Leo-pharma A/s

Leo Pharmaceutical Products, Ltd.

Heinz Wilhelm Dannacher

Erik Rytter Ottosen

Fredrik Bjorkling

Novel pyridyl cyanoguanidine compounds of general formula I (I) wherein R, X, Rand Rare as defined herein, exhibit a high antiproliferative activity and may be used in the treatment of hyperproliferative and neo-plastic diseases. 

Cyanoguanidine compounds

The present invention relates to compounds of formula (I) wherein R, Rand Rindependently represent one or more, same or different substituents selected from the group consisting of hydrogen, halogen, hydroxy, mercapto, trifluoromethyl, amino, (C-C)alkyl, (C-C)olefinic group, (C-C)alkoxy, (C-C)alkylthio, (C-C)alkylamino, (C-C)alkoxycarbonyl, cyano, carbamoyl, or phenyl; Rand Rfurther represented by nitro and Rby carboxy; Rrepresents hydrogen, (C-C)alkyl, or allyl; Q represents a bond, or &#x2014;C(R)(R)(&#x2014;O&#x2014;C&#x2550;O)&#x2014;, in which formula Rand Rindependently represent hydrogen, trifluoromethyl, or (C-C)alkyl; Y represents either (C-C)alkyl, (C-C)olefinic group, (C-C)monocyclic hydrocarbon, or phenyl, any of which may be optionally substituted with one or more, same or different substituents represented by the formula R; or (C-C)alkyl substituted with at least one or more substituents with the formula R; or Y represents a group of formula &#x2014;CH&#x2014;(Z&#x2014;O)&#x2014;Z where Z is a (C-C)alkyl, where n is a integer&#x3e;1 and no continuous linear sequence of atoms in the group Y&#x3e;15; Rrepresents halogen, hydroxy, mercapto, trifluoromethyl, amino, (C-C)alkoxy, (C-C)alkylthio, (C-C)alkylamino, (C-C)alkoxycarbonyl, cyano, azido, nitro, &#x2014;COOH, &#x2014;CONH, &#x2014;CONHR', or &#x2014;COONR&#x2032;R&#x2032; wherein R&#x2032; stands for (C-C)alkyl; X represents oxygen or sulphur, or a pharmaceutically acceptable salt thereof, or a hydrate or solvate thereof. The compounds are valuable in the human and veterinary therapy.

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Skovlunde, Denmark

Heinz Wilhelm Dannacher