HRP20020671A2 - A method for synthesizing leflunomide - Google Patents

A method for synthesizing leflunomide Download PDF

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Publication number
HRP20020671A2
HRP20020671A2 HRP20020671A HRP20020671A2 HR P20020671 A2 HRP20020671 A2 HR P20020671A2 HR P20020671 A HRP20020671 A HR P20020671A HR P20020671 A2 HRP20020671 A2 HR P20020671A2
Authority
HR
Croatia
Prior art keywords
leflunomide
methylisoxazole
carboxylic acid
chloride
trifluoromethylphenyl
Prior art date
Application number
Other languages
English (en)
Croatian (hr)
Inventor
Ilya Avrutov
Neomi Gershon
Anita Liberman
Original Assignee
Teva Pharma
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 Pharma filed Critical Teva Pharma
Publication of HRP20020671A2 publication Critical patent/HRP20020671A2/hr

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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)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pain & Pain Management (AREA)
  • Transplantation (AREA)
  • Otolaryngology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Obesity (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)
HRP20020671 2000-02-15 2001-02-08 A method for synthesizing leflunomide HRP20020671A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US18263500P 2000-02-15 2000-02-15
PCT/US2001/004095 WO2001060363A1 (en) 2000-02-15 2001-02-08 A method for synthesizing leflunomide

Publications (1)

Publication Number Publication Date
HRP20020671A2 true HRP20020671A2 (en) 2004-12-31

Family

ID=22669359

Family Applications (1)

Application Number Title Priority Date Filing Date
HRP20020671 HRP20020671A2 (en) 2000-02-15 2001-02-08 A method for synthesizing leflunomide

Country Status (18)

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

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ATE207065T1 (de) * 1997-08-08 2001-11-15 Aventis Pharma Gmbh Kristallform von n-(4-trifluormethylphenyl)-5- methylisoxazol-4-carbonsäureamid
HUP0204069A3 (en) * 1999-12-16 2005-01-28 Teva Pharma Novel processes for making- and a new crystalline form of- leflunomide and pharmaceutical composition containing it
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
RU2365373C2 (ru) * 2003-05-27 2009-08-27 Роберт Пер Хэгерквист Применение ингибитора тирозинкиназы для лечения диабета
EP1694308A1 (en) * 2003-10-30 2006-08-30 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 (en) * 2006-01-24 2007-08-02 Unichem Laboratories Limited An improved process for preparation of 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
CA2772275A1 (en) 2009-09-18 2011-03-24 Sanofi (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
US10526279B2 (en) 2015-06-17 2020-01-07 Biocon Limited Process for the preparation of teriflunomide
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
AU649421B2 (en) * 1990-05-18 1994-05-26 Sanofi-Aventis Deutschland Gmbh Isoxazole-4-carboxamides and hydroxyalkylidene-cyanoacetamides, drugs containing these compounds and use of such drugs
ES2124800T3 (es) 1993-01-08 1999-02-16 Hoechst Ag Empleo de leflunomida para la inhibicion de interleuquina 1 beta.
US5610173A (en) 1994-01-07 1997-03-11 Sugen, Inc. Formulations for lipophilic compounds
ATE207065T1 (de) * 1997-08-08 2001-11-15 Aventis Pharma Gmbh Kristallform von n-(4-trifluormethylphenyl)-5- methylisoxazol-4-carbonsäureamid
DE19908527C2 (de) * 1999-02-26 2001-08-30 Aventis Pharma Gmbh Verfahren zur Kristallisation von N-(4-Trifluormethylphenyl)-5-methyl-isoxazol-4-carboxamid
HUP0204069A3 (en) * 1999-12-16 2005-01-28 Teva Pharma Novel processes for making- and a new crystalline form of- leflunomide and pharmaceutical composition containing it

Also Published As

Publication number Publication date
CZ20023024A3 (cs) 2003-05-14
WO2001060363A1 (en) 2001-08-23
AU2001234943A1 (en) 2001-08-27
IL151196A0 (en) 2003-04-10
YU61602A (sh) 2006-01-16
ES2237553T3 (es) 2005-08-01
PL366088A1 (en) 2005-01-24
DE60110043D1 (de) 2005-05-19
CA2400290A1 (en) 2001-08-23
KR20020072312A (ko) 2002-09-14
ZA200206494B (en) 2003-08-20
DE60110043T2 (de) 2006-03-02
EP1257270A1 (en) 2002-11-20
SK12992002A3 (sk) 2003-05-02
EP1257270A4 (en) 2003-05-07
US6723855B2 (en) 2004-04-20
US20040127532A1 (en) 2004-07-01
HUP0301865A2 (hu) 2003-09-29
US20020022646A1 (en) 2002-02-21
JP2004500380A (ja) 2004-01-08
HUP0301865A3 (en) 2005-12-28
EP1257270B1 (en) 2005-04-13
ATE292966T1 (de) 2005-04-15

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