发明名称 Compounds for Treatment of Alzheimer's Disease
摘要 The invention is directed to the use of a compound of formula I, as defined herein, to a pharmaceutically acceptable salt thereof; to a pharmaceutical composition containing a compound of formula I, and to a combination of a compound of formula I with a pharmacologically effective cholinesterase inhibitor to treat a mammal, including a human, for a disorder or condition selected from the list including Alzheimer's disease, Huntington's disease, Parkinson's disease, non-Alzheimer's dementias and ALS.
申请公布号 US2016158209(A1) 申请公布日期 2016.06.09
申请号 US201514854928 申请日期 2015.09.15
申请人 Godek Dennis Michael;Howard Harry Ralph 发明人 Godek Dennis Michael;Howard Harry Ralph
分类号 A61K31/443;A61K45/06;A61K31/343 主分类号 A61K31/443
代理机构 代理人
主权项 1. A method of treating a disorder or condition, selected from the group consisting of Alzheimer's disease, Parkinson's disease, Huntington's disease, ALS and non-Alzheimer's dementias, comprising administering to a mammal in need of said treatment an effective amount of a compound of the formula I:or the pharmaceutically acceptable salt(s) thereof, wherein: X1 is selected from the group consisting of H, (C1-C4)-alkyl, (C1-C4)-alkoxyl, CF3, F, Cl, Br, I and CN. X2 is H, I, Br, Cl, or F; n is zero, one or two; R1 is H, methyl, or dimethyl; R2 is H or (C1-C6)-alkyl; R3 is H, (C1-C6)-alkyl, (C3-C12)-cycloalkyl (optionally containing a S or O atom), aryl (optionally substituted by X3) or ((C1-C6)-alkyl)-aryl; R4 is (C1-C6)-alkyl or aryl (optionally substituted by X4); or R3 and R4 together with the atoms to which they are attached form a 5-12 membered mono- or bi-cyclic ring system, said ring system containing up to two additional heteroatoms selected from N, O or S and said ring optionally substituted at available positions by one or more groups from the list consisting of (C1-C6)-alkyl, (C1-C6)-alkoxyl and aryl, with said ring system including 4,5-dihydro-imidazol-2-yl; 1,3,4-oxadiazol-2-yl, 1,2,4-triazol-3-yl, tetrazole-5-yl, 3,4-dihydro-quinolin-2-yl; 3,4-dihydro-2H-pyrrol-5-yl; 2,3,4,5-tetrahydro-pyridin-6-yl; 1,2,3,6-tetrahydro-pyrazin-2-yl; 3,6-dihydro-2H-1,4-oxazin-5-yl; 1,2-dihydro-quinoxalin-3-yl; 4,5-dihydro-3H-2-benzazepin-1-yl; and 2,5-dihydro-1H-3-benzazepin-4-yl; X3 and X4 are independently selected from the list consisting of: H, F, Cl, Br, I, CN, (C1-C6)alkyl, (C3-C12)cycloalkyl, CF3, C2F5, OCF3, O—(C1-C6)-alkyl, O—(C1-C6)-alkoxyl, OH, NO2, NH2, NHR7 and NR7R8; wherein R7 and R8 are independently selected from the list including (C1-C6)-alkyl, (C3-C12)-cycloalkyl and phenyl, or wherein R7 and R8 together with the N to which they are attached form a 4-12 membered mono- or bi-cyclic ring.
地址 Glastonbury CT US