Carbonyl-piperazinyl and piperidinyl compounds which inhibit...

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 213/56 (2006.01) A61K 31/435 (2006.01) A61K 31/495 (2006.01) A61K 31/535 (2006.01) A61K 31/54 (2006.01) C07D 211/32 (2006.01) C07D 211/34 (2006.01) C07D 211/38 (2006.01) C07D 211/50 (2006.01) C07D 213/89 (2006.01) C07D 241/04 (2006.01) C07D 401/00 (2006.01) C07D 401/06 (2006.01) C07D 401/12 (2006.01) C07D 401/14 (2006.01) C07D 403/00 (2006.01) C07D 405/00 (2006.01) C07D 409/00 (2006.01) C07D 417/00 (2006.01)

Patent

CA 2217351

Novel carbonyl piperazinyl and piperidinyl compounds of formula (1.0) or (1.1) and pharmaceutical compositions are disclosed. Also disclosed is a method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells. The method comprises administering the novel carbonyl piperazinyl or piperidinyl compound to a biological system. In particular, the method inhibits the abnormal growth cells in a mammal such as the human being. A compound of formula (1.0) and (1.1) or a pharmaceutically acceptable salt or solvate thereof, wherein Z is a group which is (i), (ii) or (iii), wherein X1 is CH or N; X2 can be the same or different and can be CH, N, or N-O; b is 0, 1, 2, 3, 4; n and nn independently represent 0, 1, 2, 3, 4 or when X2 is CH, n and nn can be 5; R20 and R21, R1, R2 and R3 are as given in the description.

L'invention décrit de nouveaux composés de pipérazinyle et pipéridinyle carbonyles de formule (1.0) ou (1.1) ainsi que des compositions pharmaceutiques. L'invention décrit également un procédé d'inhibition de la fonction Ras et par conséquent l'inhibition de la croissance anormale des cellules. Le procédé consiste en l'administration du nouveau composé de pipérazinyle et pipéridinyle carbonyles à un système biologique. En particulier, le procédé inhibe la croissance anormale des cellules chez un mammifère tel que l'être humain. La présente invention décrit un composé de formules (1.0) et (1.1) ou un sel ou solvate pharmaceutiquement acceptable, dans lequel Z est un groupe de formule (i), (ii) ou (iii), dans laquelle X1 représente CH ou N; X2 peut être identique ou différent et peut représenter CH, N ou N-O; b vaut 0, 1, 2, 3, 4; n et nn représentent indépendamment 0, 1, 2, 3, 4 ou lorsque X2 représente CH, n et nn peuvent valoir 5; R20 et R21, R1, R2 et R3 sont tels que décrits dans la description.

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