2-SACCHARINYLMETHYL(ARYL OR ARYLHYDROXY) ACETATES, OR THEIR SALTS FORMED BY ADDITION OF ACIDS TO THESE BASIC COMPOUNDS, OR THEIR SALTS FORMED BY BASES ADDITION TO THESE ACID COMPOUNDS, AND PHARMACEUTICAL COMPOSITION INHIBITING ACTIVITY OF PROTEOLYTIC ENZYMES

4-R -R -2-Saccharinylmethyl aryl and aryloxy acetates, having the formula: wherein: m is zero or one, n is zero or one, and the sum of m + n is zero or one; R is hydrogen or lower-alkyl; R is hydrogen or lower-alkyl; R is phenyl or phenyl substituted by from one to three, the same or different, memb...

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Hauptverfasser: RICHARD POL DANLEP, LI GAMILTON LEJTIMER
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LI GAMILTON LEJTIMER
description 4-R -R -2-Saccharinylmethyl aryl and aryloxy acetates, having the formula: wherein: m is zero or one, n is zero or one, and the sum of m + n is zero or one; R is hydrogen or lower-alkyl; R is hydrogen or lower-alkyl; R is phenyl or phenyl substituted by from one to three, the same or different, members of the group consisting of lower-alkyl perfluorolower-alkyl, lower-alkoxy and halogen; R is hydrogen, halogen, lower-alkyl, perfluorolower-alkyl, perchlorolower-alkyl, lower-alkenyl, lower-alkynyl, cyano, carboxamido, amino, lower-alkylamino, dilower-alkylamino, lower-alkoxy, benzyloxy, lower-alkoxycarbonyl, hydroxy or phenyl; and R is hydrogen or from one to two substituents in any of the 5-, 6- or 7-positions. The compounds of the present invention inhibit the activity of serine proteases, specifically human leukocyte elastase and the chymotrypsin-like enzymes, and are thus useful in the treatment of degenerative disease conditions such as emphysema, rheumatoid arthritis, pancreatitis, cysticfibrosis, chronic bronchitis, adult respiratory distress syndrome, inflammatory bowel disease, psoriasis, bullous pemphigoid and alpha-1-antitrypsin deficiency.
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The compounds of the present invention inhibit the activity of serine proteases, specifically human leukocyte elastase and the chymotrypsin-like enzymes, and are thus useful in the treatment of degenerative disease conditions such as emphysema, rheumatoid arthritis, pancreatitis, cysticfibrosis, chronic bronchitis, adult respiratory distress syndrome, inflammatory bowel disease, psoriasis, bullous pemphigoid and alpha-1-antitrypsin deficiency.</description><edition>6</edition><language>eng</language><subject>CHEMISTRY ; HETEROCYCLIC COMPOUNDS ; HUMAN NECESSITIES ; HYGIENE ; MEDICAL OR VETERINARY SCIENCE ; METALLURGY ; ORGANIC CHEMISTRY ; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES ; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS</subject><creationdate>1997</creationdate><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&amp;date=19970620&amp;DB=EPODOC&amp;CC=RU&amp;NR=2081871C1$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,308,780,885,25563,76318</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&amp;date=19970620&amp;DB=EPODOC&amp;CC=RU&amp;NR=2081871C1$$EView_record_in_European_Patent_Office$$FView_record_in_$$GEuropean_Patent_Office$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>RICHARD POL DANLEP</creatorcontrib><creatorcontrib>LI GAMILTON LEJTIMER</creatorcontrib><title>2-SACCHARINYLMETHYL(ARYL OR ARYLHYDROXY) ACETATES, OR THEIR SALTS FORMED BY ADDITION OF ACIDS TO THESE BASIC COMPOUNDS, OR THEIR SALTS FORMED BY BASES ADDITION TO THESE ACID COMPOUNDS, AND PHARMACEUTICAL COMPOSITION INHIBITING ACTIVITY OF PROTEOLYTIC ENZYMES</title><description>4-R -R -2-Saccharinylmethyl aryl and aryloxy acetates, having the formula: wherein: m is zero or one, n is zero or one, and the sum of m + n is zero or one; R is hydrogen or lower-alkyl; R is hydrogen or lower-alkyl; R is phenyl or phenyl substituted by from one to three, the same or different, members of the group consisting of lower-alkyl perfluorolower-alkyl, lower-alkoxy and halogen; R is hydrogen, halogen, lower-alkyl, perfluorolower-alkyl, perchlorolower-alkyl, lower-alkenyl, lower-alkynyl, cyano, carboxamido, amino, lower-alkylamino, dilower-alkylamino, lower-alkoxy, benzyloxy, lower-alkoxycarbonyl, hydroxy or phenyl; and R is hydrogen or from one to two substituents in any of the 5-, 6- or 7-positions. The compounds of the present invention inhibit the activity of serine proteases, specifically human leukocyte elastase and the chymotrypsin-like enzymes, and are thus useful in the treatment of degenerative disease conditions such as emphysema, rheumatoid arthritis, pancreatitis, cysticfibrosis, chronic bronchitis, adult respiratory distress syndrome, inflammatory bowel disease, psoriasis, bullous pemphigoid and alpha-1-antitrypsin deficiency.</description><subject>CHEMISTRY</subject><subject>HETEROCYCLIC COMPOUNDS</subject><subject>HUMAN NECESSITIES</subject><subject>HYGIENE</subject><subject>MEDICAL OR VETERINARY SCIENCE</subject><subject>METALLURGY</subject><subject>ORGANIC CHEMISTRY</subject><subject>PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES</subject><subject>SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS</subject><fulltext>true</fulltext><rsrctype>patent</rsrctype><creationdate>1997</creationdate><recordtype>patent</recordtype><sourceid>EVB</sourceid><recordid>eNqNjkFLAzEQhavgQdT_MEcFC2492OtsMmsGksySzIrxUorEk2ih_n_MUlFP4ukNzPc-3unR8WqZ0RiHiWPxgdQVf4mpeJAEc7pikzyWK0BDikr5ev6oI06Q0WuGQVIgC30BtJaVJYIMDWebQWVGM0GPmQ0YCaNM0f4laSTlH9W3YRb-FmC0MLbdoQ2blA36wzcfehwd9-2M962p_MBa5lljEiXxpRWA4lMJlM8XJy_b1329-MqzBQykxi3r7n1T97vtc32rH5s0rW7W3fquM93tP5BPn1FeZg</recordid><startdate>19970620</startdate><enddate>19970620</enddate><creator>RICHARD POL DANLEP</creator><creator>LI GAMILTON LEJTIMER</creator><scope>EVB</scope></search><sort><creationdate>19970620</creationdate><title>2-SACCHARINYLMETHYL(ARYL OR ARYLHYDROXY) ACETATES, OR THEIR SALTS FORMED BY ADDITION OF ACIDS TO THESE BASIC COMPOUNDS, OR THEIR SALTS FORMED BY BASES ADDITION TO THESE ACID COMPOUNDS, AND PHARMACEUTICAL COMPOSITION INHIBITING ACTIVITY OF PROTEOLYTIC ENZYMES</title><author>RICHARD POL DANLEP ; LI GAMILTON LEJTIMER</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-epo_espacenet_RU2081871C13</frbrgroupid><rsrctype>patents</rsrctype><prefilter>patents</prefilter><language>eng</language><creationdate>1997</creationdate><topic>CHEMISTRY</topic><topic>HETEROCYCLIC COMPOUNDS</topic><topic>HUMAN NECESSITIES</topic><topic>HYGIENE</topic><topic>MEDICAL OR VETERINARY SCIENCE</topic><topic>METALLURGY</topic><topic>ORGANIC CHEMISTRY</topic><topic>PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES</topic><topic>SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS</topic><toplevel>online_resources</toplevel><creatorcontrib>RICHARD POL DANLEP</creatorcontrib><creatorcontrib>LI GAMILTON LEJTIMER</creatorcontrib><collection>esp@cenet</collection></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext_linktorsrc</fulltext></delivery><addata><au>RICHARD POL DANLEP</au><au>LI GAMILTON LEJTIMER</au><format>patent</format><genre>patent</genre><ristype>GEN</ristype><title>2-SACCHARINYLMETHYL(ARYL OR ARYLHYDROXY) ACETATES, OR THEIR SALTS FORMED BY ADDITION OF ACIDS TO THESE BASIC COMPOUNDS, OR THEIR SALTS FORMED BY BASES ADDITION TO THESE ACID COMPOUNDS, AND PHARMACEUTICAL COMPOSITION INHIBITING ACTIVITY OF PROTEOLYTIC ENZYMES</title><date>1997-06-20</date><risdate>1997</risdate><abstract>4-R -R -2-Saccharinylmethyl aryl and aryloxy acetates, having the formula: wherein: m is zero or one, n is zero or one, and the sum of m + n is zero or one; R is hydrogen or lower-alkyl; R is hydrogen or lower-alkyl; R is phenyl or phenyl substituted by from one to three, the same or different, members of the group consisting of lower-alkyl perfluorolower-alkyl, lower-alkoxy and halogen; R is hydrogen, halogen, lower-alkyl, perfluorolower-alkyl, perchlorolower-alkyl, lower-alkenyl, lower-alkynyl, cyano, carboxamido, amino, lower-alkylamino, dilower-alkylamino, lower-alkoxy, benzyloxy, lower-alkoxycarbonyl, hydroxy or phenyl; and R is hydrogen or from one to two substituents in any of the 5-, 6- or 7-positions. The compounds of the present invention inhibit the activity of serine proteases, specifically human leukocyte elastase and the chymotrypsin-like enzymes, and are thus useful in the treatment of degenerative disease conditions such as emphysema, rheumatoid arthritis, pancreatitis, cysticfibrosis, chronic bronchitis, adult respiratory distress syndrome, inflammatory bowel disease, psoriasis, bullous pemphigoid and alpha-1-antitrypsin deficiency.</abstract><edition>6</edition><oa>free_for_read</oa></addata></record>
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subjects CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
title 2-SACCHARINYLMETHYL(ARYL OR ARYLHYDROXY) ACETATES, OR THEIR SALTS FORMED BY ADDITION OF ACIDS TO THESE BASIC COMPOUNDS, OR THEIR SALTS FORMED BY BASES ADDITION TO THESE ACID COMPOUNDS, AND PHARMACEUTICAL COMPOSITION INHIBITING ACTIVITY OF PROTEOLYTIC ENZYMES
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