1,2-annelated quinoline derivatives

Details 1,2-annelated quinoline derivatives 1,2-annelated quinoline derivatives

2005-07-05

2005-07-05

Raymond, Richard L. (Department: 1624)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

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

C514S292000, C514S293000, C514S294000

Reexamination Certificate

active

06914066

ABSTRACT:
This invention concerns compounds of formulathe pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein ═X1—X2—X3— is a trivalent radical,; >Y1—Y2— is a trivalent radical; r and s are each independently 0, 1, 2, 3, 4 or 5; t is 0, 1, 2 or 3; each R1and R2are independently hydroxy, halo, cyano, C1-6alkyl, trihalomethyl, trihalomethoxy, C2-6alkenyl, C1-6alkyloxy, hydroxyC1-6alkyloxy, C1-6alkylthio, C1-6alkyloxyC1-6alkyloxy, C1-6alkyloxycarbonyl, aminoC1-6alkyloxy, mono- or di(C1-6alkyl)amino, mono- or di(C1-6alkylaminoC1-6alkyloxy, aryl, arylC1-6alkyl, aryloxy or arylC1-6alkyloxy, hydroxycarbonyl, C1-6alkyloxycarbonyl; or two R1or R2on adjacent positions form together a bivalent radical; R3is hydrogen, halo, C1-6alkyl, cyano, haloC1-6alkyl, hydroxyC1-6alkyl, cyanoC1-6alkyl, aminoC1-6alkyl, C1-6alkyloxyC1-6alkyl, C1-6alkylthio-C1-6alkyl, aminocarbonylC1-6alkyl, hydroxycarbonyl, hydroxycarbonylC1-6alkyl, C1-6alkyoxycarbonylC1-6alkyl, C1-6alkylcarbonylC1-6alkyl, C1-6alkyloxycarbonyl, aryl, arylC1-6alkyloxyC1-6alkyl, mono- or di(C1-6alkyl)aminoC1-6alkyl, or a radical of formula —O—R10, —S—R10or —NR11R12; R4is an optionally substituted imidazolyl; aryl is an optionally substituted phenyl or naphthalenyl; having farnesyl transferase and geranylgeranyl transferase inhibiting activity; their preparation, compositions containing them and their use as a medicine.

REFERENCES:
patent: 0371564 (1990-06-01), None
patent: 97/16443 (1997-05-01), None
patent: 97/21701 (1997-06-01), None
patent: 98/40383 (1998-09-01), None
patent: 98/49157 (1998-11-01), None
Kohl et al, “Selective Inhibition of ras-Dependent Transformation by a Farnesyltransferase Inhibitor”,Science, 1993, 260, 1934-1937.
Rak, J. et al., “Mutant ras Oncogenes Upregulate VEGF/VPF Expression: Implications for Induction and Inhibition of Tumor Angiogenesis”,Cancer Res., 1995, 55, 4575-4580.

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