发明公开
- 专利标题： Amino-methyl substituted tetracycline compounds
- 专利标题（中）： 氨基甲基取代物四环素 - 维生素
-
申请号： EP10184869.5申请日： 2003-03-10
-
公开(公告)号： EP2311451A1公开(公告)日： 2011-04-20
- 发明人: Nelson, Mark L. , Ohemeng, Kwasi , Frechette, Roger , Ismail, Mohamed Y , Honeyman, Laura , Bowser, Todd , Abato, Paul , Amoo, Victor , Assefa, Haregewein , Bhatia, Beena , Berniac, Joel , Chen, Jackson , Kim, Oak , Mechiche, Rachid , Reddy, Laxma N. , Verma, Atul K. , Viski, Peter , Warchol, Tadeusz , Yanachkov, Ivan
- 申请人： Paratek Pharmaceuticals, Inc.
- 申请人地址： 75 Kneeland Street Boston, MA 02111 US
- 专利权人： Paratek Pharmaceuticals, Inc.
- 当前专利权人： Paratek Pharmaceuticals, Inc.
- 当前专利权人地址： 75 Kneeland Street Boston, MA 02111 US
- 代理机构： Nash, David Allan
- 优先权： US362654P 20020308; US395495P 20020712
- 主分类号： A61K31/40
- IPC分类号： A61K31/40 ; A61K31/41 ; A61K31/42 ; A61K31/44 ; A61K31/415 ; A61K31/445 ; A61K31/65 ; C07C235/66 ; C07D207/00 ; C07D207/30 ; C07D311/06 ; A61P31/04
摘要：
A tetracycline compound of the formula (II):
wherein:
J 1 is hydrogen, substituted or unsubstituted alkyl, aryl, sulfonyl, acyl or substituted carbonyl; J 2 is hydrogen, aryl, sulfonyl or acyl; or J 1 and J 2 are linked to form a ring; provided that at least one of J 1 or J 2 is not hydrogen; J 3 and J 4 are each alkyl, halogen or hydrogen; X is CHC(R 13 Y'Y), CR 6 'R 6 , C=CR 6 R 6 , S, NR 6 or O; R 2 , R 4 and R 4" are each independently hydrogen, alkyl, alkenyl, alkynyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, arylalkyl, aryl, heterocyclic or heteroaromatic; R 4 is NR 4 'R 4 ", alkyl, alkenyl, alkynyl, aryl, hydroxyl, halogen or hydrogen; R 2' , R 3 , R 10 R 11 and R 12 are each hydrogen; R 5 is hydroxyl, hydrogen, thiol, alkanoyl, aroyl, alkaroyl, aryl, heteroaromatic, alkyl, alkenyl, alkynyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, arylalkyl, alkyl carbonyloxy or aryl carbonyloxy; R 6 and R 6 ' are each independently hydrogen, methylene, hydroxyl, halogen, thiol, alkyl, alkenyl, alkynyl, aryl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino or arylalkyl; R 9 is hydrogen; R 8 is hydrogen, hydroxyl, halogen, thiol, alkyl, alkenyl, alkynyl, aryl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino or arylalkyl; R 13 is hydrogen, hydroxyl, alkyl, alkenyl, alkynyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino or arylalkyl; and Y' and Y are each independently hydrogen, halogen, hydroxyl, cyano, sulfhydryl, amino, alkyl, alkenyl, alkynyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino or arylalkyl, or pharmaceutically acceptable salts or esters thereof.
wherein:
J 1 is hydrogen, substituted or unsubstituted alkyl, aryl, sulfonyl, acyl or substituted carbonyl; J 2 is hydrogen, aryl, sulfonyl or acyl; or J 1 and J 2 are linked to form a ring; provided that at least one of J 1 or J 2 is not hydrogen; J 3 and J 4 are each alkyl, halogen or hydrogen; X is CHC(R 13 Y'Y), CR 6 'R 6 , C=CR 6 R 6 , S, NR 6 or O; R 2 , R 4 and R 4" are each independently hydrogen, alkyl, alkenyl, alkynyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, arylalkyl, aryl, heterocyclic or heteroaromatic; R 4 is NR 4 'R 4 ", alkyl, alkenyl, alkynyl, aryl, hydroxyl, halogen or hydrogen; R 2' , R 3 , R 10 R 11 and R 12 are each hydrogen; R 5 is hydroxyl, hydrogen, thiol, alkanoyl, aroyl, alkaroyl, aryl, heteroaromatic, alkyl, alkenyl, alkynyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, arylalkyl, alkyl carbonyloxy or aryl carbonyloxy; R 6 and R 6 ' are each independently hydrogen, methylene, hydroxyl, halogen, thiol, alkyl, alkenyl, alkynyl, aryl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino or arylalkyl; R 9 is hydrogen; R 8 is hydrogen, hydroxyl, halogen, thiol, alkyl, alkenyl, alkynyl, aryl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino or arylalkyl; R 13 is hydrogen, hydroxyl, alkyl, alkenyl, alkynyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino or arylalkyl; and Y' and Y are each independently hydrogen, halogen, hydroxyl, cyano, sulfhydryl, amino, alkyl, alkenyl, alkynyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino or arylalkyl, or pharmaceutically acceptable salts or esters thereof.
信息查询
