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KR950701638A - Antiviral phosphonic acid derivatives of purine analogues - Google Patents

Antiviral phosphonic acid derivatives of purine analogues

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Publication number
KR950701638A
KR950701638A KR1019940703269A KR19940703269A KR950701638A KR 950701638 A KR950701638 A KR 950701638A KR 1019940703269 A KR1019940703269 A KR 1019940703269A KR 19940703269 A KR19940703269 A KR 19940703269A KR 950701638 A KR950701638 A KR 950701638A
Authority
KR
South Korea
Prior art keywords
compound
hydrogen
amino
phenyl
acyl
Prior art date
Application number
KR1019940703269A
Other languages
Korean (ko)
Inventor
레이먼드 하안덴 마이클
베일리 스튜어트
테레사 세라피노우스키 핼리나
Original Assignee
데이빗 로버츠
스미스클라인 비이참 피이엘시이
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.)
Filing date
Publication date
Application filed by 데이빗 로버츠, 스미스클라인 비이참 피이엘시이 filed Critical 데이빗 로버츠
Publication of KR950701638A publication Critical patent/KR950701638A/en

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Classifications

    • 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
    • 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
    • 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

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Oncology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Communicable Diseases (AREA)
  • Virology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

하기 일반식(Ⅰ)의 화합물, 또는 이들의 제약학적으로 허용가능한 염:A compound of formula (I), or a pharmaceutically acceptable salt thereof:

상기 식에서, X는 -CH2O -CH2또는 -CH(CH2OR6)0이며 이때 R6는 수소 또는 아실이고: Y는 0 또는 S이고; R1은 히드록시 또는 아미노이고; R2은 아미노 또는 수소이고; R3은 수소이고, 또는 X가 CH2O이고 Y가 0일때, R3는 CH2OR7일 수 있으며 이때 R7은 수소 또는 아실이며; R4및 R5는 둘다 페닐, 4-브로모페닐, 4-메틸페닐, 4-메톡시페닐, 2-아세톡시페닐 또는 2-메틸페닐임; 및 비루스성 질병의 치료시 그들의 제약학적 사용.Wherein X is —CH 2 O —CH 2 or —CH (CH 2 OR 6 ) 0 wherein R 6 is hydrogen or acyl: Y is 0 or S; R 1 is hydroxy or amino; R 2 is amino or hydrogen; When R 3 is hydrogen or X is CH 2 O and Y is 0, R 3 may be CH 2 OR 7 , wherein R 7 is hydrogen or acyl; R 4 and R 5 are both phenyl, 4-bromophenyl, 4-methylphenyl, 4-methoxyphenyl, 2-acetoxyphenyl or 2-methylphenyl; And their pharmaceutical use in the treatment of viral diseases.

Description

푸린 동족체의 항비루스성 포스폰산 유도체(Antiviral phosphonic acid derivatives of purine analogues)Antiviral phosphonic acid derivatives of purine analogues

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

Claims (17)

하기 일반식(Ⅰ)의 화합물, 또는 이들의 제약학적으로 허용가능한 염:A compound of formula (I), or a pharmaceutically acceptable salt thereof: 상기 식에서, X는 -CH2O -CH2또는 -CH(CH2OR6)0이며 이때 R6는 수소 또는 아실이고: Y는 0 또는 S이고; R1은 히드록시 또는 아미노이고; R2은 아미노 또는 수소이고; R3은 수소이고, 또는 X가 CH2O이고 Y가 0일때, R3는 CH2OR7일 수 있으며 이때 R7은 수소 또는 아실이며; R4및 R5는 둘다 페닐, 4-브로모페닐, 4-메틸페닐, 4-메톡시페닐, 2-아세톡시페닐 또는 2-페닐이다.Wherein X is —CH 2 O —CH 2 or —CH (CH 2 OR 6 ) 0 wherein R 6 is hydrogen or acyl: Y is 0 or S; R 1 is hydroxy or amino; R 2 is amino or hydrogen; When R 3 is hydrogen or X is CH 2 O and Y is 0, R 3 may be CH 2 OR 7 , wherein R 7 is hydrogen or acyl; R 4 and R 5 are both phenyl, 4-bromophenyl, 4-methylphenyl, 4-methoxyphenyl, 2-acetoxyphenyl or 2-phenyl. 제1항에 있어서, R1이 히드록시이고 R2가 아미노인 화합물.The compound of claim 1, wherein R 1 is hydroxy and R 2 is amino. 제1항에 있어서, R1이 아미노이고 R2가 수소인 화합물.The compound of claim 1, wherein R 1 is amino and R 2 is hydrogen. 제1항 내지 제3항 중 어느 한 항에 있어서, R4및 R5둘 다 페닐인 화합물.The compound of any one of claims 1-3, wherein both R 4 and R 5 are phenyl. 제1항 내지 제4항 중 어느 한 항에 있어서, X가 -CH2O이고 R3가 수소인 화합물.The compound of any one of claims 1-4 where X is —CH 2 O and R 3 is hydrogen. 제1항 내지 제4항중 어느 한 항에 있어서, X가 -CH2O이고 R3가 제1항에 정의된 바의 CH2OR7인 화합물.5. The compound of claim 1, wherein X is —CH 2 O and R 3 is CH 2 OR 7 as defined in claim 1. 제1항 내지 제4항 중 어느 한 항에 있어서, X가 제1항에 정의된 바의 -CH(CH2OR6)O이고 R3가 수소인 화합물.5. The compound of claim 1, wherein X is —CH (CH 2 OR 6 ) O as defined in claim 1 and R 3 is hydrogen. 제1항 내지 제4항 중 어느 한 항에 있어서, X가 -CH2이고 R3가 수소인 화합물.The compound of any one of claims 1-4 where X is —CH 2 and R 3 is hydrogen. 제1항 내지 제4항 중 어느 한 항에 있어서, X가 -CH2이고 R3가 제1항에 정의된 바의 CH2OR7인 화합물.5. The compound of claim 1, wherein X is —CH 2 and R 3 is CH 2 OR 7 as defined in claim 1. 실시예 중 어느 하나에 관하여 본원에 서술된 바의 화합물.A compound as described herein with respect to any of the examples. 제1항 내지 제10항 중 어느 한 항에 따른 화합물 및 제약학적으로 허용가능한 부형제로 구성된 제약학적 조성물.A pharmaceutical composition consisting of the compound according to any one of claims 1 to 10 and a pharmaceutically acceptable excipient. 제1항 내지 제10항 중 어느 한 항에 있어서, 유효 치료 물질로서 사용하기 위한 화합물.The compound according to claim 1, for use as an effective therapeutic substance. 제1항 내지 제10항 중 어느 한 항에 있어서, 비투스성 질병을 치료하는데 사용하기 위한 화합물.The compound of any one of claims 1 to 10 for use in treating a non-tussive disease. 비루스성 질병의 치료에 사용하기 위한 약물의 제조시 제1항 내지 제10항 중 어느 한 항에 따른 화합물의 사용.Use of a compound according to any one of claims 1 to 10 in the manufacture of a medicament for use in the treatment of viral diseases. 비루스성 질병의 치료를 필요로하는 포유류에게, 유효량의 제1-10항 중 어느 한 항에 따른 화합물을 투여하는 것으로 구성되는, 포유류에 있어서 비루스성 질병의 치료 방법.A method of treating a viral disease in a mammal, comprising administering to a mammal in need thereof an effective amount of a compound according to any one of claims 1-10. 제13,14 또는 15항 중 어느 한 항에 있어서, 비루스성 감염이 사람 면역 결핍 비루스 감염인 화합물, 사용 또는 방법.The compound, use or method of any one of claims 13, 14 or 15, wherein the viral infection is a human immunodeficiency viral infection. 9-[2-비스(페녹시)포스포릴메톡시]에톡시]아데닌 히드로클로라이드.9- [2-bis (phenoxy) phosphorylmethoxy] ethoxy] adenine hydrochloride. ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.※ Note: The disclosure is based on the initial application.
KR1019940703269A 1992-03-18 1993-03-18 Antiviral phosphonic acid derivatives of purine analogues KR950701638A (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB929205917A GB9205917D0 (en) 1992-03-18 1992-03-18 Pharmaceuticals
GB9205917.9 1992-03-18
PCT/GB1993/000560 WO1993019075A1 (en) 1992-03-18 1993-03-18 Antiviral phosphonic acid derivatives of purine analogues

Publications (1)

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KR950701638A true KR950701638A (en) 1995-04-28

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KR1019940703269A KR950701638A (en) 1992-03-18 1993-03-18 Antiviral phosphonic acid derivatives of purine analogues

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EP (1) EP0631583A1 (en)
JP (1) JPH07504666A (en)
KR (1) KR950701638A (en)
AU (1) AU3760793A (en)
CA (1) CA2132303A1 (en)
GB (1) GB9205917D0 (en)
WO (1) WO1993019075A1 (en)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003095665A2 (en) 2002-05-13 2003-11-20 Metabasis Therapeutics, Inc. Pmea and pmpa cyclic producing synthesis
US7214668B2 (en) 2002-05-13 2007-05-08 Metabasis Therapeutics, Inc. Phosphonic acid based prodrugs of PMEA and its analogues
KR20070029196A (en) 2004-06-08 2007-03-13 메타베이시스 테라퓨틱스, 인크. Lewis acid mediated synthesis of cyclic esters
WO2006066074A2 (en) 2004-12-16 2006-06-22 The Regents Of The University Of California Lung-targeted drugs
WO2013095684A1 (en) 2011-12-22 2013-06-27 Geron Corporation Guanine analogs as telomerase substrates and telomere length affectors
CN103665043B (en) 2012-08-30 2017-11-10 江苏豪森药业集团有限公司 A kind of tenofovir prodrug and its application in medicine
CA2906680A1 (en) 2013-03-15 2014-09-18 The Regents Of The University Of California Acyclic nucleoside phosphonate diesters
CN114404427A (en) 2014-02-13 2022-04-29 配体药物公司 Prodrug compound and use thereof
US9994600B2 (en) 2014-07-02 2018-06-12 Ligand Pharmaceuticals, Inc. Prodrug compounds and uses therof
PL3194411T3 (en) 2014-09-15 2022-06-20 The Regents Of The University Of California Nucleotide analogs
WO2017048956A1 (en) 2015-09-15 2017-03-23 The Regents Of The University Of California Nucleotide analogs
AU2019207625A1 (en) 2018-01-09 2020-07-30 Ligand Pharmaceuticals, Inc. Acetal compounds and therapeutic uses thereof

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* Cited by examiner, † Cited by third party
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ATE113601T1 (en) * 1987-11-30 1994-11-15 Beecham Group Plc LINKS.
EP0353955A3 (en) * 1988-08-02 1991-08-14 Beecham Group Plc Novel compounds
GB8912043D0 (en) * 1989-05-25 1989-07-12 Beecham Group Plc Novel compounds
ATE167679T1 (en) * 1990-09-14 1998-07-15 Acad Of Science Czech Republic PHOSPHONATE PRECURSORS

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Publication number Publication date
EP0631583A1 (en) 1995-01-04
AU3760793A (en) 1993-10-21
WO1993019075A1 (en) 1993-09-30
JPH07504666A (en) 1995-05-25
CA2132303A1 (en) 1993-09-30
GB9205917D0 (en) 1992-04-29

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