JP2016534047A5 - - Google Patents
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- Publication number
- JP2016534047A5 JP2016534047A5 JP2016522025A JP2016522025A JP2016534047A5 JP 2016534047 A5 JP2016534047 A5 JP 2016534047A5 JP 2016522025 A JP2016522025 A JP 2016522025A JP 2016522025 A JP2016522025 A JP 2016522025A JP 2016534047 A5 JP2016534047 A5 JP 2016534047A5
- Authority
- JP
- Japan
- Prior art keywords
- tenofovir disoproxil
- dihydrogen phosphate
- solution
- added dropwise
- phosphoric acid
- 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.)
- Ceased
Links
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 claims description 16
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 claims description 12
- YXFVVABEGXRONW-UHFFFAOYSA-N Toluene Chemical compound CC1=CC=CC=C1 YXFVVABEGXRONW-UHFFFAOYSA-N 0.000 claims description 6
- 229910000147 aluminium phosphate Inorganic materials 0.000 claims description 6
- VCMJCVGFSROFHV-WZGZYPNHSA-N tenofovir disoproxil fumarate Chemical compound OC(=O)\C=C\C(O)=O.N1=CN=C2N(C[C@@H](C)OCP(=O)(OCOC(=O)OC(C)C)OCOC(=O)OC(C)C)C=NC2=C1N VCMJCVGFSROFHV-WZGZYPNHSA-N 0.000 claims description 6
- 229960001355 tenofovir disoproxil Drugs 0.000 claims description 5
- JFVZFKDSXNQEJW-CQSZACIVSA-N tenofovir disoproxil Chemical compound N1=CN=C2N(C[C@@H](C)OCP(=O)(OCOC(=O)OC(C)C)OCOC(=O)OC(C)C)C=NC2=C1N JFVZFKDSXNQEJW-CQSZACIVSA-N 0.000 claims description 5
- 229960004693 tenofovir disoproxil fumarate Drugs 0.000 claims description 5
- 238000001816 cooling Methods 0.000 claims description 4
- NBIIXXVUZAFLBC-UHFFFAOYSA-M dihydrogenphosphate Chemical compound OP(O)([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-M 0.000 claims description 4
- 239000007858 starting material Substances 0.000 claims description 3
- 238000004519 manufacturing process Methods 0.000 claims description 2
- 239000003960 organic solvent Substances 0.000 claims description 2
- 238000000034 method Methods 0.000 claims 2
- 239000011541 reaction mixture Substances 0.000 claims 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 1
- 229910019142 PO4 Inorganic materials 0.000 claims 1
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 claims 1
- 239000010452 phosphate Substances 0.000 claims 1
- 238000000634 powder X-ray diffraction Methods 0.000 claims 1
- -1 proxyl dihydrogen phosphate Chemical compound 0.000 claims 1
- 229960004556 tenofovir Drugs 0.000 claims 1
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 3
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 3
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 description 2
- LRHPLDYGYMQRHN-UHFFFAOYSA-N N-Butanol Chemical compound CCCCO LRHPLDYGYMQRHN-UHFFFAOYSA-N 0.000 description 2
- DJCLNKKHALBVLK-PFEQFJNWSA-N [[(2R)-1-(6-aminopurin-9-yl)propan-2-yl]oxymethyl-(propan-2-yloxycarbonyloxymethoxy)phosphoryl]oxymethyl propan-2-yl carbonate phosphoric acid Chemical compound OP(O)(O)=O.N1=CN=C2N(C[C@@H](C)OCP(=O)(OCOC(=O)OC(C)C)OCOC(=O)OC(C)C)C=NC2=C1N DJCLNKKHALBVLK-PFEQFJNWSA-N 0.000 description 2
- 239000013078 crystal Substances 0.000 description 2
- 238000004128 high performance liquid chromatography Methods 0.000 description 2
- 239000002245 particle Substances 0.000 description 2
- 239000000725 suspension Substances 0.000 description 2
- 229950010595 tenofovir disoproxil phosphate Drugs 0.000 description 2
- 150000001298 alcohols Chemical class 0.000 description 1
- 238000002425 crystallisation Methods 0.000 description 1
- 230000008025 crystallization Effects 0.000 description 1
- 238000009826 distribution Methods 0.000 description 1
- 239000001530 fumaric acid Substances 0.000 description 1
- 238000002360 preparation method Methods 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP13004844.0A EP2860184B1 (en) | 2013-10-09 | 2013-10-09 | Dihydrogenphosphate salt of Tenofovir disoproxil |
| EP13004844.0 | 2013-10-09 | ||
| PCT/EP2014/002562 WO2015051875A1 (en) | 2013-10-09 | 2014-09-22 | Dihydrogenphosphate salt of tenofovir disoproxil |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2016534047A JP2016534047A (ja) | 2016-11-04 |
| JP2016534047A5 true JP2016534047A5 (enExample) | 2018-12-13 |
Family
ID=49354420
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016522025A Ceased JP2016534047A (ja) | 2013-10-09 | 2014-09-22 | テノホビルジソプロキシルの二水素リン酸塩 |
Country Status (10)
| Country | Link |
|---|---|
| EP (1) | EP2860184B1 (enExample) |
| JP (1) | JP2016534047A (enExample) |
| KR (1) | KR20160067843A (enExample) |
| CN (1) | CN105612167A (enExample) |
| BR (1) | BR112016007617A2 (enExample) |
| EA (1) | EA201690622A1 (enExample) |
| IL (1) | IL244848A0 (enExample) |
| MX (1) | MX2016003757A (enExample) |
| PT (1) | PT2860184T (enExample) |
| WO (1) | WO2015051875A1 (enExample) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20160003532A (ko) * | 2014-07-01 | 2016-01-11 | 한미약품 주식회사 | 테노포비어 디소프록실 인산염과, 비금속염 붕해제 및 비금속염 활택제를 포함하는 약학 조성물 |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1998004569A1 (en) | 1996-07-26 | 1998-02-05 | Gilead Sciences, Inc. | Nucleotide analogs |
| PT915894E (pt) | 1996-07-26 | 2003-10-31 | Gilead Sciences Inc | Analogos de nucleotidos |
| US5935946A (en) | 1997-07-25 | 1999-08-10 | Gilead Sciences, Inc. | Nucleotide analog composition and synthesis method |
| ATE305009T1 (de) | 1997-07-25 | 2005-10-15 | Gilead Sciences Inc | Nukleotid-analog zusamensetzung und synthese verfahren |
| WO2007013086A1 (en) | 2005-07-26 | 2007-02-01 | Hetero Drugs Limited | Novel polymorphs of tenofovir disoproxil fumarate |
| WO2008007392A2 (en) | 2006-07-12 | 2008-01-17 | Matrix Laboratories Limited | Process for the preparation of tenofovir |
| WO2008140302A1 (en) | 2007-05-14 | 2008-11-20 | Ultimorphix Technologies B.V. | Polymorphic forms of tenofovir disoproxil fumarate |
| WO2008143500A1 (en) | 2007-05-22 | 2008-11-27 | Ultimorphix Technologies B.V. | Tenofovir disoproxil hemi-fumaric acid co-crystal |
| WO2009064174A1 (en) | 2007-11-14 | 2009-05-22 | Ultimorphix Technologies B.V. | Polymorphic form of tenofovir disoproxil fumarate, method for its preparation and use |
| EP2220098A2 (en) * | 2007-12-12 | 2010-08-25 | Ultimorphix Technologies B.v. | Solid forms of tenofovir disoproxil |
| NZ588796A (en) * | 2008-04-25 | 2012-07-27 | Cipla Ltd | Crystalline form of tenofovir disoproxil and a process for its preparation |
| WO2010142761A1 (en) | 2009-06-10 | 2010-12-16 | Ultimorphix Technologies B.V. | The succinate of tenofovir disoproxil |
| CN101781334B (zh) * | 2010-03-04 | 2012-11-28 | 福建广生堂药业股份有限公司 | 替诺福韦酯的盐化合物，其制备方法和药物应用 |
| 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 |
| WO2013132314A1 (en) * | 2012-03-05 | 2013-09-12 | Laurus Labs Private Limited | Tenofovir phosphate, processes for the preparation and pharmaceutical composition thereof |
-
2013
- 2013-10-09 PT PT13004844T patent/PT2860184T/pt unknown
- 2013-10-09 EP EP13004844.0A patent/EP2860184B1/en active Active
-
2014
- 2014-09-22 MX MX2016003757A patent/MX2016003757A/es unknown
- 2014-09-22 EA EA201690622A patent/EA201690622A1/ru unknown
- 2014-09-22 KR KR1020167007764A patent/KR20160067843A/ko not_active Withdrawn
- 2014-09-22 BR BR112016007617A patent/BR112016007617A2/pt not_active IP Right Cessation
- 2014-09-22 CN CN201480055828.5A patent/CN105612167A/zh active Pending
- 2014-09-22 JP JP2016522025A patent/JP2016534047A/ja not_active Ceased
- 2014-09-22 WO PCT/EP2014/002562 patent/WO2015051875A1/en not_active Ceased
-
2016
- 2016-03-31 IL IL244848A patent/IL244848A0/en unknown
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