218610-53-8Relevant academic research and scientific papers
Bradykinin B1 antagonists: SAR studies in the 2,3-diaminopyridine series
Kuduk, Scott D.,Chang, Ronald K.,Ng, Christina,Murphy, Kathy L.,Ransom, Richard W.,Tang, Cuyue,Prueksaritanont, Thomayant,Freidinger, Roger M.,Pettibone, Douglas J.,Bock, Mark G.
, p. 3925 - 3929 (2007/10/03)
SAR study of the biphenyl region of 2,3-diaminopyridine bradykinin B 1 antagonists was investigated with non-aromatic carbo- and heterocyclic rings. A piperidine ring was found to be a good replacement for the proximal phenyl ring while replacement of the distal phenyl was optimal with a cyclohexyl group leading to a dramatic improvement in affinity for the B 1 receptor.
Alpha 1a adrenergic receptor antagonists
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, (2008/06/13)
This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as alpha 1a adrenergic receptor antagonists. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia are achieved.
