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公开(公告)号：EP2301534A1
公开(公告)日：2011-03-30
申请号：EP10184858.8
申请日：2003-03-10
发明人： Nelson, Mark L. , Ohemeng, Kwasi , Frechette, Roger , Ismail, Mohamed Y. , Honeyman, Laura , Bowser, Todd , Abato, Paul , Amoo, Victor , Assefa, Haregewein , Berniac, Joel , Bhatia, Beena , Chen, Jackson , Kim, Oak , Mechiche, Rachid , Reddy, Laxma N. , Verma, Atul K. , Viski, Peter , Warchol, Tadeusz , Yanachkov, Ivan
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
CPC分类号： C07D207/404 , C07C237/26 , C07C239/20 , C07C255/58 , C07C271/22 , C07C275/34 , C07C323/60 , C07C335/12 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2603/46 , C07D207/16 , C07D207/20 , C07D207/335 , C07D209/44 , C07D211/58 , C07D211/70 , C07D213/20 , C07D213/64 , C07D213/82 , C07D213/89 , C07D231/12 , C07D261/10 , C07D261/14 , C07D261/18 , C07D277/42 , C07D277/56 , C07D295/116 , C07D295/155 , C07D295/215 , C07D307/52 , C07D307/54 , C07D317/66 , C07D335/02
摘要： 1. A tetracycline compound having the following formula:
wherein:
J 5 and J 6 are each independently hydrogen, alkyl, alkenyl, alkynyl, aryl, sulfonyl, acyl, substituted carbonyl or substituted thiocarbonyl, or linked to form a ring;
J 7 and J 8 are each alkyl, halogen, or hydrogen; and
R 7 is hydrogen,
or pharmaceutically acceptable salts thereof.摘要翻译： 1.具有下式的四环素化合物：其中：J 5和J 6各自独立地为氢，烷基，烯基，炔基，芳基，磺酰基，酰基，取代的羰基或取代的硫代羰基，或连接形成环; J 7和J 8各自为烷基，卤素或氢; 和R 7是氢，或其药学上可接受的盐。
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公开(公告)号：EP2316450A1
公开(公告)日：2011-05-04
申请号：EP10184863.8
申请日：2003-03-10
发明人： Nelson, Mark L. , Ohemeng, Kwasi , Frechette, Roger , Ismail, Mohamed Y , Honeyman, Laura , Bowser, Todd , Abato, Paul , Amoo, Victor , Assefa, Haregewein , Berniac, Joel , Bhatia, Beena , Chen, Jackson , Kim, Oak , Mechiche, Rachid , Reddy, N. Laxma , Verma, Atul K. , Viski, Peter , Warchol, Tadeusz , Yanachkov, Ivan
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
CPC分类号： C07D207/404 , C07C237/26 , C07C239/20 , C07C255/58 , C07C271/22 , C07C275/34 , C07C323/60 , C07C335/12 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2603/46 , C07D207/16 , C07D207/20 , C07D207/335 , C07D209/44 , C07D211/58 , C07D211/70 , C07D213/20 , C07D213/64 , C07D213/82 , C07D213/89 , C07D231/12 , C07D261/10 , C07D261/14 , C07D261/18 , C07D277/42 , C07D277/56 , C07D295/116 , C07D295/155 , C07D295/215 , C07D307/52 , C07D307/54 , C07D317/66 , C07D335/02
摘要： A tetracycline compound having the following formula:
wherein:
J 5 and J 6 are each independently hydrogen, alkyl, alkenyl, alkynyl, aryl, sulfonyl, acyl, substituted carbonyl or substituted thiocarbonyl, or linked to form a ring;
J 7 and J 8 are each alkyl, halogen, or hydrogen;
R 7 dimethylamino; and
R 8 is hydrogen, hydroxyl, halogen, thiol, alkyl, alkenyl, alkynyl, aryl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, or an arylalkyl, or pharmaceutically acceptable salts thereof.摘要翻译： 具有下式的四环素化合物：其中：J 5和J 6各自独立地为氢，烷基，烯基，炔基，芳基，磺酰基，酰基，取代的羰基或取代的硫代羰基，或连接形成环; J 7和J 8各自为烷基，卤素或氢; R 7二甲基氨基; 其中R 8为氢，羟基，卤素，硫醇，烷基，烯基，炔基，芳基，烷氧基，烷硫基，烷基亚磺酰基，烷基磺酰基，烷基氨基或芳基烷基。
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公开(公告)号：EP2311451A1
公开(公告)日：2011-04-20
申请号：EP10184869.5
申请日：2003-03-10
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
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
CPC分类号： C07D207/404 , C07C237/26 , C07C239/20 , C07C255/58 , C07C271/22 , C07C275/34 , C07C323/60 , C07C335/12 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2603/46 , C07D207/16 , C07D207/20 , C07D207/335 , C07D209/44 , C07D211/58 , C07D211/70 , C07D213/20 , C07D213/64 , C07D213/82 , C07D213/89 , C07D231/12 , C07D261/10 , C07D261/14 , C07D261/18 , C07D277/42 , C07D277/56 , C07D295/116 , C07D295/155 , C07D295/215 , C07D307/52 , C07D307/54 , C07D317/66 , C07D335/02
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.摘要翻译： 式（II）的四环素化合物：其中：J 1是氢，取代或未取代的烷基，芳基，磺酰基，酰基或取代的羰基; J 2是氢，芳基，磺酰基或酰基; 或J 1和J 2连接形成环; 条件是J 1或J 2中的至少一个不是氢; J 3和J 4各自为烷基，卤素或氢; X是CHC（R 13 Y'Y），CR 6'R 6，C = CR 6 R 6，S，NR 6或O; R 2，R 4和R 4“各自独立地为氢，烷基，烯基，炔基，烷氧基，烷硫基，烷基亚磺酰基，烷基磺酰基，烷基氨基，芳基烷基，芳基，杂环或杂芳族; R 4为NR 4' 烯基，炔基，芳基，羟基，卤素或氢; R 2'，R 3，R 10 R 11和R 12各自为氢; 烷基，链烯基，炔基，烷氧基，烷硫基，烷基亚磺酰基，烷基磺酰基，烷基氨基，芳基烷基，烷基羰基氧基或芳基羰基氧基; R 6和R 6'各自独立地为氢，亚甲基，羟基，卤素，硫醇，烷基，烯基，炔基，芳基，烷氧基，烷硫基，烷基亚磺酰基，烷基磺酰基，烷基氨基或芳基烷基; R 9是氢; R 8为氢，羟基，卤素，硫醇，烷基，烯基，炔基，芳基，烷氧基，烷硫基，烷基亚磺酰基，烷基磺酰基，烷基氨基或芳基烷基; R 13是氢，羟基，烷基，烯基，炔基，烷氧基，烷硫基，烷基亚磺酰基，烷基磺酰基，烷基氨基或芳基烷基; 其中Y'和Y各自独立地为氢，卤素，羟基，氰基，巯基，氨基，烷基，烯基，炔基，烷氧基，烷硫基，烷基亚磺酰基，烷基磺酰基，烷基氨基或芳基烷基或其药学上可接受的盐或酯。
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