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KR870011129A - 디스타마이신 a 동족체 및 이의 제조방법 - Google Patents

디스타마이신 a 동족체 및 이의 제조방법 Download PDF

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KR870011129A
KR870011129A KR870004929A KR870004929A KR870011129A KR 870011129 A KR870011129 A KR 870011129A KR 870004929 A KR870004929 A KR 870004929A KR 870004929 A KR870004929 A KR 870004929A KR 870011129 A KR870011129 A KR 870011129A
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carboxamido
pyrrole
methyl
compound
unsubstituted
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KR950011408B1 (ko
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라자리 에토레
아르카모네 페데리코
펜코 세르지오
안토니에타 베리니 마리아
몬겔리 니콜라
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비토리노 페라리오
팜이탈리아 카를로 엘바 에스.피.에이.
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/30Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/34Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms

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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pyrrole Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Plural Heterocyclic Compounds (AREA)
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  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
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Abstract

내용 없음

Description

디스타마이신 A 동족체 및 이의 제조방법
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (9)

  1. 일반식(Ⅰ)의 화합물 및 약제학적으로 허용되는 이의 염.
    상기 식에서,
    n은 2,3 또는 4이고;
    및 Het-(여기서, Het는 피롤을 제외한 5원 또는 6원 헤테로모노사이클릭 환이다)으로부터 선택한 2가 라디칼이며, 이 라디칼은 C1-C6알킬, C1-C6알콕시, 시아노 및 트리플루오로메틸로부터 선택한 하나 이상의 치환제로 치환되거나 비치환되며;
    R1및 R2중의 하나는 수소이고, 다른 하나는 a)그룹(여기서, R3는 할로겐원자로 치환되거나 비치환된 C1-C6알킬; 페닐; 또는 사이클로헥실이다)또는 b) 그룹-CO-(CH2)m-R4(여기서, m은 0,1,2 또는 3이고, R4는 수소, 할로겐, 하이드록시, 아지리디닐 또는 옥시라닐이다)이거나, R1및 R2는 동일하고, 둘다 수소, 또는 할로겐, 하이드록시 또는 C1-C6알콕시로 치환되거나 비치환된 C1-C6알킬그룹이다.
  2. 제 1 항에 있어서, n이 3이고 ; A가및 그룹-Het-〔여기서, -Het-는 산소, 황 및 질소로부터 선택한 1개 또는 2개의 헤테로원자를 함유하고 C1-C6알킬로 치환되거나 비치환된 5원 또는 6원 헤테로모노사이클릭 환(단, 피롤은 제외)이다〕으로부터 선택한 2가 라디칼이며;그룹는 (i)(여기서, R3는 비치환되거나, 할로-치환된 C1-C6알킬이다) 또는(ii)〔여기서 R1′및 R2′는 동일하고, 각각 할로-치환된 C1-C6알킬이다)〕인 일반식 (Ⅰ)의 화합물 및 약제학적으로 허용되는 이의 염.
  3. 제 2 항에 있어서, 5원 또는 6원 헤테로모노 사이클릭 환이 티오펜, 티아졸, 피리딘, 이소옥사졸, 푸란. 트리아졸, 이미다졸 또는 1-메틸-이미다졸인 화합물.
  4. 염산염 형태의,
    β-〔1-메틸-4-〔1-메틸-4-〔1-메틸-4-〔4-(N′-메틸-N′-니트로소우레이도벤젠)-1-카복스아미도〕피롤-2-카복스아미도〕피롤-2-카복스아미도〕피롤-2-카복스아미도〕프로피온아미딘;
    β-〔1-메틸-4-〔1-메틸-4-〔1-메틸-4-〔4-(N′-(2-클로로에틸)-N′-니트로소우레이도벤젠)-1-카복스아미도〕피롤-2-카복스아미도〕피롤-2-카복스아미도〕피롤-2-카복스아미도〕프로피온아미딘;
    β-〔1-메틸-4-〔1-메틸-4-〔1-메틸-4-〔4-N,N-비스(2-클로로에틸)아미노티오펜-2-카복스아미도〕피롤-2-카복스아미도〕피롤-2-카복스아미도〕피롤-2-카복스아미도〕프로피온아미딘;
    β-〔1-메틸-4-〔1-메틸-4-〔1-메틸-4-〔4-N,N-비스(2-클로로에틸)아미노벤젠-1-카복스아미도〕피롤-2-카복스아미도〕피롤-2-카복스아미도〕피롤-2-카복스아미도〕프로피온아미딘, 및 β-〔1-메틸-4-〔1-메틸-4-〔1-메틸-4-〔3-N,N-비스(2-클로로에틸)아미노벤젠-1-카복스아미도〕피헤-2-카복스아미도〕피롤-2-카복스아미도〕피롤-2-카복스아미도〕프로피온아미딘으로 이루어진 그룹 중에서 선택한 화합물.
  5. 일반식(Ⅱ)의 화합물을 일반식(Ⅲ)의 화합물과 반응시키고, 경우에 따라 일반식(Ⅰ)의 화합물을 염화하거나 염으로부터 유리 화합물을 수득하고/하거나, 경우에 따라, 일반식(Ⅰ)의 이성체 혼합물을 단일이성체로 분리시킴을 특징으로 하여 일반식(I)의 화합물 또는 약제학적으로 허용되는 이의 염을 제조하는 방법.
    상기 식에서,
    n은 2,3 또는 4이고 ;
    A는
    및 Het-(여기서, Het는 피롤을 제외한 5원 또는 6원 헤테로모노사이클릭 환이다)으로부터 선택한 2가 라디칼이며, 이 라디칼은 C1-C6알킬, C1-C6알콕시, 시아노 및 트리플루오로메틸로부터 선택한 하나 이상의 치환제로 치환되거나 비치환되고 ;
    R1및 R2중의 하나는 수소이고, 다른 하나는 a) 그룹(여기서, R3는 할로겐원자로 치환되거나 비치환된 C1-C6알킬;페닐;또는 사이클로헥실이다)또는 b) 그룹--CO-(CH2)m-R4(여기서, m은 0,1,2 또는 3이고, R4는 수소, 할로겐, 하이드록시, 아지리디닐 또는 옥시라닐이다)이거나, R1및 R2는 동일하고, 둘다 수소, 또는 할로겐, 하이드록시 또는 C1-C6알콕시로 치환되거나 비치환된 C1-C6알킬그룹이며 ;
    X 는 하이드록시 또는 이탈그룹이다.
  6. 활성 성분으로서 제 1 항에 따르는 일반식(Ⅰ)의 화합물 또는 약제학적으로 허용되는 이의 염과 , 약제학적으로 허용되는 담체 및/ 또는 희석제를 합유하는 약제학적 조성물.
  7. 항종양제 및 항바이러스제로서 사용하기 위한 제 1 항에 따르는 일반식(Ⅰ)의 화합물.
  8. 항종양제 및 항바이러스제로서 사용하기 위한 제 6 항에 따르는 약제학적 조성물.
  9. 항종양제 및 항바이러스제로서의 활성을 갖는 제 6 항에 따르는 약제학적 조성물을 제조하기 위한 제 1 항에 따르는 일반식(Ⅰ)의 화합물의 용도.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019870004929A 1986-05-20 1987-05-19 디스타마이신 a 동족체의 제조방법 Expired - Fee Related KR950011408B1 (ko)

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FR86210E (ko) * 1963-04-04 1966-03-23
FR141F (ko) * 1963-07-26
BR6461040D0 (pt) * 1963-07-26 1973-08-02 Farmaceutici Italia Processo para preparar novos derivados de pirrol
DE1795539A1 (de) * 1963-07-26 1972-01-13 Farmaceutici Italia Verfahren zur Herstellung von neuen Pyrrolderivaten und ihren Salzen
NL130086C (ko) * 1964-07-14 1970-06-15
CN85103908A (zh) * 1985-07-16 1986-11-05 法米塔利·卡洛·埃尔巴有限公司 制备4′-表多克索红菌素的新方法
GB8517922D0 (en) * 1985-07-16 1985-08-21 Erba Farmitalia Carboxamido derivatives

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EP0246868B1 (en) 1992-09-16
US5017599A (en) 1991-05-21
SU1528316A3 (ru) 1989-12-07
DE3781716T2 (de) 1993-03-11
IL82553A (en) 1991-06-10
NZ220361A (en) 1990-04-26
HUT44044A (en) 1988-01-28
FI872173A0 (fi) 1987-05-18
JPH0623193B2 (ja) 1994-03-30
PT84896B (pt) 1990-02-08
AU597659B2 (en) 1990-06-07
ATE80617T1 (de) 1992-10-15
CA1314551C (en) 1993-03-16
IE60198B1 (en) 1994-06-15
CS413791A3 (en) 1992-09-16
DK254587D0 (da) 1987-05-19
UA5928A1 (uk) 1994-12-29
PT84896A (en) 1987-06-01
BR1101017A (pt) 1999-12-07
MX9203122A (es) 1992-07-01
IE871292L (en) 1987-11-20
HU201336B (en) 1990-10-28
IL82553A0 (en) 1987-11-30
FI86543B (fi) 1992-05-29
FI86543C (fi) 1992-09-10
ES2046202T3 (es) 1994-02-01
GR3006163T3 (ko) 1993-06-21
FI872173L (fi) 1987-11-21
DE3781716D1 (de) 1992-10-22
DK254587A (da) 1987-11-21
JPS62294653A (ja) 1987-12-22
EP0246868A1 (en) 1987-11-25
BG60531B2 (bg) 1995-07-28
SG3793G (en) 1993-03-12
ZA873593B (en) 1987-11-12
KR950011408B1 (ko) 1995-10-04
GB8612218D0 (en) 1986-06-25
HK31993A (en) 1993-04-08
AU7316387A (en) 1987-11-26

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