JP2016028085A5 - - Google Patents
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- Publication number
- JP2016028085A5 JP2016028085A5 JP2015182821A JP2015182821A JP2016028085A5 JP 2016028085 A5 JP2016028085 A5 JP 2016028085A5 JP 2015182821 A JP2015182821 A JP 2015182821A JP 2015182821 A JP2015182821 A JP 2015182821A JP 2016028085 A5 JP2016028085 A5 JP 2016028085A5
- Authority
- JP
- Japan
- Prior art keywords
- water
- darunavir hydrate
- crystalline
- hydrate
- darunavir
- 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
- JKQULTRRXSDLJN-VBTXLZOXSA-N [(3as,4r,6ar)-2,3,3a,4,5,6a-hexahydrofuro[2,3-b]furan-4-yl] n-[(2s,3r)-4-[(4-aminophenyl)sulfonyl-(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]carbamate;hydrate Chemical compound O.C([C@@H]([C@H](O)CN(CC(C)C)S(=O)(=O)C=1C=CC(N)=CC=1)NC(=O)O[C@@H]1[C@@H]2CCO[C@@H]2OC1)C1=CC=CC=C1 JKQULTRRXSDLJN-VBTXLZOXSA-N 0.000 claims 13
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims 6
- 238000004519 manufacturing process Methods 0.000 claims 6
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 5
- 239000000203 mixture Substances 0.000 claims 4
- 239000007787 solid Substances 0.000 claims 4
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 3
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 claims 3
- YXFVVABEGXRONW-UHFFFAOYSA-N Toluene Chemical compound CC1=CC=CC=C1 YXFVVABEGXRONW-UHFFFAOYSA-N 0.000 claims 3
- ZMANZCXQSJIPKH-UHFFFAOYSA-N Triethylamine Chemical compound CCN(CC)CC ZMANZCXQSJIPKH-UHFFFAOYSA-N 0.000 claims 3
- 239000002904 solvent Substances 0.000 claims 3
- 238000003756 stirring Methods 0.000 claims 3
- YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 claims 2
- 208000031886 HIV Infections Diseases 0.000 claims 2
- 208000037357 HIV infectious disease Diseases 0.000 claims 2
- WYURNTSHIVDZCO-UHFFFAOYSA-N Tetrahydrofuran Chemical compound C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 claims 2
- 238000002441 X-ray diffraction Methods 0.000 claims 2
- 239000003125 aqueous solvent Substances 0.000 claims 2
- 238000001035 drying Methods 0.000 claims 2
- 238000001914 filtration Methods 0.000 claims 2
- 208000033519 human immunodeficiency virus infectious disease Diseases 0.000 claims 2
- KBPYLZJQXANQPM-WLUDYRNVSA-N [(3aS,4R,6aR)-2,3,3a,4,5,6a-hexahydrofuro[2,3-b]furan-4-yl] hydrogen carbonate 1-methylpyrrolidine-2,5-dione Chemical compound CN1C(=O)CCC1=O.O1CC[C@H]2[C@@H](OC(=O)O)CO[C@H]21 KBPYLZJQXANQPM-WLUDYRNVSA-N 0.000 claims 1
- 239000013078 crystal Substances 0.000 claims 1
- CJBJHOAVZSMMDJ-HEXNFIEUSA-N darunavir Chemical compound C([C@@H]([C@H](O)CN(CC(C)C)S(=O)(=O)C=1C=CC(N)=CC=1)NC(=O)O[C@@H]1[C@@H]2CCO[C@@H]2OC1)C1=CC=CC=C1 CJBJHOAVZSMMDJ-HEXNFIEUSA-N 0.000 claims 1
- 229960005107 darunavir Drugs 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
- YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IN33MU2010 | 2010-01-05 | ||
| IN33/MUM/2010 | 2010-01-05 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012546497A Division JP2013516397A (ja) | 2010-01-05 | 2010-10-06 | ダルナビルの多形及びその製造方法 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2016028085A JP2016028085A (ja) | 2016-02-25 |
| JP2016028085A5 true JP2016028085A5 (enExample) | 2016-04-07 |
Family
ID=43125640
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012546497A Pending JP2013516397A (ja) | 2010-01-05 | 2010-10-06 | ダルナビルの多形及びその製造方法 |
| JP2015182821A Pending JP2016028085A (ja) | 2010-01-05 | 2015-09-16 | ダルナビルの多形及びその製造方法 |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012546497A Pending JP2013516397A (ja) | 2010-01-05 | 2010-10-06 | ダルナビルの多形及びその製造方法 |
Country Status (9)
| Country | Link |
|---|---|
| US (2) | US20130029945A1 (enExample) |
| EP (1) | EP2521728B1 (enExample) |
| JP (2) | JP2013516397A (enExample) |
| KR (1) | KR20120123077A (enExample) |
| AU (1) | AU2010340799B2 (enExample) |
| CA (1) | CA2785998A1 (enExample) |
| NZ (1) | NZ600994A (enExample) |
| WO (1) | WO2011083287A2 (enExample) |
| ZA (1) | ZA201204365B (enExample) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2767539B1 (en) | 2002-05-16 | 2017-07-12 | Janssen Sciences Ireland UC | Pseudopolymorphic forms of a HIV protease inhibitor |
| US8921415B2 (en) | 2009-01-29 | 2014-12-30 | Mapi Pharma Ltd. | Polymorphs of darunavir |
| CN102725295A (zh) | 2010-01-28 | 2012-10-10 | Mapi医药公司 | 制备达芦那韦和达芦那韦中间体的方法 |
| US9216990B2 (en) * | 2011-12-05 | 2015-12-22 | Mylan Labs Limited | Crystalline Darunavir |
| CN103509031B (zh) * | 2012-06-20 | 2016-04-27 | 上海迪赛诺药业有限公司 | 制备达芦那韦无定形物的方法 |
| ES2969589T3 (es) | 2012-07-24 | 2024-05-21 | Laurus Labs Ltd | Solvato de Propionato de Darunavir |
| WO2016092525A1 (en) | 2014-12-12 | 2016-06-16 | Lupin Limited | Darunavir n-propanol solvate and process for preparation thereof |
| CN106854212A (zh) * | 2015-12-08 | 2017-06-16 | 浙江九洲药业股份有限公司 | 一种达芦那韦无定型的制备方法 |
| CN106242307A (zh) * | 2016-08-11 | 2016-12-21 | 京东方科技集团股份有限公司 | 用于强化制品的边缘的方法、玻璃及显示装置 |
| EP3532478B1 (en) | 2016-10-27 | 2021-05-26 | Gilead Sciences, Inc. | Crystalline form of darunavir free base |
| CN108727401A (zh) * | 2017-04-20 | 2018-11-02 | 盐城迪赛诺制药有限公司 | 达鲁那韦新晶型及其制备方法和应用 |
| CN108794498A (zh) * | 2017-05-03 | 2018-11-13 | 江苏瑞科医药科技有限公司 | 一种达芦那韦无定型的制备方法 |
| CN109053753A (zh) * | 2018-08-05 | 2018-12-21 | 浙江大学 | 一种制备达卢那韦二水合物晶型的方法 |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU7669794A (en) | 1993-08-24 | 1995-03-21 | G.D. Searle & Co. | Hydroxyethylamino sulphonamides useful as retroviral protease inhibitors |
| ES2604662T3 (es) | 1998-06-23 | 2017-03-08 | The United States Of America, Represented By The Secretary, Department Of Health And Human Services | Ensayo de acondicionamiento físico y métodos para reducir la resistencia del VIH a la terapia |
| EP2767539B1 (en) | 2002-05-16 | 2017-07-12 | Janssen Sciences Ireland UC | Pseudopolymorphic forms of a HIV protease inhibitor |
| HRP20090488T1 (hr) | 2003-12-23 | 2009-10-31 | Tibotec Pharmaceuticals Ltd. | Postupak za pripravu (3r,3as,6ar)-heksahidrofuro[2,3-b]furan-3-il(1s,23)-3-[[(4-aminofenil)sulfonil](izobutil)amino]-1-benzil-2-hidroksipropilkarbamata |
| US8703980B2 (en) * | 2009-09-17 | 2014-04-22 | Siva Rama Prasad Vellanki | Process for the preparation of darunavir |
| CN102686594A (zh) * | 2009-12-16 | 2012-09-19 | 熙德隆研究基金会 | 地瑞那韦的多晶型物 |
-
2010
- 2010-10-06 US US13/519,817 patent/US20130029945A1/en not_active Abandoned
- 2010-10-06 KR KR1020127020434A patent/KR20120123077A/ko not_active Ceased
- 2010-10-06 CA CA2785998A patent/CA2785998A1/en not_active Abandoned
- 2010-10-06 JP JP2012546497A patent/JP2013516397A/ja active Pending
- 2010-10-06 AU AU2010340799A patent/AU2010340799B2/en not_active Ceased
- 2010-10-06 EP EP10765473.3A patent/EP2521728B1/en not_active Not-in-force
- 2010-10-06 WO PCT/GB2010/001874 patent/WO2011083287A2/en not_active Ceased
- 2010-10-06 NZ NZ600994A patent/NZ600994A/en not_active IP Right Cessation
-
2012
- 2012-06-14 ZA ZA2012/04365A patent/ZA201204365B/en unknown
-
2015
- 2015-01-30 US US14/610,349 patent/US20150141383A1/en not_active Abandoned
- 2015-09-16 JP JP2015182821A patent/JP2016028085A/ja active Pending
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