Novel thyroid hormone receptor ligand, medicinal...

C - Chemistry – Metallurgy – 07 – C

Patent

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C07C 59/72 (2006.01) A61K 31/19 (2006.01) A61K 31/22 (2006.01) A61K 31/223 (2006.01) A61K 31/225 (2006.01) A61K 31/27 (2006.01) A61K 31/341 (2006.01) A61K 31/351 (2006.01) A61K 31/40 (2006.01) A61K 31/426 (2006.01) A61K 31/44 (2006.01) A61K 31/4406 (2006.01) A61K 31/50 (2006.01) A61K 31/5375 (2006.01) A61K 31/54 (2006.01) A61P 1/16 (2006.01) A61P 3/04 (2006.01) A61P 3/10 (2006.01) A61P 5/14 (2006.01) A61P 5/16 (2006.01) A61P 9/04 (2006.01) A61P 9/06 (2006.01) A61P 9/10 (2006.01) A61P 9/12 (2006.01) A61P 17/

Patent

CA 2473162

It is intended to provide compounds represented by the following general formula (I) which have a high affinity for human thyroid hormone receptors, in particular, human thyroid hormone receptor .beta., medicinal compositions containing the same, and use thereof: (I) wherein W represents O, S(O)m, CH2, etc.; R1 represents halogeno, lower alkyl, halo(lower alkyl), CN, etc.; R2 represents hydrogen, halogeno, lower alkyl, etc.; R3 represents hydroxy, etc.; R4 represents hydrogen, halogeno, alkyl, halo(lower alkyl), substituted alkyl, aryl, aralkyl, alkoxy, substituted alkoxy, alkanoyl, aroyl, -CONR7(R8), - S(O)mR9, -SO2NR7(R8), etc.; R5 represents hydrogen, halogeno, alkyl, substituted alkyl, etc.; and A represents -N(R6)CO-A1-COR10, etc.

L'invention porte sur des composés représentés par la formule générale (I), présentant une affinité élevée pour les récepteurs de l'hormone thyroïdienne humaine, notamment, le récepteur .beta. de l'hormone thyroïdienne, sur des préparations médicinales les contenant, et sur leur utilisation. Dans ladite formule (I), W représente O, S(O)¿m?, CH¿2?, etc. ; R?1¿ représente halogéno, alkyle inférieur, halo(alkyle inférieur), CN, etc. ; et R?2¿ représente hydrogène, halogéno, alkyle inférieur, etc. ; R?3¿ représente hydroxy, etc. ; R?4¿ représente hydrogène, halogéno, alkyle, halo(alykle inférieur), alkyle substitué, aryle, aralkyle, alcoxy, alcoxy substitué, alcanoyle, aroyle, -CONR?7¿(R?8¿), -S(O)¿m?R?9¿, -SO¿2?NR?7¿(R?8¿), etc. ; R?5¿ représente hydrogène, halogéno, alkyle substitué, etc. ; et A représente N(R?6¿)CO-A?1¿-COR?10¿ etc.

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