131770-85-9

Upstream product

• 2746-25-0 p-Methoxybenzyl bromide 
• 824-94-2 p-methoxybenzyl chloride 
• 554-84-7 meta-nitrophenol 

Downstream Products

• 1442656-75-8 C₁₆H₁₅N₃O₃ 
• 1228102-80-4 6-(5-(1,3-dioxolane-2-yl)thiophen-2-yl)-N-(3-(4-methoxybenzyloxy)phenyl)thieno[3,2-d]pyrimidin-4-amine 
• 1228102-81-5 5-(4-(3-(4-methoxybenzyloxy)phenylamino)thieno[3,2-d]pyrimidin-6-yl)thiophene-2-carboxaldehyde 
• 1228102-90-6 4-(7-(3-(4-methoxybenzyloxy)phenylamino)thieno[3,2-b]pyridin-2-yl)benzaldehyde 
• 1228102-91-7 3-(7-(3-(4-methoxybenzyloxy)phenylamino)thieno[3,2-b]pyridin-2-yl)benzaldehyde 
• 1228103-15-8 N-(3-(4-methoxybenzyloxy)phenyl)-6-(5-(pyrrolidin-1-ylmethyl)thiophen-2-yl)thieno[3,2-d]pyrimidin-4-amine 
• 1228103-34-1 N-(3-(4-methoxybenzyloxy)phenyl)-2-(4-(piperidin-1-ylmethyl)phenyl)thieno[3,2-b]pyridin-7-amine 
• 1228102-50-8 3-(2-(4-(piperidin-1-ylmethyl)phenyl)thieno[3,2-b]pyridin-7-ylamino)phenol trifluoroacetic acid 
• 1228103-41-0 N-(3-(4-methoxybenzyloxy)phenyl)-2-(3-(piperidin-1-ylmethyl)phenyl)thieno[3,2-b]pyridin-7-amine 
• 1228103-53-4 N-(3-(4-methoxybenzyloxy)phenyl)-2-(4-methylpiperazin-1-yl)thiazolo[4,5-d]pyrimidin-7-amine 
• 1228102-66-6 3-(2-(4-methylpiperazin-1-yl)thiazolo[4,5-d]pyrimidin-7-ylamino)phenol trifluoroacetic acid 
• 1228102-79-1 3-(4-(3-(4-methoxybenzyloxy)phenylamino)thieno[3,2-d]pyrimidin-6-yl)benzaldehyde 
• 1228102-89-3 2-bromo-N-(3-(4-methoxybenzyloxy)phenyl)thieno[3,2-b]pyridin-7-amine 
• 1228102-97-3 N-(3-(4-methoxybenzyloxy)phenyl)-2-(methylthio)thiazolo[4,5-d]pyrimidin-7-amine 

Relevant academic research and scientific papers

Synthesis and biological evaluation of direct thrombin inhibitors bearing 4-(piperidin-1-yl)pyridine at the P1 position with potent anticoagulant activity

The design and synthesis of a new class of nonpeptide direct thrombin inhibitors, built on the structure of 1-(pyridin-4-yl)piperidine-4-carboxamide, are described. Starting from a strongly basic 1-amidinopiperidine derivative (6) showing poor thrombin (fIIa) and factor Xa (fXa) inhibition activities, anti-fIIa activity and artificial membrane permeability were considerably improved by optimizing the basic P1 and the X-substituted phenyl P4 binding moieties. Structure-activity relationship studies, usefully complemented with molecular modeling results, led us to identify compound 13b, which showed excellent fIIa inhibition (Ki = 6 nM), weak anti-Xa activity (K i = 5.64 μM), and remarkable selectivity over other serine proteases (e.g., trypsin). Compound 13b showed in vitro anticoagulant activity in the low micromolar range and significant membrane permeability. In mice (ex vivo), 13b demonstrated anticoagulant effects at 2 h after oral dosing (100 mg·kg-1), with a significant 43% prolongation of the activated partial thromboplastin time (aPTT), over controls (P 0.05).

ANTI-INFLAMMATORY COMPOUND HAVING INHIBITORY ACTIVITY AGAINST MULTIPLE TYROSINE KINASES AND PHARMACEUTICAL COMPOSITION CONTAINING SAME

The present invention is for the anti-inflammatory compounds that have an inhibitory activity against protein tyrosine kinases and their pharmaceutical composition(s) containing the compound as the active ingredient. Since the compounds of the present invention can inhibit multiple protein kinases associated with inflammatory diseases and immune disorders, they are useful for their prevention or treatment.

Design, synthesis, and anticonvulsant activity evaluation of 4-(3-Alkoxy-phenyl)-2,4-dihydro-[1,2,4]triazol-3-ones

A series of 4-(3-alkoxy-phenyl)-2,4-dihydro-[1,2,4]triazol-3-ones were synthesized using the appropriate synthetic route and evaluated experimentally in the maximal electroshock test; their neurotoxicities were evaluated by the rotarod neurotoxicity test. The structures of these compounds were confirmed by IR, MS, 1H-NMR, and elementary analysis. All target compounds exhibited anticonvulsant activity to varying degrees in the maximal electroshock test. 4-(3-Benzyloxy-phenyl)-2,4-dihydro-[1,2,4]triazol-3-one (4i) was the most promising compound with an ED50 value of 30.5 mg/kg and a protective index (PI) of 18.63, showing a higher safety than the standard carbamazepine (PI = 6.45). In addition, the potency of compound 4i against seizures induced by pentylenetetrazole and 3-mercaptopropionic acid suggested its broad-spectrum activity, and the mechanisms of action including inhibition of voltage-gated ion channels and modulation of GABAergic activity might be involved in its anticonvulsant activity. Copyright

CHEMICAL COMPOUNDS

Triazine derivatives of formula (I) or salts thereof, wherein R1 represents a halogen atom or a group selected from hydroxy; C1-8 alkyl C1-6 alkoxy; C1-3 alkoxy C1-3 alkoxy; phenoxy or phenyl C1-3 alkoxy, wherein the phenyl group is optionally substituted by a halogen atom or a group selected from C1-3 alkyl, C1.3 alkoxy, or hydroxy; fluoro C1-3 alkyl; cyano; -CO2R3, wherein R3 represents a hydrogen atom or a C1-4 alkyl group; - CONR4R5, wherein R4 and R5 each independently represents a hydrogen atom or a C1-4 alkyl group, or, together with the nitrogen atom to which they are attached, form a saturated 5- to 7- membered ring, which ring optionally contains one or more atoms selected from an oxygen or a sulphur atom, or a group selected from -NH- or -N(CH3)-; and R2 represents a hydrogen or halogen atom, or a group selected from hydroxy, C1-6 alkyl or C1-6 alkoxy; are inhibitors of the enzyme 5-lipoxygenase. Processes for preparing the triazine derivatives of formula (I) and compositions containing them are also described