870249-31-3

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Relevant academic research and scientific papers

1-Arylpiperazinyl-4-cyclohexylamine derived isoindole-1,3-diones as potent and selective α-1a/1d adrenergic receptor ligands

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.

(Phenylpiperazinyl)cyclohexylureas: Discovery of α1a/1d-selective adrenergic receptor antagonists for the treatment of benign prostatic hyperplasia/lower urinary tract symptoms (BPH/LUTS)

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 {4(4-PHENYL-PIPERAZIN-1YL)-CYCLOHEXYL}-UREA COMPOUNDS

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

SUBSTITUTED ISOINDOLE-1,3-DIONES

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

(Arylpiperazinyl)cyclohexylsufonamides: Discovery of α1a/1d-selective adrenergic receptor antagonists for the treatment of Benign Prostatic Hyperplasia/Lower Urinary Tract Symptoms (BPH/LUTS)

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)

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

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.

ADRENERGIC RECEPTOR ANTAGONISTS

This invention relates to α1a and/or α1d adrenergic receptor antagonists. Compounds disclosed herein can function as α1a and/or α1d adrenergic receptor antagonist and can be used for the treatment of diseases or disorder mediated through α1a and/or α1d adrenergic receptors. Compounds disclosed herein can be used for the treatment of benign prostatic hyperplasia and the related symptoms thereof. Compounds disclosed herein can be used for the treatment of lower urinary tract symptoms associated with or without benign prostatic hyperplasia. Processes for the preparation of compounds disclosed herein, pharmaceutical compositions containing the compounds disclosed herein, and methods of treating benign prostatic hyperplasia or related symptoms thereof are also provided. Formula (I) Its pharmaceutically acceptable acid addition salts,pharmaceutically acceptable solvates, enantiomers, diastereomers, N-oxides, polymorphs or metabolites,wherein; A represents a Formula (F.a or ,F.b or F.c wherein) N represents 1 or 2; Y represents cycloalkyl (C5-C7) group; optionally substituted with halogen atom(s) or lower alkyl (C1-C4) group; and R is selected from optionally substituted non_aromatic or aromatic monocyclic or bicyclic ring system having 0 to 4 heteroatom(s),the substituent(s) may be selected from the group consisting of halogen, lower alkyl (C1-C4),halogenated lower alkyl (C1-c4),cyano, hydroxy, lower alkoxy (C1-C4),cycloalkoxy (C3-C6),amino,lower alkylamino (C1-C4) and lower alkylamino (C1-C4) carbonyl group.