179483-00-2Relevant articles and documents
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. 4. Structure-activity relationship in the dihydropyrimidine series
Wong, Wai C.,Sun, Wanying,Lagu, Bharat,Tian, Dake,Marzabadi, Mohammad R.,Zhang, Fengqi,Nagarathnam, Dhanapalan,Miao, Shou W.,Wetzel, John M.,Peng, Jian,Forray, Carlos,Chang, Raymond S. L.,Chen, Tsing B.,Ransom, Richard,O'Malley, Stacey,Broten, Theodore P.,Kling, Paul,Vyas, Kamlesh P.,Zhang, Kanyin,Gluchowski, Charles
, p. 4804 - 4813 (2007/10/03)
We have previously disclosed dihydropyridines such as 1a,b as selective α(1a) antagonists as a potential treatment for benign prostatic hyperplasia (BPH). The propensity of dihydropyridines toward an oxidation led us to find suitable replacements of the core unit. The accompanying papers describe the structure-activity relationship (SAR) of dihydropyrimidinones 2a,b as selective α(1a) antagonists. We report herein the SAR of dihydropyrimidines such as 4 and highlight the similarities and differences between the dihydropyrimidine and dihydropyrimidinone series of compounds.
