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    • 3. 发明专利
    • 5-lipoxygenase-activating protein (flap) inhibitors
    • NZ592541A
    • 2012-11-30
    • NZ59254106
    • 2006-10-30
    • PANMIRA PHARMACEUTICALS LLC
    • HUTCHINSON JOHN HOWARDPRASIT PETPIBOON PEPPIMORAN MARKEVANS JILLIAN FLI YIWEISTOCK NICHOLAS SIMONSTEARNS BRIAN ANDREWROPPE JEFFREY ROGERZUNIC JASMINE ELEANORARRUDA JEANNIE MHADDACH MUSTAPHA
    • C07D403/02A61K31/415C07D209/00C07D417/02
    • Disclosed herein are indole compounds of formula (G) wherein the substituents are as defined within the specification, processes for their preparation, compositions comprising said compounds and uses thereof. Said compounds are useful as 5-lipoxygenase-activating protein (FLAP) inhibitors are and therefore useful in the treatment of inflammation, respiratory disease, cardiovascular disease and obstructive pulmonary disease. Examples of preferred compounds include: · 3-[3-tert-butylsulfanyl-l-(4-pyridin-2-yl-benzyl)-5-(pyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethyl-propionamide (Compound 1-1); · 3-[3-tert-butylsulfanyl-l-[4-(6-methoxypyridin-3-yl)-benzyl]-5-(pyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethyl-propionic acid ethyl ester (Compound 1-2); · 3-[3-tert-butylsulfanyl-l-[4-(6-methoxy-pyridin-3-yl)-benzyl]-5-(pyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethyl-propionic acid 6-hydroxy-hexyl ester (Compound 1-3); · 1-[3-tert-butylsulfanyl-l-(4-pyridin-2-yl-benzyl)-5-(pyridin-2-ylmethoxy)1H-indol-2-yl]-2-methyl-propan-2-ol (Compound 1-4); · 3-[3-cyclopropanecarbonyl-5-(pyridin-2-ylmethoxy)-1-(4-thiazol-2-yl-benzyl)-1H-indol-2-yl]-2,2-dimethyl-propionic acid (Compound 2-15); · 3-[3-cyclobutanecarbonyl-5-(pyridin-2-ylmethoxy)-1-( 4-thiazol-2-yl-benzyl)-1H-indol-2-yl]-2,2-dimethyl-propionic acid (Compound 2-16); · 3-[3-tert-butylsulfanyl-1-[ 4-(6-hydroxy-pyridazin-3-yl)-benzyl]-5-(pyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethyl-propionic acid (Compound 2-17); · 3-[3-tert-butylsulfanyl-1-( 4-pyridin-4-yl-benzyl)-5-(pyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethyl-propionic acid (Compound 2-18); · 3-[3-tert-butylsulfanyl-1-[ 4-( 6-methoxy-pyridin-3-yl)-benzyl]-5-(pyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethyl-propionic acid (Compound 2-19).