KR970021066A - Novel Sulfonylaminopyrimidines - Google Patents

Novel Sulfonylaminopyrimidines Download PDF

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Publication number
KR970021066A
KR970021066A KR1019960045457A KR19960045457A KR970021066A KR 970021066 A KR970021066 A KR 970021066A KR 1019960045457 A KR1019960045457 A KR 1019960045457A KR 19960045457 A KR19960045457 A KR 19960045457A KR 970021066 A KR970021066 A KR 970021066A
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KR
South Korea
Prior art keywords
alkyl
hydrogen
phenyl
hydroxy
heterocyclyl
Prior art date
Application number
KR1019960045457A
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Korean (ko)
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KR100521950B1 (en
Inventor
하인쯔 란트샤이트
에트빈 리쩌
알렉산더 클라우세너
알렝 리옹델
장-미쉘 폴
볼커 브로
쟝-마리에 카쌀
죠르쥬 이르트
마르셀 뮐러
앙리 라뮈즈
카스파 뷰리
마르틴느 크로젤
베른트-미카엘 뢰플러
베르너 네이하르트
Original Assignee
클라우스 로이터, 귄터 슈마허
바이엘 악티엔게젤샤프트
리에 미쉘
엘프 아토켐 에스.에이.
클라우스너 프리돌린, 보러 롤란드
에프. 호프만-라 롯슈 아크티엔게젤샤프트
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from FR9512150A external-priority patent/FR2739854B1/en
Priority claimed from DE19540073A external-priority patent/DE19540073A1/en
Application filed by 클라우스 로이터, 귄터 슈마허, 바이엘 악티엔게젤샤프트, 리에 미쉘, 엘프 아토켐 에스.에이., 클라우스너 프리돌린, 보러 롤란드, 에프. 호프만-라 롯슈 아크티엔게젤샤프트 filed Critical 클라우스 로이터, 귄터 슈마허
Publication of KR970021066A publication Critical patent/KR970021066A/en
Application granted granted Critical
Publication of KR100521950B1 publication Critical patent/KR100521950B1/en

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic 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
    • C07D239/28Heterocyclic 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
    • C07D239/69Benzenesulfonamido-pyrimidines

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

하기 화학식(1)의 화합물은 약제로서, 특히 엔도텔린 활성과 연관된 장애를 치료하기 위해 사용될 수 있다 :The compounds of formula (1) may be used as medicaments, in particular for treating disorders associated with endothelin activity:

상기 식에서, R1내지 R6, Ra, Rb, X ,Y, Z, m 및 n은 하기의 상세한 설명에서 제시된 의미를 갖는다.Wherein R 1 to R 6 , R a , R b , X, Y, Z, m and n have the meanings given in the detailed description below.

Description

신규한 설포닐아미노피리미딘Novel Sulfonylaminopyrimidines

본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음Since this is an open matter, no full text was included.

Claims (4)

화학식(1)의 화합물 및 약학적으로 사용가능한 이의 염 :Compounds of formula (1) and pharmaceutically usable salts thereof: 상기 식에서, R1은 페닐, 치환된 페닐 또는 헤테로사이클릴이고; R2는 페닐 또는 치환된 페닐이고; R3는 하이드록시, 저급 알콕시 또는 -NR4R5잔기이고; R4는 수소 또는 -R6잔기이고, R5는 수소 또는 - (CH2)mR6잔기이거나 R4및 R5는 이들이 부착된 N 원자와 함께 N-헤테로사이클릭 잔기이고; R6는 페닐, 치환된 페닐, 사이클로알킬, 헤테로사이클릴, 저급 알킬, 하이드록시-저급-알킬, 아미노-저급-알킬, 카복시-저급-알킬 또는 저급-알콕시카보닐-저급-알킬이고; Ra는 수소, 저급알킬 또는 하이드록시이고; Rb는 수소 또는 저급 알킬이고; X는 산소 또는 황이고; Y는 산소 또는 황이고; Z는 수소, 저급 알킬, 아릴, 아릴-저급-알킬, 헤테로사이클릭 또는 헤테로사이클릴-저급-알킬이고; m은 0, 1 또는 2이고; n은 0, 1 또는 2이다.Wherein R 1 is phenyl, substituted phenyl or heterocyclyl; R 2 is phenyl or substituted phenyl; R 3 is hydroxy, lower alkoxy or —NR 4 R 5 residue; R 4 is hydrogen or —R 6 residues, R 5 is hydrogen or — (CH 2 ) mR 6 residues or R 4 and R 5 together with the N atom to which they are attached are N-heterocyclic residues; R 6 is phenyl, substituted phenyl, cycloalkyl, heterocyclyl, lower alkyl, hydroxy-lower-alkyl, amino-lower-alkyl, carboxy-lower-alkyl or lower-alkoxycarbonyl-lower-alkyl; R a is hydrogen, lower alkyl or hydroxy; R b is hydrogen or lower alkyl; X is oxygen or sulfur; Y is oxygen or sulfur; Z is hydrogen, lower alkyl, aryl, aryl-lower-alkyl, heterocyclic or heterocyclyl-lower-alkyl; m is 0, 1 or 2; n is 0, 1 or 2. 하기 일반식의 화합물.Compound of the following general formula. 상기 식에서, A는 포밀 또는 푸란-2-일이고, R1, R2, X, Z, Ra, Rb, Y 및 n은 제1항에 제시된 의미를 갖고, 여기서 화학식(2)에 OZ로 표시된 하이드록시 그룹 및 Ra로서 제시될 수 있는 하이드록시 그룹은 보호 형태로 제시될 수 있다.Wherein A is formyl or furan-2-yl and R 1 , R 2 , X, Z, R a , R b , Y and n have the meaning set forth in claim 1, wherein OZ in formula (2) The hydroxy group represented by and the hydroxy group which can be presented as R a can be presented in protective form. 제1항 내지 제10항의 화합물 및 사용가능한 담체 물질과 보조제를 함유하는 약학적 제제.A pharmaceutical formulation comprising the compound of claim 1 and a carrier material and adjuvant which can be used. 엔도텔린 활성, 특히 고혈압, 허혈, 혈관경련 및 협심증 등의 순환계 장애와 연관된 장애를 치료하는 약제의 제조를 위한 활성 성분으로서의 제1항 내지 제10항의 화합물의 용도.Use of the compound of claim 1 as an active ingredient for the manufacture of a medicament for the treatment of endothelin activity, in particular disorders associated with circulatory disorders such as hypertension, ischemia, vasospasm and angina pectoris. ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.※ Note: The disclosure is based on the initial application.
KR1019960045457A 1995-10-12 1996-10-11 Sulfonylaminopyrimidine KR100521950B1 (en)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
CH2893/95 1995-10-12
CH289395 1995-10-12
FR9512150A FR2739854B1 (en) 1995-10-17 1995-10-17 PROCESS FOR THE PREPARATION OF ALKYLIMIDAZOLIDONE (METH) ACRYLATES
FR9512150 1995-10-17
DE19540073A DE19540073A1 (en) 1995-10-27 1995-10-27 Process for the preparation of carbazates
DE19540073.9 1995-10-27

Publications (2)

Publication Number Publication Date
KR970021066A true KR970021066A (en) 1997-05-28
KR100521950B1 KR100521950B1 (en) 2006-02-03

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ID=66289974

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1019960045457A KR100521950B1 (en) 1995-10-12 1996-10-11 Sulfonylaminopyrimidine

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