133777-96-5

Upstream product

• 1622-32-8 2-Chloroethanesulfonyl chloride 
• 17061-62-0 N,N-bis(p-methoxybenzyl)amine 
• 123-11-5 4-methoxy-benzaldehyde 
• 2393-23-9 4-methoxy-benzylamine 
• 6608-47-5 vinylsulfonyl chloride 
• 854391-95-0 bis(4-methoxybenzyl)amine hydrochloride 

Downstream Products

• 133778-24-2 methyl α-<2-<amino>-sulfonyl>ethyl>-4-<2-(1,1-dimethylethoxy)-2-oxoethoxy>benzeneacetate 
• 133777-97-6 methyl α-<2-<amino>-sulfonyl>ethyl>benzeneacetate 
• 133778-01-5 4-[Bis-(4-methoxy-benzyl)-sulfamoyl]-2-{2-[bis-(4-methoxy-benzyl)-sulfamoyl]-ethyl}-2-phenyl-butyric acid methyl ester 
• 133777-99-8 methyl 4-(benzoyloxy)-α-<2-<amino>sulfonyl>ethyl>benzeneacetate 
• 133778-03-7 Benzoic acid 4-(3-[bis-(4-methoxy-benzyl)-sulfamoyl]-1-{2-[bis-(4-methoxy-benzyl)-sulfamoyl]-ethyl}-1-methoxycarbonyl-propyl)-phenyl ester 

Relevant academic research and scientific papers

Discovery and Pharmacokinetics of Sulfamides and Guanidines as Potent Human Arginase 1 Inhibitors

We designed and synthesized a series of arginase inhibitors as derivatives of the well-known 2-(S)-amino-6-boronohexanoic acid (ABH) with basic and neutral side chains in the α-position relative to the amino acid group. In an effort to improve the pharmacokinetic profile of literature examples and retain potent enzymatic activity, sulfamido moieties were introduced to generate hydrogen bond interaction with the aspartic acid residue in the arginase active site. The compounds with basic guanidine-containing side chains were even more potent arginase inhibitors. Both groups of compounds, as designed, demonstrated low clearance in their pharmacokinetic profile. The most active inhibitor 15aa showed high nanomolar potency with IC50 = 32 nM toward human arginase 1 and demonstrated low clearance (4.2 mL/min/kg), long t1/2, and moderate volume of distribution in rat pharmacokinetic studies.

FUSED TRIAZOLE AGONISTS OF THE APJ RECEPTOR

Compounds of Formula I, pharmaceutically acceptable salts thereof, tautomers thereof, pharmaceutically acceptable salts of the tautomers, or mixtures thereof are agonists of the APJ Receptor and may have use in treating cardiovascular and other conditions. Compounds of Formula (I) have the following structure: where the definitions of the variables are provided herein.

HETEROARYL-SUBSTITUTED TRIAZOLES AS APJ RECEPTOR AGONISTS

Compounds of Formula (I) and Formula (II), pharmaceutically acceptable salt thereof, stereoisomers of any of the foregoing, or mixtures thereof are agonists of the APJ Receptor and may have use in treating cardiovascular and other conditions. Compounds of Formula I and Formula II have the following structures: where the definitions of the variables are provided herein.

TRIAZOLE AGONISTS OF THE APJ RECEPTOR

Compounds of Formula I and Formula II, pharmaceutically acceptable salt thereof, stereoisomers of any of the foregoing, or mixtures thereof are agonists of the APJ Receptor and have use in treating cardiovascular and other conditions. Compounds of Formula I and Formula II have the following structures where the definitions of the variables are provided herein.

Chemo- and Regioselective Direct Functional Group Installation through Catalytic Hydroxy Group Selective Conjugate Addition of Amino Alcohols to α,β-Unsaturated Sulfonyl Compounds

A chemoselective functional group installation through catalytic hydroxy group selective conjugate addition of amino alcohols to a variety of functionalized α,β-unsaturated sulfonyl derivatives was developed. Azide group installation for click chemistry and facile fluorescent labeling onto the less reactive hydroxy group demonstrated the synthetic utility of the present chemoselective catalysis. Moreover, chemo- and regioselective reaction of an unprotected amino diol was achieved for the first time.

ARGINASE INHIBITORS AND THEIR THERAPEUTIC APPLICATIONS

The inventive compounds are small molecule therapeutics that are potent inhibitors of arginase 1 and arginase 2 activity. The inventions also provides pharmaceutical compositions and methods for using the inventive compounds for treating or preventing a disease or condition associated with arginase activity.

BENZENESULFONYL-CHROMANE, THIOCHROMANE, TETRAHYDRONAPHTHALENE AND RELATED GAMMA SECRETASE INHIBITORS

Disclosed are novel gamma secretase inhibitors of the formula (I): or a pharmaceutically acceptable salt, solvate, or ester thereof, wherein L1, n, X, Ar, Y, Z, Q, and Q1 are as defined herein. Also disclosed are methods for inhibiti