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1. 发明授权

US08227463B2 Amorphous body composed of heterocyclic compound, solid dispersion and pharmaceutical preparation each comprising the same, and process for production of the same 有权
标题翻译：由杂环化合物，固体分散体和各自含有它们的药物制剂组成的无定形体及其制备方法
公开(公告)号：US08227463B2
公开(公告)日：2012-07-24
申请号：US12744160
申请日：2008-11-21
申请人： Tadaaki Sugama , Nobuhiro Ishihara , Yoshiharu Tanaka , Masayuki Takahashi , Shinichi Yaguchi , Tetsuo Watanabe
发明人： Tadaaki Sugama , Nobuhiro Ishihara , Yoshiharu Tanaka , Masayuki Takahashi , Shinichi Yaguchi , Tetsuo Watanabe
IPC分类号： A61K31/535 , C07D413/14
CPC分类号： C07D403/04 , A61K9/1652 , A61K9/1694 , A61K9/2054 , C07D413/14 , C07D417/14
摘要： [Problems] The object is to improve the absorbability of a heterocyclic compound including s-triazine and a pyrimidine derivative in vitro. [Means for Solving Problems] Disclosed is, for example, an amorphous body of a heterocyclic compound as represented by the general formula (I) [wherein each of R's and others is as defined in the description] including s-triazine and a pyrimidine derivative, or a hydrate, a solvate or a pharmaceutically acceptable salt of the heterocyclic compound. Also disclosed is a process for producing the amorphous body. Further disclosed are: a solid dispersion comprising the amorphous body; and a medicinal preparation comprising the solid dispersion.
摘要翻译： [问题]本发明的目的是提高包括s-三嗪和嘧啶衍生物在内的杂环化合物的吸收性。 [解决问题的手段]公开了例如由通式（I）表示的杂环化合物的无定形体，其中R及其它各自如说明书中所定义）包括s-三嗪和嘧啶衍生物，或杂环化合物的水合物，溶剂合物或药学上可接受的盐。还公开了一种生产非晶体的方法。进一步公开的是：包含非晶体的固体分散体; 和含有固体分散体的药物制剂。

2. 发明授权

US07767824B2 Heterocyclic compounds and cerebral function improvers containing the same as the active ingredient 有权
标题翻译：含有与活性成分相同的杂环化合物和脑功能改善剂
公开(公告)号：US07767824B2
公开(公告)日：2010-08-03
申请号：US11433416
申请日：2006-05-15
申请人： Seiichiro Kawashima , Toshiyuki Matsuno , Naoki Fukuda , Kenichi Saitoh , Yoshimasa Yamaguchi , Masaya Higashi
发明人： Seiichiro Kawashima , Toshiyuki Matsuno , Naoki Fukuda , Kenichi Saitoh , Yoshimasa Yamaguchi , Masaya Higashi
IPC分类号： C07D513/04 , A61K31/429
CPC分类号： C07D471/04 , C07D487/04 , C07D513/04
摘要： Heterocyclic compound represented by the formula I wherein represents or the like; R1 represents hydrogen atom, C1-C6 alkyl or benzyloxy; R2 represents methyl or nil; R3 represents hydrogen atom, C1-C6 alkyl, C2-C6 alkenyl, C3-C8 cycloalkyl or —CH2R5 [wherein R5 represents phenyl (which may be substituted with C1-C6 alkyl, halogen atom or cyano)] or thienyl; R4 represents C1-C6 alkyl, C2-C6 alkenyl, C3-C8 cycloalkyl or —CH2R6 [wherein R6 represents phenyl (which may be substituted with C1-C6alkyl, halogen atom or cyano), naphtyl or thienyl]; or R3 is coupled with R4.
摘要翻译：由式I表示的杂环化合物，其中表示等; R1表示氢原子，C1-C6烷基或苄氧基; R2表示甲基或无; R 3表示氢原子，C 1 -C 6烷基，C 2 -C 6烯基，C 3 -C 8环烷基或-CH 2 R 5 [其中R 5表示苯基（其可以被C 1 -C 6烷基，卤素原子或氰基取代）]或噻吩基; R 4表示C 1 -C 6烷基，C 2 -C 6烯基，C 3 -C 8环烷基或-CH 2 R 6 [其中R 6表示苯基（其可以被C 1 -C 6烷基，卤素原子或氰基取代），萘基或噻吩基]。或R3与R4结合。

3. 发明申请

US20090221554A1 METHOD OF TREATING COGNITIVE IMPAIRMENT 审中-公开
标题翻译：治疗认知障碍的方法
公开(公告)号：US20090221554A1
公开(公告)日：2009-09-03
申请号：US12039192
申请日：2008-02-28
申请人： Yoshimasa YAMAGUCHI , Toshiyuki Matsuno , Kenichi Saitoh
发明人： Yoshimasa YAMAGUCHI , Toshiyuki Matsuno , Kenichi Saitoh
IPC分类号： A61K31/55 , A61K31/437 , A61P25/16 , A61P25/28
CPC分类号： A61K31/437 , A61K31/438 , A61K31/444 , A61K31/445 , A61K31/55 , A61K45/06 , A61K2300/00
摘要： Disclosed is an method of treating cognitive impairment, including administering to a subject in need thereof a combination of a therapeutic agent for neurodegenerative disease and a therapeutically effective amount of a heterocyclic compound represented by the following general formula (I):
摘要翻译：公开了一种治疗认知障碍的方法，包括向有需要的受试者施用神经变性疾病的治疗剂和治疗有效量的由以下通式（I）表示的杂环化合物的组合：

4. 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。

5. 发明授权

US4565813A 1,4-Thiazine derivatives 失效
标题翻译： 1,4-噻嗪衍生物
公开(公告)号：US4565813A
公开(公告)日：1986-01-21
申请号：US650530
申请日：1984-09-14
申请人： Muneaki Takase , Kimitomo Yoshioka , Hiroaki Yamazaki
发明人： Muneaki Takase , Kimitomo Yoshioka , Hiroaki Yamazaki
IPC分类号： A61K31/54 , A61P7/02 , A61P9/04 , A61P9/08 , A61P9/10 , A61P11/08 , C07D417/04 , C07D401/04
CPC分类号： C07D417/04
摘要： Disclosed is a novel 1,4-thiazine derivatives represented by the following general formula I and a pharmaceutically acceptable acid addition salt thereof: ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 respectively represent a hydrogen atom or a lower alkyl group. Also disclosed are processes for preparation of a novel thiazine derivative represented by the general formula I, which comprise reacting a compound of the general formula III with a compound of the general formula A-X' in a compound containing a pyridinyl group as a solvent to obtain a compound of the general formula II: ##STR2## wherein R.sub.1, R.sub.2 and R.sub.3 are as defined above, A represents a group ##STR3## in which X represents a halogen atom and n is a number of 1 to 3, and X' represents a halogen atom which may be the same as or different from X, and reacting the compound of the general formula II with sulfur at elevated temperature or stirring the compound of the general formula II in a solution system comprising zinc and a carboxylic acid. Further disclosed is a cardiotonic agent comprising a pharmaceutically acceptable excipient and, as the active component thereof, an effective amount of the novel 1,4-thiazine derivative having the general formula I.
摘要翻译：公开了由以下通式I表示的新颖的1,4-噻嗪衍生物及其药学上可接受的酸加成盐：其中R 1，R 2和R 3分别表示氢原子或低级烷基。还公开了制备由通式I表示的新型噻嗪衍生物的方法，其包括将通式III的化合物与通式为AX'的化合物反应在含吡啶基作为溶剂的化合物中，得到通式II的化合物：其中R 1，R 2和R 3如上定义，A表示其中X表示卤素原子且n为1至3的数的基团， X'表示可以与X相同或不同的卤原子，并且在升高的温度下使通式II的化合物与硫反应，或在包含锌和羧酸的溶液体系中搅拌通式II的化合物酸。进一步公开的是强心剂，其包含药学上可接受的赋形剂，并且作为其活性组分，有效量的具有通式I的新的1,4-噻嗪衍生物。

6. 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

7. 发明授权

US4044713A Tumbing apparatus 失效
标题翻译：水龙带
公开(公告)号：US4044713A
公开(公告)日：1977-08-30
申请号：US608988
申请日：1975-08-29
申请人： Muneaki Takase
发明人： Muneaki Takase
IPC分类号： A61J3/00 , B01J2/00 , B05C3/08
CPC分类号： A61J3/005 , B01J2/006
摘要： A coating 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. Particles are disposed in a generally annular volume and supported on a generally rotary disk which is closely confined within a fixed cylinder and closely spaced from an inner fixed cylinder; said cylinder forming said annular volume. Partition means adjustably spaced from said plate, divide said volume into separate coating, water feed and drying chambers. The partitions form a sealing relationship with the particles.
摘要翻译：一种用于通过高速旋转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装置，加入涂布液并同时干燥。颗粒被设置在大致环形的体积中，并且被支撑在一个大致旋转的盘上，该旋转盘紧密地限制在固定的气缸内并与内部固定的气缸紧密地间隔开; 所述圆筒形成所述环形体积。分隔装置可调节地与所述板间隔开，将所述体积分成单独的涂层，给水和干燥室。隔板与颗粒形成密封关系。

8. 发明授权

US5773449A Thioquinolone compounds which have useful pharmaceutical activity 失效
标题翻译：具有有用的药物活性的硫醌类化合物
公开(公告)号：US5773449A
公开(公告)日：1998-06-30
申请号：US809722
申请日：1997-04-07
申请人： Masataka Konishi , Naoki Fukuda , Yukio Oku , Hiroaki Yamazaki , Kazuhiro Imaizumi , Hideshi Kobayashi
发明人： Masataka Konishi , Naoki Fukuda , Yukio Oku , Hiroaki Yamazaki , Kazuhiro Imaizumi , Hideshi Kobayashi
IPC分类号： C07D215/36 , C07D215/38 , C07D221/08 , C07D401/12 , C07D471/04 , C07D491/04 , C07D491/048 , A61K31/47
CPC分类号： C07D401/12 , C07D215/36 , C07D215/38 , C07D221/08 , C07D471/04 , C07D491/04
摘要： Disclosed is a thioquinolone derivative which exhibits highly selective antibacterial activity against Helicobacter pylori.
摘要翻译： PCT No.PCT / JP95 / 02052 Sec。 371日期1997年4月7日 102（e）日期1997年4月7日PCT提交1995年10月6日PCT公布。公开号WO96 / 11187 日期1996年4月18日公开是对幽门螺杆菌表现出高选择性抗菌活性的硫喹酮酮衍生物。

9. 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。

10. 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.

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