35715-70-9Relevant academic research and scientific papers
Neladenoson Bialanate Hydrochloride: A Prodrug of a Partial Adenosine A1 Receptor Agonist for the Chronic Treatment of Heart Diseases
Meibom, Daniel,Albrecht-Küpper, Barbara,Diedrichs, Nicole,Hübsch, Walter,Kast, Raimund,Kr?mer, Thomas,Krenz, Ursula,Lerchen, Hans-Georg,Mittendorf, Joachim,Nell, Peter G.,Süssmeier, Frank,Vakalopoulos, Alexandros,Zimmermann, Katja
supporting information, p. 728 - 737 (2017/05/26)
Adenosine is known to be released under a variety of physiological and pathophysiological conditions to facilitate the protection and regeneration of injured ischemic tissues. The activation of myocardial adenosine A1 receptors (A1Rs) has been shown to inhibit myocardial pathologies associated with ischemia and reperfusion injury, suggesting several options for new cardiovascular therapies. When full A1R agonists are used, the desired protective and regenerative cardiovascular effects are usually overshadowed by unintended pharmacological effects such as induction of bradycardia, atrioventricular (AV) blocks, and sedation. These unwanted effects can be overcome by using partial A1R agonists. Starting from previously reported capadenoson we evaluated options to tailor A1R agonists to a specific partiality range, thereby optimizing the therapeutic window. This led to the identification of the potent and selective agonist neladenoson, which shows the desired partial response on the A1R, resulting in cardioprotection without sedative effects or cardiac AV blocks. To circumvent solubility and formulation issues for neladenoson, a prodrug approach was pursued. The dipeptide ester neladenoson bialanate hydrochloride showed significantly improved solubility and exposure after oral administration. Neladenoson bialanate hydrochloride is currently being evaluated in clinical trials for the treatment of heart failure.
PYRAZOLYL PYRIMIDINAMINE COMPOUND AND APPLICATION THEREOF
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Paragraph 0372; 0373, (2016/12/01)
Disclosed are pyrazolyl pyrimidinamine compounds with structures as shown in Formula I: The definitions of each of the substituents can be seen in the description. The compounds of present invention have a broad spectrum of bactericidal, insecticidal and acaricidal activity, and have good control effect on downy mildew of cucumber, powdery mildew of wheat, corn rust, anthracnosis of cucumber and the like, and especially have better control effect on downy mildew of cucumber, powdery mildew of wheat and anthracnosis of cucumber. The compounds of present invention also show good insecticidal activity, part of the compounds, at very low doses, have excellent control effect on diseases caused by Plutella xylostella, armyworm, Myzus persicae, Tetranychus cinnabarinus etc.
