KR950032111A - 당 알콜의 신규한 황산 에스테르 - Google Patents

당 알콜의 신규한 황산 에스테르 Download PDF

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KR950032111A
KR950032111A KR1019950000506A KR19950000506A KR950032111A KR 950032111 A KR950032111 A KR 950032111A KR 1019950000506 A KR1019950000506 A KR 1019950000506A KR 19950000506 A KR19950000506 A KR 19950000506A KR 950032111 A KR950032111 A KR 950032111A
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sulfo
penta
sodium salt
bis
glucit
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슈콜로프스키 알렉산더
핑게를 위르겐
이베르크 니기
페터 메르키 한스
뮐러 리타
페흐 미카엘
루우즈 마리안네
슈미트 제라르
쵸프 토마스
페터 베셀 한스
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프리돌린 클라우스너, 롤란드 보러
에프. 호프만-라 롯슈 아크티엔게젤샤프트
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Publication of KR950032111A publication Critical patent/KR950032111A/ko

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Abstract

본 발명은 하기 일반식 ( I ) 의 당 알콜 및 당 알콜-유사 화합물 및 그의 염의 신규한 황산 에스테르에 관한 것이다.
상기식에서, A는 하나 이상의 하이드록시 그룹이 황산으로 에스테르화된, 1-하이드록시 그룹이 없는 당 알콜 또는 이들의 유도체의 잔기이거나 또는 트리스-(하이드록시메틸)메틸 잔기이고; X는 -NR1CO-, -NHCONH-, -NHCSNH-, -NHSO2-, -NR1또는 -O-이고; m 및 p는 각각 독립적으로 O 또는 1이고; R1은 수소, 저급-알킬 또는 하이드록시-저급-알킬이며; B는 공액화된 다중 결합 시스템이다.
또한 본 발명은 일반식 (I)의 화합물 또는 그의 염을 함유하는 약학 제제; 특히 혈관 벽에서의 동맥경화성변화의 치료 및/또는 예방(예 : 관상 또는 말단 혈관성형술 또는 보조 수술 후의 재발협착증의 예방)을 위한 약제로서의 일반식 (I)의 화합물 및 그의 염의 용도; 일반식 (I )의 화합물 및 그의 염의 제조 방법 뿐만 아니라 상기 징후를 위한 약제의 제조에 관한 것이다.

Description

당 알콜의 신규한 황산 에스테르
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (10)

  1. 하기 일반식 (I)의 화합물 및 그의 염 :
    상기식에서, A는 하나 이상의 하이드록시 그룹이 황산으로 에스테르화된, 1-하이드록시 그룹이 없는 당 알콜 또는 이들의 유도체의 잔기이거나 또는 트리스-(하이드록시메틸)메틸 잔기이고; X는 -NR1CO-, -NHCONH-, -NHCSNH-, -NHSO2-, -NR1또는 -O-이고; m 및 p는 각각 독립적으로 0 또는 1이고; R1은 수소, 저급-알킬 또는 하이드록시-저급-알킬이며; B는 공액화된 다중 결합 시스템이다.
  2. 제1항에 있어서, X가 -NR1CO-, -NHCONH-, -NHCSNH-, -NHSO2-또는 -O-이고; B가 공액화된 이중 결합 시스템인 화합물 및 그의 염.
  3. 제1항에 있어서, A가 -(CHR2)nCH2R2이고, n은 1 내지 5의 정수이고, R2는 H, -OSO3H 또는 OZ이고, Z가 보호그룹이고, 적어도 하나의 잔기 R2가 -OSO3H인 화합물.
  4. 제1항 내지 제3항 중 어느 한 항에 있어서, 상기 공액화된 다중 결합 시스템 B가 2 내지 8개의 공액화된 다중 결합을 지닌 폴리엔 또는 폴리린 탄화수소 잔기인 화합물.
  5. 제1항 내지 제4항 중 어느 한 항에 있어서, 상기 공액화된 다중 결합 시스템 B가 공액화된 이중 결합의 시스템인 화합물.
  6. 제5항에 있어서, 상기 공액화된 이중 결합 시스템이 방향족 고리 시스템인 화합물.
  7. 제6항에 있어서, 상기 방향족 고리 시스템이 페닐렌; 저급-알킬 치환된 페닐렌; 나프틸렌, 플루오레닐렌; 또는 하기 일반식 (a) 내지 (s)중 하나의 잔기인 화합물 :
    상기식에서, Y는 탄소-탄소 결합, -O-, -CO-, -CH2-, -CH2-CH2-, -C≡C-, -CH(O)CH-, -CH=CH-, -SO2-, -C(CF3)2-, -CONR1-, -NHC0NH-, -NHCOCONH-, 페닐렌 또는 페닐렌디옥시이고; R1은 수소, 저급-알킬 또는 하이드록시-저급-알킬이고; R3및 R4는 수소, 저급-알킬, 저급-알콕시, 할로겐 또는 -SO3H이고; R5는 저급-알콕시-저급-알콕시, 페녹시 또는 할로겐에 의해 치환된 페녹시이고; R6은 수소 또는 SO5H이고; D는 -CH2CH2- 또는 -CH=CH-이며; V는 -CH=CH-, -CH2CH2- 또는 단일 결합을 의미한다.
  8. (Z)-부텐디오산(Z)-〔3-비페닐-4-일옥시메틸-5-〔3-(2,3,4,5,6-펜타-O-설포-D-글루시트-1-일카바모일)-아크릴로일아미노〕-페닐아미드〕-(2,3,4,5,6-펜타-O-설포-D-글루시트-1-일)-아미드 10나트륨 염, (E)-2-클로로스틸벤-4,4′-디카복실산 비스-(2,3,4,5,6-펜타-O-설포-D-글루시트-1-일아미드) 10나트륨 염, (Z)-스틸벤-4,4′-디카복실산 비스-(2,3,4,5,6-펜타-O-설포-D-글루시트-1-일아미드) 10나트륨 염,(2E,4E,6E,8E,1OE,12E,14E)-2,6,11,15-테트라메틸-헥사데카-2,4,6,8,10,12,14-헵타엔디카복실산 비스-(2,3,4,5,6-펜타-O-설포-D-글루시트-1-일아미드) 1O나트륨 염,4,4′-에틸렌-디벤조산 비스-(2,3,4,5,6-펜타-O-설포-D-글루시트-1-일아미드) 1O 나트륨 염, 3,3′-비스-(2,3,4,5,6-펜타-O-설포-D-글루시트-1-일)-1,1′-톨루엔-2,6-디일)-디우레아 1O 나트륨 염, 4,4′-비스-(2,3,4,5,6-펜타-O-설포-D-글루시트-1-일아미노)-3,3′-디니트로-N,N′-(4,4′-메틸렌-디페닐)-디벤즈아미드 10나트륨 염. N,N′-비스-(2,3,4,5,6-펜타-O-설포-D-글루시트-l-일)-2,2′-디니트로-4,4′-설포닐디아닐린 10나트륨 염, (Z)-스틸벤-4,4′-디카복실산 비스-(2,3,4,5,6-펜타-O-설포-L-람니트-1-일아미드) 8나트륨 염, 나프탈렌-1,5-디설폰산 비스-(2,3,4,5, 6-펜타-0-설포-D-글루시트-1-일아미드) 1O 나트륨 염, N,N′-비스-〔4-(2,3,4,5-테트라-O-설포-D-아라비니트-1-일옥시)-페닐〕-이소프탈아미드 8나트륨 염, 1,3-비스- 〔4-〔2,3,4,5,6-펜타-O-설포-D-갈락티트-6-일옥시)-페닐〕-우레아 10나트륨 염, N,N′-비스-〔4-〔3-(2,3,4,5,6-펜타-O-설포-D-글루시트-1-일)-우레이도〕-페닐〕-이소프탈아미드 10나트륨 염, 9-옥소-9H-플루오렌-2,7-디카복실산 비스-〔메틸-(2,3,4,5,6-펜타-O-설포-D-글루시트-1-일)아미드〕 10나트륨 염, 4,4′-메틸렌-디벤조산 비스-(2,3,4,5,6-펜타-O-설포-D-글루시트-1-일아미드) 10나트륨 염, 나프탈렌-2,6-디카복실산 비스-(2,3.4,5,6-펜타-O-설포-D-글루시트-1-일아미드) 10나트륨 염, N.N′-비스-(2,3,4,5,6-펜타-O-설포-D-글루시트-1-일)-이소프탈아미드 10나트륨 염, N,N′-비스-〔4-〔3-(2,3,4,5,6-펜타-O-설포-D-글루시트-1-일)-우레이도〕-페닐〕-푸마르아미드 1O나트륨 염, 4,4′-설포닐-디벤조산 비스-(2,3,4,5,6-펜타 -O-설포-D-글루시트-1-일아미드) 10나트륨 염.
  9. 특히 혈관벽중 동맥경화성 변화의 치료 및/또는 예방을 위한, 제1항 내지 제8항 중 어느 한 항에 따른 화합물, 및 치료적으로 불활성인 담체를 함유하는 약제.
  10. 제1항 내지 제8항 중 어느 한 항에 따른 화합물의 상응하는 비-황산화된 화합물을 황산화제와 반응시킴을 포함하는 제1항 내지 제8항 중 어느 한 항에 따른 화합물의 제조 방법.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019950000506A 1994-01-14 1995-01-13 당 알콜의 신규한 황산 에스테르 KR950032111A (ko)

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