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公开(公告)号：US08785481B2
公开(公告)日：2014-07-22
申请号：US13247009
申请日：2011-09-28
申请人： Douglas C. Beshore , Vadim Dudkin , Robert M. Garbaccio , Adam W. Johnson , Scott D. Kuduk , Jason W. Skudlarek , Cheng Wang , Mark E. Fraley
发明人： Douglas C. Beshore , Vadim Dudkin , Robert M. Garbaccio , Adam W. Johnson , Scott D. Kuduk , Jason W. Skudlarek , Cheng Wang , Mark E. Fraley
IPC分类号： A61K31/4245 , C07D249/04
CPC分类号： C07D249/18 , C07D401/12 , C07D403/12 , C07D413/12 , C07D417/12 , C07D471/04
摘要： The present invention is directed to ether benzotriazole derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.
摘要翻译： 本发明涉及作为代谢型谷氨酸受体，特别是mGluR2受体的增强剂的醚苯并三唑衍生物，其可用于治疗或预防与谷氨酸能力障碍相关的神经和精神病学障碍以及涉及代谢型谷氨酸受体的疾病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及代谢型谷氨酸受体的疾病中的用途。
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公开(公告)号：US20120135977A1
公开(公告)日：2012-05-31
申请号：US13247009
申请日：2011-09-28
申请人： Douglas C. Beshore , Vadim Dudkin , Robert M. Garbaccio , Adam W. Johnson , Scott D. Kuduk , Jason W. Skudlarek , Cheng Wang , Mark E. Fraley
发明人： Douglas C. Beshore , Vadim Dudkin , Robert M. Garbaccio , Adam W. Johnson , Scott D. Kuduk , Jason W. Skudlarek , Cheng Wang , Mark E. Fraley
IPC分类号： A61K31/4192 , C07D401/12 , A61K31/4439 , C07D403/12 , A61K31/506 , A61K31/497 , C07D471/04 , A61K31/437 , A61K31/496 , C07D413/12 , A61K31/5377 , A61K31/454 , A61K31/551 , A61K31/55 , C07D417/12 , A61K31/541 , A61P25/00 , A61P25/18 , C07D249/18
CPC分类号： C07D249/18 , C07D401/12 , C07D403/12 , C07D413/12 , C07D417/12 , C07D471/04
摘要： The present invention is directed to ether benzotriazole derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.
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公开(公告)号：US20130210768A1
公开(公告)日：2013-08-15
申请号：US13701039
申请日：2011-06-06
IPC分类号： C07D471/04 , C07F7/10 , C07D519/00
CPC分类号： C07D471/04 , C07D519/00 , C07F7/10
摘要： The present invention is directed to 5-substituted 1,3-dihydro-2H-imidazo[4,5-b]pyridine-2-one derivatives which are positive allosteric modulators of the mGluR2 receptor, useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 receptor is involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved, such as schizophrenia.
摘要翻译： 本发明涉及作为mGluR2受体的正变构调节剂的5-取代的1,3-二氢-2H-咪唑并[4,5-b]吡啶-2-酮衍生物，其可用于治疗或预防神经和 与谷氨酸功能障碍相关的精神疾病和涉及mGluR2受体的疾病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及代谢型谷氨酸受体的疾病如精神分裂症中的用途。
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公开(公告)号：US07531181B2
公开(公告)日：2009-05-12
申请号：US11145084
申请日：2005-06-03
CPC分类号： C07K14/005 , A61K38/00 , A61K39/12 , A61K39/21 , A61K2039/55577 , A61K2039/6018 , A61K2039/6081 , A61K2039/627 , C07K1/1077 , C07K14/375 , C07K14/505 , C12N2740/16122 , C12N2740/16134
摘要： The present invention provides multi-antigenic constructs comprising one or more carbohydrate antigens having the formula: wherein R1, R2A, R2B, R3, R4, W1, W2 and W3 are as defined herein; and additionally provides compositions thereof, and methods for their use in the treatment and/or prevention of HIV infection, and methods for inducing HIV-specific antibodies in a subject, comprising administering to a subject in need thereof, an effective amount of any of the inventive compounds as disclosed herein, either in conjugated form or unconjugated and in combination with a suitable immunogenic carrier. In another aspect, the invention provides an antibody or antibody fragment which binds specifically to a gp120 glycan or glycopeptide of the invention.
摘要翻译： 本发明提供包含一种或多种具有下式的碳水化合物抗原的多抗原构建体：其中R1，R2A，R2B，R3，R4，W1，W2和W3如本文所定义; 并且还提供其组合物及其用于治疗和/或预防HIV感染的方法，以及在受试者中诱导HIV-特异性抗体的方法，包括向有需要的受试者施用有效量的任何 本文公开的本发明化合物，其以缀合形式或未缀合并与合适的免疫原性载体组合。 另一方面，本发明提供了与本发明的gp120聚糖或糖肽特异性结合的抗体或抗体片段。
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公开(公告)号：US20110014226A1
公开(公告)日：2011-01-20
申请号：US12921890
申请日：2009-03-17
申请人： Michael J. Caulfield , Michael D. Miller , Joseph G. Joyce , Paul D. Zuck , Krista L. Getty , Vadim Dudkin , Elizabeth A. Ottinger
发明人： Michael J. Caulfield , Michael D. Miller , Joseph G. Joyce , Paul D. Zuck , Krista L. Getty , Vadim Dudkin , Elizabeth A. Ottinger
IPC分类号： A61K39/385 , C40B30/04 , A61K39/21 , A61K39/29 , A61K39/095 , A61K39/00 , C07D401/12 , C07D211/60 , A61P37/04 , A61P31/18 , A61P31/14 , A61P31/04 , A61P37/02 , A61P29/00 , A61P3/10 , A61P25/00
CPC分类号： G01N33/564 , C07D211/60 , C07D211/62 , C07D401/12 , C12Q1/18 , G01N2333/162 , G01N2333/18 , G01N2333/22 , G01N2500/02
摘要： A method to identify small molecules useful as therapeutics and/or vaccines to prevent, alleviate or ameliorate a pathogenic infection or an autoimmune disorder. The method can be used to screen small molecule test compounds for the ability to disrupt particular antigen-antibody interactions of interest. In one embodiment, the antigen is a pathogen-derived antigen and the antibody decreases or inhibits virulence of the pathogen when bound to the antigen (e.g., a neutralizing antibody, antibody with serum bactericidal activity, etc.). In another embodiment, the antigen is a self-antigen (autoantigen) and the antibody is an autoantibody that is known to be associated with a pathological condition (e.g., autoimmune disorder). Compounds that bind to the antigen or antibody disrupt binding can be used as therapeutics to decrease or inhibit the autoimmune disorder.
摘要翻译： 用于鉴定可用作治疗剂和/或疫苗以预防，减轻或改善病原体感染或自身免疫性疾病的小分子的方法。 该方法可用于筛选小分子测试化合物以破坏感兴趣的特定抗原 - 抗体相互作用的能力。 在一个实施方案中，抗原是病原体衍生的抗原，当与抗原结合时，抗体降低或抑制病原体的毒力（例如，中和抗体，具有血清杀菌活性的抗体等）。 在另一个实施方案中，抗原是自身抗原（自身抗原），抗体是已知与病理状况（例如自身免疫性疾病）相关的自身抗体。 与抗原或抗体结合的化合物破坏结合可用作治疗剂以减少或抑制自身免疫性疾病。
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公开(公告)号：US07645454B2
公开(公告)日：2010-01-12
申请号：US11145002
申请日：2005-06-03
申请人： Samuel J. Danishefsky , Vadim Dudkin , Justin Miller , David A. Scheinberg , Christophe Antczak
发明人： Samuel J. Danishefsky , Vadim Dudkin , Justin Miller , David A. Scheinberg , Christophe Antczak
IPC分类号： A61K38/04
CPC分类号： C07K14/005 , A61K38/00 , A61K39/12 , A61K39/21 , A61K2039/55577 , A61K2039/6018 , A61K2039/6081 , A61K2039/627 , C07K9/00 , C07K16/3069 , C12N9/6445 , C12N2740/16122 , C12N2740/16134 , C12Y304/21077
摘要： The present invention provides compounds having formula (I): wherein W1, W2, R1, R3, R4, R2A and R2B are as defined herein. In another aspect, the invention provides an antibody or antibody fragment which binds specifically to a normal or transformed PSA glycan or glycopeptide of the invention.
摘要翻译： 本发明提供具有式（I）的化合物：其中W1，W2，R1，R3，R4，R2A和R2B如本文所定义。 另一方面，本发明提供了与本发明的正常或转化的PSA聚糖或糖肽特异性结合的抗体或抗体片段。
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公开(公告)号：US20060229432A1
公开(公告)日：2006-10-12
申请号：US11145084
申请日：2005-06-03
CPC分类号： C07K14/005 , A61K38/00 , A61K39/12 , A61K39/21 , A61K2039/55577 , A61K2039/6018 , A61K2039/6081 , A61K2039/627 , C07K1/1077 , C07K14/375 , C07K14/505 , C12N2740/16122 , C12N2740/16134
摘要： The present invention provides multi-antigenic constructs comprising one or more carbohydrate antigens having the formula: wherein R1, R2A, R2B, R3, R4, W1, W2 and W3 are as defined herein; and additionally provides compositions thereof, and methods for their use in the treatment and/or prevention of HIV infection, and methods for inducing HIV-specific antibodies in a subject, comprising administering to a subject in need thereof, an effective amount of any of the inventive compounds as disclosed herein, either in conjugated form or unconjugated and in combination with a suitable immunogenic carrier. In another aspect, the invention provides an antibody or antibody fragment which binds specifically to a gp120 glycan or glycopeptide of the invention.
摘要翻译： 本发明提供了包含一种或多种具有下式的碳水化合物抗原的多抗原构建体：其中R 1，R 2，R 2，R 2，R 2，R 3，4，4，W 1，W 2，W 3，SO 3，SO 3， 本文定义; 并且还提供其组合物及其用于治疗和/或预防HIV感染的方法，以及在受试者中诱导HIV-特异性抗体的方法，包括向有需要的受试者施用有效量的任何 本文公开的本发明化合物，其以缀合形式或未缀合并与合适的免疫原性载体组合。 另一方面，本发明提供了与本发明的gp120聚糖或糖肽特异性结合的抗体或抗体片段。
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公开(公告)号：US20060223744A1
公开(公告)日：2006-10-05
申请号：US11145002
申请日：2005-06-03
CPC分类号： C07K14/005 , A61K38/00 , A61K39/12 , A61K39/21 , A61K2039/55577 , A61K2039/6018 , A61K2039/6081 , A61K2039/627 , C07K9/00 , C07K16/3069 , C12N9/6445 , C12N2740/16122 , C12N2740/16134 , C12Y304/21077
摘要： The present invention provides compounds having formula (I): wherein W1, W2, R1, R3, R4, R2A and R2B are as defined herein. In another aspect, the invention provides an antibody or antibody fragment which binds specifically to a normal or transformed PSA glycan or glycopeptide of the invention.
摘要翻译： 本发明提供具有式（I）的化合物：其中W 1，W 2，R 1，R 3， >，R 4，R 2A和R 2B如本文所定义。 另一方面，本发明提供了与本发明的正常或转化的PSA聚糖或糖肽特异性结合的抗体或抗体片段。
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公开(公告)号：US08765784B2
公开(公告)日：2014-07-01
申请号：US13701039
申请日：2011-06-06
IPC分类号： C07D471/04 , A61K31/415
CPC分类号： C07D471/04 , C07D519/00 , C07F7/10
摘要： The present invention is directed to 5-substituted 1,3-dihydro-2H-imidazo[4,5-b]pyridine-2-one derivatives which are positive allosteric modulators of the mGluR2 receptor, useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 receptor is involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved, such as schizophrenia.
摘要翻译： 本发明涉及作为mGluR2受体的正变构调节剂的5-取代的1,3-二氢-2H-咪唑并[4,5-b]吡啶-2-酮衍生物，其可用于治疗或预防神经和 与谷氨酸功能障碍相关的精神疾病和涉及mGluR2受体的疾病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及代谢型谷氨酸受体的疾病如精神分裂症中的用途。
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