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The amino acid derivativges comprising disulfide group as enkephalinase and Aminopeptidase N mixed inhibitor
专利权人:
PHARMALEADS;领先药物公司;領先藥物公司
发明人:
ROQUES, Bernard,贝纳德.罗克,貝納德.羅克,FOURNIEZALUSKI, MarieClaude,马里克洛德.富尼耶扎武斯基,馬里克洛德.富尼耶扎武斯基,贝纳德.罗克,貝納德.羅克,马里克洛德.富尼耶扎武斯基,馬里克洛德.富尼耶扎武斯基
申请号:
MOJ001280
公开号:
MOJ001280B
申请日:
2013.11.12
申请国别(地区):
MO
年份:
2014
代理人:
摘要:
The present invention relates to the new compounds of formula (I): H2N-CH (R1)-CH2-S-S-CH2-CH (R2)-CONH-R5, in which: R1 is hydrocarbon chain, phenyl or benzyl, the methylene that is replaced by 5 atoms or 6 atom heterocycles; R2 is phenyl or benzyl, 5 atoms or 6 atom heteroaromatics, the methylene replaced by 5 atoms or 6 atom heterocycles; R5 is CH (R3)-COOR4 groups, wherein R3 is hydrogen, OH or OR bases, saturated hydrocarbyl, phenyl or benzyl and OR4 is hydrophilic ester, or R5 is the heteroatomic 5- or 6-membered heterocycle that nitrogen, sulphur and oxygen are selected from comprising several, and two nitrogen-atoms are included at least, wherein the heterocycle is replaced by the alkyl, phenyl or benzyl of C1-C6. Also disclose the purposes of the compounds of this invention of medicament forms, pharmaceutical composition comprising the compound and pharmaceutically acceptable excipient reinstates the analgesia of the new compound of what enhancing formula (I) and the purposes of antidepressant effect at least one of cannabinoid derivatives type and/or morphine or derivatives thereof one.本發明涉及式(I)的新型化合物:H2N-CH(R1)-CH2-S-S-CH2-CH(R2)-CONH-R5,其中:R1是烴鏈、苯基或苄基、被5原子或6原子雜環取代的亞甲基;R2是苯基或苄基、5原子或6原子芳雜環、被5原子或6原子雜環取代的亞甲基;R5是CH(R3)-COOR4基團,其中R3是氫、OH或OR基、飽和烴基、苯基或苄基並且OR4是親水的酯,或者R5是包含若干個選自氮、硫和氧的雜原子的5元或6元雜環,並且至少包含兩個氮原子,其中所述雜環被C1-C6的烷基、苯基或苄基取代。還公開了藥物形式的本發明化合物的用途,包含所述化合物和藥學可接受的賦形劑的藥物組合物,與大麻素衍生物中的至少一種類型和/或嗎啡或其衍生物一起用於增強式(I)的新型化合物的鎮痛和抗抑鬱作用的用途。
来源网站:
中国工程科技知识中心
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