SK8332002A3 - 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
SK8332002A3
SK8332002A3 SK833-2002A SK8332002A SK8332002A3 SK 8332002 A3 SK8332002 A3 SK 8332002A3 SK 8332002 A SK8332002 A SK 8332002A SK 8332002 A3 SK8332002 A3 SK 8332002A3
Authority
SK
Slovakia
Prior art keywords
leflunomide
solvent
form iii
solution
crystals
Prior art date
Application number
SK833-2002A
Other languages
English (en)
Slovak (sk)
Inventor
Ilya Avrutov
Neomi Gershon
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 SK8332002A3 publication Critical patent/SK8332002A3/sk

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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
    • 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)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Rheumatology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Physical Education & Sports Medicine (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)
SK833-2002A 1999-12-16 2000-12-14 Novel processes for making- and a new crystalline form of leflunomide SK8332002A3 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US17122899P 1999-12-16 1999-12-16
US17123799P 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
SK8332002A3 true SK8332002A3 (en) 2003-04-01

Family

ID=27496942

Family Applications (1)

Application Number Title Priority Date Filing Date
SK833-2002A SK8332002A3 (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 (ko)
EP (1) EP1242077A4 (ko)
JP (1) JP2003517011A (ko)
KR (1) KR20020067545A (ko)
CN (1) CN1411373A (ko)
AU (1) AU779931B2 (ko)
CA (1) CA2397601A1 (ko)
CZ (1) CZ20022000A3 (ko)
HR (2) HRP20020521A2 (ko)
HU (1) HUP0204069A3 (ko)
IL (1) IL149792A0 (ko)
PL (1) PL356243A1 (ko)
SK (1) SK8332002A3 (ko)
WO (1) WO2001043742A1 (ko)
YU (1) YU45102A (ko)

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ATE207065T1 (de) * 1997-08-08 2001-11-15 Aventis Pharma Gmbh Kristallform von n-(4-trifluormethylphenyl)-5- methylisoxazol-4-carbonsäureamid
CZ20022000A3 (cs) * 1999-12-16 2003-02-12 Teva Pharmaceuticals Industries Ltd. Způsoby přípravy a nová krystalická forma leflunomidu
EP1255565A1 (de) * 2000-01-13 2002-11-13 MERCK PATENT GmbH Pharmazeutische zubereitungen enthaltend 2-pyrrolidon als lösungsvermittler
EP1257270B1 (en) * 2000-02-15 2005-04-13 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
AU2008272685B2 (en) 2007-06-29 2013-04-18 Generics [Uk] Limited Process for introduction of hydroxyethoxy side chain in bosentan
CN101939303B (zh) 2007-10-24 2014-06-11 基因里克斯(英国)有限公司 波生坦的晶型
CN101939301B (zh) 2008-02-08 2016-07-06 基因里克斯(英国)有限公司 用于制备波生坦的方法
CA2741928A1 (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
CR20160222U (es) 2013-11-15 2016-08-26 Akebia Therapeutics Inc Formas solidas de acido { [ -(3- clorofenil) -3- hidroxipiridin -2-carbonil] amino} acetico, composiciones, y usos de las mismas
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
DE3534440A1 (de) * 1985-09-27 1987-04-02 Hoechst Ag Arzneimittel gegen chronische graft-versus-host-krankheiten sowie gegen autoimmunerkrankungen, insbesondere systemischen lupus erythematodes
US5268382A (en) * 1985-09-27 1993-12-07 Hoechst Aktiengesellschaft Medicaments to combat autoimmune diseases, in particular systemic lupus erythematosus
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
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
ATE207065T1 (de) 1997-08-08 2001-11-15 Aventis Pharma Gmbh Kristallform von n-(4-trifluormethylphenyl)-5- methylisoxazol-4-carbonsäureamid
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
ATE248835T1 (de) * 1999-06-25 2003-09-15 Vertex Pharma Prodrugs von impdh-inhibierenden carbamaten
CZ20022000A3 (cs) * 1999-12-16 2003-02-12 Teva Pharmaceuticals Industries Ltd. Způsoby přípravy a nová krystalická forma leflunomidu
EP1257270B1 (en) * 2000-02-15 2005-04-13 Teva Pharmaceutical Industries Ltd. A method for synthesizing leflunomide
WO2001072298A1 (en) * 2000-03-27 2001-10-04 The General Hospital Corporation Treatments for immune-mediated ear disorders
US20020077485A1 (en) * 2000-08-14 2002-06-20 Ilya Avrutov Micronized leflunomide
AU2001285230C1 (en) * 2000-08-24 2008-03-13 University Of Tennessee Research Foundation Selective androgen receptor modulators and methods of use thereof
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
JP2007502281A (ja) * 2003-08-13 2007-02-08 メドトロニック・インコーポレーテッド 混和性ポリマー配合物を含む活性剤放出系、医療機器、及び方法
JP2008511339A (ja) * 2003-08-13 2008-04-17 メドトロニック・インコーポレーテッド 相溶性ポリマーブレンドの単層を含む活性薬剤送達システム、医療用デバイス、及び方法
WO2005023201A2 (en) * 2003-09-09 2005-03-17 Medarex, Inc. Methods for treating rheumatoid arthritis

Also Published As

Publication number Publication date
HRP20050176A2 (en) 2005-08-31
HUP0204069A3 (en) 2005-01-28
US6610718B2 (en) 2003-08-26
US20050004191A1 (en) 2005-01-06
IL149792A0 (en) 2002-11-10
EP1242077A1 (en) 2002-09-25
CA2397601A1 (en) 2001-06-21
EP1242077A4 (en) 2006-01-04
PL356243A1 (en) 2004-06-28
HRP20020521A2 (en) 2004-08-31
US6806373B2 (en) 2004-10-19
HUP0204069A2 (hu) 2003-04-28
JP2003517011A (ja) 2003-05-20
US20030203952A1 (en) 2003-10-30
WO2001043742A1 (en) 2001-06-21
CN1411373A (zh) 2003-04-16
AU2578801A (en) 2001-06-25
KR20020067545A (ko) 2002-08-22
YU45102A (sh) 2006-01-16
CZ20022000A3 (cs) 2003-02-12
US20010031878A1 (en) 2001-10-18
AU779931B2 (en) 2005-02-17

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