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1. 发明授权

US08129377B2 6-(pyridinyl)-4-pyrimidone derivates as tau protein kinase 1 inhibitors 有权
标题翻译： 6-（吡啶基）-4-嘧啶酮衍生物作为tau蛋白激酶1抑制剂
公开(公告)号：US08129377B2
公开(公告)日：2012-03-06
申请号：US11576062
申请日：2005-09-29
申请人： Kazutoshi Watanabe , Kenji Fukunaga , Toshiyuki Kohara , Fumiaki Uehara , Shinsuke Hiki , Satoshi Yokoshima
发明人： Kazutoshi Watanabe , Kenji Fukunaga , Toshiyuki Kohara , Fumiaki Uehara , Shinsuke Hiki , Satoshi Yokoshima
IPC分类号： A61K31/535 , A61K31/505 , A01N43/54 , C07D413/00
CPC分类号： C07D401/04 , C07D401/14 , C07D409/14 , C07D413/14
摘要： A compound represented by the formula (I), an optically active isomer thereof, or a pharmaceutical acceptable salt thereof: wherein R1 represents a C1-C12 alkyl; R2 represents a hydrogen atom or the like; R3 represents a halogen or the like; q represents an integer of 1 to 7; R4 represents a halogen or the like; p represents 0 or an integer of 1 to 5; R5 represents a C6-C10 aryl, a heterocycle or the like; and X represents oxygen, NH, or the like, which is used for preventive and/or therapeutic treatment of a disease caused by tau protein kinase 1 hyperactivity such as a neurodegenerative diseases (e.g. Alzheimer disease).
摘要翻译：由式（I）表示的化合物，其光学活性异构体或其药学上可接受的盐：其中R1表示C1-C12烷基; R2表示氢原子等; R3表示卤素等; q表示1〜7的整数， R4表示卤素等; p表示0或1〜5的整数。 R5表示C6-C10芳基，杂环等; X代表氧，NH等，其用于预防和/或治疗由tau蛋白激酶1多动症如神经变性疾病（例如阿尔茨海默病）引起的疾病。

2. 发明授权

US08106045B2 2-morpholino-4-pyrimidone compound 有权
标题翻译： 2-吗啉代-4-嘧啶酮化合物
公开(公告)号：US08106045B2
公开(公告)日：2012-01-31
申请号：US11573476
申请日：2005-09-09
申请人： Kazutoshi Watanabe , Fumiaki Uehara , Shinsuke Hiki , Toshiyuki Kohara , Kenji Fukunaga , Satoshi Yokoshima
发明人： Kazutoshi Watanabe , Fumiaki Uehara , Shinsuke Hiki , Toshiyuki Kohara , Kenji Fukunaga , Satoshi Yokoshima
IPC分类号： A61K31/535 , A61K31/54 , C07D413/00 , C07D413/14
CPC分类号： C07D413/14
摘要： A compound represented by the formula (I), an optically active isomer thereof, or a pharmaceutical acceptable salt thereof: wherein X represents CH or N; represents a C1-C12 alkyl; R2 represents a hydrogen atom, or the like; R′ represents a C1-C6 alkyl or the like; q represents 0 or an integer of 1 to 7; Y represents a C1-C6 alkyl or the like; p represents 0 or an integer of 1 to 5; R represents a 2,3-dihydroindolyl or the like, which is used for preventive and/or therapeutic treatment of a disease caused by tau protein kinase 1 hyperactivity such as a neurodegenerative diseases (e.g. Alzheimer disease).
摘要翻译：由式（I）表示的化合物，其光学活性异构体或其药学上可接受的盐：其中X表示CH或N; 表示C1-C12烷基; R2表示氢原子等; R'表示C1-C6烷基等; q表示0或1〜7的整数， Y表示C1-C6烷基等; p表示0或1〜5的整数。 R表示2,3-二氢吲哚基等，其用于预防和/或治疗由tau蛋白激酶1多动症如神经变性疾病（例如阿尔茨海默病）引起的疾病。

3. 发明申请

US20090239864A1 6- (PYRIDINYL) -4-PYRIMIDONE DERIVATES AS TAU PROTEIN KINASE 1 INHIBITORS 有权
标题翻译： 6-（吡啶基）-4-吡啶酮衍生物作为TAU蛋白激酶1抑制剂
公开(公告)号：US20090239864A1
公开(公告)日：2009-09-24
申请号：US11576062
申请日：2005-09-29
申请人： Kazutoshi Watanabe , Kenji Fukunaga , Toshiyuki Kohara , Fumiaki Uehara , Shinsuke Hiki , Satoshi Yokoshima
发明人： Kazutoshi Watanabe , Kenji Fukunaga , Toshiyuki Kohara , Fumiaki Uehara , Shinsuke Hiki , Satoshi Yokoshima
IPC分类号： A61K31/5377 , C07D413/14 , A61P25/28 , A61P27/06 , A61P25/16 , A61P3/10
CPC分类号： C07D401/04 , C07D401/14 , C07D409/14 , C07D413/14
摘要： A compound represented by the formula (I), an optically active isomer thereof, or a pharmaceutical acceptable salt thereof: wherein R1 represents a C1-C12 alkyl; R2 represents a hydrogen atom or the like; R3 represents a halogen or the like; q represents an integer of 1 to 7; R4 represents a halogen or the like; p represents 0 or an integer of 1 to 5; R5 represents a C6-C10 aryl, a heterocycle or the like; and X represents oxygen, NH, or the like, which is used for preventive and/or therapeutic treatment of a disease caused by tau protein kinase 1 hyperactivity such as a neurodegenerative diseases (e.g. Alzheimer disease).
摘要翻译：由式（I）表示的化合物，其光学活性异构体或其药学上可接受的盐：其中R1表示C1-C12烷基; R2表示氢原子等; R3表示卤素等; q表示1〜7的整数， R4表示卤素等; p表示0或1〜5的整数， R5表示C6-C10芳基，杂环等; X代表氧，NH等，其用于预防和/或治疗由tau蛋白激酶1多动症如神经变性疾病（例如阿尔茨海默病）引起的疾病。

4. 发明授权

US07504411B2 2,3,6-Trisubstituted-4-pyrimidone derivatives 失效
标题翻译： 2,3,6-三取代-4-嘧啶酮衍生物
公开(公告)号：US07504411B2
公开(公告)日：2009-03-17
申请号：US10550299
申请日：2004-03-26
申请人： Kazutoshi Watanabe , Fumiaki Uehara , Shinsuke Hiki , Satoshi Yokoshima , Yoshihiro Usui , Masahiro Okuyama , Aya Shoda , Keiichi Aritomo , Toshiyuki Kohara , Kenji Fukunaga
发明人： Kazutoshi Watanabe , Fumiaki Uehara , Shinsuke Hiki , Satoshi Yokoshima , Yoshihiro Usui , Masahiro Okuyama , Aya Shoda , Keiichi Aritomo , Toshiyuki Kohara , Kenji Fukunaga
IPC分类号： C07D401/14 , C07D403/14 , A61K31/496 , A61K31/506 , A61P3/10 , A61P25/28
CPC分类号： C07D401/04 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： A pyrimidone derivative having tau protein kinase 1 inhibitory activity which is represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof; useful for prventive and/or therapeutic treatment of diseass such as neurodegenerative diseases (e.g. Alzheimer disease); wherein Q represents CH or nitrogen atom; R represents a C1-C12 alkyl group; the ring of Formula (I): represents piperazine ring or piperidine ring; each X independently represents a C1-C8 alkyl group, an optionally partially hydrogenated C6-C10 aryl ring, an indan ring or the like; m represents an integer of 1 to 3; each independently represents a halogen atom, a hydroxy group, a cyano group, a C1-C6 alkyl group or the like; n represents an integer of 0 to 8; when X and Y or two Y groups are attached on the same carbon atom, they may combine to each other to form a C2-C6 alkylene group.
摘要翻译：具有由式（I）表示的tau蛋白激酶1抑制活性的嘧啶酮衍生物或其盐或其溶剂合物或其水合物; 可用于疾病的预防和/或治疗性治疗，例如神经变性疾病（例如阿尔茨海默病）; 其中Q表示CH或氮原子; R代表C1-C12烷基; 式（I）的环表示哌嗪环或哌啶环; 每个X独立地表示C1-C8烷基，任选部分氢化的C 6 -C 10芳基环，茚满环等; m表示1〜3的整数，各自独立地表示卤素原子，羟基，氰基，C1-C6烷基等; n表示0〜8的整数，当X和Y或两个Y基团连接在同一个碳原子上时，它们可以彼此结合形成C 2 -C 6亚烷基。

5. 发明申请

US20060252768A1 2,3,6-Trisubstituted-4-pyrimidone derivatives 失效
标题翻译： 2,3,6-三取代-4-嘧啶酮衍生物
公开(公告)号：US20060252768A1
公开(公告)日：2006-11-09
申请号：US10550299
申请日：2004-03-26
申请人： Kazutoshi Watanabe , Fumiaki Uehara , Shinsuke Hiki , Satoshi Yokoshima , Yoshihiro Usui , Masahiro Okuyama , Aya Shoda , Keiichi Aritomo , Toshiyuki Kohara , Kenji Fukunaga
发明人： Kazutoshi Watanabe , Fumiaki Uehara , Shinsuke Hiki , Satoshi Yokoshima , Yoshihiro Usui , Masahiro Okuyama , Aya Shoda , Keiichi Aritomo , Toshiyuki Kohara , Kenji Fukunaga
IPC分类号： A61K31/513 , C07D403/14
CPC分类号： C07D401/04 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： A pyrimidone derivative having tau protein kinase 1 inhibitory activity which is represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof; useful for prventive and/or therapeutic treatment of diseass such as neurodegenerative diseases (e.g. Alzheimer disease); wherein Q represents CH or nitrogen atom; R represents a C1-C12 alkyl group; the ring of Formula (I): represents piperazine ring or piperidine ring; each X independently represents a C1-C8 alkyl group, an optionally partially hydrogenated C6-C10 aryl ring, an indan ring or the like; m represents an integer of 1 to 3; each independently represents a halogen atom, a hydroxy group, a cyano group, a C1-C6 alkyl group or the like; n represents an integer of 0 to 8; when X and Y or two Y groups are attached on the same carbon atom, they may combine to each other to form a C2-C6 alkylene group.
摘要翻译：具有由式（I）表示的tau蛋白激酶1抑制活性的嘧啶酮衍生物或其盐或其溶剂合物或其水合物; 可用于疾病的预防和/或治疗性治疗，例如神经变性疾病（例如阿尔茨海默病）; 其中Q表示CH或氮原子; R表示C 1 -C 12烷基; 式（I）的环表示哌嗪环或哌啶环; 每个X独立地表示C 1 -C 8烷基，任选部分氢化的C 6 -C 10烷基，芳环，茚满环等; m表示1〜3的整数，各自独立地表示卤素原子，羟基，氰基，C 1 -C 6烷基等; n表示0〜8的整数，当X和Y或两个Y基团连接在同一个碳原子上时，它们可以彼此结合形成C 2 -C 6亚烷基。

6. 发明申请

US20090233918A1 2-(CYCLIC AMINO)-PYRIMIDONE DERIVATIVES 失效
标题翻译： 2-（环丙氨基） - 吡咯烷酮衍生物
公开(公告)号：US20090233918A1
公开(公告)日：2009-09-17
申请号：US12282396
申请日：2007-03-14
申请人： Kenji Fukunaga , Toshiyuki Kohara , Kazutoshi Watanabe , Yoshihiro Usui , Fumiaki Uehara , Satoshi Yokoshima , Daiki Sakai , Shin-ichi Kusaka , Kazuki Nakayama
发明人： Kenji Fukunaga , Toshiyuki Kohara , Kazutoshi Watanabe , Yoshihiro Usui , Fumiaki Uehara , Satoshi Yokoshima , Daiki Sakai , Shin-ichi Kusaka , Kazuki Nakayama
IPC分类号： A61K31/538 , C07D403/02 , A61K31/506 , A61P25/00 , A61P3/00
CPC分类号： C07D413/14 , C07D401/04 , C07D401/14 , C07D403/14 , C07D409/14 , C07D453/06 , C07D493/04
摘要： A compound represented by the formula (I), an optically active isomer thereof, or a pharmaceutical acceptable salt thereof: wherein R2 represents a hydrogen or the like; R3 represents methyl group or the like; R20 represents a halogen atom or the like; q represents an integer of 0 to 3; Z represent nitrogen atom, CH, or the like; R4 represents hydrogen or the like; R5 represents hydrogen or the like; R6 represents a substituted alkyloxy and the like; p represents an integer of 0 to 3; X represents bond, CH2, oxygen atom, NH, or the like; any one or more of R5 and R6, R5 and R4, R6 and R4, X and R5, X and R4, X and R6, and R6 and R6 may combine to each other to form a ring, which is used for preventive and/or therapeutic treatment of a disease caused by tau protein kinase 1 hyperactivity such as a neurodegenerative diseases (e.g. Alzheimer disease).
摘要翻译：由式（I）表示的化合物或其光学活性异构体或其药学上可接受的盐：其中R2表示氢等; R3表示甲基等; R 20表示卤素原子等; q表示0〜3的整数， Z表示氮原子，CH等; R4表示氢等; R5表示氢等; R6表示取代的烷氧基等; p表示0〜3的整数， X表示键，CH2，氧原子，NH等; R 5和R 6，R 5和R 4，R 6和R 4，X和R 5，X和R 4，X和R 6以及R 6和R 6中的任何一个或多个可以彼此结合形成环，其用于预防和/ 或治疗由tau蛋白激酶1多动症如神经变性疾病（例如阿尔茨海默病）引起的疾病。

7. 发明授权

US08569294B2 2-(cyclic amino)-pyrimidone derivatives 失效
标题翻译： 2-（环状氨基） - 嘧啶酮衍生物
公开(公告)号：US08569294B2
公开(公告)日：2013-10-29
申请号：US12282396
申请日：2007-03-14
申请人： Kenji Fukunaga , Toshiyuki Kohara , Kazutoshi Watanabe , Yoshihiro Usui , Fumiaki Uehara , Satoshi Yokoshima , Daiki Sakai , Shin-ichi Kusaka , Kazuki Nakayama
发明人： Kenji Fukunaga , Toshiyuki Kohara , Kazutoshi Watanabe , Yoshihiro Usui , Fumiaki Uehara , Satoshi Yokoshima , Daiki Sakai , Shin-ichi Kusaka , Kazuki Nakayama
IPC分类号： A61K31/535
CPC分类号： C07D413/14 , C07D401/04 , C07D401/14 , C07D403/14 , C07D409/14 , C07D453/06 , C07D493/04
摘要： A compound represented by the formula (I), an optically active isomer thereof, or a pharmaceutical acceptable salt thereof: wherein R2 represents a hydrogen or the like; R3 represents methyl group or the like; R20 represents a halogen atom or the like; q represents an integer of 0 to 3; Z represent nitrogen atom, CH, or the like; R4 represents hydrogen or the like; R5 represents hydrogen or the like; R6 represents a substituted alkyloxy and the like; p represents an integer of 0 to 3; X represents bond, CH2, oxygen atom, NH, or the like; any one or more of R5 and R6, R5 and R4, R6 and R4, X and R5, X and R4, X and R6, and R6 and R6 may combine to each other to form a ring, which is used for preventive and/or therapeutic treatment of a disease caused by tau protein kinase 1 hyperactivity such as a neurodegenerative diseases (e.g. Alzheimer disease).
摘要翻译：由式（I）表示的化合物或其光学活性异构体或其药学上可接受的盐：其中R2表示氢等; R3表示甲基等; R 20表示卤素原子等; q表示0〜3的整数， Z表示氮原子，CH等; R4表示氢等; R5表示氢等; R6表示取代的烷氧基等; p表示0〜3的整数， X表示键，CH2，氧原子，NH等; R 5和R 6，R 5和R 4，R 6和R 4，X和R 5，X和R 4，X和R 6以及R 6和R 6中的任何一个或多个可以彼此结合形成环，其用于预防和/ 或治疗由tau蛋白激酶1多动症如神经变性疾病（例如阿尔茨海默病）引起的疾病。

8. 发明授权

US07420052B2 Intermediates for synthesis of vinblastine, process for preparation of the intermediates and process for synthesis of vinblastines 失效
标题翻译：用于合成长春花碱的中间体，中间体的制备方法和长春花碱的合成方法
公开(公告)号：US07420052B2
公开(公告)日：2008-09-02
申请号：US11464560
申请日：2006-08-15
申请人： Tohru Fukuyama , Hidetoshi Tokuyama , Satoshi Yokoshima
发明人： Tohru Fukuyama , Hidetoshi Tokuyama , Satoshi Yokoshima
IPC分类号： C07D487/04
CPC分类号： C07D487/04 , C07D519/04 , C07F7/1804
摘要： An intermediate for vinblastine synthesis represented by general formula A. general formula A. (in the formula, R1, R2, R3 and R4 are the group selected independently from the group consisting of H, lower alkyl group, lower alkoxy group, halogen, lower perfluoroalkyl group, lower alkylthio group, hydroxy group, amino group, mono- or di-alkyl or acylamino group, lower alkyl or arylsulfonyloxy group. R5 is H, or a lower alkyl group or a substituted or non-substituted aryl group, R6 is an alkyl group of carbon number 4 or less, R7 is a substituted or non-substituted aryl group, R8 is a substituted or non-substituted aryl group or lower alkyl group and R9 is an acyl group or trialkylsilyl group.) A method for synthesis of the compound of general formula A utilizing radical ring forming reaction of thioanilides and using the compound of general formula B as the starting material, synthesizing thioanilide of general formula C by the reaction with compound 1 and the formation of a 11-membered ring by intramolecular alkylation of 2-nitrobenzenesulfonamide by which the reactions can proceed under mild conditions and high yield can be accomplished.
摘要翻译：通式A表示的长春花碱合成中间体（通式A）（式中，R 1，R 2，R 3，和 R 4是独立地选自H，低级烷基，低级烷氧基，卤素，低级全氟烷基，低级烷硫基，羟基，氨基，单 - 或二 - 烷基或酰氨基，低级烷基或芳基磺酰氧基，R 5是H或低级烷基或取代或未取代的芳基，R 6是烷基碳原子数4以下的基团，R 7是取代或未取代的芳基，R 8是取代或未取代的芳基或低级烷基， R 9是酰基或三烷基甲硅烷基。）通过使用硫代苯酰苯胺的自由基形成反应合成通式A的化合物的方法，使用通式B的化合物作为起始原料，合成通过与化合物1的反应和通过2-硝基苯磺酰胺的分子内烷基化形成11元环的通式C的硫代苯胺，可以在温和条件下进行反应并获得高产率。

9. 发明申请

US20100010225A1 ISOQUINUCLIDINE DERIVATIVE AND METHOD FOR MANUFACTURING 1-CYCLOHEXENE-1-CARBOXYLIC ACID DERIVATIVE USING THE SAME 审中-公开
标题翻译：使用该化合物的异喹啉衍生物及其制备1-环己基-1-羧酸衍生物的方法
公开(公告)号：US20100010225A1
公开(公告)日：2010-01-14
申请号：US12309674
申请日：2007-07-27
申请人： Tohru Fukuyama , Satoshi Yokoshima , Nobuhiro Satoh
发明人： Tohru Fukuyama , Satoshi Yokoshima , Nobuhiro Satoh
IPC分类号： C07D221/22 , C07D453/02
CPC分类号： C07C271/24 , C07C269/00 , C07C2601/16 , C07D453/06 , C07D491/18 , Y02P20/55
摘要： The present invention provides an isoquinuclidine derivative which can be used to easily synthesize oseltamivir or an analog thereof. In particular, the present invention provides an isoquinuclidine derivative represented by the following formula (1) or an enantiomer thereof: wherein in the formula (1), A represents a protective group for the nitrogen atom; R1 to R1 each independently represent an alkyl group which may have a substituent, an aryl group which may have a substituent, or a hydrogen atom; and X represents a halogen atom.
摘要翻译：本发明提供了可用于容易地合成奥司他韦或其类似物的异奎宁环衍生物。特别是本发明提供下述式（1）所示的异奎宁环衍生物或其对映异构体：其中，在式（1）中，A表示氮原子的保护基; R 1〜R 1各自独立地表示可以具有取代基的烷基，可以具有取代基的芳基或氢原子; X表示卤素原子。

10. 发明授权

US07238802B2 Intermediates for synthesis of vinblastines, process for preparation of the intermediates and process for synthesis on vinblastines 失效
标题翻译：用于合成长春花碱的中间体，中间体的制备方法和长春花碱合成方法
公开(公告)号：US07238802B2
公开(公告)日：2007-07-03
申请号：US10486384
申请日：2002-08-09
申请人： Tohru Fukuyama , Hidetoshi Tokuyama , Satoshi Yokoshima
发明人： Tohru Fukuyama , Hidetoshi Tokuyama , Satoshi Yokoshima
IPC分类号： C07D487/04 , C07D519/04 , C07F7/18
CPC分类号： C07D487/04 , C07D519/04 , C07F7/1804
摘要： An intermediate for vinblastine synthesis represented by general formula A. general formula A. (in the formula, R1, R2, R3 and R4 are the group selected independently from the group consisting of H, lower alkyl group, lower alkoxy group, halogen, lower perfluoroalkyl group, lower alkylthio group, hydroxy group, amino group, mono- or di-alkyl or acylamino group, lower alkyl or arylsulfonyloxy group. R5 is H, or a lower alkyl group or a substituted or non-substituted aryl group, R6 is an alkyl group of carbon number 4 or less, R7 is a substituted or non-substituted aryl group, R8 is a substituted or non-substituted aryl group or lower alkyl group and R9 is an acyl group or trialkylsilyl group.) A method for synthesis of the compound of general formula A utilizing radical ring forming reaction of thioanilides and using the compound of general formula B as the starting material, synthesizing thioanilide of general formula C by the reaction with compound 1 and the formation of a 11-membered ring by intramolecular alkylation of 2-nitrobenzenesulfonamide by which the reactions can proceed under mild conditions and high yield can be accomplished.
摘要翻译：通式A表示的长春花碱合成中间体（通式A）（式中，R 1，R 2，R 3，和 R 4是独立地选自H，低级烷基，低级烷氧基，卤素，低级全氟烷基，低级烷硫基，羟基，氨基，单 - 或二 - 烷基或酰氨基，低级烷基或芳基磺酰氧基，R 5是H或低级烷基或取代或未取代的芳基，R 6是烷基碳原子数4以下的基团，R 7是取代或未取代的芳基，R 8是取代或未取代的芳基或低级烷基， R 9是酰基或三烷基甲硅烷基。）通过使用硫代苯酰苯胺的自由基形成反应合成通式A的化合物的方法，使用通式B的化合物作为起始原料，合成通过与化合物1的反应和通过2-硝基苯磺酰胺的分子内烷基化形成11元环的通式C的硫代苯胺，可以在温和条件下进行反应并获得高产率。

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