Phosphonic acid diester derivatives

C - Chemistry – Metallurgy – 07 – F

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C07F 9/6553 (2006.01) A61K 31/67 (2006.01) A61K 31/675 (2006.01) C07F 9/6509 (2006.01) C07F 9/6539 (2006.01) C07F 9/6558 (2006.01) C07F 9/6561 (2006.01)

Patent

CA 2241679

A phosphonic diester derivative represented by the following formula (1): (see formula I) wherein R1 represents a cycloalkyl group; a phenyl group which may have 1 to 3 substituents selected from the group consisting of a lower alkoxy group, a lower alkyl group, a halogen atom, a halogen-substituted lower alkyl group, a lower alkanoyl group, a nitro group, a benzoyl group, a cyano group, an N-lower alkylcarbamoyl group, an N-phenyl-lower alkylcarbamoyl group, an N-(halogen- substituted phenyl)carbamoyl group and an N,N-di-lower alkylcarbamoyl group; a 1,3,4-thiadiazol-2-yl group having a halogen-substituted lower alkyl group as a substituent; a thiazolyl group; a pyridyl group which may be,substituted by a halogen atom; a benzothiazol-2-yl group having 1 to 2 lower alkoxy groups on the phenyl ring; or a 4,5-dihydrothieno[3,2-e]benzothiazol-2-yl group; R2 represents a hydrogen atom or a phenyl lower alkyl group; R3 and R4 each represents a lower alkyl group; and A represents a heterocyclic ring selected from the group consisting of a pyrazine ring, a thiophene ring and a phenyl-substituted thiazole ring; the derivative being of value as an agent for treating and preventing hyperlipidemia, diabetes and cataract, or as an antitumor agent.

Dérivés de diester d'acide phosphonique représentés par la formule générale (1) et qui sont utilisés en tant que remède pour traiter l'hyperlipidémie et le diabète, comme agent antitumoral et agent prophylactique ou pour traiter la cataracte. Dans cette formule, R<1> représente cycloalkyle, etc.; R<2> représente hydrogène, phényle ou alkyle inférieur; R<3> et R<4> représentent chacun alkyle inférieur; et A représente un hétérocycle sélectionné parmi des noyaux thiazole à substitution phényle, pyrazine, et thiophène.

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