Anregende Aminosäuren Antagonisten
This invention provides novel decahydroisoquinoline compounds which are useful as excitatory amino acid receptor antagonists and in the treatment of neurological disorders. This invention also provides synthetic methods for preparing decahydroisoquinolines, as well as, novel intermediates in the syn...
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creator | ARNOLD, MACKLIN BRIAN HANSEN, MARVIN MARTIN SCHOEPP, DARRYLE DARWIN AUGENSTEIN, NANCY KAY ORNSTEIN, PAUL LESLIE MARTINELLI, MICHAEL JOHN BERTSCH, CARL FRANKLIN HARKNESS, ALLEN ROBERT HUFF, BRET EUGENE LUNN, WILLIAM HENRY WALKER |
description | This invention provides novel decahydroisoquinoline compounds which are useful as excitatory amino acid receptor antagonists and in the treatment of neurological disorders. This invention also provides synthetic methods for preparing decahydroisoquinolines, as well as, novel intermediates in the synthesis thereof. The novel pharmaceutical compounds have the formula wherein: R is hydrogen, C1-C10 alkyl, arylalkyl, alkoxycarbonyl or acyl; R is hydrogen, C1-C6 alkyl, substituted alkyl, cycloalkyl, or arylalkyl; R is CO2H, SO3H, CONHSO2R , or a group of formula W is (CH2)n, S, SO, SO2; Y is CHR , NR , O, S, SO, or SO2; Z is NR , CHR , or CH; or W and Y together are HC=CH or C IDENTICAL C, or Y and Z together are HC=CH or C IDENTICAL C; R is hydrogen, C1-C4 alkyl, phenyl, or acyl; R is hydrogen, C1-C4 alkyl, CF3, phenyl, hydroxy, amino, bromo, iodo, or chloro; R is acyl; R is independently hydrogen, C1-C4 alkyl, phenyl, or substituted phenyl; R is C1-C4 alkyl or tetrazole-5-yl; and n is 0, 1, or 2; provided that when Y is NR , O, S, SO, or SO2, W is (CH2)n and Z is CHR or CH; further provided that when W is S, SO, or SO2, Y is CHR , Z is CHR or CH, or Y and Z together are HC=CH or C IDENTICAL C; further provided that when W and Z are CH2, Y is not S; further provided that when W and Y together are HC=CH or C IDENTICAL C, Z is CHR ; or a pharmaceutically acceptable salt thereof. 1, |
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This invention also provides synthetic methods for preparing decahydroisoquinolines, as well as, novel intermediates in the synthesis thereof. The novel pharmaceutical compounds have the formula wherein: R is hydrogen, C1-C10 alkyl, arylalkyl, alkoxycarbonyl or acyl; R is hydrogen, C1-C6 alkyl, substituted alkyl, cycloalkyl, or arylalkyl; R is CO2H, SO3H, CONHSO2R , or a group of formula W is (CH2)n, S, SO, SO2; Y is CHR , NR , O, S, SO, or SO2; Z is NR , CHR , or CH; or W and Y together are HC=CH or C IDENTICAL C, or Y and Z together are HC=CH or C IDENTICAL C; R is hydrogen, C1-C4 alkyl, phenyl, or acyl; R is hydrogen, C1-C4 alkyl, CF3, phenyl, hydroxy, amino, bromo, iodo, or chloro; R is acyl; R is independently hydrogen, C1-C4 alkyl, phenyl, or substituted phenyl; R is C1-C4 alkyl or tetrazole-5-yl; and n is 0, 1, or 2; provided that when Y is NR , O, S, SO, or SO2, W is (CH2)n and Z is CHR or CH; further provided that when W is S, SO, or SO2, Y is CHR , Z is CHR or CH, or Y and Z together are HC=CH or C IDENTICAL C; further provided that when W and Z are CH2, Y is not S; further provided that when W and Y together are HC=CH or C IDENTICAL C, Z is CHR ; or a pharmaceutically acceptable salt thereof. 1,</description><edition>7</edition><language>ger</language><subject>ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAININGELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN,SULFUR, SELENIUM OR TELLURIUM ; 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>2004</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=20040617&DB=EPODOC&CC=DE&NR=69332754T2$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,308,780,885,25564,76547</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=20040617&DB=EPODOC&CC=DE&NR=69332754T2$$EView_record_in_European_Patent_Office$$FView_record_in_$$GEuropean_Patent_Office$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>ARNOLD, MACKLIN BRIAN</creatorcontrib><creatorcontrib>HANSEN, MARVIN MARTIN</creatorcontrib><creatorcontrib>SCHOEPP, DARRYLE DARWIN</creatorcontrib><creatorcontrib>AUGENSTEIN, NANCY KAY</creatorcontrib><creatorcontrib>ORNSTEIN, PAUL LESLIE</creatorcontrib><creatorcontrib>MARTINELLI, MICHAEL JOHN</creatorcontrib><creatorcontrib>BERTSCH, CARL FRANKLIN</creatorcontrib><creatorcontrib>HARKNESS, ALLEN ROBERT</creatorcontrib><creatorcontrib>HUFF, BRET EUGENE</creatorcontrib><creatorcontrib>LUNN, WILLIAM HENRY WALKER</creatorcontrib><title>Anregende Aminosäuren Antagonisten</title><description>This invention provides novel decahydroisoquinoline compounds which are useful as excitatory amino acid receptor antagonists and in the treatment of neurological disorders. This invention also provides synthetic methods for preparing decahydroisoquinolines, as well as, novel intermediates in the synthesis thereof. The novel pharmaceutical compounds have the formula wherein: R is hydrogen, C1-C10 alkyl, arylalkyl, alkoxycarbonyl or acyl; R is hydrogen, C1-C6 alkyl, substituted alkyl, cycloalkyl, or arylalkyl; R is CO2H, SO3H, CONHSO2R , or a group of formula W is (CH2)n, S, SO, SO2; Y is CHR , NR , O, S, SO, or SO2; Z is NR , CHR , or CH; or W and Y together are HC=CH or C IDENTICAL C, or Y and Z together are HC=CH or C IDENTICAL C; R is hydrogen, C1-C4 alkyl, phenyl, or acyl; R is hydrogen, C1-C4 alkyl, CF3, phenyl, hydroxy, amino, bromo, iodo, or chloro; R is acyl; R is independently hydrogen, C1-C4 alkyl, phenyl, or substituted phenyl; R is C1-C4 alkyl or tetrazole-5-yl; and n is 0, 1, or 2; provided that when Y is NR , O, S, SO, or SO2, W is (CH2)n and Z is CHR or CH; further provided that when W is S, SO, or SO2, Y is CHR , Z is CHR or CH, or Y and Z together are HC=CH or C IDENTICAL C; further provided that when W and Z are CH2, Y is not S; further provided that when W and Y together are HC=CH or C IDENTICAL C, Z is CHR ; or a pharmaceutically acceptable salt thereof. 1,</description><subject>ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAININGELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN,SULFUR, SELENIUM OR TELLURIUM</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>2004</creationdate><recordtype>patent</recordtype><sourceid>EVB</sourceid><recordid>eNrjZFB2zCtKTU_NS0lVcMzNzMsvPryktCg1T8ExryQxPT8vs7gkNY-HgTUtMac4lRdKczMoubmGOHvophbkx6cWFyQmp-allsS7uJpZGhsbmZuahIQYGROlCACO8ygY</recordid><startdate>20040617</startdate><enddate>20040617</enddate><creator>ARNOLD, MACKLIN BRIAN</creator><creator>HANSEN, MARVIN MARTIN</creator><creator>SCHOEPP, DARRYLE DARWIN</creator><creator>AUGENSTEIN, NANCY KAY</creator><creator>ORNSTEIN, PAUL LESLIE</creator><creator>MARTINELLI, MICHAEL JOHN</creator><creator>BERTSCH, CARL FRANKLIN</creator><creator>HARKNESS, ALLEN ROBERT</creator><creator>HUFF, BRET EUGENE</creator><creator>LUNN, WILLIAM HENRY WALKER</creator><scope>EVB</scope></search><sort><creationdate>20040617</creationdate><title>Anregende Aminosäuren Antagonisten</title><author>ARNOLD, MACKLIN BRIAN ; HANSEN, MARVIN MARTIN ; SCHOEPP, DARRYLE DARWIN ; AUGENSTEIN, NANCY KAY ; ORNSTEIN, PAUL LESLIE ; MARTINELLI, MICHAEL JOHN ; BERTSCH, CARL FRANKLIN ; HARKNESS, ALLEN ROBERT ; HUFF, BRET EUGENE ; LUNN, WILLIAM HENRY WALKER</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-epo_espacenet_DE69332754TT23</frbrgroupid><rsrctype>patents</rsrctype><prefilter>patents</prefilter><language>ger</language><creationdate>2004</creationdate><topic>ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAININGELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN,SULFUR, SELENIUM OR TELLURIUM</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>ARNOLD, MACKLIN BRIAN</creatorcontrib><creatorcontrib>HANSEN, MARVIN MARTIN</creatorcontrib><creatorcontrib>SCHOEPP, DARRYLE DARWIN</creatorcontrib><creatorcontrib>AUGENSTEIN, NANCY KAY</creatorcontrib><creatorcontrib>ORNSTEIN, PAUL LESLIE</creatorcontrib><creatorcontrib>MARTINELLI, MICHAEL JOHN</creatorcontrib><creatorcontrib>BERTSCH, CARL FRANKLIN</creatorcontrib><creatorcontrib>HARKNESS, ALLEN ROBERT</creatorcontrib><creatorcontrib>HUFF, BRET EUGENE</creatorcontrib><creatorcontrib>LUNN, WILLIAM HENRY WALKER</creatorcontrib><collection>esp@cenet</collection></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext_linktorsrc</fulltext></delivery><addata><au>ARNOLD, MACKLIN BRIAN</au><au>HANSEN, MARVIN MARTIN</au><au>SCHOEPP, DARRYLE DARWIN</au><au>AUGENSTEIN, NANCY KAY</au><au>ORNSTEIN, PAUL LESLIE</au><au>MARTINELLI, MICHAEL JOHN</au><au>BERTSCH, CARL FRANKLIN</au><au>HARKNESS, ALLEN ROBERT</au><au>HUFF, BRET EUGENE</au><au>LUNN, WILLIAM HENRY WALKER</au><format>patent</format><genre>patent</genre><ristype>GEN</ristype><title>Anregende Aminosäuren Antagonisten</title><date>2004-06-17</date><risdate>2004</risdate><abstract>This invention provides novel decahydroisoquinoline compounds which are useful as excitatory amino acid receptor antagonists and in the treatment of neurological disorders. This invention also provides synthetic methods for preparing decahydroisoquinolines, as well as, novel intermediates in the synthesis thereof. The novel pharmaceutical compounds have the formula wherein: R is hydrogen, C1-C10 alkyl, arylalkyl, alkoxycarbonyl or acyl; R is hydrogen, C1-C6 alkyl, substituted alkyl, cycloalkyl, or arylalkyl; R is CO2H, SO3H, CONHSO2R , or a group of formula W is (CH2)n, S, SO, SO2; Y is CHR , NR , O, S, SO, or SO2; Z is NR , CHR , or CH; or W and Y together are HC=CH or C IDENTICAL C, or Y and Z together are HC=CH or C IDENTICAL C; R is hydrogen, C1-C4 alkyl, phenyl, or acyl; R is hydrogen, C1-C4 alkyl, CF3, phenyl, hydroxy, amino, bromo, iodo, or chloro; R is acyl; R is independently hydrogen, C1-C4 alkyl, phenyl, or substituted phenyl; R is C1-C4 alkyl or tetrazole-5-yl; and n is 0, 1, or 2; provided that when Y is NR , O, S, SO, or SO2, W is (CH2)n and Z is CHR or CH; further provided that when W is S, SO, or SO2, Y is CHR , Z is CHR or CH, or Y and Z together are HC=CH or C IDENTICAL C; further provided that when W and Z are CH2, Y is not S; further provided that when W and Y together are HC=CH or C IDENTICAL C, Z is CHR ; or a pharmaceutically acceptable salt thereof. 1,</abstract><edition>7</edition><oa>free_for_read</oa></addata></record> |
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subjects | ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAININGELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN,SULFUR, SELENIUM OR TELLURIUM 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 | Anregende Aminosäuren Antagonisten |
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