C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
167/228, 260/272
C07D 451/00 (2006.01) A61K 31/44 (2006.01) C07D 401/12 (2006.01) C07D 451/12 (2006.01) C07D 451/14 (2006.01) C07D 453/02 (2006.01) C07D 453/06 (2006.01) C07D 487/08 (2006.01)
Patent
CA 1337347
Pharmaceutically active benzimidazoline-2-oxo-1-carbo- xylic acid derivatives are described which are 5- HT receptor antagonists useful as antiemetic agents and as gastric prokinetic agents, of the following formula: Image (I) wherein R represents a hydrogen atom, or a C1-6 alkyl, C2-6 alkenyl or C2-6 alkynyl group; R1 and R2, which may be the same or different, represent a hydrogen atom, halogen atom, trifluoromethyl, C1-6 alkyl, C1-6 alkoxy, C1-6 alkylthio, C1-6 acyl, carboxyl, C1-6 alkoxycarbonyl, hydroxy, nitro, or amino group, optionally N-mono or di-substituted by a C1-4 alkyl group, C1-6 acylamino, C1-6 alkoxycar- bonylamino, carbamoyl optionally N-mono or di-substitu- ted by C1-4 alkyl group, cyano, C1-6 alkylsulphinyl, C1-6 alkylsulphonyl, aminosulphonyl optionally N- mono or di-substituted by a C1-4 alkyl group, aminosul- phonylamino optionally N-mono or di-substituted by C1-4 alkyl group; Y is oxygen or represents N - R3 in which R3 is a hydrogen atom, a C1-6 alkyl or benzyl group, optionally substituted by one or more C1-6 alkoxy groups; A is a group selected from: Image (a) Image (b) Image (c) Image (d) wherein p is 0 or 1; r is 0, 1, 2, or 3; R4 is a hydrogen atom or a C1-4 alkyl group; R5 is a hydrogen atom, C1-6 alkyl, C3-8 cycloalkyl, a C3-8 cycloalkylalkyl group having 1-4 carbons in the alkyl moiety or a phenylalkyl group having 1-4 carbons in the alkyl moiety or R5 is a group of formula Image wherein R6 is a hydrogen atom, C1-4 alkyl or an amino group and R7 is a hydrogen atom or C1-6 alkyl group. The processes for the preparation of the compounds of formula (I) as well as pharmaceutical compositions containing them are also described.
577840
Donetti Arturo
Giachetti Antonio
Micheletti Rosamaria
Montagna Ernesto
Nicola Massimo
Boehringer Ingelheim Italia S.p.a
Fetherstonhaugh & Co.
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