Title:
NEW BENZATHINE SALTS OF ACE INHIBITORS, PROCESS FOR THEIR PREPARATION AND THEIR USE FOR THE TREATMENT OF CARDIOVASCULAR DISEASES
Document Type and Number:
WIPO Patent Application WO/2011/034509
Kind Code:
A3
Abstract:
The present invention describes new salts of ACE inhibitors with N5N'-dibenzylethylenediamine (abbr.: benzathine salts), a process for their preparation in crystal and amorphous forms by the reaction of two moles of ACE inhibitors with one mole of N,N'-dibenzylethylenediamine, a process for the preparation of pharmaceutical formulations containing these salts and their use for the treatment of cardiovascular diseases.
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Inventors:
RUCMAN RUDOLF (SI)
ZUPET PAVEL (SI)
ZUPET PAVEL (SI)
Application Number:
PCT/SI2010/000052
Publication Date:
May 12, 2011
Filing Date:
September 17, 2010
Export Citation:
Assignee:
SILVERSTONE PHARMA (LI)
RUCMAN RUDOLF (SI)
ZUPET PAVEL (SI)
RUCMAN RUDOLF (SI)
ZUPET PAVEL (SI)
International Classes:
A61K31/403; A61K31/401; A61K31/551; A61K31/675; A61K45/06; A61P9/00; A61P9/10; A61P9/12; C07D209/42; C07D209/52
Domestic Patent References:
| WO2008065431A1 | 2008-06-05 | |||
| WO2004041290A1 | 2004-05-21 | |||
| WO1999011260A1 | 1999-03-11 | |||
| WO2001080847A2 | 2001-11-01 |
Foreign References:
| JP2004250447A | 2004-09-09 | |||
| EP0391462A1 | 1990-10-10 | |||
| EP0545194A1 | 1993-06-09 | |||
| EP1296947A1 | 2003-04-02 |
Other References:
SUH J T ET AL: "Angiotensin-converting enzyme inhibitors. New orally active antihypertensive (mercaptoalkanoyl)- and [(acylthio)alkanoyl]glycine derivatives.", JOURNAL OF MEDICINAL CHEMISTRY JAN 1985 LNKD- PUBMED:2981324, vol. 28, no. 1, January 1985 (1985-01-01), pages 57 - 66, XP007917592, ISSN: 0022-2623
SCHWAB A ET AL: "Inhibition of angiotensin-converting enzym by derivaties of 3-mercapto-2-methyloropanoyl glycine", BIOCHEMICAL PHARMACOLOGY, PERGAMON, OXFORD, GB, vol. 32, no. 12, 15 June 1983 (1983-06-15), pages 1957 - 1960, XP023728404, ISSN: 0006-2952, [retrieved on 19830615], DOI: DOI:10.1016/0006-2952(83)90067-9
BYRN S R ET AL: "Chemical reactivity in solid-state pharmaceuticals: formulation implications.", ADVANCED DRUG DELIVERY REVIEWS 16 MAY 2001 LNKD- PUBMED:11325479, vol. 48, no. 1, 16 May 2001 (2001-05-16), pages 115 - 136, XP002628347, ISSN: 0169-409X
BASTIN R J ET AL: "Salt Selection and Optimisation for Pharmaceutical New Chemical Entities", ORGANIC PROCESS RESEARCH AND DEVELOPMENT, CAMBRIDGE, GB, vol. 4, no. 5, 1 January 2000 (2000-01-01), pages 427 - 435, XP002228592, DOI: DOI:10.1021/OP000018U
CAIRA M R: "CRYSTALLINE POLYMORPHISM OF ORGANIC COMPOUNDS", TOPICS IN CURRENT CHEMISTRY, SPRINGER, BERLIN, DE, vol. 198, 1 January 1998 (1998-01-01), pages 163 - 208, XP001156954, ISSN: 0340-1022, ISBN: 978-3-540-36760-4, DOI: DOI:10.1007/3-540-69178-2_5
SCHWAB A ET AL: "Inhibition of angiotensin-converting enzym by derivaties of 3-mercapto-2-methyloropanoyl glycine", BIOCHEMICAL PHARMACOLOGY, PERGAMON, OXFORD, GB, vol. 32, no. 12, 15 June 1983 (1983-06-15), pages 1957 - 1960, XP023728404, ISSN: 0006-2952, [retrieved on 19830615], DOI: DOI:10.1016/0006-2952(83)90067-9
BYRN S R ET AL: "Chemical reactivity in solid-state pharmaceuticals: formulation implications.", ADVANCED DRUG DELIVERY REVIEWS 16 MAY 2001 LNKD- PUBMED:11325479, vol. 48, no. 1, 16 May 2001 (2001-05-16), pages 115 - 136, XP002628347, ISSN: 0169-409X
BASTIN R J ET AL: "Salt Selection and Optimisation for Pharmaceutical New Chemical Entities", ORGANIC PROCESS RESEARCH AND DEVELOPMENT, CAMBRIDGE, GB, vol. 4, no. 5, 1 January 2000 (2000-01-01), pages 427 - 435, XP002228592, DOI: DOI:10.1021/OP000018U
CAIRA M R: "CRYSTALLINE POLYMORPHISM OF ORGANIC COMPOUNDS", TOPICS IN CURRENT CHEMISTRY, SPRINGER, BERLIN, DE, vol. 198, 1 January 1998 (1998-01-01), pages 163 - 208, XP001156954, ISSN: 0340-1022, ISBN: 978-3-540-36760-4, DOI: DOI:10.1007/3-540-69178-2_5
Attorney, Agent or Firm:
PATENTNA PISARNA D.O.O. (Pob 1725, 1000 Ljubljana, SI)
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