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1. 发明公开

EP2039359A1 ANALGESIC AGENT 审中-公开
标题翻译： ANALGETISCHES MITTEL
公开(公告)号：EP2039359A1
公开(公告)日：2009-03-25
申请号：EP06768120.5
申请日：2006-07-12
申请人： ASKA Pharmaceutical Co., Ltd.
发明人： HAMURA, Hiroki , SHIMIZU, Kenji , KANAZAWA, Hashime
IPC分类号： A61K31/485 , A61K31/167 , A61K31/192 , A61K45/00 , A61P25/02 , 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：提供了用于缓解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）非吡唑啉酮解热镇痛药（例如对乙酰氨基酚）和（c）阿片类止痛剂（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重量份的镇痛剂（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. 发明授权

EP1559716B1 PYRAZOLONAPHTHYRIDINE DERIVATIVE 有权
标题翻译：吡唑并萘啶衍生物
公开(公告)号：EP1559716B1
公开(公告)日：2011-09-14
申请号：EP03810609.2
申请日：2003-11-05
申请人： ASKA Pharmaceutical Co., Ltd.
发明人： KANAZAWA, Hashime , AOTSUKA, Tomoji , KUMAZAWA, Kentarou , ISHITANI, Kouki , NOSE, Takashi
IPC分类号： C07D471/14 , A61K31/4375 , A61K31/444 , A61P11/00 , A61P29/00 , A61P43/00
CPC分类号： A61K31/4375 , A61K31/444 , C07D471/14
摘要： A PDE IV inhibitor which is excellent in antiasthatic effect and the effect of prevention of or treatments for COPD and is highly safe. A compound represented by the general formula (1): (1) (wherein A is a phenyl, pyridyl, 1-oxypyridyl, or thienyl group optionally substituted by one or more substituents selected from the group consisting of hydroxy, halogeno, cyano, nitro, lower alkyl, lower alkoxy, lower alkylcarbonyloxy, amino, carboxy, lower alkoxycarbonyl, carboxy(lower alkylene), (lower alkoxy)carbonyl(lower alkylene), lower alkylsulfonyl, lower alkylsulfonylamino, and ureido; R1 is hydrogen or a substituent selected from the group consisting of hydroxy, halogeno, cyano, nitro, lower alkoxy, amino, carboxy, and lower alkoxycarbonyl; R2 is hydrogen or lower alkyl; and m is an integer of 1 to 3) or a pharmaceutically acceptable salt of the compound has excellent PDE IV inhibitory activity and is highly safe. They are useful as an antasthmatic and preventive/therapeutic agent for COPD.
摘要翻译：一种PDE IV抑制剂，其具有优异的抗癌作用和预防或治疗COPD的效果，并且是高度安全的。由通式（1）表示的化合物：（1）（其中A是苯基，吡啶基，1-氧基吡啶基或噻吩基，其任选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; R1是氢或选自由羟基，卤代，氰基，硝基，低级烷氧基，氨基，羧基和低级烷氧基羰基组成的基团; R2是氢或低级烷基; m是1-3的整数）或该化合物的药学上可接受的盐具有优异的 PDE IV抑制活性并且非常安全。它们可用作COPD的平喘和预防/治疗剂。

3. 发明授权

EP1925617B1 HETEROCYCLIC COMPOUND, AND PRODUCTION PROCESS AND USE THEREOF 有权
标题翻译：杂环化合物，使用方法和用途
公开(公告)号：EP1925617B1
公开(公告)日：2012-11-14
申请号：EP06810190.6
申请日：2006-09-15
申请人： ASKA Pharmaceutical Co., Ltd.
发明人： KANAZAWA, Hashime , AOTSUKA, Tomoji , KUMAZAWA, Kentarou , ISHITANI, Kouki , NOSE, Takashi
IPC分类号： C07D471/04 , A61K31/4375 , A61K31/4745 , A61P1/02 , A61P1/04 , A61P1/16 , A61P1/18 , A61P3/04 , A61P3/10 , A61P5/00 , A61P5/14 , A61P5/38 , A61P7/00 , A61P7/02 , A61P7/04 , A61P7/06 , A61P9/00 , A61P9/04 , A61P9/06 , A61P9/10
CPC分类号： C07D471/14 , C07D471/04

4. 发明公开

EP2047851A1 DRUG FORMULATION CONTAINING FIBRATE MEDICAMENT AND PROCESS FOR PRODUCING THE SAME 审中-公开
标题翻译：维多利亚ZU IHRER HERSTELLUNG的ARZNEIFORMULIERUNG MIT EINEM FIBRAT-MEDIKAMENT
公开(公告)号：EP2047851A1
公开(公告)日：2009-04-15
申请号：EP06782392.2
申请日：2006-08-04
申请人： ASKA Pharmaceutical Co., Ltd.
发明人： KANAZAWA, Hashime , MORIMOTO, Masaya , TANIMORI, Naoto
IPC分类号： A61K31/47 , A61K31/216 , A61P1/16 , A61P1/18 , A61P3/00 , A61P3/06 , A61P3/08 , A61P3/10 , A61P7/02
CPC分类号： A61K31/216 , A61K31/47
摘要： A preparation (pharmaceutical composition) reducing a concentration of a free fatty acid and/or fibrinogen in the blood is prepared. The preparation contains a statin agent comprising at least a statin compound having a benzopyridine skeleton (e.g., pitavastatin) and a fibrate agent (e.g., fenofibrate). The preparation is useful as a preventive or treating agent for hyper-free fatty acidemia, metabolic syndrome, or type II diabetes.
摘要翻译：制备降低血液中游离脂肪酸和/或纤维蛋白原浓度的制剂（药物组合物）。该制剂含有至少包含具有苯并吡啶骨架的他汀类化合物（例如匹伐他汀）和贝特类药物（例如非诺贝特）的他汀类药物。该制剂可用作高游离脂肪酸血症，代谢综合征或II型糖尿病的预防或治疗剂。

5. 发明公开

EP1925617A1 HETEROCYCLIC COMPOUND, AND PRODUCTION PROCESS AND USE THEREOF 有权
标题翻译： HETEROZYKLISCHE VERBINDUNG，HERSTELLUNGSVERFAHREN SOWIE VERWENDUNG
公开(公告)号：EP1925617A1
公开(公告)日：2008-05-28
申请号：EP06810190.6
申请日：2006-09-15
申请人： ASKA Pharmaceutical Co., Ltd.
发明人： KANAZAWA, Hashime , AOTSUKA, Tomoji , KUMAZAWA, Kentarou , ISHITANI, Kouki , NOSE, Takashi
IPC分类号： C07D471/04 , A61K31/4375 , A61K31/4745 , A61P1/02 , A61P1/04 , A61P1/16 , A61P1/18 , A61P3/04 , A61P3/10 , A61P5/00 , A61P5/14 , A61P5/38 , A61P7/00 , A61P7/02 , A61P7/04 , A61P7/06 , A61P9/00 , A61P9/04 , A61P9/06 , A61P9/10
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）的吡唑并萘并喹啉骨架，具有磷酸二酯酶IV抑制活性。在吡唑啉基萘啶骨架的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. 发明授权

EP2251038B1 SOLID DISPERSION, PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME, AND PROCESSES FOR THE PRODUCTION OF BOTH 有权
标题翻译：固体分散体，含有其的药物组合物以及用于生产两者的方法
公开(公告)号：EP2251038B1
公开(公告)日：2017-05-10
申请号：EP09718988.0
申请日：2009-03-10
申请人： ASKA Pharmaceutical Co., Ltd.
发明人： YOSHIDA, Kazushi , OKUBO, Norimichi , SAKATA, Junichi , KANAZAWA, Hashime
IPC分类号： A61K9/16 , A61K9/20 , A61K47/30 , A61K47/36 , A61K47/02
CPC分类号： A61K9/2009 , A61K9/1611 , A61K9/1652 , A61K9/2054 , A61K9/2077

7. 发明公开

EP2251038A1 SOLID DISPERSION, PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME, AND PROCESSES FOR THE PRODUCTION OF BOTH 有权
标题翻译： FESTE DISPERSION，PHARMAZEUTISCHE ZUSAMMENSETZUNGEN DAMIT UND VERFAHREN ZU IHRER HERSTELLUNG
公开(公告)号：EP2251038A1
公开(公告)日：2010-11-17
申请号：EP09718988.0
申请日：2009-03-10
申请人： ASKA Pharmaceutical Co., Ltd.
发明人： YOSHIDA, Kazushi , OKUBO, Norimichi , SAKATA, Junichi , KANAZAWA, Hashime
IPC分类号： A61K47/04 , A61K9/20 , A61K47/30 , A61K47/36
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/100g. 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℃的温度下加热损失不超过4重量％2小时（例如球状含硅载体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。

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