C - Chemistry – Metallurgy – 07 – C
Patent
C - Chemistry, Metallurgy
07
C
C07C 229/60 (2006.01) A61K 31/195 (2006.01) C07C 37/00 (2006.01) C07C 39/205 (2006.01) C07C 65/19 (2006.01) C07C 65/28 (2006.01) C07C 69/76 (2006.01) C07C 69/94 (2006.01) C07C 69/95 (2006.01) C07C 215/68 (2006.01) C07C 225/22 (2006.01) C07C 225/28 (2006.01) C07C 229/64 (2006.01) C07C 237/30 (2006.01) C07F 9/38 (2006.01) C07F 9/40 (2006.01)
Patent
CA 2321307
Disubstituted lavendustin A analogs that are PTK inhibitors having antiproliferative activity are described. Preferred compounds of the present invention, without limitation, satisfy either Formula (1) or Formula (2). Currently preferred compounds, based on in vivo biological activity, are 4'- adamantylbenzoate-1'-N-1,4-dihydroxybenzylamine and 4'-adamantylmethylbenzoate- 1'-N-1,4-dihydroxybenzylamine. The present invention also provides pharmaceutical compositions comprising effective amounts of disubstituted lavendustin A analogs. Such compositions also may comprise other active ingredients, other materials conventionally used in the formulation of pharmaceutical compositions, and mixtures thereof. The compounds and compositions of the present invention can be used for treating subjects to, for example, inhibit the proliferation of living cells in the treatment of proliferative diseases.
L'invention concerne des analogues de lavendustine A disubstitués qui sont des inhibiteurs de PTK (Protéine Tyrosine Kinase) possédant une activité antiproliférative. De préférence, les composés de la présente invention correspondent, sans restriction, soit à la formule (1), soit à la formule (2). Les composés préférés actuellement, sur la base d'une activité biologique in vivo sont 4'-adamantylbenzoate-1'-N-1,4-dihydroxybenzylamine et 4'-adamantylméthylbenzoate-1'-N-1,4-dihydroxybenzylamine. La présente invention concerne également des compositions pharmaceutiques comprenant des quantités effectives d'analogues de lavendustine A disubstitués. Ces compositions peuvent également comprendre d'autres ingrédients actifs, d'autres matières s'utilisant en général dans la formulation de compositions pharmaceutiques et leurs mélanges. les composés et compositions de la présente invention peuvent s'utiliser pour le traitement de sujets afin, par exemple, d'inhiber la prolifération de cellules vivantes dans le traitement de maladies prolifératives.
Kaur Gurmeet
Narayanan Venkatachala L.
Sausville Edward A.
Varma Ravi K.
Smart & Biggar
The United States Of America As Represented By The Secretary Of
LandOfFree
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