63377-88-8

Upstream product

• 107-04-0 1-Bromo-2-chloroethane 
• 6640-24-0 N-(m-chlorophenyl)piperazine 
• 13078-15-4 1-(3-chlorophenyl)piperazine hydrochloride 

Downstream Products

• 1092766-48-7 2-{2-[2-(3-methoxyphenyl)ethyl]phenoxy}ethyl-4-(3'-chlorophenyl)piperazine 
• 1334582-07-8 C₂₀H₂₂ClN₅ 
• 1334582-17-0 C₂₀H₂₂ClN₅ 

Relevant academic research and scientific papers

Benzo-aza-alkyl aryl piperazine derivative and applications in preparation of drugs

The invention discloses a benzo-aza-alkyl aryl piperazine derivative and applications in preparation of drugs. The derivative shows the effect on central nervous systems, especially on the double highaffinity activity of a 5-HT acceptor and a Sigma-1 acceptor. Various physiological and pharmacological effects are brought into play in the body; and the compound can be used as a pharmaceuticalactive substance, especially used for anti-depression, anti-anxiety, anti-bipolar affective disorder and anti-neuropathic pain, and can also be used as an intermediate to prepare other pharmaceuticalactive compounds. The compound is fast in effect and small in toxic and side effect, and can meet demands of clinical applications; and the compound is a compound or a free base or salt thereof havingthe following structural formula (IV). The structure of the compound or the free base or salt thereof is shown as the structural formula (IV).

Design, synthesis, and biological evaluation of arylpiperazine-benzylpiperidines with dual serotonin and norepinephrine reuptake inhibitory activities

The limitations of established serotonin (5-hydroxytryptamine, 5-HT) and norepinephrine (NE) reuptake inhibitors necessitate the development of safer and more effective therapeutic agents. Based on the structures of 4-benzylpiperidine carboxamides and trazodone, arylpiperazine-benzylpiperidines with chemical scaffolds different from those of marketed drugs were designed, synthesized, and evaluated for their neurotransmitter reuptake inhibitory activities. The majority of the synthesized compounds showed greater NE than 5-HT reuptake inhibition. The activities were even greater than those of the standard drug, venlafaxine hydrochloride were. The derivatives with a three-carbon linker showed better activities than the derivatives with a two-carbon linker. Among the newly synthesized compounds, 2d exhibited the strongest reuptake inhibition of the neurotransmitters (IC50 = 0.38 μM for NE and 1.18 μM for 5-HT). The biological activity data demonstrate that arylpiperazine-benzylpiperidines have the potential to be developed as a new class of therapeutic agents to treat neuropsychiatric and neurodegenerative disorders.

TREATMENT OF ORGANOPHOSPHATE EXPOSURE WITH TETRAHYDROINDOLONE ARYLPIPERAZINE COMPOUNDS

A method of treating exposure to organophosphate agents through the use of compounds comprising tetrahydroindolone and arylpiperazine moieties.

Composition and method for treating emesis

Methods for treating emesis using compositions comprising a bicyclic ring moiety covalently linked to a substituted arylpiperazine moiety are disclosed.

Tetrahydroindolone and purine derivatives linked to arylpiperazines

Pharmaceutical composite compositions comprising tetrahydroindolones linked to arylpiperazines and derivatives thereof are disclosed. Specifically, composite compositions useful in treating anti-psychotic disorders are disclosed. The composite compositions disclosed herein can effectively ameliorate symptoms and treat psychotic disorders without causing a decrease in cognitive function. Generally, the composite compounds consist of two moieties, moiety A and B in which a tetrahydroindolone comprises a moiety A linked through a linker L to a moiety B, where B is an arylpiperazinyl moiety. The composite compound provides anti-psychotic actively by interaction with GABA, seratoninne and dopamine receptors. The composite molecules with the combined activities will provide treat psychiatric and neurological diseases without cognitive impairment.

TETRAHYDROINDOLONE AND PURINE DERIVATIVES LINKED TO ARYLPIPERAZINES

Pharmaceutical composite compositions comprising tetrahydroindolones linked to arylpiperazines and derivatives thereof are disclosed. Specifically, composite compositions useful in treating anti-psychotic disorders are disclosed. The composite compositions disclosed herein can effectively ameliorate symptoms and treat psychotic disorders without causing a decrease in cognitive function. Generally, the composite compounds consist of two moieties, moiety A and B in which a tetrahydroindolone comprises a moiety A linked through a linker L to a moiety B, where B is an arylpiperazinyl moiety. The composite compound provides anti-psychotic actively by interaction with GABA, seratoninne and dopamine receptors. The composite molecules with the combined activities will provide treat psychiatric and neurological diseases without cognitive impairment.

Synthesis of new 1,2,3-benzotriazin-4-one-arylpiperazine derivatives as 5-HT(1A) serotonin receptor ligands

A series of novel 1,2,3-benzotriazin-4-one derivatives was prepared and evaluated as ligands for 5-HT receptors. Radioligand binding assays proved that the majority of the novel compounds behaved as good to excellent ligands at the 5-HT(1A) receptor, some of which were selective with respect 5-HT(2A) and 5-HT(2C) receptors. Six analogues (1a, 2a, 2b, 2c, 2e and 2i) were selected and further evaluated for their binding affinities on D1, D2 dopaminergic and α1-, α2-adrenergic receptors. A o-OCH3 derivative (2e) bound at 5-HT(1A) sites with subnanomolar affinity (IC50=0.059 nM) and shows high selectivity over all considered receptors and may offer a new lead for the development of therapeutically efficacious agents. Copyright (C) 2000 Elsevier Science Ltd.

Synthesis and biological activity of benzotriazole derivatives structurally related to trazodone

This paper outlines the synthesis and the pharmacological screening of a series of novel 1- and 2-ethyl>benzotriazoles and 1-propoxy>benzotriazoles, which are structurally related to trazodone.Antiserotonergic, antiadrenergic and antihistaminic in vitro activity and in vivo analgesic action are described.Some of the investigated compounds show overall pharmacological profiles similar to that of the antidepressant trazodone. benzotriazole / antiserotonergic activity / antiadrenergic activity / antihistaminic activity / analgesic activity