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1. 发明公开

EP2995610A1 4-DEDIMETHYLAMINO TETRACYCLINE COMPOUNDS 审中-公开
标题翻译： 4-去二甲氨基 - 四环素VERBINDUNGEN
公开(公告)号：EP2995610A1
公开(公告)日：2016-03-16
申请号：EP15176495.8
申请日：2003-01-06
申请人： Paratek Pharmaceuticals, Inc.
发明人： NELSON, Mark L. , OHEMENG, Kwasi
IPC分类号： C07C235/70 , C07C235/32 , C07D209/02 , C07D265/30 , C07D333/50 , C07D419/00 , A61K31/65 , A61P31/04
CPC分类号： A61K31/65 , C07C235/70 , C07C237/26 , C07C251/48 , C07C255/41 , C07C271/22 , C07C271/54 , C07C271/58 , C07C275/42 , C07C275/54 , C07C279/18 , C07C311/06 , C07C311/08 , C07C333/08 , C07C335/22 , C07C381/10 , C07C2601/08 , C07C2601/10 , C07C2601/16 , C07C2603/46 , C07D295/155 , C07D295/185 , C07D317/60 , C07F9/2475 , C07F9/4006
摘要： The present invention pertains, at least in part, to novel substituted 4-dedimethylamino 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.
摘要翻译：本发明至少部分地涉及新的取代的4-脱二甲基氨基四环素化合物。这些四环素化合物可用于治疗多种四环素化合物反应状态，例如细菌感染和肿瘤，以及其它已知的米诺环素和四环素化合物的一般应用，例如阻断四环素外排和调节基因表达。

2. 发明公开

EP1656341A1 PRODRUGS OF 9-AMINOMETHYL TETRACYCLINE COMPOUNDS 审中-公开
标题翻译： 9-氨基甲基四氮杂萘化合物的前体物
公开(公告)号：EP1656341A1
公开(公告)日：2006-05-17
申请号：EP04756044.6
申请日：2004-06-25
申请人： Paratek Pharmaceuticals, Inc.
发明人： OHEMENG, Kwasi , AMOO, Victor , KIM, Oak , BOWSER, Todd , ASSEFA, Haregewein , BHATIA, Beena , BERNIAC, Joel , CHEN, Jackson , GRIER, Mark , HONEYMAN, Laura , PAN, Jingwen , MECHICHE, Rachid
IPC分类号： C07C237/26 , A61K31/65
CPC分类号： C07D211/18 , C07C237/26 , C07C271/22 , C07C271/54 , C07C275/28 , C07C275/30 , C07C2601/14 , C07C2603/46
摘要： The invention pertains to prodrugs of 9-aminomethyl substituted tetracycline compounds, methods of using the compounds, and pharmaceutical compositions containing them.
摘要翻译：本发明涉及9-氨基甲基取代的四环素化合物的前体药物，使用该化合物的方法和含有它们的药物组合物。

3. 发明公开

EP1482926A2 AMINO-METHYL SUBSTITUTED TETRACYCLINE COMPOUNDS 审中-公开
标题翻译：氨甲基取代的四环素化合物
公开(公告)号：EP1482926A2
公开(公告)日：2004-12-08
申请号：EP03716416.7
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. , MCINTYRE, Laura , BOWSER, Todd
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 , C07D211/68 , C07D211/80 , C07D241/04
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： Aminomethyl substituted tetracycline compounds, pharmaceutical compositions, and methods of use thereof are discussed.

4. 发明公开

EP1474380A2 4-DEDIMETHYLAMINO TETRACYCLINE COMPOUNDS 审中-公开
标题翻译： 4-DESDIMETHYL AMINO TETRA CYCLIN VERBINDUNGEN
公开(公告)号：EP1474380A2
公开(公告)日：2004-11-10
申请号：EP03729351.1
申请日：2003-01-06
申请人： Paratek Pharmaceuticals, Inc.
发明人： NELSON, Mark, L. , OHEMENG, Kwasi
IPC分类号： C07C235/32 , C07D209/02 , C07D265/30 , C07D333/50 , C07D419/00 , A61K31/65
CPC分类号： A61K31/65 , C07C235/70 , C07C237/26 , C07C251/48 , C07C255/41 , C07C271/22 , C07C271/54 , C07C271/58 , C07C275/42 , C07C275/54 , C07C279/18 , C07C311/06 , C07C311/08 , C07C333/08 , C07C335/22 , C07C381/10 , C07C2601/08 , C07C2601/10 , C07C2601/16 , C07C2603/46 , C07D295/155 , C07D295/185 , C07D317/60 , C07F9/2475 , C07F9/4006
摘要： The present invention pertains, at least in part, to novel substituted 4-dedimethylamino 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.
摘要翻译：本发明至少部分地涉及新的取代的4-脱二甲基氨基四环素化合物。这些四环素化合物可用于治疗多种四环素化合物反应状态，例如细菌感染和肿瘤，以及其它已知的米诺环素和四环素化合物的一般应用，例如阻断四环素外排和调节基因表达。

5. 发明公开

EP1524974A2 TRANSCRIPTION FACTOR MODULATING COMPOUNDS AND METHODS OF USE THEREOF 审中-公开
标题翻译：转录因子控制调节及其使用的化合物和方法
公开(公告)号：EP1524974A2
公开(公告)日：2005-04-27
申请号：EP02807554.7
申请日：2002-05-06
申请人： Paratek Pharmaceuticals, Inc.
发明人： LEVY, Stuart, B. , ALEKSHUN, Micheal, N. , PODLOGAR, Brent , OHEMENG, Kwasi , VERMA, Atul , WARCHOL, Tadeusz , BHATIA, Beena
IPC分类号： A61K31/33 , A61K31/34 , A61K31/35 , A61K31/38 , A61K31/41 , A61K31/54 , A61K31/555
CPC分类号： A61K31/47 , A61K31/40 , A61K31/407 , A61K31/415 , A61K31/4745 , A61K31/505 , A61K31/555 , Y02A50/401 , Y02A50/47 , Y02A50/471 , Y02A50/475 , Y02A50/478 , Y02A50/481 , Y02A50/483 , Y02A50/52
摘要： Methods for identifying compound useful as anti-infectives that decrease resistance, virulence, or growth of microbes are provided. In one embodiment, the method comprises contacting a microbial cell comprising: 1) a selectable marker under the control of a transcription factor responsive element and 2) a transcription factor, with a compound under conditions which allow interaction of the compound with the microbial cell; and measuring the ability of the compound to affect the growth or survival of the microbial cell as an indication of whether the test compound modulates the activity of a transcription factor.

6. 发明公开

EP1503981A2 SUBSTITUTED TETRACYCLINE COMPOUNDS 审中-公开
标题翻译：取代的四环素
公开(公告)号：EP1503981A2
公开(公告)日：2005-02-09
申请号：EP03714236.1
申请日：2003-03-18
申请人： Paratek Pharmaceuticals, Inc.
发明人： NELSON, Mark, L. , OHEMENG, Kwasi , FRECHETTE, Roger , ABATO, Paul , ASSEFA, Haregewein , BANDARAGE, Upul , BERNIAC, Joel , BHATIA, Beena , CHEN, Jackson , ISMAIL, Mohamed, Y. , KIM, Oak, A. , MATHEWS, Jude , HONEYMAN, Laura , NIHLAWI, Mohammed , PEARSON, Andre , REDDY, Laxma , SHEAHAN, Paul , SIZENSKY, Emmanuelle , TOURIGNY, Justin , VISKI, Peter , WARCHOL, Tadeusz , AMOO, Victor , MECHICHE, Rachid , VERMA, Atul K.
IPC分类号： C07C237/26 , C07C43/00 , C07C49/00
CPC分类号： C07D307/52 , C07C237/26 , C07C239/18 , C07C251/08 , C07C251/48 , C07C255/25 , C07C255/43 , C07C255/58 , C07C255/59 , C07C271/28 , C07C271/44 , C07C275/34 , C07C279/18 , C07C281/14 , C07C309/61 , C07C311/19 , C07C311/21 , C07C317/48 , C07C323/32 , C07C323/60 , C07C2603/46 , C07D207/16 , C07D211/58 , C07D213/30 , C07D213/61 , C07D213/65 , C07D213/75 , C07D239/26 , C07D239/30 , C07D239/42 , C07D261/10 , C07D261/18 , C07D295/108 , C07D295/155 , C07D295/215 , C07D307/28 , C07D307/68 , C07D317/54 , C07D401/04
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 minocycline and tetracycline compounds in general, such as blocking tetracycline efflux and modulation of gene expression.

7. 发明授权

EP1648859B1 SUBSTITUTED TETRACYCLINE COMPOUNDS 有权
标题翻译：取代的四环素
公开(公告)号：EP1648859B1
公开(公告)日：2013-02-27
申请号：EP04756012.3
申请日：2004-06-25
申请人： Paratek Pharmaceuticals, Inc.
发明人： NELSON, Mark, L. , OHEMENG, Kwasi , AMOO, Victor , KIM, Oak , ABATO, Paul , ASSEFA, Haregewein , 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 , C07C271/22 , C07C271/54 , C07C275/28 , C07C275/30
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.

8. 发明公开

EP1648859A2 SUBSTITUTED TETRACYCLINE COMPOUNDS 有权
标题翻译： SUBSTITUIERTE TETRACYCLINVERBINDUNGEN
公开(公告)号：EP1648859A2
公开(公告)日：2006-04-26
申请号：EP04756012.3
申请日：2004-06-25
申请人： Paratek Pharmaceuticals, Inc.
发明人： NELSON, Mark, L. , OHEMENG, Kwasi , AMOO, Victor , KIM, Oak , ABATO, Paul , ASSEFA, Haregewein , 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 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的化合物：其中：X是CHC（R 13 Y'Y），CR 6'R 6，S，NR 6或O; R 2，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，杂芳族或前药部分; R 4 是NR 4'R 4“，烷基，烯基，炔基，羟基，卤素或氢; R 2'，R 3，R 10，R 11和R 12各自为氢或前药部分; 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 5是羟基，氢，硫醇，烷酰基，芳酰基， R 6和R 6'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，烷基氨基或芳烷基。 R 7是乙基，全卤代烯基，取代的吡啶基，吡嗪基，呋喃基或吡唑基; 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 9 -CH 2 NR 9a R 9b; R 9a和R 9b各自独立地为氢，烷基，烯基或连接形成杂环; 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。

9. 发明公开

EP1558341A2 TRANSCRIPTION FACTOR MODULATING COMPOUNDS AND METHODS OF USE THEREOF 审中-公开
标题翻译：转录因子MODULIERENDEVERBINDUNGEN及其用途
公开(公告)号：EP1558341A2
公开(公告)日：2005-08-03
申请号：EP03783155.9
申请日：2003-11-03
申请人： Paratek Pharmaceuticals, Inc.
发明人： LEVY, Stuart, B. , ALEKSHUN, Michael, N. , PODLOGAR, Brent, L. , OHEMENG, Kwasi , VERMA, Atul, K. , WARCHOL, Tadeusz , BHATIA, Beena , BOWSER, Todd , GRIER, Mark
IPC分类号： A61P31/00 , A61K31/55 , A61K31/495 , A61K31/50 , A61K31/535 , A61K31/44 , A61K31/41 , A61K31/425 , A61K31/415 , A61K31/42 , C07D235/00
CPC分类号： C07D235/06 , A61K31/41 , A61K31/415 , A61K31/42 , A61K31/425 , A61K31/44 , A61K31/495 , A61K31/50 , A61K31/535 , A61K31/55 , C07D235/08 , C07D235/12 , C07D235/14 , C07D235/18 , C07D267/16 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D413/04 , C07D487/04 , C07D491/04 , Y02A50/401 , Y02A50/47 , Y02A50/471 , Y02A50/473 , Y02A50/475 , Y02A50/478 , Y02A50/481 , Y02A50/483
摘要： Substituted benzoimidazole compounds useful as anti-infectives that decrease resistance, virulence, or growth of microbes are provided. Methods of making and using substituted benzoimidazole compounds, as well as pharmaceutical preparations thereof, in, e.g., reducing antibiotic resistance and inhibiting biofilms.

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