JP2016507569A5 - - Google Patents
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- Publication number
- JP2016507569A5 JP2016507569A5 JP2015557055A JP2015557055A JP2016507569A5 JP 2016507569 A5 JP2016507569 A5 JP 2016507569A5 JP 2015557055 A JP2015557055 A JP 2015557055A JP 2015557055 A JP2015557055 A JP 2015557055A JP 2016507569 A5 JP2016507569 A5 JP 2016507569A5
- Authority
- JP
- Japan
- Prior art keywords
- lamivudine
- crystalline
- item
- ray powder
- powder diffraction
- 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
- JTEGQNOMFQHVDC-NKWVEPMBSA-N lamivudine Chemical compound O=C1N=C(N)C=CN1[C@H]1O[C@@H](CO)SC1 JTEGQNOMFQHVDC-NKWVEPMBSA-N 0.000 claims description 118
- 229960001627 lamivudine Drugs 0.000 claims description 107
- LEPNDALFXHAENA-UOERWJHTSA-N 4-amino-1-[(2r,5s)-2-(hydroxymethyl)-1,3-oxathiolan-5-yl]pyrimidin-2-one;hydrochloride Chemical compound Cl.O=C1N=C(N)C=CN1[C@H]1O[C@@H](CO)SC1 LEPNDALFXHAENA-UOERWJHTSA-N 0.000 claims description 75
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 claims description 62
- 238000000634 powder X-ray diffraction Methods 0.000 claims description 57
- 239000000725 suspension Substances 0.000 claims description 30
- 229910019142 PO4 Inorganic materials 0.000 claims description 29
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 claims description 29
- 239000010452 phosphate Substances 0.000 claims description 29
- 238000000034 method Methods 0.000 claims description 27
- 238000001816 cooling Methods 0.000 claims description 26
- 238000010438 heat treatment Methods 0.000 claims description 26
- 238000001237 Raman spectrum Methods 0.000 claims description 16
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims description 15
- 238000000113 differential scanning calorimetry Methods 0.000 claims description 15
- 238000001757 thermogravimetry curve Methods 0.000 claims description 15
- 239000002904 solvent Substances 0.000 claims description 12
- 239000008194 pharmaceutical composition Substances 0.000 claims description 11
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 claims description 10
- 238000004519 manufacturing process Methods 0.000 claims description 9
- QAOWNCQODCNURD-UHFFFAOYSA-N Sulfuric acid Chemical compound OS(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-N 0.000 claims description 8
- 239000013078 crystal Substances 0.000 claims description 5
- 229910000147 aluminium phosphate Inorganic materials 0.000 claims description 4
- 208000031886 HIV Infections Diseases 0.000 claims description 2
- 208000037357 HIV infectious disease Diseases 0.000 claims description 2
- 206010038997 Retroviral infections Diseases 0.000 claims description 2
- VFNGKCDDZUSWLR-UHFFFAOYSA-L disulfate(2-) Chemical compound [O-]S(=O)(=O)OS([O-])(=O)=O VFNGKCDDZUSWLR-UHFFFAOYSA-L 0.000 claims description 2
- 208000002672 hepatitis B Diseases 0.000 claims description 2
- 208000033519 human immunodeficiency virus infectious disease Diseases 0.000 claims description 2
- 239000004615 ingredient Substances 0.000 claims description 2
- 238000001179 sorption measurement Methods 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims 6
- 239000012453 solvate Substances 0.000 claims 1
- 230000004584 weight gain Effects 0.000 claims 1
- 235000019786 weight gain Nutrition 0.000 claims 1
- 235000011007 phosphoric acid Nutrition 0.000 description 3
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361762018P | 2013-02-07 | 2013-02-07 | |
| US61/762,018 | 2013-02-07 | ||
| PCT/US2014/015024 WO2014124092A2 (en) | 2013-02-07 | 2014-02-06 | Lamivudine salts |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2016507569A JP2016507569A (ja) | 2016-03-10 |
| JP2016507569A5 true JP2016507569A5 (enExample) | 2017-01-19 |
Family
ID=50151399
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015557055A Pending JP2016507569A (ja) | 2013-02-07 | 2014-02-06 | ラミブジン結晶塩 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US9688666B2 (enExample) |
| EP (1) | EP2953945A2 (enExample) |
| JP (1) | JP2016507569A (enExample) |
| CA (1) | CA2898092A1 (enExample) |
| WO (1) | WO2014124092A2 (enExample) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2898092A1 (en) | 2013-02-07 | 2014-08-14 | Tobira Therapeutics, Inc. | Lamivudine salts |
Family Cites Families (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6288033B1 (en) * | 1998-09-25 | 2001-09-11 | Sciclone Pharmaceuticals, Inc. | Treatment of hepatitis B infection with thymosin alpha 1 in combination with lamivudine or in combination with lamivudine and famciclovir |
| CN1406233A (zh) * | 2000-02-28 | 2003-03-26 | 拜尔公司 | 用于病毒性疾病的药物 |
| CA2351049C (en) * | 2001-06-18 | 2007-03-13 | Brantford Chemicals Inc. | Process for recovery of the desired cis-1,3-oxathiolane nucleosides from their undesired trans-isomers |
| ES2547002T3 (es) * | 2002-09-13 | 2015-09-30 | Novartis Ag | Beta-L-2' desoxinucleósidos para el tratamiento de cepas de VHB resistentes |
| AU2003277208A1 (en) * | 2002-10-01 | 2004-04-23 | Georgetown University | Diagnostic for long term response of hbv carrier to 3tc therapy |
| CN1517347A (zh) * | 2003-01-16 | 2004-08-04 | 北京昭衍新药研究中心 | 抗病毒核苷衍生物 |
| TWI332402B (en) * | 2003-12-19 | 2010-11-01 | Ind Tech Res Inst | An extract for treating hepatitis |
| ATE485292T1 (de) * | 2006-04-18 | 2010-11-15 | Lupin Ltd | Neue kristalline form von lamivudin |
| KR20080086687A (ko) * | 2007-03-23 | 2008-09-26 | 주식회사 파나진 | 라미부딘 내성 ｂ형 간염바이러스 검출을 위한 ρνα프로브, 키트 및 방법 |
| WO2009031026A2 (en) * | 2007-09-06 | 2009-03-12 | Combino Pharm, S.L. | Novel pharmaceutical compositions |
| WO2009037538A2 (en) * | 2007-09-17 | 2009-03-26 | Aurobindo Pharma Ltd | Process for the preparation of lamivudine form i |
| WO2009069013A1 (en) * | 2007-11-29 | 2009-06-04 | Ranbaxy Laboratories Limited | Crystalline form i of lamivudine and its preparation |
| WO2010023676A2 (en) * | 2008-09-01 | 2010-03-04 | Hetero Research Foundation | Process for preparing lamivudine polymorph form |
| US20110282046A1 (en) | 2009-01-19 | 2011-11-17 | Rama Shankar | Process for preparation of cis-nucleoside derivative |
| WO2010137027A1 (en) * | 2009-05-27 | 2010-12-02 | Hetero Research Foundation | Solid oral dosage forms of lamivudine |
| BRPI0903664B8 (pt) * | 2009-09-22 | 2021-05-25 | Fund De Amparo A Pesquisa Do Estado De Sao Paulo Fapesp | método de obtenção de nova forma cristalina de lamivudina, seu sal cloridrato monoidratado, formulações farmacêuticas e seus usos |
| KR101961601B1 (ko) * | 2009-11-16 | 2019-03-25 | 유니버시티 오브 조지아 리서치 파운데이션, 인코포레이티드 | 바이러스 감염 치료를 위한 ２＇―플루오로―６＇―메틸렌 카보사이클릭 뉴클레오사이드 및 방법 |
| US9700560B2 (en) * | 2009-11-16 | 2017-07-11 | University Of Georgia Research Foundation, Inc. | 2′-fluoro-6′-methylene carbocyclic nucleosides and methods of treating viral infections |
| US8816074B2 (en) * | 2009-11-16 | 2014-08-26 | University of Georgia Foundation, Inc. | 2′-fluoro-6′-methylene carbocyclic nucleosides and methods of treating viral infections |
| US8796452B2 (en) * | 2010-02-12 | 2014-08-05 | Merck Sharp & Dohme Corp. | Preparation of lamivudine form I |
| CN102167696B (zh) * | 2010-02-25 | 2013-09-18 | 南京正大天晴制药有限公司 | 拉米夫定草酸盐及其制备方法 |
| CN103282369A (zh) | 2011-04-08 | 2013-09-04 | 劳乐斯实验室私营有限公司 | 抗逆转录病毒化合物与抗氧化酸的固体形式、其制备方法以及其药物组合物 |
| CN102225069B (zh) * | 2011-04-29 | 2013-05-08 | 陶珍珠 | 一种耐药性显著降低的药物组合物及其制备方法和其应用 |
| CA2835272A1 (en) * | 2011-05-30 | 2012-12-06 | Cipla Limited | Pharmaceutical antiretroviral composition |
| JP2015509524A (ja) * | 2012-03-05 | 2015-03-30 | シプラ・リミテッド | ラミブジン、フェスティナビルおよびネビラピンを含んでなる抗レトロウイルス医薬組成物 |
| CA2898092A1 (en) * | 2013-02-07 | 2014-08-14 | Tobira Therapeutics, Inc. | Lamivudine salts |
-
2014
- 2014-02-06 CA CA2898092A patent/CA2898092A1/en not_active Abandoned
- 2014-02-06 EP EP14705933.1A patent/EP2953945A2/en not_active Withdrawn
- 2014-02-06 US US14/766,563 patent/US9688666B2/en not_active Expired - Fee Related
- 2014-02-06 JP JP2015557055A patent/JP2016507569A/ja active Pending
- 2014-02-06 WO PCT/US2014/015024 patent/WO2014124092A2/en not_active Ceased