Benzimidazole derivatives, preparation and therapeutic use...

Details Benzimidazole derivatives, preparation and therapeutic use... Benzimidazole derivatives, preparation and therapeutic use...

2005-12-27

2005-12-27

Kifle, Bruck (Department: 1624)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

C540S498000

Reexamination Certificate

active

06979683

ABSTRACT:
The invention relates to benzimidazole derivatives of general formula (I)in whichX represents a nitrogen atom or a carbon atom;and when X represents a nitrogen atomR3 represents in particular a hydrogen atom or a (C1-C4)alkyl group,R4 represents in particular a hydrogen atom; a (C1-C6)alkyl; (C3-C7)cycloalkyl; 4-piperidyl; —(CH2)p—NR5R6; —(CH2)p—CONR5R6; —CO—(CH2)p—NR5R6; —(CH2)p-phenyl; —(CH2)p-morpholinyl; —(CH2)p-pyrrolidinyl; —(CH2)p-tetrahydroisoquinoline; —(CH2)p-heteroaryl; heteroarylcarbonyl; phenylcarbonyl; (C1-C6)alkylcarbonyl; —(CH2)p—COOR′; or phenylsulphonyl group;and when X represents a carbon atomR3 represents a hydrogen atom; a group —NR5R6; —NHCOR7; —CONHR5; —COR7; —NHCONH2; —OH or —CH2OH,R4 represents in particular a hydrogen atom; an optionally substituted group —(CH2)p-phenyl; a group —(CH2)p-heteroaryl; or a group —(CH2)tNR7R8.Preparation process and therapeutic application.

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patent: 6448271 (2002-09-01), Lubisch et al.
patent: 6548494 (2003-04-01), Webber et al.
patent: 2171579 (1996-09-01), None
patent: 0 732 334 (1986-09-01), None
patent: 0 646 583 (1995-04-01), None
patent: WO 00/32579 (2000-06-01), None
Emanuela Mazzon et al., “GPI 6150, a poly (ADP-ribose) polymerase inhibitor, exhibits an anti- inflammatory effect in rat models of inflammation,”European Journal of Pharmacology415:85-94 (2001).
Andrew A. Pieper et al., “Poly (ADP-ribose) polymerase, nitric oxide and cell death,”Trends in Pharmaceutical Sciences20:171-181 (1999).
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Derwent abstract for EP 0 646 583, dated Apr. 5, 1995.
Derwent abstract for EP 0 732 334, dated Sep. 18, 1886.
Derwent abstract for WO 00/32579, dated Jun. 8, 2000.

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