AR013838A1 - Compuestos de 2-metil-4-(4-metil-1-piperazinil)-10h-tieno[2,3-b]benzodiazepina-dihidratos; los dihidratos b,d y e de dicho compuesto y proceso para preparar la forma ii sustancialmente pura de la olanzapina a partir de dichos dihidratos - Google Patents
Compuestos de 2-metil-4-(4-metil-1-piperazinil)-10h-tieno[2,3-b]benzodiazepina-dihidratos; los dihidratos b,d y e de dicho compuesto y proceso para preparar la forma ii sustancialmente pura de la olanzapina a partir de dichos dihidratosInfo
- Publication number
- AR013838A1 AR013838A1 ARP970104362A ARP970104362A AR013838A1 AR 013838 A1 AR013838 A1 AR 013838A1 AR P970104362 A ARP970104362 A AR P970104362A AR P970104362 A ARP970104362 A AR P970104362A AR 013838 A1 AR013838 A1 AR 013838A1
- Authority
- AR
- Argentina
- Prior art keywords
- olanzapine
- dihydrates
- methyl
- substantially pure
- piperazinyl
- Prior art date
Links
- KVWDHTXUZHCGIO-UHFFFAOYSA-N olanzapine Chemical compound C1CN(C)CCN1C1=NC2=CC=CC=C2NC2=C1C=C(C)S2 KVWDHTXUZHCGIO-UHFFFAOYSA-N 0.000 title abstract 7
- 229960005017 olanzapine Drugs 0.000 title abstract 7
- 150000004683 dihydrates Chemical class 0.000 title abstract 4
- 238000000034 method Methods 0.000 title abstract 4
- -1 4-METHYL-1-PIPERAZINYL Chemical class 0.000 title abstract 2
- 150000001875 compounds Chemical class 0.000 title 2
- 238000004519 manufacturing process Methods 0.000 abstract 2
- ZVAPWJGRRUHKGP-UHFFFAOYSA-N 1h-1,5-benzodiazepine Chemical compound N1C=CC=NC2=CC=CC=C12 ZVAPWJGRRUHKGP-UHFFFAOYSA-N 0.000 abstract 1
- FUOBHGGXKJHKDF-UHFFFAOYSA-N 2-methyl-4-(4-methylpiperazin-1-yl)-10H-thieno[2,3-b][1,5]benzodiazepine dihydrate Chemical compound O.O.C1CN(C)CCN1C1=NC2=CC=CC=C2NC2=C1C=C(C)S2 FUOBHGGXKJHKDF-UHFFFAOYSA-N 0.000 abstract 1
- 208000028017 Psychotic disease Diseases 0.000 abstract 1
- 239000003125 aqueous solvent Substances 0.000 abstract 1
- 238000009472 formulation Methods 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 239000003960 organic solvent Substances 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
-
- 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
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Neurology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Biomedical Technology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Psychiatry (AREA)
- Pharmacology & Pharmacy (AREA)
- Neurosurgery (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Un proceso para preparar 2-metil-4-(metil-1-piperazinil)-1OH-tieno[2,3-b] 1,5 benzodiacepina (denominada en la presente olanzapina y ciertosintermediarios dihidratos. La olanzapina resulta util en el tratamiento de pacientes psicoticos, yactu almente se está investigando dicha aplicacion. Lossolicitantes han descubierto que la olanzapina forma II es la forma anhidro más estable de olanzapina, y proporciona una formulacion anhidro estable concaracterísticas farmacéuticamentedeseables. (Ve r patente europea 733635). Se requiere condiciones de preparacion controladas para asegurar una olanzapina deForma II sustancialmente pura ( denominada en la presente Forma II); sin embargo los solicitantes han descubierto unproceso para prepar ar la Forma IIdeseada utilizando un intermedio olanzapina dihidrato en condiciones acuosas. En ciertas situaciones, la Formula II que ha sido preparada a partir de unsolvente acuoso puede resultar particularmente ventajosa.Dicho material Forma II resulte sustancialmente libre de todos los residuos de solvente orgánico.Este proceso puede proporcionar unmétodo ecologico especialmente deseado para proporcionar la Forma II en cuestion. La invencion que sereivindicaproporcion olazapina dihidra to que resulta especialmente util como intermedio para la preparacion de olazapina Forma II. La forma cristalina puede serespecialmente ventajosa. Un proceso para preparar la Forma II sustancialmente puraque consiste en secar una olanzapina dihi drato hasta que se prepara laForma II deseada.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US2648796P | 1996-09-23 | 1996-09-23 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR013838A1 true AR013838A1 (es) | 2001-01-31 |
Family
ID=21832120
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP970104362A AR013838A1 (es) | 1996-09-23 | 1997-09-23 | Compuestos de 2-metil-4-(4-metil-1-piperazinil)-10h-tieno[2,3-b]benzodiazepina-dihidratos; los dihidratos b,d y e de dicho compuesto y proceso para preparar la forma ii sustancialmente pura de la olanzapina a partir de dichos dihidratos |
Country Status (35)
| Country | Link |
|---|---|
| US (1) | US6020487A (es) |
| EP (1) | EP0831098B1 (es) |
| JP (2) | JP2001500877A (es) |
| KR (1) | KR100560015B1 (es) |
| CN (1) | CN1122036C (es) |
| AR (1) | AR013838A1 (es) |
| AT (1) | ATE209208T1 (es) |
| AU (1) | AU719441B2 (es) |
| BR (1) | BR9712100A (es) |
| CA (1) | CA2265712C (es) |
| CO (1) | CO4910140A1 (es) |
| CZ (1) | CZ299248B6 (es) |
| DE (1) | DE69708428T2 (es) |
| DK (1) | DK0831098T3 (es) |
| EA (1) | EA001642B1 (es) |
| EG (1) | EG23861A (es) |
| ES (1) | ES2166051T3 (es) |
| HU (1) | HU226484B1 (es) |
| ID (1) | ID27275A (es) |
| IL (1) | IL128962A (es) |
| IN (1) | IN187156B (es) |
| MY (1) | MY125565A (es) |
| NO (1) | NO323980B1 (es) |
| NZ (1) | NZ334448A (es) |
| PE (1) | PE110398A1 (es) |
| PL (3) | PL196069B1 (es) |
| PT (1) | PT831098E (es) |
| RS (1) | RS49598B (es) |
| SI (1) | SI0831098T1 (es) |
| SV (1) | SV1997000081A (es) |
| TR (1) | TR199900640T2 (es) |
| TW (1) | TW470746B (es) |
| UA (1) | UA59371C2 (es) |
| WO (1) | WO1998012199A1 (es) |
| ZA (1) | ZA978515B (es) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR0114031A (pt) * | 2000-08-31 | 2003-09-09 | Reddy S Lab Ltd | Processo para a preparação de hidratos de olanzapina e sua conversão em formas cristalinas de olanzapina |
| US6740753B2 (en) * | 2001-01-04 | 2004-05-25 | Geneva Pharmaceuticals, Inc. | Olanzapine crystal modification |
| AU2002340328A1 (en) * | 2001-10-29 | 2003-05-12 | Janet I. Cord | Olanzapine dihydrate-ii a process for its preparation and use thereof |
| CA2471341C (en) | 2001-12-24 | 2012-01-24 | Sun Pharmaceutical Industries Limited | Crystalline form i of 2-methyl-4-(4-methyl-1-piperazinyl) 10h thieno [2,3-b][1,5]benzodiazepine |
| WO2003091260A1 (en) * | 2002-04-23 | 2003-11-06 | Dr. Reddy's Laboratories Limited | Novel crystalline polymorph form-vi of olanzapine and a process for preparation thereof |
| DE60336226D1 (de) * | 2002-05-31 | 2011-04-14 | Sandoz Ag | Verfahren zur herstellung von olanzapin form i |
| SI21270A (sl) | 2002-07-15 | 2004-02-29 | Krka, Tovarna Zdravil, D.D., Novo Mesto | Kristalne oblike olanzapina in postopki za njihovo pripravo |
| EP1575962A1 (en) | 2002-12-24 | 2005-09-21 | Teva Pharmaceutical Industries Limited | Novel crystal forms of olanzapine, methods for their preparation and method for the preparation of known olanzapine crystal forms |
| AU2004291043A1 (en) * | 2003-11-18 | 2005-06-02 | 3M Innovative Properties Company | Olanzapine containing transdermal drug delivery compositions |
| PL1611139T3 (pl) * | 2003-12-22 | 2008-10-31 | Teva Pharma | Sposób wytwarzania olenzapiny |
| WO2005070938A1 (en) | 2004-01-27 | 2005-08-04 | Synthon B.V. | Stable salts of olanzapine |
| EP1716154A1 (en) * | 2004-02-19 | 2006-11-02 | Neuland Laboratories Ltd | Process for the preparation of olanzapine form 1 useful as antipsychotic drug |
| EP1781666A1 (en) * | 2004-07-14 | 2007-05-09 | Shasun Chemicals and Drugs Limited | Improved process for making form i of olanzapine. |
| ES2253091B1 (es) | 2004-07-27 | 2007-02-01 | Inke, S.A. | Solvato mixto de olanzapina, procedimiento para su obtencion y procedimiento de obtencion de la forma i de olanzapina a partir del mismo. |
| ES2303462B1 (es) | 2004-09-06 | 2009-06-05 | Shasun Chemicals And Drugs Limited | Nuevo procedimiento para la preparacion de una forma polimorfica i de olanzapina farmaceuticamente pura. |
| EA200701065A1 (ru) * | 2004-11-16 | 2007-12-28 | Элан Фарма Интернэшнл Лтд. | Инъецируемые составы, содержащие нанодисперсный оланзапин |
| US7834176B2 (en) | 2006-01-26 | 2010-11-16 | Sandoz Ag | Polymorph E of Olanzapine and preparation of anhydrous non-solvated crystalline polymorphic Form I of 2-methyl-4(4-methyl-1-piperazinyl)-10H-thieno[2,3-b][1,5] benzodiazepine (Olanzapine Form I) from the polymorphic Olanzapine Form E |
| CA2591644A1 (en) * | 2007-06-14 | 2008-12-14 | Apotex Pharmachem Inc. | Novel processes to form-i of olanzapine |
| EP2486913A1 (en) | 2011-02-14 | 2012-08-15 | Labtec GmbH | Rapidly disintegrating oral film formulation for Olanzapin |
| JP6008734B2 (ja) * | 2012-12-20 | 2016-10-19 | 株式会社トクヤマ | オランザピンｉｉ型結晶の製造方法 |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5302716A (en) * | 1986-01-16 | 1994-04-12 | Schering Corporation | Fused benzazepines |
| CA2002596A1 (en) * | 1988-11-14 | 1990-05-14 | Thomas M. Eckrich | Hydrates of b-lactam antibiotic |
| US5229382A (en) * | 1990-04-25 | 1993-07-20 | Lilly Industries Limited | 2-methyl-thieno-benzodiazepine |
| GB9009229D0 (en) * | 1990-04-25 | 1990-06-20 | Lilly Industries Ltd | Pharmaceutical compounds |
| EP0582368B1 (en) * | 1992-05-29 | 2001-01-24 | Eli Lilly And Company Limited | Thienobenzodiazepine derivatives for treatment of CNS disorders |
| US5550231A (en) * | 1993-06-15 | 1996-08-27 | Eli Lilly And Company | Loracarbef hydrochloride C1-C3 alcohol solvates and uses thereof |
| US5602124A (en) * | 1994-12-12 | 1997-02-11 | Allelix Biopharmaceuticals, Inc. | 5-HT2 receptor ligands |
| US5637584A (en) * | 1995-03-24 | 1997-06-10 | Eli Lilly And Company | Solvate of olanzapine |
| EG24221A (en) * | 1995-03-24 | 2008-11-10 | Lilly Co Eli | Process for preparing olanzapine |
| EG23659A (en) * | 1995-03-24 | 2007-03-26 | Lilly Co Eli | Process and crystal forms of methyl-thieno-benzodiazepine |
| US5631250A (en) * | 1995-03-24 | 1997-05-20 | Eli Lilly And Company | Process and solvate of 2-methyl-thieno-benzodiazepine |
| HU226167B1 (hu) * | 1996-09-23 | 2008-05-28 | Lilly Co Eli | Olanzapin-dihidrát D, elõállítása és az azt tartalmazó gyógyszerkészítmények |
-
1997
- 1997-09-02 ZA ZA978515A patent/ZA978515B/xx unknown
- 1997-09-18 TR TR1999/00640T patent/TR199900640T2/xx unknown
- 1997-09-18 WO PCT/US1997/016499 patent/WO1998012199A1/en not_active Ceased
- 1997-09-18 UA UA99031635A patent/UA59371C2/uk unknown
- 1997-09-18 RS YUP-155/99A patent/RS49598B/sr unknown
- 1997-09-18 PL PL381478A patent/PL196069B1/pl unknown
- 1997-09-18 EA EA199900326A patent/EA001642B1/ru not_active IP Right Cessation
- 1997-09-18 CA CA002265712A patent/CA2265712C/en not_active Expired - Lifetime
- 1997-09-18 IL IL12896297A patent/IL128962A/xx not_active IP Right Cessation
- 1997-09-18 BR BR9712100-2A patent/BR9712100A/pt not_active Application Discontinuation
- 1997-09-18 KR KR1019997002424A patent/KR100560015B1/ko not_active Expired - Lifetime
- 1997-09-18 PL PL97332482A patent/PL194565B1/pl unknown
- 1997-09-18 HU HU0000066A patent/HU226484B1/hu unknown
- 1997-09-18 PL PL381479A patent/PL196068B1/pl unknown
- 1997-09-18 NZ NZ334448A patent/NZ334448A/en not_active IP Right Cessation
- 1997-09-18 CZ CZ0099099A patent/CZ299248B6/cs not_active IP Right Cessation
- 1997-09-18 ID IDW990058D patent/ID27275A/id unknown
- 1997-09-18 CN CN97198137A patent/CN1122036C/zh not_active Expired - Lifetime
- 1997-09-18 AU AU44841/97A patent/AU719441B2/en not_active Expired
- 1997-09-18 JP JP10514842A patent/JP2001500877A/ja not_active Withdrawn
- 1997-09-19 IN IN1736CA1997 patent/IN187156B/en unknown
- 1997-09-22 AT AT97307383T patent/ATE209208T1/de active
- 1997-09-22 SV SV1997000081A patent/SV1997000081A/es not_active Application Discontinuation
- 1997-09-22 CO CO97055061A patent/CO4910140A1/es unknown
- 1997-09-22 MY MYPI97004392A patent/MY125565A/en unknown
- 1997-09-22 DE DE69708428T patent/DE69708428T2/de not_active Expired - Lifetime
- 1997-09-22 DK DK97307383T patent/DK0831098T3/da active
- 1997-09-22 EP EP97307383A patent/EP0831098B1/en not_active Expired - Lifetime
- 1997-09-22 ES ES97307383T patent/ES2166051T3/es not_active Expired - Lifetime
- 1997-09-22 SI SI9730288T patent/SI0831098T1/xx unknown
- 1997-09-22 PT PT97307383T patent/PT831098E/pt unknown
- 1997-09-23 EG EG98697A patent/EG23861A/xx active
- 1997-09-23 AR ARP970104362A patent/AR013838A1/es not_active Application Discontinuation
- 1997-09-23 US US08/935,884 patent/US6020487A/en not_active Expired - Lifetime
- 1997-09-23 PE PE1997000855A patent/PE110398A1/es active IP Right Grant
-
1998
- 1998-02-27 TW TW086113832A patent/TW470746B/zh not_active IP Right Cessation
-
1999
- 1999-03-22 NO NO19991382A patent/NO323980B1/no not_active IP Right Cessation
-
2009
- 2009-06-05 JP JP2009135901A patent/JP2009242407A/ja active Pending
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Legal Events
| Date | Code | Title | Description |
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| FC | Refusal |