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1. 发明申请

WO2012074960A2 FTY720-DERIVED ANTICANCER AGENTS 审中-公开
标题翻译： FTY720衍生的抗癌剂
公开(公告)号：WO2012074960A2
公开(公告)日：2012-06-07
申请号：PCT/US2011/062304
申请日：2011-11-29
申请人： THE OHIO STATE UNIVERSITY RESEARCH FOUNDATION , CHEN, Ching-Shih , KULP, Samuel, K. , WANG, Dasheng , BYRD, John, C. , MUTHUSAMY, Natarajan
发明人： CHEN, Ching-Shih , KULP, Samuel, K. , WANG, Dasheng , BYRD, John, C. , MUTHUSAMY, Natarajan
IPC分类号： C07C217/30 , C07C215/30 , A61K31/138 , A61P35/00
CPC分类号： C07C217/74 , C07C217/64 , C07C2601/02
摘要： A number of FTY720-derived compounds with antitumor activity are described. These compounds include the compounds of formula (I) wherein R 1 is independently selected from the group consisting of hydrogen, methyl, methoxy, and hydroxyl; R 2 is independently selected from the group consisting of hydrogen, methoxy, and hydroxyl; R 3 is independently selected from the group consisting of alkyl and cyclo-alkyl; and n is independently selected from 0 to 6. The compounds have lower immunosuppressive side effects as a result of not being phosphorylated by sphingosine kinase 2.
摘要翻译：描述了许多具有抗肿瘤活性的FTY720衍生的化合物。这些化合物包括其中R 1独立地选自氢，甲基，甲氧基和羟基的式（I）化合物; R 2 2独立地选自氢，甲氧基和羟基; R 3独立地选自由烷基和环烷基组成的组; 并且n独立地选自0至6.所述化合物由于未被鞘氨醇激酶2磷酸化而具有较低的免疫抑制副作用。

2. 发明申请

WO2013148994A1 GLUCOSE TRANSPORTER INHIBITORS 审中-公开
标题翻译：葡萄糖输送机抑制剂
公开(公告)号：WO2013148994A1
公开(公告)日：2013-10-03
申请号：PCT/US2013/034338
申请日：2013-03-28
申请人： THE OHIO STATE UNIVERSITY RESEARCH FOUNDATION , CHEN, Ching-Shih , WANG, Dasheng , KULP, Samuel, K.
发明人： CHEN, Ching-Shih , WANG, Dasheng , KULP, Samuel, K.
IPC分类号： A61K31/425 , A01N43/78 , C07D277/00
CPC分类号： C07D277/34
摘要： Thiazolidinedione compounds and pharmaceutically acceptable salts thereof are described. The compounds can be used in methods of treating cancer in a subject by administering to the subject a therapeutically effective amount of the compound. The compounds can also be used in methods of inhibiting glucose uptake in a cell by contacting the cell with the compound.
摘要翻译：描述了噻唑烷二酮化合物及其药学上可接受的盐。该化合物可用于通过向受试者施用治疗有效量的化合物来治疗受试者的癌症的方法。化合物也可以用于通过使细胞与化合物接触来抑制细胞中葡萄糖摄取的方法。

3. 发明申请

WO2010120711A1 PROTEIN PHOSPHATASE 2A-ACTIVATING AGENTS 审中-公开
标题翻译：蛋白磷酸酶2A激活剂
公开(公告)号：WO2010120711A1
公开(公告)日：2010-10-21
申请号：PCT/US2010/030799
申请日：2010-04-13
申请人： THE OHIO STATE UNIVERSITY RESEARCH FOUNDATION , CHEN, Ching-Shih , WANG, Dasheng , KULP, Samuel, K.
发明人： CHEN, Ching-Shih , WANG, Dasheng , KULP, Samuel, K.
IPC分类号： C07D311/00
CPC分类号： C07D311/72 , A61K31/353 , A61K31/355 , A61K31/662 , C07F9/65522
摘要： Tocopheryl succinate derivatives according to formula (I) are described. These compounds increase the activity of protein phosphatase 2A, can be included in pharmaceutical compositions, and can be used for the treatment of androgen receptor-dependent cancers such as prostate cancer.
摘要翻译：描述了式（I）的生育酚琥珀酸酯衍生物。这些化合物增加蛋白磷酸酶2A的活性，可以包括在药物组合物中，并且可以用于治疗依赖于雄激素受体的癌症如前列腺癌。

4. 发明申请

WO2008144263A1 POTENT INDOLE-3-CARBINOL-DERIVED ANTITUMOR AGENTS 审中-公开
标题翻译： POTENT INDOLE-3-CARBINOL衍生的抗菌剂
公开(公告)号：WO2008144263A1
公开(公告)日：2008-11-27
申请号：PCT/US2008/063323
申请日：2008-05-09
申请人： THE OHIO STATE UNIVERSITY RESEARCH FOUNDATION , CHEN, Ching-Shih , WANG, Dasheng , WENG, Jing-Ru
发明人： CHEN, Ching-Shih , WANG, Dasheng , WENG, Jing-Ru
IPC分类号： C07D209/12 , C07D209/14 , A61K31/404 , A61P35/00
CPC分类号： C07D209/12 , C07D209/14
摘要： Compounds and methods for treating cancer and inducing apoptosis in unwanted rapidly proliferating cells. The compounds are shown in formula (I): wherein X is hydroxyl or amino; Y is carboxyl or sulfonyl; R 1 , R 2 , R 3 , and R 4 can be the same or different and are selected from hydrogen, halogen, methoxy, trifluoromethyl, hydroxyl and combinations thereof; R 5 , R 6 , and R 7 may be the same or different and are selected from hydrogen, chloro, bromo, nitro, phenyl, amino, methoxy, and combinations thereof; and derivatives or metabolites thereof.
摘要翻译：用于治疗癌症并诱导不期望的快速增殖细胞凋亡的化合物和方法。化合物示于式（I）中：其中X是羟基或氨基; Y是羧基或磺酰基; R 1，R 2，R 3和R 4可以相同或不同，并且选自氢，卤素，甲氧基，三氟甲基，羟基及其组合; R5，R6和R7可以相同或不同，并且选自氢，氯，溴，硝基，苯基，氨基，甲氧基及其组合; 及其衍生物或代谢物。

5. 发明申请

WO2007098139A2 ANTICANCER AGENTS 审中-公开
标题翻译：反对者代理人
公开(公告)号：WO2007098139A2
公开(公告)日：2007-08-30
申请号：PCT/US2007/004337
申请日：2007-02-21
申请人： THE OHIO STATE UNIVERSITY RESEARCH FOUNDATION , CHEN, Ching-Shih , WANG, Dasheng
发明人： CHEN, Ching-Shih , WANG, Dasheng
IPC分类号： A61K31/353
CPC分类号： C07D311/72
摘要： Compounds of formula I (Formula I) : wherein X is selected from oxygen, nitrogen and sulfur; n is 0 or 1; R 1 is selected from alkyl, carboxylic acid, carboxylate, carboxamide, ester and combinations thereof; R 2 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（式I）：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。

6. 发明申请

WO2006002088A3 AMINO-QUINAZOLINE DERIVATIVES AS ANTITUMOR AGENTS 审中-公开
公开(公告)号：WO2006002088A3
公开(公告)日：2006-01-05
申请号：PCT/US2005/021541
申请日：2005-06-17
申请人： THE OHIO STATE UNIVERSITY RESEARCH FOUNDATION , CHEN, Ching-Shih , SHAW, Yeng-Jeng
发明人： CHEN, Ching-Shih , SHAW, Yeng-Jeng
IPC分类号： A61K31/445 , A61K31/517 , A01N43/54 , A01N43/40 , C07D239/72 , C07D239/95 , C07D401/00 , C07D403/00 , A61P35/00 , C07D211/32 , C07D263/02 , C07D277/04 , C07D285/06 , C07D285/08 , C07D285/12 , C07D307/02
摘要： Antitumor compounds based on the α1-adrenoceptor antagonist, doxazosin, as well as compositions and methods of use. The disclosed compounds induce apoptosis in cancer cells.

7. 发明申请

WO2012087889A2 DNA METHYLATION INHIBITORS 审中-公开
标题翻译： DNA甲基化抑制剂
公开(公告)号：WO2012087889A2
公开(公告)日：2012-06-28
申请号：PCT/US2011/065754
申请日：2011-12-19
申请人： THE OHIO STATE UNIVERSITY RESEARCH FOUNDATION , CHEN, Ching-Shih , SHAW, Arthur, Y. , LEU, Yu-Wei , HSIAO, Chu-Huei
发明人： CHEN, Ching-Shih , SHAW, Arthur, Y. , LEU, Yu-Wei , HSIAO, Chu-Huei
IPC分类号： C07D241/04 , C07D231/56 , C12N15/09 , A61K31/416 , A61P35/00
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。

8. 发明申请

WO2007143081A2 THERAPEUTIC AGENTS FOR THE TREATMENT OF LYMPHOID MALIGNANCIES 审中-公开
标题翻译：用于治疗淋巴细胞恶性肿瘤的治疗药物
公开(公告)号：WO2007143081A2
公开(公告)日：2007-12-13
申请号：PCT/US2007/012921
申请日：2007-06-01
申请人： THE OHIO STATE UNIVERSITY RESEARCH FOUNDATION , BYRD, John, C. , PERROTTI, Danilo , CHEN, Ching-Shih , DALTON, James, T. , FRISSORA, Frank , ZHAO, Xiaobin , LIU, Qing , MUTHUSAMY, Natarajan
发明人： BYRD, John, C. , PERROTTI, Danilo , CHEN, Ching-Shih , DALTON, James, T. , FRISSORA, Frank , ZHAO, Xiaobin , LIU, Qing , MUTHUSAMY, Natarajan
IPC分类号： A61K31/137
CPC分类号： A61K31/137 , A61K45/06
摘要： Methods- for treatment and prevention of lymphoid malignancies, including, but not limited to acute lymphoblastic leukemia (ALL), chronic lymphocytic leukemia (CLL), B-cell lymphoma, Acute Myeloid leukemia (AML), and mantle cell lymphoma (MCL). The methods include administration of a therapeutically effective amount of FTY720 (2-Amino-2-[2-(4- octylphenyl) ethyl] propane 1, 3-diol hydrochloride) or a derivative, pharmaceutically acceptable salt thereof, or a prodrug thereof to a subject.
摘要翻译：方法 - 用于治疗和预防淋巴恶性肿瘤，包括但不限于急性淋巴细胞性白血病（ALL），慢性淋巴细胞白血病（CLL），B细胞淋巴瘤，急性骨髓性白血病（AML）和套细胞淋巴瘤（MCL）。所述方法包括将治疗有效量的FTY720（2-氨基-2- [2-（4-辛基苯基）乙基]丙烷-1,3-二醇盐酸盐）或其衍生物，药学上可接受的盐或其前药给予课程。

9. 发明申请

WO2011044548A1 THIAZOLIDINEDIONE ENERGY RESTRICTION-MIMETIC AGENTS 审中-公开
标题翻译：噻唑烷酮能量限制 - 物理试剂
公开(公告)号：WO2011044548A1
公开(公告)日：2011-04-14
申请号：PCT/US2010/052151
申请日：2010-10-11
申请人： THE OHIO STATE UNIVERSITY RESEARCH FOUNDATION , CHEN, Ching-Shih , GUH, Jih-Hwa
发明人： CHEN, Ching-Shih , GUH, Jih-Hwa
IPC分类号： A01N43/40
CPC分类号： A61K31/425 , A61K31/353 , A61K31/426 , A61K31/4439
摘要： A method of inhibiting glycolysis in a subject by administering a pharmaceutical composition including a thiazolidinedione derivative to the subject is described. The thiazolidinedione derivatives are effective energy restriction mimetic agents, and can therefore be used to treat or prevent cancer in a subject, treat metabolic disorder, or increase the longevity of a subject. Various thiazolidinedione derivatives are also suitable for activating adenosine phosphate-activated protein kinase or inhibiting IL-6 expression.
摘要翻译：描述了通过向受试者施用包含噻唑烷二酮衍生物的药物组合物来抑制受试者中糖酵解的方法。噻唑烷二酮衍生物是有效的能量限制模拟剂，因此可用于治疗或预防受试者的癌症，治疗代谢紊乱或增加受试者的寿命。各种噻唑烷二酮衍生物也适用于激活磷酸腺苷激活蛋白激酶或抑制IL-6表达。

10. 发明申请

WO2011025805A1 ALKYL INDOLE-3-CARBINOL-DERIVED ANTITUMOR AGENTS 审中-公开
标题翻译：烷基吲哚-3-卡宾醇衍生的抗菌剂
公开(公告)号：WO2011025805A1
公开(公告)日：2011-03-03
申请号：PCT/US2010/046578
申请日：2010-08-25
申请人： THE OHIO STATE UNIVERSITY RESEARCH FOUNDATION , CHEN, Ching-Shih , WENG, Jing-Ru
发明人： CHEN, Ching-Shih , WENG, Jing-Ru
IPC分类号： A01N43/38
CPC分类号： A61K31/404 , C07D209/12
摘要： Compounds and methods for treating cancer or inducing apoptosis in proliferating cells. The compounds are shown in formula (I): formula (I) wherein X is selected from hydroxyl, thiol, and amino; Y is selected from carboxyl and sulfonyl; R 1 , R 2 , R 3 , and R 4 are selected from hydrogen, lower alkyl, and combinations thereof; R 5 , R 6 , and R 7 are selected from hydrogen, halo, nitro, amino, methoxy, and combinations thereof; and pharmaceutically acceptable salts thereof.
摘要翻译：在增殖细胞中治疗癌症或诱导凋亡的化合物和方法。化合物如式（I）所示：式（I）其中X选自羟基，硫醇和氨基; Y选自羧基和磺酰基; R1，R2，R3和R4选自氢，低级烷基及其组合; R5，R6和R7选自氢，卤素，硝基，氨基，甲氧基及其组合; 及其药学上可接受的盐。

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