CN102046637B - N-[[4-氟-2-(5-甲基-1H-1,2,4-三唑-1-基)苯基]甲基]-4,6,7,9-四氢-3-羟基-9,9-二甲基-4-氧代-嘧啶并[2,1-c][1,4]噁嗪-2-甲酰胺钠盐一水合物的晶体形式 - Google Patents
N-[[4-氟-2-(5-甲基-1H-1,2,4-三唑-1-基)苯基]甲基]-4,6,7,9-四氢-3-羟基-9,9-二甲基-4-氧代-嘧啶并[2,1-c][1,4]噁嗪-2-甲酰胺钠盐一水合物的晶体形式 Download PDFInfo
- Publication number
- CN102046637B CN102046637B CN2009801193916A CN200980119391A CN102046637B CN 102046637 B CN102046637 B CN 102046637B CN 2009801193916 A CN2009801193916 A CN 2009801193916A CN 200980119391 A CN200980119391 A CN 200980119391A CN 102046637 B CN102046637 B CN 102046637B
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- China
- Prior art keywords
- crystalline form
- hiv
- compound
- inhibitor
- weight
- 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.)
- Expired - Fee Related
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- 0 CC(C)(C1=NC(C(NCc(c(-[n]2ncnc2C)c2)ccc2F)=O)=C2*)OCCN1C2=O Chemical compound CC(C)(C1=NC(C(NCc(c(-[n]2ncnc2C)c2)ccc2F)=O)=C2*)OCCN1C2=O 0.000 description 3
- RZIWEYKLLAQSEL-UHFFFAOYSA-N CC(C)(C1=NC(C(NCc(c(-[n]2ncnc2C)c2)ccc2F)=O)=C2O)OCCN1C2=O Chemical compound CC(C)(C1=NC(C(NCc(c(-[n]2ncnc2C)c2)ccc2F)=O)=C2O)OCCN1C2=O RZIWEYKLLAQSEL-UHFFFAOYSA-N 0.000 description 1
- YSVHIGYKMAZUEF-UHFFFAOYSA-N CC[NH+](C1=C(C(NCc(c(-[n]2ncnc2C)c2)ccc2F)=O)N=C(C(C)(C)OCC2)N2C1=O)[O-] Chemical compound CC[NH+](C1=C(C(NCc(c(-[n]2ncnc2C)c2)ccc2F)=O)N=C(C(C)(C)OCC2)N2C1=O)[O-] YSVHIGYKMAZUEF-UHFFFAOYSA-N 0.000 description 1
Images
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
-
- 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
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- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Virology (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Oncology (AREA)
- Molecular Biology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Tropical Medicine & Parasitology (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- AIDS & HIV (AREA)
- Communicable Diseases (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US3998908P | 2008-03-27 | 2008-03-27 | |
| US61/039,989 | 2008-03-27 | ||
| PCT/US2009/038362 WO2009120841A1 (en) | 2008-03-27 | 2009-03-26 | Crystalline form of n-[[4-fluoro-2-(5-methyl-1h-1,2,4-triazol-1-yl)phenyl]methyl]-4,6,7,9-tetrahydro-3-hydroxy-9,9-dimethyl-4-oxo-pyrimido[2,1-c][1,4]oxazine-2-carboxamide, sodium salt monohydrate |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN102046637A CN102046637A (zh) | 2011-05-04 |
| CN102046637B true CN102046637B (zh) | 2013-10-02 |
Family
ID=41008867
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2009801193916A Expired - Fee Related CN102046637B (zh) | 2008-03-27 | 2009-03-26 | N-[[4-氟-2-(5-甲基-1H-1,2,4-三唑-1-基)苯基]甲基]-4,6,7,9-四氢-3-羟基-9,9-二甲基-4-氧代-嘧啶并[2,1-c][1,4]噁嗪-2-甲酰胺钠盐一水合物的晶体形式 |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US7968541B2 (enExample) |
| EP (1) | EP2280980B1 (enExample) |
| JP (1) | JP2011515491A (enExample) |
| KR (1) | KR20100138959A (enExample) |
| CN (1) | CN102046637B (enExample) |
| AU (1) | AU2009228254A1 (enExample) |
| MX (1) | MX2010010244A (enExample) |
| WO (1) | WO2009120841A1 (enExample) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106478661A (zh) * | 2015-08-25 | 2017-03-08 | 华北制药集团新药研究开发有限责任公司 | 苯并恶唑并恶嗪酮类化合物wa1-089的晶型e及其制备方法 |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7157447B2 (en) * | 2004-05-28 | 2007-01-02 | Bristol-Myers Squibb Company | Bicyclic heterocycles as HIV integrase inhibitors |
| WO2007064316A1 (en) * | 2005-11-30 | 2007-06-07 | Bristol-Myers Squibb Company | Bicyclic heterocycles as hiv integrase inhibitors |
| WO2007064502A1 (en) * | 2005-12-01 | 2007-06-07 | Bristol-Myers Squibb Company | Forms of n-[(4-fluorophenyl)methyl]-4,6,7,9-tetrahydro-3-hydroxy-9,9-dimethyl-4-oxo-pyrimido[2,1-c][1,4]oxazine-2-carboxamide |
| US20070281917A1 (en) * | 2006-05-30 | 2007-12-06 | Bristol-Myers Squibb Company | HIV Integrase Inhibitors |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SK9742002A3 (en) * | 2000-01-07 | 2003-02-04 | Transform Pharmaceuticals Inc | High-throughput formation, identification, and analysis of diverse solid-forms |
| US7176196B2 (en) * | 2004-05-28 | 2007-02-13 | Bristol-Myers Squibb Company | Bicyclic heterocycles as HIV integrase inhibitors |
-
2009
- 2009-03-26 AU AU2009228254A patent/AU2009228254A1/en not_active Abandoned
- 2009-03-26 KR KR1020107021250A patent/KR20100138959A/ko not_active Withdrawn
- 2009-03-26 EP EP09725033.6A patent/EP2280980B1/en not_active Not-in-force
- 2009-03-26 WO PCT/US2009/038362 patent/WO2009120841A1/en not_active Ceased
- 2009-03-26 CN CN2009801193916A patent/CN102046637B/zh not_active Expired - Fee Related
- 2009-03-26 JP JP2011502043A patent/JP2011515491A/ja active Pending
- 2009-03-26 MX MX2010010244A patent/MX2010010244A/es active IP Right Grant
- 2009-03-26 US US12/411,475 patent/US7968541B2/en not_active Expired - Fee Related
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7157447B2 (en) * | 2004-05-28 | 2007-01-02 | Bristol-Myers Squibb Company | Bicyclic heterocycles as HIV integrase inhibitors |
| WO2007064316A1 (en) * | 2005-11-30 | 2007-06-07 | Bristol-Myers Squibb Company | Bicyclic heterocycles as hiv integrase inhibitors |
| WO2007064502A1 (en) * | 2005-12-01 | 2007-06-07 | Bristol-Myers Squibb Company | Forms of n-[(4-fluorophenyl)methyl]-4,6,7,9-tetrahydro-3-hydroxy-9,9-dimethyl-4-oxo-pyrimido[2,1-c][1,4]oxazine-2-carboxamide |
| US20070281917A1 (en) * | 2006-05-30 | 2007-12-06 | Bristol-Myers Squibb Company | HIV Integrase Inhibitors |
Also Published As
| Publication number | Publication date |
|---|---|
| WO2009120841A1 (en) | 2009-10-01 |
| EP2280980A1 (en) | 2011-02-09 |
| MX2010010244A (es) | 2010-10-05 |
| JP2011515491A (ja) | 2011-05-19 |
| KR20100138959A (ko) | 2010-12-31 |
| AU2009228254A1 (en) | 2009-10-01 |
| US7968541B2 (en) | 2011-06-28 |
| US20090253692A1 (en) | 2009-10-08 |
| CN102046637A (zh) | 2011-05-04 |
| EP2280980B1 (en) | 2016-03-23 |
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| 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 | ||
| CF01 | Termination of patent right due to non-payment of annual fee | ||
| CF01 | Termination of patent right due to non-payment of annual fee |
Granted publication date: 20131002 Termination date: 20170326 |