ES2164520A1 - "procedimiento de obtencion del polimorfo a del mesilato de doxazosina" - Google Patents
"procedimiento de obtencion del polimorfo a del mesilato de doxazosina"Info
- Publication number
- ES2164520A1 ES2164520A1 ES009900535A ES9900535A ES2164520A1 ES 2164520 A1 ES2164520 A1 ES 2164520A1 ES 009900535 A ES009900535 A ES 009900535A ES 9900535 A ES9900535 A ES 9900535A ES 2164520 A1 ES2164520 A1 ES 2164520A1
- Authority
- ES
- Spain
- Prior art keywords
- polymorph
- mesylate
- alcohol
- solvent
- doxazosine
- 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.)
- Granted
Links
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 title abstract 3
- 229960001389 doxazosin Drugs 0.000 title abstract 2
- RUZYUOTYCVRMRZ-UHFFFAOYSA-N doxazosin Chemical compound C1OC2=CC=CC=C2OC1C(=O)N(CC1)CCN1C1=NC(N)=C(C=C(C(OC)=C2)OC)C2=N1 RUZYUOTYCVRMRZ-UHFFFAOYSA-N 0.000 title abstract 2
- 238000000034 method Methods 0.000 title abstract 2
- 239000002904 solvent Substances 0.000 abstract 4
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 abstract 2
- 238000004821 distillation Methods 0.000 abstract 1
- 229960000220 doxazosin mesylate Drugs 0.000 abstract 1
- VJECBOKJABCYMF-UHFFFAOYSA-N doxazosin mesylate Chemical compound [H+].CS([O-])(=O)=O.C1OC2=CC=CC=C2OC1C(=O)N(CC1)CCN1C1=NC(N)=C(C=C(C(OC)=C2)OC)C2=N1 VJECBOKJABCYMF-UHFFFAOYSA-N 0.000 abstract 1
- 238000010438 heat treatment Methods 0.000 abstract 1
- 229940098779 methanesulfonic acid Drugs 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 230000001376 precipitating effect Effects 0.000 abstract 1
- 238000002360 preparation method Methods 0.000 abstract 1
- 238000010992 reflux Methods 0.000 abstract 1
- 239000000725 suspension Substances 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Plural Heterocyclic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Polymers With Sulfur, Phosphorus Or Metals In The Main Chain (AREA)
Abstract
"Procedimiento de obtención del polimorfo A del mesilato de doxazosina", consistente esencialmente en hacer reaccionar la doxazosina base con el ácido metansulfónico en el seno de una mezcla de disolventes que contiene un alcohol y un disolvente clorado, eliminar posteriormente por destilación el disolvente clorado y precipitar el producto deseado en el seno de un alcohol, previo calentamiento de la suspensión formada a la temperatura de reflujo del disolvente.
Priority Applications (12)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| ES009900535A ES2164520B1 (es) | 1999-03-16 | 1999-03-16 | "procedimiento de obtencion del polimorfo a del mesilato de doxazosina" |
| DE60000661T DE60000661T2 (de) | 1999-03-16 | 2000-03-13 | Eine methode zur herstellung eines polymorphes von einem doxazosin-mesylat |
| EP00909370A EP1162202B1 (en) | 1999-03-16 | 2000-03-13 | Method for obtaining polymorph a from doxazosine mesylate |
| PCT/ES2000/000086 WO2000055157A1 (es) | 1999-03-16 | 2000-03-13 | Procedimiento de obtencion del polimorfo a del mesilato de doxazosina |
| AT00909370T ATE226580T1 (de) | 1999-03-16 | 2000-03-13 | Eine methode zur herstellung eines polymorphes von einem doxazosin-mesylat |
| PT00909370T PT1162202E (pt) | 1999-03-16 | 2000-03-13 | Processo para a preparacao do polimorfo a a partir de mesilato de doxazosina |
| US09/913,778 US6525195B1 (en) | 1999-03-16 | 2000-03-13 | Method for obtaining polymorph a from doxazosine mesylate |
| ES00909370T ES2184698T3 (es) | 1999-03-16 | 2000-03-13 | Procedimiento de obtencion de polimorfo a del mesilato de doxazosina. |
| SI200030037T SI1162202T1 (en) | 1999-03-16 | 2000-03-13 | Method for obtaining polymorph a from doxazosine mesylate |
| AU31675/00A AU3167500A (en) | 1999-03-16 | 2000-03-13 | Method for obtaining polymorph a from doxazosine mesylate |
| CA2367671A CA2367671C (en) | 1999-03-16 | 2000-03-13 | Process for the preparation of the polymorph a of doxazosin mesylate |
| DK00909370T DK1162202T3 (da) | 1999-03-16 | 2000-03-13 | Fremgangsmåde til at opnå en polymorf fra Doxazosinmesylat |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| ES009900535A ES2164520B1 (es) | 1999-03-16 | 1999-03-16 | "procedimiento de obtencion del polimorfo a del mesilato de doxazosina" |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| ES2164520A1 true ES2164520A1 (es) | 2002-02-16 |
| ES2164520B1 ES2164520B1 (es) | 2003-04-01 |
Family
ID=8307680
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES009900535A Expired - Lifetime ES2164520B1 (es) | 1999-03-16 | 1999-03-16 | "procedimiento de obtencion del polimorfo a del mesilato de doxazosina" |
| ES00909370T Expired - Lifetime ES2184698T3 (es) | 1999-03-16 | 2000-03-13 | Procedimiento de obtencion de polimorfo a del mesilato de doxazosina. |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES00909370T Expired - Lifetime ES2184698T3 (es) | 1999-03-16 | 2000-03-13 | Procedimiento de obtencion de polimorfo a del mesilato de doxazosina. |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US6525195B1 (es) |
| EP (1) | EP1162202B1 (es) |
| AT (1) | ATE226580T1 (es) |
| AU (1) | AU3167500A (es) |
| CA (1) | CA2367671C (es) |
| DE (1) | DE60000661T2 (es) |
| DK (1) | DK1162202T3 (es) |
| ES (2) | ES2164520B1 (es) |
| PT (1) | PT1162202E (es) |
| WO (1) | WO2000055157A1 (es) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE19912573A1 (de) * | 1999-03-19 | 2000-09-21 | Knoll Ag | Arzneimittel, enthaltend Doxazosin-Mesylat der Kristallmodifikaton D |
| US7067700B2 (en) | 2001-05-31 | 2006-06-27 | Fermion Oy | Process for preparing sertraline hydrochloride polymorphic form II |
| JP2005536462A (ja) | 2002-04-30 | 2005-12-02 | ユン ジン ファーマスーチカル インダストリーズ カンパニー リミテッド | カスパーゼ−3阻害剤としてのキノリン誘導体、この製造方法及びこれを含む薬剤学的組成物 |
| CA2706372A1 (en) * | 2007-12-24 | 2009-07-02 | Cipla Limited | Crystalline polymorph of doxazosin mesylate (form iv) and process for preparation thereof |
| WO2016151466A1 (en) * | 2015-03-26 | 2016-09-29 | Unichem Laboratories Limited | Process of preparing potassium salt of azilsartan medoxomil |
| CN111303130B (zh) * | 2018-12-11 | 2021-09-14 | 合肥立方制药股份有限公司 | 一种多沙唑嗪甲磺酸盐晶型、其制备方法及用途 |
Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1996039406A1 (en) * | 1995-06-06 | 1996-12-12 | Pfizer Inc. | NOVEL CRYSTAL FORM OF ANHYDROUS 7-([1α, 5α, 6α]-6-AMINO-3-AZABICYCLO[3.1.0]HEX-3-YL)-6-FLUORO-1-(2,4-DIFLUOROPHENYL)-1,4-DIHYDRO-4-OXO-1,8-NAPHTHYRIDINE-3-CARBOXYLIC ACID, METHANESULFONIC ACID SALT |
| EP0848001A1 (en) * | 1996-12-13 | 1998-06-17 | Alfa Chemicals Italiana S.r.l. | Crystalline form of the doxazosin mesylate and process for its production |
| EP0849264A1 (de) * | 1996-12-20 | 1998-06-24 | HEUMANN PHARMA GmbH | Neue polymorphe Form von doxazosinmesylat (Form I) |
| EP0849265A1 (de) * | 1996-12-20 | 1998-06-24 | HEUMANN PHARMA GmbH | Neue polymorphe Form von Doxazosin-Mesylat (Form II) |
| EP0849266A1 (de) * | 1996-12-20 | 1998-06-24 | HEUMANN PHARMA GmbH | Neue polymorphe Form von Doxazosinmesylat (Form III) |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4188390A (en) | 1977-11-05 | 1980-02-12 | Pfizer Inc. | Antihypertensive 4-amino-2-[4-(1,4-benzodioxan-2-carbonyl) piperazin-1-yl or homopiperazin-1-yl]quinazolines |
| DE19800214A1 (de) | 1998-01-06 | 1999-07-15 | Knoll Ag | Verfahren zur Herstellung von Doxazosin-Mcsylat in einer als Form A bezeichneten Kristallmodifikation und ein Zwischenprodukt dafür |
-
1999
- 1999-03-16 ES ES009900535A patent/ES2164520B1/es not_active Expired - Lifetime
-
2000
- 2000-03-13 ES ES00909370T patent/ES2184698T3/es not_active Expired - Lifetime
- 2000-03-13 AT AT00909370T patent/ATE226580T1/de not_active IP Right Cessation
- 2000-03-13 PT PT00909370T patent/PT1162202E/pt unknown
- 2000-03-13 DE DE60000661T patent/DE60000661T2/de not_active Expired - Lifetime
- 2000-03-13 DK DK00909370T patent/DK1162202T3/da active
- 2000-03-13 WO PCT/ES2000/000086 patent/WO2000055157A1/es not_active Ceased
- 2000-03-13 US US09/913,778 patent/US6525195B1/en not_active Expired - Fee Related
- 2000-03-13 EP EP00909370A patent/EP1162202B1/en not_active Expired - Lifetime
- 2000-03-13 AU AU31675/00A patent/AU3167500A/en not_active Abandoned
- 2000-03-13 CA CA2367671A patent/CA2367671C/en not_active Expired - Fee Related
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1996039406A1 (en) * | 1995-06-06 | 1996-12-12 | Pfizer Inc. | NOVEL CRYSTAL FORM OF ANHYDROUS 7-([1α, 5α, 6α]-6-AMINO-3-AZABICYCLO[3.1.0]HEX-3-YL)-6-FLUORO-1-(2,4-DIFLUOROPHENYL)-1,4-DIHYDRO-4-OXO-1,8-NAPHTHYRIDINE-3-CARBOXYLIC ACID, METHANESULFONIC ACID SALT |
| EP0848001A1 (en) * | 1996-12-13 | 1998-06-17 | Alfa Chemicals Italiana S.r.l. | Crystalline form of the doxazosin mesylate and process for its production |
| EP0849264A1 (de) * | 1996-12-20 | 1998-06-24 | HEUMANN PHARMA GmbH | Neue polymorphe Form von doxazosinmesylat (Form I) |
| EP0849265A1 (de) * | 1996-12-20 | 1998-06-24 | HEUMANN PHARMA GmbH | Neue polymorphe Form von Doxazosin-Mesylat (Form II) |
| EP0849266A1 (de) * | 1996-12-20 | 1998-06-24 | HEUMANN PHARMA GmbH | Neue polymorphe Form von Doxazosinmesylat (Form III) |
Also Published As
| Publication number | Publication date |
|---|---|
| ES2184698T3 (es) | 2003-04-16 |
| ATE226580T1 (de) | 2002-11-15 |
| EP1162202B1 (en) | 2002-10-23 |
| US6525195B1 (en) | 2003-02-25 |
| PT1162202E (pt) | 2003-02-28 |
| WO2000055157A1 (es) | 2000-09-21 |
| DE60000661D1 (de) | 2002-11-28 |
| DK1162202T3 (da) | 2003-02-24 |
| CA2367671A1 (en) | 2000-09-21 |
| EP1162202A1 (en) | 2001-12-12 |
| AU3167500A (en) | 2000-10-04 |
| DE60000661T2 (de) | 2003-06-26 |
| ES2164520B1 (es) | 2003-04-01 |
| CA2367671C (en) | 2010-06-01 |
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Legal Events
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| EC2A | Search report published |
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