On December 29, 2005, Delorme, Daniel; Woo, Soon Hyung; Vaisburg, Arkadii; Moradei, Oscar; Leit, Silvana; Raeppel, Stephane; Frechette, Sylvie; Bouchain, Giliane published a patent.Category: pyridine-derivatives The title of the patent was Preparation of triazinyl and other carboxamides as inhibitors of histone deacetylase. And the patent contained the following:
The invention provides compounds and methods for inhibiting histone deacetylase enzymic activity. Such compounds include carboxamides I [Cy2 = (un)substituted cycloalkyl, aryl, heteroaryl, heterocyclyl (each of which is optionally fused to one or two aryl or heteroaryl rings, or to one or two (un)saturated cycloalkyl or heterocyclic rings); X1 = a bond, M1L2M1, L2M2L2 (wherein L2 = a bond, alkylene, alkenylene, alkynylene; M1 = O, S, SO, NHCO, etc.; M2 = M1, heteroarylene, heterocyclylene); Ar2 = (un)substituted (hetero)arylene; R5, R6 = H, alkyl, aryl, aralkyl; q = 0-1; Ay2 = (un)substituted 5-6 membered cycloalkkyl, heterocyclyl or heteroaryl substituted with an amino or hydroxy moiety; with provisos] which were prepared and claimed. E.g., a multi-step synthesis of II, starting from Me 4-(aminomethyl)benzoate.HCl, was given. The invention also provides compositions and methods for treating cell proliferative diseases and conditions. Antineoplastic effects of some I are illustrated for colorectal, pulmonary and pancreatic neoplasms; also the combined antineoplastic effect of histone deacetylase inhibitors and histone deacetylase antisense oligonucleotides on tumor cells in vivo was demonstrated. Although the methods of preparation are not claimed, hundreds of example preparations are included. The experimental process involved the reaction of N1-(5-Bromopyrid-2-yl)ethane-1,2-diamine(cas: 199522-66-2).Category: pyridine-derivatives
The Article related to carboxamide preparation inhibitor histone deacetylase hdac proliferative disease antitumor, triazinyl carboxamide preparation inhibitor histone deacetylase proliferative disease antitumor and other aspects.Category: pyridine-derivatives