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公开(公告)号：US20050192345A1
公开(公告)日：2005-09-01
申请号：US11045772
申请日：2005-01-28
申请人： Mengwei Hu , Younong Yu , Michael Dwyer , Arthur Taveras , Agnes Kim-Meade , Jianguo Yin , Xiaoyong Fu , Timothy McAllister , Shuyi Zhang , Kevin Klopfer
发明人： Mengwei Hu , Younong Yu , Michael Dwyer , Arthur Taveras , Agnes Kim-Meade , Jianguo Yin , Xiaoyong Fu , Timothy McAllister , Shuyi Zhang , Kevin Klopfer
IPC分类号： A61K31/34 , A61K31/341 , C07D307/52
CPC分类号： C07D307/52
摘要： The present invention relates to four distinct crystalline polymorphs of a monohydrate of Compound A having the following chemical structure: These four polymorphic forms, herein referred to as Forms I, II, III and IV are active as a CXC-chemokine receptor ligands. The invention is further directed to formulations, methods of treatment, and processes of synthesis of these polymorphic forms.
摘要翻译： 本发明涉及具有以下化学结构的化合物A的一水合物的四种不同的结晶多晶型物：这四种多晶型物，在本文中称为形式I，II，III和IV，作为CXC-趋化因子受体配体是有活性的。 本发明进一步涉及这些多晶形式的制剂，治疗方法和合成方法。
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公开(公告)号：US20080279822A1
公开(公告)日：2008-11-13
申请号：US12174470
申请日：2008-07-16
申请人： Mengwei Hu , Younong Yu , Michael Dwyer , Arthur Taveras , Agnes Kim-Meade , Jianguo Yin , Xiaoyong Fu , Timothy McAllister , Shuyi Zhang , Kevin Klopfer
发明人： Mengwei Hu , Younong Yu , Michael Dwyer , Arthur Taveras , Agnes Kim-Meade , Jianguo Yin , Xiaoyong Fu , Timothy McAllister , Shuyi Zhang , Kevin Klopfer
IPC分类号： A61K31/341 , C07D307/54 , A61P25/00 , A61P29/00 , A61P35/00 , A61P11/00 , A61P31/12 , A61P19/02 , A61K39/395 , A61K31/519 , A61K31/52 , A61K38/21
CPC分类号： C07D307/52
摘要： The present invention relates to four distinct crystalline polymorphs of a monohydrate of Compound A having the following chemical structure: Compound A. These four polymorphic forms, herein referred to as Forms I, II III and IV are active as a CXC-chemokine receptor ligands. The invention is further directed to formulations, methods of treatment, and processes of synthesis of these polymorphic forms.
摘要翻译： 本发明涉及具有以下化学结构的化合物A的一水合物的四种不同的结晶多晶型物：化合物A.这四种多晶型物，本文称为形式I，II III和IV作为CXC-趋化因子受体配体是有活性的。 本发明进一步涉及这些多晶形式的制剂，治疗方法和合成方法。
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公开(公告)号：US08207221B2
公开(公告)日：2012-06-26
申请号：US12174470
申请日：2008-07-16
申请人： Mengwei Hu , Younong Yu , Michael P. Dwyer , Arthur G. Taveras , Agnes Kim-Meade , Jianguo Yin , Xiaoyong Fu , Timothy L. McAllister , Shuyi Zhang , Kevin Klopfer
发明人： Mengwei Hu , Younong Yu , Michael P. Dwyer , Arthur G. Taveras , Agnes Kim-Meade , Jianguo Yin , Xiaoyong Fu , Timothy L. McAllister , Shuyi Zhang , Kevin Klopfer
IPC分类号： A61K31/341 , C07D307/504
CPC分类号： C07D307/52
摘要： The present invention relates to four distinct crystalline polymorphs of a monohydrate of Compound A having the following chemical structure: These four polymorphic forms, herein referred to as Forms I, II, III and IV are active as a CXC-chemokine receptor ligands. The invention is further directed to formulations, methods of treatment, and processes of synthesis of these polymorphic forms.
摘要翻译： 本发明涉及具有以下化学结构的化合物A的一水合物的四种不同的结晶多晶型物：这四种多晶型物，在本文中称为形式I，II，III和IV，作为CXC-趋化因子受体配体是有活性的。 本发明进一步涉及这些多晶形式的制剂，治疗方法和合成方法。
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![Synthesis of 2-hydroxy-N,N-dimethyl-3-[[2-(1(R)-(5-methyl-2-furany)propyl]amino]-3,4-dioxo-1-cyclobuten-1-yl]amino]benzamide](/abs-image/US/2006/09/14/US20060205961A1/abs.jpg.150x150.jpg)
4.发明申请Synthesis of 2-hydroxy-N,N-dimethyl-3-[[2-(1(R)-(5-methyl-2-furany)propyl]amino]-3,4-dioxo-1-cyclobuten-1-yl]amino]benzamide 有权合成2-羟基-N，N-二甲基-3 - [[2-（1（R） - （5-甲基-2-呋喃基）丙基]氨基] -3,4-二氧代-1-环丁烯-1-酮 吡啶-3-基]氨基]苯甲酰胺公开(公告)号：US20060205961A1
公开(公告)日：2006-09-14
申请号：US11430687
申请日：2006-05-09
申请人： Jianguo Yin , Xiaoyong Fu , Shuyi Zhang , Timothy McAllister , Agnes Kim-Meade , Jason Winters , Anantha Sudhakar , Doris Schumacher
发明人： Jianguo Yin , Xiaoyong Fu , Shuyi Zhang , Timothy McAllister , Agnes Kim-Meade , Jason Winters , Anantha Sudhakar , Doris Schumacher
IPC分类号： C07D307/02 , C07C237/22
CPC分类号： C07D307/52 , C07C235/60
摘要： Disclosed is a process for making the compound of formula I: using the compounds of formulas II, Q, and XI or XII: wherein A is selected from the group consisting of Br, Cl and I (with Br being preferred); and R represents (C1-C10)alkyl. Also disclosed are intermediate compounds that are made in the disclosed process.
摘要翻译： 公开了制备式I化合物的方法：使用式II，Q和XI或XII的化合物：其中A选自Br，Cl和I（其中Br优选）; R表示（C 1 -C 10）烷基。 还公开了在所公开的方法中制备的中间体化合物。
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5.发明申请Process and intermediates for the synthesis of 2-(quinolin-5-yl)-4,5 disubstituted-azole derivatives 失效用于合成2-（喹啉-5-基）-4,5二取代 - 唑衍生物的方法和中间体公开(公告)号：US20080045718A1
公开(公告)日：2008-02-21
申请号：US11891348
申请日：2007-08-10
申请人： Timothy Cutarelli , Xiaoyong Fu , Timothy McAllister , Michael Reeder , Jianguo Yin , Kelvin Yong , Shuyi Zhang
发明人： Timothy Cutarelli , Xiaoyong Fu , Timothy McAllister , Michael Reeder , Jianguo Yin , Kelvin Yong , Shuyi Zhang
IPC分类号： C07D401/04 , C07C69/34 , C07D401/14 , C07C69/76
CPC分类号： C07D413/04 , C07C271/22 , C07D413/14
摘要： This application discloses a novel process to synthesize 2-(Quinolin-5yo)-4,5-Disubstituted-Azole derivatives, which may be used, for example, as PDE IV inhibitor compounds in pharmaceutical preparations.
摘要翻译： 本申请公开了一种合成2-（喹啉-5-基）-4,5-二取代 - 唑衍生物的新方法，其可用作药物制剂中的PDE IV抑制剂化合物。
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![Synthesis of 2-Hydroxy-N,N-dimethyl-3-[[2-[[1(R)-(5-methyl-2-furanyl)propyl]amino]-3,4-dioxo-1-cyclobuten-1-yl]amino]benzamide](/abs-image/US/2011/03/22/US07910775B2/abs.jpg.150x150.jpg)
6.发明授权Synthesis of 2-Hydroxy-N,N-dimethyl-3-[[2-[[1(R)-(5-methyl-2-furanyl)propyl]amino]-3,4-dioxo-1-cyclobuten-1-yl]amino]benzamide 有权合成2-羟基-N，N-二甲基-3 - [[2 - [[1（R） - （5-甲基-2-呋喃基）丙基]氨基] -3,4-二氧代-1-环丁烯-1 - 基]氨基]苯甲酰胺公开(公告)号：US07910775B2
公开(公告)日：2011-03-22
申请号：US12253356
申请日：2008-10-17
申请人： Jianguo Yin , Xiaoyong Fu , Shuyi Zhang , Timothy L. McAllister , Agnes S. Kim-Meade , Jason L. Winters , Anantha Sudhakar , Doris P. Schumacher
发明人： Jianguo Yin , Xiaoyong Fu , Shuyi Zhang , Timothy L. McAllister , Agnes S. Kim-Meade , Jason L. Winters , Anantha Sudhakar , Doris P. Schumacher
IPC分类号： C07C231/02 , C07C233/05
CPC分类号： C07D307/52 , C07C235/60
摘要： Disclosed is a process for making the compound of formula I: using the compounds of formulas II, Q, and XI or XII: wherein A is selected from the group consisting of Br, Cl and I (with Br being preferred); and R represents (C1-C10)alkyl. Also disclosed are intermediate compounds that are made in the disclosed process.
摘要翻译： 公开了制备式I化合物的方法：使用式II，Q和XI或XII的化合物：其中A选自Br，Cl和I（其中Br优选）; R表示（C1-C10）烷基。 还公开了在所公开的方法中制备的中间体化合物。
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7.发明授权Process and intermediates for the synthesis of 2-(quinolin-5-yl)-4,5 disubstituted-azole derivatives 失效用于合成2-（喹啉-5-基）-4,5二取代 - 唑衍生物的方法和中间体公开(公告)号：US07985860B2
公开(公告)日：2011-07-26
申请号：US11891348
申请日：2007-08-10
申请人： Timothy D. Cutarelli , Xiaoyong Fu , Timothy L. McAllister , Michael R. Reeder , Jianguo Yin , Kelvin H. Yong , Shuyi Zhang
发明人： Timothy D. Cutarelli , Xiaoyong Fu , Timothy L. McAllister , Michael R. Reeder , Jianguo Yin , Kelvin H. Yong , Shuyi Zhang
IPC分类号： C07D215/38
CPC分类号： C07D413/04 , C07C271/22 , C07D413/14
摘要： This application discloses a novel process to synthesize 2-(Quinolin-5yo)-4,5-Disubstituted-Azole derivatives, which may be used, for example, as PDE IV inhibitor compounds in pharmaceutical preparations.
摘要翻译： 本申请公开了一种合成2-（喹啉-5-基）-4,5-二取代 - 唑衍生物的新方法，其可用作药物制剂中的PDE IV抑制剂化合物。
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![Synthesis of 2-hydroxy-n,n-dimethyl-3-[[2-[[1(r)-(5-methyl-2-furanyl)propyl]amino]-3,4-dioxo-1-cyclobuten-1-yl]amino]benzamide](/abs-image/US/2008/12/09/US07462740B2/abs.jpg.150x150.jpg)
8.发明授权Synthesis of 2-hydroxy-n,n-dimethyl-3-[[2-[[1(r)-(5-methyl-2-furanyl)propyl]amino]-3,4-dioxo-1-cyclobuten-1-yl]amino]benzamide 有权合成2-羟基-N，正二甲基-3 - [[2 - [[1（R） - （5-甲基-2-呋喃基）丙基]氨基] -3,4-二氧代-1-环丁烯-1 - 基]氨基]苯甲酰胺公开(公告)号：US07462740B2
公开(公告)日：2008-12-09
申请号：US11430687
申请日：2006-05-09
申请人： Jianguo Yin , Xiaoyong Fu , Shuyi Zhang , Timothy L. McAllister , Agnes S. Kim-Meade , Jason L. Winters , Anantha Sudhakar , Doris P. Schumacher
发明人： Jianguo Yin , Xiaoyong Fu , Shuyi Zhang , Timothy L. McAllister , Agnes S. Kim-Meade , Jason L. Winters , Anantha Sudhakar , Doris P. Schumacher
IPC分类号： C07C231/02 , C07C233/65
CPC分类号： C07D307/52 , C07C235/60
摘要： Disclosed is a process for making the compound of formula I: using the compounds of formulas II, Q, and XI or XII: wherein A is selected from the group consisting of Br, Cl and I (with Br being preferred); and R represents (C1-C10)alkyl. Also disclosed are intermediate compounds that are made in the disclosed process.
摘要翻译： 公开了制备式I化合物的方法：使用式II，Q和XI或XII的化合物：其中A选自Br，Cl和I（其中Br优选）; R表示（C1-C10）烷基。 还公开了在所公开的方法中制备的中间体化合物。
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9.发明授权Process and intermediates for the synthesis of 1,2-substituted 3,4-dioxo-1-cyclobutene compounds 有权用于合成1,2-取代的3,4-二氧代-1-环丁烯化合物的方法和中间体公开(公告)号：US08519168B2
公开(公告)日：2013-08-27
申请号：US12665913
申请日：2008-07-01
申请人： Xiaoyong Fu , Frank Bruno Guenter , Agnes S. Kim-Meade , Kenneth Stanley Matthews , Mathew Thomas Maust , Gerald Werne , Jason L. Winters , Jianguo Yin , Shuyi Zhang , David J. Moloznik
发明人： Xiaoyong Fu , Frank Bruno Guenter , Agnes S. Kim-Meade , Kenneth Stanley Matthews , Mathew Thomas Maust , Timothy L. McAllister , Gerald Werne , Jason L. Winters , Jianguo Yin , Shuyi Zhang
IPC分类号： C07D307/40
CPC分类号： C07D307/52 , C07C231/12 , C07C237/44
摘要： This application discloses a novel process for the preparation of 1,2-substituted 3,4-dioxo-1-cyclobutene compounds, which have utility, for example, in the treatment of CXC chemokine-mediated diseases, and intermediates useful in the synthesis thereof.
摘要翻译： 本申请公开了一种制备1,2-取代的3,4-二氧代-1-环丁烯化合物的新方法，其可用于例如治疗CXC趋化因子介导的疾病，以及可用于其合成的中间体 。
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![Synthesis of 2-hydroxy-N,N-dimethyl-3-[ [2-[1 (R)-(5-methyl-2-furanyl)propyl]amino]-3,4-dioxo-1-cyclobuten-1-yl]aminobenzamide](/abs-image/US/2006/07/04/US07071342B2/abs.jpg.150x150.jpg)
10.发明授权Synthesis of 2-hydroxy-N,N-dimethyl-3-[ [2-[1 (R)-(5-methyl-2-furanyl)propyl]amino]-3,4-dioxo-1-cyclobuten-1-yl]aminobenzamide 有权合成2-羟基-N，N-二甲基-3 - [[2- [1（R） - （5-甲基-2-呋喃基）丙基]氨基] -3,4-二氧代-1-环丁烯-1-酮 吡啶-3-基]氨基苯甲酰胺公开(公告)号：US07071342B2
公开(公告)日：2006-07-04
申请号：US10826456
申请日：2004-04-16
申请人： Jianguo Yin , Xiaoyong Fu , Shuyi Zhang , Timothy L. McAllister , Agnes S. Kim-Meade , Jason L. Winters , Anantha Sudhakar , Doris P. Schumacher
发明人： Jianguo Yin , Xiaoyong Fu , Shuyi Zhang , Timothy L. McAllister , Agnes S. Kim-Meade , Jason L. Winters , Anantha Sudhakar , Doris P. Schumacher
IPC分类号： C07D307/54
CPC分类号： C07D307/52 , C07C235/60
摘要： Disclosed is a process for making the compound of formula I: using the compounds of formulas II, Q, and XI or XII: wherein A is selected from the group consisting of Br, Cl and I (with Br being preferred); and R represents (C1–C10)alkyl. Also disclosed are intermediate compounds that are made in the disclosed process.
摘要翻译： 公开了制备式I化合物的方法：使用式II，Q和XI或XII的化合物：其中A选自Br，Cl和I（其中Br优选）; R表示（C 1 -C 10）烷基。 还公开了在所公开的方法中制备的中间体化合物。
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