KR920700643A - 면역억제제 및 그 제조방법 - Google Patents

면역억제제 및 그 제조방법

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Publication number
KR920700643A
KR920700643A KR1019910700795A KR910700795A KR920700643A KR 920700643 A KR920700643 A KR 920700643A KR 1019910700795 A KR1019910700795 A KR 1019910700795A KR 910700795 A KR910700795 A KR 910700795A KR 920700643 A KR920700643 A KR 920700643A
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carbon atoms
alkyl
hydrogen
carbons
represented
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KR940008032B1 (ko
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히로시 나가세
코오지 카와이
슈우 마쯔모토
타카시 엔도오
요시아키 카쯔라
코오헤이 아라카와
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마에다 카쯔노수케
도오레 가부시키가이샤
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/12—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains three hetero rings
    • C07D491/18—Bridged systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/485—Morphinan derivatives, e.g. morphine, codeine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D489/00—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula:
    • C07D489/09—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: containing 4aH-8, 9 c-Iminoethano- phenanthro [4, 5-b, c, d] furan ring systems condensed with carbocyclic rings or ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/12—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains three hetero rings
    • C07D491/20—Spiro-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Emergency Medicine (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
  • Light Receiving Elements (AREA)
  • Amplifiers (AREA)

Abstract

내용 없음

Description

면역억제제 및 그 제조방법
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
제1도는 본 발명의 면역억제제인 나룩시인도올(NLL)의 농도변화에 의한 길항작용을 표시하는도 제2도는 나르톨인도올(NTI)의 농도변화에 의한 길항작용을 표시하는 도이다.

Claims (8)

  1. δ-오피오이드 안타고니스트 또는 그 약리학적으로 허용되는 염을 유효성분으로 하는 것을 특징으로 하는 면역억제제.
  2. 제1항에 있어서, 전기한 S-오피오이드 안타고니스트는 일반식[Ⅰ]
    [식중, R1은 탄소수 1내지 5의 알킬, 탄소수 3내지 6의 시클로알킬알킬, 탄소수 5내지 7의 시클로 알케닐알킬, 아릴, 아랄킬, 탄소수 4내지 5의 트랜스알케닐, 알릴 또는 푸란-2-일알킬을 표현하고, R2는 수소, 히드록시 또는 탄소수 1내지 5의 알카노일옥시를 표현하며, R3는 수소, 탄소수 1내지 5의 알킬 또는 탄소수 1내지 5의 알카노일을 표현하고, M은 질소 또는 메탄올 표현하며, R4와 R5는 별개로 수소, 불소, 염소, 취소, 아미노, 니트로, 탄소수 1내지 5의 알킬, 탄소수 1내지 5의 알콕시 또는 R4, R5을 결합하여 벤조를 표현한다]으로 표시되는 것을 특징으로 하는 면역억제제.
  3. 제1항에 있어서, 전기한 δ-오피오이드 안타로니스트는 일반식[2]
  4. 제2항에 있어서, 일반식[1]에 있어서, R1은 탄소수 1내지 5의 알킬, 탄소수 3내지 6의 시클로알킬알킬, 탄소수 5내지 7의 시클로알케닐, 알킬, 탄소수 7내지 10의 아랄킬, 탄소수 4내지 5의 트랜스알케닐, 알릴 또는 푸란-2-이소알킬이고, R2는 수소 또는 히드록시이며, R3은 수소이고, R4는 수소, 불소, 메틸, 메톡시 또는 니트로이며, R5는 수소, X는 산소 또는 NR6(여기서, R6은 수소 또는 탄소수 1내지 5의 알킬)인 것을 특징으로 하는 면역 어제제.
  5. 제4항에 있어서, 전기한 일반식[Ⅰ]로 표시되는 S-오피오이드 안타고니스트는 하기식[3]으로 표현되는 것을 특징으로 하는 면역억제제.
    [식중, R1은 탄소수 1내지 5의 알킬, 탄소수 3내지 6의 시클로알킬알킬, 탄소수 5내지 7의 시클로알케닐알킬, 아릴, 아랄킬, 탄소수 4내지 5의 트랜스알케닐, 알릴 또는 푸란-2-일알킬을 표현하고, R는 수소,히드록시 또는 탄소수 1내지 5의 알카노일옥시를 표현하며, R는 수소, 탄소수 1내지 5의 아킬 또는 탄소수 1내지 5의 알카노일을 표현하며, X는, 산소, 유황 또는 Y가 결합한 질소를 표현하고, Y는 수소 또는 탄소수 1내지 5의 알킬기를 표현하며, R와 R은 별개로 수소, 불소, 염소, 취소, 아미노, 니트로,탄소수 1내지5의 알킬, 탄소수 1내지 5의 알콕시 또는 R, R을 결합하여 벤조를 표현한다]으로 표시하는 것을 특징으로 하는 면역억제제.
  6. 제4항에 있어서, 전기한 일반식[1]으로 표현되는 δ-오피오이드 안타로니스트는 하기식[4]으로 표현되는 것을 특징으로 하는 면역억제제.
  7. 제4항에 있어서, 전기한 일반식[1]으로 표현되는 δ-오피오이드 안타로니스트는 하기식[5]으로 표현되는 것을 특징으로하는 면역억제제.
  8. 나르트렉숀 또는 그 염과 페닐히드라린 유도체를 용매 속 메탄술폰산 존재하에 반응시키는 것을 특징으로 하는 하기식[6].
    [식중, R은 수소, 염소, 취소, 불소, 메틸, 메톡시 또는 니트로를 표현한다]으로 표시되는 나트롤인도을 유도체의 제조방법.
    ※ 참고사항 : 최초출원 내용에 의하여 공개되는 것임.
KR1019910700795A 1989-11-28 1990-11-28 면역억제제 및 그 제조방법 Expired - Fee Related KR940008032B1 (ko)

Applications Claiming Priority (10)

Application Number Priority Date Filing Date Title
JP???1-?308491? 1989-11-28
JP1-308491 1989-11-28
JP30849189 1989-11-28
JP1-322160 1989-12-11
JP32216089 1989-12-11
JP???1-?322160? 1989-12-11
JP32694189 1989-12-15
JP1-326941 1989-12-15
JP???1-?326941? 1989-12-15
PCT/JP1990/001541 WO1991007966A1 (en) 1989-11-28 1990-11-28 Immunosuppressant and process for preparing the same

Publications (2)

Publication Number Publication Date
KR920700643A true KR920700643A (ko) 1992-08-10
KR940008032B1 KR940008032B1 (ko) 1994-09-01

Family

ID=27338974

Family Applications (1)

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KR1019910700795A Expired - Fee Related KR940008032B1 (ko) 1989-11-28 1990-11-28 면역억제제 및 그 제조방법

Country Status (14)

Country Link
US (1) US5332818A (ko)
EP (1) EP0456833B1 (ko)
JP (1) JP2906654B2 (ko)
KR (1) KR940008032B1 (ko)
AT (1) ATE119039T1 (ko)
AU (1) AU639053B2 (ko)
CA (1) CA2045481C (ko)
DE (1) DE69017434T2 (ko)
DK (1) DK0456833T3 (ko)
ES (1) ES2069100T3 (ko)
FI (1) FI913583A7 (ko)
GR (1) GR3015266T3 (ko)
NO (1) NO912940L (ko)
WO (1) WO1991007966A1 (ko)

Families Citing this family (23)

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US5852030A (en) * 1992-09-29 1998-12-22 Toray Industries, Inc. Indole derivatives, process for producing the same and medicinal uses of the same
JP3605825B2 (ja) * 1992-09-29 2004-12-22 東レ株式会社 インドール誘導体，その製造方法およびその医薬用途
CA2130457A1 (en) * 1992-12-22 1994-07-07 Hiroshi Nagase Antitussive
US5464841A (en) * 1993-11-08 1995-11-07 Univ Minnesota Use of delta opioid receptor antagonists to treat immunoregulatory disorders
SE9304236D0 (sv) * 1993-12-22 1993-12-22 Astra Ab New use
SE9401727D0 (sv) * 1994-05-18 1994-05-18 Astra Ab New compounds I
SE9401728D0 (sv) * 1994-05-18 1994-05-18 Astra Ab New compounds II
US5578725A (en) * 1995-01-30 1996-11-26 Regents Of The University Of Minnesota Delta opioid receptor antagonists
US5994327A (en) * 1995-11-17 1999-11-30 Astra Ab Process for the preparation of morphinans
ES2188888T3 (es) * 1996-01-10 2003-07-01 Glaxosmithkline Spa Derivados morfinoides 8ii) con condensados con heterociclos.
EP0894799B1 (en) * 1997-01-16 2004-04-07 Toray Industries, Inc. Indolomorphinane derivatives and remedies/preventives for cerebral disorders
DE69839508D1 (de) 1997-03-31 2008-07-03 Toray Industries Chinolinmorphinan-derivate und ihre medizinische anwendung
US6359111B1 (en) 1998-05-28 2002-03-19 Neorx Corporation Opioid receptor targeting
US7232829B2 (en) 2001-04-06 2007-06-19 Regents Of The University Of Minnesota Therapeutic compounds and methods
US6809104B2 (en) 2001-05-04 2004-10-26 Tularik Inc. Fused heterocyclic compounds
WO2002089729A2 (en) 2001-05-04 2002-11-14 Tularik Inc. Fused heterocyclic compounds
WO2003063779A2 (en) * 2002-01-25 2003-08-07 Regents Of The University Of Minnesota Selective analgesic agents
EP1522542A1 (en) * 2002-07-11 2005-04-13 Toray Industries, Inc. Therapeutic or preventive agent for nausea/vomiting
WO2004043958A1 (en) 2002-11-06 2004-05-27 Amgen Inc. Fused heterocyclic compounds
CA2580694A1 (en) * 2004-09-23 2006-03-30 Alexander Michalow Methods for regulating neurotransmitter systems by inducing counteradaptations
US20080045610A1 (en) * 2004-09-23 2008-02-21 Alexander Michalow Methods for regulating neurotransmitter systems by inducing counteradaptations
CN1298718C (zh) * 2005-03-18 2007-02-07 中国科学院上海有机化学研究所 C环连接有吡嗪环的青藤碱衍生物、合成方法及其用途
US20070185145A1 (en) * 2006-02-03 2007-08-09 Royds Robert B Pharmaceutical composition containing a central opioid agonist, a central opioid antagonist, and a peripheral opioid antagonist, and method for making the same

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4443605A (en) * 1982-07-30 1984-04-17 Miles Laboratories, Inc. 7β-Arylalkyl-6α, 7 α-oxymethylene-3-methoxy or 3-hydroxy-4, 5α-epoxy-17 methyl or 17-cycloalkyl-methyl morphinans
HU196376B (en) * 1985-05-23 1988-11-28 Sandoz Ag Process for preparing morphinane derivatives and pharmaceutical compositions containing such compounds
US4816586A (en) * 1987-07-29 1989-03-28 Regents Of The University Of Minnesota Delta opioid receptor antagonists
US4857533A (en) * 1988-12-15 1989-08-15 Baker Cummins Pharmaceuticals, Inc. Method of treatment for autoimmune diseases

Also Published As

Publication number Publication date
EP0456833B1 (en) 1995-03-01
KR940008032B1 (ko) 1994-09-01
ATE119039T1 (de) 1995-03-15
DE69017434T2 (de) 1995-06-29
JP2906654B2 (ja) 1999-06-21
FI913583A0 (fi) 1991-07-26
NO912940D0 (no) 1991-07-29
DK0456833T3 (da) 1995-05-01
NO912940L (no) 1991-07-29
CA2045481C (en) 1995-11-14
CA2045481A1 (en) 1991-05-29
US5332818A (en) 1994-07-26
WO1991007966A1 (en) 1991-06-13
ES2069100T3 (es) 1995-05-01
FI913583A7 (fi) 1991-07-26
AU6876891A (en) 1991-06-26
AU639053B2 (en) 1993-07-15
GR3015266T3 (en) 1995-06-30
JPH03223288A (ja) 1991-10-02
EP0456833A1 (en) 1991-11-21
EP0456833A4 (en) 1992-03-18
DE69017434D1 (de) 1995-04-06

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