Melanin-concentrating hormone receptor antagonists...

C - Chemistry – Metallurgy – 07 – D

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C07D 211/26 (2006.01) A61K 31/438 (2006.01) A61K 31/4439 (2006.01) A61K 31/445 (2006.01) A61P 1/00 (2006.01) A61P 1/16 (2006.01) A61P 3/00 (2006.01) A61P 3/04 (2006.01) A61P 3/06 (2006.01) A61P 3/10 (2006.01) A61P 3/12 (2006.01) A61P 5/00 (2006.01) A61P 9/04 (2006.01) A61P 9/06 (2006.01) A61P 9/10 (2006.01) A61P 9/12 (2006.01) A61P 11/00 (2006.01) A61P 13/12 (2006.01) A61P 15/00 (2006.01) A61P 15/06 (2006.01) A61P 15/10 (2006.01) A61P 17/00 (2006.01) A61P 25/02 (2006.01) A61P 25/08 (2006.01) A61P 25/14 (200

Patent

CA 2515717

Melanin-concentrating hormone receptor antagonists containing as the active ingredient piperidine derivatives represented by the general formula [I]: [wherein R1 is hydrogen, hydroxyl, lower alkyl, or the like; R2, R3a, R3b, R4a, R4b, R5a, R5b and R6 are each hydrogen, halogeno, or the like; W1 and W2 are each independently -O-, -CH2-,or the like; Y1, Y2, Y3 and Y4 are each -CH- , -CF-, -N-, or the like; Z is lower alkyl, a hetero-alicyclic group, or the like; Ar is a mono- or bi-cyclic aliphatic heterocycle or an aromatic heterocycle; and n is an integer of 1 to 8]. The compounds act as antagonist against melanin -concentrating hormone receptor and are useful as drugs for central diseases, circulatory diseases, or metabolic diseases.

La présente invention se rapporte à des antagonistes des récepteurs de l'hormone concentrant la mélanine qui contiennent en tant que principe actif des dérivés de pipéridine représentés par la formule générale [I] ; dans laquelle R?1¿ est hydrogène, hydroxyle, alkyle inférieur, ou analogue ; R?2¿, R?3a¿¿, ?R?3b¿¿,? R?4a¿, R?4b¿, R?5a¿, R?5b¿, et R?6¿ sont chacun hydrogène, halogéno ou analogue ; W?1¿ et W?2¿ sont chacun indépendamment -O, -CH¿2?-, ou analogue ; Y?1¿, Y?2¿, Y?3¿ et Y?4¿ sont chacun -CH-, -CF-, -N-, ou analogue ; Z est alkyle inférieur, un groupe éthéro-alicyclique, ou analogue ; Ar est un hétérocycle aliphatique mono- ou bi-cyclique ou un hétérocycle aromatique ; et n est un entier compris entre 1 et 8. Ces composés se comportent comme des antagonistes dirigés contre les récepteurs de l'hormone concentrant la mélanine et ils sont utiles en tant que médicaments pour les maladies d'un système central, les maladies circulatoires ou les maladies métaboliques.

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