NZ600994A - Darunavir polymorph and process for preparation thereof - Google Patents
Darunavir polymorph and process for preparation thereofInfo
- Publication number
- NZ600994A NZ600994A NZ600994A NZ60099410A NZ600994A NZ 600994 A NZ600994 A NZ 600994A NZ 600994 A NZ600994 A NZ 600994A NZ 60099410 A NZ60099410 A NZ 60099410A NZ 600994 A NZ600994 A NZ 600994A
- Authority
- NZ
- New Zealand
- Prior art keywords
- darunavir
- water
- solid
- mixture
- stirring
- Prior art date
Links
- 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 title abstract 3
- 229960005107 darunavir Drugs 0.000 title abstract 3
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 abstract 6
- 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 abstract 5
- 239000000203 mixture Substances 0.000 abstract 4
- 239000007787 solid Substances 0.000 abstract 4
- 238000004519 manufacturing process Methods 0.000 abstract 3
- 238000003756 stirring Methods 0.000 abstract 3
- 239000003125 aqueous solvent Substances 0.000 abstract 2
- 238000001035 drying Methods 0.000 abstract 2
- 238000001914 filtration Methods 0.000 abstract 2
- 239000002904 solvent Substances 0.000 abstract 2
- NUMJNKDUHFCFJO-UHFFFAOYSA-N 4-amino-n-(3-amino-2-hydroxy-4-phenylbutyl)-n-(2-methylpropyl)benzenesulfonamide Chemical compound C=1C=C(N)C=CC=1S(=O)(=O)N(CC(C)C)CC(O)C(N)CC1=CC=CC=C1 NUMJNKDUHFCFJO-UHFFFAOYSA-N 0.000 abstract 1
- VCFNCYVHQSHFRH-MHYGZLNHSA-N [(3as,4r,6ar)-2,3,3a,4,5,6a-hexahydrofuro[2,3-b]furan-4-yl] (2,5-dioxopyrrolidin-1-yl) carbonate Chemical compound O([C@@H]1[C@@H]2CCO[C@@H]2OC1)C(=O)ON1C(=O)CCC1=O VCFNCYVHQSHFRH-MHYGZLNHSA-N 0.000 abstract 1
- 239000013078 crystal Substances 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
- C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
- C07D493/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
- A61K31/341—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Virology (AREA)
- AIDS & HIV (AREA)
- Tropical Medicine & Parasitology (AREA)
- Molecular Biology (AREA)
- Engineering & Computer Science (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Emergency Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicinal Preparation (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IN33MU2010 | 2010-01-05 | ||
| PCT/GB2010/001874 WO2011083287A2 (en) | 2010-01-05 | 2010-10-06 | Darunavir polymorph and process for preparation thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| NZ600994A true NZ600994A (en) | 2014-04-30 |
Family
ID=43125640
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| NZ600994A NZ600994A (en) | 2010-01-05 | 2010-10-06 | Darunavir polymorph and process for preparation thereof |
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 |
|---|---|---|---|---|
| US7700645B2 (en) | 2002-05-16 | 2010-04-20 | Tibotec Pharmaceuticals Ltd. | Pseudopolymorphic forms of a HIV protease inhibitor |
| US8921415B2 (en) | 2009-01-29 | 2014-12-30 | Mapi Pharma Ltd. | Polymorphs of darunavir |
| PL2528923T3 (pl) | 2010-01-28 | 2015-01-30 | Mapi Pharma Ltd | Sposób wytwarzania darunawiru i pochodnych darunawiru |
| 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 |
| EP3795572B1 (en) | 2012-07-24 | 2023-11-15 | Laurus Labs Limited | Darunavir propionate solvate |
| 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 |
|---|---|---|---|---|
| ES2127938T3 (es) | 1993-08-24 | 1999-05-01 | Searle & Co | Hidroxietilamino sulfonamidas utiles como inhibidores de proteasas retroviricas. |
| PT2336134T (pt) | 1998-06-23 | 2016-10-19 | The Board Of Trustees Of The Univ Of Illionis | Ensaio de aptidão e métodos para reduzir a resistência do hiv à terapia |
| US7700645B2 (en) * | 2002-05-16 | 2010-04-20 | Tibotec Pharmaceuticals Ltd. | Pseudopolymorphic forms of a HIV protease inhibitor |
| KR101192859B1 (ko) | 2003-12-23 | 2012-10-19 | 얀센 알 앤드 디 아일랜드 | （3ｒ,3ａｓ,6ａｒ）-헥사하이드로푸로〔2,3-ｂ〕푸란-3-일（1ｓ,2ｒ）-3-〔〔（4-아미노페닐）설포닐〕（이소부틸）아미노〕-1-벤질-2-하이드록시프로필카바메이트의 제조방법 |
| CA2776807C (en) * | 2009-09-17 | 2018-10-16 | Mylan Laboratories Limited | An improved process for the preparation of darunavir |
| WO2011073993A1 (en) * | 2009-12-16 | 2011-06-23 | Hetero Research Foundation | Polymorphs of darunavir |
-
2010
- 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
- 2010-10-06 KR KR1020127020434A patent/KR20120123077A/ko not_active Ceased
- 2010-10-06 US US13/519,817 patent/US20130029945A1/en not_active Abandoned
- 2010-10-06 CA CA2785998A patent/CA2785998A1/en not_active Abandoned
- 2010-10-06 AU AU2010340799A patent/AU2010340799B2/en not_active Ceased
- 2010-10-06 JP JP2012546497A patent/JP2013516397A/ja active Pending
- 2010-10-06 EP EP10765473.3A patent/EP2521728B1/en not_active Not-in-force
-
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
Also Published As
| Publication number | Publication date |
|---|---|
| WO2011083287A2 (en) | 2011-07-14 |
| JP2013516397A (ja) | 2013-05-13 |
| CA2785998A1 (en) | 2011-07-14 |
| JP2016028085A (ja) | 2016-02-25 |
| ZA201204365B (en) | 2013-12-23 |
| AU2010340799A1 (en) | 2012-07-05 |
| WO2011083287A3 (en) | 2011-09-15 |
| EP2521728B1 (en) | 2016-09-07 |
| US20130029945A1 (en) | 2013-01-31 |
| US20150141383A1 (en) | 2015-05-21 |
| EP2521728A2 (en) | 2012-11-14 |
| AU2010340799B2 (en) | 2015-06-11 |
| KR20120123077A (ko) | 2012-11-07 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PSEA | Patent sealed | ||
| RENW | Renewal (renewal fees accepted) |
Free format text: PATENT RENEWED FOR 3 YEARS UNTIL 06 OCT 2017 BY CPA GLOBAL Effective date: 20140822 |
|
| LAPS | Patent lapsed |