发明名称 Glycosidase inhibitors
摘要 Novel compounds of formula (I); wherein R1 to R4 and X have the meaning according to the claims, are glucosidase inhibitors, and can be employed, inter alia, for the treatment of Alzheimer's disease.
申请公布号 US9469657(B2) 申请公布日期 2016.10.18
申请号 US201414502213 申请日期 2014.09.30
申请人 Merck Patent GmbH 发明人 Donnelly Marianne;Qiu Hui;Yu Henry;Liu-Bujalski Lesley;Goutopoulos Andreas
分类号 A61K31/429;C07D513/04;A61K31/4439;A61K31/454 主分类号 A61K31/429
代理机构 EMD Serono Research Institute 代理人 EMD Serono Research Institute
主权项 1. A method for treating a condition selected from the group of tauopathy, Parkinson's disease and amyotrophic lateral sclerosis, said method comprising administering an effective amount of at least one compound of formula (I) wherein R1 denotes Y, COA, COOA, COO—(CH2)n—Ar or COO—(CH2)n-Cyc; R2, R3 denote independently from one another Y or SO2Y; R4 denotes Cl, Br, I, COOY, SO2Y, CN, CAr3, (CH2)m—Ar, R5 denotes (CH2)n—Ar, (CH2)n-Cyc, (CH2)n-Het, (CH2)n—O—Ar, (CH2)n—CY(OH)—Ar, (CH2)n—CO—Ar or (CH2)n—NY—Ar; X denotes CH2, CO or CH(OH); Y denotes H or A; A denotes unbranched or branched alkyl having 1-10 C atoms, in which 1-7 H atoms can be replaced independently from one another by Hal or in which one CH2 group can be replaced by a —CH═CH— group; Cyc denotes cycloalkyl having 3-7 C atoms, in which 1-4 H atoms can be replaced independently from one another by Hal or which can be substituted by Ar; Ar denotes an unsaturated or aromatic mono- or bicyclic carbocycle having 3-12 C atoms, which can be substituted by at least one substituent selected from the group of Hal, A, (CY2)n—OY, (CY2)n—NYY, COOY, CONYY, NHCOY, SO2Y, CN and phenoxy; Het denotes an unsaturated or aromatic mono-, bi- or tricyclic heterocycle having 1-12 C atoms and 1-4 N atoms, which can be substituted by at least one substituent selected from the group of Hal, A, (CY2)n—OY, (CY2)n—NYY, COOY, CONYY, NHCOY, SO2Y, SO2Ar, CN and thiophenyl; Hal denotes F, Cl, Br or I; m denotes 1, 2 or 3; and n denotes 0, 1, 2, 3, 4, 5 or 6;or a physiologically acceptable salt thereof to a mammal in need of such treatment.
地址 Darmstadt DE