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公开(公告)号：US06184382B2
公开(公告)日：2001-02-06
申请号：US09481979
申请日：2000-01-12
申请人： Diane C. Salazar , Walter Rodriguez , James P. Sherbine , Rick G. Woodward , Adam W. Sledeski , Matthew R. Powers , Michael K. O'Brien
发明人： Diane C. Salazar , Walter Rodriguez , James P. Sherbine , Rick G. Woodward , Adam W. Sledeski , Matthew R. Powers , Michael K. O'Brien
IPC分类号： C07D40912
CPC分类号： C07D409/12 , C07D471/04
摘要： The invention is directed to improved methods for preparing N6-substituted adenosine derivatives, to intermediates useful therefor and to methods of preparing these intermediates.
摘要翻译： 本发明涉及用于制备N6-取代的腺苷衍生物的改进方法，对其有用的中间体以及制备这些中间体的方法。
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2.发明授权Stable non-hygroscopic crystalline form of N-[N-[N-4-(piperidin-4-yl)butanoyl)-N-ethylglycyl] aspartyl]-L-.beta.-cyclohexyl alanine amide 失效N- [N- [N-4-（哌啶-4-基）丁酰基）-N-乙基甘氨酰]天冬氨酰基] -L-β-环己基丙氨酸酰胺的稳定的非吸湿结晶形式
公开(公告)号：US6153588A
公开(公告)日：2000-11-28
申请号：US251030
申请日：1999-02-18
申请人： Zofia J. Chrzan , James J. Mencel , David Toledo-Velasquez , Vincent Windisch , Rick G. Woodward , Diane C. Salazar, deceased , Narasimha M. Vemuri , Anthony J. Gardetto , Matthew R. Powers , Gregory G. Kubiak , Robert C. Liu , Benoit J. Vanasse , James P. Sherbine , Walter Rodriguez , Adam W. Sledeski
发明人： Zofia J. Chrzan , James J. Mencel , David Toledo-Velasquez , Vincent Windisch , Rick G. Woodward , Diane C. Salazar, deceased , Narasimha M. Vemuri , Anthony J. Gardetto , Matthew R. Powers , Gregory G. Kubiak , Robert C. Liu , Benoit J. Vanasse , James P. Sherbine , Walter Rodriguez , Adam W. Sledeski
IPC分类号： C07D211/70 , A61K38/00 , A61P7/02 , A61P9/10 , C07D211/34 , C07K5/02 , C07K5/062 , C07K5/083 , A61K38/06 , C07K5/00
CPC分类号： C07K5/021 , C07D211/34 , C07K5/0806 , Y02P20/55
摘要： The invention is directed to a non-hygroscopic stable crystalline form of the antithrombotic compound N-[N-[N-(4-piperdin-4-yl)butanoyl)-N-ethylglycyl]-(L)-aspartyl]-(L)-.beta.-cyclohexyl-alanine amide, to processes for preparing said stable crystalline form, to a pharmaceutical composition thereof, and intermediates thereof, and the invention is directed also to processes for preparing a compound of the formula ##STR1## wherein: A, B, Z, E.sup.1, E.sup.2, G, R, m, n, and p are as defined herein.
摘要翻译： 本发明涉及抗血栓形成的化合物N- [N- [N-（4-哌啶-4-基）丁酰基）-N-乙基甘氨酰] - （L） - 天门冬酰基] - （L ）-β-环己基 - 丙氨酸酰胺，制备所述稳定结晶形式的方法，其制备方法及其中间体，本发明还涉及制备下式化合物的方法：其中：A，B，Z ，E1，E2，G，R，m，n和p如本文所定义。
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3.发明授权Pharmaceutically useful dibenzofurancarboxamides of specific stereo-configuration 失效具有特定立体结构的药学上有用的二苯并呋喃甲酰胺
公开(公告)号：US5246942A
公开(公告)日：1993-09-21
申请号：US887594
申请日：1992-05-29
申请人： Raymond D. Youssefyeh , Henry F. Campbell , Donald E. Kuhla , John E. Airey , Scott I. Klein , Matthew R. Powers
发明人： Raymond D. Youssefyeh , Henry F. Campbell , Donald E. Kuhla , John E. Airey , Scott I. Klein , Matthew R. Powers
IPC分类号： C07D405/12 , C07D451/14 , C07D453/02 , C07D471/08 , C07D498/08
CPC分类号： C07D405/12 , C07D451/14 , C07D453/02 , C07D471/08
摘要： This invention is directed to certain dibenzofurancarboxamides and their use as 5HT.sub.3 antagonists having unique CNS, anti-emetic and gastric prokinctic activity void of any significant D.sub.2 receptor binding properties. This invention also describes novel processes necessary for their preparation.
摘要翻译： 本发明涉及某些二苯并呋喃甲酰胺及其作为5HT3拮抗剂的用途，其具有独特的CNS，抗呕吐和胃原性活性，没有任何显着的D2受体结合性质。 本发明还描述了其制备所需的新方法。
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公开(公告)号：US06429315B1
公开(公告)日：2002-08-06
申请号：US09489276
申请日：2000-01-21
申请人： Adam W. Sledeski , Luc Grondard , Matthew R. Powers , Tory H. Powner , Michael K. O'Brien , Ching T. Tsuei , Patrick Leon , Gregory G. Kubiak , Laurence Pailleres-Hubert , Benoit Viguier
发明人： Adam W. Sledeski , Luc Grondard , Matthew R. Powers , Tory H. Powner , Michael K. O'Brien , Ching T. Tsuei , Patrick Leon , Gregory G. Kubiak , Laurence Pailleres-Hubert , Benoit Viguier
IPC分类号： C07D47102
CPC分类号： C07D409/12 , C07D471/04
摘要： This invention is directed to a process for preparing N6-substituted adenosine derivatives, to intermediates useful therefor and to methods of preparing these intermediates.
摘要翻译： 本发明涉及制备N6-取代的腺苷衍生物的方法，其用途的中间体和制备这些中间体的方法。
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公开(公告)号：USH1406H
公开(公告)日：1995-01-03
申请号：US54982
申请日：1993-04-30
申请人： Matthew R. Powers
发明人： Matthew R. Powers
IPC分类号： C07D307/91
CPC分类号： C07D307/91
摘要： The present invention is directed to the synthesis of 2-chloro-cis-[5a(S)-9a(S)-(5a,6,7,8,9,9a-hexahydro)]dibenzofuran-4-carboxylic acid by a stereospecific catalytic heteroannulation synthesis free of undesirable 8-chloro-2,6-methano-2H-3,4,5,6-tetrahydro-1-benzoxocin-10-carboxylic.
摘要翻译： 本发明涉及2-氯 - 顺式 - [5a（S）-9a（S） - （5a，6,7,8,9,9a-六氢）]二苯并呋喃-4-羧酸的合成 没有不合需要的8-氯-2,6-亚甲基-2H-（3,4,5,6-四氢-1-苯并二氧杂环己烯-10-羧酸）的立体定向催化杂化合成合成。
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公开(公告)号：US5086179A
公开(公告)日：1992-02-04
申请号：US586669
申请日：1990-09-24
IPC分类号： C07D405/04 , C07C231/08 , C07C231/18 , C07C233/58 , C07D405/12 , C07D451/14 , C07D453/02 , C07D471/08 , C07D491/052 , C07D491/056 , C07D493/04 , C07D495/04 , C07D497/04 , C07D498/08
CPC分类号： C07D405/12 , C07C231/18 , C07D451/14 , C07D453/02 , C07D471/08
摘要： This invention is directed to certain dibenzofurancarboxamides and dibenzofurancarboxamide acids and their use as 5HT.sub.3 antagonists having unique CNS, anti-emetic and gastric prokinetic activity void of any significant D.sub.2 receptor binding properties. Further, this invention relates to a process for the synthesis of stereoisomeric compounds having such CNS, anti-emetic and gastric prokinetic activity.
摘要翻译： 本发明涉及某些二苯并呋喃甲酰胺和二苯并呋喃甲酰胺酸及其作为具有独特的CNS，抗呕吐和胃动力学活性的5HT3拮抗剂的作用，没有任何显着的D2受体结合性质。 此外，本发明涉及一种合成具有这种CNS，抗呕吐和胃动力学活性的立体异构体化合物的方法。
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公开(公告)号：US20100184979A1
公开(公告)日：2010-07-22
申请号：US12639507
申请日：2009-12-16
IPC分类号： C07D239/47
CPC分类号： C07D239/47 , C07D239/36
摘要： This invention is directed to a process for preparing 2-(3-{6-[2-(2,4-dichloro-phenyl)-ethylamino]-2-methoxy-pyrimidin-4-yl}-phenyl)-2-methyl-propionic acid.
摘要翻译： 本发明涉及制备2-（3- {6- [2-（2,4-二氯 - 苯基） - 乙基氨基] -2-甲氧基 - 嘧啶-4-基} - 苯基）-2-甲基 - 丙酸。
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8.发明授权Steroespecific preparation of chiral 1-aryl- and 1-heteroaryl-2-substituted ethyl-2-amines 失效手性1-芳基和1-杂芳基-2-取代的乙基-2-胺的立体特异性制备公开(公告)号：US06433172B1
公开(公告)日：2002-08-13
申请号：US09426403
申请日：1999-10-25
申请人： Luc Grondard , Jean-Paul Casimir , Patrick Leon , Michael K. O'Brien , Matthew R. Powers , Daniel Robin
发明人： Luc Grondard , Jean-Paul Casimir , Patrick Leon , Michael K. O'Brien , Matthew R. Powers , Daniel Robin
IPC分类号： C07D22118
CPC分类号： C07D333/28 , C07B2200/07 , C07C303/40 , C07D203/24
摘要： This invention is directed to methods for stereospecifically preparing [(1-optionally substituted aryl)- or (1-optionally substituted heteroaryl)]-2-substituted ethyl-2-amines, having chirality at the 2-position, and to intermediates to the substituted ethyl-2-amines.
摘要翻译： 本发明涉及立体选择性制备在2-位具有手性的[（1-任选取代的芳基） - 或（1-任选取代的杂芳基）] -2-取代的乙基-2-胺的方法， 取代的乙基-2-胺。
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![STABLE NON-HYGROSCOPIC CRYSTALLINE FORM OF N-[N-[N-(4-(PIPERIDIN-4-YL)BUTANOYL)-N-ETHYLGLYCYL]ASPARTYL]-L-&bgr;-CYCLOHEXYL ALANINE AMIDE, INTERMEDIATES THEREOF, AND PREPARATION THEREOF AND OF ANTITHROMBOTIC AZACYCLOALKYLALKANOYL PEPTIDES AND PSEUDOPEPTIDES](/abs-image/US/2004/06/22/US06753409B1/abs.jpg.150x150.jpg)
9.发明授权STABLE NON-HYGROSCOPIC CRYSTALLINE FORM OF N-[N-[N-(4-(PIPERIDIN-4-YL)BUTANOYL)-N-ETHYLGLYCYL]ASPARTYL]-L-&bgr;-CYCLOHEXYL ALANINE AMIDE, INTERMEDIATES THEREOF, AND PREPARATION THEREOF AND OF ANTITHROMBOTIC AZACYCLOALKYLALKANOYL PEPTIDES AND PSEUDOPEPTIDES 有权N- [N- [N-（4-（哌啶-4-基）丁酰基）-N-乙基甘氨酸] ASPARTYL] -L-β-环己基氨基酰胺的稳定的非水解结晶形式，其中间体及其制备方法 抗菌素亚卡那卡因胆碱酯酶和PSEUDOPEPTIDS公开(公告)号：US06753409B1
公开(公告)日：2004-06-22
申请号：US09639634
申请日：2000-08-15
申请人： Zofia J. Chrzan , James J. Mencel , David Toledo-Velasquez , Vincent Windisch , Rick G. Woodward , Diane C. Salazar , Narasimha M. Vemuri , Anthony J. Gardetto , Matthew R. Powers , Gregory G. Kubiak , Robert C. Liu , Benoit J. Vanasse , James P. Sherbine , Walter Rodriguez , Adam W. Sledeski
发明人： Zofia J. Chrzan , James J. Mencel , David Toledo-Velasquez , Vincent Windisch , Rick G. Woodward , Diane C. Salazar , Narasimha M. Vemuri , Anthony J. Gardetto , Matthew R. Powers , Gregory G. Kubiak , Robert C. Liu , Benoit J. Vanasse , James P. Sherbine , Walter Rodriguez , Adam W. Sledeski
IPC分类号： C07K508
CPC分类号： C07D211/34 , C07K5/021 , C07K5/0806
摘要： The invention is directed to a non-hygroscopic stable crystalline form of the antithrombotic compound N-[N-[N-(4-piperdin-4-yl)butanoyl)-N-ethylglycyl]-(L)-aspartyl]-(L)-&bgr;-cyclohexyl-alanine amide, to processes for preparing said stable crystalline form, to a pharmaceutical composition thereof, and intermediates thereof, and the invention is directed also to processes for preparing a compound of the formula wherein: A, B, Z, E1, E2, G, R, m, n, and p are as defined herein.
摘要翻译： 本发明涉及抗血栓形成的化合物N- [N- [N-（4-哌啶-4-基）丁酰基）-N-乙基甘氨酰] - （L） - 天门冬酰基] - （L ） - 环己基 - 丙氨酸酰胺，制备所述稳定结晶形式的方法，其制备方法及其中间体，本发明还涉及制备糠醛的化合物的方法：A，B，Z， E 1，E 2，G，R，m，n和p如本文所定义。
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10.发明授权Stereospecific preparation of chiral 1-aryl-and 1-heteroaryl-2-substituted ethyl-2-amines 失效手性1-芳基和1-杂芳基-2-取代的乙基-2-胺的立体特异性制备
公开(公告)号：US6127550A
公开(公告)日：2000-10-03
申请号：US266641
申请日：1999-03-11
申请人： Luc Grondard , Jean-Paul Casimir , Patrick Leon , Michael K. O'Brien , Matthew R. Powers , Daniel Robin
发明人： Luc Grondard , Jean-Paul Casimir , Patrick Leon , Michael K. O'Brien , Matthew R. Powers , Daniel Robin
IPC分类号： C07C303/38 , C07B53/00 , C07C211/27 , C07C213/00 , C07C215/08 , C07C303/00 , C07C303/40 , C07C307/00 , C07C311/16 , C07D203/04 , C07D203/24 , C07D221/18 , C07D333/20 , C07D333/28 , C07F1/02
CPC分类号： C07D333/28 , C07C303/40 , C07D203/24 , C07B2200/07
摘要： This invention is directed to methods for stereospecifically preparing [(1-optionally substituted aryl)- or (1-optionally substituted heteroaryl)]-2-substituted ethyl-2-amines, having chirality at the 2-position, and to intermediates to the substituted ethyl-2-amines.
摘要翻译： 本发明涉及立体选择性制备在2-位具有手性的[（1-任选取代的芳基） - 或（1-任选取代的杂芳基）] -2-取代的乙基-2-胺的方法， 取代的乙基-2-胺。
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