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1. 发明公开

EP2292590A3 Prodrugs of 9-aminomethyl tetracycline compounds 审中-公开
标题翻译：的9-氨甲基四环素化合物的前体药物
公开(公告)号：EP2292590A3
公开(公告)日：2012-05-02
申请号：EP10181641.1
申请日：2004-06-25
申请人： Paratek Pharmaceuticals, Inc.
发明人： Kwasi, Ohemeng , Amoo, Victor , Kim, Oak, K. , Bowser, Todd , Assefa, Haregewein , Bhatia, Beena , Berniac, Joel , Chen, Jackson , Grier, Mark , Honeyman, Laura , Pan, Jingwen , Mechiche, Rachid
IPC分类号： C07C237/26 , C07C271/22 , A61K31/65 , A61P31/04
CPC分类号： C07D211/18 , C07C237/26 , C07C271/22 , C07C271/54 , C07C275/28 , C07C275/30 , C07C2601/14 , C07C2603/46
摘要： A compound of the formula (II):

wherein Q' is a prodrug moiety or a pharmaceutically acceptable salt thereof.

2. 发明公开

EP2345637A3 3, 10, and 12a substituted tetracycline compounds 审中-公开
标题翻译： 3，10和12取代的四环素化合物
公开(公告)号：EP2345637A3
公开(公告)日：2012-02-15
申请号：EP11161936.7
申请日：2003-07-14
申请人： Paratek Pharmaceuticals, Inc.
发明人： Nelson, Mark L. , Ismail, Mohamed Y. , Chen, Jackson , Bandarage, Upul
IPC分类号： C07C237/26 , A61K31/65
CPC分类号： C07C237/26 , A61K31/65 , C07D265/12 , C07D317/54 , Y02A50/411
摘要： The present invention pertains to novel 3, 10 and/or 12a-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 minocycline and tetracycline compounds in general, such as blocking tetracycline efflux and modulation of gene expression. Methods of preparing the novel 3, 10 and/or 12a-substituted tetracycline compounds are also disclosed.

3. 发明公开

EP2295404A3 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：EP2295404A3
公开(公告)日：2011-05-11
申请号：EP10184570.9
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 , A61P11/00 , A61P19/00 , A61P29/00 , A61P31/00 , A61P33/00 , A61P35/00 , C07D213/38 , C07D307/52 , C07D239/26 , C07D233/61 , C07D211/18
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 I:

wherein:
X is CHC(R 13 Y'Y), 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, 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 ethyl, perhalogenated alkenyl, substituted pyridinyl, pyrazinyl, furanyl, or pyrazolyl;
R 8 is hydrogen, hydroxyl, halogen, thiol, alkyl, alkenyl, alkynyl, aryl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, or an arylalkyl;
R 9 -CH 2 NR 9a R 9b ;
R 9a and R 9b are each independently hydrogen, alkyl, alkenyl or linked to form a heterocycle;
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I化合物：其中：X是CHC（R 13 Y'Y），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，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是乙基，全卤代链烯基，取代的吡啶基，吡嗪基，呋喃基或吡唑基; 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-CH2NR9aR9b; R9a和R9b各自独立地为氢，烷基，烯基或连接形成杂环; 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。

4. 发明公开

EP2295419A2 Substituted tetracycline compounds 审中-公开
公开(公告)号：EP2295419A2
公开(公告)日：2011-03-16
申请号：EP10182872.1
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： C07D295/185 , C07D211/14 , A61P31/04 , A61P31/12 , A61P33/00 , A61K31/65
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

EP2295404A2 Substituted tetracycline compounds 审中-公开
公开(公告)号：EP2295404A2
公开(公告)日：2011-03-16
申请号：EP10184570.9
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 , A61P11/00 , A61P19/00 , A61P29/00 , A61P31/00 , A61P33/00 , A61P35/00 , C07D213/38 , C07D307/52 , C07D239/26 , C07D233/61 , C07D211/18
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 I:

wherein:
X is CHC(R 13 Y'Y), 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, 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 ethyl, perhalogenated alkenyl, substituted pyridinyl, pyrazinyl, furanyl, or pyrazolyl;
R 8 is hydrogen, hydroxyl, halogen, thiol, alkyl, alkenyl, alkynyl, aryl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, or an arylalkyl;
R 9 -CH 2 NR 9a R 9b ;
R 9a and R 9b are each independently hydrogen, alkyl, alkenyl or linked to form a heterocycle;
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.

6. 发明公开

EP2284150A2 Substituted tetracycline compounds 审中-公开
公开(公告)号：EP2284150A2
公开(公告)日：2011-02-16
申请号：EP10182869.7
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, Mohamed, 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.

7. 发明公开

EP2949644A2 SUBSTITUTED TETRACYCLINE COMPOUNDS 审中-公开
标题翻译： SUBSTITUIERTE TETRACYCLIN-VERBINDUNGEN
公开(公告)号：EP2949644A2
公开(公告)日：2015-12-02
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.
摘要翻译：本发明至少部分地涉及新的取代的四环素化合物。这些四环素化合物可用于治疗许多四环素化合物反应状态，例如细菌感染和肿瘤，以及四环素化合物的其它已知应用，例如阻断四环素外排和调节基因表达。

8. 发明公开

EP2284152A3 Substituted tetracycline compounds 审中-公开
公开(公告)号：EP2284152A3
公开(公告)日：2011-10-05
申请号：EP10182876.2
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 , C07D207/10 , C07D213/73 , C07D239/34 , C07D235/00 , C07D241/12 , 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.

9. 发明公开

EP2295419A3 Substituted tetracycline compounds 审中-公开
公开(公告)号：EP2295419A3
公开(公告)日：2011-09-21
申请号：EP10182872.1
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： C07D295/185 , C07D211/14 , A61P31/04 , A61P31/12 , A61P33/00 , A61K31/65
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.

10. 发明公开

EP2287140A3 Substituted tetracycline compounds 审中-公开
公开(公告)号：EP2287140A3
公开(公告)日：2011-09-21
申请号：EP10184262.3
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： C07B59/00 , C07C237/26 , 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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