KR920700217A - 항 바이러스성 화합물 - Google Patents

항 바이러스성 화합물

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Publication number
KR920700217A
KR920700217A KR1019900702612A KR900702612A KR920700217A KR 920700217 A KR920700217 A KR 920700217A KR 1019900702612 A KR1019900702612 A KR 1019900702612A KR 900702612 A KR900702612 A KR 900702612A KR 920700217 A KR920700217 A KR 920700217A
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South Korea
Prior art keywords
formula
compound
phosphate
methylsulfonyl
compound according
Prior art date
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KR1019900702612A
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English (en)
Inventor
리차드 토마스 워커
알버트 스탠리 존스
Original Assignee
리차드 토마스 워커
알버트 스탠리 존스
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Priority claimed from GB898908355A external-priority patent/GB8908355D0/en
Application filed by 리차드 토마스 워커, 알버트 스탠리 존스 filed Critical 리차드 토마스 워커
Publication of KR920700217A publication Critical patent/KR920700217A/ko

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    • 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
    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/06—Pyrimidine radicals
    • C07H19/10—Pyrimidine radicals with the saccharide radical esterified by phosphoric or polyphosphoric acids
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
    • C07F9/65586—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system at least one of the hetero rings does not contain nitrogen as ring hetero atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
    • C07F9/65616—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings containing the ring system having three or more than three double bonds between ring members or between ring members and non-ring members, e.g. purine or analogs
    • 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
    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/16—Purine radicals
    • C07H19/20—Purine radicals with the saccharide radical esterified by phosphoric or polyphosphoric acids

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Biotechnology (AREA)
  • Genetics & Genomics (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Communicable Diseases (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Virology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)

Abstract

내용 없음

Description

항 바이러스성 화합물
내용없음

Claims (30)

  1. 하기 일반식(Ⅰ)의 화합물 또는 약리학적으로 허용 가능한 이들의 염:
    상기식에서, R1은 지방족 히드로카르빌기이고; Ar은 치환 또는 비치환된 방향족핵이고; X는 －SO2－ 또는 －CO－이고; R2및 R3는 같거나 다를 수 있으며 하기 일반식(a), (b), (c), (d), (e), (f), (g), (h) 또는 (ⅰ)의 부분들이고:
    상기식에서, B는 하기 일반식(A), (G), (C), (H) 또는 (T)의 뉴클레오시드염기의 잔기이며:
    단, R2및 R3가 일반식(a)의 비치환된 부분일 경우, B는 일반식(A), (G), (C) 또는 (H)의 뉴클레오시드염기이다.
  2. 제1항에 있어서, Ar이 치환 또는 비치환된 벤젠고리임을 특징으로 하는 화합물.
  3. 제2항에 있어서, R1X 및 인산염 치환기들의 서로 파라배열을 갖는 것을 특징으로 하는 화합물.
  4. 제1항에 있어서, Ar이 치환된 방향족 핵이어서 화합물(Ⅰ)의 독성에 잘 견디는 대응하는 페놀 R1XArOH로 쉽게 가수분해되는 것을 특징으로 하는 화합물.
  5. 제1항에 있어서, A는 같거나 다를 수 있는 하나 이상의 치환기를 (예로서, 할로겐원자, 플루오로알킬, 알콕시, 플루오로알콕시, 카르보알콕시, 아미노 또는 아미도기)에 의해 치환된 벤젠기임을 특징으로 하는 화합물.
  6. 제1항에 있어서, X는 술포닐기임을 특징으로 하는 화합물.
  7. 제1 내지 제6항중 어느 한항에 있어서, R2및 R3는 각각 일반식(a), (b), (d) 또는 (f)의 부분임을 특징으로 하는 화합물.
  8. 제7항에 있어서, R2및 R3가 각각 일반식(f)의 부분임을 특징으로 하는 화합물.
  9. 제7항에 있어서, R2및 R3가 각각 하기 일반식(ⅰ) 내지 (x)중 어느 하나임을 특징으로 하는 화합물;
  10. 제9항에 있어서, R2및 R3가 각각 일반식(i), (v), (vi) 또는 (ix)임을 특징으로 하는 화합물.
  11. 4－(메틸술포닐)페닐 비스(3´－이지도 티미딘－5´－일)인산염.
  12. 4－(메틸술포닐)페닐 비스(2´, 3´－디데히드로－2´, 3´－디데옥시시티딘－5´－일)인산염
  13. 4－(메틸술포닐)페닐 비스(2´, 3´－디데히드로－2´, 3´－디데옥시시티딘－5´－일)인산염
  14. 4－(메틸술포닐)페닐 비스(2´, 3´－디데옥시아데노신－5´－일)인산염
  15. 4－(메틸술포닐)페닐 비스(2´, 3´－디데히드로－2´, 3´－디데옥시 티미딘－5´－일)인산염
  16. 하기 일반식(Ⅲ)의 포스포로디할로겐화물을 일반식(Ⅱ)의 화합물 또는 R2의 뉴클레오시드염기 내 그룹이 보호된 유도체와 반응시키는 것으로 이루어진 일반식(Ⅰ)의 화합물의 제조방법;
    R1XArOP(O)Y2(Ⅲ)
    R2OH (Ⅱ)
    상기식에서, R1, R2, Ar 및 X는 제1항에 기재된 바와같고, Y는 할로겐원자이다.
  17. 제16항에 있어서, R2내 뉴클레오시드 염기가 아실화에 의해 보호된 시토신임을 특징으로 하는 방법.
  18. 제16 또는 17항에 있어서, 반응이 염기 존재하에 수행되는 것을 특징으로 하는 화합물.
  19. 제18항에 있어서, 염기가 1－메틸이미다졸임을 특징으로 하는 화합물.
  20. R1, Ar, R2및 R3기 제1항에 기재된 바와같은 일반식(Ⅳ): R1SArOP(O)(OR2)(OR3) 또는 일반식(Ⅴ): R1SOArOP(O)(OR2)(OR3)의 화합물을 산화시키는 것을 특징으로 하는, 일반식(Ⅰ)의 화합물의 제조방법.
  21. 제20항에 있어서, 산화가 과(per)산에 의해 수행되는 것을 특징으로 하는 방법.
  22. 일반식(Ⅳ)의 중간체.
  23. 일반식(Ⅴ)의 중간체.
  24. 치료에 사용하기 위한 일반식(Ⅰ)의 화합물.
  25. 사람의 레트로바이러스감염의 치료 또는 예방에 유용한 의약을 제조하기 위한 일반식(Ⅰ)의 화합물 사용.
  26. 아이러스복제를 억제 또는 방해하는데에 유효량의 일반식(Ⅰ)의 화합물을 바이러스로 감염된 객체에 투여하는 것으로 이루어진 사람의 레트로 바이러스 감염의 치료 또는 예방방법.
  27. 바이러스복제를 억제 또는 방해하는 데에 유효량의 일반식(Ⅰ)의 화합물을 가지고서 바이러스로 감염된 혈액을 치료하는 것으로 이루어진 사람의 레트로바이러스감염의 치료 또는 예방방법.
  28. 제26 또는 27항에 있어서, 바이러스가 사람의 면역결핍 바이러스(HIV)임을 특징으로 하는 방법.
  29. 일반식(Ⅰ)의 화합물과 함께 약리학적으로 허용 가능한 이들의 담체를 포함하는 것으로 이루어진, 사람의 레트로바이러스감염의 치료 또는 예방용 제제.
  30. 투여 형태로서의 제29항에 따른 제제.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019900702612A 1989-04-13 1990-04-10 항 바이러스성 화합물 KR920700217A (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB898908355A GB8908355D0 (en) 1988-04-18 1989-04-13 Output apparatus antiviral compounds
GB89083554 1989-04-13
PCT/GB1990/000542 WO1990012023A1 (en) 1989-04-13 1990-04-10 Antiviral compounds

Publications (1)

Publication Number Publication Date
KR920700217A true KR920700217A (ko) 1992-02-19

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KR1019900702612A KR920700217A (ko) 1989-04-13 1990-04-10 항 바이러스성 화합물

Country Status (16)

Country Link
EP (1) EP0392791B1 (ko)
JP (1) JPH03505880A (ko)
KR (1) KR920700217A (ko)
CN (1) CN1046531A (ko)
AT (1) ATE125817T1 (ko)
AU (1) AU5407890A (ko)
CA (1) CA2028151A1 (ko)
DE (1) DE69021242T2 (ko)
ES (1) ES2077643T3 (ko)
FI (1) FI906113A0 (ko)
GB (1) GB2230266B (ko)
NZ (1) NZ233197A (ko)
OA (1) OA09553A (ko)
PT (1) PT93743A (ko)
WO (1) WO1990012023A1 (ko)
ZA (1) ZA902784B (ko)

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DE69021242D1 (de) 1995-09-07
EP0392791B1 (en) 1995-08-02
NZ233197A (en) 1991-11-26
ATE125817T1 (de) 1995-08-15
AU5407890A (en) 1990-11-05
GB2230266A (en) 1990-10-17
GB9008105D0 (en) 1990-06-06
WO1990012023A1 (en) 1990-10-18
GB2230266B (en) 1992-08-12
EP0392791A1 (en) 1990-10-17
PT93743A (pt) 1990-11-20
CA2028151A1 (en) 1990-10-14
ES2077643T3 (es) 1995-12-01
JPH03505880A (ja) 1991-12-19
CN1046531A (zh) 1990-10-31
OA09553A (en) 1993-01-31
ZA902784B (en) 1991-12-24
FI906113A0 (fi) 1990-12-12
DE69021242T2 (de) 1996-01-11

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