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תולדות של טטראהידרוקרבאזול בעלות פעילות ביולוגית משופרת ומסיסות משופרת המשמשות כליגנדים עבור קולטנים מצומדים לחלבוני g
专利权人:
AETERNA ZENTARIS GMBH
发明人:
申请号:
IL17906706
公开号:
IL179067A
申请日:
2006.11.06
申请国别(地区):
IL
年份:
2013
代理人:
摘要:
Tetrahydrocarbazole compounds (I) and their salts, derivatives or analogues; or their racemates, pure enantiomers and/or diastereomers, tautomers, solvates and hydrates, or polymorphic forms are new, where the salts are obtained by neutralizing the bases with inorganic or organic acids or by neutralizing the acids with inorganic or organic bases. Tetrahydrocarbazole compounds of formula (I) and their salts, derivatives or analogues; or their racemates, pure enantiomers and/or diastereomers, tautomers, solvates and hydrates, or polymorphic forms are new, where the salts are obtained by neutralizing the bases with inorganic or organic acids or by neutralizing the acids with inorganic or organic bases. X1 : S or O; X2, X3 : O or geminally linked H 2; R1, R2 : H (preferred), aryl, alkyl or arylalkyl radicals (optionally substituted in the alkyl and/or aryl group by up to 3 substituents of -hal, -CN or -O-alkyl); R3 : alkyl, arylalkyl or heteroarylalkyl radical (optionally substituted by up to 3 substituents -hal, -CN, -CO-O-R12, -CO-NR12R12a, -OH, -O-R13, -O-CO-R13, -O-SO 2, -OR12, -O-SO 2-R12, -SO 2, -SO-R12, -SO-R12, -O-PO(OR12)(OR12a), -O-PO(NR12R12a) 2, -O-CO-O-R13, -O-CO-NR12R12a, -O-CS-NR12R12a, -S-R12, -NR12R12a, -NH-CO-R13, -NH-SO 2-R12, -NH-CO-O-R13, -NH-CO-NHR12 or -NH-C(NH)-NH 2); R4-R7 : H, -Hal, -CN, -CONH 2, -COOH, -CF 3, -O-alkyl, -OCF 3, -NO 2, alkyl, arylalkyl or heteroarylalkyl radicals; R9 : H, alkyl, aryl, heteroaryl, arylalkyl or heteroarylalkyl radical; R10 : H or -R11, -CO-R11, -CO-OR11, -CO-NHR11, -C(NH)-NHR11, -SO 2-R11 or -SO 2-NHR11; R11 : alkyl, aryl, heteroaryl, arylalkyl or heteroarylalkyl radical (optionally substituted by one or more -hal, -CN, -alkyl, -CF 3, -OCF 3, -OH, -O-alkyl or -O-(CH 2CH 2-O) n-CH 3); R8 : 1-6C alkyl-aryl or 1-6C-alkyl-heteroaryl (where the aryl or heteroaryl group is substituted by 1-3 substituents of -O-(CH 2CH 2O) n-CH 3, -O-CO-R 12, -O-CO-(CH 2CH 2-O) n-CH 3, -O-SO 2-OR12, -O-SO 2-R12, -O-PO(OR12)(OR12a), -O-PO
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