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Indeno-, naphtho-, and benzocyclohepta-dihydrothiazole derivatives, the production thereof and their use as anorectic medicaments

机译:茚并,萘和苯并环庚二氢噻唑衍生物,其生产及其作为厌食药的用途

摘要

The invention relates to compounds of the formula I (see below), wherein Y is a direct bond, X represents CH2, R1, R1' independently of one another are H, F, Cl, Br R2 is H, (C1-C6) R3 is H, F R4 represents (C8-C16) cycloalkyl, wherein one or more hydrogen(s) can be substituted in the alkyl groups by fluorine or a hydrogen can be substituted by OH, OC(O)CH3, OC(O)H, O-CH2-Ph or O-(C1-C4) alkyl; (CH2)n-A-R8, with n = 1-6, with the group -CH2-O-CH2-phenyl, wherein phenyl is unsubstituted, being excluded; (CH2)r-B-R9, with r = 1-6; A is O, S, SO, SO2; B is NH, N-(C1-C6) alkyl, NCHO, N(CO-CH3); R8 represents (C5-C24) alkyl, (C3-C10) cycloalkyl, wherein one or more hydrogen(s) can be substituted in the alkyl groups by fluorine or hydrogen can be substituted by OH, OC(O)CH3, OC(O)H, O-CH2-Ph or O-(C1-C4) alkyl; (CH2)m aryl, with m = 0-6, and aryl is phenyl, naphthyl, biphenyl, thienyl or pyridyl and the aryl part can be substituted up to two times; The invention also relates to the physiologically acceptable salts of compound I and to methods for producing them. The inventive compounds are suitable for use as anorectic agents, as a medicament for the prophylaxis and treatment of obesity and type II diabetes.
机译:本发明涉及式I的化合物(参见下文),其中Y是直接键,X代表CH 2,R 1,R 1'彼此独立地是H,F,Cl,Br R 2是H,(C 1 -C 6) R 3是H,F R 4代表(C 8 -C 16)环烷基,其中一个或多个氢可在烷基中被氟取代或氢可被OH,OC(O)CH 3,OC(O)取代H,O-CH 2 -Ph或O-(C 1 -C 4)烷基;排除n = 1-6的(CH 2)n -A-R 8,其中-CH 2 -O-CH 2-苯基,其中苯基未被取代的基团; (CH2)r-B-R9,r = 1-6; A是O,S,SO,SO2; B是NH,N-(C1-C6)烷基,NCHO,N(CO-CH3); R 8代表(C 5 -C 24)烷基,(C 3 -C 10)环烷基,其中一个或多个氢可在烷基中被氟取代或氢可被OH,OC(O)CH 3,OC(O)取代H,O-CH2-Ph或O-(C1-C4)烷基; (CH 2)m芳基,m = 0-6,且芳基为苯基,萘基,联苯基,噻吩基或吡啶基,且芳基部分最多可被取代两次;本发明还涉及化合物I的生理学上可接受的盐及其制备方法。本发明的化合物适合用作厌食剂,作为预防和治疗肥胖症和II型糖尿病的药物。

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