发明名称 7-Pyrollyl 9-Aminoacyl Tetracycline Compounds and Methods of Use Thereof
摘要 A compound of formula (I): wherein: A represents an aromatic 5 membered heterocycle, optionally containing, in addition to the nitrogen atom indicated in formula (I), one to three additional nitrogen atoms and optionally substituted by one or more groups "R" selected from halogen, -NRaRb, C1-6 alkyl, C2-6 alkenyl, C3-6 alkynyl, aryl, heteroaryl, hydroxy, -OC1-6 alkyl, formyl, cyano, trifluoromethyl, -CHNORa, -CO2Ra, -CONRaRb, -NRaC(O)Ra, -NRaC(O)ORa, -OC(O)NRaRb, -OC(O)Ra, -OC(O)ORa, or a C1-6 alkyl group substituted by one or more groups selected from hydroxy, -NRaRb, -OC1-6 alkyl, -SRa, -CHNORa, -CO2Ra, -CONRaRb, -NRaC(O)Ra, -NRaC(O)ORa, -OC(O)NRaRb, -OC(O)Ra, -OC(O)ORa X represents -NRxRy or -OC1-6 alkyl optionally substituted by one or more groups selected from hydroxy, methoxy, halogen, amino and trifluoromethyl. Ra and Rb independently represent hydrogen or C1-6 alkyl (preferably methyl); R1 represents hydrogen, C1-6 alkyl or together R1 and R2 represent a CH2 moiety; R2 represents hydrogen, -OC1-6 alkyl, -O(O)C1-6 alkyl or hydroxy; R3 represents hydrogen, hydroxy or together R3 and R1 represent a CH2 moiety; R4 represents hydrogen, or C1-6 alkyl, optionally substituted by one or more groups selected from hydroxy, methoxy, halogen, amino and trifluoromethyl; Rx and Ry independently represent hydrogen, benzyl, C3-6cycloalkyl, C3-6alkenyl, C3-6alkynyl, C1-6 alkyl optionally substituted by one or more groups selected from hydroxy, methoxy, halogen, NRaRb and trifluoromethyl, -C1-6 alkylcycloalkyl, -C1-6 alkylheterocycle, C1-6 alkylamino and C1-6 alkylthio or together Rx and Ry form a heterocycle; and pharmaceutically acceptable derivatives and solvates thereof.
申请公布号 US2009054379(A1) 申请公布日期 2009.02.26
申请号 US20070949392 申请日期 2007.12.03
申请人 PARATEK PHARMACEUTICALS, INC. 发明人 HUSS SOPHIE;FIANDOR JOSE M.;FRECHETTE ROGER
分类号 A61K31/65;C07C50/36;C07D207/32;C07D207/333;C07D207/34 主分类号 A61K31/65
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