公开(公告)号：EP2329824A1

公开(公告)日：2011-06-08

申请号：EP09813104.8

申请日：2009-09-10

申请人： Astellas Pharma Inc.

发明人： TAKESHITA, Nobuaki ,  NISHIGAKI, Fusako ,  AOKI, Toshiaki ,  TAMURA, Seiji ,  KIKUCHI, Kazumi ,  KURODA, Akio

IPC分类号： A61K31/5375 ,  A61P25/04 ,  C07D265/30

CPC分类号： C07D265/30 ,  A61K31/5375

摘要： Provided is a novel potent pharmaceutical composition for treating nociceptive pain.
The present invention relates to a pharmaceutical composition for treating nociceptive pain, containing a morpholine derivative or a pharmaceutically acceptable salt thereof, as an active ingredient. The present invention is useful in providing an excellent pharmaceutical composition for treating nociceptive pain. In addition, the present invention is particularly useful in providing a pharmaceutical composition for treating pain accompanying a disease selected from the group consisting of rheumatoid arthritis, rheumatoid spondylitis, osteoarthritis, spondylosis deformans, gouty arthritis, juvenile arthritis, scapulohumeral periarthritis, and cervical syndrome, lumbago, lumbago accompanying spondylosis deformans, menalgia, pain and tumentia after inflammation, operation or injury, pain after odontectomy, and cancer pain. In addition, the present invention is particularly useful for alleviating pain in a damaged cartilage region, and is particularly useful for osteoarthritis in which NSAIDs are not effective.

摘要翻译： 提供了用于治疗伤害性疼痛的新型有效药物组合物。 本发明涉及含有吗啉衍生物或其药学上可接受的盐作为活性成分的伤害性疼痛的治疗药物组合物。 本发明可用于提供用于治疗伤害性疼痛的优良药物组合物。 此外，本发明特别可用于提供用于治疗伴随选自以下的疾病的药物组合物：选自类风湿性关节炎，类风湿性脊椎炎，骨关节炎，变形性软骨病，痛风性关节炎，幼年型关节炎，肩周炎性关节炎和子宫颈综合征， 腰痛，腰痛伴椎关节僵硬，月经痛，炎症，手术或损伤后的疼痛和胸痛，odontectomy后的疼痛和癌症疼痛。 此外，本发明特别可用于缓解软骨损伤区域的疼痛，并且特别适用于其中NSAIDs无效的骨关节炎。

公开(公告)号：EP2177505A1

公开(公告)日：2010-04-21

申请号：EP08792314.0

申请日：2008-08-07

申请人： Astellas Pharma Inc.

发明人： KINOYAMA, Isao ,  MIYAMOTO, Satoshi ,  MIYAZAKI, Takehiro ,  KOGANEMARU, Yohei ,  KAWAMOTO, Yuichiro ,  SHIRAISHI, Nobuyuki ,  HOSHII, Hiroaki ,  KURODA, Akio ,  YAMAZAKI, Mayako ,  YASUDA, Minoru ,  MIZUNO, Hiroaki

IPC分类号： C07C279/22 ,  A61K31/341 ,  A61K31/352 ,  A61K31/495 ,  A61P25/28 ,  A61P43/00 ,  C07D295/12 ,  C07D307/52 ,  C07D311/04

CPC分类号： C07D295/12 ,  C07C279/22 ,  C07C317/44 ,  C07C2601/02 ,  C07C2602/10 ,  C07C2602/12 ,  C07D213/56 ,  C07D213/61 ,  C07D213/64 ,  C07D215/12 ,  C07D231/12 ,  C07D239/26 ,  C07D241/12 ,  C07D261/08 ,  C07D277/30 ,  C07D295/155 ,  C07D307/52 ,  C07D307/54 ,  C07D309/04 ,  C07D311/04 ,  C07D311/58 ,  C07D313/08 ,  C07D319/18 ,  C07D333/24 ,  C07D333/54 ,  C07D333/56 ,  C07D335/06 ,  C07D405/04 ,  C07D407/04 ,  C07D409/04 ,  C07D471/04

摘要： An object of the present invention is to provide a novel and excellent agent for treating or preventing dementia, schizophrenia, and the like, based on the serotonin 5-HT 5A receptor modulating action.
It was confirmed that a bicyclic acylguanidine derivative which has a characteristic structure that guanidine is bonded to one ring of a bicyclic structure such as chromene and dihydronaphthalene through a carbonyl group and a cyclic group is bonded on the other ring, has a potent 5-HT 5A receptor modulating action and an excellent pharmacological action based on this mechanism. The present invention is useful as an excellent agent for treating or preventing dementia, schizophrenia, bipolar disorder, or attention deficit hyperactivity disorder.

摘要翻译： 本发明的目的在于提供基于血清素5-HT5A受体调节作用的新型优异的痴呆症，精神分裂症等的治疗或预防剂。 已证实具有特征结构的双环酰基胍衍生物具有强效的5-HT5A，所述双环酰基胍衍生物具有特征结构，其中胍与色烯和二氢萘的双环结构的一个环经由羰基和环状基团键合， 受体调节作用和基于这种机制的优异药理作用。 本发明作为治疗或预防痴呆症，精神分裂症，双相性精神障碍或注意力缺陷多动症的优异药剂是有用的。

公开(公告)号：EP3904294A1

公开(公告)日：2021-11-03

申请号：EP19902655.0

申请日：2019-12-27

申请人： Astellas Pharma Inc.

发明人： KIKUCHI, Takashi ,  MIZUTANI, Tsuyoshi ,  TOYA, Hiroki ,  KURODA, Akio ,  GOTO, Yota ,  HIRASAWA, Shun ,  SUGIMORI, Toshiyuki

IPC分类号： C01G49/00 ,  C01G49/02 ,  C01G49/06 ,  C01G49/08 ,  A61K49/06 ,  B01J31/02

摘要： [Problem]
A novel method for producing a nanoparticle having a metal particle which contains iron oxide to which one or more hydrophilic ligands are coordination bonded is provided, where the nanoparticle is useful as a contrast agent for magnetic resonance imaging.
[Means for Solution]
As the novel method for producing a nanoparticle having a metal particle which contains iron oxide to which one or more hydrophilic ligands are coordination bonded, by performing ligand exchange to a hydrophilic ligand from an iron oxide nanoparticle having a surface to which a hydrophobic ligand is coordination bonded in one step using a phase transfer catalyst, it is possible to expect shortening of production processs and reduction of hydrophilic ligands used.
Furthermore, by producing an iron oxide nanoparticle having a surface to which a hydrophobic ligand is coordination bonded using a dropwise addition method, it is possible to avoid a rapid temperature rise and a reaction at a high temperature of 200°C or higher, which is more advantageous for industrial production.

公开(公告)号：EP2330099A1

公开(公告)日：2011-06-08

申请号：EP09813105.5

申请日：2009-09-10

申请人： Astellas Pharma Inc.

发明人： KIKUCHI, Kazumi ,  KURODA, Akio ,  MIZOGUCHI, Ryo ,  SAKAMOTO, Kenichirou ,  TAKEGUCHI, Kazuhiro

IPC分类号： C07D265/30

CPC分类号： C07D265/30

摘要： [Problem]
Provided are an acid addition salt of (+)-2-[(inden-7-yloxy)methyl]morpholine (compound A) and a novel crystal thereof, which are for use as a medicament or a drug substance, and which has high storage stability, particularly high stability against humidity and light.
[Means for Solution]
An acid addition salt of the compound A with an acid selected from benzenesulfonic acid and hydrobromic acid is a compound which is isolated in the form of a crystal, is a solid at room temperature, exhibits no hygroscopicity at such a level that causes a problem for use as a medicament or a drug substance, has stability against humidity and light, and is therefore extremely useful as a medicament or a drug substance.

摘要翻译： [问题]提供用作药物或药物的（+） - 2 - [（茚-7-基氧基）甲基]吗啉（化合物A）及其新结晶的酸加成盐， 其具有高储存稳定性，特别是对湿度和光的高稳定性。 [解决方案]化合物A的酸加成盐与选自苯磺酸和氢溴酸的酸是化合物，其以结晶形式分离，在室温下为固体，在这种水平下表现出不吸湿性 这导致用作药物或药物的问题，对湿度和光线具有稳定性，因此作为药物或药物物质非常有用。