KR960701022A - 헤테로사이클릭 화합물, 이의 용도 및 제조방법(Heterocyclic compounds, their use and preparation) - Google Patents

헤테로사이클릭 화합물, 이의 용도 및 제조방법(Heterocyclic compounds, their use and preparation) Download PDF

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KR960701022A
KR960701022A KR1019950703762A KR19950703762A KR960701022A KR 960701022 A KR960701022 A KR 960701022A KR 1019950703762 A KR1019950703762 A KR 1019950703762A KR 19950703762 A KR19950703762 A KR 19950703762A KR 960701022 A KR960701022 A KR 960701022A
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compound
methyl
benzazine
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formula
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홀벡 롤프
바르트럼 닐젠 에릭
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앤 세셔
노보 노르디스크 에이/에스
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/20—Hypnotics; Sedatives
    • 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
    • A61P25/24—Antidepressants
    • 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
    • A61P25/26—Psychostimulants, e.g. nicotine, cocaine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D223/00—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
    • C07D223/14—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D223/00—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
    • C07D223/14—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D223/32—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems containing carbocyclic rings other than six-membered
    • 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
    • C07D491/02—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 two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems

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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
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Abstract

본 발명은 중추신경계의 특정한 질환, 예를 들면, 정신병, 통증, 우울증, 불면증, 운동이상증, 파킨슨씨병, 발작의 치료에 유용한 일반식 (I)의 트리사이클릭 벤즈아제핀 또는 약제학적으로 허용되는 이의염에 관한 것이다.
상기식에서 A는-와β-로 나타낸 탄소원자와 함께 사이ㅏ클로펜텐, 사이클로헥센, 푸란, 디하이드로푸란, 피란, 디하이드로피란, 티오펜, 옥사졸, 피롤, 피롤린, 테트라하이드피리딘 또는 디옥솔 환을 형성하고, R1은 수소 또는 C1-6알킬이고, R2와 R3은 독립적으로 수소, 알콕시, 할로겐, 니트로, 시아노 또는 하이드록시이거나, R2와 R3은 함께 푸란, 디하이드로푸란, 사이클로펜텐 또는 디옥솔 환을 형성할 수 있으며, R4는 수소,알콕시, 니트로, 시아노, 하이드록시 또는 할로겐이다.

Description

헤테로사이클릭 화합물, 이의용도 및 제조방법(Herterocyclic compunds, their use and proparation)
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (10)

  1. 일반식(I)의 트리사이클릭 2,3,4,5-테트라하이드로-1H-3-벤즈아제핀 및 약제학적으로 허용되는 이의염.
    상기식에서, A는-와 β-로 나타낸 탄소원자와 함께 사이클로펜텐, 사이클로헥센, 푸란, 디하이드로푸란, 피란, 디하이드로피란, 티오펜, 옥사졸, 피롤, 피롤린, 테트라하이드로피리딘 또는 디옥솔 환을 형성하고, R1은 수소 또는 C1-6알킬이고, R2와 R3은 독립적으로 수소, C1-6알콕시, 할로겐, 니트로, 시아노 또는 하이드록시이거나, R2와 R3은 함께 푸란, 디하이드로푸란, 사이클로페네텐 또는 디옥솔 환을 형성할 수 있으며, R4는 수소, C1-6-알콕시, 니트로, 시아노, 하이드록시 또는 할로겐이다.
  2. 제1항에 있어서, R1이 메틸인 화합물.
  3. 제1항에 있어서, 6-(벤조푸란-7-일)-8-메틸-7,8,9,10-테트라하이드로-6H-푸로〔2,3,-g〕〔3〕벤즈아제핀,6-(2,3-디하이드로벤조푸란-7-일)-8-메틸-2,3,7,8,9,
    10,-헥사하이드로-6H-푸로〔2,3-g〕〔3〕벤지아제핀, 5-(벤조푸란-7-일)-3-메틸-1,2,3,4,5,8,9,10-옥타하이드로인데노〔4,5-d〕아제핀, 6-(벤조푸란-7-일)-6,7-메틸렌디옥시-3-메틸-2,3,4,5-테트라하이드로-1H-3-벤즈아제핀,3-메틸-5페닐-1,2,3,4,5,8,9,10-옥타하이드로인데노〔4,5-d〕아제핀,3-메틸-5-페닐-2,3,4,5,8,9,10,11-옥타하이드로-1H-나프트〔1,2-d〕아제핀 및 8-메틸-6-페닐-7,8,9,10-테트라하이드로-6H-옥사졸로 〔4,5-g〕〔3〕벤즈아제핀인 화합물.
  4. 제1항 내지 제3항 중 어느 한 항에 따르는 화합물 또는 약제학적으로 허용되는 이의 산 부가염과 약제학적으로 허용되는 담체 또는 희석제를 포함하는 약제학적 조성물.
  5. 약제학적으로 허용되는 담체 또는 희석제와 함께 제1항 내지 제3항 중의 어느 한 항에 따른 화합물을 포함하는 중추신경계 질환 치료용 약제학적 조성물.
  6. 제4항 또는 제5항에 있어서, 활성 화합물 0.1 내지100㎎을 함유하는 경구 용량 단위 형태의 약제학적 조성물.
  7. 중추신경계 질환과 관련된 질병 치룡용의 약제학적 조성물을 제조하기 위한, 제1항 내지 제3항 중의 어느 한 항에 따르면 화합물의 용도.
  8. 중추신경계 질환의 치료를 필요로 한는 환잦에게 제1항 내지 제3항중 어느 한항에 따르는 화합물을 이러한 질환을 정감시키기에 유효한 양으로 투여함을 포함하여, 중추신경계 질환을 치료하는 방법.
  9. 중추신경계 질환의 치료를 필요로 하는 환자에게 약제학적으로 허용되는 담체 또는 희석제와 함께 존재하는, 약제학적 조성물 형태의 제1항 내지 제3항 중의 어느 한 항에 따르면 화합물을 이러한 질환을 경감시키기에 유효한 양으로 투여하는 단계를 포함하여, 중추신경계 질환을 치료하는 방법.
  10. a) 일반식(Ⅳ)의 2-아릴에틸아민을 일반식(Ⅲ)의 옥시란과 반응시키고 50 내지 110℃의 온도로 가열함으로써 일반식(Ⅱ)의 화합물을 형성시키고, 일반식(Ⅱ)의 아미노알콜을 산성 첨가제 또는 탈수제와 반응시킴으로써 수행되는 분자내 페환반응을 이용하여 일반식(Ⅱ)의 화합물을 일반식(I)의 목적하는 벤즈아제핀으로 전환시키건, b) 일반식(Ⅴ)의 2-아릴에틸아민을 일반식(Ⅲ)의 옥시란과 반응시키고 50 내지 110℃의 온도로 가열함으로서 일반식(Ⅵ)의 화합물을 형성시키고, 일반식(Ⅵ)의 아미노알콜을 산성 첨가제 또는 탈수제와 반응시킴으로써 수행되는 분자내 폐환반응을 이용하여 일반식(Ⅵ)의 화합물을 일반식(Ⅶ)의 벤즈아제핀으로 전환 시킨 다음 일반식(Ⅷ)의 벤즈아제핀을 용매속에서 디할로메탄 및 염기와 페환부가반응시킴으로써 일반식(Ⅶ)의 벤즈아제핀을 일반식(I)의 화합물로 전환시킴을 포함하는 제1항에 따르는 화합물의 제조방법.
    상기식에서, R1은 수소 또는 저급 알킬이고, A, R2, R3및 R4는 제1항에서 정의한 바와 같으며, R5및 R6은 독립적으로 하이드록시, 머캅토, 아미노 또는 카복시이거나, 독립적으로 당해 분야의 통상의 전문가에서 공지된 표준 방법으로 하이드록시, 머캅토, 아미노, 또는 카복시 그룹으로 전환될 수 있는 치환체를 나타낸다.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019950703762A 1993-03-10 1994-02-18 헤테로사이클릭 화합물, 이의 용도 및 제조방법(Heterocyclic compounds, their use and preparation) KR960701022A (ko)

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DK0267/93 1993-03-10
DK93267A DK26793D0 (da) 1993-03-10 1993-03-10 Benzofuranyl- eller dihydrobenzofuranyl-substituerede tricycliske benzazepiner, der anvendelse og fremstilling
PCT/DK1994/000069 WO1994020472A1 (en) 1993-03-10 1994-02-18 Heterocyclic compounds, their use and preparation

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EP (1) EP0688320B1 (ko)
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FI954229A (fi) 1995-09-08
JPH08507498A (ja) 1996-08-13
EP0688320A1 (en) 1995-12-27
CN1121710A (zh) 1996-05-01
ES2133542T3 (es) 1999-09-16
DE69418321D1 (de) 1999-06-10
JP3779319B2 (ja) 2006-05-24
ZA941377B (en) 1995-08-28
NO953543L (no) 1995-09-08
IL108730A0 (en) 1994-05-30
AU682494B2 (en) 1997-10-09
NZ262098A (en) 1996-11-26
AU6138694A (en) 1994-09-26
US5512562A (en) 1996-04-30
TW279861B (ko) 1996-07-01
ATE179700T1 (de) 1999-05-15
CA2157668A1 (en) 1994-09-15
EP0688320B1 (en) 1999-05-06
DK0688320T3 (da) 1999-11-01
FI954229A0 (fi) 1995-09-08
DK26793D0 (da) 1993-03-10
CN1045957C (zh) 1999-10-27
DE69418321T2 (de) 1999-12-30
WO1994020472A1 (en) 1994-09-15
NO953543D0 (no) 1995-09-08
GR3030864T3 (en) 1999-11-30
IL108730A (en) 1999-08-17
FI111944B (fi) 2003-10-15
CA2157668C (en) 2006-05-30

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