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KR930007925A - 탁솔의 수용성 유도체 - Google Patents

탁솔의 수용성 유도체 Download PDF

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Publication number
KR930007925A
KR930007925A KR1019920017573A KR920017573A KR930007925A KR 930007925 A KR930007925 A KR 930007925A KR 1019920017573 A KR1019920017573 A KR 1019920017573A KR 920017573 A KR920017573 A KR 920017573A KR 930007925 A KR930007925 A KR 930007925A
Authority
KR
South Korea
Prior art keywords
taxol
salt
taxolsodium
taxols
oxy
Prior art date
Legal status (The legal status 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 status listed.)
Ceased
Application number
KR1019920017573A
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English (en)
Inventor
지.아이.킹스톤 데이비드
쟈오 지-양
Original Assignee
디오도르 콘
버지니아 테크 인텔렉츄얼 프러퍼티즈 인코포레이티드
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
Application filed by 디오도르 콘, 버지니아 테크 인텔렉츄얼 프러퍼티즈 인코포레이티드 filed Critical 디오도르 콘
Publication of KR930007925A publication Critical patent/KR930007925A/ko
Ceased legal-status Critical Current

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D305/00Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms
    • C07D305/14Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms condensed with carbocyclic rings or ring systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Epoxy Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

술폰화한 2'-아크로일 탁솔과 술폰화한 2′-0-아실란 탁솔 유도체는 생체활성은 유지하면서 수용성과 안정성이 증가하도록 합성된다. 특히 2′-〔(3-술포-1-옥소프로필)옥시〕탁솔소듐염은 탁솔을 아크릴산과 반응시키고, 2′-아크릴로일탁솔을 바이설파이트와 마이클 반응시킴으로써 얻어진다. 2′-{〔4-((2-슬포에틸)아미노)1.4-디옥소부틸〕옥시)탁솔소듐염과 2′-{〔4-((2-슬포에틸)아미노)1.4-디옥소부틸〕옥시)탁솔소듐염이 2′-숙시닐탁솔을 타우린의 테트라부틸 암모니움염과 3-아미노프로필술폰산과 각각 반응시키고, 후에 암모니움을 소둠으로 교환함으로써 얻어진다. 개선된 수용성을 갖는 2′-0-아실란 탁솔의 글리콜 유도체는 글리콜을 2′-0-아실란 탁솔과 반응시킴으로써 얻어진다.

Description

탁솔의 수용성 유도체
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
제 1 도는 탁솔의 구조와 대응하는 탁솔 구조의 부분에 따라 표시된 피크를 갖는 탁솔의 NMR 스펙트럼이다.
제 2 도는 2′-0-신나모일탁솔(2′-신나모일탁솔)의 NMR 스펙트럼이다.
제 3 도는 2′-2-크로토닐탁솔(2′-크로토닐탁솔)의 NMR 스펙트럼이다.

Claims (2)

  1. 다음의 일반식을 갖는 탁솔 유도체 :
    상기식에서 X.Y 및 Z는 H, 알킬, 아릴로 이루어진 군에서 선택된다.(단, Y나 Z의 어느 하나가 H 인 경우, 나머지 하나는 X와 같을수 없다.)
  2. 다음의 일반식을 갖는 탁솔의 수용성 유체.
    상기식에서, X,Y,Z 및 W는 H, 알킬과 아릴로 이루어진 군에서 선택되어지고, M은 H, 알칼리 금속과 암모니오기로 이루어진 군에서 선택되어진다.(단, W나 X의 어느 하나가 H이고, Y나 Z의 어느 하나가 H인 경우, 각각의 나머지 하나는 서로 같지 않다.)
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019920017573A 1991-10-15 1992-09-26 탁솔의 수용성 유도체 Ceased KR930007925A (ko)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US07/774,107 1991-10-15
US07/774,107 US5278324A (en) 1990-08-28 1991-10-15 Water soluble derivatives of taxol

Publications (1)

Publication Number Publication Date
KR930007925A true KR930007925A (ko) 1993-05-20

Family

ID=25100263

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1019920017573A Ceased KR930007925A (ko) 1991-10-15 1992-09-26 탁솔의 수용성 유도체

Country Status (13)

Country Link
US (1) US5278324A (ko)
EP (1) EP0537905B1 (ko)
KR (1) KR930007925A (ko)
AT (1) ATE135002T1 (ko)
CA (1) CA2080393A1 (ko)
CZ (1) CZ312292A3 (ko)
DE (1) DE69208802T2 (ko)
DK (1) DK0537905T3 (ko)
ES (1) ES2086669T3 (ko)
FI (1) FI924678L (ko)
GR (1) GR3020109T3 (ko)
NZ (1) NZ244754A (ko)
PL (2) PL296256A1 (ko)

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Also Published As

Publication number Publication date
FI924678L (fi) 1993-04-16
FI924678A0 (fi) 1992-10-15
CA2080393A1 (en) 1993-04-16
EP0537905A1 (en) 1993-04-21
PL296256A1 (en) 1993-10-18
CZ312292A3 (en) 1993-05-12
GR3020109T3 (en) 1996-08-31
DE69208802D1 (de) 1996-04-11
EP0537905B1 (en) 1996-03-06
NZ244754A (en) 1995-03-28
ATE135002T1 (de) 1996-03-15
DK0537905T3 (da) 1996-07-22
DE69208802T2 (de) 1996-10-02
ES2086669T3 (es) 1996-07-01
PL299303A1 (en) 1994-01-10
US5278324A (en) 1994-01-11

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