LU90466I2 - 5-methylisoxazole-4-acide carboxylique-4-trifluoromethylanilide (inn leflunomide)(arava) - Google Patents

5-methylisoxazole-4-acide carboxylique-4-trifluoromethylanilide (inn leflunomide)(arava)

Info

Publication number
LU90466I2
LU90466I2 LU90466C LU90466C LU90466I2 LU 90466 I2 LU90466 I2 LU 90466I2 LU 90466 C LU90466 C LU 90466C LU 90466 C LU90466 C LU 90466C LU 90466 I2 LU90466 I2 LU 90466I2
Authority
LU
Luxembourg
Prior art keywords
trifluoromethylanilide
arava
methylisoxazole
leflunomide
inn
Prior art date
Application number
LU90466C
Other languages
English (en)
Original Assignee
Hoechst Ag
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 Hoechst Ag filed Critical Hoechst Ag
Publication of LU90466I2 publication Critical patent/LU90466I2/fr

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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pulmonology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Chemical And Physical Treatments For Wood And The Like (AREA)
  • Lubricants (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
LU90466C 1978-12-16 1999-10-27 5-methylisoxazole-4-acide carboxylique-4-trifluoromethylanilide (inn leflunomide)(arava) LU90466I2 (fr)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE19782854439 DE2854439A1 (de) 1978-12-16 1978-12-16 Ein isoxazolderivat, verfahren zu seiner herstellung, diese verbindung enthaltende mittel und verwendung

Publications (1)

Publication Number Publication Date
LU90466I2 true LU90466I2 (fr) 2000-01-03

Family

ID=6057414

Family Applications (1)

Application Number Title Priority Date Filing Date
LU90466C LU90466I2 (fr) 1978-12-16 1999-10-27 5-methylisoxazole-4-acide carboxylique-4-trifluoromethylanilide (inn leflunomide)(arava)

Country Status (25)

Country Link
US (2) US4284786A (fr)
EP (1) EP0013376B1 (fr)
JP (1) JPS5583767A (fr)
AR (2) AR222680A1 (fr)
AT (1) ATE1067T1 (fr)
AU (1) AU529341B2 (fr)
BG (1) BG60764B2 (fr)
CA (1) CA1129867A (fr)
DE (2) DE2854439A1 (fr)
DK (1) DK149886C (fr)
EG (1) EG13926A (fr)
ES (2) ES486758A1 (fr)
FI (1) FI64154C (fr)
GR (1) GR72731B (fr)
HU (1) HU178015B (fr)
IE (1) IE49126B1 (fr)
IL (1) IL58951A (fr)
LU (1) LU90466I2 (fr)
MX (2) MX6174E (fr)
NL (1) NL990037I1 (fr)
NO (1) NO148925C (fr)
NZ (1) NZ192400A (fr)
PH (1) PH16627A (fr)
PT (1) PT70596A (fr)
ZA (1) ZA796793B (fr)

Families Citing this family (60)

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DE3247454A1 (de) * 1982-12-22 1984-06-28 Laboratorios Bago S.A., Buenos Aires Substituierte 3-phenyl-5-methyl-isoxazol-4-carboxy-anilide, verfahren zu ihrer herstellung und diese verbindungen enthaltende arzneimittel
FR2538806B1 (fr) * 1982-12-30 1986-02-21 Bago Sa Labor Composes phenyl-3 methyl isoxazole-5 carboxy-4 anilides substitues, actifs therapeutiquement contre l'inflammation et la douleur
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
US4935434A (en) * 1988-01-26 1990-06-19 Bristol-Myers Company Antiarthritic isoxazole-4-carboxamides
US5258397A (en) * 1988-11-30 1993-11-02 Novapharme 3-Isoxazoyl derivatives endowed with anticonvulsant activity, procedure for their preparation and their pharmaceutical compositions
FR2662692B1 (fr) * 1990-05-30 1995-04-28 Novapharme Derives heterocycliques doues d'activite anticonvulsivante, procede de preparation et composition pharmaceutique.
DD297328A5 (de) * 1989-08-18 1992-01-09 �������@���������k���Kk�� 5-methyl-isoxalol-4-carbonsaeureanilide und 2 hydroxyethyliden-cyanoessigsaeureanilide zur behandlung von augenerkrankungen
US5583150A (en) * 1989-08-18 1996-12-10 Alcon Laboratories, Inc. 5-methyl-isoxazole-4-carboxylic acid anilides and 2-hydroxyethylidene-cyano acetic anilides for the treatment of ocular diseases
US5001124A (en) * 1990-02-02 1991-03-19 Syntex (U.S.A.) Inc. 4-isoxazolecarboxamide derivatives
US5108999A (en) * 1990-02-02 1992-04-28 Syntex (U.S.A.) Inc. 4-isoxazolecarboxamide derivatives
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
DE4127737A1 (de) * 1991-08-22 1993-02-25 Hoechst Ag Arzneimittel zur behandlung von abstossungsreaktionen bei organverpflanzungen
US6133301A (en) * 1991-08-22 2000-10-17 Aventis Pharma Deutschland Gmbh Pharmaceuticals for the treatment of rejection reactions in organ transplantations
EP0607777B1 (fr) * 1993-01-08 1998-12-09 Hoechst Aktiengesellschaft Utilisation de leflunomid pour inhiber interleukin 8
DE59407413D1 (de) * 1993-01-08 1999-01-21 Hoechst Ag Verwendung von Leflunomid zur Hemmung von Interleukin 1 beta
ATE174219T1 (de) * 1993-01-08 1998-12-15 Hoechst Ag Verwendung von leflunomid zur hemmung von tumornekrosefaktor alpha
DE59407412D1 (de) * 1993-01-08 1999-01-21 Hoechst Ag Verwendung von Leflunomid zur Hemmung von Interleukin 1 alpha
TW314467B (fr) * 1993-03-31 1997-09-01 Hoechst Ag
DE4323636A1 (de) * 1993-07-15 1995-01-19 Hoechst Ag Arzneistoffzubereitungen aus umhüllten, schwerstwasserlöslichen Arzneistoffen für Inhalationsarzneiformen und Verfahren zu ihrer Herstellung
LT3589B (en) 1993-11-30 1995-12-27 Hoechst Ag Using of known combination for treatment of rejection reaction by transplantation of organs
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
US6335356B1 (en) 1994-01-07 2002-01-01 Sugen, Inc. Method of treating a patient by parenteral administration of a lipophilic compound
US5519042A (en) * 1994-01-13 1996-05-21 Hoechst Aktiengesellschaft Method of treating hyperproliferative vascular disease
US5624946A (en) * 1994-07-05 1997-04-29 Williams; James Use of leflunomide to control and reverse chronic allograft rejection
AU695907B2 (en) * 1994-10-17 1998-08-27 Hoechst Pharmaceuticals & Chemicals K.K. Pharmaceutical composition for prophylaxis and treatment of type I allergic diseases
US5721277A (en) * 1995-04-21 1998-02-24 Sugen, Inc. Compounds and methods for inhibiting hyper-proliferative cell growth
US6331555B1 (en) 1995-06-01 2001-12-18 University Of California Treatment of platelet derived growth factor related disorders such as cancers
DE19539638A1 (de) * 1995-10-25 1997-04-30 Hoechst Ag Die Verwendung von Isoxazol- und Crotonsäureamidderivaten zur Behandlung von Krebserkrankungen
DE19702988A1 (de) * 1997-01-28 1998-07-30 Hoechst Ag Isoxazol- und Crotonsäureamidderivate und deren Verwendung als Arzneimittel und Diagnostika
US6316479B1 (en) 1997-05-19 2001-11-13 Sugen, Inc. Isoxazole-4-carboxamide compounds active against protein tryosine kinase related disorders
ATE207065T1 (de) * 1997-08-08 2001-11-15 Aventis Pharma Gmbh Kristallform von n-(4-trifluormethylphenyl)-5- methylisoxazol-4-carbonsäureamid
US7691890B2 (en) 1998-03-11 2010-04-06 James W. Williams Anti-viral uses of leflunomide products
US20050255071A1 (en) * 1998-12-10 2005-11-17 Aventis Pharma Deutschland Gmbh Preparation having improved therapeutic breadth comprising nucleotide synthesis inhibitors
DE19908527C2 (de) * 1999-02-26 2001-08-30 Aventis Pharma Gmbh Verfahren zur Kristallisation von N-(4-Trifluormethylphenyl)-5-methyl-isoxazol-4-carboxamid
US6566395B1 (en) 1999-05-25 2003-05-20 Biomedicines, Inc. Methods of treating proliferative disorders
DE19960443C2 (de) * 1999-12-15 2002-05-08 Aventis Pharma Gmbh Verfahren zur Auffindung von Nukleotidsyntheseinhibitoren mit weniger Nebenwirkungen
CZ20022000A3 (cs) * 1999-12-16 2003-02-12 Teva Pharmaceuticals Industries Ltd. Způsoby přípravy a nová krystalická forma leflunomidu
EP1257270B1 (fr) 2000-02-15 2005-04-13 Teva Pharmaceutical Industries Ltd. Procede permettant d'effectuer la synthese du leflunomide
EP1473035A1 (fr) * 2000-02-15 2004-11-03 Teva Pharmaceutical Industries Ltd. Leflunomide d'une pureté elevée
US20020077485A1 (en) * 2000-08-14 2002-06-20 Ilya Avrutov Micronized leflunomide
DE60226855D1 (de) 2001-04-05 2008-07-10 Aventis Pharma Inc Verwendung von (z)-2-cyano-3-hydroxy-but-2-ensäure-(4'-trifluoromethylphenyl)-amid zur behandlung der multiplen sklerose
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 (fr) * 2001-11-09 2003-05-22 Geneva Pharmaceuticals, Inc. Procede de preparation de (4'-trifluoromethyl)-anilide5-methylisoxazole-4-carboxylique
US20050158371A1 (en) * 2002-02-12 2005-07-21 Sumitomo Pharmaceuticals Co., Ltd. Novel external agent
CA2571710A1 (fr) 2004-06-24 2006-11-02 Nicholas Valiante Immuno-potentialisateurs a petites molecules et analyses visant a detecter leur presence
US20060024376A1 (en) * 2004-07-30 2006-02-02 The University Of Chicago Methods and compositions for reducing toxicity associated with leflunomide treatment
WO2007026737A1 (fr) * 2005-08-31 2007-03-08 Kowa Co., Ltd. Procédé prophylactique et/ou thérapeutique pour lutter contre l'arthrite rhumatoïde
US9073997B2 (en) * 2007-02-02 2015-07-07 Vegenics Pty Limited Growth factor antagonists for organ transplant alloimmunity and arteriosclerosis
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
US9205577B2 (en) * 2010-02-05 2015-12-08 Allergan, Inc. Porogen compositions, methods of making and uses
US9138309B2 (en) 2010-02-05 2015-09-22 Allergan, Inc. Porous materials, methods of making and uses
US11202853B2 (en) * 2010-05-11 2021-12-21 Allergan, Inc. Porogen compositions, methods of making and uses
JOP20190207A1 (ar) 2017-03-14 2019-09-10 Actelion Pharmaceuticals Ltd تركيبة صيدلانية تشتمل على بونيسيمود
JP2021519334A (ja) 2018-03-26 2021-08-10 クリア クリーク バイオ， インコーポレイテッド ジヒドロオロト酸デヒドロゲナーゼを阻害するための組成物および方法
US20230123588A1 (en) 2020-03-06 2023-04-20 Actelion Pharmaceuticals Ltd Methods of slowing brain volume loss
WO2021189018A1 (fr) 2020-03-20 2021-09-23 Clear Creek Bio, Inc. Procédés de traitement d'infections virales à l'aide d'inhibiteurs de voies de synthèse nucléotidique
EP4415699A1 (fr) 2021-10-11 2024-08-21 Laboratoires Juvise Pharmaceuticals Méthodes de traitement de la sclérose en plaques
US20240261268A1 (en) 2022-02-11 2024-08-08 Vanda Pharmaceuticals Inc. Methods of slowing an increase in brain ventricular volume

Family Cites Families (4)

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Publication number Priority date Publication date Assignee Title
US4087534A (en) * 1974-05-22 1978-05-02 David Ovadia N-haloalkylmio urazole pesticides
DE2524959C2 (de) * 1975-06-05 1983-02-10 Hoechst Ag, 6000 Frankfurt 5-Methyl-isoxazol-4-carbonsäureanilide, Verfahren zu ihrer Herstellung, diese Verbindungen enthaltende Mittel
ES448386A1 (es) * 1975-06-05 1978-04-16 Hoechst Ag Procedimiento para la preparacion de anilidas de acido 5-me-til-isoxazol-4-carboxilico.
DE2654797A1 (de) * 1976-12-03 1978-06-08 Hoechst Ag Verfahren zur herstellung von isoxazolderivaten

Also Published As

Publication number Publication date
BG60764B2 (bg) 1996-02-29
FI64154B (fi) 1983-06-30
FI793899A (fi) 1980-06-17
MX6174E (es) 1984-12-04
DK149886C (da) 1987-04-21
DK534279A (da) 1980-06-17
ES486758A1 (es) 1980-05-16
AU529341B2 (en) 1983-06-02
IE792426L (en) 1980-06-16
IL58951A (en) 1984-01-31
IL58951A0 (en) 1980-03-31
NL990037I2 (nl) 2000-01-03
ATE1067T1 (de) 1982-06-15
DE2962929D1 (en) 1982-07-08
ES486750A1 (es) 1980-06-16
AU5385379A (en) 1980-06-19
US4284786A (en) 1981-08-18
US4351841A (en) 1982-09-28
FI64154C (fi) 1983-10-10
PH16627A (en) 1983-12-05
EG13926A (en) 1982-09-30
JPH0133470B2 (fr) 1989-07-13
AR222680A1 (es) 1981-06-15
NZ192400A (en) 1982-02-23
PT70596A (de) 1980-01-01
NO148925B (no) 1983-10-03
HU178015B (en) 1982-02-28
DE2854439A1 (de) 1980-07-03
IE49126B1 (en) 1985-08-07
GR72731B (fr) 1983-12-01
NO794094L (no) 1980-06-17
DK149886B (da) 1986-10-20
AR226894A1 (es) 1982-08-31
EP0013376A3 (en) 1980-09-17
NL990037I1 (nl) 2000-01-03
NO148925C (no) 1984-01-11
JPS5583767A (en) 1980-06-24
EP0013376A2 (fr) 1980-07-23
EP0013376B1 (fr) 1982-05-19
ZA796793B (en) 1980-11-26
MX8403A (es) 1994-03-31
CA1129867A (fr) 1982-08-17

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