Title:
PROCESS FOR PRODUCING FINGOLIMOD SALTS
Document Type and Number:
WIPO Patent Application WO/2011/009634
Kind Code:
A3
Abstract:
The invention relates to a process for producing pharmaceutically acceptable salts of fingolimod (I), comprising the step of reacting N-[1,1-bis hydroxymethyl-3-(4-octyl phenyl)-propyl]-acylamide (II) with an acidic compound. Furthermore, the invention provides different pharmaceutically acceptable salts of fingolimod and a polymorphic form of fingolimod hydrochloride.
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Inventors:
GIDWANI RAMESH MATIORAM (IN)
HIREMATH CHANNAVEERAYYA (IN)
HIREMATH CHANNAVEERAYYA (IN)
Application Number:
PCT/EP2010/004547
Publication Date:
November 10, 2011
Filing Date:
July 23, 2010
Export Citation:
Assignee:
RATIOPHARM GMBH (DE)
GIDWANI RAMESH MATIORAM (IN)
HIREMATH CHANNAVEERAYYA (IN)
GIDWANI RAMESH MATIORAM (IN)
HIREMATH CHANNAVEERAYYA (IN)
International Classes:
C07C55/07; C07C213/08; C07C55/10; C07C55/14; C07C59/50; C07C215/28; C07C231/12; C07C233/18
Domestic Patent References:
| WO2007143081A2 | 2007-12-13 | |||
| WO2007041368A2 | 2007-04-12 | |||
| WO2003097028A1 | 2003-11-27 | |||
| WO2009115534A1 | 2009-09-24 | |||
| WO2010055027A2 | 2010-05-20 |
Foreign References:
| CN1814583A | 2006-08-09 | |||
| JPH11310556A | 1999-11-09 | |||
| EP0812588A1 | 1997-12-17 | |||
| US6476004B1 | 2002-11-05 |
Other References:
FUJITA, T. ET AL.: "Potent immunosuppressants, 2-alkyl-2-aminopropane-1,3-diols", J. MED. CHEM., vol. 39, 1996, pages 4451 - 4459, XP002646477
CHIBA, K. ET AL.: "FTY720. 2-Amino-2[2-(4-octylphenyl)ethyl]-1,3-propanediol hydrochloride", DRUGS OF THE FUTURE, PROUS SCIENCE, ES, vol. 22, no. 1, 1997, pages 18 - 22, XP008128504, ISSN: 0377-8282
KIUCHI, M. ET AL.: "Synthesis and immunosuppressive activity of 2-substituted 2-aminopropane-1,3-diols and 2-aminoethanols", JOURNAL OF MEDICINAL CHEMISTRY, vol. 43, 2000, pages 2946 - 2961, XP002271142, ISSN: 0022-2623, DOI: DOI:10.1021/JM000173Z
CHINO, M. ET AL.: "An efficient total synthesis of a sphingosine-1-phosphate receptor agonist KRP-203", TETRAHEDRON, vol. 64, no. 17, 2008, pages 3859 - 3866, XP022520419, ISSN: 0040-4020, DOI: DOI:10.1016/J.TET.2008.01.086
GOULD P L: "SALT SELECTION FOR BASIC DRUGS", INTERNATIONAL JOURNAL OF PHARMACEUTICS, ELSEVIER BV, NL, vol. 33, no. 1/03, 1 January 1986 (1986-01-01), pages 201 - 217, XP002074725, ISSN: 0378-5173, DOI: 10.1016/0378-5173(86)90055-4
CHIBA, K. ET AL.: "FTY720. 2-Amino-2[2-(4-octylphenyl)ethyl]-1,3-propanediol hydrochloride", DRUGS OF THE FUTURE, PROUS SCIENCE, ES, vol. 22, no. 1, 1997, pages 18 - 22, XP008128504, ISSN: 0377-8282
KIUCHI, M. ET AL.: "Synthesis and immunosuppressive activity of 2-substituted 2-aminopropane-1,3-diols and 2-aminoethanols", JOURNAL OF MEDICINAL CHEMISTRY, vol. 43, 2000, pages 2946 - 2961, XP002271142, ISSN: 0022-2623, DOI: DOI:10.1021/JM000173Z
CHINO, M. ET AL.: "An efficient total synthesis of a sphingosine-1-phosphate receptor agonist KRP-203", TETRAHEDRON, vol. 64, no. 17, 2008, pages 3859 - 3866, XP022520419, ISSN: 0040-4020, DOI: DOI:10.1016/J.TET.2008.01.086
GOULD P L: "SALT SELECTION FOR BASIC DRUGS", INTERNATIONAL JOURNAL OF PHARMACEUTICS, ELSEVIER BV, NL, vol. 33, no. 1/03, 1 January 1986 (1986-01-01), pages 201 - 217, XP002074725, ISSN: 0378-5173, DOI: 10.1016/0378-5173(86)90055-4
Attorney, Agent or Firm:
AECHTER, Bernd (Ter Meer Steinmeister & Partner GBRMauerkircherstraße 45, München, DE)
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