Compositions useful as inhibitors of erk

A - Human Necessities – 61 – K

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Details

A61K 31/4155 (2006.01) A61K 31/395 (2006.01) A61K 31/40 (2006.01) A61K 31/4439 (2006.01) A61K 31/497 (2006.01) A61K 31/501 (2006.01) A61K 31/506 (2006.01) A61K 31/53 (2006.01) A61L 27/54 (2006.01)

Patent

CA 2369502

This invention provides a method of treating a disease state in mammals that is alleviated by treatment with a protein kinase inhibitor, especially an ERK inhibitor, which method comprises administering a compound having the pharmacophric features Grp1, Grp2 and Grp3: Grp 1 is an optionally substituted aryl or aliphatic group; Grp 2 is a heteroaromatic ring having one to three nitrogens, said ring comprising a hydrogen bond acceptor HBA2 optinally bonded to a hydrogen bond donor HBD2, and Grp3 is a heteroaromatic ring comprisng a hydrogen bond donor HBD1, with distances between the phrmacophoric features defined in the specification. The method is useful for treating cancer, stroke, diabetes, hepatomegaly, cardiovascular disease, Alzheimer's disease, cystic fibrosis, viral disease, autoimmune diseases, atherosclerosis, restenosis, psoriasis, allergic reactions, inflammation, neurological disorders or a hormone-related disease.

La présente invention concerne une méthode de traitement d'une maladie chez les mammifères consistant à en atténuer les symptômes par un traitement à base d'un inhibiteur de la protéine kinase, particulièrement un inhibiteur de type ERK. Cette méthode consiste à administrer un composé présentant les caractéristiques pharmacophoriques Grp1, Grp2 et Grp3: Grp 1 représente aryle éventuellement substitué ou un groupe aliphatique; Grp 2 représente un noyau hétéroaromatique à un ou trois azotes, ledit noyau comprenant un accepteur de liaison d'hydrogène HBA2 éventuellement lié à un donneur de liaison d'hydrogène HBD2, et Grp3 représente un noyau hétéroaromatique comprenant un donneur de liaison d'hydrogène HBD1, avec des distances entre les caractéristiques pharmacophoriques définies dans le descriptif. En outre, cette méthode est utile pour traiter le cancer, les attaques, le diabète, l'hépatomégalie, les maladies cardio-vasculaires, la maladie d'Alzheimer, la fibrose kystique, les maladies virales, les maladies auto-immunes, l'athérosclérose, la resténose, le psoriasis, les réactions allergiques, l'inflammation, et les troubles neurologiques ou les maladies hormonales.

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