54013-91-1

Upstream product

• 110-85-0 piperazine 
• 701-07-5 1-bromo-2-isopropoxybenzene 
• 119695-87-3 fumarate salt of 4-(2-isopropyloxyphenyl)piperazine 
• 29026-74-2 2-isopropoxy-phenylamine 

Downstream Products

• 155106-81-3 1-(3-Chloromethyl-benzyl)-4-(2-isopropoxy-phenyl)-piperazine 
• 134208-17-6 1-[3-[[4-[2-(1-methylethoxy)phenyl]-1-piperazinyl]methyl]benzoyl]piperidine 
• 748746-20-5 1-(4-Chloromethyl-benzyl)-4-(2-isopropoxy-phenyl)-piperazine 
• 157531-35-6 1-<(4-bromo-2-thienyl)methyl>-4-<2-(1-methylethoxy)phenyl>piperazine 
• 171855-36-0 6-<<1-<2-(1-methylethoxy)phenyl>-4-piperazinyl>methyl>-2-(chloromethyl)pyridine 
• 171855-38-2 1-allyl-4-(2-isopropoxy-phenyl)-piperazine 
• 171855-30-4 1-(2-Isopropoxy-phenyl)-4-prop-2-ynyl-piperazine 
• 148888-29-3 1-(4-Bromo-phenyl)-4-[4-(2-isopropoxy-phenyl)-piperazin-1-yl]-butan-1-one 
• 216252-67-4 1-(2-phthalimidoethyl)-4-(2-isopropyloxyphenyl)piperazine 
• 223253-61-0 1-[4-(2-isopropoxy-phenyl)-piperazin-1-yl]-propan-2-one 
• 223253-64-3 2-[4-(2-isopropoxy-phenyl)-piperazin-1-yl]-ethanol 
• 478811-75-5 1-(5-bromo-thiophen-2-ylmethyl)-4-(2-isopropoxy-phenyl)-piperazine 
• 223254-21-5 1-[4-(tert-butyl-diphenyl-silanyloxymethyl)-thiophen-2-ylmethyl]-4-(2-isopropoxy-phenyl)-piperazine 

Relevant academic research and scientific papers

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

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.

Synthesis and Structure-Activity Relationships of Novel Arylpiperazines as Potent and Selective Agonists of the Melanocortin Subtype-4 Receptor

The melanocortin receptors have been implicated as potential targets for a number of important therapeutic indications, including inflammation, sexual dysfunction, and obesity. We identified compound 1, an arylpiperazine attached to the dipeptide H-D-Tic-D-p-Cl-Phe-OH, as a novel melanocortin subtype-4 receptor (MC4R) agonist through iterative directed screening of nonpeptidyl G-protein-coupled receptor biased libraries. Structure-activity relationship (SAR) studies demonstrated that substitutions at the ortho position of the aryl ring improved binding and functional potency. For example, the o-isopropyl-substituted compound 29 (Ki = 720 nM) possessed 9-fold better binding affinity compared to the unsubstituted aryl ring (Ki = 6600 nM). Sulfonamide 39 (Ki = 220 nM) fills this space with a polar substituent, resulting in a further 2-fold improvement in binding affinity. The most potent compounds such as the diethylamine 44 (Ki = 60 nM) contain a basic group at this position. Basic heterocycles such as the imidazole 50 (Ki = 110 nM) were similarly effective. We also demonstrated good oral bioavailability for sulfonamide 39.

Acetamides and benzamides that are useful in treating sexual dysfunction

The present invention relates to the use of compounds of formula (I) for the treatment of sexual dysfunction and to compositions containing compounds of formula (I) for the treatment of sexual dysfunction.

Heterocycles useful in the treatment of benign prostatic hyperplasia

This invention relates a to a series of heterocyclic substituted piperazines of Formula I pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention selectively inhibit binding to the α-1a adrenergic receptor, a receptor which has been implicated in benign prostatic hyperplasia. As such the compounds are potentially useful in the treatment of this disease.