Crystals of benzimidazole derivatives and their production

C - Chemistry – Metallurgy – 07 – D

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C07D 401/12 (2006.01) A61K 31/4439 (2006.01) A61P 1/04 (2006.01)

Patent

CA 2269053

A substantially solvent-free and stable crystal of the compound of formula (I) wherein the ring A may optionally be substituted R1 represents hydrogen or an N-protecting group, each of R2, R3 and R4 is (1) a hydrogen atom, (2) an alkyl group which may optionally be substituted with halogen atom(s) or (3) an alkoxy group which may optionally be substituted with halogen atoms(s) or alkoxy; or its salt, is produced by subjecting a solvate of the compound (I) or its salt to de-solvent treatment, in an industrially advantageous method.

La présente invention concerne une forme cristalline, sensiblement exempt de solvant et stable, du composé représenté par la formule générale (I), ou de l'un des sels de ce composé. Dans cette formule générale, le cycle A peut être éventuellement substitué. R<1> est hydrogène ou un groupe de protection en N. R<2>, R<3>, et R<4> sont chacun (1) un atome hydrogène, (2) un groupe alkyl éventuellement substitué par un ou plusieurs atomes halogène ou (3) un groupe alcoxy éventuellement substitué par un ou plusieurs atomes halogène ou alcoxy. La production de ce composé consiste à soumettre un solvat du composé ou de son sel à une désolvatation au moyen d'un procédé permettant une production industrielle.

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