886206-08-2Relevant academic research and scientific papers
(Phenylpiperazinyl)cyclohexylureas: Discovery of α1a/1d-selective adrenergic receptor antagonists for the treatment of benign prostatic hyperplasia/lower urinary tract symptoms (BPH/LUTS)
Chiu, George,Li, Shengjian,Connolly, Peter J.,Pulito, Virginia,Liu, Jingchun,Middleton, Steven A.
, p. 640 - 644 (2008/09/17)
Benign prostatic hyperplasia/lower urinary tract symptoms (BPH/LUTS) can be effectively treated with α1 adrenergic receptor antagonists. Unfortunately, currently marketed α1 blockers produce CV-related side effects that are caused by
SUBSTITUTED ISOINDOLE-1,3-DIONES
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Page/Page column 26, (2008/06/13)
The present invention relates to substituted isoindole-1,3-dione compounds of Formula (I) and pharmaceutically acceptable forms thereof, as α1a/α1d adrenoreceptor modulators for the treatment of benign prostatic hypertrophy and lower
1-Arylpiperazinyl-4-cyclohexylamine derived isoindole-1,3-diones as potent and selective α-1a/1d adrenergic receptor ligands
Li, Shengjian,Chiu, George,Pulito, Virginia L.,Liu, Jingchun,Connolly, Peter J.,Middleton, Steven A.
, p. 1646 - 1650 (2007/10/03)
Subtype-selective α-1a and/or α-1d adrenergic receptor antagonists may be useful for the treatment of benign prostatic hyperplasia (BPH) and lower urinary tract symptoms (LUTS) with fewer adverse effects than non-selective drugs. A series of 1-arylpiperazinyl-4-cyclohexylamine derived isoindole-1,3-diones has been synthesized, displaying in vitro α1a and α1d binding affinity Ki values in the range of 0.09-38 nM with Ki(α1b)/Ki(α1a) and Ki(α1b)/Ki(α1d) selectivity ratios up to 3607-fold.
SUBSTITUTED {4(4-PHENYL-PIPERAZIN-1YL)-CYCLOHEXYL}-UREA COMPOUNDS
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Page/Page column 31, (2008/06/13)
The present invention relates to substituted [4-(4-phenyl-piperazin-1-yl)-cyclohexyl]-urea compounds of Formula (I) and pharmaceutically acceptable forms thereof, as a1a/a1d adrenoreceptor modulators for the treatment of benign prostatic hypertrophy and l
(Arylpiperazinyl)cyclohexylsufonamides: Discovery of α1a/1d-selective adrenergic receptor antagonists for the treatment of Benign Prostatic Hyperplasia/Lower Urinary Tract Symptoms (BPH/LUTS)
Chiu, George,Li, Shengjian,Connolly, Peter J.,Pulito, Virginia,Liu, Jingchun,Middleton, Steven A.
, p. 3292 - 3297 (2008/02/07)
Benign Prostatic Hyperplasia/Lower Urinary Tract Symptoms (BPH/LUTS) can be effectively treated by α1-adrenergic receptor antagonists. Unfortunately, all currently marketed α1 blockers produced CV related side effects that are caused by the subtype non-selective nature of the drugs. To overcome this problem, it was postulated that a α1a/1d subtype selective antagonist would bring more benefit for the treatment of BPH/LUTS. In developing selective α1a/1d ligands, (arylpiperazinyl)cyclohexylsulfonamides were synthesized and their binding profiles against three cloned human α1-adrenergic receptor subtypes were evaluated. Many compounds show equal affinity for both α1a and α1d subtypes with good selectivity against the α1b subtype. They also overcome the problem of dopamine receptor affinity that previous analogues had exhibited.
Aminocyclohexylsulfonamides: Discovery of metabolically stable α1a/1d-selective adrenergic receptor antagonists for the treatment of benign prostatic hyperplasia/lower urinary tract symptoms (BPH/LUTS)
Chiu, George,Li, Shengjian,Cai, Hong,Connolly, Peter J.,Peng, Sean,Stauber, Kathe,Pulito, Virginia,Liu, Jingchun,Middleton, Steven A.
, p. 6123 - 6128 (2008/03/14)
Benign prostatic hyperplasia/lower urinary tract symptoms (BPH/LUTS) can be effectively treated by α1 adrenergic receptor antagonists, but these drugs also produce side effects that are related to their subtype non-selective nature. To overcome
CYCLOHEXYLDIAMINES AS SELECTIVE ALPHA 1A/1D ADRENORECEPTOR ANTAGONISTS FOR THE TREATMENT OF BENIGN PROSTATE HYPERTROPHY AND LOWER URINARY TRACT SYMPTOMS
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Page/Page column 63-66, (2010/11/30)
The present invention relates to compounds of Formula (I) or a pharmaceutically acceptable form thereof, as dual selective a1a / a 1d adrenoreceptor antagonists for the treatment of benign prostatic hypertrophy and lower urinary tract symptoms. The present invention also relates to pharmaceutical compositions comprising said new compounds, new processes to prepare these new compounds and new uses as a medicine as well as method of treatments.
