1-(2-benzimidazolyl)-1,5-diazacyclooctane compounds

C - Chemistry – Metallurgy – 07 – D

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C07D 403/04 (2006.01) A61K 31/415 (2006.01) C07D 235/30 (2006.01)

Patent

CA 2161876

1-(2-benzimidazolyl)-1,5-diazacyclooctane compounds represented by the formula: Image wherein X represents a hydrogen atom or a halogen atom; Y represents a covalent bond, a straight- or branched-chain alkylene group having 1 to 6 carbon atoms, or a straight- or branched-chain alkenylene group having 2 to 6 carbon atoms; R represents a hydrogen atom, or a straight- or branched-chain alkyl group having 1 to 6 carbon atoms; and pharmaceutically acceptable salts thereof. The compounds represented above are novel potent and long-lasting histamine H1-receptor antagonist with less topical irritation, and can be applied to topical administration by an inhalation for the treatment of bronchial asthma.

Dérivé 1-(2-benzimidazolyl)-1,5-diazacyclooctane représenté par la formule générale (I), dans laquelle X représente hydrogène ou halogène; Y représente une liaison simple, alkylène ramifié ou linéaire C1-C6 ou bien alcénylène ramifié ou linéaire C2-C6; et R représente hydrogène ou bien alkyle ramifié ou linéaire C1-C6. L'invention concerne également un sel pharmaceutiquement acceptable dudit dérivé. Ce composé constitue un antagoniste du récepteur de l'histamine H<1> qui peut être administré localement, par inhalation, pour soigner l'asthme bronchique.

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