Title:
ペリンドプリルエルブミンの新しい結晶型
Document Type and Number:
Japanese Patent JP2007507418
Kind Code:
A
Abstract:
Disclosed are two new crystalline forms, δ and ε, of perindopril erbumine. Those forms are suitable as therapeutic active substances for medicaments for the treatment of cardiovascular diseases, especially high blood pressure and heart failure. The ε crystalline form is obtained in the crystallization of perindopril erbumine at from 30 to 45° C., preferably from 34 to 45° C., from MTBE containing from 1.5 to 2.5% (v/v) water; the crystallization is advantageously carried out with stirring. If the water is then removed, advantageously by azeotropic distillation, preferably at from 35 to 37° C., and stirring is then continued for at least 15 h at from 30 to 45° C., preferably from 35 to 37° C., the ε crystalline form is converted to the δ crystalline form. The δ crystalline form can also be obtained by stirring the α or β crystalline form at from 33 to 38° C. in tert.-butyl methyl ether containing from 0.9 to 1.4% (v/v) water with seeding with the δ crystalline form. The ε crystalline form can also be obtained by stirring the α or β crystalline form at from 28 to 35° C. in tert.-butyl methyl ether containing from 0.9 to 1.4% (v/v) water with seeding with the ε crystalline form; or by stirring the α or β crystalline form at from 35 to 38° C. in tert.-butyl methyl ether containing from 1.5 to 2.0% (v/v) water.
Inventors:
Christoph Stressler
Vito Lelek
Roger Fesler
Vito Lelek
Roger Fesler
Application Number:
JP2006515624A
Publication Date:
March 29, 2007
Filing Date:
June 18, 2004
Export Citation:
Assignee:
LES LABORATOIRES SERVIER
International Classes:
C07D209/42; A61K31/404; A61P9/10; A61P9/12; A61P43/00
Foreign References:
| WO2001087835A1 | 2001-11-22 | |||
| WO2001087836A1 | 2001-11-22 | |||
| WO2001083439A2 | 2001-11-08 | |||
| WO1994015957A1 | 1994-07-21 |
Other References:
緒方章, 化学実験操作法 上巻, vol. 第２７版, JPN6009048171, 20 November 1963 (1963-11-20), pages 366 - 399, ISSN: 0001846064
社団法人日本化学会編, 第４版実験化学講座１基本操作Ｉ, JPN7008003682, 1990, pages 184 - 189, ISSN: 0001846065
J.MED.CHEM., vol. 34, JPN4003010488, 1991, pages 663 - 669, ISSN: 0001707949
社団法人日本化学会編, 第４版実験化学講座１基本操作Ｉ, JPN7008003682, 1990, pages 184 - 189, ISSN: 0001846065
J.MED.CHEM., vol. 34, JPN4003010488, 1991, pages 663 - 669, ISSN: 0001707949
Attorney, Agent or Firm:
Kyousei Tamura
Yushiro Tsuboi
Masahiro Nitta
Yushiro Tsuboi
Masahiro Nitta