ANTAGONISTAS DE RECEPTORES DE AMINOACIDOS EXCITADORES
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 | MICHAEL JOHN MARTINELLI ALLEN ROBERT HARKNESS CARL FRANKLIN BERTSCH DARRYLE DARWIN SCHOEPP NANCY KAY AUGENSTEIN PAUL LESLIE ORNSTEIN MARVIN MARTIN HANSEN BRET EUGENE HUFF MACKLIN BRIAN ARNOLD WILLIAM HENRY WALKER LUNN |
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, |
format | Patent |
fullrecord | <record><control><sourceid>epo_EVB</sourceid><recordid>TN_cdi_epo_espacenet_PT590789EE</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><sourcerecordid>PT590789EE</sourcerecordid><originalsourceid>FETCH-epo_espacenet_PT590789EE3</originalsourceid><addsrcrecordid>eNrjZDB19AtxdPf38wwOcQxWcHFVCHJ1dg0I8Q9yBfMcfT39_B2dPV38gxVcI5w9QxxdQFI8DKxpiTnFqbxQmptB3s01xNlDN7UgPz61uCAxOTUvtSQ-IMTU0sDcwtLV1ZiwCgBnrSdY</addsrcrecordid><sourcetype>Open Access Repository</sourcetype><iscdi>true</iscdi><recordtype>patent</recordtype></control><display><type>patent</type><title>ANTAGONISTAS DE RECEPTORES DE AMINOACIDOS EXCITADORES</title><source>esp@cenet</source><creator>MICHAEL JOHN MARTINELLI ; ALLEN ROBERT HARKNESS ; CARL FRANKLIN BERTSCH ; DARRYLE DARWIN SCHOEPP ; NANCY KAY AUGENSTEIN ; PAUL LESLIE ORNSTEIN ; MARVIN MARTIN HANSEN ; BRET EUGENE HUFF ; MACKLIN BRIAN ARNOLD ; WILLIAM HENRY WALKER LUNN</creator><creatorcontrib>MICHAEL JOHN MARTINELLI ; ALLEN ROBERT HARKNESS ; CARL FRANKLIN BERTSCH ; DARRYLE DARWIN SCHOEPP ; NANCY KAY AUGENSTEIN ; PAUL LESLIE ORNSTEIN ; MARVIN MARTIN HANSEN ; BRET EUGENE HUFF ; MACKLIN BRIAN ARNOLD ; WILLIAM HENRY WALKER LUNN</creatorcontrib><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><edition>7</edition><language>por</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>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=20030731&DB=EPODOC&CC=PT&NR=590789E$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,308,780,885,25564,76419</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=20030731&DB=EPODOC&CC=PT&NR=590789E$$EView_record_in_European_Patent_Office$$FView_record_in_$$GEuropean_Patent_Office$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>MICHAEL JOHN MARTINELLI</creatorcontrib><creatorcontrib>ALLEN ROBERT HARKNESS</creatorcontrib><creatorcontrib>CARL FRANKLIN BERTSCH</creatorcontrib><creatorcontrib>DARRYLE DARWIN SCHOEPP</creatorcontrib><creatorcontrib>NANCY KAY AUGENSTEIN</creatorcontrib><creatorcontrib>PAUL LESLIE ORNSTEIN</creatorcontrib><creatorcontrib>MARVIN MARTIN HANSEN</creatorcontrib><creatorcontrib>BRET EUGENE HUFF</creatorcontrib><creatorcontrib>MACKLIN BRIAN ARNOLD</creatorcontrib><creatorcontrib>WILLIAM HENRY WALKER LUNN</creatorcontrib><title>ANTAGONISTAS DE RECEPTORES DE AMINOACIDOS EXCITADORES</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>2003</creationdate><recordtype>patent</recordtype><sourceid>EVB</sourceid><recordid>eNrjZDB19AtxdPf38wwOcQxWcHFVCHJ1dg0I8Q9yBfMcfT39_B2dPV38gxVcI5w9QxxdQFI8DKxpiTnFqbxQmptB3s01xNlDN7UgPz61uCAxOTUvtSQ-IMTU0sDcwtLV1ZiwCgBnrSdY</recordid><startdate>20030731</startdate><enddate>20030731</enddate><creator>MICHAEL JOHN MARTINELLI</creator><creator>ALLEN ROBERT HARKNESS</creator><creator>CARL FRANKLIN BERTSCH</creator><creator>DARRYLE DARWIN SCHOEPP</creator><creator>NANCY KAY AUGENSTEIN</creator><creator>PAUL LESLIE ORNSTEIN</creator><creator>MARVIN MARTIN HANSEN</creator><creator>BRET EUGENE HUFF</creator><creator>MACKLIN BRIAN ARNOLD</creator><creator>WILLIAM HENRY WALKER LUNN</creator><scope>EVB</scope></search><sort><creationdate>20030731</creationdate><title>ANTAGONISTAS DE RECEPTORES DE AMINOACIDOS EXCITADORES</title><author>MICHAEL JOHN MARTINELLI ; ALLEN ROBERT HARKNESS ; CARL FRANKLIN BERTSCH ; DARRYLE DARWIN SCHOEPP ; NANCY KAY AUGENSTEIN ; PAUL LESLIE ORNSTEIN ; MARVIN MARTIN HANSEN ; BRET EUGENE HUFF ; MACKLIN BRIAN ARNOLD ; WILLIAM HENRY WALKER LUNN</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-epo_espacenet_PT590789EE3</frbrgroupid><rsrctype>patents</rsrctype><prefilter>patents</prefilter><language>por</language><creationdate>2003</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>MICHAEL JOHN MARTINELLI</creatorcontrib><creatorcontrib>ALLEN ROBERT HARKNESS</creatorcontrib><creatorcontrib>CARL FRANKLIN BERTSCH</creatorcontrib><creatorcontrib>DARRYLE DARWIN SCHOEPP</creatorcontrib><creatorcontrib>NANCY KAY AUGENSTEIN</creatorcontrib><creatorcontrib>PAUL LESLIE ORNSTEIN</creatorcontrib><creatorcontrib>MARVIN MARTIN HANSEN</creatorcontrib><creatorcontrib>BRET EUGENE HUFF</creatorcontrib><creatorcontrib>MACKLIN BRIAN ARNOLD</creatorcontrib><creatorcontrib>WILLIAM HENRY WALKER LUNN</creatorcontrib><collection>esp@cenet</collection></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext_linktorsrc</fulltext></delivery><addata><au>MICHAEL JOHN MARTINELLI</au><au>ALLEN ROBERT HARKNESS</au><au>CARL FRANKLIN BERTSCH</au><au>DARRYLE DARWIN SCHOEPP</au><au>NANCY KAY AUGENSTEIN</au><au>PAUL LESLIE ORNSTEIN</au><au>MARVIN MARTIN HANSEN</au><au>BRET EUGENE HUFF</au><au>MACKLIN BRIAN ARNOLD</au><au>WILLIAM HENRY WALKER LUNN</au><format>patent</format><genre>patent</genre><ristype>GEN</ristype><title>ANTAGONISTAS DE RECEPTORES DE AMINOACIDOS EXCITADORES</title><date>2003-07-31</date><risdate>2003</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 | ANTAGONISTAS DE RECEPTORES DE AMINOACIDOS EXCITADORES |
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