ES2546866T3 - Polimorfos de darunavir - Google Patents
Polimorfos de darunavir Download PDFInfo
- Publication number
- ES2546866T3 ES2546866T3 ES09852224.6T ES09852224T ES2546866T3 ES 2546866 T3 ES2546866 T3 ES 2546866T3 ES 09852224 T ES09852224 T ES 09852224T ES 2546866 T3 ES2546866 T3 ES 2546866T3
- Authority
- ES
- Spain
- Prior art keywords
- darunavir
- polymorphs
- solvate
- alcohol
- image
- 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.)
- Active
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 2
- 229960005107 darunavir Drugs 0.000 title abstract 2
- AMQJEAYHLZJPGS-UHFFFAOYSA-N N-Pentanol Chemical compound CCCCCO AMQJEAYHLZJPGS-UHFFFAOYSA-N 0.000 abstract 1
- 239000012453 solvate 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
- A61K31/33—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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- 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
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Virology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- AIDS & HIV (AREA)
- Tropical Medicine & Parasitology (AREA)
- Molecular Biology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Steroid Compounds (AREA)
Abstract
Un solvato de alcohol C5 de darunavir.
Description
Claims (1)
-
imagen1
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| PCT/IN2009/000724 WO2011073993A1 (en) | 2009-12-16 | 2009-12-16 | Polymorphs of darunavir |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2546866T3 true ES2546866T3 (es) | 2015-09-29 |
Family
ID=44166823
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES09852224.6T Active ES2546866T3 (es) | 2009-12-16 | 2009-12-16 | Polimorfos de darunavir |
Country Status (7)
| Country | Link |
|---|---|
| US (3) | US20110313035A1 (es) |
| EP (1) | EP2513116B1 (es) |
| CN (1) | CN102686594A (es) |
| CA (1) | CA2784131C (es) |
| ES (1) | ES2546866T3 (es) |
| PT (1) | PT2513116E (es) |
| WO (1) | WO2011073993A1 (es) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8921415B2 (en) | 2009-01-29 | 2014-12-30 | Mapi Pharma Ltd. | Polymorphs 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 |
| NZ600994A (en) * | 2010-01-05 | 2014-04-30 | Cipla Ltd | Darunavir polymorph and process for preparation thereof |
| EP2528923B1 (en) | 2010-01-28 | 2014-07-30 | Mapi Pharma Limited | Process for the preparation of darunavir and darunavir intermediates |
| WO2011145099A1 (en) | 2010-05-20 | 2011-11-24 | Hetero Research Foundation | Crystalline hydrochloride salt of darunavir |
| WO2012107889A1 (en) * | 2011-02-10 | 2012-08-16 | Ranbaxy Laboratories Limited | Process for the preparation of amorphous darunavir |
| US9643976B2 (en) * | 2012-01-18 | 2017-05-09 | Aurobindo Pharma Ltd. | Solvates of 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 |
| CN107235987A (zh) * | 2016-03-28 | 2017-10-10 | 浙江九洲药业股份有限公司 | 一种地瑞那韦甲醇溶剂化物及其制备方法和用途 |
| ES2881949T3 (es) | 2016-10-27 | 2021-11-30 | Gilead Sciences Inc | Forma cristalina de base libre de darunavir |
| 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 |
Family Cites Families (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NL7310889A (es) | 1972-08-12 | 1974-02-14 | ||
| US4670578A (en) * | 1983-08-29 | 1987-06-02 | Merck & Co., Inc. | Process for crystalline salts of L or (S)-3-(3,4-dihydroxyphenyl)-2-methylalanine esters |
| US4692438A (en) * | 1984-08-24 | 1987-09-08 | Hoffmann-La Roche Inc. | Pyridazo-diazepines, diazocines, and -triazepines having anti-hypertensive activity |
| US5968942A (en) | 1992-08-25 | 1999-10-19 | G. D. Searle & Co. | α- and β-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors |
| US5315016A (en) * | 1992-10-13 | 1994-05-24 | Nycomed Dak A/S | Process for preparing pure podophyllotoxin |
| EP0715618B1 (en) | 1993-08-24 | 1998-12-16 | G.D. Searle & Co. | Hydroxyethylamino sulphonamides useful as retroviral protease inhibitors |
| CA2872424C (en) | 1998-06-23 | 2017-03-07 | The United States Of America, Represented By The Secretary, Department Of Health And Human Services | Bisfuran derivatives useful in preventing the emergence of multidrug resistant hiv strains and treatment of hiv |
| US20030125336A1 (en) | 2001-05-30 | 2003-07-03 | Fleitz Fred J. | Hydrohalide salts of an HIV protease inhibitor |
| BRPI0311176B8 (pt) * | 2002-05-16 | 2021-05-25 | Janssen Sciences Ireland Uc | pseudopolimorfo na forma de etanolato, seu uso, processo de preparação do mesmo e composição farmacêutica |
| JP2005533822A (ja) * | 2002-06-27 | 2005-11-10 | エスビー・ファルムコ・プエルト・リコ・インコーポレイテッド | 臭化水素酸カルベジロール |
| CN101160290B (zh) * | 2004-12-02 | 2011-01-19 | 第一三共株式会社 | 7-元环化合物、其制备方法和药物用途 |
| WO2006067795A2 (en) * | 2004-12-23 | 2006-06-29 | Jubilant Organosys Limited | Novel polymorphic forms of atorvastatin lactone and process for preparing the same |
| WO2007054969A2 (en) * | 2005-09-21 | 2007-05-18 | Torrent Pharmaceuticals Limited | Process for the preparation of lercanidipine and amorphous form of lercanidipine hydrochloride |
| AR057182A1 (es) | 2005-11-28 | 2007-11-21 | Tibotec Pharm Ltd | Compuestos de aminofenilsulfonamida sustituida como inhibidores de proteasa del vih |
| CN102432621B (zh) | 2006-11-09 | 2016-02-17 | 爱尔兰詹森科学公司 | 六氢呋喃并[2,3-b]呋喃-3-醇的制备方法 |
| MX2011007790A (es) | 2009-01-29 | 2011-11-18 | Mapi Pharma Ltd | Polimorfos de darunavir. |
| US8921415B2 (en) | 2009-01-29 | 2014-12-30 | Mapi Pharma Ltd. | Polymorphs of darunavir |
| KR20120006047A (ko) * | 2009-04-09 | 2012-01-17 | 산도즈 아게 | 삭사글립틴의 결정 형태 |
| 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 |
| WO2011145099A1 (en) | 2010-05-20 | 2011-11-24 | Hetero Research Foundation | Crystalline hydrochloride salt of darunavir |
-
2009
- 2009-12-16 CN CN2009801630706A patent/CN102686594A/zh active Pending
- 2009-12-16 CA CA2784131A patent/CA2784131C/en active Active
- 2009-12-16 WO PCT/IN2009/000724 patent/WO2011073993A1/en not_active Ceased
- 2009-12-16 ES ES09852224.6T patent/ES2546866T3/es active Active
- 2009-12-16 US US13/128,157 patent/US20110313035A1/en not_active Abandoned
- 2009-12-16 EP EP09852224.6A patent/EP2513116B1/en not_active Not-in-force
- 2009-12-16 PT PT98522246T patent/PT2513116E/pt unknown
-
2012
- 2012-06-22 US US13/530,844 patent/US9624236B2/en active Active
-
2013
- 2013-10-07 US US14/047,243 patent/US9580440B2/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| US9580440B2 (en) | 2017-02-28 |
| EP2513116A1 (en) | 2012-10-24 |
| CA2784131C (en) | 2017-07-11 |
| US20120288563A1 (en) | 2012-11-15 |
| EP2513116A4 (en) | 2013-05-08 |
| US20140200356A1 (en) | 2014-07-17 |
| CA2784131A1 (en) | 2011-06-23 |
| PT2513116E (pt) | 2015-10-14 |
| EP2513116B1 (en) | 2015-08-19 |
| CN102686594A (zh) | 2012-09-19 |
| US20110313035A1 (en) | 2011-12-22 |
| WO2011073993A1 (en) | 2011-06-23 |
| US9624236B2 (en) | 2017-04-18 |
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