Jnk activation inhibitor

A - Human Necessities – 61 – K

Patent

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A61K 31/5025 (2006.01) A61K 45/00 (2006.01) A61P 1/00 (2006.01) A61P 1/04 (2006.01) A61P 1/18 (2006.01) A61P 5/14 (2006.01) A61P 7/00 (2006.01) A61P 7/02 (2006.01) A61P 9/00 (2006.01) A61P 9/10 (2006.01) A61P 11/00 (2006.01) A61P 11/02 (2006.01) A61P 11/06 (2006.01) A61P 13/12 (2006.01) A61P 15/00 (2006.01) A61P 17/00 (2006.01) A61P 17/02 (2006.01) A61P 17/04 (2006.01) A61P 17/06 (2006.01) A61P 19/02 (2006.01) A61P 19/06 (2006.01) A61P 19/08 (2006.01) A61P 21/04 (2006.01) A61P 25/00 (2006.01) A61P 25/24 (20

Patent

CA 2458131

Inhibitors against c-Jun N-terminal kinase, containing compounds represented by the general formula (A) or salts or prodrugs thereof: (A) wherein Ara and Arb are each an optionally substituted aromatic group, or Ara and Arb together with the carbon atom adjacent thereto may form a fused ring; Ba is an optionally substituted nitrogenous heterocycle; Xa and Ya are each independently (1) a free valency, (2) oxygen, (3) S(O)p (wherein p is an integer of 0 to 2), (4) NRd (wherein Rd is hydrogen or lower alkyl), or (5) a bivalent linear lower hydrocarbon group which may be substituted and/or interrupted by one to three heteroatoms; Aa is an optionally substituted five- membered ring; Ra and Rb are each independently (1) hydrogen, (2) halogeno, (3) optionally substituted hydrocarbyl, (4) acyl, or (5) optionally substituted hydroxyl; and Rc is (1) hydrogen, (2) hydroxyl which may be substituted with lower alkyl, or (3) carboxyl.

L'invention concerne des inhibiteurs de c-Jun kinase N-terminale contenant des composés de la formule générale (A) ou des sels ou promédicaments de ces composés. Dans ladite formule, Ar?a ¿et Ar?b¿ sont chacun un groupe aromatique éventuellement substitué, ou Ar?a ¿et Ar?b ¿et l'atome de carbone qui leur est adjacent forment des cycles accolés ; B?a¿ est un hétérocycle azoté éventuellement substitué ; X?a¿ et Y?a¿ sont chacun indépendamment (1) une valence libre, (2) oxygène, (3) S(O)¿p? (p étant un entier de 0 à 2), (4) NR?d¿ (R?d¿ étant hydrogène ou alkyl de faible poids moléculaire), ou (5) un groupe hydrocarbure linéaire bivalent de faible poids moléculaire pouvant être substitué ou interrompu par un ou trois hétéroatomes ; A?a ¿est un cycle à cinq éléments éventuellement substitué ; R?a ¿et R?b ¿sont chacun indépendamment (1) hydrogène, (2) halogéno, (3) hydrocarbyl éventuellement substitué, (4) acyl, ou (5) hydroxyl éventuellement substitué ; et, R?c¿ est (1) hydrogène, (2) hydroxyl pouvant être substitué avec alkyl de faible poids moléculaire, ou (3) carboxyl.

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