YU61602A - Postupak za dobijanje leflunomida - Google Patents
Postupak za dobijanje leflunomidaInfo
- Publication number
- YU61602A YU61602A YU61602A YUP61602A YU61602A YU 61602 A YU61602 A YU 61602A YU 61602 A YU61602 A YU 61602A YU P61602 A YUP61602 A YU P61602A YU 61602 A YU61602 A YU 61602A
- Authority
- YU
- Yugoslavia
- Prior art keywords
- leflunomide
- trifluoromethylphenyl
- isoxazole
- carboxamide
- methyl
- Prior art date
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
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/02—Nasal agents, e.g. decongestants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- 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
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- 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
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Pulmonology (AREA)
- Diabetes (AREA)
- Epidemiology (AREA)
- Rheumatology (AREA)
- Endocrinology (AREA)
- Physical Education & Sports Medicine (AREA)
- Pain & Pain Management (AREA)
- Emergency Medicine (AREA)
- Ophthalmology & Optometry (AREA)
- Dermatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Transplantation (AREA)
- Hematology (AREA)
- Otolaryngology (AREA)
- Obesity (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
Abstract
Obezbeđen je postupak za sintezu lefluonomida iz 5-metilizoksazol-4-karboksilne kiseline i 4-trifluorometilanilina. Dalje je obezbeđen leflunomid pripremljen inventivnim postupkom, koji je gotovo potpuno bez nečistoća koje je teško izdvojiti, koje se obično nalaze u leflunomidu pripremljenom poznatim metodama, uključujući N-(4-trifluorometilfenil)-2-cijano-3-hidroksikrotonamid, 5-metil-N-(4-metilfenil)-izoksazol-4-karboksamid i N-(4-trifluorometilfenil)-3-metil-izoksazol-4-karboksamida. Pronalazak dalje obezbeđuje farmaceutske preparate i dozne oblike koji sadrže leflunomid visoke čistoće i metode tretiranja bolesti korišćenjem leflunomida.[A process for synthesizing leflunomide from 5-methylisoxazole-4-carboxylic acid and 4-trifluoromethylaniline is provided. Further provided is the leflunomide prepared by the inventive process, which is substantially free of difficult-to-separate impurities often found in leflunomide prepared by known methods, including N-(4-trifluoromethylphenyl)-2-cyano-3-hydroxycrotonamide, 5-methyl-N-(4- methylphenyl)-isoxazole-4-carboxamide and N-(4-trifluoromethylphenyl)-3-methyl-isoxazole-4-carboxamide. The invention further provides pharmaceutical compositions and dosage forms containing highly pure leflunomide and methods of treating disease using the leflunomide.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US18263500P | 2000-02-15 | 2000-02-15 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| YU61602A true YU61602A (sh) | 2006-01-16 |
Family
ID=22669359
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| YU61602A YU61602A (sh) | 2000-02-15 | 2001-02-08 | Postupak za dobijanje leflunomida |
Country Status (18)
| Country | Link |
|---|---|
| US (2) | US6723855B2 (sh) |
| EP (1) | EP1257270B1 (sh) |
| JP (1) | JP2004500380A (sh) |
| KR (1) | KR20020072312A (sh) |
| AT (1) | ATE292966T1 (sh) |
| AU (1) | AU2001234943A1 (sh) |
| CA (1) | CA2400290A1 (sh) |
| CZ (1) | CZ20023024A3 (sh) |
| DE (1) | DE60110043T2 (sh) |
| ES (1) | ES2237553T3 (sh) |
| HR (1) | HRP20020671A2 (sh) |
| HU (1) | HUP0301865A3 (sh) |
| IL (1) | IL151196A0 (sh) |
| PL (1) | PL366088A1 (sh) |
| SK (1) | SK12992002A3 (sh) |
| WO (1) | WO2001060363A1 (sh) |
| YU (1) | YU61602A (sh) |
| ZA (1) | ZA200206494B (sh) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK0987256T3 (da) * | 1997-08-08 | 2002-02-11 | Aventis Pharma Gmbh | Krystalform af N-(4-trifluormethylphenyl)-5-methylisoxazol-4-carboxylsyreamid |
| KR20020067545A (ko) * | 1999-12-16 | 2002-08-22 | 테바 파마슈티컬 인더스트리즈 리미티드 | 레플루노마이드의 신규 제조 방법 및 이의 신규 결정형 |
| 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 (en) * | 2001-11-09 | 2003-05-22 | Geneva Pharmaceuticals, Inc. | Process for preparing 5-methylisoxazole-4-carboxylic-(4'-trifluoromethyl)-anilide |
| WO2004105763A2 (en) * | 2003-05-27 | 2004-12-09 | Haegerkvist Robert Per | Use of tyrosine kinase inhibitor to treat diabetes |
| US20060188568A1 (en) * | 2003-10-30 | 2006-08-24 | Lupin Limited | Stable formulations of ace inhibitors and methods for preparation thereof |
| US20060024376A1 (en) * | 2004-07-30 | 2006-02-02 | The University Of Chicago | Methods and compositions for reducing toxicity associated with leflunomide treatment |
| DE102005017592A1 (de) * | 2005-04-16 | 2006-10-19 | Lindner, Jürgen, Dr. med. | Darreichungsformen und Kombinationspräparate von Pyrimidinbiosyntheseinhibitoren zur Erzielung zusätzlicher Wirkungen auf das Immunsystem |
| WO2007086076A2 (en) * | 2006-01-24 | 2007-08-02 | Unichem Laboratories Limited | An improved process for preparation of leflunomide |
| 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 |
| DK2477611T3 (en) | 2009-09-18 | 2017-07-10 | Sanofi Sa | (Z) -2-CYANO-3-HYDROXYBUT-2-ENIC ACID (4'-TRIFLUORMETHYLPHENYL) AMID TABLE FORMULATIONS WITH IMPROVED STABILITY |
| CN102002009B (zh) * | 2010-10-18 | 2012-11-07 | 齐鲁制药有限公司 | 一种5-甲基异恶唑-4-甲酰氯的制备方法 |
| AU2016280243B2 (en) * | 2015-06-17 | 2020-12-03 | Biocon Limited | A novel process for the preparation of teriflunomide |
| JOP20190207A1 (ar) | 2017-03-14 | 2019-09-10 | Actelion Pharmaceuticals Ltd | تركيبة صيدلانية تشتمل على بونيسيمود |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE2854439A1 (de) | 1978-12-16 | 1980-07-03 | Hoechst Ag | Ein isoxazolderivat, verfahren zu seiner herstellung, diese verbindung enthaltende mittel und verwendung |
| GB8619432D0 (en) | 1986-08-08 | 1986-09-17 | Lilly Industries Ltd | Pharmaceutical compounds |
| DK0527736T3 (da) * | 1990-05-18 | 1997-10-20 | Hoechst Ag | Isoxazol-4-carboxylsyreamider og hydroxyalkyliden-cyanoacetamider, lægemidler indeholdende disse forbindelser og anvendelsen af disse lægemidler. |
| ES2124800T3 (es) * | 1993-01-08 | 1999-02-16 | Hoechst Ag | Empleo de leflunomida para la inhibicion de interleuquina 1 beta. |
| US5610173A (en) * | 1994-01-07 | 1997-03-11 | Sugen, Inc. | Formulations for lipophilic compounds |
| DK0987256T3 (da) * | 1997-08-08 | 2002-02-11 | Aventis Pharma Gmbh | Krystalform af N-(4-trifluormethylphenyl)-5-methylisoxazol-4-carboxylsyreamid |
| DE19908527C2 (de) * | 1999-02-26 | 2001-08-30 | Aventis Pharma Gmbh | Verfahren zur Kristallisation von N-(4-Trifluormethylphenyl)-5-methyl-isoxazol-4-carboxamid |
| KR20020067545A (ko) * | 1999-12-16 | 2002-08-22 | 테바 파마슈티컬 인더스트리즈 리미티드 | 레플루노마이드의 신규 제조 방법 및 이의 신규 결정형 |
-
2001
- 2001-02-08 WO PCT/US2001/004095 patent/WO2001060363A1/en not_active Application Discontinuation
- 2001-02-08 YU YU61602A patent/YU61602A/sh unknown
- 2001-02-08 JP JP2001559460A patent/JP2004500380A/ja active Pending
- 2001-02-08 SK SK1299-2002A patent/SK12992002A3/sk unknown
- 2001-02-08 CZ CZ20023024A patent/CZ20023024A3/cs unknown
- 2001-02-08 ES ES01907127T patent/ES2237553T3/es not_active Expired - Lifetime
- 2001-02-08 IL IL15119601A patent/IL151196A0/xx unknown
- 2001-02-08 DE DE60110043T patent/DE60110043T2/de not_active Expired - Fee Related
- 2001-02-08 CA CA002400290A patent/CA2400290A1/en not_active Abandoned
- 2001-02-08 PL PL01366088A patent/PL366088A1/xx not_active Application Discontinuation
- 2001-02-08 US US09/779,928 patent/US6723855B2/en not_active Expired - Fee Related
- 2001-02-08 EP EP01907127A patent/EP1257270B1/en not_active Expired - Lifetime
- 2001-02-08 AT AT01907127T patent/ATE292966T1/de not_active IP Right Cessation
- 2001-02-08 KR KR1020027010595A patent/KR20020072312A/ko not_active Application Discontinuation
- 2001-02-08 HU HU0301865A patent/HUP0301865A3/hu unknown
- 2001-02-08 AU AU2001234943A patent/AU2001234943A1/en not_active Abandoned
-
2002
- 2002-08-14 HR HRP20020671 patent/HRP20020671A2/hr not_active Application Discontinuation
- 2002-08-14 ZA ZA200206494A patent/ZA200206494B/en unknown
-
2003
- 2003-12-10 US US10/730,949 patent/US20040127532A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| HUP0301865A3 (en) | 2005-12-28 |
| EP1257270A4 (en) | 2003-05-07 |
| WO2001060363A1 (en) | 2001-08-23 |
| ZA200206494B (en) | 2003-08-20 |
| SK12992002A3 (sk) | 2003-05-02 |
| DE60110043T2 (de) | 2006-03-02 |
| DE60110043D1 (de) | 2005-05-19 |
| EP1257270A1 (en) | 2002-11-20 |
| EP1257270B1 (en) | 2005-04-13 |
| HUP0301865A2 (hu) | 2003-09-29 |
| JP2004500380A (ja) | 2004-01-08 |
| ES2237553T3 (es) | 2005-08-01 |
| ATE292966T1 (de) | 2005-04-15 |
| PL366088A1 (en) | 2005-01-24 |
| KR20020072312A (ko) | 2002-09-14 |
| CA2400290A1 (en) | 2001-08-23 |
| AU2001234943A1 (en) | 2001-08-27 |
| US20020022646A1 (en) | 2002-02-21 |
| CZ20023024A3 (cs) | 2003-05-14 |
| US20040127532A1 (en) | 2004-07-01 |
| US6723855B2 (en) | 2004-04-20 |
| IL151196A0 (en) | 2003-04-10 |
| HRP20020671A2 (en) | 2004-12-31 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| IL151196A0 (en) | A method for synthesizing leflunomide | |
| MXPA03011515A (es) | Nuevas composiciones de medicamentos sobre la base de agentes anticolinergicos, corticoesteroides y agentes betamimeticos. | |
| PL365683A1 (en) | Selected fused pyrrolocarbazoles | |
| HUP0301802A2 (hu) | Eljárás carvedilol elżállítására, kristályos carvedilol, eljárás elżállítására és a vegyületet tartalmazó gyógyszerkészítmény | |
| NO20006645D0 (no) | Ny form av irbesartan, fremgangsmåte for å oppnå den nevnte form og farmasöytiske preparater inneholdende den samme | |
| JO2216B1 (en) | 5 chloro-3 (4-methane sulfonyl phenyl) -6-methyl- (2.3) | |
| PL364598A1 (en) | Stable polymorph of flibanserin, technical process for its preparation and the use thereof for preparing medicaments | |
| NO20061791L (no) | Polymorf form av 3-fenylsulfonyl-8-piperazin-1-yl-kinolin | |
| HUP0500001A2 (hu) | Pramipexol alkalmazása amiotrófiás laterálszklerózis kezelésére | |
| HUP0204010A2 (hu) | Új szertralin-hidroklorid polimorfok, eljárás az előállításukra, az új polimorfokat tartalmazó gyógyszerkészítmények és alkalmazásuk | |
| HUP0302874A2 (hu) | Eljárás risperidon előállítására | |
| SG149045A1 (en) | Novel fused pyrrolocarbazoles | |
| IL160171A0 (en) | Depsipeptide derivatives, processes for the preparation thereof and pharmaceutical compositions containing the same | |
| ATE171873T1 (de) | Antiglucocorticoidsteroide zur behandlung von angststörungen | |
| MY149041A (en) | Novel fused pyrrolocarbazoles | |
| MXPA04002256A (es) | Uso de gonadotropina corionica humana (gch) en hiperestimulacion ovarica controlada. | |
| HUP0204069A2 (hu) | Új eljárás leflunomid előállítására és a leflunomid új kristályformája és ezt tartalmazó gyógyszerkészítmény | |
| MY126117A (en) | Pharmaceutical compositions | |
| TR200503401T1 (tr) | Kuetiapin (Quetiapine) Fumarat'ın yeni polimorfları | |
| YU21104A (sh) | Upotreba hcg i lh u kontrolisanoj hiperstimulaciji ovarijuma | |
| HUP0401234A2 (hu) | Pravastatin stabil gyógyászati kompozíciója és eljárás az előállítására | |
| ATE496038T1 (de) | Verfahren zur herstellung von quetiapin | |
| DE60204014D1 (de) | Chlormethylierung von thiophene | |
| ATE259784T1 (de) | Propanolaminotetraline, verfahren zu ihrer herstellung sowie diese verbindungen enthaltende pharmazeutische zusammensetzungen | |
| UA87829C2 (en) | Fused pyrrolocarbazoles |