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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 USE

Info

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
Application number
ARP100102490A
Other languages
Spanish (es)
Inventor
Lilian A Radesca
Michael B Maurin
Shelley R Rabel
James R Moore
Original Assignee
Bristol Myers Squibb Pharma Co
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=22214647&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR077407(A2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Bristol Myers Squibb Pharma Co filed Critical Bristol Myers Squibb Pharma Co
Publication of AR077407A2 publication Critical patent/AR077407A2/en

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.

ARP100102490A 1998-06-11 2010-07-08 FORM 5 OF EFAVIRENZ CRISTALINO, PROCESS TO OBTAIN IT AND METHODS OF USE AR077407A2 (en)

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) SG111981A1 (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)

* Cited by examiner, † Cited by third party
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
US20060235008A1 (en) 2004-08-19 2006-10-19 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
US8222273B2 (en) * 2008-02-04 2012-07-17 Pfizer Limited Polymorphic form of a [1,2,4]triazole[4,3-A] pyridine derivative 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
CA2898145C (en) * 2013-01-23 2021-08-31 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)

* Cited by examiner, † Cited by third party
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
AU3736197A (en) * 1996-07-26 1998-02-20 Du Pont Pharmaceuticals Company A practical synthesis of benzoxazinones useful as hiv reverse transcripta se inhibitors
WO1998014436A1 (en) * 1996-10-02 1998-04-09 Dupont Pharmaceuticals Company 4,4-disubstituted-1,4-dihydro-2h-3,1-benzoxazin-2-ones useful as hiv reverse transcriptase inhibitors and intermediates and processes for making the same
KR100573192B1 (en) * 1997-02-05 2006-04-24 머크 앤드 캄파니 인코포레이티드 Process for the crystallization of a reverse transcriptase inhibitor using an anti-solvent and crystal forms of the same

Also Published As

Publication number Publication date
PL345221A1 (en) 2001-12-03
BR9911523A (en) 2001-09-18
PL198504B1 (en) 2008-06-30
AU758114C (en) 2003-10-30
NO20006255D0 (en) 2000-12-08
UA74324C2 (en) 2005-12-15
NZ507713A (en) 2003-08-29
SG134977A1 (en) 2007-09-28
SG111981A1 (en) 2005-06-29
AU758114B2 (en) 2003-03-13
MY126450A (en) 2006-10-31
HRP990182A2 (en) 2000-02-29
CA2333550A1 (en) 1999-12-16
IL139793A0 (en) 2002-02-10
IL139793A (en) 2006-10-31
HUP0103819A2 (en) 2002-02-28
ZA200006173B (en) 2001-10-31
AU4436499A (en) 1999-12-30
TWI235152B (en) 2005-07-01
AR077469A2 (en) 2011-08-31
CN1307568A (en) 2001-08-08
EE200000743A (en) 2002-10-15
AR018670A1 (en) 2001-11-28
JP2002517487A (en) 2002-06-18
SG111980A1 (en) 2005-06-29
EE05547B1 (en) 2012-06-15
WO1999064405A1 (en) 1999-12-16
NO20006255L (en) 2001-02-12
SK18182000A3 (en) 2001-08-06
EP1086087A1 (en) 2001-03-28
HUP0103819A3 (en) 2003-05-28

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