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1. 发明申请

WO2004050711A3 GP120 SPECIFIC ANTIGENS, CONJUGATES THEREOF, METHODS FOR THEIR PREPARATION AND USES THEREOF 审中-公开
标题翻译： GP120特异性抗原，与其结合，其制备方法及其用途
公开(公告)号：WO2004050711A3
公开(公告)日：2005-01-27
申请号：PCT/US0338471
申请日：2003-12-03
申请人： SLOAN KETTERING INST CANCER , DANISHEFSKY SAMUEL J , DUDKIN VADIM , GENG XUDONG , MANDAL MIHIRBARAN
发明人： DANISHEFSKY SAMUEL J , DUDKIN VADIM , GENG XUDONG , MANDAL MIHIRBARAN
IPC分类号： A61K39/21 , C07K1/107 , C07K14/16 , C07K14/375 , C07K14/505
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 compounds having formula (I): wherein R , R , R , R , R , W , W and W are as defined herein; and additionally provides methods for the synthesis thereof, compositions thereof, and methods of use thereof in the treatment of HIV, methods for the prevention of HIV, 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 gp 120 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R 1，R 2A，R 2B，R 3，R 4，W 1，W 2和W 3 >如本文定义; 并且另外提供其合成方法，其组合物及其用于治疗HIV的方法，用于预防HIV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，有效量的本文公开的任何本发明化合物，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。

2. 发明申请

WO2004060915A3 PROSTATE SPECIFIC ANTIGENS, CONJUGATES THEREOF, METHODS FOR THEIR PREPARATION AND USES THEREOF. 审中-公开
标题翻译：前列腺特异性抗原，与其结合，其制备方法及其用途。
公开(公告)号：WO2004060915A3
公开(公告)日：2005-03-03
申请号：PCT/US0338453
申请日：2003-12-03
申请人： SLOAN KETTERING INST CANCER , DANISHEFSKY SAMUEL J , DUDKIN VADIM , MILLER JUSTIN
发明人： DANISHEFSKY SAMUEL J , DUDKIN VADIM , MILLER JUSTIN
IPC分类号： A61K39/21 , C07K14/16 , C12N9/64 , C07K9/00 , G01N33/574
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 W , W , R , R , R , R and R are as defined herein; and additionally provides methods for the synthesis thereof, compositions thereof, and methods of use thereof in the treatment of cancer, methods for the prevention of recurrence of cancer, and methods for inducing 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 normal or transformed PSA glycan or glycopeptide of the invention. In another aspect, the invention provides an immunoassay method for the quantitative determination of normal or transformed PSA in a biological sample. In another aspect, the invention provides an immunoassay kit for assessing the presence and/or amount of normal or transformed PSA in a sample. In another aspect, the invention provides a diagnostic kit for diagnosing an adenocarcinoma of the prostate in an individual suspected of suffering therefrom, or for differentiating between a benign pathology of the prostate and an adenocarcinoma of the prostate in an individual suspected of suffering therefrom.
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 ; 并且另外提供其合成方法，其组合物及其在癌症治疗中的应用方法，用于预防癌症复发的方法，以及在受试者中诱导抗体的方法，包括向有需要的受试者施用，有效量的本文公开的任何本发明化合物，其以缀合形式或未偶联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。另一方面，本发明提供了用于定量测定生物样品中正常或转化的PSA的免疫测定方法。在另一方面，本发明提供了用于评估样品中正常或转化的PSA的存在和/或量的免疫测定试剂盒。另一方面，本发明提供了一种诊断试剂盒，用于诊断怀疑患有其的个体中的前列腺腺癌，或用于区分怀疑患有前列腺的前列腺的良性病理和前列腺腺癌。

3. 发明申请

WO2006017180A3 GLYCOPEPTIDE DIMERS AND USES THEREOF 审中-公开
标题翻译：谷氨酸二聚体及其用途
公开(公告)号：WO2006017180A3
公开(公告)日：2006-07-20
申请号：PCT/US2005024273
申请日：2005-07-08
申请人： PROGENICS PHARM INC , SLOAN KETTERING INST CANCER , DANISHEFSKY SAMUEL , DUDKIN VADIM , GENG XUDONG , MANDAL MIHIRIBARAN , OLSON WILLIAM , ORLOVA MARIANNA
发明人： DANISHEFSKY SAMUEL , DUDKIN VADIM , GENG XUDONG , MANDAL MIHIRIBARAN , OLSON WILLIAM , ORLOVA MARIANNA
IPC分类号： A61K38/16
CPC分类号： C07K9/00 , Y02P20/55
摘要： This invention provides compounds represented by the formula: (A-X---) n wherein each A- is independently a carbohydrate represented by the general structure: wherein each of B, C, D, E, F, G, H, I, and J independently represents a sugar moiety, a sugar moiety having a protecting group attached thereto, a hydrogen, or an oxygen protecting group, provided that no more than two of B, C, D, and E is simultaneously a sugar moiety or a sugar moiety having a protecting group attached thereto and that no more than one of F, G, H, and I is simultaneously a sugar moiety or a sugar moiety having a protecting group attached thereto and wherein represents a covalent bond between the carbohydrate and the peptide; wherein each R 1 independently represents a hydrogen or an oxygen protecting group; wherein each R 2A and each R 2B is independently a hydrogen or a nitrogen protecting group; wherein X is a peptide; wherein --- represents a disulfide bond; and wherein n represents an integer = 2.
摘要翻译：本发明提供由下式表示的化合物：其中每个A-独立地是由通式结构表示的碳水化合物：其中B，C，D，E，F， G，H，I和J独立地表示糖部分，具有与其连接的保护基的糖部分，氢或氧保护基，条件是B，C，D和E中不超过两个同时糖部分或具有与其连接的保护基的糖部分，并且F，G，H和I中不超过一个同时是糖部分或具有与其连接的保护基的糖部分，并且其中表示碳水化合物和肽; 其中每个R 1独立地表示氢或氧保护基; 其中每个R 2A和每个R 2B独立地是氢或氮保护基; 其中X是肽; 其中---表示二硫键; 并且其中n表示整数= 2。

4. 发明申请

WO2012054366A2 SUBSTITUTED AMINO-TRIAZOLYL PDE10 INHIBITORS 审中-公开
标题翻译：取代的氨基三唑基PDE10抑制剂
公开(公告)号：WO2012054366A2
公开(公告)日：2012-04-26
申请号：PCT/US2011056504
申请日：2011-10-17
申请人： MERCK SHARP & DOHME , SHIPPS GERALD W JR , SAUVAGNAT BERENEGERE , BRACKEN JACK , MCELROY WILLIAM T , COX CHRISTOPHER D , HO GINNY , MCGAUGHEY GEORGIA , DENG YONGQI , ZHU LIANG , DUDKIN VADIM , STEELE THOMAS G , STEEN JUSTIN T
发明人： SHIPPS GERALD W JR , SAUVAGNAT BERENEGERE , BRACKEN JACK , MCELROY WILLIAM T , COX CHRISTOPHER D , HO GINNY , MCGAUGHEY GEORGIA , DENG YONGQI , ZHU LIANG , DUDKIN VADIM , STEELE THOMAS G , STEEN JUSTIN T
IPC分类号： A61K31/506
CPC分类号： C07D403/14 , C07D249/14 , C07D401/14 , C07D403/04 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04
摘要： The present invention is directed to substituted amino-triazolyl compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
摘要翻译：本发明涉及可用作治疗与磷酸二酯酶10（PDE10）相关的中枢神经系统疾病的治疗剂的取代的氨基 - 三唑基化合物。本发明还涉及这些化合物用于治疗神经和精神疾病如精神分裂症，精神病或亨廷顿氏病以及与纹状体功能减退或基底神经节功能障碍相关的疾病的用途。

5. 发明申请

WO2011156245A3 POSITIVE ALLOSTERIC MODULATORS OF MGLUR2 审中-公开
标题翻译： MGLUR2的阳性免疫调节剂
公开(公告)号：WO2011156245A3
公开(公告)日：2012-04-19
申请号：PCT/US2011039205
申请日：2011-06-06
申请人： MERCK SHARP & DOHME , ARRINGTON KENNETH L , DUDKIN VADIM , LAYTON MARK E , PERO JOSEPH E , REIF ALEXANDER J
发明人： ARRINGTON KENNETH L , DUDKIN VADIM , LAYTON MARK E , PERO JOSEPH E , REIF ALEXANDER J
IPC分类号： A01N43/50 , 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。

6. 发明申请

WO2009117409A3 A HIGH THROUGHPUT PROTEIN INTERACTION ASSAY 审中-公开
标题翻译：高通量蛋白质相互作用测定
公开(公告)号：WO2009117409A3
公开(公告)日：2009-12-30
申请号：PCT/US2009037390
申请日：2009-03-17
申请人： MERCK & CO INC , CAULFIELD MICHAEL J , MILLER MICHAEL D , JOYCE JOSEPH , ZUCK PAUL D , GETTY KRISTA L , DUDKIN VADIM , OTTINGER ELIZABETH A
发明人： CAULFIELD MICHAEL J , MILLER MICHAEL D , JOYCE JOSEPH , ZUCK PAUL D , GETTY KRISTA L , DUDKIN VADIM , OTTINGER ELIZABETH A
IPC分类号： C40B30/04
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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