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    • 1. 发明申请
    • O-ACYL-4-PHENYL-CYCLOHEXANOLS, THEIR SALTS, MEDICAMENTS CONTAINING SUCH COMPOUNDS AND THEIR USE, AS WELL AS A METHOD OF PREPARING THEM
    • O-酰基-4-苯基 - 环己醇,它们的盐,药物含有它们的使用和用于生产
    • WO1995029148A1
    • 1995-11-02
    • PCT/EP1994001276
    • 1994-04-25
    • DR. KARL THOMAE GMBHWOITUN, EberhardMAIER, RolandMÜLLER, PeterHURNAUS, RudolfMARK, MichaelEISELE, BernhardBUDZINSKI, Ralph-MichaelHALLERMAYER, Gerhard
    • DR. KARL THOMAE GMBH
    • C07C219/24
    • C07D295/096C07C219/24C07C237/06C07C2601/14
    • The invention concerns O-acyl-4-phenyl-cyclohexanols of the general formula (I) in which n stands for the numbers 0 or 1, m stands for the numbers 1 or 2, p stands for the numbers 0 or 1, R and R each stand for hydrogen, lower alkyl, alkenyl or alkinyl, these groups possibly being further substituted or, together with the intermediate nitrogen atom, forming 5 to 7-member saturated, monocyclic, heterocyclic rings which may possibly be further interrupted by an oxygen or sulphur atom or an imino group, R , R , R and R stand for hydrogen or lower alkyl, R additionally also stands for lower alkoxy, R stands for hydrogen, cycloalkyl, phenyl or substituted phenyl, naphthyl, tetrahydronaphthyl, thienyl, furyl or pyridyl and A stands for a chemical bond or alkyl, alkenyl or alkinyl having up to 17 carbon atoms. The invention further concerns a method of preparing said compounds, medicaments containing said compounds and the use of said medicaments which are effective in cholesterol biosynthesis. The anti-hypercholesterolemic substances are used for the treatment and prevention of atherosclerosis and inhibit the enzyme 2,3-epoxysqualene-lanosterol-cyclase.
    • 描述了O-酰基-4-苯基 - 环己醇的通式(I),其中n为数字0或1,m是1或2,p个数字0或1,R <1>和R <2> 形成各氢,低级烷基,烯基或炔基,这些基团任选地可以与处于中间的氮原子上被取代,或者一起表示5至7元饱和的单环,杂环还任选被氧或硫原子或 亚氨基可以被中断,R <3>,R <4>,R <5>和R <6>是氢或低级烷基,R <5>除,低级烷氧基,R <7>为氢,环烷基,苯基或取代的苯基 基,萘基,四氢萘基,噻吩基,呋喃基或吡啶基,且a是最多17个C原子的化学键或烷基,烯基或炔基,还涉及它们的制备方法,含有这些化合物的药物组合物,并且其在使用这些药物的 胆囊 从事甾醇生物合成。 用于治疗动脉粥样硬化和预防的物质antihypercholesterolämischen,它可以抑制酶2,3-环氧角鲨烯 - 羊毛甾醇环化酶。