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1. 发明授权

US4452786A Condurango glycoside compounds, processes for their preparation, antitumor agents comprising them and compositions 失效
标题翻译： Condurango糖苷化合物，其制备方法，包含它们的抗肿瘤剂和组合物
公开(公告)号：US4452786A
公开(公告)日：1984-06-05
申请号：US320974
申请日：1981-11-02
申请人： Hiroshi Mitsuhashi , Den-ichi Mizuno , Koji Hayashi , Shigeru Abe , Muneaki Takase , Toshiharu Narita
发明人： Hiroshi Mitsuhashi , Den-ichi Mizuno , Koji Hayashi , Shigeru Abe , Muneaki Takase , Toshiharu Narita
IPC分类号： A61K36/27 , C07H15/24 , C07J17/00 , C07J71/00 , A61K31/71 , A61K31/705
CPC分类号： C07J71/0005 , A61K36/27 , C07J17/005
摘要： Novel condurango glycoside compounds, antitumor agents comprising them and processes for their preparation, compositions containing them and methods of treating tumor with them are disclosed herein in which the novel condurango glycoside compounds are represented by the following formula (I): ##STR1## where X together with the 13 and 14 position carbon atoms is a group selected from the group consisting of ##STR2##
摘要翻译： PCT No.PCT / JP81 / 00045 Sec。 371日期：1981年11月2日 102（e）1981年11月2日PCT PCT Fils 3月5日PCT PCT。出版物WO81 / 02577 日本9月17日，1981年公开了新颖的糠醛糖苷化合物，包含它们的抗肿瘤剂及其制备方法，含有它们的组合物和与它们一起治疗肿瘤的方法，其中新的糠醛糖苷化合物由下式（I ）：其中X与13和14位碳原子一起是选自 + TR

2. 发明授权

US4320120A Extracts of Marsdenia cundurango Reichenbach fil 失效
标题翻译： Marsdenia cundurango Reichenbach fil提取物
公开(公告)号：US4320120A
公开(公告)日：1982-03-16
申请号：US179001
申请日：1980-08-18
申请人： Hiroshi Mitsuhashi , Den-ichi Mizuno , Koji Hayashi , Shigeru Abe , Muneaki Takase , Toshiharu Narita
发明人： Hiroshi Mitsuhashi , Den-ichi Mizuno , Koji Hayashi , Shigeru Abe , Muneaki Takase , Toshiharu Narita
IPC分类号： A61K36/00 , A61K36/27 , A61K31/705 , A61K35/78
CPC分类号： A61K36/27
摘要： New extracts of Marsdenia cundurango Reichenbach fil., processes for preparing them, antitumor agents comprising them, compositions containing them and methods of treating tumor with them are described herein in which the extracts consist essentially of the portion of Marsdenia cundurango Reichenbach fil. which is soluble in lower alcohols and in chlorinated hydrocarbons other than carbon tetrachloride and insoluble in carbon tetrachloride or aromatic hydrocarbons.
摘要翻译：本文描述了Marsdenia cundurango Reichenbach fil。的新提取物，其制备方法，包含它们的抗肿瘤剂，含有它们的组合物和用它们治疗肿瘤的方法，其中提取物基本上由Marsdenia cundurango Reichenbach fil的部分组成。其可溶于低级醇和除四氯化碳以外的氯代烃，并且不溶于四氯化碳或芳族烃。

3. 发明授权

US5393889A Water soluble bis-dioxopiperazine derivatives 失效
标题翻译：水溶性双二氧代哌嗪衍生物
公开(公告)号：US5393889A
公开(公告)日：1995-02-28
申请号：US835927
申请日：1992-03-02
申请人： Muneaki Takase , Toshiharu Narita , Toshihiko Komatsu
发明人： Muneaki Takase , Toshiharu Narita , Toshihiko Komatsu
IPC分类号： A61K31/495 , A61K31/496 , A61P35/00 , C07D241/00 , C07D241/08 , C07D403/14 , C07D417/14
CPC分类号： C07D403/14 , C07D241/08 , C07D417/14
摘要： A pharmaceutically-acceptable acid addition salt of a bis-dioxopiperazine derivative of the formula (I): ##STR1## which derivative exhibits anti-tumor potency and is water-soluble, wherein R.sup.1 is a C.sub.1-6 alkyl group,R.sup.2 represents a hydrogen atom or: ##STR2## R.sup.3 represents a hydrogen atom, a C.sub.1-6 alkyl group or (CH.sub.2).sub.n A, wherein A respresents carboxyl, benzyloxycarbonyl, mercapto, amino, benzyloxycarbonylamino or: ##STR3## and n is an integer of 1, 2, 3 or 4, and R.sup.4 represents a hydrogen atom or is coupled with R.sup.3 into a 5-membered ring, which may contain one sulfur atom as an additional ring heteroatom.
摘要翻译： PCT No.PCT / JP91 / 00894 Sec。 371日期：1992年3月2日 102（e）1992年3月2日PCT PCT 1991年7月3日PCT公布。出版物WO92 / 00971 1991年1月23日授权。式（I）的双二氧代哌嗪衍生物的药学上可接受的酸加成盐：该衍生物具有抗肿瘤效力并且是水溶性的，其中R1是C1-6 烷基，R 2表示氢原子或：R 3表示氢原子，C 1-6烷基或（CH 2）n A，其中A表示羧基，苄氧羰基，巯基，氨基，苄氧羰基氨基或：是1,2,3或4的整数，R 4表示氢原子或与R 3连接成5元环，其可以含有一个硫原子作为另外的环杂原子。

4. 发明授权

US4501736A Extract from barrenwort 失效
标题翻译：从小麦提取物
公开(公告)号：US4501736A
公开(公告)日：1985-02-26
申请号：US520760
申请日：1983-08-08
申请人： Susumu Mitsuhashi , Muneaki Takase , Sosuke Yasui , Ichiro Washizawa , Kimitomo Yoshioka
发明人： Susumu Mitsuhashi , Muneaki Takase , Sosuke Yasui , Ichiro Washizawa , Kimitomo Yoshioka
IPC分类号： A61K36/296 , A61K39/39 , A61K35/78
CPC分类号： A61K39/39 , A61K36/296 , A61K2039/55588
摘要： The present invention provides an extract obtained by extracting a plant belonging to the genus Epimedium sp. with a mixed solvent of water and a water-miscible organic solvent or with water, defatting the obtained aqueous extract and collecting a high-molecular compounds-containing fraction from the defatted aqueous extract, a process for preparation of this extract, an antibacterial agent comprising this extract as an effective component and an antibacterial therapy by using this extract.
摘要翻译：本发明提供通过提取属于淫羊藿属属植物的植物而获得的提取物。与水和水混溶性有机溶剂的混合溶剂或与水混合，使得到的水提取物脱脂并从脱脂水提取物中收集含高分子化合物的级分，该提取物的制备方法，包含该提取物作为有效成分，通过使用该提取物进行抗菌治疗。

5. 发明授权

US3968277A Process for coating solid particles with a digestive tract-soluble film 失效
标题翻译：用消化道溶解膜涂覆固体颗粒的方法
公开(公告)号：US3968277A
公开(公告)日：1976-07-06
申请号：US444056
申请日：1974-02-20
申请人： Muneaki Takase
发明人： Muneaki Takase
IPC分类号： A61J3/00 , A61K9/28 , A61K9/30 , A61K9/32 , A61K9/50 , C08F27/08
CPC分类号： A61K9/2893 , A61J3/005 , A61K9/5089 , Y10S514/951 , Y10S514/96
摘要： A coating process and apparatus for manufacturing of solid particles with digestive tracts-soluble film by rolling water-containing solid particles at high speed, adding a coating liquid and drying them simultaneously.
摘要翻译：一种用于通过高速滚动含水固体颗粒制造具有消化道可溶性薄膜的固体颗粒的涂布方法和装置，加入涂布液并同时干燥。

6. 发明授权

US4877803A Bis-dioxopiperazine derivatives and pharmaceutical compositions containing the same 失效
标题翻译：双二氧代哌嗪衍生物和含有它们的药物组合物
公开(公告)号：US4877803A
公开(公告)日：1989-10-31
申请号：US31011
申请日：1987-02-24
申请人： Jun-Chao Cai , Muneaki Takase
发明人： Jun-Chao Cai , Muneaki Takase
IPC分类号： C07D401/14 , A61K31/495 , A61K31/535 , A61K31/54 , A61P35/00 , C07D241/08
CPC分类号： C07D241/08
摘要： Novel bis-dioxopiperazine derivatives represented by the following formula (I) and having a broader antitumor spectrum as well as pharmaceutical compositions containing the compounds as antitumor active components: ##STR1## wherein R.sup.1 represents a lower alkyl group; A represents an oxygen atom, a sulfur atom or a group of ##STR2## wherein R.sup.2 represents a hydrogen atom, a lower alkyl group or phenyl; R.sup.3 represents a lower alkyl group, phenyl or benzyl; and X and Y, which are respectively independent and are the same or different, represent a hydrogen atom or a lower alkyl group.
摘要翻译： PCT No.PCT / JP86 / 00324 Sec。 371日期1987年2月24日 102（e）1987年2月24日PCT PCT 1986年6月25日PCT公布。公开号WO87 / 00170 日本1987年1月15日。由下式（I）表示并具有更广泛的抗肿瘤谱的新型双二氧代哌嗪衍生物以及含有作为抗肿瘤活性成分的化合物的药物组合物：其中R1表示低级烷基; A表示氧原子，硫原子或一组，其中R2表示氢原子，低级烷基或苯基; R3表示低级烷基，苯基或苄基; 分别独立地表示相同或不同的X，Y表示氢原子或低级烷基。

7. 发明授权

US4868303A Bis-dioxopiperazine derivatives 失效
标题翻译：双二氧代哌嗪衍生物
公开(公告)号：US4868303A
公开(公告)日：1989-09-19
申请号：US124932
申请日：1987-09-25
申请人： Muneaki Takase , Jun-Chao Cai
发明人： Muneaki Takase , Jun-Chao Cai
IPC分类号： A61K31/495 , A61P35/00 , C07D241/06 , C07D241/08 , C07D405/14
CPC分类号： C07D405/14 , C07D241/08 , Y02P20/55
摘要： Novel bis-dioxopiperazine derivatives or pharmaceutically acceptable salts thereof having broader antitumor spectra and represented by the following formula (I): ##STR1## wherein R.sup.1 represents a lower alkyl group;R.sup.2 represents a hydrogen atom or a group of ##STR2## and R.sup.3 represents a lower alkyl group, a substituted or unsubstituted phenyl group, a substituted or unsubstituted furyl group, a substituted or unsubstituted styryl group or a group of --(CH.sub.2).sub.n --R.sup.4, ##STR3## or --OR.sup.7 in whichR.sup.4 represents a carboxyl group, a substituted or unsubstituted phenyl group or a substituted or unsubstituted phenoxy group,R.sup.5 and R.sup.6 respectively represent a hydrogen atom or a protective group for amino group,R.sup.7 represents a lower alkyl group or a substituted or unsubstituted benzyl group, andn is an integer and 1 or 2.

8. 发明授权

US4800201A 1,4-thiazine derivative, and cardiotonic agent comprising it as effective component 失效
标题翻译： 1,4-噻嗪衍生物和强心剂包含它作为有效成分
公开(公告)号：US4800201A
公开(公告)日：1989-01-24
申请号：US876860
申请日：1986-06-03
申请人： Muneaki Takase , Kimitomo Yoshioka , Hiroaki Yamazaki
发明人： Muneaki Takase , Kimitomo Yoshioka , Hiroaki Yamazaki
IPC分类号： C07D279/12 , C07D417/04 , A61K31/54
CPC分类号： C07D417/04 , C07D279/12
摘要： A novel 1,4-thiazine derivative represented by the formula I, a pharmaceutically acceptable acid addition salt thereof, a process for preparation thereof and a cardiotonic agent comprising it as an effective component; ##STR1## wherein R.sub.1 and R.sub.2 represent respectively hydrogen atom, lower alkyl group, lower alkoxy group, amino group, lower alkyl-amino group, aryl-amino group, hydroxy group, aryl group or 5- or 6-membered heterocyclic residue;R.sub.3 and R.sub.4 represent hydrogen atom or lower alkyl group; andR.sub.5 represents N-containing heterocyclic residue and is not pyridinyl group when R.sub.1 and R.sub.2 represent hydrogen atom and R.sub.3 and R.sub.4 represent hydrogen atom or lower alkyl group.
摘要翻译： PCT No.PCT / JP85 / 00548 Sec。 371日期：1986年6月3日 102（e）日期1986年6月3日PCT提交1985年10月3日PCT公布。出版物WO86 / 02074 日期：1986年4月10日。由式I表示的新颖的1,4-噻嗪衍生物，其药学上可接受的酸加成盐，其制备方法和强心剂，其包含其作为有效成分; 其中R1和R2分别表示氢原子，低级烷基，低级烷氧基，氨基，低级烷基 - 氨基，芳基 - 氨基，羟基，芳基或5-或6-元杂环残基; R3和R4代表氢原子或低级烷基; 并且当R 1和R 2表示氢原子且R 3和R 4表示氢原子或低级烷基时，R 5表示含氮杂环残基，不是吡啶基。

9. 发明授权

US4528188A Polysaccharide PS-A obtained from barrenwort deriving from plants belonging to the genus Epimedium, process for preparation thereof and phylactic and immunostimulating agents comprising said polysaccharide PS-A effective component 失效
公开(公告)号：US4528188A
公开(公告)日：1985-07-09
申请号：US456027
申请日：1982-12-30
申请人： Susumu Mitsuhashi , Muneaki Takase , Sosuke Yasui , Ichiro Washizawa , Kimitomo Yoshioka
发明人： Susumu Mitsuhashi , Muneaki Takase , Sosuke Yasui , Ichiro Washizawa , Kimitomo Yoshioka
IPC分类号： A61K31/715 , A61K36/00 , A61K36/296 , C08B37/00 , C12P19/04
CPC分类号： A61K36/296 , A61K31/715
摘要： A polysaccharide PS-A obtained from plants belonging to the genus Epimedium and having the following physicochemical properties, a process for preparation thereof and use as phylactic and immunostimulating agents comprising the polysaccharide PS-A as an effective component:1. Elementary analysis: C=40.92; H=6.17; Ash=very small;2. Molecular weight: 75,000.+-.25,000 (average molecular weight);3. Decomposition point: 205.degree. C.;4. pH: 7.0 (solution of 100 mg of PS-A in 50 ml of water);5. Specific rotatory power: [.alpha.].sub.D.sup.19 =-23.6.degree. (in H.sub.2 O, c=0.527);6. Infrared absorption spectrum: .nu..sub.max.sup.KBr (cm.sup.-1)/3400, 2900, 1620, 1400, 1230, 1060;7. Ultraviolet absorption spectrum: Maximum absorption is not recognized in the range of 240-400 nm.;8. Outward form: White or faint brown, amorphous powder;9. Solubility:(a) Soluble in water;(b) Insoluble in methanol, ethanol, acetone, ethyl acetate, diethyl ether, hexane and chloroform;10. Color reactions:Positive to the following reactions: (a) anthrone-sulfuric acid reaction; (b) Molisch's reaction; (c) skatol reaction; and (d) Bial's reaction;Negative to the following reactions: (a) ninhydrin reaction; (b) 2,4-DNP reaction; (c) Selivanoff's reaction; (d) naphthoresorcinol reaction; and (e) carbazol-sulfuric acid reaction;11. Component sugars: Arabinose and galactose;12. Homogeneity: Homogeneity is proved according to ultracentrifugation, electrophoresis and gel filtration.

10. 发明授权

US4650799A Bis-dioxopiperazine derivatives, process for their preparation, antitumor agents comprising them and compositions containing them 失效
标题翻译：双二氧代哌嗪衍生物，其制备方法，包含它们的抗肿瘤剂和含有它们的组合物
公开(公告)号：US4650799A
公开(公告)日：1987-03-17
申请号：US664700
申请日：1984-10-25
申请人： Jun-Chao Cai , Muneaki Takase
发明人： Jun-Chao Cai , Muneaki Takase
IPC分类号： A61K31/495 , A61P35/00 , C07D241/08 , C07D317/00 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/14 , C07D403/06
CPC分类号： C07D401/14 , C07D241/08 , C07D405/14 , C07D409/14
摘要： Disclosed are novel bis-dioxopiperazine derivatives and non-toxic salts thereof, process for their preparation, antitumor agents comprising them and compositions containing them.The bis-dioxopiperazine derivatives are represented by the following general formula (I): ##STR1## wherein R represents an alkyl radical having 1 to 17 carbon atoms, a cycloalkyl radical having 3 to 7 carbon atoms, a lower alkyl radical having a substituent or substituents selected from the group consisting of halogeno, carboxy, alkoxycarbonyl having 2 to 5 carbon atoms, lower alkoxy, substituted or unsubstituted phenoxy, naphthyloxy, substituted or unsubstituted phenylthio, substituted or unsubstituted phenyl and naphthyl, a substituted or unsubstituted phenyl lower alkenyl radical, a substituted or unsubstituted phenyl radical, a naphthyl radical, a heterocyclic radical selected from the group consisting of pyridyl, furyl and thienyl, an alkoxy radical having 1 to 8 carbon atoms, a substituted or unsubstituted phenyl lower alkoxy radical, or a substituted or unsubstituted phenoxy radical. A substituent or substituents on R may be selected from the group consisting of lower alkyl, halogeno, lower alkoxy, acyloxy having 2 to 5 carbon atoms, methylenedioxy, carboxy, amino, methanesulfonylamino and nitro. The above-mentioned "lower alkyl", "lower alkoxy" and "lower alkenyl" respectively refer to alkyl having 1 to 4 carbon atoms, alkoxy having 1 to 4 carbon atoms and alkenyl having 2 to 4 carbon atoms.
摘要翻译：公开了新的双 - 二氧代哌嗪衍生物及其无毒盐，其制备方法，包含它们的抗肿瘤剂和含有它们的组合物。双二氧代哌嗪衍生物由以下通式（I）表示：其中R表示碳原子数1〜17的烷基，碳原子数3〜7的环烷基，低级烷基，取代或选自卤代，羧基，碳原子数2〜5的烷氧羰基，低级烷氧基，取代或未取代的苯氧基，萘氧基，取代或未取代的苯硫基，取代或未取代的苯基和萘基，取代或未取代的苯基低级烯基，取代或未取代的苯基，萘基，选自吡啶基，呋喃基和噻吩基的杂环基，具有1至8个碳原子的烷氧基，取代或未取代的苯基低级烷氧基，或取代或未取代的苯氧基。 R上的取代基可以选自低级烷基，卤代，低级烷氧基，具有2-5个碳原子的酰氧基，亚甲二氧基，羧基，氨基，甲磺酰基氨基和硝基。上述“低级烷基”，“低级烷氧基”和“低级烯基”分别表示具有1至4个碳原子的烷基，具有1至4个碳原子的烷氧基和2至4个碳原子的烯基。

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