Acryloyl substituted pyrrole derivatives

Details Acryloyl substituted pyrrole derivatives Acryloyl substituted pyrrole derivatives

C - Chemistry, Metallurgy

07

D

C07D 207/34 (2006.01) A61K 31/40 (2006.01) A61K 31/415 (2006.01) A61K 31/505 (2006.01) C07D 403/00 (2006.01) C07D 403/12 (2006.01) C07K 5/04 (2006.01)

Patent

CA 2030519

The invention relates to acryloyl substituted pyrrole derivatives of formula (I) (see formula I) wherein n is an integer of 1 to 5; each of R1 and R2, which may be the same or different, is hydrogen, halogen, - CN, -NO2, C1-C4 alkyl, or a group (see formula II) R3 is hydrogen, halogen, -CN, or NO2; each R4 is, independently, hydrogen or C1-C4 alkyl; A is a bond, a group (see formula III) ,or a group NH-Het-CO-, wherein Het is a saturated or unsaturated pentatomic or hexatomic heteromonocyclic ring; and (see formula IV), or B is a group (see formula V) in which m is 1, 2 or 3 and each R5 is, independently, a C1- C4 alkyl group; and pharmaceutically acceptable salts thereof, which are useful as antineoplastic agents.

La pr'sente invention se rapporte . des d'riv's de pyrrole . substitution acryloyle, repr'sent's par la formule (I), o- n repr'sente un nombre entier compris entre 1 et 5; chacun des compos's R1 et R2, qui peuvent ¬tre identiques ou diff'rents repr'sente un hydrogSne, un halogSne, -CN, -NO2, un alkyle C1-C4 ou un groupe (a); R3 repr'sente un hydrogSne, un halogSne, -CN ou NO2; chaque R4 repr'sente s'par'ment un hydrogSne ou un alkyle C1-C4; A repr'sente une liaison, un groupe (b) ou un groupe -NH-Het-CO-, o- Het repr'sente une chaOne ferm'e h't'romonocyclique pentatomique ou hexatomique satur'e ou non satur'e; et B repr'sente un groupe (c), (d), (e), (f) ou (g) o- m est 'gal . 1, . 2 ou . 3 et chaque R5 repr'sente s'par'ment un groupe alkyle C1-C4, ainsi qu'. des sels pharmaceutiquement acceptables de ces d'riv's, utiles comme agents antin'oplastie.

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