首页> 外国专利> Derivatives of 1 - oxa - 2.8 - Grabarsky, IT's The Wrong Guy spiro 4.5 dec - 2 - substituted Eno, processes for their preparation, their use for Preparation of Drugs and drugs containing these compounds

Derivatives of 1 - oxa - 2.8 - Grabarsky, IT's The Wrong Guy spiro 4.5 dec - 2 - substituted Eno, processes for their preparation, their use for Preparation of Drugs and drugs containing these compounds

机译:1-oxa-2.8-Grabarsky的衍生物,IT的The Guy螺[4.5] dec-2-取代的Eno,其制备方法,其在制备药物中的用途以及包含这些化合物的药物

摘要

1-oxa-2, 8-diaza-helix [4.5] dec-2-eno [4.5] substituted by general formula (1),Racemic, pure stereoisomers, especially enantiomers or enantiomers, or in any proportion, in the form or form of their acids or bases, or in the form of their salts, or in a mixture of their stereoisomers, especially their enantiomers and enantiomers, In particular, the physiologically tolerable salts, especially in the form of hydrochloric acid or solution, especially hydrate, wherein: R1 and R2 represent h, c1-8, c1-8, c3-10 (C1-12 tar) - cyclo-10, arilo (C1-12 tar) - arilo and isocyclohexane, respectively,(C1-12) - isopropene or nh-c (= O) - arilo, wherein at least one R1 and R2 is different from h, or R1 and R2 jointly represent - (cr4r5) m - (cr6r7) n-y - (cr8r9) P - (cr10r11) Q, m, N, P and Q respectively, provided that m + n is 1 and P + Q is 1, O represents - ch2-ch2-c (Arlo) = CH2 -;R3 represents H, SO2R12 or COR13; R4, R5, R6, R7, R8, R9, R10 and R11 independently represent H, C1-10alkyl, C3-8cycloalkyl, (C1-6alkyl) -C3-8cycloalkyl, aryl, (C1-6alkyl ) -aryl, heterocyclyl, (C1-6alkyl) -heterocyclyl or C (= O) R14; Y represents CR15R16, NR17 or O; R12 and R13 independently represent one another C1-10alkyl, C3-10cycloalkyl, (C1-6alkyl) -C3-10cycloalkyl, aryl, (C1-6alkyl) -aryl, heterocyclyl, (C1-6alkyl) -heterocyclyl or NR18R19; R14 represents H, C1-10alkyl, C3-8cycloalkyl, (C1-6alkyl) -C3-8cycloalkyl, aryl, (C1-6alkyl) -aryl, heterocyclyl, (C1-6alkyl) -heterocyclyl or OR20;R15 and R16 independently represent H, C1-10alkyl, C3-8cycloalkyl, (C1-6alkyl) -C3-8cycloalkyl, aryl, (C1-6alkyl) -aryl, heterocyclyl, (C1-6alkyl) -heterocyclyl, or C (= O) R21; R17 represents H, C1-10alkyl, C3-8cycloalkyl, (C1-6alkyl) -C3-8cycloalkyl, aryl, (C1-6alkyl) -aryl, heterocyclyl, (C1-6alkyl) -heterocyclyl or C ( = O) R22; R18 and R19 independently represent each other represents H, C1-10alkyl, C3-8cycloalkyl, (C1-6alkyl) -C3-8cycloalkyl, aryl, (C1-6alkyl) -aryl, heterocyclyl, or (C1-alkyl 6) -heterocyclyl; R20 represents represents H, C1-10 alkyl, C3-8 cycloalkyl, (C1-6 alkyl) -C3-8 cycloalkyl, aryl,(C1-6alkyl) -aryl, heterocyclyl, or (C1-6alkyl) -heterocyclyl; R21 represents represents H, C1-10alkyl, C3-8cycloalkyl, (C1-6alkyl) -C3-8cycloalkyl, aryl, (C1-6alkyl) -aryl, heterocyclyl, (C1-6alkyl) -heterocyclyl or OR23 ; R22 represents represents H, C1-10alkyl, C3-8cycloalkyl, (C1-6alkyl) -C3-8cycloalkyl, aryl, (C1-6alkyl) -aryl, heterocyclyl, (C1-6alkyl) -heterocyclyl or OR24 ; and R23 and R24 independently represent each other represents H, C1-10alkyl, C3-8cycloalkyl, (C1-6alkyl) -C3-8cycloalkyl, aryl, (C1-6alkyl) -aryl, heterocyclyl, or (C1alkyl -6) -heterocyclyl; procedures for its preparation,3. For the production of drugs containing these compounds. These compounds are suitable for pain treatment and ultimately for neurological and chronic pain.
机译:用通式(1)取代的1-oxa-2、8-二氮杂螺旋[4.5] -2--2-烯基[4.5],一种或多种形式的外消旋的,纯的立体异构体,特别是对映体或对映体它们的酸或碱或其盐的形式,或它们的立体异构体的混合物,特别是其对映异构体和对映异构体的混合物,特别是生理上可耐受的盐,尤其是盐酸或溶液形式,尤其是水合物形式, :R1和R2分别代表h,c1-8,c1-8,c3-10(C1-12焦油)-环10,芳基(C1-12焦油)-芳基和异环己烷,(C1-12)-异丙烯或nh-c(= O)-arilo,其中至少一个R1和R2与h不同,或R1和R2共同代表-(cr4r5)m-(cr6r7)ny-(cr8r9)P-(cr10r11)Q,分别为m,N,P和Q,只要m + n为1且P + Q为1,O代表-ch2-ch2-c(Arlo)= CH2--; R3代表H,SO2R12或COR13; R 4,R 5,R 6,R 7,R 8,R 9,R 10和R 11分别代表H,C 1-10烷基,C 3-8环烷基,(C 1-6烷基)-C 3-8环烷基,芳基,(C 1-6烷基)-芳基,杂环基,( C 1-6烷基)-杂环基或C(= O)R14; Y代表CR15R16,NR17或O; R12和R13独立地彼此代表C1-10烷基,C3-10环烷基,(C1-6烷基)-C3-10环烷基,芳基,(C1-6烷基)-芳基,杂环基,(C1-6烷基)-杂环基或NR18R19; R14代表H,C1-10烷基,C3-8环烷基,(C1-6烷基)-C3-8环烷基,芳基,(C1-6烷基)-芳基,杂环基,(C1-6烷基)-杂环基或OR20; R15和R16独立地代表H ,C 1-10烷基,C 3-8环烷基,(C 1-6烷基)-C 3-8环烷基,芳基,(C 1-6烷基)-芳基,杂环基,(C 1-6烷基)-杂环基或C(= O)R 21; R17代表H,C1-10烷基,C3-8环烷基,(C1-6烷基)-C3-8环烷基,芳基,(C1-6烷基)-芳基,杂环基,(C1-6烷基)-杂环基或C(= O)R22; R 18和R 19彼此独立地表示H,C 1-10烷基,C 3-8环烷基,(C 1-6烷基)-C 3-8环烷基,芳基,(C 1-6烷基)-芳基,杂环基或(C 1-烷基6)-杂环基; R20代表H,C1-10烷基,C3-8环烷基,(C1-6烷基)-C3-8环烷基,芳基,(C1-6烷基)-芳基,杂环基或(C1-6烷基)-杂环基; R 21代表H,C 1-10烷基,C 3-8环烷基,(C 1-6烷基)-C 3-8环烷基,芳基,(C 1-6烷基)-芳基,杂环基,(C 1-6烷基)-杂环基或OR 23; R 22代表H,C 1-10烷基,C 3-8环烷基,(C 1-6烷基)-C 3-8环烷基,芳基,(C 1-6烷基)-芳基,杂环基,(C 1-6烷基)-杂环基或OR 24; R 23和R 24彼此独立地表示H,C 1-10烷基,C 3-8环烷基,(C 1-6烷基)-C 3-8环烷基,芳基,(C 1-6烷基)-芳基,杂环基或(C 1烷基-6)-杂环基。准备程序; 3。用于生产含有这些化合物的药物。这些化合物适用于疼痛治疗,并最终适用于神经性和慢性疼痛。

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