AU2001234943A1 - A method for synthesizing leflunomide - Google Patents

A method for synthesizing leflunomide

Info

Publication number
AU2001234943A1
AU2001234943A1 AU2001234943A AU3494301A AU2001234943A1 AU 2001234943 A1 AU2001234943 A1 AU 2001234943A1 AU 2001234943 A AU2001234943 A AU 2001234943A AU 3494301 A AU3494301 A AU 3494301A AU 2001234943 A1 AU2001234943 A1 AU 2001234943A1
Authority
AU
Australia
Prior art keywords
leflunomide
methylisoxazole
carboxylic acid
trifluoromethylphenyl
acid chloride
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.)
Abandoned
Application number
AU2001234943A
Other languages
English (en)
Inventor
Ilya Avrutov
Neomi Gershon
Anita Liberman
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.)
Teva Pharmaceutical Industries Ltd
Original Assignee
Teva Pharmaceutical Industries Ltd
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
Application filed by Teva Pharmaceutical Industries Ltd filed Critical Teva Pharmaceutical Industries Ltd
Publication of AU2001234943A1 publication Critical patent/AU2001234943A1/en
Abandoned legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
    • C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
    • C07D261/06—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
    • C07D261/10—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D261/18—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Dermatology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pain & Pain Management (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Otolaryngology (AREA)
  • Transplantation (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Emergency Medicine (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
AU2001234943A 2000-02-15 2001-02-08 A method for synthesizing leflunomide Abandoned AU2001234943A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US18263500P 2000-02-15 2000-02-15
US60182635 2000-02-15
PCT/US2001/004095 WO2001060363A1 (fr) 2000-02-15 2001-02-08 Procede permettant d'effectuer la synthese du leflunomide

Publications (1)

Publication Number Publication Date
AU2001234943A1 true AU2001234943A1 (en) 2001-08-27

Family

ID=22669359

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2001234943A Abandoned AU2001234943A1 (en) 2000-02-15 2001-02-08 A method for synthesizing leflunomide

Country Status (18)

Country Link
US (2) US6723855B2 (fr)
EP (1) EP1257270B1 (fr)
JP (1) JP2004500380A (fr)
KR (1) KR20020072312A (fr)
AT (1) ATE292966T1 (fr)
AU (1) AU2001234943A1 (fr)
CA (1) CA2400290A1 (fr)
CZ (1) CZ20023024A3 (fr)
DE (1) DE60110043T2 (fr)
ES (1) ES2237553T3 (fr)
HR (1) HRP20020671A2 (fr)
HU (1) HUP0301865A3 (fr)
IL (1) IL151196A0 (fr)
PL (1) PL366088A1 (fr)
SK (1) SK12992002A3 (fr)
WO (1) WO2001060363A1 (fr)
YU (1) YU61602A (fr)
ZA (1) ZA200206494B (fr)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0903345B1 (fr) * 1997-08-08 2000-10-04 Aventis Pharma Deutschland GmbH Forme cristalline de N-(4-trifluorométhylphényl)-5-méthylisoxazole-4-carboxamid
CA2397601A1 (fr) * 1999-12-16 2001-06-21 Teva Pharmaceutical Industries, Ltd. Nouveaux procedes de preparation d'une nouvelle forme cristalline de leflunomide et nouvelle forme cristalline de leflunomide
GB0123571D0 (en) * 2001-04-05 2001-11-21 Aventis Pharm Prod Inc Use of (Z)-2-cyano-3-hydroxy-but-2-enoic acid-(4'-trifluoromethylphenyl)-amide for treating multiple sclerosis
US20030139606A1 (en) * 2001-11-09 2003-07-24 Ray Anup Kumar Process for preparing 5-methylisoxazole-4-carboxylic- (4'-trifluoromethyl)-anilide
JP4776537B2 (ja) * 2003-05-27 2011-09-21 ロベルト・ペール・ヘーガークヴィスト 糖尿病処置のためのチロシンキナーゼ阻害剤の使用
AU2003300692A1 (en) * 2003-10-30 2005-05-19 Lupin Ltd. Stable formulations of ace inhibitors and methods for preparation thereof
US20060024376A1 (en) * 2004-07-30 2006-02-02 The University Of Chicago Methods and compositions for reducing toxicity associated with leflunomide treatment
DE102005017592A1 (de) * 2005-04-16 2006-10-19 Lindner, Jürgen, Dr. med. Darreichungsformen und Kombinationspräparate von Pyrimidinbiosyntheseinhibitoren zur Erzielung zusätzlicher Wirkungen auf das Immunsystem
WO2007086076A2 (fr) * 2006-01-24 2007-08-02 Unichem Laboratories Limited Procede ameliore de preparation de leflunomide
CN101817797B (zh) * 2009-02-26 2013-04-10 江苏亚邦爱普森药业有限公司 高纯度3-甲基-n-[4-(三氟甲基)苯基]-4-异噁唑甲酰胺的合成方法
NZ617025A (en) 2009-09-18 2014-03-28 Sanofi Sa (z)-2-cyano-3-hydroxy-but-2-enoic acid-(4’-trifluormethylphenyl)-amide tablet formulations with improved stability
CN102002009B (zh) * 2010-10-18 2012-11-07 齐鲁制药有限公司 一种5-甲基异恶唑-4-甲酰氯的制备方法
KR20180018697A (ko) 2015-06-17 2018-02-21 바이오콘 리미티드 테리플루노미드의 신규한 제조 공정
JOP20190207A1 (ar) 2017-03-14 2019-09-10 Actelion Pharmaceuticals Ltd تركيبة صيدلانية تشتمل على بونيسيمود

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2854439A1 (de) 1978-12-16 1980-07-03 Hoechst Ag Ein isoxazolderivat, verfahren zu seiner herstellung, diese verbindung enthaltende mittel und verwendung
GB8619432D0 (en) 1986-08-08 1986-09-17 Lilly Industries Ltd Pharmaceutical compounds
BR9008022A (pt) * 1990-05-18 1993-04-06 Hoechst Ag Amida de acido isoxazol-4-carboxilico e amidas de acido hidroxialquilideno-cianoacetico,medicamentos contendo estes compostos e sua aplicacao
ATE174218T1 (de) 1993-01-08 1998-12-15 Hoechst Ag Verwendung von leflunomid zur hemmung von interleukin 1 beta
US5610173A (en) 1994-01-07 1997-03-11 Sugen, Inc. Formulations for lipophilic compounds
EP0903345B1 (fr) * 1997-08-08 2000-10-04 Aventis Pharma Deutschland GmbH Forme cristalline de N-(4-trifluorométhylphényl)-5-méthylisoxazole-4-carboxamid
DE19908527C2 (de) * 1999-02-26 2001-08-30 Aventis Pharma Gmbh Verfahren zur Kristallisation von N-(4-Trifluormethylphenyl)-5-methyl-isoxazol-4-carboxamid
CA2397601A1 (fr) * 1999-12-16 2001-06-21 Teva Pharmaceutical Industries, Ltd. Nouveaux procedes de preparation d'une nouvelle forme cristalline de leflunomide et nouvelle forme cristalline de leflunomide

Also Published As

Publication number Publication date
HRP20020671A2 (en) 2004-12-31
HUP0301865A3 (en) 2005-12-28
YU61602A (sh) 2006-01-16
CZ20023024A3 (cs) 2003-05-14
DE60110043T2 (de) 2006-03-02
JP2004500380A (ja) 2004-01-08
WO2001060363A1 (fr) 2001-08-23
EP1257270A4 (fr) 2003-05-07
SK12992002A3 (sk) 2003-05-02
CA2400290A1 (fr) 2001-08-23
PL366088A1 (en) 2005-01-24
HUP0301865A2 (hu) 2003-09-29
US20040127532A1 (en) 2004-07-01
IL151196A0 (en) 2003-04-10
ZA200206494B (en) 2003-08-20
US6723855B2 (en) 2004-04-20
US20020022646A1 (en) 2002-02-21
DE60110043D1 (de) 2005-05-19
EP1257270B1 (fr) 2005-04-13
ES2237553T3 (es) 2005-08-01
ATE292966T1 (de) 2005-04-15
EP1257270A1 (fr) 2002-11-20
KR20020072312A (ko) 2002-09-14

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