KR920700202A - 아크릴로일 치환된 피롤 유도체 - Google Patents

아크릴로일 치환된 피롤 유도체

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Publication number
KR920700202A
KR920700202A KR1019900702495A KR900702495A KR920700202A KR 920700202 A KR920700202 A KR 920700202A KR 1019900702495 A KR1019900702495 A KR 1019900702495A KR 900702495 A KR900702495 A KR 900702495A KR 920700202 A KR920700202 A KR 920700202A
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KR
South Korea
Prior art keywords
methyl
pyrrole
carboxamido
compound
salt
Prior art date
Application number
KR1019900702495A
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English (en)
Other versions
KR0170767B1 (ko
Inventor
몬젤리 니콜라
비아솔리 지오반니
카폴롱고 라우라
페쪼니 가브리엘라
Original Assignee
비토리노 페라리오
팜이탈리아 카를로 에르바 에스. 알. 엘.
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.)
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Application filed by 비토리노 페라리오, 팜이탈리아 카를로 에르바 에스. 알. 엘. filed Critical 비토리노 페라리오
Publication of KR920700202A publication Critical patent/KR920700202A/ko
Application granted granted Critical
Publication of KR0170767B1 publication Critical patent/KR0170767B1/ko

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic 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
    • C07D207/30—Heterocyclic 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
    • C07D207/34—Heterocyclic 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

Abstract

내용 없음

Description

아크릴로일 치환된 피롤 유도체
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (9)

  1. 하기 일반식(Ⅰ)의 화합물 및 이의 약제학적으로 허용가능한 염:
    상기식에서, n은 1 내지 5의 정수이고; R1및 R2는 각각 동일하거나 상이하며, 수소, 할로겐, －CN, －NO2, C1－C4알킬 또는 그룹이고; R3는 수소, 할로겐, －CN, －NO2,이며; R4는 각각 독립적으로 수소 또는 C1－C4알킬이고; A는 결합, 그룹또는 그룹 －NH－헤트－CO－(여기에서, 헤트는 포화 또는 불포화 펜타토믹 또는 헥사토믹 헤테로모노사이틀릭 환이다)이며 B는 그룹또는(여기에서 m은 1, 2 또는 3이고, R5는 각각 독립적으로 C1－C4알킬그룹이다)이다.
  2. 제1항에 있어서, n은 3, 4 또는 5이고; A는 결합 또는 그룹이며; B는 그룹이고;R1및 R2는 수소이며; R3는 염소 또는 브롬이고, R4는 메틸인 일반식(Ⅰ)의 화합물 및 이의 약제학적으로 허용가능한 산과의 염.
  3. N－데포밀－N(α－클로로아크릴로일)디스타마아신 A; β－(N－메틸－4－(N－메틸－4－(N－메틸－4－(N-메틸-4(α－클로로－아클릴아미도)피롤－2－카복스아미도)피롤－2－카복스아미도)피롤－2－카복스아미도)피롤－2－카복스아미도)프로피온아미딘; N－데포밀－N－(α－브로모아크릴로일)디스타마이신 A; β－(N－메틸－4－(N－메틸－4－(N－메틸－4－(N－메틸－4－(α－브로모아크릴－아미도)피롤－2－카복스아미도)피롤－2－카복스아미도)피롤－2－카복스아미도)피롤－2－카복스아미도)프로피온아미딘; β－(N－메틸－4－(N－메틸－4－(N－메틸－4－N－메틸－4－(N－메틸－4(α－브로모아크릴아미도)피롤－2－카복스아미도)피롤－2－카복스아미도)피롤－2－카복스아미도)피롤－2－카복스아미도)피롤－2－카복스아미도)프로피온아미딘; N－데포밀－N－(4－(α－브로모아크릴아미도) 벤조일)－디스타마아신 A; 3－(N－메틸－4－(N－메틸－4－4(N－메틸－4－(α－클로로아크릴아미도)피롤－2－카복스아미도)피롤－2－자복스아미도)피롤－2－자복스아미도)피놀－2－자복스아미도프로필－디메틸아민중에서 선택된 화합물 및 이의 약제학적으로 허용가능한 염.
  4. 제1항 내지 3항중 어느 한 항에 있어서, 염이 하이드로클로라이드인 염.
  5. A) 하기 일반식(Ⅱ)의 화합물 또는 이의 염을 일반식(Ⅲ)의 화합물과 반응시켜 일반식(Ⅰ)의 화합물 또는 이의 염을 수득하거나; B)하기 일반식(Ⅳ)의 화합물 또는 이의 염을 하기 일반식(Ⅴ)의 화합물과 반응시켜, A가 그룹또는 －NH－헤트인 일반식(Ⅰ)의 화합물 또는 이의 염을 수득함을 특징으로 하여, 제1항에 따른 일반식(Ⅰ)의 화합물 또는 이의 염을 제조하는 방법.
    상기식에서, R1, R2, R3, R4, A, B, 헤트 및 n은 제1항에서 정의된 것과 같으며; X는 하이드록시 또는 이탈그룹이고; Z은또는 H2N－헤트－CO－ 이다.
  6. 적합한 담체 및/또는 희석제 및 주요 활성물질로서 제1항에 따른 일반식(Ⅰ)의 화합물 또는 이의 약제학적으로 허용가능한 염을 함유하는 약제학적 조성물.
  7. 항종양제로서 유용한 제1항에 따른 화합물(Ⅰ)의 화합물 또는 이의 염.
  8. 항종양제로서 유용한 제6항에 따른 약제학적 조성물.
  9. 항종양제로서 유용한 약제학적 조성물의 제조에 있어서, 제1항에 따른 일반식(Ⅰ)의 화합물 또는 이의 염의 용도.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019900702495A 1989-03-23 1990-03-22 아크릴로일 치환된 피롤 유도체 KR0170767B1 (ko)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
GB8906709.4 1989-03-23
GB898906709A GB8906709D0 (en) 1989-03-23 1989-03-23 Acryloyl substituted pyrrole derivatives
GB89067094 1989-03-23
PCT/EP1990/000471 WO1990011277A1 (en) 1989-03-23 1990-03-22 Acryloyl substituted pyrrole derivatives

Publications (2)

Publication Number Publication Date
KR920700202A true KR920700202A (ko) 1992-02-19
KR0170767B1 KR0170767B1 (ko) 1999-02-01

Family

ID=10653895

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1019900702495A KR0170767B1 (ko) 1989-03-23 1990-03-22 아크릴로일 치환된 피롤 유도체

Country Status (22)

Country Link
US (1) US5175182A (ko)
EP (2) EP0388948B1 (ko)
JP (1) JP2986208B2 (ko)
KR (1) KR0170767B1 (ko)
AT (1) ATE98634T1 (ko)
AU (1) AU635733B2 (ko)
CA (1) CA2030519C (ko)
DE (1) DE69005164T2 (ko)
DK (1) DK0388948T3 (ko)
ES (1) ES2062143T3 (ko)
FI (1) FI95463C (ko)
GB (1) GB8906709D0 (ko)
HK (1) HK1006456A1 (ko)
HU (1) HU213507B (ko)
IE (1) IE64654B1 (ko)
IL (1) IL93816A0 (ko)
MY (1) MY106406A (ko)
NZ (1) NZ233015A (ko)
PT (1) PT93552B (ko)
RU (1) RU2094430C1 (ko)
WO (1) WO1990011277A1 (ko)
ZA (1) ZA902221B (ko)

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IT1247878B (it) * 1991-02-15 1995-01-05 Menarini Farma Ind Derivati poli-4-aminopirrol-2-carbossiamidici,processi di preparazione e composizioni farmaceutiche che li contengono
IT1262921B (it) * 1992-01-10 1996-07-22 Federico Arcamone Agenti antitumorali analoghi di oligopeptidi pirrol-amidinici retroversi processi di preparazione e prodotti farmaceutici che li contengono
IT1271456B (it) * 1993-03-01 1997-05-28 Menarini Farma Ind Composti pirrol-amidinici, e loro sali farmaceuticamente accettabili, processi di preparazione e composizioni farmaceutiche che li contengono
GB9416005D0 (en) * 1994-08-08 1994-09-28 Erba Carlo Spa Peptidic compounds analogous to distamycin a and process for their preparation
WO1997010208A1 (fr) * 1995-09-12 1997-03-20 Kyowa Hakko Kogyo Co., Ltd. Composes de souche uch 15
WO1998045284A1 (en) 1996-02-26 1998-10-15 California Institute Of Technology Stereochemical control of the dna binding affinity, sequence specificity, and orientation-preference of chiral hairpin polyamides in the minor groove
US6143901A (en) * 1996-07-31 2000-11-07 Genesoft, Inc. Complex formation between dsDNA and pyrrole imidazole polyamides
AU734715B2 (en) 1996-02-26 2001-06-21 California Institute Of Technology Improved polyamides for binding in the minor groove of double stranded DNA
US6555692B1 (en) 1996-02-26 2003-04-29 California Institute Of Technology Preparation and use of bifunctional molecules having DNA sequence binding specificity
US6635417B1 (en) 1996-07-31 2003-10-21 California Institute Of Technology Complex formation between DSDNA and oligomer of cyclic heterocycles
US6090947A (en) 1996-02-26 2000-07-18 California Institute Of Technology Method for the synthesis of pyrrole and imidazole carboxamides on a solid support
US6506906B1 (en) 1996-02-26 2003-01-14 California Institute Of Technology Preparation and use of bifunctional molecules having DNA sequence binding specificity
GB9615692D0 (en) * 1996-07-25 1996-09-04 Pharmacia Spa Acryloyl substituted distamycin derivatives, process for preparing them, and their use as antitumor and antiviral agents
US5998140A (en) * 1996-07-31 1999-12-07 The Scripps Research Institute Complex formation between dsDNA and oligomer of cyclic heterocycles
GB9806689D0 (en) * 1998-03-27 1998-05-27 Pharmacia & Upjohn Spa Acryloyl derivatives analogous to distamycin,process for preparing them,and their use as antitumour and antiviral agents
US6559125B1 (en) 2000-01-28 2003-05-06 California Institute Of Technology Polyamide-alkylator conjugates and related products and method
GB0011059D0 (en) * 2000-05-08 2000-06-28 Pharmacia & Upjohn Spa Use of substituted acryloyl distamycin derivatives in the treatment of tumours associated with high levels of glutathione
GB0015446D0 (en) 2000-06-23 2000-08-16 Pharmacia & Upjohn Spa Combined therapy against tumors comprising substituted acryloyl distamycin derivates,taxanes and/or antimetabolites
GB0015447D0 (en) 2000-06-23 2000-08-16 Pharmacia & Upjohn Spa Combined therapy against tumors comprising substituted acryloyl derivates and alkylating agents
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Also Published As

Publication number Publication date
CA2030519C (en) 2000-07-11
EP0416075A1 (en) 1991-03-13
AU635733B2 (en) 1993-04-01
JPH03504863A (ja) 1991-10-24
MY106406A (en) 1995-05-30
US5175182A (en) 1992-12-29
HU213507B (en) 1997-07-28
CA2030519A1 (en) 1990-09-24
PT93552B (pt) 1997-04-30
AU5276190A (en) 1990-10-22
DE69005164D1 (de) 1994-01-27
FI905758A0 (fi) 1990-11-21
IL93816A0 (en) 1990-12-23
ZA902221B (en) 1990-12-28
DK0388948T3 (da) 1994-01-24
FI95463B (fi) 1995-10-31
ES2062143T3 (es) 1994-12-16
KR0170767B1 (ko) 1999-02-01
GB8906709D0 (en) 1989-05-10
HU902839D0 (en) 1991-03-28
FI95463C (fi) 1996-02-12
EP0388948A1 (en) 1990-09-26
JP2986208B2 (ja) 1999-12-06
RU2094430C1 (ru) 1997-10-27
EP0388948B1 (en) 1993-12-15
ATE98634T1 (de) 1994-01-15
HK1006456A1 (en) 1999-02-26
IE901003L (en) 1990-09-23
HUT54981A (en) 1991-04-29
WO1990011277A1 (en) 1990-10-04
NZ233015A (en) 1991-09-25
DE69005164T2 (de) 1994-03-31
PT93552A (pt) 1990-11-07
IE64654B1 (en) 1995-08-23

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