshi
发明人： Torao Ishida , Minoru Akiyama , Yoshio Sakurai , Shigeru Tsukagoshi
IPC分类号： C07H19/10
CPC分类号： C07H19/10
摘要： A nucleotide derivative represented by the general formula: ##STR1## wherein R represents an acyl group having 14 - 22 carbon atoms and having an aliphatic acyl moiety; X represents a hydrogen atom, a halogen atom, an alkyl group having 1 - 4 carbon atoms, or a trifluoromethyl group; and at least one, but not all, of Y.sub.1, Y.sub.2, and Y.sub.3 represents a phosphate, a pyrophosphate, a triphosphate, or a salt thereof, the balance of Y.sub.1, Y.sub.2 and Y.sub.3 representing a hydroxyl group; or in case of ribosyl, Y.sub.1 and Y.sub.3, or Y.sub.2 and Y.sub.3 represent, at the same time, the aforesaid phosphate, pyrophosphate, triphosphate or salt thereof and the remaining group of Y.sub.1, Y.sub.2 or Y.sub.3 represents a hydroxyl group; or in case of arabinosyl, Y.sub.1 and Y.sub.2, or Y.sub.2 and Y.sub.3 represent, at the same time, the aforesaid phosphate, pyrophosphate, triphosphate or salt therof and the remaining group of Y.sub.1, Y.sub.2 or Y.sub.3 represents a hydroxyl group. The nontoxic salts of these phosphates are useful as an antileukemialagent for mice which is soluble in water and has high stability.
摘要翻译：由以下通式表示的核苷酸衍生物：其中R表示具有14-22个碳原子且具有脂族酰基部分的酰基; X表示氢原子，卤素原子，具有1-4个碳原子的烷基或三氟甲基; Y1，Y2和Y3中的至少一个但不是全部表示磷酸酯，焦磷酸酯，三磷酸酯或其盐，余量的Y1，Y2和Y3表示羟基; 或在核糖基，Y1和Y3的情况下，或Y2和Y3同时表示上述磷酸盐，焦磷酸盐，三磷酸盐或其盐，剩余的Y 1，Y 2或Y 3基团表示羟基; 或在阿糖基，Y1和Y2的情况下，或Y2和Y3同时表示上述磷酸盐，焦磷酸盐，三磷酸盐或盐，而剩余的Y1，Y2或Y3基团表示羟基。这些磷酸盐的无毒盐可用作可溶于水并具有高稳定性的小鼠的抗白血病细胞。

2. 发明授权

US4097665A Diacylnucleosides and process for preparing the same 失效
标题翻译：二酰基核苷及其制备方法
公开(公告)号：US4097665A
公开(公告)日：1978-06-27
申请号：US634706
申请日：1975-11-24
申请人： Torao Ishida , Minoru Akiyama , Daikichi Nishimura , Hiroshi Hayashi , Yoshio Sakurai , Shigeru Tsukagoshi
发明人： Torao Ishida , Minoru Akiyama , Daikichi Nishimura , Hiroshi Hayashi , Yoshio Sakurai , Shigeru Tsukagoshi
IPC分类号： C07H19/09 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61K31/7068 , A61K31/7076 , A61P35/02 , C07H19/06 , C07H19/20 , C07H19/08
CPC分类号： C07H19/06 , Y02P20/55 , Y10S514/908
摘要： Compounds represented by formula (I) ##STR1## wherein one of Z.sub.1 ', Z.sub.2 ', Z.sub.3 ' and Z.sub.4 ' represents R, another one of Z.sub.1 ', Z.sub.2 ', Z.sub.3 ' and Z.sub.4 ' represents Z, and the remaining two moieties of Z.sub.1 ', Z.sub.2 ', Z.sub.3 ' and Z.sub.4 ' represents a hydrogen atom and/or a protective group, one of R and Z represents A.sub.1 and the other represents A.sub.2, A.sub.1 being an acyl group having 14 to 22 carbon atoms which does not contain a carboxylic group and A.sub.2 being an acyl group having 2 to 14 carbon atoms and having one carboxyl group, X represents a hydrogen atom or a halogen atom (hereinafter referred to as Compound Ia); a 2,2'-anhydro product of Compound Ia wherein Z.sub.2 ' represents a hydrogen atom (hereinafter referred to as Compound Ib); an arabinosylation product of Compound Ia (hereinafter referred to as Compound Ic); a deamination product of Compound Ia (hereinafter referred to as Compound Id); a 2'-deoxy product of Compound Id wherein Z.sub.2 ' represents a hydrogen atom (hereinafter referred to as Compound Ie); a salt of Compound Ia, Ib, Ic, or Id or Ie having an A.sub.2 group with a base (hereinafter referred to as Compound If); and a salt of Compound Ia, Ib or Ic wherein Z.sub.1 ' represents a hydrogen atom with an acid (hereinafter referred to as Compound Ih); and processes for preparing the same.
摘要翻译：由式（I）表示的化合物其中Z1'，Z2'，Z3'和Z4'之一表示R，Z1'，Z2'，Z3'和Z4'中的另一个表示Z，剩余的 Z1'，Z2'，Z3'和Z4'的两个部分表示氢原子和/或保护基，R和Z之一表示A1，另一个表示A2，A1表示具有14-22个碳原子的酰基，不含羧基，A2为碳原子数2〜14的酰基，具有1个羧基，X表示氢原子或卤素原子（以下称为化合物Ia）。化合物Ia的2,2'-脱水产物，其中Z2'表示氢原子（以下称为化合物Ib）; 化合物Ia的阿拉伯糖基化产物（以下称为化合物Ic）; 化合物Ia的脱氨产物（以下称为化合物Id）; 化合物Id的2'-脱氧产物，其中Z2'表示氢原子（以下称为化合物Ie）; 具有A2基团的化合物Ia，Ib，Ic或Id或Ie的盐（以下称为化合物If）; 和化合物Ia，Ib或Ic的盐，其中Z1'表示氢原子与酸（以下称为化合物Ih）; 及其制备方法。

3. 发明授权

US3991045A N.sup.4 -acylarabinonucleosides 失效
标题翻译： N {HU 4 {B-酰基阿糖胞苷
公开(公告)号：US3991045A
公开(公告)日：1976-11-09
申请号：US540294
申请日：1975-01-10
申请人： Torao Ishida , Kageyasu Akashi , Koichi Yoshida , Minoru Akiyama , Yoshio Sakurai , Shigeru Tsukagoshi
发明人： Torao Ishida , Kageyasu Akashi , Koichi Yoshida , Minoru Akiyama , Yoshio Sakurai , Shigeru Tsukagoshi
IPC分类号： C07H19/06
CPC分类号： C07H19/06
摘要： An N.sup.4 -acyl-1-.beta.-D-arabinofuranosylcytosine having the following formula ##SPC1##Wherein R is an aliphatic acyl group having 3 to 35 carbon atoms. The compounds of this invention are useful as a cancer chemotherapeutic agent for controlling tumors, e.g., in mice, an insecticide, and a fungicidal surface active agent.
摘要翻译：具有下式的N 4 - 酰基-1-β-D-阿拉伯呋喃糖基胞嘧啶R是具有3至35个碳原子的脂族酰基。本发明的化合物可用作控制肿瘤的癌症化学治疗剂，例如在小鼠，杀虫剂和杀真菌剂表面活性剂中。

4. 发明授权

US4520162A Polymeric compounds with sustained anti-tumor activity and a method for the preparation thereof 失效
标题翻译：具有持续抗肿瘤活性的聚合化合物及其制备方法
公开(公告)号：US4520162A
公开(公告)日：1985-05-28
申请号：US651343
申请日：1984-09-17
申请人： Takashi Hirano , Shinichi Ohashi , Satoshi Morimoto , Masaru Shiraki , Keishiro Tsuda , Tomowo Kobayashi , Shigeru Tsukagoshi
发明人： Takashi Hirano , Shinichi Ohashi , Satoshi Morimoto , Masaru Shiraki , Keishiro Tsuda , Tomowo Kobayashi , Shigeru Tsukagoshi
IPC分类号： A61K47/48 , C08F8/30 , C08F8/32
CPC分类号： A61K47/48176 , C08F8/44
摘要： The novel polymeric compound proposed in the invention has a backbone structure formed of a copolymeric moiety of maleic anhydride and divinyl ether and pendant groups thereon derived from an anthracycline-type anti-tumor agent, e.g. adriamycin and daunomycin, or 1-.beta.-D-arabinofuranosylcytosine bonded to the maleic anhydride units in the backbone structure by forming amide linkages, the remaining anhydride units in the backbone structure being hydrolyzed into free acid form or a salt thereof. Both in vitro and in vivo tests indicate that the anti-tumor active pendant groups in the polymeric compound can be released sustainedly to exhibit the anti-tumor activity with greatly decreased side effects unavoidable when the above mentioned anti-tumor agents as such are administrated to a patient in a relatively large dose.
摘要翻译：本发明中提出的新型聚合物具有由马来酸酐和二乙烯基醚的共聚部分和其上衍生自蒽环类抗肿瘤剂的侧基形成的骨架结构，例如。阿霉素和道诺霉素，或通过形成酰胺键键合到主链结构中的马来酸酐单元的1-β-D-阿拉伯呋喃糖基胞嘧啶，主链结构中剩余的酸酐单元被水解成游离酸形式或其盐。体外和体内试验均表明，当将上述抗肿瘤药物施用于上述抗肿瘤药物时，可以持续释放聚合物中的抗肿瘤活性侧基，以显示抗肿瘤活性，其显着降低的副作用是不可避免的相对较大剂量的患者。

5. 发明授权

US4948784A Platinum containing pullulan derivatives and compositions containing the same 失效
标题翻译：含铂的支链淀粉衍生物和含有其的组合物
公开(公告)号：US4948784A
公开(公告)日：1990-08-14
申请号：US163961
申请日：1988-01-20
申请人： Fumio Mori , Masafumi Okada , Shuji Miki , Iwao Ebashi , Takashi Nishida , Kouichiro Kawai , Tazuko Tashiro , Shigeru Tsukagoshi
发明人： Fumio Mori , Masafumi Okada , Shuji Miki , Iwao Ebashi , Takashi Nishida , Kouichiro Kawai , Tazuko Tashiro , Shigeru Tsukagoshi
IPC分类号： C08B37/00
CPC分类号： C08B37/0018
摘要： A pullulan derivative having one or more active sites resulting from introduction of sulfuric acid, phosphoric acid, a sulfonic acid or a carboxylic acid, wherein one hydrogen atom of the group of the formula ##STR1## occurring at said active sites is partly substituted by a group of the general formula ##STR2## wherein L.sup.1 and L.sup.2 each independently is ammine or a unidentate ligand amine or combinedly represent a bidentate ligand amine and Y is an anionic ligand, and/or two hydrogen atoms of the group ##STR3## or of two ##STR4## groups bound to one and the same carbon atom or to two neighboring carbon atoms as occurring at said active sites are, each independently, partly substituted by a group of the general formula ##STR5## wherein L.sup.1 and L.sup.2 are as defined above, and a pharmacologically acceptable salt thereof.The above compound has anticancer activity and is useful as anticancer agents.The present invention is concerned with said compound, a process for producing the same and a pharmaceutical use thereof.

6. 发明授权

US5100877A Platinum containing pullulan derivatives and pharmaceutical compositions comprising the same 失效
标题翻译：含铂的支链淀粉衍生物和包含其的药物组合物
公开(公告)号：US5100877A
公开(公告)日：1992-03-31
申请号：US282398
申请日：1988-12-05
申请人： Fumio Mori , Masafumi Okada , Shuji Miki , Iwao Ebashi , Takashi Nishida , Kouichiro Kawai , Tazuko Tashiro , Shigeru Tsukagoshi
发明人： Fumio Mori , Masafumi Okada , Shuji Miki , Iwao Ebashi , Takashi Nishida , Kouichiro Kawai , Tazuko Tashiro , Shigeru Tsukagoshi
IPC分类号： C08B37/00
CPC分类号： C08B37/0018 , Y10S514/908
摘要： A pullulan derivative having one or more active sites resulting from introduction of sulfuric acid, phosphoric acid, a sulfonic acid or a carboxylic acid, wherein one hydrogen atom of the group of the formula ##STR1## occurring at said active sites is partly substituted by a group of the general formula ##STR2## wherein L.sup.1 and L.sup.2 each independently is amine or a unidentate ligand amine or combinedly represent a bidentate ligand amine and Y is an anionic ligand, and/or two hydrogen atoms of the group ##STR3## groups bound to one and the same carbon atom or to two neighboring carbon atoms as occurring at said active sites are, each independently, partly substituted by a group of the general formula ##STR4## wherein L.sup.1 and L.sup.2 are as defined above, and a pharmacologically acceptable salt thereof.The above compound has anticancer activity and is useful as anticancer agents.The present invention is concerned with said compound, a process for producing the same and a pharmaceutical use thereof.
摘要翻译：具有由引入硫酸，磷酸，磺酸或羧酸产生的一个或多个活性位点的支链淀粉衍生物，其中在所述活性位点发生的式“IMAGE”基团的一个氢原子部分被通式为“IMAGE”的基团，其中L1和L2各自独立地为胺或一元配体胺，或者组合表示二齿配体胺，Y为阴离子配位体，和/或组中的两个氢原子结合至在所述活性位点处发生的同一个碳原子或两个相邻的碳原子各自独立地部分地被通式“IMAGE”所示的基团取代，其中L1和L2如上所定义，及其药理学上可接受的盐。上述化合物具有抗癌活性，可用作抗癌剂。本发明涉及所述化合物，其制备方法及其药物用途。

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