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21. 发明授权

US08039502B2 Anti-infective agents against intracellular pathogens 有权
标题翻译：针对细胞内病原体的抗感染剂
公开(公告)号：US08039502B2
公开(公告)日：2011-10-18
申请号：US12179134
申请日：2008-07-24
申请人： Ching-Shih Chen , Hao-Chieh Chiu , Dasheng Wang , John S. Gunn , Larry S. Schlesinger
发明人： Ching-Shih Chen , Hao-Chieh Chiu , Dasheng Wang , John S. Gunn , Larry S. Schlesinger
IPC分类号： C07D231/12 , A61K31/415
CPC分类号： C07D231/12 , C07D403/04 , C07D403/10 , C07D405/04 , C07D417/04 , C07D417/10 , C07D417/12 , C07D417/14 , C12N2501/06
摘要： A new class of phosphoinositide-dependent kinase-1 (PDK-1) inhibitors of Formula I: wherein X wherein X is —CF3, Ar is selected from and R is selected from where R′ is L-Lys, D-Lys, β-Ala, L-Lue, L-Ile, Phe, SO2CH2CH2NH2, SO2NH2, Asn, Glu or Gyl, and R″ is methyl, ethyl, allyl, CH2CH2OH, CH2CN, CH2CH2CN, CH2CONH2,
摘要翻译：一类新的式I的磷酸肌醇依赖性激酶-1（PDK-1）抑制剂：其中X为X为-CF 3，Ar为选自R为选自其中R'为L-Lys，D-Lys，bgr ; -Ala，L-Lue，L-Ile，Phe，SO2CH2CH2NH2，SO2NH2，Asn，Glu或Gyl，R“为甲基，乙基，烯丙基，CH2CH2OH，CH2CN，CH2CH2CN，CH2CONH2，

22. 发明申请

US20090111799A1 ANTI-INFECTIVE AGENTS AGAINST INTRACELLULAR PATHOGENS 有权
标题翻译：抗细菌病毒的抗感染药物
公开(公告)号：US20090111799A1
公开(公告)日：2009-04-30
申请号：US12179134
申请日：2008-07-24
申请人： Ching-Shih Chen , Hao-Chieh Chiu , Dasheng Wang
发明人： Ching-Shih Chen , Hao-Chieh Chiu , Dasheng Wang
IPC分类号： A61K31/5415 , C07D231/10 , C12N5/00 , A61K31/415 , C07D257/04 , A61P35/00 , A61P31/00 , A61K31/41 , C07D403/02 , A61K31/496 , C07D279/18
CPC分类号： C07D231/12 , C07D403/04 , C07D403/10 , C07D405/04 , C07D417/04 , C07D417/10 , C07D417/12 , C07D417/14 , C12N2501/06
摘要： A new class of phosphoinositide-dependent kinase-1 (PDK-1) inhibitors of Formula I: wherein X wherein X is —CF3, Ar is selected from and R is selected from where R′ is L-Lys, D-Lys, β-Ala, L-Lue, L-Ile, Phe, SO2CH2CH2NH2, SO2NH2, Asn, Glu or Gyl, and R″ is methyl, ethyl, allyl, CH2CH2OH, CH2CN, CH2CH2CN, CH2CONH2,
摘要翻译：式I的新一类磷酸肌醇依赖性激酶-1（PDK-1）抑制剂：其中X为X为-CF 3，Ar为选自其中R为选自其中R'为L-Lys，D-Lys，β -Ala，L-Lue，L-Ile，Phe，SO2CH2CH2NH2，SO2NH2，Asn，Glu或Gyl，R“为甲基，乙基，烯丙基，CH2CH2OH，CH2CN，CH2CH2CN，CH2CONH2，

23. 发明申请

US20080009545A1 Anticancer agents 审中-公开
标题翻译：抗癌剂
公开(公告)号：US20080009545A1
公开(公告)日：2008-01-10
申请号：US11708792
申请日：2007-02-21
申请人： Ching-Shih Chen , Dasheng Wang
发明人： Ching-Shih Chen , Dasheng Wang
IPC分类号： A61K31/355 , A61K31/353 , A61P35/00 , C07D315/00
CPC分类号： C07D311/72
摘要： Compounds of formula I: wherein X is selected from oxygen, nitrogen and sulfur; n is 0 or 1; R1 is selected from alkyl, carboxylic acid, carboxylate, carboxamide, ester and combinations thereof; R2 is selected from alkyl, substituted alkyl, carboxylic acid, carboxylate, carboxamide, sulfonyl, sulfonamide and combinations thereof; and derivatives and metabolites thereof. Further provided are methods of using a compound of formula I to prevent and/or treat a subject having a condition characterized by unwanted cell proliferation. Also provided are pharmaceutical compounds comprising one or more compounds of formula I, or derivatives or pharmaceutically acceptable salts thereof.
摘要翻译：式I化合物：其中X选自氧，氮和硫; n为0或1; R 1选自烷基，羧酸，羧酸酯，羧酰胺，酯及其组合; R 2选自烷基，取代的烷基，羧酸，羧酸酯，羧酰胺，磺酰基，磺酰胺及其组合; 及其衍生物和代谢物。还提供了使用式I化合物预防和/或治疗具有不想要的细胞增殖特征的病症的受试者的方法。还提供了包含一种或多种式I化合物或其衍生物或药学上可接受的盐的药物化合物。

24. 发明申请

US20140364477A1 INDOLYL OR INDOLINYL HYDROXAMATE COMPOUNDS 有权
标题翻译：吲哚或吲哚啉酸羟化物化合物
公开(公告)号：US20140364477A1
公开(公告)日：2014-12-11
申请号：US14468408
申请日：2014-08-26
申请人： Ching-Shih Chen , Jing-Ping Liou , Hsing-Jin Liu , Kuo-Sheng Hung , Pei-Wen Shan , Wen-Ta Chiu , Che-Ming Teng
发明人： Ching-Shih Chen , Jing-Ping Liou , Hsing-Jin Liu , Kuo-Sheng Hung , Pei-Wen Shan , Wen-Ta Chiu , Che-Ming Teng
IPC分类号： C07D209/08 , C07D209/30 , C07D209/18
CPC分类号： C07D209/08 , C07D209/12 , C07D209/18 , C07D209/30 , C07D209/40
摘要： Indolyl or indolinyl compounds of formula (I): wherein bond, n, R1, R2, R3, R4, R5, and R6, are defined herein. Also disclosed is a method for treating cancer with these compounds.
摘要翻译：式（I）的吲哚基或二氢吲哚基化合物：其中键，n，R 1，R 2，R 3，R 4，R 5和R 6在本文中定义。还公开了用这些化合物治疗癌症的方法。

25. 发明授权

US08580827B2 Anti-Francisella agents 有权
标题翻译：抗狂犬病毒药物
公开(公告)号：US08580827B2
公开(公告)日：2013-11-12
申请号：US13610967
申请日：2012-09-12
申请人： Ching-Shih Chen , Hao-Chieh Chiu , Samuel Kulp , John S. Gunn , Larry S. Schlesinger
发明人： Ching-Shih Chen , Hao-Chieh Chiu , Samuel Kulp , John S. Gunn , Larry S. Schlesinger
IPC分类号： A61K31/41
CPC分类号： C07D231/12
摘要： A series of celecoxib derivatives defined by Formula I: were prepared and evaluated for their ability to inhibit the gram-negative bacteria Francisella tularensis. Pharmaceutical compositions including celecoxib derivatives and their use in methods for treating or preventing infection by Francisella tularensis in a subject are described.
摘要翻译：制备由式I定义的一系列塞来昔布衍生物，并评价其抑制革兰氏阴性细菌弗兰西斯拉氏弧菌的能力。描述了包括塞来昔布衍生物的药物组合物及其在治疗或预防受试者中的弗朗西斯氏菌感染的方法中的用途。

26. 发明授权

US08546397B2 DNA methylation inhibitors 有权
标题翻译： DNA甲基化抑制剂
公开(公告)号：US08546397B2
公开(公告)日：2013-10-01
申请号：US13329593
申请日：2011-12-19
申请人： Ching-Shih Chen , Arthur Y. Shaw , Yu-Wei Leu , Shu-Huei Hsiao
发明人： Ching-Shih Chen , Arthur Y. Shaw , Yu-Wei Leu , Shu-Huei Hsiao
IPC分类号： A61K31/497
CPC分类号： G01N33/57415 , A61K31/121 , A61K31/352 , A61K31/416 , A61K31/495 , G01N33/57419 , G01N33/57423 , G01N33/57434 , G01N2500/00
摘要： A number of DNA methylation inhibitors are described. The DNA methylation inhibitors were identified using a two-component enhanced green fluorescent protein reporter system to screen a compound library containing procainamide derivatives. The DNA methylation inhibitors can be used for cancer therapy and prevention.
摘要翻译：描述了许多DNA甲基化抑制剂。使用双组分增强的绿色荧光蛋白报道系统鉴定DNA甲基化抑制剂以筛选含有普鲁卡因酰胺衍生物的化合物文库。 DNA甲基化抑制剂可用于癌症治疗和预防。

27. 发明申请

US20120108823A1 ANTI-FRANCISELLA AGENTS 审中-公开
标题翻译：抗血清代谢物
公开(公告)号：US20120108823A1
公开(公告)日：2012-05-03
申请号：US12428035
申请日：2009-04-22
申请人： Ching-Shih Chen , Hao-Shieh Chiu , Samuel K. Kulp
发明人： Ching-Shih Chen , Hao-Shieh Chiu , Samuel K. Kulp
IPC分类号： C07D231/12 , A61P31/04 , A61K31/415
CPC分类号： C07D231/12
摘要： A series of celecoxib derivatives defined by Formula I: were prepared and evaluated for their ability to inhibit the gram-negative bacteria Francisella tularensis. Pharmaceutical compositions including celecoxib derivatives and their use in methods for treating or preventing infection by Francisella tularensis in a subject are described.
摘要翻译：制备由式I定义的一系列塞来昔布衍生物，并评价其抑制革兰氏阴性细菌弗兰西斯拉氏弧菌的能力。描述了包括塞来昔布衍生物的药物组合物及其在治疗或预防受试者中的弗朗西斯氏菌感染的方法中的用途。

28. 发明申请

US20110245315A1 INDOLYL OR INDOLINYL HYDROXAMATE COMPOUNDS 有权
标题翻译：吲哚或吲哚啉酸羟化物化合物
公开(公告)号：US20110245315A1
公开(公告)日：2011-10-06
申请号：US13074312
申请日：2011-03-29
申请人： Ching-Shih Chen , Jing-Ping Liou , Hsing-Jin Liu , Kuo-Sheng Hung , Pei-Wen Shan , Wen-Ta Chiu , Che-Ming Teng
发明人： Ching-Shih Chen , Jing-Ping Liou , Hsing-Jin Liu , Kuo-Sheng Hung , Pei-Wen Shan , Wen-Ta Chiu , Che-Ming Teng
IPC分类号： A61K31/4045 , C07D209/08 , A61P35/00
CPC分类号： C07D209/08 , C07D209/12 , C07D209/18 , C07D209/30 , C07D209/40
摘要： Indolyl or indolinyl compounds of formula (I): wherein bond, n, R1, R2, R3, R4, R5, and R6, are defined herein. Also disclosed is a method for treating cancer with these compounds.
摘要翻译：式（I）的吲哚基或二氢吲哚基化合物：其中键，n，R 1，R 2，R 3，R 4，R 5和R 6在本文中定义。还公开了用这些化合物治疗癌症的方法。

29. 发明申请

US20100168184A1 SMALL MOLECULE BCL-X1/BCL-2 BINDING INHIBITORS 失效
标题翻译：小分子BCL-X1 / BCL-2结合抑制剂
公开(公告)号：US20100168184A1
公开(公告)日：2010-07-01
申请号：US12652456
申请日：2010-01-05
申请人： Ching-Shih Chen , Chung-Wai Shiau
发明人： Ching-Shih Chen , Chung-Wai Shiau
IPC分类号： A61K31/352 , A61K31/427 , A61K31/4439 , A61K31/426 , A61P35/00
CPC分类号： C07D417/12 , C07D277/34 , C07D311/58 , C07D417/14
摘要： Bcl-xL/Bcl-2 binding inhibitors useful in the treatment of unwanted proliferating cells, including cancers and precancers, in subjects in need of such treatment. Also provided are methods of treating a subject having unwanted proliferating cells comprising administering a therapeutically effective amount of a Bcl-xL/Bcl-2 binding inhibitor described herein to a subject in need of such treatment. Also provided are methods of preventing the proliferation of unwanted proliferating cells, such as cancers and precancers, in a subject comprising the step of administering a therapeutically effective amount of a Bcl-xL/Bcl-2 binding inhibitor described herein to a subject at risk of developing a condition characterized by unwanted proliferating cells.
摘要翻译： Bcl-xL / Bcl-2结合抑制剂可用于治疗需要这种治疗的受试者中不需要的增殖细胞，包括癌症和预处理剂。还提供了治疗具有不想要的增殖细胞的受试者的方法，包括向需要这种治疗的受试者施用治疗有效量的本文所述的Bcl-xL / Bcl-2结合抑制剂。还提供了防止不想要的增殖细胞如癌症和预处理剂在受试者中增殖的方法，包括将治疗有效量的本文所述的Bcl-xL / Bcl-2结合抑制剂施用于患有风险的受试者的步骤发展以不想要的增殖细胞为特征的病症。

30. 发明申请

US20090170865A1 Treatment of Prostate Cancer with Angiogenesis-Targeting Quinazoline-Based Anti-Cancer Compounds 审中-公开
标题翻译：用血管发生靶向喹唑啉类抗癌化合物治疗前列腺癌
公开(公告)号：US20090170865A1
公开(公告)日：2009-07-02
申请号：US12323073
申请日：2008-11-25
申请人： Natasha Kyprianou , Jason B. Garrison , Ching-Shih Chen
发明人： Natasha Kyprianou , Jason B. Garrison , Ching-Shih Chen
IPC分类号： A61K31/517 , C12N5/06
CPC分类号： A61K31/517
摘要： Provided is a method of inhibiting the growth of prostate cancer cells comprising administering an effective amount of DZ-50 (2-[4-biphenyl-4-sulfonyl)-piperazin-1-yl]-6,7-diisopropoxyquinazolin-4-yl-amine) to a patient in need thereof. In another aspect, a method is provided for inhibiting the initiation of prostate cancer comprising administering an effective amount of DZ-50 to a patient in need thereof. In yet another aspect, a method is provided for inhibiting the formation of a prostate tumor-derived metastatic lesion comprising administering an effective amount of DZ-50 to a patient in need thereof. In any of the aforementioned methods, a quinazoline-based drug which induces apoptosis of a prostate cancer cell may be coadministered with DZ-50. Also provided is a composition comprising DZ-50, a quinazoline-based drug which induces apoptosis of a prostate cancer cell, and a pharmaceutically acceptable carrier.
摘要翻译：提供了抑制前列腺癌细胞生长的方法，其包括给予有效量的DZ-50（2- [4-联苯-4-磺酰基] - 哌嗪-1-基] -6,7-二异丙氧基喹唑啉-4-基 - 胺）给有需要的患者。另一方面，提供了一种抑制前列腺癌起始的方法，包括向有需要的患者施用有效量的DZ-50。在另一方面，提供了一种用于抑制前列腺肿瘤衍生的转移性病变的形成的方法，包括向有需要的患者施用有效量的DZ-50。在任何上述方法中，诱导前列腺癌细胞凋亡的基于喹唑啉的药物可以与DZ-50共同施用。还提供了包含诱导前列腺癌细胞凋亡的基于喹唑啉的药物DZ-50和药学上可接受的载体的组合物。

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