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Substituted 4-arylmethylene-2-imino-2,3-dihydrothiazoles and derivatives and their pharmaceutical use

机译:取代的4-芳基亚甲基-2-亚氨基-2,3-二氢噻唑及其衍生物及其药学用途

摘要

Compounds of Formula I ;including pharmaceutically acceptable salts thereof in the form of individual enantiomers, racemates, or other mixtures of enantiomers, in which;Ar is phenyl, naphthyl or benzobthiophenyl, each of which may be optionally substituted; R1 and R2, which may be the same or different, independently are a) H, b) an alkyl group containing 1 to 6 carbon atoms, c) an alkenyl group containing 3 to 6 carbon atoms, d) a cycloalkyl group containing 3 to 7 carbon atoms, e) a cycloalkylmethyl group in which the ring contains 3 to 7 carbon atoms, f) an aryl or heteroaryl group optionally substituted g) an arylalkyl or heteroarylalkyl group each optionally substituted; or R1 and R2 form an alkylene chain optionally substituted by one or more alkyl groups each containing 1 to 3 carbon atoms, such that, together with the atoms to which they are attached, they form a 5 or 6 membered ring; R3 is a) H, b) an aryl or heteroaryl group each optionally substituted c) an optionally substituted arylmethyl group; or d) an alkoxyalkyl group containing 3 to 6 carbon atoms; and R4 and R5, which may be the same or different, independently are an alkyl group containing 1 to 3 carbon atoms, or R4 and R5 together with the atom to which they are attached form a cycloalkyl ring containing 3 to 6 carbon atoms; processes to prepare such compounds; compositions containing such compounds and their use in the treatment of depression, anxiety, Parkinson's disease, obesity, cognitive disorders, seizures, neurological disorders and as neuroprotective agents; are described.
机译:式I的化合物<化学id =“ CHEM-US-00001”> <图像文件=“ US06187802-20010213-C00001.GIF” imgContent =“ undefined” imgFormat =“ GIF” /> ;包括其药学上可接受的盐,呈单独形式对映异构体,外消旋体或对映异构体的其他混合物,其中; Ar是苯基,萘基或苯并噻吩基,它们各自可以被取代。 R 1 和R 2 可以相同或不同,分别是a)H,b)含1-6个碳原子的烷基,c)烯基含3至6个碳原子的基团,d)含3至7个碳原子的环烷基,e)其中环含有3至7个碳原子的环烷基甲基,f)任选被取代的芳基或杂芳基,g)芳基烷基或杂芳基烷基各自任选地被取代;或R 1 和R 2 形成亚烷基链,该亚烷基链任选被一个或多个各自含有1至3个碳原子的烷基取代,从而与它们所连接的原子一起连接后,它们形成5或6元环; R 3 是a)H,b)各自任选取代的芳基或杂芳基; c)任选取代的芳基甲基; d)含有3至6个碳原子的烷氧基烷基;或和R 4 和R 5 可以相同或不同,分别是含1至3个碳原子的烷基或R 4 和R 5 与它们所连接的原子一起形成含有3至6个碳原子的环烷基环;制备此类化合物的过程;包含此类化合物的组合物及其在治疗抑郁症,焦虑症,帕金森氏病,肥胖症,认知障碍,癫痫发作,神经系统疾病中的用途以及作为神经保护剂的用途;描述。

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