KR920018052A - 사이클로프로판 유도체 - Google Patents

사이클로프로판 유도체 Download PDF

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KR920018052A
KR920018052A KR1019920003673A KR920003673A KR920018052A KR 920018052 A KR920018052 A KR 920018052A KR 1019920003673 A KR1019920003673 A KR 1019920003673A KR 920003673 A KR920003673 A KR 920003673A KR 920018052 A KR920018052 A KR 920018052A
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formula
cyclopropane
salt
isomer
compound
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KR1019920003673A
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KR100232619B1 (ko
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다카아키 세키야마
다카시 쓰지
아키라 하쓰다니
사토시 이와야마
마사히코 오쿠니시
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도바 다다스
아지노모토 가부시키가이샤
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
    • C07D473/18—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 one oxygen and one nitrogen atom, e.g. guanine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • 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
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/20—Antivirals for DNA viruses
    • A61P31/22—Antivirals for DNA viruses for herpes viruses
    • 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
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Virology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Molecular Biology (AREA)
  • Biotechnology (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

내용 없음

Description

사이클로프로판 유도체
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (14)

  1. 하기 일반식(Ⅰ)의 사이클로프로판 유도체, 이의 기하 또는 광학이성체, 또는 약제학적으로 허용되는 이의 염.
    상기식에서, B1은 푸린 잔기 또는 피리미딘 잔기이고, R1및 R2는 독립적으로 수소 또는 하이드록실 보호 그룹이며, k, m 및 n은 각각 독립적으로 1 또는 2이다.
  2. 제1항에 있어서, k, m 및 n은 각각 1인 사이클로프로판 유도체, 이의 염 또는 이성체.
  3. 제1항 또는 제2항에 있어서, R1및 R2가 각각 수소인 사이클로프로판 유도체, 이의 염 또는 이성체.
  4. 제1항 내지 제3항중 어느 한 항에 있어서, B1이 푸린-9-일 또는 피리미딘-1-일 그룹인 사이클로프로판 유도체, 이의 염 또는 이성체.
  5. 제4항에 있어서, B1이 하기 구조식(Ⅱ)의 구아닌, 구조식(Ⅲ)의 아데닌, 구조식(Ⅳ)의 2-아미노-6-사이클로푸린, 구조식(Ⅴ)의 2-아미노푸리느 구조식(Ⅵ)의 2,6-디아미노푸린, 구조식(Ⅶ)의 크산틴 및 구조식(Ⅷ)의 하이포크산틴으로부터 선택된 푸린 잔기의 사이클로프로판 유도체, 이의 염 또는 이성체.
  6. 제4항에 있어서, B1이 하기 구조식(Ⅸ)의 시토신, 구조식(Ⅹ)의 티민 및 구조식(ⅩⅠ)의 우라실로부터 선택된 피리미딘인 사이클로프로판 유도체, 이의 염 또는 이성체.
  7. 제1항 내지 제6항중 어느 한 항에 있어서, 사이클로프로판 잔기가 하기 일반식(ⅩⅡ)에 제시된 바와 같은 1S, 2R 배위를 갖는 사이클로프로판 유도체, 이의 염 또는 이성체.
  8. 제1항 내지 제6항중 어느 한 항에 있어서, 사이클로프로판 잔기가 하기 일반식(ⅩⅢ)에 제시된 바와 같은 1S, 2R 배위를 갖는 사이클로프로판 유도체, 이의 염 또는 이성체.
  9. 제1항 내지 제8항중 어느 한 항에 있어서, 약제학적 용도를 위한 사이클로프로판 유도체, 이의 염 또는 이성체.
  10. 제1항 내지 제9항중 어느 한 항의 사이클로프로판 유도체, 이의 염 또는 이성체 및 약제학적으로 허용되는 부형제, 희석제 또는 담체를 포함하는 약제학적 조성물.
  11. 비루스 감염 치료용 약제의 제조에 있어서의 제1항 내지 제9항중 어느 한 항의 사이클로프로판 유도체, 이의 염 또는 이성체.
  12. (a) 일반식(Ⅰ)의 화합물을 산 또는 알칼리와 반응시켜 약제학적으로 허용되는 염을 형성하는 단계 ; (b) R1및 R2중 하나 이상이 보호그룹인 일반식(Ⅰ) 화합물의 보호그룹을 제거하여 R1및 R2가 각각 수소인 일반식(Ⅰ)화합물을 수득하는 단계 ; (c) R1및 R2중 하나 이상이 하이드록실인 일반식(Ⅰ) 화합물을 에스테르화하여 R1및 R2중 하나 또는 모두가 아실 보호그룹인 일반식(Ⅰ) 화합물을 수득하는 단계 ; (d) 하기 일반식(ⅩⅣ)의 화합물을 임의의 보호된 푸린 또는 피리미딘과 반응시킨 다음, 임의로 보호그룹을 제거하는 단계중 적어도 하나를 포함하는, 제1항 내지 제9항중 어느 한 항의 사이클로프로판 유도체, 이의 염 또는 이성체의 제조방법.
    상기식에서, R1, R2, k, m 및 n은 제1항에서 정의한 바와 같으며, X는 이탈 그룹이다.
  13. 제1항 내지 제9항중 어느 한 항의 사이클로프로판 유도체, 이의 염 또는 이성체를 제조하기 위한 일반식(ⅩⅤ)의 중간체.
    상기식에서, Y는 이탈그룹 또는 OH이고, R1, R2, k, m 및 n은 제1항에서 정의한 바와 같다.
  14. 제1항 내지 제9항에중 어느 한 항의 사이클로프로판 유도체 및 약제학적으로 허용되는 부형제, 희석제 또는 담체를 혼합함을 특징으로 하는 약제학적 조성물의 제조방법.
    ※참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019920003673A 1991-03-05 1992-03-05 사이클로프로판 유도체, 이의 제조방법 및 이를 함유하는 약제학적 조성물 KR100232619B1 (ko)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
JP91-123239 1991-03-05
JP12323991 1991-03-05
JP91-184709 1991-07-24
JP18470991 1991-07-24

Publications (2)

Publication Number Publication Date
KR920018052A true KR920018052A (ko) 1992-10-21
KR100232619B1 KR100232619B1 (ko) 1999-12-01

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US (2) US5342840A (ko)
EP (1) EP0502690B1 (ko)
JP (1) JP2923933B2 (ko)
KR (1) KR100232619B1 (ko)
AT (1) ATE187173T1 (ko)
CA (1) CA2062299C (ko)
DE (1) DE69230349T2 (ko)
DK (1) DK0502690T3 (ko)
ES (1) ES2139588T3 (ko)

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JP3769737B2 (ja) * 1994-03-30 2006-04-26 味の素株式会社 シクロプロパン誘導体及びその製造法
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KR950014110A (ko) * 1993-11-18 1995-06-15 도바 다다스 사이클로프로판 유도체 및 이를 포함하는 항바이러스제

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ES2139588T3 (es) 2000-02-16
CA2062299C (en) 1999-05-25
EP0502690B1 (en) 1999-12-01
ATE187173T1 (de) 1999-12-15
DE69230349T2 (de) 2000-07-27
JP2923933B2 (ja) 1999-07-26
US5449840A (en) 1995-09-12
CA2062299A1 (en) 1992-09-06
DE69230349D1 (de) 2000-01-05
DK0502690T3 (da) 2000-05-22
US5342840A (en) 1994-08-30
EP0502690A2 (en) 1992-09-09
JPH0578357A (ja) 1993-03-30
EP0502690A3 (en) 1992-12-09
KR100232619B1 (ko) 1999-12-01

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