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1. 发明申请

WO2016065290A1 SEMI-SYNTHESIS PROCEDURES 审中-公开
标题翻译：半合成程序
公开(公告)号：WO2016065290A1
公开(公告)日：2016-04-28
申请号：PCT/US2015/057167
申请日：2015-10-23
申请人： TETRAPHASE PHARMACEUTICALS, INC.
发明人： ZHANG, Wu-Yan , LAFRANCE, Danny , RONN, Magnus, P.
IPC分类号： C07D207/06 , C07C231/12 , C07C245/20 , C07C237/26
CPC分类号： C07D295/15 , C07C231/12 , C07C237/26 , C07C245/20 , C07C2603/46 , C07D207/06
摘要： Provided herein are improved processes tor convening C7-amino-substituted tetracyclines to C7-fluoro-substituted tetracyclines, as well as intermediates produced by or used in these processes. In one embodiment, a thermal fluorination method is provided in which a suspension comprising a non-polar organic solvent and a C7-diazo-substituted tetracycline hexafluorophosphate, hexafluoarsenate or hexafluorosilicate salt, or a salt, solvate or combination thereof, is healed to provide a C7-fluoro-substituted tetracycline, or salt, solvate or combination thereof. In another embodiment, a photolytic fluorination is provided in which a solution comprising an ionic liquid and a C-7diazo-substituted tetracycline tetrafluoroborate, hexafluorophosphate, hexafluoroarsenate or hexafluorosilicate salt, or a salt, solvate or combination thereof, is irradiated to provide a C7-fluoro-substituted tetracycline, or salt, solvate or combination thereof.
摘要翻译：本文提供了将C7-氨基取代的四环素转化为C7-氟取代的四环素的改进方法，以及由这些方法制备或用于其中的中间体。在一个实施方案中，提供了一种热氟化方法，其中包含非极性有机溶剂和C7-重氮取代的四环素六氟磷酸盐，六氟代砷酸盐或六氟硅酸盐或其盐，溶剂合物或其组合的悬浮液被愈合以提供 C7-氟取代的四环素，或其盐，溶剂合物或其组合。在另一个实施方案中，提供光解氟化，其中照射包含离子液体和C-7重氮取代的四氟环四氟硼酸盐，六氟磷酸盐，六氟砷酸盐或六氟硅酸盐或其盐，溶剂合物或其组合的溶液，以提供C7- 氟取代的四环素或其盐，溶剂合物或其组合。

2. 发明申请

WO2011063977A1 REDUCTION OF ORGANIC COMPOUNDS WITH LOW AMOUNTS OF HYDROGEN 审中-公开
标题翻译：减少氢含量低的有机化合物
公开(公告)号：WO2011063977A1
公开(公告)日：2011-06-03
申请号：PCT/EP2010/007193
申请日：2010-11-26
申请人： SANDOZ AG , DECRISTOFORO, Martin
发明人： DECRISTOFORO, Martin
IPC分类号： C07B31/00
CPC分类号： C07B31/00 , C07C5/08 , C07C231/12 , C07C2521/18 , C07C2523/44 , C07C2603/46 , C07C15/50 , C07C237/48
摘要： The present invention relates to a process for the reaction of a compound with hydrogen wherein the reaction is conducted using a hydrogen-containing gas comprising up to about 10 vol.% hydrogen and at least about 90 vol.% of an inert gas and wherein the compound to be reacted with hydrogen is provided in a liquid phase. The process of the present invention is particularly suitable for hydrogenation and hydrogenolysis reactions.
摘要翻译：本发明涉及一种化合物与氢气反应的方法，其中该反应是使用包含至多约10体积％氢气和至少约90体积％惰性气体的含氢气体进行的，其中在液相中提供与氢反应的化合物。本发明的方法特别适用于氢化和氢解反应。

3. 发明申请

WO2011025982A2 TETRACYCLINE COMPOUNDS 审中-公开
标题翻译：四环素化合物
公开(公告)号：WO2011025982A2
公开(公告)日：2011-03-03
申请号：PCT/US2010/047035
申请日：2010-08-27
申请人： TETRAPHASE PHARMACEUTICALS, INC. , DENG, Yonghong , PLAMONDON, Louis , SUN, Cuixiang , XIAO, Xiao-Yi , ZHOU, Jingye , SUTCLIFFE, Joyce, A. , RONN, Magnus, P.
发明人： DENG, Yonghong , PLAMONDON, Louis , SUN, Cuixiang , XIAO, Xiao-Yi , ZHOU, Jingye , SUTCLIFFE, Joyce, A. , RONN, Magnus, P.
IPC分类号： C07C237/26
CPC分类号： C07C311/08 , C07C237/26 , C07C307/10 , C07C311/09 , C07C311/13 , C07C311/21 , C07C311/29 , C07C311/44 , C07C2101/02 , C07C2101/04 , C07C2101/08 , C07C2101/14 , C07C2103/40 , C07C2103/44 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/16 , C07C2603/40 , C07C2603/44 , C07C2603/46 , C07D205/04 , C07D207/12 , C07D207/16 , C07D209/44 , C07D209/52 , C07D211/54 , C07D211/60 , C07D213/70 , C07D213/74 , C07D213/82 , C07D223/06 , C07D231/18 , C07D233/60 , C07D233/84 , C07D295/15 , C07D307/64
摘要： The present invention is directed to a compound represented by Structural Formula (1): or a pharmaceutically acceptable salt thereof. The variables for Structural Formula (I) are defined herein. Also described is a pharmaceutical composition comprising the compound of Structural Formula (I) and its therapeutic use.
摘要翻译：本发明涉及由结构式（1）表示的化合物或其药学上可接受的盐。结构式（I）的变量在本文中定义。还描述了包含结构式（I）的化合物及其治疗用途的药物组合物。

4. 发明申请

WO2010129057A3 TETRACYCLINE COMPOUNDS 审中-公开
标题翻译：四环素化合物
公开(公告)号：WO2010129057A3
公开(公告)日：2011-01-06
申请号：PCT/US2010001350
申请日：2010-05-07
申请人： TETRAPHASE PHARMACEUTICALS INC , CHEN CHI-LI , CLARK ROGER B , DENG YONGHONG , HE MINSHENG , PLAMONDON LOUIS , SUN CUIXIANG , XIAO XIAO-YI
发明人： CHEN CHI-LI , CLARK ROGER B , DENG YONGHONG , HE MINSHENG , PLAMONDON LOUIS , SUN CUIXIANG , XIAO XIAO-YI
IPC分类号： C07C237/26 , C07C275/24 , C07C311/06 , C07C311/19 , C07D205/04 , C07D207/06 , C07D207/08 , C07D209/04 , C07D211/34 , C07D221/20 , C07D223/04 , C07D223/32 , C07D295/03
CPC分类号： C07D471/10 , C07C237/26 , C07C275/24 , C07C311/06 , C07C311/19 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2602/08 , C07C2602/24 , C07C2602/42 , C07C2602/50 , C07C2603/46 , C07C2603/74 , C07D205/04 , C07D207/06 , C07D207/08 , C07D207/09 , C07D207/10 , C07D207/14 , C07D207/16 , C07D209/04 , C07D209/14 , C07D209/44 , C07D209/52 , C07D211/14 , C07D211/34 , C07D213/74 , C07D221/20 , C07D223/04 , C07D223/14 , C07D223/32 , C07D261/20 , C07D295/13 , C07D295/135 , C07D295/15 , C07D295/155 , C07D295/185 , C07D295/26 , C07D307/22 , C07D401/04 , C07D413/06
摘要： The present invention is directed to a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. The variables for Structural Formula I are defined herein. Also described is a pharmaceutical composition comprising the compound of Structural Formula I and its therapeutic use.
摘要翻译：本发明涉及由结构式（I）表示的化合物：或其药学上可接受的盐。结构式I的变量在本文中定义。还描述了包含结构式I的化合物及其治疗用途的药物组合物。

5. 发明申请

WO2009052152A2 TIGECYCLINE AND METHODS OF PREPARING INTERMEDIATES 审中-公开
标题翻译： TIGECYCLINE和制备中间体的方法
公开(公告)号：WO2009052152A2
公开(公告)日：2009-04-23
申请号：PCT/US2008079950
申请日：2008-10-15
申请人： WYETH CORP , BERNATCHEZ MICHEL , CHEW WARREN , DAIGNEAULT SYLVAIN , PALUS ERNEST , MIRMEHRABI MAHMOUD , BOUCHARD LUC
发明人： BERNATCHEZ MICHEL , CHEW WARREN , DAIGNEAULT SYLVAIN , PALUS ERNEST , MIRMEHRABI MAHMOUD , BOUCHARD LUC
IPC分类号： C07C231/02 , C07C237/26
CPC分类号： C07C237/26 , C07C231/10 , C07C2603/46
摘要： Methods of preparing and purifying 9-nitrominocycline and 9-aminominocycline and salts thereof used in the process of making tigecycline, are disclosed. In one embodiment, the invention is directed to a method of preparing the compound of formula 1 or a pharmaceutically acceptable salt thereof, comprising: (a) reacting nitric acid with the compound of formula 2, or a salt thereof, to produce a reaction mixture comprising an intermediate; and (b) further reacting the intermediate to form the compound of formula 1, wherein the intermediate is isolated from the reaction mixture, the method further comprising sparging with an inert gas prior to step (a).
摘要翻译：披露了制备和提纯制备替加环素过程中使用的9-硝基米诺环素和9-氨基米诺环素及其盐的方法。在一个实施方案中，本发明涉及制备式1化合物或其药学上可接受的盐的方法，其包括：（a）使硝酸与式2化合物或其盐反应以产生反应混合物包含中间体; 和（b）使中间体进一步反应形成式1化合物，其中中间体从反应混合物中分离出来，该方法还包括在步骤（a）之前用惰性气体喷射。

6. 发明申请

WO2008137740A1 FULVENE AND FULVALENE ANALOGS AND THEIR USE IN TREATING CANCERS 审中-公开
标题翻译： FULVENE和FULVALENE模拟及其在治疗癌症中的应用
公开(公告)号：WO2008137740A1
公开(公告)日：2008-11-13
申请号：PCT/US2008/062497
申请日：2008-05-02
申请人： EMORY UNIVERSITY , ARBISER, Jack, L.
发明人： ARBISER, Jack, L.
IPC分类号： A61K31/045 , A61K31/403 , A61K31/4164 , A61P35/00
CPC分类号： C07D209/14 , A61K31/015 , A61K31/045 , A61K31/167 , A61K31/341 , A61K31/357 , A61K31/403 , A61K31/4164 , A61K31/444 , A61K31/5375 , A61K31/573 , C07C13/28 , C07C13/40 , C07C13/465 , C07C13/58 , C07C13/66 , C07C25/18 , C07C35/32 , C07C39/23 , C07C43/215 , C07C43/23 , C07C69/608 , C07C211/50 , C07C215/46 , C07C233/44 , C07C237/26 , C07C251/28 , C07C275/64 , C07C2601/10 , C07C2602/08 , C07C2602/42 , C07C2603/24 , C07C2603/40 , C07C2603/46 , C07D209/82 , C07D209/86 , C07D213/53 , C07D233/58 , C07D233/68 , C07D261/08 , C07D277/40 , C07D295/03 , C07D295/135 , C07D307/58 , C07D309/38 , C07D311/58 , C07D311/60 , C07D311/82 , C07D407/04 , C07D471/10 , C07D473/34
摘要： Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are fulvene and/or fulvalene analogs. The compounds and compositions can be used to treat and/or prevent a wide variety of cancers, including drug resistant cancers, as well as numerous inflammatory, degenerative and vascular diseases, including various ocular diseases. Representative fulvene and/or fulvalene analogs include fulvene and fulvalene analogues of various dyes, hormones, sugars, peptides, oligonucleotides, amino acids, nucleotides, nucleosides, and polyols. The compounds are believed to function, at least, by inhibiting Nox or ROS. In some embodiments, the Nox is one that is selectively expressed in cancer cells over normal cells, or one that is expressed in higher amounts in cancer cells over normal cells. Thus, the compounds are novel therapeutic agents for a variety of cancers and other diseases.
摘要翻译：公开了化合物，包括该化合物的药物组合物，及其制备和使用方法。化合物是富烯和/或富瓦烯类似物。化合物和组合物可用于治疗和/或预防多种癌症，包括耐药性癌症，以及许多炎性，退行性和血管性疾病，包括各种眼部疾病。代表性的富烯和/或富瓦烯类似物包括各种染料，激素，糖，肽，寡核苷酸，氨基酸，核苷酸，核苷和多元醇的富烯和富瓦烯类似物。据信这些化合物至少通过抑制Nox或ROS起作用。在一些实施方案中，Nox是在癌细胞中在正常细胞上选择性表达的，或在癌细胞中以比正常细胞更高量表达的那些。因此，这些化合物是用于各种癌症和其它疾病的新型治疗剂。

7. 发明申请

WO2008079363A2 SUBSTITUTED TETRACYCLINE COMPOUNDS FOR TREATMENT OF INFLAMMATORY SKIN DISORDERS 审中-公开
标题翻译：用于治疗炎性皮肤病的替代四环素化合物
公开(公告)号：WO2008079363A2
公开(公告)日：2008-07-03
申请号：PCT/US2007026220
申请日：2007-12-21
申请人： PARATEK PHARM INNC , OAK K KIM , ASSEFA HAREGEWEIN , BHATIA BEENA , DRAPER MICHAEL , HONEYMAN LAURA , MOLNAR DENNIS P
发明人： ASSEFA HAREGEWEIN , BHATIA BEENA , DRAPER MICHAEL , HONEYMAN LAURA , MOLNAR DENNIS P
IPC分类号： A61K31/65 , A61P17/00 , A61P17/06 , A61P17/10 , A61P43/00
CPC分类号： C07C237/48 , A61K31/65 , C07C237/26 , C07C2103/46 , C07C2603/46
摘要： Methods and compositions for the treatment of skin disorders (e.g., acne, rosacea) are described.
摘要翻译：描述了用于治疗皮肤病症（例如痤疮，红斑痤疮）的方法和组合物。

8. 发明申请

WO2007117639A9 SYNTHESIS OF TETRACYCLINES AND ANALOGUES THEREOF 审中-公开
标题翻译：四环素及其类似物的合成
公开(公告)号：WO2007117639A9
公开(公告)日：2008-04-17
申请号：PCT/US2007008647
申请日：2007-04-06
申请人： HARVARD COLLEGE , MYERS ANDREW G , BRUBAKER JASON D , SUN CUIXIANG , WANG QIU
发明人： MYERS ANDREW G , BRUBAKER JASON D , SUN CUIXIANG , WANG QIU
IPC分类号： A61K31/65
CPC分类号： C07C237/26 , C07C323/61 , C07C2601/02 , C07C2601/08 , C07C2603/46 , C07C2603/52 , C07D205/04 , C07D213/56 , C07D277/30 , C07D277/66 , C07D295/155
摘要： The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The modular synthesis of tetracyclines and tetracycline analogs described provides an efficient and enantioselective route to a variety of tetracycline analogs and polycyclines previously inaccessible via earlier tetracycline syntheses and semi-synthetic methods. These analogs may be used as anti- microbial agents or anti-pro liferative agents in the treatment of diseases of humans or other animals.
摘要翻译：四环素类抗生素在过去50年的传染病治疗中发挥了重要作用。然而，四环素在人类和兽医药物中的使用量的增加已经导致了以前易受四环素抗生素影响的许多生物体之间的抵抗。所述四环素和四环素类似物的模块合成为通过先前的四环素合成和半合成方法先前无法接近的各种四环素类似物和聚环状体提供了有效和对映选择性的途径。这些类似物可以用作抗微生物剂或抗增生剂来治疗人类或其他动物的疾病。

9. 发明申请

WO2007117639A2 SYNTHESIS OF TETRACYCLINES AND ANALOGUES THEREOF 审中-公开
标题翻译：四环素及其类似物的合成
公开(公告)号：WO2007117639A2
公开(公告)日：2007-10-18
申请号：PCT/US2007/008647
申请日：2007-04-06
申请人： THE PRESIDENT AND FELLOWS OF HARVARD COLLEGE , MYERS, Andrew, G. , BRUBAKER, Jason, D. , SUN, Cuixiang , WANG, Qiu
发明人： MYERS, Andrew, G. , BRUBAKER, Jason, D. , SUN, Cuixiang , WANG, Qiu
IPC分类号： A61K31/65
CPC分类号： C07C237/26 , C07C323/61 , C07C2601/02 , C07C2601/08 , C07C2603/46 , C07C2603/52 , C07D205/04 , C07D213/56 , C07D277/30 , C07D277/66 , C07D295/155
摘要： The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The modular synthesis of tetracyclines and tetracycline analogs described provides an efficient and enantioselective route to a variety of tetracycline analogs and polycyclines previously inaccessible via earlier tetracycline syntheses and semi-synthetic methods. These analogs may be used as anti- microbial agents or anti-pro liferative agents in the treatment of diseases of humans or other animals.
摘要翻译：四环素类抗生素在过去50年的传染病治疗中发挥了重要作用。然而，四环素在人类和兽医药物中的使用量的增加已经导致了以前易受四环素抗生素影响的许多生物体之间的抵抗。所述四环素和四环素类似物的模块合成为通过先前的四环素合成和半合成方法先前无法接近的各种四环素类似物和聚环状体提供了有效和对映选择性的途径。这些类似物可以用作抗微生物剂或抗增生剂来治疗人类或其他动物的疾病。

10. 发明申请

WO2006047756A3 SUBSTITUTED TETRACYCLINE COMPOUNDS 审中-公开
公开(公告)号：WO2006047756A3
公开(公告)日：2006-07-20
申请号：PCT/US2005039014
申请日：2005-10-25
申请人： PARATEK PHARM INNC , ABATO PAUL , ASSEFA HAREGEWEIN , BERNIAC JOEL , BHATIA BEENA , BOWSER TODD , CHEN JACKSON , GRIER MARK , HONEYMAN LAURA , ISMAIL MOHAMED Y , NELSON MARK , KWASI OHEMENG , PAN JINGWEN
发明人： ABATO PAUL , ASSEFA HAREGEWEIN , BERNIAC JOEL , BHATIA BEENA , BOWSER TODD , CHEN JACKSON , GRIER MARK , HONEYMAN LAURA , ISMAIL MOHAMED Y , NELSON MARK , KWASI OHEMENG , PAN JINGWEN
IPC分类号： C07C237/26 , A61K31/65 , A61P25/28 , A61P31/04 , A61P31/12 , A61P33/06 , C07D295/155 , C07D307/54 , C07D405/06
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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