83631-87-2

Upstream product

• 100-58-3 phenylmagnesium bromide 
• 209391-72-0 8-[Chloro-(toluene-4-sulfinyl)-methylene]-1,4-dioxa-spiro[4.5]decane 
• 4746-97-8 cyclohexanedione monoethylene ketal 
• 667458-78-8 benzyl 3,5-bis(trifluoromethyl)phenyl sulfone 
• 1080-32-6 O,O-diethyl benzylphosphonate 
• 1449-46-3 benzyltriphenylphosphonium bromide 
• 209392-00-7 Acetic acid 8-[chloro-(toluene-4-sulfinyl)-methyl]-1,4-dioxa-spiro[4.5]dec-8-yl ester 
• 209391-67-3 8-[Chloro-(toluene-4-sulfinyl)-methyl]-1,4-dioxa-spiro[4.5]decan-8-ol 
• 100-39-0 benzyl bromide 
• 863560-55-8 [3,5-bis(trifluoromethyl)phenyl] benzyl sulfide 

Downstream Products

• 1453492-62-0 (1S,4S)-4-benzylcyclohexyl 2-pyridyl carbonate 
• 1453492-63-1 (1R,4R)-4-benzylcyclohexyl 2-pyridyl carbonate 
• 1453492-55-1 (1S,4S)-4-benzylcyclohexyl 2-oxopyridine-1-carboxylate 
• 141191-74-4 trans-4-Benzylcyclohexan-1-ol 
• 1439367-70-0 (2R,3S)-3-hydroxy-2-[({[(1s,4s)-4-benzylcyclohexyl]oxy}carbonyl)amino]butanoic acid 
• 1439367-69-7 (2R,3S)-3-hydroxy-2-[({[(1s,4s)-4-benzylcyclohexyl]oxy}carbonyl)amino]butanoic acid 
• 1439367-67-5 4-benzylcyclohexyl pyridin-2-yl carbonate 
• 1439367-68-6 4-benzylcyclohexyl 2-oxopyridine-1-carboxylate 
• 1411975-91-1 4-benzylidenecyclohexanol 

Relevant academic research and scientific papers

SELECTIVE LIGANDS OF HUMAN CONSTITUTIVE ANDROSTANE RECEPTOR

The present invention provides a structurally novel class of heterocyclic compounds of general formula I wherein L1 is heteroaryl and L2 is heteroaryl or aryl. The novel compounds are useful in a method of prevention or treatment of a condition which is m

Disubstituted beta-lactones as inhibitors of N-acylethanolamine acid amidase (NAAA)

The present invention provides compounds and pharmaceutical compositions for inhibiting N-acylethanolamine acid amidase (NAAA). Inhibition of NAAA is contemplated as a method to sustain the levels of palmitoylethanolamide (PEA) and oleylethanolamide (OEA), two substrates of NAAA, in conditions characterized by reduced concentrations of PEA and OEA. The invention also provides methods for treating inflammatory diseases and pain, and other disorders in which decreased levels of PEA and OEA are associated with the disorder.

CARBAMATE DERIVATIVES OF LACTAM BASED N-ACYLETHANOLAMINE ACID AMIDASE (NAAA) INHIBITORS

Described herein are compounds and pharmaceutical compositions which inhibit N-acylethanolamine acid amidase (NAAA). Described herein are methods for synthesizing the compounds set forth herein and methods for formulating these compounds as pharmaceutical compositions which include these compounds. Also described herein are methods of inhibiting NAAA in order to sustain the levels of palmitoylethanolamide (PEA) and other N-acylethanolamines (NAE) that are substrates for NAAA, in conditions characterized by reduced concentrations of NAE. Also, described here are methods of treating and ameliorating pain, inflammation, inflammatory diseases, and other disorders in which modulation of fatty acid ethanolamides is clinically or therapeutically relevant or in which decreased levels of NAE are associated with the disorder.

Synthesis and structure-activity relationship (SAR) of 2-methyl-4-oxo-3- oxetanylcarbamic acid esters, a class of potent N-acylethanolamine acid amidase (NAAA) inhibitors

N-Acylethanolamine acid amidase (NAAA) is a lysosomal cysteine hydrolase involved in the degradation of saturated and monounsaturated fatty acid ethanolamides (FAEs), a family of endogenous lipid agonists of peroxisome proliferator-activated receptor-α, which include oleoylethanolamide (OEA) and palmitoylethanolamide (PEA). The β-lactone derivatives (S)-N-(2-oxo-3-oxetanyl)-3-phenylpropionamide (2) and (S)-N-(2-oxo-3-oxetanyl)- biphenyl-4-carboxamide (3) inhibit NAAA, prevent FAE hydrolysis in activated inflammatory cells, and reduce tissue reactions to pro-inflammatory stimuli. Recently, our group disclosed ARN077 (4), a potent NAAA inhibitor that is active in vivo by topical administration in rodent models of hyperalgesia and allodynia. In the present study, we investigated the structure-activity relationship (SAR) of threonine-derived β-lactone analogues of compound 4. The main results of this work were an enhancement of the inhibitory potency of β-lactone carbamate derivatives for NAAA and the identification of (4-phenylphenyl)-methyl-N-[(2S,3R)-2-methyl-4-oxo-oxetan-3-yl]carbamate (14q) as the first single-digit nanomolar inhibitor of intracellular NAAA activity (IC50 = 7 nM on both rat NAAA and human NAAA).

DISUBSTITUTED BETA-LACTONES AS INHIBITORS OF N-ACYLETHANOLAMINE ACID AMIDASE (NAAA)

The present invention provides compounds and pharmaceutical compositions for inhibiting N-acylethanolamine acid amidase (NAAA). Inhibition of NAAA is contemplated as a method to sustain the levels of palmitoylethanolamide (PEA) and oleylethanolamide (OEA), two substrates of NAAA, in conditions characterized by reduced concentrations of PEA and OEA. The invention also provides methods for treating inflammatory diseases and pain, and other disorders in which decreased levels of PEA and OEA are associated with the disorder.

CYCLOHEXANE SUBSTITUTED AMINO CYCLOPENTANE DERIVATIVES AS USEFUL CCR2 ANTAGONISTS

Disclosed are the CCR2 antagonists of Formula I: I or pharmaceutically acceptable salts thereof, wherein A, B, R, and R6 are as defined herein. Also disclosed are pharmaceutical compositions containing the compounds, methods of treatment using the compoun

An efficient route into synthetically challenging bridged achiral 1,2,4,5-tetraoxanes with antimalarial activity

Here we present an efficient route into synthetically challenging bridged 1,2,4,5-tetraoxanes. The key to the success of this route is the use of H2O2 and catalytic I2 to form the gem-dihydroperoxide followed by a Ag2

3,5-Bis(trifluoromethyl)phenyl sulfones in the Julia-Kocienski olefination - Application to the synthesis of tri- and tetrasubstituted olefins

3,5-Bis(trifluoromethyl)phenyl (BTFP) sulfones 8a-d are successfully employed in the modified Julia olefination reaction with carbonyl compounds employing phosphazene base P4-tBu at room temp. in THF, affording tri- and tetrasubstituted olefins in good yi

2-Cyclohexyl quinazoline NMDA/NR2B antagonists

4-substituted cyclohexanes substituted in the 1-position with quinazoline either directly or through a C1-C4alkyl, C1-C4alkenyl, C1-C4alkynyl, C1-C4alkoxy, amino, amin

2-CYCLOHEXYL IMIDAZOPYRIDINE NMDA/NR2B ANTAGONISTS

4-substituted cyclohexanes substituted in the 1-position with imidazopyridine either directly or through a C1-C4alkyl, C1-C4alkenyl, C1-C4alkynyl, C 1-C4alkoxy, amino, aminoC1-C4alkyl, hydroxyC1-C4alkyl, carbonyl, cycloC3-C 6alkyl or aminocarbonyl chain a