C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 401/14 (2006.01) A61K 31/435 (2006.01) C07D 401/04 (2006.01) C07D 405/14 (2006.01) C07F 9/59 (2006.01) C07F 9/6558 (2006.01) C07H 19/04 (2006.01)
Patent
CA 2265763
Novel tricyclic compounds of formula (1.0) or a pharmaceutically acceptable salt or solvate thereof, wherein: one of a, b, c, and d represents N or NR9, wherein R9 is O-, -CH3 or -(CH2)nCO2H wherein n is 1 to 3, and the remaining a, b, c and d groups represent CR1 or CR2; or each of a, b, c and d is independently selected from CR1 or CR2; each R1 and each R2 is independently selected from H, halo, -CR3, -OR10, -COR10, -SR10, -S(O)tR11 (wherein t is 0, 1 or 2), -SCN, -N(R10)2, -NR10R11, -NO2, -OC(O)R10, -CO2R10, -OCO2R11, -CN, - NHC(O)R10, -NHSO2R10, -CONHR10, -CONHCH2CH2OH, -NR10COOR11, -SR11C(O)OR11, - SR11N(R75)2; n is 0 (zero), 1, 2, 3, 4, 5 or 6; T is -CO-; -SO-; -SO2-; or - CR30R31-; Z represents alkyl, aryl, aralkyl, heteroalkyl, heteroaryl, heteroarylalkyl, heterocycloalkyl, heterocycloalkylalkyl, -OR40, -SR40, - CR40R42, -NR40R42, formulae (i), (ii), (iii), (iv), (v) and (vi). Pharmaceutical compositions are disclosed which are inhibitors of the enzyme, farnesyl protein transferase. Also disclosed is a method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells. The method comprises administering the novel tricyclic compound to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammal such as a human.
L'invention porte sur de nouveaux composés tricycliques de formule (1.0) ou leur sels ou solvates pharmacocompatibles dans laquelle: l'un de a, b, c ou d représente N ou NR?9¿ où R?9¿ est O-, -CH¿3? ou -(CH¿2?)¿n?CO¿2?H où n est 1 à 3, et les groupes a, b, c et d restants représentent CR?1¿ ou CR?2¿; ou bien chacun de a, b, c et d est sélectionné indépendamment parmi CR?1¿ ou CR?2¿; chaque R?1¿ et chaque R?2¿ est sélectionné indépendamment parmi H, halo, -CF¿3?, -OR?10¿, -COR?10¿, SR?10¿, -S(O)¿t?R?11¿(où t est 0, 1 ou 2), -SCN, -N(R?10¿)¿2?, -NR?10¿R?11¿, -NO¿2?, -OC(O)R?10¿, -CO¿2?R?10¿, -OCO¿2?R?11¿, -CN, -NHC(O)R?10¿, -NHSO¿2?R?10¿, -CONHR?10¿, -CONHCH¿2?CH¿2?OH, -NR?10¿COOR?11¿, -SR?11¿C(O)OR?11¿, -SR?11¿N(R?75¿)¿2?; n est zéro, 1, 2, 3, 4, 5 ou 6; T est -CO-, -SO-, -SO¿2?- ou -CR?30¿R?31¿-; Z représente alkyle, aryle, aralkyle, hétéroalkyle, hétéroaryle, hétéroarylalkyle, hétérocycloalkyle, hétérocycloalkylalkyle, -OR?40¿, -SR?40¿, -CR?40¿R?42¿, -NR?40¿R?42¿, les formules (i), (ii), (iii), (iv), (v) ou la formule (vi). L'invention porte également sur des compositions pharmaceutiques inhibitrices de la farnésyl-protéine transférase et sur un procédé d'inhibition de la fonction Ras et par là de la croissance anormale des cellules, consistant à administrer les nouveaux composés tricycliques à un système biologique. Lesdits procédés inhibent en particulier la croissance anormale des cellules, en particulier chez des mammifères tels que l'homme.
Baldwin John J.
Cooper Alan B.
Doll Ronald J.
Girijavallabhan Viyyoor M.
Mallams Alan K.
Ogilvy Renault Llp/s.e.n.c.r.l.,s.r.l.
Pharmacopeia Inc.
Pharmacopeia Drug Discovery Inc.
Schering Corporation
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