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1. 发明申请

WO2006036266A1 THIENOPYRIMIDINES USEFUL AS AURORA KINASE INHIBITORS 审中-公开
标题翻译：作为AURORA激酶抑制剂有用的三烯酰基嘧啶
公开(公告)号：WO2006036266A1
公开(公告)日：2006-04-06
申请号：PCT/US2005/025340
申请日：2005-07-15
申请人： SUNESIS PHARMACEUTICALS, INC. , LEW, Willard , BASKARAN, Subramanian , OSLOB, Johan, D. , YOBURN, Josh , ZHONG, Min
发明人： LEW, Willard , BASKARAN, Subramanian , OSLOB, Johan, D. , YOBURN, Josh , ZHONG, Min
IPC分类号： C07D495/04 , A61K31/519
CPC分类号： C07D495/04
摘要： The present invention provides compounds having the formula (I) wherein R 1 , R 2 , X 1 , X 2 , L 1 , L 2 , Y and Z are as defined in classes and subclasse herein, and pharmaceutical compositions thereof, as described generally and in subclasses herein, which compounds are useful as inhibitors of protein kinase ( e.g ., Aurora), and thus are useful, for example, for the treatment of Aurora mediated diseases.
摘要翻译：本发明提供具有式（I）的化合物，其中R

2. 发明申请

WO2004087672A1 MIGRASTATIN ANALOG COMPOSITIONS AND USES THEREOF 审中-公开
标题翻译：莫替沙星类似物组合物及其用途
公开(公告)号：WO2004087672A1
公开(公告)日：2004-10-14
申请号：PCT/US2004/009380
申请日：2004-03-26
申请人： CORNELL RESEARCH FOUNDATION, INC. , SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH , HUANG, Xin-Yun , DANISHEFSKY, Samuel, J. , GAUL, Christoph , NJARDARSON, Jón, T.
发明人： HUANG, Xin-Yun , DANISHEFSKY, Samuel, J. , GAUL, Christoph , NJARDARSON, Jón, T.
IPC分类号： C07D225/02
CPC分类号： C07D313/00 , A61K31/365 , A61K31/395 , A61K31/435 , C07D225/02 , C07D405/06 , C07D495/04 , A61K2300/00
摘要： In one aspect, the present invention provides pharmaceutical compositions comprising a therapeutically effective amount of a compound of general formula (I), wherein R 1 -R 6 , R a -R C , Q, Y 1 , Y 2 and n are as defined herein, whereby the composition is formulated for administration to a subject at a dosage between about 0.1 mg/kg to about 50 mg/kg of body weight. In another aspect, the present invention provides a method for treating breast tumor metastasis in a subject comprising administering to a subject in need thereof a therapeutically effective amount of the inventive composition described directly above and a pharmaceutically acceptable carrier, adjuvant or vehicle.
摘要翻译：一方面，本发明提供包含治疗有效量的通式（I）化合物的药物组合物，其中R 1 -R 6，R a-RC，Q，Y 1，Y 2和n如本文所定义，其中组合物为配制成以约0.1mg / kg至约50mg / kg体重的剂量施用于受试者。另一方面，本发明提供一种用于治疗受试者的乳腺肿瘤转移的方法，其包括向有需要的受试者施用治疗有效量的上述直接描述的本发明组合物和药学上可接受的载体，佐剂或媒介物。

3. 发明申请

WO2004060915A2 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：WO2004060915A2
公开(公告)日：2004-07-22
申请号：PCT/US2003/038453
申请日：2003-12-03
申请人： SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH , DANISHEFSKY, Samuel, J. , DUDKIN, Vadim , MILLER, Justin
发明人： DANISHEFSKY, Samuel, J. , DUDKIN, Vadim , MILLER, Justin
IPC分类号： C07K14/47
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 1 , W 2 , R 1 , R 3 , R 4 , R 2A and R 2B 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。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学和前列腺腺癌之间的差异。

4. 发明申请

WO2004058721A2 SMALL MOLECULE MODULATORS OF HEPATOCYTE GROWTH FACTOR (SCATTER FACTOR) ACTIVITY 审中-公开
标题翻译：肝细胞生长因子（散射因子）活性的小分子调节剂
公开(公告)号：WO2004058721A2
公开(公告)日：2004-07-15
申请号：PCT/US2003/040917
申请日：2003-12-19
申请人： ANGION BIOMEDICA CORP. , ZEMBOWER, David, E. , EIZNHAMER, David
发明人： ZEMBOWER, David, E. , EIZNHAMER, David
IPC分类号： C07D231/00
CPC分类号： C07D231/12 , A61K31/4155 , C07D401/06 , C07D403/06 , C07D405/06 , C07D405/14 , C07D409/06 , C07D409/14
摘要： The present invention provides compounds having formula (I) and pharmaceutically acceptable derivatives thereof, wherein R 1 , R 2 and B are as described generally and n classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of any of a number of conditions or diseases in which HGF/SF or the activities thereof, or agonists or antagonists thereof have a therapeutically useful role.
摘要翻译：本发明提供具有式（I）化合物及其药学上可接受的衍生物，其中R 1，R 2和B如本文所述，n类和亚类，另外提供其药物组合物，以及用于其用于治疗其中HGF / SF或其活性或其激动剂或拮抗剂具有治疗有用作用的许多病症或疾病中的任何一种。

5. 发明申请

WO2006127024A1 REAGENTS AND METHODS FOR LABELING TERMINAL OLEFINS 审中-公开
标题翻译：用于标记终端油脂的试剂和方法
公开(公告)号：WO2006127024A1
公开(公告)日：2006-11-30
申请号：PCT/US2005/030669
申请日：2005-08-29
申请人： EISAI CO. LTD. , HORSTMANN, Thomas, E. , LEWIS, Bryan, M.
发明人： HORSTMANN, Thomas, E. , LEWIS, Bryan, M.
IPC分类号： C07C11/02 , A61K51/00 , C07B59/00 , C07D493/22
CPC分类号： C07D407/14 , A61K51/0421 , A61K51/0453 , C07B59/00 , C07D493/22
摘要： In one aspect, the present invention provides a method for labeling a terminal olefin, the method comprising a step of treating a terminal olefin substrate having the structure: Formula (I); with a labeled ethylene reagent in the presence of a suitable catalyst under suitable olefin metathesis reaction conditions to form a labeled terminal olefin having the structure: Formula (II) wherein R A and R B are independently hydrogen, or an aliphatic, alicyclic, heteroaliphatic, heterocyclic, aryl or heteroaryl moiety, with the proviso that R A and R B are not each hydrogen, or R A and R B taken together with the carbon atom to which they are attached form an alicyclic or heterocyclic moiety; and in Formula (II), * denotes the presence of an isotopic label on the terminal carbon atom.
摘要翻译：一方面，本发明提供一种用于标记末端烯烃的方法，该方法包括处理具有以下结构的末端烯烃基材的步骤：式（I）; 在合适的烯烃复分解反应条件下，在合适的催化剂存在下用标记的乙烯试剂形成具有以下结构的标记的末端烯烃：式（II）其中R A和R B均为 SUP>独立地是氢或脂族，脂环族，杂脂族，杂环，芳基或杂芳基部分，条件是R A和R B不是每个氢，或与它们所连接的碳原子一起形成脂环族或杂环部分的R A和R B连接; 在式（II）中，*表示在末端碳原子上存在同位素标记。

6. 发明申请

WO2006036981A2 SMALL MOLECULE MODULATORS OF CYTOKINE ACTIVITY 审中-公开
标题翻译：小分子细胞因子活性调节剂
公开(公告)号：WO2006036981A2
公开(公告)日：2006-04-06
申请号：PCT/US2005/034669
申请日：2005-09-28
申请人： ANGION BIOMEDICA CORP. , ZEMBOWER, David, E. , SINGH, Jasbir , MISHRA, Rama, K.
发明人： ZEMBOWER, David, E. , SINGH, Jasbir , MISHRA, Rama, K.
IPC分类号： C07D237/32 , C07D401/10 , C07D403/10 , C07D403/14 , A61K31/502 , A61P35/00
CPC分类号： C07D401/10 , C07D237/32 , C07D401/14 , C07D403/10 , C07D403/14
摘要： The present invention provides compounds having formula (I) or (II): Formula (I), formula (II) and pharmaceutically acceptable derivatives thereof, wherein m, p, R 1 , R 2 , R 3 and R 4 are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of any of a number of diseases, disorders or conditions associated with HGF/SF or other cytokine activity.
摘要翻译：本发明提供具有式（I）或（II）的化合物：式（I），式（II）及其药学上可接受的衍生物，其中m，p，R

7. 发明申请

WO2005056572A2 CLUSTERED MULTI-ANTIGENIC CARBOHYDRATE CONSTRUCTS, METHODS FOR THEIR PREPARATION AND USES THEREOF 审中-公开
标题翻译：分簇的多抗原碳水化合物构成物，其制备方法及其用途
公开(公告)号：WO2005056572A2
公开(公告)日：2005-06-23
申请号：PCT/US2004/040253
申请日：2004-12-01
申请人： SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH , DANISHEFSKY, Samuel, J. , KEDING, Stacy, J.
发明人： DANISHEFSKY, Samuel, J. , KEDING, Stacy, J.
IPC分类号： C07H15/04
CPC分类号： C07H15/18 , A61K31/70 , A61K31/715 , A61K38/00 , A61K39/0011 , A61K2039/55555 , A61K2039/55577 , A61K2039/55594 , A61K2039/6031 , A61K2039/6081 , A61K2039/627 , A61K2039/64 , C07B2200/11 , C07H15/04 , C07H15/10 , C07K1/1077 , C07K5/06139 , C07K9/00 , C07K14/43509
摘要： The present invention provides novel clustered multi-antigenic; constructs having the structure (I) and methods for the synthesis thereof. In still another aspect, the present invention provides methods for the treatment of cancer, preferably for the prevention of recurrence of cancer, and methods for inducing antibodies in a subject, comprising administering to a subject in need, an effective amount of any of the inventive constructs as disclosed herein, either in conjugated form or unconjugated and in combination with a suitable immunogenic carrier.
摘要翻译：本发明提供了新的成簇的多抗原性的; 具有结构（I）的构建体及其合成方法。又一方面，本发明提供了用于治疗癌症的方法，优选用于预防癌症复发，以及用于在受试者中诱导抗体的方法，所述方法包括向有需要的受试者施用有效量的任何本发明的如本文所公开的构建体，可以以缀合形式或未缀合并与合适的免疫原性载体组合。

8. 发明申请

WO2005030794A3 HEMIASTERLIN DERIVATIVES AND USES THEREOF 审中-公开
公开(公告)号：WO2005030794A3
公开(公告)日：2005-04-07
申请号：PCT/US2004/030921
申请日：2004-09-22
申请人： EISAI CO. LTD. , KOWALCZYK, James, J. , KUZNETSOV, Galina , SCHILLER, Shawn , SELETSKY, Boris, M. , SPYVEE, Mark , YANG, Hu , CAMPAGNA, Silvio, A. , FANG, Francis, G.
发明人： KOWALCZYK, James, J. , KUZNETSOV, Galina , SCHILLER, Shawn , SELETSKY, Boris, M. , SPYVEE, Mark , YANG, Hu , CAMPAGNA, Silvio, A. , FANG, Francis, G.
IPC分类号： C07K5/00
摘要： The present invention provides compounds having formula (I): and additionally provides methods for the synthesis thereof and methods for the use thereof in the treatment of cancer, wherein R 1 -R 7 , X 1 , X 2 , R, Q, and n are as defined herein.

9. 发明申请

WO2005023294A3 POLYACETAL DRUG CONJUGATES AS RELEASE SYSTEM 审中-公开
公开(公告)号：WO2005023294A3
公开(公告)日：2005-03-17
申请号：PCT/US2004/029130
申请日：2004-09-04
申请人： THE GENERAL HOSPITAL CORPORATION , PAPISOV, Mikhail, I. , YURKOVETSKIY, Alexander
发明人： PAPISOV, Mikhail, I. , YURKOVETSKIY, Alexander
IPC分类号： A61K47/48
摘要： The present invention relates to conjugate comprising a carrier substituted with one or more occurrences of a moiety having the structure (I): wherein each occurrence of M is independently a modifier having a molecular weight ≤ 10 kDa; denotes direct of indirect attachment of M to linker L M ; and each occurrence of L M is independently an optionally substituted succinamide-containing linker, whereby the modifier M is directly or indirectly attached to the succinamide linker through an amide bond, and the carrier is linked directly or indirectly to each occurrence of the succinamide linker through an ester bond. In another aspect, the invention provides compositions comprising the conjugates, methods for their preparation, and methods of use thereof in the treatment of various disorder, including, but not limited to cancer.

10. 发明申请

WO2004050711A2 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：WO2004050711A2
公开(公告)日：2004-06-17
申请号：PCT/US2003/038471
申请日：2003-12-03
申请人： SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH , 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： C08B37/00
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 l , R 2A , R 2B , R 3 , R 4 , W 1 , W 2 and W 3 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 >如本文所定义; 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。

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