首页> 外国专利> Derivatives of (1,2,4) - ditiazoli (DI), inductors, glutathione-s-transferase and NADPH quinone oxide reductase, for prophylaxis and Treatment of adverse conditions associated with cytotoxicity and apoptosis in particular in general

Derivatives of (1,2,4) - ditiazoli (DI), inductors, glutathione-s-transferase and NADPH quinone oxide reductase, for prophylaxis and Treatment of adverse conditions associated with cytotoxicity and apoptosis in particular in general

机译:(1,2,4)-地替唑(DI)的衍生物,诱导剂,谷胱甘肽S-转移酶和NADPH醌氧化还原酶,用于预防和治疗与细胞毒性和细胞凋亡相关的不良状况,尤其是在一般情况下

摘要

It also relates to the use of a compound described in the present for the manufacture of a Medicament useful for the prophylaxis and Treatment of adverse conditions associated with cytotoxicity and apoptosis in general in particular.Claim 2: compounds of the General formula (1) wherein the dotted Lines between the C Atom Number 5 and its neighbouring Atoms of n links represent single or double, with the condition that one of the two Links is a simple Link and one is a double Bond, with the condition that When the double bond is between the C Atom and N Atom Number 5, Number 4,R4 there and when the double bond is between the C Atom and N Atom Number 5 of the exo, r2no exists; R1, R2, R3 and R4 independently represent an alkyl group c1-4 branched or unbranched, optionally containing sulfoxide s Atoms or groups, amide, ketone, or sulfon tiocetona A, and is optionally substituted halogeno, cyano, mono - or dialkyl C1 - 4amino, trifluoromethyl,C1-4 alkoxy or hydroxyl, or R1 and R2 together with the N Atom which are United to form a system of rings, 4 to 8 members which may be present in other heteroatoms (substituted) chosen of N, o and S, and the system of rings which can be optionally substituted alkyl C 1 - 4, branched or unbranched, halogeno, cyano, mono - or dialkyl C1 - 4amino, trifluoromethyl,The hydroxyl or alkoxy c1-4 which Ring system contains functions tiocetona, amide, ketone sulfone or sulfoxide, R3 represents h, alkyl, c1-4, branched or unbranched, optionally containing sulfoxide s Atoms or groups, amide, ketone, tiocetona or sulfone, and optionally its Replace with mono halogeno, cyano, trifluoromethyl or dialkyl C1 - 4amino, c1-4 alkoxy, c1-4 alkyl, S,Sh or hydroxyl Group, and R3 represents an optionally substituted aryl, alkyl groups with branched or unbranched c1-4 alkyl, aryl, C1 - 4arilo s, sh, c1-4 alkyl, halogeno, cyano, mono - or dialkyl C1 - 4amino, CF3, ocf3, scf3 Hydroxy or alkoxy, Nitro, C1 - 4, and - tautomeros, stereoisomers Oxides thereof, and pharmacologically acceptable salts,Hydrates and solvates of said compounds of formula (1) and its tautomeros, stereoisomers and N - oxides.
机译:本发明还涉及本发明描述的化合物在制备药物中的用途,所述药物特别用于预防和治疗与细胞毒性和细胞凋亡相关的不良条件。权利要求2:通式(1)的化合物,其中n个链接的C原子数5和其相邻原子之间的虚线表示单或双,其中两个链接之一是简单链接,一个是双键,条件是当双键为在C Atom与N Atom 5号4号R4之间,当双键在exo的C Atom与N Atom 5号之间时,r2no存在; R 1,R 2,R 3和R 4独立地表示分支或未分支的烷基c1-4,任选地包含亚砜原子或酰胺基,酮或磺基噻吩酮A,并且是任选取代的卤素,氰基,单或二烷基C1- 4个氨基,三氟甲基,C1-4烷氧基或羟基,或R1和R2与N原子一起形成环系统,环中可以存在4至8个成员,这些原子可以存在于选自N,o和O的其他杂原子(取代的)中S,和环系统,其可以是任选取代的烷基C 1-4,支链或直链的,卤代,氰基,单或二烷基C 1-4氨基,三氟甲基,环系统含有噻吩并官能团的羟基或烷氧基c1-4,酰胺,酮砜或亚砜,R3代表h,烷基,c1-4,支链或直链的,可选地包含亚砜。原子或基团,酰胺,酮,噻吩酮或砜,及其可选地被单卤代,氰基,三氟甲基或二烷基取代C1-4氨基,C1-4烷氧基,C1-4烷基烷基,S,Sh或羟基,并且R3表示一个可选取代的芳基,具有支链或直链c1-4烷基,芳基,C1-4芳基,sh,c1-4烷基,卤代,氰基,单-或二烷基的烷基C 1-4氨基,CF 3,ocf 3,scf 3羟基或烷氧基,硝基,C 1-4和-互变异构体,立体异构体,其氧化物以及所述式(1)化合物及其互变异构体,立体异构体和N的可药用盐,水合物和溶剂化物-氧化物。

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