Drugs containing enzyme inhibitors as the active ingredient

Details Drugs containing enzyme inhibitors as the active ingredient Drugs containing enzyme inhibitors as the active ingredient

A - Human Necessities

61

K

A61K 45/00 (2006.01) A61K 31/70 (2006.01)

Patent

CA 2284094

Drugs capable of selectively inhibiting the proliferation or metabolism of target cells such as cancer cells without affecting normal cells. Such a drug contains as the active ingredient an enzyme inhibitor and satisfies the following requirements: 1) the enzyme inhibitor being capable of inhibiting at least one enzyme essentially required in the first metabolic pathway of a compound essentially required in the survival of cells (i.e., an essential compound); 2) the essential compound being metabolizable in a second pathway which is different from the first pathway and not inhibited by the enzyme inhibitor; and 3) at least one enzyme essentially required in the second metabolic pathway lacking its function in the target cells the proliferation of which is to be inhibited by the drug.

Cette invention se rapporte à des médicaments aptes à inhiber sélectivement la prolifération ou le métabolisme de cellules cibles, telles que des cellules cancéreuses, sans affecter les cellules normales. Un tel médicament contient en tant que principe actif un inhibiteur d'enzymes et il satisfait aux exigences suivantes: (1) l'inhibiteur d'enzymes est capable d'inhiber au moins un enzyme sensiblement indispensable à la première voie métabolique d'un composé sensiblement indispensable à la survie des cellules (par, exemple, un composé essentiel); (2) ledit composé essentiel est métabolisable selon une seconde voie qui est différente de la première voie et n'est pas inhibée par l'inhibiteur d'enzymes et (3) au moins un enzyme indispensable à la seconde voie métabolique n'est pas fonctionnel dans les cellules cibles dont la prolifération doit être inhibée par le médicament en question.

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