HRP20020521A2 - Novel processes for making - and a new crystalline form of - leflunomide - Google Patents

Novel processes for making - and a new crystalline form of - leflunomide Download PDF

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Publication number
HRP20020521A2
HRP20020521A2 HR20020521A HRP20020521A HRP20020521A2 HR P20020521 A2 HRP20020521 A2 HR P20020521A2 HR 20020521 A HR20020521 A HR 20020521A HR P20020521 A HRP20020521 A HR P20020521A HR P20020521 A2 HRP20020521 A2 HR P20020521A2
Authority
HR
Croatia
Prior art keywords
leflunomide
solvent
form iii
crystals
solution
Prior art date
Application number
HR20020521A
Other languages
English (en)
Croatian (hr)
Inventor
Neomi Gershon
Ilya Avrutov
Judith Aronhime
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 HRP20020521A2 publication Critical patent/HRP20020521A2/hr

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
    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Rheumatology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Immunology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Medicinal Preparation (AREA)
HR20020521A 1999-12-16 2000-12-14 Novel processes for making - and a new crystalline form of - leflunomide HRP20020521A2 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US17123799P 1999-12-16 1999-12-16
US17122899P 1999-12-16 1999-12-16
US18264700P 2000-02-15 2000-02-15
US20241600P 2000-05-08 2000-05-08
PCT/US2000/033866 WO2001043742A1 (en) 1999-12-16 2000-12-14 Novel processes for making- and a new crystalline form of- leflunomide

Publications (1)

Publication Number Publication Date
HRP20020521A2 true HRP20020521A2 (en) 2004-08-31

Family

ID=27496942

Family Applications (2)

Application Number Title Priority Date Filing Date
HR20020521A HRP20020521A2 (en) 1999-12-16 2000-12-14 Novel processes for making - and a new crystalline form of - leflunomide
HR20050176A HRP20050176A2 (en) 1999-12-16 2000-12-14 Novel processes for making - and a new crystalline form of-leflunomide

Family Applications After (1)

Application Number Title Priority Date Filing Date
HR20050176A HRP20050176A2 (en) 1999-12-16 2000-12-14 Novel processes for making - and a new crystalline form of-leflunomide

Country Status (15)

Country Link
US (3) US6610718B2 (enExample)
EP (1) EP1242077A4 (enExample)
JP (1) JP2003517011A (enExample)
KR (1) KR20020067545A (enExample)
CN (1) CN1411373A (enExample)
AU (1) AU779931B2 (enExample)
CA (1) CA2397601A1 (enExample)
CZ (1) CZ20022000A3 (enExample)
HR (2) HRP20020521A2 (enExample)
HU (1) HUP0204069A3 (enExample)
IL (1) IL149792A0 (enExample)
PL (1) PL356243A1 (enExample)
SK (1) SK8332002A3 (enExample)
WO (1) WO2001043742A1 (enExample)
YU (1) YU45102A (enExample)

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ES2150808T3 (es) * 1997-08-08 2000-12-01 Aventis Pharma Gmbh Forma cristalina de (4-trifluorometil)-anilida de acido 5-metilisoxazol-4-carboxilico.
AU779931B2 (en) * 1999-12-16 2005-02-17 Teva Pharmaceutical Industries Ltd. Novel processes for making- and a new crystalline form of- leflunomide
AU2001228454A1 (en) * 2000-01-13 2001-07-24 Merck Patent G.M.B.H Pharmaceutical preparations containing 2-pyrrolidone as the dissolving intermediary
AU2001234943A1 (en) * 2000-02-15 2001-08-27 Teva Pharmaceutical Industries Ltd. A method for synthesizing leflunomide
US20050158371A1 (en) * 2002-02-12 2005-07-21 Sumitomo Pharmaceuticals Co., Ltd. Novel external agent
WO2006103506A1 (en) * 2005-03-31 2006-10-05 Ranbaxy Laboratories Limited Sertraline-containing pharmaceutical compositions and a process for preparation thereof
CN101563082A (zh) * 2006-09-05 2009-10-21 窦德献 治疗免疫介导性皮肤病的组合物和方法
CN101143834B (zh) * 2006-09-15 2010-09-08 欣凯医药化工中间体（上海）有限公司 N-(4-三氟甲基苯)-2-氰基-3-羟基丁烯酰胺钠盐的多晶型及其制备方法
WO2009004374A1 (en) 2007-06-29 2009-01-08 Generics [Uk] Limited Process for introduction of hydroxyethoxy side chain in bosentan
US8530488B2 (en) 2007-10-24 2013-09-10 Generics [Uk] Limited Crystalline forms of bosentan
ES2650247T3 (es) 2008-02-08 2018-01-17 Generics [Uk] Limited Procedimiento de preparación del bosentán
WO2010061210A1 (en) 2008-11-03 2010-06-03 Generics [Uk] Limited Hplc method for the analysis of bosentan and related substances and use of these substances as reference standards and markers
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
AR099354A1 (es) 2013-11-15 2016-07-20 Akebia Therapeutics Inc Formas sólidas de ácido {[5-(3-clorofenil)-3-hidroxipiridin-2-carbonil]amino}acético, composiciones, y sus usos
US11801232B2 (en) * 2019-11-27 2023-10-31 Yale University Targeting of ARID1A-deficient cancers by inhibiting de novo pyrimidine synthesis pathway
CN112898215B (zh) * 2021-02-04 2022-11-08 美罗药业股份有限公司 一种来氟米特晶型i的制备方法

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DE2854439A1 (de) * 1978-12-16 1980-07-03 Hoechst Ag Ein isoxazolderivat, verfahren zu seiner herstellung, diese verbindung enthaltende mittel und verwendung
US5268382A (en) * 1985-09-27 1993-12-07 Hoechst Aktiengesellschaft Medicaments to combat autoimmune diseases, in particular systemic lupus erythematosus
DE3534440A1 (de) * 1985-09-27 1987-04-02 Hoechst Ag Arzneimittel gegen chronische graft-versus-host-krankheiten sowie gegen autoimmunerkrankungen, insbesondere systemischen lupus erythematodes
GB8619432D0 (en) * 1986-08-08 1986-09-17 Lilly Industries Ltd Pharmaceutical compounds
JP2995086B2 (ja) * 1990-05-18 1999-12-27 ヘキスト・アクチエンゲゼルシヤフト イソオキサゾール−４−カルボキサミド類およびヒドロキシアルキリデンシアノアセトアミド類を含有する製剤
US5700823A (en) * 1994-01-07 1997-12-23 Sugen, Inc. Treatment of platelet derived growth factor related disorders such as cancers
US5610173A (en) * 1994-01-07 1997-03-11 Sugen, Inc. Formulations for lipophilic compounds
DE19610955A1 (de) * 1996-03-20 1997-09-25 Hoechst Ag Kombinationspräparat, enthaltend 5-Methylisoxazol-4-carbonsäure-(4-trifluormethyl)- anilid und N-(4-Trifluormethylphenyl)-2-cyan-3- hydroxycrotonsäureamid
GB9624038D0 (en) * 1996-11-19 1997-01-08 Sandoz Ltd Organic compounds
DE19711800A1 (de) * 1997-03-21 1998-09-24 Hoechst Ag Verlängerung der Expression von transgenen Proteinen durch immunmodulierende Behandlung
ES2150808T3 (es) * 1997-08-08 2000-12-01 Aventis Pharma Gmbh Forma cristalina de (4-trifluorometil)-anilida de acido 5-metilisoxazol-4-carboxilico.
EP0933633A1 (en) * 1997-12-11 1999-08-04 Hoechst Marion Roussel Deutschland GmbH Process for obtaining L-dihydroorotic acid and use thereof
US7691890B2 (en) * 1998-03-11 2010-04-06 James W. Williams Anti-viral uses of leflunomide products
US6303652B1 (en) * 1998-08-21 2001-10-16 Hughes Institute BTK inhibitors and methods for their identification and use
US6248363B1 (en) * 1999-11-23 2001-06-19 Lipocine, Inc. Solid carriers for improved delivery of active ingredients in pharmaceutical compositions
DE19908527C2 (de) * 1999-02-26 2001-08-30 Aventis Pharma Gmbh Verfahren zur Kristallisation von N-(4-Trifluormethylphenyl)-5-methyl-isoxazol-4-carboxamid
PT1196414E (pt) * 1999-06-25 2003-12-31 Vertex Pharma Pro-farmacos de inibidores carbamato de impdh
AU779931B2 (en) * 1999-12-16 2005-02-17 Teva Pharmaceutical Industries Ltd. Novel processes for making- and a new crystalline form of- leflunomide
AU2001234943A1 (en) * 2000-02-15 2001-08-27 Teva Pharmaceutical Industries Ltd. A method for synthesizing leflunomide
AU2001251011A1 (en) * 2000-03-27 2001-10-08 The General Hospital Corporation Treatments for immune-mediated ear disorders
US20020077485A1 (en) * 2000-08-14 2002-06-20 Ilya Avrutov Micronized leflunomide
ATE344233T1 (de) * 2000-08-24 2006-11-15 Univ Tennessee Res Corp Selektive modulatoren des andro genrezeptors und methoden zu deren verwendung
JP4212278B2 (ja) * 2001-03-01 2009-01-21 日本たばこ産業株式会社 移植片拒絶反応抑制剤
US20040229849A1 (en) * 2002-09-24 2004-11-18 Jost-Price Edward Roydon Methods and reagents for the treatment of diseases and disorders associated with increased levels of proinflammatory cytokines
US20050064005A1 (en) * 2003-08-13 2005-03-24 Dinh Thomas Q. Active agent delivery systems including a miscible polymer blend, medical devices, and methods
US20050064038A1 (en) * 2003-08-13 2005-03-24 Dinh Thomas Q. Active agent delivery systems including a single layer of a miscible polymer blend, medical devices, and methods
US20050053600A1 (en) * 2003-09-09 2005-03-10 Lane Thomas E. Methods for treating rheumatoid arthritis

Also Published As

Publication number Publication date
PL356243A1 (en) 2004-06-28
US20010031878A1 (en) 2001-10-18
JP2003517011A (ja) 2003-05-20
YU45102A (sh) 2006-01-16
US6610718B2 (en) 2003-08-26
HRP20050176A2 (en) 2005-08-31
US20050004191A1 (en) 2005-01-06
HUP0204069A3 (en) 2005-01-28
SK8332002A3 (en) 2003-04-01
HUP0204069A2 (hu) 2003-04-28
EP1242077A4 (en) 2006-01-04
AU779931B2 (en) 2005-02-17
WO2001043742A1 (en) 2001-06-21
KR20020067545A (ko) 2002-08-22
IL149792A0 (en) 2002-11-10
AU2578801A (en) 2001-06-25
CA2397601A1 (en) 2001-06-21
US6806373B2 (en) 2004-10-19
CN1411373A (zh) 2003-04-16
US20030203952A1 (en) 2003-10-30
EP1242077A1 (en) 2002-09-25
CZ20022000A3 (cs) 2003-02-12

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