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21. 发明申请

WO2008070823A2 SUBSTRATE-MIMETIC AKT INHIBITOR 审中-公开
标题翻译：基质 - 模拟AKT抑制剂
公开(公告)号：WO2008070823A2
公开(公告)日：2008-06-12
申请号：PCT/US2007086751
申请日：2007-12-07
申请人： UNIV SOUTH FLORIDA , UNIV YALE , SEBTI SAID M , CHENG JIN Q , HAMILTON ANDREW D , KAYSER KATHERINE
发明人： SEBTI SAID M , CHENG JIN Q , HAMILTON ANDREW D , KAYSER KATHERINE
IPC分类号： A61K38/08
CPC分类号： C12N9/12 , A61K31/132 , A61K31/404 , A61K38/00 , C07C255/50 , C07C255/51 , C07C255/60 , C07C279/12 , C07C2601/16 , C07D209/04 , C07D209/14 , C07K5/02 , C07K5/0207 , C07K5/06 , C07K5/08 , C07K5/10 , C07K7/02 , C07K7/06 , C12N9/1205 , C12Y207/11001
摘要： Disclosed herein is a species of peptide and non-peptide inhibitors of Akt, an oncogenic protein. Beginning with a residue of Akt target substrate GSK-3, the functional domains of the GSK-3 residue were characterized. Functionally homologous non-peptide groups were substituted for the amino acids of the GSK-3 creating a hybrid peptide-non-peptide and non-peptide compounds capable of binding to Akt. The non-peptide compounds show increased stability and rigidity compared to peptide counterparts and are less susceptible to degradation. The bound non-peptide compounds exhibit an inhibitory effect on Akt, similar to peptide-based Akt inhibitors.
摘要翻译：本文公开了一种致癌蛋白Akt的肽和非肽抑制剂。从Akt靶底物GSK-3的残基开始，表征GSK-3残基的功能结构域。功能上同源的非肽基团取代了GSK-3的氨基酸，形成了能够结合Akt的杂合肽 - 非肽和非肽化合物。与肽对应物相比，非肽化合物显示增加的稳定性和刚性，并且不易降解。与基于肽的Akt抑制剂类似，结合的非肽化合物对Akt表现出抑制作用。

22. 发明申请

WO2008070697A2 STAT3 INHIBITOR HAVING ANTI-CANCER ACTIVITY AND ASSOCIATED METHODS 审中-公开
标题翻译：具有抗癌活性的STAT3抑制剂和相关方法
公开(公告)号：WO2008070697A2
公开(公告)日：2008-06-12
申请号：PCT/US2007086453
申请日：2007-12-05
申请人： UNIV CENTRAL FLORIDA RES FOUND , TURKSON JAMES , HAMILTON ANDREW D , JOVE RICHARD , SEBTI SAID M
发明人： TURKSON JAMES , HAMILTON ANDREW D , JOVE RICHARD , SEBTI SAID M
IPC分类号： C07F9/653
CPC分类号： C07F9/653
摘要： A small-molecule Stat3 dimerization inhibitor, S3I-M2001. is described and the dynamics of intracellular processing of activated Stat3 within the context of the biochemical and biological effects of the Stat3 chemical probe inhibitor are elucidated. S3I-M2001 is a newly-identified oxazole-based peptidomimetic of the Stat3 Src Homology (SH) 2 domain-binding phosphotyrosine peptide that selectively disrupts active Stat3:Stat3 dimers. Stat3-dependent malignant transformation, survival, and migration and invasion of mouse and human cancer cells harboring persistently-activated Stat3 were inhibited by S3I-M2001. S3I-M2001 inhibited Stat3-dependent transcriptional regulation of tumor survival genes, such as Bcl-xL. The disclosed compound is useful as a new potential treatment for certain cancers.
摘要翻译：小分子Stat3二聚化抑制剂，S3I-M2001。描述了在Stat3化学探针抑制剂的生物化学和生物学效应范围内激活的Stat3的细胞内加工动力学。 S3I-M2001是Stat3 Src同源性（SH）2结构域结合磷酸酪氨酸肽的新鉴定的基于恶唑的肽模拟物，其选择性破坏活性Stat3：Stat3二聚体。 S3I-M2001抑制了Stat3依赖性恶性转化，存活以及携带持续激活Stat3的小鼠和人癌细胞的迁移和侵袭。 S3I-M2001抑制肿瘤存活基因如Bcl-xL的Stat3依赖性转录调控。所公开的化合物可用作某些癌症的新型潜在治疗剂。

23. 发明申请

WO2008060581A2 COMPOSITIONS INCLUDING TRICIRIBINE AND TRASTUZUMAB AND METHODS OF USE THEREOF 审中-公开
标题翻译：包括TRICUIBA和TRASTUZUMAB的组合物及其使用方法
公开(公告)号：WO2008060581A2
公开(公告)日：2008-05-22
申请号：PCT/US2007023963
申请日：2007-11-15
申请人： CLEVELAND CLINIC FOUNDATION , GREENLEAF DANIEL , AKINSANMI LAWRENCE , CHENG JIN Q , SEBTI SAID M
发明人： GREENLEAF DANIEL , AKINSANMI LAWRENCE , CHENG JIN Q , SEBTI SAID M
CPC分类号： A61K31/7064 , A61K39/395 , A61K39/39558 , A61K2300/00
摘要： This application relates to combination therapies including triciribine and related compounds and trastuzumab or a salt thereof and compositions with reduced toxicity for the treatment and prevention of tumors, cancer, and other disorders associated with abnormal cell roliferation.
摘要翻译：本申请涉及组合疗法，包括三苯呋嗪和相关化合物以及曲妥珠单抗或其盐以及对治疗和预防与异常细胞增殖有关的肿瘤，癌症和其它病症的毒性降低的组合物。

24. 发明申请

WO0197828A3 RHOB AS A SUPPRESSOR OF CANCER CELL GROWTH AND CELL TRANSFORMATION 审中-公开
标题翻译： RHOB作为癌细胞生长抑制因子和细胞转化
公开(公告)号：WO0197828A3
公开(公告)日：2003-01-09
申请号：PCT/US0119432
申请日：2001-06-18
申请人： UNIV SOUTH FLORIDA , SEBTI SAID M
发明人： SEBTI SAID M
IPC分类号： A61K38/46 , A61K48/00 , A61P35/00 , C12N9/16 , C12N15/55
CPC分类号： C12N9/16 , A61K38/00 , A61K48/00 , C12Y306/01
摘要： The protein RhoB and its variants as a supressor of cancer cell growth, inhibitor of malignant cell transformation, and modulator of oncogenic signaling, wherein introducing RhoB directly, or indirectly via a nucleic acid, into a malignantly transformed cell or a cancerous cell decreases phosphorylation of Erk and Akt proteins inhibiting the PI3-kinase/Akt cell survival pathway and promoting apoptotic cell death. Methods and compositions are disclosed of administering to cancer patients, a prophylactic treatment to minimize the risk of malignant transformation, and advantageous combination of RhoB therapy with existing cancer treatments. The protein RhoB and the variants of the present invention are prenylated with either geranylgeranyl or farnesyl, and provision is made for selection of the prenylating moiety.
摘要翻译： RhoB及其变体作为癌细胞生长的抑制剂，恶性细胞转化的抑制剂和致癌信号传导调节剂，其中RhoB直接或间接地通过核酸引入恶性转化的细胞或癌细胞中，从而降低磷酸化 Erk和Akt蛋白抑制PI3激酶/ Akt细胞存活途径并促进凋亡细胞死亡。公开了给予癌症患者的方法和组合物，其是使恶性转化的风险最小化的预防性治疗，以及RhoB治疗与现有癌症治疗的有利组合。蛋白质RhoB和本发明的变体用香叶基香叶基或法呢基进行去甲基化，并且提供选择预结构部分。

25. 发明申请

WO2009009793A2 INHIBITORS OF AKT/PKB WITH ANTI-TUMOR ACTIVITY 审中-公开
标题翻译： AKT / PKB抑制剂具有抗肿瘤活性
公开(公告)号：WO2009009793A2
公开(公告)日：2009-01-15
申请号：PCT/US2008069974
申请日：2008-07-14
申请人： UNIV SOUTH FLORIDA , CHENG JIN Q , SUN MEI , SEBTI SAID M
发明人： CHENG JIN Q , SUN MEI , SEBTI SAID M
IPC分类号： A61K31/517 , A61K31/13 , A61K31/53
CPC分类号： C07D471/04 , C07H19/23
摘要： The subject invention concerns materials and methods for inhibiting the Akt/PKB pathway. In one embodiment, a compound of the invention inhibits kinase activity and/or phosphorylation levels of Akt proteins. The subject invention also concerns methods for inhibiting or killing a cancer cell or other cell in which expression of an Akt protein is elevated or constitutively active, comprising contacting the cell with an effective amount of a compound of formula I. The subject invention also concerns methods for treating cancer or a tumor in a person or animal comprising administering an effective amount of a compound of formula I to the person or animal.
摘要翻译：本发明涉及用于抑制Akt / PKB途径的材料和方法。在一个实施方案中，本发明化合物抑制Akt蛋白的激酶活性和/或磷酸化水平。本发明还涉及用于抑制或杀死其中Akt蛋白的表达升高或组成性活性的癌细胞或其他细胞的方法，包括使细胞与有效量的式I化合物接触。本发明还涉及方法用于治疗人或动物中的癌症或肿瘤，所述方法包括给予人或动物有效量的式I化合物。

26. 发明申请

WO2008070833A2 USE OF SH2 STAT3/STAT1 PEPTIDOMIMETICES AS ANTICANCER DRUGS 审中-公开
标题翻译：使用SH2 STAT3 / STAT1作为抗药物的肽
公开(公告)号：WO2008070833A2
公开(公告)日：2008-06-12
申请号：PCT/US2007086779
申请日：2007-12-07
申请人： UNIV SOUTH FLORIDA , UNIV YALE , SEBTI SAID M , HAMILTON ANDREW D , TURKSON JAMES , JOVE RICHARD
发明人： SEBTI SAID M , HAMILTON ANDREW D , TURKSON JAMES , JOVE RICHARD
IPC分类号： A61K38/04
CPC分类号： C07K5/06078 , A61K38/00
摘要： The subject invention concerns compositions and methods for blocking cancer cell growth or proliferation and/or inducing cancer cell death. Compositions of the present invention are peptidomimetics that inhibit STAT function. Peptidomimetics of the invention display selective inhibition of specific STAT isoform homo-dimerization. The peptidomimetic probes of STAT1 function, described herein, provide the means to preferentially inhibit STAT1 over STAT3 through the exploration of the C-terminus.
摘要翻译：本发明涉及用于阻断癌细胞生长或增殖和/或诱导癌细胞死亡的组合物和方法。本发明的组合物是抑制STAT功能的肽模拟物。本发明的肽模拟物显示特异性STAT同种型同二聚化的选择性抑制。本文所述的STAT1功能的拟肽探针提供了通过探索C末端优先抑制STAT1的STAT1功能的方法。

27. 发明申请

WO2008002611A3 DELTA-TOCOTRIENOL TREATMENT AND PREVENTION OF PANCREATIC CANCER 审中-公开
标题翻译： DELTA-TOCOTRIENOL治疗和预防胰腺癌
公开(公告)号：WO2008002611A3
公开(公告)日：2008-05-29
申请号：PCT/US2007014912
申请日：2007-06-27
申请人： UNIV SOUTH FLORIDA , MALAFA MOKENGE P , SEBTI SAID M
发明人： MALAFA MOKENGE P , SEBTI SAID M
IPC分类号： A61K36/00 , A61P37/00
CPC分类号： A61K31/355 , A61K31/513 , A61K31/7052 , A61K31/7105 , C12Q1/6886 , C12Q2600/158 , G01N33/5011 , G01N2333/4739 , G01N2800/52
摘要： Methods are disclosed for treating neoplastic disorders, such as pancreatic cancer, using tocotrienols; namely, gamma-tocotrienol and delta tocotrienol. The antitumorogenic effects of these compounds are shown both in vitro and in vivo using several human pancreatic cancer cell lines and MIA- PAC A2 human pancreatic cancer cells xenografted in nude mice. Also disclosed are methods of testing the efficacy of potential chemotherapeutic agents by measuring their effect on surrogate endpoint biomarkers, such as Ki-67 and p27. Associated compounds are also disclosed.
摘要翻译：公开了使用生育三烯酚治疗赘生性疾病如胰腺癌的方法; 即γ-生育三烯酚和δ生育三烯酚。使用在裸鼠中异种移植的几种人类胰腺癌细胞系和MIA-PAC A2人类胰腺癌细胞，体外和体内显示了这些化合物的抗肿瘤作用。还公开了通过测量其对替代终点生物标志物如Ki-67和p27的作用来测试潜在化学治疗剂功效的方法。还公开了相关化合物。

28. 发明申请

WO2007062222A3 INHIBITION OF CELL PROLIFERATION 审中-公开
标题翻译：抑制细胞增殖
公开(公告)号：WO2007062222A3
公开(公告)日：2008-01-03
申请号：PCT/US2006045410
申请日：2006-11-22
申请人： UNIV SOUTH FLORIDA , SEBTI SAID M , CHELLAPPAN SRIKUMAR , LAWRENCE NICHOLAS JAMES
发明人： SEBTI SAID M , CHELLAPPAN SRIKUMAR , LAWRENCE NICHOLAS JAMES
IPC分类号： A61K39/00 , A61K39/395
CPC分类号： C07C323/45 , C07C279/06 , C07C335/32 , C07D213/53 , C07D215/12 , C07D233/30 , C07D233/84 , C07D235/28 , C07D249/12 , C07D249/14 , C07D277/40 , C07D277/42 , C07D317/56 , C07D317/58
摘要： The disclosed modulators of Rb:Raf-1 interactions are potent, selective disruptors of Rb:Raf-1 binding, with IC 50 values ranging from 80 nM to 500 nM. Further, these compounds are surprisingly effective in inhibiting a wide variety of cancer cells, including osteosarcoma, epithelial lung carcinoma, non small cell lung carcinoma, three different pancreatic cancer cell lines, two different glioblastoma cell lines, metastatic breast cancer, melanoma, and prostate cancer. Moreover, the disclosed compounds effectively disrupt angiogenesis and significantly inhibited tumors in nude mice derived from human epithelial lung carcinoma tumors. Accordingly, the disclosed compounds, pharmaceutical compositions comprising the compounds, methods of inhibiting cell proliferation, methods of treating subjects with cancer, and methods of preparing the disclosed compounds are provided.
摘要翻译：所公开的Rb：Raf-1相互作用的调节剂是Rb：Raf-1结合的有效的选择性破坏剂，80nM至500nM的IC 50 N值。此外，这些化合物在抑制多种癌细胞方面令人惊奇地有效，包括骨肉瘤，上皮性肺癌，非小细胞肺癌，三种不同的胰腺癌细胞系，两种不同的胶质母细胞瘤细胞系，转移性乳腺癌，黑素瘤和前列腺癌症。此外，所公开的化合物有效地破坏了血管发生，并显着抑制了源自人上皮性肺癌肿瘤的裸鼠中的肿瘤。因此，提供了所公开的化合物，包含该化合物的药物组合物，抑制细胞增殖的方法，治疗患有癌症的受试者的方法以及制备所公开的化合物的方法。

29. 发明申请

WO2007092278A3 WITHACNISTIN COMPOUNDS FOR TREATMENT OF CANCER 审中-公开
标题翻译：用于治疗癌症的抗坏血酸化合物
公开(公告)号：WO2007092278A3
公开(公告)日：2007-12-06
申请号：PCT/US2007002827
申请日：2007-02-02
申请人： UNIV SOUTH FLORIDA , SEBTI SAID M
发明人： SEBTI SAID M
IPC分类号： A61K31/58
CPC分类号： A61K31/585 , A61K31/12 , A61K31/58 , A61K45/06 , A61K2300/00
摘要： The subject invention pertains to the treatment of tumors and cancerous tissues and the prevention of tumorigenesis and malignant transformation through the modulation of STAT3 intracellular signaling. The subject invention concerns pharmaceutical compositions containing one or more withacnistin compounds, or a pharmaceutically acceptable salt or derivative thereof. In one embodiment, the subject invention concerns a composition comprising a mixture of withacnistin, 3-methoxy-2,3-dihydrowithacnistin, and 3-ethoxy-2,3-dihydrowithacnistin, or a salt or derivative of any of the foregoing.,Another aspect of the invention concerns methods of inhibiting the growth of a tumor by administering one or more withacnistin compounds, or a pharmaceutically acceptable salt or derivative thereof, to a patient, wherein the tumor is characterized by the constitutive activation of the STAT3 intracellular signaling pathway. The present invention further pertains to methods of moderating the STAT3 signaling pathway in vitro or in vivo using one or more withacnistin compounds, or a pharmaceutically acceptable salt or derivative thereof.
摘要翻译：本发明涉及通过调节STAT3细胞内信号传导来治疗肿瘤和癌组织以及预防肿瘤发生和恶性转化。本发明涉及含有一种或多种维他命原素化合物或其药学上可接受的盐或衍生物的药物组合物。在一个实施方案中，本发明涉及一种组合物，所述组合物包含三氯生黄素，3-甲氧基-2,3-二氢化黄素和3-乙氧基-2,3-二氢化黄霉素的混合物，或任何前述物质的盐或衍生物。本发明的一个方面涉及通过向患者施用一种或多种益生菌素化合物或其药学上可接受的盐或衍生物来抑制肿瘤生长的方法，其中所述肿瘤的特征在于STAT3细胞内信号传导途径的组成型活化。本发明进一步涉及使用一种或多种维他命原素化合物或其药学上可接受的盐或衍生物体外或体内调节STAT3信号传导途径的方法。

30. 发明申请

WO2007117699A2 INHIBITION OF SHP2/PTPN11 PROTEIN TYROSINE PHOSPHATASE BY NSC-87877, NSC-117199 AND THEIR ANALOGS 审中-公开
标题翻译： NSC-87877，NSC-117199及其类似物对SHP2 / PTPN11蛋白酪氨酸磷酸化酶的抑制作用
公开(公告)号：WO2007117699A2
公开(公告)日：2007-10-18
申请号：PCT/US2007008876
申请日：2007-04-09
申请人： UNIV SOUTH FLORIDA , H LEE MOFFITT CANCER CT AND RE , WU JIE , LAWRENCE NICHOLAS JAMES , SEBTI SAID M , LAWRENCE HARSHANI RITHMA
发明人： WU JIE , LAWRENCE NICHOLAS JAMES , SEBTI SAID M , LAWRENCE HARSHANI RITHMA
IPC分类号： A61K31/405
CPC分类号： A61K31/405 , C07D209/40
摘要： Compounds and associated methods for inhibiting a protein tyrosine phosphatase. By a combination of experimental and virtual screenings of the NCI Diversity Set chemical library, NSC-87877 and NSC-117199 have been identified as Shp2 PTP inhibitors. Significantly, NSC-87877 is active in cell-based assays and has no detectable off-target effects in the EGF-stimulated Erkl/2 activation pathway. Additionally, a number of analogs of NSC-1 17199 have been produced. These analogs exhibit enhanced protein tyrosine phosphatase inhibition and arc found to be potent and/or selectiv e inhibitors of Shp l and/or Shp2 protein tyrosine phosphatases.
摘要翻译：用于抑制蛋白质酪氨酸磷酸酶的化合物和相关方法。通过NCI多样性集化学库的实验和虚拟筛选的组合，NSC-87877和NSC-117199已被鉴定为Shp2 PTP抑制剂。显着地，NSC-87877在基于细胞的测定中是有活性的，并且在EGF刺激的Erk1 / 2激活途径中没有检测到的脱靶作用。此外，已经生产了许多NSC-17199的类似物。这些类似物表现出增强的蛋白酪氨酸磷酸酶抑制，并且发现弧是Shp1和/或Shp2蛋白酪氨酸磷酸酶的有效和/或选择性抑制剂。

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