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公开(公告)号：US20110257175A1
公开(公告)日：2011-10-20
申请号：US13082944
申请日：2011-04-08
申请人： Stëphane Raeppel , Lijie Zhan , Stephen William Claridge , Franck Raeppel , Frëdëric Gaudette , Arkadii Vaisburg
发明人： Stëphane Raeppel , Lijie Zhan , Stephen William Claridge , Franck Raeppel , Frëdëric Gaudette , Arkadii Vaisburg
IPC分类号： A61K31/5377 , A61K31/496 , A61P27/02 , C07D495/04 , A61K31/4365
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：US20110098293A1
公开(公告)日：2011-04-28
申请号：US12920676
申请日：2009-02-27
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： A61K31/5377 , C07D495/04 , C12N9/99 , A61K31/4365 , C07D401/02 , A61K31/496 , C07D413/14 , A61P9/00 , A61P35/00 , A61P27/02
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.
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：US20080227826A1
公开(公告)日：2008-09-18
申请号：US12043450
申请日：2008-03-06
申请人： Sylvie Frechette , Lubo Isakovic , Isabelle Paquin , Simon Roy , Oscar Moradei , Arkadii Vaisburg
发明人： Sylvie Frechette , Lubo Isakovic , Isabelle Paquin , Simon Roy , Oscar Moradei , Arkadii Vaisburg
IPC分类号： A61K31/4439 , C07D207/14 , A61K31/402 , A61P35/00 , C12N9/99 , C07D401/12
CPC分类号： C07D401/12 , C07D207/14 , C07D401/04 , C07D403/04 , C07D405/12
摘要： The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions. One aspect of the invention provides compounds of formula (1): in which T, A and X are as described herein.
摘要翻译： 本发明涉及抑制组蛋白脱乙酰酶。 本发明提供了抑制组蛋白脱乙酰酶酶活性的化合物和方法。 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。 本发明的一个方面提供式（1）的化合物：其中T，A和X如本文所述。
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公开(公告)号：US07259172B2
公开(公告)日：2007-08-21
申请号：US10884435
申请日：2004-07-02
IPC分类号： C07D401/02 , C07D333/02 , A61K31/44
CPC分类号： C07F9/2491 , C07F9/3808 , C07F9/4006 , C07F9/4084 , C07F9/425 , C07F9/4407 , C07F9/572 , C07F9/5728 , C07F9/58 , C07F9/60 , C07F9/6506 , C07F9/6524 , C07F9/65312 , C07F9/6539 , C07F9/65395 , C07F9/6541 , C07F9/65515 , C07F9/65517 , C07F9/655345 , C07F9/655354 , C07F9/65583 , C07F9/65586
摘要： The intention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel β-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic β-lactamase inhibitors presently available, and which do not require a β-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.
摘要翻译： 意图涉及细菌抗生素抗性，特别涉及克服细菌抗生素抗性的组合物和方法。 本发明提供了新型β-内酰胺酶抑制剂，其在结构上与目前可获得的天然产物和半合成β-内酰胺酶抑制剂无关，并且不需要β-内酰胺药效团。 本发明还提供用于抑制细菌生长的药物组合物和方法。
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公开(公告)号：US07253204B2
公开(公告)日：2007-08-07
申请号：US11090713
申请日：2005-03-25
申请人： Daniel Delorme , Arkadii Vaisburg , Oscar Moradei , Silvana Leit , Stephane Raeppel , Sylvie Frechette , Giliane Bouchain , Zhihong Zhou , Isabelle Paquin , Frederic Gaudette , Ljubomir Isakovic
发明人： Daniel Delorme , Arkadii Vaisburg , Oscar Moradei , Silvana Leit , Stephane Raeppel , Sylvie Frechette , Giliane Bouchain , Zhihong Zhou , Isabelle Paquin , Frederic Gaudette , Ljubomir Isakovic
IPC分类号： A61K31/4025 , C07D207/14
CPC分类号： C07C237/40 , C07C311/21 , C07C311/39 , C07D209/42 , C07D213/38 , C07D213/74 , C07D231/38 , C07D235/16 , C07D237/20 , C07D239/42 , C07D239/48 , C07D263/58 , C07D271/06 , C07D307/84 , C07D333/38 , C07D401/04 , C07D401/12 , C07D403/12 , C07D409/04 , C07D417/04 , C07D495/04
摘要： The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.
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公开(公告)号：US20060074056A1
公开(公告)日：2006-04-06
申请号：US11191617
申请日：2005-07-28
申请人： Arkadii Vaisburg , Stephen Claridge , Franck Raeppel , Oscar Saavedra , Naomy Berstein , Marie-Claude Granger , Lijie Zhan , Amal Wahhab , David Llewellyn
发明人： Arkadii Vaisburg , Stephen Claridge , Franck Raeppel , Oscar Saavedra , Naomy Berstein , Marie-Claude Granger , Lijie Zhan , Amal Wahhab , David Llewellyn
IPC分类号： A61K31/655 , A61K31/522 , C07D473/02 , C07D487/02
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：US20050245518A1
公开(公告)日：2005-11-03
申请号：US11090713
申请日：2005-03-25
申请人： Daniel Delorme , Arkadii Vaisburg , Oscar Moradei , Silvana Leit , Stephane Raeppel , Sylvie Frechette , Giliane Bouchain , Zhihong Zhou , Isabelle Paquin , Frederic Gaudette , Ljubomir Isakovic
发明人： Daniel Delorme , Arkadii Vaisburg , Oscar Moradei , Silvana Leit , Stephane Raeppel , Sylvie Frechette , Giliane Bouchain , Zhihong Zhou , Isabelle Paquin , Frederic Gaudette , Ljubomir Isakovic
IPC分类号： A61K31/4035 , A61K31/405 , A61K31/4439 , A61K31/496 , A61K31/4965 , A61K31/5377
CPC分类号： C07C237/40 , C07C311/21 , C07C311/39 , C07D209/42 , C07D213/38 , C07D213/74 , C07D231/38 , C07D235/16 , C07D237/20 , C07D239/42 , C07D239/48 , C07D263/58 , C07D271/06 , C07D307/84 , C07D333/38 , C07D401/04 , C07D401/12 , C07D403/12 , C07D409/04 , C07D417/04 , C07D495/04
摘要： The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.
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公开(公告)号：US08729268B2
公开(公告)日：2014-05-20
申请号：US12920676
申请日：2009-02-27
申请人： Michael Mannion , Stéphane Raeppel , Stephen William Claridge , Frédéric Gaudette , Lijie Zhan , Ljubomir Isakovic , Oscar Mario Saavedra , Tetsuyuki Uno , Masashi Kishida , Arkadii Vaisburg
发明人： Michael Mannion , Stéphane Raeppel , Stephen William Claridge , Frédéric Gaudette , Lijie Zhan , Ljubomir Isakovic , Oscar Mario Saavedra , Tetsuyuki Uno , Masashi Kishida , Arkadii Vaisburg
IPC分类号： A61K31/4365 , C07D513/04
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.
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：US08598168B2
公开(公告)日：2013-12-03
申请号：US11696880
申请日：2007-04-05
申请人： Oscar Moradei , Isabelle Paquin , Sylvie Frechette , Tammy Mallais , Simon Roy , Roger Machaalani , Arkadii Vaisburg , Jeffrey M Besterman , Pierre Tessier , David Smil , Silvana Leit , Robert Déziel
发明人： Oscar Moradei , Isabelle Paquin , Sylvie Frechette , Tammy Mallais , Simon Roy , Roger Machaalani , Arkadii Vaisburg , Jeffrey M Besterman , Pierre Tessier , David Smil , Silvana Leit , Robert Déziel
IPC分类号： A61K31/535 , A61K31/445 , A61K31/44 , A61K31/42 , A61K31/415 , A61K31/40 , A61K31/28
CPC分类号： C07D333/36 , C07C235/56 , C07C237/40 , C07C271/28 , C07D207/12 , C07D207/14 , C07D207/325 , C07D209/08 , C07D213/40 , C07D213/56 , C07D213/61 , C07D213/89 , C07D267/08 , C07D277/28 , C07D277/36 , C07D295/155 , C07D307/52 , C07D317/58 , C07D333/20 , C07D333/28 , C07D333/38 , C07D333/70 , C07D401/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12 , C07D417/14 , C07D487/08
摘要： The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.
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公开(公告)号：US20120083482A1
公开(公告)日：2012-04-05
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
IPC分类号： A61K31/4365 , A61P35/00 , A61K31/498 , A61K31/5377 , A61K31/496
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。 本发明提供了通式（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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