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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South Korea
Prior art keywords
carbon atoms
alkyl
hydrogen
carbons
represented
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KR1019910700795A
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English (en)
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KR940008032B1 (ko
Inventor
히로시 나가세
코오지 카와이
슈우 마쯔모토
타카시 엔도오
요시아키 카쯔라
코오헤이 아라카와
Original Assignee
마에다 카쯔노수케
도오레 가부시키가이샤
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Publication of KR920700643A publication Critical patent/KR920700643A/ko
Application granted granted Critical
Publication of KR940008032B1 publication Critical patent/KR940008032B1/ko

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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)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Immunology (AREA)
  • Emergency Medicine (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Transplantation (AREA)
  • Pain & Pain Management (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (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 KR940008032B1 (ko)

Applications Claiming Priority (10)

Application Number Priority Date Filing Date Title
JP???1-?308491? 1989-11-28
JP30849189 1989-11-28
JP32216089 1989-12-11
JP???1-?322160? 1989-12-11
JP1-322160 1989-12-15
JP32694189 1989-12-15
JP1-308491 1989-12-15
JP1-326941 1989-12-15
JP???1-?326941? 1989-12-15
PCT/JP1990/001541 WO1991007966A1 (fr) 1989-11-28 1990-11-28 Immunosuppresseur et procede de preparation d'un tel medicament

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)

Application Number Title Priority Date Filing Date
KR1019910700795A 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) FI913583A0 (ko)
GR (1) GR3015266T3 (ko)
NO (1) NO912940D0 (ko)
WO (1) WO1991007966A1 (ko)

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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
WO1994007896A1 (en) * 1992-09-29 1994-04-14 Toray Industries, Inc. Indole derivative, process for producing the same, and medicinal use thereof
DE69318710T2 (de) * 1992-12-22 1998-09-10 Toray Industries Antitussivum
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
SE9401728D0 (sv) * 1994-05-18 1994-05-18 Astra Ab New compounds II
SE9401727D0 (sv) * 1994-05-18 1994-05-18 Astra Ab New compounds I
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
ATE229958T1 (de) 1996-01-10 2003-01-15 Glaxosmithkline Spa Heterocyclische kondensierte morphin-derivate
US6156762A (en) * 1997-01-16 2000-12-05 Toray Industries, Inc. Indolomorphinan derivative and agent for curing and preventing cerebral disorder
EP0911334B1 (en) 1997-03-31 2008-05-21 Toray Industries, Inc. Quinolinomorphinane derivatives and medicinal use thereof
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
ES2319619T3 (es) 2001-05-04 2009-05-11 Amgen Inc. Compuestos heterociclicos condensados.
CA2474306A1 (en) * 2002-01-25 2003-08-07 Regents Of The University Of Minnesota Selective analgesic agents
WO2004007503A1 (ja) * 2002-07-11 2004-01-22 Toray Industries, Inc. 悪心・嘔吐の治療または予防剤
NZ540328A (en) 2002-11-06 2008-02-29 Amgen Inc Fused heterocyclic compounds
US20080045610A1 (en) * 2004-09-23 2008-02-21 Alexander Michalow Methods for regulating neurotransmitter systems by inducing counteradaptations
CN101065014A (zh) * 2004-09-23 2007-10-31 亚历山大·米哈洛 通过诱导逆适应调节神经递质系统的方法
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)

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

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PJ2001 Appeal

Appeal kind category: Appeal against decision to decline refusal

Decision date: 19941112

Appeal identifier: 1994201001053

Request date: 19940607

PB0901 Examination by re-examination before a trial

Comment text: Request for Trial against Decision on Refusal

Patent event date: 19940607

Patent event code: PB09011R01I

Comment text: Amendment to Specification, etc.

Patent event date: 19931116

Patent event code: PB09011R02I

G160 Decision to publish patent application
PG1605 Publication of application before grant of patent

Comment text: Decision on Publication of Application

Patent event code: PG16051S01I

Patent event date: 19940809

B701 Decision to grant
PB0701 Decision of registration after re-examination before a trial

Patent event date: 19941112

Comment text: Decision to Grant Registration

Patent event code: PB07012S01D

Patent event date: 19940728

Comment text: Transfer of Trial File for Re-examination before a Trial

Patent event code: PB07011S01I

GRNT Written decision to grant
PR0701 Registration of establishment

Comment text: Registration of Establishment

Patent event date: 19941130

Patent event code: PR07011E01D

PR1002 Payment of registration fee

Payment date: 19941130

End annual number: 3

Start annual number: 1

FPAY Annual fee payment

Payment date: 19970821

Year of fee payment: 4

PR1001 Payment of annual fee

Payment date: 19970821

Start annual number: 4

End annual number: 4

LAPS Lapse due to unpaid annual fee
PC1903 Unpaid annual fee