EXCITATORY AMINO ACID RECEPTOR ANTAGONISTS
본 발명은 흥분성 아미노산 수용체 길항물질제로서 유용하고 신경 질환의 치료에 유용한 신규한 데카하이드로이소퀴놀린 화합물을 제공한다. 본 발명은 또한 데카하이드로이소퀴놀린 뿐 아니라, 그의 합성에 신규한 중간체의 제조를 위한 합성 방법을 제공한다. This invention provides novel decahydroisoquinoline compounds which are useful as excitatory amino acid receptor antagonists and in the treatment of neurological...
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Main Authors | , , , , , , , , , |
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Format | Patent |
Language | English Korean |
Published |
15.12.2000
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Edition | 7 |
Subjects | |
Online Access | Get full text |
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Abstract | 본 발명은 흥분성 아미노산 수용체 길항물질제로서 유용하고 신경 질환의 치료에 유용한 신규한 데카하이드로이소퀴놀린 화합물을 제공한다. 본 발명은 또한 데카하이드로이소퀴놀린 뿐 아니라, 그의 합성에 신규한 중간체의 제조를 위한 합성 방법을 제공한다.
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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AbstractList | 본 발명은 흥분성 아미노산 수용체 길항물질제로서 유용하고 신경 질환의 치료에 유용한 신규한 데카하이드로이소퀴놀린 화합물을 제공한다. 본 발명은 또한 데카하이드로이소퀴놀린 뿐 아니라, 그의 합성에 신규한 중간체의 제조를 위한 합성 방법을 제공한다.
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, |
Author | LUNN, WILLIAM HENRY WALKER HARKNESS, ALLEN ROBERT ORNSTEIN, PAUL LESLIE MARTINELLI, MICHAEL JOHN ARNOLD, MACKLIN BRIAN BERTSCH, CARL FRANKLIN HANSEN, MARVIN MARTIN AUGENSTEIN, NANCY KAY SCHOEPP, DARRYLE DARWIN HUFF, BRET EUGENE |
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Snippet | 본 발명은 흥분성 아미노산 수용체 길항물질제로서 유용하고 신경 질환의 치료에 유용한 신규한 데카하이드로이소퀴놀린 화합물을 제공한다. 본 발명은 또한 데카하이드로이소퀴놀린 뿐 아니라, 그의 합성에 신규한 중간체의 제조를 위한 합성 방법을 제공한다.
This invention... |
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Title | EXCITATORY AMINO ACID RECEPTOR ANTAGONISTS |
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