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1. 发明授权

US08263607B2 1-substituted tetrahydroisoquinoline compound 有权
标题翻译： 1-取代的四氢异喹啉化合物
公开(公告)号：US08263607B2
公开(公告)日：2012-09-11
申请号：US12600503
申请日：2008-05-20
申请人： Jun-ichi Shishikura , Makoto Inoue , Takashi Ogiyama , Koichi Yonezawa , Susumu Yamaki , Kazuhiro Yokoyama , Shuichirou Kakimoto , Hidetsugu Okada
发明人： Jun-ichi Shishikura , Makoto Inoue , Takashi Ogiyama , Koichi Yonezawa , Susumu Yamaki , Kazuhiro Yokoyama , Shuichirou Kakimoto , Hidetsugu Okada
IPC分类号： C07D217/04 , C07D491/04 , A61K31/472
CPC分类号： C07D217/04 , C07D217/14 , C07D217/16 , C07D221/20 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/06 , C07D491/06
摘要： Provided is a compound useful as an N-type Ca2+ channel blocker. As a result of intensive studies of compounds having an action of blocking N-type Ca2+ channels, the present inventors found that a tetrahydroisoquinoline compound of the present invention having a substituent at the 1-position has an action of blocking the N-type Ca2+ channels, an antinociceptive pain action, an antineuropathic pain action, an abdominal pain-inhibitory action and an opioid-induced constipation-improving action, and the present invention has been completed based on these findings. The compound of the present invention can be used as a pharmaceutical composition for preventing and/or treating various pains such as neuropathic pain and nociceptive pain, headaches such as migraine and cluster headache, central nervous system diseases such as anxiety, depression, epilepsy, cerebral stroke and restless legs syndrome, abdominal symptoms such as abdominal pain and abdominal distension, stool abnormalities such as diarrhea and constipation, digestive system diseases such as irritable bowel syndrome, urinary system diseases such as overactive bladder and interstitial cystitis, etc.
摘要翻译：提供可用作N型Ca2 +通道阻断剂的化合物。通过对具有阻塞N型Ca 2+通道作用的化合物的深入研究，本发明人发现在1位具有取代基的本发明的四氢异喹啉化合物具有阻断N型Ca 2+通道的作用抗痛知性疼痛作用，抗神经病性疼痛作用，腹痛抑制作用和阿片样物质诱导的便秘改善作用，并且基于这些发现完成了本发明。本发明的化合物可以用作预防和/或治疗诸如神经性疼痛和伤害性疼痛，头痛如偏头痛和丛集性头痛，中枢神经系统疾病如焦虑，抑郁，癫痫，脑的各种疼痛的药物组合物中风和不宁腿综合症，腹痛，腹胀等腹部症状，腹泻便秘等粪便异常，肠易激综合征等消化系统疾病，膀胱过多膀胱炎，间质性膀胱炎等泌尿系统疾病等。

2. 发明授权

US07989634B2 Melanocortin receptor agonists 失效
标题翻译：黑皮质素受体激动剂
公开(公告)号：US07989634B2
公开(公告)日：2011-08-02
申请号：US10579042
申请日：2004-11-12
申请人： Koo Lee , Heui-Sul Park , In-Ae Ahn , Hyun-Ju Yoo , Jong-Yup Kim , Deog-Young Choi , Hyeon-Joo Yim , Kyung-Ha Chung , Dong-Sup Shim , Sang-Kyun Lee , Yutaka Kondoh , Ryoji Hirabayashi , Shugo Honda , Hidetaka Kaku , Jun-ichi Shishikura , Hiroyuki Ito , Takeshi Kurama
发明人： Koo Lee , Heui-Sul Park , In-Ae Ahn , Hyun-Ju Yoo , Jong-Yup Kim , Deog-Young Choi , Hyeon-Joo Yim , Kyung-Ha Chung , Dong-Sup Shim , Sang-Kyun Lee , Yutaka Kondoh , Ryoji Hirabayashi , Shugo Honda , Hidetaka Kaku , Jun-ichi Shishikura , Hiroyuki Ito , Takeshi Kurama
IPC分类号： C07D213/46 , C07D211/70 , C07D401/00
CPC分类号： C04B35/632 , C07D205/04 , C07D207/14 , C07D211/58 , C07D401/12 , C07D403/12 , C07D405/12
摘要： The present invention relates a compound of formula 1, and pharmaceutically acceptable salt, hydrate, solvate, or isomer thereof effective as agonist of melanocortin receptor, and an agonistic composition of melanocortin receptor comprising the same as active ingredient.
摘要翻译：本发明涉及有效作为黑皮质素受体激动剂的式1化合物及其药学上可接受的盐，水合物，溶剂化物或异构体，以及包含与活性成分相同的黑皮质素受体激动剂组合物。

3. 发明授权

US6096743A 1,2,3,4-tetrahydroquinoxalinedione derivative 失效
标题翻译： 1,2,3,4-四氢喹喔啉二酮衍生物
公开(公告)号：US6096743A
公开(公告)日：2000-08-01
申请号：US809087
申请日：1997-03-05
申请人： Jun-ichi Shishikura , Hiroshi Inami , Shuichi Sakamoto , Shin-ichi Tsukamoto , Masao Sasamata , Masamichi Okada , Mitsuo Fujii
发明人： Jun-ichi Shishikura , Hiroshi Inami , Shuichi Sakamoto , Shin-ichi Tsukamoto , Masao Sasamata , Masamichi Okada , Mitsuo Fujii
IPC分类号： C07D403/04 , A61K31/498 , A61K31/4985 , A61P25/14 , A61P25/28 , C07D241/44 , C07D471/04 , C07D521/00 , C07D403/10
CPC分类号： C07D231/12 , C07D233/56 , C07D241/44 , C07D249/08
摘要： A 1,2,3,4-tetrahydroquinoxalinedione derivative represented by the following formula (I) or salt thereof, an NMDA-glycine receptor and/or AMPA receptor antagonist or kainic acid neurotoxicity inhibitor containing the derivative or salt. In addition, a pharmaceutical composition comprising said compound and a pharmaceutically acceptable carrier: ##STR1## wherein the substituents are as described in the specification.
摘要翻译： PCT No.PCT / JP95 / 01922 Sec。 371日期1997年3月5日 102（e）1997年3月5日PCT PCT 1995年9月25日PCT公布。公开号WO96 / 10023 日本1996年4月4日由下式（I）表示的1,2,3,4-四氢喹喔啉二酮衍生物或其盐，含有该衍生物或盐的NMDA-甘氨酸受体和/或AMPA受体拮抗剂或红藻氨酸神经毒性抑制剂。此外，包含所述化合物和药学上可接受的载体的药物组合物：其中取代基如说明书中所述。

4. 发明授权

US6121264A Imidazole-substituted quinoxalinedione derivatives 失效
标题翻译：咪唑取代的喹喔啉二酮衍生物
公开(公告)号：US6121264A
公开(公告)日：2000-09-19
申请号：US194750
申请日：1998-12-02
申请人： Shuichi Sakamoto , Junya Ohmori , Jun-ichi Shishikura , Masamichi Okada , Masao Sasamata
发明人： Shuichi Sakamoto , Junya Ohmori , Jun-ichi Shishikura , Masamichi Okada , Masao Sasamata
IPC分类号： C07D403/04 , A61K31/495 , C07D521/00 , A61K31/498 , C07D403/10 , C07D403/14
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08
摘要： Imidazole-substituted quinoxalinedione derivatives represented by the following general formula (I) or pharmaceutically acceptable salts thereof and pharmaceutical compositions useful as glutamate receptor antagonists and the like, which comprise said compounds or salts thereof and pharmaceutically acceptable carriers. ##STR1## (Each symbol in the formula has the following meaning: A: a group represented by a formula (CH.sub.2).sub.m or a group represented by a formula Ph--(CH.sub.2).sub.p (Ph: a phenyl group),X: an oxygen atom or a group represented by a formula NR.sup.4,R.sup.1 : a hydrogen atom, a hydroxyl group or a triazolyl group, with the proviso that X may be a bond when R.sup.1 is a triazolyl group,R.sup.2 : a hydrogen atom, a nitro group, a halogeno-lower alkyl group, a cyano group, an amino group, a mono- or di-lower alkylamino group or a halogen atom,R.sup.3 and R.sup.4 : may be the same or different from each other and each represents a hydrogen atom or a lower alkyl group,n: 0, 1 or 2,m: an integer of 2 to 6, andp: an integer of 1 to 6.
摘要翻译： PCT No.PCT / JP97 / 01905 Sec。 371日期1998年12月2日第 102（e）日期1998年12月2日PCT提交1997年6月5日PCT公布。公开号WO97 / 46555 日期：1997年12月11日由以下通式（I）表示的咪唑取代的喹喔啉二酮衍生物或其药学上可接受的盐以及用作谷氨酸受体拮抗剂等的药物组合物，其包含所述化合物或其盐和药学上可接受的载体。（式中的每个符号具有以下含义：A：由式（CH 2）m表示的基团或由式Ph-（CH 2）p（Ph：苯基）表示的基团，X：氧原子或由式NR4表示的基团，R1：氢原子，羟基或三唑基，条件是当R 1为三唑基时，X可以为键，R 2为氢原子，硝基，卤代低级烷基，氰基，氨基，一或二低级烷基氨基或卤素原子，R 3和R 4可以相同或不同，表示氢原子或低级烷基基团，n：0,1或2，m为2〜6的整数，p为1〜6的整数。

5. 发明申请

US20100168154A1 1-SUBSTITUTED TETRAHYDROISOQUINOLINE COMPOUND 有权
标题翻译： 1-取代的四氢喹啉化合物
公开(公告)号：US20100168154A1
公开(公告)日：2010-07-01
申请号：US12600503
申请日：2008-05-20
申请人： Jun-Ichi Shishikura , Makoto Inoue , Takashi Ogiyama , Koichi Yonezawa , Susumu Yamaki , Kazuhiro Yokoyama , Shuichirou Kakimoto , Hidetsugu Okada
发明人： Jun-Ichi Shishikura , Makoto Inoue , Takashi Ogiyama , Koichi Yonezawa , Susumu Yamaki , Kazuhiro Yokoyama , Shuichirou Kakimoto , Hidetsugu Okada
IPC分类号： A61K31/437 , C07D217/04 , C07D491/04 , A61K31/4725 , A61K31/472 , A61P25/00
CPC分类号： C07D217/04 , C07D217/14 , C07D217/16 , C07D221/20 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/06 , C07D491/06
摘要： Provided is a compound useful as an N-type Ca2+ channel blocker. As a result of intensive studies of compounds having an action of blocking N-type Ca2+ channels, the present inventors found that a tetrahydroisoquinoline compound of the present invention having a substituent at the 1-position has an action of blocking the N-type Ca2+ channels, an antinociceptive pain action, an antineuropathic pain action, an abdominal pain-inhibitory action and an opioid-induced constipation-improving action, and the present invention has been completed based on these findings. The compound of the present invention can be used as a pharmaceutical composition for preventing and/or treating various pains such as neuropathic pain and nociceptive pain, headaches such as migraine and cluster headache, central nervous system diseases such as anxiety, depression, epilepsy, cerebral stroke and restless legs syndrome, abdominal symptoms such as abdominal pain and abdominal distension, stool abnormalities such as diarrhea and constipation, digestive system diseases such as irritable bowel syndrome, urinary system diseases such as overactive bladder and interstitial cystitis, etc.
摘要翻译：提供可用作N型Ca2 +通道阻断剂的化合物。通过对具有阻塞N型Ca 2+通道作用的化合物的深入研究，本发明人发现在1位具有取代基的本发明的四氢异喹啉化合物具有阻断N型Ca 2+通道的作用抗痛知性疼痛作用，抗神经病性疼痛作用，腹痛抑制作用和阿片样物质诱导的便秘改善作用，并且基于这些发现完成了本发明。本发明的化合物可以用作预防和/或治疗诸如神经性疼痛和伤害性疼痛，头痛如偏头痛和丛集性头痛，中枢神经系统疾病如焦虑，抑郁，癫痫，脑的各种疼痛的药物组合物中风和不宁腿综合症，腹痛，腹胀等腹部症状，腹泻便秘等粪便异常，肠易激综合征等消化系统疾病，膀胱过多膀胱炎，间质性膀胱炎等泌尿系统疾病等。

6. 发明申请

US20070129346A1 Melanocortin receptor agonists 失效
标题翻译：黑皮质素受体激动剂
公开(公告)号：US20070129346A1
公开(公告)日：2007-06-07
申请号：US10579042
申请日：2004-11-12
申请人： Koo Lee , Heui-Sul Park , In-Ae Ahn , Hyun-Ju Yoo , Jong-Yup Kim , Deog-Young Choi , Hyeon-Joo Yim , Kyung-Ha Chung , Dong-Sup Shim , Sang-Kyun Lee , Yutaka Kondoh , Ryoji Hirabayashi , Shugo Honda , Hidetaka Kaku , Jun-ichi Shishikura , Hiroyuki Ito , Takeshi Kurama
发明人： Koo Lee , Heui-Sul Park , In-Ae Ahn , Hyun-Ju Yoo , Jong-Yup Kim , Deog-Young Choi , Hyeon-Joo Yim , Kyung-Ha Chung , Dong-Sup Shim , Sang-Kyun Lee , Yutaka Kondoh , Ryoji Hirabayashi , Shugo Honda , Hidetaka Kaku , Jun-ichi Shishikura , Hiroyuki Ito , Takeshi Kurama
IPC分类号： A61K31/397 , A61K31/401 , A61K31/445 , C07D211/06
CPC分类号： C04B35/632 , C07D205/04 , C07D207/14 , C07D211/58 , C07D401/12 , C07D403/12 , C07D405/12
摘要： The present invention relates a compound of formula 1, and pharmaceutically acceptable salt, hydrate, solvate, or isomer thereof effective as agonist of melanocortin receptor, and an agonistic composition of melanocortin receptor comprising the same as active ingredient.
摘要翻译：本发明涉及有效作为黑皮质素受体激动剂的式1化合物及其药学上可接受的盐，水合物，溶剂化物或异构体，以及包含与活性成分相同的黑皮质素受体激动剂组合物。

7. 发明授权

US6133258A Inhibitor of kainic acid neurotoxicity and pyridothiazine derivative 失效
标题翻译：红藻氨酸神经毒性抑制剂和吡啶并噻嗪衍生物
公开(公告)号：US6133258A
公开(公告)日：2000-10-17
申请号：US68534
申请日：1998-05-13
申请人： Jun-ichi Shishikura , Hiroshi Inami , Tomoyuki Yasunaga , Masaaki Hirano , Shuichi Sakamoto , Kazushige Ohno , Masamichi Okada , Shin-ichi Tsukamoto
发明人： Jun-ichi Shishikura , Hiroshi Inami , Tomoyuki Yasunaga , Masaaki Hirano , Shuichi Sakamoto , Kazushige Ohno , Masamichi Okada , Shin-ichi Tsukamoto
IPC分类号： A61K31/5415 , A61K31/542 , C07D513/04
CPC分类号： A61K31/5415
摘要： Neuroprotective agents based on inhibition of kainic acid neurotoxicity and compounds useful as neuroprotective agents based on inhibition of kainic acid neurotoxicity. An inhibitors of kainic acid neurotoxicity, comprising as an active ingredient a pyridothiazine derivative represented by the following general formula (I) or a pharmaceutically acceptable salt thereof, and a pyridothiazine derivative represented by the following general formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein symbols in the formula have the following respective meanings: the ring A: a pyridine ring; ##STR2## R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 may be the same or different and each represent a hydrogen atom or a lower alkyl, cycloalkyl, alkenyl, aryl, carboxyl or lower alkoxycarbonyl group which may have substituent(s), or are not present, with the proviso that R.sup.2 and R.sup.3 may together form a nitrogen-containing heterocyclic group which may have nitrogen atoms as another hetero atom, may be fused with a benzene ring and may have a lower alkyl group as a substituent.
摘要翻译： PCT No.PCT / JP96 / 03339 Sec。 371日期1998年5月13日 102（e）日期1998年5月13日PCT 1996年11月14日PCT PCT。出版物WO97 / 17970 日期1997年5月22日基于抑制红藻氨酸神经毒性的神经保护剂和基于抑制红藻氨酸神经毒性作用的神经保护剂的化合物。作为活性成分的红藻氨酸神经毒性抑制剂，含有下述通式（I）所示的吡哆噻嗪衍生物或其药学上可接受的盐，以及下述通式（I）表示的吡哒嗪衍生物或其药学上可接受的盐其中式中的符号具有以下各自的含义：环A：吡啶环; R 1，R 2，R 3，R 4和R 5可以相同或不同，各自表示氢原子或可以具有取代基或不存在的低级烷基，环烷基，烯基，芳基，羧基或低级烷氧基羰基，条件是R2和R3可以一起形成可以具有氮原子作为另一个杂原子的含氮杂环基，可以与苯环稠合并且可以具有低级烷基作为取代基。

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