KR870010052A - 벤조 디아제핀 유도체의 제조 방법 - Google Patents

벤조 디아제핀 유도체의 제조 방법 Download PDF

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KR870010052A
KR870010052A KR870003552A KR870003552A KR870010052A KR 870010052 A KR870010052 A KR 870010052A KR 870003552 A KR870003552 A KR 870003552A KR 870003552 A KR870003552 A KR 870003552A KR 870010052 A KR870010052 A KR 870010052A
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compound
formula
reacting
general formula
alkyl
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KR870003552A
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KR940009784B1 (ko
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뵈쩬 프란크
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에이/에스 페로산
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Neurosurgery (AREA)
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  • General Health & Medical Sciences (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
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Abstract

내용 없음.

Description

벤조 디아제핀 유도체의 제조방법
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (7)

  1. 일반식(I)의 벤조디아제핀 유도체
    상기 식에서,
    X1및 X2는 독립적으로,
    또는 COOR1(여기서, R1은 C1-3알킬, C3-5-사이클로알킬, C|1-3-알콕시메틸, C1-3-하이드록실 알킬 또는 아릴이다)이고,
    R4는 수소이며,
    R5는 C1-6-알킬이거나, R4및 R5가 함께는 2 내지 4원 알킬렌쇄를 형성한다.
  2. 제1항에 있어서, 7-에톡시카보닐-5,6-디하이드로-5-메틸-3-(3-사이클로로프로필-1,2,4-옥사디아졸-5-일)-6-옥소-4H-이미다조(1,5-a)(1,4) 벤조디아제핀인 화합물.
  3. 제1항에 있어서, 7-에톡시카보닐-5,6-디하이드로-5-메틸-3-(5-메틸-1,2,4-옥사디아졸-3-일)-6-옥소-4H-이미다조벤조(1,5-a)(1,4) 디아제핀인 화합물.
  4. 약제학적으로 허용되는 담체 또는 희석제와 중추신경제 질병을 완화시키는데 유효한 양의 제1항의 화합물로 이루어진 중추신경제 질병의 치료에 사용하기에 적합한 약제학적 조성물.
  5. 제4항에 있어서, 1내지 100mXg의 활성 화합물을 함유하는 경구용 단위 용량형태의 약제학적 조성물.
  6. a) 일반식(Ⅱ)의 화합물 일반식(Ⅲ)의 화합물과 반응시키거나,
    b) 일반식(Ⅳ)의 화합물의 반응성 유도체를 일반식(Ⅴ)의 화합물과 반응시켜, 임의로 일반식(Ⅵ)의 중간물질을 거쳐, X1이인 일반식(I)의 화합물을 형성시키거나,
    c) 일반식(Ⅶ)의 화합물을 일반식(Ⅷ)의 화합물과 반응시켜 일반식(Ⅸ)의 화합물을 형성시킨 다음, 일반식(Ⅸ)의 화합물을 NH2OH 또는 다른 아민화제와 반응시켜 X1이인 일반식(I)의 화합물을 형성시키거나,
    d) 일반식(Ⅹ)의 화합물을 NH2OH와 반응시켜 일반식(XI)의 화합물을 형성시킨 다음, 일반식(XI)의 화합물을 R1-COCl 또는 (R1CO)2O와 반응시켜, X1이인 일반식(I)의 화합물을 형성시키거나,
    e) 일반식(XⅡ)의 화합물의 반응성 유도체를 일반식(XⅢ)의 화합물과 반응시켜, 임의로 일반식(XⅣ)의 중간체를 거쳐, X2가인 일반식(I)의 화합물을 형성시키거나,
    f) 일반식(XV)의 화합물을 일반식(XⅥ)의 화합물과 반응시켜 일반식(XⅦ)의 화합물을 형성시킨 다음, 일반식(XⅦ)의 화합물을 NH2OH 또는 다른 아민화제와 반응시켜 X2가 인 일반식(I)의 화합물을 형성시키거나,
    g) 일반식(XⅧ)의 화합물을 NH2OH와 반응시켜 일반식(XⅨ)의 화합물을 형성시킨 다음, 일반식(XⅨ)의 화합물을 R1-COC1 또는 (R1CO)2O와 반응시켜 X2가인 일반식(I)의 화합물을 형성시킴을 특징으로 하는 일반식(I)의 화합물을 제조하는 방법.
    상기 식에서, X1및 X2는 독립적으로
    또는 COOR1(여기서, R1은 C1-3알킬, C3-5-사이클로알킬, C13-알콕시메틸, C1-3-하이드록실알킬 또는 아릴이다)이고,
    R4는 수소이며,
    R5는 C1-6-알킬이거나, R4및 R5가 함께는 2 내지 4원 알킬렌쇄를 형성하고,
    Y는 탈그룹이다.
  7. 제6항에 있어서, 단계 a)의 반응을 알칼리성 조건하에 수행하는 방법.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019870003552A 1986-04-16 1987-04-14 벤조디아제핀 유도체의 제조방법 KR940009784B1 (ko)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DK174086A DK174086D0 (da) 1986-04-16 1986-04-16 Nye benzodiazepinderivater samt fremgangsmaade til fremstilling af samme
DK1740/86 1986-04-16

Publications (2)

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KR870010052A true KR870010052A (ko) 1987-11-30
KR940009784B1 KR940009784B1 (ko) 1994-10-17

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Country Status (19)

Country Link
US (1) US4772599A (ko)
EP (1) EP0241682B1 (ko)
JP (1) JPH07116195B2 (ko)
KR (1) KR940009784B1 (ko)
AT (1) ATE58737T1 (ko)
AU (1) AU588994B2 (ko)
CA (1) CA1293724C (ko)
DE (2) DE241682T1 (ko)
DK (1) DK174086D0 (ko)
ES (1) ES2037673T3 (ko)
FI (1) FI87458C (ko)
GR (1) GR3001160T3 (ko)
IE (1) IE60488B1 (ko)
IL (1) IL82117A (ko)
NO (1) NO164655C (ko)
NZ (1) NZ219915A (ko)
PH (1) PH22406A (ko)
PT (1) PT84690B (ko)
ZA (1) ZA872630B (ko)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR100283474B1 (ko) * 1999-01-18 2001-02-15 박호군 Ｎ₂ｓ₂리간드가 포함된 플루마제닐 유도체 및 그의 제조방법

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4622321A (en) * 1985-05-17 1986-11-11 As Ferrosan Oxadiazolylimidazobenzodiazepine, compositions, and method
AU594676B2 (en) * 1985-05-17 1990-03-15 Novo Nordisk A/S Oxadiazolyl imidazobenaodiazepine compound, pharmaceutical composition containing said compound, method of preparing said compound and method of treating a central nervous system ailment
FI880814A (fi) * 1987-03-10 1988-09-11 Hoffmann La Roche Imidazodiazepin-derivat.
GB8720414D0 (en) * 1987-08-28 1987-10-07 Roussel Lab Ltd Chemical compounds
CA2015336A1 (en) * 1989-05-19 1990-11-19 F. Hoffmann-La Roche Ag Imidazodiazepines for the treatment of neurological symptoms
US4904654A (en) * 1989-07-26 1990-02-27 Merck & Co., Inc. 7-chloro-5,6-dihydro-3-(5-(2-hydroxy-isopropyl)-1,2,4-oxadiazol-3-yl)-5-methyl-6-oxo-4H-imidazo[1,5a][1,4]benzodiazepine
CA2143246C (en) * 1994-03-16 2000-08-22 Thierry Godel Imidazodiazepines
US5438035A (en) * 1994-06-24 1995-08-01 American Cyanamid Company Methods for controlling undesirable plant species with benzodiazepine compounds
US5706829A (en) * 1996-06-06 1998-01-13 Creighton University Method for treating neurocardiogenic syncope
TWI239333B (en) 2000-11-16 2005-09-11 Hoffmann La Roche Benzodiazepine derivatives as GABA A receptor modulators
CN101039678B (zh) * 2004-10-12 2011-06-15 弗·哈夫曼-拉罗切有限公司 用于治疗认知障碍的咪唑并[1,5-a]三唑并[1,5-d]苯并二氮杂䓬衍生物
RU2007112940A (ru) * 2004-10-20 2008-11-27 Ф.Хоффманн-Ля Рош Аг (Ch) Производные имидазобензодиазепина
RU2007114763A (ru) * 2004-10-20 2008-11-27 Ф.Хоффманн-Ля Рош Аг (Ch) Галогенозамещенные производные бензодиазепинов
PL1828194T3 (pl) * 2004-12-14 2008-11-28 Hoffmann La Roche Tetracykliczne imidazo-benzodiazepiny jako modulatory receptorów GABA
US20090054412A1 (en) * 2007-08-20 2009-02-26 John Alan Kemp Treatment of Sleep Disorders
CA2696703C (en) 2007-08-20 2016-07-26 Evotec Neurosciences Gmbh Treatment of sleep disorders

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CA1143728A (en) * 1979-10-04 1983-03-29 Max Gerecke Imidazodiazepine derivatives
JPS57123180A (en) * 1980-12-17 1982-07-31 Schering Ag 3-substituted beta-carboline, manufacture and psychotropic drug containing same
CA1185602A (en) * 1981-02-27 1985-04-16 Emilio Kyburz Imidazodiazepines
MC1528A1 (fr) * 1982-07-21 1984-04-13 Hoffmann La Roche Imidazobenzodiazepines
DK151808C (da) * 1982-11-16 1988-06-20 Ferrosan As Analogifremgangsmaade til fremstilling af oxadiazolylimidazo-oe1,4aa-benzodiazepinderivater
FI850191L (fi) * 1984-01-19 1985-07-20 Hoffmann La Roche Imidazodiazepinderivat.
CA1259612A (en) * 1985-02-28 1989-09-19 Emilio Kyburz Imidazodiazepine derivatives
AU587802B2 (en) * 1985-03-08 1989-08-31 Ferrosan A/S Novel oxadiazolyl imidazobenzodiazepine derivatives and methods of preparing such compounds
AU594676B2 (en) * 1985-05-17 1990-03-15 Novo Nordisk A/S Oxadiazolyl imidazobenaodiazepine compound, pharmaceutical composition containing said compound, method of preparing said compound and method of treating a central nervous system ailment
DE202441T1 (de) * 1985-05-17 1987-03-19 Aktieselskabet Ferrosan, Soeborg, Dk Oxadiazolylimidazobenzodiazepine, verfahren zu ihrer herstellung und pharmazeutische zubereitungen.
US4622321A (en) * 1985-05-17 1986-11-11 As Ferrosan Oxadiazolylimidazobenzodiazepine, compositions, and method
DK476885D0 (da) * 1985-10-17 1985-10-17 Ferrosan As Heterocycliske forbindelser og fremgangsmaader til fremstilling heraf

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR100283474B1 (ko) * 1999-01-18 2001-02-15 박호군 Ｎ₂ｓ₂리간드가 포함된 플루마제닐 유도체 및 그의 제조방법

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Publication number Publication date
CA1293724C (en) 1991-12-31
US4772599A (en) 1988-09-20
NZ219915A (en) 1989-04-26
ES2037673T3 (es) 1993-07-01
DE241682T1 (de) 1988-02-25
NO871459D0 (no) 1987-04-07
ZA872630B (en) 1987-10-02
NO871459L (no) 1987-10-19
AU588994B2 (en) 1989-09-28
EP0241682A3 (en) 1988-10-26
JPH07116195B2 (ja) 1995-12-13
ATE58737T1 (de) 1990-12-15
PT84690A (en) 1987-05-01
FI87458B (fi) 1992-09-30
EP0241682B1 (en) 1990-11-28
PH22406A (en) 1988-08-26
AU7158387A (en) 1987-10-22
EP0241682A2 (en) 1987-10-21
GR3001160T3 (en) 1992-06-30
FI87458C (fi) 1993-01-11
DK174086D0 (da) 1986-04-16
IE60488B1 (en) 1994-07-27
FI871615A0 (fi) 1987-04-13
IL82117A (en) 1992-03-29
IL82117A0 (en) 1987-10-30
NO164655C (no) 1990-10-31
IE870981L (en) 1987-10-16
PT84690B (pt) 1989-11-30
NO164655B (no) 1990-07-23
DE3766401D1 (de) 1991-01-10
JPS62249985A (ja) 1987-10-30
KR940009784B1 (ko) 1994-10-17
FI871615A (fi) 1987-10-17

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