Therapeutic applications of 2-substituted...

A - Human Necessities – 61 – K

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A61K 31/506 (2006.01) A61P 5/48 (2006.01) A61P 9/00 (2006.01) A61P 17/14 (2006.01) A61P 25/00 (2006.01)

Patent

CA 2502138

The present invention relates to the use of a compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein (A) one of X and Y is S, and the other is N; or one of X and Y is NH or N-R5, and the other is C-R6; "a" is a single bond; "b", "c", "d", "e" and "f' are single or double bonds so as to form a heteroaryl ring; R1 is is R7 with the proviso that R1 is other than H or Me; or (B) one of X and Y is S, and the other is NH or N-R5; "a" and "d" are each double bonds; "b", "c", "e" and "f' are each single bonds; R1 is oxo; and R2, R3, R4, R5, and R6 are each independently H or R7; R7 is a group (CH2)n-R8, wherein n is 0, 1, 2, 3 or 4 and wherein R8is selected from alkyl, aryl, heteroaryl, heterocycloalkyl, F, Cl, Br, I, CF3, NO2, CN, OH, O-alkyl, O- aryl, 0~- heteroaryl, 0-heterocycloalkyl, CO-alkyl, CO-aryl, CO-heteroaryl, CO- heterocycloalkyl, COO-alkyl, NH2, NH-alkyl, NH-aryl, N(alkyl)2, NH-heteroaryl, NH-heterocycloalkyl, COOH, CONH2, CONH-alkyl, CON(alkyl)2, CONH-aryl, CONH- heteroaryl, CONH~heterocycloalkyl, SO3H, S02-alkyl, SO2-aryl, S02-heteroaryl, SO2-heterocycloalkyl, SO2NH2, SO2NH-alkyl, SO2N(alkyl)2, SO2NH-aryl, SO2NH- heteroaryl, or SO2NH~heterocycloalkyl, wherein said alkyl, aryl, heteroaryl, and heterocycloalkyl groups are optionally substituted with one or more groups selected from halogeno, NO2, OH, 0~methyl, NH2, COOH, CONH2 and CF3; in the preparation of a medicament for treating diabetes. The compounds of the invention also have applications in the treatment of CNS disorders, alopecia, cardiovascular disorders and stroke.

La présente invention concerne l'utilisation d'un composé représenté par la formule générale (I) ou l'un de ses sels pharmaceutiquement admis. Dans cette formule, (A) l'un de X et Y est S, l'autre étant N, ou l'un de X et Y est NH ou N-R?5¿, l'autre étant C-R?6¿; "a" est une liaison simple; "b", "c", "d", "e" et "f' sont des liaisons simples ou doubles de façon à former un cycle hétéroaryle; R?1¿ est R?7¿ sous la réserve que R?1¿ soit autre chose que H ou Me; ou (B) l'un de X et Y est S, l'autre étant NH ou N-R?5¿; "a" et "d" sont chacun des liaisons doubles; "b", "c", "e" et "f' sont chacun des liaisons simples; R?1¿ est oxo; et R?2¿, R?3¿, R?4¿, R?5¿, et R?6¿ sont chacun indépendamment H ou R?7¿; R?7¿ est un groupe (CH¿2?)¿n?-R?8¿, dans lequel n vaut 0, 1, 2, 3 ou 4 et dans lequel R?8¿ est choisi parmi les alkyle, aryle, hétéroaryle, hétérocycloalkyle, F, Cl, Br, I, CF¿3?, NO¿2?, CN, OH, O-alkyle, O-aryle, O-hétéroaryle, O-hétérocycloalkyle, CO-alkyle, CO-aryle, CO-hétéroaryle, CO-hétérocycloalkyle, COO-alkyle, NH¿2?, NH-alkyle, NH-aryle, N(alkyle)¿2?, NH-hétéroaryle, NH-hétérocycloalkyle, COOH, CONH¿2?, CONH-alkyle, CON(alkyle)¿2?, CONH-aryle, CONH-hétéroaryle, CONH-hétérocycloalkyle, SO¿3?H, SO¿2?-alkyle, SO¿2?-aryle, SO¿2?-hétéroaryle, SO¿2?-hétérocycloalkyle, SO¿2?NH¿2?, SO¿2?NH-alkyle, SO¿2?N(alkyle)¿2?, SO¿2?NH-aryle, SO¿2?NH-hétéroaryle, ou SO¿2?NH-hétérocycloalkyle, ces groupes alkyle, aryle, hétéroaryle, et hétérocycloalkyle étant éventuellement substitué par au moins un groupe choisi parmi les halogène, NO, OH, O-méthyle, NH¿2?, COOH, CONH¿2? et CF¿3?; ces composés conviennent pour l'élaboration d'un médicament servant au traitement du diabète. Les composés de l'invention trouvent également à s'appliquer pour le traitement de troubles du système nerveux central, l'alopécie, les troubles cardiovasculaires et les accidents cérébrovasculaires.

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