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公开(公告)号：US09238628B2
公开(公告)日：2016-01-19
申请号：US13913362
申请日：2013-06-07
发明人： Christopher John Burns , Andrew Donohue , John Thomas Feutrill , Thao Lien Thi Nguyen , Andrew Frederick Wilks , Jun Zeng
IPC分类号： C07D413/00 , A61K31/535 , C07D239/42 , C07D295/02 , C07D295/12 , C07D401/12 , C07D403/12 , C07D405/12 , C07D417/12 , C07D401/14
CPC分类号： C07D239/42 , C07D295/02 , C07D295/12 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D417/12
摘要： The present invention relates to phenyl amino pyrimidine compounds which are inhibitors of protein kinases including JAK kinases. In particular the compounds are selective for JAK2 kinases. The kinase inhibitors can be used in the treatment of kinase associated diseases such as immunological and inflammatory diseases including organ transplants; hyperproliferative diseases including cancer and myeloproliferative diseases; viral diseases; metabolic diseases; and vascular diseases.
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公开(公告)号：US20130137660A1
公开(公告)日：2013-05-30
申请号：US13747343
申请日：2013-01-22
IPC分类号： C07D241/20 , C07D401/14 , C07D409/14 , C07F9/6558 , C07D405/14 , C07D213/82 , C07D417/12 , C07D403/12 , C07D405/12 , C07D241/18 , C07D241/24 , C07D401/04 , C07D213/75 , C07D241/28 , C07D403/04 , C07D401/12
CPC分类号： C07D241/20 , C07D213/75 , C07D213/82 , C07D241/18 , C07D241/24 , C07D241/28 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/12 , C07D417/12 , C07F9/65583
摘要： The present invention relates to pyridines or pyrazines that inhibit kinases. In particular the compounds of the invention inhibit members of the class III PTK receptor family such as FMS (CSF-IR), c-KIT, PDGFRβ, PDGFRα or FLT3 and KDR, SRC, EphA2, EphA3, EphA8, FLT1, FLT4, HCK, LCK, PTK5 (FRK), SYK, DDR1 and DDR2 and RET. The compounds of the invention are useful in the treatment of kinase associated diseases such as immunological and inflammatory diseases; hyperproliferative diseases including cancer and diseases involving neo-angiogenesis; renal and kidney diseases; bone remodeling diseases; metabolic diseases; and vascular diseases.
摘要翻译： 本发明涉及抑制激酶的吡啶或吡嗪。 特别地，本发明的化合物抑制III类PTK受体家族的成员，例如FMS（CSF-IR），c-KIT，PDGFRβ，PDGFRα或FLT3和KDR，SRC，EphA2，EphA3，EphA8，FLT1，FLT4，HCK ，LCK，PTK5（FRK），SYK，DDR1和DDR2和RET。 本发明的化合物可用于治疗激酶相关疾病如免疫和炎性疾病; 过度增生性疾病，包括癌症和涉及新血管生成的疾病; 肾肾疾病; 骨重塑疾病; 代谢疾病; 和血管疾病。
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公开(公告)号：US09732046B2
公开(公告)日：2017-08-15
申请号：US14811503
申请日：2015-07-28
发明人： Christopher John Burns , Andrew Frederick Wilks , Michael Francis Harte , Harrison Sikanyika , Emmanuelle Fantino
IPC分类号： A61K31/53 , C07D253/07 , C07D213/74 , C07D239/42 , C07D241/20 , C07D401/12 , C07D401/14 , C07D403/12
CPC分类号： C07D253/07 , C07D213/74 , C07D239/42 , C07D241/20 , C07D401/12 , C07D401/14 , C07D403/12
摘要： Compounds of general formula (I), (II), (III) and (V) are described for use in modulating microtubule polymerization and in the treatment of associated disease states. Use of compounds (I), (III) and (V) in the treatment of kinase-associated disease states is also described. Further described are novel compounds of formula (II), (III) and (V).
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公开(公告)号：US20140005161A1
公开(公告)日：2014-01-02
申请号：US13830152
申请日：2013-03-14
IPC分类号： C07D491/107 , C07D491/08
CPC分类号： C07D491/107 , C07D413/08 , C07D491/08 , C07D498/08
摘要： The present invention relates to phenyl amino pyrimidine bicyclic compounds formula I which are inhibitors of protein kinases including JAK kinases. In particular the compounds are active against JAK1, JAK2, JAK3 and TYK2 kinases. The kinase inhibitors can be used in the treatment of kinase associated diseases such as immunological and inflammatory diseases including organ transplants; hyperproliferative diseases including cancer and myeloproliferative diseases; viral diseases; metabolic diseases; and vascular diseases.
摘要翻译： 本发明涉及作为蛋白激酶（包括JAK激酶）的抑制剂的苯基氨基嘧啶双环化合物式I。 特别地，这些化合物对JAK1，JAK2，JAK3和TYK2激酶具有活性。 激酶抑制剂可用于治疗激酶相关疾病，例如免疫学和炎性疾病，包括器官移植物; 过度增生性疾病，包括癌症和骨髓增生性疾病; 病毒性疾病 代谢疾病; 和血管疾病。
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公开(公告)号：US20160031835A1
公开(公告)日：2016-02-04
申请号：US14811503
申请日：2015-07-28
发明人： Christopher John Burns , Andrew Frederick Wilks , Michael Francis Harte , Harrison Sikanyika , Emmanuelle Fantino
IPC分类号： C07D253/07
CPC分类号： C07D253/07 , C07D213/74 , C07D239/42 , C07D241/20 , C07D401/12 , C07D401/14 , C07D403/12
摘要： Compounds of general formula (I), (II), (III) and (V) are described for use in modulating microtubule polymerisation and in the treatment of associated disease states. Use of compounds (I), (III) and (V) in the treatment of kinase-associated disease states is also described. Further described are novel compounds of formula (II), (III) and (V).
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公开(公告)号：US09029386B2
公开(公告)日：2015-05-12
申请号：US13747343
申请日：2013-01-22
IPC分类号： A61K31/435 , C07D213/74 , C07D241/20 , C07D213/75 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D409/14 , C07D413/12 , C07D417/12 , C07D213/82 , C07D241/18 , C07D241/24 , C07D241/28 , C07D405/12 , C07D405/14 , C07F9/6558
CPC分类号： C07D241/20 , C07D213/75 , C07D213/82 , C07D241/18 , C07D241/24 , C07D241/28 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/12 , C07D417/12 , C07F9/65583
摘要： Derivatives of pyridine of the formula wherein one of Y and A is CR and the other is N are kinase inhibitors useful in treating conditions associated with excess kinase activity.
摘要翻译： 下式吡啶的衍生物，其中Y和A之一是CR，另一个是N是可用于治疗与过量激酶活性相关的病症的激酶抑制剂。
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公开(公告)号：US20210309615A1
公开(公告)日：2021-10-07
申请号：US14960710
申请日：2015-12-07
发明人： Christopher John Burns , Andrew Craig Donohue , John Thomas Feutrill , Thao Lien Thi Nguyen , Andrew Frederick Wilks , Jun Zeng
IPC分类号： C07D239/42 , C07D295/02 , C07D295/12 , C07D401/12 , C07D403/12 , C07D405/12 , C07D417/12 , C07D401/14
摘要： The present invention relates to phenyl amino pyrimidine compounds which are inhibitors of protein kinases including JAK kinases. In particular the compounds are selective for JAK2 kinases. The kinase inhibitors can be used in the treatment of kinase associated diseases such as immunological and inflammatory diseases including organ transplants; hyperproliferative diseases including cancer and myeloproliferative diseases; viral diseases; metabolic diseases; and vascular diseases.
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公开(公告)号：US09139560B2
公开(公告)日：2015-09-22
申请号：US14194543
申请日：2014-02-28
发明人： Christopher John Burns , Andrew Frederick Wilks , Michael Francis Harte , Harrison Sikanyika , Emmanuelle Fantino
IPC分类号： A61K31/4965 , C07D241/20 , C07D401/12 , C07D213/74 , C07D239/42 , C07D253/07 , C07D401/14 , C07D403/12
CPC分类号： C07D253/07 , C07D213/74 , C07D239/42 , C07D241/20 , C07D401/12 , C07D401/14 , C07D403/12
摘要： Compounds of general formula (I), (II), (III) and (V) are described for use in modulating microtubule polymerization and in the treatment of associated disease states. Use of compounds (I), (III) and (V) in the treatment of kinase-associated disease states is also described. Further described are novel compounds of formula (II), (III) and (V).
摘要翻译： 描述了通式（I），（II），（III）和（V）的化合物用于调节微管聚合和治疗相关疾病状态。 还描述了化合物（I），（III）和（V）在激酶相关疾病状态的治疗中的用途。 进一步描述的是式（II），（III）和（V）的新化合物。
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公开(公告)号：US08809359B2
公开(公告)日：2014-08-19
申请号：US13830152
申请日：2013-03-14
IPC分类号： A01N43/54 , A61K31/505
CPC分类号： C07D491/107 , C07D413/08 , C07D491/08 , C07D498/08
摘要： The present invention relates to phenyl amino pyrimidine bicyclic compounds formula I which are inhibitors of protein kinases including JAK kinases. In particular the compounds are active against JAK1, JAK2, JAK3 and TYK2 kinases. The kinase inhibitors can be used in the treatment of kinase associated diseases such as immunological and inflammatory diseases including organ transplants; hyperproliferative diseases including cancer and myeloproliferative diseases; viral diseases; metabolic diseases; and vascular diseases.
摘要翻译： 本发明涉及作为蛋白激酶（包括JAK激酶）的抑制剂的苯基氨基嘧啶双环化合物式I。 特别地，这些化合物对JAK1，JAK2，JAK3和TYK2激酶具有活性。 激酶抑制剂可用于治疗激酶相关疾病，例如免疫学和炎性疾病，包括器官移植物; 过度增生性疾病，包括癌症和骨髓增生性疾病; 病毒性疾病 代谢疾病; 和血管疾病。
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公开(公告)号：US08765755B2
公开(公告)日：2014-07-01
申请号：US13706293
申请日：2012-12-05
发明人： David Gerard Bourke , Christopher John Burns , Anthony Nicholas Cuzzupe , John Thomas Feutrill , Marcel Robert Kling , Tracy Leah Nero
IPC分类号： C07D487/04 , C07D495/04
CPC分类号： C07D495/04 , C07D471/04 , C07D487/04 , C07D513/04
摘要： The present invention relates to N-containing heterocyclic compounds that are inhibitors of protein kinases including JAK kinases. In particular, the compounds are selective for JAK1, JAK2, JAK3 or TYK2 kinases and combinations thereof such as JAK1 and JAK2. The kinase inhibitors can be used in the treatment of kinase associated diseases such as immunological and inflammatory diseases including organ transplants; hyperproliferative diseases including cancer and myeloproliferative diseases; viral diseases; metabolic diseases; and vascular diseases.
摘要翻译： 本发明涉及作为包括JAK激酶的蛋白激酶抑制剂的含氮杂环化合物。 特别地，这些化合物对JAK1，JAK2，JAK3或TYK2激酶及其组合如JAK1和JAK2是选择性的。 激酶抑制剂可用于治疗激酶相关疾病，例如免疫学和炎性疾病，包括器官移植物; 过度增生性疾病，包括癌症和骨髓增生性疾病; 病毒性疾病 代谢疾病; 和血管疾病。
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