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    • 4. 发明授权
    • Phenylethylamine derivatives
    • 苯乙胺衍生物
    • US06251938B1
    • 2001-06-26
    • US09335555
    • 1999-06-18
    • Michael ChorevTamar GorenYacov HerzigJeffrey SterlingMarta Weinstock-RosinMoussa B. H. Youdim
    • Michael ChorevTamar GorenYacov HerzigJeffrey SterlingMarta Weinstock-RosinMoussa B. H. Youdim
    • A61K3127
    • C07C271/42C07C271/56
    • This invention is directed to compounds of the following formula: wherein m is from 0-4; X is O or S; Y is halogeno; R1 is hydrogen or C1-4 alkyl; R2 is hydrogen, C1-4 alkyl or optionally substituted propargyl; and R3 and R4 are each independently hydrogen, C1-8 alkyl, C6-12 aryl, C6-12 cycloalkyl or C6-12 aralkyl, R5 is hydrogen or C1-4 alkyl; and pharmaceutically acceptable salts thereof, provided that when X is O, R2 is optionally substituted propargyl. This invention is also directed to the use of these compounds for treating depression, Attention Deficit Disorder (ADD), Attention Deficit and Hyperactivity Disorder (ADHD), Tourette's Syndrome, Alzheimer's Disease and other dementia's such as senile dementia, dementia of the Parkinson's type, vascular dementia and Lewy body dementia. This invention is further directed to a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.
    • 本发明涉及下式的化合物:其中m为0-4; X是O或S; Y为卤素; R1是氢或C1-4烷基; R2是氢,C1-4烷基或任选取代的炔丙基; 并且R 3和R 4各自独立地为氢,C 1-8烷基,C 6-12芳基,C 6-12环烷基或C 6-12芳烷基,R 5为氢或C 1-4烷基; 其中X为O时,R2为任选取代的炔丙基。本发明还涉及这些化合物用于治疗抑郁症,注意力缺陷症(ADD),注意力缺陷和多动症(ADHD)的用途, Tourette综合征,阿尔茨海默病和其他痴呆症如老年性痴呆,帕金森氏型痴呆,血管性痴呆和路易体痴呆。本发明还涉及一种药物组合物,其包含治疗有效量的上述化合物和药学上可接受的 载体