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公开(公告)号:US08680133B2
公开(公告)日:2014-03-25
申请号:US13429779
申请日:2012-03-26
Applicant: Ching-Shih Chen , Jing-Ru Weng
Inventor: Ching-Shih Chen , Jing-Ru Weng
IPC: A61K31/404 , C07D209/04
CPC classification number: A61K31/404 , C07D209/12
Abstract: Compounds and methods for treating cancer or inducing apoptosis in proliferating cells. The compounds are shown in formula I: wherein X is selected from hydroxyl, thiol, and amino; Y is selected from carboxyl and sulfonyl; R1, R2, R3, and R4 are selected from hydrogen, lower alkyl, and combinations thereof; R5, R6, and R7 are selected from hydrogen, halo, ni tro, amino, methoxy, and combinations thereof; and pharmaceutically acceptable salts thereof.
Abstract translation: 用于在增殖细胞中治疗癌症或诱导细胞凋亡的化合物和方法。 化合物示于式I中:其中X选自羟基,硫醇和氨基; Y选自羧基和磺酰基; R 1,R 2,R 3和R 4选自氢,低级烷基及其组合; R5,R6和R7选自氢,卤素,氨基,甲氧基及其组合; 及其药学上可接受的盐。
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公开(公告)号:US08658647B2
公开(公告)日:2014-02-25
申请号:US13300872
申请日:2011-11-21
Applicant: Ching-Shih Chen , Su-Lin Lee , Samuel K. Kulp
Inventor: Ching-Shih Chen , Su-Lin Lee , Samuel K. Kulp
IPC: A61K31/496 , C07D403/10
CPC classification number: C07D231/14 , C07D231/12
Abstract: A number of compounds and use of the compounds in a method for treating or preventing cancer in a subject by administering to the subject a pharmaceutical composition including a compound of formula I or a pharmaceutically acceptable salt thereof are described. The compounds can also be used to inhibit integrin-linked kinase in a cell, which has an effect on the Akt signaling pathway.
Abstract translation: 描述了通过向受试者施用包含式I化合物或其药学上可接受的盐的药物组合物来治疗或预防受试者癌症的方法中的许多化合物和化合物的用途。 该化合物也可用于抑制细胞中的整联蛋白连接的激酶,其对Akt信号通路具有影响。
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公开(公告)号:US20130289004A1
公开(公告)日:2013-10-31
申请号:US13882897
申请日:2011-10-31
Applicant: Ching-Shih Chen , Hao-Chieh Chiu , Dasheng Wang , Samuel K. Kulp
Inventor: Ching-Shih Chen , Hao-Chieh Chiu , Dasheng Wang , Samuel K. Kulp
IPC: C07D231/12 , C07D405/04 , C07D471/04
CPC classification number: C07D471/04 , A61K31/415 , A61K31/5415 , C07D231/12 , C07D405/04
Abstract: A method of treating infection by Staphylococcus in a subject by administering a pharmaceutical composition including a celecoxib derivative of formula I or a pharmaceutically acceptable salt thereof is described. The preparation of numerous celecoxib derivatives for testing as potential anti-staphylococcal agents is also described.
Abstract translation: 描述了通过施用包含式I的塞来昔布衍生物或其药学上可接受的盐的药物组合物来治疗受试者中葡萄球菌感染的方法。 还描述了用于测试作为潜在的抗葡萄球菌剂的众多塞来昔布衍生物的制备。
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公开(公告)号:US08546441B2
公开(公告)日:2013-10-01
申请号:US12476772
申请日:2009-06-02
Applicant: Ching-Shih Chen
Inventor: Ching-Shih Chen
IPC: A61K31/415 , C07D231/10
CPC classification number: C07D231/12
Abstract: A new class of phosphoinositide-dependent kinase-1 (PDK-1) inhibitors of formula I: wherein X is selected from the group consisting of alkyl and haloalkyl; Ar is an aryl radical selected from the group consisting of phenyl, biphenyl, naphthyl, anthryl, phenanthryl, and fluorenyl; and wherein Ar is optionally substituted with one or more radicals selected from the group consisting of halo, C1-C4 alkyl, C1-C4 haloalkyl, azido, C1-C4 azidoalkyl, aryl, alkylaryl, haloaryl, haloalkylaryl, and combinations thereof; and R is selected from the group consisting of nitrile, acetonitrile, ethylnitrile, propylnitrile, carboxamide, amidine, tetrazole, oxime, hydrazone, acetamidine, aminoacetamide, guanidine, and urea. Also provided are methods of using the compounds for the treatment and prevention of cancer in humans.
Abstract translation: 新型的式I的磷酸肌醇依赖性激酶-1(PDK-1)抑制剂:其中X选自烷基和卤代烷基; Ar是选自苯基,联苯基,萘基,蒽基,菲基和芴基的芳基; 并且其中Ar任选被一个或多个选自卤素,C 1 -C 4烷基,C 1 -C 4卤代烷基,叠氮基,C 1 -C 4叠氮基烷基,芳基,烷基芳基,卤代芳基,卤代烷基芳基及其组合的基团取代。 并且R选自腈,乙腈,乙腈,丙腈,甲酰胺,脒,四唑,肟,腙,乙脒,氨基乙酰胺,胍和脲。 还提供了使用该化合物治疗和预防人类癌症的方法。
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公开(公告)号:US08377948B2
公开(公告)日:2013-02-19
申请号:US11570966
申请日:2005-06-17
Applicant: Ching-Shih Chen , Yeng-Jeng Shaw , Jason B. Garrison , Natasha Kyprianou
Inventor: Ching-Shih Chen , Yeng-Jeng Shaw , Jason B. Garrison , Natasha Kyprianou
IPC: A01N43/54 , A61K31/517 , C07D239/72
CPC classification number: A61K31/7072 , C07D239/95 , C07D405/12 , C07D409/12
Abstract: 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.
Abstract translation: 基于α1-肾上腺素受体拮抗剂的抗肿瘤化合物,多沙唑嗪,以及组合物和使用方法。 所公开的化合物诱导癌细胞凋亡。
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公开(公告)号:US08309768B2
公开(公告)日:2012-11-13
申请号:US13305927
申请日:2011-11-29
Applicant: Ching-Shih Chen , Samuel K. Kulp , Dasheng Wang , John C. Byrd , Natarajan Muthusamy
Inventor: Ching-Shih Chen , Samuel K. Kulp , Dasheng Wang , John C. Byrd , Natarajan Muthusamy
IPC: C07C215/00 , C07C211/00 , C07C213/00
CPC classification number: C07C217/74 , C07C217/64 , C07C2601/02
Abstract: A number of FTY720-derived compounds with antitumor activity are described. These compounds include the compounds of formula I: wherein R1 is independently selected from the group consisting of hydrogen, methyl. methoxy, and hydroxyl; R2 is independently selected from the group consisting of hydrogen, methoxy, and hydroxyl; R3 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.
Abstract translation: 描述了许多具有抗肿瘤活性的衍生自FTY720的化合物。 这些化合物包括式I化合物:其中R 1独立地选自氢,甲基。 甲氧基和羟基; R2独立地选自氢,甲氧基和羟基; R3独立地选自烷基和环烷基; 并且n独立地选自0至6.由于不被鞘氨醇激酶2磷酸化,所述化合物具有较低的免疫抑制副作用。
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公开(公告)号:US20120142702A1
公开(公告)日:2012-06-07
申请号:US13300872
申请日:2011-11-21
Applicant: Ching-Shih Chen , Su-Lin Lee , Samuel K. Kulp
Inventor: Ching-Shih Chen , Su-Lin Lee , Samuel K. Kulp
IPC: A61K31/496 , C07D231/14 , C12N9/99 , C07D231/12 , A61P35/02 , A61P35/00 , C07D403/10 , A61K31/415
CPC classification number: C07D231/14 , C07D231/12
Abstract: A number of compounds and use of the compounds in a method for treating or preventing cancer in a subject by administering to the subject a pharmaceutical composition including a compound of formula I or a pharmaceutically acceptable salt thereof are described. The compounds can also be used to inhibit integrin-linked kinase in a cell, which has an effect on the Akt signaling pathway.
Abstract translation: 描述了通过向受试者施用包含式I化合物或其药学上可接受的盐的药物组合物来治疗或预防受试者癌症的方法中的许多化合物和化合物的用途。 该化合物也可用于抑制细胞中的整联蛋白连接的激酶,其对Akt信号通路具有影响。
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公开(公告)号:US20120136063A1
公开(公告)日:2012-05-31
申请号:US13305927
申请日:2011-11-29
Applicant: Ching-Shih Chen , Samuel K. Kulp , Dasheng Wang , John C. Byrd , Natarajan Muthusamy
Inventor: Ching-Shih Chen , Samuel K. Kulp , Dasheng Wang , John C. Byrd , Natarajan Muthusamy
IPC: A61K31/137 , A61P35/00 , C07C215/28
CPC classification number: C07C217/74 , C07C217/64 , C07C2601/02
Abstract: A number of FTY720-derived compounds with antitumor activity are described. These compounds include the compounds of formula I: wherein R1 is independently selected from the group consisting of hydrogen, methyl. methoxy, and hydroxyl; R2 is independently selected from the group consisting of hydrogen, methoxy, and hydroxyl; R3 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.
Abstract translation: 描述了许多具有抗肿瘤活性的衍生自FTY720的化合物。 这些化合物包括式I化合物:其中R 1独立地选自氢,甲基。 甲氧基和羟基; R2独立地选自氢,甲氧基和羟基; R3独立地选自烷基和环烷基; 并且n独立地选自0至6.由于不被鞘氨醇激酶2磷酸化,所述化合物具有较低的免疫抑制副作用。
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公开(公告)号:US08039502B2
公开(公告)日:2011-10-18
申请号:US12179134
申请日:2008-07-24
Applicant: Ching-Shih Chen , Hao-Chieh Chiu , Dasheng Wang , John S. Gunn , Larry S. Schlesinger
Inventor: Ching-Shih Chen , Hao-Chieh Chiu , Dasheng Wang , John S. Gunn , Larry S. Schlesinger
IPC: C07D231/12 , A61K31/415
CPC classification number: C07D231/12 , C07D403/04 , C07D403/10 , C07D405/04 , C07D417/04 , C07D417/10 , C07D417/12 , C07D417/14 , C12N2501/06
Abstract: 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,
Abstract translation: 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,
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公开(公告)号:US20110054002A1
公开(公告)日:2011-03-03
申请号:US12547036
申请日:2009-08-25
Applicant: Ching-Shih Chen , Jing-Ru Weng
Inventor: Ching-Shih Chen , Jing-Ru Weng
IPC: A61K31/404 , C07D209/12 , A61P35/00 , C12N5/00
CPC classification number: A61K31/404 , C07D209/12
Abstract: Compounds and methods for treating cancer or inducing apoptosis in proliferating cells. The compounds are shown in formula I: wherein X is selected from hydroxyl, thiol, and amino; Y is selected from carboxyl and sulfonyl; R1, R2, R3, and R4 are selected from hydrogen, lower alkyl, and combinations thereof; R5, R6, and R7 are selected from hydrogen, halo, nitro, amino, methoxy, and combinations thereof; and pharmaceutically acceptable salts thereof.
Abstract translation: 用于在增殖细胞中治疗癌症或诱导细胞凋亡的化合物和方法。 化合物示于式I中:其中X选自羟基,硫醇和氨基; Y选自羧基和磺酰基; R 1,R 2,R 3和R 4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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