公开(公告)号：WO1997035839A1

公开(公告)日：1997-10-02

申请号：PCT/EP1996001324

申请日：1996-03-27

Applicant: SCHERING AKTIENGESELLSCHAFT ,  KLAR, Ulrich ,  GRAF, Hermann ,  BLECHERT, Siegfried ,  SACHSE, Anke

Inventor： SCHERING AKTIENGESELLSCHAFT

IPC: C07C271/02

CPC classification number: C07D303/16 ,  C07C233/83 ,  C07C271/22 ,  C07C2602/42 ,  C07F7/1804

Abstract: The disclosure relates to borneol derivatives of general formula (I) wherein: R represents a phenyl residue optionally substituted by halogen atoms, C1-C4 alkyl groups, C1-C4 alkoxy groups, C1-C6 alkoxycarbonyl groups or C1-C8 acyloxy groups; R stands for a hydrogen atom, a C1-C4 alkyl group, substituted aryl, a C1-C6 alkoxycarbonyl group or a C1-C8 acyl group; R stands for a hydrogen atom, a C1-C4 alkyl group, a C1-C4 acyl group or a tri-C1-C4 alkylsilyl group; R and R represent a hydrogen atom, a C1-C4 alkyl residue or a phenyl residue optionally substituted by halogen atoms, C1-C4 alkyl group, C1-C9 alkoxy groups, C1-C4 alkoxycarbonyl groups or C1-C8 acyloxy groups; R and R stand for a hydrogen atom, hydroxy group or a C1-C8 acyloxy group, or together represent a carbon-carbon bond or oxygen atom; or R and R and/or R and R respectively stand together for a carbonyl group, a C1-C4 alkylidene group or if required an oxirane group substituted by a C1-C3 alkyl group. Also disclosed are the salts of these derivatives with physiologically tolerable acids, their alpha -, beta - or gamma -cyclodextrin clathrates and compounds of general formula (I) encapsulated in liposomes.

Abstract translation: Borneolderivate通式（I）中有所描述，其中R <1>表示任选被卤原子，C1-C4烷基，C1-C4烷氧基，C1-C6烷氧羰基或C 1 -C 8 - 酰氧基苯基取代; [R <2>表示一个氢原子，一个C1-C4烷基，取代的芳基，一个C1-C6烷氧基羰基或C1-C8酰基基团; [R <3>代表氢原子，C1-C4烷基，C1-C4酰基或三C1-C4烷基甲硅烷基，并且其中; [R <4>和R <7>代表氢原子，C1-C4烷基或任选地被卤素原子，C1-C4烷基，C1-C9烷氧基，C1-C4烷氧羰基或C 1 -C 8 - 酰氧基苯基取代的 且R <5>和R <6>代表氢原子，羟基或C1-C8-酰氧基或一起代表碳 - 碳键或氧原子，或R <4>和R <5>和/或R <6> 且R <7>的每个一起表示羰基，C1-C4亚烷基，或者，如果需要的话，由一个C1-C3烷基取代的环氧乙烷基团，和任选地它们的盐与生理上可接受的酸，以及它们的α - ，β - 或伽马-Cyclodextrinclathrate和 通式（I）的脂质体包裹的化合物的意思。