N-SUBSTITUTED AZEHETEROCYCLIC CARBOXYLIC ACIDS AND THEIR ESTERS
N-Substituted azaheterocyclic carboxylic acids and their esters, of the formula:- wherein: n is a positive whole integer 2, 3 or 4; m is zero; R4 is hydrogen, or lower alkyl of from 1 to 4 carbon atoms; the dotted line represents an optional bond; R5 is hydrogen, or hydroxy, or when the dotted line...
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| creator | WILLIAM E. BONDINELL JOHN J. LAFFERTY CHARLES L. ZIRKLE |
| description | N-Substituted azaheterocyclic carboxylic acids and their esters, of the formula:- wherein: n is a positive whole integer 2, 3 or 4; m is zero; R4 is hydrogen, or lower alkyl of from 1 to 4 carbon atoms; the dotted line represents an optional bond; R5 is hydrogen, or hydroxy, or when the dotted line forms a double bond, hydrogen; B is wherein R1 is hydrogen, fluorine, chlorine, methyl or methoxy; Y is -C(A)=C(R3)-, -CH -CHR3- in which case n is 3 or 4, or -C IDENTICAL C-, wherein R2 is hydrogen, fluorine, chlorine, methyl or methoxy, R3 is hydrogen or methyl, and A is 2-thienyl, 3-thienyl or cyclohexyl; or B-Y is (cyclohexyl)2C=C(R3)-; or when Y is a -C(A)=C(R3)- m may also be one: or a pharmaceutically acceptable acid addition salt thereof, useful as inhibitors of GABA uptake, are prepared by reacting an appropriate N-alkylating derivative with an ester of an N-unsubstituted azaheterocyclic carboxylic acid followed by hydrolysis of the ester. |
| format | Patent |
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ZIRKLE</creatorcontrib><description>N-Substituted azaheterocyclic carboxylic acids and their esters, of the formula:- wherein: n is a positive whole integer 2, 3 or 4; m is zero; R4 is hydrogen, or lower alkyl of from 1 to 4 carbon atoms; the dotted line represents an optional bond; R5 is hydrogen, or hydroxy, or when the dotted line forms a double bond, hydrogen; B is wherein R1 is hydrogen, fluorine, chlorine, methyl or methoxy; Y is -C(A)=C(R3)-, -CH -CHR3- in which case n is 3 or 4, or -C IDENTICAL C-, wherein R2 is hydrogen, fluorine, chlorine, methyl or methoxy, R3 is hydrogen or methyl, and A is 2-thienyl, 3-thienyl or cyclohexyl; or B-Y is (cyclohexyl)2C=C(R3)-; or when Y is a -C(A)=C(R3)- m may also be one: or a pharmaceutically acceptable acid addition salt thereof, useful as inhibitors of GABA uptake, are prepared by reacting an appropriate N-alkylating derivative with an ester of an N-unsubstituted azaheterocyclic carboxylic acid followed by hydrolysis of the ester.</description><edition>4</edition><language>eng</language><subject>ACYCLIC OR CARBOCYCLIC COMPOUNDS ; 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>1986</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=19860522&DB=EPODOC&CC=AU&NR=552050B2$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,308,780,885,25563,76418</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=19860522&DB=EPODOC&CC=AU&NR=552050B2$$EView_record_in_European_Patent_Office$$FView_record_in_$$GEuropean_Patent_Office$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>WILLIAM E. 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ZIRKLE</creatorcontrib><title>N-SUBSTITUTED AZEHETEROCYCLIC CARBOXYLIC ACIDS AND THEIR ESTERS</title><description>N-Substituted azaheterocyclic carboxylic acids and their esters, of the formula:- wherein: n is a positive whole integer 2, 3 or 4; m is zero; R4 is hydrogen, or lower alkyl of from 1 to 4 carbon atoms; the dotted line represents an optional bond; R5 is hydrogen, or hydroxy, or when the dotted line forms a double bond, hydrogen; B is wherein R1 is hydrogen, fluorine, chlorine, methyl or methoxy; Y is -C(A)=C(R3)-, -CH -CHR3- in which case n is 3 or 4, or -C IDENTICAL C-, wherein R2 is hydrogen, fluorine, chlorine, methyl or methoxy, R3 is hydrogen or methyl, and A is 2-thienyl, 3-thienyl or cyclohexyl; or B-Y is (cyclohexyl)2C=C(R3)-; or when Y is a -C(A)=C(R3)- m may also be one: or a pharmaceutically acceptable acid addition salt thereof, useful as inhibitors of GABA uptake, are prepared by reacting an appropriate N-alkylating derivative with an ester of an N-unsubstituted azaheterocyclic carboxylic acid followed by hydrolysis of the ester.</description><subject>ACYCLIC OR CARBOCYCLIC COMPOUNDS</subject><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>1986</creationdate><recordtype>patent</recordtype><sourceid>EVB</sourceid><recordid>eNrjZLD30w0OdQoO8QwJDXF1UXCMcvVwDXEN8neOdPbxdFZwdgxy8o-IBDEdnT1dghUc_VwUQjxcPYMUXIOB6oJ5GFjTEnOKU3mhNDeDgptriLOHbmpBfnxqcUFicmpeakm8Y6ipqZGBqYGTk5ExEUoAVJEqTA</recordid><startdate>19860522</startdate><enddate>19860522</enddate><creator>WILLIAM E. 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ZIRKLE</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-epo_espacenet_AU552050BB23</frbrgroupid><rsrctype>patents</rsrctype><prefilter>patents</prefilter><language>eng</language><creationdate>1986</creationdate><topic>ACYCLIC OR CARBOCYCLIC COMPOUNDS</topic><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>WILLIAM E. BONDINELL</creatorcontrib><creatorcontrib>JOHN J. LAFFERTY</creatorcontrib><creatorcontrib>CHARLES L. ZIRKLE</creatorcontrib><collection>esp@cenet</collection></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext_linktorsrc</fulltext></delivery><addata><au>WILLIAM E. BONDINELL</au><au>JOHN J. LAFFERTY</au><au>CHARLES L. ZIRKLE</au><format>patent</format><genre>patent</genre><ristype>GEN</ristype><title>N-SUBSTITUTED AZEHETEROCYCLIC CARBOXYLIC ACIDS AND THEIR ESTERS</title><date>1986-05-22</date><risdate>1986</risdate><abstract>N-Substituted azaheterocyclic carboxylic acids and their esters, of the formula:- wherein: n is a positive whole integer 2, 3 or 4; m is zero; R4 is hydrogen, or lower alkyl of from 1 to 4 carbon atoms; the dotted line represents an optional bond; R5 is hydrogen, or hydroxy, or when the dotted line forms a double bond, hydrogen; B is wherein R1 is hydrogen, fluorine, chlorine, methyl or methoxy; Y is -C(A)=C(R3)-, -CH -CHR3- in which case n is 3 or 4, or -C IDENTICAL C-, wherein R2 is hydrogen, fluorine, chlorine, methyl or methoxy, R3 is hydrogen or methyl, and A is 2-thienyl, 3-thienyl or cyclohexyl; or B-Y is (cyclohexyl)2C=C(R3)-; or when Y is a -C(A)=C(R3)- m may also be one: or a pharmaceutically acceptable acid addition salt thereof, useful as inhibitors of GABA uptake, are prepared by reacting an appropriate N-alkylating derivative with an ester of an N-unsubstituted azaheterocyclic carboxylic acid followed by hydrolysis of the ester.</abstract><edition>4</edition><oa>free_for_read</oa></addata></record> |
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| subjects | ACYCLIC OR CARBOCYCLIC COMPOUNDS 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 | N-SUBSTITUTED AZEHETEROCYCLIC CARBOXYLIC ACIDS AND THEIR ESTERS |
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