KR20020072312A - 레플루노미드를 합성하는 방법 - Google Patents

레플루노미드를 합성하는 방법 Download PDF

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Publication number
KR20020072312A
KR20020072312A KR1020027010595A KR20027010595A KR20020072312A KR 20020072312 A KR20020072312 A KR 20020072312A KR 1020027010595 A KR1020027010595 A KR 1020027010595A KR 20027010595 A KR20027010595 A KR 20027010595A KR 20020072312 A KR20020072312 A KR 20020072312A
Authority
KR
South Korea
Prior art keywords
leflunomide
methylisoxazole
carboxylic acid
trifluoromethylphenyl
hydroxycrotonamide
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.)
Ceased
Application number
KR1020027010595A
Other languages
English (en)
Korean (ko)
Inventor
아브루토브일리야
게르손네오미
리베르만아니타
Original Assignee
테바 파마슈티컬 인더스트리즈 리미티드
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 테바 파마슈티컬 인더스트리즈 리미티드 filed Critical 테바 파마슈티컬 인더스트리즈 리미티드
Publication of KR20020072312A publication Critical patent/KR20020072312A/ko
Ceased 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)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Endocrinology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Emergency Medicine (AREA)
  • Ophthalmology & Optometry (AREA)
  • Dermatology (AREA)
  • Hematology (AREA)
  • Transplantation (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Otolaryngology (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)
KR1020027010595A 2000-02-15 2001-02-08 레플루노미드를 합성하는 방법 Ceased KR20020072312A (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US18263500P 2000-02-15 2000-02-15
US60/182,635 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
KR20020072312A true KR20020072312A (ko) 2002-09-14

Family

ID=22669359

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020027010595A Ceased KR20020072312A (ko) 2000-02-15 2001-02-08 레플루노미드를 합성하는 방법

Country Status (18)

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

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ATE196764T1 (de) * 1997-08-08 2000-10-15 Aventis Pharma Gmbh Kristallform von 5-methylisoxazol-4-carbonsäure- (4-trifluormethyl)-anilid
CN1411373A (zh) * 1999-12-16 2003-04-16 特瓦制药工业有限公司 制备来氟米特的新方法和新晶形的来氟米特
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
WO2003042193A1 (en) * 2001-11-09 2003-05-22 Geneva Pharmaceuticals, Inc. Process for preparing 5-methylisoxazole-4-carboxylic-(4'-trifluoromethyl)-anilide
CA2526594C (en) * 2003-05-27 2011-11-08 Robert Per Haegerkvist Use of tyrosine kinase inhibitors to treat diabetes
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
US20120172427A1 (en) 2009-09-18 2012-07-05 Sanofi (z)-2-cyano-3-hydroxy-but-2-enoic acid-(4'-trifluoromethylphenyl)-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
CA2989394C (en) * 2015-06-17 2023-08-01 Biocon Limited A novel 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
DE59010701D1 (de) * 1990-05-18 1997-05-22 Hoechst Ag Isoxazol-4-carbonsäureamide und hydroxyalkyliden-cyanessigsäureamide, diese verbindungen enthaltende arzneimittel und deren verwendung
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
ATE196764T1 (de) * 1997-08-08 2000-10-15 Aventis Pharma Gmbh Kristallform von 5-methylisoxazol-4-carbonsäure- (4-trifluormethyl)-anilid
DE19908527C2 (de) * 1999-02-26 2001-08-30 Aventis Pharma Gmbh Verfahren zur Kristallisation von N-(4-Trifluormethylphenyl)-5-methyl-isoxazol-4-carboxamid
CN1411373A (zh) * 1999-12-16 2003-04-16 特瓦制药工业有限公司 制备来氟米特的新方法和新晶形的来氟米特

Also Published As

Publication number Publication date
IL151196A0 (en) 2003-04-10
YU61602A (sh) 2006-01-16
HUP0301865A2 (hu) 2003-09-29
EP1257270A4 (en) 2003-05-07
PL366088A1 (en) 2005-01-24
EP1257270A1 (en) 2002-11-20
US6723855B2 (en) 2004-04-20
SK12992002A3 (sk) 2003-05-02
ZA200206494B (en) 2003-08-20
AU2001234943A1 (en) 2001-08-27
US20020022646A1 (en) 2002-02-21
CA2400290A1 (en) 2001-08-23
JP2004500380A (ja) 2004-01-08
DE60110043T2 (de) 2006-03-02
WO2001060363A1 (en) 2001-08-23
EP1257270B1 (en) 2005-04-13
HRP20020671A2 (en) 2004-12-31
DE60110043D1 (de) 2005-05-19
CZ20023024A3 (cs) 2003-05-14
HUP0301865A3 (en) 2005-12-28
US20040127532A1 (en) 2004-07-01
ATE292966T1 (de) 2005-04-15
ES2237553T3 (es) 2005-08-01

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