MY126450A - Crystalline efavirenz - Google Patents

Crystalline efavirenz

Info

Publication number
MY126450A
MY126450A MYPI99002384A MYPI19992384A MY126450A MY 126450 A MY126450 A MY 126450A MY PI99002384 A MYPI99002384 A MY PI99002384A MY PI19992384 A MYPI19992384 A MY PI19992384A MY 126450 A MY126450 A MY 126450A
Authority
MY
Malaysia
Prior art keywords
efavirenz
crystalline
crystalline efavirenz
differaction
hiv
Prior art date
Application number
MYPI99002384A
Inventor
B Maurin Michael
A Radesca Lilian
R Rabel Shelley
R Moore James
Original Assignee
Bristol Myers Squibb Pharma Company
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=MY126450(A) "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 Company filed Critical Bristol Myers Squibb Pharma Company
Publication of MY126450A publication Critical patent/MY126450A/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)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Virology (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (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

THE POTENT REVERSE TRANSCRIPTASE INHIBITOR EFAVIRENZ IS PRODUCED IN CRYSTALLINE FORM. CRYSTALLINE EFAVIRENZ EXISTS IN SEVERAL PHYSICAL FORMS WHICH ARE DESIGNATED FORM 1, 2, 3, 4, AND 5 AND ARE CHARACTERIZED BY X-RAY POWDER DIFFERACTION AND DIFFERENTIAL SCANNING CALORIMENTRY. PHARMACEUTICAL COMPOSITIONS AND METHODS ARE USEFUL FOR THE TREATMENT OF THE HUMAN IMMUNODEFICIENCY VIRUS (HIV).(FIG 2)
MYPI99002384A 1998-06-11 1999-06-10 Crystalline efavirenz MY126450A (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
MY126450A true MY126450A (en) 2006-10-31

Family

ID=22214647

Family Applications (1)

Application Number Title Priority Date Filing Date
MYPI99002384A MY126450A (en) 1998-06-11 1999-06-10 Crystalline efavirenz

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)

* 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
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
SI2303267T1 (en) 2008-02-04 2013-09-30 Pfizer Limited Polymorphic form of a s1, 2, 4c triazolo s4, 3-acpyridine 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
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
WO1995020389A1 (en) * 1994-01-28 1995-08-03 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
CA2268953A1 (en) * 1996-10-02 1998-04-09 Du Pont 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
SK284935B6 (en) * 1997-02-05 2006-02-02 Merck & Co., Inc. Form I of (-)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl- 1,4-dihydro-2H-3,1-benzoxazin-2-one and method for its crystallization

Also Published As

Publication number Publication date
SK18182000A3 (en) 2001-08-06
NO20006255D0 (en) 2000-12-08
PL345221A1 (en) 2001-12-03
IL139793A (en) 2006-10-31
EP1086087A1 (en) 2001-03-28
TWI235152B (en) 2005-07-01
CN1307568A (en) 2001-08-08
NO20006255L (en) 2001-02-12
WO1999064405A1 (en) 1999-12-16
UA74324C2 (en) 2005-12-15
BR9911523A (en) 2001-09-18
SG111981A1 (en) 2005-06-29
ZA200006173B (en) 2001-10-31
EE200000743A (en) 2002-10-15
JP2002517487A (en) 2002-06-18
AU758114C (en) 2003-10-30
HUP0103819A2 (en) 2002-02-28
HUP0103819A3 (en) 2003-05-28
CA2333550A1 (en) 1999-12-16
PL198504B1 (en) 2008-06-30
AR077407A2 (en) 2011-08-24
EE05547B1 (en) 2012-06-15
AR018670A1 (en) 2001-11-28
AU758114B2 (en) 2003-03-13
IL139793A0 (en) 2002-02-10
AR077469A2 (en) 2011-08-31
AU4436499A (en) 1999-12-30
HRP990182A2 (en) 2000-02-29
SG134977A1 (en) 2007-09-28
SG111980A1 (en) 2005-06-29
NZ507713A (en) 2003-08-29

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