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1. 发明申请

US20200283421A1 5-BROMO-INDIRUBINS 审中-公开
公开(公告)号：US20200283421A1
公开(公告)日：2020-09-10
申请号：US16790611
申请日：2020-02-13
申请人： City of Hope , National and Kapodistrian University of Athens
发明人： Richard Jove , Sangkil Nam , David Horne , Jun Xie , Alexios Leandros Skaltsounis , Marina Kritsanida , Nicolas Gaboriaud-Kolar
IPC分类号： C07D403/14 , C07D401/14 , A61K31/496 , A61K31/4439 , A61K31/404 , A61K45/06 , C07D209/48 , C07D209/40 , C07D401/04
摘要： Disclosed herein inter alia are compositions and methods for treating cancer using 5-Br-indirubin derivatives.

2. 发明申请

US20160068517A1 5-BROMO-INDIRUBINS 审中-公开
公开(公告)号：US20160068517A1
公开(公告)日：2016-03-10
申请号：US14850579
申请日：2015-09-10
申请人： City of Hope , National and Kapodistrian University of Athens
发明人： Richard Jove , Sangkil Nam , David Horne , Jun Xie , Alexios Leandros Skaltsounis , Marina Kritsanida , Nicolas Gaboriaud-Kolar
IPC分类号： C07D403/14 , C07D209/40 , A61K45/06 , C07D401/14 , A61K31/4439 , A61K31/404 , A61K31/496
CPC分类号： C07D403/14 , A61K31/404 , A61K31/4439 , A61K31/496 , A61K45/06 , C07D209/40 , C07D209/48 , C07D401/04 , C07D401/14
摘要： Disclosed herein inter alia are compositions and methods for treating cancer using 5-Br-indirubin derivatives.
摘要翻译：本文公开了尤其是使用5-Br-靛玉红衍生物治疗癌症的组合物和方法。

3. 发明授权

US10435367B2 Indirubin derivatives, and uses thereof 有权
公开(公告)号：US10435367B2
公开(公告)日：2019-10-08
申请号：US13826204
申请日：2013-03-14
申请人： CITY OF HOPE , THE NATIONAL AND KAPODISTRIAN UNIVERSITY OF ATHENS
发明人： Sangkil Nam , Richard Jove , Leandros Skaltsounis
IPC分类号： C07D209/40 , C07D401/14
摘要： Indirubin is the major active anti-tumor component of a traditional Chinese herbal medicine used for treatment of chronic myelogenous leukemia (CML). Indirubin derivatives (IRDs) potently reduce the viabilities of various cancer cells and affect kinase activities. IRDs disclosed herein provide new therapeutics for cancer and conditions regulated by the kinase activities.

4. 发明授权

US11306072B2 5-bromo-indirubins 有权
公开(公告)号：US11306072B2
公开(公告)日：2022-04-19
申请号：US16790611
申请日：2020-02-13
申请人： City of Hope , National and Kapodistrian University of Athens
发明人： Richard Jove , Sangkil Nam , David Horne , Jun Xie , Alexios Leandros Skaltsounis , Marina Kritsanida , Nicolas Gaboriaud-Kolar
IPC分类号： C07D403/14 , C07D401/04 , C07D209/40 , C07D209/48 , A61K45/06 , A61K31/404 , A61K31/4439 , A61K31/496 , C07D401/14
摘要： Disclosed herein inter alia are compositions and methods for treating cancer using 5-Br-indirubin derivatives.

5. 发明申请

US20180170915A1 5-BROMO-INDIRUBINS 审中-公开
公开(公告)号：US20180170915A1
公开(公告)日：2018-06-21
申请号：US15898151
申请日：2018-02-15
申请人： City of Hope , National and Kapodistrian University of Athens
发明人： Richard Jove , Sangkil Nam , David Horne , Jun Xie , Alexios Leandros Skaltsounis , Marina Kritsanida , Nicolas Gaboriaud-Kolar
IPC分类号： C07D403/14 , A61K45/06 , C07D401/14 , A61K31/496 , C07D401/04 , A61K31/404 , C07D209/48 , C07D209/40 , A61K31/4439
CPC分类号： C07D403/14 , A61K31/404 , A61K31/4439 , A61K31/496 , A61K45/06 , C07D209/40 , C07D209/48 , C07D401/04 , C07D401/14
摘要： Disclosed herein inter alia are compositions and methods for treating cancer using 5-Br-indirubin derivatives.

6. 发明授权

US11524937B2 Indirubin derivatives, and uses thereof 有权
公开(公告)号：US11524937B2
公开(公告)日：2022-12-13
申请号：US16594894
申请日：2019-10-07
申请人： CITY OF HOPE , THE NATIONAL AND KAPODISTRIAN UNIVERSITY OF ATHENS
发明人： Sangkil Nam , Richard Jove , Leandros Skaltsounis
IPC分类号： C07D209/40 , C07D401/14
摘要： Indirubin is the major active anti-tumor component of a traditional Chinese herbal medicine used for treatment of chronic myelogenous leukemia (CML). Indirubin derivatives (IRDs) potently reduce the viabilities of various cancer cells and affect kinase activities. IRDs disclosed herein provide new therapeutics for cancer and conditions regulated by the kinase activities.

7. 发明申请

US20200032255A1 METHODS AND COMPOSITIONS FOR THE TREATMENT OF CANCER OR OTHER DISEASES 审中-公开
公开(公告)号：US20200032255A1
公开(公告)日：2020-01-30
申请号：US16294537
申请日：2019-03-06
申请人： CITY OF HOPE
发明人： Hua Yu , Marcin Kortylewski , Richard Jove , Piotr Marek Swiderski , John J. Rossi
IPC分类号： C12N15/113 , A61K31/7105 , A61K31/713 , C07H21/02 , A61K47/54 , A61K47/55 , C07K14/47 , A61K47/61 , A61K47/64
摘要： The present invention relates to methods and compositions for the treatment of diseases, including cancer, infectious diseases and autoimmune diseases. The present invention also relates to methods and compositions for improving immune function. More particularly, the present invention relates to multifunctional molecules that are capable of being delivered to cells of interest for the treatment of diseases and for the improvement in immune function.

8. 发明申请

US20180155367A1 ETP DERIVATIVES 审中-公开
公开(公告)号：US20180155367A1
公开(公告)日：2018-06-07
申请号：US15796363
申请日：2017-10-27
申请人： City of Hope , The Regents of the University of California
发明人： Larry Eugene Overman , Marcus Baumann , Sangkil Nam , David Horne , Richard Jove , Jun Xie , Claudia Kowolik
IPC分类号： C07D513/18 , A61K31/44 , A61K31/706 , A61K31/7068 , A61K45/06 , C07D487/04 , A61K31/548
CPC分类号： C07D513/18 , A61K31/44 , A61K31/548 , A61K31/706 , A61K31/7068 , A61K45/06 , C07D487/04 , A61K2300/00
摘要： Provided herein, inter alia, is the synthesis of ETP derivatives. The uses of the ETP derivatives described herein include treatment of cancer.

9. 发明授权

US09828342B2 Isatin derivatives, pharmaceutical compositions thereof, and methods of use thereof 有权
公开(公告)号：US09828342B2
公开(公告)日：2017-11-28
申请号：US13776374
申请日：2013-02-25
申请人： CITY OF HOPE , THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
发明人： David A. Horne , Richard Jove , Christopher Lincoln , Sangkil Nam , Larry Overman , Jun Xie
IPC分类号： C07D209/38 , C07D401/10 , C07D401/04
CPC分类号： C07D209/38 , C07D401/04 , C07D401/10
摘要： One aspect of the invention relates to novel isatin derivative compounds and the pharmaceutical composition thereof. Another aspect of the invention relates to methods of using the isatin derivative compounds disclosed herein and the pharmaceutical compositions thereof. In certain embodiments, the method is used to treat a cancer or a tumor in a subject including, without limitation, prostate cancer, melanoma, pancreatic cancer, ovarian cancer, and lymphoma. In certain embodiment, the method is used to treat a condition in a subject that can be regulated by the activation of one or more proteins such as EGFR, Erk1/2, Her2/Neu, Jak2, Src, Stat3, Akt, Cyclin B1, and Cdc25C. In certain embodiment, the method is used to treat a condition in a subject that can be regulated by the disruption of microtubule formations.

10. 发明申请

US20130210834A1 INDIRUBIN DERIVATIVES AND USES THEREOF IN TREATING CHRONIC MYELOGENOUS LEUKEMIA 有权
标题翻译： INDIRUBIN衍生物及其在治疗慢性髓性白血病中的应用
公开(公告)号：US20130210834A1
公开(公告)日：2013-08-15
申请号：US13758921
申请日：2013-02-04
申请人： CITY OF HOPE
发明人： Richard Jove , Sangkil Nam , Alexios-Leandros Skaltsounis
IPC分类号： C07D209/40 , C07D403/14
CPC分类号： C07D209/40 , C07D209/34 , C07D403/14
摘要： Indirubin is the major active anti-tumor component of a traditional Chinese herbal medicine used for treatment of chronic myelogenous leukemia (CML). One aspect of the invention relates to a method of treating CML using at least one indirubin derivative compound or a pharmaceutical composition thereof. Indirubin derivatives (IRDs) potently inhibited Signal Transducer and Activator of Transcription 5 (Stat5) protein in CML cells. Compound IRD 810 inhibits Bcr-Abl/Stat5 or Src/Stat5 signaling in human KCL-22 CML and imatinib-resistant human KCL-22 CML cells expressing the T315I mutant Bcr-Abl. Previous studies indicate that SFKs cooperate with Bcr-Abl to activate downstream Stat5 signaling. Activation of Stat5 was strongly blocked by IRD 810 in CML cells. IRDs disclosed herein have been identified as potent inhibitors of Bcr-Abl/Stat5 or SFK/Stat5 signaling pathway. IRDs disclosed herein are new therapeutics for wild type or T315I mutant Bcr-Abl-positive CML patients, and may also treat other solid tumors, including prostate cancer and lymphoma.
摘要翻译：靛玉红是用于治疗慢性骨髓性白血病（CML）的中草药的主要活性抗肿瘤成分。本发明的一个方面涉及使用至少一种靛玉红衍生物化合物或其药物组合物治疗CML的方法。靛玉红衍生物（IRD）在CML细胞中有效抑制了转录5（Stat5）蛋白的信号转导和激活因子。化合物IRD 810抑制表达T315I突变体Bcr-Abl的人KCL-22 CML和伊马替尼耐药性人KCL-22 CML细胞中的Bcr-Abl / Stat5或Src / Stat5信号传导。以前的研究表明SFKs与Bcr-Abl合作激活下游Stat5信号传导。 CCR5的激活被CML细胞中的IRD 810强烈阻断。本文公开的IRD已被鉴定为Bcr-Abl / Stat5或SFK / Stat5信号通路的有效抑制剂。本文公开的IRD是野生型或T315I突变型Bcr-Abl阳性CML患者的新治疗剂，还可治疗其他实体瘤，包括前列腺癌和淋巴瘤。

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