首页> 外国专利> Sigma ligands for the potentiation of the Analgesic effect of opioids and opiates in the postoperative pain and the Attenuation of the unit with the same

Sigma ligands for the potentiation of the Analgesic effect of opioids and opiates in the postoperative pain and the Attenuation of the unit with the same

机译:Sigma配体可增强阿片类药物和阿片类药物在术后疼痛中的镇痛作用,并具有相同的单位衰减

摘要

A combination including sigma formula (1) ligation and opiates or opiates for the prevention and / or treatment of pain caused by surgery, especially marginal neuralgia, alodine, causal pain, hypertension, hypertension, hypertension, nerve failure, Neurological or neurological disorders: sigma formula ligation (1) for enhancing the analgesic effect of opiates or opiates and / or reducing opiate dependence,When opiates or opiates are used to prevent and / or treat pain due to surgery, requirement 1: is used in combination for simultaneous, separate or sequential management, including at least one formula sigma match (1),or a pharmaceutically acceptable salt, isomer, prodrug or solvate thereof, and at least one opioid or opioid, for use in the prevention and / or treatment of pain developed as a result of surgery in which R1 is selected from the group formed by hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted aryl, substituted or unsubstituted arylalkyl, aromatic or unsubstituted heterocyclyl, substituted or unsubstituted, substituted or unsubstituted heterocyclyl alkyl , -COR8, -C (O) OR8, -C (O) NR8R9, -CH = NR8, -CN, -OR8, -OC (O) R8, -S (O) t-R8, -NR8R9, -NR8C (O) R9, -NO2, -N = CR8R9,Or halogen; R2 is selected from hydrogen, substituted or unsubstituted tar, substituted or unsubstituted cyclopentyl compound, substituted or unsubstituted Halon, substituted or unsubstituted arilalquilo, aromatic or non aromatic isocyclohexane, substituted or unsubstituted components, Propylpropylpropylpropylpropylpropylpropylpropylpropyl Substituted or unsubstitutedsubstituted or unsubstituted aryl, substituted or unsubstituted arylalkyl, aromatic or non-aromatic heterocyclyl, substituted or unsubstituted, substituted or unsubstituted heterocyclyl alkyl, -COR8, -C (O) OR8, -C (O) NR8R9, -CH = NR8 , -CN, -OR8, -OC (O) R8, -S (O) t-R8, -NR8R9, -NR8C (O) R9, -NO2, -N = CR8R9, or halogen, or together form a system of condensed rings optionally substituted; R5 and R6 are independently selected from the group consisting of hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted aryl, substituted or unsubstituted arylalkyl, aromatic or non-aromatic heterocyclyl,substituted or unsubstituted, substituted or unsubstituted heterocyclylalkyl, -COR8, -C (O) OR8, -C (O) NR8R9, -CH = NR8, -CN, -OR8, -OC (O) R8, -S (O ) t-R8, -NR8R9, -NR8C (O) R9, -NO2, -N = CR8R9, or halogen; or together they form, with the nitrogen atom to which they are attached, an aromatic or non-aromatic, substituted or unsubstituted heterocyclyl group; n is selected from 1, 2, 3, 4, 5, 6, 7 or 8; t is 1, 2 or 3; R8 and R9 are each independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted aryl, aromatic or non-aromatic, substituted or unsubstituted heterocyclyl,Substituted or unsubstituted oxy group, substituted or unsubstituted oxy group or halogen. 11. Claim 10: a combination of a group of opiates or opiates consisting of morphine, tramadol, sufentanil, remifentanilo, Fentanil, tapendadol, oxycodone, buprenorphine or similar substances, in accordance with any of the above requirements.
机译:包括sigma公式(1)的结扎剂和鸦片或鸦片制剂的组合,用于预防和/或治疗由手术引起的疼痛,尤其是边缘神经痛,阿洛丁,因果性疼痛,高血压,高血压,高血压,神经衰竭,神经或神经系统疾病:sigma式结扎(1)用于增强阿片或阿片的镇痛作用和/或减轻阿片依赖性,当使用阿片或阿片预防和/或治疗因手术引起的疼痛时,要求1:同时使用,分开使用或联合使用用于预防和/或治疗由此引起的疼痛的序贯治疗方法,包括至少一种式子sigma match(1)或其药学上可接受的盐,异构体,前药或溶剂化物,以及至少一种阿片样物质或阿片样物质R1选自氢,取代或未取代的烷基,取代或未取代的环烷基,取代或未取代的烯基,取代或未取代的芳基,取代或未取代的芳基烷基,芳族或未取代的杂环基,取代或未取代的,取代或未取代的杂环基烷基,-COR8,-C(O)OR8,-C(O)NR8R9,-CH = NR8,-CN -OR8,-OC(O)R8,-S(O)t-R8,-NR8R9,-NR8C(O)R9,-NO2,-N = CR8R9或卤素; R 2选自氢,取代或未取代的焦油,取代或未取代的环戊基化合物,取代或未取代的卤代烃,取代或未取代的芳烃基,芳族或非芳香族异环己烷,取代或未取代的组分,丙基丙基丙基丙基丙基丙基丙基丙基丙基丙基取代或未取代的取代或未取代的芳基,取代或未取代的芳烷基,芳族或非芳族杂环基,取代或未取代的,取代或未取代的杂环烷基,-COR8,-C(O)OR8,-C(O)NR8R9,-CH = NR8,-CN,-OR8,-OC(O R8,-S(O),t-R8,-NR8R9,-NR8C(O)R9,-NO2,-N = CR8R9或卤素,或一起形成任选取代的稠环系统; R 5和R 6独立地选自氢,取代或未取代的烷基,取代或未取代的环烷基,取代或未取代的烯基,取代或未取代的芳基,取代或未取代的芳烷基,芳族或非芳族杂环基,取代或未取代的,取代的。或未取代的杂环基烷基,-COR8,-C(O)OR8,-C(O)NR8R9,-CH = NR8,-CN,-OR8,-OC(O)R8,-S(O)t-R8,-NR8R9 ,-NR8C(O)R9,-NO2,-N = CR8R9或卤素;它们或与它们所连接的氮原子一起形成芳族或非芳族的,取代或未取代的杂环基; n选自1、2、3、4、5、6、7或8; t是1、2或3; R 8和R 9各自独立地选自氢,取代或未取代的烷基,取代或未取代的环烷基,取代或未取代的烯基,取代或未取代的芳基,芳族或非芳香族的,取代或未取代的杂环基,取代或未取代的氧基,取代或未取代的氧基或卤素。 11.权利要求10:根据上述要求中的任何一项,由吗啡,曲马多,舒芬太尼,瑞芬太尼洛,芬太尼,塔潘达多,羟考酮,丁丙诺啡或类似物质组成的一组鸦片或鸦片的组合。

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