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1. 发明公开

EP2949644A3 SUBSTITUTED TETRACYCLINE COMPOUNDS 审中-公开
标题翻译：取代的四环素化合物
公开(公告)号：EP2949644A3
公开(公告)日：2016-04-20
申请号：EP15165987.7
申请日：2005-10-25
申请人： Paratek Pharmaceuticals, Inc.
发明人： Abato, Paul , Assefa, Haregewein , Berniac, Joel , Bowser, Todd , Bhatia, Beena , Chen, Jackson , Grier, Mark , Honeyman, Laura , Ismail, Mohammed, Y. , Nelson, Mark , Kwasi, Ohemeng , Pan, Jingwen
IPC分类号： C07C237/26 , C07D211/34 , C07D295/155 , A61K31/65 , A61P31/04 , A61P31/12 , A61P33/00
CPC分类号： C07D471/04 , C07C237/26 , C07C251/48 , C07C255/59 , C07C259/10 , C07C271/18 , C07C271/22 , C07C271/24 , C07C2601/02 , C07C2603/46 , C07D207/335 , C07D207/337 , C07D211/70 , C07D213/30 , C07D213/38 , C07D213/61 , C07D213/73 , C07D213/74 , C07D213/84 , C07D231/12 , C07D233/64 , C07D239/26 , C07D239/42 , C07D241/12 , C07D261/08 , C07D263/32 , C07D277/28 , C07D277/30 , C07D295/096 , C07D295/155 , C07D295/192 , C07D307/46 , C07D307/52 , C07D307/54 , C07D309/14 , C07D333/20 , C07D333/24 , C07D333/38 , C07D403/06 , C07D405/06 , C07D405/12 , C07D413/12 , C07D487/04
摘要： The present invention pertains, at least in part, to novel substituted tetracycline compounds. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for tetracycline compounds such as blocking tetracycline efflux and modulation of gene expression.

2. 发明公开

EP2287150A3 Substituted tetracycline compounds 审中-公开
公开(公告)号：EP2287150A3
公开(公告)日：2011-10-19
申请号：EP10184202.9
申请日：2005-10-25
申请人： Paratek Pharmaceuticals, Inc.
发明人： Abato, Paul , Assefa, Haregewein , Berniac, Joel , Bowser, Todd , Bhatia, Beena , Chen, Jackson , Grier, Mark , Honeyman, Laura , Ismail, Mohamed, Y. , Nelson, Mark , Kwasi, Ohemeng , Pan, Jongwen
IPC分类号： C07C271/22 , A61K31/65 , A61P31/04 , A61P31/12 , A61P33/00
CPC分类号： C07D471/04 , C07C237/26 , C07C251/48 , C07C255/59 , C07C259/10 , C07C271/18 , C07C271/22 , C07C271/24 , C07C2601/02 , C07C2603/46 , C07D207/335 , C07D207/337 , C07D211/70 , C07D213/30 , C07D213/38 , C07D213/61 , C07D213/73 , C07D213/74 , C07D213/84 , C07D231/12 , C07D233/64 , C07D239/26 , C07D239/42 , C07D241/12 , C07D261/08 , C07D263/32 , C07D277/28 , C07D277/30 , C07D295/096 , C07D295/155 , C07D295/192 , C07D307/46 , C07D307/52 , C07D307/54 , C07D309/14 , C07D333/20 , C07D333/24 , C07D333/38 , C07D403/06 , C07D405/06 , C07D405/12 , C07D413/12 , C07D487/04
摘要： The present invention pertains, at least in part, to novel substituted tetracycline compounds. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for tetracycline compounds such as blocking tetracycline efflux and modulation of gene expression.

3. 发明授权

EP2204361B1 13-substituted methacycline compounds 有权
标题翻译： 13-SUBSTITUIERTE METHACYCLINVERBINDUNGEN
公开(公告)号：EP2204361B1
公开(公告)日：2011-09-28
申请号：EP10160000.5
申请日：2001-06-29
申请人： TRUSTEES OF TUFTS COLLEGE , Paratek Pharmaceuticals, Inc.
发明人： Nelson, Mark L. , Mcintyre, Laura , Rennie, Glen , Bhatia, Beena
IPC分类号： C07C237/26 , A61K31/65 , C07C231/12 , A61P31/04
CPC分类号： C07C237/26 , C07C2603/46

4. 发明公开

EP2284151A3 Substituted tetracycline compounds 审中-公开
公开(公告)号：EP2284151A3
公开(公告)日：2011-09-21
申请号：EP10182871.3
申请日：2005-10-25
申请人： Paratek Pharmaceuticals, Inc.
发明人： Abato, Paul , Assefa, Haregewein , Berniac, Joel , Bowser, Todd , Bhatia, Beena , Chen, Jackson , Grier, Mark , Honeyman, Laura , Ismail, Mohamed, Y. , Nelson, Mark , Kwasi, Ohemeng , Pan, Jingwen
IPC分类号： C07C237/26 , C07C237/48 , C07C255/02 , C07D213/38 , C07D207/335 , C07D307/52 , C07D309/14 , A61K31/65 , A61P31/04 , A61P31/12 , A61P33/00
CPC分类号： C07D471/04 , C07C237/26 , C07C251/48 , C07C255/59 , C07C259/10 , C07C271/18 , C07C271/22 , C07C271/24 , C07C2601/02 , C07C2603/46 , C07D207/335 , C07D207/337 , C07D211/70 , C07D213/30 , C07D213/38 , C07D213/61 , C07D213/73 , C07D213/74 , C07D213/84 , C07D231/12 , C07D233/64 , C07D239/26 , C07D239/42 , C07D241/12 , C07D261/08 , C07D263/32 , C07D277/28 , C07D277/30 , C07D295/096 , C07D295/155 , C07D295/192 , C07D307/46 , C07D307/52 , C07D307/54 , C07D309/14 , C07D333/20 , C07D333/24 , C07D333/38 , C07D403/06 , C07D405/06 , C07D405/12 , C07D413/12 , C07D487/04
摘要： The present invention pertains, at least in part, to novel substituted tetracycline compounds. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for tetracycline compounds such as blocking tetracycline efflux and modulation of gene expression.

5. 发明公开

EP2269985A3 Substituted tetracycline compounds 审中-公开
公开(公告)号：EP2269985A3
公开(公告)日：2011-09-21
申请号：EP10182880.4
申请日：2005-10-25
申请人： Paratek Pharmaceuticals, Inc.
发明人： Abato, Paul , Assefa, Haregewein , Berniac, Joel , Bowser, Todd , Bhatia, Beena , Chen, Jackson , Grier, Mark , Honeyman, Laura , Ismail, Mohamed, Y. , Nelson, Mark , Kwasi, Ohemeng , Pan, Jingwen
IPC分类号： C07D207/337 , C07D307/54 , C07D405/12 , C07D413/12 , A61K31/65 , A61P31/12 , A61P31/04 , A61P33/00
CPC分类号： C07D471/04 , C07C237/26 , C07C251/48 , C07C255/59 , C07C259/10 , C07C271/18 , C07C271/22 , C07C271/24 , C07C2601/02 , C07C2603/46 , C07D207/335 , C07D207/337 , C07D211/70 , C07D213/30 , C07D213/38 , C07D213/61 , C07D213/73 , C07D213/74 , C07D213/84 , C07D231/12 , C07D233/64 , C07D239/26 , C07D239/42 , C07D241/12 , C07D261/08 , C07D263/32 , C07D277/28 , C07D277/30 , C07D295/096 , C07D295/155 , C07D295/192 , C07D307/46 , C07D307/52 , C07D307/54 , C07D309/14 , C07D333/20 , C07D333/24 , C07D333/38 , C07D403/06 , C07D405/06 , C07D405/12 , C07D413/12 , C07D487/04
摘要： The present invention pertains, at least in part, to novel substituted tetracycline compounds. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for tetracycline compounds such as blocking tetracycline efflux and modulation of gene expression.

6. 发明公开

EP2319829A1 9-substituted tetracycline compounds 审中-公开
标题翻译： 9-subsituierte四环素 - Verbindungen
公开(公告)号：EP2319829A1
公开(公告)日：2011-05-11
申请号：EP10184736.6
申请日：2004-06-25
申请人： Paratek Pharmaceuticals, Inc.
发明人： Nelson, Mark, L. , Amoo, Victor , Kim, Oak, K. , Abato, Paul , Ohemeng, Kwasi , Assefa, Haregwein , Berniac, Joel , Bhatia, Beena , Bowser, Todd , Chen, Jackson , Grier, Mark , Honeyman, Laura , Ismail, Mohamed, Y. , Mechiche, Rachid , Mathews, Jude
IPC分类号： C07C237/26 , A61K31/65
CPC分类号： C07C237/48 , A61K31/65 , C07C237/26 , C07C271/22 , C07C271/54 , C07C275/28 , C07C275/30 , C07C2601/02 , C07C2601/14 , C07C2601/16 , C07C2603/46
摘要： 1. A compound of formula II:

wherein:
X is CR 6' R 6 ;
R 3 is hydrogen;
R 2 , R 2' , R 5 , R 6 , R 6' , R 8 , R 10 , R 11 , and R 12 are each hydrogen;
R 4' , R 4" , R 7' and R 7" are each lower alkyl;
R 4 is NR 4 'R 4" ;
R 7 is NR 7' R 7" or hydrogen;
R 9 is -CH 2 NR 9a R 9b or linked with R 10 to form a furanyl ring;
R 9a is alkyl, alkenyl or arylalkyl; and
R 9b is hydrogen or alkyl;

or wherein R 9a and R 9b are linked to form a pyrrolidinyl, piperazinyl, piperidinyl, pyrazinyl, azapanyl, thiomorpholinyl, morpholinyl, tetrahydroquinolinyl, or decahydroquinolinyl ring;
or a pharmaceutically acceptable salt, ester or prodrug thereof.
摘要翻译： 1.式II的化合物：其中：X是CR 6'R 6; R 3是氢; R 2，R 2'，R 5，R 6，R 6'，R 8，R 10，R 11和R 12各自为氢; R 4'，R 4“，R 7'和R 7”各自为低级烷基; R 4是NR 4'R 4“; R 7是NR 7'R 7”或氢; R 9是-CH 2 NR 9a R 9b或与R 10连接以形成呋喃基环; R 9a是烷基，烯基或芳基烷基; R 9b为氢或烷基; 或其中R 9a和R 9b连接形成吡咯烷基，哌嗪基，哌啶基，吡嗪基，氮杂基，硫代吗啉基，吗啉基，四氢喹啉基或十氢喹啉基环; 或其药学上可接受的盐，酯或前药。

7. 发明公开

EP2298322A3 Substituted tetracycline compounds 审中-公开
标题翻译：被取代的四环素化合物
公开(公告)号：EP2298322A3
公开(公告)日：2011-05-11
申请号：EP10184642.6
申请日：2004-06-25
申请人： Paratek Pharmaceuticals, Inc.
发明人： Nelson, Mark, L. , Amoo, Victor , Kim, Oak, K. , Abato, Paul , Ohemeng, Kwasi , Assefa, Haregwein , Berniac, Joel , Bhatia, Beena , Bowser, Todd , Chen, Jackson , Grier, Mark , Honeyman, Laura , Ismail, Mohamed, Y. , Mechiche, Rachid , Mathews, Jude
IPC分类号： C07C237/26 , A61K31/65
CPC分类号： C07C237/48 , A61K31/65 , C07C237/26 , C07C271/22 , C07C271/54 , C07C275/28 , C07C275/30 , C07C2601/02 , C07C2601/14 , C07C2601/16 , C07C2603/46
摘要： A compound of formula III:

wherein:
X is CHC(R 13 Y'Y), CR 6' R 6 , C=CR 6' R 6 , S, NR 6 , or O;
R 2 , R 2' , R 4' , and R 4" are each independently hydrogen, alkyl, alkenyl, alkynyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, arylalkyl, aryl, heterocyclic, heteroaromatic or a prodrug moiety;
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 or a pro-drug moiety;
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, absent, hydroxyl, halogen, thiol, alkyl, alkenyl, alkynyl, aryl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, or an arylalkyl;
R 7 is substituted or unsubstituted pyrazolyl, furanyl, thiophenyl, thiazolyl, aminoalkyl substituted phenyl;
R 8 is hydrogen, hydroxyl, halogen, thiol, alkyl, alkenyl, alkynyl, aryl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, or an arylalkyl;
R 9 is hydrogen;
R 13 is hydrogen, hydroxy, alkyl, alkenyl, alkynyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, or an arylalkyl; and
Y' and Y are each independently hydrogen, halogen, hydroxyl, cyano, sulfhydryl, amino, alkyl, alkenyl, alkynyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, or an arylalkyl, or a pharmaceutically acceptable salt thereof.
摘要翻译：式III的化合物：其中：X是CHC（R 13 Y'Y），CR 6'R 6，C = CR 6'R 6，S，NR 6或O; 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，杂环基，杂芳基或前药部分; R4为NR4'R4“ ，烷基，烯基，炔基，芳基，羟基，卤素或氢; R2'，R3，R10，R11和R12各自为氢或前药部分; 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，烷基羰氧基或芳基羰氧基; R 5为羟基，氢，硫醇，烷酰基，芳酰基， R6和R6'各自独立地为氢，亚甲基，不存在，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; R7是取代或未取代的吡唑基，呋喃基，噻吩基，噻唑基，氨基烷基取代的苯基; R8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; R9是氢; R13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; 和Y'和Y各自独立地为氢，卤素，羟基，氰基，巯基，氨基，烷基，链烯基，炔基，烷氧基，烷硫基，烷基亚磺酰基，烷基磺酰基，烷基氨基或芳基烷基，或其药学上可接受的盐。

8. 发明公开

EP2311451A1 Amino-methyl substituted tetracycline compounds 审中-公开
标题翻译：氨基甲基取代物四环素 - 维生素
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
申请人： Paratek Pharmaceuticals, Inc.
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。

9. 发明公开

EP2298323A2 Substituted tetracycline compounds 审中-公开
标题翻译：取代四环素 - 维生素
公开(公告)号：EP2298323A2
公开(公告)日：2011-03-23
申请号：EP10184671.5
申请日：2004-06-25
申请人： Paratek Pharmaceuticals, Inc.
发明人： Nelson, Mark, L. , Amoo, Victor , Kim, Oak, K. , Abato, Paul , Ohemeng, Kwasi , Assefa, Haregwein , Berniac, Joel , Bhatia, Beena , Bowser, Todd , Chen, Jackson , Grier, Mark , Honeyman, Laura , Ismail, Mohamed, Y. , Mechiche, Rachid , Mathews, Jude
IPC分类号： A61K31/65 , C07C237/26 , C07D213/56 , C07D317/60 , C07D279/10 , C07D307/77 , C07D233/64 , A61P31/00 , A61P33/00
CPC分类号： C07C237/48 , A61K31/65 , C07C237/26 , C07C271/22 , C07C271/54 , C07C275/28 , C07C275/30 , C07C2601/02 , C07C2601/14 , C07C2601/16 , C07C2603/46
摘要： A compound of formula II:

wherein:
X is CHC(R 13 Y'Y), CR 6' R 6 , S, NR 6 , or O;
R 2 , R 4' , R 4" , R 7' and R 7" are each hydrogen, alkyl, alkenyl, alkynyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, arylalkyl, aryl, heterocyclic, heteroaromatic or a prodrug moiety;
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 or a pro-drug moiety;
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 independently hydrogen, methylene, absent, hydroxyl, halogen, thiol, alkyl, alkenyl, alkynyl, aryl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, or an arylalkyl;
R 7 is NR 7' R 7" , alkyl, alkenyl, alkynyl, aryl, hydroxyl, halogen, or hydrogen;
R 8 is hydrogen, hydroxyl, halogen, thiol, alkyl, alkenyl, alkynyl, aryl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, or an arylalkyl;
R 9 is -CH 2 NR 9a R 9b or linked with R 10 to form a furanyl ring;
R 9a is hydrogen, alkyl, alkenyl, alkynyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, arylalkyl, aryl, heterocyclic,or heteroaromatic;
R 9b is hydrogen or alkyl;
R 8 is hydrogen, hydroxyl, halogen, thiol, alkyl, alkenyl, alkynyl, aryl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, or an arylalkyl;
R 13 is hydrogen, hydroxy, alkyl, alkenyl, alkynyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, or an arylalkyl;
Y' and Y are each independently hydrogen, halogen, hydroxyl, cyano, sulfhydryl, amino, alkyl, alkenyl, alkynyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, or an arylalkyl, or a pharmaceutically acceptable salt, ester or prodrug thereof.
摘要翻译：式II化合物：其中：X为CHC（R 13 Y'Y），CR 6'R 6，S，NR 6或O; R 2，R 4'，R 4“，R 7'和R 7”各自为氢，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，杂芳族或前药部分; R 4是NR 4'R 4“，烷基，烯基，炔基，芳基，羟基，卤素或氢; R 2'，R 3，R 10，R 11和R 12各自是氢或前药部分; 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' 烷基，链烯基，炔基，芳基，烷氧基，烷硫基，烷基亚磺酰基，烷基磺酰基，烷基氨基或芳烷基; R 7为NR 7'R 7“，烷基，烯基，炔基，芳基，羟基，卤素或氢; 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 9是-CH 2 NR 9a R 9b或与R 10连接以形成呋喃基环; R 9a是氢，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，芳烷基，芳基，杂环或杂芳族; R 9b是氢或烷基; 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; 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，烷基氨基或芳烷基，或其药学上可接受的盐，酯或前药。

10. 发明公开

EP2287150A2 Substituted tetracycline compounds 审中-公开
公开(公告)号：EP2287150A2
公开(公告)日：2011-02-23
申请号：EP10184202.9
申请日：2005-10-25
申请人： Paratek Pharmaceuticals, Inc.
发明人： Abato, Paul , Assefa, Haregewein , Berniac, Joel , Bowser, Todd , Bhatia, Beena , Chen, Jackson , Grier, Mark , Honeyman, Laura , Ismail, Mohamed, Y. , Nelson, Mark , Kwasi, Ohemeng , Pan, Jongwen
IPC分类号： C07C271/22 , A61K31/65 , A61P31/04 , A61P31/12 , A61P33/00
CPC分类号： C07D471/04 , C07C237/26 , C07C251/48 , C07C255/59 , C07C259/10 , C07C271/18 , C07C271/22 , C07C271/24 , C07C2601/02 , C07C2603/46 , C07D207/335 , C07D207/337 , C07D211/70 , C07D213/30 , C07D213/38 , C07D213/61 , C07D213/73 , C07D213/74 , C07D213/84 , C07D231/12 , C07D233/64 , C07D239/26 , C07D239/42 , C07D241/12 , C07D261/08 , C07D263/32 , C07D277/28 , C07D277/30 , C07D295/096 , C07D295/155 , C07D295/192 , C07D307/46 , C07D307/52 , C07D307/54 , C07D309/14 , C07D333/20 , C07D333/24 , C07D333/38 , C07D403/06 , C07D405/06 , C07D405/12 , C07D413/12 , C07D487/04
摘要： The present invention pertains, at least in part, to novel substituted tetracycline compounds. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for tetracycline compounds such as blocking tetracycline efflux and modulation of gene expression.

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