Benzimidazolinone derivatives

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 235/26 (2006.01) A61K 31/415 (2006.01) A61K 31/535 (2006.01) C07D 401/06 (2006.01) C07D 403/06 (2006.01) C07D 413/06 (2006.01) C07D 521/00 (2006.01)

Patent

CA 2040235

ABSTRACT OF THE DISCLOSURE Benzimidazolinone derivatives of the general formula (I): Image (I) wherein R1, R2 and R3, which may be the same or different, each is a hydrogen or halogen atom or a lower alkyl, halo- lower alkyl, hydroxy-lower alkyl, hydroxyl, lower alkoxy, aryloxy, acyl, cyano, carboxyl, a lower alkoxycarbonyl, carbamoyl, nitro or nitrogen-containing 5- or 6-membered heterocyclic group; A is an ethylene group which may optionally have at least one branch; R'' and R5, which may be the same or different, each is a lower alkyl group or R4 and R5, together with the adjacent nitrogen atom, represent a pyrrolidinyl, piperidino or a morpholino group provided that when Image is a piperidino or diethylamino group, at least one of R1, R2 and R3 is other than a hydrogen atom, or pharmaceutically acceptable salts thereof, methods of producing the same and pharmaceutical compositions containing the same are disclosed. Pharmacologically, the above compounds (I) have pulmonary surfactant secretion promoting activity. - 140 -

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