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公开(公告)号：US11185535B2
公开(公告)日：2021-11-30
申请号：US17180234
申请日：2021-02-19
发明人： Michael D. Kaufman , Scott Bone , Corey Bloom , Fred Jordan
IPC分类号： A61K9/46 , A61K31/4375 , A61K9/16 , A61K9/20
摘要： Provided herein is an amorphous compound represented by Formula (I): and compositions thereof, which are useful in the treatment of disorders related to the activity of the c-KIT and PDGFRα kinases, and oncogenic forms thereof.
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公开(公告)号：US20210275518A1
公开(公告)日：2021-09-09
申请号：US17193707
申请日：2021-03-05
发明人： Rodrigo Ruiz Soto , Keisuke Kuida , Haroun Achour
IPC分类号： A61K31/4709 , A61K31/337 , A61K31/475 , A61K31/436 , A61K31/404 , A61K31/704 , A61K31/44 , A61K31/513 , A61K31/7068 , A61K31/519 , A61K31/495 , A61K33/243 , A61K31/282 , A61K31/675 , A61K31/427 , A61K31/517 , A61K31/496 , A61K31/4545 , A61K31/506 , A61K31/437 , A61K31/454 , A61K31/502 , A61K31/55 , A61P35/00
摘要： Described herein are methods of treating various disorders in patients in need thereof, comprising administering to the patient the compound of Formula (I) or a pharmaceutically acceptable salt thereof. Exemplary disorders that can be treated by the methods described herein include gynecologic carcinosarcomas, endometrial adenocarcinomas, mesotheliomas, ovarian cancers, pancreatic ductal adenocarcinomas, and lung cancers.
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公开(公告)号：US20210196693A1
公开(公告)日：2021-07-01
申请号：US17180241
申请日：2021-02-19
发明人： Michael D. Kaufman , Scott Bone , Corey Bloom , Fred Jordan
IPC分类号： A61K31/4375 , A61K9/10 , A61K9/00 , A61K47/38
摘要： Provided herein are low impurity compositions comprising a compound represented by Formula (I): which are useful in the treatment of disorders related to the activity of the c-KIT and PDGFRα kinases, and oncogenic forms thereof.
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公开(公告)号：US20210196692A1
公开(公告)日：2021-07-01
申请号：US17180234
申请日：2021-02-19
发明人： Michael D. Kaufman , Scott Bone , Corey Bloom , Fred Jordan
IPC分类号： A61K31/4375 , A61K9/16 , A61K9/20
摘要： Provided herein is an amorphous compound represented by Formula (I): and compositions thereof, which are useful in the treatment of disorders related to the activity of the c-KIT and PDGFRα kinases, and oncogenic forms thereof.
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![USE OF 1-[4-BROMO-5-[1-ETHYL-7-(METHYLAMINO)-2-OXO-1,2-DIHYDRO-1,6-NAPHTHYRIDIN-3-YL]-2-FLUOROPHENYL]-3-PHENYLUREA AND ANALOGS FOR THE TREATMENT OF CANCERS ASSOCIATED WITH GENETIC ABNORMALITIES IN PLATELET DERIVED GROWTH FACTOR RECEPTOR ALPHA](/abs-image/US/2021/01/21/US20210015801A1/abs.jpg.150x150.jpg)
公开(公告)号：US20210015801A1
公开(公告)日：2021-01-21
申请号：US17028591
申请日：2020-09-22
IPC分类号： A61K31/4375 , A61P35/04 , A61K31/495
摘要： The present disclosure relates to the use of 1-[4-bromo-5-[1-ethyl-7-(methylamino)-2-oxo-1,2-dihydro-1,6-naphthyridin-3-yl]-2-fluorophenyl]-3-phenylurea or 1-(5-(7-amino-1-ethyl-2-oxo-1,2-dihydro-1,6-naphthyridin-3-yl)-4-bromo-2-fluorophenyl)-3-phenylurea in the treatment of cancers. Specifically, the disclosure is directed to methods of inhibiting PDGFR kinases and treating cancers and disorders associated with inhibition of PDGFR kinases including lung adenocarcinoma, squamous cell lung cancer, glioblastoma, pediatric glioma, astrocytomas, sarcomas, gastrointestinal stromal tumors, malignant peripheral nerve sheath sarcoma, intimal sarcomas, hypereosinophilic syndrome, idiopathic hypereosinophilic syndrome, chronic eosinophilic leukemia, eosinophilia-associated acute myeloid leukemia, or lymphoblastic T-cell lymphoma.
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26.发明授权Imidazolidinones and analogs exhibiting anti-cancer and anti-proliferative activities 有权具有抗癌和抗增殖活性的咪唑啉酮和类似物公开(公告)号：US09133183B2
公开(公告)日：2015-09-15
申请号：US14214134
申请日：2014-03-14
发明人： Daniel L. Flynn , Michael D. Kaufman , Thiwanka Samarakoon , Timothy Malcolm Caldwell , Lakshminarayana Vogeti , YuMi Ahn , William C. Patt , Karen M. Yates
IPC分类号： A61K31/497 , C07D417/14 , C07D401/14 , C07D405/14 , C07D413/14
CPC分类号： C07D417/14 , C07B59/002 , C07B2200/05 , C07D401/14 , C07D405/14 , C07D413/14
摘要： Described are compounds of Formula I which find utility in the treatment of cancer, autoimmune diseases and metabolic bone disorders through inhibition of c-FMS (CSF-1R), c-KIT, and/or PDGFR kinases. These compounds also find utility in the treatment of other mammalian diseases mediated by c-FMS, c-KIT, or PDGFR kinases.
摘要翻译： 描述了通过抑制c-FMS（CSF-1R），c-KIT和/或PDGFR激酶在治疗癌症，自身免疫疾病和代谢性骨骼疾病中有用的式I化合物。 这些化合物也可用于治疗由c-FMS，c-KIT或PDGFR激酶介导的其它哺乳动物疾病。
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27.发明授权Pyridone amides and analogs exhibiting anti-cancer and anti-proliferative activities 有权表现出抗癌和抗增殖活性的吡啶酮酰胺和类似物公开(公告)号：US09012635B2
公开(公告)日：2015-04-21
申请号：US14214127
申请日：2014-03-14
IPC分类号： C07D319/02 , C07D401/00 , C07D401/14 , A61K31/505 , C07D239/02
CPC分类号： C07D401/14 , A61K31/505 , C07D239/02 , C07D401/00
摘要： Compounds useful in the treatment of mammalian cancers and especially human cancers according to Formula I are disclosed. Pharmaceutical compositions and methods of treatment employing the compounds disclosed herein are also disclosed.
摘要翻译： 公开了可用于治疗哺乳动物癌症，特别是根据式I的人类癌症的化合物。 还公开了使用本文公开的化合物的药物组合物和治疗方法。
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28.发明授权Cyclopropyl dicarboxamides and analogs exhibiting anti-cancer and anti-proliferative activities 有权表现出抗癌和抗增殖活性的环丙基二甲酰胺和类似物公开(公告)号：US08637672B2
公开(公告)日：2014-01-28
申请号：US13559170
申请日：2012-07-26
IPC分类号： C07D213/30 , C07D213/28 , C07D401/12 , C07D401/14 , A61K31/44 , A61P35/00
CPC分类号： C07D401/12 , A61K31/44 , A61K31/505 , C07D213/75 , C07D239/47
摘要： The disclosed compounds are useful in the treatment of mammalian cancers and especially human cancers. Compounds, pharmaceutical compositions, and methods of Formula I are disclosed: or a pharmaceutically acceptable salt, hydrate, solvate, enantiomer, stereoisomer, or tautomer thereof.
摘要翻译： 所公开的化合物可用于治疗哺乳动物癌症，特别是人类癌症。 公开了化合物，药物组合物和式I的方法：或其药学上可接受的盐，水合物，溶剂合物，对映异构体，立体异构体或其互变异构体。
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29.发明申请PYRIDONE AMIDES AND ANALOGS EXHIBITING ANTI-CANCER AND ANTI-PROLIFERATIVE ACTIVITIES 有权吡咯烷酮和类似物展示抗癌和抗增生活性公开(公告)号：US20120172382A1
公开(公告)日：2012-07-05
申请号：US13098247
申请日：2011-04-29
IPC分类号： A61K31/444 , A61K31/506 , A61P35/00 , A61P11/00 , A61P25/28 , A61P27/02 , A61P29/00 , A61P11/06 , C07D401/14 , A61P1/00
CPC分类号： C07D401/14
摘要： Compounds useful in the treatment of mammalian cancers and especially human cancers according to Formula I are disclosed. Pharmaceutical compositions and methods of treatment employing the compounds disclosed herein are also disclosed.
摘要翻译： 公开了可用于治疗哺乳动物癌症，特别是根据式I的人类癌症的化合物。 还公开了使用本文公开的化合物的药物组合物和治疗方法。
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公开(公告)号：US20090312349A1
公开(公告)日：2009-12-17
申请号：US11721026
申请日：2005-12-23
申请人： Daniel L. Flynn , Peter A. Petillo
发明人： Daniel L. Flynn , Peter A. Petillo
IPC分类号： A61K31/519 , C07D401/12 , A61K31/4439 , C07D471/04 , A61P35/00 , C12N9/12
CPC分类号： C07D487/04 , C07D209/46 , C07D231/40 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/12 , C07D409/14 , C07D413/10 , C07D417/10 , C07D417/12 , C07D417/14 , C12Q1/485
摘要： Novel compounds and methods of using those compounds for the treatment of inflammatory conditions, hyperproliferative diseases, cancer, and diseases characterized by hyper-vascularization are provided. In a preferred embodiment, modulation of the activation state of p38 kinase protein, abl kinase protein, bcr-abl kinase protein, braf kinase protein, VEGFR kinase protein, or PDGFR kinase protein comprises the step of contacting said kinase protein with the novel compounds.
摘要翻译： 提供了新型化合物和使用这些化合物治疗炎性病症，过度增殖性疾病，癌症和以血管新生血管瘤为特征的疾病的方法。 在优选的实施方案中，调节p38激酶蛋白，abl激酶蛋白，bcr-abl激酶蛋白，braf激酶蛋白，VEGFR激酶蛋白或PDGFR激酶蛋白的激活状态包括使所述激酶蛋白与新化合物接触的步骤。
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