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dc.contributorWichita State University
dc.contributor.authorGroutas, William C.
dc.date.accessioned2016-11-08T02:08:47Z
dc.date.available2016-11-08T02:08:47Z
dc.date.issued2002-12-17
dc.date.submitted2000-04-19
dc.identifierUS 6,495,358 B1
dc.identifier.citationGroutas, William C., inventor. Wichita State University, assignee. Sulfamide and bis-sulfamide amino acid derivatives as inhibitors of proteolytic enzymes. United States patent US 6,495,358. 2002, Dec.17.
dc.identifier.urihttp://patft.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&Sect2=HITOFF&d=PALL&p=1&u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&r=1&f=G&l=50&s1=6,495,358.PN.&OS=PN/6,495,358&RS=PN/6,495,358
dc.identifier.urihttp://hdl.handle.net/10057/12560
dc.descriptionWSU inventor: William C. Groutas, Dept. of Chemistry, College of Liberal Arts and Sciences
dc.descriptionAppl. No.: 09/552,554 filed Apr 19, 2000. Patent No.: U.S. 6,495,358 granted Dec 17, 2002.
dc.description.abstractCompounds of the general formula I are provided: ##STR1## and pharmaceutically acceptable salts thereof, wherein, Z is a chemical species or R.sub.i capable of binding at a primary specificity site of a protease; Y is a chemical species reactive to a specific class of protease; each of R.sub.2, R.sub.3, R.sub.5 and R.sub.7 is independently selected from the group consisting hydrogen, alkyls, aryls, substituted aryls, alkylaryls and arylalkyls; R.sub.4 and R.sub.6 are independently selected from the group consisting of: (a) H, alkyl, aryl, arylalkyl, alkylaryl, substituted derivatives thereof, and R.sub.i ; (b) --C(O)OH and derivatives thereof, said derivatives selected from the group consisting of --C(O)OQ, --C(O)NR.sub.Y R.sub.Z, --C(O)[NHCHR.sub.i(q) C(O)].sub.q OQ, and --C(O)[NHCHR.sub.i(q) C(O)].sub.q NR.sub.Y R.sub.Z ; and (c) --CHR.sub.i NH.sub.2 and derivatives thereof, said derivatives selected from the group consisting of --CHR.sub.i NHW, --CHR.sub.i NHC(O)OQ, --CHR.sub.i NHC(O)R, --CHR.sub.i NHC(O)NR.sub.Y R.sub.Z, --CHR.sub.i NHC(O)[NHCHR.sub.i(q) C(O)].sub.q OQ, --CHR.sub.i NHSO.sub.2 R, and --CHR.sub.i NH[C(O)CHR.sub.i(r) NH].sub.r W, where q and r independently are integers from 1 to 10 inclusive; J is a carboxyl protecting group; G is an amino protecting group; Q is H, R or J; W is H, R or G; each R.sub.i is independently selected from naturally or non-naturally occurring amino acid side chains; R is alkyl, aryl, substituted aryl, alkylaryl, arylalkyl, or heterocyclic radical; and each R.sub.Y and R.sub.Z is independently H, alkyl, aryl, substituted aryl, alkylaryl, arylalkyl, or heterocyclic radical.
dc.format.extent30 claims; 12 drawing sheets; 29 pages.
dc.languageen_US
dc.publisherUnited States Patent and Trademark Office
dc.rightsIn public domain (2020-04-19 Anticipated expiration; Status: Expired - Fee Related)
dc.subject.classificationUSPC.: 435/212
dc.subject.classificationCPC: C07C 307/06 (20130101); Y02P 20/55 (20151101)
dc.subject.classificationIPC.: C07C 307/00 (20060101); C07C 307/06 (20060101); C12N 009/48 (); C12N 009/50 (); A01N 041/06 (); A61K 031/18 ()
dc.titleSulfamide and bis-sulfamide amino acid derivatives as inhibitors of proteolytic enzymes
dc.typePatent


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