EXCITATORY AMINO ACID RECEPTOR ANTAGONISTS

• Main Authors: 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
• Format: Patent
• Language: English; Korean
• Published: 15.12.2000
• Edition: 7
• 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

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,