21279-57-2

Usage

Uses

Used in Pharmaceutical Industry:
1-Pyrimidin-2-yl-1,4-diazepane is used as a building block for the synthesis of new drugs, leveraging its unique heterocyclic structure to create novel therapeutic agents. Its potential applications in medicinal chemistry research may lead to the development of drugs with improved efficacy and selectivity.
Used in Medicinal Chemistry Research:
1-Pyrimidin-2-yl-1,4-diazepane serves as a valuable compound in medicinal chemistry research, where it can be studied and modified to explore its potential as a precursor for new drug candidates. Its structural features make it a promising candidate for further investigation and optimization in the quest for innovative therapeutic agents.

InChI:InChI=1/C9H14N4/c1-4-11-9(12-5-1)13-7-2-3-10-6-8-13/h1,4-5,10H,2-3,6-8H2

Upstream product

• 505-66-8 1,4-Diazacycloheptane 
• 1722-12-9 2-chloropyrimidine 
• 1100227-52-8 C₁₄H₂₂N₄O₂ 

Downstream Products

• 1100227-58-4 C₂₄H₃₀F₃N₅O₃ 

Relevant academic research and scientific papers

Synthesis and biological evaluation of homopiperazine derivatives with β-aminoacyl group as dipeptidyl peptidase IV inhibitors

Compounds with homopiperazine skeleton are designed to find a potent DPP-IV inhibitor without inhibiting CYP. Thus a series of β-aminoacyl-containing homopiperazine derivatives was synthesized and evaluated. Compounds with acid moiety were found to be potent inhibitors of DPP-IV without inhibiting CYP 3A4. More specifically, compound 7m showed nanomolar activity with no inhibition towards five subtypes of CYPs, was considered as a prototype for further derivatization. Based on its X-ray co-crystal structure with human DPP-IV, we identified compounds 7s and 7t which showed good in vitro activity, no CYP inhibition, and good selectivity.

METHODS OF TREATING COGNITIVE IMPAIRMENT AND DEMENTIA

This invention relates to methods for treating, managing and preventing cognitive impairment associated with various diseases and disorders, age-associated memory impairment, and dementia.

Multicyclic compounds and methods of their use

This invention relates to multicyclic compounds, pharmaceutical compositions comprising them, and methods of their use in, for example, the treatment of cognitive disorders.

Piperazinylacylpiperidine derivatives, their preparation and therapeutic use thereof

The invention relates to substituted 1-piperazinylacylpiperidine derivatives of general formula (I) in which: n is 1 or 2; p is 1 or 2; R1 represents a halogen atom; a trifluoromethyl radical; a (C1-C4)alkyl; a (C1-C4)alkoxy; a trifluoromethoxy radical; R2 represents a hydrogen atom or a halogen atom; R3 represents a hydrogen atom; a group —OR5; a group —CH2OR5; a group —NR6R7; a group —NR8COR9; a group —NR8CONR10R11; a group —CH2NR12R13; a group —CH2NR8CONR14R15; a (C1-C4)alkoxycarbonyl; a group —CONR16R17; or else R3 constitutes a double bond between the carbon atom to which it is attached and the adjacent carbon atom of the piperidine ring; R4 represents an aromatic group selected from: the said aromatic groups being unsubstituted or being mono- or disubstituted by a substituent selected independently from a halogen atom; a (C1-C4)alkyl; a (C1-C4)alkoxy; a trifluoromethyl radical; Preparation process and therapeutic application.

Trifluoromethylquinolinecarboxylic acid derivative

This invention relates to a 8-trifluoromethylquinolinecaboxylic acid derivative represented by the following formula (I): (wherein R1 represents a lower alkyl group, a halogeno-lower alkyl group or a cycloalkyl group, R2 represents a phenyl group which may be substituted by R0, a 5-membered or 6-membered aromatic heteromonocyclic ring group containing 1 or 2 hetero atoms selected from N, O and S, which may be substituted by R0, or an aromatic heterocyclic fused ring group in which the said aromatic heteromonocyclic ring group and a benzene ring are fused, R0 represents a group selected from a halogen, a lower alkyl, a fluorine-substituted lower alkyl, a lower alkoxy or a lower alkylthio, R3 represents hydrogen or a lower alkyl group, and m represents an integer of 2 or 3.) or a pharmaceutically acceptable salt thereof or an ester thereof.

REMEDIES OR PREVENTIVES FOR AIDS

The present invention is to provide the combined use of one kind or two or more kinds of a quinolone carboxylic acid having anti-HIV activity and one kind or two or more kinds of a reverse transcriptase inhibitor or HIV protease inhibitor, and an AIDS therapeutic agent or preventive agent containing as its active ingredients one kind or two or more kinds of a quinolone carboxylic acid having anti-HIV activity and one kind or two or more kinds of a reverse transcriptase inhibitor or HIV protease inhibitor.

Synthesis and anxiolytic activity of N-substituted cyclic imides (1R*,2S*3R*,4S*)-N-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-2,3-b icyclo[2.2.1]heptanedicarboxime (Tandospirone) and related compounds

A series of cyclic imides bearing a ω-(4-aryl and 4-heteroaryl-1-piperazinyl)alkyl moieties was synthesized and tested in vivo for anxiolytic activity. The in vitro binding affinities of these compounds were also examined for 5-HT(1A) receptor sites. Structure-activity relationships within these series are discussed. One of these compounds, (1R*,2S*,3R*,4S*)-N-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-2,3- bicyclo[2.2.1]heptanedicarboximide (1: tandospirone), was found to be equipotent with buspirone in its anxiolytic activity and more anxio-selective than buspirone and diazepam. Tandospirone (1) is currently undergoing clinical evaluation as a selective anxiolytic agent.