AR077407A2 - FORM 5 OF EFAVIRENZ CRISTALINO, PROCESS TO OBTAIN IT AND METHODS OF USE - Google Patents
FORM 5 OF EFAVIRENZ CRISTALINO, PROCESS TO OBTAIN IT AND METHODS OF USEInfo
- Publication number
- AR077407A2 AR077407A2 ARP100102490A ARP100102490A AR077407A2 AR 077407 A2 AR077407 A2 AR 077407A2 AR P100102490 A ARP100102490 A AR P100102490A AR P100102490 A ARP100102490 A AR P100102490A AR 077407 A2 AR077407 A2 AR 077407A2
- Authority
- AR
- Argentina
- Prior art keywords
- methods
- efavirenz
- cristalino
- hiv
- describes
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
- C07D265/04—1,3-Oxazines; Hydrogenated 1,3-oxazines
- C07D265/12—1,3-Oxazines; Hydrogenated 1,3-oxazines condensed with carbocyclic rings or ring systems
- C07D265/14—1,3-Oxazines; Hydrogenated 1,3-oxazines condensed with carbocyclic rings or ring systems condensed with one six-membered ring
- C07D265/18—1,3-Oxazines; Hydrogenated 1,3-oxazines condensed with carbocyclic rings or ring systems condensed with one six-membered ring with hetero atoms directly attached in position 2
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/04—Immunostimulants
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Immunology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Virology (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- AIDS & HIV (AREA)
- Engineering & Computer Science (AREA)
- Tropical Medicine & Parasitology (AREA)
- Molecular Biology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Abstract
Forma 5 de efavirenz cristalino que presenta un patron de difraccion de partículas por rayos X que comprende cuatro o más valores 2 seleccionados del grupo formado por: 10,2 +- 0,2; 11,4 +- 0,2; 11,6 +- 0,2; 12,6 +- 0,2; 19,1 +- 0,2; 20,6 +- 0,2; 21,3 +- 0-2; 22,8 +- 0,2; 24,8 +- 0,2; 27,4 +- 0,2; 28,2 +- 0,2; y 31,6 +- 0,2. También se describe el proceso para obtenerla y métodos de uso, util para el HIV.Form 5 of crystalline efavirenz that has an X-ray particle diffraction pattern comprising four or more 2 values selected from the group consisting of: 10.2 + - 0.2; 11.4 + - 0.2; 11.6 + - 0.2; 12.6 + - 0.2; 19.1 + - 0.2; 20.6 + - 0.2; 21.3 + - 0-2; 22.8 + - 0.2; 24.8 + - 0.2; 27.4 + - 0.2; 28.2 + - 0.2; and 31.6 + - 0.2. It also describes the process to obtain it and methods of use, useful for HIV.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US8898198P | 1998-06-11 | 1998-06-11 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR077407A2 true AR077407A2 (en) | 2011-08-24 |
Family
ID=22214647
Family Applications (3)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP990102809A AR018670A1 (en) | 1998-06-11 | 1999-06-11 | CRYSTALLINE COMPOUND (S) -6-CHLORO-4-CICLOPROPILETINIL-4-TRIFLUORMETIL-1,4-DIHIDRO-2H-3,1-BENZOXACIN-2-ONA (EFAVIRENZ) IN ITS FORMS 1 TO 5 AND PHARMACEUTICAL COMPOSITION CONTAINING IT |
ARP100102490A AR077407A2 (en) | 1998-06-11 | 2010-07-08 | FORM 5 OF EFAVIRENZ CRISTALINO, PROCESS TO OBTAIN IT AND METHODS OF USE |
ARP100102491A AR077469A2 (en) | 1998-06-11 | 2010-07-08 | PROCESS TO PREPARE FORM 1 OF EFAVIRENZ CRISTALINO |
Family Applications Before (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP990102809A AR018670A1 (en) | 1998-06-11 | 1999-06-11 | CRYSTALLINE COMPOUND (S) -6-CHLORO-4-CICLOPROPILETINIL-4-TRIFLUORMETIL-1,4-DIHIDRO-2H-3,1-BENZOXACIN-2-ONA (EFAVIRENZ) IN ITS FORMS 1 TO 5 AND PHARMACEUTICAL COMPOSITION CONTAINING IT |
Family Applications After (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP100102491A AR077469A2 (en) | 1998-06-11 | 2010-07-08 | PROCESS TO PREPARE FORM 1 OF EFAVIRENZ CRISTALINO |
Country Status (21)
Country | Link |
---|---|
EP (1) | EP1086087A1 (en) |
JP (1) | JP2002517487A (en) |
CN (1) | CN1307568A (en) |
AR (3) | AR018670A1 (en) |
AU (1) | AU758114C (en) |
BR (1) | BR9911523A (en) |
CA (1) | CA2333550A1 (en) |
EE (1) | EE05547B1 (en) |
HR (1) | HRP990182A2 (en) |
HU (1) | HUP0103819A3 (en) |
IL (1) | IL139793A (en) |
MY (1) | MY126450A (en) |
NO (1) | NO20006255L (en) |
NZ (1) | NZ507713A (en) |
PL (1) | PL198504B1 (en) |
SG (3) | SG134977A1 (en) |
SK (1) | SK18182000A3 (en) |
TW (1) | TWI235152B (en) |
UA (1) | UA74324C2 (en) |
WO (1) | WO1999064405A1 (en) |
ZA (1) | ZA200006173B (en) |
Families Citing this family (15)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5965729A (en) | 1997-02-05 | 1999-10-12 | Merck & Co., Inc. | Process for the crystallization of a reverse transcriptase inhibitor using an anti-solvent |
WO2006018853A2 (en) | 2004-08-19 | 2006-02-23 | Hetero Drugs Limited | Novel polymorphs of efavirenz |
US7205402B2 (en) * | 2004-09-02 | 2007-04-17 | Bristol-Myers Squibb Company | Synthesis of a benzoxazinone |
WO2008108630A1 (en) * | 2007-03-02 | 2008-09-12 | Ultimorphix Technologies B.V. | Polymorphic forms of efavirenz |
WO2009011567A1 (en) * | 2007-07-16 | 2009-01-22 | Ultimorphix Technologies B.V. | Crystalline forms of efavirenz |
NZ587094A (en) * | 2008-02-04 | 2011-07-29 | Pfizer Ltd | Polymorphic form of a [1, 2, 4] triazolo [4, 3-a] pyridine derivative for treating inflammatory diseases |
US8383811B2 (en) | 2008-12-22 | 2013-02-26 | Hetero Research Foundation | Process for preparing efavirenz polymorph |
DE102009041443A1 (en) | 2009-09-16 | 2011-03-31 | Archimica Gmbh | Salts of 6-chloro-4- (cyclopropylethynyl) -1,4-dihydro-4- (trifluoromethyl) -2H-3,1-benzoxazin-2-one and their synthesis, purification and use as precursors of efavirenz |
EP2471783A1 (en) | 2010-12-23 | 2012-07-04 | Esteve Química, S.A. | Novel polymorphic form of efavirenz |
CN103508973B (en) * | 2012-06-25 | 2016-04-27 | 上海迪赛诺药业有限公司 | Prepare the method for efavirenz I type crystallization |
CN102924398B (en) * | 2012-11-22 | 2015-11-18 | 安徽贝克生物制药有限公司 | For removing the method for the corresponding isomer of efavirenz |
AU2013375157B2 (en) * | 2013-01-23 | 2018-07-12 | Alienor Farma | Increased dosage of Efavirenz for the treatment of cancer |
CN105037175B (en) * | 2014-07-18 | 2017-02-22 | 盐城迪赛诺制药有限公司 | Method of improving optical purity of efavirenz intermediate |
CN105001101B (en) * | 2015-05-28 | 2017-11-28 | 乐平市瑞盛制药有限公司 | A kind of synthetic method of the trifluoroacetyl aniline hydrate hydrochloride of 4 chlorine 2 |
CN108947855B (en) * | 2018-08-10 | 2021-10-22 | 江苏沙星化工有限公司 | Synthesis method of efavirenz key intermediate |
Family Cites Families (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
IL106507A (en) * | 1992-08-07 | 1997-11-20 | Merck & Co Inc | Pharmaceutical compositions containing benzoxazinones and some novel compounds of this type |
AU1694295A (en) * | 1994-01-28 | 1995-08-15 | Merck & Co., Inc. | Benzoxazinones as inhibitors of hiv reverse transcriptase |
US5633405A (en) * | 1995-05-25 | 1997-05-27 | Merck & Co., Inc. | Asymmetric synthesis of (-)-6-chloro-4-cyclopropyl-ethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxanzin-2-one |
CA2260922A1 (en) * | 1996-07-26 | 1998-02-05 | Du Pont Pharmaceuticals Company | A practical synthesis of benzoxazinones useful as hiv reverse transcriptase inhibitors |
AU4802797A (en) * | 1996-10-02 | 1998-04-24 | Du Pont Pharmaceuticals Company | 4,4-disubstituted-1,4-dihydro-2h-3,1-benzoxazin-2-ones useful as hiv rever se transcriptase inhibitors and intermediates and processes for making the same |
WO1998033782A1 (en) * | 1997-02-05 | 1998-08-06 | Merck & Co., Inc. | Process for the crystallization of a reverse transcriptase inhibitor using an anti-solvent |
-
1999
- 1999-06-08 HR HR60/088,981A patent/HRP990182A2/en not_active Application Discontinuation
- 1999-06-10 PL PL345221A patent/PL198504B1/en unknown
- 1999-06-10 SG SG200207226-2A patent/SG134977A1/en unknown
- 1999-06-10 IL IL139793A patent/IL139793A/en not_active IP Right Cessation
- 1999-06-10 CN CN99807219A patent/CN1307568A/en active Pending
- 1999-06-10 MY MYPI99002384A patent/MY126450A/en unknown
- 1999-06-10 BR BR9911523-9A patent/BR9911523A/en not_active Application Discontinuation
- 1999-06-10 EP EP99927468A patent/EP1086087A1/en not_active Withdrawn
- 1999-06-10 EE EEP200000743A patent/EE05547B1/en unknown
- 1999-06-10 HU HU0103819A patent/HUP0103819A3/en unknown
- 1999-06-10 WO PCT/US1999/013199 patent/WO1999064405A1/en active Search and Examination
- 1999-06-10 NZ NZ507713A patent/NZ507713A/en not_active IP Right Cessation
- 1999-06-10 SK SK1818-2000A patent/SK18182000A3/en unknown
- 1999-06-10 JP JP2000553414A patent/JP2002517487A/en active Pending
- 1999-06-10 AU AU44364/99A patent/AU758114C/en not_active Expired
- 1999-06-10 UA UA2000127048A patent/UA74324C2/en unknown
- 1999-06-10 CA CA002333550A patent/CA2333550A1/en not_active Abandoned
- 1999-06-10 SG SG200207221A patent/SG111981A1/en unknown
- 1999-06-10 SG SG200207220A patent/SG111980A1/en unknown
- 1999-06-11 AR ARP990102809A patent/AR018670A1/en not_active Application Discontinuation
- 1999-07-03 TW TW088109817A patent/TWI235152B/en not_active IP Right Cessation
-
2000
- 2000-10-31 ZA ZA200006173A patent/ZA200006173B/en unknown
- 2000-12-08 NO NO20006255A patent/NO20006255L/en not_active Application Discontinuation
-
2010
- 2010-07-08 AR ARP100102490A patent/AR077407A2/en not_active Application Discontinuation
- 2010-07-08 AR ARP100102491A patent/AR077469A2/en not_active Application Discontinuation
Also Published As
Publication number | Publication date |
---|---|
AU758114C (en) | 2003-10-30 |
JP2002517487A (en) | 2002-06-18 |
AR077469A2 (en) | 2011-08-31 |
AU4436499A (en) | 1999-12-30 |
NO20006255D0 (en) | 2000-12-08 |
TWI235152B (en) | 2005-07-01 |
AU758114B2 (en) | 2003-03-13 |
HRP990182A2 (en) | 2000-02-29 |
MY126450A (en) | 2006-10-31 |
HUP0103819A3 (en) | 2003-05-28 |
NZ507713A (en) | 2003-08-29 |
IL139793A (en) | 2006-10-31 |
EE200000743A (en) | 2002-10-15 |
SK18182000A3 (en) | 2001-08-06 |
IL139793A0 (en) | 2002-02-10 |
EE05547B1 (en) | 2012-06-15 |
AR018670A1 (en) | 2001-11-28 |
CA2333550A1 (en) | 1999-12-16 |
WO1999064405A1 (en) | 1999-12-16 |
SG111980A1 (en) | 2005-06-29 |
UA74324C2 (en) | 2005-12-15 |
CN1307568A (en) | 2001-08-08 |
NO20006255L (en) | 2001-02-12 |
SG134977A1 (en) | 2007-09-28 |
PL345221A1 (en) | 2001-12-03 |
SG111981A1 (en) | 2005-06-29 |
ZA200006173B (en) | 2001-10-31 |
PL198504B1 (en) | 2008-06-30 |
HUP0103819A2 (en) | 2002-02-28 |
EP1086087A1 (en) | 2001-03-28 |
BR9911523A (en) | 2001-09-18 |
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Legal Events
Date | Code | Title | Description |
---|---|---|---|
FC | Refusal |