| 摘要 |
PURPOSE: A compound of formula (I) in which Y is hydrogen, halogen or alkoxy; R is hydrogen or alkylthio; R1 is hydrogen or alkyl; X is hydrogen, halogen, alkoxy, alkyl or phenyl; n is one of the integers 1, 2, 3 or 4; or a pharmaceutically acceptable salt thereof are inhibitors of dopamine synthesis and release, useful in the treatment of shizophrenia, Parkinson's Disease, Tourette's Syndrome, alcohol addiction, cocaine addiction, and addiction to analogous drugs. CONSTITUTION: The compounds are 4-aminoethoxy-1,3dihydro-indol-2-one derivatives which are illustrated by Formula 1. in which: Y is hydrogen, halogen or alkoxy of 1 to 6 carbon atoms; R is hydrogen or alkylthio of 1 to 6 carbon atoms; R1 is hydrogen or alkyl of 1 to 6 carbon atoms; X is hydrogen, halogen, alkoxy of 1 to 6 carbon atoms, alkyl of 1 to 6 carbon atoms or phenyl; n is one of the integers 1, 2, 3 or 4; or a pharmaceutically acceptable salt thereof. A preferred group of compounds are those in which Y is hydrogen, chloro or fluoro; R is hydrogen or alkylthio of 1 to 3 carbon atoms; R1 is hydrogen or alkyl of 1 to 3 atoms; X is hydrogen and n is the integers 2 and 3; or a pharmaceutically acceptable salt thereof. The compounds of the Formula I also may be used in the form of a pharmaceutically acceptable acid addition salt having the utility of the free base. Such salts, prepared by methods well known to the art are formed with both inorganic or organic acids, for example: fumaric, maleic, benzoic, ascorbic, succinic, bismethylenesalicylic, methanesulfonic, ethanedisulfonic, acetic, oxalic, propionic, tartaric, salicyclic, citric, gluconic, lactic, malic, mandelic, cinnamic, citraconic, aspartic, stearic, palmitic, itaconic, glycolic, p-aminobenzoic, glutamic, benzenesulfonic, hydrochloric hydrobromic, sulfuric, cyclohexylsulfamic, phosphoric and nitric acids.
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