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1. 发明申请

US20100048708A1 TAMIBAROTENE CAPSULE PREPARATION 有权
标题翻译： TAMIBAROTENE胶囊制剂
公开(公告)号：US20100048708A1
公开(公告)日：2010-02-25
申请号：US12593866
申请日：2008-03-28
申请人： Hisao Ekimoto
发明人： Hisao Ekimoto
IPC分类号： A61K31/196 , A61P35/00
CPC分类号： A61K31/192 , A61K9/4866 , A61K9/4875 , A61K47/10 , A61K47/14
摘要： The present invention provides a practical preparation form of Tamibarotene and dosage form thereof, which exhibit high absorptivity by the body with minimized toxicity, and which are safe and stable without any risk of contamination. It is provided a Tamibarotene capsule preparation which encapsulates a composition comprising an oil component as its base and Tamibarotene as an active ingredient dissolved in the base. It is preferred that the oil component be propylene glycol fatty acid esters or polyethylene glycols. It is also preferred that the Tamibarotene capsule preparation comprise 0.1-50 mg/mL of the Tamibarotene based on the oil component.
摘要翻译：本发明提供了Tamibarotene及其剂型的实用制剂形式，它以体积最小的毒性显示出高吸收性，并且是安全和稳定的，没有任何污染的风险。提供了一种Tamibarotene胶囊制剂，其包含以油组分为基础的组合物和作为活性成分溶解在基质中的Tamibarotene。油成分优选为丙二醇脂肪酸酯或聚乙二醇。还优选的是，Tamibarotene胶囊制剂包含基于油组分的0.1-50mg / mL的Tamibarotene。

2. 发明申请

US20080069901A1 Therapeutic Agent for Metastatic Cancer and Cancer Metastasis Inhibitor 审中-公开
标题翻译：转移癌和癌转移抑制剂的治疗剂
公开(公告)号：US20080069901A1
公开(公告)日：2008-03-20
申请号：US11792519
申请日：2005-12-06
申请人： Hisao Ekimoto
发明人： Hisao Ekimoto
IPC分类号： A61K33/24 , A61P35/00
CPC分类号： A61K31/663 , A61K33/24 , A61K2300/00
摘要： To provide a therapeutic agent for metastatic cancer and a cancer metastasis inhibitor which are highly safe and efficaciously treat metastatic cancer and inhibit cancer metastasis, and especially efficaciously treat and inhibit cancer metastasis to bone and liver. There are provided a therapeutic agent for metastatic cancer and a cancer metastasis inhibitor each of which includes a platinum complex having an anticancer activity as an active ingredient. The platinum complex is preferably cisplatin. The therapeutic agent for metastatic cancer is advantageously usable for treating metastatic cancer to bone and/or liver. The cancer metastasis inhibitor is advantageously usable as a cancer metastasis inhibitor for inhibiting metastasis to bone and/or liver. These agents can advantageously further include a bisphosphonate as another active ingredient.
摘要翻译：提供高度安全，有效地治疗转移性癌症并抑制癌症转移的转移癌治疗剂和癌症转移抑制剂，特别是有效治疗和抑制对骨和肝癌的转移。提供了用于转移性癌症的治疗剂和癌症转移抑制剂，其各自包括具有抗癌活性的铂络合物作为活性成分。铂络合物优选为顺铂。用于转移性癌症的治疗剂有利地用于治疗对骨和/或肝的转移性癌症。癌转移抑制剂有利地用作癌转移抑制剂，用于抑制对骨和/或肝的转移。这些试剂可以有利地进一步包括双膦酸盐作为另一活性成分。

3. 发明授权

US5130450A Platinum complexes 失效
标题翻译：铂复合物
公开(公告)号：US5130450A
公开(公告)日：1992-07-14
申请号：US688903
申请日：1991-04-19
申请人： Osamu Kogawa , Kenji Iwata , Hisao Ekimoto , Tadashi Ishii , Kimihiko Takada
发明人： Osamu Kogawa , Kenji Iwata , Hisao Ekimoto , Tadashi Ishii , Kimihiko Takada
IPC分类号： C07F15/00
CPC分类号： C07F15/0093
摘要： A platinum (II) complex represented by the general formula: ##STR1## [wherein A's are each ammonia or two A's jointly represent 1,2-diaminocyclohexane, 1-amino-1-aminomethylcyclohexane or 1,4-diamino-2-methylbutane; and B's may be same or different and represent ##STR2## (wherein m is 0, 1 or 2; n is 0 or 1; R.sub.1 is a C.sub.3 -C.sub.6 alkyl group substituted with one or two hydroxyl groups) or two B's jointly represent ##STR3## (wherein R.sub.2 is a C.sub.2 -C.sub.5 alkyl group substituted with one hydroxyl group)].These platinum (II) complexes have high potencies for use as an antitumor agent.

4. 发明授权

US5747502A Process for preparing benzo�c!phenanthridinium derivatives, novel compounds prepared by said process, and antitumor agents 失效
标题翻译：制备苯并[c]菲啶鎓衍生物，通过所述方法制备的新化合物和抗肿瘤剂的方法
公开(公告)号：US5747502A
公开(公告)日：1998-05-05
申请号：US851853
申请日：1992-03-16
申请人： Miyoji Hanaoka , Hisao Ekimoto , Fumiko Kobayashi , Yukio Irie , Katsutoshi Takahashi , Masanobu Suzuki , Takeshi Nakanishi , Osamu Kogawa , Keizou Ishikawa
发明人： Miyoji Hanaoka , Hisao Ekimoto , Fumiko Kobayashi , Yukio Irie , Katsutoshi Takahashi , Masanobu Suzuki , Takeshi Nakanishi , Osamu Kogawa , Keizou Ishikawa
IPC分类号： A61K31/473 , A61K31/44 , C07D471/00
CPC分类号： A61K31/473 , Y10S514/883 , Y10S514/908
摘要： The present invention relates to benzo�c!phenanthridinium derivative of the general formula A: ##STR1## wherein M and N individually represent a hydroxyl or lower alkoxy group, or M and N simultaneously represent a hydrogen atom or together form a methylenedioxy group, X.sup.- represents an acid residue or a hydrogen acid residue, and R represents a lower alkyl group, and a process for preparing such derivatives. The compounds exhibit both potent antitumor activity and platelet aggregation inhibition activity, and are expected to be useful for the treatment of tumors. The process has good reproducibility and may be effected under moderate conditions, and therefore the process is practically useful. In addition, hydrogen salts of the present compounds have an enhanced stability, which is an advantage in formulating the same into pharmaceutical preparations.
摘要翻译：本发明涉及通式A的苯并[c]菲啶鎓衍生物：其中M和N各自表示羟基或低级烷氧基，或M和N同时代表氢原子或一起形成亚甲二氧基基团，X-表示酸残基或氢酸残基，R表示低级烷基，以及制备该衍生物的方法。该化合物表现出有效的抗肿瘤活性和血小板聚集抑制活性，并且预期可用于治疗肿瘤。该方法具有良好的再现性并且可以在中等条件下进行，因此该方法实际上是有用的。此外，本发明化合物的氢盐具有增强的稳定性，这将其配制成药物制剂是有利的。

5. 发明授权

US4952409A Agent for prevention and remedy of injuries caused by ischemia 失效
标题翻译：预防和治疗由缺血引起的损伤的药剂
公开(公告)号：US4952409A
公开(公告)日：1990-08-28
申请号：US352752
申请日：1989-05-16
申请人： Ko Bando , Yoshimasa Senoo , Minoru Noji , Kazuo Ootsuki , Hisao Ekimoto , Yukio Irie
发明人： Ko Bando , Yoshimasa Senoo , Minoru Noji , Kazuo Ootsuki , Hisao Ekimoto , Yukio Irie
IPC分类号： A01N1/02 , A61K9/127 , A61K38/44 , A61P9/00 , A61P9/08 , A61P9/10
CPC分类号： A61K38/446 , A61K9/127 , Y10S436/829
摘要： Disclosed is an agent for prevention and remedy of injuries caused by ischemia, which comprises, as an active ingredient, an SOD-containing liposome comprising a superoxidase dismutase (SOD) retained in a liposome having an electrically neutral or negative membrane.

6. 发明申请

US20120277295A1 KIT FOR CANCER TREATMENT AND PHARMACEUTICAL COMPOSITION FOR CANCER TREATMENT 审中-公开
标题翻译：用于癌症治疗的癌症治疗和药物组合物
公开(公告)号：US20120277295A1
公开(公告)日：2012-11-01
申请号：US13547758
申请日：2012-07-12
申请人： Hisao EKIMOTO
发明人： Hisao EKIMOTO
IPC分类号： A61K31/196 , A61K31/337 , A61P35/00
CPC分类号： A61K45/06 , A61K31/196 , A61K31/198 , A61K31/20 , A61K31/337 , A61K31/513 , A61K31/53 , A61K31/573 , A61K31/704 , A61K33/36 , A61K2300/00
摘要： To provide a kit for cancer treatment and a pharmaceutical composition for cancer treatment that can inhibit the growth of tumors and cancers in mammals more than ever.The kit for cancer treatment includes a combination of two different drugs in a kit formulation. The first drug contains a synthetic retinoid or a pharmaceutically acceptable organic or inorganic acid addition salt thereof, and the second drug contains a chemotherapeutic agent for cancer treatment. A synthetic retinoid that can be suitably used is a benzoic acid derivative represented by the following formula (I): or a pharmaceutically acceptable organic or inorganic acid addition salt thereof.
摘要翻译：提供用于癌症治疗的试剂盒和用于癌症治疗的药物组合物，其可以比以往任何时候都能抑制哺乳动物肿瘤和癌症的生长。用于癌症治疗的试剂盒包括两种不同药物在试剂盒配方中的组合。第一种药物含有合成的类视色素或其药学上可接受的有机或无机酸加成盐，第二种药物含有癌症治疗用化学治疗剂。可合适地使用的合成类视黄醇是由下式（I）表示的苯甲酸衍生物或其药学上可接受的有机酸或无机酸加成盐。

7. 发明授权

US08252837B2 Tamibarotene capsule preparation 有权
标题翻译：他米巴罗汀胶囊制剂
公开(公告)号：US08252837B2
公开(公告)日：2012-08-28
申请号：US12593866
申请日：2008-03-28
申请人： Hisao Ekimoto
发明人： Hisao Ekimoto
IPC分类号： A61K31/195 , A61K9/48
CPC分类号： A61K31/192 , A61K9/4866 , A61K9/4875 , A61K47/10 , A61K47/14
摘要： The present invention provides a practical preparation form of Tamibarotene and dosage form thereof, which exhibit high absorptivity by the body with minimized toxicity, and which are safe and stable without any risk of contamination. It is provided a Tamibarotene capsule preparation which encapsulates a composition comprising an oil component as its base and Tamibarotene as an active ingredient dissolved in the base. It is preferred that the oil component be propylene glycol fatty acid esters or polyethylene glycols. It is also preferred that the Tamibarotene capsule preparation comprise 0.1-50 mg/mL of the Tamibarotene based on the oil component.
摘要翻译：本发明提供了Tamibarotene及其剂型的实用制剂形式，它以体积最小的毒性显示出高吸收性，并且是安全和稳定的，没有任何污染的风险。提供了一种Tamibarotene胶囊制剂，其包含以油组分为基础的组合物和作为活性成分溶解在基质中的Tamibarotene。油成分优选为丙二醇脂肪酸酯或聚乙二醇。还优选的是，Tamibarotene胶囊制剂包含基于油组分的0.1-50mg / mL的Tamibarotene。

8. 发明授权

US06458848B1 Remedy for autoimmune diseases 失效
公开(公告)号：US06458848B1
公开(公告)日：2002-10-01
申请号：US10044064
申请日：2002-01-10
申请人： Junpei Itoh , Osamu Miyazaki , Hisao Ekimoto , Michinori Koyama , Tetsushi Saino , Lauri Kangas , Anni Warri , Christer Granberg
发明人： Junpei Itoh , Osamu Miyazaki , Hisao Ekimoto , Michinori Koyama , Tetsushi Saino , Lauri Kangas , Anni Warri , Christer Granberg
IPC分类号： A61K3135
CPC分类号： A61K31/138 , A61K31/00 , A61K31/135 , A61K31/56 , A61K31/57 , A61K2300/00
摘要： Disclosed is use of nonsteroidal anti-estrogen compounds such as toremifene citrate as active ingredient for treating autoimmune diseases.

9. 发明授权

US06184253B2 Remedy for autoimmune diseases 失效
标题翻译：补救自身免疫性疾病
公开(公告)号：US06184253B2
公开(公告)日：2001-02-06
申请号：US09192990
申请日：1998-11-16
申请人： Junpei Itoh , Osamu Miyazaki , Hisao Ekimoto , Michinori Koyama , Tetsushi Saino , Lauri Kangas , Anni Warri , Christer Granberg
发明人： Junpei Itoh , Osamu Miyazaki , Hisao Ekimoto , Michinori Koyama , Tetsushi Saino , Lauri Kangas , Anni Warri , Christer Granberg
IPC分类号： A01N4500
CPC分类号： A61K31/138 , A61K31/135 , A61K31/56 , A61K2300/00
摘要： Disclosed is use of nonsteroidal anti-estrogen compounds such as toremifene citrate as active ingredient for treating autoimmune diseases.
摘要翻译：公开了使用非甾体抗雌激素化合物如托瑞米芬柠檬酸盐作为治疗自身免疫疾病的活性成分。

10. 发明授权

US4824955A Selenium oxy chloride-pyridine or bipyridine complexes 失效
标题翻译：氯氧化硒 - 吡啶或联吡啶配合物
公开(公告)号：US4824955A
公开(公告)日：1989-04-25
申请号：US928551
申请日：1986-11-10
申请人： Hisao Ekimoto , Masanobu Suzuki , Takao Izawa , Katsutoshi Takahashi , Tokuji Nakatani , Akio Fujii
发明人： Hisao Ekimoto , Masanobu Suzuki , Takao Izawa , Katsutoshi Takahashi , Tokuji Nakatani , Akio Fujii
IPC分类号： C07D207/20 , C07D213/06 , C07D213/22 , C07D213/61 , C07D213/64 , C07D213/68 , C07D213/73 , C07D213/74 , C07D213/79 , C07D213/80 , C07D213/84 , C07D213/85 , C07D213/89 , C07D215/06 , C07D215/18 , C07D215/22 , C07D215/233 , C07D215/24 , C07D217/02 , C07D233/68 , C07D235/06 , C07D235/08 , C07D471/04 , C07D473/08 , C07D473/10 , C07D473/12 , C07D521/00 , C07F9/11 , C07D401/04 , C07D213/65
CPC分类号： C07D213/06 , C07D207/20 , C07D213/22 , C07D213/61 , C07D213/64 , C07D213/68 , C07D213/73 , C07D213/74 , C07D213/79 , C07D213/80 , C07D213/84 , C07D213/85 , C07D213/89 , C07D215/06 , C07D215/18 , C07D215/233 , C07D215/24 , C07D217/02 , C07D231/12 , C07D233/56 , C07D233/68 , C07D235/06 , C07D235/08 , C07D249/08 , C07D471/04 , C07D473/08 , C07D473/10 , C07D473/12 , C07F9/11
摘要： This invention relates to the novel selenium compounds which are useful as an antineoplastic agent. The compounds are represented by the general formula (I):Se(O).sub.a (R).sub.b (X).sub.c (A).sub.n (Y).sub.m (I)wherein R, X, A and Y represent the groups specified below, a represents a number of 0 or 1, b represents a number of 0, 1 or 2, and (1) when a is 0 and b is also 0, c is 4, n is 1 or 2 and m is 0, (2) when a is 1 and b is 0, c is 2, n is 1 or 2 and m is 0 or 1, and (3) when b is 1 or 2, c, n and m are all 0;(i) when b is 2, R represents (1) a C.sub.4-10 alkoxy group substituted with a halogen atom, (2) a lower alkoxyl group substituted with a halogen atom and a phenyl group, or (3) a cycloalkyloxy group substituted with a halogen atom, and (ii) when b is 1, R represents a group represented by the formula ##STR1## (wherein R.sub.0 is a C.sub.2-6 alkyl group); X represents a halogen atom;A represents a compound represented by the formula ##STR2## (wherein R.sub.1 and R.sub.2 may be the same or different and represent a hydrogen atom, a hydroxyl group, a lower alkyl group, a halogen atom, a phenyl group, a cyano group, a lower alkoxycarbonly group, a phenoxycarbonyl group, an amino group (to which a lower alkyl, lower alkylaminocarbonyl, lower halogenoalkylaminocarbonyl or lower alkoxycarbonyl group may be bonded), a benzoyl group, a loweralkoxyl group, a carbamyl group or an allyloxycarbonyl group; R.sub.7 represents a hydrogen atom, a lower alkyl group or a group represented by the formula ##STR3## (wherein R.sub.9 represents an amino group or a lowr alkoxyl group); Y represents H.sub.2 O.
摘要翻译：本发明涉及可用作抗肿瘤剂的新型硒化合物。这些化合物由通式（I）表示：Se（O）a（R）b（X）c（A）n（Y）m（I）其中R，X，A和Y表示下面规定的基团， a表示0或1的数，b表示0,1或2的数，以及（1）当a为0且b为0时，c为4，n为1或2，m为0，（2））当a为1且b为0时，c为2，n为1或2，m为0或1，（3）当b为1或2时，c，n和m均为0; （i）当b为2时，R表示（1）被卤素原子取代的C 4-10烷氧基，（2）被卤素原子和苯基取代的低级烷氧基，或（3）环烷氧基取代和（ii）当b为1时，R表示由式“IMAGE”表示的基团（其中R 0为C 2-6烷基）; X表示卤原子; A表示由式“IMAGE”表示的化合物（其中R 1和R 2可以相同或不同，表示氢原子，羟基，低级烷基，卤原子，苯基，氰基，苯氧基羰基，氨基（可以键合有低级烷基，低级烷基氨基羰基，低级卤代烷基氨基羰基或低级烷氧基羰基），苯甲酰基，低级烷氧基，氨基甲酰基或烯丙氧基羰基; R7表示氢原子，低级烷基或下式表示的基团（其中R9表示氨基或低级烷氧基）; Y表示H 2 O。

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