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1.发明申请Methods of synthesizing substituted 3-cyanoquinolines and intermediates thereof 审中-公开合成取代的3-氰基喹啉的方法及其中间体公开(公告)号：US20060270668A1
公开(公告)日：2006-11-30
申请号：US11439984
申请日：2006-05-25
申请人： Warren Chew , Gloria Cheal , Jacqueline Lunetta
发明人： Warren Chew , Gloria Cheal , Jacqueline Lunetta
IPC分类号： A61K31/5377 , A61K31/506 , A61K31/496 , A61K31/4709 , C07D413/02 , C07D403/02
CPC分类号： C07D401/12 , C07D215/56 , C07D403/02 , C07D413/02
摘要： The invention is directed to methods of making substituted 3-cyanoquinolines, including compounds according to the following formula: The methods are amenable to large scale manufacture, avoid the use of chromatographic separations, and provide stable, high purity product more efficiently than in the prior art.
摘要翻译： 本发明涉及制备取代的3-氰基喹啉的方法，包括根据下式的化合物：该方法适于大规模生产，避免使用色谱分离，并且比先前的方法更有效地提供稳定的高纯度产品 艺术。
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![Process for the scalable synthesis of 1,3,4,9-tetrahydropyrano[3,4-b]-indole derivatives](/abs-image/US/2006/03/16/US20060058532A1/abs.jpg.150x150.jpg)
2.发明申请Process for the scalable synthesis of 1,3,4,9-tetrahydropyrano[3,4-b]-indole derivatives 审中-公开用于可伸缩合成1,3,4,9-四氢吡喃并[3,4-b] - 吲哚衍生物的方法公开(公告)号：US20060058532A1
公开(公告)日：2006-03-16
申请号：US11223312
申请日：2005-09-09
IPC分类号： C07D209/36
CPC分类号： C07D491/04 , C07D209/36
摘要： The invention is directed to a process of synthesizing compounds of formula (VI): wherein R1-R9, R3′, R4′ and Y are as set forth in the specification, and said method is useful for large scale synthesis thereof. The invention is also directed to useful intermediates for synthesizing the compounds of formula (VI) and processes of preparing said intermediates.
摘要翻译： 本发明涉及合成式（Ⅵ）化合物的方法：
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公开(公告)号：US20090264648A1
公开(公告)日：2009-10-22
申请号：US12353896
申请日：2009-01-14
申请人： Warren Chew , Zheng Wang , Gloria Cheal , Martial Bertrand , John Potoski , Mahmoud Mirmehrabi , Arianna Nencini , Riccardo Zanaletti
发明人： Warren Chew , Zheng Wang , Gloria Cheal , Martial Bertrand , John Potoski , Mahmoud Mirmehrabi , Arianna Nencini , Riccardo Zanaletti
IPC分类号： C07D243/08
CPC分类号： C07D403/12
摘要： The present invention provides compounds and compositions, methods of making them, and methods of using them to modulate α7 nicotinic acetylcholine receptors and/or to treat any of a variety of disorders, diseases, and conditions. Provided compounds can affect, among other things, neurological, psychiatric and/or inflammatory system.
摘要翻译： 本发明提供化合物和组合物，制备它们的方法，以及使用它们调节α7烟碱乙酰胆碱受体和/或治疗多种疾病，疾病和病症中的任何一种的方法。 提供的化合物可以影响神经系统，精神和/或炎症系统。
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4.发明申请Maleate Salts of (E)-N--4-(Dimethylamino)-2-Butenamide and Crystalline Forms Thereof 有权（E）-N-4-（二甲基氨基）-2-丁烯酰胺的马来酸盐及其结晶形式公开(公告)号：US20120289545A1
公开(公告)日：2012-11-15
申请号：US13441168
申请日：2012-04-06
申请人： Qinghong Lu , Mannching Sherry Ku , Warren Chew , Gloria Cheal , Anthony F. Hadfield , Mahmoud Mirmehrabi
发明人： Qinghong Lu , Mannching Sherry Ku , Warren Chew , Gloria Cheal , Anthony F. Hadfield , Mahmoud Mirmehrabi
IPC分类号： A61K31/4709 , C07D401/14 , A61P35/00 , C07D401/12
CPC分类号： C07D401/12 , A61K31/4709 , C07C51/412 , C07C57/145
摘要： The present invention relates to maleate salt forms of (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy)anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide, methods of preparing crystalline maleate salt forms, the associated compounds, and pharmaceutical compositions containing the same. The maleate salts are useful in treating cancers, particularly those affected by kinases of the epidermal growth factor receptor family.
摘要翻译： 本发明涉及（E）-N- {4- [3-氯-4-（2-吡啶基甲氧基）苯胺基] -3-氰基-7-乙氧基-6-喹啉基} -4-（二甲基氨基 ）-2-丁烯酰胺，制备结晶马来酸盐形式的方法，相关化合物和含有它们的药物组合物。 马来酸盐可用于治疗癌症，特别是受表皮生长因子受体家族激酶影响的癌症。
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![Maleate salts of (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy)anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide and crystalline forms thereof](/abs-image/US/2011/09/20/US08022216B2/abs.jpg.150x150.jpg)
5.发明授权Maleate salts of (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy)anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide and crystalline forms thereof 有权（E）-N- {4- [3-氯-4-（2-吡啶基甲氧基）苯胺基] -3-氰基-7-乙氧基-6-喹啉基} -4-（二甲基氨基）-2-丁烯酰胺的马来酸盐和 其结晶形式公开(公告)号：US08022216B2
公开(公告)日：2011-09-20
申请号：US12251924
申请日：2008-10-15
申请人： Qinghong Lu , Mannching Sherry Ku , Warren Chew , Gloria Cheal , Anthony F. Hadfield , Mahmoud Mirmehrabi
发明人： Qinghong Lu , Mannching Sherry Ku , Warren Chew , Gloria Cheal , Anthony F. Hadfield , Mahmoud Mirmehrabi
IPC分类号： C07D215/44
CPC分类号： C07D401/12 , A61K31/4709 , C07C51/412 , C07C57/145
摘要： The present invention relates to maleate salt forms of (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy)anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide, methods of preparing crystalline maleate salt forms, the associated compounds, and pharmaceutical compositions containing the same. The maleate salts are useful in treating cancers, particularly those affected by kinases of the epidermal growth factor receptor family.
摘要翻译： 本发明涉及（E）-N- {4- [3-氯-4-（2-吡啶基甲氧基）苯胺基] -3-氰基-7-乙氧基-6-喹啉基} -4-（二甲基氨基 ）-2-丁烯酰胺，制备结晶马来酸盐形式的方法，相关化合物和含有它们的药物组合物。 马来酸盐可用于治疗癌症，特别是受表皮生长因子受体家族激酶影响的癌症。
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6.发明申请MALEATE SALTS OF (E)-N--4-(DIMETHYLAMINO)-2-BUTENAMIDE AND CRYSTALLINE FORMS THEREOF 有权（E）-N-4-（二甲基氨基）-2-丁酮及其结晶形式的色谱柱公开(公告)号：US20090176827A1
公开(公告)日：2009-07-09
申请号：US12251924
申请日：2008-10-15
申请人： Qinghong Lu , Mannching Sherry Ku , Warren Chew , Gloria Cheal , Anthony F. Hadfield , Mahmoud Mirmehrabi
发明人： Qinghong Lu , Mannching Sherry Ku , Warren Chew , Gloria Cheal , Anthony F. Hadfield , Mahmoud Mirmehrabi
IPC分类号： A61K31/4709 , C07D401/12 , C07D401/14
CPC分类号： C07D401/12 , A61K31/4709 , C07C51/412 , C07C57/145
摘要： The present invention relates to maleate salt forms of (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy)anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide, methods of preparing crystalline maleate salt forms, the associated compounds, and pharmaceutical compositions containing the same. The maleate salts are useful in treating cancers, particularly those affected by kinases of the epidermal growth factor receptor family.
摘要翻译： 本发明涉及（E）-N- {4- [3-氯-4-（2-吡啶基甲氧基）苯胺基] -3-氰基-7-乙氧基-6-喹啉基} -4-（二甲基氨基 ）-2-丁烯酰胺，制备结晶马来酸盐形式的方法，相关化合物和含有它们的药物组合物。 马来酸盐可用于治疗癌症，特别是受表皮生长因子受体家族激酶影响的癌症。
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![Maleate salts of (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy)anilino]-3-cyano-7-ethoxy-6-quinolinyl)-4-(dimethylamino)-2-buteramide and crystalline forms thereof](/abs-image/US/2013/03/12/US08394959B2/abs.jpg.150x150.jpg)
7.发明授权Maleate salts of (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy)anilino]-3-cyano-7-ethoxy-6-quinolinyl)-4-(dimethylamino)-2-buteramide and crystalline forms thereof 有权（E）-N- {4- [3-氯-4-（2-吡啶基甲氧基）苯胺基] -3-氰基-7-乙氧基-6-喹啉基）-4-（二甲基氨基）-2-丁酰胺的马来酸盐和 其结晶形式公开(公告)号：US08394959B2
公开(公告)日：2013-03-12
申请号：US13441168
申请日：2012-04-06
申请人： Qinghong Lu , Mannching Sherry Ku , Warren Chew , Gloria Cheal , Anthony F. Hadfield , Mahmoud Mirmehrabi
发明人： Qinghong Lu , Mannching Sherry Ku , Warren Chew , Gloria Cheal , Anthony F. Hadfield , Mahmoud Mirmehrabi
IPC分类号： C07D215/38
CPC分类号： C07D401/12 , A61K31/4709 , C07C51/412 , C07C57/145
摘要： The present invention relates to maleate salt forms of (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy)anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide, methods of preparing crystalline maleate salt forms, the associated compounds, and pharmaceutical compositions containing the same. The maleate salts are useful in treating cancers, particularly those affected by kinases of the epidermal growth factor receptor family.
摘要翻译： 本发明涉及（E）-N- {4- [3-氯-4-（2-吡啶基甲氧基）苯胺基] -3-氰基-7-乙氧基-6-喹啉基} -4-（二甲基氨基 ）-2-丁烯酰胺，制备结晶马来酸盐形式的方法，相关化合物和含有它们的药物组合物。 马来酸盐可用于治疗癌症，特别是受表皮生长因子受体家族激酶影响的癌症。
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![Maleate salts of (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy)anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide and crystalline forms thereof](/abs-image/US/2012/05/08/US08173814B2/abs.jpg.150x150.jpg)
8.发明授权Maleate salts of (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy)anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide and crystalline forms thereof 有权（E）-N- {4- [3-氯-4-（2-吡啶基甲氧基）苯胺基] -3-氰基-7-乙氧基-6-喹啉基} -4-（二甲基氨基）-2-丁烯酰胺的马来酸盐和 其结晶形式公开(公告)号：US08173814B2
公开(公告)日：2012-05-08
申请号：US13181375
申请日：2011-07-12
申请人： Qinghong Lu , Mannching Sherry Ku , Warren Chew , Gloria Cheal , Anthony F. Hadfield , Mahmoud Mirmehrabi
发明人： Qinghong Lu , Mannching Sherry Ku , Warren Chew , Gloria Cheal , Anthony F. Hadfield , Mahmoud Mirmehrabi
IPC分类号： C07D215/44
CPC分类号： C07D401/12 , A61K31/4709 , C07C51/412 , C07C57/145
摘要： The present invention relates to maleate salt forms of (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy)anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide, methods of preparing crystalline maleate salt forms, the associated compounds, and pharmaceutical compositions containing the same. The maleate salts are useful in treating cancers, particularly those affected by kinases of the epidermal growth factor receptor family.
摘要翻译： 本发明涉及（E）-N- {4- [3-氯-4-（2-吡啶基甲氧基）苯胺基] -3-氰基-7-乙氧基-6-喹啉基} -4-（二甲基氨基 ）-2-丁烯酰胺，制备结晶马来酸盐形式的方法，相关化合物和含有它们的药物组合物。 马来酸盐可用于治疗癌症，特别是受表皮生长因子受体家族激酶影响的癌症。
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9.发明申请MALEATE SALTS OF (E)-N--4-(DIMETHYLAMINO)-2-BUTENAMIDE AND CRYSTALLINE FORMS THEREOF 有权（E）-N-4-（二甲基氨基）-2-丁酮及其结晶形式的色谱柱公开(公告)号：US20110313166A1
公开(公告)日：2011-12-22
申请号：US13181375
申请日：2011-07-12
申请人： Qinghong LU , Mannching Sherry Ku , Warren Chew , Gloria Cheal , Anthony F. Hadfield , Mahmoud Mirmehrabi
发明人： Qinghong LU , Mannching Sherry Ku , Warren Chew , Gloria Cheal , Anthony F. Hadfield , Mahmoud Mirmehrabi
IPC分类号： C07D401/12
CPC分类号： C07D401/12 , A61K31/4709 , C07C51/412 , C07C57/145
摘要： The present invention relates to maleate salt forms of (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy)anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide, methods of preparing crystalline maleate salt forms, the associated compounds, and pharmaceutical compositions containing the same. The maleate salts are useful in treating cancers, particularly those affected by kinases of the epidermal growth factor receptor family.
摘要翻译： 本发明涉及（E）-N- {4- [3-氯-4-（2-吡啶基甲氧基）苯胺基] -3-氰基-7-乙氧基-6-喹啉基} -4-（二甲基氨基 ）-2-丁烯酰胺，制备结晶马来酸盐形式的方法，相关化合物和含有它们的药物组合物。 马来酸盐可用于治疗癌症，特别是受表皮生长因子受体家族激酶影响的癌症。
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10.发明申请Quinoline Intermediates of Receptor Tyrosine Kinase Inhibitors and the Synthesis Thereof 审中-公开喹啉中间体受体酪氨酸激酶抑制剂及其合成公开(公告)号：US20090030197A1
公开(公告)日：2009-01-29
申请号：US12200120
申请日：2008-08-28
申请人： Warren Chew , Maria Papamichelakis , Youchu Wang
发明人： Warren Chew , Maria Papamichelakis , Youchu Wang
IPC分类号： C07D413/02
CPC分类号： C07D215/54
摘要： This invention is directed to methods of preparing 4-substituted quinoline compounds as intermediates in the manufacture of receptor tyrosine kinase inhibitors and intermediate compounds used in the methods thereof, wherein the 4-substituted quinoline compound has the following general formula (I): wherein substitutions at LG″, PG, A, G, R1 and R4 are set forth in the specification.
摘要翻译： 本发明涉及制备4-取代喹啉化合物作为制备受体酪氨酸激酶抑制剂和其方法中使用的中间体化合物的中间体的方法，其中4-取代喹啉化合物具有以下通式（I）：其中取代 在LG“，PG，A，G，R1和R4在本说明书中列出。
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