WO2008090565B1 - Novel thermodynamically stable polymorphic form-l of letrozole - Google Patents
Novel thermodynamically stable polymorphic form-l of letrozoleInfo
- Publication number
- WO2008090565B1 WO2008090565B1 PCT/IN2007/000112 IN2007000112W WO2008090565B1 WO 2008090565 B1 WO2008090565 B1 WO 2008090565B1 IN 2007000112 W IN2007000112 W IN 2007000112W WO 2008090565 B1 WO2008090565 B1 WO 2008090565B1
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- letrozole
- polymorphic form
- novel crystalline
- preparation
- crystalline polymorphic
- 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.)
- Ceased
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
- C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
- C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
The present invention relates to a novel crystalline Form L of letrozole and a process for preparing the same. Letrozole is useful for the first-line treatment in post-menopausal women with hormone receptor positive (or) locally advanced (or) metastatic breast cancer.
Claims
AMENDED CLAIMS received by the International Bureau on 25 January 2008 (25.01.08) original claims 1-3 and 6 are amended, remaining unchanged claims.
1) A crystalline thermodynamically stable polymorphic form of Letrozole designated as Form L having the XPRD characteristics given in Table-I and Fig -1 TABLE-I
2) A thermodynamically stable polymorphic form of letrozole designated as form L having IR and DSC characteristics as in figs. 2 and 3.
3) A process for the preparation of a novel crystalline polymorphic form of Letrozole designated as Form L, comprising crystallization from solvents methanol, chloroform, acetone, ethyl acetate, dioxane.
4) A process for the preparation of novel crystalline polymorphic form L of letrozole comprising lyophilization of a solution of the drug substance in an alcoholic solvent like methanol.
14
5) A process for the preparation of novel crystalline polymorphic form L of letrozole comprising precipitation from solutions in solvents like methanol, DMF, acetic acid by anti-solvents like water, isopropanol and isopropyl ether.
6) A process for the preparation of novel crystalline polymorphic form L of letrozole comprising regeneration from solution in acids like Hydrochloric acid, sulfuric acid and acetic acid by bases ammonia or sodium hydroxide.
7) A process for the preparation of novel crystalline polymorphic form L of letrozole substantially as herein described with reference to the examples 1-16
8) A pharmaceutical composition containing the novel crystalline polymorphic form L of Letrozole substantially as herein described with reference to example 17
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP07736572A EP2155698A1 (en) | 2007-01-22 | 2007-03-20 | Novel thermodynamically stable polymorphic form-l of letrozole |
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IN148/CHE/2007 | 2007-01-22 | ||
| IN148CH2007 | 2007-01-22 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| WO2008090565A1 WO2008090565A1 (en) | 2008-07-31 |
| WO2008090565B1 true WO2008090565B1 (en) | 2008-11-06 |
Family
ID=38617241
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PCT/IN2007/000112 Ceased WO2008090565A1 (en) | 2007-01-22 | 2007-03-20 | Novel thermodynamically stable polymorphic form-l of letrozole |
Country Status (2)
| Country | Link |
|---|---|
| EP (1) | EP2155698A1 (en) |
| WO (1) | WO2008090565A1 (en) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2008516005A (en) | 2005-07-06 | 2008-05-15 | シコール インコーポレイティド | Improved preparation of letrozole |
| CN102070541B (en) * | 2010-10-25 | 2013-07-10 | 深圳海王药业有限公司 | Letrozole I-type crystal and preparation method thereof |
| CN109721558B (en) * | 2017-10-27 | 2025-11-18 | 中国医学科学院药物研究所 | Letrozole crystal type III solid substance, its preparation method, its pharmaceutical composition and uses |
| CN109721557B (en) * | 2017-10-27 | 2025-11-18 | 中国医学科学院药物研究所 | Letrozole crystal type II solid substance, its preparation method, its pharmaceutical composition and uses |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4978672A (en) * | 1986-03-07 | 1990-12-18 | Ciba-Geigy Corporation | Alpha-heterocyclc substituted tolunitriles |
| WO2004076409A2 (en) * | 2003-02-06 | 2004-09-10 | Sun Pharmaceutical Industries Limited | Regiospecific process for the preparation of 4-[1- (4-cyanophenyl)-1-(1,2,4-triazol-1-yl)methyl]benzonitrile |
| US20070100149A1 (en) * | 2005-11-02 | 2007-05-03 | Palle Venkata Raghavendra A | Process for preparing letrozole |
| US7465749B2 (en) * | 2005-11-14 | 2008-12-16 | Chemagis, Ltd. | Letrozole purification process |
-
2007
- 2007-03-20 EP EP07736572A patent/EP2155698A1/en not_active Withdrawn
- 2007-03-20 WO PCT/IN2007/000112 patent/WO2008090565A1/en not_active Ceased
Also Published As
| Publication number | Publication date |
|---|---|
| EP2155698A1 (en) | 2010-02-24 |
| WO2008090565A1 (en) | 2008-07-31 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| 121 | Ep: the epo has been informed by wipo that ep was designated in this application |
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