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TRPV4 antagonist
专利权人:
グラクソスミスクライン、インテレクチュアル、プロパティー、(ナンバー2)、リミテッド
发明人:
カール、エイ.ブルックス,パトリック、シュトイ,グォセン、イェ
申请号:
JP2018560587
公开号:
JP2019520327A
申请日:
2017.05.18
申请国别(地区):
JP
年份:
2019
代理人:
摘要:
The present invention relates to novel compounds useful as TRPV4 antagonists, specifically compound 1-(((5S, 7R) -3- (5-cyclopropylpyrazin-2-yl) -7-hydroxy-2-oxo. -1-oxa-3-azaspiro [4.5] decan-7-yl) methyl) -1H-benzo [d] imidazole-6-carbonitrile, a pharmaceutically acceptable salt thereof, and a medicament containing the compound It relates to a composition. The compounds of the present invention can be used in atherosclerosis, vasogenic edema, postoperative intraperitoneal edema, eye edema, brain edema, disorders related to local and systemic edema, fluid retention, sepsis, hypertension, inflammation, Bone-related disorders and congestive heart failure, lung disorders, chronic obstructive pulmonary disorders, ventilator-induced lung injury, high altitude induced pulmonary edema, acute respiratory distress syndrome, acute lung injury, pulmonary fibrosis, sinusitis / rhinitis, Asthma, acute cough, cough including subacute cough and chronic cough, pulmonary hypertension, overactive bladder, cystitis, pain, motor neuron disorder, hereditary gain-of-function disorder, cardiovascular disease, renal dysfunction, stroke, glaucoma Retinopathy, endometriosis, premature labor, dermatitis, pruritus, pruritus in liver disease, diabetes, metabolic disorder, obesity, migraine, pancreatitis, tumor suppression, immunosuppression, osteoarthritis, Crohn's disease, colitis , Diarrhea, intestinal irregularities (hypersensitivity / anti Reduction), fecal incontinence, irritable bowel syndrome (IBS), constipation, pain and spasm of the intestine, celiac disease can be useful lactose intolerance, as well as in the treatment of a condition selected from flatulence.本発明は、TRPV4拮抗薬として有用な新規化合物、具体的には、化合物1-(((5S,7R)-3-(5-シクロプロピルピラジン-2-イル)-7-ヒドロキシ-2-オキソ-1-オキサ-3-アザスピロ[4.5]デカン-7-イル)メチル)-1H-ベンゾ[d]イミダゾール-6-カルボニトリル、その薬学的に許容可能な塩および前記化合物を含有する医薬組成物に関する。本発明の化合物は、アテローム性動脈硬化症、血管原性浮腫、術後腹腔内浮腫、眼の浮腫、脳浮腫、局部および全身性浮腫に関連する障害、体液貯留、敗血症、高血圧症、炎症、骨関連障害および鬱血性心不全、肺障害、慢性閉塞性肺障害、人工呼吸器誘発性肺損傷、高地誘発性肺水腫、急性呼吸窮迫症候群、急性肺損傷、肺線維症、副鼻腔炎/
来源网站:
中国工程科技知识中心
来源网址:
http://www.ckcest.cn/home/

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