Loading...
Sulfamide and bis-sulfamide amino acid derivatives as inhibitors of proteolytic enzymes
Groutas, William C.
Groutas, William C.
Files
Loading...
U.S. 6,495,35
Adobe PDF, 1.49 MB
Authors
Other Names
Location
Time Period
Advisors
Original Date
Digitization Date
Issue Date
2002-12-17
Type
Patent
Genre
Keywords
Subjects (LCSH)
Citation
Groutas, 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.
Abstract
Compounds 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.
Table of Contents
Description
WSU inventor: William C. Groutas, Dept. of Chemistry, College of Liberal Arts and Sciences
Appl. No.: 09/552,554 filed Apr 19, 2000. Patent No.: U.S. 6,495,358 granted Dec 17, 2002.
Appl. No.: 09/552,554 filed Apr 19, 2000. Patent No.: U.S. 6,495,358 granted Dec 17, 2002.
Publisher
United States Patent and Trademark Office
Journal
Book Title
Series
Digital Collection
Finding Aid URL
Use and Reproduction
In public domain (2020-04-19
Anticipated expiration;
Status: Expired - Fee Related)