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KR910009700A - 3-피페리디닐-1,2-벤즈이속사졸 - Google Patents

3-피페리디닐-1,2-벤즈이속사졸 Download PDF

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KR910009700A
KR910009700A KR1019890016114A KR890016114A KR910009700A KR 910009700 A KR910009700 A KR 910009700A KR 1019890016114 A KR1019890016114 A KR 1019890016114A KR 890016114 A KR890016114 A KR 890016114A KR 910009700 A KR910009700 A KR 910009700A
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compound
alkyl
general formula
acid addition
formula
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KR0146053B1 (ko
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게리두스 마리아 쟈안센 코르비루우스
귀리엘무스 크냅스 알폰수스
에드몬트 죠셉핀 케니스 루도
반덴베르크 쟈안
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구스타프 반 리이트
쟈안센 파아마슈우티카 엔.부이
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

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  • Engineering & Computer Science (AREA)
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  • Neurosurgery (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic 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)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

내용 없음

Description

3-피페리디닐-1,2-벤즈이속사졸
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (10)

  1. 일반식(Ⅰ)의 화합물 그 산부가염 또는 그 입체 이성체.
    위의 일반식에서, AIk는 C1-4알칸리일이고, R1은 수소, C1-4알킬 또는 할로이고, R2는 C1-4알킬이고, R3는 히드록시 또는 R4-C(=O)O이고, R4는 C1-19알킬이다.
  2. 제1항에 있어서, R3이 6,7,8,9-테트라히드로-2-C1-4알킬-4H-피리도[1,2-a]피리미딘-4-온 부분의 9위치에 치환된 일반식(I)의 화합물, 그 산부가염 또는 그 입체 이성체.
  3. 제2항에 있어서, AIk가 에탄리일, R1이 할로이고, R2가 메틸인 일반식(I)의 화합물, 그 산부가염 또는 그 입체이성체.
  4. 제1항에 있어서, 3-[2-[4-(6-플루오로-1,2-벤즈이속사졸-3-일)-1-피페리디닐]에틸-6,7,8,9-테트라히드로-9-히드록시-2-메틸-4H-피리도[1,2-a]피리미딘-4-온, 그 산부가염 또는 그 거울상체(enatiomer)인 화합물.
  5. 유효성분으로 일반식(I)의 화합물, 그 산부가염 또는 그 입체이성체를 항정신병성 치료효과량과 함께 불활성 담체로 조성된 항정신병성 약제조성물.
    위의 일반식에서, AIk는 C1-4알칸리일이고, R1은 수소, C1-4알킬 또는 할로이고, R2는 C1-4알킬이고, R3는 히드록시 또는 R4-C(=O)O이고, R4는 C1-19알킬이다.
  6. 제5항에 있어서, R3이 6,7,8,9-테트라히드로-2-C1-4알킬-4H-피리도[1,2-a]피리미딘-4-온 부분의 9위치에 치환된 약제조성물.
  7. 제5항에 있어서, 3-[2-[4-(6-플루오로-1,2-벤즈이속사졸-3-일)-1-피페리디닐]에틸]-6,7,8,9-테트라히드로-9-히드록시-2-메틸-4H-피리도[1,2-a]피리미딘-4-온, 그 산부가염 또는 그 거울상체인 약제 조성물.
  8. 일반식(I)의 화합물, 그 산부가염 또는 그 입체이성체를 항정신병성 치료효과량 온형동물에 투여하여, 정신병성 질환에 걸린 온혈동물을 치료하는 방법.
    위의 일반식에서, AIk는 C1-4알칸리일이고, R1은 수소, C1-4알킬 또는 할로이고, R2는 C1-4알킬이고, R3는 히드록시 또는 R4-C(=O)O이고, R4는 C1-19알킬이다.
  9. 제8항에 있어서, R3이 6,7,8,9-테트라히드로-2-C1-4알킬-4H-피리도[1,2-a]피리미딘-4-온 부분의 9위치에 치환된 일반식(I)의 화합물, 그 산부가염 또는 입체이성체를 항정신병성 치료효과량 온형동물에 투여하여, 정신병성 질환에 걸린 온형동물을 치료하는 방법.
  10. a)일반식(Ⅱ)의 3-피페리디닐-1,2-벤즈이속사졸을 불활성 용매중에서 승온하에 일반식(Ⅲ)의 화합물로 N-알킬화하거나, b)일반식(Ⅳ)의 욕심을 반응불활성 용매중에서 염기와 함께 승온하에 폐환 반응시키거나, c)일반식(V)의 활성옥심을 불활성 용매중에서 염기와 함께 승온하에 폐환 반응시키거나, d)일반식(I-a)의 화합물을 일반식(Ⅵ)의 카르복시산 또는 그 반응성 유도체를 불활성 용매 중에서 O-아실화하거나, e)일반식(VⅡ)의 아미딘을 일반식(VⅢ)의 -디카르보닐 중간화합물로 불활성용매중에서 승온하에 폐환 반응시키거나, f)일반식(IX)의 화합물을 일반식(X)의 에나민을 불활성 용매중에서 승온하에 폐환 반응시키거나, g)일반식(I-a)의 화합물의 라세미체 혼합물을, 분해제에 의해 부분입체 이성질체염 또는 화합물의 혼합물로 전환시키기고, 부분입체이성체 또는 화합물의 혼합물을 분리한후, 분리한 부분입체 이성체염 또는 화합물을 일반식(I-a)의 화합물의 상응하는 거울상체로 전환시켜 일반식(I)의 화합물, 그 산부가염 또는 그 입체이성체를 제조하는 방법.
    위의 일반식에서, AIk는 C1-4알칸디일이고, R1은 수소, C1-4알킬 또는 할로이고, R2는 C1-4알킬이고, R3는 히드록시 또는 R4-C(=O)O이고, R4는 C1-19알킬이고, Y는 반응성 이탈기이고, L은 산의 잔기이고, R5는 반응성 이탈기이다.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019890016114A 1988-11-07 1989-11-07 3-피페리디닐-1,2-벤즈이속사졸 Expired - Lifetime KR0146053B1 (ko)

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US26785788A 1988-11-07 1988-11-07
US267857 1988-11-07
US267,857 1988-11-07

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KR910009700A true KR910009700A (ko) 1991-06-28
KR0146053B1 KR0146053B1 (ko) 1998-08-17

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EP (1) EP0368388B1 (ko)
JP (1) JP2758045B2 (ko)
KR (1) KR0146053B1 (ko)
AT (1) ATE122349T1 (ko)
AU (1) AU614437B2 (ko)
CA (1) CA2000786C (ko)
CL (1) CL43432B (ko)
CY (2) CY1926A (ko)
DE (2) DE68922577T2 (ko)
DK (1) DK169923B1 (ko)
ES (1) ES2075036T3 (ko)
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HK (1) HK131696A (ko)
IE (1) IE66370B1 (ko)
IL (1) IL92208A0 (ko)
LU (1) LU91362I2 (ko)
NL (1) NL300298I2 (ko)
NO (2) NO173015C (ko)
NZ (1) NZ231062A (ko)
PT (1) PT92206B (ko)
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FI895261A0 (fi) 1989-11-06
ES2075036T3 (es) 1995-10-01
NL300298I1 (nl) 2007-12-03
NO173015B (no) 1993-07-05
NO894411L (no) 1990-05-08
JP2758045B2 (ja) 1998-05-25
IL92208A0 (en) 1990-07-26
CY2007025I2 (el) 2009-11-04
FI92201C (fi) 1994-10-10
NO173015C (no) 1993-10-13
DK551989D0 (da) 1989-11-06
DE122007000081I2 (de) 2010-01-28
DK169923B1 (da) 1995-04-03
DE68922577D1 (de) 1995-06-14
CY2007025I1 (el) 2009-11-04
AU614437B2 (en) 1991-08-29
EP0368388B1 (en) 1995-05-10
DE68922577T2 (de) 1995-09-28
HK131696A (en) 1996-07-26
CL43432B (es) 2005-06-03
CA2000786C (en) 1999-01-26
EP0368388A2 (en) 1990-05-16
PT92206B (pt) 1995-07-06
CA2000786A1 (en) 1990-05-07
EP0368388A3 (en) 1991-07-17
IE66370B1 (en) 1995-12-27
KR0146053B1 (ko) 1998-08-17
NL300298I2 (nl) 2008-03-03
PT92206A (pt) 1990-05-31
NO894411D0 (no) 1989-11-06
JPH02191276A (ja) 1990-07-27
AU4443689A (en) 1990-05-10
NO2007017I1 (no) 2008-01-14
LU91362I2 (fr) 2007-11-12
IE893564L (en) 1990-05-07
DK551989A (da) 1990-05-08
DE122007000081I1 (de) 2008-02-28
CY1926A (en) 1989-10-30
FI92201B (fi) 1994-06-30
NZ231062A (en) 1991-09-25
NO2007017I2 (no) 2010-01-25
ATE122349T1 (de) 1995-05-15
ZA898436B (en) 1991-07-31

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