JP3418626B2 - 逆溶媒を使用する逆転写酵素阻害剤の結晶化方法 - Google Patents

逆溶媒を使用する逆転写酵素阻害剤の結晶化方法

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Publication number
JP3418626B2
JP3418626B2 JP53319098A JP53319098A JP3418626B2 JP 3418626 B2 JP3418626 B2 JP 3418626B2 JP 53319098 A JP53319098 A JP 53319098A JP 53319098 A JP53319098 A JP 53319098A JP 3418626 B2 JP3418626 B2 JP 3418626B2
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JP
Japan
Prior art keywords
solvent
antisolvent
volume
compound
slurry
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Lifetime
Application number
JP53319098A
Other languages
English (en)
Japanese (ja)
Other versions
JP2000507972A (ja
Inventor
クラーク，ウイリアム
クロツカー，ルイス・エス
ククラ，ジヨ−ジフ・エル・ザ・セカンド
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck and Co Inc
Original Assignee
Merck and Co Inc
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=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=JP3418626(B2) "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 Merck and Co Inc filed Critical Merck and Co Inc
Publication of JP2000507972A publication Critical patent/JP2000507972A/ja
Application granted granted Critical
Publication of JP3418626B2 publication Critical patent/JP3418626B2/ja
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

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)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Virology (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • AIDS & HIV (AREA)
  • Communicable Diseases (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (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)
JP53319098A 1997-02-05 1998-02-02 逆溶媒を使用する逆転写酵素阻害剤の結晶化方法 Expired - Lifetime JP3418626B2 (ja)

Applications Claiming Priority (11)

Application Number Priority Date Filing Date Title
US3738597P 1997-02-05 1997-02-05
US60/037,385 1997-02-05
GB9706046.1 1997-03-24
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
US60/042,807 1997-04-08
GB60/037,385 1997-05-07
GBGB9709348.8A GB9709348D0 (en) 1997-05-07 1997-05-07 Process for the crystallization of a reverse transcriptase inhibitor using an anti-solvent
GB60/042,807 1997-05-07
GB9709348.8 1997-05-07
PCT/US1998/001999 WO1998033782A1 (en) 1997-02-05 1998-02-02 Process for the crystallization of a reverse transcriptase inhibitor using an anti-solvent

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2002163198A Division JP2003040874A (ja) 1997-02-05 2002-06-04 逆溶媒を使用する逆転写酵素阻害剤の結晶化方法

Publications (2)

Publication Number Publication Date
JP2000507972A JP2000507972A (ja) 2000-06-27
JP3418626B2 true JP3418626B2 (ja) 2003-06-23

Family

ID=27451618

Family Applications (6)

Application Number Title Priority Date Filing Date
JP53319098A Expired - Lifetime JP3418626B2 (ja) 1997-02-05 1998-02-02 逆溶媒を使用する逆転写酵素阻害剤の結晶化方法
JP2002163198A Withdrawn JP2003040874A (ja) 1997-02-05 2002-06-04 逆溶媒を使用する逆転写酵素阻害剤の結晶化方法
JP2010202879A Expired - Lifetime JP5295190B2 (ja) 1997-02-05 2010-09-10 逆溶媒を使用する逆転写酵素阻害剤の結晶化方法
JP2013089216A Pending JP2013139484A (ja) 1997-02-05 2013-04-22 逆溶媒を使用する逆転写酵素阻害剤の結晶化方法
JP2015146631A Expired - Lifetime JP6126172B2 (ja) 1997-02-05 2015-07-24 逆溶媒を使用する逆転写酵素阻害剤の結晶化方法
JP2017002745A Pending JP2017061575A (ja) 1997-02-05 2017-01-11 逆溶媒を使用する逆転写酵素阻害剤の結晶化方法

Family Applications After (5)

Application Number Title Priority Date Filing Date
JP2002163198A Withdrawn JP2003040874A (ja) 1997-02-05 2002-06-04 逆溶媒を使用する逆転写酵素阻害剤の結晶化方法
JP2010202879A Expired - Lifetime JP5295190B2 (ja) 1997-02-05 2010-09-10 逆溶媒を使用する逆転写酵素阻害剤の結晶化方法
JP2013089216A Pending JP2013139484A (ja) 1997-02-05 2013-04-22 逆溶媒を使用する逆転写酵素阻害剤の結晶化方法
JP2015146631A Expired - Lifetime JP6126172B2 (ja) 1997-02-05 2015-07-24 逆溶媒を使用する逆転写酵素阻害剤の結晶化方法
JP2017002745A Pending JP2017061575A (ja) 1997-02-05 2017-01-11 逆溶媒を使用する逆転写酵素阻害剤の結晶化方法

Country Status (18)

Country Link
EP (1) EP0975609B1 (https=)
JP (6) JP3418626B2 (https=)
KR (1) KR100573192B1 (https=)
CN (2) CN1073991C (https=)
AT (1) ATE486065T1 (https=)
AU (1) AU738545C (https=)
CA (1) CA2279198C (https=)
CZ (2) CZ297535B6 (https=)
DE (1) DE69841972D1 (https=)
EA (1) EA001805B1 (https=)
EE (1) EE03827B1 (https=)
HU (1) HU229087B1 (https=)
IL (1) IL130715A (https=)
NO (1) NO320128B1 (https=)
NZ (1) NZ336510A (https=)
PL (1) PL197740B1 (https=)
SK (1) SK284935B6 (https=)
WO (1) WO1998033782A1 (https=)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2015205914A (ja) * 1997-02-05 2015-11-19 メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． 逆溶媒を使用する逆転写酵素阻害剤の結晶化方法

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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
US8318930B2 (en) * 2007-12-24 2012-11-27 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
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
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
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
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
US12365689B2 (en) 2015-10-16 2025-07-22 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
SG10201913990RA (en) 2015-10-16 2020-03-30 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

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US5665720A (en) * 1992-08-07 1997-09-09 Merck & Co., Inc. Benzoxazinones as inhibitors of HIV reverse transcriptase
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
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
HU229087B1 (en) * 1997-02-05 2013-07-29 Merck Sharp & Dohme Process for the crystallization of a reverse transcriptase inhibitor using an anti-solvent
AU6876898A (en) * 1997-04-07 1998-10-30 Du Pont Pharmaceuticals Company Asymmetric synthesis of benzoxazinones via new intermediates

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ＴＨＯＭＰＳＯＮ，Ａ．Ｓ．，ｅｔ ａｌ．，"Ｕｓｅ ｏｆ ａｎ Ｅｐｈｅｄｒｉｎｅ Ａｌｋｏ

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2015205914A (ja) * 1997-02-05 2015-11-19 メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． 逆溶媒を使用する逆転写酵素阻害剤の結晶化方法

Also Published As

Publication number Publication date
CA2279198C (en) 2009-04-14
JP2013139484A (ja) 2013-07-18
CN1073991C (zh) 2001-10-31
CN1385425A (zh) 2002-12-18
JP6126172B2 (ja) 2017-05-10
NZ336510A (en) 2001-04-27
JP2015205914A (ja) 2015-11-19
CZ304186B6 (cs) 2013-12-11
CA2279198A1 (en) 1998-08-06
IL130715A (en) 2003-07-31
HU229087B1 (en) 2013-07-29
NO993779D0 (no) 1999-08-04
EA001805B1 (ru) 2001-08-27
ATE486065T1 (de) 2010-11-15
EP0975609A1 (en) 2000-02-02
EA199900720A1 (ru) 2000-04-24
WO1998033782A1 (en) 1998-08-06
PL197740B1 (pl) 2008-04-30
CZ297535B6 (cs) 2007-01-03
PL334478A1 (en) 2000-02-28
CN1191242C (zh) 2005-03-02
JP5295190B2 (ja) 2013-09-18
DE69841972D1 (de) 2010-12-09
JP2000507972A (ja) 2000-06-27
NO320128B1 (no) 2005-10-31
EP0975609A4 (en) 2001-02-21
JP2003040874A (ja) 2003-02-13
CZ276599A3 (cs) 2000-02-16
EE03827B1 (et) 2002-08-15
NO993779L (no) 1999-10-05
SK284935B6 (sk) 2006-02-02
EE9900341A (et) 2000-02-15
HUP0001313A3 (en) 2002-12-28
HUP0001313A2 (hu) 2000-10-28
AU738545B2 (en) 2001-09-20
KR100573192B1 (ko) 2006-04-24
AU738545C (en) 2004-06-17
JP2017061575A (ja) 2017-03-30
CN1246113A (zh) 2000-03-01
JP2011006472A (ja) 2011-01-13
KR20000070735A (ko) 2000-11-25
AU6263298A (en) 1998-08-25
IL130715A0 (en) 2000-06-01
EP0975609B1 (en) 2010-10-27
SK105599A3 (en) 2000-05-16

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