KR880006256A - 항비루스성 포스포노메톡시알킬렌푸린과 피리미딘 유도체 - Google Patents

항비루스성 포스포노메톡시알킬렌푸린과 피리미딘 유도체 Download PDF

Info

Publication number
KR880006256A
KR880006256A KR1019870012967A KR870012967A KR880006256A KR 880006256 A KR880006256 A KR 880006256A KR 1019870012967 A KR1019870012967 A KR 1019870012967A KR 870012967 A KR870012967 A KR 870012967A KR 880006256 A KR880006256 A KR 880006256A
Authority
KR
South Korea
Prior art keywords
compound
guanine
phosphonomethoxy
ethyl
hydrogen
Prior art date
Application number
KR1019870012967A
Other languages
English (en)
Other versions
KR950009195B1 (ko
Inventor
알. 웨브 2세 로버트
제이. 브론슨 죠안느
씨. 마틴 존
Original Assignee
이삭 쟈코브스키
브리스톨 마이어즈 캄파니
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=26812069&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=KR880006256(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by 이삭 쟈코브스키, 브리스톨 마이어즈 캄파니 filed Critical 이삭 쟈코브스키
Publication of KR880006256A publication Critical patent/KR880006256A/ko
Application granted granted Critical
Publication of KR950009195B1 publication Critical patent/KR950009195B1/ko

Links

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
    • 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
    • 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
    • C07F9/645—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having two nitrogen atoms as the only ring hetero atoms
    • C07F9/6509—Six-membered rings
    • C07F9/6512—Six-membered rings having the nitrogen atoms in positions 1 and 3

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (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

내용 없음

Description

항비루스성 포스포노메톡시알킬렌푸린과 피리미딘 유도체
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (27)

  1. B가 아데닌, 크산틴, 하이포잔틴, 구아니, 8-브로모구아닌, 8-클로로구아닌, 8-아미노구아닌, 8-히드라지노구아닌, 8-히드록시구아닌, 8-메틸구아닌, 8-티오구아닌, 2-아미노푸란, 2,6-디아미노푸린, 시토신, 5-에틸시토신, 5-메틸시토신, 티민, 우라실, 5-브로모우라실, 5-에틸우라실, 5-요오드우라실, 5-프로필우라실, 5-비닐우라실 및 5-브로모비닐우라실로 이루어지는 그룹으로 부터 선택되는 푸린이나 피리미딘 염기이며; B가 아데닌이며 alk1이 메틸렌인 경우 alk2는 화학 결합이 될 수 없다는 것을 조건으로 하여 alk1,alk2,alk3는 화학 결합이나 C1-4알킬렌으로 부터 독립적으로 선택되며, B가 아데닌이고, Q가 수소인 경우 alk1은 단지 C4H8만이 될 수 있음을 조건으로 하여 Q는 수소 및 수산기이고; R1과 R2는 수소 및 C1-4알킬로부터 독립적으로 선택되고; R3및 R4는 수소, C1-6알킬, 페닐 및 페닐-C1-4-알킬렌으로 부터 독립적으로 선택되는 다음 일반식 I의 화합물 및 그에 상응하는 염, 양성이온, 및/또는 용매화합물.
  2. B가 푸린염기인 제1항의 화합물.
  3. 푸린염기가 구아닌 성분인 제2항의 화합물.
  4. B가 피리미딘 염기인 제1항의 화합물.
  5. R1,R2및 Q가 수소인 제2항의 화합물.
  6. R3와 R4가 수소인 제1항의 화합물.
  7. R3와 R4중 하나가 수소이고 다른 하나가 C1-6알킬인 제1항의 화합물.
  8. 9-(3-히드록시-2-포스포노메톡시프로필)구아닌인 제1항의 화합물.
  9. 9-(2-포스포노메톡시)에틸)구아닌인 제1항의 화합물.
  10. 9-(3-포스포노메톡시)프로필)구아닌인 제1항의 화합물.
  11. 9-(4-포스포노메톡시)부틸)구아닌인 제1항의 화합물.
  12. 8-브로모-9-(2-포스포노메톡시)에틸)구아닌인 제1항의 화합물.
  13. 1-(4-포스포노메톡시)부틸)티민인 제1항의 화합물.
  14. 9-(1-메틸-2-(포스포노메톡시)에틸)구아닌인 제1항의 화합물.
  15. 9-(2-(포스포노메톡시)-1-프로필)구아닌인 제1항의 화합물.
  16. 9-(2-히드록시메틸-3-(포스포노메톡시)프로필)구아닌인 제1항의 화합물.
  17. 9-(2-히드록시메틸-3-(포스포노메톡시)프로필)아데닌인 제1항의 화합물.
  18. 8-메틸-9-(2-(포스포노메톡시)에틸)구아닌인 제1항의 화합물.
  19. 9-(4-히드록시-3-(포스포노메톡시)부틸)구아닌인 제1항의 화합물.
  20. 9-(4-히드록시-3-(포스포노메톡시)부틸)아데닌인 제1항의 화합물.
  21. 9-(2-단일에틸포스포노메톡시)에틸)구아닌인 제1항의 화합물.
  22. 9-(2-단일메틸포스포노메톡시)에틸)구아닌인 제1항의 화합물.
  23. 9-(2-단일-n-프로필포스포노메톡시)에틸)구아닌인 제1항의 화합물.
  24. 9-(2-단일-이소프로필포스포노메톡시)에틸)구아닌인 제1항의 화합물.
  25. 9-(2-(1-포스포노-1-에톡시)에틸)구아닌인 제1항의 화합물.
  26. 제1항 화합물의 효과적인 항비루스양과 제약학적으로 허용되는 담체가 혼합되어 이루어지는 항비루스용 제약학적 조성물.
  27. 항비루스 화합물이 9-(2-(포스포노메톡시)에틸)구아닌인 제26항의 제약학적 조성물.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019870012967A 1986-11-18 1987-11-18 항 비루스성 포스포노메톡시알킬렌 푸린 및 피리미딘 유도체 KR950009195B1 (ko)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US93211286A 1986-11-18 1986-11-18
US932,112 1986-11-18
US932112 1986-11-18
US11434087A 1987-11-04 1987-11-04

Publications (2)

Publication Number Publication Date
KR880006256A true KR880006256A (ko) 1988-07-22
KR950009195B1 KR950009195B1 (ko) 1995-08-16

Family

ID=26812069

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1019870012967A KR950009195B1 (ko) 1986-11-18 1987-11-18 항 비루스성 포스포노메톡시알킬렌 푸린 및 피리미딘 유도체

Country Status (12)

Country Link
EP (1) EP0269947B2 (ko)
JP (1) JP2593895B2 (ko)
KR (1) KR950009195B1 (ko)
AU (1) AU613592B2 (ko)
CA (1) CA1339780C (ko)
DE (1) DE3780581T3 (ko)
DK (1) DK170049B1 (ko)
EG (1) EG19346A (ko)
ES (1) ES2033774T5 (ko)
GR (2) GR3005256T3 (ko)
IL (1) IL84477A (ko)
NZ (1) NZ222553A (ko)

Families Citing this family (36)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CS264222B1 (en) * 1986-07-18 1989-06-13 Holy Antonin N-phosphonylmethoxyalkylderivatives of bases of pytimidine and purine and method of use them
IL84477A (en) * 1986-11-18 1995-12-08 Bristol Myers Squibb Co History of Phosphonomethoxyalkylene Purinopyrimidine and Pharmaceutical Preparations Containing Them
EP0338168A1 (en) * 1988-04-19 1989-10-25 Merrell Dow Pharmaceuticals Inc. Phosphonoalkylpurine derivatives
US5266722A (en) * 1988-11-09 1993-11-30 W. R. Grace & Co.-Conn. Polyether bis-phosphonic acid compounds
US5688778A (en) * 1989-05-15 1997-11-18 Institute Of Organic Chemistry And Biochemistry Of The Academy Of Sciences Of The Czech Republic Nucleoside analogs
DE69110528T2 (de) * 1990-04-20 1996-03-14 Inst Of Organic Chemistry And Chirale 2-(Phosphonomethoxy)propyl-Guanine als antivirale Agentien.
US5302585A (en) * 1990-04-20 1994-04-12 Institute Of Organic Chemistry And Biochemistry Of The Academy Of Sciences Of The Czech Republic Use of chiral 2-(phosphonomethoxy)propyl guanines as antiviral agents
CZ285420B6 (cs) * 1990-04-24 1999-08-11 Ústav Organické Chemie A Biochemie Avčr N-(3-Fluor-2-fosfonylmethoxypropyl)deriváty purinových a pyrimidinových heterocyklických bazí, způsoby jejich přípravy a použití
EP0481214B1 (en) * 1990-09-14 1998-06-24 Institute Of Organic Chemistry And Biochemistry Of The Academy Of Sciences Of The Czech Republic Prodrugs of phosphonates
US5208221A (en) * 1990-11-29 1993-05-04 Bristol-Myers Squibb Company Antiviral (phosphonomethoxy) methoxy purine/pyrimidine derivatives
CZ287745B6 (cs) * 1991-10-11 2001-01-17 Ústav organické chemie a biochemie AV ČR Acyklické fosfonomethoxyalkylsubstituované alkenylové a alkinylové deriváty purinu a pyrimidinu
US6057305A (en) * 1992-08-05 2000-05-02 Institute Of Organic Chemistry And Biochemistry Of The Academy Of Sciences Of The Czech Republic Antiretroviral enantiomeric nucleotide analogs
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
US5656745A (en) * 1993-09-17 1997-08-12 Gilead Sciences, Inc. Nucleotide analogs
US5798340A (en) * 1993-09-17 1998-08-25 Gilead Sciences, Inc. Nucleotide analogs
IT1270008B (it) * 1994-09-23 1997-04-16 Ist Superiore Sanita Derivati purinici ed 8-azapurinici atti al trattamento terapeutico dell'aids
US5977061A (en) * 1995-04-21 1999-11-02 Institute Of Organic Chemistry And Biochemistry Of The Academy Of Sciences Of The Czech Republic N6 - substituted nucleotide analagues and their use
US5717095A (en) * 1995-12-29 1998-02-10 Gilead Sciences, Inc. Nucleotide analogs
CA2261619C (en) * 1996-07-26 2006-05-23 Gilead Sciences, Inc. Nucleotide analogs
US5922695A (en) * 1996-07-26 1999-07-13 Gilead Sciences, Inc. Antiviral phosphonomethyoxy nucleotide analogs having increased oral bioavarilability
AU740264C (en) * 1997-09-11 2002-06-06 Commonwealth Scientific And Industrial Research Organisation Antiviral agents
IL159494A0 (en) 2001-06-29 2004-06-01 Acad Of Science Czech Republic 6-2'-(phosphonomethoxy) alkoxy pyrimidine derivatives having antiviral activity
WO2003087298A2 (en) * 2001-11-14 2003-10-23 Biocryst Pharmaceuticals, Inc. Nucleosides preparation thereof and use as inhibitors of rna viral polymerases
US7388002B2 (en) 2001-11-14 2008-06-17 Biocryst Pharmaceuticals, Inc. Nucleosides, preparation thereof and use as inhibitors of RNA viral polymerases
AU2004206827A1 (en) 2003-01-14 2004-08-05 Gilead Sciences, Inc. Compositions and methods for combination antiviral therapy
US7371852B2 (en) 2003-01-22 2008-05-13 Serenex, Inc. Alkyl-linked nucleotide compositions
CA2527805C (en) 2003-06-16 2012-08-21 Institute Of Organic Chemistry And Biochemistry, Academy Of Sciences Of The Czech Republic Pyrimidine compounds having phosphonate groups as antiviral nucleotide analogs
US20060252729A1 (en) 2003-07-30 2006-11-09 Krawczyk Steven H Nucleobase phosphonate analogs for antiviral treatment
WO2005090370A1 (en) 2004-02-05 2005-09-29 The Regents Of The University Of California Pharmacologically active agents containing esterified phosphonates and methods for use thereof
TWI375560B (en) 2005-06-13 2012-11-01 Gilead Sciences Inc Composition comprising dry granulated emtricitabine and tenofovir df and method for making the same
TWI471145B (zh) 2005-06-13 2015-02-01 Bristol Myers Squibb & Gilead Sciences Llc 單一式藥學劑量型
TWI444384B (zh) 2008-02-20 2014-07-11 Gilead Sciences Inc 核苷酸類似物及其在治療惡性腫瘤上的用途
MX2013006127A (es) 2010-12-10 2013-09-26 Sigmapharm Lab Llc Composiciones sumamente estables de analogos nucleotidicoas oralmente activos o profarmacos analogos nucleotidicos oralmente activos.
DK2794624T3 (da) 2011-12-22 2019-07-22 Geron Corp Guanin-analoger som telomerase-substrater og påvirkere af telomer-længde
CN103665043B (zh) 2012-08-30 2017-11-10 江苏豪森药业集团有限公司 一种替诺福韦前药及其在医药上的应用
EP3194411B1 (en) * 2014-09-15 2022-05-04 The Regents of the University of California Nucleotide analogs

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CS233665B1 (en) * 1983-01-06 1985-03-14 Antonin Holy Processing of isomere o-phosphonylmethylderivative of anantiomere racemic vicinal diene
CS263952B1 (en) * 1985-04-25 1989-05-12 Holy Antonin Remedy with antiviral effect
CS263951B1 (en) * 1985-04-25 1989-05-12 Antonin Holy 9-(phosponylmethoxyalkyl)adenines and method of their preparation
CS264222B1 (en) * 1986-07-18 1989-06-13 Holy Antonin N-phosphonylmethoxyalkylderivatives of bases of pytimidine and purine and method of use them
IL84477A (en) * 1986-11-18 1995-12-08 Bristol Myers Squibb Co History of Phosphonomethoxyalkylene Purinopyrimidine and Pharmaceutical Preparations Containing Them

Also Published As

Publication number Publication date
JPS63170388A (ja) 1988-07-14
NZ222553A (en) 1991-07-26
AU8125087A (en) 1988-05-19
JP2593895B2 (ja) 1997-03-26
IL84477A (en) 1995-12-08
DK604087A (da) 1988-05-19
KR950009195B1 (ko) 1995-08-16
AU613592B2 (en) 1991-08-08
DE3780581T2 (de) 1992-12-17
ES2033774T3 (es) 1993-04-01
DE3780581T3 (de) 1997-06-05
DE3780581D1 (de) 1992-08-27
GR3005256T3 (en) 1993-05-24
EP0269947B1 (en) 1992-07-22
EP0269947A1 (en) 1988-06-08
ES2033774T5 (es) 1997-03-16
CA1339780C (en) 1998-03-24
DK604087D0 (da) 1987-11-17
EG19346A (en) 1995-01-31
GR3021389T3 (en) 1997-01-31
DK170049B1 (da) 1995-05-08
EP0269947B2 (en) 1996-10-16

Similar Documents

Publication Publication Date Title
KR880006256A (ko) 항비루스성 포스포노메톡시알킬렌푸린과 피리미딘 유도체
TR200103328T2 (tr) Çamaşır yumuşatıcı bileşimlerin dengelenmesi yöntemi.
RU2694252C3 (ru) Производные 4-(замещенного фениламино)хиназолина или их фармацевтически приемлемые соли, способ ингибирования рецепторной тирозинкиназы и фармацевтическая композиция
TR200002953T2 (tr) İki halkalı hidroksamik asit türevleri
IL134167A0 (en) Flouropyrazole- biphenylamide fungicides
BR0011521A (pt) Composto nucleósidos de purina de 4' -c-etinila
EP1330004A3 (en) 2-Piece ladder rack bracket
DE60101223D1 (de) Antivirale pyrimidin nucleoside derivate
KR920000746A (ko) 아미노벤조디아제핀
KR920012047A (ko) 우라실 유도체 및 이를 활성 성분으로 함유하는 제초제
IL103410A0 (en) Acyclic phosphonomethoxyalkyl substituted,alkenyl and alkynyl purine and pyrimidine derivatives and pharmaceutical compositions comprising them
ATE132752T1 (de) Antivirale zusammensetzung
KR970027071A (ko) 피롤릴벤즈이미다졸유도체
DK1165560T3 (da) 2-Hydroxymethylcyclopropylidenmethylpuriner som antivirale midler
ATE231836T1 (de) Anti-tumor-mittel
BR0317917A (pt) Processo para dinamicamente alocar largura de banda de elo em anel de pacote resiliente
BR0011754A (pt) Tira de borda para uma placa de catodo e placa de catodo
DK1305296T3 (da) 5-substituerede pyrimidinderivater af konformationsfastlagte nucleosidanaloge
KR880007494A (ko) 5-아릴-3h-1,2,4-트리아졸-3-온 및 진경제로서의 그들의 용도
PT86156A (en) Process for the preparation of phosphonomethoxyalkylene purine and pyrimidine derivatives and of pharmaceutical compositions containing the same
BR9907426A (pt) Tetrahidronaftalenos
CA2228078A1 (en) Composition for oral administration containing pyridazinone compounds
KR920002601A (ko) 신규 핵산 유도체
KR850006191A (ko) 티오시아노 피리미딘 유도체의 제조방법
KR880007479A (ko) 살균제용 이미다졸 및 트리아졸 유도체

Legal Events

Date Code Title Description
A201 Request for examination
G160 Decision to publish patent application
E902 Notification of reason for refusal
N231 Notification of change of applicant
E701 Decision to grant or registration of patent right
GRNT Written decision to grant
FPAY Annual fee payment

Payment date: 20090811

Year of fee payment: 15

EXPY Expiration of term