ES2197001A1 - Procedimiento de obtencion de un compuesto farmacuticamente activo. - Google Patents
Procedimiento de obtencion de un compuesto farmacuticamente activo.Info
- Publication number
- ES2197001A1 ES2197001A1 ES200200713A ES200200713A ES2197001A1 ES 2197001 A1 ES2197001 A1 ES 2197001A1 ES 200200713 A ES200200713 A ES 200200713A ES 200200713 A ES200200713 A ES 200200713A ES 2197001 A1 ES2197001 A1 ES 2197001A1
- Authority
- ES
- Spain
- Prior art keywords
- granisetron
- preparing
- compound
- formula
- active compound
- 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
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
- C07D453/06—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing isoquinuclidine ring systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/08—Bridged systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Hospice & Palliative Care (AREA)
- Pharmacology & Pharmacy (AREA)
- Otolaryngology (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Saccharide Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
Abstract
Procedimiento de obtención de un compuesto farmacéuticamente activo. Se refiere a un procedimiento de preparación de granisetrón, o una sal farmacéuticamente aceptable del mismo, que comprende: a) la ciclación de un compuesto de fórmula (I) en un disolvente inerte y a una temperatura comprendida entre 0-100°C, en presencia de un ácido fuerte, para rendir el compuesto de fórmula (II); b) la metilación del compuesto de fórmula (II), con un agente alquilante, en presencia de una base, en un disolvente inerte y a una temperatura comprendida entre 0°C-160°C, y opcionalmente formar una sal farmacéuticamente aceptable. Con el procedimiento de la invención se obtiene un granisetrón de alta pureza, evitándose las impurezas por desmetilación, al realizarse la metilación no antes sino después de la ciclación y con un mayor rendimiento.
Priority Applications (14)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| ES200200713A ES2197001B1 (es) | 2002-03-26 | 2002-03-26 | Procedimiento de obtencion de un compuesto farmaceuticamente activo. |
| AT03706845T ATE299144T1 (de) | 2002-03-26 | 2003-03-21 | Verfahren zur herstellung einer pharmazeutisch aktiven verbindung (granisetron) |
| KR1020047015135A KR100835553B1 (ko) | 2002-03-26 | 2003-03-21 | 약제학적 활성 화합물(그라니세트론)의 제조방법 |
| JP2003578360A JP4560293B2 (ja) | 2002-03-26 | 2003-03-21 | 医薬上有効な化合物（グラニセトロン）の製造方法 |
| DE60300986T DE60300986D1 (de) | 2002-03-26 | 2003-03-21 | Verfahren zur herstellung einer pharmazeutisch aktiven verbindung (granisetron) |
| PCT/IB2003/001058 WO2003080606A1 (en) | 2002-03-26 | 2003-03-21 | Process for preparing a pharmaceutically active compound (granisetron) |
| US10/508,493 US7071209B2 (en) | 2002-03-26 | 2003-03-21 | Process for preparing a pharmaceutically active compound (granisetron) |
| AU2003208552A AU2003208552A1 (en) | 2002-03-26 | 2003-03-21 | Process for preparing a pharmaceutically active compound (granisetron) |
| CA002481703A CA2481703A1 (en) | 2002-03-26 | 2003-03-21 | Process for preparing granisetron |
| PL374447A PL211464B1 (pl) | 2002-03-26 | 2003-03-21 | Sposób wytwarzania granisetronu, lub jego farmaceutycznie dopuszczalnej soli |
| PT03706845T PT1487833E (pt) | 2002-03-26 | 2003-03-21 | Processo de preparacao de um composto activo sob o ponto de vista farmaceutico (granisetron) |
| EP03706845A EP1487833B1 (en) | 2002-03-26 | 2003-03-21 | Process for preparing a pharmaceutically active compound (granisetron) |
| TW092106806A TWI291959B (en) | 2002-03-26 | 2003-03-26 | Process for preparing granisetron |
| IL16474204A IL164742A0 (en) | 2002-03-26 | 2004-10-20 | Process for prepating a pharmaceutically active compound (granisetron) |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| ES200200713A ES2197001B1 (es) | 2002-03-26 | 2002-03-26 | Procedimiento de obtencion de un compuesto farmaceuticamente activo. |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| ES2197001A1 true ES2197001A1 (es) | 2003-12-16 |
| ES2197001B1 ES2197001B1 (es) | 2004-11-16 |
Family
ID=28051970
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES200200713A Expired - Fee Related ES2197001B1 (es) | 2002-03-26 | 2002-03-26 | Procedimiento de obtencion de un compuesto farmaceuticamente activo. |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US7071209B2 (es) |
| EP (1) | EP1487833B1 (es) |
| JP (1) | JP4560293B2 (es) |
| KR (1) | KR100835553B1 (es) |
| AT (1) | ATE299144T1 (es) |
| AU (1) | AU2003208552A1 (es) |
| CA (1) | CA2481703A1 (es) |
| DE (1) | DE60300986D1 (es) |
| ES (1) | ES2197001B1 (es) |
| IL (1) | IL164742A0 (es) |
| PL (1) | PL211464B1 (es) |
| PT (1) | PT1487833E (es) |
| TW (1) | TWI291959B (es) |
| WO (1) | WO2003080606A1 (es) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EE05516B1 (et) | 2002-09-25 | 2012-02-15 | Memory@Pharmaceuticals@Corporation | Indasoolid bensotiasoolid ja bensoisotiasoolid nende valmistamine ning kasutamine |
| ES2295973T3 (es) | 2003-12-22 | 2008-04-16 | Memory Pharmaceuticals Corporation | Indoles, 1h-indazoles, 1,2-bencisoxazoles, y 1,2-bencisotiazoles, y preparacion y usos de los mismos. |
| EP1735306A2 (en) | 2004-03-25 | 2006-12-27 | Memory Pharmaceuticals Corporation | Indazoles, benzothiazoles, benzoisothiazoles, benzisoxazoles, and preparation and uses thereof |
| DE602005024677D1 (de) | 2004-04-22 | 2010-12-23 | Memory Pharm Corp | Indole, 1h-indazole, 1,2-benzisoxazole, 1,2-benzoisothiazole, deren herstellung und verwendungen |
| BRPI0510212A (pt) | 2004-05-07 | 2007-10-16 | Memory Pharm Corp | 1h-indazóis, benzotiazóis, 1,2 - benzoisoxazóis, 1,2-benzoisotiazóis, e cromonas e a preparação e usos dos mesmos |
| RU2418797C2 (ru) | 2004-12-22 | 2011-05-20 | Мемори Фармасьютиклз Корпорейшн | Лиганды никотинового рецептора альфа-7, их получение и применение |
| RU2420525C2 (ru) | 2005-07-11 | 2011-06-10 | Мицубиси Танабе Фарма Корпорейшн | Производные оксимов и их получение |
| US8911751B2 (en) | 2005-10-11 | 2014-12-16 | Yissum Research Development Company Of The Hebrew University Of Jerusalem | Compositions for nasal delivery |
| WO2007088557A1 (en) * | 2006-02-01 | 2007-08-09 | Natco Pharma Limited | Process for highly pure crystalline granisetron base |
| US20080242696A1 (en) * | 2007-03-27 | 2008-10-02 | Chemagis Ltd. | Crystalline granisetron base and production process therefor |
| WO2008151677A1 (en) | 2007-06-13 | 2008-12-18 | Inke, S.A. | Polymorphic form of granisetron base, methods for obtaining it and formulation containing it |
| EP2323654A4 (en) * | 2008-08-19 | 2012-10-24 | Scinopharm Taiwan Ltd | POLYMORPHIC FORMS OF GRANISETRONHYDROCHLORIDE AND METHOD FOR THE PRODUCTION THEREOF |
| US20120101089A1 (en) * | 2010-10-26 | 2012-04-26 | Ashwani Agarwal | Anti-Emetic Substance |
| CN112778203B (zh) * | 2021-01-29 | 2022-02-15 | 兰州交通大学 | 1h-吲唑-3-羧酸衍生物及格拉斯琼和氯尼达明的制备方法 |
| CN115372487B (zh) * | 2021-05-18 | 2023-10-10 | 成都倍特得诺药业有限公司 | 盐酸格拉司琼中杂质e的hplc测定方法 |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1997030049A1 (en) * | 1996-02-13 | 1997-08-21 | Smithkline Beecham Plc | Process for the preparation of granisetron |
| ES2129349A1 (es) * | 1996-02-13 | 1999-06-01 | Smithkline Beecham Plc | Procedimiento para preparar granisetron. |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE3650772T2 (de) | 1985-04-27 | 2003-04-03 | F. Hoffmann-La Roche Ag, Basel | Derivate von Indazole-3-carboxamide und -3-carboxylsäure |
| GB9404055D0 (en) * | 1994-03-03 | 1994-04-20 | Smithkline Beecham Plc | Novel process |
-
2002
- 2002-03-26 ES ES200200713A patent/ES2197001B1/es not_active Expired - Fee Related
-
2003
- 2003-03-21 JP JP2003578360A patent/JP4560293B2/ja not_active Expired - Fee Related
- 2003-03-21 KR KR1020047015135A patent/KR100835553B1/ko not_active IP Right Cessation
- 2003-03-21 EP EP03706845A patent/EP1487833B1/en not_active Expired - Lifetime
- 2003-03-21 AT AT03706845T patent/ATE299144T1/de not_active IP Right Cessation
- 2003-03-21 AU AU2003208552A patent/AU2003208552A1/en not_active Abandoned
- 2003-03-21 US US10/508,493 patent/US7071209B2/en not_active Expired - Fee Related
- 2003-03-21 PL PL374447A patent/PL211464B1/pl not_active IP Right Cessation
- 2003-03-21 PT PT03706845T patent/PT1487833E/pt unknown
- 2003-03-21 DE DE60300986T patent/DE60300986D1/de not_active Expired - Lifetime
- 2003-03-21 CA CA002481703A patent/CA2481703A1/en not_active Abandoned
- 2003-03-21 WO PCT/IB2003/001058 patent/WO2003080606A1/en active IP Right Grant
- 2003-03-26 TW TW092106806A patent/TWI291959B/zh active
-
2004
- 2004-10-20 IL IL16474204A patent/IL164742A0/xx unknown
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1997030049A1 (en) * | 1996-02-13 | 1997-08-21 | Smithkline Beecham Plc | Process for the preparation of granisetron |
| ES2129349A1 (es) * | 1996-02-13 | 1999-06-01 | Smithkline Beecham Plc | Procedimiento para preparar granisetron. |
Also Published As
| Publication number | Publication date |
|---|---|
| DE60300986D1 (de) | 2005-08-11 |
| KR100835553B1 (ko) | 2008-06-09 |
| TW200305572A (en) | 2003-11-01 |
| WO2003080606A1 (en) | 2003-10-02 |
| EP1487833A1 (en) | 2004-12-22 |
| PL374447A1 (en) | 2005-10-17 |
| US7071209B2 (en) | 2006-07-04 |
| WO2003080606A8 (en) | 2005-03-17 |
| US20050124650A1 (en) | 2005-06-09 |
| EP1487833B1 (en) | 2005-07-06 |
| ATE299144T1 (de) | 2005-07-15 |
| IL164742A0 (en) | 2005-12-18 |
| ES2197001B1 (es) | 2004-11-16 |
| JP2006511439A (ja) | 2006-04-06 |
| AU2003208552A1 (en) | 2003-10-08 |
| JP4560293B2 (ja) | 2010-10-13 |
| TWI291959B (en) | 2008-01-01 |
| PL211464B1 (pl) | 2012-05-31 |
| CA2481703A1 (en) | 2003-10-02 |
| KR20040099361A (ko) | 2004-11-26 |
| PT1487833E (pt) | 2005-11-30 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| EC2A | Search report published |
Date of ref document: 20031216 Kind code of ref document: A1 |
|
| FG2A | Definitive protection |
Ref document number: 2197001B1 Country of ref document: ES |
|
| FD2A | Announcement of lapse in spain |
Effective date: 20220629 |