KR960703912A - 중추신경계 활성을 갖는 헤테로사이클 아민(heterocyclic amines having central nervous system activity) - Google Patents

중추신경계 활성을 갖는 헤테로사이클 아민(heterocyclic amines having central nervous system activity)

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KR960703912A
KR960703912A KR1019960700407A KR19960700407A KR960703912A KR 960703912 A KR960703912 A KR 960703912A KR 1019960700407 A KR1019960700407 A KR 1019960700407A KR 19960700407 A KR19960700407 A KR 19960700407A KR 960703912 A KR960703912 A KR 960703912A
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sub
compound
och
imidazo
dihydro
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KR1019960700407A
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KR100335548B1 (ko
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아서 지. 로메로
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로렌스 티. 웰츠
디 업존 캄파니
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    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
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Abstract

본 발명은 불안제거 및 항우울 활성 및 중추신경계 활성을 갖는 하기 일반식(Ⅰ)의 트리사이클 질소-함유 화합물 및 그의 약학적으로 허용되는 염에 관한 것이다 :
상기 식에서, R1및 R2는 독립적으로 수소, C1-6알킬이거나, 또는 R1및 R2가 결합하여 피롤리딘, 피페리딘, 모르폴린 또는 이미다졸을 형성하고, X는 OCH3, SO2R3, SO2CF3또는 CN이고; R3는 C1-6알킬 또는 아릴이고; Y는 수소, Cl, Br, F, CN, CONR1R2, CF3, OCH3, SO2NR1R2이다.
이들 신규한 화합물은 불안완화증, 정신분열증, 파킨슨 병, 불안증, 우울증의 치료 또는 이러한 치료가 필요한 환자의 혈압 강하 또는 편두통 치료에 적합하다.

Description

중추신경계 활성을 갖는 헤테로사이클 아민(HETEROCYCLIC AMINES HAVING CENTRAL NERVOUS SYSTEM ACTIVITY)
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (9)

  1. 하기 일반식의 화합물 및 그의 약학적으로 허용되는 염 :
    상기 식에서, R1및 R2는 독립적으로 수소, C1-6알킬이거나, 또는 R1및 R2가 결합하여 피롤리딘, 피페리딘, 모르폴린 또는 이미다졸을 형성하고, X는 OCH3, SO2R3, SO2CF3또는 CN이고; R3는 C1-6알킬 또는 아릴이고; Y는 수소, Cl, Br, F, CN, CONR1R2, CF3, OCH3, SO2NR1R2이다.
  2. 제 1항에 있어서, R1및 R2가 각각 프로필인 화합물.
  3. 제 1항에 있어서, R1및 R2가 각각 메틸인 화합물.
  4. 제 1항에 있어서, X가 OCH3인 화합물.
  5. 제 1항에 있어서, Y가 수소인 화합물.
  6. 제 1항에 있어서, a) (R)-5-메틸아미노-1-메톡시-5,6-디하이드로-4H-이미다조[4,5,1-ij]-키놀린-2(1H)-온, b) (R)-5-디메틸아미노-1-메톡시-5,6-디하이드로-4H-이미다조[4,5,1-ij]-키놀린-2(1H)-온, c) (R)-5-프로필아미노-1-메톡시-5,6-디하이드로-4H-이미다조[4,5,1-ij]-키놀린-2(1H)-온, d) (R)-5-디프로필아미노-1-메톡시-5,6-디하이드로-4H-이미다조[4,5,1-ij]-키놀린-2(1H)-온인 화합물.
  7. 동물 또는 인간 숙주에게 약학적으로 효과량의 일반식(Ⅰ)의 화합물을 투여함을 포함하는, 상기 동물 또는 인간 숙주의 중추신경계 질병을 치료하는데 유용한 약제를 제조하기 위한 제 1항의 일반식(Ⅰ)의 화합물의 용도.
  8. 제 7항에 있어서, 상기 화합물을 하루에 약 10 내지 약 1200㎎의 양으로 경구투여하는 용도.
  9. 제 1항에 있어서, 상기 화합물을 불안완화 질환의 치료를 위해 투여하는 용도.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019960700407A 1993-07-27 1994-06-17 중추신경계활성을갖는헤테로사이클아민 KR100335548B1 (ko)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US9760893A 1993-07-27 1993-07-27
US08/097,608 1993-07-27
US08/097608 1993-07-27
PCT/US1994/006648 WO1995004056A1 (en) 1993-07-27 1994-06-17 Heterocyclic amines having central nervous system activity

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KR960703912A true KR960703912A (ko) 1996-08-31
KR100335548B1 KR100335548B1 (ko) 2002-10-04

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US6001936A (en) * 1997-10-24 1999-12-14 3M Innovative Properties Company Dye enhanced durability through controlled dye environment
US6455564B1 (en) * 1999-01-06 2002-09-24 Pharmacia & Upjohn Company Method of treating sexual disturbances
US20060040929A1 (en) * 1999-01-06 2006-02-23 Mccall Robert B (5R)-(methylamino)-5,6-dihydro-4H-imidazo[4,5,1-ij]quinoline-2(1H)-thione and method of preparation thereof
CA2358865A1 (en) 1999-02-05 2000-08-10 Pharmacia & Upjohn Company Process to prepare (5r)-(methylamino)-5,6-dihydro-4h-imidazo[4,5,1-ij]-quinolin-2(1h)-one
NZ522112A (en) * 2000-04-21 2004-10-29 Upjohn Co Substituted phenylazacycloalkane-type compounds for treating fibromyalgia and chronic fatigue syndrome
AR033520A1 (es) * 2000-04-27 2003-12-26 Upjohn Co (5r)-(metilamino) -5,6-dihidro-4h-imidazo[4,5,1-ij] quinolin-2(1h)-tiona
CA2500919A1 (en) * 2002-10-04 2004-04-22 Pharmacia Corporation Compositions and methods for treating sexual dysfunction
CN1728998A (zh) * 2002-10-25 2006-02-01 法玛西雅厄普约翰有限责任公司 杂环胺类化合物作为神经保护剂的用途
MXPA06001081A (es) * 2003-07-31 2006-04-24 Irm Llc Compuestos biciclicos y composiciones como inhibidores de pdf.
CN113117376B (zh) * 2019-12-30 2022-08-19 中国科学院高能物理研究所 一种邻菲罗啉衍生的萃取剂及其制法和应用

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US4110339A (en) 1977-11-25 1978-08-29 Eli Lilly And Company 4-(Di-n-propyl)amino-1,3,4,5-tetrahydrobenz[cd]indole
DE3346573A1 (de) 1983-12-23 1985-07-04 Troponwerke GmbH & Co KG, 5000 Köln 1,3,4,5-tetrahydrobenz(c,d)indole, ein verfahren zu ihrer herstellung und ihre verwendung
IL74222A (en) 1984-02-06 1988-07-31 Lilly Co Eli 6-substituted-4-dialkylamino tetrahydrobenz(c,d)indoles,their preparation and pharmaceutical compositions comprising them
JPS63502032A (ja) 1985-12-31 1988-08-11 ジ・アップジョン・カンパニ− 抗精神病薬としての２，３−ジヒドロ−１ｈ−フェナレン−２−アミノ化合物
AU8325987A (en) 1986-12-11 1988-06-30 Upjohn Company, The Antipsychotic amino-polyhydro-benz-(iso)quinolines and intermediates
CA2051697C (en) * 1989-06-09 1996-10-08 Malcolm Wilson Moon Heterocyclic amines having central nervous system activity
JP2899757B2 (ja) * 1989-06-26 1999-06-02 持田製薬株式会社 ジヒドロイミダゾキノリノンオキシムスルホン酸誘導体
GB9012062D0 (en) * 1990-05-30 1990-07-18 Phillips Cables Ltd Moisture-impermeable stranded electric conductor

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CA2166700A1 (en) 1995-02-09
CN1043574C (zh) 1999-06-09
ATE159943T1 (de) 1997-11-15
EP0724584A1 (en) 1996-08-07
AU684808B2 (en) 1998-01-08
CA2166700C (en) 2000-04-18
NZ269018A (en) 1996-12-20
EP0724584B1 (en) 1997-11-05
KR100335548B1 (ko) 2002-10-04
USRE40278E1 (en) 2008-04-29
AU7246194A (en) 1995-02-28
DE69406678D1 (de) 1997-12-11
DK0724584T3 (da) 1998-05-25
JPH09500898A (ja) 1997-01-28
WO1995004056A1 (en) 1995-02-09
US5652245A (en) 1997-07-29
GR3025482T3 (en) 1998-02-27
MX9405676A (es) 1995-01-31
ES2108474T3 (es) 1997-12-16
CN1128030A (zh) 1996-07-31
US20020187981A1 (en) 2002-12-12
DE69406678T2 (de) 1998-03-26
JP3433804B2 (ja) 2003-08-04

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