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1. 发明授权

US08034801B2 Analgesic agent 失效
标题翻译：止痛药
公开(公告)号：US08034801B2
公开(公告)日：2011-10-11
申请号：US12309180
申请日：2006-07-12
申请人： Hiroki Hamura , Kenji Shimizu , Hashime Kanazawa
发明人： Hiroki Hamura , Kenji Shimizu , Hashime Kanazawa
IPC分类号： A01N37/18 , A01N57/00
CPC分类号： A61K31/167 , A61K31/192 , A61K31/485 , A61K45/06
摘要： A pharmaceutical preparation useful for alleviating or treating a pain, e.g., a chronic pain (particularly, a neuropathic pain) is provided. The pharmaceutical preparation contains (a) a propionic acid-derived nonsteroidal anti-inflammatory agent (e.g., ibuprofen), (b) a non-pyrazolone antipyretic analgesic agent (e.g., acetaminophen), and (c) an opioid analgesic agent (e.g., codeine phosphate, dihydrocodeine phosphate). The pharmaceutical preparation may contain 5 to 100 parts by weight of the antipyretic analgesic agent (b) or 0.5 to 500 parts by weight of the analgesic agent (c) relative to 100 parts by weight of the anti-inflammatory agent (a). The pharmaceutical preparation may be substantially free from a nontoxic N-methyl-D-aspartate receptor antagonist and may contain 20 to 80 parts by weight of the antipyretic analgesic agent (b) and 1 to 100 parts by weight of the analgesic agent (c) relative to 100 parts by weight of the anti-inflammatory agent (a).
摘要翻译：提供了用于减轻或治疗疼痛的药物制剂，例如慢性疼痛（特别是神经性疼痛）。药物制剂包含（a）丙酸衍生的非甾体抗炎药（例如布洛芬），（b）非吡唑啉酮解热止痛剂（例如对乙酰氨基酚）和（c）阿片样镇痛药（例如，磷酸可待因，磷酸二氢可待因）。相对于100重量份抗炎剂（a），药物制剂可以含有5-100重量份的解热止痛剂（b）或0.5-500重量份的止痛剂（c）。药物制剂可以基本上不含无毒的N-甲基-D-天冬氨酸受体拮抗剂，并且可以包含20至80重量份的解热止痛剂（b）和1至100重量份的止痛剂（c）相对于100重量份的抗炎剂（a）。

2. 发明申请

US20090253729A1 Analgesic Agent 失效
标题翻译：止痛剂
公开(公告)号：US20090253729A1
公开(公告)日：2009-10-08
申请号：US12309180
申请日：2006-07-12
申请人： Hiroki Hamura , Kenji Shimizu , Hashime Kanazawa
发明人： Hiroki Hamura , Kenji Shimizu , Hashime Kanazawa
IPC分类号： A61K31/485 , A61P25/04
CPC分类号： A61K31/167 , A61K31/192 , A61K31/485 , A61K45/06
摘要： A pharmaceutical preparation useful for alleviating or treating a pain, e.g., a chronic pain (particularly, a neuropathic pain) is provided. The pharmaceutical preparation contains (a) a propionic acid-derived nonsteroidal anti-inflammatory agent (e.g., ibuprofen), (b) a non-pyrazolone antipyretic analgesic agent (e.g., acetaminophen), and (c) an opioid analgesic agent (e.g., codeine phosphate, dihydrocodeine phosphate). The pharmaceutical preparation may contain 5 to 100 parts by weight of the antipyretic analgesic agent (b) or 0.5 to 500 parts by weight of the analgesic agent (c) relative to 100 parts by weight of the anti-inflammatory agent (a). The pharmaceutical preparation may be substantially free from a nontoxic N-methyl-D-aspartate receptor antagonist and may contain 20 to 80 parts by weight of the antipyretic analgesic agent (b) and 1 to 100 parts by weight of the analgesic agent (c) relative to 100 parts by weight of the anti-inflammatory agent (a).
摘要翻译：提供了用于减轻或治疗疼痛的药物制剂，例如慢性疼痛（特别是神经性疼痛）。药物制剂包含（a）丙酸衍生的非甾体抗炎药（例如布洛芬），（b）非吡唑啉酮解热止痛剂（例如对乙酰氨基酚）和（c）阿片样镇痛药（例如，磷酸可待因，磷酸二氢可待因）。相对于100重量份抗炎剂（a），药物制剂可以含有5-100重量份的解热止痛剂（b）或0.5-500重量份的止痛剂（c）。药物制剂可以基本上不含无毒的N-甲基-D-天冬氨酸受体拮抗剂，并且可以包含20至80重量份的解热止痛剂（b）和1至100重量份的止痛剂（c）相对于100重量份的抗炎剂（a）。

3. 发明授权

US06326360B1 Bubbling enteric coated preparations 失效
标题翻译：冒泡肠溶包衣制剂
公开(公告)号：US06326360B1
公开(公告)日：2001-12-04
申请号：US09623706
申请日：2000-09-25
申请人： Hashime Kanazawa , Kenji Shimizu , Kazuhiro Sasaki , Tetsuya Sugimoto
发明人： Hashime Kanazawa , Kenji Shimizu , Kazuhiro Sasaki , Tetsuya Sugimoto
IPC分类号： A61K31715
CPC分类号： A61K31/704 , A61K9/0007 , A61K9/2866 , A61K9/4891 , A61K9/5042 , A61K47/12 , A61K47/14
摘要： An object of the present invention is to obtain an oral glycyrrhizin preparation not only manufacturable by a simple method but also having an excellent property of being absorbed from the digestive tract. In the present invention, such oral preparations are made into enteric forms wherein glycyrrhizin is admixed with an effervescent agent in combination with an absorption enhancer such as a medium-chain fatty acid or a salt thereof. In the preparation of the present invention, it is now possible to achieve an excellent absorption of glycyrrhizin from the digestive tract by addition of an effervescent agent and, moreover, the preparation can be manufactured by a simple, convenient method without special steps.
摘要翻译：本发明的目的是获得口服甘草甜素制剂，其不仅可以通过简单的方法制造，而且具有从消化道吸收的优异性能。在本发明中，将这种口服制剂制成肠溶形式，其中甘草甜素与泡腾剂与吸收促进剂如中链脂肪酸或其盐的组合。在本发明的制备中，现在可以通过加入泡腾剂从消化道获得优异的甘草甜素吸收，此外，可以通过简单且方便的方法制造没有特殊步骤的制剂。

4. 发明授权

US08722094B2 Solid dispersion and pharmaceutical composition of the same, and production processes thereof 有权
标题翻译：固体分散体及其药物组合物及其制备方法
公开(公告)号：US08722094B2
公开(公告)日：2014-05-13
申请号：US12922029
申请日：2009-03-10
申请人： Kazushi Yoshida , Norimichi Okubo , Junichi Sakata , Hashime Kanazawa
发明人： Kazushi Yoshida , Norimichi Okubo , Junichi Sakata , Hashime Kanazawa
IPC分类号： A61K9/14
CPC分类号： A61K9/2009 , A61K9/1611 , A61K9/1652 , A61K9/2054 , A61K9/2077
摘要： A powdery porous carrier comprising a porous silicon-containing carrier is impregnated with a solution containing an organic solvent and an active ingredient hardly soluble in water, and the organic solvent is removed to give a solid dispersion having the active ingredient supported to the porous carrier without a treatment with a supercritical fluid. The porous silicon-containing carrier has a heating loss of not more than 4% by weight at a temperature of 950° C. for 2 hours (e.g., a spherical silicon-containing carrier such as a spherical porous silica). The porous silicon-containing carrier may be a spherical silica having a mean pore size of 10 to 40 nm and an oil absorption of 175 to 500 ml/100 g. A pharmaceutical composition (e.g., tablets, granules, or capsules) may be prepared from the solid dispersion and a pharmaceutically acceptable carrier. This invention provides a solid dispersion and a pharmaceutical composition (or a pharmaceutical preparation) which allows improvement in a solubility and a bioavailability of an active ingredient hardly soluble in water (e.g., a fibrate compound).
摘要翻译：包含多孔含硅载体的粉状多孔载体用含有有机溶剂和难溶于水的活性成分的溶液浸渍，除去有机溶剂，得到固体分散体，其中活性成分负载在多孔载体上，没有用超临界流体处理。多孔含硅载体在950℃的温度下具有不超过4重量％的加热损失2小时（例如球形含硅载体，例如球形多孔二氧化硅）。多孔含硅载体可以是平均孔径为10〜40nm，吸油量为175〜500ml / 100g的球状二氧化硅。可以从固体分散体和药学上可接受的载体制备药物组合物（例如片剂，颗粒剂或胶囊剂）。本发明提供一种固体分散体和药物组合物（或药物制剂），其允许改善难溶于水的活性成分（例如贝特类化合物）的溶解度和生物利用度。

5. 发明授权

US08193356B2 Heterocycle compound, and production process and application thereof 失效
标题翻译：杂环化合物及其制备方法和应用
公开(公告)号：US08193356B2
公开(公告)日：2012-06-05
申请号：US11991858
申请日：2006-09-15
申请人： Hashime Kanazawa , Tomoji Aotsuka , Kentarou Kumazawa , Kouki Ishitani , Takashi Nose
发明人： Hashime Kanazawa , Tomoji Aotsuka , Kentarou Kumazawa , Kouki Ishitani , Takashi Nose
IPC分类号： C07D471/04 , A61K31/437 , A61P11/00 , A61P11/06
CPC分类号： C07D471/14 , C07D471/04
摘要： The compound of the present invention is a novel compound which has a specific heterocycle skeleton, particularly a pyrazolonaphthyridine or pyrazoloquinoline skeleton having an organic group (e.g., a carbocycle and a heterocycle) bonding through an alkylene group at 3-position and a carbocycle bonding at 5-position and has a phosphodiesterase IV inhibitory activity. At least one of the ring (the carbocycle or the heterocycle) bonding at 3-position of the pyrazolonaphthyridine skeleton and the carbocycle bonding at 5-position may have a halogenated alkyl group and/or a halogenated alkoxy group as a substituent. Such a compound or a salt thereof is useful as a phosphodiesterase IV inhibitor and the like. According to the present invention, a novel compound having a high phosphodiesterase IV inhibitory effect can be provided.
摘要翻译：本发明的化合物是具有特定杂环骨架的新型化合物，特别是具有通过3-位亚烷基键合的有机基团（例如，碳环和杂环）的吡唑并萘并吡啶骨架，具有磷酸二酯酶IV抑制活性。在吡唑并萘啶骨架的3位键合的环（碳环或杂环）中的至少一个和在5位键合的碳环可以具有卤代烷基和/或卤代烷氧基作为取代基。这种化合物或其盐可用作磷酸二酯酶IV抑制剂等。根据本发明，可以提供具有高磷酸二酯酶IV抑制作用的新型化合物。

6. 发明申请

US20100056613A1 SPIROQUINONE COMPOUND AND PHARMACEUTICAL COMPOSITION 失效
标题翻译：螺旋体化合物和药物组合物
公开(公告)号：US20100056613A1
公开(公告)日：2010-03-04
申请号：US12312640
申请日：2007-11-21
申请人： Shinji Yokoyama , Hashime Kanazawa , Tomoji Aotsuka
发明人： Shinji Yokoyama , Hashime Kanazawa , Tomoji Aotsuka
IPC分类号： A61K31/385 , C07D339/06 , A61P9/12 , A61P25/00 , A61P3/10 , A61P3/04 , A61P13/12 , A61P29/00
CPC分类号： C07D339/06
摘要： A novel spiroquinone derivative having a high ABCA1 stabilization effect and being useful for prophylactic and/or therapeutic agents for various diseases developing hypo-high density lipoproteinemia is obtained. The novel spiroquinone derivative is a compound represented by the following formula: wherein R1a, R1b, R1c and R1d each represents a hydrogen atom, a halogen atom, an alkyl group which may have a substituent, or an alkoxy group which may have a substituent, and R2a and R2b each represents a hydrogen atom, or an alkyl group which may have a substituent (e.g., a carboxyl group, an alkoxycarbonyl group, a carbamoyl group, and an N-substituted carbamoyl group), the groups R2a and R2b may bond together to form a hydrocarbon ring with an adjacent carbon atom, provided that compounds in which all of the groups R1a, R1b, R1c and R1d are t-butyl groups, and both of the groups R2a and R2b are hydrogen atoms or both of the groups R2a and R2b are methyl groups are excluded; or a pharmacologically acceptable salt thereof.
摘要翻译：获得具有高ABCA1稳定作用并可用于发生低密度脂蛋白血症的各种疾病的预防和/或治疗剂的新型螺醌衍生物。新型螺醌衍生物为下式表示的化合物：其中R1a，R1b，R1c和R1d各自表示氢原子，卤素原子，可具有取代基的烷基或可具有取代基的烷氧基， R2a和R2b各自表示氢原子或可具有取代基的烷基（例如羧基，烷氧基羰基，氨基甲酰基和N-取代氨基甲酰基），基团R 2a和R 2b可以键合一起形成具有相邻碳原子的烃环，条件是其中所有基团R 1a，R 1b，R 1c和R 1d都是叔丁基，并且基团R 2a和R 2b各自为氢原子或两个基团 R2a和R2b是甲基; 或其药理学上可接受的盐。

7. 发明申请

US20110020455A1 SOLID DISPERSION AND PHARMACEUTICAL COMPOSITION OF THE SAME, AND PRODUCTION PROCESSES THEREOF 有权
标题翻译：其固体分散体及其药物组合物及其生产工艺
公开(公告)号：US20110020455A1
公开(公告)日：2011-01-27
申请号：US12922029
申请日：2009-03-10
申请人： Kazushi Yoshida , Norimichi Okubo , Junichi Sakata , Hashime Kanazawa
发明人： Kazushi Yoshida , Norimichi Okubo , Junichi Sakata , Hashime Kanazawa
IPC分类号： A61K9/14 , A61K31/216 , A61K31/47 , A61K31/505 , A61K31/40 , A61K31/351 , A61P9/12 , A61P3/04 , A61P3/00 , A61P7/10 , A61P7/02 , A61P3/10
CPC分类号： A61K9/2009 , A61K9/1611 , A61K9/1652 , A61K9/2054 , A61K9/2077
摘要： A powdery porous carrier comprising a porous silicon-containing carrier is impregnated with a solution containing an organic solvent and an active ingredient hardly soluble in water, and the organic solvent is removed to give a solid dispersion having the active ingredient supported to the porous carrier without a treatment with a supercritical fluid. The porous silicon-containing carrier has a heating loss of not more than 4% by weight at a temperature of 950° C. for 2 hours (e.g., a spherical silicon-containing carrier such as a spherical porous silica). The porous silicon-containing carrier may be a spherical silica having a mean pore size of 10 to 40 nm and an oil absorption of 175 to 500 ml/100 g. A pharmaceutical composition (e.g., tablets, granules, or capsules) may be prepared from the solid dispersion and a pharmaceutically acceptable carrier. This invention provides a solid dispersion and a pharmaceutical composition (or a pharmaceutical preparation) which allows improvement in a solubility and a bioavailability of an active ingredient hardly soluble in water (e.g., a fibrate compound).
摘要翻译：包含多孔含硅载体的粉状多孔载体用含有有机溶剂和难溶于水的活性成分的溶液浸渍，除去有机溶剂，得到固体分散体，其中活性成分负载在多孔载体上，没有用超临界流体处理。多孔含硅载体在950℃的温度下具有不超过4重量％的加热损失2小时（例如球形含硅载体，例如球形多孔二氧化硅）。多孔含硅载体可以是平均孔径为10〜40nm，吸油量为175〜500ml / 100g的球状二氧化硅。可以从固体分散体和药学上可接受的载体制备药物组合物（例如片剂，颗粒剂或胶囊剂）。本发明提供一种固体分散体和药物组合物（或药物制剂），其允许改善难溶于水的活性成分（例如贝特类化合物）的溶解度和生物利用度。

8. 发明申请

US20100093782A1 Pyrazolonaphthyridine derivatives 审中-公开
标题翻译：吡唑并萘啶衍生物
公开(公告)号：US20100093782A1
公开(公告)日：2010-04-15
申请号：US12585430
申请日：2009-09-15
申请人： Hashime Kanazawa , Tomoji Aotsuka , Kentarou Kumazawa , Kouki Ishitani , Takashi Nose
发明人： Hashime Kanazawa , Tomoji Aotsuka , Kentarou Kumazawa , Kouki Ishitani , Takashi Nose
IPC分类号： A61K31/4375 , C07D471/14 , A61P11/06
CPC分类号： A61K31/4375 , A61K31/444 , C07D471/14
摘要： The target is to provide PDE IV inhibitors which have a highly potent anti-asthmatic and/or COPD-prophylactic/therapeutic profile with unexpectedly excellent safety. A compound of the formula (1): wherein A is phenyl, pyridyl, 1-oxypyridyl, or thienyl, which may be unsubstituted or optionally substituted with one or more members selected from the group consisting of hydroxyl, halogen, cyano, nitro, lower alkyl, lower alkoxy, lower alkylcarbonyloxy, amino, carboxyl, lower alkoxy-carbonyl, carboxy-lower alkylene, lower alkoxycarbonyl-lower alkylene, lower alkylsulfonyl, lower alkylsulfonyl-amino, and ureido; R1 is a group selected from the group consisting of hydrogen, hydroxyl, halogen, cyano, nitro, lower alkoxy, amino, carboxyl, and lower alkoxycarbonyl; R2 is hydrogen or lower alkyl; and m is an integer of 1 to 3; or a pharmaceutically acceptable salt thereof, possesses highly excellent PDE IV-specific inhibitory actions and is useful as an anti-asthmatic drug and/or a prophylactic/therapeutic drug for COPD with high safety.
摘要翻译：目标是提供具有非常有效的抗哮喘和/或COPD预防/治疗特征的PDE IV抑制剂，具有出人意料的极好的安全性。式（1）的化合物：其中A是苯基，吡啶基，1-氧代吡啶基或噻吩基，其可以是未取代的或任选地被一个或多个选自羟基，卤素，氰基，硝基，低级烷基，低级烷氧基，低级烷基羰基氧基，氨基，羧基，低级烷氧基 - 羰基，羧基 - 低级亚烷基，低级烷氧基羰基 - 低级亚烷基，低级烷基磺酰基，低级烷基磺酰基 - 氨基和脲基。 R 1是选自氢，羟基，卤素，氰基，硝基，低级烷氧基，氨基，羧基和低级烷氧基羰基的基团。 R2是氢或低级烷基; m为1〜3的整数。或其药学上可接受的盐具有非常优异的PDE IV特异性抑制作用，并且可用作具有高度安全性的抗哮喘药和/或用于COPD的预防/治疗药物。

9. 发明授权

US07608716B2 Pyrazolonaphthyridine derivative 有权
标题翻译：吡唑并萘啶衍生物
公开(公告)号：US07608716B2
公开(公告)日：2009-10-27
申请号：US10533806
申请日：2003-11-05
申请人： Hashime Kanazawa , Tomoji Aotsuka , Kentarou Kumazawa , Kouki Ishitani , Takashi Nose
发明人： Hashime Kanazawa , Tomoji Aotsuka , Kentarou Kumazawa , Kouki Ishitani , Takashi Nose
IPC分类号： A61K31/4375 , C07D471/14 , C07D471/16
CPC分类号： A61K31/4375 , A61K31/444 , C07D471/14
摘要： The target is to provide PDE IV inhibitors which have a highly potent anti-asthmatic and/or COPD-prophylactic/therapeutic profile with unexpectedly excellent safety. A compound of the formula (1): wherein A is phenyl, pyridyl, 1-oxypyridyl, or thienyl, which may be unsubstituted or optionally substituted with one or more members selected from the group consisting of hydroxyl, halogen, cyano, nitro, lower alkyl, lower alkoxy, lower alkylcarbonyloxy, amino, carboxyl, lower alkoxycarbonyl, carboxy-lower alkylene, lower alkoxycarbonyl-lower alkylene, lower alkylsulfonyl, lower alkylsulfonylamino, and ureido; R1 is a group selected from the group consisting of hydrogen, hydroxyl, halogen, cyano, nitro, lower alkoxy, amino, carboxyl, and lower alkoxycarbonyl; R2 is hydrogen or lower alkyl; and m is an integer of 1 to 3; or a pharmaceutically acceptable salt thereof, possesses highly excellent PDE IV-specific inhibitory actions and is useful as an anti-asthmatic drug and/or a prophylactic/therapeutic drug for COPD with high safety.
摘要翻译：目标是提供具有非常有效的抗哮喘和/或COPD预防/治疗特征的PDE IV抑制剂，具有出人意料的极好的安全性。式（1）的化合物：其中A是苯基，吡啶基，1-氧代吡啶基或噻吩基，其可以是未取代的或任选地被一个或多个选自羟基，卤素，氰基，硝基，低级烷基，低级烷氧基，低级烷基羰基氧基，氨基，羧基，低级烷氧基羰基，羧基 - 低级亚烷基，低级烷氧基羰基 - 低级亚烷基，低级烷基磺酰基，低级烷基磺酰基氨基和脲基。 R 1是选自氢，羟基，卤素，氰基，硝基，低级烷氧基，氨基，羧基和低级烷氧基羰基的基团。 R2是氢或低级烷基; m为1〜3的整数。或其药学上可接受的盐具有非常优异的PDE IV特异性抑制作用，并且可用作具有高度安全性的抗哮喘药和/或用于COPD的预防/治疗药物。

10. 发明申请

US20090131467A1 Heterocycle Compound, and Production Process and Application Thereof 失效
标题翻译：杂环化合物及其制备方法及应用
公开(公告)号：US20090131467A1
公开(公告)日：2009-05-21
申请号：US11991858
申请日：2006-09-15
申请人： Hashime Kanazawa , Tomoji Aotsuka , Kentarou Kumazawa , Kouki Ishitani , Takashi Nose
发明人： Hashime Kanazawa , Tomoji Aotsuka , Kentarou Kumazawa , Kouki Ishitani , Takashi Nose
IPC分类号： A61K31/437 , C07D471/04 , A61P11/06 , A61P11/00
CPC分类号： C07D471/14 , C07D471/04
摘要： The compound of the present invention is a novel compound which has a specific heterocycle skeleton, particularly a pyrazolonaphthyridine or pyrazoloquinoline skeleton having an organic group (e.g., a carbocycle and a heterocycle) bonding through an alkylene group at 3-position and a carbocycle bonding at 5-position and has a phosphodiesterase IV inhibitory activity. At least one of the ring (the carbocycle or the heterocycle) bonding at 3-position of the pyrazolonaphthyridine skeleton and the carbocycle bonding at 5-position may have a halogenated alkyl group and/or a halogenated alkoxy group as a substituent. Such a compound or a salt thereof is useful as a phosphodiesterase IV inhibitor and the like. According to the present invention, a novel compound having a high phosphodiesterase IV inhibitory effect can be provided.
摘要翻译：本发明的化合物是具有特定杂环骨架的新型化合物，特别是具有通过3-位亚烷基键合的有机基团（例如，碳环和杂环）的吡唑并萘并吡啶骨架，具有磷酸二酯酶IV抑制活性。在吡唑并萘啶骨架的3位键合的环（碳环或杂环）中的至少一个和在5位键合的碳环可以具有卤代烷基和/或卤代烷氧基作为取代基。这种化合物或其盐可用作磷酸二酯酶IV抑制剂等。根据本发明，可以提供具有高磷酸二酯酶IV抑制作用的新型化合物。

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