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    TRPV4 ANTAGONIST
    2.
    发明公开
    TRPV4 ANTAGONIST 审中-公开

    公开(公告)号：EP3458451A1

    公开(公告)日：2019-03-27

    申请号：EP17726035.3

    申请日：2017-05-18

    申请人： GlaxoSmithKline Intellectual Property (No. 2) Limited

    发明人： BROOKS, Carl A. ,  STOY, Patrick ,  YE, Guosen

    IPC分类号： C07D413/14 ,  A61K31/497 ,  A61P9/10

    摘要： The present invention relates to a novel compound useful as a TRPV4 antagonist, specifically the 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, pharmaceutically acceptable salts thereof and pharmaceutical compositions containing the compound. The compound of the invention can be useful in the treatment of a disease state selected from: atherosclerosis, disorders related to vasogenic edema, postsurgical abdominal edema, ocular edema, cerebral edema, local and systemic edema, fluid retention, sepsis, hypertension, inflammation, bone related dysfunctions and congestive heart failure, pulmonary disorders, chronic obstructive pulmonary disorder, ventilator induced lung injury, high altitude induced pulmonary edema, acute respiratory distress syndrome, acute lung injury, pulmonary fibrosis, sinusitis/rhinitis, asthma, cough; including acute cough, sub-acute cough and chronic cough, pulmonary hypertension, overactive bladder, cystitis, pain, motor neuron disorders, genetic gain of function disorders, cardiovascular disease, renal dysfunction, stroke, glaucoma, retinopathy, endometriosis, pre-term labor, dermatitis, pruritus, pruritus in liver disease, diabetes, metabolic disorder, obesity, migraine, pancreatitis, tumor suppression, immunosuppression, osteoarthritis, crohn's disease, colitis, diarrhea, intestinal irregularity (hyperreactivity/hyporeactivity), fecal incontinence, irritable bowel syndrome (IBS), constipation, intestinal pain and cramping, celiac disease, lactose intolerance, and flatulence.

    COMBINATIONS OF TRPV4 ANTAGONISTS
    8.
    发明公开
    COMBINATIONS OF TRPV4 ANTAGONISTS 审中-公开
    TRPV4-ANTAGONISTEN KOMBINATIONEN

    公开(公告)号：EP3121177A1

    公开(公告)日：2017-01-25

    申请号：EP16162808.6

    申请日：2012-06-15

    申请人： GlaxoSmithKline Intellectual Property (No. 2) Limited

    发明人： BROOKS, Carl ,  CHEUNG, Mui ,  EIDAM, Hilary, Schenck ,  GOODMAN, Krista, B ,  HAMMOND, Marlys ,  HILFIKER, Mark, A ,  HOANG, Tram, H ,  PATTERSON, Jaclyn, R ,  STOY, Patrick ,  YE, Guosen

    IPC分类号： C07D413/14 ,  C07D417/14 ,  C07D419/14 ,  C07D495/04 ,  A61K31/422 ,  A61P9/00 ,  A61P11/00

    CPC分类号： C07D413/14 ,  C07D417/14 ,  C07D419/14 ,  C07D495/04 ,  C07F9/65583

    摘要： A combination comprising a compound of Formula (I):

    or a pharmaceutically acceptable salt thereof;
    and one or more other therapeutic agents, selected from the group consisting of endothelin receptor antagonists, angiotensin converting enzyme (ACE) inhibitors, angiotension II receptor antagonists, vasopeptidase inhibitors, vasopressin receptor modulators, diuretics, digoxin, beta blocker, aldosterone antagonists, iontropes, NSAIDS, nitric oxide donors, calcium channel modulators, muscarinic antagonists, steroidal anti-inflammatory drugs, bronchodilators, anti-histamines, leukotriene antagonist, HMG-CoA reductase inhibitors, dual non-selective β-adrenoceptor and α 1 -adrenoceptor antagonists, type-5 phosphodiesterase inhibitors, and renin inhibitors.

    摘要翻译： 包含式（I）化合物或其药学上可接受的盐的组合： 和一种或多种选自内皮素受体拮抗剂，血管紧张素转换酶（ACE）抑制剂，血管紧张素II受体拮抗剂，血管肽酶抑制剂，加压素受体调节剂，利尿剂，地高辛，β阻断剂，醛固酮拮抗剂，离子转运体， NSAIDS，一氧化氮供体，钙通道调节剂，毒蕈碱拮抗剂，甾体抗炎药，支气管扩张剂，抗组胺药，白三烯拮抗剂，HMG-CoA还原酶抑制剂，双重非选择性肾上腺素受体和±1-肾上腺素能受体拮抗剂， 5磷酸二酯酶抑制剂和肾素抑制剂。