Quinoline derivatives process of synthesis and medicaments...

Details Quinoline derivatives process of synthesis and medicaments... Quinoline derivatives process of synthesis and medicaments...

2006-06-20

2006-06-20

Davis, Zinna Northington (Department: 1625)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

C546S169000, C514S314000

Reexamination Certificate

active

07064133

ABSTRACT:
The invention relates to derivatives corresponding to formula I:in whichX is an alkyl-(CH2)n— chain with n=0, 1 or 2, or O or N,Z is an aromatic which may contain heteroatoms chosen from O, N or S, as substitutions for the carbon atoms constituting said aromatic ring, this ring being substituted or otherwise with Rb,Rb represents 1 to 3 substituents chosen from —OH, —OR, —COOH, —COOR, —COH, —COR, —NH2, —NH(R), —NH(R,R′), —SH, —SR and CN,Ra is H or —(CH2)n′—Y, with n′=0, 1, 2 or 3 and Y and —CH3, —COOH, —COOR, —CN, —OH, —OR, SR, or an aryl group optionally substituted with Rb,R and R′ represent a linear or branched alkyl chain of 1 to 4 C, and their pharmaceutically acceptable salts. Application as active ingredient of medicaments inhibiting retrovirus integrases.

REFERENCES:
patent: 2 761 687 (1998-10-01), None
patent: WO 98 45269 (1998-10-01), None
Zouhiri, F., et al., “Structure-activity relatioships and binding mode of styrylquinolines as Potent inhibitors of HIV-1 Integrase and replication of HIV-1 in Cell Culture”, Journal of medicinal Chemistry, American Cehmical Society, Washington, vol. 43, pp. 1533-1540 (2000) XP000926747.

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