803736-69-8

Upstream product

• 912482-18-9 (E)-N'-(ethoxymethylene)hydrazinecarboxylic acid methyl ester 
• 50541-93-0 4-amino-1-benzylpiperidine 
• 864933-14-2 methyl 2-[(dimethylamino)methylene]hydrazinecarboxylate 
• 73889-19-7 tert-butyl (1-benzylpiperidin-4-yl)carbamate 
• 100-44-7 benzyl chloride 
• 73874-95-0 (piperidin-4-yl)carbamic acid tert-butyl ester 
• 873947-74-1 methyl 2-(ethoxymethylene)hydrazinecarboxylate 
• 803736-68-7 2-formyl-N-[1-(phenylmethyl)-4-piperidinyl]-hydrazinecarboxamide 

Relevant academic research and scientific papers

Efficient one-pot formation of 4-N-substituted 2,4-dihydro-3H-1,2,4-triazolin-3-ones from primary amines using N′-(ethoxymethylene)hydrazinecarboxylic acid methyl ester

(E)-N′-(Ethoxymethylene)hydrazinecarboxylic acid methyl ester was synthesized in one step in good yield. This reagent was successfully applied to the one-pot synthesis of 4-substituted 2,4-dihydro-3H-1,2,4-triazolin-3-ones from readily available primary alkyl and aryl amines. This reaction process is relatively mild and easy to carry out. It is especially useful for the formation of sterically hindered triazolinones, which are otherwise difficult to obtain via existing literature procedures. A possible mechanistic pathway for the transformation is outlined.

Synthesis and studies on anticonvulsant and antibacterial activities of 1-Alkyl-4-(4H-1,2,4-triazol-4-yl)piperidine derivatives

Two series of 1-Alkyl-4-(4H-1,2,4-triazol-4-yl)piperidines and 1-Alkyl-4-(2H-1,2,4-triazol-3-one-4-yl) piperidines were synthesized and their anticonvulsant and antibacterial activities were evaluated. Pharmacological tests showed that three of the synthesized compounds (6c, 6k, 7m) displayed 100% protection at a dose of 100 mg/kg. 4-(1-Octylpiperidin-4-yl)-2,4-dihydro-3H-1,2,4-triazol-3-one (6c) was the most active compound in this study, with an ED50 of 65.4 mg/kg and a TD50 value of 241.2 mg/kg, resulting in a PI of 3.6. Four of the synthesized compounds showed potent inhibitory activity against gram positive bacteria staphylococcus aureus (RN4220, KCTC 209 and KCTC 503), especially against the strains of multidrug-resistant clinical isolates (MRSA3167/3506 and QRSA3505/3519). Among which compound 1-tetradeyl-4-(4H-1,2,4-triazol-4-yl)piperidine (7f) showed the most potent levels of activity (MIC = 2 ug/mL) against the gram-positive strains.

PIPERIDINYL CYCLIC AMIDO ANTIVIRAL AGENTS

Provided are compounds of Formula (I) and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and their use for treating viral infections mediated by a member of the Flaviviridae family of viruses such as hepatitis C virus (HCV).

TRIAZOLONE, TETRAZOLONE AND IMIDAZOLONE DERIVATIVES FOR USE AS ALPHA-2C ADRENORECEPTOR ANTAGONISTS

The present invention concerns substituted triazolone, tetrazolone and imidazolone derivatives according to the general Formula (I) a pharmaceutically acceptable acid or base addition salt thereof, a stereochemically isomeric form thereof, an N-oxide form thereof or a quaternary ammonium salt thereof, wherein the variables are defined in Claim 1, having selective α2C-adrenoceptor antagonist activity. It further relates to their preparation, compositions comprising them and their use as a medicine. The compounds according to the invention are usefull for the prevention and/or treatment of central nervous system disorders, mood disorders, anxi- ety disorders, stress-related disorders associated with depression and/or anxiety, cognitive disorders, personality disorders, schizoaffective disorders, Parkinson's disease, dementia of the Alzheimer's type, chronic pain conditions, neurodegenerative diseases, addiction disorders, mood disorders and sexual dysfunction.

QUINOLINE DERIVATES AND THEIR USE IN THERAPY

The invention provides compounds of formula (I) wherein n, p, q, X, R1, R2, R3, R4, R5 and R6 are as defined in the specification; processes for their preparation, pharmaceutical compositio

NEW P2X7 RECEPTOR ANTAGONISTS AND THEIR USE

The invention provides compounds of formula (IA), processes for their preparation, pharmaceutical compositions containing them, and their use in therapy. [Chemical formula should be inserted here. Please see paper copy] (IA)