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公开(公告)号：US09452998B2
公开(公告)日：2016-09-27
申请号：US14818778
申请日：2015-08-05
IPC分类号： C07D401/14 , A61K31/497 , C07D413/14
CPC分类号： C07D401/14 , A61K31/497 , C07D413/14
摘要： PKC inhibitors are disclosed. The PKC inhibitors are useful for treating PKC associated diseases, including certain cancers. The PKC inhibitors have improved efficacy at lower dosage amounts to achieve tumor regression, improved potency, PK profile, absorption, gastrointestinal tolerance and kinase selectivity.
摘要翻译： 公开了PKC抑制剂。 PKC抑制剂可用于治疗PKC相关疾病，包括某些癌症。 PKC抑制剂在较低剂量下具有改善的功效以实现肿瘤消退，改善效力，PK分布，吸收，胃肠道耐受和激酶选择性。
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2.发明申请NOVEL 2-PIPERIDIN-1-YL-ACETAMIDE COMPOUNDS FOR USE AS TANKYRASE INHIBITORS 有权新型2-哌啶-1-基乙酰胺化合物用作丹麦酯抑制剂公开(公告)号：US20150025070A1
公开(公告)日：2015-01-22
申请号：US14154161
申请日：2012-07-13
申请人： Atwood Kim Cheung , Donovan Noel Chin , Jianmei Fan , Karen Marie Miller-Moslin , Michael David Shultz , Troy D. Smith , Ronald Charles Tomlinson , Bakary-Barry Toure , Michael Scott Visser
发明人： Atwood Kim Cheung , Donovan Noel Chin , Jianmei Fan , Karen Marie Miller-Moslin , Michael David Shultz , Troy D. Smith , Ronald Charles Tomlinson , Bakary-Barry Toure , Michael Scott Visser
IPC分类号： C07D491/052 , C07D493/04 , C07D401/12
CPC分类号： C07D491/052 , A61K31/453 , A61K31/4545 , C07D401/12 , C07D409/14 , C07D493/04
摘要： The present invention provides for compounds of formula (I): wherein R1-R5 and L are defined herein. The present invention also provides for pharmaceutical compositions and combinations comprising a compound of formula (I) as well as for the use of such compounds as tankyrase inhibitors and in the treatment of Wnt signaling and tankyrase 1 and 2 signaling related disorders which include, but are not limited to, cancer.
摘要翻译： 本发明提供式（I）化合物：其中R1-R5和L在本文中定义。 本发明还提供药物组合物和组合物，其包含式（I）化合物以及使用这些化合物作为阻断酶抑制剂和用于治疗Wnt信号传导和阻断酶1和2信号传导相关疾病，其包括但是是 不限于癌症。
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公开(公告)号：US20160347737A1
公开(公告)日：2016-12-01
申请号：US15237880
申请日：2016-08-16
IPC分类号： C07D401/14 , A61K31/497
CPC分类号： C07D401/14 , A61K31/497 , C07D413/14
摘要： PKC inhibitors are disclosed. The PKC inhibitors are useful for treating PKC associated diseases, including certain cancers. The PKC inhibitors have improved efficacy at lower dosage amounts to achieve tumor regression, improved potency, PK profile, absorption, gastrointestinal tolerance and kinase selectivity.
摘要翻译： 公开了PKC抑制剂。 PKC抑制剂可用于治疗PKC相关疾病，包括某些癌症。 PKC抑制剂在较低剂量下具有改善的功效以实现肿瘤消退，改善效力，PK分布，吸收，胃肠道耐受和激酶选择性。
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公开(公告)号：US20160046605A1
公开(公告)日：2016-02-18
申请号：US14818778
申请日：2015-08-05
IPC分类号： C07D401/14
CPC分类号： C07D401/14 , A61K31/497 , C07D413/14
摘要： PKC inhibitors are disclosed. The PKC inhibitors are useful for treating PKC associated diseases, including certain cancers. The PKC inhibitors have improved efficacy at lower dosage amounts to achieve tumor regression, improved potency, PK profile, absorption, gastrointestinal tolerance and kinase selectivity.
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5.发明申请COMPOUNDS FOR INHIBITING THE INTERACTION OF BCL2 WITH BINDING PARTNERS 审中-公开用于抑制BCL2与结合合作伙伴相互作用的化合物公开(公告)号：US20140357666A1
公开(公告)日：2014-12-04
申请号：US14366854
申请日：2012-12-12
申请人： Michael Scott Visser , Naeem Yusuff
发明人： Michael Scott Visser , Naeem Yusuff
IPC分类号： C07D409/14 , A61K31/4725 , C07D401/10
CPC分类号： C07D409/14 , A61K31/4725 , C07D401/10
摘要： The present invention relates to compounds of formula I: in which R1, R2, R3 and R4 are as defined in the Summary of the Invention. Compounds of formula I are capable of disrupting the BCL-2 interations with proteins containing a BH3 domain. Disrupting this interaction can restore the anti-apoptotic function of BCL-2 in cancer cells and tumor tissue expressing BCL-2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancerous diseases.
摘要翻译： 本发明涉及式I化合物：其中R 1，R 2，R 3和R 4如发明概述中所定义。 式I的化合物能够破坏含有BH3结构域的蛋白质的BCL-2相互作用。 破坏这种相互作用可以恢复BCL-2在癌细胞和表达BCL-2的肿瘤组织中的抗凋亡功能。 本发明还提供了制备本发明化合物的方法，包含这些化合物的药物制剂和使用这些化合物治疗癌性疾病的方法。
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公开(公告)号：US20120165298A1
公开(公告)日：2012-06-28
申请号：US13394525
申请日：2010-09-08
IPC分类号： A61K31/635 , C07D487/04 , A61P35/00 , A61P29/00 , C07D471/04 , C07D498/08
CPC分类号： C07D471/04
摘要： The present invention includes novel compound and methods of treating a disease or disorder by antagonizing Bcl-2 family proteins, particularly compounds of formula (I): or pharmaceutically acceptable salt thereof, as well as methods of treating a disease, disorder, or syndrome associated with Bcl-2 inhibition, particularly hyperproliferative diseases. The present invention also includes pharmaceutical compositions including compounds of formula I and pharmaceutically acceptable salts thereof.
摘要翻译： 本发明包括新型化合物和通过拮抗Bcl-2家族蛋白，特别是式（I）化合物或其药学上可接受的盐来治疗疾病或病症的方法，以及治疗疾病，病症或综合征相关的方法 Bcl-2抑制，特别是过度增生性疾病。 本发明还包括包含式I化合物及其药学上可接受的盐的药物组合物。
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7.发明授权公开(公告)号：US09181266B2
公开(公告)日：2015-11-10
申请号：US14154161
申请日：2012-07-13
申请人： Atwood Kim Cheung , Donovan Noel Chin , Jianmei Fan , Karen Marie Miller-Moslin , Michael David Shultz , Troy D Smith , Ronald Charles Tomlinson , Bakary-Barry Toure , Michael Scott Visser , Zhuoliang Chen
发明人： Atwood Kim Cheung , Donovan Noel Chin , Jianmei Fan , Karen Marie Miller-Moslin , Michael David Shultz , Troy D Smith , Ronald Charles Tomlinson , Bakary-Barry Toure , Michael Scott Visser , Zhuoliang Chen
IPC分类号： C07D401/12 , C07D409/14 , A61K31/453 , A61K31/4545 , C07D491/052 , C07D493/04
CPC分类号： C07D491/052 , A61K31/453 , A61K31/4545 , C07D401/12 , C07D409/14 , C07D493/04
摘要： The present invention provides for compounds of formula (I): wherein R1-R5 and L are defined herein. The present invention also provides for pharmaceutical compositions and combinations comprising a compound of formula (I) as well as for the use of such compounds as tankyrase inhibitors and in the treatment of Wnt signaling and tankyrase 1 and 2 signaling related disorders which include, but are not limited to, cancer.
摘要翻译： 本发明提供式（I）化合物：其中R1-R5和L在本文中定义。 本发明还提供药物组合物和组合物，其包含式（I）化合物以及使用这些化合物作为阻断酶抑制剂和用于治疗Wnt信号传导和阻断酶1和2信号传导相关疾病，其包括但是是 不限于癌症。
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8.发明授权Sulfonamides as inhibitors of Bcl-2 family proteins for the treatments of cancer 有权磺酰胺作为Bcl-2家族蛋白的抑制剂用于治疗癌症公开(公告)号：US08809352B2
公开(公告)日：2014-08-19
申请号：US13394525
申请日：2010-09-08
IPC分类号： A01N43/62 , A61K31/55 , A61K31/497 , A01N43/90 , A61K31/519 , A01N43/64 , A61K31/41 , C07D471/00 , C07D487/00 , C07D471/04
CPC分类号： C07D471/04
摘要： The present invention includes novel compound and methods of treating a disease or disorder by antagonizing Bcl-2 family proteins, particularly compounds of formula (I): or pharmaceutically acceptable salt thereof, as well as methods of treating a disease, disorder, or syndrome associated with Bcl-2 inhibition, particularly hyperproliferative diseases. The present invention also includes pharmaceutical compositions including compounds of formula I and pharmaceutically acceptable salts thereof.
摘要翻译： 本发明包括新型化合物和通过拮抗Bcl-2家族蛋白，特别是式（I）化合物或其药学上可接受的盐来治疗疾病或病症的方法，以及治疗疾病，病症或综合征相关的方法 Bcl-2抑制，特别是过度增生性疾病。 本发明还包括包含式I化合物及其药学上可接受的盐的药物组合物。
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