KR900012916A - 치환된 피리미딘 유도체, 이의 제조방법 및 툴(tool)로서의 이의 용도 - Google Patents

치환된 피리미딘 유도체, 이의 제조방법 및 툴(tool)로서의 이의 용도 Download PDF

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KR900012916A
KR900012916A KR1019900002027A KR900002027A KR900012916A KR 900012916 A KR900012916 A KR 900012916A KR 1019900002027 A KR1019900002027 A KR 1019900002027A KR 900002027 A KR900002027 A KR 900002027A KR 900012916 A KR900012916 A KR 900012916A
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alkyl
formula
hydrogen
compound
carbamoyl
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가이센 카를
요켄 랑 한스
님메스게른 할데가르트
바이드만 클라우스
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엔겔하르트, 벡커
훽스트 아크티엔게젤샤프트
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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
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/42—One nitrogen atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K49/00—Preparations for testing in vivo
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics

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  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Diabetes (AREA)
  • Life Sciences & Earth Sciences (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
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  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)

Abstract

내용 없음

Description

치환된 피리미딘 유도체, 이의 제조방법 및 툴(tool)로서의 이의용도
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (6)

  1. 일반식(Ⅰ)의 피리미딘 유사체 및 이의 생리학적으로 허용되는 염.
    상기식에서, R1, R4및 R5는 동일하거나 상이하며, 수소, 할로겐, 시아노, 니트로, 트리플루오로메틸, (C1-C6)-알킬, (C1-C6)-하이드록시알킬, (C1-C6)-알콕시, (C6-C12) 아릴 또는 아미노를 나타내고, R2및 R3는 동일하거나 상이하며, 수소 (C1-C6)-알킬, (C6-C12)-아릴 또는 1 내지 4개의 탄소원자를 갖는 (C6-C12)-아르알킬이거나, R2및 R3가 이들이 결합된 질소와 함께는 아제티디노, 피롤리디노, 피페리디노, 피페라지노, 또는 모르폴리노 그룹, 또는 동일하거나 상이한 그룹 R6및 R7에 의해 치환된 아제티디노, 피롤리디노, 피페리디노, 피페라지노 또는 모르폴리노 그룹을 형성하며, R6및 R7은 (C1-C6)-알킬 : 설파모일 : N-(C1-C4)-알킬카바모닐 : N,N-(C1-C4)-디알킬 설파모일, (C1-C6)-알콕시카보닐, N,N-(C1-C4)-디알킬 카바모일, N-(C1-C4)-알킬카바모일, N-(C6-C12)-아릴카바모일 : 아릴 라디칼에서 (C1-C4)-알킬, (C1-C4)-알콕시, 할로겐, NO2, NH2, CN 또는 CF3에 의해 치환된 (C6-C12)-아릴카바모일 : 카바모일 : (C1-C6)-알킬카보닐 : (C6-C12)-아릴카보닐 : 아릴 라디칼에서 (C1-C4)-알킬, (C1-C4)-알콕시, 할로겐, NO2, NH2, CN 또는 CF3에 의해 치환된 (C6-C12) 아릴카보닐 : (C1-C6)-알킬설포닐 : (C1-C6)-알킬설피닐 : (C6-C12) 아릴설포닐 : 아릴 라디칼에서 (C1-C4)-알콕시, 할로겐, NO2, NH2, CN 또는 CF3에 의해 치환된 (C6-C12) 아릴설포닐 : 헤테로아릴카보일 : 또는 헤테로아릴설포닐 이거나, 치환체 R6및 R7중 하나는 수소이다.
  2. 제1항에 있어서, R1, R4및 R5는 동일하거나 상이하며, 수소 또는 (C1-C6)-알킬이고, R2및 R3가 이들이 결합된 질소와 함께 동일하거나 상이한 그룹 R6및 R7에 의해 임의로 치환된 피페리진환을 형성하며, R6및 R7이 (C1-C6)-알킬 : 설파모일 : N-(C1-C4)-알킬설파모일 : N,N-(C1-C4)-디알킬 설파모일 : (C1-C6)-알콕시카보닐; N, N-(C1-C4)-알킬카바모일: 카바보일: (C 1-C6-알콕시카보닐: N, N-(C1-C4)-디알킬카바모일: 카바모일: (C1-C6)-알킬카보닐: (C6-C12)-아릴카보닐: 아릴 라디칼에서 (C1-C4)-알킬, (C1-C4)-알콕시, 할로겐 NO2, NH2, CN 또는 CF3에 의해 치환된 (C6-C12) 아릴카보닐 : (C1-C6) 알킬설포닐 : (C1-C6)-알킬 설피닐 : (C1-C12)-아릴설포닐 : 아릴 라디칼에서 (C1-C4)-알킬, (C1-C4)-알콕시, 할로겐 NO2, NH2, CN 또는 CF3에 의해 치환된 (C6-C12) 아릴 설포닐 : 헤테로아릴카보닐 : 또는 헤테로아릴설포닐 이거나, 치환체 R6및 R7중 하나가 수소인 일반식(Ⅰ)의 피리미딘 유사체 및 이의 생리학적으로 허용되는 염.
  3. 제1항에 있어서, R1, R4및 R5는 동일하거나 상이하며, 수소 또는 (C1-C4)-알킬이고, R2및 R3가 이들이 결합된 질소와 함께 위치 4에서 또다른 치환체 R6를 임의로 갖는 피페라진 환을 형성하며, R6가 설파모일 : N-(C1-C4)-알킬설파모일 : N,N-(C1-C4)-디알킬설파모일 : 카바모일, N-(C1-C4)-알킬 카바모일, N,N-(C1-C4)-디알킬설파모일, (C1-C6)-알킬카보닐 : (C6-C12)-아릴카보닐 : 아릴 라디칼에서 (C1-C4)-알킬, (C1-C4)-알콕시, 할로겐, NO2, NH2, CN 또는 CF3에 의해 치환된 (C6-C12) 아릴카보닐 : 또는 피리딘카보닐인 일반식(Ⅰ)의 피리미딘 유사체 및 이의 생리학적으로 허용되는 염.
  4. 제1항에 있어서, R1이 수소 또는 (C1-C6)-알킬, 특히 메틸이고, R4가 수소 또는 (C1-C2)-알킬, 특히 수소이며, R5가 수소이고, R2및 R3가 이들이 결합된 질소와 함께 위치 4에서 또다른 치환체 R6를 임의로 갖는 피페리진환을 형성하며, R6가 N-(C1-C3)-알킬설파모일 : N,N(C1-C2)-디알킬설파모일 : N-(C1-C2)-알킬카바모일 : N,N-(C1-C2)-디알칼카바모일 : (C1-C2)-알킬카보닐 : 페닐 라디칼에서 (C1-C2)-알킬, 염소 또는 NO2에 의해 치환된 페닐카보닐 : 또는 피리딘카보닐, 특히 N,N-디메틸설파모일, 페닐카보닐 또는 피리딘카보닐인 일반식(Ⅰ)의 피리미딘 유도체 및 이의 생리학적으로 허용되는 염.
  5. (a) 일반식(Ⅱ)의 화합물 또는 이의 산부가염을 일반식(Ⅲ)의 화합물 또는 이의 염기 부가염과 반응시켜 일반식(Ⅳ)의 화합물을 수득하고, (b) 생성된 화합물(Ⅳ)을 무기산 염화물과 반응시켜 일반식(Ⅴ)의 피리미딘 유도체를 수득한 후, (c) 생성된 일반식(Ⅴ)의 화합물을 일반식(Ⅵ)의 아민과 반응시켜 일반식(Ⅰ)의 화합물을 수득하고, (d) 필요한 경우, 치환체 R2/R3중 하나 또는 두 개 모두가 수소인 일반식(Ⅰ)의 화합물을 R2/R3가 일반식(Ⅰ)에서 정의된 의미(여기에서 수소는 제외된다)를 갖는 일반식(Ⅰ)의 화합물로 전환시키거나, (e)필요한 경우, R2및 R3가 이들이 결합된 질소원자가 함께 아제티디노, 피롤리디노, 피페리디노 피페라지노 또는 모르폴리노 라디칼을 형성하는 일반식(Ⅰ)의 화합물에 라디칼 R6/R7을 도입시키거나, (f) 필요한 경우, 생성된 일반식(Ⅰ)의 화합물을 생리학적으로 허용되는 염으로 전환시킴을 특징으로 하여, 일반식(Ⅰ)의 화합물을 제조하는 방법.
    상기식에서, R1,R2,R3,R4및 R5는 제1항에서 정의한 바와 같고, R8은 메틸 또는 에틸이다.
  6. 약물학적 모델에서 툴(tool)로서의 제1항에 따른 일반식(Ⅰ)의 화합물 및 이의 염의 용도.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019900002027A 1989-02-22 1990-02-20 치환된 피리미딘 유도체 KR0142189B1 (ko)

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DE3905364A DE3905364A1 (de) 1989-02-22 1989-02-22 Substituierte pyrimidin-derivate, verfahren zu ihrer herstellung und ihre verwendung als tool
DEP3905364.4 1989-02-22

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KR900012916A true KR900012916A (ko) 1990-09-03
KR0142189B1 KR0142189B1 (ko) 1998-06-01

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PH27222A (en) 1993-05-04
NO900822L (no) 1990-08-23
NO900822D0 (no) 1990-02-21
EP0384370A1 (de) 1990-08-29
EP0384370B1 (de) 1993-11-03
DE59003274D1 (de) 1993-12-09
US5138058A (en) 1992-08-11
CA2010588A1 (en) 1990-08-22
FI95694C (fi) 1996-03-11
AU4997590A (en) 1990-08-30
ZA901309B (en) 1990-10-31
NZ232601A (en) 1991-12-23
IE63570B1 (en) 1995-05-17
CA2010588C (en) 2000-01-18
IL93465A0 (en) 1990-11-29
ES2060829T3 (es) 1994-12-01
FI900839A0 (fi) 1990-02-20
JP2955318B2 (ja) 1999-10-04
AU634751B2 (en) 1993-03-04
JPH02255662A (ja) 1990-10-16
PT93224A (pt) 1990-08-31
NO178431C (no) 1996-03-27
IL93465A (en) 1995-03-30
FI95694B (fi) 1995-11-30
KR0142189B1 (ko) 1998-06-01
IE900627L (en) 1990-08-22
ATE96787T1 (de) 1993-11-15
NO178431B (no) 1995-12-18
DE3905364A1 (de) 1990-08-23
PT93224B (pt) 1996-09-30
DK0384370T3 (da) 1994-03-07

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