4-aminotétracyclines et procédés d'utilisation associés

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专利权人:

Paratek Pharmaceuticals; Inc.

发明人:

申请号：

EP10183114.7

公开号：

EP2301912A3

申请日:

2005.10.25

申请国别(地区):

EP

年份:

2012

代理人:

摘要：

A compound of formula II:wherein:R2'and R2" are each independently hydrogen, alkyl, alkenyl, alkynyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, arylalkyl, aryl, heterocyclic, heteroaromatic or a prodrug moiety；R10, R11 and R12 are each independently hydrogen, alkyl, aryl, benzyl, arylalkyl, or a pro-drug moiety；R3' is hydroxyl, hydrogen, or a pro-drug moiety；R4 is NR4cR4d；R4c and R4d are each independently hydrogen, sulfonyl, arylcarbonyl, arylaminocarbonyl, aryloxycarbonyl, alkylcarbonyl, alkylaminocarbonyl, alkyloxycarbonyl, acyl, alkyl, alkenyl, alkynyl, or aryl；R5 and R5' are each independently hydroxyl, hydrogen, thiol, alkanoyl, aroyl, alkaroyl, aryl, heteroaromatic, alkyl, alkenyl, alkynyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, arylalkyl, alkyl carbonyloxy, or aryl carbonyloxy；R6 and R6' are each independently hydrogen, methylene, absent, hydroxyl, halogen, thiol, alkyl, alkenyl, alkynyl, aryl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, or an arylalkyl；R7 is hydrogen, hydroxyl, halogen, thiol, nitro, alkyl, alkenyl, alkynyl, aryl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, arylalkyl, amino, arylalkenyl, arylalkynyl, acyl, aminoalkyl, heterocyclic, thionitroso, or-(CH2)0-3(NR7c)0-1CC(=W')WR7a；R8 is hydrogen, hydroxyl, halogen, thiol, nitro, alkyl, alkenyl, alkynyl, aryl, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, amino, arylalkenyl, arylalkynyl, alkoxy, acyl, aminoalkyl, heterocyclic, thionitroso, or-(CH2)0-3(NR8c)0-1C(=E')ER8a；R9 is hydrogen, hydroxyl, halogen, thiol, nitro, alkyl, alkenyl, alkynyl, aryl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, arylalkyl, amino, arylalkenyl, arylalkynyl, acyl, aminoalkyl, heterocyclic, thionitroso, or-(CH2)0-3(NR9c)0-1C(=Z')ZR9a；R7a, R7b, R7c, R7d, R7e, R7f, R8a, R8b, R8c, R8d, R8e, R8f, R9a, R9b, R9c, R9d, R9e, and R9f are each independently hydrogen, acyl, alkyl, alkenyl, alkynyl, alkoxy, alkylthio, alkylsulfinyl,

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