专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

WO2010107786A2 CT ATLAS OF THE BRISBANE 2000 SYSTEM OF LIVER ANATOMY FOR RADIATION ONCOLOGISTS 审中-公开
标题翻译： 2000年度BRISBANE系统CT扫描分析
公开(公告)号：WO2010107786A2
公开(公告)日：2010-09-23
申请号：PCT/US2010027470
申请日：2010-03-16
申请人： H LEE MOFFITT CANCER CT AND RE , UNIV SOUTH FLORIDA , FINKELSTEIN STEVEN ERIC , HOFFE SARAH E , RUSSELL MARK S
发明人： FINKELSTEIN STEVEN ERIC , HOFFE SARAH E , RUSSELL MARK S
IPC分类号： A61B6/00
CPC分类号： A61B90/36 , A61B90/37 , A61B2090/364 , G06T7/33 , G06T2207/20128 , G06T2207/30056
摘要： The method includes the steps of obtaining atlas data in an atlas coordinate set from a computer-readable atlas of hepatic anatomical information including three orders of division. The three orders of division include a first order separating the liver into two (right and left) hemi-livers, a second order transverse to the first order and dividing the liver into (anterior, posterior and medial) sections, and a third order (segments) transverse to the second order and approximately parallel to the first order and dividing the liver into segments. The first order of division approximately correlates to Cantlie's Line. The second order of division is approximately correlated to the portal vein. The third order of division is approximately correlated to the hepatic vein. In total, these three orders of division divide the liver into 7 segments, with the left hemiliver divided into three segments and the right hemiliver is divided into 4 segments.
摘要翻译：该方法包括以下步骤：从包括三个分割的肝解剖信息的计算机可读图集获取图集坐标集中的图集数据。三个分裂阶段包括将肝脏分成两个（右和左）半肝的第一级，第二级横向于第一级并将肝脏分成（前部，后部和内侧）部分和第三级（段）横向于第二级并且大致平行于第一级并将肝脏分成段。分区的第一个顺序与坎特里线相关。分割的第二级与门静脉大致相关。三分割与肝静脉近似相关。总共三个这样的划分，将肝脏划分为7个部分，左半肝分为3个部分，右半肝分为4个部分。

2. 发明申请

WO2009135000A3 INHIBITION OF SHP2/PTPN11 PROTEIN TYROSINE PHOSPHATASE BY NSC-117199 AND ANALOGS 审中-公开
标题翻译： NSC-117199和模拟物对SHP2 / PTPN11蛋白酪氨酸磷酸化酶的抑制作用
公开(公告)号：WO2009135000A3
公开(公告)日：2010-02-18
申请号：PCT/US2009042305
申请日：2009-04-30
申请人： H LEE MOFFITT CANCER CT AND RE , UNIV SOUTH FLORIDA , WU JIE , LAWRENCE NICHOLAS J , SEBTI SAID M , LAWRENCE HARSHANI R
发明人： WU JIE , LAWRENCE NICHOLAS J , SEBTI SAID M , LAWRENCE HARSHANI R
IPC分类号： A61K31/404 , A61P35/00 , C07D209/34
CPC分类号： C07D209/40
摘要： Protein tyrosine phosphatase (PTP) Shp2 is a non-receptor PTP that involved in cell signaling and regulation of cell proliferation, differentiation, and migration. Shp2 mediates activation of kinases that are involved in the pathogenesis of human carcinoma. NSC-117199 was identified as a porent inhibitor of the protein tyrosine phosphatase (PTPa) Shp2. A focused library of analogs incorporating an isatin scaffold was designed and evaluated for inhibition of Shp2 and Shp1 PTP activities. Several compounds were identified that selectively inhibit Shp2 over Shp1 and PTP1B with low to sub-micromolar activity. Also disclosed are methods of inhibiting a protein tyrosine phosphatase in a cell and treating cancer through selective inhibition of Shp2.
摘要翻译：蛋白酪氨酸磷酸酶（PTP）Shp2是参与细胞信号传导和调节细胞增殖，分化和迁移的非受体PTP。 Shp2介导参与人类癌症发病机制的激酶活化。 NSC-117199被鉴定为蛋白酪氨酸磷酸酶（PTPa）Shp2的细胞抑制剂。设计了一个重点的掺入靛红支架的类似物库，并评估了Shp2和Shp1 PTP活性的抑制作用。鉴定出几种化合物选择性地抑制Shp1与Shp1和PTP1B的低亚微摩尔活性。还公开了抑制细胞中的蛋白质酪氨酸磷酸酶并通过选择性抑制Shp2治疗癌症的方法。

3. 发明申请

WO2009158040A3 CANCER PLATINUM RESISTANCE DETECTION AND SENSITIZATION METHOD 审中-公开
标题翻译：癌症耐铂检测和敏感方法
公开(公告)号：WO2009158040A3
公开(公告)日：2010-04-22
申请号：PCT/US2009003863
申请日：2009-06-26
申请人： UNIV SOUTH FLORIDA , H LEE MOFFITT CANCER CT AND RE , LANCASTER JONATHAN , COTTRILL HOPE , CHEN NING , BLOOM GREGORY , ESCHRICH STEVEN , XIONG YIN , HUMPHREY MARCIA
发明人： LANCASTER JONATHAN , COTTRILL HOPE , CHEN NING , BLOOM GREGORY , ESCHRICH STEVEN , XIONG YIN , HUMPHREY MARCIA
IPC分类号： C12Q1/68 , A61K48/00 , C12N15/09 , G01N33/50
CPC分类号： G01N33/57449 , G01N33/57484 , G01N2800/52
摘要： The phosphorylation status of the BAD protein is a determinant of ovarian cancer cell responsiveness to platinum chemotherapy. Indirect manipulation of BAD phosphorylation status influences cisplatin sensitivity. BAD phosphorylation represents a biomarker that predicts platinum sensitivity and is a therapeutic target to increase platinum sensitivity. The methods employ phospho-specific antibody against a particular amino acid residue or site. Phospho-specific protein characterization methods include immunohistochemical (IHC), flow cytometric, immunofluorescent, capture-and- detection, or reversed phase assay.
摘要翻译： BAD蛋白的磷酸化状态是卵巢癌细胞对铂化疗反应的决定因素。间接操作BAD磷酸化状态影响顺铂敏感性。 BAD磷酸化代表了预测铂敏感性的生物标志物，并且是增加铂敏感性的治疗靶标。该方法使用针对特定氨基酸残基或位点的磷酸特异性抗体。磷酸特异性蛋白质表征方法包括免疫组织化学（IHC），流式细胞术，免疫荧光，捕获和检测或反相测定。

4. 发明申请

WO2009018541A8 5'-SUBSTITUTED ADENOSYNES, PREPARATION THEREOF AND USE AS INHIBITORS OF S-ADENOSYLMETHIONINE DECARBOXYLASE 审中-公开
标题翻译： 5'-取代腺苷，其制备方法和用作S-腺嘧啶脱乙酰酶的抑制剂
公开(公告)号：WO2009018541A8
公开(公告)日：2010-03-04
申请号：PCT/US2008071999
申请日：2008-08-01
申请人： SOUTHERN RES INST , UNIV CORNELL , PENN STATE RES FOUND , H LEE MOFFITT CANCER CT AND RE , SECRIST JOHN A III , EALICK STEVE , BALE SHRIDHAR , PEGG ANTHONY E , MCCLOSKEY DIANE E , GUIDA WAYNE C
发明人： SECRIST JOHN A III , EALICK STEVE , BALE SHRIDHAR , PEGG ANTHONY E , MCCLOSKEY DIANE E , GUIDA WAYNE C
IPC分类号： A01N43/04
CPC分类号： C07H19/167 , A61K9/20
摘要： The crystal structure of the complex of S-adenosylmethionine methyl ester with h?doMetDC F223A, a mutant where the stacking of the aromatic rings of F7, adenine and F223 would be eliminated. The structure of this mutant with the ester shows that the ligand still maintains a syn conformation aided by pi-pi interactions to F7, hydrogen bonds to the backbone of Glu67, and electrostatic interactions. Several series of AdoMet substrate analogues with a variety of substituents at the 8 position of adenine were synthesized and analyzed for their ability to inhibit hAdoMetDC. To understand these results, virtual modeling of the enzyme inhibitor complexes and the crystal structures of human AdoMetDC with 5'-deoxy-5'-[N-methyl-N-[2- (aminooxy)ethyl]amino-8-rnethyl]adenosine (MAOEMA) and 5'-deoxy-5'-[N-methyl-N-[4- (aminooxy)butyl]amino-8-ethyl]adenosine (MAOBEA) at the active site have been determined experimentally.
摘要翻译： S-腺苷甲硫氨酸甲酯与h？doMetDC F223A的复合物的晶体结构，其中F7，腺嘌呤和F223的芳环的堆叠将被消除。该突变体与酯的结构显示配体仍然保持通过与F7的π-π相互作用，与Glu67的主链的氢键和静电相互作用的顺序构象。合成了多个在腺嘌呤8位具有多种取代基的AdoMet底物类似物，并分析其抑制hAdoMetDC的能力。为了理解这些结果，使用5'-脱氧-5' - [N-甲基-N- [2-（氨基氧基）乙基]氨基-8-甲基]腺苷的酶抑制剂复合物和人AdoMetDC的晶体结构的虚拟建模（MAOEMA）和5'-脱氧-5' - [N-甲基-N- [4-（氨基氧基）丁基]氨基-8-乙基]腺苷（MAOBEA）在活性位点已经通过实验测定。

5. 发明申请

WO2009117484A2 SMALL MOLECULE E2F INHIBITOR 审中-公开
标题翻译：小分子E2F抑制剂
公开(公告)号：WO2009117484A2
公开(公告)日：2009-09-24
申请号：PCT/US2009037510
申请日：2009-03-18
申请人： UNIV SOUTH FLORIDA , H LEE MOFFITT CANCER CT AND RE , CRESS DOUGLAS W , MA YIHONG
发明人： CRESS DOUGLAS W , MA YIHONG
IPC分类号： C07D215/16
CPC分类号： C07D215/26
摘要： A small molecular inhibitor of E2F (HLM006474) was identified using a computer-based virtual screen and the known crystal structure of the DNA bound E2F4/DP2 heterodimer. Treatment of multiple cell lines resulted in the loss of intracellular E2F4 DNA-binding activity. Overnight exposure to HLM006474 resulted in down regulation of total E2F4 protein as well as several known E2F targets. The effects of treatment on different cell lines included a reduction in cell proliferation and an increase in apoptosis. Apoptosis was induced in a manner distinct from cisplatin and doxorubicin. E2F4-null MEFs were less sensitive than wildtype counterparts to the apoptosis-inducing activity of the compound revealing its biological specificity. A375 cells were extremely sensitive to the apoptosis-inducing activity of the compound in two-dimensional culture and HLM006474 was a potent inhibitor of melanocytes proliferation and subsequent invasion in a three-dimensional tissue culture model system.
摘要翻译：使用基于计算机的虚拟屏幕和DNA结合的E2F4 / DP2异源二聚体的已知晶体结构鉴定了E2F的小分子抑制剂（HLM006474）。多种细胞系的治疗导致细胞内E2F4 DNA结合活性的丧失。过夜暴露于HLM006474导致总E2F4蛋白以及几种已知的E2F靶的下调。治疗对不同细胞系的作用包括细胞增殖的减少和凋亡的增加。以不同于顺铂和多柔比星的方式诱导细胞凋亡。 E2F4-null MEFs比野生型对照组对该化合物的细胞凋亡诱导活性敏感，表明其生物学特异性。 A375细胞对二维培养中化合物的细胞凋亡诱导活性非常敏感，HLM006474是三维组织培养模型系统中黑色素细胞增殖和随后侵袭的有效抑制剂。

6. 发明申请

WO2007013997A3 INHIBITION OF THE RAF/MEK/P-ERK PATHWAY FOR TREATING CANCER 审中-公开
标题翻译：用于治疗癌症的RAF / MEK / P-ERK途径的抑制
公开(公告)号：WO2007013997A3
公开(公告)日：2009-04-23
申请号：PCT/US2006028294
申请日：2006-07-21
申请人： H LEE MOFFITT CANCER CT AND RE , SEBTI SAID M
发明人： SEBTI SAID M
IPC分类号： C07K16/00 , C12N5/06 , G01N33/574
CPC分类号： A61K31/138 , G01N33/574
摘要： The invention disclosed herein provides for methods of treating cancer using inhibitors of the Raf/Mek/P-Erk 1/2 pathway. These inhibitors include B2AR agonists (such as ARA-211 (pirbuterol) and isoproterenol), adenylyl cyclase activators, cAMP analogs and Epac activators. The invention also provides methods for diagnosing cancer in an individual.
摘要翻译：本文公开的本发明提供了使用Raf / Mek / P-Erk 1/2途径的抑制剂治疗癌症的方法。这些抑制剂包括B2AR激动剂（例如ARA-211（吡布特罗）和异丙肾上腺素），腺苷酸环化酶激活剂，cAMP类似物和Epac激活剂。本发明还提供了诊断个体癌症的方法。

7. 发明申请

WO2006071812A3 PLATINUM IV COMPLEX INHIBITOR 审中-公开
标题翻译：铂IV络合物抑制剂
公开(公告)号：WO2006071812A3
公开(公告)日：2006-12-07
申请号：PCT/US2005046921
申请日：2005-12-23
申请人： H LEE MOFFITT CANCER CT AND RE , TURKSON JAMES , JOVE RICHARD , SEBTI SAID
发明人： TURKSON JAMES , JOVE RICHARD , SEBTI SAID
IPC分类号： A61K33/24
CPC分类号： A61K31/282 , A61K31/555 , A61K33/24 , A61K45/06 , A61K2300/00
摘要： The invention disclosed herein provides methods for diagnosing and treating diseases and/or conditions associated with dysregulated Stat3-mediated activity.
摘要翻译：本文公开的发明提供了用于诊断和治疗与调节异常的Stat3介导的活性相关的疾病和/或病症的方法。

8. 发明申请

WO2010091354A2 AKT TYROSINE 176 PHOSPHORYLATION CANCER BIOMARKER 审中-公开
标题翻译： AKT TYROSINE 176磷酸化生物标志物
公开(公告)号：WO2010091354A2
公开(公告)日：2010-08-12
申请号：PCT/US2010023487
申请日：2010-02-08
申请人： H LEE MOFFITT CANCER CT AND RE , MAHAJAN NUPAM P , MAHAJAN KIRAN N
发明人： MAHAJAN NUPAM P , MAHAJAN KIRAN N
IPC分类号： G01N33/68 , A61K31/7105 , C07K16/40 , C12Q1/68 , G01N33/574
CPC分类号： C07K16/40 , C07K16/44 , C12Q1/485 , G01N33/57407 , G01N33/57415 , G01N33/57423 , G01N33/57426 , G01N33/57434 , G01N33/57438 , G01N33/57449 , G01N2333/9121 , G01N2800/50 , G01N2800/52 , G01N2800/56
摘要： AKT/PKB kinase is a key signaling component of one of the most frequently activated pathways in cancer and is a major target of cancer drug development. The present study uncovered that growth factors binding to RTKs lead to activation of a non-receptor tyrosine kinase, Ack1 (TNK2), which directly phosphorylates AKT at a conserved tyrosine 176 residue. Tyr176-phosphorylated AKT binds to phosphatidic acid and localizes to the plasma membrane, leading to AKT activation. Expression levels of Tyr176-phosphorylated-AKT and Tyr284-phosphorylated-Ack1 were positively correlated with the severity of disease progression, and inversely correlated with the survival of breast, prostate, lung and pancreatic cancer patients.
摘要翻译： AKT / PKB激酶是癌症中最常激活途径之一的关键信号成分，是癌症药物开发的主要靶标。本研究发现结合RTK的生长因子导致非受体酪氨酸激酶Ack1（TNK2）的激活，其直接磷酸化保守的酪氨酸176残基上的AKT。 Tyr176磷酸化AKT与磷脂酸结合并定位于质膜，导致AKT活化。 Tyr176磷酸化AKT和Tyr284磷酸化Ack1的表达水平与疾病进展的严重程度呈正相关，与乳腺癌，前列腺癌，肺癌和胰腺癌患者的生存率呈负相关。

9. 发明申请

WO2010005534A3 PROTEASOME INHIBITORS FOR SELECTIVELY INDUCING APOPTOSIS IN CANCER CELLS 审中-公开
标题翻译：用于选择性诱导癌细胞凋亡的抑制剂
公开(公告)号：WO2010005534A3
公开(公告)日：2010-04-08
申请号：PCT/US2009003926
申请日：2009-06-30
申请人： H LEE MOFFITT CANCER CT AND RE , UNIV SOUTH FLORIDA , LAWRENCE HARSHANI , GE YIYU , SEBTI SAID M , GUIDA WAYNE
发明人： LAWRENCE HARSHANI , GE YIYU , SEBTI SAID M , GUIDA WAYNE
IPC分类号： A61K31/38 , A61K31/192 , A61K31/255 , A61P35/00
CPC分类号： C07C323/52 , C07C311/20 , C07C311/43 , C07C323/62 , C07C2602/10 , C07D213/76 , C07D231/42 , C07D239/69 , C07D261/16 , C07D277/52 , C07D285/135 , C07D333/34 , C07D409/12
摘要： The subject invention concerns compounds having activity as inhibitors of proteasomes and methods of using the subject compounds. In one embodiment, a compound of the invention has the chemical structure shown in Formula (I), wherein R1 is an organic cyclic ring structure bonded to a sulfonamide structure; R2 is H, halogen, alkyl, -NR6R7, or heteroalkyl; R3 is H, halogen, -OH, -O-alkyl, alkyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, -NO2, -NH2 or substituted amines; R4 is H, alkyl, heteroalkyl, aryl, or heteroaryl, any of which can be optionally substituted with one or more of -NO2, alkyl, heteroalkyl, aryl, or heteroaryl, or halogen; R5 is H, -OH, halogen, alkyl, aryl, heteroaryl, cycloalkyl, heterocycloalkyl, -O-alkyl, -O- aryl, heteroalkyl, -NO2, -NH2, or substituted amine; and R6 and R7 are independently H, O, alkyl, aryl, heterocycloalkyl, or heteroaryl, or together can form a heterocycloalkyl or a heteroaryl, any of which can be optionally substituted with one or more of -NO2, alkyl, heteroalkyl, aryl, or halogen; or a pharmaceutically acceptable salt or hydrate thereof. In another embodiment, a compound of the invention has the chemical structure shown in Formula (II), wherein Q, W, X, Y, Z are each independently carbon, oxygen, or nitrogen; R1 is H, or X1R8; R2 is heteroalkyl, which can be optionally substituted with one or more of -OH, halogen, -C(O)OR4, alkyl, heteroalkyl, heterocycloalkyl, or heteroaryl; R3 is heterocycloalkyl, aryl, heteroaryl, any of which can be optionally substituted with one or more of a halogen or -OH; and R4 is H or alkyl; R5 is halogen, alkyl or nitro; R6 is nitro, X2R9 or a halogen; R7 is H or alkyl; R8 is H, alkyl, aryl, CH2-alkyl-aryl, -alkyl-C(O)OH, or alkyl-tetrazole (aromatic and aliphatic heterocyclic groups); R9 is H or alkyl; X1 is oxygen, nitrogen, or sulfur; X2 is oxygen, nitrogen, or sulfur; or a pharmaceutically acceptable salt or hydrate thereof.
摘要翻译：本发明涉及具有作为蛋白酶体抑制剂的活性的化合物和使用本发明化合物的方法。在一个实施方案中，本发明的化合物具有式（I）所示的化学结构，其中R 1是与磺酰胺结构键合的有机环状结构; R2是H，卤素，烷基，-NR6R7或杂烷基; R 3是H，卤素，-OH，-O-烷基，烷基，环烷基，杂环烷基，芳基，杂芳基，-NO 2，-NH 2或取代的胺; R4是H，烷基，杂烷基，芳基或杂芳基，其中任何一个可以任选被一个或多个-NO 2，烷基，杂烷基，芳基或杂芳基或卤素取代; R5是H，-OH，卤素，烷基，芳基，杂芳基，环烷基，杂环烷基，-O-烷基，-O-芳基，杂烷基，-NO2，-NH2或取代的胺; 或者一起可以形成杂环烷基或杂芳基，其中任何一个可以任选被一个或多个-NO 2，烷基，杂烷基，芳基，杂芳基，杂芳基，或卤素; 或其药学上可接受的盐或水合物。在另一个实施方案中，本发明的化合物具有式（II）所示的化学结构，其中Q，W，X，Y，Z各自独立地为碳，氧或氮; R1是H或X1R8; R 2是杂烷基，其可任选被一个或多个-OH，卤素，-C（O）OR 4，烷基，杂烷基，杂环烷基或杂芳基取代; R 3是杂环烷基，芳基，杂芳基，其中任何一个可以任选被一个或多个卤素或-OH取代; R4为H或烷基; R5是卤素，烷基或硝基; R6是硝基，X2R9或卤素; R7是H或烷基; R8是H，烷基，芳基，CH2-烷基 - 芳基， - 烷基-C（O）OH或烷基 - 四唑（芳香族和脂肪族杂环基）。 R9为H或烷基; X1是氧，氮或硫; X2是氧，氮或硫; 或其药学上可接受的盐或水合物。

10. 发明申请

WO2009105746A3 TRIAZOLES AND PROCESSES FOR PRODUCING THE SAME 审中-公开
标题翻译：用于生产它们的三元共聚物和方法
公开(公告)号：WO2009105746A3
公开(公告)日：2009-11-19
申请号：PCT/US2009034845
申请日：2009-02-23
申请人： UNIV SOUTH FLORIDA , H LEE MOFFITT CANCER CT AND RE , MANETSCH ROMAN , WANG HONG-GANG , HU XIANGDONG , KULKARNI SAMEER , SUN JIAZHI G
发明人： MANETSCH ROMAN , WANG HONG-GANG , HU XIANGDONG , KULKARNI SAMEER , SUN JIAZHI G
IPC分类号： C07D249/02 , C07D249/04 , C07D249/06
CPC分类号： C07D249/06
摘要： The present disclosure relates to triazoles and processes for their preparation. The processes involve a target-guided synthesis approach, whereby an alkyne and an azide are reacted in the presence of a biological target protein, a Bcl-2 family protein, to form the triazole.
摘要翻译：本公开涉及三唑及其制备方法。该方法涉及靶向指导的合成方法，其中炔和叠氮化物在生物靶蛋白Bcl-2家族蛋白的存在下反应以形成三唑。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式