Inhibitors of dna methylation in tumor cells

Details Inhibitors of dna methylation in tumor cells Inhibitors of dna methylation in tumor cells

C - Chemistry, Metallurgy

07

D

C07D 209/48 (2006.01) A61K 31/4035 (2006.01) A61P 35/00 (2006.01) C07D 233/66 (2006.01) C07D 471/04 (2006.01)

Patent

CA 2557581

The present invention relates to compounds according to the general formula (I) wherein the dotted lines denote a single bond which is optionally present, with 2 dotted lines denoting a double bond; wherein, in case no double bond is present and a free valence exists, this valence is occupied by H; and wherein the symbols in particular have the following meanings: R1 and R2 are independently from each other selected from the group consisting of: H; OH; (=O); halogens; pseudohalogens;. NH2; S(O)mR5; SO2NH2 ; C(O)R8; C(O)OR9; CONH2; C1-C2-alkyl susbtituted by NH2, OH, S(O)mR5, SO2NH2, C(O)R8, C(O)OR9, CONH2; C1-C2-alkoxy substituted by NH2, OH, S(O)mR5, SO2NH2, C(O)R8, C(O)OR9, CONH2; Ar denotes an unsubstituted mononuclear aryl group having 6 or 7 members, which aryl group is annulated to the neighbouring 5-membered cycle, and which may carry 1, 2 or 3 heteroatoms from the group N, O and S in its cycle; Y, Z denote independently from each other a nitrogen atom or a methylene group; X is a nitrogen atom or a methylene group; A is selected from the group consisting of: H; halogens and pseudohalogens; OH; =N(OH); NR12R13; OSO3- ; S(O)mR14; SO2NR15 R16 ; C(O)R17; C(O)OR18; CONR19R20; C(S)R21, C(S)OR22; unsubstituted and at least monosubstituted C1-C6-alkyl which can carry in its chain one or more non-adjacent heteroatoms from the group nitrogen and oxygen. These compounds are used as inhibitors of DNA methylation and therefore useful in the treatment of various forms of cancer.

L'invention concerne des composés de formule (I), dans laquelle des lignes en tirets représentent une liaison simple, éventuellement présente, les lignes à double-tirets représentent une double liaison. Dans le cas où une double liaison n'est pas présente et qu'une valence libre existe, ladite valence est occupée par H. Dans la formule (I), les symboles sont spécifiés dans la description. L'invention concerne également un des sels pharmaceutiquement actif du composé, ces derniers étant utilisés dans la fabrication de médicaments permettant d'inhiber la méthylation de l'ADN, les méthyltransférases de l'ADN, et peuvent être utilisés dans la fabrication de produits pharmaceutiques permettant de traiter des troubles du développement, tels que le syndrome de Prader-Willi, le syndrome d'Angelman (ou syndrome du pantin hilare), le syndrome de Beckwith-Wiedemann, et les maladies proliférantes, telles que les resténose coronaire, les maladies néoplasiques, en particulier le carcinome du colon, le carcinome à polypose adénomateuse familière, et le cancer colorectal non polypose héréditaire, le carcinome de la prostate, le mélanome, le lymphome non Hodgkin, la leucémie lymphatique aiguë, la leucémie lymphatique chronique, la leucémie myéloïde aiguë, la leucémie myéloïde chronique, ou le carcinome hépatocellulaire. Lesdits composés peuvent être également utilisés dans d'autres applications notamment l'induction de la différentiation cellulaire, le diagnostic et l'utilisation dans des essais de criblage.

Affiliated with

Also associated with

Rating

Inhibitors of dna methylation in tumor cells does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Inhibitors of dna methylation in tumor cells, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Inhibitors of dna methylation in tumor cells will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFCA-PAI-O-1442143