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公开(公告)号:US07521452B2
公开(公告)日:2009-04-21
申请号:US11326155
申请日:2006-01-05
申请人: Wenxue Wu , Loc Thanh Tran , Bosco D'Sa , Feng Liang , William Leong , Hong-Chang Lee , Kevin Klopfer , Vijay Sabesen
发明人: Wenxue Wu , Loc Thanh Tran , Bosco D'Sa , Feng Liang , William Leong , Hong-Chang Lee , Kevin Klopfer , Vijay Sabesen
IPC分类号: A61K31/497 , C07D239/02
CPC分类号: C07D401/14
摘要: The present invention is generally directed to a process to directly prepare pharmaceutically acceptable salts enriched with respect to selected rotameric salts of a basic compound, by creative choice of an acid and a solvent medium. The process is particularly useful in preparing specific rotamers of pharmaceutically useful salts in desired preponderance of a rotamer.
摘要翻译: 本发明一般涉及通过创造性地选择酸和溶剂介质来直接制备相对于选择的碱性化合物的旋转异构酸盐富集的药学上可接受的盐的方法。 该方法在制备旋转异构体所需优势的药学上有用的盐的特定旋转异构体时特别有用。
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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:US07192962B2
公开(公告)日:2007-03-20
申请号:US10449650
申请日:2003-05-30
申请人: Vilas H. Dahanukar , Hoa N. Nguyen , Cecilia A. Orr , Funcheng Zhang , Ilia A. Zavialov , Kevin Klopfer , Jeffrey M. Skell , Albert W. Buchholz, Jr. , Craig D. Boyle
发明人: Vilas H. Dahanukar , Hoa N. Nguyen , Cecilia A. Orr , Funcheng Zhang , Ilia A. Zavialov , Kevin Klopfer , Jeffrey M. Skell , Albert W. Buchholz, Jr. , Craig D. Boyle
IPC分类号: A07D473/04 , A61K31/522 , A61P9/12 , A61P15/10
CPC分类号: C07D473/04
摘要: Crystalline polymorphs of 1-ethyl-3,7-dihydro-8-[(1R,2R) -(hydroxycyclopentyl)amino]-3-(2-hydroxyethyl)-7-[(3-bromo-4-methoxyphenyl)methyl]-1H-Purine-2,6-dione in Form 1 and Form 2, which exhibit x-ray powder diffraction profiles substantially the same as those shown in FIGS. 5 and 6, respectively, and which exhibit differential scanning calorimtery profiles substantially the same as those shown in FIGS. 2 and 4, respectively, and are represented by the formula: Pharmaceutical compositions comprising the polymorph Form 1 or 2 of Compound 13 and at least one excipient or carrier, and methods of using the polymorph Form 1 or 2 of Compound 13 to treat a variety of physiological disorders, such as erectile dysfunction.
摘要翻译: 1-乙基-3,7-二氢-8 - [(1R,2R) - (羟基环戊基)氨基] -3-(2-羟乙基)-7 - [(3-溴-4-甲氧基苯基)甲基] 形式1和形式2的-1H-嘌呤-2,6-二酮,其显示与图1和2所示的X-射线粉末衍射分布基本相同的X-射线粉末衍射分布。 分别示出了与图1和图2所示的相似的差示扫描量热分析图。 2和4,并且由下式表示:包含化合物13的多晶型物1或2和至少一种赋形剂或载体的药物组合物,以及使用化合物13的多晶型物1或2的方法来处理多种 的生理障碍,如勃起功能障碍。
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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: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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公开(公告)号:US20090093496A1
公开(公告)日:2009-04-09
申请号:US12331948
申请日:2008-12-10
申请人: Wenxue Wu , Loc Thanh Tran , Bosco D'Sa , Feng Liang , William Leong , Hong-Chang Lee , Kevin Klopfer , Vijay Sabesan
发明人: Wenxue Wu , Loc Thanh Tran , Bosco D'Sa , Feng Liang , William Leong , Hong-Chang Lee , Kevin Klopfer , Vijay Sabesan
IPC分类号: A61K31/506 , C07D401/14
CPC分类号: C07D401/14
摘要: The present invention is generally directed to a process to directly prepare pharmaceutically acceptable salts enriched with respect to selected rotameric salts of a basic compound, by creative choice of an acid and a solvent medium. The process is particularly useful in preparing specific rotamers of pharmaceutically useful salts in desired preponderance of a rotamer.
摘要翻译: 本发明一般涉及通过创造性地选择酸和溶剂介质来直接制备相对于选择的碱性化合物的旋转异构酸盐富集的药学上可接受的盐的方法。 该方法在制备旋转异构体所需优势的药学上有用的盐的特定旋转异构体时特别有用。
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公开(公告)号:US20060241295A1
公开(公告)日:2006-10-26
申请号:US11326155
申请日:2006-01-05
申请人: Wenxue Wu , Loc Tran , Bosco D'Sa , Feng Liang , William Leong , Hong-Chang Lee , Kevin Klopfer , Vijay Sabesen
发明人: Wenxue Wu , Loc Tran , Bosco D'Sa , Feng Liang , William Leong , Hong-Chang Lee , Kevin Klopfer , Vijay Sabesen
IPC分类号: C07D403/14
CPC分类号: C07D401/14
摘要: The present invention is generally directed to a process to directly prepare pharmaceutically acceptable salts enriched with respect to selected rotameric salts of a basic compound, by creative choice of an acid and a solvent medium. The process is particularly useful in preparing specific rotamers of pharmaceutically useful salts in desired preponderance of a rotamer.
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