JP2011515491A5 - - Google Patents
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- Publication number
- JP2011515491A5 JP2011515491A5 JP2011502043A JP2011502043A JP2011515491A5 JP 2011515491 A5 JP2011515491 A5 JP 2011515491A5 JP 2011502043 A JP2011502043 A JP 2011502043A JP 2011502043 A JP2011502043 A JP 2011502043A JP 2011515491 A5 JP2011515491 A5 JP 2011515491A5
- Authority
- JP
- Japan
- Prior art keywords
- inhibitors
- hiv
- crystalline form
- ray diffraction
- compound
- 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.)
- Pending
Links
- 239000003112 inhibitor Substances 0.000 claims 10
- 230000002401 inhibitory effect Effects 0.000 claims 10
- 102000015084 HIV Reverse Transcriptase Human genes 0.000 claims 4
- 108010078851 HIV Reverse Transcriptase Proteins 0.000 claims 4
- 241000580858 Simian-Human immunodeficiency virus Species 0.000 claims 4
- 239000003795 chemical substances by application Substances 0.000 claims 4
- 150000001875 compounds Chemical class 0.000 claims 4
- 239000002777 nucleoside Substances 0.000 claims 4
- 150000003833 nucleoside derivatives Chemical class 0.000 claims 4
- 238000000634 powder X-ray diffraction Methods 0.000 claims 4
- 239000003419 rna directed dna polymerase inhibitor Substances 0.000 claims 4
- 208000005721 HIV Infections Diseases 0.000 claims 3
- 201000001820 human immunodeficiency virus infectious disease Diseases 0.000 claims 3
- 206010000565 Acquired immunodeficiency syndrome Diseases 0.000 claims 2
- 102100012080 CCR5 Human genes 0.000 claims 2
- 101700043583 CCR5 Proteins 0.000 claims 2
- 102100002212 CXCR4 Human genes 0.000 claims 2
- 101710003734 CXCR4 Proteins 0.000 claims 2
- 102000000642 HIV Integrase Human genes 0.000 claims 2
- 108010002459 HIV Integrase Proteins 0.000 claims 2
- 230000034303 cell budding Effects 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 239000002835 hiv fusion inhibitor Substances 0.000 claims 2
- 239000004030 hiv protease inhibitor Substances 0.000 claims 2
- 230000035800 maturation Effects 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 238000005259 measurement Methods 0.000 claims 1
- 238000002844 melting Methods 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 238000001757 thermogravimetry curve Methods 0.000 claims 1
- 230000004580 weight loss Effects 0.000 claims 1
- GNUKHSNJBQGSGJ-UHFFFAOYSA-N CC(C)(C1=NC(C(NCc(c(-[n]2ncnc2C)c2)ccc2F)=O)=C2[N+]([O-])=C=C)OCCN1C2=O Chemical compound CC(C)(C1=NC(C(NCc(c(-[n]2ncnc2C)c2)ccc2F)=O)=C2[N+]([O-])=C=C)OCCN1C2=O GNUKHSNJBQGSGJ-UHFFFAOYSA-N 0.000 description 1
Claims (11)
- ａ）結晶形の粉末Ｘ線回折パターンの測定が約２５℃の温度において、３.３±０.２；６.７±０.２；１０.０±０.２；１１.８±０.２；１３.３±０.２；１４.７±０.２；１５.８±０.２；１６.６±０.２；２１.２±０.２；および２２.１±０.２から選択される５つ以上の２θ値（ＣｕＫα λ＝１.５４１８Å）を含む粉末Ｘ線回折パターン；
ｂ）結晶形の単位格子パラメータの測定が約２５℃の温度において、下表：
に実質的に等しい単位格子パラメータ；
ｃ）約２９８℃の範囲の融点；および／または
ｄ）約２１０℃の温度に加熱して、約３.９〜約４.４重量％の範囲で重量減少を有する熱重量分析サーモグラム；
の特徴を有するＨ−１型を含む、化合物（Ｉ）：
の結晶形。 - 実質的に図１に示されたシミュレーションされた粉末Ｘ線回折パターン；および／または実質的に図１に示された観測された粉末Ｘ線回折パターンの特徴を有するＨ−１型を含む、化合物（Ｉ）：
の結晶形。 - 本質的に前記Ｈ−１型からなる、請求項１または２の結晶形。
- 実質的に純粋である、請求項１または２の結晶形。
- 少なくとも約９０重量％の前記結晶形がＨ−１型で構成されている、請求項１または２の結晶形。
- 化合物（Ｉ）：
の結晶形Ｈ−１、並びに少なくとも１つの医薬的に許容される担体および／または希釈剤を含む医薬組成物。 - 前記結晶形が実質的に純粋な形態である、請求項６の医薬組成物。
- ヌクレオシドＨＩＶ逆転写酵素阻害剤、非ヌクレオシドＨＩＶ逆転写酵素阻害剤、ＨＩＶプロテアーゼ阻害剤、ＨＩＶ融合阻害剤、ＨＩＶ結合阻害剤、ＣＣＲ５阻害剤、ＣＸＣＲ４阻害剤、ＨＩＶ出芽もしくは成熟阻害剤、およびＨＩＶインテグラーゼ阻害剤からなる群から選択される、ＡＩＤＳまたはＨＩＶ感染の治療に用いられる治療有効量の少なくとも１つの他の薬剤、並びに医薬的に許容される担体をさらに含む、請求項６の組成物。
- 化合物（Ｉ）：
の結晶形Ｈ−１を含む、ＨＩＶ感染の治療剤。 - 該結晶形が実質的に純粋な形態である、請求項９の剤。
- ヌクレオシドＨＩＶ逆転写酵素阻害剤、非ヌクレオシドＨＩＶ逆転写酵素阻害剤、ＨＩＶプロテアーゼ阻害剤、ＨＩＶ融合阻害剤、ＨＩＶ結合阻害剤、ＣＣＲ５阻害剤、ＣＸＣＲ４阻害剤、ＨＩＶ出芽もしくは成熟阻害剤、およびＨＩＶインテグラーゼ阻害剤からなる群から選択される、ＡＩＤＳまたはＨＩＶ感染の治療に用いられる少なくとも１つの他の薬剤を含む、請求項９の剤。
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 |
|---|---|
| JP2011515491A JP2011515491A (ja) | 2011-05-19 |
| JP2011515491A5 true JP2011515491A5 (ja) | 2012-03-01 |
Family
ID=41008867
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011502043A Pending JP2011515491A (ja) | 2008-03-27 | 2009-03-26 | Ｎ−［［４−フルオロ−２−（５−メチル−１Ｈ−１，２，４−トリアゾール−１−イル）フェニル］メチル］−４，６，７，９−テトラヒドロ−３−ヒドロキシ−９，９−ジメチル−４−オキソ−ピリミド［２，１−ｃ］［１，４］オキサジン−２−カルボキシアミド，ナトリウム塩一水和物の結晶形 |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US7968541B2 (ja) |
| EP (1) | EP2280980B1 (ja) |
| JP (1) | JP2011515491A (ja) |
| KR (1) | KR20100138959A (ja) |
| CN (1) | CN102046637B (ja) |
| AU (1) | AU2009228254A1 (ja) |
| MX (1) | MX2010010244A (ja) |
| WO (1) | WO2009120841A1 (ja) |
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 |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20020048610A1 (en) * | 2000-01-07 | 2002-04-25 | Cima Michael J. | 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 |
| 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 |
| WO2007143446A1 (en) * | 2006-05-30 | 2007-12-13 | Bristol-Myers Squibb Company | Spiro-condensed heterotricyclic compounds as hiv integrase inhibitors |
-
2009
- 2009-03-26 CN CN2009801193916A patent/CN102046637B/zh not_active Expired - Fee Related
- 2009-03-26 MX MX2010010244A patent/MX2010010244A/es active IP Right Grant
- 2009-03-26 JP JP2011502043A patent/JP2011515491A/ja active Pending
- 2009-03-26 AU AU2009228254A patent/AU2009228254A1/en not_active Abandoned
- 2009-03-26 US US12/411,475 patent/US7968541B2/en not_active Expired - Fee Related
- 2009-03-26 KR KR1020107021250A patent/KR20100138959A/ko not_active Application Discontinuation
- 2009-03-26 WO PCT/US2009/038362 patent/WO2009120841A1/en active Application Filing
- 2009-03-26 EP EP09725033.6A patent/EP2280980B1/en not_active Not-in-force
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