KR970706251A - Bis- (2-haloethyl) aminophenyl substituted distamycin derivatives as antitumor and antiviral agents as antitumor agents and antiviral agents, - Google Patents

Bis- (2-haloethyl) aminophenyl substituted distamycin derivatives as antitumor and antiviral agents as antitumor agents and antiviral agents,

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Publication number
KR970706251A
KR970706251A KR1019970701796A KR19970701796A KR970706251A KR 970706251 A KR970706251 A KR 970706251A KR 1019970701796 A KR1019970701796 A KR 1019970701796A KR 19970701796 A KR19970701796 A KR 19970701796A KR 970706251 A KR970706251 A KR 970706251A
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KR
South Korea
Prior art keywords
carboxamido
pyrrole
methyl
bis
propionamidine
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KR1019970701796A
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Korean (ko)
Inventor
파올로 코찌
이탈로 베리아
라우라 카폴론고
크리스티나 프란쩨띠
Original Assignee
메텔리 라펠라
파마시아 앤드 업죤 에스 피 에이
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Application filed by 메텔리 라펠라, 파마시아 앤드 업죤 에스 피 에이 filed Critical 메텔리 라펠라
Publication of KR970706251A publication Critical patent/KR970706251A/en

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    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents

Abstract

본 발명은 신규한 항종양제 및 항바이러스제인 화학식(Ⅰ)의 화합물 및 이의 염에 관한 것이다.The present invention relates to novel antitumor agents and antiviral agents, compounds of formula (I) and salts thereof.

상기 식에서, n은 2,3 또는 4이고, R 및 R1중의 하나는 수소, C1-C4알킬, CF3또는 C1-C4알콕시이고 다른 하나는 독립적으로 CF3, C1-C4알킬 또는 C1-C4알콕시이며, X는 할로겐이다.Wherein n is 2, 3 or 4 and one of R and R 1 is hydrogen, C 1 -C 4 alkyl, CF 3 or C 1 -C 4 alkoxy and the other is independently CF 3 , C 1 -C 4 alkyl or C 1 -C 4 alkoxy, and X is halogen.

Description

항종양제 및 항바이러스제로서의 비스-(2-할로에틸)아미노페닐 치환된 디스타마이신 유도체(Bis-(2-haloethyl)aminophenyl substituted distamycin derivatives as antitumor and antiviral agents)Bis- (2-haloethyl) aminophenyl substituted distamycin derivatives as antitumor and antiviral agents as antitumor agents and antiviral agents,

본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음Since this is a trivial issue, I did not include the contents of the text.

Claims (10)

화학식(Ⅰ)의 화합물 및 이의 약제학적으로 허용되는 염.Compounds of formula (I) and pharmaceutically acceptable salts thereof. 상기 식에서, 2,3 또는 4이고, R 및 R1중의 하나는 수소, C1-C4알킬, CF3또는 C1-C4알콕시이고 다른 하나는 독립적으로 CF3, C1-C4알킬 또는 C1-C4콕시이며, X는 할로겐이다.Wherein one of R and R 1 is hydrogen, C 1 -C 4 alkyl, CF 3 or C 1 -C 4 alkoxy and the other is independently CF 3 , C 1 -C 4 alkyl Or C 1 -C 4 alkoxy, and X is halogen. 제1항에 있어서, n이 3이고, X가 클로로이며, R 및 R1중의 하나는 수소, C1-C4알킬이고 다른 하나는 C1-C4알킬, CF3또는 C1-C4알콕시인 화학식(Ⅰ)의 화합물 및 이의 약제학적으로 허용되는 염.According to claim 1, wherein n is 3, X is chloro, one of R and R 1 is hydrogen, C 1 -C 4 alkyl, the other is C 1 -C 4 alkyl, CF 3 or C 1 -C 4 Lt; RTI ID = 0.0 > (I) < / RTI > and pharmaceutically acceptable salts thereof. β-[1-메틸-4-[1-메틸-4-[1-메틸-4-[3-메틸-4-N,N-비스(2-클로로에틸)아미노벤젠-1-카복스아미도]피롤-2-카복스아미도]피롤-2-카복스아미도]피롤-2-카복스아미도]프로피온아미딘; β-[1-메틸-4-[1-메틸-4-[1-메틸-4-[3,5-디메틸-4-N,N-비스(2-클로로에틸)아미노벤젠-1-카복스아미도]피롤-2-카복스아미도]피롤-2-카복스아미도]피롤-2-카복스아미도]프로피온아미딘; β-[1-메틸-4-[1-메틸-4-[3-에틸-4-N,N-비스(2-클로로에틸)아미노벤젠-1-카복스아미도]피롤-2-카복스아미도]피롤-2-카복스아미도]피롤-2-카복스아미도]프로피온아미딘; β-[1-메틸-4-[1-메틸-4-[1-메틸-4-[3,3-디에틸-4-N,N-비스(2-클로로에틸)아미노벤젠-1-카복스아미도]피롤-2-카복스아미도]피롤-2-카복스아미도]피롤-2-카복스아미도]프로피온아미딘; β-[1-메틸-4-[1-메틸-4-[1-메틸-4-[3-메톡시-4-N,N-비스(2-클로로에틸)아미노벤젠-1-카복스아미도]피롤-2-카복스아미도]피롤-2-카복스아미도]피롤-2-카복스아미도]프로피온아미딘; β-[1-메틸-4-[1-메틸-4-[1-메틸-4-[2-메톡시-4-N,N-비스(2-클로로에틸)아미노벤젠-1-카복스아미도]피롤-2-카복스아미도]피롤-2-카복스아미도]피롤-2-카복스아미도]프로피온아미딘; β-[1-메틸-4-[1-메틸-4-[1-메틸-4-[2-메틸-4-N,N-비스(2-클로로에틸)아미노벤젠-1-카복스아미도]피롤-2-카복스아미도]피롤-2-카복스아미도]피롤-2-카복스아미도]프로피온아미딘; β-[1-메틸-4-[1-메틸-4-[2-메틸-4-N,N-비스(2-클로로에틸)아미노벤젠-1-카복스아미도]피롤-2-카복스아미도]피롤-2-카복스아미도]피롤-2-카복스아미도]프로피온아미딘; β-[1-메틸-4-[1-메틸-4-[1-메틸-4-[3-트리프루오로메틸-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-[3-트리플루오로메틸-5-메틸-4-N,N-비스(2-클로로에틸)아미노벤젠-1-카복스아미도]피롤-2-카복스아미도]피롤-2-카복스아미도]프로피온아미딘중에서 선택된 화합물 및 이의 약제학적으로 허용되는 염.methyl-4- [1-methyl-4- [3-methyl-4-N, N- bis (2-chloroethyl) aminobenzene-1-carboxamido ] Pyrrole-2-carboxamido] pyrrole-2-carboxamido] pyrrole-2-carboxamido] propionamidine; methyl-4- [1-methyl-4- [3,5-dimethyl-4-N, N-bis (2-chloroethyl) aminobenzene- Amido] pyrrole-2-carboxamido] pyrrole-2-carboxamido] pyrrole-2-carboxamido] propionamidine; methyl-4- [3-ethyl-4-N, N-bis (2-chloroethyl) aminobenzene-1-carboxamido] pyrrole- Amido] pyrrole-2-carboxamido] pyrrole-2-carboxamido] propionamidine; methyl-4- [1-methyl-4- [3,3-diethyl-4-N, N-bis (2-chloroethyl) aminobenzene- 2-carboxamido] pyrrole-2-carboxamido] pyrrole-2-carboxamido] propionamidine; methyl-4- [1-methyl-4- [3-methoxy-4-N, N- bis (2- chloroethyl) aminobenzene- Carboxamido] pyrrole-2-carboxamido] pyrrole-2-carboxamido] propionamidine; methyl-4- [1-methyl-4- [2-methoxy-4-N, N-bis (2-chloroethyl) aminobenzene- Carboxamido] pyrrole-2-carboxamido] pyrrole-2-carboxamido] propionamidine; methyl-4- [1-methyl-4- [2-methyl-4-N, N-bis (2-chloroethyl) aminobenzene-1-carboxamido ] Pyrrole-2-carboxamido] pyrrole-2-carboxamido] pyrrole-2-carboxamido] propionamidine; methyl-4- [2-methyl-4-N, N-bis (2-chloroethyl) aminobenzene-1-carboxamido] pyrrole- Amido] pyrrole-2-carboxamido] pyrrole-2-carboxamido] propionamidine; methyl-4- [1-methyl-4- [3-trifluoromethyl-4-N, N- bis (2- chloroethyl) Carboxamido] pyrrole-2-carboxamido] pyrrole-2-carboxamido] pyrrole-2-carboxamido] propionamidine and [ 4-N, N-bis (2-chloroethyl) aminobenzene-1-carboxamido] pyrrole-2- carboxamido] pyrrole- ≪ / RTI > carboxamido] propionamidine, and pharmaceutically acceptable salts thereof. 제3항에 있어서, 하이드로클로라이드 염인 화합물.4. The compound of claim 3 which is a hydrochloride salt. 화학식(Ⅱ)의 화합물을 화하식(Ⅲ)의 화합물과 반응시키고, 경우에 따라 화학식(Ⅰ)의 화합물을 염화하거나 이의 염으로부터 유리 화합물을 수득하고/하거나, 경우에 따라 화학식(Ⅰ)의 화합물의 이성체의 혼합물을 단일 이성체로 분리함을 특징으로 하여, 제1항에 따른 화학식(Ⅰ)의 화합물 또는 이의 염을 제조하는 방법.Reacting a compound of the formula (II) with a compound of the formula (III), optionally chlorinating the compound of the formula (I) or obtaining a free compound from the salt thereof and / (I) according to claim 1, or a salt thereof, characterized in that a mixture of isomers of formula (I) is separated into a single isomer. 상기 식에서, R, R1및 X는 제1항에 정의된 바와 같고, Y는 하이드록시 또는 이탈 그룹이다.Wherein R, R 1 and X are as defined in claim 1 and Y is hydroxy or a leaving group. 적합한 담체 및/또는 희석제 및 활성 성분으로서 제1항에 따른 화학식(Ⅰ)의 화합물 또는 이의 약제학적으로 허용되는 염을 함유하는 약제학적 조성물.A pharmaceutical composition comprising a suitable carrier and / or diluent and as active ingredient a compound of formula (I) according to claim 1, or a pharmaceutically acceptable salt thereof. 제1항에 있어서, 항종양제 및 항바이러스제로서 사용하기 위한 화학식(Ⅰ)의 화합물 또는 이의 약제학적으로 허용되는 염.The compound of formula (I) according to claim 1 for use as an antitumor agent and an antiviral agent, or a pharmaceutically acceptable salt thereof. 항암 치료시 동시에, 별도로 또는 연속적으로 사용하기 위한 배합 제제로서의 제1항에 따른 화학식(Ⅰ)의 화합물 또는 이의 약제학적으로 허용되는 염 및 추가의항종양제를 함유하는 제품.An article of manufacture comprising a compound of formula (I) according to claim 1, or a pharmaceutically acceptable salt thereof, and an additional antineoplastic agent as combination preparations for simultaneous, separate or sequential use in chemotherapy. 항종양제 및 항바이러스제로서 사용하기위한 약제학적 조성물의 제조에서 제1항에 따른 화학식(Ⅰ)의 화합물 또는 이의 약제학적으로 허용되는 염의 용도.Use of a compound of formula (I) according to claim 1, or a pharmaceutically acceptable salt thereof, in the manufacture of a pharmaceutical composition for use as an antitumor agent and an antiviral agent. 치료학적 유효량의 제1항에 따른 화학식(Ⅰ)의 화합물 또는 이의 약제학적으로 허용되는 염을 항종양제를 필요로 하는 포유동물에게 투여함을 특징으로 하여, 상기 포유 동물을 치료하는 방법.A therapeutically effective amount of a compound of formula (I) according to claim 1, or a pharmaceutically acceptable salt thereof, is administered to a mammal in need of such treatment. ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.※ Note: It is disclosed by the contents of the first application.
KR1019970701796A 1995-07-21 1996-09-19 Bis- (2-haloethyl) aminophenyl substituted distamycin derivatives as antitumor and antiviral agents as antitumor agents and antiviral agents, KR970706251A (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GBGB9514993.6A GB9514993D0 (en) 1995-07-21 1995-07-21 Site specific phenyl nitrogen mustards
GB9514993.6 1995-07-21
PCT/EP1996/002659 WO1997003957A1 (en) 1995-07-21 1996-06-19 Bis-(2-haloethyl)aminophenyl substituted distamycin derivatives as antitumor and antiviral agents

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KR970706251A true KR970706251A (en) 1997-11-03

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EP (1) EP0787126A1 (en)
JP (1) JPH10506410A (en)
KR (1) KR970706251A (en)
CN (1) CN1159183A (en)
AR (1) AR003456A1 (en)
AU (1) AU6357996A (en)
BR (1) BR9606528A (en)
CA (1) CA2199635A1 (en)
EA (1) EA000033B1 (en)
GB (1) GB9514993D0 (en)
HU (1) HUP9702393A3 (en)
IL (1) IL120342A0 (en)
MX (1) MX9701949A (en)
NO (1) NO971142D0 (en)
PL (1) PL319352A1 (en)
TW (1) TW367325B (en)
WO (1) WO1997003957A1 (en)
ZA (1) ZA965028B (en)

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WO1998037066A1 (en) 1996-02-26 1998-08-27 California Institute Of Technology Improved polyamides for binding in the minor groove of double stranded dna
US6635417B1 (en) 1996-07-31 2003-10-21 California Institute Of Technology Complex formation between DSDNA and oligomer of cyclic heterocycles
US5998140A (en) 1996-07-31 1999-12-07 The Scripps Research Institute Complex formation between dsDNA and oligomer of cyclic heterocycles
GB9623522D0 (en) * 1996-11-11 1997-01-08 Pharmacia & Upjohn Spa Benzoheterocycle distamycin derivatives process for preparing them and their use as antitumour and antiviral agents
GB9816652D0 (en) * 1998-07-30 1998-09-30 Pharmacia & Upjohn Spa Sulfurated distamycin derivatives process for preparing them and their use as antitumor agents
GB9907414D0 (en) 1999-03-31 1999-05-26 Cancer Res Campaign Tech Improvements relating to prodrugs
US6559125B1 (en) 2000-01-28 2003-05-06 California Institute Of Technology Polyamide-alkylator conjugates and related products and method
WO2002101007A2 (en) 2001-06-13 2002-12-19 Genesoft Pharmaceuticals, Inc Antipathogenic benzamide compounds
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EP1587529A4 (en) 2002-12-10 2009-08-12 Oscient Pharmaceuticals Corp Antibacterial compounds having a (pyrrole carboxamide)-(benzamide)-(imidazole carboxamide) motif
EP2792355A1 (en) 2013-04-17 2014-10-22 Albert-Ludwigs-Universität Freiburg Compounds for use as bromodomain inhibitors
CN115414356A (en) * 2022-09-27 2022-12-02 广西科技大学 Application of indenopyrrole derivatives in preparation of antitumor pharmaceutical composition

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EP0787126A1 (en) 1997-08-06
EA000033B1 (en) 1998-02-26
HUP9702393A2 (en) 1998-04-28
EA199700046A1 (en) 1997-12-30
GB9514993D0 (en) 1995-09-20
BR9606528A (en) 1997-12-23
ZA965028B (en) 1997-01-23
CA2199635A1 (en) 1997-02-06
WO1997003957A1 (en) 1997-02-06
AR003456A1 (en) 1998-08-05
MX9701949A (en) 1997-06-28
JPH10506410A (en) 1998-06-23
AU6357996A (en) 1997-02-18
IL120342A0 (en) 1997-06-10
TW367325B (en) 1999-08-21
CN1159183A (en) 1997-09-10
HUP9702393A3 (en) 1998-05-28
PL319352A1 (en) 1997-08-04
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