KR950025044A - Pyrimidine Acyclonucleoside Derivatives - Google Patents

Pyrimidine Acyclonucleoside Derivatives Download PDF

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Publication number
KR950025044A
KR950025044A KR1019940003794A KR19940003794A KR950025044A KR 950025044 A KR950025044 A KR 950025044A KR 1019940003794 A KR1019940003794 A KR 1019940003794A KR 19940003794 A KR19940003794 A KR 19940003794A KR 950025044 A KR950025044 A KR 950025044A
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South Korea
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group
formula
compound represented
methyl
selenyl
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KR1019940003794A
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Korean (ko)
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KR0128542B1 (en
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김대기
감종식
김강혁
김영우
임진수
김훈택
김기협
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김준웅
주식회사 선경인더스트리
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Priority to BR9408370A priority patent/BR9408370A/en
Priority to AU73512/94A priority patent/AU693107B2/en
Priority to PCT/KR1994/000102 priority patent/WO1995023138A1/en
Priority to US08/545,682 priority patent/US5889013A/en
Priority to JP7507220A priority patent/JP2683297B2/en
Priority to EP94922386A priority patent/EP0748316B1/en
Priority to DE69430587T priority patent/DE69430587T2/en
Priority to CA002159817A priority patent/CA2159817C/en
Publication of KR950025044A publication Critical patent/KR950025044A/en
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Publication of KR0128542B1 publication Critical patent/KR0128542B1/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/56—One oxygen atom and one sulfur atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52—Two oxygen atoms
    • C07D239/54—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/01—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing oxygen

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • General Health & Medical Sciences (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

본 발명은 다음 구조식(I)로 표시되는 신규한 피리미딘 아사이클로뉴클레오시드 유도체 및 이를 유효성분으로 하는 항바이러스제에 관한 것이다.The present invention relates to a novel pyrimidine acyclonucleoside derivative represented by the following structural formula (I) and an antiviral agent comprising the same as an active ingredient.

상기식에서, R1은 에틸기 또는 이소프로필기이다. R2는 치환되거나 치환되지 않은 페닐셀레네닐기이고, 치환기로는 C1∼C3의 알킬기 또는 할로겐원자이다. R3는 수소원자, C1∼C3의 알킬기, C1∼C3의 하이드록시알킬기, 아실옥시알킬기, 또는 치환되거나 치환되지 않은 페닐기로서 치환기로는 C1∼C3의 알킬기, C1∼C3의 알콕시기 또는 할로겐원자이다.In the above formula, R 1 is an ethyl group or an isopropyl group. R 2 is phenyl Selene group is optionally substituted, the substituent is an alkyl group or a halogen atom of the C 1 ~C 3. R 3 is a hydrogen atom, a C 1 -C 3 alkyl group, a C 1 -C 3 hydroxyalkyl group, an acyloxyalkyl group, or a substituted or unsubstituted phenyl group, and examples of the substituent include a C 1 -C 3 alkyl group, C 1- C 3 is an alkoxy group or halogen atom.

X는 산소원자 또는 황원자이다. 단, 동시에 R1이 에틸기이고, R2가 페닐셀레네닐기이고 R3가 메틸기이고 X가 산소원자인 화합물은 제외한다.X is an oxygen atom or a sulfur atom. However, at the same time, a compound in which R 1 is an ethyl group, R 2 is a phenylselenyl group, R 3 is a methyl group and X is an oxygen atom is excluded.

Description

피리미딘 아사이클로뉴클레오시드 유도체Pyrimidine Acyclonucleoside Derivatives

본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음Since this is an open matter, no full text was included.

Claims (14)

다음 구조식(I)로 표시되는 피리미딘 아사이클로뉴클레오시드 유도체 및 이를 약제학으로 허용 가능한 염.A pyrimidine acyclonucleoside derivative represented by the following structural formula (I) and a pharmaceutically acceptable salt thereof. 상기식에서, R1은 에틸기 또는 이소프로필기이다. R2는 치환되거나 치환되지 않은 페닐셀레네닐기이고, 치환기로는 C1∼C3의 알킬기 또는 할로겐원자이다. R3는 수소원자, C1∼C3의 알킬기, C1∼C3의 하이드록시알킬기, 아실옥시알킬기, 또는 치환되거나 치환되지 않은 페닐기로서 치환기로는 C1∼C3의 알킬기, C1∼C3의 알콕시기 또는 할로겐원자이다. X는 산소원자 또는 황원자이다. 단, 동시에 R1이 에틸기이고, R2가 페닐셀레네닐기이고 R3가 메틸기이고 X가 산소원자인 화합물은 제외한다.In the above formula, R 1 is an ethyl group or an isopropyl group. R 2 is phenyl Selene group is optionally substituted, the substituent is an alkyl group or a halogen atom of the C 1 ~C 3. R 3 is a hydrogen atom, a C 1 -C 3 alkyl group, a C 1 -C 3 hydroxyalkyl group, an acyloxyalkyl group, or a substituted or unsubstituted phenyl group, and examples of the substituent include a C 1 -C 3 alkyl group, C 1- C 3 is an alkoxy group or halogen atom. X is an oxygen atom or a sulfur atom. However, at the same time, a compound in which R 1 is an ethyl group, R 2 is a phenylselenyl group, R 3 is a methyl group and X is an oxygen atom is excluded. 제1항에 있어서, 상기 구조식(I)로 표시되는 화합물은 6-[3,5-디메틸페닐)셀레네닐]-5-에틸-1-[(2-하이드록시에톡시)메틸]우라실.The compound represented by formula (I) is 6- [3,5-dimethylphenyl) selenyl] -5-ethyl-1-[(2-hydroxyethoxy) methyl] uracil. 제1항에 있어서, 상기 구조식(I)로 표시되는 화합물은 6-[3,5-디메틸페닐)셀레네닐]-1-에틸-[(2-하이드록시에톡시)메틸]-5-이소프로필우라실.A compound according to claim 1, wherein the compound represented by the formula Uracil. 제1항에 있어서, 상기 구조식(I)로 표시되는 화합물은 6-[3,5-디메틸페닐)셀레네닐]-1-(에톡시메틸)-5-에틸우라실.The compound represented by formula (I) is 6- [3,5-dimethylphenyl) selenyl] -1- (ethoxymethyl) -5-ethyluracil. 제1항에 있어서, 상기 구조식(I)로 표시되는 화합물은 1-[(벤질옥시)메틸]-5-에틸-6-(페닐셀레네닐)우라실.The compound represented by formula (I) is 1-[(benzyloxy) methyl] -5-ethyl-6- (phenylselenyl) uracil. 제1항에 있어서, 상기 구조식(I)로 표시되는 화합물은 1-[(벤질옥시)메틸]-5-에틸-6-[(3-메틸페닐)셀레네닐]우라실.The compound represented by formula (I) is 1-[(benzyloxy) methyl] -5-ethyl-6-[(3-methylphenyl) selenyl] uracil. 제1항에 있어서, 상기 구조식(I)로 표시되는 화합물은 1-[(벤질옥시)메틸]-6-[(3,5-디메틸페닐)셀레네닐]-5-에틸우라실.The compound represented by formula (I) is 1-[(benzyloxy) methyl] -6-[(3,5-dimethylphenyl) selenyl] -5-ethyluracil. 제1항에 있어서, 상기 구조식(I)로 표시되는 화합물은 1-[(에톡시메틸)-5-이소프로필-6-[(3-메틸페닐)셀레네닐]우라실.The compound represented by formula (I) is 1-[(ethoxymethyl) -5-isopropyl-6-[(3-methylphenyl) selenyl] uracil. 제1항에 있어서, 상기 구조식(I)로 표시되는 화합물은 6-[(3,5-디메틸페닐)셀레네닐]-1-(에톡시메틸)-5-이소프로필우라실.The compound represented by formula (I) is 6-[(3,5-dimethylphenyl) selenyl] -1- (ethoxymethyl) -5-isopropyluracil. 제1항에 있어서, 상기 구조식(I)로 표시되는 화합물은 1-[(벤질옥시)메틸]-5-이소프로필-6-(페닐셀레네닐)우라실.The compound represented by formula (I) is 1-[(benzyloxy) methyl] -5-isopropyl-6- (phenylselenyl) uracil. 제1항에 있어서, 상기 구조식(I)로 표시되는 화합물은 1-[(벤질옥시)메틸]-5-이소프로필-6-[(3-메틸페닐)셀레네닐]우라실.The compound represented by formula (I) is 1-[(benzyloxy) methyl] -5-isopropyl-6-[(3-methylphenyl) selenyl] uracil. 제1항에 있어서, 상기 구조식(I)로 표시되는 화합물은 1-[(벤질옥시)메틸]-6-[(3,5-디메틸페닐)셀레네닐]-5-이소프로필우라실.The compound represented by formula (I) is 1-[(benzyloxy) methyl] -6-[(3,5-dimethylphenyl) selenyl] -5-isopropyluracil. 다음 구조식(I)로 표시되는 피리미딘 아사이클로뉴클레오시드 유도체 또는 이들의 약제학적으로 허용 가능한 염이 유효성분으로 함유된 항바이러스제.An antiviral agent containing a pyrimidine acyclonucleoside derivative represented by the following formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient. 상기식에서, R1, R2, R3및 X는 상기 제1항에 정의한 바와 같다.Wherein R 1 , R 2 , R 3 and X are as defined in claim 1 above. 다음 구조식(I)로 표시되는 피리미딘 아사이클로뉴클레오시드 유도체 또는 이들의 약제학적으로 허용 가능한 염과 약제학적 부형제가 함유된 약제학적 조성물.A pharmaceutical composition containing a pyrimidine acyclonucleoside derivative represented by the following formula (I) or a pharmaceutically acceptable salt thereof and a pharmaceutical excipient. 상기식에서, R1, R2, R3및 X는 상기 제1항에 정의한 바와 같다.Wherein R 1 , R 2 , R 3 and X are as defined in claim 1 above. ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.※ Note: The disclosure is based on the initial application.
KR1019940003794A 1994-02-28 1994-02-28 Pyrimidine acyclonucleoside derivatives KR0128542B1 (en)

Priority Applications (9)

Application Number Priority Date Filing Date Title
KR1019940003794A KR0128542B1 (en) 1994-02-28 1994-02-28 Pyrimidine acyclonucleoside derivatives
AU73512/94A AU693107B2 (en) 1994-02-28 1994-07-29 Pyrimidine acyclonucleoside derivatives
PCT/KR1994/000102 WO1995023138A1 (en) 1994-02-28 1994-07-29 Pyrimidine acyclonucleoside derivatives
US08/545,682 US5889013A (en) 1994-02-28 1994-07-29 Pyrimidine acyclonucleoside derivatives
BR9408370A BR9408370A (en) 1994-02-28 1994-07-29 Pyrimidine acyclonucleoside derivatives
JP7507220A JP2683297B2 (en) 1994-02-28 1994-07-29 Pyrimidine acyclonucleoside derivative
EP94922386A EP0748316B1 (en) 1994-02-28 1994-07-29 Pyrimidine acyclonucleoside derivatives
DE69430587T DE69430587T2 (en) 1994-02-28 1994-07-29 PYRIMIDINE-ACYCLONUKLEOSID DERIVATIVES
CA002159817A CA2159817C (en) 1994-02-28 1994-07-29 Pyrimidine acyclonucleoside derivatives

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KR1019940003794A KR0128542B1 (en) 1994-02-28 1994-02-28 Pyrimidine acyclonucleoside derivatives

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KR950025044A true KR950025044A (en) 1995-09-15
KR0128542B1 KR0128542B1 (en) 1998-04-04

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