60407-35-4

Usage

Chemical Properties

White powder

InChI:InChI=1/C12H18N2.2ClH/c13-12-7-4-8-14(10-12)9-11-5-2-1-3-6-11;;/h1-3,5-6,12H,4,7-10,13H2;2*1H

Upstream product

• 72551-53-2 ethyl 1-benzylpiperidine-3-carboxylate 
• 14813-01-5 1-benzyl-3-hydroxypiperidine 
• 60169-69-9 3-azido-1-benzylpiperidine 
• 71962-74-8 Ethyl nipecotate 
• 100-39-0 benzyl bromide 
• 478828-62-5 (1-benzylpiperidin-3-yl)carbamic acid tert-butyl ester 
• 100-44-7 benzyl chloride 
• 184637-48-7 t-butyl piperidin-3-ylcarbamate 
• 60169-74-6 3-(N-acetamino)-1-benzylpiperidine 
• 5810-55-9 N-(piperidin3-yl)acetamide 
• 182919-58-0 (±)-1-benzylpiperidine-3-carbohydrazide 

Downstream Products

• 141762-05-2 6-Chloro-4-methyl-3-oxo-3,4-dihydro-2H-benzo[1,4]oxazine-8-carboxylic acid (1-benzyl-piperidin-3-yl)-amide 
• 84332-21-8 2-Amino-4-methoxy-pyrimidine-5-carboxylic acid (1-benzyl-piperidin-3-yl)-amide 
• 115661-47-7 (1-benzyl-piperidin-3-yl)-phenyl-amine 
• 478828-62-5 (1-benzylpiperidin-3-yl)carbamic acid tert-butyl ester 
• 61694-72-2 N-(1-benzyl-3-piperidinyl)-4-amino-5-chloro-2-methoxybenzamide 
• 61609-33-4 2-hydroxy-N-(1-methylpiperidin-3-yl)-2,2-diphenylacetamide 

Relevant academic research and scientific papers

Novel 1,5-diaryl pyrazole-3-carboxamides as selective COX-2/sEH inhibitors with analgesic, anti-inflammatory, and lower cardiotoxicity effects

COX-2 selective drugs have been withdrawn from the market due to cardiovascular side effects, just a few years after their discovery. As a result, a new series of 1,5-diaryl pyrazole carboxamides 19–31 was synthesized as selective COX-2/sEH inhibitors wit

Synthesis, biological evaluation, docking study and ulcerogenicity profiling of some novel quinoline-2-carboxamides as dual COXs/LOX inhibitors endowed with anti-inflammatory activity

A series of novel quinoline-2-carboxamides 15–28 was synthesized and evaluated in?vitro as dual COXs/LOX inhibitors. Compounds 19 and 27 exhibited the highest potency and selectivity for COX-2 inhibitory activity (IC50?=?1.21 and 1.13?μM, respe

Design, synthesis and biological evaluation of new phthalimide and saccharin derivatives with alicyclic amines targeting cholinesterases, beta-secretase and amyloid beta aggregation

The complexity of Alzheimer's disease (AD) calls for search of multifunctional compounds as potential candidates for effective therapy. A series of phthalimide and saccharin derivatives linked by different alicyclic fragments (piperazine, hexahydropyrimidine, 3-aminopyrrolidine or 3-aminopiperidine) with phenylalkyl moieties attached have been designed, synthesized, and evaluated as multifunctional anti-AD agents with cholinesterase, β-secretase and β-amyloid inhibitory activities. In?vitro studies showed that the majority of saccharin derivatives with piperazine moiety and one phthalimide derivative with 3-aminopiperidine fragment exhibited inhibitory potency toward acetylcholinesterase (AChE) with EeAChE IC50values ranging from 0.83?μM to 19.18?μM. The target compounds displayed inhibition of human β-secretase-1 (hBACE1) ranging from 26.71% to 61.42% at 50?μM concentration. Among these compounds, two multifunctional agents (26, [2-(2-(4-benzylpiperazin-1-yl)ethyl)benzo[d]isothiazol-3(2H)-one 1,1-dioxide] and 52, 2-(2-(3-(3,5-difluorobenzylamino)piperidin-1-yl)ethyl)isoindoline-1,3-dione) have been identified. Compound 26 exhibited the highest inhibitory potency against EeAChE (IC50?=?0.83?μM) and inhibitory activity against hBACE1 (33.61% at 50?μM). Compound 52 is a selective AChE inhibitor (IC50 AChE?=?6.47?μM) with BACE1 inhibitory activity (26.3% at 50?μM) and it displays the most significant Aβ anti-aggregating properties among all the obtained compounds (39% at 10?μM). Kinetic and molecular modeling studies indicate that 26 may act as non-competitive AChE inhibitor able to interact with both catalytic and peripheral active site of the enzyme.

NOVEL COMPOUNDS AS ANTI-TUBERCULAR AGENTS

The present invention relates to novel compounds of formula (1): The present invention also discloses compounds of formula (1) along with other pharmaceutical acceptable excipients and use of the compounds as anti-tubercular agents.

NOVEL COMPOUND HAVING ANGIOGENESIS INHIBITORY ACTIVITY, METHOD FOR PREPARING SAME, AND PHARMACEUTICAL COMPOSITION COMPRISING SAME

Disclosed are an anti-angiogenic compound, represented by Chemical Formula I, or a pharmaceutically acceptable salt thereof, a preparation method thereof, and a pharmaceutically acceptable composition including the same. Because the compound of Chemical Formular I potently suppresses the angiogenesis, the compound of Chemical Formula I is applicable to the prevention and treatment of diseases caused by aberrant activity of vascular endothelial growth factor, and available as an anti-angiogenic agent.

Novel Compound Having Angiogenesis Inhibitory Activity, Method for Preparing Same, and Pharmaceutical Composition Comprising Same

Disclosed are an anti-angiogenic compound, represented by Chemical Formula I, or a pharmaceutically acceptable salt thereof, a preparation method thereof, and a pharmaceutically acceptable composition including the same. Because the compound of Chemical Formula I potently suppresses the angiogenesis, the compound of Chemical Formula I is applicable to the prevention and treatment of diseases caused by aberrant activity of vascular endothelial growth factor, and available as an anti-angiogenic agent.

A convenient route to 1-benzyl 3-aminopyrrolidine and 3-aminopiperidine

1-Benzyl 3-aminopyrrolidine 1 and 1-benzyl 3-aminopiperidine 2 were prepared rapidly mainly in aqueous conditions in 55 and 75% yields, respectively, on a multi-gram scale starting from inexpensive and commercially available starting materials. The key step involved the Curtius rearrangement mediated by sodium nitrite and trifluoroacetic acid of the appropriate acylhydrazides. All the reactions (except LAH reductions) were performed in water.

N-(AMIDINOPHENYL) CYCLOUREA ANALOGS AS FACTOR XA INHIBITORS

The present application describes N-(amidinophenyl)cyclourea analogs of formula I: STR1 which are useful as inhibitors of factor Xa.

Dibenzo-epines: Effect of the basic side-chain on neuroleptic activity

Structure-activity relationships in a series of dibenzo[b,f][1,4]thiazepines and -oxazepines and dibenzo[b,e][1,4]diazepines having different basic substituents in the 11-position were studied with reference to their neuroleptic activity. A high degree of structure-specificity was found for the piperazinyl moiety as well as for the distances between the distal nitrogen atom of this group and the tricyclic ring system, which distances are probably of importance for receptor binding. It was shown that the N-oxides of the neuroleptic agents clotiapine, loxapine and clozapine were inactive in in vitro binding tests involving central dopaminergic receptors, and it is very likely therefore that the in vivo activity of these N-oxides in the rat is due to their enzymatic reduction to the active parent compounds. All derivatives having a basic side-chain other than N-alkylpiperazinyl were inactive neuroleptically, with the exception of the N-methyl-4-piperidyl derivative which showed relatively weak effects.