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Antiviral properties ketone derivative and its preparation method and application (by machine translation)

The invention relates to the field of medical technology, in particular to has the following chemical structure formula of a new class of antiviral properties ketone derivatives and their pharmaceutically acceptable salts: Pharmacological experiment shows, the invention the derivative or salt, to the KRAS – PDEdelta protein interaction with very strong inhibiting activity, but also has strong in vitro anti-tumor activity. The invention also provides the above-mentioned derivatives and their pharmaceutically acceptable salts, and in the preparation of KRAS – PDEdelta inhibitor and an anti-tumor drug. (by machine translation)

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Reference£º
Piperidine – Wikipedia,
Piperidine | C5H12350N – PubChem

 

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ANILIDE DERIVATIVE, PRODUCTION AND USE THEREOF

This invention is to provide a compound of the formula: STR1 wherein R 1 is an optionally substituted 5-to 6-membered ring: C is a divalent group of the formula: STR2 wherein the ring A is an optionally substituted 5-to 6-membered aromatic ring, X is an optionally substituted C, N or O atom, and the ring B is an optionally substituted 5-to 7-membered ring; Z is a chemical bond or a divalent group; R 2 is (1) an optionally substituted amino group in which a nitrogen atom may form a quaternary ammonium, etc., or a salt thereof, which is useful for antagonizing MCP-1 receptor.

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Reference£º
Piperidine – Wikipedia,
Piperidine | C5H12175N – PubChem

 

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Benzofuran- and benzopyran-carboxamide derivatives

Benzofuran- and benzopyran-carboxamide derivatives of the formula: STR1 wherein l is 1 or 2; X is hydrogen atom, amino group or halogen atom; Y is –S(O)m –R3 wherein R3 is lower alkyl group and m is 0, 1 or 2, or STR2 wherein R4 and R5 are the same or different and are each hydrogen atom or lower alkyl group; R1 is hydrogen atom, lower alkyl group, arylthiomethyl group, halogenomethyl group or STR3 wherein R6 and R7 are the same or different and are each hydrogen atom or lower alkyl group or R6 and R7 together with the adjacent nitrogen atom form a hetrocycle; R2 is hydrogen atom or lower alkyl group; and Z is STR4 wherein p is 2 or 3, R8 and R9 are the same or different and are each lower alkyl group or R8 and R9 together with the adjacent nitrogen atom form a heterocycle, or STR5 wherein q is 0 or 1, n is 1 or 2, R10 is lower alkyl group, lower alkenyl group, lower alkinyl group, aralkyl group or cycloalkyl group and R11 is hydrogen atom or lower alkyl group, their physiologically acceptable salts or their optical isomers, and a method of preparing same. These compounds are useful as psychotropic and antipsychotic agents.

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Reference£º
Piperidine – Wikipedia,
Piperidine | C5H11915N – PubChem

 

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SUBSTITUTED 3,5-DIHYDRO-4H-IMIDAZOL-4-ONES FOR THE TREATMENT OF OBESITY

This invention relates to substituted 3,5-dihydro-4H-imidazol-4-ones compounds which are useful in the treatment of obesity and obesity-related disorders, and as weight-loss and weight-control agents. The invention also provides methods for synthesis of the compounds, pharmaceutical compositions comprising the compounds, and methods of using such compositions for inducing weight loss and treating obesity and obesity-related disorders.

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Reference£º
Piperidine – Wikipedia,
Piperidine | C5H12159N – PubChem

 

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Acetamide Derivatives of Chromen-2-ones as Potent Cholinesterase Inhibitors

Alzheimer’s disease (AD), a neurodegenerative disorder, is a serious medical issue worldwide with drastic social consequences. Inhibition of cholinesterase is one of the rational and effective approaches to retard the symptoms of AD and, hence, consistent efforts are being made to develop efficient anti-cholinesterase agents. In pursuit of this, a series of 19 acetamide derivatives of chromen-2-ones were synthesized and evaluated for their acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory potential. All the synthesized compounds exhibited significant anti-AChE and anti-BChE activity, with IC50 values in the range of 0.24?10.19 muM and 0.64?30.08 muM, respectively, using donepezil hydrochloride as the standard. Out of 19 compounds screened, 3 compounds, viz. 22, 40, and 43, caused 50% inhibition of AChE at 0.24, 0.25, and 0.25 muM, respectively. A kinetic study revealed them to be mixed-type inhibitors, binding with both the CAS and PAS sites of AChE. The above-selected compounds were found to be effective inhibitors of AChE-induced and self-mediated Abeta1?42 aggregation. ADMET predictions demonstrated that these compounds may possess suitable blood?brain barrier (BBB) permeability. Hemolytic assay results revealed that these compounds did not lyse human RBCs up to a thousand times of their IC50 value. MTT assays performed for the shortlisted compounds showed them to be negligibly toxic after 24 h of treatment with the SH-SY5Y neuroblastoma cells. These results provide insights for further optimization of the scaffolds for designing the next generation of compounds as lead cholinesterase inhibitors.

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Reference£º
Piperidine – Wikipedia,
Piperidine | C5H11948N – PubChem

 

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Small molecular CD4 mimics as HIV entry inhibitors

Derivatives of CD4 mimics were designed and synthesized to interact with the conserved residues of the Phe43 cavity in gp120 to investigate their anti-HIV activity, cytotoxicity, and CD4 mimicry effects on conformational changes of gp120. Significant potency gains were made by installation of bulky hydrophobic groups into the piperidine moiety, resulting in discovery of a potent compound with a higher selective index and CD4 mimicry. The current study identified a novel lead compound 11 with significant anti-HIV activity and lower cytotoxicity than those of known CD4 mimics.

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Reference£º
Piperidine – Wikipedia,
Piperidine | C5H11873N – PubChem

 

Discovery of 4-Amino-1-benzylpiperidine

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TRIAZINE DERIVATIVES HAVING INHIBITORY ACTIVITY AGAINST ACETYL-COA CARBOXYLASE

The present invention relates to a novel triazine derivative or a pharmaceutically acceptable salt thereof, and an Acetyl-CoA Carboxylase (ACC) comprising same as an active ingredient. The triazine derivative of the present invention effectively inhibits the activity of ACC and it may be used for preventing or treating obesity, diabetes, dyslipidemia and diseases related to metabolic syndrome.

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Reference£º
Piperidine – Wikipedia,
Piperidine | C5H12274N – PubChem

 

The important role of 4-Amino-1-benzylpiperidine

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Synthesis, pharmacological assessment, and molecular modeling of 6-chloro-pyridonepezils: New dual AChE inhibitors as potential drugs for the treatment of Alzheimer’s disease

6-Chloro-pyridonepezils are chloropyridineedonepezil hybrids designed by combining the N-benzylpiperidine moiety present in donepezil with the 2-chloropyridine-3,5-dicarbonitrile heterocyclic ring system, both connected by an appropriate polymethylene linker. 6-Chloro-pyridonepezils 1-8 were prepared by reaction of 2,6-dichloro-4-phenylpyridine-3,5-dicarbonitrile (13) [or 2,6-dichloropyridine-3,5-dicarbonitrile (14)] with suitable 2-(1- benzylpiperidin-4-yl)alkylamines (9-12). The biological evaluation showed that these new compounds are cholinesterase inhibitors, in the submicromolar range, one of them (6) being a potent hBuChE inhibitor (IC50 = 0.47 ¡À 0.08 muM). 6-Chloro-pyridonepezils 4, 7 and 8 are potent hAChE inhibitors showing IC50 in the 0.013-0.054 muM range. Particularly, 6-chloro-pyridonepezil 8 is 625-fold more selective for hAChE than for hBuChE and compared to donepezil is equipotent for the inhibition of hAChE. Molecular modeling investigation on 6-chloro-pyridonepezils 4, 6-8 supports its dual AChE inhibitory profile, by binding simultaneously at the catalytic active and at peripheral anionic sites of the enzyme. The in vitro Blood Brain Barrier (BBB) and theoretical ADME analysis of 6-chloro-pyridonepezils 1-8 have been carried out. Overall, compound 8, is a permeable potent and selective dual AChEI that can be considered as a good candidate with potential impact for further pharmacological development in Alzheimer’s therapy.

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Reference£º
Piperidine – Wikipedia,
Piperidine | C5H12081N – PubChem

 

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The discovery and SAR of indoline-3-carboxamides – A new series of 5-HT6 antagonists

Antagonists of the 5-HT6 receptor have been shown to improve cognitive function in a wide range of animal models and as such may prove to be attractive agents for the symptomatic treatment of cognitive disorders such as Alzheimer’s disease (AD) and schizophrenia. We report herein the identification and SAR around N-(2-aminoalkyl)-1-(arylsulfonyl)indoline-3-carboxamides – a novel chemotype of 5-HT6 antagonists.

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Reference£º
Piperidine – Wikipedia,
Piperidine | C5H11929N – PubChem

 

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QUINAZOLINE DERIVATIVES AS ANTIVIRAL AGENTS

The present invention relates to the use of quinazoline derivatives of formula (I) wherein A, B, R1, R2, R3 and R4 are defined herein, and pharmaceutically acceptable salts thereof, for the treatment or prevention of infection by hepatitis C virus.

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Reference£º
Piperidine – Wikipedia,
Piperidine | C5H12223N – PubChem