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公开(公告)号：US07074890B2
公开(公告)日：2006-07-11
申请号：US10926148
申请日：2004-08-25
IPC分类号： A61K38/00
摘要： Disclosed are processes for preparing glycopeptide phosphonate derivatives having an amino-containing side chain. Several of the process steps are conducted in a single reaction vessel without isolation of intermediate reaction products, thereby generating less waste and improving the overall efficiency and yield of the process.
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公开(公告)号：US06831150B2
公开(公告)日：2004-12-14
申请号：US09847060
申请日：2001-05-01
申请人： Martin S. Linsell
发明人： Martin S. Linsell
IPC分类号： A61K3800
CPC分类号： B82Y5/00 , A61K9/0014 , A61K9/0019 , A61K38/00 , A61K47/40 , C07K9/008
摘要： The invention provides a novel reductive alkylation method useful for selectively alkylating saccharide-amines of glycopeptide antibiotics.
摘要翻译： 本发明提供了一种用于选择性烷基化糖肽抗生素的糖胺的还原性烷基化方法。
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公开(公告)号：US06562854B2
公开(公告)日：2003-05-13
申请号：US09874412
申请日：2001-06-04
申请人： Timothy J. Church , Neil Scott Cutshall , Anthony R. Gangloff , Thomas E. Jenkins , Martin S. Linsell , Joane Litvak , Kenneth D. Rice , Jeffrey R. Spencer , Vivian R. Wang
发明人： Timothy J. Church , Neil Scott Cutshall , Anthony R. Gangloff , Thomas E. Jenkins , Martin S. Linsell , Joane Litvak , Kenneth D. Rice , Jeffrey R. Spencer , Vivian R. Wang
IPC分类号： A61K314184
CPC分类号： C07D231/12 , A61F5/445 , C07D233/56 , C07D235/20 , C07D249/08 , C07D401/14 , C07D403/14 , C07D413/06 , C07D413/14 , C07D471/04 , C07F7/0812
摘要： Novel compounds, compositions and methods effective for the prevention and treatment of mast-cell mediated inflammatory disorders are described. The compounds, compositions and methods are effective for the prevention and treatment of inflammatory diseases associated with the respiratory tract, such as asthma and allergic rhinitis, as well as other types of immunomediated inflammatory disorders, such as rheumatoid arthritis, conjunctivitis and inflammatory bowel disease, various dermatological conditions, as well as certain viral conditions. The compounds comprise potent and selective inhibitors of the mast cell protease tryptase. The compositions for treating these conditions include oral, inhalant, topical and parenteral preparations as well as devices comprising such preparations.
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公开(公告)号：US06518242B1
公开(公告)日：2003-02-11
申请号：US09253670
申请日：1999-02-19
申请人： Qi-Qi Chen , John H. Griffin , Thomas E. Jenkins , J. Kevin Judice , Martin S. Linsell , Michael R. Leadbetter
发明人： Qi-Qi Chen , John H. Griffin , Thomas E. Jenkins , J. Kevin Judice , Martin S. Linsell , Michael R. Leadbetter
IPC分类号： A61K3812
摘要： Novel antibacterial agents that act as multibinding agents are disclosed. The compounds of the invention comprise from 2-10 ligands covalently connected, each of said ligands being capable of binding to a transglycosylase enzyme substrate thereby modulating the biological processes/functions thereof.
摘要翻译： 公开了作为多结合剂的新型抗菌剂。 本发明的化合物包含共价连接的2-10个配体，每个所述配体能够结合转糖基酶底物，从而调节其生物学过程/功能。
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公开(公告)号：US20120058989A1
公开(公告)日：2012-03-08
申请号：US13082269
申请日：2011-04-07
申请人： Allan S. Wagman , Heinz E. Moser , Glenn A. McEnroe , James B. Aggen , Martin S. Linsell , Adam A. Goldblum , John H. Griffin , Lloyd J. Simons , Thomas R. Belliotti , Christina R. Harris , Toni-Jo Poel , Michael J. Melnick , Ricky D. Gaston
发明人： Allan S. Wagman , Heinz E. Moser , Glenn A. McEnroe , James B. Aggen , Martin S. Linsell , Adam A. Goldblum , John H. Griffin , Lloyd J. Simons , Thomas R. Belliotti , Christina R. Harris , Toni-Jo Poel , Michael J. Melnick , Ricky D. Gaston
IPC分类号： A61K31/553 , A61P31/04 , C07D498/14 , C07D471/14 , A61K31/55 , A61K31/5517
CPC分类号： C07D471/14 , C07D498/14 , C07D513/14
摘要： Compounds having antibacterial activity are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein A, B, D, E, G, R1, R2, R3, R4, R5, R6 and R7 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
摘要翻译： 公开了具有抗菌活性的化合物。 该化合物具有以下结构（I）：包括其立体异构体，药学上可接受的盐和前药，其中A，B，D，E，G，R 1，R 2，R 3，R 4，R 5，R 6和R 7如本文所定义。 还公开了与这种化合物的制备和使用相关的方法以及包含这些化合物的药物组合物。
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公开(公告)号：US08093354B2
公开(公告)日：2012-01-10
申请号：US12759076
申请日：2010-04-13
摘要： Disclosed are processes for preparing glycopeptide phosphonate derivatives having an amino-containing side chain. Several of the process steps are conducted in a single reaction vessel without isolation of intermediate reaction products, thereby generating less waste and improving the overall efficiency and yield of the process.
摘要翻译： 公开了制备具有含氨基侧链的糖肽膦酸酯衍生物的方法。 几个工艺步骤在单个反应容器中进行，而不分离中间反应产物，从而产生较少的废物并提高该方法的总体效率和产率。
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57.发明申请公开(公告)号：US20090215982A1
公开(公告)日：2009-08-27
申请号：US12437778
申请日：2009-05-08
申请人： J. Kevin Judice , Paul Ross Fatheree , Bernice M.T. Lam , Michael R. Leadbetter , Martin S. Linsell , YongQi Mu , Sean Gary Trapp , Guang Yang , Yan Zhu
发明人： J. Kevin Judice , Paul Ross Fatheree , Bernice M.T. Lam , Michael R. Leadbetter , Martin S. Linsell , YongQi Mu , Sean Gary Trapp , Guang Yang , Yan Zhu
IPC分类号： C07K9/00
摘要： Disclosed are derivatives of glycopeptide compounds having at least one substituent of the formula: —Ra—Y—Rb-(Z)x where Ra, Rb, Y, Z and x are as defined, and pharmaceutical compositions containing such glycopeptide derivatives. The disclosed glycopeptide derivatives are useful as antibacterial agents.
摘要翻译： 公开了具有至少一个下式的取代基的糖肽化合物的衍生物：<？in-line-formula description =“In-line formula”end =“lead”→> Ra-Y-Rb-（Z）x < 其中Ra，Rb，Y，Z和x如上定义，以及含有这样的糖肽衍生物的药物组合物，在线公式描述=“In-line Formulas”end =“tail”？ 所公开的糖肽衍生物可用作抗菌剂。
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公开(公告)号：US20090111850A1
公开(公告)日：2009-04-30
申请号：US12112726
申请日：2008-04-30
IPC分类号： A61K31/47 , A61K31/165 , A61P11/00
CPC分类号： C07C233/43 , C07D215/26 , C07D215/38
摘要： The invention provides novel β2 adrenergic receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with β2 adrenergic receptor activity, and processes and intermediates useful for preparing such compounds.
摘要翻译： 本发明提供新颖的β2肾上腺素能受体激动剂化合物。 本发明还提供包含这些化合物的药物组合物，使用这些化合物治疗与β2肾上腺素能受体活性有关的疾病的方法，以及可用于制备这些化合物的方法和中间体。
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公开(公告)号：US20080312407A1
公开(公告)日：2008-12-18
申请号：US11977429
申请日：2007-10-24
IPC分类号： C07K9/00
CPC分类号： C07K9/008 , A61K9/0014 , A61K9/0019 , A61K9/0095 , A61K9/02 , A61K9/19 , A61K9/2018 , A61K9/4858 , A61K38/14 , A61K47/06 , A61K47/12 , A61K47/26 , A61K47/40 , A61K47/6951 , B82Y5/00
摘要： Disclosed are glycopeptides that are substituted with one or more substituents each comprising one or more phosphono groups; and pharmaceutical compositions containing such glycopeptide derivatives. The disclosed glycopeptide derivatives are useful as antibacterial agents.
摘要翻译： 公开了被一个或多个各自包含一个或多个膦酰基的取代基取代的糖肽; 和含有这些糖肽衍生物的药物组合物。 所公开的糖肽衍生物可用作抗菌剂。
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公开(公告)号：US07101964B2
公开(公告)日：2006-09-05
申请号：US11128901
申请日：2005-05-13
申请人： Martin S. Linsell
发明人： Martin S. Linsell
IPC分类号： C07K7/50
摘要： This invention provides 9-fluorenylmethoxycarbonyl compounds that are useful as intermediates for preparing glycopeptide antibiotics.
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