EA199900720A1 - Способ кристаллизации ингибитора обратной транскриптазы с применением противорастворителя - Google Patents

Способ кристаллизации ингибитора обратной транскриптазы с применением противорастворителя

Info

Publication number
EA199900720A1
EA199900720A1 EA199900720A EA199900720A EA199900720A1 EA 199900720 A1 EA199900720 A1 EA 199900720A1 EA 199900720 A EA199900720 A EA 199900720A EA 199900720 A EA199900720 A EA 199900720A EA 199900720 A1 EA199900720 A1 EA 199900720A1
Authority
EA
Eurasian Patent Office
Prior art keywords
solvent
crystallizing
application
reverse transcriptase
transcriptase inhibitor
Prior art date
Application number
EA199900720A
Other languages
English (en)
Other versions
EA001805B1 (ru
Inventor
Уильям Кларк
Луис С. Крокер
Джозеф Л. II Кукура
Original Assignee
Мерк Энд Ко., Инк.
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=27451618&utm_source=***_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=EA199900720(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Priority claimed from GBGB9706046.1A external-priority patent/GB9706046D0/en
Priority claimed from GBGB9709348.8A external-priority patent/GB9709348D0/en
Application filed by Мерк Энд Ко., Инк. filed Critical Мерк Энд Ко., Инк.
Publication of EA199900720A1 publication Critical patent/EA199900720A1/ru
Publication of EA001805B1 publication Critical patent/EA001805B1/ru

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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (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)
  • Public Health (AREA)
  • Molecular Biology (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Saccharide Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)

Abstract

Настоящее изобретение описывает способ кристаллизации (-)-6-хлор-4-циклопропилэтинил-4-трифторметил-1,4-дигидро-2H-3,1-бензоксазин-2-она из системы растворителя и противорастворителя и получения кристаллического продукта. Желательная конечная кристаллическая форма, являющаяся формой I, может быть получена при применении метанола или этанола. Из 2-пропанола выделяют форму II и ее можно превратить при низких температурах сушки, например при температурах между около 40 и 50°C, в желательную кристаллическую форму.Международная заявка была опубликована вместе с отчетом о международном поиске.
EA199900720A 1997-02-05 1998-02-02 Способ кристаллизации ингибитора обратной транскриптазы с применением противорастворителя EA001805B1 (ru)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US3738597P 1997-02-05 1997-02-05
GBGB9706046.1A GB9706046D0 (en) 1997-03-24 1997-03-24 Process for the crystallization of a reverse transcriptase inhibitor using an anti-solvent
US4280797P 1997-04-08 1997-04-08
GBGB9709348.8A GB9709348D0 (en) 1997-05-07 1997-05-07 Process for the crystallization of a reverse transcriptase inhibitor using an anti-solvent
PCT/US1998/001999 WO1998033782A1 (en) 1997-02-05 1998-02-02 Process for the crystallization of a reverse transcriptase inhibitor using an anti-solvent

Publications (2)

Publication Number Publication Date
EA199900720A1 true EA199900720A1 (ru) 2000-04-24
EA001805B1 EA001805B1 (ru) 2001-08-27

Family

ID=27451618

Family Applications (1)

Application Number Title Priority Date Filing Date
EA199900720A EA001805B1 (ru) 1997-02-05 1998-02-02 Способ кристаллизации ингибитора обратной транскриптазы с применением противорастворителя

Country Status (18)

Country Link
EP (1) EP0975609B1 (ru)
JP (6) JP3418626B2 (ru)
KR (1) KR100573192B1 (ru)
CN (2) CN1191242C (ru)
AT (1) ATE486065T1 (ru)
AU (1) AU738545C (ru)
CA (1) CA2279198C (ru)
CZ (2) CZ304186B6 (ru)
DE (1) DE69841972D1 (ru)
EA (1) EA001805B1 (ru)
EE (1) EE03827B1 (ru)
HU (1) HU229087B1 (ru)
IL (1) IL130715A (ru)
NO (1) NO320128B1 (ru)
NZ (1) NZ336510A (ru)
PL (1) PL197740B1 (ru)
SK (1) SK284935B6 (ru)
WO (1) WO1998033782A1 (ru)

Families Citing this family (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998033782A1 (en) * 1997-02-05 1998-08-06 Merck & Co., Inc. Process for the crystallization of a reverse transcriptase inhibitor using an anti-solvent
AR011731A1 (es) * 1997-05-16 2000-08-30 Merck & Co Inc Un proceso de reaccion de adicion enantioselectiva eficiente utilizando un reactivo de organozinc.
US20010014352A1 (en) 1998-05-27 2001-08-16 Udit Batra Compressed tablet formulation
HRP990182A2 (en) * 1998-06-11 2000-02-29 Du Pont Pharm Co Crystalline efavirenz
GB9828721D0 (en) * 1998-12-24 1999-02-17 Glaxo Group Ltd Novel apparatus and process
WO2006018853A2 (en) 2004-08-19 2006-02-23 Hetero Drugs Limited Novel polymorphs of efavirenz
WO2008108630A1 (en) * 2007-03-02 2008-09-12 Ultimorphix Technologies B.V. Polymorphic forms of efavirenz
WO2009087679A2 (en) * 2007-12-24 2009-07-16 Matrix Laboratories Limited Process for preparing polymorphic forms of (s)-6-chloro-(cyclopropylethynyl)-1,4-dihydro-4-(trifluoromethyl)-2h-3,1-benzoxazin-2-one
US8383811B2 (en) 2008-12-22 2013-02-26 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
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
US11512092B2 (en) 2015-10-16 2022-11-29 Abbvie Inc. Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-n-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
US10550126B2 (en) 2015-10-16 2020-02-04 Abbvie Inc. Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-A]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
US11773106B2 (en) 2015-10-16 2023-10-03 Abbvie Inc. Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
US11365198B2 (en) 2015-10-16 2022-06-21 Abbvie Inc. Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
WO2017066775A1 (en) 2015-10-16 2017-04-20 Abbvie Inc. PROCESSES FOR THE PREPARATION OF (3S,4R)-3-ETHYL-4-(3H-IMIDAZO[1,2-a]PYRROLO[2,3-e]-PYRAZIN-8-YL)-N-(2,2,2-TRIFLUOROETHYL)PYRROLIDINE-1-CARBOXAMIDE AND SOLID STATE FORMS THEREOF
US11524964B2 (en) 2015-10-16 2022-12-13 Abbvie Inc. Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-n-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
CN114195761B (zh) * 2021-12-23 2023-04-14 浙江普洛家园药业有限公司 一种高纯度西他沙星3/2水合物的制备方法

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA1282405C (en) * 1984-05-21 1991-04-02 Michael R. Violante Method for making uniformly sized particles from water-insoluble organic compounds
IL106507A (en) * 1992-08-07 1997-11-20 Merck & Co Inc Pharmaceutical compositions containing benzoxazinones and some novel compounds of this type
US5665720A (en) * 1992-08-07 1997-09-09 Merck & Co., Inc. Benzoxazinones as inhibitors of HIV reverse transcriptase
AU1694295A (en) * 1994-01-28 1995-08-15 Merck & Co., Inc. Benzoxazinones as inhibitors of hiv reverse transcriptase
US5663467A (en) * 1995-01-23 1997-09-02 Merck & Co., Inc. Synthesis of cyclopropylacetylene
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
WO1998033782A1 (en) * 1997-02-05 1998-08-06 Merck & Co., Inc. Process for the crystallization of a reverse transcriptase inhibitor using an anti-solvent
CA2285000A1 (en) * 1997-04-07 1998-10-15 Dupont Pharmaceuticals Company Asymmetric synthesis of benzoxazinones via new intermediates

Also Published As

Publication number Publication date
HUP0001313A3 (en) 2002-12-28
IL130715A (en) 2003-07-31
CA2279198C (en) 2009-04-14
ATE486065T1 (de) 2010-11-15
PL334478A1 (en) 2000-02-28
CA2279198A1 (en) 1998-08-06
NO993779D0 (no) 1999-08-04
CZ304186B6 (cs) 2013-12-11
AU6263298A (en) 1998-08-25
IL130715A0 (en) 2000-06-01
AU738545B2 (en) 2001-09-20
CZ276599A3 (cs) 2000-02-16
NZ336510A (en) 2001-04-27
EP0975609A4 (en) 2001-02-21
KR100573192B1 (ko) 2006-04-24
HU229087B1 (en) 2013-07-29
EP0975609A1 (en) 2000-02-02
JP6126172B2 (ja) 2017-05-10
EP0975609B1 (en) 2010-10-27
JP2015205914A (ja) 2015-11-19
WO1998033782A1 (en) 1998-08-06
PL197740B1 (pl) 2008-04-30
KR20000070735A (ko) 2000-11-25
HUP0001313A2 (hu) 2000-10-28
JP5295190B2 (ja) 2013-09-18
SK105599A3 (en) 2000-05-16
JP2013139484A (ja) 2013-07-18
NO993779L (no) 1999-10-05
CZ297535B6 (cs) 2007-01-03
NO320128B1 (no) 2005-10-31
AU738545C (en) 2004-06-17
CN1246113A (zh) 2000-03-01
JP2011006472A (ja) 2011-01-13
JP2017061575A (ja) 2017-03-30
EA001805B1 (ru) 2001-08-27
CN1191242C (zh) 2005-03-02
DE69841972D1 (de) 2010-12-09
JP2003040874A (ja) 2003-02-13
EE03827B1 (et) 2002-08-15
JP3418626B2 (ja) 2003-06-23
SK284935B6 (sk) 2006-02-02
CN1073991C (zh) 2001-10-31
CN1385425A (zh) 2002-12-18
JP2000507972A (ja) 2000-06-27
EE9900341A (et) 2000-02-15

Similar Documents

Publication Publication Date Title
EA199900720A1 (ru) Способ кристаллизации ингибитора обратной транскриптазы с применением противорастворителя
EA199900166A1 (ru) Замещенные 6,6-гетеробициклические производные
ES2038310T3 (es) Procedimiento para la sintesis de derivados de 3-tio-4-quinolona y sus compuestos intermedios.
DK441389A (da) Fremgangsmaade til fremstilling af 1-adamantan-derivater
ATE326477T1 (de) Synthese von 9-deoxo-9a-aza 11,12-deoxy-9a-methyl-9a-homoerythromycin a 11,12-hydrogenorthoborat- dihydrat
EA199900552A1 (ru) Асимметрический способ получения бензоксазинонов
EA199900911A1 (ru) Асимметрический синтез бензоксазинонов через новые промежуточные соединения
EA200201017A1 (ru) Кристаллическая форма ii каберголина
ES2173179T3 (es) Procedimiento para preparar composiciones de avermectina/ceina.
DK0804410T3 (da) Fremgangsmåde til fremstilling af retrovirale proteaseinhibitor-mellemprodukter
DE69513657D1 (de) Verfahren zur Herstellung von 1-substituierten 2-Cyanoimidazolen
KR970065513A (ko) N-메틸-n'-니트로구아니딘의 제조 방법
EA199800034A1 (ru) Способ получения n-монозамещенных и n,n'-дизамещенных асимметричных циклических мочевин
KR950008491A (ko) 1-치환된-5(4h)-테트라졸리논의 제조방법
BR9912870A (pt) Processo para sìntese de derivados de (1h) - benzo (c)quinolizina-3-onas
EA199900235A1 (ru) Аморфные бензотиофены, способы получения и способы применения
ES2167999T3 (es) Procedimiento para el aislamiento de 14-beta hidroxi-10-deacetil baccatina iii.
NO894626D0 (no) Fremgangsmaate for fremstilling av 63 karboksyamider av teicoplanin-antibiotika.
DE69809888D1 (de) Verfahren zur Herstellung von alpha-Aminoketonen
EA199700391A1 (ru) Способ получения производных карбоновых кислот
BR9503845A (pt) Processo para a preparação de um composto e composto obtido
DK0841985T3 (da) Katalysator, fremgangsmåde til fremstilling af denne samt dens anvendelse til en fremgangsmåde til fremstilling af methylam
DE69900214T2 (de) Herstellung von (s)-n-tert-butyl-1,2,3,4-tetrahydroisoquinolin-3-carboxamid
BR9803388A (pt) Processo para a preparação de um composto de 4,6-bi (arilóxi)-pirimidina assimétrico.
KR840009105A (ko) 1,4-디하이드로피리딘 유도체의 제조방법

Legal Events

Date Code Title Description
PD4A Registration of transfer of a eurasian patent in accordance with the succession in title
ND4A Extension of term of a eurasian patent
PD4A Registration of transfer of a eurasian patent in accordance with the succession in title
MK4A Patent expired

Designated state(s): AM AZ KZ KG MD TJ TM RU

MK4A Patent expired

Designated state(s): BY