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![PYRIDO[3,4-B]PYRAZINE DERIVATIVES AS SYK INHIBITORS](/abs-image/US/2014/01/02/US20140005188A1/abs.jpg.150x150.jpg)
公开(公告)号：US20140005188A1
公开(公告)日：2014-01-02
申请号：US14004375
申请日：2012-03-08
申请人： Francis Louis Atkinson , Stephen John Atkinson , Michael David Barker , Clement Douault , Neil Stuart Garton , John Liddle , Vipulkumar Kantibhai Patel , Alexander G. Preston , Tracy Jane Shipley , David Matthew Wilson , Robert J. Watson
发明人： Francis Louis Atkinson , Stephen John Atkinson , Michael David Barker , Clement Douault , Neil Stuart Garton , John Liddle , Vipulkumar Kantibhai Patel , Alexander G. Preston , Tracy Jane Shipley , David Matthew Wilson , Robert J. Watson
IPC分类号： C07D471/04 , C07D487/04
CPC分类号： C07D471/04 , C07D487/04 , C07D519/00
摘要： A compound of formula (I): or a salt thereof; which is an inhibitor of spleen tyrosine kinase (Syk) and therefore potentially of use in treating diseases resulting from inappropriate activation of mast cells, macrophages, and B-cells and related inflammatory responses and tissue damage, for instance inflammatory disease and/or allergic disorders, and in cancer therapy, specifically heme malignancies, and autoimmune conditions.
摘要翻译： 式（I）的化合物或其盐; 其是脾脏酪氨酸激酶（Syk）的抑制剂，因此潜在地用于治疗由肥大细胞，巨噬细胞和B细胞的不适当活化引起的疾病以及相关的炎症反应和组织损伤，例如炎性疾病和/或过敏性疾病 ，以及癌症治疗，特别是血红素恶性肿瘤和自身免疫病症。
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2.发明申请7-(lH-PYRAZOL-4-YL)-1,6-NAPHTHYRIDINE COMPOUNDS AS SYK INHIBITORS 失效7-（1H-吡唑-4-基）-1,6-萘啶化合物作为SYK抑制剂公开(公告)号：US20130040984A1
公开(公告)日：2013-02-14
申请号：US13642338
申请日：2011-04-27
申请人： Francis Louis Atkinson , Michael David Barker , Clement Douault , Neil Stuart Garton , John Liddle , Vipulkumar Kantibhai Patel , Alexander George Steven Preston , David Matthew Wilson
发明人： Francis Louis Atkinson , Michael David Barker , Clement Douault , Neil Stuart Garton , John Liddle , Vipulkumar Kantibhai Patel , Alexander George Steven Preston , David Matthew Wilson
IPC分类号： A61K31/4545 , A61P37/06 , A61P17/00 , C07D471/04
CPC分类号： C07D471/04
摘要： The present invention relates to a compound of formula (I): or a salt thereof; which is an inhibitor of spleen tyrosine kinase (Syk) and therefore potentially of use in treating diseases resulting from inappropriate activation of mast and/or basophil cells, macrophages, and B-cells and related inflammatory responses and tissue damage, for instance inflammatory disease and/or allergic disorders, and in cancer therapy, specifically heme malignancies, chronic spontaneous urticaria and autoimmune conditions.
摘要翻译： 本发明涉及式（I）化合物或其盐; 其是脾脏酪氨酸激酶（Syk）的抑制剂，因此潜在地用于治疗由桅杆和/或嗜碱性粒细胞，巨噬细胞和B细胞的不适当活化引起的疾病以及相关的炎症反应和组织损伤，例如炎性疾病和 /或过敏性疾病，以及癌症治疗，特别是血红素恶性肿瘤，慢性自发性荨麻疹和自身免疫性疾病。
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3.发明申请PYRIDINYL- AND PYRAZINYL-METHYLOXY-ARYL DERIVATIVES USEFUL AS INHIBITORS OF SPLEEN TYROSINE KINASE (SYK) 审中-公开作为缓冲型酪氨酸激酶（SYK）的抑制剂有用的吡啶基 - 和吡嗪并 - 甲基衍生物公开(公告)号：US20140005177A1
公开(公告)日：2014-01-02
申请号：US14004388
申请日：2012-03-08
IPC分类号： C07D401/12 , A61K31/4725 , A61K31/55 , C07D403/12 , A61K45/06 , C07D401/14
CPC分类号： C07D403/12 , A61K9/0014 , A61K31/4725 , A61K31/55 , A61K45/06 , C07D401/12 , C07D401/14
摘要： A compound of formula (I): or a salt thereof; which is an inhibitor of spleen tyrosine kinase (SYK) and therefore potentially of use in treating diseases resulting from inappropriate activation of mast cells, macrophages, and B-cells and related inflammatory responses and tissue damage, for instance inflammatory diseases and/or allergic conditions, in cancer therapy, specifically heme malignancies, and autoimmune conditions.
摘要翻译： 式（I）的化合物或其盐; 其是脾脏酪氨酸激酶（SYK）的抑制剂，因此潜在地用于治疗由肥大细胞，巨噬细胞和B细胞的不适当活化引起的疾病以及相关的炎症反应和组织损伤，例如炎症性疾病和/或过敏性疾病 ，在癌症治疗中，特别是血红素恶性肿瘤和自身免疫病症。
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公开(公告)号：US20120232061A1
公开(公告)日：2012-09-13
申请号：US13414873
申请日：2012-03-08
IPC分类号： A61K31/55 , A61P37/06 , A61P19/04 , A61P19/02 , A61P7/00 , A61P17/00 , A61P13/12 , A61P29/00 , C07D401/12 , A61P9/00
CPC分类号： C07D403/12 , A61K9/0014 , A61K31/4725 , A61K31/55 , A61K45/06 , C07D401/12 , C07D401/14
摘要： A compound of formula (I): or a salt thereof; which is an inhibitor of spleen tyrosine kinase (SYK) and therefore potentially of use in treating diseases resulting from inappropriate activation of mast cells, macrophages, and B-cells and related inflammatory responses and tissue damage, for instance inflammatory diseases and/or allergic conditions, in cancer therapy, specifically heme malignancies, and autoimmune conditions.
摘要翻译： 式（I）的化合物或其盐; 其是脾脏酪氨酸激酶（SYK）的抑制剂，因此潜在地用于治疗由肥大细胞，巨噬细胞和B细胞的不适当活化引起的疾病以及相关的炎症反应和组织损伤，例如炎症性疾病和/或过敏性疾病 ，在癌症治疗中，特别是血红素恶性肿瘤和自身免疫病症。
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5.发明授权7-(1H-pyrazol-4-yl)-1,6-naphthyridine compounds as Syk inhibitors 失效7-（1H-吡唑-4-基）-1,6-萘啶化合物作为Syk抑制剂公开(公告)号：US08633319B2
公开(公告)日：2014-01-21
申请号：US13642338
申请日：2011-04-27
申请人： Francis Louis Atkinson , Michael David Barker , Clement Douault , Neil Stuart Garton , John Liddle , Vipulkumar Kantibhai Patel , Alexander George Steven Preston , David Matthew Wilson
发明人： Francis Louis Atkinson , Michael David Barker , Clement Douault , Neil Stuart Garton , John Liddle , Vipulkumar Kantibhai Patel , Alexander George Steven Preston , David Matthew Wilson
IPC分类号： C07D471/04 , A61K31/4375
CPC分类号： C07D471/04
摘要： The present invention relates to a compound of formula (I): or a salt thereof; which is an inhibitor of spleen tyrosine kinase (Syk) and therefore potentially of use in treating diseases resulting from inappropriate activation of mast and/or basophil cells, macrophages, and B-cells and related inflammatory responses and tissue damage, for instance inflammatory disease and/or allergic disorders, and in cancer therapy, specifically heme malignancies, chronic spontaneous urticaria and autoimmune conditions.
摘要翻译： 本发明涉及式（I）化合物或其盐; 其是脾脏酪氨酸激酶（Syk）的抑制剂，因此潜在地用于治疗由桅杆和/或嗜碱性粒细胞，巨噬细胞和B细胞的不适当活化引起的疾病以及相关的炎症反应和组织损伤，例如炎性疾病和 /或过敏性疾病，以及癌症治疗，特别是血红素恶性肿瘤，慢性自发性荨麻疹和自身免疫性疾病。
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公开(公告)号：US08993560B2
公开(公告)日：2015-03-31
申请号：US13414873
申请日：2012-03-08
IPC分类号： A61K31/55 , C07D401/12 , C07D403/12 , A61K31/4725 , A61K45/06 , C07D401/14
CPC分类号： C07D403/12 , A61K9/0014 , A61K31/4725 , A61K31/55 , A61K45/06 , C07D401/12 , C07D401/14
摘要： A compound of formula (I): or a salt thereof; which is an inhibitor of spleen tyrosine kinase (SYK) and therefore potentially of use in treating diseases resulting from inappropriate activation of mast cells, macrophages, and B-cells and related inflammatory responses and tissue damage, for instance inflammatory diseases and/or allergic conditions, in cancer therapy, specifically heme malignancies, and autoimmune conditions.
摘要翻译： 式（I）的化合物或其盐; 其是脾脏酪氨酸激酶（SYK）的抑制剂，因此潜在地用于治疗由肥大细胞，巨噬细胞和B细胞的不适当活化引起的疾病以及相关的炎症反应和组织损伤，例如炎症性疾病和/或过敏性疾病 ，在癌症治疗中，特别是血红素恶性肿瘤和自身免疫病症。
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公开(公告)号：US08470835B2
公开(公告)日：2013-06-25
申请号：US13144136
申请日：2010-01-11
IPC分类号： A01N43/54 , C07D239/42
CPC分类号： C07D405/12
摘要： The present invention relates to the compound of formula (I): or a salt, preferably a pharmaceutically acceptable salt, thereof; is an inhibitor of spleen tyrosine kinase (SYK) and therefore potentially of use in treating diseases resulting from inappropriate mast cell activation, for instance allergic and inflammatory diseases, as well of potential use in cancer therapy, specifically heme malignancies.
摘要翻译： 本发明涉及式（I）化合物或其盐，优选其药学上可接受的盐; 是脾脏酪氨酸激酶（SYK）的抑制剂，因此潜在地用于治疗由不适当的肥大细胞活化导致的疾病，例如过敏性和炎症性疾病，以及在癌症治疗中的潜在用途，特别是血红素恶性肿瘤。
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公开(公告)号：US08383635B2
公开(公告)日：2013-02-26
申请号：US13058251
申请日：2009-08-12
申请人： Francis Louis Atkinson , Jeffrey Michael Axten , Maria Cichy-Knight , Michael Lee Moore , Vipulkumar Kantibhai Patel , Xinrong Tian , Christopher Roland Wellaway , Allison K. Dunn
发明人： Francis Louis Atkinson , Jeffrey Michael Axten , Maria Cichy-Knight , Michael Lee Moore , Vipulkumar Kantibhai Patel , Xinrong Tian , Christopher Roland Wellaway , Allison K. Dunn
IPC分类号： A01N43/90 , A61K31/519 , C07D471/00
CPC分类号： C07D471/04
摘要： The invention is directed to pyrido[4,3-d]pyrimidin-5(6H)-one derivatives. Specifically, the invention is directed to compounds according to Formula I: wherein R1, R2, R3, and R4 are defined below. The compounds of the invention are inhibitors of PDK1 and can be useful in the treatment of disorders characterized by constitutively activated ACG kinases such as cancer and more specifically cancers of the breast, colon, and lung. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting PDK1 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
摘要翻译： 本发明涉及吡啶并[4,3-d]嘧啶-5（6H） - 酮衍生物。 具体地，本发明涉及式I化合物：其中R1，R2，R3和R4定义如下。 本发明的化合物是PDK1的抑制剂，可用于治疗特征在于组成型激活的ACG激酶（例如癌症，更特别是乳腺癌，结肠癌和肺癌）的病症。 因此，本发明进一步涉及包含本发明化合物的药物组合物。 本发明还涉及抑制PDK1活性的方法和使用本发明化合物或与本发明化合物组合的药物组合物治疗与之相关的病症的方法。
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公开(公告)号：US20110275655A1
公开(公告)日：2011-11-10
申请号：US13144136
申请日：2010-01-11
IPC分类号： A61K31/506 , A61P35/00 , A61P29/00 , A61P37/08 , A61P17/00 , A61P11/06 , A61P1/04 , A61P1/00 , A61P17/06 , C07D405/12 , A61P11/00
CPC分类号： C07D405/12
摘要： The present invention relates to the compound of formula (I): or a salt, preferably a pharmaceutically acceptable salt, thereof; is an inhibitor of spleen tyrosine kinase (SYK) and therefore potentially of use in treating diseases resulting from inappropriate mast cell activation, for instance allergic and inflammatory diseases, as well of potential use in cancer therapy, specifically heme malignancies.
摘要翻译： 本发明涉及式（I）化合物或其盐，优选其药学上可接受的盐; 是脾脏酪氨酸激酶（SYK）的抑制剂，因此潜在地用于治疗由不适当的肥大细胞活化导致的疾病，例如过敏性和炎症性疾病，以及在癌症治疗中的潜在用途，特别是血红素恶性肿瘤。
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公开(公告)号：US20110136838A1
公开(公告)日：2011-06-09
申请号：US13058251
申请日：2009-08-12
申请人： Francis Louis Atkinson , Jeffrey Michael Axten , Maria Cichy-Knight , Michael Lee Moore , Vipulkumar Kantibhai Patel , Xinrong Tian , Christopher Roland Wellaway , Allison K. Dunn
发明人： Francis Louis Atkinson , Jeffrey Michael Axten , Maria Cichy-Knight , Michael Lee Moore , Vipulkumar Kantibhai Patel , Xinrong Tian , Christopher Roland Wellaway , Allison K. Dunn
IPC分类号： A61K31/519 , C07D471/04 , A61P35/00
CPC分类号： C07D471/04
摘要： The invention is directed to pyrido[4,3-d]pyrimidin-5(6H)-one derivatives. Specifically, the invention is directed to compounds according to Formula I: wherein R1, R2, R3, and R4 are defined below.The compounds of the invention are inhibitors of PDK1 and can be useful in the treatment of disorders characterized by constitutively activated ACG kinases such as cancer and more specifically cancers of the breast, colon, and lung. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting PDK1 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
摘要翻译： 本发明涉及吡啶并〔4,3-d〕嘧啶-5（6H） - 酮衍生物。 具体地，本发明涉及式I化合物：其中R1，R2，R3和R4定义如下。 本发明的化合物是PDK1的抑制剂，可用于治疗特征在于组成型激活的ACG激酶（例如癌症，更特别是乳腺癌，结肠癌和肺癌）的病症。 因此，本发明进一步涉及包含本发明化合物的药物组合物。 本发明还涉及抑制PDK1活性的方法和使用本发明化合物或与本发明化合物组合的药物组合物治疗与之相关的病症的方法。
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