KR920000733A - 약학적활성 cns 화합물 - Google Patents

약학적활성 cns 화합물

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KR920000733A
KR920000733A KR1019910009010A KR910009010A KR920000733A KR 920000733 A KR920000733 A KR 920000733A KR 1019910009010 A KR1019910009010 A KR 1019910009010A KR 910009010 A KR910009010 A KR 910009010A KR 920000733 A KR920000733 A KR 920000733A
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amino
pyrimidine
compound
piperazinyl
trichlorophenyl
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KR1019910009010A
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존 리치 마이클
스터트 놉스 말콤
이어 라마칸드란
레오나드 이츠 클리브
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엠.피.잭슨
더 웰컴 파운데이숀 리미티드
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Publication of KR920000733A publication Critical patent/KR920000733A/ko

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48—Two nitrogen atoms
    • C07D239/49—Two nitrogen atoms with an aralkyl radical, or substituted aralkyl radical, attached in position 5, e.g. trimethoprim
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48—Two nitrogen atoms
    • 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
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

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  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurology (AREA)
  • Pharmacology & Pharmacy (AREA)
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  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
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  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
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Abstract

내용 없음

Description

약학적활성 CNS화합물
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (9)

  1. 하기 화합물들과 이들의 염으로 구성되는 군에서 선택된 화합물 :
    1. 2,4-디아미노-5-(3.5-디클로로페닐)-6-트리클루오로메틸 피리미딘;
    2. 2,4-디아미노-6-메틸-5-(2,3,6-트리클로로페닐)피리미딘;
    3. 2,4-디 아미노-5-(4-아미노-2,3,5-트리클로로페닐)피리미딘;
    4. 4-아미노-2-(4-메틸-1-피페라지닐)-6-메틸-5-(3,4,5-트리클로로페닐)피라미딘;
    5. 2,4-디아미노-5-(3,4,5-트리클로로페닐)-6-메틸피리미딘;
    6. 4-아미노-디에틸아미노-5-(2,3,5-트리클로로페닐)피리미딘;
    7. 4-아미노-2-(2-이소-프로필아미노)-5-(2,3,5-트리클로로페닐)피리미딘;
    8. 4-아미노-5-(3,5-디클로로페닐)-2-(4-메틸-1-피페라지닐)피라미딘;
    9. 2,4-디아미노-5-(4-요오드-2,3,5-트리클로로페닐)피리미딘;
    10. 4-아미노-2-(4-메틸-4-옥사이드-1-피페라지닐)-5-(2,3,5-트리클로로페닐)-6-트리플루오로메틸-피리미딘;
    11. 4-아미노-5-(3.5-디클로로페닐)-6-메톡시메틸-2-(4-메틸-1-피페라지닐)피리미딘;
    12. 2,4-디아미노-5[4-(N',N'-디메틸설파모일)-2,3,5-트리클로로페닐]피리미딘;
    13. 2-아미노-5-(2,3-디클로로페닐]-4-(1-피페리디닐)피티미딘;
    14. 4-아미노-5-(3,5-디클로로페닐)-2-(4-메틸-1-피페라디닐)-6-트리플루오로메틸 피리미딘;
    15. 2,4-디아미노-5(2,3,4,5-테트라클로로페닐)피리미딘;
    16. 시스 4-아미노-2-(3,5-디메틸-1-피페라지닐)-5-(2,3,5-트리클로로페닐)피리미딘;
    17. 4-아미노-2-(4-n-프로필-1-피페라지닐)-5-(2,3,5-트리클로로페닐)피리미딘;
    18. 4-아미노-2-(4-메틸-4-옥사이드-1-피페라지닐)-5-(2,3,5-트리클로로페닐)피리미딘;
    19. 2,4-디아미노-5-(3,5-디클로로-2-니트로페닐)-5-메틸피리미딘;
    20. 2-아미노-5-(2,3-디클로로페닐)-4-(4-메틸-1-피페라지닐)피리미딘;
    21. 2-아미노-5-(2,3-디클로로페닐)-4-(N-모르폴리노)피리미딘;
    22. 4-아미노-2-(4-벤질-1-피페라지닐)-5-(2,3,5-트리클로로페닐)피리미딘;
    23. 4-아미노-2-(N-모르폴리노)-5-(3,5-트리클로로페닐)-6-메틸피리미딘 ;
    24. 4-아미노-2-(N-모르폴리노)-5-(3,5-트리클로로페닐)-6-트리플루오로메틸 피리미딘;
    25. 2,4-다아미노-5-(3,5-디클로로-4-아미노페닐)피리미딘;
    26. 2,4-다아미노-5-(3.5-디클로로-4-아미노페닐)-6- 메틸피리미딘;
    27. 2,4-다아미노-5-(3,5-디클로로-4-아미노페닐)-6-트리플루오로메틸 피리미딘;
    28. 4-아미노-2-(4-n-부틸-1-피페라지닐)-5-(2,3,5-트리클로로메틸)피리미딘 ;
    29. 4-아미노-2-(4-에틸-1-피페라지닐)-5-(2,3,5-트리클로로메틸)피리미딘;
    30. 4-아미노-2-(4-이소프로필-1-피페라지닐)-5-(2,3,5-트리클로로메틸)피리미딘;
    31. 4-아미노-2-(4-시클로프로필-1-피페라지닐)-5-(2,3,5-트리클로로메틸)피리미딘;
    32. 4-아미노-2-(4-에틸-1-피페라지닐)-5-(3,5-디클로로메틸)-6-트리플루오로메틸 피리미딘;
    33. 4-아미노-2-(4-이소프로필-1-피페라지닐)-5-(3,5-더클로로메틸)-6-트리플루오로메틸 피리미딘;
    34. 4-아미노-2-(4-시클로프로필-1-피페라지닐)-5-(3,5-디클로로메틸)-6-트리플루오로메틸 피리미딘;
  2. 제1항에 있어서, 상기 화합물이 2,4-다아미노-5(4-아미노-2,3,5-트리클로로페닐)피리미딘: 4-아미노-5-(3,5-디클로로페닐)-2-(4-메틸-1-피페라지닐)피리미딘 : 4-아미노-2-(4-n-프로필-1-피페라지닐)-5-(2,3,5-트리클로로페닐)피리미딘; 4-아미노-2-(4-에틸-1-피페라지닐)-5-(2,3,5-트리클로로페닐)피리미딘: 또는 이들의 염인 화합물.
  3. 하기 일반식(I)의 화합물 또는 이들의 염 :
    상기식중, R1및 R2는 동일 또는 상이한 것으로 각각 -NR13R14(여기에서, R13및 R14는 각각 수소 또는 알킬이다)를 나타내거나, 이들이 결합된 질소원자와 함께 하나 이상의 알킬 또는 아릴알킬기에 의해 임의치환 되고 부가의 헤테로원자를 임의로 함유하는 헤테로시클릭고리를 형성하며 ; R3는 수소, 할로알킬, 알콕시메틸 또는 Cl-4알킬이며, R4는 수소 또는 니트로 또는 할로이며, R5는 수소 또는 할로이며, R6는 수소, 할로, 아미노, 알킬아미노 또는 디알킬아미노 이며, R7은 수소 또는 할로이며, R8은 수소 또는 할로이다.
  4. 제3항에 있어서, R1이 아미노, N-알킬아미노, N, N-디알킬아미노, N-모르폴리노, N-피페라지닐, N-4-알킬피페라진1-일 또는 N-4- (아릴알킬)피페라진-1-일이고; R2가 아미노 N-모르폴리노 또는 N-피페리디노인 화합물.
  5. 제3항 또는 제4항에 있어서, R5, R6및 R7이 각각 클로로 또는 요오드인 화할물.
  6. 제3항 또는 제4항에 있어서, R6이 아미노 이고 R5및 R7이 각각 클로로인 화합물.
  7. 제3항 또는 제4항에 있어서, R4및 R8이 모두 수소이고 R5및 R7이 모두 클로로이며, 단 R6이 수소, R2가 아미노, Rl이 아미노 또는 N-메틸피페라지닐일때는 R3가 메틸 또는 메톡시메틸인 화합물.
  8. (A)하기 일반식(Ⅱ)의 적당한 화합물 또는 이들의 염을 하기 일반식 (Ⅲ)희 적당한 화합물과 반응시킨후,필요에 따라 존재하는 보호기를 제거하거나 (일반식 (Ⅱ)및 (Ⅲ)의 화합물중 하나 또는 양자의 화합물은 선택적으로 이들의 보호된 유도체 형태로 사용된다) : (B)일반식 (Ⅱ)의 화합물 또는 이들의 염을 하기 일반식 (Ⅳ)의 화합물과 반응시킨후, 필요에 따라 존재하는 보호기를 제거하거나(일반식(Ⅱ) 및 (Ⅳ)의 화합물중 하나 또는 양자의 화합물은 선택적으로 이들의 보호된 유도체 형태로 사용된다) ; (C) 일반식 (Ⅱ)의 화합물 또는 이들의 염을 하기 일반식 (Ⅱ)의 화합물과 반응시킨후, 필요에 따라 존재하는 보호기를 제거하거나(일반식(Ⅱ) 및 (Ⅴ)의 화합물중 하나 또는 양자의 화합물은 선택적으로 이들의 보호된 유도체 형태로 사용된다) ; (D)상응하는 디히드로피미딘 또는 이들의 보호된 유도체를 탈수소화 시킨후, 필요에 따라 존재하는 보호기를 제거하거나; (E)제1항 내지 제7항중 어느 한항의 화합물을 다른 화합물로 상호 전환시키고: 선택적으로 생성된 유리염기 형태의 화합물을 염으로 전환시키거나 생성된 염을 다른 염으로 전환시키는 것으로 구성되는 제1항 내지 제7항중 어느 한항의 화합물 또는 이들의 염을 제조하는 방법.
    상기식중, R1및R2내지 R3은 제조하고자 하는 화합물에 적당한 의미를 가지며,;Y는 시아노,카로복시,카르보닐 또는 알콕시카르보닐이고; L은 이탈기이며, R11및 R1는 각각 알킬이거나 함께 기(CR2)n(여기서 n은 2내지 4이고 R은 각각 수소 또는 알킬이다)을 형성한다.
  9. 제1항 내지 제7항중 어느 한항의 화합물 또는 이들의 약학적 허용 염과 적어도 하나의 약학적허용 담체를 포함하는 약학 조성물.
    ※ 참고사항 : 최초출원 내용에 의하여 공개되는 것임.
KR1019910009010A 1990-06-01 1991-05-31 약학적활성 cns 화합물 KR920000733A (ko)

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GB909012316A GB9012316D0 (en) 1990-06-01 1990-06-01 Pharmacologically active cns compounds
GB9012316.7 1990-06-01

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FI895821A0 (fi) * 1988-12-07 1989-12-05 Wellcome Found Farmaceutiskt aktiva cns foereningar.
FR2671970B1 (fr) * 1991-01-30 1995-06-23 Wellcome Found Comprimes dispersables dans l'eau.
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AU652753B2 (en) 1994-09-08
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DE69121317D1 (de) 1996-09-19
TW224460B (ko) 1994-06-01
GR3021237T3 (en) 1997-01-31
PL166656B1 (pl) 1995-06-30
ATE141263T1 (de) 1996-08-15
FI912623A (fi) 1991-12-02
NO180375B (no) 1996-12-30
ZA914165B (en) 1993-03-01
EP0459819A3 (en) 1992-03-11
CA2043640A1 (en) 1991-12-02
JPH06340634A (ja) 1994-12-13
SK278444B6 (en) 1997-05-07
PT97827A (pt) 1992-03-31
FI912623A0 (fi) 1991-05-31
GB9012316D0 (en) 1990-07-18
HU911826D0 (en) 1991-12-30
CZ281070B6 (cs) 1996-06-12
ES2093078T3 (es) 1996-12-16
PT97827B (pt) 1998-10-30
IL113599A0 (en) 1995-08-31
MY109958A (en) 1997-10-31
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NO912100L (no) 1991-12-02
AU7809791A (en) 1991-12-05
AU680252B2 (en) 1997-07-24
EP0459819A2 (en) 1991-12-04
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RU2091374C1 (ru) 1997-09-27
NZ248501A (en) 1997-03-24
HU211649A9 (en) 1995-12-28
HUT58707A (en) 1992-03-30
IL98330A (en) 1996-10-31
EP0459819B1 (en) 1996-08-14
CS164391A3 (en) 1992-02-19
NO912100D0 (no) 1991-05-31
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MY136248A (en) 2008-08-29
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AU6745594A (en) 1994-09-15
PL170373B1 (pl) 1996-12-31
IE911861A1 (en) 1991-12-04

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