The role of sulfamide derivatives in medicinal chemistry: a patent review (2006-2008).
BACKGROUND
The sulfamide (R(2)NSO(2)NR(2)) functionality is an acceptable functional group in medicinal chemistry when incorporated into putative small-molecule therapeutics, as it has the potential to form several electrostatic interactions with protein and other targets. The clinically-useful broad spectrum antibiotic doripenem contains a mono-substituted sulfamide. The sulfamide functional group is often found to substitute for sulfonamide, sulfamate or urea functionality.


OBJECTIVE
During the period of 2006-2008, there were nine published patents in which all or most reported compounds contained the sulfamide functional group. There are also patents in which the structures disclosed contain a cyclic sulfamide functional group. Further, there are patents published during this timeframe that contain only a few sulfamide-containing examples, typically as a bioisosteric replacement for a sulfonamide moiety. In this review, we focus on those published patents in which most compounds disclosed are sulfamides and only briefly highlight examples in which sulfamides are included among a large list of other suitable functionalities.


CONCLUSIONS
While the sulfamide functionality is still fairly under-represented in medicinal chemistry, it is a valuable and versatile group that will gain increasing acceptance and favor in the future.
Reitz
Allen B
AB
ALS Biopharma, LLC, 3805 Old Easton Rd., Doylestown, PA 18902, USA. Allen.reitz@IHVR.org
Smith
Garry R
GR
Parker
Michael H
MH
D000818:Animals; D002626:Chemistry, Pharmaceutical; D015195:Drug Design; D006801:Humans; D015394:Molecular Structure; D010330:Patents as Topic; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000737:chemistry / Q000494:pharmacology*; D013997:Time Factors
D013449:Sulfonamides