Dibenzylamine compounds and pharmaceutical use thereof

C - Chemistry – Metallurgy – 07 – D

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C07D 257/06 (2006.01) A61K 31/196 (2006.01) A61K 31/41 (2006.01) A61K 31/415 (2006.01) A61K 31/4196 (2006.01) A61K 31/42 (2006.01) A61K 31/421 (2006.01) A61K 31/4245 (2006.01) A61K 31/425 (2006.01) A61K 31/426 (2006.01) A61K 31/433 (2006.01) A61K 31/4402 (2006.01) A61K 31/4406 (2006.01) A61K 31/505 (2006.01) A61P 3/04 (2006.01) A61P 3/06 (2006.01) A61P 9/10 (2006.01) C07C 229/46 (2006.01) C07C 255/58 (2006.01) C07D 213/74 (2006.01) C07D 231/38 (2006.01) C07D 239/42 (2006.01) C07D 249/14 (2006.01) C07D 261/1

Patent

CA 2464846

A dibenzylamine compound represented by the formula (1) (see formula 1) wherein R1 and R2 are each a C1-6alkyl group optionally substituted by halogen atoms and the like; R3, R4 and R5 are each a hydrogen atom, a halogen atom and the like, or R3 and R4 may form, together with carbon atoms bonded thereto, a homocyclic or heterocyclic ring optionally having substituent(s); A is -N(R7)(R8) and the like; ring B is an aryl group or a heterocyclic residue; R6 is a hydrogen atom, a halogen atom, a nitro group, a C1-6 alkyl group and the like; n is an integer of 1 to 3, a prodrug thereof and a pharmaceutically acceptable salt thereof show selective and potent CETP inhibitory activity, and therefore, they can be provided as therapeutic or prophylactic agents for hyperlipidemia or arteriosclerosis and the like.

La présente invention se rapporte à un composé dibenzylamine représenté par la formule générale (1), dans laquelle R?1¿ et R?2¿ sont chacun alkyle C¿1-6? éventuellement halogéné, etc. ; R?3¿, R?4¿ et R?5¿ sont chacun hydrogène, halogéno, etc. ; à condition que R?3¿ et R?4¿ puissent former un homocycle ou hétérocycle éventuellement substitué avec les atomes de carbone qui leur sont associés ; A est -N(R?7¿)(R?8¿), etc. ; le noyau B est aryle ou un résidu hétérocyclique ; R?6¿ est hydrogène, halogéno, nitro, alkyle C¿1-6?, etc. et n est un entier compris entre 1 et 3. L'invention se rapporte également à un promédicament de ce composé ou un sel pharmaceutiquement acceptable du composé ou dudit promédicament. Le composé et son promédicament possèdent une puissante activité sélective d'inhibition de la CETP et sont par conséquent utiles, par exemple, en tant que médicament permettant de traiter ou de prévenir l'hyperlipidémie, l'artériosclérose, etc..

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