Benzotiazina Derivatives, their Preparation and application as Medicines for inhibition of 11beta hydroxysteroid dehydrogenase Type 1 (11betahsd1)

摘要

Derivados de benzotiazina que tienen la capacidad de inhibir 11beta-HSD1 no solo en el nivel enzim tico sino adem s en el nivel celular Reivindicacion 1 Compuestos que tienen la formula general (1) donde R1 representa Hidrogeno alquilo C1-6 COR5 SO2R5 CO (CH2 In the case where R1, R4 and R'4 represent one kind of hydrogen, C1-6, CN, oh, CF3, ocf3, ome, SME; cyclopentyl; or Oh, CONH2, so2me, so2nh2; C1-6 arilo or cyclopentyl glycol are not replaced or replaced by one or more groups selected from C1-6 halides or hydrocarbon groups; Conditions: R2 group always combines with carbides through carbon atoms; if R2 is a phenyl, cor7 substitute will never be in the position of 4 in terms of carbides; R3 represents methyl or ethyl; R4 and R'4 are the same or different, representing: hydrogen; halogen; C1-6 tar; CN; CF3; ocf3; SME; ome; nr7r8; R5 for: C1-6 tar; phenyl,Or not replaced with one or more selected halogen groups, C1-6 asphalt, CN, oh, CF3, ocf3, SME, a naphthalene, or one or more selected C1-6 halogen or asphalt groups, CN, oh, CF3, ocf3, SME, cyclopentadiene, or one CONH2, so2me, so2nh2, isobutylene, or other substances. Not represented by one or more selected halogen groups, C1-6 tar, CN, oh, CF3, ocf3, SME, R6: hydrogen, C1-6 phenyl tar, or not replaced or replaced by one or more selected halogen groups, C1-6 tar, CN, oh, CF3, ocf3, SME; North Atlantic or heterocycle,Or not replaced or replaced with one or more selected C1-6 halogens or hydrocarbons, CN, oh, CF3, ocf3, SME; cyclopentyl; or not replaced or replaced with CONH2, so2me, so2nh2; R7 for hydrogen, C1-6 tar; R8 for hydrogen, C1-6 tar, phenyl, 1. Not replaced or replaced with one or more selected halogen groups, C1-6 tar, CN, oh, CF3, ocf3, SME; or not replaced or replaced with one or more selected halogen groups, C1-6 tar, CN, oh, CF3, ocf3, SME; or not replaced or replaced with CONH2, so2me, so2nh2;R7 and R8 together can form a cycle of 4 to 6 members, and the nitrogen atom connected to it may contain one or more heteroatoms selected from n, s or O, and may not be replaced or replaced by one or more groups selected from C1-6 tar, C1-6 arilo or arilo; R10 stands for halide, COOH, cour7; R11 stands for hydrogen, C1-6 tar, C1-6 cyclododecyl tar, cyclododecyl tar, arilo, C1-6 arilo tar; and acceptable therapeutic stereoisomers, salts, and solutions.