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：EP2123643A1

公开(公告)日：2009-11-25

申请号：EP08722106.5

申请日：2008-03-14

申请人： Astellas Pharma Inc.

发明人： AOKI, Toshiaki ,  MURAI, Nobuhito ,  TAMURA, Seiji ,  YAMAMOTO, Hiroko ,  HAMAKAWA, Nozomu

IPC分类号： C07D265/30 ,  A61K31/5375 ,  A61P3/10 ,  A61P25/04

CPC分类号： C07D265/30 ,  A61K31/5375

摘要： The present invention relates to an agent for preventing and/or treating diabetic neuropathy comprising a 2-[(substituted-inden-7-yloxy)methyl]morpholine of the formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient. The invention is useful for providing an excellent agent for preventing and/or treating diabetic neuropathy, and particularly useful for providing an agent for preventing and/or treating diabetic motor neuropathy (such as muscle weakness disorder (such as muscle weakness disorder with inability to walk independently)), diabetic sensory neuropathy (such as paresthesia (such as vibration perception abnormality), allodynia, hypoesthesia (such as numbness of extremities or cold sensation), or pain), or diabetic autonomic neuropathy (such as stool abnormality (such as constipation or diarrhea), urination disorder, impotence, orthostatic hy-potension, sudomotor dysfunction, abnormal heart rate variability, or delayed gastric emptying). Further, the invention is particularly useful for providing an agent for improving pathophysiology of diabetic neuropathy.

摘要翻译： 本发明涉及用于预防和/或治疗糖尿病性神经病变的药物，其包含式（I）的2 - [（取代的茚-7-基氧基）甲基]吗啉或其药学上可接受的盐作为活性成分。 本发明可用于提供用于预防和/或治疗糖尿病性神经病变的优异剂，特别可用于提供用于预防和/或治疗糖尿病运动神经病变（例如肌肉无力障碍（例如无力行走的肌肉无力障碍） 独立）），糖尿病性感觉神经病变（如感觉异常（如振动感知异常），异常性疼痛，麻醉（如四肢麻木或感冒）或疼痛）或糖尿病性自主神经病变（如便秘） 或腹泻），排尿障碍，阳ence，直立性血压，苏州功能障碍，心率异常异常或延迟胃排空）。 此外，本发明特别可用于提供改善糖尿病性神经病变病理生理学的药剂。

公开(公告)号：EP2123642A1

公开(公告)日：2009-11-25

申请号：EP08722105.7

申请日：2008-03-14

申请人： Astellas Pharma Inc.

发明人： AOKI, Toshiaki ,  TAMURA, Seiji

IPC分类号： C07D265/30 ,  A61K31/5375 ,  A61P3/10 ,  A61P25/04

CPC分类号： A61K31/5375

摘要： The present invention relates to an agent for preventing and/or treating neuropathic pain comprising a 2-[(substituted-inden-7-yloxy)methyl]morpholine of the formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient. The invention is useful for providing an excellent agent for preventing and/or treating neuropathic pain, and particularly useful for providing an agent for preventing and/or treating allodynia, hyperalgesia, hyperesthesia, spontaneous pain, cancer pain, trigeminal neuralgia, phantom Limb pain, postherpetic neuralgia, fibromyalgia, low back/leg pain, thalamic pain, entrapment (compressive) peripheral neuropathy, atypical facial pain, pain accompanying spinal cord injury, pain accompanying multiple sclerosis, pain accompanying chemotherapy-induced neuropathy, cancer pain on which an analgesic effect of a narcotic analgesic such as morphine is insufficient, pain accompanying diabetic neuropathy, and the like.

摘要翻译： 本发明涉及用于预防和/或治疗神经性疼痛的药剂，其包含式（I）的2 - [（取代 - 茚-7-基氧基）甲基]吗啉或其药学上可接受的盐作为活性成分。 本发明可用于提供用于预防和/或治疗神经性疼痛的优异剂，特别可用于提供预防和/或治疗异常性疼痛，痛觉过敏，感觉过敏，自发性疼痛，癌症疼痛，三叉神经痛，幻肢痛， 带状疱疹后神经痛，纤维肌痛，腰背痛，丘脑疼痛，包扎（压迫性）周围神经病变，非典型面部疼痛，伴随脊髓损伤的疼痛，伴随多发性硬化的疼痛，伴随化疗诱导的神经病变的疼痛，止痛效果 麻醉性镇痛药如吗啡不足，伴有糖尿病性神经病变的疼痛等。

公开(公告)号：EP1709968A1

公开(公告)日：2006-10-11

申请号：EP05704173.3

申请日：2005-01-27

申请人： Astellas Pharma Inc.

发明人： KAKIMOTO, Shuichiro ,  TAMURA, Seiji ,  NAGAKURA, Yukinori

IPC分类号： A61K31/663 ,  A61P19/08 ,  A61P25/04 ,  A61P29/00 ,  A61P35/00 ,  A61P35/04 ,  A61P43/00 ,  C07F9/6561

CPC分类号： A61K31/663 ,  C07F9/6561

摘要： The present inventors have carried out intensive screening of a new type compound which inhibits the P2X 2/3,3 receptor and found as a result that minodronic acid as a bisphosphonate having bone resorption inhibitory action shows excellent P2X 2/3,3 receptor inhibitory action and can be used as a preventive or therapeutic agent for various pains, thus accomplishing the invention. That is, the invention relates to a P2X 2/3,3 receptor inhibitor, particularly an analgesic, which comprises minodronic acid or a salt thereof as the active ingredient.
Since the "P2X 2/3 and/or P2X 3 receptor inhibitor" of the invention inhibits the function of P2X 2/3,3 receptor known as a molecule which is concerned in various pains consisting of nociceptive pain, inflammatory pain and neurogenic pain, it is useful for the prevention or treatment of various pains in which the P2X 2/3,3 receptor is concerned in the pain transduction.

摘要翻译： 本发明人对抑制P2X 2 / 3,3受体的新型化合物进行了深入筛选，结果发现作为具有骨吸收抑制作用的二膦酸的米诺膦酸显示优异的P2X 2 / 3,3受体抑制作用 并且可以用作各种疼痛的预防或治疗剂，从而完成本发明。 也就是说，本发明涉及一种P2X 2 / 3,3受体抑制剂，特别是一种止痛剂，其包含米诺膦酸或其盐作为活性成分。 由于本发明的“P2X 2/3和/或P2X 3受体抑制剂”抑制了被称为分子的P2X 2 / 3,3受体的作用，该分子涉及由伤害性疼痛，炎性疼痛和神经源性疼痛组成的各种疼痛， 它可用于预防或治疗其中P2X 2 / 3,3受体涉及疼痛转导的各种疼痛。