133760-08-4Relevant academic research and scientific papers
2-SACCHARINYLMETHYL PHOSPHATES, PHOSPHONATES AND PHOSPHINATES USEFUL AS PROTEOLYTIC ENZYME INHIBITORS AND COMPOSITIONS AND METHOD OF USE THEREOF
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, (2008/06/13)
4-R 1-R 2-R 3-2-Saccharinylmethyl and 4,7-C-4,5, 6,7-tetrahydro-2-saccharinylmethyl phosphates, phosphonates and phosphinates of formulas I and IIA respectively herein, useful in the treatment of degenerative diseases, and compositions containing them, methods for using them to treat degenerative diseases, and processes for their preparation by reaction of the corresponding 2-halomethylsaccharins with a phosphate, phosphonate or phosphinic acid of formula III herein in the presence of an acid-acceptor.
Saccharin derivatives useful as proteolytic enzyme inhibitors and compositions and method of use thereof
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, (2008/06/13)
Novel 2-substituted saccharins which inhibit the enzymatic activity of proteolytic enzymes, are useful in the treatment of degenerative diseases and have the formula STR1 wherein: L is --O--, --S--, --SO-- or --SO2 --; m and n are each independently 0 or 1; R1 is halo, lower-alkanoyl, 1-oxophenalenyl, phenyl or substituted phenyl, heterocyclyl or substituted heterocyclyl or, when L is --O-- and n is 1, cycloheptatrienon-2-yl or, when L is --S-- and n is 1, cyano or lower-alkoxythiocarbonyl or, when L is --SO2 -- and n is 1, lower-alkyl or trifluoromethyl; R2 is hydrogen, lower-alkoxycarbonyl, phenyl or phenylthio; and R3 and R4 are each hydrogen or various substituents and processes for preparation and pharmaceutical compositions and method of use thereof are disclosed.
2-SACCHARINYLMETHYL AND 4,5,6,7-TETRAHYDRO-2-SACCHARINYLMETHYL PHOSPHATES, PHOSPHONATES AND PHOSPHINATES USEFUL AS PROTEOLYTIC ENZYME INHIBITORS AND COMPOSITIONS AND METHOD OF USE THEREOF
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, (2008/06/13)
4-R 1-R 2-R 3-2-Saccharinylmethyl, 4-R 4-4-R 5-6-R 6-4,5,6,7-tetrahydro-2-saccharinylmethyl and 4,7-C-4,5, 6,7-tetrahydro-2-saccharinylmethyl phosphates, phosphonates and phosphinates of formulas I, II and IIA respectively herein, useful in the treatment of degenerative diseases, and compositions containing them, methods for using them to treat degenerative diseases, and processes for their preparation by reaction of the corresponding 2-halomethylsaccharins with a phosphate, phosphonate or phosphinic acid of formula III herein in the presence of an acid-acceptor.
PROTEOLYTIC ENZYME INHIBITION METHOD
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, (2008/06/13)
4-R 4-R 5-2-Saccharinylmethyl aryl carboxylates, useful in the treatment of degenerative diseases, are prepared by reacting a 4-R. sup.4-R 5-2-halomethylsaccharin with an arylcarboxylic acid in the presence of an acid-acceptor.
