Piperdine-amino-benzimidazole derivatives as inhibitors of...

Details Piperdine-amino-benzimidazole derivatives as inhibitors of... Piperdine-amino-benzimidazole derivatives as inhibitors of...

2008-04-08

2008-04-08

Seaman, D. Margaret (Department: 1625)

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

Reexamination Certificate

active

07355051

ABSTRACT:
The present invention concerns piperidine-amino-benzimidazoles having inhibitory activity on the replication of the respiratory syncytial virus and having the formulatheir prodrugs, N-oxides, addition salts, quaternary amines, metal complexes and stereochemically isomeric forms wherein Q is C1−6alkyl optionally substituted with trifluoromethyl, C3-7cycloalkyl, Ar2, hydroxy, C1−4alkoxy, C1−4alkylthio, Ar2-oxy-, Ar2-thio-, Ar2(CH2)noxy, Ar2(CH2)nthio, hydroxycarbonyl, aminocarbonyl, C1−4alkyl-carbonyl, Ar2carbonyl, C1−4alkoxycarbonyl, Ar2(CH2)ncarbonyl, aminocarbonyloxy, C1−4alkylcarbonyloxy, Ar2carbonyloxy, Ar2(CH2)ncarbonyloxy, C1−4alkoxy-carbonyl(CH2)noxy, mono- or di(C1−4alkyl)aminocarbonyl, mono- or di(C1−4alkyl)-aminocarbonyloxy, aminosulfonyl, mono- or di(C1−4alkyl)aminosulfonyl or a heterocycles selected from the group consisting of pyrrolidinyl, pyrrolyl, dihydropyrrolyl, imidazolyl, triazolyl, piperidinyl, homopiperidinyl, piperazinyl, morpholinyl, thiomorpholinyl, 1-oxo-thiomorpholinyl, 1,1-dioxothiomorpholinyl, pyridyl and tetrahydropyridyl, wherein each of said heterocycle may optionally be substituted with oxo or C1−6alkyl; G is a direct bond or optionally substituted C1-10alkanediyl; R1is Ar1or a monocyclic or bicyclic heterocycle; one of R2aand R3ais C1−6alkyl and the other one of R2aand R3ais hydrogen; in case R2ais different from hydrogen then R2bis hydrogen or C1−6alkyl, and R3bis hydrogen; in case R3ais different from hydrogen then R3bis hydrogen or C1−6alkyl, and R2bis hydrogen; t is 1, 2 or 3; Ar1is phenyl or substituted phenyl; and Ar2is phenyl or substituted phenyl. It further concerns their preparation and compositions comprising them, as well as their use as a medicine.

REFERENCES:
patent: 4219559 (1980-08-01), Janssens et al.
patent: 0005318 (1979-11-01), None
patent: 0099139 (1983-06-01), None
patent: 0145037 (1984-09-01), None
patent: WO 92/01687 (1992-02-01), None
patent: WO 01/00611 (2001-01-01), None
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 et al. Journal of Medicinal Chemistry, 1985, 28, 1934-1943; p. 1939, Example 87.
International Search Report, International Application No. PCT/EP2004/053606, Date of Mailing of International Search Report, Apr. 15, 2005.
Benet, et al., “Pharmacokinetics: The Dynamics of Drug Absorption, Distribution, and Elimination.”,Goodman and Gilman's The Pharmacological Basis of Therapeutics, Eighth Edition, pp. 13-20, McGraw-Hill Inc.
Janssens, F. et al., “New Antihistamine N-Heterocyclic 4-Piperidinamines.2. Synthesis and Antihistaminic Activity of 1-(4-Fluorophenyl)-1H-Benzimidazol-2-Amines.”,Journal of Medicinal Chemistry, Dec. 1985, vol. 28, No. 121, pp. 1934-1943, American Chemical Society, Washington, US, XP000881979.

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