CN1411373A - 制备来氟米特的新方法和新晶形的来氟米特 - Google Patents

制备来氟米特的新方法和新晶形的来氟米特 Download PDF

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Publication number
CN1411373A
CN1411373A CN00817283A CN00817283A CN1411373A CN 1411373 A CN1411373 A CN 1411373A CN 00817283 A CN00817283 A CN 00817283A CN 00817283 A CN00817283 A CN 00817283A CN 1411373 A CN1411373 A CN 1411373A
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CN
China
Prior art keywords
leflunomide
solvent
iii
crystals
type
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.)
Pending
Application number
CN00817283A
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English (en)
Chinese (zh)
Inventor
I·阿夫鲁托夫
N·格尔雄
J·阿伦希梅
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Teva Pharmaceutical Industries Ltd
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Teva Pharmaceutical Industries Ltd
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 Pharmaceutical Industries Ltd filed Critical Teva Pharmaceutical Industries Ltd
Publication of CN1411373A publication Critical patent/CN1411373A/zh
Pending legal-status Critical Current

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    • 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)
  • 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)
CN00817283A 1999-12-16 2000-12-14 制备来氟米特的新方法和新晶形的来氟米特 Pending CN1411373A (zh)

Applications Claiming Priority (8)

Application Number Priority Date Filing Date Title
US17123799P 1999-12-16 1999-12-16
US17122899P 1999-12-16 1999-12-16
US60/171,237 1999-12-16
US60/171,228 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

Publications (1)

Publication Number Publication Date
CN1411373A true CN1411373A (zh) 2003-04-16

Family

ID=27496942

Family Applications (1)

Application Number Title Priority Date Filing Date
CN00817283A Pending CN1411373A (zh) 1999-12-16 2000-12-14 制备来氟米特的新方法和新晶形的来氟米特

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)

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008040149A1 (en) * 2006-09-05 2008-04-10 Dexian Dou Composition and method for treating immune-mediated skin disorders
CN101817797A (zh) * 2009-02-26 2010-09-01 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
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
CN112898215A (zh) * 2021-02-04 2021-06-04 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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DE59801792D1 (de) * 1997-08-08 2001-11-22 Aventis Pharma Gmbh Kristallform von N-(4-Trifluormethylphenyl)-5-methylisoxazol-4-carbonsäureamid
PL356243A1 (en) * 1999-12-16 2004-06-28 Teva Pharmaceuticals Industries Ltd. Novel processes for making- and a new crystalline form of- leflunomide
WO2001051089A1 (de) * 2000-01-13 2001-07-19 Merck Patent Gmbh Pharmazeutische zubereitungen enthaltend 2-pyrrolidon als lösungsvermittler
DE60110043T2 (de) * 2000-02-15 2006-03-02 Teva Pharmaceutical Industries Ltd. Methode zur synthetisierung von leflunomid
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
WO2009004374A1 (en) 2007-06-29 2009-01-08 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
ES2650247T3 (es) 2008-02-08 2018-01-17 Generics [Uk] Limited Procedimiento de preparación del bosentán
JP2012507497A (ja) 2008-11-03 2012-03-29 ジェネリクス・（ユーケー）・リミテッド ボセンタンおよび関連物質のｈｐｌｃ分析方法、ならびに参照スタンダードまたはマーカーとしてのこれら物質の使用
TWI846166B (zh) 2013-11-15 2024-06-21 美商阿克比治療有限公司 {[5-(3-氯苯基)-3-羥基吡啶-2-羰基]胺基}乙酸之固體型式，其組合物及用途
US11801232B2 (en) * 2019-11-27 2023-10-31 Yale University Targeting of ARID1A-deficient cancers by inhibiting de novo pyrimidine synthesis pathway

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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
RU2142937C1 (ru) * 1990-05-18 1999-12-20 Хехст АГ Амиды органических кислот, способ их получения и фармацевтическая композиция
US5610173A (en) * 1994-01-07 1997-03-11 Sugen, Inc. Formulations for lipophilic compounds
US5700823A (en) * 1994-01-07 1997-12-23 Sugen, Inc. Treatment of platelet derived growth factor related disorders such as cancers
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
DE59801792D1 (de) * 1997-08-08 2001-11-22 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
CA2377278C (en) * 1999-06-25 2010-03-23 Vertex Pharmaceuticals Incorporated Prodrugs of carbamate inhibitors of impdh
PL356243A1 (en) * 1999-12-16 2004-06-28 Teva Pharmaceuticals Industries Ltd. Novel processes for making- and a new crystalline form of- leflunomide
DE60110043T2 (de) * 2000-02-15 2006-03-02 Teva Pharmaceutical Industries Ltd. Methode zur synthetisierung von leflunomid
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
ES2321933T3 (es) * 2000-08-24 2009-06-15 University Of Tennessee Research Foundation Moduladores selectivos del receptor de androgeno y metodos de uso de los mismos.
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
WO2005018702A2 (en) * 2003-08-13 2005-03-03 Medtronic, Inc. Active agent delivery systems including a miscible polymer blend, medical devices, and methods
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
WO2005023201A2 (en) * 2003-09-09 2005-03-17 Medarex, Inc. Methods for treating rheumatoid arthritis

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008040149A1 (en) * 2006-09-05 2008-04-10 Dexian Dou Composition and method for treating immune-mediated skin disorders
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
CN101817797A (zh) * 2009-02-26 2010-09-01 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
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
CN112898215A (zh) * 2021-02-04 2021-06-04 美罗药业股份有限公司 一种来氟米特晶型i的制备方法

Also Published As

Publication number Publication date
US20030203952A1 (en) 2003-10-30
US6610718B2 (en) 2003-08-26
AU779931B2 (en) 2005-02-17
IL149792A0 (en) 2002-11-10
CZ20022000A3 (cs) 2003-02-12
HRP20020521A2 (en) 2004-08-31
SK8332002A3 (en) 2003-04-01
US20050004191A1 (en) 2005-01-06
WO2001043742A1 (en) 2001-06-21
EP1242077A1 (en) 2002-09-25
HUP0204069A2 (hu) 2003-04-28
EP1242077A4 (en) 2006-01-04
US6806373B2 (en) 2004-10-19
HUP0204069A3 (en) 2005-01-28
PL356243A1 (en) 2004-06-28
AU2578801A (en) 2001-06-25
KR20020067545A (ko) 2002-08-22
US20010031878A1 (en) 2001-10-18
CA2397601A1 (en) 2001-06-21
HRP20050176A2 (en) 2005-08-31
YU45102A (sh) 2006-01-16
JP2003517011A (ja) 2003-05-20

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C06 Publication
PB01 Publication
C02 Deemed withdrawal of patent application after publication (patent law 2001)
WD01 Invention patent application deemed withdrawn after publication