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1. 发明授权

US09399635B2 Pyrazole derivative 有权
标题翻译：吡唑衍生物
公开(公告)号：US09399635B2
公开(公告)日：2016-07-26
申请号：US14110188
申请日：2012-04-11
申请人： Hachiro Sugimoto , Michiaki Okuda , Takashi Takahashi , Ichiro Hijikuro , Hidetaka Suzuki , Shinichi Nakayama
发明人： Hachiro Sugimoto , Michiaki Okuda , Takashi Takahashi , Ichiro Hijikuro , Hidetaka Suzuki , Shinichi Nakayama
IPC分类号： C07D401/14 , C07D403/10 , C07D405/14 , C07D209/12 , C07D401/12 , C07D403/06 , C07D405/12 , C07D409/12 , C07D409/14 , C07D417/12 , C07D417/14 , C07H15/203 , C07D403/14 , C07H15/26
CPC分类号： C07D401/14 , C07D209/12 , C07D401/12 , C07D403/06 , C07D403/10 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D417/12 , C07D417/14 , C07H15/203 , C07H15/26
摘要： Provided is a novel therapeutic means for Alzheimer's disease. In particular, provided is a compound represented by the following general formula (I): [wherein Ar1 represents 2-methoxy-4-(2-pyridylmethoxy)phenyl etc. and Ar2 represents a 1H-indol-6-yl group etc.] or a salt thereof.
摘要翻译：提供了阿尔茨海默病的新型治疗方法。特别地，提供由以下通式（I）表示的化合物：[其中Ar 1表示2-甲氧基-4-（2-吡啶基甲氧基）苯基等，Ar 2表示1H-吲哚-6-基等] 或其盐。

2. 发明申请

US20140088029A1 NOVEL PYRAZOLE DERIVATIVE 有权
标题翻译：新型吡咯衍生物
公开(公告)号：US20140088029A1
公开(公告)日：2014-03-27
申请号：US14110188
申请日：2012-04-11
申请人： Hachiro Sugimoto , Michiaki Okuda , Takashi Takahashi , Ichiro Hijikuro , Hidetaka Suzuki , Shinichi Nakayama
发明人： Hachiro Sugimoto , Michiaki Okuda , Takashi Takahashi , Ichiro Hijikuro , Hidetaka Suzuki , Shinichi Nakayama
IPC分类号： C07D401/14 , C07D403/10 , C07H15/26 , C07D405/14 , C07D403/06
CPC分类号： C07D401/14 , C07D209/12 , C07D401/12 , C07D403/06 , C07D403/10 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D417/12 , C07D417/14 , C07H15/203 , C07H15/26
摘要： Provided is a novel therapeutic means for Alzheimer's disease. In particular, provided is a compound represented by the following general formula (I): [wherein Ar1 represents 2-methoxy-4-(2-pyridylmethoxy)phenyl etc. and Ar2 represents a 1H-indol-6-yl group etc.] or a salt thereof.
摘要翻译：提供了阿尔茨海默病的新型治疗方法。特别地，提供由以下通式（I）表示的化合物：[其中Ar 1表示2-甲氧基-4-（2-吡啶基甲氧基）苯基等，Ar 2表示1H-吲哚-6-基等] 或其盐。

3. 发明申请

US20110082295A1 NOVEL CURCUMIN DERIVATIVE 失效
标题翻译：新的CURCUMIN DERIVATIVE
公开(公告)号：US20110082295A1
公开(公告)日：2011-04-07
申请号：US12994472
申请日：2009-05-27
申请人： Hachiro Sugimoto , Takashi Takahashi , Ichiro Hijikuro , Michiaki Okuda
发明人： Hachiro Sugimoto , Takashi Takahashi , Ichiro Hijikuro , Michiaki Okuda
IPC分类号： C07D243/08 , C07C49/248 , C07C205/56 , C07C211/45 , C07C69/78 , C07D213/76 , C07D209/12 , C07D209/14 , C07C309/63 , C07D249/08 , C07D249/04 , C07C247/18 , C07D257/04 , C07D211/04 , C07D241/04
CPC分类号： C07C225/22 , C07C49/248 , C07C69/76 , C07C69/94 , C07C205/45 , C07C311/29 , C07C317/24 , C07D209/08 , C07D211/14 , C07D211/32 , C07D213/30 , C07D213/61 , C07D241/04 , C07D243/08 , C07D249/04 , C07D249/06 , C07D249/08 , C07D257/04 , C07D295/06 , C07D295/112 , C07D295/205
摘要： To develop a highly safe measure to treat Alzheimer's disease using a secretase-inhibiting substance, there is provided a compound represented by the following general formula (I) or a salt thereof: wherein A represents a phenyl group or the like, R1 represents a chlorine atom, a bromine atom, or a nitro group or the like, R2, R3, R4, and R5 each represent a hydrogen atom or the like, and L represents CH2—CH2 or CH═CH.
摘要翻译：为了开发使用分泌酶抑制物质治疗阿尔茨海默病的高度安全的措施，提供了由以下通式（I）表示的化合物或其盐：其中A表示苯基等，R 1表示氯原子，溴原子或硝基等，R 2，R 3，R 4和R 5各自表示氢原子等，L表示CH 2 -CH 2或CH = CH。

4. 发明授权

US08552220B2 Therapeutic agent for Alzheimer's disease 失效
标题翻译：阿尔茨海默病治疗剂
公开(公告)号：US08552220B2
公开(公告)日：2013-10-08
申请号：US12994472
申请日：2009-05-27
申请人： Hachiro Sugimoto , Takashi Takahashi , Ichiro Hijikuro , Michiaki Okuda
发明人： Hachiro Sugimoto , Takashi Takahashi , Ichiro Hijikuro , Michiaki Okuda
IPC分类号： C07C49/248
CPC分类号： C07C225/22 , C07C49/248 , C07C69/76 , C07C69/94 , C07C205/45 , C07C311/29 , C07C317/24 , C07D209/08 , C07D211/14 , C07D211/32 , C07D213/30 , C07D213/61 , C07D241/04 , C07D243/08 , C07D249/04 , C07D249/06 , C07D249/08 , C07D257/04 , C07D295/06 , C07D295/112 , C07D295/205
摘要： To develop a highly safe measure to treat Alzheimer's disease using a secretase-inhibiting substance, there is provided a compound represented by the following general formula (I) or a salt thereof: wherein A represents a phenyl group or the like, R1 represents a chlorine atom, a bromine atom, or a nitro group or the like, R2, R3, R4, and R5 each represent a hydrogen atom or the like, and L represents CH2—CH2 or CH═CH.
摘要翻译：为了开发使用分泌酶抑制物质治疗阿尔茨海默病的高度安全的措施，提供了由以下通式（I）表示的化合物或其盐：其中A表示苯基等，R 1表示氯原子，溴原子或硝基等，R 2，R 3，R 4和R 5各自表示氢原子等，L表示CH 2 -CH 2或CH = CH。

5. 发明申请

US20110294850A1 INDOLINE DERIVATIVES 失效
标题翻译：吲哚衍生物
公开(公告)号：US20110294850A1
公开(公告)日：2011-12-01
申请号：US13148011
申请日：2010-02-03
申请人： Hachiro Sugimoto , Jun Takahashi , Takashi Takahashi , Ichiro Hijikuro
发明人： Hachiro Sugimoto , Jun Takahashi , Takashi Takahashi , Ichiro Hijikuro
IPC分类号： A61K31/475 , C07D403/06 , C07D405/12 , C07D401/12 , A61P25/00 , C07D403/12 , A61K31/404 , A61K31/4439 , A61K31/454 , A61P25/28 , C07D209/08 , C07D401/06
CPC分类号： C07D405/14 , C07D209/08 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D409/12
摘要： The present invention provides a novel indoline derivative or a pharmacologically acceptable salt thereof or a solvate of the derivative or a salt thereof represented by the following formula (1) that has an excellent butyrylcholinesterase inhibitory activity. In the formula, R1 represents an alkyl group, a cycloalkyl group, a heterocycloalkyl group, an aryl group, a heteroaryl group, an arylalkyl group, a heteroarylalkyl group, a cycloalkylalkyl group, a heterocycloalkylalkyl group, a dihydrofurylalkyl group, an alkenyl group, a tetrahydronaphthyl group, or an indanyl group; R2 represents a hydrogen atom, an alkyl group, an arylalkyl group, a cycloalkylalkyl group, a heteroarylalkyl group, a heterocycloalkylalkyl group, an aryl group, or an acyl group; R3 each independently represents a hydrogen atom, an alkyl group, or a dialkylaminocarbonyl group; R4 each independently represents a hydrogen atom or an alkyl group; and R5 represents a hydrogen atom or an alkyl group. Each functional group may have a substituent.
摘要翻译：本发明提供具有优异的丁酰胆碱酯酶抑制活性的新型二氢吲哚衍生物或其药理学上可接受的盐或其由下式（1）表示的衍生物或其盐的溶剂合物。在该式中，R 1表示烷基，环烷基，杂环烷基，芳基，杂芳基，芳烷基，杂芳基烷基，环烷基烷基，杂环烷基烷基，二氢呋喃基烷基，烯基，四氢萘基或茚满基; R2表示氢原子，烷基，芳基烷基，环烷基烷基，杂芳基烷基，杂环烷基烷基，芳基或酰基; R3各自独立地表示氢原子，烷基或二烷基氨基羰基; R4各自独立地表示氢原子或烷基; R 5表示氢原子或烷基。每个官能团可以具有取代基。

6. 发明申请

US20100048901A1 NOVEL CURCUMIN DERIVATIVE 有权
标题翻译：新的CURCUMIN DERIVATIVE
公开(公告)号：US20100048901A1
公开(公告)日：2010-02-25
申请号：US12516948
申请日：2007-11-30
申请人： Takashi Takahashi , Ichiro Hijikuro , Hachiro Sugimoto , Takeshi Kihara , Yoshiari Shimmyo , Tetsuhiro Niidome
发明人： Takashi Takahashi , Ichiro Hijikuro , Hachiro Sugimoto , Takeshi Kihara , Yoshiari Shimmyo , Tetsuhiro Niidome
IPC分类号： C07C49/203 , C07D211/82 , C07D241/40
CPC分类号： C07D209/08 , A61K31/404 , C07D209/12
摘要： The present invention provides a novel compound that is structurally similar to curcumin and has a suppressive effect on Aβ aggregation, a degradative effect on Aβ aggregates, an inhibitory effect on β-secretase, and a protective effect on neurons. The novel compound is a compound represented by the following general formula (Ia) or a salt thereof: wherein R1 represents a 4-hydroxy-3-methoxyphenyl group or the like, and R2 represents a 1H-indol-6-yl group or the like.
摘要翻译：本发明提供了结构上类似于姜黄素并对A＆Bgr具有抑制作用的新型化合物; 聚集，对A＆Bgr的降解作用; 聚集体，对分泌酶的抑制作用，以及对神经元的保护作用。新化合物是由下列通式（Ia）表示的化合物或其盐：其中R1表示4-羟基-3-甲氧基苯基等，R2表示1H-吲哚-6-基或喜欢。

7. 发明授权

US08962674B2 Curcumin derivative 有权
标题翻译：姜黄素衍生物
公开(公告)号：US08962674B2
公开(公告)日：2015-02-24
申请号：US12516948
申请日：2007-11-30
申请人： Takashi Takahashi , Ichiro Hijikuro , Hachiro Sugimoto , Takeshi Kihara , Yoshiari Shimmyo , Tetsuhiro Niidome
发明人： Takashi Takahashi , Ichiro Hijikuro , Hachiro Sugimoto , Takeshi Kihara , Yoshiari Shimmyo , Tetsuhiro Niidome
IPC分类号： A61K31/404 , C07D209/12 , C07D209/08
CPC分类号： C07D209/08 , A61K31/404 , C07D209/12
摘要： The present invention provides a novel compound that is structurally similar to curcumin and has a suppressive effect on Aβ aggregation, a degradative effect on Aβ aggregates, an inhibitory effect on β-secretase, and a protective effect on neurons. The novel compound is a compound represented by the following general formula (Ia) or a salt thereof: wherein R1 represents a 4-hydroxy-3-methoxyphenyl group or the like, and R2 represents a 1H-indol-6-yl group or the like.
摘要翻译：本发明提供了结构上类似于姜黄素并对A＆Bgr具有抑制作用的新型化合物; 聚集，对A＆Bgr的降解作用; 聚集体，对分泌酶的抑制作用，以及对神经元的保护作用。新化合物是由下列通式（Ia）表示的化合物或其盐：其中R1表示4-羟基-3-甲氧基苯基等，R2表示1H-吲哚-6-基或喜欢。

8. 发明授权

US08686024B2 Indoline derivatives 失效
标题翻译：二氢吲哚衍生物
公开(公告)号：US08686024B2
公开(公告)日：2014-04-01
申请号：US13148011
申请日：2010-02-03
申请人： Hachiro Sugimoto , Jun Takahashi , Takashi Takahashi , Ichiro Hijikuro
发明人： Hachiro Sugimoto , Jun Takahashi , Takashi Takahashi , Ichiro Hijikuro
IPC分类号： A61K31/404 , C07D209/10
CPC分类号： C07D405/14 , C07D209/08 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D409/12
摘要： The present invention provides a novel indoline derivative or a pharmacologically acceptable salt thereof or a solvate of the derivative or a salt thereof represented by the following formula (1) that has an excellent butyrylcholinesterase inhibitory activity. In the formula, R1 represents an alkyl group, a cycloalkyl group, a heterocycloalkyl group, an aryl group, a heteroaryl group, an arylalkyl group, a heteroarylalkyl group, a cycloalkylalkyl group, a heterocycloalkylalkyl group, a dihydrofurylalkyl group, an alkenyl group, a tetrahydronaphthyl group, or an indanyl group; R2 represents a hydrogen atom, an alkyl group, an arylalkyl group, a cycloalkylalkyl group, a heteroarylalkyl group, a heterocycloalkylalkyl group, an aryl group, or an acyl group; R3 each independently represents a hydrogen atom, an alkyl group, or a dialkylaminocarbonyl group; R4 each independently represents a hydrogen atom or an alkyl group; and R5 represents a hydrogen atom or an alkyl group. Each functional group may have a substituent.
摘要翻译：本发明提供具有优异的丁酰胆碱酯酶抑制活性的新型二氢吲哚衍生物或其药理学上可接受的盐或其由下式（1）表示的衍生物或其盐的溶剂合物。在该式中，R 1表示烷基，环烷基，杂环烷基，芳基，杂芳基，芳烷基，杂芳基烷基，环烷基烷基，杂环烷基烷基，二氢呋喃基烷基，烯基，四氢萘基或茚满基; R2表示氢原子，烷基，芳基烷基，环烷基烷基，杂芳基烷基，杂环烷基烷基，芳基或酰基; R3各自独立地表示氢原子，烷基或二烷基氨基羰基; R4各自独立地表示氢原子或烷基; R 5表示氢原子或烷基。每个官能团可以具有取代基。

9. 发明授权

US5620976A Benzoxazine derivatives 失效
标题翻译：苯并恶嗪衍生物
公开(公告)号：US5620976A
公开(公告)日：1997-04-15
申请号：US449739
申请日：1995-05-25
申请人： Hachiro Sugimoto , Masahiro Yonaga , Norio Karibe , Youichi Iimura , Satoshi Nagato , Atsushi Sasaki , Yoshiharu Yamanishi , Hiroo Ogura , Takashi Kosasa , Kumi Uchikoshi , Kiyomi Yamatsu
发明人： Hachiro Sugimoto , Masahiro Yonaga , Norio Karibe , Youichi Iimura , Satoshi Nagato , Atsushi Sasaki , Yoshiharu Yamanishi , Hiroo Ogura , Takashi Kosasa , Kumi Uchikoshi , Kiyomi Yamatsu
IPC分类号： A61K31/40 , A61K31/00 , A61K31/395 , A61K31/42 , A61K31/423 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/445 , A61K31/454 , A61K31/495 , A61K31/496 , A61K31/4985 , A61K31/505 , A61K31/517 , A61K31/519 , A61K31/535 , A61K31/536 , A61K31/5365 , A61K31/5377 , A61K31/55 , A61P9/00 , A61P25/00 , A61P25/02 , A61P25/28 , A61P43/00 , C07D207/16 , C07D263/58 , C07D265/18 , C07D265/26 , C07D401/04 , C07D401/06 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/06 , C07D413/12 , C07D413/14 , C07D471/04 , C07D475/02 , C07D487/04 , C07D495/04 , C07D498/04 , C12N9/99
CPC分类号： C07D401/06 , C07D401/14 , C07D413/06 , C07D413/14 , C07D471/04 , C07D487/04 , C07D495/04
摘要： The cyclic amide derivative is defined by the formula (I) or a salt thereof: R.sup.1 --(CH2)n--Z in which R.sup.1 is a group derived from a cyclic amide compound, substituted or unsubstituted, n is zero or an integer of 1 to 10 and Z is ##STR1## R.sup.2 being an aryl, a substituted aryl, a cycloalkyl or a heterocyclic group, m being an integer of 1 to 6, R.sup.3 being hydrogen or a lower alkyl, R.sup.4 being an aryl or a substituted aryl, a cycloalkyl or a heterocyclic group, p being an integer of 1 to 6, provided that the cyclic amide compound is quinazoline-on or quinazoline-dion, R2 and R4 are neither aryl nor substituted aryl. The cyclic amide compound is pharmacologically effective to prevent and treat diseases due to insufficiency of the central choline functions.
摘要翻译：环酰胺衍生物由式（I）或其盐定义：R 1（CH 2）n Z，其中R 1是衍生自环状酰胺化合物的基团，取代或未取代的，n为0或1〜10的整数 Z为芳基，取代芳基，环烷基或杂环基，m为1〜6的整数，R3为氢或低级烷基，R4为芳基或取代芳基，环烷基或杂环基，p为1〜6的整数，条件是环酰胺化合物为喹唑啉或喹唑啉二酮，R2和R4既不是芳基也不是取代的芳基。环酰胺化合物在预防和治疗由于中枢胆碱功能不足引起的疾病方面具有药理作用。

10. 发明授权

US5292735A Cyclic amide derivatives 失效
标题翻译：环状酰胺衍生物
公开(公告)号：US5292735A
公开(公告)日：1994-03-08
申请号：US715754
申请日：1991-06-14
申请人： Hachiro Sugimoto , Masahiro Yonaga , Norio Karibe , Youichi Iimura , Satoshi Nagato , Atsushi Sasaki , Yoshiharu Yamanishi , Hiroo Ogura , Takashi Kosasa , Kumi Uchikoshi , Kiyomi Yamatsu
发明人： Hachiro Sugimoto , Masahiro Yonaga , Norio Karibe , Youichi Iimura , Satoshi Nagato , Atsushi Sasaki , Yoshiharu Yamanishi , Hiroo Ogura , Takashi Kosasa , Kumi Uchikoshi , Kiyomi Yamatsu
IPC分类号： A61K31/40 , A61K31/00 , A61K31/395 , A61K31/42 , A61K31/423 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/445 , A61K31/454 , A61K31/495 , A61K31/496 , A61K31/4985 , A61K31/505 , A61K31/517 , A61K31/519 , A61K31/535 , A61K31/536 , A61K31/5365 , A61K31/5377 , A61K31/55 , A61P9/00 , A61P25/00 , A61P25/02 , A61P25/28 , A61P43/00 , C07D207/16 , C07D263/58 , C07D265/18 , C07D265/26 , C07D401/04 , C07D401/06 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/06 , C07D413/12 , C07D413/14 , C07D471/04 , C07D475/02 , C07D487/04 , C07D495/04 , C07D498/04 , C12N9/99
CPC分类号： C07D401/06 , C07D401/14 , C07D413/06 , C07D413/14 , C07D471/04 , C07D487/04 , C07D495/04
摘要： The cyclic amide derivative is defined by the formula (I) or a salt thereof: R1--(CH2)n-z in which R1 is a group derived from a cyclic amide compound, substituted or unsubstituted, n is zero or an integer of 1 to 10 and Z is ##STR1## R2 being an aryl, a substituted aryl, a cycloalkyl or a heterocyclic group, m being an integer of 1 to 6, R3 being hydrogen or a lower alkyl, R4 being an aryl or a substituted aryl, a cycloalkyl or a heterocyclic group, p being an integer of 1 to 6, provided that the cyclic amide compound is quinazoline-on or quinazoline-dion, R2 and R4 are neither aryl nor substituted aryl. The cyclic amide compound is pharmacologically effective to prevent and treat diseases due to insufficiency of the central choline functions.
摘要翻译：环酰胺衍生物由式（I）或其盐定义：R 1（CH 2）n z，其中R 1是衍生自环状酰胺化合物的基团，被取代或未取代的，n为0或1〜10的整数 Z为（*化学结构*）（1）或（*化学结构*）（2）R2为芳基，取代芳基，环烷基或杂环基，m为1〜6的整数，R3为氢或低级烷基，R4为芳基或取代芳基，环烷基或杂环基，p为1〜6的整数，条件是环酰胺化合物为喹唑啉或喹唑啉二酮，R2和R4均不为芳基或取代的芳基。环酰胺化合物在预防和治疗由于中枢胆碱功能不足引起的疾病方面具有药理作用。

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