299181-33-2

Upstream product

• 353467-19-3 methyl 4-methoxy-3-(morpholinosulfonyl)benzoate 
• 100-09-4 4-methoxybenzoic acid 
• 110-91-8 morpholine 
• 50803-29-7 3-chlorosulfonyl-4-methoxybenzoic acid 

Downstream Products

• 299180-68-0 4,4'-bis[4-methoxy-3-(morpholine-4-sulfonyl)benzoylamino]biphenyl-2,2'-(bis)sulfonic acid 
• 299180-69-1 2,2'-Thiobis[5-[[4-methoxy-3-(4-morpholinylsulfonyl)benzoyl]amino]benzenesulfonic Acid] 
• 1025772-17-1 (R)-N-(1-(3-chlorophenyl)ethyl)-4-methoxy-3-(morpholinosulfonyl)benzamide 

Relevant academic research and scientific papers

Synthesis and Biological Evaluation of 4-Sulfamoylphenyl/Sulfocoumarin Carboxamides as Selective Inhibitors of Carbonic Anhydrase Isoforms hCA II, IX, and XII

With the aim to develop potent and selective human carbonic anhydrase inhibitors (hCAIs), we synthesized 4-sulfamoylphenyl/sulfocoumarin benzamides (series 5 a–r and series 7 a–q) and evaluated their inhibition profiles against five isoforms of the zinc-containing human carbonic anhydrase (hCA, EC 4.2.1.1): cytosolic hCA I and II, and the transmembrane isozymes hCA IV, IX, and XII. Compounds 5 a–r were found to selectively inhibit hCA II in the nanomolar range, while being less effective against the other hCA isoforms. As noted from the literature, sulfocoumarin (1,2-benzoxathiine 2,2-dioxide) acts as a “prodrug” inhibitor and is hydrolyzed by the esterase activity of hCA to form 2-hydroxyphenylvinylsulfonic acid, which thereafter binds to the enzyme in a manner similar to that of coumarins and sulfoxocoumarins. All these sulfocoumarins (compounds 7 a–q) were found to be very weak or ineffective as inhibitors of the housekeeping off-target hCA isoforms I and II, and effectively inhibited the transmembrane tumor-associated isoforms IX and XII in the high nanomolar to micromolar ranges. Further structural modifications of these molecules could be useful for the development of effective hCA inhibitors used for the treatment of glaucoma, epilepsy, and cancer.

Calcium receptor modulating agents

The present invention relates generally to compounds represented in Formula I, pharmaceutical compositions comprising them and methods of treating of diseases or disorders related to the function of the calcium sensing receptor. The invention also relates to processes for making such compounds and to intermediates useful in these processes.

Aryl sulfonic acids and derivatives as FSH antagonists

This invention provides compounds of formula I having the structure wherein R1, Ar, Ar′, and Q are as defined in the specification, or a pharmaceutically acceptable salt thereof, which are useful as contraceptive agents.