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。

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。

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。

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。

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.

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.

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。

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.

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。

公开(公告)号：US20110034714A1

公开(公告)日：2011-02-10

申请号：US12667741

申请日：2008-07-04

申请人： Hisao Ekimoto

发明人： Hisao Ekimoto

IPC分类号： C07F15/00

CPC分类号： C07F9/2495 ,  C07F9/4028 ,  C07F9/4031 ,  C07F9/4034 ,  C07F9/405 ,  C07F15/0093

摘要： A metal complex compound which exhibits a high degree of adsorption to bone or inhibition of cell growth, and is highly effective for therapy of a cancer metastasized to bone and therapy of the primary carcinoma thereof; a therapeutic agent composition for a cancer containing as an active ingredient the metal complex compound or a physiologically acceptable salt thereof; and an intermediate for the metal complex compound are provided. More concretely, a metal complex compound represented by the following General Formula (1): (wherein R1 independently represents C1-C10 alkyl which may be branched or have a substituent; or a C3-C30 cyclic group which may have a substituent; and X represents CHR2, an oxygen atom or NR5);a therapeutic agent composition for a cancer containing it as an active ingredient; and an intermediate for the metal complex compound are provided.

摘要翻译： 表现出高度吸附骨骼或抑制细胞生长的金属络合物，对于转移到骨骼上的癌症及其原发性癌症的治疗方法是非常有效的; 含有作为活性成分的金属络合物或其生理学上可接受的盐的癌症治疗剂组合物; 和金属络合物的中间体。 更具体地说，由以下通式（1）表示的金属配位化合物：其中，R 1独立地表示可以具有支链或取代基的C1-C10烷基，或可具有取代基的C3-C30环基; X 表示CHR2，氧原子或NR5）; 含有它作为活性成分的癌症治疗剂组合物; 和金属络合物的中间体。