Morpholinyl containing benzimidazoles as inhibitors of...

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...

Reexamination Certificate

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C544S132000

Reexamination Certificate

active

07449463

ABSTRACT:
The present invention concerns morpholinyl containing benzimidazoles having inhibitory activity on the replication of the respiratory syncytial virus and having the formulaa prodrug, N-oxide, addition salt, quaternary amine, metal complex or stereochemically isomeric form thereof wherein G is a direct bond or optionally substituted C1-10alkanediyl; R1is Ar1or a monocyclic or bicyclic heterocycle Q is R7, pyrrolidinyl substituted with R7, piperidinyl substituted with R7or homopiperidinyl substituted with R7; one of R2aand R3ais selected from halo, optionally mono- or polysubstituted C1-6alkyl, optionally mono- or polysubstituted C2-6alkenyl, nitro, hydroxy, Ar2, N(R4aR4b), N(R4aR4b)sulfonyl, N(R4aR4b)carbonyl, C1-6alkyloxy, Ar2oxy, Ar2C1-6alkyloxy, carboxyl, C1-6alkyloxycarbonyl, or —C(=Z)Ar2; and the other one of R2aand R3ais hydrogen; in case R2ais different from hydrogen then R2bis hydrogen, C1-6alkyl or halogen and R3bis hydrogen; in case R3ais different from hydrogen then R3bis hydrogen, C1-6alkyl or halogen and R2bis hydrogen. It further concerns the preparation thereof and compositions comprising these compounds, as well as the use thereof as a medicine.

REFERENCES:
patent: WO 01/00611 (2001-01-01), None
patent: WO 01/00612 (2001-01-01), None
patent: WO 01/00615 (2001-01-01), None
Janssens F et al: “New Antihistamine N-Heterocyclic 4-Piperidinamines. 2. Synthesis and Antihistaminic Activity of 1-(4-Flourophenyl) Methyl-N-(4-Piperidinyl)-1H-Benzidazol-2-amines”. Journal of Medicinal Chemistry, American Chemical Society. Washington, US, vol. 28, No. 12, Dec. 1985. pp. 1934-1943, XP000881979 ISSN: 0022-2623 example 8.

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