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1. 发明授权

US06348461B1 6,7-asymmetrically disubstituted quinoxalinecarboxylic acid derivatives, addition salts thereof, and processes for the preparation of both 失效
标题翻译： 6,7-不对称二取代的喹喔啉羧酸衍生物，其加成盐，以及二者的制备方法
公开(公告)号：US06348461B1
公开(公告)日：2002-02-19
申请号：US09485716
申请日：2000-03-01
申请人： Yasuo Takano , Futoshi Shiga , Masanori Takadoi , Hideharu Uchiki , Jun Asano , Tsuyoshi Anraku , Kazunori Fukuchi , Junichiro Uda , Naoki Ando
发明人： Yasuo Takano , Futoshi Shiga , Masanori Takadoi , Hideharu Uchiki , Jun Asano , Tsuyoshi Anraku , Kazunori Fukuchi , Junichiro Uda , Naoki Ando
IPC分类号： C07D24144
CPC分类号： C07D231/12 , C07D233/56 , C07D241/44 , C07D249/08 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14
摘要： The present invention provides 6,7-asymmetrically disubstituted quinoxalinecarboxylic acid compounds and their addition salts, and processes for preparing them, which have antagonism against excitatory amino acid receptors, in particular, an AMPA receptor. The 6,7-asymmetrically disubstituted quinoxalinecarboxylic acid compounds and their addition salts of the present invention are represented by formula (1) wherein Q, R, R1 and R2 are as described in the specification.
摘要翻译：本发明提供对兴奋性氨基酸受体，特别是AMPA受体具有拮抗作用的6,7-不对称二取代的喹喔啉羧酸化合物及其加成盐及其制备方法。本发明的6,7-不对称二取代的喹喔啉羧酸化合物及其加成盐由式（1）表示，其中Q，R，R 1和R 2如说明书中所述。

2. 发明授权

US06632813B1 6-subtituted-7-heteroquinoxalinecarboxylic acid derivatives and addition salts thereof and processes for the preparation of both 失效
标题翻译： 6-取代-7-异喹喔啉羧酸衍生物及其加成盐及其制备方法
公开(公告)号：US06632813B1
公开(公告)日：2003-10-14
申请号：US09926057
申请日：2001-08-22
申请人： Yasuo Takano , Futoshi Shiga , Tsuyoshi Anraku , Kazunori Fukuchi
发明人： Yasuo Takano , Futoshi Shiga , Tsuyoshi Anraku , Kazunori Fukuchi
IPC分类号： C07D24702
CPC分类号： A61K31/498
摘要： The invention provides compounds with antagonism against excitatory amino acid receptors, in particular, AMPA receptor having 6-substituted-7-heteroquinoxalinecarboxylic acid derivatives and addition salts thereof as effective ingredients, and processes for the preparation of both. The compounds are 6-substituted-7-heteroquinoxalinecarboxylic acid derivatives represented by the formula (1) where A denotes a single bond or methylene (CH2), Y denotes a nitrogen atom or ═CH—, V denotes a single bond or methylene (CH2), T denotes a hydroxyl group, amino group, lower alkoxycarbonyl group, carboxyl group, aldehyde group or the like, Q denotes a halogen atom, lower alkyl group or lower alkoxy group, and R1 denotes a hydroxyl group, lower alkoxy group or the like, and addition salts thereof.
摘要翻译：本发明提供具有对兴奋性氨基酸受体的拮抗作用的化合物，特别是具有6-取代-7-异喹喔啉羧酸衍生物的AMPA受体及其加成盐作为有效成分，以及二者的制备方法。化合物是由式（1）表示的6-取代-7-异喹喔啉羧酸衍生物，其中A表示单键或亚甲基（CH 2 PDAT>），Y表示氮原子或= CH-，V表示单键或亚甲基（CH 2 PDAT>），T表示羟基，氨基，低级烷氧基羰基，羧基，醛基或 Q表示卤素原子，低级烷基或低级烷氧基，R 1表示羟基，低级烷氧基等，及其加成盐。

3. 发明授权

US07425563B2 4-(Substituted aryl)-5-hydroxyisoquinolinone derivative 失效
标题翻译： 4-（取代的芳基）-5-羟基异喹啉酮衍生物
公开(公告)号：US07425563B2
公开(公告)日：2008-09-16
申请号：US10521565
申请日：2003-07-23
申请人： Futoshi Shiga , Takahiro Kanda , Tetsuya Kimura , Yasuo Takano , Jyunichi Ishiyama , Tomoyuki Kawai , Tsuyoshi Anraku , Kumi Ishikawa
发明人： Futoshi Shiga , Takahiro Kanda , Tetsuya Kimura , Yasuo Takano , Jyunichi Ishiyama , Tomoyuki Kawai , Tsuyoshi Anraku , Kumi Ishikawa
IPC分类号： C07D217/24 , C07D401/12 , A61K31/47
CPC分类号： C07D401/10 , A61K31/472 , A61K31/4725 , A61K31/496 , A61K31/5377 , C07D217/24 , C07D409/04
摘要： The invention provides 4-substituted aryl-5-hydroxyisoquinolinone derivatives and their pharmacologically acceptable addition salts with excellent inhibitory effect on poly (ADP-ribose) synthetase.4-Substituted aryl-5-hydroxyisoquinolinone derivatives, represented by a general formula (1) and their pharmacologically acceptable addition salts.
摘要翻译：本发明提供对聚（ADP-核糖）合成酶具有优异抑制作用的4-取代芳基-5-羟基异喹啉酮衍生物及其药理学上可接受的加成盐。 4-取代的由通式（1）表示的芳基-5-羟基异喹啉酮衍生物及其药理学上可接受的加成盐。

4. 发明申请

US20060173039A1 4-(Substituted aryl)-5-hydroxyisoquinolinone derivative 失效
标题翻译： 4-（取代的芳基）-5-羟基异喹啉酮衍生物
公开(公告)号：US20060173039A1
公开(公告)日：2006-08-03
申请号：US10521565
申请日：2003-07-23
申请人： Futoshi Shiga , Takahiro Kanda , Tetsuya Kimura , Yasuo Takano , Jyunichi Ishiyama , Tomoyuki Kawai , Tsuyoshi Anraku , Kumi Ishikawa
发明人： Futoshi Shiga , Takahiro Kanda , Tetsuya Kimura , Yasuo Takano , Jyunichi Ishiyama , Tomoyuki Kawai , Tsuyoshi Anraku , Kumi Ishikawa
IPC分类号： A61K31/47
CPC分类号： C07D401/10 , A61K31/472 , A61K31/4725 , A61K31/496 , A61K31/5377 , C07D217/24 , C07D409/04
摘要： The invention provides 4-substituted aryl-5-hydroxyisoquinolinone derivatives and their pharmacologically acceptable addition salts with excellent inhibitory effect on poly (ADP-ribose) synthetase. 4-Substituted aryl-5-hydroxyisoquinolinone derivatives, represented by a general formula (1) and their pharmacologically acceptable addition salts.
摘要翻译：本发明提供对聚（ADP-核糖）合成酶具有优异抑制作用的4-取代芳基-5-羟基异喹啉酮衍生物及其药理学上可接受的加成盐。 4-取代的由通式（1）表示的芳基-5-羟基异喹啉酮衍生物及其药理学上可接受的加成盐。

5. 发明申请

US20110172444A1 METHOD FOR PURIFYING AMINOACETYLPYRROLIDINECARBONITRILE DERIVATIVE AND SALT THEREOF 审中-公开
标题翻译：净化氨基乙酰胆碱衍生物及其盐的方法
公开(公告)号：US20110172444A1
公开(公告)日：2011-07-14
申请号：US13119274
申请日：2009-09-15
申请人： Futoshi Shiga
发明人： Futoshi Shiga
IPC分类号： C07D207/09 , C07D207/10
CPC分类号： C07D207/16 , C07B63/02
摘要： The present invention herein provides a simple, efficient and industrially useful method for purifying an aminoacetylpyrrolidinecarbonitrile derivative which is useful as a DPP-IV inhibitor. The method comprises the steps of acting an acid such as maleic acid on an aminoacetylpyrrolidinecarbonitrile derivative represented by the following Formula 1 to form a salt, isolating the salt and then regenerating the foregoing derivative from the salt: (In the formula, A represents CH2, CHF or CF2; R represents a C1 to C6 alkyl group which may have a substitutent, a C3 to C8 cycloalkyl group which may have a substitutent, an arylmethyl group which may have a substitutent, an arylethyl group which may have a substitutent, an aromatic hydrocarbon ring which may have a substitutent, an aromatic hetero ring which may have a substitutent, or an aliphatic hetero ring which may have a substitutent; and n represents 1 or 2).
摘要翻译：本发明提供了用作纯化用作DPP-IV抑制剂的氨基乙酰基吡咯烷腈衍生物的简单，有效和工业上有用的方法。该方法包括以下步骤：将下述式1表示的氨基乙酰基吡咯烷腈衍生物作用于马来酸等酸，形成盐，分离盐，然后从盐中再生上述衍生物：（式中，A表示CH 2， CHF或CF 2; R表示可以具有取代基的C1〜C6烷基，可具有取代基的C3〜C8环烷基，可具有取代基的芳基甲基，可具有取代基的芳基乙基，芳香族可具有取代基的烃环，可具有取代基的芳族杂环，或可具有取代基的脂族杂环; n表示1或2）。

6. 发明申请

US20090048454A1 Process for Producing Aminoacetyl Pyrrolidine Carbonitrile Derivative and Intermediate for Production Thereof 失效
标题翻译：生产氨基乙酰基吡咯烷腈衍生物及其制备方法
公开(公告)号：US20090048454A1
公开(公告)日：2009-02-19
申请号：US12224849
申请日：2007-02-02
申请人： Yoshikazu Asahina , Yasumichi Fukuda , Futoshi Shiga
发明人： Yoshikazu Asahina , Yasumichi Fukuda , Futoshi Shiga
IPC分类号： C07D207/16
CPC分类号： C07D207/16
摘要： Novel intermediates for the production of aminoacetyl pyrrolidine carbonitrile derivatives ensure the safe and efficient production of the compounds. Specifically, the present invention provides a sulfonyloxyacetyl pyrrolidine derivative, represented by the following formula:(Chemical Formula 1) (wherein R1 is a substituted or unsubstituted C1-C6 alkyl group, a substituted or unsubstituted C3-C6 cycloalkyl group, a substituted or unsubstituted arylmethyl group, a substituted or unsubstituted aromatic hydrocarbon, a substituted or unsubstituted aromatic heterocyclic ring or a substituted or unsubstituted aliphatic heterocyclic ring; R2 is CONH2 or CN; and X is CH2, CHF or CF2.)
摘要翻译：用于生产氨基乙酰基吡咯烷腈衍生物的新型中间体可确保化合物的安全高效生产。具体地说，本发明提供由下式表示的磺酰氧基乙酰基吡咯烷衍生物：（化学式1）（其中，R 1为取代或未取代的C 1 -C 6烷基，取代或未取代的C 3〜C 6环烷基，取代或未取代的芳基甲基，取代或未取代的芳族烃，取代或未取代的芳族杂环或取代或未取代的脂族杂环; R2为CONH2或CN; X为CH2，CHF或CF2）

7. 发明授权

US07915427B2 Process for producing aminoacetyl pyrrolidine carbonitrile derivative and intermediate for production thereof 失效
标题翻译：制备氨基乙酰基吡咯烷腈衍生物及其制备方法
公开(公告)号：US07915427B2
公开(公告)日：2011-03-29
申请号：US12224849
申请日：2007-02-02
申请人： Yoshikazu Asahina , Yasumichi Fukuda , Futoshi Shiga
发明人： Yoshikazu Asahina , Yasumichi Fukuda , Futoshi Shiga
IPC分类号： C07D207/04
CPC分类号： C07D207/16
摘要： Novel intermediates for the production of aminoacetyl pyrrolidine carbonitrile derivatives ensure the safe and efficient production of the compounds. Specifically, the present invention provides a sulfonyloxyacetyl pyrrolidine derivative, represented by the following formula:(Chemical Formula 1) (wherein R1 is a substituted or unsubstituted C1-C6 alkyl group, a substituted or unsubstituted C3-C6 cycloalkyl group, a substituted or unsubstituted arylmethyl group, a substituted or unsubstituted aromatic hydrocarbon, a substituted or unsubstituted aromatic heterocyclic ring or a substituted or unsubstituted aliphatic heterocyclic ring; R2 is CONH2 or CN; and X is CH2, CHF or CF2.)
摘要翻译：用于生产氨基乙酰基吡咯烷腈衍生物的新型中间体可确保化合物的安全高效生产。具体地说，本发明提供由下式表示的磺酰氧基乙酰基吡咯烷衍生物：（化学式1）（其中，R 1为取代或未取代的C 1 -C 6烷基，取代或未取代的C 3〜C 6环烷基，取代或未取代的芳基甲基，取代或未取代的芳族烃，取代或未取代的芳族杂环或取代或未取代的脂族杂环; R2为CONH2或CN; X为CH2，CHF或CF2）

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