119022-76-3

Upstream product

• 79359-40-3 2-amino-4-phenyl-6-phenylsulfanyl-pyridine-3,5-dicarbonitrile 
• 109-02-4 4-methyl-morpholine 
• 7357-70-2 Cyanothioacetamide 
• 2700-22-3 Benzylidenemalononitrile 
• 42754-56-3 2-(methoxyphenylmethylene)malononitrile 
• 100-52-7 benzaldehyde 
• 109-77-3 malononitrile 
• 110-89-4 piperidine 
• 4341-85-9 malonitrile 
• 5292-53-5 diethyl benzalmalonate 
• 102434-73-1 2,6-diamino-4-phenyl-3,5-dicyano-4H-thiopyran 
• 119044-83-6 N-methylmorpholinium 6-amino-4-phenyl-3,5-dicyano-2-pyridinethiolate 
• 96583-92-5 6-amino-2-chloro-4-phenylpyridine-3,5-dicarbonitrile 

Downstream Products

• 189278-39-5 2-amino-6-(2-oxo-2-phenylethylsulfanyl)-4-phenylpyridine-3,5-dicarbonitrile 
• 220757-42-6 2-amino-6-[(cyanomethyl)thio]-4-phenylpyridine-3,5-dicarbonitrile 
• 331984-47-5 3,6-diamino-4-phenylthieno[2,3-b]pyridine-2,5-dicarbonitrile 
• 413606-58-3 ethyl 3,6-diamino-5-cyano-4-phenylthieno[2,3-b]pyridine-2-carboxylate 

Relevant academic research and scientific papers

Discovery of Highly Potent Adenosine A1Receptor Agonists: Targeting Positron Emission Tomography Probes

Adenosine receptor (AR) radiotracers for positron emission tomography (PET) have provided knowledge on the in vivo biodistribution of ARs in the central nervous system (CNS), which is of therapeutic interest for various neuropsychiatric disorders. Additio

Design, synthesis, characterization and biological evaluation of Thieno[2,3?b]pyridines?chitosan nanocomposites as drug delivery systems for colon targeting

Thieno[2,3?b]pyridine derivatives DATPa?c have been synthesized based on Thorpe?Ziegler Cyclization. The reaction of arylidene malononitrile derivatives (Ia?c) with thiocyanoacetamide (II) in basic medium (piperidine) followed by alkylation using ethyl chloroacetate and finally, cyclization in sodium ethoxide yielded DATPa?c. Thieno[2,3?b]pyridine?chitosan nanocomposites CS?DATPa?c were prepared from the DATPa?c and CS nanoparticles using sodium tripolyphosphate (TPP). CS?DATPa?c nanocomposites were characterized using FTIR, TEM and XRD techniques and showed a relatively narrow size distribution of monodispersed nanoparticles with the average size of 14–78 nm. The in vitro release studies of CS?DAΤPa?c nanocomposites were investigated and showed that the drug release rate is pH-dependent and the trend is as follows: basic > neutral > acidic. The faster release rate in basic medium effectively prolongs drug delivery in gastric pH. Additionally, the antibacterial investigation showed that DATPa?c and CS?DATPa?c nanocomposites exhibited antibacterial activity against both Gram-positive and Gram-negative bacteria but CS?DATPa?c nanocomposites showed much higher antibacterial activity compared to the DATPa?c, which in agreement with the particle size measurements as DATPa?c are in the bulky structure whereas, CS?DATPa?c are in the nanostructure. The results may have applications of drug design for colon targeting.

Neladenoson Bialanate Hydrochloride: A Prodrug of a Partial Adenosine A1 Receptor Agonist for the Chronic Treatment of Heart Diseases

Adenosine is known to be released under a variety of physiological and pathophysiological conditions to facilitate the protection and regeneration of injured ischemic tissues. The activation of myocardial adenosine A1 receptors (A1Rs) has been shown to inhibit myocardial pathologies associated with ischemia and reperfusion injury, suggesting several options for new cardiovascular therapies. When full A1R agonists are used, the desired protective and regenerative cardiovascular effects are usually overshadowed by unintended pharmacological effects such as induction of bradycardia, atrioventricular (AV) blocks, and sedation. These unwanted effects can be overcome by using partial A1R agonists. Starting from previously reported capadenoson we evaluated options to tailor A1R agonists to a specific partiality range, thereby optimizing the therapeutic window. This led to the identification of the potent and selective agonist neladenoson, which shows the desired partial response on the A1R, resulting in cardioprotection without sedative effects or cardiac AV blocks. To circumvent solubility and formulation issues for neladenoson, a prodrug approach was pursued. The dipeptide ester neladenoson bialanate hydrochloride showed significantly improved solubility and exposure after oral administration. Neladenoson bialanate hydrochloride is currently being evaluated in clinical trials for the treatment of heart failure.

Cascade synthesis of thieno[2,3-b]pyridines by using intramolecular cyclization reactions of 3-cyano-2-(organylmethylthio)pyridines

2-Amino-4-aryl-6-mercaptopyridine-3,5-dicarbonitriles as starting materials have been prepared by reducing of 2-amino-4-aryl-6-(phenylthio)pyridine-3,5-dicarbonitrile derivatives which were synthesized on stepwise one-pot three component reaction of malon

Synthesis of Novel Fused Heterocycles Based on 6-Amino-4-phenyl-2-thioxo-1,2-dihydropyridine-3,5-dicarbonitrile

Under phase transfer catalysis conditions, 6-amino-4-phenyl-2-thioxo-1,2-dihydropyridine-3,5-dicarbonitrile (1) was allowed to react with halo compounds, acrylonitrile, chloroacetyl chloride, ethyl cyanoacetate, formamide, triethylorthoformate, or formic acid to give new derivatives of fused pyridines 2–22, respectively. Acetylation of compound 1 using acetic anhydride afforded product 23, which in turn underwent intramolecular cyclization in pyridine to give the corresponding pyrido[2,3-d]pyrimidine 24.

SUBSTITUTED DICYANOPYRIDINES AND USE THEREOF

The present application relates to novel substituted dicyanopyridines, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prophylaxis of cardiovascular disorders.

SUBSTITUTED AZABICYCLIC COMPOUNDS AND THE USE THEREOF

The present application relates to novel substituted pyrrolopyridine, pyrazolopyridine and isoxazolopyridine derivatives, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, preferably for the treatment and/or prevention of cardiovascular disorders.

Structure-activity relationship study of prion inhibition by 2-aminopyridine-3,5-dicarbonitrile-based compounds: Parallel synthesis, bioactivity, and in vitro pharmacokinetics

2-Aminopyridine-3,5-dicarbonitrile compounds were previously identified as mimetics of dominant-negative prion protein mutants and inhibit prion replication in cultured cells. Here, we report findings from a comprehensive structure-activity relationship study of the 6-aminopyridine-3,5-dicarbonitrile scaffold. We identify compounds with significantly improved bioactivity (approximately 40-fold) against replication of the infectious prion isoform (PrPSc) and suitable pharmacokinetic profiles to warrant evaluation in animal models of prion disease.

PYRIDOTHIOPHENE COMPOUNDS

The use of compounds of formula (I) in therapy, particularly for the treatment of a disorder mediated by excessive or inappropriate HSP90 activity formula (I), wherein R2 is a group of formula (IA): -(Arl)m-(Alkl)p-(Z)r-(Alk2)S-Q (IA) Arl,Alk1, Z, Alk2 and Q being as defined in the specification; m, p, r and s are independently 0 or 1; R3 is hydrogen, an optional substituent, or an optionally substituted (Cl-C6)alkyl, aryl or heteroaryl radical; and R4 is a carboxylic ester, carboxamide or sulfonamide group; or a salt, N-oxide, hydrate, or solvate thereof.

New, non-adenosine, high-potency agonists for the human adenosine A 2B receptor with an improved selectivity profile compared to the reference agonist N-ethylcarboxamidoadenosine

The adenosine A2B receptor is the least well characterized of the four known adenosine receptor subtypes because of the absence of potent, selective agonists. Here, we present five non-adenosine agonists. Among them, 2-amino-4-(4-hydroxyphenyl)