首页> 外国专利> SUBSTITUTED 4-ARYLMETHYLENE-2-IMINO-2,3-DIHYDROTHIAZOLES, THEIR DERIVATIVES AND APPLICATION IN THE PHARMACEUTICAL INDUSTRY

SUBSTITUTED 4-ARYLMETHYLENE-2-IMINO-2,3-DIHYDROTHIAZOLES, THEIR DERIVATIVES AND APPLICATION IN THE PHARMACEUTICAL INDUSTRY

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和在医药工业中的应用

摘要

The compounds, including their pharmaceutically acceptable salts in the form of individual enantiomers, racemates and other enantiomer mixtures have the general formula where Ar is phenyl, naphthyl or benzo(b)thiophenyl each of which can optionally be substituted; R1 & R2 can be the same or different meaning individually H, alkyl group with 1 to 6 carbon atoms, alkenyl group with 3 to 6 carbon atoms, cycloalkyl group with 3 to 7 carbon atoms, cycloalkylmethyl group the ring of which is with 3 to 7 carbon atoms, aryl or heteroaryl group, optionally substituted, arylalkyl or heteroarylalkyl group, optionally substituted, or R1 and R2 form alkylene chain optionally substituted with one or more alkyl group with 1 to 3 carbon atoms so that together with the atoms to which they are adjuncted can form 5- or 6-member ring, R3 is H, aryl or heteroaryl group, optionally substituted, arylmethyl group optionally substituted, or alkoxyalkyl group with 3 to 6 carbon atoms, and R4 & R5 can be the same or different and individually mean alkyl group with 1 to 3 carbon atoms, and R4 & R5 together with the atom to which they are adjuncted, form cycloalkyl ring containing 3 to 6 carbon atoms. The invention also relates to a method for the preparation of the above compounds, to compositions containing them and to their application for the treatment of depression, anxiety, Parkinson, neurological disease and as a neuroprotective means. 17 claims
机译:化合物,包括其各自的对映异构体,外消旋物和其他对映异构体混合物形式的药学上可接受的盐,其通式为:其中Ar是苯基,萘基或苯并(b)噻吩基,它们各自可以被取代; R 1和R 2可以分别相同或不同,表示H,碳数为1至6的烷基,碳数为3至6的烯基,碳数为3至7的环烷基,环的环数为3至3的环烷基甲基。 7个碳原子,任选取代的芳基或杂芳基,任选取代的芳烷基或杂芳基烷基或R1和R2形成任选被一个或多个具有1-3个碳原子的烷基取代的亚烷基链,以便与它们所取代的原子一起相邻的可形成5或6元环,R 3为H,芳基或杂芳基,任选取代的,任选取代的芳基甲基或具有3至6个碳原子的烷氧基烷基,并且R 4和R 5可以相同或不同,并且R 4和R 5分别是指具有1至3个碳原子的烷基,并且R 4和R 5与它们所邻接的原子一起形成含有3至6个碳原子的环烷基环。本发明还涉及制备上述化合物的方法,涉及包含它们的组合物,以及它们在治疗抑郁症,焦虑症,帕金森氏症,神经疾病和作为神经保护手段中的应用。 17件

著录项

  • 公开/公告号BG103754A

    专利类型

  • 公开/公告日2000-06-30

    原文格式PDF

  • 申请/专利权人 KNOLL AKTIENGESELLSCHAFT;

    申请/专利号BG19990103754

  • 申请日1999-09-24

  • 分类号C07D513/10;C07D277/42;A61K31/425;C07D417/12;C07D513/04;

  • 国家 BG

  • 入库时间 2022-08-22 01:57:29

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