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2. 发明申请

US20050009789A1 Cyclooxygenase inhibition with nitroxyl 审中-公开
标题翻译：用硝酰基抑制环加氧酶
公开(公告)号：US20050009789A1
公开(公告)日：2005-01-13
申请号：US10845619
申请日：2004-05-12
申请人： David Wink , Katrina Miranda , Christopher Bradbury , David Gius , Jon Fukuto , Martin Feelisch
发明人： David Wink , Katrina Miranda , Christopher Bradbury , David Gius , Jon Fukuto , Martin Feelisch
IPC分类号： A61K31/655
CPC分类号： A61K31/655
摘要： Nitroxyl is used to inhibit COX-2 activity and particularly to selectively inhibit COX-2 activity. Nitroxyl also is used to treat conditions that respond favorably to inhibition of COX-2 activity in subjects having such conditions. In some cases nitroxyl is used to treat conditions that respond favorably to inhibition of COX-2 activity in subjects having such conditions and who also have at least one other condition for which inhibition of COX-1 activity is disadvantageous. Nitroxyl can be provided directly, but typically is provided with the use of a nitroxyl donor. Nitroxyl donors include any agent or compound (or combination thereof) that donates HNO or NO−. Diazeniumdiolates are used in some cases as nitroxyl donors. In particular instances, diazeniumdiolates having a primary amine group are used as nitroxyl donors. Nitroxyl-donating compounds also are screened for selective COX-2 inhibition for identification as therapeutic agents.
摘要翻译：硝酸用于抑制COX-2活性，特别是选择性抑制COX-2活性。硝酸还用于治疗对具有这种病症的受试者中COX-2活性的抑制作用有利的病症。在某些情况下，硝酰基用于治疗对具有这种病症的受试者中对COX-2活性的抑制作用有利的条件，并且还具有抑制COX-1活性的至少一种其它病症是不利的。可以直接提供硝基，但通常使用硝酰基供体。硝基供体包括提供HNO或NO - 的任何试剂或化合物（或其组合）。在一些情况下使用二氮烯二硫代吗啉作为硝酰基供体。在具体情况下，使用具有伯胺基团的二氮烯鎓二醇作为硝酰基供体。硝酸氧基化合物也被筛选用于选择性COX-2抑制用于鉴定作为治疗剂。

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