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12 条记录 (耗时 0.024 秒)

    Methods for preventing and treating cancer using N-thiolated β-lactam compounds and analogs thereof
    2.
    发明授权
    Methods for preventing and treating cancer using N-thiolated β-lactam compounds and analogs thereof 有权
    使用N-硫醇化β-内酰胺化合物及其类似物预防和治疗癌症的方法

    公开(公告)号：US07026472B2

    公开(公告)日：2006-04-11

    申请号：US10431113

    申请日：2003-05-06

    申请人： Q. Ping Dou ,  Edward Turos ,  David M. Smith

    发明人： Q. Ping Dou ,  Edward Turos ,  David M. Smith

    IPC分类号： C07D205/08 ,  A61K31/397 ,  A61P37/06

    CPC分类号： C07D491/04 ,  C07D205/08

    摘要： The subject invention concerns N-thiolated β-lactam compounds of formula A, wherein R1 is a hydrocarbon group having 1–8 carbon atoms; R3 is an organothio group; and R4 is alkyl, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl, heterocycloalkyl, cycloalkenyl, or heterocycloalkenyl, and analogs and pharmaceutically acceptable salts, esters and amides thereof. The subject invention also concerns methods for inducing tumor cell death or inhibiting tumor cell proliferation, and methods for inducing DNA damage, inhibiting DNA replication, activating p38 MAP kinase, or activating caspase cascade activation, or releasing cytochrome C from mitochondria into the cytoplasm in a tumor cell. Methods for treating cancer using N-thiolated β-lactam compounds, as well as pharmaceutical compositions comprising the same are further disclosed.

    摘要翻译： 本发明涉及式A的N-硫醇化β-内酰胺化合物，其中R 1是具有1-8个碳原子的烃基; R 3是有机硫基; 和R 4是烷基，烯基，炔基，芳基，杂芳基，环烷基，杂环烷基，环烯基或杂环烯基，以及其类似物和药学上可接受的盐，酯和酰胺。 本发明还涉及诱导肿瘤细胞死亡或抑制肿瘤细胞增殖的方法，以及用于诱导DNA损伤，抑制DNA复制，激活p38 MAP激酶或激活胱天蛋白酶级联活化或将细胞色素C从线粒体释放到细胞质中的方法 肿瘤细胞。 使用N-硫醇化β-内酰胺化合物治疗癌症的方法以及包含其的药物组合物进一步公开。

    Tea polyphenol esters and analogs thereof for cancer prevention and treatment
    5.
    发明授权
    Tea polyphenol esters and analogs thereof for cancer prevention and treatment 有权
    茶多酚酯及其类似物用于癌症预防和治疗

    公开(公告)号：US06713506B2

    公开(公告)日：2004-03-30

    申请号：US09973834

    申请日：2001-10-11

    申请人： Q. Ping Dou ,  Sangkil Nam ,  David M. Smith

    发明人： Q. Ping Dou ,  Sangkil Nam ,  David M. Smith

    IPC分类号： A01N4316

    CPC分类号： A61K31/353 ,  C07D311/60

    摘要： Disclosed herein are ester-bond containing tea polyphenols that has a susceptibility to nucleophilic attack, their analogs and pharmaceutically acceptable salts, method for inhibiting proteasomal chymotrypsin-like activity in vivo and in vitro, methods for cancer treatment with tea-derived polyphenols, such as EGCG, ECG, GCG, or CG, as well as pharmaceutical compositions comprising the same.

    摘要翻译： 本文公开了具有对亲核攻击的易感性的含酯键的茶多酚，其类似物和药学上可接受的盐，体内和体外抑制蛋白酶体糜蛋白酶样活性的方法，用茶衍生的多酚进行癌症治疗的方法，例如 EGCG，ECG，GCG或CG，以及包含其的药物组合物。

    Gold (III) complexes with oligopeptides functionalized with sulfur donors and use thereof as antitumor agents
    6.
    发明授权
    Gold (III) complexes with oligopeptides functionalized with sulfur donors and use thereof as antitumor agents 有权
    金（III）与与硫供体官能化的寡肽复合，并将其用作抗肿瘤剂

    公开(公告)号：US08481496B2

    公开(公告)日：2013-07-09

    申请号：US13257684

    申请日：2009-03-20

    申请人： Dolores Fregona ,  Luca Ronconi ,  Fernando Formaggio ,  Q. Ping Dou ,  Donatella Aldinucci

    发明人： Dolores Fregona ,  Luca Ronconi ,  Fernando Formaggio ,  Q. Ping Dou ,  Donatella Aldinucci

    IPC分类号： A61K38/04

    CPC分类号： A61K31/555 ,  C07K5/06026 ,  C07K5/0806

    摘要： The invention concerns Au(III) complexes of the type [AuIIIX2(Pdtc)] (X=halogen, pseudo-halogen; pdtc=peptide-/esterified peptidedithiocarbamato) which are able to both maintain the antitumor properties and the lack of nephrotoxic side-effects of the previously reported Au(III)-dithiocarbamato complexes, together with an improved bioavailability through the peptide-mediated cellular internalization. The Au(III) complexes described have shown a significant biological activity on human tumor cell lines and, thus, they can be advantageously used as antineoplastic agents. The preparation method and use for the treatment of tumor pathologies of the Au(III) complexes of the invention are further described.

    摘要翻译： 本发明涉及能够保持抗肿瘤性质和缺乏肾毒性副作用的[AuIIIX2（Pdtc）]（X =卤素，假卤素; pdtc =肽/酯化的肽二硫代氨基甲酸酯）类型的Au（III） 先前报道的Au（III） - 二硫代氨基甲酸复合物的作用，以及通过肽介导的细胞内化改善的生物利用度。 所描述的Au（III）配合物已经显示出对人肿瘤细胞系的显着的生物活性，因此它们可以有利地用作抗肿瘤剂。 进一步描述了用于治疗本发明的Au（III）复合物的肿瘤病理学的制备方法和用途。

    Methods for preventing and treating cancer using N-thiolated β-lactam compounds and analogs thereof
    9.
    发明授权
    Methods for preventing and treating cancer using N-thiolated β-lactam compounds and analogs thereof 有权
    使用N-硫醇化β-内酰胺化合物及其类似物预防和治疗癌症的方法

    公开(公告)号：US07635693B2

    公开(公告)日：2009-12-22

    申请号：US11374814

    申请日：2006-03-14

    申请人： Q. Ping Dou ,  Edward Turos ,  David M. Smith

    发明人： Q. Ping Dou ,  Edward Turos ,  David M. Smith

    IPC分类号： A61K31/397 ,  C07D205/08 ,  A61P37/06

    CPC分类号： C07D491/04 ,  C07D205/08

    摘要： The subject invention concerns N-thiolated β-lactam compounds of formula A, wherein R1 is a hydrocarbon group having 1-8 carbon atoms; R3 is an organothio group; and R4 is alkyl, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl, heterocycloalkyl, cycloalkenyl, or heterocycloalkenyl, and analogs and pharmaceutically acceptable salts, esters and amides thereof. The subject invention also concerns methods for inducing tumor cell death or inhibiting tumor cell proliferation, and methods for inducing DNA damage, inhibiting DNA replication, activating p38 MAP kinase, or activating caspase cascade activation, or releasing cytochrome C from mitochondria into the cytoplasm in a tumor cell. Methods for treating cancer using N-thiolated β-lactam compounds, as well as pharmaceutical compositions comprising the same are further disclosed.

    摘要翻译： 本发明涉及式A的N-硫醇化β-内酰胺化合物，其中R 1是具有1-8个碳原子的烃基; R3是有机硫基团; 和R4是烷基，烯基，炔基，芳基，杂芳基，环烷基，杂环烷基，环烯基或杂环烯基，以及其类似物和药学上可接受的盐，酯和酰胺。 本发明还涉及诱导肿瘤细胞死亡或抑制肿瘤细胞增殖的方法，以及用于诱导DNA损伤，抑制DNA复制，激活p38 MAP激酶或激活胱天蛋白酶级联活化或将细胞色素C从线粒体释放到细胞质中的方法 肿瘤细胞。 使用N-硫醇化β-内酰胺化合物治疗癌症的方法以及包含其的药物组合物进一步公开。

    GOLD (III) COMPLEXES WITH OLIGOPEPTIDES FUNCTIONALIZED WITH SULFUR DONORS AND USE THEREOF AS ANTITUMOR AGENTS
    10.
    发明申请
    GOLD (III) COMPLEXES WITH OLIGOPEPTIDES FUNCTIONALIZED WITH SULFUR DONORS AND USE THEREOF AS ANTITUMOR AGENTS 有权
    金（III）与具有硫代谢功能的寡核苷酸的复合物，并用作抗肿瘤剂

    公开(公告)号：US20120101044A1

    公开(公告)日：2012-04-26

    申请号：US13257684

    申请日：2009-03-20

    申请人： Dolores Fregona ,  Luca Ronconi ,  Fernando Formaggio ,  Q. Ping Dou ,  Donatella Aldinucci

    发明人： Dolores Fregona ,  Luca Ronconi ,  Fernando Formaggio ,  Q. Ping Dou ,  Donatella Aldinucci

    IPC分类号： A61K38/03 ,  A61P35/00 ,  C07K7/06 ,  C07K1/14 ,  C07K4/00 ,  C07K5/083

    CPC分类号： A61K31/555 ,  C07K5/06026 ,  C07K5/0806

    摘要： The invention concerns Au(III) complexes of the type [AuIIIX2(Pdtc)] (X=halogen, pseudo-halogen; pdtc=peptide-/esterified peptidedithiocarbamato) which are able to both maintain the antitumor properties and the lack of nephrotoxic side-effects of the previously reported Au(III)-dithiocarbamato complexes, together with an improved bioavailability through the peptide-mediated cellular internalization. The Au(III) complexes described have shown a significant biological activity on human tumor cell lines and, thus, they can be advantageously used as antineoplastic agents. The preparation method and use for the treatment of tumor pathologies of the Au(III) complexes of the invention are further described.

    摘要翻译： 本发明涉及能够保持抗肿瘤性质和缺乏肾毒性副作用的[AuIIIX2（Pdtc）]（X =卤素，假卤素; pdtc =肽/酯化的肽二硫代氨基甲酸酯）类型的Au（III） 先前报道的Au（III） - 二硫代氨基甲酸复合物的作用，以及通过肽介导的细胞内化改善的生物利用度。 所描述的Au（III）配合物已经显示出对人肿瘤细胞系的显着的生物活性，因此它们可以有利地用作抗肿瘤剂。 进一步描述了用于治疗本发明的Au（III）复合物的肿瘤病理学的制备方法和用途。