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    • 6. 发明申请
    • Amorphous Composition
    • 无定形组成
    • US20080096924A1
    • 2008-04-24
    • US11722008
    • 2005-12-16
    • Hideo MasudaHikaru SugiharaAkio Nishiura
    • Hideo MasudaHikaru SugiharaAkio Nishiura
    • A61K31/454A61P25/00C07D417/12
    • A61K9/1652A61K9/0043A61K9/006A61K9/1635A61K9/2027A61K9/2054C07D417/12
    • 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).
    • 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)。
    • 7. 发明申请
    • COMPOUND FOR TREATING CARTILAGE DISORDERS
    • 化合物用于治疗消化系统疾病
    • US20140171388A1
    • 2014-06-19
    • US14237037
    • 2012-08-03
    • Tetsuo ObitsiKousuke TaniHikaru SugiharaAkio NishiuraShinsei Fujimura
    • Tetsuo ObitsiKousuke TaniHikaru SugiharaAkio NishiuraShinsei Fujimura
    • C07C405/00C07C235/16C07C59/56C07C65/28
    • C07C59/56A61K9/0019A61K47/26A61K47/6951C07C235/06C07C235/16C07C405/00C07C2601/04C07C2601/08Y10T428/2982
    • 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.
    • 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。