Rapamycin hdroxyesters, process for their preparation and pharmaceutical compositions containing them
A compound of structure (I) wherein R 1 and R 2 are each, independently, hydrogen or - CO(CR 3 R 4 ) b (CR 5 R 6 ) d CR 7 R 8 R 9 ; R 3 and R 4 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, trifluoromethyl, or -F; R 5 and R 6 are each, independently, hydrogen, alkyl, alkenyl, alkynyl,...
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creator | CHRISTINA LOUISE LEONE JERAULD STANLEY SKOTNICKI GUY ALAN SCHIEHSER |
description | A compound of structure (I)
wherein R 1 and R 2 are each, independently, hydrogen or - CO(CR 3 R 4 ) b (CR 5 R 6 ) d CR 7 R 8 R 9 ;
R 3 and R 4 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, trifluoromethyl, or -F;
R 5 and R 6 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, -(CR 3 R 4 ) f OR 10 , -CF 3 , -F, or -CO 2 R 11 , or R 5 and R 6 may be taken together to form X or a cycloalkyl ring that is optionally mono-, di-, or tri-substituted with - (CR 3 R 4 ) f OR 10 ;
R 7 is hydrogen, alkyl, alkenyl, alkynyl, -(CR 3 R 4 ) f OR 10 , -CF 3 , -F, or -CO 2 R 11 ;
R 8 and R 9 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, -(CR 3 R 4 ) f OR 10 , -CF 3 , -F, or -CO 2 R 11 , or R 8 and R 9 may be taken together to form X or a cycloalkyl ring that is optionally mono-, di-, or tri-substituted with -(CR 3 R 4 ) f OR 10 ;
R 10 is hydrogen, alkyl, alkenyl, alkynyl, tri-(alkyl)silyl, tri-(alkyl)silylethyl, triphenylmethyl, benzyl, alkoxymethyl, tri-(alkyl)silylethoxymethyl, chloroethyl, or tetrahydropyranyl;
R 11 is hydrogen, alkyl, alkenyl, alkynyl, or phenylalkyl;
X is 5-(2,2-dialkyl)[1,3]dioxanyl, 5-(2,2-dicycloalkyl)[1,3]dioxanyl, 4-(2,2-dialkyl)[1,3]-dioxanyl, 4-(2,2-dicycloalkyl)[1,3]dioxanyl, 4-(2,2-dialkyl)[1,3]dioxalanyl, or 4-(2,2-dicycloalkyl)[1,3]dioxalanyl;
b = 0-6;
d = 0-6; and
f = 0-6
with the proviso that R 1 and R 2 are both not hydrogen and further provided that either R 1 or R 2 contains at least one -(CR 3 R 4 ) f OR 10 , X, or -(CR 3 R 4 ) f OR 10 substituted cycloalkyl group, or a pharmaceutically acceptable salt thereof which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent. |
format | Patent |
fullrecord | <record><control><sourceid>epo_EVB</sourceid><recordid>TN_cdi_epo_espacenet_HK1048816A1</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><sourcerecordid>HK1048816A1</sourcerecordid><originalsourceid>FETCH-epo_espacenet_HK1048816A13</originalsourceid><addsrcrecordid>eNqNjEEKwlAMRLtxIeodcgAFiyLdiigFd-K-hN_UfuhPQvIFe3tb8ACuhpk3M8uCHqiYxhAZ-tbkM5JnMt-CmgRyh04Mck_RpoQUDXMUBuQWtEdLGOidY8ABgiQVjzP2yXDGyJFf8ziti0WHg9Pmp6sCbtfnpd6RSkOu0wtTbup7uT9WVXk6l4c_Kl9jIkAo</addsrcrecordid><sourcetype>Open Access Repository</sourcetype><iscdi>true</iscdi><recordtype>patent</recordtype></control><display><type>patent</type><title>Rapamycin hdroxyesters, process for their preparation and pharmaceutical compositions containing them</title><source>esp@cenet</source><creator>CHRISTINA LOUISE LEONE ; JERAULD STANLEY SKOTNICKI ; GUY ALAN SCHIEHSER</creator><creatorcontrib>CHRISTINA LOUISE LEONE ; JERAULD STANLEY SKOTNICKI ; GUY ALAN SCHIEHSER</creatorcontrib><description>A compound of structure (I)
wherein R 1 and R 2 are each, independently, hydrogen or - CO(CR 3 R 4 ) b (CR 5 R 6 ) d CR 7 R 8 R 9 ;
R 3 and R 4 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, trifluoromethyl, or -F;
R 5 and R 6 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, -(CR 3 R 4 ) f OR 10 , -CF 3 , -F, or -CO 2 R 11 , or R 5 and R 6 may be taken together to form X or a cycloalkyl ring that is optionally mono-, di-, or tri-substituted with - (CR 3 R 4 ) f OR 10 ;
R 7 is hydrogen, alkyl, alkenyl, alkynyl, -(CR 3 R 4 ) f OR 10 , -CF 3 , -F, or -CO 2 R 11 ;
R 8 and R 9 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, -(CR 3 R 4 ) f OR 10 , -CF 3 , -F, or -CO 2 R 11 , or R 8 and R 9 may be taken together to form X or a cycloalkyl ring that is optionally mono-, di-, or tri-substituted with -(CR 3 R 4 ) f OR 10 ;
R 10 is hydrogen, alkyl, alkenyl, alkynyl, tri-(alkyl)silyl, tri-(alkyl)silylethyl, triphenylmethyl, benzyl, alkoxymethyl, tri-(alkyl)silylethoxymethyl, chloroethyl, or tetrahydropyranyl;
R 11 is hydrogen, alkyl, alkenyl, alkynyl, or phenylalkyl;
X is 5-(2,2-dialkyl)[1,3]dioxanyl, 5-(2,2-dicycloalkyl)[1,3]dioxanyl, 4-(2,2-dialkyl)[1,3]-dioxanyl, 4-(2,2-dicycloalkyl)[1,3]dioxanyl, 4-(2,2-dialkyl)[1,3]dioxalanyl, or 4-(2,2-dicycloalkyl)[1,3]dioxalanyl;
b = 0-6;
d = 0-6; and
f = 0-6
with the proviso that R 1 and R 2 are both not hydrogen and further provided that either R 1 or R 2 contains at least one -(CR 3 R 4 ) f OR 10 , X, or -(CR 3 R 4 ) f OR 10 substituted cycloalkyl group, or a pharmaceutically acceptable salt thereof which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.</description><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>2003</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&date=20030417&DB=EPODOC&CC=HK&NR=1048816A1$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,308,776,881,25543,76294</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=20030417&DB=EPODOC&CC=HK&NR=1048816A1$$EView_record_in_European_Patent_Office$$FView_record_in_$$GEuropean_Patent_Office$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>CHRISTINA LOUISE LEONE</creatorcontrib><creatorcontrib>JERAULD STANLEY SKOTNICKI</creatorcontrib><creatorcontrib>GUY ALAN SCHIEHSER</creatorcontrib><title>Rapamycin hdroxyesters, process for their preparation and pharmaceutical compositions containing them</title><description>A compound of structure (I)
wherein R 1 and R 2 are each, independently, hydrogen or - CO(CR 3 R 4 ) b (CR 5 R 6 ) d CR 7 R 8 R 9 ;
R 3 and R 4 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, trifluoromethyl, or -F;
R 5 and R 6 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, -(CR 3 R 4 ) f OR 10 , -CF 3 , -F, or -CO 2 R 11 , or R 5 and R 6 may be taken together to form X or a cycloalkyl ring that is optionally mono-, di-, or tri-substituted with - (CR 3 R 4 ) f OR 10 ;
R 7 is hydrogen, alkyl, alkenyl, alkynyl, -(CR 3 R 4 ) f OR 10 , -CF 3 , -F, or -CO 2 R 11 ;
R 8 and R 9 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, -(CR 3 R 4 ) f OR 10 , -CF 3 , -F, or -CO 2 R 11 , or R 8 and R 9 may be taken together to form X or a cycloalkyl ring that is optionally mono-, di-, or tri-substituted with -(CR 3 R 4 ) f OR 10 ;
R 10 is hydrogen, alkyl, alkenyl, alkynyl, tri-(alkyl)silyl, tri-(alkyl)silylethyl, triphenylmethyl, benzyl, alkoxymethyl, tri-(alkyl)silylethoxymethyl, chloroethyl, or tetrahydropyranyl;
R 11 is hydrogen, alkyl, alkenyl, alkynyl, or phenylalkyl;
X is 5-(2,2-dialkyl)[1,3]dioxanyl, 5-(2,2-dicycloalkyl)[1,3]dioxanyl, 4-(2,2-dialkyl)[1,3]-dioxanyl, 4-(2,2-dicycloalkyl)[1,3]dioxanyl, 4-(2,2-dialkyl)[1,3]dioxalanyl, or 4-(2,2-dicycloalkyl)[1,3]dioxalanyl;
b = 0-6;
d = 0-6; and
f = 0-6
with the proviso that R 1 and R 2 are both not hydrogen and further provided that either R 1 or R 2 contains at least one -(CR 3 R 4 ) f OR 10 , X, or -(CR 3 R 4 ) f OR 10 substituted cycloalkyl group, or a pharmaceutically acceptable salt thereof which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.</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>2003</creationdate><recordtype>patent</recordtype><sourceid>EVB</sourceid><recordid>eNqNjEEKwlAMRLtxIeodcgAFiyLdiigFd-K-hN_UfuhPQvIFe3tb8ACuhpk3M8uCHqiYxhAZ-tbkM5JnMt-CmgRyh04Mck_RpoQUDXMUBuQWtEdLGOidY8ABgiQVjzP2yXDGyJFf8ziti0WHg9Pmp6sCbtfnpd6RSkOu0wtTbup7uT9WVXk6l4c_Kl9jIkAo</recordid><startdate>20030417</startdate><enddate>20030417</enddate><creator>CHRISTINA LOUISE LEONE</creator><creator>JERAULD STANLEY SKOTNICKI</creator><creator>GUY ALAN SCHIEHSER</creator><scope>EVB</scope></search><sort><creationdate>20030417</creationdate><title>Rapamycin hdroxyesters, process for their preparation and pharmaceutical compositions containing them</title><author>CHRISTINA LOUISE LEONE ; JERAULD STANLEY SKOTNICKI ; GUY ALAN SCHIEHSER</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-epo_espacenet_HK1048816A13</frbrgroupid><rsrctype>patents</rsrctype><prefilter>patents</prefilter><language>eng</language><creationdate>2003</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>CHRISTINA LOUISE LEONE</creatorcontrib><creatorcontrib>JERAULD STANLEY SKOTNICKI</creatorcontrib><creatorcontrib>GUY ALAN SCHIEHSER</creatorcontrib><collection>esp@cenet</collection></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext_linktorsrc</fulltext></delivery><addata><au>CHRISTINA LOUISE LEONE</au><au>JERAULD STANLEY SKOTNICKI</au><au>GUY ALAN SCHIEHSER</au><format>patent</format><genre>patent</genre><ristype>GEN</ristype><title>Rapamycin hdroxyesters, process for their preparation and pharmaceutical compositions containing them</title><date>2003-04-17</date><risdate>2003</risdate><abstract>A compound of structure (I)
wherein R 1 and R 2 are each, independently, hydrogen or - CO(CR 3 R 4 ) b (CR 5 R 6 ) d CR 7 R 8 R 9 ;
R 3 and R 4 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, trifluoromethyl, or -F;
R 5 and R 6 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, -(CR 3 R 4 ) f OR 10 , -CF 3 , -F, or -CO 2 R 11 , or R 5 and R 6 may be taken together to form X or a cycloalkyl ring that is optionally mono-, di-, or tri-substituted with - (CR 3 R 4 ) f OR 10 ;
R 7 is hydrogen, alkyl, alkenyl, alkynyl, -(CR 3 R 4 ) f OR 10 , -CF 3 , -F, or -CO 2 R 11 ;
R 8 and R 9 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, -(CR 3 R 4 ) f OR 10 , -CF 3 , -F, or -CO 2 R 11 , or R 8 and R 9 may be taken together to form X or a cycloalkyl ring that is optionally mono-, di-, or tri-substituted with -(CR 3 R 4 ) f OR 10 ;
R 10 is hydrogen, alkyl, alkenyl, alkynyl, tri-(alkyl)silyl, tri-(alkyl)silylethyl, triphenylmethyl, benzyl, alkoxymethyl, tri-(alkyl)silylethoxymethyl, chloroethyl, or tetrahydropyranyl;
R 11 is hydrogen, alkyl, alkenyl, alkynyl, or phenylalkyl;
X is 5-(2,2-dialkyl)[1,3]dioxanyl, 5-(2,2-dicycloalkyl)[1,3]dioxanyl, 4-(2,2-dialkyl)[1,3]-dioxanyl, 4-(2,2-dicycloalkyl)[1,3]dioxanyl, 4-(2,2-dialkyl)[1,3]dioxalanyl, or 4-(2,2-dicycloalkyl)[1,3]dioxalanyl;
b = 0-6;
d = 0-6; and
f = 0-6
with the proviso that R 1 and R 2 are both not hydrogen and further provided that either R 1 or R 2 contains at least one -(CR 3 R 4 ) f OR 10 , X, or -(CR 3 R 4 ) f OR 10 substituted cycloalkyl group, or a pharmaceutically acceptable salt thereof which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.</abstract><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 | Rapamycin hdroxyesters, process for their preparation and pharmaceutical compositions containing them |
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