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 (cg-RX-API-DMAC7.html) | 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 (cg-RX-API-DMAC7.html) |
| EP (1) | EP2953945A2 (cg-RX-API-DMAC7.html) |
| JP (1) | JP2016507569A (cg-RX-API-DMAC7.html) |
| CA (1) | CA2898092A1 (cg-RX-API-DMAC7.html) |
| WO (1) | WO2014124092A2 (cg-RX-API-DMAC7.html) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2953945A2 (en) | 2013-02-07 | 2015-12-16 | 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 |
| US20030187028A1 (en) * | 2000-02-28 | 2003-10-02 | Michael Brands | Medicament for viral diseases |
| 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 |
| US7186700B2 (en) * | 2002-09-13 | 2007-03-06 | Idenix Pharmaceuticals, Inc. | β-L-2′-deoxynucleosides for the treatment of resistant HBV strains and combination therapies |
| WO2004031729A2 (en) * | 2002-10-01 | 2004-04-15 | 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 |
| DE602007009957D1 (de) * | 2006-04-18 | 2010-12-02 | 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 |
| AR068374A1 (es) * | 2007-09-06 | 2009-11-11 | Combino Pharm Sl | Nuevas composiciones farmaceuticas del complejo lamivudina beta - ciclodextrina |
| WO2009037538A2 (en) * | 2007-09-17 | 2009-03-26 | Aurobindo Pharma Ltd | Process for the preparation of lamivudine form i |
| BRPI0820222A2 (pt) * | 2007-11-29 | 2015-06-16 | Ranbaxy Lab Ltd | Forma i cristalina estável de lamivudina e processo de preparação |
| WO2010023676A2 (en) * | 2008-09-01 | 2010-03-04 | Hetero Research Foundation | Process for preparing lamivudine polymorph form |
| WO2010082128A1 (en) | 2009-01-19 | 2010-07-22 | Aurobindo Pharma Limited | Process for the preparation of cis-nucleoside derivative |
| EP2435052B1 (en) * | 2009-05-27 | 2015-07-15 | Hetero Research Foundation | Solid oral dosage forms of lamivudine with isomalt |
| 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 |
| 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 |
| 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 |
| CA2781054A1 (en) * | 2009-11-16 | 2011-05-19 | Chung K. Chu | 2'-fluoro-6'-methylene carbocyclic nucleosides and methods of treating viral infections |
| AU2011215878A1 (en) * | 2010-02-12 | 2012-08-09 | 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 |
| EP2697238B1 (en) | 2011-04-08 | 2019-03-20 | Laurus Labs Limited | Solid forms of antiretroviral compounds, process for the preparation and their pharmaceutical composition thereof |
| 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 |
| AU2012264475A1 (en) * | 2011-05-30 | 2013-10-31 | Cipla Limited | Pharmaceutical antiretroviral composition |
| BR112014021927A2 (pt) * | 2012-03-05 | 2019-09-24 | Cipla Ltd | composição farmacêutica antirretroviral, processo para preparar uma composição farmacêutica antirretroviral, método para o tratamento ou profilaxia de doenças causadas por retrovírus, e, uso de lamivudina, festinavir e nevirapina |
| EP2953945A2 (en) * | 2013-02-07 | 2015-12-16 | Tobira Therapeutics, Inc. | Lamivudine salts |
-
2014
- 2014-02-06 EP EP14705933.1A patent/EP2953945A2/en not_active Withdrawn
- 2014-02-06 JP JP2015557055A patent/JP2016507569A/ja active Pending
- 2014-02-06 US US14/766,563 patent/US9688666B2/en not_active Expired - Fee Related
- 2014-02-06 CA CA2898092A patent/CA2898092A1/en not_active Abandoned
- 2014-02-06 WO PCT/US2014/015024 patent/WO2014124092A2/en not_active Ceased