ES2197001B1 - Procedimiento de obtencion de un compuesto farmaceuticamente activo. - Google Patents
Procedimiento de obtencion de un compuesto farmaceuticamente activo.Info
- Publication number
- ES2197001B1 ES2197001B1 ES200200713A ES200200713A ES2197001B1 ES 2197001 B1 ES2197001 B1 ES 2197001B1 ES 200200713 A ES200200713 A ES 200200713A ES 200200713 A ES200200713 A ES 200200713A ES 2197001 B1 ES2197001 B1 ES 2197001B1
- Authority
- ES
- Spain
- Prior art keywords
- procedure
- compound
- obtaining
- pharmaceutically active
- formula
- 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.)
- Expired - Fee Related
Links
- 150000001875 compounds Chemical class 0.000 title abstract 5
- 238000000034 method Methods 0.000 title abstract 4
- MFWNKCLOYSRHCJ-BTTYYORXSA-N granisetron Chemical compound C1=CC=C2C(C(=O)N[C@H]3C[C@H]4CCC[C@@H](C3)N4C)=NN(C)C2=C1 MFWNKCLOYSRHCJ-BTTYYORXSA-N 0.000 abstract 2
- 229960003727 granisetron Drugs 0.000 abstract 2
- 239000012442 inert solvent Substances 0.000 abstract 2
- 230000011987 methylation Effects 0.000 abstract 2
- 238000007069 methylation reaction Methods 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 239000002253 acid Substances 0.000 abstract 1
- 229940100198 alkylating agent Drugs 0.000 abstract 1
- 239000002168 alkylating agent Substances 0.000 abstract 1
- 230000001351 cycling effect Effects 0.000 abstract 1
- 230000017858 demethylation Effects 0.000 abstract 1
- 238000010520 demethylation reaction Methods 0.000 abstract 1
- 239000012535 impurity Substances 0.000 abstract 1
- 238000007363 ring formation reaction Methods 0.000 abstract 1
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
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Otolaryngology (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Hospice & Palliative Care (AREA)
- Life Sciences & Earth Sciences (AREA)
- Bioinformatics & Cheminformatics (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
0-100ºC, 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
0ºC-160ºC, 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. |
| PCT/IB2003/001058 WO2003080606A1 (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 |
| EP03706845A EP1487833B1 (en) | 2002-03-26 | 2003-03-21 | Process for preparing a pharmaceutically active compound (granisetron) |
| PT03706845T PT1487833E (pt) | 2002-03-26 | 2003-03-21 | Processo de preparacao de um composto activo sob o ponto de vista farmaceutico (granisetron) |
| US10/508,493 US7071209B2 (en) | 2002-03-26 | 2003-03-21 | Process for preparing a pharmaceutically active compound (granisetron) |
| DE60300986T DE60300986D1 (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 |
| PL374447A PL211464B1 (pl) | 2002-03-26 | 2003-03-21 | Sposób wytwarzania granisetronu, lub jego farmaceutycznie dopuszczalnej soli |
| AU2003208552A AU2003208552A1 (en) | 2002-03-26 | 2003-03-21 | Process for preparing a pharmaceutically active compound (granisetron) |
| 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 |
| AT03706845T ATE299144T1 (de) | 2002-03-26 | 2003-03-21 | Verfahren zur herstellung einer pharmazeutisch aktiven verbindung (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 ES2197001A1 (es) | 2003-12-16 |
| ES2197001B1 true 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 |
|---|---|---|---|---|
| PL210065B1 (pl) | 2002-09-25 | 2011-11-30 | Memory Pharm Corp | Związki indazole, benzotiazole i benzoizotiazole, kompozycje farmaceutyczne je zawierające oraz zastosowanie związków |
| EP1697378B1 (en) | 2003-12-22 | 2007-11-21 | Memory Pharmaceuticals Corporation | Indoles, 1h-indazoles, 1,2-benzisoxazoles, and 1,2-benzisothiazoles, and preparation and uses thereof |
| EP1735306A2 (en) | 2004-03-25 | 2006-12-27 | Memory Pharmaceuticals Corporation | Indazoles, benzothiazoles, benzoisothiazoles, benzisoxazoles, and preparation and uses thereof |
| EP1742944B1 (en) | 2004-04-22 | 2010-11-10 | Memory Pharmaceuticals Corporation | Indoles, 1h-indazoles, 1,2-benzisoxazoles, 1,2-benzoisothiazoles, and preparation and uses thereof |
| KR20070015607A (ko) | 2004-05-07 | 2007-02-05 | 메모리 파마슈티칼스 코포레이션 | 1ｈ-인다졸, 벤조티아졸, 1,2-벤조이속사졸,1,2-벤조이소티아졸, 및 크로몬 및 그의 제조법 및 용도 |
| ATE455776T1 (de) | 2004-12-22 | 2010-02-15 | Memory Pharm Corp | Nikotinische alpha-7-rezeptorliganden gegen erkrankungen des zns |
| AR057661A1 (es) | 2005-07-11 | 2007-12-12 | Tanabe Seiyaku Co | Un derivado de oxima y sus preparaciones |
| 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 |
| JP2012500276A (ja) * | 2008-08-19 | 2012-01-05 | サイノファーム タイワン リミテッド | グラニセトロン塩酸塩の多形体とその製造方法 |
| 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 |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0200444B1 (en) | 1985-04-27 | 1992-11-11 | Beecham Group Plc | Azabicyclononyl-indazole-carboxamide having 5-ht antagonist activity |
| GB9404055D0 (en) | 1994-03-03 | 1994-04-20 | Smithkline Beecham Plc | Novel process |
| GB9602866D0 (en) * | 1996-02-13 | 1996-04-10 | Smithkline Beecham Plc | Novel process |
| GB9602862D0 (en) * | 1996-02-13 | 1996-04-10 | Smithkline Beecham Plc | Novel process |
-
2002
- 2002-03-26 ES ES200200713A patent/ES2197001B1/es not_active Expired - Fee Related
-
2003
- 2003-03-21 KR KR1020047015135A patent/KR100835553B1/ko not_active Expired - Fee Related
- 2003-03-21 JP JP2003578360A patent/JP4560293B2/ja not_active Expired - Fee Related
- 2003-03-21 AT AT03706845T patent/ATE299144T1/de not_active IP Right Cessation
- 2003-03-21 US US10/508,493 patent/US7071209B2/en not_active Expired - Fee Related
- 2003-03-21 AU AU2003208552A patent/AU2003208552A1/en not_active Abandoned
- 2003-03-21 EP EP03706845A patent/EP1487833B1/en not_active Expired - Lifetime
- 2003-03-21 PL PL374447A patent/PL211464B1/pl not_active IP Right Cessation
- 2003-03-21 CA CA002481703A patent/CA2481703A1/en not_active Abandoned
- 2003-03-21 DE DE60300986T patent/DE60300986D1/de not_active Expired - Lifetime
- 2003-03-21 WO PCT/IB2003/001058 patent/WO2003080606A1/en not_active Ceased
- 2003-03-21 PT PT03706845T patent/PT1487833E/pt unknown
- 2003-03-26 TW TW092106806A patent/TWI291959B/zh active
-
2004
- 2004-10-20 IL IL16474204A patent/IL164742A0/xx unknown
Also Published As
| Publication number | Publication date |
|---|---|
| ES2197001A1 (es) | 2003-12-16 |
| DE60300986D1 (de) | 2005-08-11 |
| JP2006511439A (ja) | 2006-04-06 |
| WO2003080606A8 (en) | 2005-03-17 |
| IL164742A0 (en) | 2005-12-18 |
| JP4560293B2 (ja) | 2010-10-13 |
| AU2003208552A1 (en) | 2003-10-08 |
| TW200305572A (en) | 2003-11-01 |
| PL374447A1 (en) | 2005-10-17 |
| PL211464B1 (pl) | 2012-05-31 |
| CA2481703A1 (en) | 2003-10-02 |
| ATE299144T1 (de) | 2005-07-15 |
| EP1487833B1 (en) | 2005-07-06 |
| KR100835553B1 (ko) | 2008-06-09 |
| KR20040099361A (ko) | 2004-11-26 |
| US7071209B2 (en) | 2006-07-04 |
| TWI291959B (en) | 2008-01-01 |
| EP1487833A1 (en) | 2004-12-22 |
| WO2003080606A1 (en) | 2003-10-02 |
| US20050124650A1 (en) | 2005-06-09 |
| 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 |
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| FD2A | Announcement of lapse in spain |
Effective date: 20220629 |