NOVEL CRYSTALLINE FORMS OF ENTACAPONE AND PRODUCTION THEREOF

WIPO Patent Application WO2005063696

A3

The invention relates to three novel forms of entacapone. These are peripheral and selective COMT inhibitors which in combination with levodopa and decarboxylase inhibitors can be used to treating Parkinson's syndrome. Said novel forms arise by crystallization of entacapone in respectively determined conditions. In certain cases, entacapone can be used as a raw product, in a special case it can be used in situ as the product of Knoevenagel condensation of 3,4-dihydroxy-5-nitro-benzaldehyde and N,N-diethyl-2-cyano-acetamide. Also disclosed are improvements of said condensation in relation to the catalyst and the production of the two components thereof.

BADER THOMAS (CH)
FUREGATI MARKUS (US)
JUNGMANN OLIVER (DE)

PCT/CH2004/000754

September 09, 2005

December 27, 2004

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CILAG AG (CH)
BADER THOMAS (CH)
FUREGATI MARKUS (US)
JUNGMANN OLIVER (DE)

C07C253/30; C07C255/41; (IPC1-7): C07C255/41; A61K31/277; A61P25/16; C07C253/30

EP0426468A2

1991-05-08

J. LEPPÄNEN ET AL.: "Structural Studies of acyl esters of entacapone", J. MOL. STRUCT., vol. 562, 2001, pages 129 - 135, XP002300342
HALEBLIAN J K: "CHARACTERIZATION OF HABITS AND CRYSTALLINE MODIFICATION OF SOLIDS AND THEIR PHARMACEUTICAL APPLICATIONS", JOURNAL OF PHARMACEUTICAL SCIENCES, AMERICAN PHARMACEUTICAL ASSOCIATION. WASHINGTON, US, vol. 64, no. 8, August 1975 (1975-08-01), pages 1269, XP009031935, ISSN: 0022-3549

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