A - Human Necessities – 61 – K
Patent
A - Human Necessities
61
K
A61K 45/06 (2006.01) A61K 31/4409 (2006.01) A61P 35/00 (2006.01)
Patent
CA 2449442
Pharmaceutical composition comprising, as a first anti-neoplastic drug, cyanoguanidine IKK inhibitors, and in particular compounds of formula (I) wherein n is 0, 1 or 2; each R independently represents halogen, trifluoromethyl, hydroxy, C1-4alkyl, C1-4alkoxy, C1-4alkoxycarbonyl, nitro, sulfo, cyano, amino or carboxy groups; Q is a straight or branched, saturated or unsaturated C4-20 divalent hydrocarbon radical; X is a bond, amino, O, S, carbonyl, carbonylamino, aminocarbonyl, oxycarbonyloxy, oxycarbonyl, carbonyloxy, aminocarbonyloxy, aminothiocarbonyloxy, oxycarbonylamino or oxythiocarbonylamino; A is di-(C1-4alkoxy)phospinoyloxy, C1-4alkoxycarbonyl, C1-4alkoxycarbonylamino, C3-12 carbocyclic ring or C3-12 heterocarbocyclic ring optionally subtituted with one or more R1; R1 being independently selected from the group consisting of halogen, trifluoromethyl, hydroxy, C1- 4alkyl, C1-4alkoxy, C1-4alkoxycarbonyl, nitro, cyano, amino, sulfo, carboxy, carboxamido, sulfamoyl or C1-4hydroxyalkyl; in combination with a second anti- neoplastic drug are provided.
L'invention porte sur une composition pharmaceutique comprenant, comme premier médicament antinéoplasique, des inhibiteurs IKK de cyanoguanidine et des composés spécifiques de la formule (I) dans laquelle n représente 0, 1 ou 2; chaque R représente indépendamment des groupes halogène, trifluorométhyle, hydroxy, C¿1-4?alkyle, C¿1-4?alcoxy, C¿1-4?alcoxycarbonyle, nitro, sulfo, cyano, amino ou carboxy; Q représente un radical d'hydrocarbure divalent C¿4-20?, saturé ou insaturé, à chaîne droite ou ramifiée; X représente une liaison, amino, O, S, carbonyle, carbonylamino, aminocarbonyle, oxycarbonyloxy, oxycarbonyle, carbonyloxy, aminocarbonyloxy, aminothiocarbonyloxy, oxycarbonylamino ou oxythiocarbonylamino; A représente di-(C¿1-4?alcoxy)phospinoyloxy, C¿1-4?alcoxycarbonyl, C¿1-4?alcoxycarbonylamino, un noyau carboxylique C¿3-12? ou un noyau hétérocarbocyclique C¿3-12? éventuellement substitué par un ou plusieurs R¿1?; R¿1? étant sélectionné indépendamment dans le groupe comprenant halogène, trifluorométhyle, hydroxy, C¿1-4?alkyle, C¿1-4?alcoxy, C¿1-4?alcoxycarbonyle, nitro, cyano, amino, sulfo, carboxy, carboxamido, sulfamoyle or C¿1-4?hydroxyalkyle; en combinaison avec un second médicament antinéoplasique.
Binderup Lise
Bramm Erik
Hamberg Karin Jexner
Hjarnaa Pernille-Julia Vig
Leo Pharma A/s
Osler Hoskin & Harcourt Llp
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