C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 401/04 (2006.01) A61K 31/44 (2006.01) A61K 31/47 (2006.01) A61K 31/495 (2006.01) A61K 31/535 (2006.01) C07D 401/14 (2006.01) C07D 403/04 (2006.01) C07D 403/14 (2006.01) C07D 405/14 (2006.01) C07D 409/14 (2006.01) C07D 413/14 (2006.01) C07D 417/14 (2006.01) C07D 471/04 (2006.01) C07D 471/10 (2006.01) C07D 473/00 (2006.01) C07F 7/22 (2006.01)
Patent
CA 2234701
The present invention addresses substituted pyridyl pyrroles, as well as compositions containing such compounds and methods of treatment. The compounds in the present invention are glucagon antagonists and inhibitors of the biosynthesis and action of TNF-.alpha. and IL1. The compounds block the action of glucagon at its receptors and thereby decrease the levels of plasma glucose. The instant pyrroles are also inhibitors of TNF-.alpha. and IL1 and may be used as antidiabetic agents as well as other cytokine mediated diseases. Cytokine mediated diseases refer to diseases or conditions in which excessive or unregulated production of one or more cytokines occurs. Interleukin-1 (IL-1) and Tumor Necrosis Factor (TNF) are cytokines produced by a variety of cells, which are involved in immunoregulation and other physiological conditions, such as inflammation.
La présente invention concerne des pyrroles de pyridyle substitués, des compositions contenant de tels composés et leur utilisation thérapeutique. Les composés de la présente invention sont des antagoniste du glucagon et des inhibiteurs de la biosynthèse et de l'action du facteur TNF-.alpha. et de l'IL1. Ces composés bloquent l'action du glucagon au niveau de ses récepteurs, ce qui diminue les niveaux de glucose du plasma. Les pyrroles de l'invention, qui sont également des inhibiteurs du facteur TNF-.alpha. et de l'IL1, peuvent servir d'antidiabétiques et contre d'autres affections à médiation des cytokines. L'interleukine-1 (IL-1) et le facteur de nécrose tumorale (TNF) sont des cytokines produites par diverses cellules qui interviennent au niveau de la régulation immunitaire et au niveau d'autres états physiologiques tels que les états inflammatoires.
Chang Linda L.
de Laszlo Stephen E.
Kim Dooseop
Mantlo Nathan B.
Merck & Co. Inc.
Ogilvy Renault
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