191353-81-8Relevant academic research and scientific papers
5-(heterocyclic alkyl)-6-aryl-dihydropyrimidines
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, (2008/06/13)
This invention is directed to dihydropyrimidine compounds of the following formula: which are selective antagonists for human α1Areceptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotency, cardiac arrhythmia and for the treatment of any disease where antagonism of the α1Areceptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.
5-(heterocyclic alkyl)-6-aryl-dihydropyrimidines
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, (2008/06/13)
This invention is directed to dihydropyrimidine compounds of the following formula: which are selective antagonists for human α1Creceptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotence, cardiac arrhythmia and for the treatment of any disease where antagonism of the α1Creceptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.
Design and synthesis of novel α(1a) adrenoceptor-selective antagonists. 1. Structure-activity relationship in dihydropyrimidinones
Nagarathnam, Dhanapalan,Miao, Shou Wu,Lagu, Bharat,Chiu, George,Fang, James,Dhar, T. G. Murali,Zhang, Jack,Tyagarajan, Sriram,Marzabadi, Mohammad R.,Zhang, Fengqi,Wong, Wai C.,Sun, Wanying,Tian, Dake,Wetzel, John M.,Forray, Carlos,Chang, Raymond S. L.,Broten, Theodore P.,Ransom, Richard W.,Schorn, Terry W.,Chen, Tsing B.,O'Malley, Stacey,Kling, Paul,Schneck, Kathryn,Bendesky, Robert,Harrell, Charles M.,Vyas, Kamlesh P.,Gluchowski, Charles
, p. 4764 - 4777 (2007/10/03)
Dihydropyrimidinones such as compound 12 exhibited high binding affinity and subtype selectivity for the cloned human α(1a) receptor. Systematic modifications of 12 led to identification of highly potent and subtype- selective compounds such as (+)-30 and
