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公开(公告)号：US08906852B2
公开(公告)日：2014-12-09
申请号：US13082923
申请日：2011-04-08
申请人： Stéphane Raeppel , Franck Raeppel , Stephen William Claridge , Lijie Zhan , Frédéric Gaudette , Michael Mannion , Norifumi Sato , Yohei Yuki , Masashi Kishida , Arkadii Vaisburg
发明人： Stéphane Raeppel , Franck Raeppel , Stephen William Claridge , Lijie Zhan , Frédéric Gaudette , Michael Mannion , Norifumi Sato , Yohei Yuki , Masashi Kishida , Arkadii Vaisburg
IPC分类号： A61K38/00 , C07K14/47 , A61P35/00 , C07K14/515 , A61P9/10 , A61P27/02 , A61K38/05 , A01N57/00 , A61K31/675 , A61K31/535 , A61K31/497 , A01N43/42 , A61K31/44 , C07F9/06 , C07F9/28 , C07D513/02 , C07D495/04 , C07F9/6561 , C07D519/00
CPC分类号： C07D495/04 , A61K38/005 , C07D519/00 , C07F9/6561 , C07K5/06
摘要： This invention relates to compounds that inhibit protein tyrosine kinase activity. In particular the invention relates to compounds that inhibit the protein tyrosine kinase activity of growth factor receptors, resulting in the inhibition of receptor signaling, for example, the inhibition of VEGF receptor signaling. The invention also provides compounds, compositions and methods for treating cell proliferative diseases and conditions and ophthalmic diseases, disorders and conditions.
摘要翻译： 本发明涉及抑制蛋白酪氨酸激酶活性的化合物。 特别地，本发明涉及抑制生长因子受体的蛋白酪氨酸激酶活性的化合物，导致受体信号传导的抑制，例如VEGF受体信号传导的抑制。 本发明还提供了用于治疗细胞增殖性疾病和病症以及眼科疾病，病症和病症的化合物，组合物和方法。
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公开(公告)号：US08470850B2
公开(公告)日：2013-06-25
申请号：US12775090
申请日：2010-05-06
申请人： Arkadii Vaisburg , Stephen William Claridge , Franck Raeppel , Oscar Mario Saavedra , Noemy Berstein , Marie-Claude Granger , Lijie Zhan , Amal Wahhab , David Liewellyn
发明人： Arkadii Vaisburg , Stephen William Claridge , Franck Raeppel , Oscar Mario Saavedra , Noemy Berstein , Marie-Claude Granger , Lijie Zhan , Amal Wahhab , David Liewellyn
IPC分类号： C07D495/04 , C07D413/04 , A61K31/4365 , A61K31/519 , A61P35/04 , A61P9/10 , C07D413/06 , C07D413/12 , C07D413/10 , C07D223/04
CPC分类号： C07D495/04 , C07D471/04 , C07D487/04
摘要： The invention relates to the inhibition of VEGF receptor signaling and HGF receptor signaling. The invention provides compounds and methods for inhibiting VEGF receptor signaling and HGF receptor signaling. The invention also provides compositions and methods for treating cell proliferative diseases and conditions
摘要翻译： 本发明涉及VEGF受体信号传导和HGF受体信号传导的抑制。 本发明提供了用于抑制VEGF受体信号传导和HGF受体信号传导的化合物和方法。 本发明还提供了治疗细胞增殖性疾病和病症的组合物和方法
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公开(公告)号：US08455484B2
公开(公告)日：2013-06-04
申请号：US13082944
申请日：2011-04-08
申请人： Stéphane Raeppel , Lijie Zhan , Stephen William Claridge , Franck Raeppel , Frédéric Gaudette , Arkadii Vaisburg
发明人： Stéphane Raeppel , Lijie Zhan , Stephen William Claridge , Franck Raeppel , Frédéric Gaudette , Arkadii Vaisburg
IPC分类号： A61K31/5377 , A61K31/496 , A61K31/4365 , C07D413/14 , C07D471/04
CPC分类号： C07D495/04 , A61K38/005 , C07D519/00 , C07F9/6561 , C07K5/06
摘要： The invention provides new compounds and compositions thereof. The invention also provides methods for treating ophthalmic diseases, disorders and conditions.
摘要翻译： 本发明提供了新的化合物及其组合物。 本发明还提供了治疗眼科疾病，病症和病症的方法。
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公开(公告)号：US20120108628A1
公开(公告)日：2012-05-03
申请号：US13341604
申请日：2011-12-30
申请人： Stephen William Claridge , Ljubomir Isakovic , Michael Mannion , Stephane Raeppel , Oscar Mario Saavedra , Frédéric Gaudette , Lijie Zhan , Arkadii Vaisburg
发明人： Stephen William Claridge , Ljubomir Isakovic , Michael Mannion , Stephane Raeppel , Oscar Mario Saavedra , Frédéric Gaudette , Lijie Zhan , Arkadii Vaisburg
IPC分类号： A61K31/4365 , A61P43/00
CPC分类号： C07D495/04
摘要： This invention relates to compounds that inhibit protein tyrosine kinase activity. In particular the invention relates to compounds that inhibit the protein tyrosine kinase activity of growth factor receptors, resulting in the inhibition of receptor signaling, for example, the inhibition of VEGF receptor signaling and HGF receptor signaling. More particularly, the invention relates to compounds, compositions and methods for the inhibition of VEGF receptor signaling and HGF receptor signaling. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.
摘要翻译： 本发明涉及抑制蛋白酪氨酸激酶活性的化合物。 特别地，本发明涉及抑制生长因子受体的蛋白酪氨酸激酶活性的化合物，导致受体信号传导的抑制，例如VEGF受体信号传导和HGF受体信号传导的抑制。 更具体地，本发明涉及用于抑制VEGF受体信号传导和HGF受体信号传导的化合物，组合物和方法。 本发明还提供了治疗细胞增殖性疾病和病症的组合物和方法。
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5.发明申请Processes and intermediates for preparing fused heterocyclic kinase inhibitors 有权制备融合杂环激酶抑制剂的方法和中间体公开(公告)号：US20090286984A1
公开(公告)日：2009-11-19
申请号：US12231297
申请日：2008-08-29
申请人： Franck Raeppel , Ljubomir Isakovic , Stephen William Claridge , Michael Mannion , Lijie Zhan , Marie-Claude Granger , Arkadii Vaisburg , Miguel Nantel
发明人： Franck Raeppel , Ljubomir Isakovic , Stephen William Claridge , Michael Mannion , Lijie Zhan , Marie-Claude Granger , Arkadii Vaisburg , Miguel Nantel
IPC分类号： C07D495/04
CPC分类号： C07D495/04 , C07D213/38 , C07D213/51 , C07D213/61
摘要： This invention relates to processes and intermediates for manufacturing fused heterocyclic-type kinase inhibitor compounds, such as thienopyridine-based compounds, and to processes and intermediates for preparing intermediates that are useful in the manufacture of fused heterocyclic-type kinase inhibitor compounds, such as thienopyridine-based compounds, particularly at an industrial level.
摘要翻译： 本发明涉及用于制备稠合杂环型激酶抑制剂化合物（例如噻吩并吡啶类化合物）的方法和中间体，以及用于制备可用于制备稠合杂环型激酶抑制剂化合物如噻吩并吡啶的中间体的方法和中间体 的化合物，特别是在工业水平。
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公开(公告)号：US20090264440A1
公开(公告)日：2009-10-22
申请号：US12200939
申请日：2008-08-29
申请人： Stephen William Claridge , Ljubomir Isakovic , Michael Mannion , Stephane Raeppel , Oscar Mario Saavedra , Frederic Gaudette , Lijie Zhan , Nancy Z. Zhou , Franck Raeppel , Robert Deziel , Arkadii Vaisburg , Tetsuyuki Uno
发明人： Stephen William Claridge , Ljubomir Isakovic , Michael Mannion , Stephane Raeppel , Oscar Mario Saavedra , Frederic Gaudette , Lijie Zhan , Nancy Z. Zhou , Franck Raeppel , Robert Deziel , Arkadii Vaisburg , Tetsuyuki Uno
IPC分类号： A61K31/496 , C07D495/04 , C12N9/99 , A61K31/4365
CPC分类号： C07D495/04
摘要： This invention relates to compounds that inhibit protein tyrosine kinase activity. In particular the invention relates to compounds that inhibit the protein tyrosine kinase activity of growth factor receptors, resulting in the inhibition of receptor signaling, for example, the inhibition of VEGF receptor signaling and HGF receptor signaling. More particularly, the invention relates to compounds, compositions and methods for the inhibition of VEGF receptor signaling and HGF receptor signaling. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.
摘要翻译： 本发明涉及抑制蛋白酪氨酸激酶活性的化合物。 特别地，本发明涉及抑制生长因子受体的蛋白酪氨酸激酶活性的化合物，导致受体信号传导的抑制，例如VEGF受体信号传导和HGF受体信号传导的抑制。 更具体地，本发明涉及用于抑制VEGF受体信号传导和HGF受体信号传导的化合物，组合物和方法。 本发明还提供了治疗细胞增殖性疾病和病症的组合物和方法。
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7.发明授权Processes and intermediates for preparing fused heterocyclic kinase inhibitors 有权制备融合杂环激酶抑制剂的方法和中间体公开(公告)号：US08907091B2
公开(公告)日：2014-12-09
申请号：US12231297
申请日：2008-08-29
申请人： Franck Raeppel , Ljubomir Isakovic , Stephen William Claridge , Michael Mannion , Lijie Zhan , Marie-Claude Granger , Arkadii Vaisburg , Miguel Nantel
发明人： Franck Raeppel , Ljubomir Isakovic , Stephen William Claridge , Michael Mannion , Lijie Zhan , Marie-Claude Granger , Arkadii Vaisburg , Miguel Nantel
IPC分类号： C07D513/04 , C07D213/51 , C07D495/04 , C07D213/61 , C07D213/38
CPC分类号： C07D495/04 , C07D213/38 , C07D213/51 , C07D213/61
摘要： This invention relates to processes and intermediates for manufacturing fused heterocyclic-type kinase inhibitor compounds, such as thienopyridine-based compounds, and to processes and intermediates for preparing intermediates that are useful in the manufacture of fused heterocyclic-type kinase inhibitor compounds, such as thienopyridine-based compounds, particularly at an industrial level.
摘要翻译： 本发明涉及用于制备稠合杂环型激酶抑制剂化合物（例如噻吩并吡啶类化合物）的方法和中间体，以及用于制备可用于制备稠合杂环型激酶抑制剂化合物如噻吩并吡啶的中间体的方法和中间体 的化合物，特别是在工业水平。
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公开(公告)号：US08759522B2
公开(公告)日：2014-06-24
申请号：US12964289
申请日：2010-12-09
申请人： Michael Mannion , Stephane Raeppel , Stephen William Claridge , Frederic Gaudette , Lijie Zhan , Ljubomir Isakovic , Oscar Mario Saavedra , Tetsuyuki Uno , Masashi Kishida , Arkadii Vaisburg
发明人： Michael Mannion , Stephane Raeppel , Stephen William Claridge , Frederic Gaudette , Lijie Zhan , Ljubomir Isakovic , Oscar Mario Saavedra , Tetsuyuki Uno , Masashi Kishida , Arkadii Vaisburg
IPC分类号： C07D513/04 , A61K31/4365
CPC分类号： C07D495/04 , C07F9/6561
摘要： This invention relates to compounds that inhibit protein tyrosine kinase activity. In particular the invention relates to compounds that inhibit the protein tyrosine kinase activity of growth factor receptors, resulting in the inhibition of receptor signaling, for example, the inhibition of VEGF receptor signaling. The invention also provides compounds, compositions and methods for treating cell proliferative diseases and conditions and opthalmological diseases, disorders and conditions.
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公开(公告)号：US08389541B2
公开(公告)日：2013-03-05
申请号：US13341604
申请日：2011-12-30
申请人： Stephen William Claridge , Ljubomir Isakovic , Michael Mannion , Stephane Raeppel , Oscar Mario Saavedra , Frederic Gaudette , Lijie Zhan , Arkadii Vaisburg
发明人： Stephen William Claridge , Ljubomir Isakovic , Michael Mannion , Stephane Raeppel , Oscar Mario Saavedra , Frederic Gaudette , Lijie Zhan , Arkadii Vaisburg
IPC分类号： A01N43/42 , C07D413/00
CPC分类号： C07D495/04
摘要： This invention relates to compounds that inhibit protein tyrosine kinase activity. In particular the invention relates to compounds that inhibit the protein tyrosine kinase activity of growth factor receptors, resulting in the inhibition of receptor signaling, for example, the inhibition of VEGF receptor signaling and HGF receptor signaling. More particularly, the invention relates to compounds, compositions and methods for the inhibition of VEGF receptor signaling and HGF receptor signaling. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.
摘要翻译： 本发明涉及抑制蛋白酪氨酸激酶活性的化合物。 特别地，本发明涉及抑制生长因子受体的蛋白酪氨酸激酶活性的化合物，导致受体信号传导的抑制，例如VEGF受体信号传导和HGF受体信号传导的抑制。 更具体地，本发明涉及用于抑制VEGF受体信号传导和HGF受体信号传导的化合物，组合物和方法。 本发明还提供了治疗细胞增殖性疾病和病症的组合物和方法。
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公开(公告)号：US08329726B2
公开(公告)日：2012-12-11
申请号：US13314362
申请日：2011-12-08
申请人： Oscar Mario Saavedra , Stephen William Claridge , Lijie Zhan , Franck Raeppel , Arkadii Vaisburg , Stephane Raeppel , Michael Mannion , Frederic Gaudette , Ljubomir Isakovic , Marie-Claude Granger , Naomy Bernstein
发明人： Oscar Mario Saavedra , Stephen William Claridge , Lijie Zhan , Franck Raeppel , Arkadii Vaisburg , Stephane Raeppel , Michael Mannion , Frederic Gaudette , Ljubomir Isakovic , Marie-Claude Granger , Naomy Bernstein
CPC分类号： C07D495/04
摘要： The invention relates to the inhibition of VEGF receptor signaling and HGF receptor signaling. The invention provides compounds of general formula (A) wherein A1 is sulfur, A3 is CH, A2 is CH, D is heterocycle, Z is oxygen, SO0-2 or NR, Ar is phenyl and G is not a ring, and methods for inhibiting VEGF receptor signaling and HGF receptor signaling. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.
摘要翻译： 本发明涉及VEGF受体信号传导和HGF受体信号传导的抑制。 本发明提供通式（A）的化合物，其中A 1为硫，A 3为CH，A 2为CH，D为杂环，Z为氧，SOO 2或NR，Ar为苯基且G不为环， 抑制VEGF受体信号传导和HGF受体信号转导。 本发明还提供了治疗细胞增殖性疾病和病症的组合物和方法。
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