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1.发明公开
公开(公告)号：EP2740724A1
公开(公告)日：2014-06-11
申请号：EP12822308.8
申请日：2012-08-03
IPC分类号： C07C405/00 , A61K9/10 , A61K31/5575 , A61K47/10 , A61K47/26 , A61K47/34 , A61K47/36 , A61K47/40 , A61K47/44 , A61P19/08 , C07C69/732 , C07C69/92 , C07C235/16
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： 本发明提供活性形式由式（A）表示的化合物。 并且其可以注射到作为疾病的部分的关节腔中，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（其中全部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的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。 由于可以注射使用该化合物制成的悬浮液，而不需要切开患部，可以减轻患者的负担，作为药剂极为有用。
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公开(公告)号：EP2085088A1
公开(公告)日：2009-08-05
申请号：EP07830589.3
申请日：2007-10-25
发明人： NISHIURA, Akio , SUGIHARA, Hikaru , ABE, Kazuya
IPC分类号： A61K31/5575 , A61K9/70 , A61K47/34 , A61P1/00 , A61P1/04 , A61P7/02 , A61P7/10 , A61P9/00 , A61P9/12
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： 具有包含两种成分即4 - {[2 - （（1R，2R，3R）-3-羟基-2 - {（1E，3S，4R） ）-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}丁酸和硅氧烷基压敏粘合剂。 这是一种稳定有效且安全的制剂，其皮肤永久性几乎没有变化，并且不会迅速而持续地释放药物。
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公开(公告)号：EP2740724B1
公开(公告)日：2016-12-28
申请号：EP12822308.8
申请日：2012-08-03
IPC分类号： C07C405/00 , A61K9/10 , A61K31/5575 , A61K47/10 , A61K47/26 , A61K47/34 , A61K47/36 , A61K47/40 , A61K47/44 , A61P19/08 , C07C69/732 , C07C69/92 , C07C235/16
CPC分类号： C07C59/56 , A61K9/0019 , A61K47/26 , A61K47/6951 , C07C235/06 , C07C235/16 , C07C405/00 , C07C2601/04 , C07C2601/08 , Y10T428/2982
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4.发明公开PARTICLE AND PREPARATION CONTAINING THE PARTICLE 审中-公开TEILCHEN UNDESES TEILCHEN ENTHALTENDE ZUBEREITUNG
公开(公告)号：EP1857114A1
公开(公告)日：2007-11-21
申请号：EP06728775.5
申请日：2006-03-08
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。
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