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11. 发明申请

WO2013012500A1 TRPV4 ANTAGONISTS 审中-公开
公开(公告)号：WO2013012500A1
公开(公告)日：2013-01-24
申请号：PCT/US2012/042622
申请日：2012-06-15
申请人： GLAXOSMITHKLINE LLC , 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
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： C07D263/52 , C07D498/00
CPC分类号： C07D413/14 , C07D417/14 , C07D419/14 , C07D495/04 , C07F9/65583
摘要： The present invention relates to spirocarbamate compounds of Formula (I) in which R1, (R2)Y, R3, R4, X and A have the meanings given in the specification. The invention further provides pharmaceutical compositions containing the compounds or pharmaceutically acceptable salts thereof and relates to their use of these compounds as TRPV4 antagonists in treating or preventing conditions associated with TRPV4 imbalance.
摘要翻译：本发明涉及其中R1，（R2）Y，R3，R4，X和A具有本说明书中给出的含义的式（I）的螺氨酸甲酯化合物。本发明还提供含有化合物或其药学上可接受的盐的药物组合物，并且涉及它们在治疗或预防与TRPV4不平衡相关的病症中作为TRPV4拮抗剂的用途。

12. 发明申请

WO2012174340A1 TRPV4 ANTAGONISTS 审中-公开
公开(公告)号：WO2012174340A1
公开(公告)日：2012-12-20
申请号：PCT/US2012/042603
申请日：2012-06-15
申请人： GLAXOSMITHKLINE LLC , BROOKS, Carl , CHEUNG, Mui , GOODMAN, Krista, B. , HAMMOND, Marlys
发明人： BROOKS, Carl , CHEUNG, Mui , GOODMAN, Krista, B. , HAMMOND, Marlys
IPC分类号： A61K31/423
CPC分类号： C07D413/14 , C07D413/06 , C07D413/08
摘要： The present invention relates to spirocarbamate analogs, pharmaceutical compositions containing them and their use as TRPV4 antagonists. The TRPV4 antagonist may be administered alone or in conjunction with one or more other therapeutic agents, ego agents being selected from the group consisting of endothelin receptor antagonists, angiotensin converting enzyme (ACE) inhibitors, angiotensin 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 padrenoceptor and u1 -adrenoceptor antagonists, type-5 phosphodiesterase inhibitors, and renin inhibitors.
摘要翻译：本发明涉及螺氨酸甲酯类似物，含有它们的药物组合物及其作为TRPV4拮抗剂的用途。 TRPV4拮抗剂可以单独给药或与一种或多种其它治疗剂联合施用，所述治疗剂选自由内皮素受体拮抗剂，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阻滞剂，醛固酮拮抗剂，离子诱导剂，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，选择性受体受体和u1-肾上腺素受体拮抗剂，5型磷酸二酯酶抑制剂和肾素抑制剂。

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