AR018670A1 - Compuesto cristalino (s)-6-cloro-4-ciclopropiletinil-4-trifluormetil-1,4-dihidro-2h-3,1-benzoxacin-2-ona (efavirenz) en sus formas 1 a 5 y composicion farmaceutica que lo contiene - Google Patents

Compuesto cristalino (s)-6-cloro-4-ciclopropiletinil-4-trifluormetil-1,4-dihidro-2h-3,1-benzoxacin-2-ona (efavirenz) en sus formas 1 a 5 y composicion farmaceutica que lo contiene

Info

Publication number
AR018670A1
AR018670A1 ARP990102809A ARP990102809A AR018670A1 AR 018670 A1 AR018670 A1 AR 018670A1 AR P990102809 A ARP990102809 A AR P990102809A AR P990102809 A ARP990102809 A AR P990102809A AR 018670 A1 AR018670 A1 AR 018670A1
Authority
AR
Argentina
Prior art keywords
efavirenz
pharmaceutical composition
composition containing
ciclopropiletinil
trifluormetil
Prior art date
Application number
ARP990102809A
Other languages
English (en)
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=AR018670(A1) "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 AR018670A1 publication Critical patent/AR018670A1/es

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)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Virology (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Molecular Biology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • AIDS & HIV (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (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)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Dicho compuesto está representado en la formula (I), y la forma cristalina seleccionada entre 1, 2, 3, 4 y 5 (que son las denominaciones de susformas físicas posibles). Una composicion farmacéutica que contiene dicho compuesto y el método para inhibir la replicacion viral por una transcriptasainversa codificada por el virus. El compuesto efavirenz no solamente es un inhibidor muy potente de la transcriptasa inversa sino que también eseficaz contra la resistencia de la transcriptasa inversa del VIH (virus de la inmunodeficiencia humana).
ARP990102809A 1998-06-11 1999-06-11 Compuesto cristalino (s)-6-cloro-4-ciclopropiletinil-4-trifluormetil-1,4-dihidro-2h-3,1-benzoxacin-2-ona (efavirenz) en sus formas 1 a 5 y composicion farmaceutica que lo contiene AR018670A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US8898198P 1998-06-11 1998-06-11

Publications (1)

Publication Number Publication Date
AR018670A1 true AR018670A1 (es) 2001-11-28

Family

ID=22214647

Family Applications (3)

Application Number Title Priority Date Filing Date
ARP990102809A AR018670A1 (es) 1998-06-11 1999-06-11 Compuesto cristalino (s)-6-cloro-4-ciclopropiletinil-4-trifluormetil-1,4-dihidro-2h-3,1-benzoxacin-2-ona (efavirenz) en sus formas 1 a 5 y composicion farmaceutica que lo contiene
ARP100102491A AR077469A2 (es) 1998-06-11 2010-07-08 Proceso para preparar la forma 1 de efavirenz cristalino
ARP100102490A AR077407A2 (es) 1998-06-11 2010-07-08 Forma 5 de efavirenz cristalino, proceso para obtenerla y metodos de uso

Family Applications After (2)

Application Number Title Priority Date Filing Date
ARP100102491A AR077469A2 (es) 1998-06-11 2010-07-08 Proceso para preparar la forma 1 de efavirenz cristalino
ARP100102490A AR077407A2 (es) 1998-06-11 2010-07-08 Forma 5 de efavirenz cristalino, proceso para obtenerla y metodos de uso

Country Status (21)

Country Link
EP (1) EP1086087A1 (es)
JP (1) JP2002517487A (es)
CN (1) CN1307568A (es)
AR (3) AR018670A1 (es)
AU (1) AU758114C (es)
BR (1) BR9911523A (es)
CA (1) CA2333550A1 (es)
EE (1) EE05547B1 (es)
HR (1) HRP990182A2 (es)
HU (1) HUP0103819A3 (es)
IL (1) IL139793A (es)
MY (1) MY126450A (es)
NO (1) NO20006255L (es)
NZ (1) NZ507713A (es)
PL (1) PL198504B1 (es)
SG (3) SG111980A1 (es)
SK (1) SK18182000A3 (es)
TW (1) TWI235152B (es)
UA (1) UA74324C2 (es)
WO (1) WO1999064405A1 (es)
ZA (1) ZA200006173B (es)

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
PE20060587A1 (es) * 2004-09-02 2006-07-09 Bristol Myers Squibb Co Sintesis de (s)-6-cloro-4-ciclopropiletinil-4-trifluorometil-1,4-dihidro-2h-3,1-benzoxazin-2-ona
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
EP2367804B1 (en) 2008-12-22 2013-11-06 Hetero Research Foundation Process for preparing efavirenz polymorph
DE102009041443A1 (de) 2009-09-16 2011-03-31 Archimica Gmbh Salze des 6-Chlor-4-(cyclopropylethinyl)-1,4-dihydro-4-(trifluormethyl)-2H-3,1-benzoxazin-2-ons und deren Synthese, Aufreinigung und Anwendung als Vorstufen für Efavirenz
EP2471783A1 (en) 2010-12-23 2012-07-04 Esteve Química, S.A. Novel polymorphic form of efavirenz
CN103508973B (zh) * 2012-06-25 2016-04-27 上海迪赛诺药业有限公司 制备依非韦伦i型结晶的方法
CN102924398B (zh) * 2012-11-22 2015-11-18 安徽贝克生物制药有限公司 用于除去依非韦伦对应异构体的方法
WO2014114971A1 (en) * 2013-01-23 2014-07-31 Alienor Farma Increased dosage of efavirenz for the treatment of cancer
CN105037175B (zh) * 2014-07-18 2017-02-22 盐城迪赛诺制药有限公司 一种用于提高依非韦伦中间体光学纯度的方法
CN105001101B (zh) * 2015-05-28 2017-11-28 乐平市瑞盛制药有限公司 一种4‑氯‑2‑三氟乙酰基苯胺水合物盐酸盐的合成方法
CN108947855B (zh) * 2018-08-10 2021-10-22 江苏沙星化工有限公司 一种依非韦伦关键中间体的合成方法

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
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
CZ297535B6 (cs) * 1997-02-05 2007-01-03 Merck & Co., Inc. Způsob krystalizace inhibitoru na bázi benzoxazinonu

Also Published As

Publication number Publication date
SK18182000A3 (sk) 2001-08-06
NO20006255L (no) 2001-02-12
SG111980A1 (en) 2005-06-29
NZ507713A (en) 2003-08-29
HUP0103819A2 (hu) 2002-02-28
WO1999064405A1 (en) 1999-12-16
UA74324C2 (uk) 2005-12-15
AU758114B2 (en) 2003-03-13
SG111981A1 (en) 2005-06-29
AU758114C (en) 2003-10-30
PL198504B1 (pl) 2008-06-30
JP2002517487A (ja) 2002-06-18
IL139793A0 (en) 2002-02-10
BR9911523A (pt) 2001-09-18
PL345221A1 (en) 2001-12-03
EE200000743A (et) 2002-10-15
AU4436499A (en) 1999-12-30
SG134977A1 (en) 2007-09-28
EE05547B1 (et) 2012-06-15
CN1307568A (zh) 2001-08-08
NO20006255D0 (no) 2000-12-08
CA2333550A1 (en) 1999-12-16
TWI235152B (en) 2005-07-01
AR077469A2 (es) 2011-08-31
HUP0103819A3 (en) 2003-05-28
AR077407A2 (es) 2011-08-24
IL139793A (en) 2006-10-31
EP1086087A1 (en) 2001-03-28
MY126450A (en) 2006-10-31
HRP990182A2 (en) 2000-02-29
ZA200006173B (en) 2001-10-31

Similar Documents

Publication Publication Date Title
AR018670A1 (es) Compuesto cristalino (s)-6-cloro-4-ciclopropiletinil-4-trifluormetil-1,4-dihidro-2h-3,1-benzoxacin-2-ona (efavirenz) en sus formas 1 a 5 y composicion farmaceutica que lo contiene
MX9403380A (es) Inhibidores de proteasa de vih utiles para el tratamiento de sida.
UY28084A1 (es) Derivados antivirales de nucleosidos
MX9204454A (es) Derivados de tiourea para inhibir la replicacion del virus de inmunodeficiencia humana y formulado farmaceutico que los contiene.
ECSP055801A (es) Compuestos benzofuránicos, composiciones y métodos para el tratamiento y profilaxis de infecciones virales de hepatitis c y enfermedades asociadas
ES2192201T3 (es) Compuestos de piranona utiles para el tratamiento de infecciones retrovirales.
AR024227A1 (es) Pirimidinas inhibidoras de replicacion de hiv, un proceso para su preparacion, el uso de las mismas para la manufactura de un medicamento, composiciones farmaceuticas, y un proceso para prepararlas
PE20061372A1 (es) Composicion farmaceutica que contiene un vector adenovirus
ES2186787T3 (es) Utilizacion de ritonavir (abt-538) para mejorar la farmacocinetica de medicamentos metabolizados por el citocromo p450 en un metodo de tratamiento del sida.
ECSP066959A (es) Compuestos macrociclicos como inhibidores de la replicación viral
UY27333A1 (es) Nucleótidos 4` sustituidos
LV12719A (lv) Benzoxazinones as inhibitors of hiv reverse transcriptase
DK0545966T3 (da) Phospholipidderivater af nucleosider, deres fremstilling samt deres anvendelse som anti-virale lægemidler
EA200401437A1 (ru) Ненуклеозидные ингибиторы обратной транскриптазы для лечения вич инфекции, способ их получения (варианты), способ увеличения периода полупревращения ненуклеозидного соединения, обладающего активностью против ретровирусов, и способ получения фармацевтической композиции, обладающей специфичностью к лейкоцитам
ES2146300T3 (es) Utilizacion de composiciones antihelminticas para el tratamiento de infecciones causadas por anoplocephala perfoliata en equidos.
UY29320A1 (es) 18-metil-19-nor-17-pregn-4-en-21, 17-carbolactonas, así como preparaciones farmacéuticas que las contienen
BR9909474A (pt) Formas ii, cristalina e v de 5,6-dicloro-2-(isopropilamino)-1-beta-l-ribofuranosil -1h-benzimidazol, solvato de etanol de 5,6-dicloro-2-(isopropilamino)-1-beta-l-ribofuranosil -1h-benzimidazol, composição, composto, uso de 5,6-dicloro-2-(isopropilamino)-1-beta-l-ribofuranosil -1h-benzimidazol, e, processos para o tratamento de uma infecção viral em um humano e para a produção de 5,6-dicloro-2-(isopropilamino)-1-beta-l-ribofuranosil -1h-benzimidazol
ES2192101T3 (es) Formas cristalinas de eto2c-ch2-(r)cgl-aze-pab-oh.
AR013079A1 (es) Derivados sustituidos de tetrahidrofurano-3-onas, de tetrahidropirano-3- onas y tetrahidrotiofen-3-onas, un procedimiento para su preparacion unacomposicion farmaceutica de un medicamento util como inhibidores de proteasas e intermediarios
UY26920A1 (es) 7 - oxo piridopirimidinas
AR007997A1 (es) Un derivado de distamicina sustituida con acriloilo, sus utilizaciones, un procedimiento para producirlo y una composicion farmaceutica que lo comprende.
MX9300399A (es) Derivados heterotriciclicos.
CO4130200A1 (es) Inhibidores de proteasa del hiv utiles en el tratamiento del sida
BR0306927A (pt) Compostos tricìclicos de 2-pirimidona úteis como inibidores de transcriptase reversa de hiv
MX9302681A (es) Nuevas quinazolinas como inhibidores de transcriptasa inversa hiv.

Legal Events

Date Code Title Description
FC Refusal