178671-99-3

Upstream product

• 821-48-7 bis-(2-chloroethyl)amine hydrochloride 
• 57946-60-8 2-(2',2',2'-trifluoroethoxy)aniline 
• 88-75-5 2-hydroxynitrobenzene 
• 87014-28-6 1-(2,2,2-trifluoroethoxy)-2-nitrobenzene 

Downstream Products

• 186387-84-8 3-benzyloxy-2,2-dimethyl-1-{4-[2-(2,2,2-trifluoroethoxy)phenyl]piperazin-1-yl}-1-propanone 
• 886206-13-9 C₂₃H₃₄F₃N₃O₃ 
• 335087-78-0 2-phenyl-8-<2-{4-[2-(2,2,2-trifluoroethoxy)-phenyl]-1-piperazinyl}-ethylcarbamoyl>-3-methyl-4-oxo-4H-1-benzopyran 
• 335087-42-8 8-<3-{4-[2-(2,2,2-trifluoroethoxy)-phenyl]-1-piperazinyl}propylcarbamoyl>-3-methyl-4-oxo-2-phenyl-4H-1-benzopyran 
• 334930-12-0 1-[2-(2,2,2-trifluoroethoxy)-phenyl]-4-[3-(N-phthalimido)-propyl]-piperazine 
• 1025909-31-2 8-Chloro-4-(3-{4-[2-(2,2,2-trifluoro-ethoxy)-phenyl]-piperazin-1-yl}-propylamino)-quinoline-3-carboxylic acid 
• 334930-13-1 1-(3-Aminopropyl)-4-[2-(2,2,2-trifluoroethoxy)-phenyl]-piperazine 
• 186386-09-4 1-benzyl-3-(3-{4-[2-(2,2,2-trifluoroethoxy)phenyl]piperazin-1-yl}-2,2-dimethylpropyl)-5-methyl-2,4(1H,3H)-pyrimidinedione 
• 592527-80-5 toluene-4-sulfonic acid 2,2-dimethyl-3-{4-[2-(2,2,2-trifluoro-ethoxy)-phenyl]-piperazin-1-yl}-propyl ester 
• 186387-85-9 3-benzyloxy-2,2-dimethyl-1-{4-[2-(2,2,2-trifluoroethoxy)phenyl]piperazin-1-yl}propane 
• 186387-86-0 2,2-dimethyl-3-{4-[2-(2,2,2-trifluoroethoxy)phenyl]piperazin-1-yl}-1-propanol 
• 186385-55-7 1-benzyl-5-methyl-3-(1-{4-[2-(2,2,2-trifluoro-ethoxy)-phenyl]-piperazin-1-ylmethyl}-cyclopropylmethyl)-1H-pyrimidine-2,4-dione 

Relevant academic research and scientific papers

NOVEL AMINO- AND IMINO-ALKYLPIPERAZINES

Described are novel amino- and iminoalkyl piperazines having affinity for serotonergic receptors and pharmacological compositions thereof. These compounds and their isomers, including optical isomers, enantiomers, diastereomers, N-oxides, polymorphs, hydr

N-Arylpiperazinyl-N'-propylamino derivatives of heteroaryl amides as functional uroselective α1-adrenoceptor antagonists

Novel arylpiperazines were identified as α1-adrenoceptor (AR) subtype- selective antagonists by functional in vitro screening. 3-[4-(ortho- Substituted phenyl)piperazin-1:yl]propylamines were derivatized with N,N- dimethyl anthranilamides, nicotinamides, as well as carboxamides of quinoline, 1,8-naphthyridine, pyrazolo[3,4-b]pyridine, isoxazolo[3,4- b]pyridine, imidazo[4,5-b]pyridine, and pyrazolo[1,5-a]pyrimidines. Strips of rabbit bladder neck were employed as a predictive assay for antagonism in the human lower tract. Rings of rat aorta were used as a 'negative screen' for the test antagonists. Binding to α1-ARs was relatively sensitive to size and electronic features of the arylpiperazine portion of the antagonists and permissive to these features on the heteroaryl carboxamide side. These structure-affinity findings were exploited to produce nicotinamides (e.g. 13ii and 25x) and pyrazolo[3,4-b]pyridines (e.g. 37f and 37y) ligands with nanomolar affinity at the α1-AR subtype prevalent in the human lower urinary tract (pA2 values: 8.8, 10.7, 9.3, and 9.9, respectively) and displaying 2-3 orders of magnitude selectivity over the α(1D)-AR.

[3-(4-phenylpiperazin-1-yl)propyl-amino, thio and oxy]-pyridine, pyrimidine and benzene derivatives as α1 -adrenoceptor antagonists

The present invention relates to novel α 1 -adrenoceptor antagonists of Formula I: STR1 in which: p is 0 or 1;t is 0, 1 or 2;X is O, S or NR 6 (in which R 6 is hydro or (C 1-6)alkyl);Y and Z are independently CH or N;R 1 is hydro, hydroxy, halo, nitro, amino, cyano, (C 1-4)alkylthio, acetylamino, trifluoroacetylamino, methylsulfonylamino, (C 1-6)alkyl, (C 3-6)cycloalkyl, (C 3-6)cycloalkyl (C 1-4)alkyl, oxazol-2-yl, aryl, heteroaryl, aryl (C 1-4)alkyl, heteroaryl (C 1-4)alkyl, (C 1-6)alkyloxy, (C 3-6)cycloalkyloxy, (C 3-6)cycloalkyl (C 1-4)alkyloxy, 2-propynyloxy, aryloxy, heteroaryloxy, aryl (C 1-4)alkyloxy or heteroaryl (C 1-4)alkyloxy (wherein alkyl is optionally substituted with one to three halo atoms and aryl or heteroaryl is optionally substituted with one to two substituents independently selected from halo and cyano);R 2 is hydro, hydroxy, halo, cyano, (C 1-6)alkyl or (C 1-6)alkyloxy (wherein alkyl is optionally substituted with one to three halo atoms);R 3 is -C (O)R 7 (wherein R 7 is (C 1-6)alkyl, (C 3-6)cycloalkyl, di(C 1-4)alkylamino, N-(C 1-4)alkyl-N-(C 1-4)alkyloxyamino, (C 1-4)alkyl((C 1-4)alkyloxy)amino, pyrrolidin-1-yl, piperidin-1-yl, morpholin-4-yl or piperazin-1-yl);R 4 is halo, hydroxy, cyano, (C 1-6)alkyl or (C 1-6)alkyloxy; andR 5 is (C 1-6)alkyl; and the pharmaceutically acceptable salts and N-oxides thereof.