Aza-indoles and related compounds having...

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 471/04 (2006.01) A61K 31/437 (2006.01) A61K 31/4985 (2006.01) A61K 31/5025 (2006.01) A61K 31/519 (2006.01) A61P 9/00 (2006.01) A61P 29/00 (2006.01) C07D 487/04 (2006.01)

Patent

CA 2729552

The present invention provides compounds having the formula: (I), (II), Wherein n is I or 2; m is 0 or 1; p is 0, 1 or 2; R1 is aryl, heteroaryl or alkyl: R2 is C1-6 hydrocarbyl, alkylacyl or hydroxyalkyl; R3 is aryl, heteroaryl, or alkyl; R4 is H, OH, --O-(C1-6 alkyl), -NH-(C1-6 alkyl), or oxide; R5 is H, halogen, C1-6 alkyl, O-(C1-6 alkyl), aryl, heteroaryl, -C(=O)(C1-6 alkyl), substituted or un-substituted oxazolin-2-yl; X = 0, NH -C(=0)- or -N=CH-; and Each L is independently alkylene and carbonyl. This compounds are SI P antagonists useful for treating a disease selected from: glaucoma, dry eye, angiogenesis, cardiovascular conditions and diseases, wounds, and pain.

La présente invention porte sur des composés représentés par la formule : (I), (II), dans lesquelles n représente 1 ou 2 ; m représente 0 ou 1 ; p représente 0, 1 ou 2 ; R1 représente aryle, hétéroaryle ou alkyle ; R2 représente hydrocarbyle en C1-6, alkylacyle ou hydroxyalkyle ; R3 représente aryle, hétéroaryle ou alkyle ; R4 représente H, OH, -O-(alkyle en C1-6), -NH-(alkyle en C1-6) ou oxyde ; R5 représente H, halogène, alkyle en C1-6, -O-(alkyle en C1-6), aryle, hétéroaryle, -C(=O)(alkyle en C1-6), oxazolin-2-yle substitué ou non substitué ; X = O, NH-C(=O)- ou -N=CH- ; et chaque L représente indépendamment alkylène ou carbonyle. Ces composés sont des antagonistes de S1P utiles pour le traitement d'une maladie choisie parmi : le glaucome, la sécheresse de l'il, l'angiogenèse, les affections et maladies cardiovasculaires, les plaies et la douleur.

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