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1. 发明授权

US09085523B2 Compound for treating cartilage disorders 有权
标题翻译：用于治疗软骨疾病的化合物
公开(公告)号：US09085523B2
公开(公告)日：2015-07-21
申请号：US14237037
申请日：2012-08-03
申请人： Tetsuo Obitsu , Kousuke Tani , Hikaru Sugihara , Akio Nishiura , Shinsei Fujimura
发明人： Tetsuo Obitsu , Kousuke Tani , Hikaru Sugihara , Akio Nishiura , Shinsei Fujimura
IPC分类号： A01N37/08 , A61K31/215 , C07C59/56 , C07C405/00 , C07C235/06 , C07C235/16 , C07C65/28 , A61K9/00 , A61K47/26 , A61K47/48
CPC分类号： C07C59/56 , A61K9/0019 , A61K47/26 , A61K47/6951 , C07C235/06 , C07C235/16 , C07C405/00 , C07C2601/04 , C07C2601/08 , Y10T428/2982
摘要： The present invention provides a compound of which active |form| is represented by a formula (A). and which can be injected into a joint cavity which is an affected part of disorders and can be accumulated in the joint cavity to exert the pharmacological effect thereof in a sustained manner, for the purpose of ameliorating cartilage disorders without developing any side effect. A compound according to the present invention, which is represented by a formula (I): (wherein all of symbols are as defined in the description), is a compound that can achieve the above-mentioned purpose. This compound does not exhibit any side effect on the cardiovascular system even when the compound is administered in an effective amount for exhibiting a cartilage regeneration activity, and is therefore extremely useful as a safe and effective preventive and/or therapeutic agent for cartilage disorders. Since a suspension produced using this compound can be injected without requiring the incision of the affected part, it can reduce the burden on patients, and is extremely useful as a medicinal agent.
摘要翻译：本发明提供了一种活性成分的化合物由式（A）表示。并且其可以注射到作为疾病的一部分的关节腔中，并且可以以持续的方式累积在关节腔中以发挥其药理作用，以改善软骨疾病而不产生副作用。由式（I）表示的本发明化合物（其中所有符号如说明书中所定义）是可以实现上述目的的化合物。即使当化合物以有效量施用以显示软骨再生活性时，该化合物也不会对心血管系统显示任何副作用，因此作为软骨疾病的安全有效的预防和/或治疗剂非常有用。由于使用该化合物制备的悬浮液可以不需要切开患者部位而被注射，所以能够减轻患者的负担，作为药剂非常有用。

2. 发明申请

US20140171388A1 COMPOUND FOR TREATING CARTILAGE DISORDERS 有权
标题翻译：化合物用于治疗消化系统疾病
公开(公告)号：US20140171388A1
公开(公告)日：2014-06-19
申请号：US14237037
申请日：2012-08-03
申请人： Tetsuo Obitsi , Kousuke Tani , Hikaru Sugihara , Akio Nishiura , Shinsei Fujimura
发明人： Tetsuo Obitsi , Kousuke Tani , Hikaru Sugihara , Akio Nishiura , Shinsei Fujimura
IPC分类号： C07C405/00 , C07C235/16 , C07C59/56 , C07C65/28
CPC分类号： C07C59/56 , A61K9/0019 , A61K47/26 , A61K47/6951 , C07C235/06 , C07C235/16 , C07C405/00 , C07C2601/04 , C07C2601/08 , Y10T428/2982
摘要： The present invention provides a compound of which active |form| is represented by a formula (A). and which can be injected into a joint cavity which is an affected part of disorders and can be accumulated in the joint cavity to exert the pharmacological effect thereof in a sustained manner, for the purpose of ameliorating cartilage disorders without developing any side effect. A compound according to the present invention, which is represented by a formula (I): (wherein all of symbols are as defined in the description), is a compound that can achieve the above-mentioned purpose. This compound does not exhibit any side effect on the cardiovascular system even when the compound is administered in an effective amount for exhibiting a cartilage regeneration activity, and is therefore extremely useful as a safe and effective preventive and/or therapeutic agent for cartilage disorders. Since a suspension produced using this compound can be injected without requiring the incision of the affected part, it can reduce the burden on patients, and is extremely useful as a medicinal agent.
摘要翻译：本发明提供了一种活性成分的化合物由式（A）表示。并且其可以注射到作为疾病的一部分的关节腔中，并且可以以持续的方式累积在关节腔中以发挥其药理作用，以改善软骨疾病而不产生副作用。由式（I）表示的本发明化合物（其中所有符号如说明书中所定义）是可以实现上述目的的化合物。即使当化合物以有效量施用以显示软骨再生活性时，该化合物也不会对心血管系统显示任何副作用，因此作为软骨疾病的安全有效的预防和/或治疗剂非常有用。由于使用该化合物制备的悬浮液可以不需要切开患者部位而被注射，所以能够减轻患者的负担，作为药剂非常有用。

3. 发明申请

US20090074844A1 TRENADERMAL ABSORPTION PREPARATION 审中-公开
标题翻译： TRENADERMAL吸收制剂
公开(公告)号：US20090074844A1
公开(公告)日：2009-03-19
申请号：US11912997
申请日：2006-04-27
申请人： Akio Nishiura , Hikaru Sugihara , Harumi Arai , Toshiya Kanaji
发明人： Akio Nishiura , Hikaru Sugihara , Harumi Arai , Toshiya Kanaji
IPC分类号： A61K31/216 , A61L15/44 , A61P7/00 , A61P19/00
CPC分类号： A61K9/0014 , A61K9/7053 , A61K31/5575
摘要： The present invention relates to a blood concentration regulation type percutaneous absorption preparation, which comprises an ester form of 4-{[2-((1R,2R,3R)-3-hydroxy-2-{(1E,3S)-3-hydroxy-4-[3-(methoxymethyl)phenyl]but-1-enyl}-5-oxocyclopentyl)ethyl]sulfanyl}butanoic acid and a base for external preparations. The blood concentration regulation type percutaneous absorption preparation of the present invention can stably maintain blood concentration of the active form of the present invention and is safe since there are no side effects. Therefore, it can be used as a percutaneous absorption preparation which can be persistently administered.
摘要翻译：本发明涉及血液浓度调节型经皮吸收制剂，其包含4 - {[2 - （（1R，2R，3R）-3-羟基-2 - {（1E，3S）-3- 羟基-4- [3-（甲氧基甲基）苯基]丁-1-烯基} -5-氧代环戊基）乙基]硫烷基}丁酸和外用制剂的碱。本发明的血液浓度调节型经皮吸收制剂能够稳定地维持本发明的活性形式的血药浓度，因为没有副作用，因此是安全的。因此，可以作为能够持续施用的经皮吸收制剂使用。

4. 发明申请

US20090022915A1 PARTICLE AND PREPARATION CONTAINING THE PARTICLE 审中-公开
标题翻译：颗粒和包含颗粒的制备
公开(公告)号：US20090022915A1
公开(公告)日：2009-01-22
申请号：US11908091
申请日：2006-03-08
申请人： Hideo Masuda , Hikaru Sugihara , Akio Nishiura , Kazuyuki Hayashi
发明人： Hideo Masuda , Hikaru Sugihara , Akio Nishiura , Kazuyuki Hayashi
IPC分类号： C07D417/02 , B32B1/02 , B32B5/16
CPC分类号： A61K9/0075 , A61K9/1623 , A61K9/1652 , Y10T428/13 , Y10T428/2982
摘要： The present invention relates to a particle having a mean particle size of 0.01 to 20 μm, containing tert-butyl (4R)-4-{[((1R)-2-[(1-benzylpiperidin-4-yl)amino]-1-{[(cyclohexylmethyl)thio]methyl}-2-oxoethyl)amino]carbonyl}-1,3-thiazolidine-3-carboxylate. A preparation containing the particle is excellent in pulmonary delivery through inhalation and is easy to handle because of excellent dispersibility of the particle, and thus the present compound can be used as a pulmonary preparation.
摘要翻译：本发明涉及平均粒度为0.01〜20μm的颗粒，其含有（4R）-4 - {[（1R）-2 - [（1-苄基哌啶-4-基）氨基] - 1 - {[（环己基甲基）硫基]甲基} -2-氧代乙基）氨基]羰基} -1,3-噻唑烷-3-羧酸乙酯。含有该颗粒的制剂在通过吸入的肺部输送中是优异的，并且由于颗粒的优异的分散性而易于处理，因此本发明化合物可用作肺制剂。

5. 发明申请

US20080096924A1 Amorphous Composition 审中-公开
标题翻译：无定形组成
公开(公告)号：US20080096924A1
公开(公告)日：2008-04-24
申请号：US11722008
申请日：2005-12-16
申请人： Hideo Masuda , Hikaru Sugihara , Akio Nishiura
发明人： Hideo Masuda , Hikaru Sugihara , Akio Nishiura
IPC分类号： A61K31/454 , A61P25/00 , C07D417/12
CPC分类号： A61K9/1652 , A61K9/0043 , A61K9/006 , A61K9/1635 , A61K9/2027 , A61K9/2054 , C07D417/12
摘要： To provide an amorphous composition for nasal administration or for administration by adhering to oral mucosa in which absorption property and chemical and physical stabilities of (2R)—N-(1-benzylpiperidin-4-yl)-3-cyclohexylmethylthio-2-[(4R)-3-tert-butoxycarbonylthiazolidin-4-ylcarbonylamino]propanamide which is useful as an N type calcium channel inhibitor are improved. A preparation comprising the amorphous composition of the present invention has been found to be excellent in physical stability and chemical stability and to be useful as a nasal preparation or a preparation for adhering to the oral mucosa. As a result, the resulting preparation has a high BA value and is useful for prevention and/or the treatment of a disease mediated by the N type calcium channel including pain (such as neuropathic pain, cancerous pain, intractable pain, postoperative pain, acute pain, chronic pain, neuralgia and infectious pain).
摘要翻译：为了提供用于鼻腔给药或通过粘附口服粘膜给药的无定形组合物，其中（2R）-N-（1-苄基哌啶-4-基）-3-环己基甲硫基-2 - [（ 4R）-3-叔丁氧基羰基噻唑烷-4-基羰基氨基]丙酰胺，其可用作N型钙通道抑制剂。已经发现包含本发明的无定形组合物的制剂具有优异的物理稳定性和化学稳定性，并且可用作鼻制剂或粘附于口腔粘膜的制剂。结果，所得制剂具有高BA值，可用于预防和/或治疗由N型钙通道介导的疾病，包括疼痛（例如神经性疼痛，癌性疼痛，顽固性疼痛，术后疼痛，急性疼痛，慢性疼痛，神经痛和感染性疼痛）。

6. 发明授权

US08410171B2 Adhesive preparation 失效
标题翻译：粘合剂制备
公开(公告)号：US08410171B2
公开(公告)日：2013-04-02
申请号：US12447215
申请日：2007-10-25
申请人： Akio Nishiura , Hikaru Sugihara , Kazuya Abe
发明人： Akio Nishiura , Hikaru Sugihara , Kazuya Abe
IPC分类号： A61K31/557
CPC分类号： A61K31/5575 , A61K9/7053 , A61K9/7069 , A61K9/7076
摘要： An adhesive preparation which has a pressure-sensitive adhesive layer comprising two components, i.e., a C1-4 alcohol ester of 4-{[2-((1R,2R,3R)-3-hydroxy-2-{(1E,3S)-3-hydroxy-4-[3-(methoxymethyl)phenyl]but-1-enyl}-5-osocyclopentyl)ethyl]sulfanyl}butanoic acid and a silicone-based pressure-sensitive adhesive. This is an effective and safe preparation which is stable, shows little change in skin permability and release a drug not rapidly but continuously.
摘要翻译：一种粘合剂制剂，其具有包含两种组分的压敏粘合剂层，即4 - {[2 - （（1R，2R，3R）-3-羟基-2 - {（1E，3S ）-3-羟基-4- [3-（甲氧基甲基）苯基]丁-1-烯基} -5-邻环戊基）乙基]硫烷基}丁酸和硅氧烷基压敏粘合剂。这是一种稳定的有效安全的制剂，皮肤渗透性几乎没有变化，药物不能快速但不断地释放。

7. 发明申请

US20100041758A1 ADHESIVE PREPARATION 失效
标题翻译：胶粘制品
公开(公告)号：US20100041758A1
公开(公告)日：2010-02-18
申请号：US12447215
申请日：2007-10-25
申请人： Akio Nishiura , Hikaru Sugihara , Kazuya Abe
发明人： Akio Nishiura , Hikaru Sugihara , Kazuya Abe
IPC分类号： A61K31/19 , A61P19/08
CPC分类号： A61K31/5575 , A61K9/7053 , A61K9/7069 , A61K9/7076
摘要： An adhesive preparation which has a pressure-sensitive adhesive layer comprising two components, i.e., a C1-4 alcohol ester of 4-{[2-((1R,2R,3R)-3-hydroxy-2-{(1E,3S)-3-hydroxy-4-[3-(methoxymethyl)phenyl]but-1-enyl}-5-osocyclopentyl)ethyl]sulfanyl}butanoic acid and a silicone-based pressure-sensitive adhesive. This is an effective and safe preparation which is stable, shows little change in skin permability and release a drug not rapidly but continuously.
摘要翻译：一种粘合剂制剂，其具有包含两种组分的压敏粘合剂层，即4 - {[2 - （（1R，2R，3R）-3-羟基-2 - {（1E，3S ）-3-羟基-4- [3-（甲氧基甲基）苯基]丁-1-烯基} -5-邻环戊基）乙基]硫烷基}丁酸和硅氧烷基压敏粘合剂。这是一种稳定的有效安全的制剂，皮肤渗透性几乎没有变化，药物不能快速但不断地释放。

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