71207-29-9

Upstream product

• 7144-05-0 4-Aminomethylpiperidine 
• 100-52-7 benzaldehyde 

Downstream Products

• 120687-50-5 N-{(S)-1-Benzyl-2-oxo-2-[4-({[1-phenyl-meth-(E)-ylidene]-amino}-methyl)-piperidin-1-yl]-ethyl}-acetamide 
• 304905-24-6 N-((1-benzylpiperidin-4-yl)methyl)-1-phenylmethanimine 
• 177948-71-9 4-(benzylaminomethyl)piperidine 
• 144222-21-9 4-({[1-Phenyl-meth-(E)-ylidene]-amino}-methyl)-piperidine-1-carboxylic acid tert-butyl ester 
• 796847-63-7 1-{1-[2-(4-nitrophenyl)ethyl]piperidin-4-yl}methanamine 
• 750649-69-5 2-[4-(aminomethyl)piperidin-1-yl]-N-phenylacetamide 
• 1046381-08-1 C₂₃H₂₈N₂O₂ 
• 1046381-12-7 C₂₀H₃₀N₂O₂ 
• 1403470-14-3 (4-((benzylamino)methyl)piperidin-1-yl)(phenyl)methanone 
• 1403470-50-7 N-benzyl-N-((1-benzylpiperidin-4-yl)methyl)acetamide 
• 1403470-51-8 N-benzyl-N-((1-benzylpiperidin-4-yl)methyl)benzamide 
• 1331746-43-0 N-benzyl-N-((1-(4-chlorobenzyl)piperidin-4-yl)methyl)acetamide 
• 1403470-52-9 N-benzyl-N-((1-(4-chlorobenzyl)piperidin-4-yl)methyl)acetamide 
• 1403470-30-3 (4-((benzyl(methyl)amino)methyl)piperidin-1-yl)(phenyl)methanone 

Relevant academic research and scientific papers

Hypoxia-Triggered Self-Assembly of Ultrasmall Iron Oxide Nanoparticles to Amplify the Imaging Signal of a Tumor

Hypoxia is a common phenomenon among most solid tumors that significantly influences tumor response toward chemo- and radiotherapy. Understanding the distribution and extent of tumor hypoxia in patients will be very important to provide personalized thera

Structural investigation on thiazolo[5,4-d]pyrimidines to obtain dual-acting blockers of CD73 and adenosine A2A receptor as potential antitumor agents

Adenosine pathway, including its generating enzyme (CD73) and its receptors represents a key target for cancer immunotherapy. Here we aimed to search for novel compounds able to co-target the CD73 and the A2A adenosine receptor (A2A

Piperazine-and piperidine-containing thiazolo[5,4-d]pyrimidine derivatives as new potent and selective adenosine a2a receptor inverse agonists

The therapeutic use of A2A adenosine receptor (AR) antagonists for the treatment of neurodegenerative disorders, such as Parkinson and Alzheimer diseases, is a very promising approach. Moreover, the potential therapeutic role of A2A AR antagonists to avoid both immunoescaping of tumor cells and tumor development is well documented. Herein, we report on the synthesis and biological evaluation of a new set of piperazine-and piperidine-containing 7-amino-2-(furan-2-yl)thiazolo[5,4-d]pyrimidine derivatives designed as human A2A AR antagonists/inverse agonists. Binding and potency data indicated that a good number of potent and selective hA2A AR inverse agonists were found. Amongst them, the 2-(furan-2-yl)-N5-(2-(4-phenylpiperazin-1-yl)ethyl)thiazolo[5,4-d]pyrimidine-5,7-diamine 11 exhibited the highest A2A AR binding affinity (Ki = 8.62 nM) as well as inverse agonist potency (IC50 = 7.42 nM). In addition, bioinformatics prediction using the web tool SwissADME revealed that 8, 11, and 19 possessed good drug-likeness profiles.

Nitrogen-containing heterocyclic compound and preparation method and application thereof

The invention provides a nitrogen-containing heterocyclic compound and a preparation method and application thereof. The nitrogen-containing heterocyclic compound is unique in synthesis method, simplein process, easily available in raw materials, small in

Targeting Serotonin 2A and Adrenergic α1 Receptors for Ocular Antihypertensive Agents: Discovery of 3,4-Dihydropyrazino[1,2-b]indazol-1(2H)-one Derivatives

Glaucoma affects millions of people worldwide and causes optic nerve damage and blindness. The elevation of the intraocular pressure (IOP) is the main risk factor associated with this pathology, and decreasing IOP is the key therapeutic target of current pharmacological treatments. As potential ocular hypotensive agents, we studied compounds that act on two receptors (serotonin 2A and adrenergic α1) linked to the regulation of aqueous humour dynamics. Herein we describe the design, synthesis, and pharmacological profiling of a series of novel bicyclic and tricyclic N2-alkyl-indazole-amide derivatives. This study identified a 3,4-dihydropyrazino[1,2-b]indazol-1(2H)-one derivative with potent serotonin 2A receptor antagonism, >100-fold selectivity over other serotonin subtype receptors, and high affinity for the α1 receptor. Moreover, upon local administration, this compound showed superior ocular hypotensive action in vivo relative to the clinically used reference compound timolol.

Probes for Imaging of Hypoxia

Exemplary probes for detecting hypoxic cells and tissue have the structure of

Another brick in the wall. Validation of the σ1 receptor 3d model by computer-assisted design, synthesis, and activity of new σ1 ligands

Originally considered an enigmatic polypeptide, the σ1 receptor has recently been identified as a unique ligand-regulated protein. Many studies have shown the potential of σ1 receptor ligands for the treatment of various diseases of the central nervous system (CNS); nevertheless, almost no information about the 3D structure of the receptor and/or the possible modes of interaction of the σ1 protein with its ligands have been unveiled so far. With the present work we validated our σ1 3D homology model and assessed its reliability as a platform for σ1 ligand structure-based drug design. To this purpose, the 3D σ1 model was exploited in the design of 33 new σ1 ligands and in their ranking for receptor affinity by extensive molecular dynamics simulation-based free energy calculations. Also, the main interactions involved in receptor/ligand binding were analyzed by applying a per residue free energy deconvolution and in silico alanine scanning mutagenesis calculations. Subsequently, all compounds were synthesized in our laboratory and tested for σ1 binding activity in vitro. The agreement between in silico and in vitro results confirms the reliability of the proposed σ1 3D model in the a priori prediction of the affinity of new σ1 ligands. Moreover, it also supports and corroborates the currently available biochemical data concerning the σ1 protein residues considered essential for σ1 ligand binding and activity.

Design, synthesis, and biological evaluation of new 5-ht4 receptor agonists: Application as amyloid cascade modulators and potential therapeutic utility in alzheimer's disease

Serotonin 5-HT4 receptor (5-HT4R) agonists are of particular interest for the treatment of Alzheimer's disease because of their ability to ameliorate cognitive deficits and to modulate production of amyloid β-protein (Aβ). However, d

2 -ALKYL- INDAZOLE COMPOUNDS FOR THE TREATMENT OF CERTAIN CNS-RELATED DISORDERS

2-Alkyl-indazole compound and its pharmaceutically acceptable salts of acid addition, method and intermediates for preparing them, a pharmaceutical composition containing them and use of the latter. The 2-alkyl-indazole compound has the following general formula (I) in which R1, R2, R3, R4, R6, R7, X, Y, W, n, p, and m have the meanings stated in the description.

Identification and characterization of 4-methylbenzyl 4-[(pyrimidin-2- ylamino)methyl]piperidine-1-carboxylate, an orally bioavailable, brain penetrant NR2B selective N-methyl-D-aspartate receptor antagonist

The discovery of a novel series of NR2B subtype selective N-methyl-D-aspartate (NMDA) antagonists is reported. Initial optimization of a high-throughput screening lead afforded an aminopyridine derivative 13 with significant NR2B antagonist potency but limited selectivity over hERG-channel and other off-target activities. Further structure-activity studies on the aminoheterocycle moiety and optimization of the carbamate led to the highly potent 2-aminopyrimidine derivative 20j with a significantly improved off-target activity profile and oral bioavailability in multiple species coupled with good brain penetration. Compound 20j demonstrated efficacy in in vivo rodent models of antinociception, allodynia, and Parkinson's disease.