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公开(公告)号：US5420228A
公开(公告)日：1995-05-30
申请号：US182862
申请日：1994-01-14
摘要： A fluorescent-labelled bleomycin analog useful as a probe for measuring cellular uptake of bleomycin and bleomycin derivatives, including methods of making and using same. The analog may further be used as a therapeutic agent as well as a diagnostic tool.
摘要翻译： 可用作测量博来霉素和博来霉素衍生物的细胞摄取的探针的荧光标记的博来霉素类似物，包括制备和使用它们的方法。 该类似物还可用作治疗剂以及诊断工具。
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公开(公告)号：US09453049B2
公开(公告)日：2016-09-27
申请号：US14472966
申请日：2014-08-29
IPC分类号： A61K31/404 , A61K31/132 , C07D209/04 , C07C255/50 , C07C255/51 , C07K7/06 , C07K5/02 , C12N9/12 , C07C255/60 , C07C279/12 , C07D209/14 , C07K5/06 , C07K5/08 , C07K5/10 , A61K38/00
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Akt的一种肽和非肽抑制剂，其是致癌蛋白。 从Akt靶基质GSK-3的残基开始，对GSK-3残基的功能结构域进行了表征。 功能同源的非肽基团被GSK-3的氨基酸取代，产生能结合Akt的杂合肽 - 非肽和非肽化合物。 与肽对应物相比，非肽化合物显示出增加的稳定性和刚性，并且不易降解。 结合的非肽化合物对Akt具有抑制作用，类似于基于肽的Akt抑制剂。
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公开(公告)号：US09359347B2
公开(公告)日：2016-06-07
申请号：US13476098
申请日：2012-05-21
申请人： Jin Q. Cheng , Mei Sun , Said M. Sebti
发明人： Jin Q. Cheng , Mei Sun , Said M. Sebti
IPC分类号： C07D471/04 , C07H19/23
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，本发明的化合物抑制Akt蛋白的激酶活性和/或磷酸化水平。 本发明还涉及抑制或杀死其中Akt蛋白表达升高或组成型活化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 用于治疗人或动物的癌症或肿瘤，包括向人或动物施用有效量的式I化合物。
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公开(公告)号：US09174969B2
公开(公告)日：2015-11-03
申请号：US13055113
申请日：2009-07-21
申请人： Jie Wu , Nicholas J. Lawrence , Said M. Sebti
发明人： Jie Wu , Nicholas J. Lawrence , Said M. Sebti
IPC分类号： A61K31/496 , C07D209/08 , C07D215/36 , C07D405/06
CPC分类号： C07D405/06 , C07D209/08 , C07D215/36
摘要： The subject invention concerns methods and compounds for inhibiting Shp2. In one embodiment, a compound of the invention has a chemical structure as shown in formula I or II: wherein X, Y, and Z are independently N or S; R1 is cycloalkyl, heterocycloalkyl, aryl, or heteroaryl, any of which can be optionally substituted with one or more of halogen; alkyl; heteroalkyl; —COOH; —C(R3)3, wherein R3 can independently be any of —H or halogen; or —OR4, wherein R4 can be any of H, alkyl, or heteroalkyl; R2 is alkyl, alkylcarbonyl, heteroalkylcarbonyl, aryl, arylcarbonyl, heterocycloalkylcarbonyl, cycloalkylcarbonyl, or —C(O)NR6R7, any of which can be optionally substituted with one or more of halogen; alkyl; heteroalkyl; carbonyl; —OR4, wherein R4 can be —H, alkyl, or heteroalkyl; —OH; —C(R3)3, wherein R3 can independently be any of —H or halogen; aryl, which can be substituted with one or more of halogen or —OR4; heterocycloalkyl; or —C(O)OR5, wherein R5 can be —H or alkyl; R6 and R7 are independently —H, alkyl, heteroalkyl, aryl, or heteroaryl; and R′ is H or alkyl; or a pharmaceutically acceptable salt or hydrate thereof.
摘要翻译： 本发明涉及抑制Shp2的方法和化合物。 在一个实施方案中，本发明的化合物具有如式I或II所示的化学结构：其中X，Y和Z独立地为N或S; R 1是环烷基，杂环烷基，芳基或杂芳基，其中任何一个可以任选被一个或多个卤素取代; 烷基; 杂烷基; -COOH; -C（R 3）3，其中R 3可以独立地为-H或卤素; 或-OR 4，其中R 4可以是H，烷基或杂烷基中的任何一个; R 2是烷基，烷基羰基，杂烷基羰基，芳基，芳基羰基，杂环烷基羰基，环烷基羰基或-C（O）NR 6 R 7，其中任何一个可以任选被一个或多个卤素取代; 烷基; 杂烷基; 羰; -OR4，其中R4可以是-H，烷基或杂烷基; -哦; -C（R 3）3，其中R 3可以独立地为-H或卤素; 芳基，其可被一个或多个卤素或-OR 4取代; 杂环烷基; 或-C（O）OR 5，其中R 5可以是-H或烷基; R6和R7独立地是-H，烷基，杂烷基，芳基或杂芳基; 和R'是H或烷基; 或其药学上可接受的盐或水合物。
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公开(公告)号：US08901086B2
公开(公告)日：2014-12-02
申请号：US13463576
申请日：2012-05-03
申请人： Jin Q. Cheng , Said M. Sebti
发明人： Jin Q. Cheng , Said M. Sebti
IPC分类号： A61K31/70 , A61K31/7052 , A61K31/7064 , A61K39/395
CPC分类号： A61K39/39558 , A61K31/7064
摘要： This invention encompasses combination therapies including TCN, TCN-P, TCN-PM and/or related compounds and one or more additional anti-cancer agents, for example, taxanes a molecule that modulates the HER2/neu (erbB2) receptor, anthracyclin compounds, epidermal growth factor receptor inhibitor compounds, one or more platinum compounds and bortezomib and derivatives thereof and compositions with reduced toxicity for the treatment and prevention of tumors, cancer, and other disorders associated with abnormal cell proliferation.
摘要翻译： 本发明包括组合疗法，包括TCN，TCN-P，TCN-PM和/或相关化合物和一种或多种另外的抗癌剂，例如紫杉烷类调节HER2 / neu（erbB2）受体的分子，蒽环类化合物， 表皮生长因子受体抑制剂化合物，一种或多种铂化合物和硼替佐米及其衍生物和对治疗和预防与异常细胞增殖相关的肿瘤，癌症和其它病症的毒性降低的组合物。
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6.发明申请公开(公告)号：US20130157972A1
公开(公告)日：2013-06-20
申请号：US13453834
申请日：2012-04-23
申请人： Jin Q. CHENG , Said M. Sebti
发明人： Jin Q. CHENG , Said M. Sebti
IPC分类号： A61K31/7064 , A61K31/69
CPC分类号： A61K38/05 , A61K31/69 , A61K31/7064 , A61K31/7076
摘要： This application relates to combination therapies including triciribine and related compounds and bortezomib and derivatives thereof analogs and compositions with reduced toxicity for the treatment and prevention of tumors, cancer, and other disorders associated with abnormal cell proliferation.
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公开(公告)号：US08435959B2
公开(公告)日：2013-05-07
申请号：US11096082
申请日：2005-03-29
申请人： Jin Q. Cheng , Said M. Sebti
发明人： Jin Q. Cheng , Said M. Sebti
IPC分类号： A61K31/70 , A61K31/7052
CPC分类号： C07H17/02 , A61K31/7064
摘要： The inventors have determined, contrary to the prior art and experience, how to successfully use triciribine to treat tumors and cancer by one or a combination of (i) administering triciribine only to patients which according to a diagnostic test described below, exhibit enhanced sensitivity to the drug; (ii) use of a described dosage level that minimizes the toxicity of the drug but yet still exhibits efficacy; or (iii) use of a described dosage regimen that minimizes the toxicity of the drug.
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公开(公告)号：US08288369B2
公开(公告)日：2012-10-16
申请号：US11768373
申请日：2007-06-26
申请人： Mokenge P. Malafa , Said M. Sebti
发明人： Mokenge P. Malafa , Said M. Sebti
IPC分类号： A61K31/355 , A61K31/513 , A61K31/7052 , A61K31/7105 , A61P35/00
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-PACA2 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肿瘤性疾病如胰腺癌的方法; 即γ-生育三烯酚和δ-生育三烯酚。 这些化合物的抗肿瘤作用在体外和体内均显示出使用在裸鼠中异种移植的几种人胰腺癌细胞系和MIA-PACA2人胰腺癌细胞。 还公开了通过测量它们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的功效的方法。 还公开了相关化合物。
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9.发明申请公开(公告)号：US20110236471A1
公开(公告)日：2011-09-29
申请号：US13158060
申请日：2011-06-10
申请人： HEIDI KAY , Jay W. Palmer , Joseph A. Stanko , Said M. Sebti
发明人： HEIDI KAY , Jay W. Palmer , Joseph A. Stanko , Said M. Sebti
IPC分类号： A61K9/127 , C07F5/05 , C07F15/00 , A61K31/282 , A61K31/69 , A61K31/555 , A61K39/395 , A61K31/513 , A61K38/14 , A61K31/7048 , A61K31/506 , A61P35/00
CPC分类号： C07F15/0093
摘要： The subject invention concerns platinum complexes that exhibit antitumor cell and/or antiparasitic activity. The subject invention also concerns the use of platinum complexes of the invention to treat oncological and inflammatory disorders. The platinum complexes of the invention can also be used to treat or prevent infection by a virus or a bacterial or parasitic organism in vivo or in vitro.
摘要翻译： 本发明涉及显示抗肿瘤细胞和/或抗寄生虫活性的铂配合物。 本发明还涉及使用本发明的铂络合物来治疗肿瘤和炎性疾病。 本发明的铂络合物还可用于治疗或预防病毒或细菌或寄生生物在体内或体外的感染。
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公开(公告)号：US20110223154A1
公开(公告)日：2011-09-15
申请号：US12992556
申请日：2008-05-12
申请人： Jin Q. Cheng , Said M. Sebti
发明人： Jin Q. Cheng , Said M. Sebti
IPC分类号： A61K39/395 , A61P35/00
CPC分类号： A61K39/39558 , A61K31/7064
摘要： This invention encompasses combination therapies including TCN, TCN-P, TCN-PM and/or related compounds and one or more additional anti-cancer agents, for example, taxanes a molecule that modulates the HER2/neu (erbB2) receptor, anthracyclin compounds, epidermal growth factor receptor inhibitor compounds, one or more platinum compounds and bortezomib and derivatives thereof and compositions with reduced toxicity for the treatment and prevention of tumors, cancer, and other disorders associated with abnormal cell proliferation.
摘要翻译： 本发明包括组合疗法，包括TCN，TCN-P，TCN-PM和/或相关化合物和一种或多种另外的抗癌剂，例如紫杉烷类调节HER2 / neu（erbB2）受体的分子，蒽环类化合物， 表皮生长因子受体抑制剂化合物，一种或多种铂化合物和硼替佐米及其衍生物和对治疗和预防与异常细胞增殖相关的肿瘤，癌症和其它病症的毒性降低的组合物。
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