208994-00-7Relevant academic research and scientific papers
Benzoxazine α-1 adrenergic compounds
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, (2008/06/13)
The present invention relates to compounds having formula I and to pharmaceutically acceptable salts thereof. Compounds of formula I inhibit α1adrenoreceptors and may be useful for treating benign prostatic hyperplasia (also called benign prost
Structure-activity studies for a novel series of tricyclic substituted hexahydrobenz[e]isoindole α(1A) adrenoceptor antagonists as potential agents for the symptomatic treatment of benign prostatic hyperplasia (BPH)
Meyer, Michael D.,Altenbach, Robert J.,Basha, Fatima Z.,Carroll, William A.,Condon, Stephen,Elmore, Steven W.,Kerwin Jr., James F.,Sippy, Kevin B.,Tietje, Karin,Wendt, Michael D.,Hancock, Arthur A.,Brune, Michael E.,Buckner, Steven A.,Drizin, Irene
, p. 1586 - 1603 (2007/10/03)
In search of a uroselective agent that exhibits a high level of selectivity for the α(1A) receptor, a novel series of tricyclic hexahydrobenz[e]isoindoles was synthesized. A generic pharmacophoric model was developed requiring the presence of a basic amine core and a fused heterocyclic side chain separated by an alkyl chain. It was shown that the 6- OMe substitution with R, R stereochemistry of the ring junction of the benz[e]isoindole and a two-carbon spacer chain were optimal. In contrast to the highly specific requirements for the benz[e]isoindole portion and linker chain, a wide variety of tricyclic fused heterocyclic attachments were tolerated with retention of potency and selectivity. In vitro functional assays for the α1 adrenoceptor subtypes were used to further characterize these compounds, and in vivo models of vascular vs prostatic tone were used to assess uroselectivity.
Benzopyranopyrrole and benzopyranopyridine alpha -1 adrenergic compounds
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, (2008/06/13)
The present invention relates to a compound of the formula and the pharmaceutically acceptable salts thereof wherein W is a bicyclic heterocyclic ring system. The compounds are alpha -1 adrenergic antagonists and are useful in the treatment of BPH; also disclosed are alpha -1 antagonist compositions and a method for antagonizing alpha -1 adrenoreceptors and treating BPH.
3-phenylpyrrolidine alpha-1 adrenergic compounds
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, (2008/06/13)
Compounds having the formula are alpha 1 adrenoreceptor antagonists. Processes for making these compounds, synthetic intermediates employed in these processes and a method for inhibiting alpha 1 adrenoreceptors and treating benign prostatic hyperplasia (also called benign prostatic hypertrophy or BPH) and other urological diseases such as BOO (bladder outlet obstruction), neurogenic bladder and gynecological syndromes such as dysmenorrhea are disclosed.
Benzopyranopyrrole and benzopyranopyridine α-1 adenergic compounds
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, (2008/06/13)
The present invention relates to a compound of the formula STR1 and the pharmaceutically acceptable salts thereof wherein W is a bicyclic heterocyclic ring system. The compounds are α-1 adrenergic antagonists and are useful in the treatment of BPH; also disclosed are α-1 antagonist compositions and a method for antagonizing α-1 adrenoreceptors and tr
