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    • 97. 发明公开
    • DIAZENIUMDIOLATE CYCLOHEXYL DERIVATIVES
    • DIAZENIUMDIOLAT环己基衍生物
    • EP2704568A1
    • 2014-03-12
    • EP12779616.7
    • 2012-04-27
    • Merck Sharp & Dohme Corp.
    • ALI, AmjadLO, Michael, Man-ChuYAN, Lin
    • A01N33/24A61K31/15C07C243/00
    • C07C247/06C07B2200/07C07C245/24C07C291/08C07C2601/14C07D231/12C07D249/04C07D317/72
    • The present invention includes diazeniumdiolate cyclohexyl derivatives, such as a compound having the structure of formula (I) wherein R
      1 -R
      13 are as defined herein, including various pharmaceutically acceptable salts and hydrates thereof, and pharmaceutical formulations comprising the diazeniumdiolate cyclohexyl derivatives. The invention also includes a method for treating hypertension, Pulmonary Arterial Hypertension (PAH), congestive heart failure, conditions resulting from excessive water retention, cardiovascular disease, diabetes, oxidative stress, endothelial dysfunction, cirrhosis, pre-eclampsia, osteoporosis or nephropathy, comprising administering a compounds of the invention to a patient having such a condition, or being at risk to having such condition.
    • 具有结构或其药学上可接受的盐的化合物,其中R 6是氢,-OH,-C 1-6烷基,-OC 1-6烷基,芳基或卤素,或与R 7一起形成氧代基团,或与R 7和 它们连接的原子形成5-7元碳环或具有1,2或3个杂原子的5-7元杂环,其中烷基和芳基是未取代的或独立地是单 - ,二 - 或 - 用R14三取代; R 7是氢,C 1-6烷基,-CF 3,芳基,-O-芳基,-O-C 1-6烷基,-C(O)OC 1-6烷基,-C(R 15 R 16)OH,5- ,2,3或4个氮原子,或卤素,或与R6一起形成氧代基团,或与R6及其连接的原子一起形成5-7元碳环或5-7元碳环, 其中烷基,芳基和杂芳基是未取代的或独立地被R 14独立地,二或三取代; R 12是氢,C 1-6烷基或 - (CH 2)1-2 OH,或者与R 13和它们所连接的氮原子一起形成含有一个氮原子和0或1个氧的4-至7-元杂环 原子,其中所述环是未取代的或独立地被卤素或-C 1-6烷基单,二或三取代; R 13是-C 1-6烷基或 - (CH 2)1-2 OH,或与R 12和它们所连接的氮原子一起形成含有一个氮原子和0或1个氧原子的4-至7-元杂环, 其中所述环是未取代的或独立地被卤素或-C 1-6烷基单,二或三取代。