Inhibitors of ikk-.beta. serine-threonine protein kinase

Details Inhibitors of ikk-.beta. serine-threonine protein kinase Inhibitors of ikk-.beta. serine-threonine protein kinase

C - Chemistry, Metallurgy

07

D

C07D 333/38 (2006.01) A61K 31/381 (2006.01) A61P 25/28 (2006.01) A61P 37/00 (2006.01)

Patent

CA 2722255

Cyclopentyl (2S,4E)-2-amino-5-{3-[4-carbamoyl-5 (carbamoylamino)-2- thienyl]phenyl}pent-4-enoate; Cy-clopentyl 5-{3-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]phenyl}-L- norvalinate; Cyclopentyl (2S,4E)-2-amino-5-{3-[4-car-bamoyl-5-(carbamoylamino)-2-thienyl]-5- methylphenyl}pent-4-enoate; Cyclopentyl (2S,4E)-2-amino-5-{5-[4-carbamoyl-5-(car-bamoylamino)-2-thienyl]-2- methylphenyl}pent-4-enoate; Cyclopentyl O-{3-[4-carbamoyl-5-(carbamoylamino)-2--thienyl]phenyl}-L-homoserinate; Cyclopentyl O-{3-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]phenyl}-L- homoserinate; Cy-clopentyl N-{3-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]benzyl}-L- alaninate; and tert-Butyl N-{3-[4-carbamoyl-5-(carbamoy-lamino)-2-thienyl]benzyl}-L-alaninate are hydrolysed to the corresponding carboxylic acids by intracellular carboxylesterases, and are useful for the inhibition of IKK.beta. activity.

Le (2S,4E)-2-amino-5-{3-[4-carbamoyl-5(carbamoylamino)-2-thiényl]phényl}pent-4-énoate de cyclopentyle ; le 5-{3-[4-carbamoyl-5-(carbamoylamino)-2-thiényl]phényl}-L-norvalinate de cyclopentyle ; le (2S,4E)-2-amino-5-{3-[4-carbamoyl-5-(carbamoylamino)-2-thiényl]-5-méthylphényl}pent-4-énoate de cyclopentyle ; le (2S,4E)-2-amino-5-{5-[4-carbamoyl-5-(carbamoylamino)-2-thiényl]-2-méthylphényl}pent-4-énoate de cyclopentyle ; le O-{3-[4-carbamoyl-5-(carbamoylamino)-2-thiényl]phényl}-L-homosérinate de cyclopentyle ; le O-{3-[4-carbamoyl-5-(carbamoylamino)-2-thiénylphényl}-L-homosérinate de cyclopentyle ; le N-{3-[4-carbamoyl-5-(carbamoylamino)-2-thiényl]benzyl}-L-alaninate de cyclopentyle ; et le N-{3-[4-carbamoyl-5-(carbamoylamino)-2-thiényl]benzyl}-L-alaninate de tert-butyle sont hydrolysés en les acides carboxyliques correspondants par des carboxylestérases intracellulaires et sont utiles pour l'inhibition de l'activité d'IKK-ß.

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