1337567-22-2Relevant academic research and scientific papers
Soluble guanylate cyclase stimulators for the treatment of hypertension: Discovery of MK-2947
Brockunier, Linda,Stelmach, John,Guo, Jian,Spencer, Tracy,Rosauer, Keith,Bansal, Alka,Cai, Sheng-Jian,Chen, Nancy,Cummings, John,Huang, Li,Johnson, Timothy,Levesque, Sonia,Luo, Lin,Maloney, Kevin,Metzger, Joseph,Mortko, Christopher,Ortega, Karen,Pai, Lee-Yuh,Pereira, Antonio,Salituro, Gino,Shang, Jackie,Shepherd, Cherrie,Sherrie Xu, Shiyao,Yang, Qifeng,Cui, Jisong,Roy, Sophie,Parmee, Emma,Raghavan, Subharekha
supporting information, (2020/10/12)
The NO-sGC-cGMP signaling pathway plays an important role in the cardiovascular system. Loss of nitric oxide tone or impaired signaling has been associated with cardiovascular diseases, such as hypertension, pulmonary hypertension and heart failure. Direct activation of sGC enzyme independent of NO represents a novel approach for modulating NO signaling with tremendous therapeutic potential. Herein, we describe the design of a structurally novel class of heme-dependent sGC stimulators containing the 3,3-dimethylpyrrolidin-2-one moiety which resulted in the identification of the potent, selective stimulator 30 (MK-2947) for the treatment of hypertension.
SOLUBLE GUANYLATE CYCLASE ACTIVATORS
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Page/Page column 39; 82, (2011/10/13)
The invention relates to compounds having the structure of Formula (I) and pharmaceutically acceptable salts thereof, which are soluble guanylate cyclase activators. The compounds are capable of modulating the body's production of cyclic guanosine monophosphate ("cGMP") and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The compounds are useful for treatment or prevention of cardiovascular diseases, endothelial dysfunction, diastolic dysfunction, atherosclerosis, hypertension, pulmonary hypertension, angina pectoris, thromboses, restenosis, myocardial infarction, strokes, cardiac insufficiency, pulmonary hypertonia, erectile dysfunction, asthma bronchiale, chronic kidney insufficiency, diabetes, or cirrhosis of the liver.
