SIGNAL ENZYMES INHIBITORS PARTICIPATING IN THE PROLIFERATION OF CELLS
Номер патента: CO6251316A2
Опубликовано: 21-02-2011
Автор(ы): Andreas Mantoulidis, Christian Klein, Ioannis Sapountzis, Irene Waizenegger, Peter Ettmayer, Steffen Steurer
Принадлежит: Boehringer Ingelheim Int
Опубликовано: 21-02-2011
Автор(ы): Andreas Mantoulidis, Christian Klein, Ioannis Sapountzis, Irene Waizenegger, Peter Ettmayer, Steffen Steurer
Принадлежит: Boehringer Ingelheim Int
Реферат: 1.- Compuestos de la fórmula general (1)en donde R1 representa un heteroarilo de 5-10 miembros, eventualmente sustituido con uno o varios radicales iguales o diferentes, en cada caso, de modo independiente entre sí, seleccionados del grupo compuesto por Ra y Rb; R2 presenta la subestructura (i) o (ii)R3 está seleccionado del grupo compuesto por hidrógeno, halógeno, -CN, -NO2, -NRhRh, -ORh, -C(O)Rh, -C(O)NRhRh, -SRh, -S(O)Rh, -S(O)2Rh, alquilo C1-4, haloalquilo C1-4, cicloalquilo C3-7 y heterocicloalquilo de 3-7 miembros; R5 está seleccionado del grupo compuesto por alquilo C1-6, -Oalquilo C1-6, haloalquilo C1-6, -Ohaloalquilo C1-6,cicloalquilo C3-7, heterocicloalquilo de 3-7 miembros, todos los radicales previamente mencionados eventualmente sustituidos con alquilo C1-6, -CN u -OH; a) en presencia de la subestructura (i) uno de los radicales R6, R7 o R8 y b) en presencia de la subestructura (ii) uno de los radicales R6 o R7 presenta una de las subestructuras (iii) a (vi) y en el caso a) los dos radicales restantes en cada caso de modo independiente entre sí y en el caso b) el segundo radical está/están seleccionados del grupo compuesto por hidrógeno, alquilo C1-6, -Oalquilo C1-6, -OH, -CN, -NHalquilo C1-6, -N(alquilo C1-6)2 y halógeno o c) en presencia de la subestructura (i) R5 representa un alquilo C1-6 o cicloalquilo C3-4 sustituido con un sustituyente -CN y R6, R7 y R8 representa en cada caso hidrógeno; ... 1.- Compounds of the general formula (1) in which R1 represents a 5-10 membered heteroaryl, optionally substituted with one or several identical or different radicals, in each case, independently from each other, selected from the group consisting of Ra and Rb; R2 has the substructure (i) or (ii) R3 is selected from the group consisting of hydrogen, halogen, -CN, -NO2, -NRhRh, -ORh, -C (O) Rh, -C (O) NRhRh, -SRh , -S (O) Rh, -S (O) 2Rh, C1-4 alkyl, C1-4 haloalkyl, C3-7 cycloalkyl and 3-7 membered heterocycloalkyl; R 5 is selected from the group consisting of C 1-6 alkyl, -C 1-6 alkyl, C 1-6 haloalkyl, C 1-6 haloalkyl, C 3-7 cycloalkyl, 3-7 membered heterocycloalkyl, all previously mentioned radicals optionally substituted by alkyl C1-6, -CN or -OH; a) in the presence of the substructure (i) one of the radicals R6, R7 or R8 and b) in the presence of the substructure (ii) one of the radicals R6 or R7 presents one of the substructures (iii) to (vi) and in case a) the two remaining radicals in each case independently of each other and in case b) the second radical is / are selected from the group consisting of hydrogen, C1-6 alkyl, -C1-6 alkyl, -OH, - CN, -N C1-6alkyl, -N (C1-6 alkyl) 2 and halogen oc) in the presence of substructure (i) R5 represents a C1-6 alkyl or C3-4 cycloalkyl substituted with a substituent -CN and R6, R7 and R8 in each case represents hydrogen; ...
Substituted n-hydroxy-3-phenylprop-2-enmide and n-hydroxy-3-phenylpropanamide derivative compounds; deacetylase enzyme inhibitors; its pharmaceutical composition; Useful in the treatment of cancer, tumors, psoriasis, Alzheimer's, among others.
Номер патента: CL2009000727A1. Автор: Lei Jiang,Young Shin Cho,Gang Liu,Michael Schultz,Christine Hiu-Tung Chen,Jianmei Fan,Dyuti Majumdar. Владелец: NOVARTIS AG. Дата публикации: 2010-03-26.