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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/2022/11/24/US20220370423A1/abs.jpg.150x150.jpg)
公开(公告)号：US20220370423A1
公开(公告)日：2022-11-24
申请号：US17845275
申请日：2022-06-21
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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公开(公告)号：US20220265622A1
公开(公告)日：2022-08-25
申请号：US17735741
申请日：2022-05-03
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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公开(公告)号：US20220257574A1
公开(公告)日：2022-08-18
申请号：US17735820
申请日：2022-05-03
发明人： Michael D. Kaufman , Scott Bone , Corey Bloom , Fred Jordan
IPC分类号： A61K31/4375 , A61K47/38 , A61K9/00 , A61K9/10
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：US20220031677A1
公开(公告)日：2022-02-03
申请号：US17504133
申请日：2021-10-18
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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公开(公告)号：US20210145805A1
公开(公告)日：2021-05-20
申请号：US16943821
申请日：2020-07-30
发明人： Daniel L. Flynn , Bryan D. Smith , Anu Gupta
IPC分类号： A61K31/4375 , A61K45/06 , A61P35/04
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, or a pharmaceutically acceptable salt thereof, in combination with a MAPKAP kinase inhibitor for the treatment of cancers, including c-KIT-mediated cancers, such as GIST.
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公开(公告)号：US09457019B2
公开(公告)日：2016-10-04
申请号：US14535900
申请日：2014-11-07
IPC分类号： A61K38/00 , A61K31/4709 , C07D401/14 , A61K45/06 , A61K31/337 , A61K31/351 , C07K16/40 , A61K31/357
CPC分类号： A61K31/4709 , A61K9/0019 , A61K31/185 , A61K31/337 , A61K31/351 , A61K31/357 , A61K45/06 , A61K47/64 , C07D401/14 , C07K16/40 , A61K2300/00
摘要： The present invention relates to methods of inhibiting TIE2 kinase useful in the treatment of tumor growth, invasiveness, intravazation, dissemination, metastasis, and immunosuppression. Specifically, the invention relates to methods of using 1-(3-tert-butyl-1-(quinolin-6-yl)-1H-pyrazol-5-yl)-3-(2-fluoro-4-(2-(methylcarbamoyl)pyridin-4-yloxy)phenyl)urea and salts thereof of Formula I.
摘要翻译： 本发明涉及抑制TIE2激酶治疗肿瘤生长，侵袭，体内，传播，转移和免疫抑制的方法。 具体地说，本发明涉及使用1-（3-叔丁基-1-（喹啉-6-基）-1H-吡唑-5-基）-3-（2-氟-4-（2-（ 甲基氨基甲酰基）吡啶-4-基氧基）苯基）脲及其盐。
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7.发明授权N-acyl-N′-(pyridin-2-yl) ureas and analogs exhibiting anti-cancer and anti-proliferative activities 有权N-酰基-N' - （吡啶-2-基）脲和表现出抗癌和抗增殖活性的类似物公开(公告)号：US09382228B2
公开(公告)日：2016-07-05
申请号：US14214185
申请日：2014-03-14
发明人： Daniel L. Flynn , Timothy Malcolm Caldwell , Michael D. Kaufman , William C. Patt , Thiwanka Samarakoon , Lakshminarayana Vogeti , Karen M. Yates
IPC分类号： C07D213/65 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/14
CPC分类号： C07D401/14 , C07D405/14 , C07D413/14 , C07D417/14
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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公开(公告)号：US09334267B2
公开(公告)日：2016-05-10
申请号：US14383799
申请日：2013-03-05
发明人： Daniel L. Flynn , Michael D. Kaufman , Lakshminarayana Vogeti , Scott Wise , Wei-Ping Lu , Bryan Smith , James R. Henry , Philip A. Hipskind , Sheng-Bin Peng
IPC分类号： C07D471/12 , C07D471/04
CPC分类号： C07D471/04 , C07D471/12
摘要： This invention provides compounds of Formula I: (Formula I should be inserted here) or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising a compound of Formula I; and use of a compound of Formula I for treating specified cancers.
摘要翻译： 本发明提供了式I化合物：（式I应该在此插入）或其药学上可接受的盐; 包含式I化合物的药物组合物; 以及式I化合物用于治疗特定癌症的用途。
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公开(公告)号：US09187474B2
公开(公告)日：2015-11-17
申请号：US14383803
申请日：2013-03-05
发明人： Daniel L. Flynn , Michael D. Kaufman , Lakshminarayana Vogeti , Scott Wise , Wei-Ping Lu , Bryan Smith , Timothy Malcolm Caldwell , William C. Patt , James R. Henry , Philip A. Hipskind , Sheng-Bin Peng
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： This invention provides compounds of Formula (I) or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising a compound of Formula (I); and use of a compound of Formula (I) for treating specified cancers.
摘要翻译： 本发明提供式（I）化合物或其药学上可接受的盐; 包含式（I）化合物的药物组合物; 以及式（I）化合物用于治疗特定癌症的用途。
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10.发明申请2-AMINOPYRIMIDIN-6-ONES AND ANALOGS EXHIBITING ANTI-CANCER AND ANTI-PROLIFERATIVE ACTIVITIES 有权2-氨基嘌呤-6-ONES和模拟物展示抗癌和抗增殖活性公开(公告)号：US20140275085A1
公开(公告)日：2014-09-18
申请号：US14214171
申请日：2014-03-14
发明人： Michael D. Kaufman , Daniel L. Flynn , YuMi Ahn , Lakshminarayana Vogeti , Timothy Malcolm Caldwell
IPC分类号： C07D401/14 , C07D405/14
CPC分类号： C07D401/14 , A61K31/506 , C07D405/14
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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