ZA200402999B - Polymorphous form of rimonabant, preparation method and pharmaceutical compositions containing same. - Google Patents
Polymorphous form of rimonabant, preparation method and pharmaceutical compositions containing same. Download PDFInfo
- Publication number
- ZA200402999B ZA200402999B ZA200402999A ZA200402999A ZA200402999B ZA 200402999 B ZA200402999 B ZA 200402999B ZA 200402999 A ZA200402999 A ZA 200402999A ZA 200402999 A ZA200402999 A ZA 200402999A ZA 200402999 B ZA200402999 B ZA 200402999B
- Authority
- ZA
- South Africa
- Prior art keywords
- temperature
- rimonabant
- methylcyclohexane
- medium
- mixture
- Prior art date
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- JZCPYUJPEARBJL-UHFFFAOYSA-N rimonabant Chemical compound CC=1C(C(=O)NN2CCCCC2)=NN(C=2C(=CC(Cl)=CC=2)Cl)C=1C1=CC=C(Cl)C=C1 JZCPYUJPEARBJL-UHFFFAOYSA-N 0.000 title claims description 77
- 229960003015 rimonabant Drugs 0.000 title claims description 66
- 239000008194 pharmaceutical composition Substances 0.000 title claims description 9
- 238000002360 preparation method Methods 0.000 title description 7
- UAEPNZWRGJTJPN-UHFFFAOYSA-N Methylcyclohexane Natural products CC1CCCCC1 UAEPNZWRGJTJPN-UHFFFAOYSA-N 0.000 claims description 82
- GYNNXHKOJHMOHS-UHFFFAOYSA-N methyl-cycloheptane Natural products CC1CCCCCC1 GYNNXHKOJHMOHS-UHFFFAOYSA-N 0.000 claims description 42
- 238000000034 method Methods 0.000 claims description 34
- 239000000203 mixture Substances 0.000 claims description 31
- 239000013078 crystal Substances 0.000 claims description 28
- 239000002904 solvent Substances 0.000 claims description 24
- 239000004480 active ingredient Substances 0.000 claims description 18
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 16
- ZMANZCXQSJIPKH-UHFFFAOYSA-N Triethylamine Chemical compound CCN(CC)CC ZMANZCXQSJIPKH-UHFFFAOYSA-N 0.000 claims description 15
- 238000001816 cooling Methods 0.000 claims description 15
- 238000010438 heat treatment Methods 0.000 claims description 15
- WYURNTSHIVDZCO-UHFFFAOYSA-N Tetrahydrofuran Chemical compound C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 claims description 12
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- UIHCLUNTQKBZGK-UHFFFAOYSA-N Methyl isobutyl ketone Natural products CCC(C)C(C)=O UIHCLUNTQKBZGK-UHFFFAOYSA-N 0.000 claims description 9
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- NTIZESTWPVYFNL-UHFFFAOYSA-N Methyl isobutyl ketone Chemical compound CC(C)CC(C)=O NTIZESTWPVYFNL-UHFFFAOYSA-N 0.000 claims description 8
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- YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 claims description 6
- CYAYCOCJAVHQSD-UHFFFAOYSA-N 5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methylpyrazole-3-carboxylic acid Chemical compound CC=1C(C(O)=O)=NN(C=2C(=CC(Cl)=CC=2)Cl)C=1C1=CC=C(Cl)C=C1 CYAYCOCJAVHQSD-UHFFFAOYSA-N 0.000 claims description 5
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- CYRMSUTZVYGINF-UHFFFAOYSA-N trichlorofluoromethane Chemical compound FC(Cl)(Cl)Cl CYRMSUTZVYGINF-UHFFFAOYSA-N 0.000 description 1
- 229940029284 trichlorofluoromethane Drugs 0.000 description 1
- UFTFJSFQGQCHQW-UHFFFAOYSA-N triformin Chemical compound O=COCC(OC=O)COC=O UFTFJSFQGQCHQW-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three 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
-
- 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
- A61P3/04—Anorexiants; Antiobesity agents
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical 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)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Child & Adolescent Psychology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Steroid Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| FR0114579A FR2831883B1 (fr) | 2001-11-08 | 2001-11-08 | Forme polymorphe du rimonabant, son procede de preparation et les compositions pharmaceutiques en contenant |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ZA200402999B true ZA200402999B (en) | 2005-04-20 |
Family
ID=8869285
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ZA200402999A ZA200402999B (en) | 2001-11-08 | 2004-04-20 | Polymorphous form of rimonabant, preparation method and pharmaceutical compositions containing same. |
Country Status (33)
| Country | Link |
|---|---|
| US (2) | US20050043356A1 (zh) |
| EP (1) | EP1446384A1 (zh) |
| JP (2) | JP4181994B2 (zh) |
| KR (2) | KR20050043774A (zh) |
| CN (1) | CN100412063C (zh) |
| AP (1) | AP1830A (zh) |
| AR (1) | AR037253A1 (zh) |
| AU (1) | AU2002350869B2 (zh) |
| BR (1) | BR0213931A (zh) |
| CA (1) | CA2464145A1 (zh) |
| CO (1) | CO5580827A2 (zh) |
| CR (1) | CR7333A (zh) |
| EA (1) | EA006771B1 (zh) |
| EC (1) | ECSP045088A (zh) |
| FR (1) | FR2831883B1 (zh) |
| GE (1) | GEP20063894B (zh) |
| HR (1) | HRP20040403A2 (zh) |
| HU (1) | HUP0402043A3 (zh) |
| IL (2) | IL161533A0 (zh) |
| IS (1) | IS7226A (zh) |
| MA (1) | MA27080A1 (zh) |
| ME (1) | MEP21908A (zh) |
| MX (1) | MXPA04004394A (zh) |
| NO (1) | NO326648B1 (zh) |
| NZ (1) | NZ532369A (zh) |
| OA (1) | OA12721A (zh) |
| PL (1) | PL369372A1 (zh) |
| RS (1) | RS36904A (zh) |
| TN (1) | TNSN04079A1 (zh) |
| TW (1) | TW200302824A (zh) |
| UA (1) | UA76776C2 (zh) |
| WO (1) | WO2003040105A1 (zh) |
| ZA (1) | ZA200402999B (zh) |
Families Citing this family (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2831883B1 (fr) * | 2001-11-08 | 2004-07-23 | Sanofi Synthelabo | Forme polymorphe du rimonabant, son procede de preparation et les compositions pharmaceutiques en contenant |
| NZ537003A (en) | 2002-07-18 | 2008-03-28 | Cytos Biotechnology Ag | Hapten-carrier conjugates comprising virus like particles and uses thereof |
| FR2861992B1 (fr) * | 2003-11-10 | 2007-07-20 | Sanofi Synthelabo | Composition pharmaceutique destinee a l'administration orale d'un derive de pyrazole-3-carboxamide. |
| AU2006264649A1 (en) | 2005-06-30 | 2007-01-11 | Prosidion Limited | GPCR agonists |
| EP1816125A1 (en) * | 2006-02-02 | 2007-08-08 | Ranbaxy Laboratories, Ltd. | Novel crystalline forms of an antagonist of CB1 cannabinoid receptor and preparation method thereof |
| FR2897060B1 (fr) * | 2006-02-08 | 2008-07-25 | Sanofi Aventis Sa | Le monohydrate de rimonabant, son procede de preparation et les compositions pharmaceutiques en contenant |
| WO2008038143A2 (en) * | 2006-06-22 | 2008-04-03 | Medichem, S.A. | Novel solid forms of rimonabant and synthetic processes for their preparation |
| AR062593A1 (es) * | 2006-08-29 | 2008-11-19 | Medichem Sa | 1-{[5-(4-clorofenil)-1-(2,4-diclorofenil)-4-metil-1h-pirazol-3-il]carbonil}-piperidina y proceso para preparar dicho compuesto; proceso para analizar la pureza de rimonabant,proceso para preparar rimonabant,rimonabant que se obtiene mediante dicho proceso y formulaciones. |
| EP2057144A4 (en) * | 2006-09-01 | 2010-06-02 | Hetero Drugs Ltd | NEW POLYMORPHIC FROM RIMONABANT |
| EP2061783A2 (en) * | 2006-09-11 | 2009-05-27 | Hetero Drugs Limited | Improved process for rimonabant |
| WO2008035023A1 (en) * | 2006-09-19 | 2008-03-27 | Cipla Limited | Polymorphs of rimonabant |
| WO2008056377A2 (en) * | 2006-11-06 | 2008-05-15 | Cadila Healthcare Limited | Polymorphic forms of rimonabant |
| WO2008064615A2 (en) * | 2006-12-01 | 2008-06-05 | Zentiva, A.S. | Crystalline and amorphous forms of rimonabant and processes for obtaining them |
| JP5222855B2 (ja) * | 2006-12-18 | 2013-06-26 | ７ティーエム ファーマ エイ／エス | Ｃｂ１受容体のモジュレーター |
| AR064736A1 (es) | 2007-01-04 | 2009-04-22 | Prosidion Ltd | Agonistas de gpcr |
| WO2008081208A1 (en) | 2007-01-04 | 2008-07-10 | Prosidion Limited | Piperidine gpcr agonists |
| GB0700122D0 (en) | 2007-01-04 | 2007-02-14 | Prosidion Ltd | GPCR agonists |
| CL2008000018A1 (es) | 2007-01-04 | 2008-08-01 | Prosidion Ltd | Compuestos derivados de heterociclos de nitrogeno y oxigeno, agonistas de gpcr; composicion farmaceutica que comprende a dicho compuesto; y uso del compuesto para el tratamiento de la obesidad, diabetes, sindrome metabolico, hiperlipidemia, toleranci |
| WO2008081204A1 (en) | 2007-01-04 | 2008-07-10 | Prosidion Limited | Piperidine gpcr agonists |
| EP1944297A1 (en) * | 2007-01-09 | 2008-07-16 | Miklós Vértessy | Solid and crystalline rimonabant and processes for preparation, and pharmaceutical composition thereof |
| WO2008088900A2 (en) * | 2007-01-18 | 2008-07-24 | Teva Pharmaceutical Industries Ltd. | Polymorphic forms of rimonabant base and processes for preparation thereof |
| EP1953144A1 (en) | 2007-01-30 | 2008-08-06 | Sandoz AG | Novel polymorphic forms of N-piperidino-5-(4-chlorophenyl)-1-(2, 4-dichlorphenyl)-4-methyl-3-pyrazolecarboxamide |
| FR2919862A1 (fr) * | 2007-08-06 | 2009-02-13 | Sanofi Aventis Sa | Le solvate de 3-methylbutan-1-ol de rimonabant, son procede de preparation et les compositions pharmaceutiques en contenant |
| FR2919864A1 (fr) * | 2007-08-06 | 2009-02-13 | Sanofi Aventis Sa | Le solvate de 1,4-dioxane de rimonabant, son procede de preparation et les compositions pharmaceutiques en contenant |
| FR2919867A1 (fr) * | 2007-08-06 | 2009-02-13 | Sanofi Aventis Sa | Le solvate de 2-methoxyethanol de rimonabant et son procede de preparation |
| FR2919863A1 (fr) * | 2007-08-06 | 2009-02-13 | Sanofi Aventis Sa | Le solvate de n-methylpyrrolidone de rimonabant, son procede de preparation et les compositions pharmaceutiques en contenant |
| FR2919865A1 (fr) * | 2007-08-06 | 2009-02-13 | Sanofi Aventis Sa | Le solvate de dmso de rimonabant, son procede de preparation et les compositions pharmaceutiques en contenant |
| GB0720389D0 (en) | 2007-10-18 | 2008-11-12 | Prosidion Ltd | G-Protein Coupled Receptor Agonists |
| GB0720390D0 (en) | 2007-10-18 | 2007-11-28 | Prosidion Ltd | G-Protein coupled receptor agonists |
| WO2009153804A1 (en) * | 2008-06-16 | 2009-12-23 | Cadila Healthcare Limited | Process for preparing form i of rimonabant |
| WO2010079241A1 (es) | 2009-01-12 | 2010-07-15 | Fundacion Hospital Nacional De Paraplejicos Para La Investigacion Y La Integracion | Uso de antagonistas y/o agonistas inversos de los receptores cb1 para la preparación de medicamentos que incrementen la excitabilidad de las motoneuronas |
| FR3008620A1 (fr) * | 2013-07-22 | 2015-01-23 | Sanofi Sa | Formulation de comprime d'un inhibiteur de phosphatidylinositol 3-kinase |
| CN114555557A (zh) * | 2019-10-16 | 2022-05-27 | 大塚制药株式会社 | 森塔纳法啶的制备方法 |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2692575B1 (fr) * | 1992-06-23 | 1995-06-30 | Sanofi Elf | Nouveaux derives du pyrazole, procede pour leur preparation et compositions pharmaceutiques les contenant. |
| FR2713225B1 (fr) * | 1993-12-02 | 1996-03-01 | Sanofi Sa | N-pipéridino-3-pyrazolecarboxamide substitué. |
| WO2003015700A2 (en) * | 2001-08-15 | 2003-02-27 | The Government Of The United States Of America As Represented By The Secretary Of The Department Of Health And Human Services | Novel vasoconstrictor cannabinoid analogs |
| FR2831883B1 (fr) * | 2001-11-08 | 2004-07-23 | Sanofi Synthelabo | Forme polymorphe du rimonabant, son procede de preparation et les compositions pharmaceutiques en contenant |
-
2001
- 2001-11-08 FR FR0114579A patent/FR2831883B1/fr not_active Expired - Fee Related
-
2002
- 2002-04-11 UA UA20040402974A patent/UA76776C2/uk unknown
- 2002-11-04 GE GE5606A patent/GEP20063894B/en unknown
- 2002-11-04 AP APAP/P/2004/003024A patent/AP1830A/en active
- 2002-11-04 HU HU0402043A patent/HUP0402043A3/hu unknown
- 2002-11-04 US US10/494,211 patent/US20050043356A1/en not_active Abandoned
- 2002-11-04 IL IL16153302A patent/IL161533A0/xx unknown
- 2002-11-04 JP JP2003542151A patent/JP4181994B2/ja not_active Expired - Fee Related
- 2002-11-04 MX MXPA04004394A patent/MXPA04004394A/es unknown
- 2002-11-04 AU AU2002350869A patent/AU2002350869B2/en not_active Ceased
- 2002-11-04 ME MEP-219/08A patent/MEP21908A/xx unknown
- 2002-11-04 KR KR1020047006969A patent/KR20050043774A/ko not_active Application Discontinuation
- 2002-11-04 EA EA200400491A patent/EA006771B1/ru not_active IP Right Cessation
- 2002-11-04 NZ NZ532369A patent/NZ532369A/en not_active IP Right Cessation
- 2002-11-04 OA OA1200400131A patent/OA12721A/fr unknown
- 2002-11-04 BR BR0213931-6A patent/BR0213931A/pt not_active IP Right Cessation
- 2002-11-04 WO PCT/FR2002/003765 patent/WO2003040105A1/fr active Application Filing
- 2002-11-04 PL PL02369372A patent/PL369372A1/xx not_active Application Discontinuation
- 2002-11-04 CA CA002464145A patent/CA2464145A1/en not_active Abandoned
- 2002-11-04 EP EP02785580A patent/EP1446384A1/fr not_active Withdrawn
- 2002-11-04 RS YU36904A patent/RS36904A/sr unknown
- 2002-11-04 CN CNB028219686A patent/CN100412063C/zh not_active Expired - Fee Related
- 2002-11-04 KR KR1020097016373A patent/KR20090089485A/ko not_active Application Discontinuation
- 2002-11-06 AR ARP020104228A patent/AR037253A1/es unknown
- 2002-11-07 TW TW091132763A patent/TW200302824A/zh unknown
-
2004
- 2004-04-19 IS IS7226A patent/IS7226A/is unknown
- 2004-04-20 ZA ZA200402999A patent/ZA200402999B/en unknown
- 2004-04-20 IL IL161533A patent/IL161533A/en not_active IP Right Cessation
- 2004-04-27 EC EC2004005088A patent/ECSP045088A/es unknown
- 2004-04-28 MA MA27659A patent/MA27080A1/fr unknown
- 2004-05-04 CO CO04040840A patent/CO5580827A2/es not_active Application Discontinuation
- 2004-05-04 CR CR7333A patent/CR7333A/es unknown
- 2004-05-06 HR HR20040403A patent/HRP20040403A2/hr not_active Application Discontinuation
- 2004-05-07 NO NO20041879A patent/NO326648B1/no not_active IP Right Cessation
- 2004-05-07 TN TNP2004000079A patent/TNSN04079A1/fr unknown
-
2008
- 2008-07-11 JP JP2008181474A patent/JP4931874B2/ja not_active Expired - Fee Related
- 2008-10-28 US US12/259,701 patent/US20100190827A1/en not_active Abandoned
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