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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Hauptverfasser: 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
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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,
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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,</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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