CN101115765A - 修饰的叠氮胸苷的5'-膦酸酯-潜在的抗病毒制剂 - Google Patents
修饰的叠氮胸苷的5'-膦酸酯-潜在的抗病毒制剂 Download PDFInfo
- Publication number
- CN101115765A CN101115765A CNA2005800467450A CN200580046745A CN101115765A CN 101115765 A CN101115765 A CN 101115765A CN A2005800467450 A CNA2005800467450 A CN A2005800467450A CN 200580046745 A CN200580046745 A CN 200580046745A CN 101115765 A CN101115765 A CN 101115765A
- Authority
- CN
- China
- Prior art keywords
- azt
- azido
- compound
- cell
- phosphonates
- Prior art date
- Legal status (The legal status 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 status listed.)
- Granted
Links
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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
-
- 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
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Molecular Biology (AREA)
- Virology (AREA)
- Biochemistry (AREA)
- Biotechnology (AREA)
- Engineering & Computer Science (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Genetics & Genomics (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Communicable Diseases (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Tropical Medicine & Parasitology (AREA)
- AIDS & HIV (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Description
化合物 | CD50,μM | ID50,μM | IS |
Ia | 300 | 0.05-0.1 | >3000 |
Ib | >500 | 1-5 | >100 |
Ic | >500 | 0.08-0.3 | >1600 |
Id | >500 | 1-5 | >100 |
Ie | >300 | 0.05-0.1 | >3000 |
Nikavir | 260 | 0.13 | 2015 |
化合物 | T1/2小时 | AUC,mg×h/L | MRT,小时 | CL,升/小时 | Tmax小时 | Cmax,mg/L |
Ie | 9.6 | 9.24 | 13.9 | 27.0 | 5.0 | 0.74 |
Nikavir | 7.2 | 16.6 | 10.4 | 15.0 | 4.0 | 1.89 |
AZT | 5.2 | 58.8 | 7.5 | 4.2 | 2.5 | 9.77 |
Claims (2)
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
RU2004134388/04A RU2322450C2 (ru) | 2004-11-25 | 2004-11-25 | Модифицированные 5'-фосфонаты азт в качестве активных компонентов для потенциальных противовирусных препаратов |
RU2004134388 | 2004-11-25 | ||
PCT/RU2005/000249 WO2006062434A1 (en) | 2004-11-25 | 2005-05-06 | Modified 5'- phosphonate azidothymidine-potential anti-viral preparations |
Publications (2)
Publication Number | Publication Date |
---|---|
CN101115765A true CN101115765A (zh) | 2008-01-30 |
CN101115765B CN101115765B (zh) | 2012-10-10 |
Family
ID=36578174
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CN2005800467450A Expired - Fee Related CN101115765B (zh) | 2004-11-25 | 2005-05-06 | 修饰的叠氮胸苷的5’-膦酸酯—潜在的抗病毒制剂 |
Country Status (7)
Country | Link |
---|---|
US (1) | US7999099B2 (zh) |
EP (1) | EP1829885B1 (zh) |
KR (1) | KR101323698B1 (zh) |
CN (1) | CN101115765B (zh) |
ES (1) | ES2550136T3 (zh) |
RU (1) | RU2322450C2 (zh) |
WO (1) | WO2006062434A1 (zh) |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN104114570A (zh) * | 2011-10-14 | 2014-10-22 | 齐多夫定生产和商业协会封闭式股份公司 | 作为人免疫缺陷病毒hiv-1产生的选择性抑制剂的氨基甲酰基膦酸酯盐 |
Family Cites Families (7)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4824850A (en) * | 1982-05-18 | 1989-04-25 | University Of Florida | Brain-specific drug delivery |
US4968788A (en) * | 1986-04-04 | 1990-11-06 | Board Of Regents, The University Of Texas System | Biologically reversible phosphate and phosphonate protective gruops |
SU1548182A1 (ru) * | 1987-12-29 | 1990-03-07 | Институт молекулярной биологии АН СССР | 5 @ -Фосфонаты 3 @ -азидо-2 @ ,3 @ -дидезоксинуклеозидов, вл ющиес специфическими ингибиторами вируса СПИД в культуре лимфоцитов человека Н9/ШВ |
US5002935A (en) * | 1987-12-30 | 1991-03-26 | University Of Florida | Improvements in redox systems for brain-targeted drug delivery |
WO1991019727A1 (en) * | 1990-06-19 | 1991-12-26 | Sloan-Kettering Institute For Cancer Research | 5'-hydrogenphosphonates and 5'-methylphosphonates of sugar modified nucleosides, compositions and uses thereof |
US5177064A (en) * | 1990-07-13 | 1993-01-05 | University Of Florida | Targeted drug delivery via phosphonate derivatives |
JP2005525358A (ja) * | 2002-02-28 | 2005-08-25 | ビオタ インコーポレーティッド | ヌクレオチド模倣体およびそのプロドラッグ |
-
2004
- 2004-11-25 RU RU2004134388/04A patent/RU2322450C2/ru not_active Application Discontinuation
-
2005
- 2005-05-06 KR KR1020077013688A patent/KR101323698B1/ko not_active IP Right Cessation
- 2005-05-06 WO PCT/RU2005/000249 patent/WO2006062434A1/ru active Application Filing
- 2005-05-06 ES ES05763842.1T patent/ES2550136T3/es active Active
- 2005-05-06 CN CN2005800467450A patent/CN101115765B/zh not_active Expired - Fee Related
- 2005-05-06 EP EP05763842.1A patent/EP1829885B1/en not_active Expired - Fee Related
- 2005-05-06 US US11/720,250 patent/US7999099B2/en not_active Expired - Fee Related
Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN104114570A (zh) * | 2011-10-14 | 2014-10-22 | 齐多夫定生产和商业协会封闭式股份公司 | 作为人免疫缺陷病毒hiv-1产生的选择性抑制剂的氨基甲酰基膦酸酯盐 |
CN104114570B (zh) * | 2011-10-14 | 2016-08-31 | 齐多夫定生产和商业协会封闭式股份公司 | 作为人免疫缺陷病毒hiv-1产生的选择性抑制剂的氨基甲酰基膦酸酯盐 |
Also Published As
Publication number | Publication date |
---|---|
RU2322450C2 (ru) | 2008-04-20 |
WO2006062434A1 (en) | 2006-06-15 |
EP1829885A4 (en) | 2013-07-10 |
EP1829885B1 (en) | 2015-07-15 |
US7999099B2 (en) | 2011-08-16 |
RU2004134388A (ru) | 2006-05-20 |
EP1829885A1 (en) | 2007-09-05 |
US20090111979A1 (en) | 2009-04-30 |
WO2006062434A8 (fr) | 2007-11-01 |
KR20070116580A (ko) | 2007-12-10 |
ES2550136T3 (es) | 2015-11-04 |
CN101115765B (zh) | 2012-10-10 |
KR101323698B1 (ko) | 2013-10-30 |
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Legal Events
Date | Code | Title | Description |
---|---|---|---|
C06 | Publication | ||
PB01 | Publication | ||
C10 | Entry into substantive examination | ||
SE01 | Entry into force of request for substantive examination | ||
C14 | Grant of patent or utility model | ||
GR01 | Patent grant | ||
ASS | Succession or assignment of patent right |
Owner name: CONONOV ALEXANDER VASILYEVICH Effective date: 20140414 Owner name: KHOKHLOV ALEKSANDER FEDOROVICH Free format text: FORMER OWNER: KONSTANTINOVN KUKHANOVA MARINA Effective date: 20140414 |
|
C41 | Transfer of patent application or patent right or utility model | ||
TR01 | Transfer of patent right |
Effective date of registration: 20140414 Address after: Russian Federation Moscow Patentee after: Khokhlov Alexander Fedorowicz Patentee after: Cononov Alexander Vasilyevich Address before: Russian Federation Moscow Patentee before: Kukhanova Marina Konstantinovn |
|
CF01 | Termination of patent right due to non-payment of annual fee |
Granted publication date: 20121010 Termination date: 20150506 |
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EXPY | Termination of patent right or utility model |