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1. 发明申请

US20160369247A1 SUBSTRATE-MIMETIC AKT INHIBITOR 有权
公开(公告)号：US20160369247A1
公开(公告)日：2016-12-22
申请号：US15251572
申请日：2016-08-30
申请人： Said M. Sebti , Jin Q. Cheng , Andrew D. Hamilton , Katherine Kayser-Bricker
发明人： Said M. Sebti , Jin Q. Cheng , Andrew D. Hamilton , Katherine Kayser-Bricker
IPC分类号： C12N9/12 , C07K7/02 , C07K5/02 , C07K7/06
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.

2. 发明授权

US08822524B2 Substrate-mimetic Akt inhibitor 有权
标题翻译：底物模拟Akt抑制剂
公开(公告)号：US08822524B2
公开(公告)日：2014-09-02
申请号：US12480329
申请日：2009-06-08
申请人： Said M. Sebti , Jin Q. Cheng , Andrew D. Hamilton , Katherine Kayser-Bricker
发明人： Said M. Sebti , Jin Q. Cheng , Andrew D. Hamilton , Katherine Kayser-Bricker
IPC分类号： A61K31/404 , A61K31/132 , C07D209/04 , C07C255/50 , C07C255/51
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。

3. 发明授权

US09453049B2 Substrate-mimetic Akt inhibitor 有权
标题翻译：底物模拟Akt抑制剂
公开(公告)号：US09453049B2
公开(公告)日：2016-09-27
申请号：US14472966
申请日：2014-08-29
申请人： Said M. Sebti , Jin Q. Cheng , Andrew D. Hamilton , Katherine Kayser-Bricker
发明人： Said M. Sebti , Jin Q. Cheng , Andrew D. Hamilton , Katherine Kayser-Bricker
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。

4. 发明申请

US20150004698A1 SUBSTRATE-MIMETIC AKT INHIBITOR 有权
标题翻译：基质 - 酮化酮抑制剂
公开(公告)号：US20150004698A1
公开(公告)日：2015-01-01
申请号：US14472966
申请日：2014-08-29
申请人： Said M. Sebti , Jin Q. Cheng , Andrew D. Hamilton , Katherine Kayser-Bricker
发明人： Said M. Sebti , Jin Q. Cheng , Andrew D. Hamilton , Katherine Kayser-Bricker
IPC分类号： C07K7/06 , C07K5/10 , C12N9/12 , C07C279/12 , C07C255/60 , C07D209/14 , C07K5/08 , C07K5/06
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。

5. 发明申请

US20100009397A1 SUBSTRATE-MIMETIC AKT INHIBITOR 有权
标题翻译：基质 - 酮化酮抑制剂
公开(公告)号：US20100009397A1
公开(公告)日：2010-01-14
申请号：US12480329
申请日：2009-06-08
申请人： Said M. Sebti , Jin Q. Cheng , Andrew D. Hamilton , Katherine Kayser-Bricker
发明人： Said M. Sebti , Jin Q. Cheng , Andrew D. Hamilton , Katherine Kayser-Bricker
IPC分类号： C12Q1/48 , C07K7/06 , C07C237/28 , C07C255/58 , C07D209/18
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。

6. 发明授权

US09359347B2 Inhibitors of Akt/PKB with anti-tumor activity 有权
标题翻译：具有抗肿瘤活性的Akt / PKB抑制剂
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。

7. 发明授权

US08901086B2 Compositions including triciribine and methods of use thereof 有权
标题翻译：组合物，包括triciribine及其使用方法
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。

8. 发明申请

US20130157972A1 COMPOSITIONS INCLUDING TRICIRIBINE AND BORTEZOMIB AND DERIVATIVES THEREOF AND METHODS OF USE THEREOF 有权
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.

9. 发明授权

US08435959B2 Effective treatment of tumors and cancer with triciribine and related compounds 有权
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.

10. 发明申请

US20110223154A1 COMPOSITIONS INCLUDING TRICIRIBINE AND METHODS OF USE THEREOF 审中-公开
标题翻译：组合物，包括其中的有关物质及其使用方法
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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