专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明授权

US08940738B2 Pyrimidone compounds 有权
标题翻译：嘧啶酮化合物
公开(公告)号：US08940738B2
公开(公告)日：2015-01-27
申请号：US13389504
申请日：2010-08-11
申请人： Daiki Sakai , Kazuki Nakayama , Kazutoshi Watanabe
发明人： Daiki Sakai , Kazuki Nakayama , Kazutoshi Watanabe
IPC分类号： A61K31/5377 , A61P25/28 , A61P9/10 , C07D413/04 , C07D401/04 , C07D413/14
CPC分类号： C07D413/04 , C07D401/04 , C07D413/14
摘要： A pyrimidone derivative represented by general formula (I) or a pharmaceutically acceptable salt thereof: wherein X represents hydrogen atom and Y represents hydroxyl group, or X represents fluorine atom and Y represents hydrogen atom; R1 represents a C1-6 alkyl group; R2 represents a morpholin-4-yl group which may be substituted, 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：由通式（I）表示的嘧啶酮衍生物或其药学上可接受的盐：其中X表示氢原子，Y表示羟基，或X表示氟原子，Y表示氢原子; R1表示C1-6烷基; R2表示可被取代的吗啉-4-基，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. 发明申请

US20120059165A1 INTERMEDIATE COMPOUND FOR SYNTHESIZING PHARMACEUTICAL AGENT AND PRODUCTION METHOD THEREOF 审中-公开
标题翻译：用于合成药物代理的中间体化合物及其生产方法
公开(公告)号：US20120059165A1
公开(公告)日：2012-03-08
申请号：US13255748
申请日：2010-03-09
申请人： Rikizou Furuya , Hiroki Ozawa , Eiji Toyofuku , Shinichi Kusaka , Hiroshi Iwamura , Daiki Sakai , Kazuki Nakayama , Kazutoshi Watanabe
发明人： Rikizou Furuya , Hiroki Ozawa , Eiji Toyofuku , Shinichi Kusaka , Hiroshi Iwamura , Daiki Sakai , Kazuki Nakayama , Kazutoshi Watanabe
IPC分类号： C07D413/10 , C07D413/14
CPC分类号： C07D413/10 , C07D413/14
摘要： A production method of an optically active 2-{4-(5-substituted-oxadiazolyl) phenyl}morpholine which is useful as an intermediate for synthesizing a pharmaceutical agent is provided and the method comprises the following steps 1) to 4): 1) reacting a bromophenylmorpholine with a hexacyanoferrate(II) or a hydrate thereof at a temperature of from 110° C. to 140° C. in a reaction mixture comprising a Na2CO3, an organophosphorus compound, and a palladium catalyst in a polar aprotic solvent alone or combination of a polar aprotic solvent and other polar aprotic solvent or hydrocarbon solvent to give a cyanophenylmorpholine; 2) reacting the cyanophenylmorpholine with hydroxylamine or hydroxylamine hydrochloride at a temperature of from 10° C. to 40° C. in an aprotic polar solvent to give a hydroxylamine derivative; 3) reacting the hydroxylamine derivative with an acylation reagent selected from the group consisting of aliphatic acyl halides, aromatic acyl halides, aliphatic acyl anhydrides and aromatic anhydrides; and 4) keeping the mixture obtained after step 3) at a temperature of from 60° C. to 140° C. to give a 2-{4-(5-substituted-oxadiazolyl) phenyl}morpholine.
摘要翻译：提供了可用作合成药剂的中间体的光学活性2- {4-（5-取代 - 恶二唑基）苯基}吗啉的制备方法，该方法包括以下步骤1）至4）：1）在包含Na 2 CO 3，有机磷化合物和钯催化剂的反应混合物中，在单极极性非质子溶剂中使溴苯基吗啉与六氰基铁酸盐（II）或其水合物在110℃至140℃的温度下反应，或极性非质子溶剂和其他极性非质子溶剂或烃溶剂的组合，得到氰基苯基吗啉; 2）使氰基苯基吗啉与羟胺或羟胺盐酸盐在非质子极性溶剂中在10℃至40℃的温度下反应，得到羟胺衍生物; 3）使羟胺衍生物与选自脂族酰基卤，芳族酰基卤，脂族酰基酸酐和芳族酸酐的酰化试剂反应; 和4）将步骤3）后获得的混合物保持在60℃至140℃的温度下，得到2- {4-（5-取代 - 恶二唑基）苯基}吗啉。

3. 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。

4. 发明授权

US09108957B2 3-[1,4]oxazepane-4-pyrimidone derivatives 有权
标题翻译： 3- [1,4]氧氮杂环庚烷-4-嘧啶酮衍生物
公开(公告)号：US09108957B2
公开(公告)日：2015-08-18
申请号：US13262396
申请日：2010-04-01
申请人： Kazutoshi Watanabe , Kazuki Nakayama , Daiki Sakai
发明人： Kazutoshi Watanabe , Kazuki Nakayama , Daiki Sakai
IPC分类号： A61K31/553 , C07D401/14 , C07D403/14 , C07D413/14
CPC分类号： C07D413/14 , C07D401/14 , C07D403/14
摘要： A compound represented by the formula (I) or a pharmaceutically acceptable salt thereof: wherein Z represents nitrogen atom, C—F or the like; R1 represents a C1-C3 alkyl group; Y represents oxygen atom or N—R7; R2, R3, R4, R5, R6 and R7 each independently represents hydrogen atom, a C1-C6 alkyl group, or a group represented by the formula (II): 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）表示的化合物或其药学上可接受的盐：其中Z表示氮原子，C-F等; R1表示C1-C3烷基; Y表示氧原子或N-R7; R2，R3，R4，R5，R6和R7各自独立地表示氢原子，C1-C6烷基或由式（II）表示的基团：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（如阿兹海默症）。

5. 发明授权

US09006232B2 Pyrimidone derivatives 有权
标题翻译：嘧啶衍生物
公开(公告)号：US09006232B2
公开(公告)日：2015-04-14
申请号：US13389512
申请日：2010-08-11
申请人： Kazuki Nakayama , Daiki Sakai , Kazutoshi Watanabe , Toshiyuki Kohara , Keiichi Aritomo
发明人： Kazuki Nakayama , Daiki Sakai , Kazutoshi Watanabe , Toshiyuki Kohara , Keiichi Aritomo
IPC分类号： A61K31/5377 , A61K31/536 , A61K31/505 , A61K31/55 , C07D403/14 , C07D413/14 , C07D265/14 , C07D401/12 , C07D233/76 , C07D401/14 , C07D407/12 , C07D409/14
CPC分类号： C07D401/12 , C07D233/76 , C07D401/14 , C07D407/12 , C07D409/14 , C07D413/14
摘要： A compound represented by the formula (I) or a pharmaceutically acceptable salt thereof: wherein Z represents nitrogen atom or C—X; X represents hydrogen atom or fluorine atom; R1 is hydrogen atom or a C1-C3 alkyl group; L represents single bond or a C1-C6 alkylene group which may be substituted; Y represents single bond, sulfur atom, oxygen atom, NH, or the like; R2 represents hydrogen atom or a cyclic group which may be substituted, which is used for preventive and/or therapeutic treatment of a disease caused by abnormal activity of tau protein kinase 1 such as a neurodegenerative diseases (e.g. Alzheimer disease).
摘要翻译：由式（I）表示的化合物或其药学上可接受的盐：其中Z表示氮原子或C-X; X表示氢原子或氟原子; R1是氢原子或C1-C3烷基; L表示单键或可以被取代的C1-C6亚烷基; Y表示单键，硫原子，氧原子，NH等; R2代表氢原子或可被取代的环状基团，其用于预防和/或治疗由tau蛋白激酶1的异常活性如神经变性疾病（例如阿尔茨海默病）引起的疾病。

6. 发明申请

US20120208797A1 PYRIMIDONE DERIVATIVES 有权
标题翻译：吡咯烷酮衍生物
公开(公告)号：US20120208797A1
公开(公告)日：2012-08-16
申请号：US13389512
申请日：2010-08-11
申请人： Kazuki Nakayama , Daiki Sakai , Kazutoshi Watanabe , Toshiyuki Kohara , Keiichi Aritomo
发明人： Kazuki Nakayama , Daiki Sakai , Kazutoshi Watanabe , Toshiyuki Kohara , Keiichi Aritomo
IPC分类号： A61K31/55 , A61K31/506 , C07D413/14 , A61K31/5377 , C07D265/14 , A61K31/536 , A61P25/28 , A61P25/00 , A61P25/16 , A61P3/10 , A61P3/04 , A61P25/24 , A61P25/18 , A61P35/00 , A61P35/02 , A61P33/06 , C07D403/14
CPC分类号： C07D401/12 , C07D233/76 , C07D401/14 , C07D407/12 , C07D409/14 , C07D413/14
摘要： A compound represented by the formula (I) or a pharmaceutically acceptable salt thereof: wherein Z represents nitrogen atom or C—X; X represents hydrogen atom or fluorine atom; R1 is hydrogen atom or a C1-C3 alkyl group; L represents single bond or a C1-C6 alkylene group which may be substituted; Y represents single bond, sulfur atom, oxygen atom, NH, or the like; R2 represents hydrogen atom or a cyclic group which may be substituted, which is used for preventive and/or therapeutic treatment of a disease caused by abnormal activity of tau protein kinase 1 such as a neurodegenerative diseases (e.g. Alzheimer disease).
摘要翻译：由式（I）表示的化合物或其药学上可接受的盐：其中Z表示氮原子或C-X; X表示氢原子或氟原子; R1是氢原子或C1-C3烷基; L表示单键或可以被取代的C1-C6亚烷基; Y表示单键，硫原子，氧原子，NH等; R2代表氢原子或可被取代的环状基团，其用于预防和/或治疗由tau蛋白激酶1的异常活性如神经变性疾病（例如阿尔茨海默病）引起的疾病。

7. 发明申请

US20120220591A1 PYRIMIDONE COMPOUNDS 有权
标题翻译：吡咯烷酮化合物
公开(公告)号：US20120220591A1
公开(公告)日：2012-08-30
申请号：US13389504
申请日：2010-08-11
申请人： Daiki Sakai , Kazuki Nakayama , Kazutoshi Watanabe
发明人： Daiki Sakai , Kazuki Nakayama , Kazutoshi Watanabe
IPC分类号： A61K31/5377 , A61P25/28 , A61P9/10 , A61P25/00 , A61P25/16 , A61P25/02 , A61P27/02 , A61P27/06 , A61P3/10 , A61P3/04 , A61P25/18 , A61P35/00 , A61P35/02 , A61P33/06 , C07D413/14
CPC分类号： C07D413/04 , C07D401/04 , C07D413/14
摘要： A pyrimidone derivative represented by general formula (I) or a pharmaceutically acceptable salt thereof: wherein X represents hydrogen atom and Y represents hydroxyl group, or X represents fluorine atom and Y represents hydrogen atom; R1 represents a C1-6 alkyl group; R2 represents a morpholin-4-yl group which may be substituted, 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：由通式（I）表示的嘧啶酮衍生物或其药学上可接受的盐：其中X表示氢原子，Y表示羟基，或X表示氟原子，Y表示氢原子; R1表示C1-6烷基; R2表示可被取代的吗啉-4-基，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. 发明申请

US20120095216A1 3-[1,4]OXAZEPANE-4-PYRIMIDONE DERIVATIVES 有权
标题翻译： 3- [1,4]氧杂环丁烷-4-吡啶酮衍生物
公开(公告)号：US20120095216A1
公开(公告)日：2012-04-19
申请号：US13262396
申请日：2010-04-01
申请人： Kazutoshi Watanabe , Kazuki Nakayama , Daiki Sakai
发明人： Kazutoshi Watanabe , Kazuki Nakayama , Daiki Sakai
IPC分类号： C07D413/14
CPC分类号： C07D413/14 , C07D401/14 , C07D403/14
摘要： A compound represented by the formula (I) or a pharmaceutically acceptable salt thereof: wherein Z represents nitrogen atom, C—F or the like; R1 represents a C1-C3 alkyl group; Y represents oxygen atom or N—R7; R2, R3, R4, R5, R6 and R7 each independently represents hydrogen atom, a C1-C6 alkyl group, or a group represented by the formula (II): 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）表示的化合物或其药学上可接受的盐：其中Z表示氮原子，C-F等; R1表示C1-C3烷基; Y表示氧原子或N-R7; R2，R3，R4，R5，R6和R7各自独立地表示氢原子，C1-C6烷基或由式（II）表示的基团：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（如阿兹海默症）。

9. 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。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式