| 主权项 |
1. A method of treatment of an individual who is suffering or is susceptible to suffering a disease caused by 11-beta-HSD1-associated disorders which comprises administering to said individual a pharmaceutical composition comprising one or more pharmaceutically acceptable excipient and a therapeutically effective amount of a compound of formula (I) or pharmaceutically acceptable salts thereof, wherein: s and p are an integer selected in an opposite manner between 0 and 1, such that when s is 1, p is 0 (to form a perhydroquinoline) and when s is 0, p is 1 (to form a perhydroisoquinoline), Y is a biradical selected from the group consisting of CO, CS and SO2, W1 and W2 is each independently a bond or a biradical selected from 0, S and NR1, wherein R1 is selected from H, C1-4 alkyl and C3-10 cycloalkyl, n is an integer selected from 0, 1, 2, 3 and 4, V is a radical selected from the groups consisting of —CO-T, —CS-T and —SO2-T, or a radical selected from the group consisting of: where T is a group selected from the groups consisting of NR2R3, R2, OR2 and SR2; or a group selected from the group consisting of wherein R2 and R3 is each independently H, COR4, SO2R4, C1-4 alkyl, aryl, benzyl, phenethyl, C2-4 alkenyl, C2-4 alkynyl, C4-10 cycloalkyl or heterocycle; wherein when R2 or R3 is an alkyl, or an alkenyl these can be optionally substituted with one or several substituents independently selected from the groups consisting of F, OR4, NR4R5, COOR4, CONR4R5, C3-10 cycloalkyl, aryl and heterocycle; wherein when R2 or R3 is an aryl, a benzyl, a phenethyl, a cycloalkyl or a heterocycle, these can be optionally substituted with one or several substituents independently selected from the group consisting of NH2, F, Cl, CN, NO2, COOH, R4, COOR4, OR4, OCF3, SH, SR4, CONR4R5, SO2NR4R5, COR4, NR1COR4, OCOR4, SOR4, SO2R4 and heterocycle; and wherein when R2 or R3 is a cycloalkyl, this can be optionally substituted with one or several fused benzene rings, the benzene could be optionally substituted with one or several substituents independently selected from the group consisting of alkyl, alkoxide and halogen, wherein R4 and R5 is each independently selected from the group consisting of H, C1-4 alkyl, aryl, benzyl, phenethyl, C2-4 alkenyl, C2-4 alkynyl, C3-40 cycloalkyl and heterocycle, or optionally R4 and R5 can be bound to one another forming a 3 to 8 membered cycle, wherein R6, R7, R8 and R9 is each independently selected from the groups consisting of H, OR4, F and Cl, and wherein R10 is independently selected from the group consisting of H, OH, F, C1-4 alkyl, COOR11, COR11, phenyl, benzyl, benzhydryl, C2-4 alkenyl, C2-4 alkynyl, C3-10 cycloalkyl and heterocycle, and wherein the alkyl, phenyl, benzyl, benzhydryl, cycloalkyl or heterocycle can be optionally substituted with one or several substituents independently selected from the group consisting of NH2, F, Cl, NO2, COOH, COOR4, OR4, CF3, SH, SR4, CONR4R5, SO2NR4R5, COR4, NR1COR4, OCOR4, SOR4, SO2R4 and C1-4 alkyl where R11 is selected from the group consisting of H, C1-4 alkyl and C3-10 cycloalkyl, so as to thereby treat the individual, wherein the disease caused by 11-beta-HSD1-associated disorders is glaucoma, elevated ocular pressure, obesity, metabolic syndrome, dyslipidemia, hypertension, diabetes, atherosclerosis, Cushing's syndrome, psoriasis, rheumatoid arthritis, Alzheimer's disease or neurodegeneration. |
