KR900003170A - 신규 화합물 - Google Patents

신규 화합물 Download PDF

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Publication number
KR900003170A
KR900003170A KR1019890011058A KR890011058A KR900003170A KR 900003170 A KR900003170 A KR 900003170A KR 1019890011058 A KR1019890011058 A KR 1019890011058A KR 890011058 A KR890011058 A KR 890011058A KR 900003170 A KR900003170 A KR 900003170A
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KR
South Korea
Prior art keywords
hydroxy
propoxy
compound
guanine
oxy
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KR1019890011058A
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English (en)
Inventor
베일리 스튜어트
레이먼드 하안든 마이클
Original Assignee
데이빗 로버츠
비이참 그루우프 피이엘시이
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Priority claimed from GB888818375A external-priority patent/GB8818375D0/en
Priority claimed from GB888827724A external-priority patent/GB8827724D0/en
Application filed by 데이빗 로버츠, 비이참 그루우프 피이엘시이 filed Critical 데이빗 로버츠
Publication of KR900003170A publication Critical patent/KR900003170A/ko

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D473/00Heterocyclic compounds containing purine ring systems
    • C07D473/02Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic System
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561Heterocyclic 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
    • C07F9/65616Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic System
    • C07F9/02Phosphorus compounds
    • C07F9/28Phosphorus compounds with one or more P—C bonds
    • C07F9/38Phosphonic acids RP(=O)(OH)2; Thiophosphonic acids, i.e. RP(=X)(XH)2 (X = S, Se)
    • C07F9/40Esters thereof
    • C07F9/4003Esters thereof the acid moiety containing a substituent or a structure which is considered as characteristic
    • C07F9/4006Esters of acyclic acids which can have further substituents on alkyl
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic System
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/645Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having two nitrogen atoms as the only ring hetero atoms
    • C07F9/6503Five-membered rings
    • C07F9/6506Five-membered rings having the nitrogen atoms in positions 1 and 3
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic System
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/645Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having two nitrogen atoms as the only ring hetero atoms
    • C07F9/6509Six-membered rings
    • C07F9/6512Six-membered rings having the nitrogen atoms in positions 1 and 3

Abstract

내용 없음

Description

신규 화합물
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (15)

  1. 일반식(Ⅰ)의 화합물 또는 제약학적으로 허용가능한 그들의 염 :
    식중에서, R1은 히드록시, 아미노, 클로로 또는 OR7(애거시 R7은 C1-6알킬, 페닐부분이 할로, C1-4알킬 또는 C1-4알콕시기 중에서 선택된 하나 또는 두개의 치환체로 치환될 수 있는 페닐 또는 페닐 C1-2알킬기임)이고 ; R2는 아미노기이거나, R1이 히드록시 또는 아미노기일때, R2는 수소가 될수 있고 ; X는 -CH2CH2- 또는 구조
    (여기서 n은 1 또는 2이고; m은 0,1 또는 2이고 ; R3는 수소이거나 아실기이고; R4는 R5및 R6가 독립적으로 수소, C1-6알킬 및 임의로 치환된 페닐기로부터 선택된 일반식
    의 기임)의 부분이다.
  2. 제1항에 있어서, R1이 히드록시기이고, R2는 아미노기이거나, R1이 아미노기이고, R2는 수소인 화합물.
  3. 제1항 또는 제2항중 어느 한 항에 있어서, X가 -CH2CH2-인 화합물.
  4. 제1항 내지 제3항중 어느 한 항에 있어서, X가 제1항에서 정의된 것과 같은 구조(a)이고, n이 1인 화합물.
  5. 제1항 내지 제4항중 어느 한항에 있어서, R5및 R6모두가 수소인 화합물.
  6. 9-[3-(디에톡시포스포릴메톡시)프로폭시]구아닌, 9-[3-(포스포메톡시)프로폭시프로폭시]구아닌, 2,6-디아미노-9-[3-(디에톡시포스포릴메톡시)프로폭시]퓨린, 2,6-디아미노-9-[3-(포스포노메톡시)프로폭시]-퓨린, 9-[3-(디에톡시포스포릴메톡시)프로폭시]아데닌, 9-[3-(포스포노메톡시)프로폭시]아데닌, 9-[3-에톡시(히드록시)포스포릴메톡시]-구아닌, 2,6-디아미노-9-[(3-디에톡시포스포릴메톡시-2-히드록시메틸)프로폭시]퓨린, 2,6-디아미노-9-[(2-히드록시메틸-3-포스포노-메톡시)프로폭시]퓨린, 9-[(3-디에톡시포스포릴메톡시-2-히드록시-메틸)프로폭시]구아닌, 9-[(2-히드록시메틸-3-포스포노메톡시)프로폭시]-구아닌, 9-[(3-디에톡시포스포릴메톡시-2-히드록시-메틸)프로폭시]아데닌, 9-[(2-히드록시메틸-3-포스포노메톡시프로폭시]-아데닌, 9-[(3-에톡시(히드록시)포스포릴메톡시-2-히드록시메틸)프로폭시]구아닌, 9-(1-디에톡시포스포릴메톡시-3-히드록시프롭-2-옥시)구아닌, 9-(1-히드록시-3-포스포노메톡시프롭-2-옥시)-구아닌, 9-(1-디에톡시포스포릴메톡시-3-히드록시프롭-2-옥시)아데닌, 9-(1-히드록시-3-포스포노메톡시프롭-2-옥시)-아데닌, 2,6-디아미노-9-[1-(디에톡시포스포릴메톡시)-3-히드록시프롭-2-옥시]퓨린, 2,6-디아미노-9-[1-히드록시-3-(포스포노메톡시)-프롭-2-옥시]퓨린, 9-[2-히드록시-3-(포스포노메톡시)프로폭시]-구아닌, 9-[3-(디에톡시포스포릴메톡시)-2-히드록시-프로폭시]아데닌, 9-[2-히드록시-3-(포스포노메톡시)프로폭시]-아데닌, 9-[4-(디에톡시포스포릴메톡시)-1-히드록시부트-2-옥시]구아닌, 9-[1-히드록시-4-(포스포노메톡시)부트-2-옥시]-구아닌, 9-[4-(디에톡시포스포릴메톡시)-1-히드록시부트-2-옥시]아데닌 및 9-[1-히드록시-4-(포스포노메톡시)부트-2-옥시]-아데닌로 구성된 군으로부터 선택된 화합물.
  7. ⅰ) Q가 아미노기 또는 아미노 유도체, 예를들면, 포밀아미노와 같이, 환화되어 이미다졸 고리를 형성할 수 있는 기인 일반식
    의 화합물의 이미다졸 고리 닫힘 ; 또는 ⅱ) 축합제와 환화되어 2-R2' 치환체를 갖는 피리미딘 고리를 형성시켜, R1이 히드록시기이고 R2가 아미노기인 일반식(Ⅰ)의 화합물을 생성시키는, Y가 아미노기이거나, 알콕시기인 일반식
    의 화합물의 피리미딘 고리 닫힘; 또는 ⅲ) Z인 이탈기인 일반식
    의 측쇄 중간체와 일반식
    의 화합물을 축합시키고, 이때 일반식(Ⅱ)-(Ⅴ)에 있어서, R1'R2'X'R4'가 각각 R1,R2,R3및 R4또는 그들로 전환 가능한 기 또는 원자이고; 그 후에, 원하거나 필요하다면, R1',R2'X' 및/또는 R4'가 아닐때 R1'R2'X' 및/또는 R4'를 R1,R4,X 및/또는 R4로 각각 전환시키고/거나 R1,R2,X 및/또는 R4일때, R1',R2',X' 및/또는 R4'를 다른 R1,R2,X 및/또는 R4로 전환시키는 것중 어느 하나로 구성되는, 제1항에 따르는 화합물의 제조방법.
  8. 제7항에서 정의된 바와같은 일반식(Ⅱ)의 중간체 화합물.
  9. 제7항에서 정의된 바와같은 일반식(Ⅲ)의 중간체 화합물.
  10. X'가 X이거나 X내의 R3가 보호기로 대치되고, R4및 X가 제1항에서 정의된 바와 같은 일반식
    R4OCH2X'ONH2의 중간체 화합물.
  11. 디에틸 3-아미노옥시프로폭시메틸포스포네이트, 디에틸 2-아세톡시메틸-3-아미노옥시프로폭시메틸포스포네이트 및 디에틸 2-아미노옥시-3-t-부틸디메틸실릴옥시프로폭시메틸포스포네이트로 구성된 군으로부터 선택된 중간체 화합물.
  12. 제1항 내지 제6항중 어느 한 항에 따른 화합물 및 약제학적으로 허용 가능한 담체로 구성된 제약학적 조성물.
  13. 활성 치료 물질로서의 사용을 위한 제1항 내지 제6항중 어느 한 항에 따른 화합물.
  14. 비루스성 감염 치료 또는 신생물 질병 치료에 있어서의 사용을 위한 제1항 내지 제6항중 어느 한 항에 따른 화합물.
  15. 비루스 감염 또는 신생물 질병의 치료에 있어서의 사용을 위한 약제의 제조에 있어서 제1항 내지 제6항중 어느 한 항에 따른 화합물의 사용.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019890011058A 1988-08-02 1989-08-01 신규 화합물 KR900003170A (ko)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
GB8818375 1988-08-02
GB888818375A GB8818375D0 (en) 1988-08-02 1988-08-02 Novel compounds
GB888827724A GB8827724D0 (en) 1988-11-28 1988-11-28 Novel compounds
GB8827724.9 1988-11-28

Publications (1)

Publication Number Publication Date
KR900003170A true KR900003170A (ko) 1990-03-23

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ID=26294230

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Application Number Title Priority Date Filing Date
KR1019890011058A KR900003170A (ko) 1988-08-02 1989-08-01 신규 화합물

Country Status (8)

Country Link
US (1) US5055458A (ko)
EP (1) EP0353955A3 (ko)
JP (1) JPH0288591A (ko)
KR (1) KR900003170A (ko)
AU (1) AU614863B2 (ko)
DK (1) DK375989A (ko)
NZ (1) NZ230144A (ko)
PT (1) PT91330A (ko)

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GB8907173D0 (en) * 1989-03-30 1989-05-10 Beecham Group Plc Novel compounds
GB8912043D0 (en) * 1989-05-25 1989-07-12 Beecham Group Plc Novel compounds
AU653542B2 (en) * 1990-07-19 1994-10-06 Beecham Group Plc Antiviral phosphono-alken derivatives of purines
DE69129650T2 (de) * 1990-09-14 1999-03-25 Acad Of Science Czech Republic Wirkstoffvorläufer von Phosphonaten
US5208221A (en) * 1990-11-29 1993-05-04 Bristol-Myers Squibb Company Antiviral (phosphonomethoxy) methoxy purine/pyrimidine derivatives
GB9026164D0 (en) * 1990-12-01 1991-01-16 Beecham Group Plc Pharmaceuticals
GB9107896D0 (en) * 1991-04-13 1991-05-29 Smithkline Beecham Plc Pharmaceuticals
EP0531597A1 (en) * 1991-09-12 1993-03-17 Merrell Dow Pharmaceuticals Inc. Novel unsaturated acyclic phosphonate derivatives of purine and pyrimidine
GB9205917D0 (en) * 1992-03-18 1992-04-29 Smithkline Beecham Plc Pharmaceuticals
WO1994022864A1 (en) * 1993-03-30 1994-10-13 Sterling Winthrop Inc. Acyclic nucleoside analogs and oligonucleotide sequences containing them
US5817647A (en) * 1993-04-01 1998-10-06 Merrell Pharmaceuticals Inc. Unsaturated acetylene phosphonate derivatives of purines
JPH09506333A (ja) * 1993-09-17 1997-06-24 ギリアード サイエンシーズ,インコーポレイテッド 治療化合物の投薬方法
US5798340A (en) 1993-09-17 1998-08-25 Gilead Sciences, Inc. Nucleotide analogs
US5789589A (en) * 1996-04-22 1998-08-04 Drug Innovation & Design, Inc. Guanine analog phosphates
EP0981532B1 (en) * 1997-05-15 2002-08-28 Drug Innovation & Design, Inc. Acyclovir diester derivatives
US6180790B1 (en) 1997-05-15 2001-01-30 Drug Innovation And Design, Inc. Methods of preparing acyclovir prodrugs
US6653318B1 (en) * 1999-07-21 2003-11-25 Yale University 5-(E)-Bromovinyl uracil analogues and related pyrimidine nucleosides as anti-viral agents and methods of use
CN100526315C (zh) 2005-06-16 2009-08-12 浙江医药股份有限公司新昌制药厂 N2-喹啉或异喹啉取代的嘌呤衍生物及其制备方法和其用途
CN101289449A (zh) 2007-04-20 2008-10-22 浙江医药股份有限公司新昌制药厂 2,6-二含氮取代的嘌呤衍生物及其制备方法和应用
CA2819548C (en) 2010-12-10 2019-04-09 Sigmapharm Laboratories, Llc Highly stable compositions of orally active nucleotide analogues or orally active nucleotide analogue prodrugs
JP6122960B2 (ja) * 2012-10-08 2017-04-26 ダウ グローバル テクノロジーズ エルエルシー 難燃性ポリウレタンフォーム用の有機リン化合物
US9523195B2 (en) 2014-06-09 2016-12-20 Johns Manville Wall insulation boards with non-halogenated fire retardant and insulated wall systems
US9815256B2 (en) 2014-06-09 2017-11-14 Johns Manville Foam boards including non-halogenated fire retardants
US9528269B2 (en) 2014-06-09 2016-12-27 Johns Manville Roofing systems and roofing boards with non-halogenated fire retardant
US9815966B2 (en) 2014-07-18 2017-11-14 Johns Manville Spray foams containing non-halogenated fire retardants

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EP0138683A3 (en) * 1983-09-30 1988-01-20 Merck & Co. Inc. Purine derivatives, their application in anti-viral compositions
CS263951B1 (en) * 1985-04-25 1989-05-12 Antonin Holy 9-(phosponylmethoxyalkyl)adenines and method of their preparation
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MY101126A (en) * 1985-12-13 1991-07-31 Beecham Group Plc Novel compounds
GB8712744D0 (en) * 1987-05-30 1987-07-01 Beecham Group Plc Active compounds
GB8713695D0 (en) * 1987-06-11 1987-07-15 Beecham Group Plc Process
GB8724765D0 (en) * 1987-10-22 1987-11-25 Beecham Group Plc Process
PT89098B (pt) * 1987-11-30 1993-03-31 Beecham Group Plc Processo para a preparacao de derivados de guanina

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DK375989A (da) 1990-02-03
AU614863B2 (en) 1991-09-12
EP0353955A2 (en) 1990-02-07
DK375989D0 (da) 1989-07-31
PT91330A (pt) 1990-03-08
EP0353955A3 (en) 1991-08-14
US5055458A (en) 1991-10-08
AU3913989A (en) 1990-02-08
JPH0288591A (ja) 1990-03-28
NZ230144A (en) 1991-09-25

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