179481-95-9Relevant 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.
Synthesis and evaluation of furo[3,4-d]pyrimidinones as selective α(1a)-adrenergic receptor antagonists
Lagu, Bharat,Tian, Dake,Chiu, George,Nagarathnam, Dhanapalan,Fang, James,Shen, Quanrong,Forray, Carlos,Ransom, Richard W.,Chang, Raymond S. L.,Vyas, Kamlesh P.,Zhang, Kanyin,Gluchowski, Charles
, p. 175 - 178 (2007/10/03)
Furo[3,4-d]pyrimidinones were found to be metabolites of dihydropyrimidinones such as 1a-b that are subtype-selective antagonists of the α(1a)-adrenergic receptor. A versatile synthesis that provides access to furo[3,4-d]pyrimidinones in high yield and in enantiomerically pure forms is described along with structure-activity relationships in the series.
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
5-(HETEROCYCLIC ALKYL)-6-ARYL-DIHYDROPYRIMIDINES
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, (2008/06/13)
This invention is directed to dihydropyrimidine compounds which are selective antagonists for human α 1C receptors and which have the structure: STR1 wherein A is aryl; R 1, R 2 and R. sub.3 are alkyl or heteroalkyl; R 4 is heterocyclic alkyl; and X is S, O or NR 3. This invention also relates to use of these compounds for the treatment of benign prostatic hyperplasia and other diseases where antagonism of the human α 1C receptor is useful. The invention further provides pharmaceutical compositions comprising a therapeutically effective amount of such a compound and a pharmaceutically acceptable carrier.
