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公开(公告)号：US09249466B2
公开(公告)日：2016-02-02
申请号：US13520472
申请日：2011-01-10
IPC分类号： C12N15/11 , C12Q1/68 , A61K45/06 , G01N33/574 , A61K31/436 , A61K31/506 , A61K31/713 , C12Q1/42 , G01N33/68
CPC分类号： C12Q1/6886 , A61K31/436 , A61K31/506 , A61K31/713 , A61K45/06 , C12Q1/42 , G01N33/57407 , G01N33/6893
摘要： We describe a method of determining whether a cancer cell is likely to be resistant to treatment by an mTOR inhibitor. The method may comprise detecting PPP2R2B (GenBank Accession Number: NM_18167) in or of the cell. It may, alternatively, or in addition, comprise detecting PDK1 (GenBank Accession Number: NM_002613), in or of the cell. The method may comprise detecting methylation of the PPP2R2B promoter in or of the cell. It may comprise detecting the expression and/or activity of PPP2R2B in or of the cell. It may comprise detecting PDK1 mediated Myc phosphorylation activity. Methods of choosing a treatment for an individual suffering from or suspected to be suffering from a cancer, determining whether an individual suffering from or suspected to be suffering from a cancer will respond to treatment by an mTOR inhibitor, increasing the sensitivity of a cancer cell to treatment by an mTOR inhibitor, for treating or preventing cancer in an individual suffering or suspected to be suffering from cancer are also provided. We further provide for a combination of an inhibitor of PDK1 expression and/or activity and an mTOR inhibitor for use in a method of treatment or prevention of cancer.
摘要翻译： 我们描述一种确定癌细胞是否可能对mTOR抑制剂治疗有抗性的方法。 该方法可以包括在细胞内或细胞中检测PPP2R2B（GenBank登录号：NM_18167）。 或者或另外还包括检测细胞内或细胞中的PDK1（GenBank登录号：NM_002613）。 该方法可以包括检测细胞内或细胞中的PPP2R2B启动子的甲基化。 它可以包括检测细胞中或细胞中的PPP2R2B的表达和/或活性。 它可以包括检测PDK1介导的Myc磷酸化活性。 为患有或怀疑患有癌症的个体选择治疗方法，确定患有或怀疑患有癌症的个体是否会对mTOR抑制剂的治疗产生反应，从而增加癌细胞的敏感性 还提供了用于治疗或预防患有或怀疑患有癌症的个体的癌症的mTOR抑制剂的治疗。 我们进一步提供PDK1表达和/或活性的抑制剂和用于治疗或预防癌症的方法中的mTOR抑制剂的组合。
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公开(公告)号：US08058258B2
公开(公告)日：2011-11-15
申请号：US12281470
申请日：2006-11-15
申请人： Qiang Yu , Jing Tan , Xiao Jing Yang
发明人： Qiang Yu , Jing Tan , Xiao Jing Yang
CPC分类号： A61K31/519 , A61K31/52
摘要： The present invention relates to a method of inducing apoptosis in a tumour cell as well as modulating pluripotency and/or self-renewing characteristics of a stem/progenitor cell. The method comprises administering to the respective cell a compound of general formula (I). In general formula A is C or N. R1, R4 and R5 are, independently selected, H or aliphatic, cycloaliphatic aromatic, arylaliphatic, or arylcycloaliphatic hydrocarbyl groups, that comprise 0-3 heteroatoms being N, O, S, or Si. R4 and R5 may optionally be linked so as to define an aliphatic hydrocarbyl bridge. R2 is H or a halogen, such as F or Cl. R3 is H, or an aliphatic or arylaliphatic hydrocarbyl group comprising 1-8 main chain carbon atoms and 0-3 heteroatoms being N, O, S, Si, or a halogen such as Cl or F. Also provided is a pharmaceutical composition for inducing apoptosis in a tumour cell and/or modulating pluripotency and/or self-renewing characteristics of a stem/progenitor cell. The pharmaceutical composition comprises a compound as defined above or a pharmaceutically acceptable salt thereof and a carrier or diluent.
摘要翻译： 本发明涉及诱导肿瘤细胞凋亡的方法以及调节干细胞/祖细胞的多能性和/或自我更新特性。 该方法包括向各细胞施用通式（I）的化合物。 通式A是C或N.R 1，R 4和R 5独立地选自H或脂族，脂环族芳族，芳基脂族或芳基环脂族烃基，其包含0-3个杂原子是N，O，S或Si。 R 4和R 5可以任选连接以限定脂族烃基桥。 R2是H或卤素，例如F或Cl。 R 3是H，或包含1-8个主链碳原子和0-3个杂原子的脂族或芳基脂族烃基是N，O，S，Si或卤素如Cl或F.还提供了用于诱导 肿瘤细胞凋亡和/或调节干细胞/祖细胞的多能性和/或自我更新特性。 药物组合物包含如上所定义的化合物或其药学上可接受的盐和载体或稀释剂。
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公开(公告)号：US20100075915A1
公开(公告)日：2010-03-25
申请号：US12281470
申请日：2006-11-15
申请人： Qiang Yu , Jing Tan , Xiao Jing Yang
发明人： Qiang Yu , Jing Tan , Xiao Jing Yang
IPC分类号： A61K31/7068 , A61K31/52 , A61K31/437 , A61K31/7052 , A61K31/502 , C12N5/00 , C12N5/07 , A61P35/00 , C12N5/071 , C12Q1/02 , C12Q1/68
CPC分类号： A61K31/519 , A61K31/52
摘要： The present invention relates to a method of inducing apoptosis in a tumour cell as well as modulating pluripotency and/or self-renewing characteristics of a stem/progenitor cell. The method comprises administering to the respective cell a compound of general formula (I). In general formula A is C or N. R1, R4 and R5 are, independently selected, H or aliphatic, cycloaliphatic aromatic, arylaliphatic, or arylcycloaliphatic hydrocarbyl groups, that comprise 0-3 heteroatoms being N, O, S, or Si. R4 and R5 may optionally be linked so as to define an aliphatic hydrocarbyl bridge. R2 is H or a halogen, such as F or Cl. R3 is H, or an aliphatic or arylaliphatic hydrocarbyl group comprising 1-8 main chain carbon atoms and 0-3 heteroatoms being N, O, S, Si, or a halogen such as Cl or F. Also provided is a pharmaceutical composition for inducing apoptosis in a tumour cell and/or modulating pluripotency and/or self-renewing characteristics of a stem/progenitor cell. The pharmaceutical composition comprises a compound as defined above or a pharmaceutically acceptable salt thereof and a carrier or diluent.
摘要翻译： 本发明涉及诱导肿瘤细胞凋亡的方法以及调节干细胞/祖细胞的多能性和/或自我更新特性。 该方法包括向各细胞施用通式（I）的化合物。 通式A是C或N.R 1，R 4和R 5独立地选自H或脂族，脂环族芳族，芳基脂族或芳基环脂族烃基，其包含0-3个杂原子是N，O，S或Si。 R 4和R 5可以任选连接以限定脂族烃基桥。 R2是H或卤素，例如F或Cl。 R 3是H，或包含1-8个主链碳原子和0-3个杂原子的脂族或芳基脂族烃基是N，O，S，Si或卤素如Cl或F.还提供了用于诱导 肿瘤细胞凋亡和/或调节干细胞/祖细胞的多能性和/或自我更新特性。 药物组合物包含如上所定义的化合物或其药学上可接受的盐和载体或稀释剂。
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公开(公告)号：US20120077841A1
公开(公告)日：2012-03-29
申请号：US13245709
申请日：2011-09-26
申请人： Qiang Yu , Jing Tan , Xiao Jing Yang
发明人： Qiang Yu , Jing Tan , Xiao Jing Yang
IPC分类号： A61K31/437 , C12N5/095 , A61P35/00 , C12N5/071 , C12N5/0735
CPC分类号： A61K31/519 , A61K31/52
摘要： The present invention relates to a method of modulating pluripotency and/or self-renewing characteristics of a stem/progenitor cell. The method comprises administering to the respective cell a compound of the general formula (I) In the general formula A is C or N. R1, R4 and R5 are, independently selected, H or aliphatic, cycloaliphatic, aromatic, arylaliphatic, or arylcycloaliphatic hydrocarbyl groups, that comprise 0-3 heteroatoms being N, O, S, or Si. R4 and R5 may optionally be linked so as to define an aliphatic hydrocarbyl bridge. R2 is H or a halogen. R3 is H, or an aliphatic or arylaliphatic hydrocarbyl group comprising 1-8 main chain carbon atoms and 0-3 heteroatoms being N, O, S, Si, or a halogen.
摘要翻译： 本发明涉及一种调节干细胞/祖细胞的多能性和/或自我更新特性的方法。 该方法包括向各细胞施用通式（I）的化合物。在通式A中是C或N.R 1，R 4和R 5独立地选自H或脂族，脂环族，芳族，芳基脂族或芳基环脂族烃基 基团，其包含0-3个杂原子是N，O，S或Si。 R 4和R 5可以任选连接以限定脂族烃基桥。 R2是H或卤素。 R3是H或包含1-8个主链碳原子和0-3个杂原子的脂族或芳基脂族烃基是N，O，S，Si或卤素。
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公开(公告)号：US20130123328A1
公开(公告)日：2013-05-16
申请号：US13520472
申请日：2011-01-10
IPC分类号： C12Q1/68 , A61K31/436 , C12Q1/42 , A61K45/06 , G01N33/68 , A61K31/506 , A61K31/713
CPC分类号： C12Q1/6886 , A61K31/436 , A61K31/506 , A61K31/713 , A61K45/06 , C12Q1/42 , G01N33/57407 , G01N33/6893
摘要： We describe a method of determining whether a cancer cell is likely to be resistant to treatment by an mTOR inhibitor. The method may comprise detecting PPP2R2B (GenBank Accession Number: NM_18167) in or of the cell. It may, alter-natively, or in addition, comprise detecting PDK1 (GenBank Accession Number: NM_002613), in or of the cell. The method may comprise detecting methylation of the PPP2R2B promoter in or of the cell. It may comprise detecting the expression and/or activity of PPP2R2B in or of the cell. It may comprise detecting PDK1 mediated Myc phosphorylation activity. Methods of choosing a treatment for an individual suffering from or suspected to be suffering from a cancer, determining whether an individual suffering from or suspected to be suffering from a cancer will respond to treatment by an mTOR inhibitor, increasing the sensitivity of a cancer cell to treatment by an mTOR inhibitor, for treating or preventing cancer in an individual suffering or suspected to be suffering from cancer are also provided. We further provide for a combination of an inhibitor of PDK1 expression and/or activity and an mTOR inhibitor for use in a method of treatment or prevention of cancer.
摘要翻译： 我们描述一种确定癌细胞是否可能对mTOR抑制剂治疗有抗性的方法。 该方法可以包括在细胞内或细胞中检测PPP2R2B（GenBank登录号：NM_18167）。 可以或者另外还包括检测细胞内或细胞中的PDK1（GenBank登录号：NM_002613）。 该方法可以包括检测细胞内或细胞中的PPP2R2B启动子的甲基化。 它可以包括检测细胞中或细胞中的PPP2R2B的表达和/或活性。 它可以包括检测PDK1介导的Myc磷酸化活性。 为患有或怀疑患有癌症的个体选择治疗方法，确定患有或怀疑患有癌症的个体是否会对mTOR抑制剂的治疗产生反应，从而增加癌细胞的敏感性 还提供了用于治疗或预防患有或怀疑患有癌症的个体的癌症的mTOR抑制剂的治疗。 我们进一步提供PDK1表达和/或活性的抑制剂和用于治疗或预防癌症的方法中的mTOR抑制剂的组合。
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公开(公告)号：US08211869B2
公开(公告)日：2012-07-03
申请号：US13245709
申请日：2011-09-26
申请人： Qiang Yu , Jing Tan , Xiao Jing Yang
发明人： Qiang Yu , Jing Tan , Xiao Jing Yang
CPC分类号： A61K31/519 , A61K31/52
摘要： The present invention relates to a method of modulating pluripotency and/or self-renewing characteristics of a stem/progenitor cell. The method comprises administering to the respective cell a compound of the general formula (I) In the general formula A is C or N. R1, R4 and R5 are, independently selected, H or aliphatic, cycloaliphatic, aromatic, arylaliphatic, or arylcycloaliphatic hydrocarbyl groups, that comprise 0-3 heteroatoms being N, O, S, or Si. R4 and R5 may optionally be linked so as to define an aliphatic hydrocarbyl bridge. R2 is H or a halogen. R3 is H, or an aliphatic or arylaliphatic hydrocarbyl group comprising 1-8 main chain carbon atoms and 0-3 heteroatoms being N, O, S, Si, or a halogen.
摘要翻译： 本发明涉及一种调节干细胞/祖细胞的多能性和/或自我更新特性的方法。 该方法包括向各细胞施用通式（I）的化合物。在通式A中是C或N.R 1，R 4和R 5独立地选自H或脂族，脂环族，芳族，芳基脂族或芳基环脂族烃基 基团，其包含0-3个杂原子是N，O，S或Si。 R 4和R 5可以任选连接以限定脂族烃基桥。 R2是H或卤素。 R3是H或包含1-8个主链碳原子和0-3个杂原子的脂族或芳基脂族烃基是N，O，S，Si或卤素。
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公开(公告)号：US08142914B2
公开(公告)日：2012-03-27
申请号：US13027944
申请日：2011-02-15
申请人： Qiang Yu , Steven W. Sucech , Brent E. Groza , Raymond J. Mlinac , Frederick T. Jones , Paul J. Henkels
发明人： Qiang Yu , Steven W. Sucech , Brent E. Groza , Raymond J. Mlinac , Frederick T. Jones , Paul J. Henkels
IPC分类号： B32B13/00
CPC分类号： C04B16/02 , C04B14/00 , C04B16/04 , C04B22/16 , C04B28/14 , C04B28/147 , C04B41/009 , C04B41/70 , C04B2111/00094 , C04B2111/00612 , C04B2111/0062 , C04B2111/00672 , C04B2111/52 , C04B2111/54 , Y10T428/192 , Y10T428/26 , Y10T428/31971 , C04B14/185 , C04B20/0048 , C04B24/16 , C04B24/38 , C04B38/10 , C04B24/32 , C04B14/38 , C04B22/004 , C04B24/383 , C04B40/0028 , C04B14/46 , C04B24/26 , C04B2103/44
摘要： The invention provides a set gypsum-containing product having increased resistance to permanent deformation and a method for preparing it comprising forming a mixture of a calcium sulfate material, water, and an appropriate amount of one or more enhancing materials chosen from condensed phosphoric acids, each of which comprises 2 or more phosphoric acid units; and salts or ions of condensed phosphates, each of which comprises 2 or more phosphate units. The mixture is then maintained under conditions sufficient for the calcium sulfate material to form a set gypsum material.
摘要翻译： 本发明提供了具有增加的对永久变形的抗性的集合的含石膏产品及其制备方法，包括形成硫酸钙材料，水和适量的一种或多种选自缩合磷酸的增强材料的混合物， 其中包含2个或更多个磷酸单元; 和缩合磷酸盐的盐或离子，其中每一个包含2个或更多个磷酸酯单元。 然后将混合物保持在足以使硫酸钙材料形成集合的石膏材料的条件下。
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公开(公告)号：US20110053882A1
公开(公告)日：2011-03-03
申请号：US12740912
申请日：2008-11-03
申请人： Qiang Yu
发明人： Qiang Yu
IPC分类号： A61K31/7064 , C12N5/071 , C12N5/07 , G01N33/53 , A61P35/00
CPC分类号： A61K31/437 , A61K31/185 , A61K31/519 , A61K31/52 , G01N33/5011 , G01N2800/52
摘要： The invention relates to a method of preventing, inhibiting, arresting or reversing tumourigenesis in a cell as well as a method of inducing apoptosis in a tumour cell. The method includes increasing the amount and/or the activity of a DACT protein, or a functional fragment thereof, in the cell. Also provided is a pharmaceutical composition that comprises a compound of general formula (I), wherein A is CH or N, R1, R4 and R5 are independent from each other H, an aliphatic group, an alicyclic group, an aromatic group, an arylaliphatic group, and an arylalicyclic group comprising 0-3 heteroatoms. The heteroatoms may be N, O, S, or Si. R4 and R5 may optionally be linked so as to define an aliphatic hydrocarbyl bridge. R2 is H or a halogen such as F, Cl, Br or L. R3 is H, F, Cl or an aliphatic or arylaliphatic group that includes 1-8 main chain carbon atoms and 0-3 heteroatoms. The pharmaceutical composition also comprises a histone deacetylase inhibitor.
摘要翻译： 本发明涉及一种在细胞中预防，抑制，阻止或逆转肿瘤发生的方法以及诱导肿瘤细胞凋亡的方法。 该方法包括增加细胞中DACT蛋白或其功能片段的量和/或活性。 还提供了包含通式（I）的化合物的药物组合物，其中A为CH或N，R 1，R 4和R 5彼此独立地为H，脂族基团，脂环族基团，芳族基团，芳基脂族基 基团和包含0-3个杂原子的芳基脂环基团。 杂原子可以是N，O，S或Si。 R 4和R 5可以任选连接以限定脂族烃基桥。 R 2是H或卤素如F，Cl，Br或L.R 3是H，F，Cl或包含1-8个主链碳原子和0-3个杂原子的脂族或芳基脂族基团。 药物组合物还包含组蛋白脱乙酰酶抑制剂。
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公开(公告)号：US07771851B2
公开(公告)日：2010-08-10
申请号：US11213529
申请日：2005-08-26
申请人： Weixin David Song , Qiang Yu , Qiangxia Liu
发明人： Weixin David Song , Qiang Yu , Qiangxia Liu
CPC分类号： B32B13/04 , B32B13/08 , B32B2250/03 , B32B2250/40 , B32B2264/06 , B32B2307/538 , B32B2307/54 , B32B2607/00 , C04B11/002 , C04B20/0076 , C04B28/146 , C04B28/147 , C04B2111/0062 , Y10T428/232 , C04B22/16 , C04B24/226 , C04B24/383
摘要： The invention provides gypsum wallboard, made from gypsum-containing slurries having outstanding hydration rate characteristics comprising alpha-hemihydrate ground to a particular particle size distribution range and having a Blaine surface area in the range from about 3100 cm2/g to about 9000 cm2/g, alone or in combination with beta-hemihydrate.
摘要翻译： 本发明提供了由具有优异水合速率特性的含石膏浆料制成的石膏墙板，其包括将半水合物研磨至特定的粒度分布范围并具有约3100cm 2 / g至约9000cm 2 / g范围内的Blaine表面积 ，单独或与β-半水合物组合。
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