Consejo Superior De Investigaciones Cientificas

Centre Hospitalier Universitaire Vaudois (c.h.u.v.)

Inmaculada Robina

Alessio Nencioni

Michel Duchosal

Faustino Mollinedo

Pierre Vogel

Nahimana Aimable

The present invention relates to novel piperidine derivatives having better cell growth inhibitory activities toward cancer cell cultures and, more particularly, PANC-1 cancer cell cultures than FK866. Accordingly, the present invention relates to compounds of formula I, wherein Aris aryl or heteroaryl, which are optionally substituted by one, two or three substituents selected from lower alkyl; lower alkoxy; formyl; hydroxyl; lower alkyl substituted by lower alkoxy or hydroxyl; A is CH, CHor CH, wherein n=4,5,6,7; B is &#x2550;N&#x2014;CN, oxo (&#x2550;O), thio (&#x2550;S); D is NH, &#x2014;CH&#x2550;CH&#x2014;; Aris aryl or heteroaryl which are optionally substituted by one, two or three halogen substituents; wherein, if B is oxo (&#x2550;O), Arand Arare not simultaneously phenyl and pyridine-3-yl; B and D are not simultaneously &#x2550;N&#x2014;CN and &#x2014;CH&#x2550;CH&#x2014;, or a pharmaceutically acceptable salt, a racemic mixture or its corresponding enantiomers and/or optical isomers. The compounds of formula I and their pharmaceutically usable addition salts possess valuable pharmacological properties. Specifically, it has been found that the compounds of the present invention, alone or in combination with other therapeutic active compounds, have an activity as chemotherapeutic agents against cancer and, more particularly, pancreatic cancers. 

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