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    AZIRIDINYL-EPOTHILONE COMPOUNDS
    1.
    发明申请
    AZIRIDINYL-EPOTHILONE COMPOUNDS 有权
    亚胺基 - 丙烯酸酯化合物

    公开(公告)号：US20070276018A1

    公开(公告)日：2007-11-29

    申请号：US11753785

    申请日：2007-05-25

    申请人： Gregory Vite ,  Francis Lee ,  Christopher Leamon ,  Iontcho Vlahov

    发明人： Gregory Vite ,  Francis Lee ,  Christopher Leamon ,  Iontcho Vlahov

    IPC分类号： A61K31/427 ,  C07D491/02

    CPC分类号： C07D491/04 ,  A61K47/551 ,  A61K47/65

    摘要： The present invention is directed to aziridinyl epothilone compounds as further described herein, and/or pharmaceutically-acceptable salts and/or solvates thereof having the following Formula: wherein K is —O—, —S—, or —NR7—; A is —(CR8R9)—(CH2)m-Z- wherein Z is —(CHR10)—, —C(═O)—, —C(═O)—C(═O)—, —OC(═O)—, —N(R11)C(═O)—, —SO2—, or —N(R11)SO2—; B1 is hydroxyl or cyano and R1 is hydrogen or B1 and R1 are taken together to form a double bond; R2, R3, and R5 are, independently, hydrogen, alkyl, substituted alkyl, aryl or substituted aryl; or R2 and R3 may be taken together with the carbon to which they are attached to form an optionally substituted cycloalkyl; R4 is hydrogen, alkyl, alkenyl, substituted alkyl, substituted alkenyl, aryl, or substituted aryl; R6 is hydrogen, alkyl or substituted alkyl; R7, R8, R9, R10, R11 and R12 are independently hydrogen, alkyl, substituted alkyl, cycloalkyl, substituted cycloalkyl, aryl, substituted aryl, heterocycloalkyl, substituted heterocycloalkyl, heteroaryl, or substituted heteroaryl; and R13 is aryl, substituted aryl, heteroaryl or substituted heteroaryl.

    摘要翻译： 本发明涉及本文进一步描述的吖丙啶基埃坡霉素化合物和/或其药学上可接受的盐和/或溶剂化物，其具有下式：其中K是-O - ， - S-或-NR 7 / SUB> - ; A是 - （CR 8 R 9） - （CH 2 2）m -Z-，其中Z是 - （CHR 10） - ， - C（-O） - ， - C（-O）-C（ - ） - ， - 11）C（-O） - ， - SO 2 - 或-N（R 11）SO 2 - ; B 1是羟基或氰基，R 1是氢或B 1和R 1一起形成 双重键 R 2，R 3和R 5独立地是氢，烷基，取代的烷基，芳基或取代的芳基; 或R 2和R 3可以与它们所连接的碳一起形成任选取代的环烷基; R 4是氢，烷基，烯基，取代的烷基，取代的烯基，芳基或取代的芳基; R 6是氢，烷基或取代的烷基; R 7，R 8，R 9，R 10，R 11和R 11和 R 12独立地是氢，烷基，取代的烷基，环烷基，取代的环烷基，芳基，取代的芳基，杂环烷基，取代的杂环烷基，杂芳基或取代的杂芳基; R 13是芳基，取代的芳基，杂芳基或取代的杂芳基。

    Identification of polynucleotides and polypetide for predicting activity of compounds that interact with protein tyrosine kinase and or protein tyrosine kinase pathways
    4.
    发明申请
    Identification of polynucleotides and polypetide for predicting activity of compounds that interact with protein tyrosine kinase and or protein tyrosine kinase pathways 审中-公开
    鉴定用于预测与蛋白酪氨酸激酶和/或蛋白酪氨酸激酶途径相互作用的化合物的活性的多核苷酸和多肽

    公开(公告)号：US20060046249A1

    公开(公告)日：2006-03-02

    申请号：US10501035

    申请日：2003-01-17

    申请人： Fei Huang ,  Craig Fairchild ,  Francis Lee ,  Peter Shaw

    发明人： Fei Huang ,  Craig Fairchild ,  Francis Lee ,  Peter Shaw

    IPC分类号： C12Q1/68 ,  C07H21/04

    CPC分类号： G01N33/5011 ,  C12Q1/6837 ,  C12Q1/6886 ,  C12Q2600/106 ,  C12Q2600/136 ,  C12Q2600/156 ,  G01N33/5023 ,  G01N2333/91215 ,  G01N2800/52 ,  G16B20/00

    摘要： The present invention describes polynucleotides and polypeptides that have been discovered to correlate to the relative intrinsic sensitivity or resistance of cells, e.g., colon cell lines, to treatment with compounds that interact with and inhibit src tyrosine kinases. These polynucleotides and polypeptides have been shown, through a weighted voting cross validation program, to have utility in predicting the intrinsic resistance and sensitivity of colon cell lines to these compounds. Such polynucleotides and polypeptides whose expression levels correlate highly with drug sensitivity or resistance comprise predictor or marker sets of polynucleotides and polypeptides that are useful in methods of predicting drug response, and as prognostic or diagnostic indicators in disease management, particularly in those disease areas in which signaling through src tyrosine kinase of the src tyrosine kinase pathway is involved with the disease process.

    摘要翻译： 本发明描述了已被发现与将细胞例如结肠细胞系相对固有的敏感性或抗性与与酪氨酸激酶相互作用并抑制酪氨酸激酶的化合物进行治疗相关的多核苷酸和多肽。 已经通过加权投票交叉验证程序显示了这些多核苷酸和多肽在预测结肠细胞系对这些化合物的固有抗性和敏感性方面具有实用性。 其表达水平与药物敏感性或抗性高度相关的这样的多核苷酸和多肽包括可用于预测药物反应的方法中的多核苷酸和多肽的预测物或标志物组，以及作为疾病管理中的预后或诊断指标，特别是在其中 通过src酪氨酸激酶信号传导src酪氨酸激酶途径参与疾病过程。

    Identification of polynucleotides and polypeptide for predicting activity of compounds that interact with protein tyrosine kinases and/or protein tyrosine kinase pathways
    5.
    发明申请
    Identification of polynucleotides and polypeptide for predicting activity of compounds that interact with protein tyrosine kinases and/or protein tyrosine kinase pathways 审中-公开
    鉴定用于预测与蛋白酪氨酸激酶和/或蛋白酪氨酸激酶途径相互作用的化合物的活性的多核苷酸和多肽

    公开(公告)号：US20070166704A1

    公开(公告)日：2007-07-19

    申请号：US10348119

    申请日：2003-01-17

    申请人： Fei Huang ,  Craig Fairchild ,  Francis Lee ,  Peter Shaw

    发明人： Fei Huang ,  Craig Fairchild ,  Francis Lee ,  Peter Shaw

    IPC分类号： C12Q1/68 ,  C07H21/04

    CPC分类号： G01N33/5011 ,  C12Q1/6837 ,  C12Q1/6886 ,  C12Q2600/106 ,  C12Q2600/136 ,  C12Q2600/156 ,  G01N33/5023 ,  G01N2333/91215 ,  G01N2800/52 ,  G16B20/00

    摘要： The present invention describes polynucleotides and polypeptides that have been discovered to correlate to the relative intrinsic sensitivity or resistance of cells, e.g., colon cell lines, to treatment with compounds that interact with and inhibit src tyrosine kinases. These polynucleotides and polypeptides have been shown, through a weighted voting cross validation program, to have utility in predicting the intrinsic resistance and sensitivity of colon cell lines to these compounds. Such polynucleotides and polypeptides whose expression levels correlate highly with drug sensitivity or resistance comprise predictor or marker sets of polynucleotides and polypeptides that are useful in methods of predicting drug response and as prognostic or diagnostic indicators in disease management, particularly in those disease areas in which signaling through src tyrosine kinase of the src tyrosine kinase pathway is involved with the disease process.

    摘要翻译： 本发明描述了已被发现与将细胞例如结肠细胞系相对固有的敏感性或抗性与与酪氨酸激酶相互作用并抑制酪氨酸激酶的化合物进行治疗相关的多核苷酸和多肽。 已经通过加权投票交叉验证程序显示了这些多核苷酸和多肽在预测结肠细胞系对这些化合物的固有抗性和敏感性方面具有实用性。 其表达水平与药物敏感性或抗性高度相关的这样的多核苷酸和多肽包括可用于预测药物反应的方法的预测因子或标志物组，以及在疾病管理中的预后或诊断指标，特别是在信号传导 通过src酪氨酸激酶的酪氨酸激酶途径参与疾病过程。

    Use of dasatinib for the treatment of bone metastasis
    7.
    发明申请
    Use of dasatinib for the treatment of bone metastasis 审中-公开
    使用达沙替尼治疗骨转移

    公开(公告)号：US20070093499A1

    公开(公告)日：2007-04-26

    申请号：US11583564

    申请日：2006-10-19

    申请人： Francis Lee ,  Feng Luo ,  Jean Feyen

    发明人： Francis Lee ,  Feng Luo ,  Jean Feyen

    IPC分类号： A61K31/506

    CPC分类号： A61K31/497

    摘要： The present disclosure is directed to a method of treating bone metastasis, hypercalcemia, and/or bone resorption comprising administering to a patient in need thereof a therapeutically effective amount of a compound of formula (I) or pharmaceutically acceptable salt, hydrate or solvate thereof.

    摘要翻译： 本公开涉及治疗骨转移，高钙血症和/或骨吸收的方法，包括向有需要的患者施用治疗有效量的式（I）化合物或其药学上可接受的盐，水合物或溶剂合物。

    Combinations, methods and compositions for treating cancer
    8.
    发明申请
    Combinations, methods and compositions for treating cancer 审中-公开
    用于治疗癌症的组合，方法和组合物

    公开(公告)号：US20060235006A1

    公开(公告)日：2006-10-19

    申请号：US11402502

    申请日：2006-04-12

    申请人： Francis Lee ,  Roberto Weinmann

    发明人： Francis Lee ,  Roberto Weinmann

    IPC分类号： A61K31/5513

    CPC分类号： A61K45/06 ,  A61K31/506 ,  A61K31/5513 ,  A61K2300/00

    摘要： The invention relates to a combination of BCR-ABL inhibitor, exemplified by ′N-(2-Chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-5-thiazolecarboxamide and/or other BCR/ABL inhibitors, and a stem cell selective cytotoxic, exemplified by (R)-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-4-(2-thienylsulfonyl)-1H-1,4-benzodiazepine-7-carbonitrile, hydrochloride salt, and or other stem cell cytotoxic agents, pharmaceutical compositions of the combination and to methods of using the pharmaceutical compositions in the treatment of oncological disorders.

    摘要翻译： 本发明涉及BCR-ABL抑制剂的组合，例如“N-（2-氯-6-甲基苯基）-2 - [[6- [4-（2-羟乙基）-1-哌嗪基] -2-甲基 -4-嘧啶基]氨基] -5-噻唑甲酰胺和/或其它BCR / ABL抑制剂和干细胞选择性细胞毒性，例如（R）-2,3,4,5-四氢-1-（1H-咪唑-2-基） 吡啶-4-基甲基）-3-（苯基甲基）-4-（2-噻吩基磺酰基）-1H-1,4-苯并二氮杂-7-甲腈盐酸盐和/或其它干细胞细胞毒性剂，组合的药物组合物和方法 使用药物组合物治疗肿瘤疾病。

    Novel bone graft composite
    9.
    发明申请
    Novel bone graft composite 审中-公开
    新型骨移植复合材料

    公开(公告)号：US20050010305A1

    公开(公告)日：2005-01-13

    申请号：US10766084

    申请日：2004-01-28

    申请人： Francis Lee

    发明人： Francis Lee

    IPC分类号： A61F2/28 ,  A61L27/42

    CPC分类号： A61L27/425 ,  A61F2002/2835 ,  A61L2430/02

    摘要： A bone graft composite comprising a bisphosphonate is provided which is suitable for treating bone destruction. The bisphosphonate provides bone graft protection.

    摘要翻译： 提供了包含二膦酸盐的骨移植复合物，其适用于治疗骨破坏。 双膦酸盐提供骨移植保护。

    Inkjet printhead chip
    10.
    发明申请
    Inkjet printhead chip 有权
    喷墨打印头芯片

    公开(公告)号：US20060238576A1

    公开(公告)日：2006-10-26

    申请号：US11180759

    申请日：2005-07-12

    申请人： Francis Lee ,  Jui-Hua Hu ,  Jia-Lin Chen ,  Wei-Fu Lai

    发明人： Francis Lee ,  Jui-Hua Hu ,  Jia-Lin Chen ,  Wei-Fu Lai

    IPC分类号： B41J2/04

    CPC分类号： B41J2/1412 ,  B41J2/14129

    摘要： An inkjet printhead chip includes a substrate, transistors, isolation structures, a dielectric layer, a resistive layer and conductive sections. Each transistor includes a gate, a source, a drain and a gate oxide disposed between the gate and the substrate. The isolation structures are on the substrate surface and isolate the transistors. The dielectric layer covers the transistors and the isolation structures, and has openings exposed the source and the drain. Several heating regions are in the resistive layer that is on the dielectric layer. In the conductive sections, the first conductive section is on the resistive layer and exposes the heating regions for forming several heating devices. Each heating device has resistance less than 95 ohm and power density less than 2 GW/m2; the second conductive section and the third conductive section are electrically coupled to the drain and the source through the openings of the dielectric layer respectively.

    摘要翻译： 喷墨打印头芯片包括基板，晶体管，隔离结构，电介质层，电阻层和导电部分。 每个晶体管包括设置在栅极和衬底之间的栅极，源极，漏极和栅极氧化物。 隔离结构在衬底表面上并隔离晶体管。 电介质层覆盖晶体管和隔离结构，并且具有露出源极和漏极的开口。 在电介质层上的电阻层中有几个加热区。 在导电部分中，第一导电部分在电阻层上并且暴露加热区域以形成几个加热装置。 每个加热装置的电阻小于95欧姆，功率密度小于2GW / m 2; 第二导电部分和第三导电部分分别通过介电层的开口电耦合到漏极和源极。