KR20020067545A - 레플루노마이드의 신규 제조 방법 및 이의 신규 결정형 - Google Patents

레플루노마이드의 신규 제조 방법 및 이의 신규 결정형 Download PDF

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Publication number
KR20020067545A
KR20020067545A KR1020027007575A KR20027007575A KR20020067545A KR 20020067545 A KR20020067545 A KR 20020067545A KR 1020027007575 A KR1020027007575 A KR 1020027007575A KR 20027007575 A KR20027007575 A KR 20027007575A KR 20020067545 A KR20020067545 A KR 20020067545A
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KR
South Korea
Prior art keywords
leflunomide
iii
solvent
type
solution
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
KR1020027007575A
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English (en)
Korean (ko)
Inventor
아브루토브일야
거손네오미
아론힘주디스
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.)
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Publication date
Application filed by 테바 파마슈티컬 인더스트리즈 리미티드 filed Critical 테바 파마슈티컬 인더스트리즈 리미티드
Publication of KR20020067545A publication Critical patent/KR20020067545A/ko
Ceased legal-status Critical Current

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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]

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  • 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)
KR1020027007575A 1999-12-16 2000-12-14 레플루노마이드의 신규 제조 방법 및 이의 신규 결정형 Ceased KR20020067545A (ko)

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
US17123799P 1999-12-16 1999-12-16
US17122899P 1999-12-16 1999-12-16
US60/171,228 1999-12-16
US60/171,237 1999-12-16
US18264700P 2000-02-15 2000-02-15
US60/182,647 2000-02-15
US20241600P 2000-05-08 2000-05-08
US60/202,416 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
KR20020067545A true KR20020067545A (ko) 2002-08-22

Family

ID=27496942

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020027007575A Ceased KR20020067545A (ko) 1999-12-16 2000-12-14 레플루노마이드의 신규 제조 방법 및 이의 신규 결정형

Country Status (15)

Country Link
US (3) US6610718B2 (https=)
EP (1) EP1242077A4 (https=)
JP (1) JP2003517011A (https=)
KR (1) KR20020067545A (https=)
CN (1) CN1411373A (https=)
AU (1) AU779931B2 (https=)
CA (1) CA2397601A1 (https=)
CZ (1) CZ20022000A3 (https=)
HR (2) HRP20050176A2 (https=)
HU (1) HUP0204069A3 (https=)
IL (1) IL149792A0 (https=)
PL (1) PL356243A1 (https=)
SK (1) SK8332002A3 (https=)
WO (1) WO2001043742A1 (https=)
YU (1) YU45102A (https=)

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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
WO2001051089A1 (de) * 2000-01-13 2001-07-19 Merck Patent Gmbh Pharmazeutische zubereitungen enthaltend 2-pyrrolidon als lösungsvermittler
CA2400290A1 (en) * 2000-02-15 2001-08-23 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
US8664390B2 (en) 2007-06-29 2014-03-04 Generics (Uk) Limited Process for the introduction of hydroxyethoxy side chain in bosentan
JP2011500780A (ja) 2007-10-24 2011-01-06 ジェネリクス・（ユーケー）・リミテッド 新規結晶形
JP5683276B2 (ja) 2008-02-08 2015-03-11 ジェネリクス・［ユーケー］・リミテッド ボセンタンの製造方法
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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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
DE59010701D1 (de) * 1990-05-18 1997-05-22 Hoechst Ag Isoxazol-4-carbonsäureamide und hydroxyalkyliden-cyanessigsäureamide, diese verbindungen enthaltende arzneimittel und deren verwendung
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
ATE196764T1 (de) * 1997-08-08 2000-10-15 Aventis Pharma Gmbh Kristallform von 5-methylisoxazol-4-carbonsäure- (4-trifluormethyl)-anilid
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
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CA2377278C (en) * 1999-06-25 2010-03-23 Vertex Pharmaceuticals Incorporated Prodrugs of carbamate inhibitors of impdh
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
CA2400290A1 (en) * 2000-02-15 2001-08-23 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
AU2001284891A1 (en) * 2000-08-14 2002-02-25 Teva Pharmaceutical Industries Ltd. Micronized leflunomide
EP1401801B1 (en) * 2000-08-24 2006-11-02 The University Of Tennessee Research Corporation 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
CA2535346A1 (en) * 2003-08-13 2005-03-03 Medtronic, Inc. Active agent delivery systems, including a single layer of a miscible polymer blend, medical devices, and methods
US20050064005A1 (en) * 2003-08-13 2005-03-24 Dinh Thomas Q. Active agent delivery systems including a miscible polymer blend, medical devices, and methods
WO2005023201A2 (en) * 2003-09-09 2005-03-17 Medarex, Inc. Methods for treating rheumatoid arthritis

Also Published As

Publication number Publication date
HRP20020521A2 (en) 2004-08-31
IL149792A0 (en) 2002-11-10
HRP20050176A2 (en) 2005-08-31
US20010031878A1 (en) 2001-10-18
US6610718B2 (en) 2003-08-26
EP1242077A4 (en) 2006-01-04
AU779931B2 (en) 2005-02-17
HUP0204069A3 (en) 2005-01-28
CN1411373A (zh) 2003-04-16
CZ20022000A3 (cs) 2003-02-12
US20030203952A1 (en) 2003-10-30
WO2001043742A1 (en) 2001-06-21
PL356243A1 (en) 2004-06-28
JP2003517011A (ja) 2003-05-20
AU2578801A (en) 2001-06-25
YU45102A (sh) 2006-01-16
US20050004191A1 (en) 2005-01-06
HUP0204069A2 (hu) 2003-04-28
SK8332002A3 (en) 2003-04-01
US6806373B2 (en) 2004-10-19
CA2397601A1 (en) 2001-06-21
EP1242077A1 (en) 2002-09-25

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