| 主权项 |
1. A method for amelioration of pain comprising administering a therapeutically effective amount of at least one compound represented by the general Formula Iwherein
R1 is —XSO2NR5R6 or —XSO2R8; X is a branched or unbranched C1-4 alkylene, wherein said C1-4 alkylene optionally can be bound to R5 or R6 to form a 5- or 6-membered heterocycle; R5 and R6 independently of each other are selected from the group consisting of hydrogen, C1-4alkyl, hydroxy-C1-4alkyl, C3-4alkenyl, C3-8-cycloalkyl, C3-8-cycloalkyl-C1-4alkyl, C4-7-heterocycloalkyl-C0-4alkyl, C4-7-aryl-C0-4alkyl, and C4-7-heteroaryl-C0-4alkyl; or wherein R5 and R6 together with the N-atom to which they are bound form a 5- to 8-membered heterocycloalkyl, wherein said cycloalkyl, heterocycloalkyl, aryl, heteroaryl or alkyl is further optionally substituted by up to 2 radicals selected from the group consisting of halo, hydroxy, aminocarbonyl, C1-4 alkyl, hydroxy-C1-4 alkyl, C1-4 alkyl-O—C1-4 alkyl, C1-4 alkyl-O—, and —NR5R6; R8 is C1-4 alkyl, hydroxy-C2-4alkyl, C3-4alkenyl, C3-8-cycloalkyl, C3-8-cycloalkyl-C1-4alkyl, or C4-7-heterocycloalkyl-C0-4 alkyl; wherein said cycloalkyl, heterocycloalkyl or alkyl is further optionally substituted by up to 2 radicals selected from the group consisting of halo, hydroxy, C1-4 alkyl, hydroxy-C1-4 alkyl, C1-4 alkyl-O—C1-4 alkyl, C1-4 alkyl-O, and —NR5R6; R2 is one or two substituents independently selected from halogen and hydrogen; R3 can be 1 to 3 substituents each independently selected from the group consisting of hydrogen, halo, hydroxy, C1-4alkyl, C3-7cycloalkyl, C1-4 alkyl -cycloalkyl, C1-4 alkyl-heterocycloalkyl, —O-heterocycloalkyl, C1-4 alkoxy, C2-4 alkenyloxy, —OCF3, C2-4 alkanoyl, C1-4alkylsulfonyl, mono- and di-(C1-C4alkyl)sulfonamido, aminocarbonyl, mono- and di-(C1-C4alkyl)aminocarbonyl, aryl-C1-4 alkoxy, heteroaryl-C1-4 alkoxy, heterocycloalkyl-C1-4-alkoxy, heterocycloalkyl-C1-4-alkyl, heteroaryl-C1-4-alkyl, C1-4 alkyloxymethyl, hydroxy-C1-4alkyloxymethyl, cyano, —COOH, and C1-C4 alkoxycarbonyl, wherein the above mentioned substituents can be further substituted by radicals selected from the group consisting of C1-4-alkyl, hydroxyl-C0-4-alkyl, C1-4-alkoxy, aminocarbonyl, halo, and NR5R6; R4a and R4b are the same or different and each is independently hydrogen, C1-4 alkyl, or —NR′R″, wherein R′ and R″ are each independently hydrogen or C1-4 alkyl; and the N-oxide derivatives, prodrug derivatives, protected derivatives, individual isomers and mixtures of isomers thereof; and the pharmaceutically acceptable salts, solvates, and hydrates of such compounds to a patient suffering from said pain. |
