145304-35-4

Upstream product

• 123-08-0 4-hydroxy-benzaldehyde 
• 2967-92-2 4-(2-fluoro-ethoxy)-benzaldehyde 
• 99-96-7 4-hydroxy-benzoic acid 
• 99-76-3 methyl 4-hydroxylbenzoate 
• 132838-34-7 methyl-4-(2-fluoroethoxyl)benzoate 

Downstream Products

• 145304-36-5 4-(2-fluoroethoxy)benzoyl chloride 
• 1200959-82-5 2-iodophenyl 4-(2-fluoroethoxy)benzoate 
• 1269797-33-2 4-(2-fluoroethoxy)-N-(4-(4-(2-methoxyphenyl)piperazin-1-yl)-trans-butyl-2-enyl)benzamide 
• 1269797-49-0 4-(2-fluoroethoxy)-N-(4-(4-(2-(2-fluoroethoxy)phenyl)piperazin-1-yl)butyl)benzamide 
• 1269797-25-2 4-(2-fluoroethoxy)-N-(4-(4-(2-methoxyphenyl)piperazin-1-yl)butyl)benzamide 
• 1397262-85-9 N-(2-(4-(2-fluoroethoxy)benzamido)ethyl)benzofuran-2-carboxamide 

Relevant academic research and scientific papers

Monoacylglycerol Lipase Modulators

Fused compounds of Formula (I) and Formula (II), pharmaceutical compositions containing them, methods of making them, and methods of using them including methods for treating disease states, disorders, and conditions associated with MGL modulation, such as those associated with pain, psychiatric disorders, neurological disorders (including, but not limited to major depressive disorder, treatment resistant depression, anxious depression, bipolar disorder), cancers and eye conditions. Wherein R1, R2, R2a, R3, R3a, R4, and R4a are defined herein.

COMPOUNDS FOR MODULATING AQUAPORINS

The invention relates to compounds of formula (I) pharmaceutical compositions thereof and methods for modulating aquaporin 9.

Design, Synthesis, and in Vitro and in Vivo Evaluation of an 18F-Labeled Sphingosine 1-Phosphate Receptor 1 (S1P1) PET Tracer

Sphingosine 1-phosphate receptor 1 (S1P1) plays a pivotal signaling role in inflammatory response; because S1P1 modulation has been identified as a therapeutic target for various diseases, a PET tracer for S1P1 would be a useful tool. Fourteen fluorine-containing analogues of S1P ligands were synthesized and their in vitro binding potency measured; four had high potency and selectivity for S1P1 (S1P1 IC50 100-fold selectivity for S1P1 over S1P2 and S1P3). The most potent ligand, 28c (IC50 = 2.63 nM for S1P1) was 18F-labeled and evaluated in a mouse model of LPS-induced acute liver injury to determine its S1P1-binding specificity. The results from biodistribution, autoradiography, and microPET imaging showed higher [18F]28c accumulation in the liver of LPS-treated mice than controls. Increased expression of S1P1 in the LPS model was confirmed by immunohistochemical analysis (IHC). These data suggest that [18F]28c is a S1P1 PET tracer with high potential for imaging S1P1 in vivo.

The flocculated acryloyldimethyltauric molecule ligand

Provided are certain benzothiazole, imidazothiazole, imidazopyrimidine and imidazopyridine compounds, including, for example: formula (I) and pharmaceutically and physiologically acceptable salts, hydrates, and solvates thereof. Such compounds can be used as diagnostic ligands or labels of tau protein and PHF.

LABELED MOLECULAR IMAGING AGENTS AND METHODS OF USE

Imaging agents are described that comprise labeled substrates capable of being introduced into cells via the cystine/glutamate antiporter. The substrates may be used for imaging or detecting oxidative stress in cells by introducing the labeled agents into

Exploration of ring size in a series of cyclic vicinal diamines with σ1 receptor affinity

Imidazolidine and 1,4-diazepane analogs of N-(2-benzofuranyl)methyl- N′-(4-alkoxybenzyl)piperazines were prepared to explore the effect of ring contraction and expansion on σ receptor affinity and subtype selectivity within a series of cyclic diamines. In vitro receptor binding assays revealed that all cyclic vicinal diamines possessed affinity and selectivity for σ1 receptors. The imidazolidines possessed nanomolar σ1 affinities (Ki = 6.45-53.5 nM), and relatively low levels of subtype selectivity (σ2/σ1 = 58-237). However, the piperazines and diazepanes achieved picomolar σ1 interactions, with Ki ranges of 0.05-10.28 and 0.10-0.194 nM, respectively. Moreover, the piperazines and diazepanes showed excellent discrimination over the σ2 receptor, with σ1 selectivities of 143-16140 and 220-11542, respectively.

Synthesis and pharmacological evaluation of fluorine-containing D 3 dopamine receptor ligands

A series of fluorine-containing N-(2-methoxyphenyl)piperazine and N-(2-fluoroethoxy)piperazine analogues were synthesized, and their affinities for human dopamine D2, D3, and D4 receptors were determined. Radioligand binding studies identified five compounds, 18a, 20a, 20c, 20e, and 21e, which bind with high affinity at D3 (K i = 0.17-5 nM) and moderate to high selectivity for D3 vs D2 receptors (ranging from ～25- to 163-fold). These compounds were also evaluated for intrinsic activity at D2 and D3 receptors using a forskolin-dependent adenylyl cyclase assay. This panel of compounds exhibits varying receptor subtype binding selectivity and intrinsic activity at D2 vs D3 receptors. These compounds may be useful for behavioral pharmacology studies on the role of D2-like dopamine receptors in neuropsychiatric and neurological disorders. Furthermore, compound 20e, which has the highest binding affinity and selectivity for the D3 receptor (Ki = 0.17 nM for D3, 163-fold selectivity for D3 vs D2 receptors), represents a candidate fluorine-18 radiotracer for in vivo PET imaging studies on the regulation of D3 receptor expression.

Amino-5,5-diphenylimidazolone derivatives for the inhibition of beta-secretase

The present invention provides a compound of formula I and the use thereof for the therapeutic treatment, prevention or amelioration of a disease or disorder characterized by elevated β-amyloid deposits or β-amyloid levels in a patient.