Phospholipid prodrugs of anti-proliferative drugs

A - Human Necessities – 61 – K

Patent

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A61K 31/56 (2006.01) A61K 9/02 (2006.01) A61K 9/06 (2006.01) A61K 9/08 (2006.01) A61K 9/10 (2006.01) A61K 9/12 (2006.01) A61K 9/20 (2006.01) A61K 9/48 (2006.01) A61K 9/72 (2006.01) A61K 31/661 (2006.01) A61K 45/00 (2006.01) A61K 47/48 (2006.01) A61P 1/04 (2006.01) A61P 9/10 (2006.01) A61P 11/06 (2006.01) A61P 17/06 (2006.01) A61P 19/02 (2006.01) A61P 21/00 (2006.01) A61P 25/00 (2006.01) A61P 25/02 (2006.01) A61P 25/06 (2006.01) A61P 25/14 (2006.01) A61P 25/16 (2006.01) A61P 25/28 (2006.01) A61P 27/02 (2006.

Patent

CA 2382633

The invention discloses prodrugs comprising anti-proliferative drugs covalently linked, via a bridging group, to a phospholipid moiety such that the active species is preferentially released, preferably by enzymatic cleavage, at the required site of action. The invention further discloses pharmaceutical compositions said prodrugs and the uses thereof for the treatment of diseases and disorders related to inflammatory, to degenerative or atrophic conditions, and to uncontrolled cell growth. Fig. 1 depicts a graph of animal survival during the course of an experiment wherein mice were i.p. transplanted with 11210 mouse leukemia cells and then treated with vehicle only (squares), MTX (triangles) or molar equivalent dose of DP-MTX071 (circles) according to the regimen described in example in Example 11.

L'invention concerne des prodrogues comportant des médicaments inhibiteurs de la prolifération cellulaire liées de manière covalente, via un groupe de liaison, à une fraction phospholipidique, de manière à ce que l espèce chimique active soit diffusée de préférence, et tout particulièrement par segmentation enzymatique, sur le site d'action désiré. L'invention concerne également des compositions pharmaceutiques comportant lesdites prodrogues et les utilisations de ces dernières, afin de traiter les maladies et troubles liés à des conditions de dégénérescence, d'atrophie ou d'inflammation et à une croissance cellulaire non contrôlée.

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