KR840001589A - 1-β-D-아라비노프라노실-(E)-5-(2-할로게노비닐) 우라실-5'-인산염 및 그 제조방법 - Google Patents
1-β-D-아라비노프라노실-(E)-5-(2-할로게노비닐) 우라실-5'-인산염 및 그 제조방법 Download PDFInfo
- Publication number
- KR840001589A KR840001589A KR1019820003969A KR820003969A KR840001589A KR 840001589 A KR840001589 A KR 840001589A KR 1019820003969 A KR1019820003969 A KR 1019820003969A KR 820003969 A KR820003969 A KR 820003969A KR 840001589 A KR840001589 A KR 840001589A
- Authority
- KR
- South Korea
- Prior art keywords
- halogenovinyl
- uracil
- formula
- dna virus
- arabinofranosyl
- Prior art date
Links
- 229910019142 PO4 Inorganic materials 0.000 title claims 4
- 239000010452 phosphate Substances 0.000 title claims 4
- 238000002360 preparation method Methods 0.000 title claims 2
- 241000700605 Viruses Species 0.000 claims 7
- 230000003172 anti-dna Effects 0.000 claims 7
- 239000000203 mixture Substances 0.000 claims 7
- 229910052736 halogen Inorganic materials 0.000 claims 5
- 150000002367 halogens Chemical group 0.000 claims 5
- ISAKRJDGNUQOIC-UHFFFAOYSA-N Uracil Chemical compound O=C1C=CNC(=O)N1 ISAKRJDGNUQOIC-UHFFFAOYSA-N 0.000 claims 4
- 239000003795 chemical substances by application Substances 0.000 claims 3
- 230000000865 phosphorylative effect Effects 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 2
- 229910052801 chlorine Inorganic materials 0.000 claims 2
- 239000000460 chlorine Substances 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 229940035893 uracil Drugs 0.000 claims 2
- ZCYVEMRRCGMTRW-UHFFFAOYSA-N 7553-56-2 Chemical compound [I] ZCYVEMRRCGMTRW-UHFFFAOYSA-N 0.000 claims 1
- DTRYYPKLEYYJTH-UHFFFAOYSA-N I.OP(O)(O)=O Chemical class I.OP(O)(O)=O DTRYYPKLEYYJTH-UHFFFAOYSA-N 0.000 claims 1
- OAICVXFJPJFONN-UHFFFAOYSA-N Phosphorus Chemical compound [P] OAICVXFJPJFONN-UHFFFAOYSA-N 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- 230000003602 anti-herpes Effects 0.000 claims 1
- 150000001875 compounds Chemical class 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 239000003889 eye drop Substances 0.000 claims 1
- 229940012356 eye drops Drugs 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 239000011630 iodine Substances 0.000 claims 1
- 229910052740 iodine Inorganic materials 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 239000002674 ointment Substances 0.000 claims 1
- 229910052698 phosphorus Inorganic materials 0.000 claims 1
- 239000011574 phosphorus Substances 0.000 claims 1
- 238000006366 phosphorylation reaction Methods 0.000 claims 1
- 230000003612 virological effect Effects 0.000 claims 1
Classifications
-
- 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
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)
- Genetics & Genomics (AREA)
- Biotechnology (AREA)
- Biochemistry (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Virology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Saccharide Compounds (AREA)
- Curing Cements, Concrete, And Artificial Stone (AREA)
Abstract
내용 없음
Description
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
Claims (20)
- 하기 구조식을 가진 1-β-D-아라비노프라노실-(E)-5-(2-할로게노비닐) 우라실-5′-인산염 및 그 제조 방법.
-
- 식중, X는 할로겐을 나타낸다.
- X가 취소, 염소 및 요오드로 구성된 그루우프에서 선택된 할로겐인 특허청구의 범위 1기재의 1-β-D-아라비노프라노실-(E)-5-(2-할로게노비닐) 우라실-5′-인산염 및 그 제조 방법.
- 하기 구조식(Ⅱ)의 1-β-D-아라비노프라노실-(E)-5-(2-할로게노비닐) 우라실을 인산화제와 반응시킴에 의하여 5′-위(位)의 히드록실기를 인산화하며, 그리고 선택적으로 상기의 형성된 산을 소망하는 염으로 변환시킴으로써 이루어지는 하기 구조식(Ⅰ)의 1-β-D-아라비노프라노실-(E)-5-(2-할로게노비닐) 우라실-5′-인산염 또는 약학적으로 받아들일 수 있는 그 염의 제조 방법.
-
- 식중, X는 할로겐을 나타낸다.
-
- 식중, X는 위에서 정의된 것과 동일하다.
- 인산화반응이 트리알킬인산염내에서 인산화제로서 포스포러스 옥시클로 라이드의 사용에 의하여 수행되어지는 특허청구의 범위 3기재의 1-β-D-아라비노프라노실-(E)-5-(2-할로게노비닐) 우라실-5′-인산염의 제조 방법.
- 유효량의 하기 구조식(Ⅰ)의 화합물 또는 약적으로 받아들일 수 있는 그 염과 약학적으로 받아들일 수 있는 담체로 이루어지는 항-DNA 바이러스제 조성물.
-
- 식중, X는 할로겐을 나타낸다.
- X가 취소, 염소 및 요오드로 구성된 그루우프에서 선택된 할로겐인 특허청구의 범위 5기재의 항-DNA 바이러스제 조성물.
- 항-헤르페스 바이러스제인 특허청구의 범위 5 또는 6기재의 항-DNA 바이러스제 조성물.
- 항-수두 바이러스제인 특허청구의 범위 5 또는 6기재의 항-DNA 바이러스제 조성물.
- 안약형태로된 특허청구의 범위 5기재의 항-DNA 바이러스제 조성물.
- 주사약형태로된 특허청구의 범위 5기재의 항-DNA 바이러스제 조성물.
- 연고형태로된 특허청구의 범위 5기재의 항-DNA 바이러스제 조성물.
- ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP56142045A JPS5843993A (ja) | 1981-09-09 | 1981-09-09 | 1−β−D−アラビノフラノシル−(E)−5−(2−ハロゲノビニル)ウラシル−5′−りん酸およびその製造法 |
JP81-142045 | 1981-09-09 |
Publications (2)
Publication Number | Publication Date |
---|---|
KR840001589A true KR840001589A (ko) | 1984-05-07 |
KR890000762B1 KR890000762B1 (ko) | 1989-04-05 |
Family
ID=15306105
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
KR8203969A KR890000762B1 (ko) | 1981-09-09 | 1982-09-03 | 1-β-D-아라비노프라노실-(E)-5-(2-할로게노비닐)우라실-5'-인산의 제조방법 |
Country Status (12)
Country | Link |
---|---|
US (1) | US4542210A (ko) |
EP (1) | EP0074101B1 (ko) |
JP (1) | JPS5843993A (ko) |
KR (1) | KR890000762B1 (ko) |
AT (1) | ATE12503T1 (ko) |
AU (1) | AU552353B2 (ko) |
CA (1) | CA1204107A (ko) |
DE (1) | DE3262887D1 (ko) |
ES (1) | ES8308570A1 (ko) |
GB (1) | GB2108964B (ko) |
MY (1) | MY8700826A (ko) |
SG (1) | SG81787G (ko) |
Families Citing this family (18)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPS5843993A (ja) * | 1981-09-09 | 1983-03-14 | Yamasa Shoyu Co Ltd | 1−β−D−アラビノフラノシル−(E)−5−(2−ハロゲノビニル)ウラシル−5′−りん酸およびその製造法 |
JPS58225097A (ja) * | 1982-06-23 | 1983-12-27 | Yamasa Shoyu Co Ltd | ヌクレオシド5′−アルキルもしくはアルケニルりん酸 |
EP0104066B1 (en) * | 1982-09-17 | 1988-08-10 | Glaxo Group Limited | 5-halovinyl-2'-deoxyuridine derivatives |
US4658044A (en) * | 1983-09-16 | 1987-04-14 | Glaxo Group Limited | Intermediates for uracil derivatives |
ZA85578B (en) * | 1985-01-24 | 1985-07-22 | Neopharmed S.P.A. | Acylated derivatives of cytidine-diphosphate-choline,process for their preparation and their therapeutic use |
GB8912972D0 (en) * | 1989-06-06 | 1989-07-26 | Wellcome Found | Therapeutic nucleosides |
KR960008669B1 (ko) * | 1991-04-24 | 1996-06-28 | 야마사 쇼오유 가부시끼가이샤 | 1-β-D-아라비노푸라노실-(E)-5-(2-할로게노비닐) 우라실 유도체 |
US5446031A (en) * | 1991-04-24 | 1995-08-29 | Yamasa Shuyu Kabushiki Kaisha | 1-β-D-arabinofuranosyl-(E)-5-(2-halogenovinyl)uracil derivatives |
CA2298681C (en) | 1997-08-08 | 2008-07-08 | Newbiotics, Inc. | Methods and compositions for overcoming resistance to biologic and chemotherapy |
US7462605B2 (en) * | 1998-01-23 | 2008-12-09 | Celmed Oncology (Usa), Inc. | Phosphoramidate compounds and methods of use |
AU753155B2 (en) | 1998-01-23 | 2002-10-10 | Kiadis Pharma Intellectual Property B.V. | Enzyme catalyzed therapeutic agents |
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 |
US6683061B1 (en) * | 1999-07-22 | 2004-01-27 | Newbiotics, Inc. | Enzyme catalyzed therapeutic activation |
MXPA02000762A (es) | 1999-07-22 | 2002-08-20 | Newbiotics Inc | Metodos para tratar tumores resistentes a terapia. |
CA2441350A1 (en) * | 2001-01-19 | 2002-07-25 | Newbiotics, Inc. | Methods to treat autoimmune and inflammatory conditions |
EP1569658A4 (en) * | 2001-12-20 | 2007-05-30 | Pharmassett Ltd | TREATMENT OF EPSTEIN-BARR VIRUS, INFECTION WITH KAPOSI-ASSOCIATED SARCOMA HERPESVIRUS AND ABNORMAL CELL PROLIFERATION |
JP4964473B2 (ja) * | 2006-02-10 | 2012-06-27 | アリジェン製薬株式会社 | ピリミジンヌクレオシド誘導体及びその塩 |
US8076302B2 (en) | 2007-02-15 | 2011-12-13 | Arigen Pharmaceuticals, Inc. | Pyrimidine nucleoside derivatives and salts thereof |
Family Cites Families (11)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
GB1157275A (en) * | 1965-07-27 | 1969-07-02 | Takeda Chemical Industries Ltd | A Method for the Production of 5'-Ribonucleotide |
US3382232A (en) * | 1965-08-26 | 1968-05-07 | Takeda Chemical Industries Ltd | Method for the production of 5'-ribonucleotide |
FR5616M (ko) * | 1966-07-29 | 1968-01-15 | ||
EP0015584A3 (de) * | 1979-03-12 | 1980-12-10 | Kailash Kumar Dr. Prof. Gauri | Neue Nukleotide, Verfahren zu ihrer Herstellung und Arzneimittel |
US4247544A (en) * | 1979-07-02 | 1981-01-27 | The Regents Of The University Of California | C-5 Substituted uracil nucleosides |
US4267171A (en) * | 1979-07-02 | 1981-05-12 | The Regents Of The University Of California | C-5 Substituted cytosine nucleosides |
GB2060604B (en) * | 1979-10-03 | 1983-11-23 | Univ Birmingham And Stichting | E15-(2-halogenovinyl)-2'-deoxycytidines |
JPS5687599A (en) * | 1979-12-19 | 1981-07-16 | Yamasa Shoyu Co Ltd | E 55 22halogenovinyl arabinofuranosyluracil and its preparation |
JPS5714598A (en) * | 1980-06-30 | 1982-01-25 | Yamasa Shoyu Co Ltd | 5-substituted-1-beta-d-arabinofuranosyluracil derivative and its preparation |
US4383990A (en) * | 1980-10-01 | 1983-05-17 | Beecham Group Limited | Antiviral agents, their preparation and use |
JPS5843993A (ja) * | 1981-09-09 | 1983-03-14 | Yamasa Shoyu Co Ltd | 1−β−D−アラビノフラノシル−(E)−5−(2−ハロゲノビニル)ウラシル−5′−りん酸およびその製造法 |
-
1981
- 1981-09-09 JP JP56142045A patent/JPS5843993A/ja active Granted
-
1982
- 1982-09-03 DE DE8282108163T patent/DE3262887D1/de not_active Expired
- 1982-09-03 US US06/414,824 patent/US4542210A/en not_active Expired - Fee Related
- 1982-09-03 AT AT82108163T patent/ATE12503T1/de not_active IP Right Cessation
- 1982-09-03 KR KR8203969A patent/KR890000762B1/ko active
- 1982-09-03 EP EP82108163A patent/EP0074101B1/en not_active Expired
- 1982-09-03 AU AU87996/82A patent/AU552353B2/en not_active Ceased
- 1982-09-08 ES ES515573A patent/ES8308570A1/es not_active Expired
- 1982-09-08 GB GB08225547A patent/GB2108964B/en not_active Expired
- 1982-09-08 CA CA000411003A patent/CA1204107A/en not_active Expired
-
1987
- 1987-10-09 SG SG817/87A patent/SG81787G/en unknown
- 1987-12-30 MY MY826/87A patent/MY8700826A/xx unknown
Also Published As
Publication number | Publication date |
---|---|
EP0074101A1 (en) | 1983-03-16 |
AU552353B2 (en) | 1986-05-29 |
EP0074101B1 (en) | 1985-04-03 |
JPS5843993A (ja) | 1983-03-14 |
DE3262887D1 (en) | 1985-05-09 |
GB2108964A (en) | 1983-05-25 |
CA1204107A (en) | 1986-05-06 |
AU8799682A (en) | 1983-03-17 |
SG81787G (en) | 1988-04-15 |
JPS637559B2 (ko) | 1988-02-17 |
ES515573A0 (es) | 1983-09-16 |
ATE12503T1 (de) | 1985-04-15 |
ES8308570A1 (es) | 1983-09-16 |
US4542210A (en) | 1985-09-17 |
MY8700826A (en) | 1987-12-31 |
KR890000762B1 (ko) | 1989-04-05 |
GB2108964B (en) | 1985-04-11 |
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