Benzimidazole aqnd azabenzimidazole derivatives which are...

C - Chemistry – Metallurgy – 07 – D

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C07D 235/16 (2006.01) A61K 31/415 (2006.01) A61K 31/435 (2006.01) C07D 235/28 (2006.01) C07D 471/04 (2006.01) C07F 9/6506 (2006.01) C07F 9/6561 (2006.01)

Patent

CA 2035710

IN THE PATENT AND TRADEMARK OFFICE PATENT APPLICATION entitled: Novel benzimidazole and azabenzimidazole derivatives which are thromboxane receptor antagonists, their methods of preparation, synthesis intermediates and pharmaceutical compositions in which they are present in the names of: Nicole BRU-MAGNIEZ Eric NICOLAI Jean-Marie TEULON Assignee: Laboratoires UPSA ABSTRACT OF THE DISCLOSURE The present invention relates to the deriva- tives of the formula Image Formula (I) in which: A is an aromatic ring or a nitrogen hetero cycle; X1, X2, X3 and X4 are independently a hydrogen atom, a halogen atom, a lower alkyl radical, a C3-C7 cycloalkyl radical, an alkoxy radical, an alkylthio radical, a sulfone group, SO2-lower alkyl, a sulfoxide group, SO-lower alkyl, a trifluoromethyl group, a nitro group, a hydroxyl group, a methylene alcohol radical or a group COOR', in which R' is a hydrogen or a lower alkyl; X3 and X4 can also form a naphthalene with the phenyl; B is CR5R6, R5 and R6 being a hydrogen atom, a lower alkyl or a C3-C7 cycloalkyl radical, or the sulfur atom; R1, R2, R3 and R4 are independently a hydrogen atom, a lower alkyl radical or a C3-C7 cycloalkyl radical; CR1R2 or CR3R4 can form with B, when the latter is CR5R6, a cycloalkyl or a cycloalkene having 3 to 7 carbon atoms; R1R2 and R3R4 can also form a ring having 3 to 7 carbon atoms; n is an integer from 1 to 4 and can be 0 if R1 and R2 are other than hydrogen; and D is a chemical group which can be: COOR7, R7 being the hydrogen atom, a lower alkyl radi- cal or a C3-C7 cycloalkyl radical, CONH-R8, R8 being the hydrogen atom, a lower alkyl radical or a C3-C7 cycloalkyl radical, or CN, and to their addition salts.

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