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    HYPERFORIN ANALOGS, METHODS OF SYNTHESIS, AND USES THEREOF
    3.
    发明申请
    HYPERFORIN ANALOGS, METHODS OF SYNTHESIS, AND USES THEREOF 审中-公开
    HYPERFORIN ANALOGS，合成方法及其用途

    公开(公告)号：WO2012167021A3

    公开(公告)日：2013-04-25

    申请号：PCT/US2012040379

    申请日：2012-06-01

    申请人： HARVARD COLLEGE ,  SHAIR MATTHEW D ,  SPARLING BRIAN A ,  MOEBIUS DAVID

    发明人： SHAIR MATTHEW D ,  SPARLING BRIAN A ,  MOEBIUS DAVID

    IPC分类号： C07C49/733 ,  C07C49/743

    CPC分类号： C07C49/753 ,  C07C45/29 ,  C07C49/733 ,  C07C49/743 ,  C07D493/08 ,  C07F7/0818 ,  C07F7/0834 ,  C07F7/1836

    摘要： The present invention provides a novel 11-step enantioselective approach to the natural product hyperforin, which enables access to a wide variety of hyperforin analogs. The present invention also provides pharmaceutical compositions comprising inventive hyperforin analogs. Hyperforin analogs synthesized using the present synthetic method are envisionsed useful in the treatment of various conditions, including, but not limited to, depression and conditions characterized by depression, inflammatory skin conditions, diabetes, asthma, chronic obstructive pulmonary disease (COPD), kidney disorders, and ischemic brain damage.

    摘要翻译： 本发明提供了对天然产物hyperforin的新型11步对映选择性方法，其能够接近各种各样的hyperforin类似物。 本发明还提供包含本发明的高福林类似物的药物组合物。 使用本合成方法合成的Hyperforin类似物被设想用于治疗各种病症，包括但不限于以抑郁症，炎性皮肤病症，糖尿病，哮喘，慢性阻塞性肺病（COPD），肾脏疾病为特征的抑郁症和病症 ，和缺血性脑损伤。

    COMPOUNDS THAT BIND OXYSTEROL BINDING PROTEINS, AND METHODS OF USE THEREOF
    4.
    发明申请
    COMPOUNDS THAT BIND OXYSTEROL BINDING PROTEINS, AND METHODS OF USE THEREOF 审中-公开
    结合OXYSTEROL结合蛋白的化合物及其使用方法

    公开(公告)号：WO2010068877A2

    公开(公告)日：2010-06-17

    申请号：PCT/US2009/067689

    申请日：2009-12-11

    申请人： PRESIDENT AND FELLOWS OF HARVARD COLLEGE ,  SHAIR, Matthew, D. ,  BURGETT, Anthony ,  ANDERSON, D., Ryan

    发明人： SHAIR, Matthew, D. ,  BURGETT, Anthony ,  ANDERSON, D., Ryan

    IPC分类号： A61K31/56 ,  A61K31/569 ,  A61K31/7056 ,  A61K31/498 ,  A61P25/28 ,  A61P35/00

    CPC分类号： A61K31/498 ,  A61K31/56 ,  A61K31/569 ,  A61K31/7056

    摘要： The invention relates in part to the discovery that certain CRAMs, such as schweinfurthin A, target OSBPs (a family of oxysterol binding proteins). Because OSBPs have been shown to be integral to atherosclerosis and Alzheimer's disease (AD), one aspect of the invention relates to the use of CRAMs, or a pharmaceutically acceptable salt, biologically active metabolite, solvate, hydrate, prodrug, enantiomer or stereoisomer thereof, in the treatment and/or prevention of atherosclerosis, Alzheimer's disease and related disorders. Another aspect of the invention relates to novel derivatives of CRAMs, or a pharmaceutically acceptable salt, biologically active metabolite, solvate, hydrate, prodrug, enantiomer or stereoisomer thereof, for the treatment and/or prevention of atherosclerosis, Alzheimer's disease and related disorders. Another aspect of the invention relates to the use of an immobilized CRAMs, such as OSW-I, to aid in screening of compounds to identify additional OSBP binders. Other aspects of the invention relate to the use of CRAMs to treat cancer, such as p21-deficient cancers.

    摘要翻译： 本发明部分涉及某些CRAMs，例如schweinfurthin A，靶向OSBPs（氧甾醇结合蛋白家族）的发现。 由于OSBP已显示为动脉粥样硬化和阿尔茨海默氏病（AD）不可缺少的一部分，因此本发明的一个方面涉及CRAM或其药学上可接受的盐，生物活性代谢物，溶剂化物，水合物，前药，对映异构体或立体异构体， 用于治疗和/或预防动脉粥样硬化，阿尔茨海默病和相关疾病。 本发明的另一方面涉及用于治疗和/或预防动脉粥样硬化，阿尔茨海默氏病和相关病症的CRAMs的新型衍生物或其药学上可接受的盐，生物活性代谢物，溶剂化物，水合物，前药，对映异构体或立体异构体。 本发明的另一方面涉及固定的CRAM例如OSW-1的用途，以帮助筛选化合物以鉴定另外的OSBP结合物。 本发明的其他方面涉及使用CRAM治疗癌症，例如p21缺陷型癌症。

    NOVEL ENEDIYNE QUINONE IMINES AND METHODS OF PREPARATION AND USE THEREOF
    6.
    发明申请
    NOVEL ENEDIYNE QUINONE IMINES AND METHODS OF PREPARATION AND USE THEREOF 审中-公开
    新型ENEDIYNE QUINONE IMINES及其制备和使用方法

    公开(公告)号：WO1996016655A1

    公开(公告)日：1996-06-06

    申请号：PCT/US1995015678

    申请日：1995-12-01

    申请人： SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH ,  DANISHEFSKY, Samuel, J. ,  SHAIR, Matthew, D. ,  YOON, Taeyoung ,  CHOU, Ting-Chao ,  MOSNY, Karoline, K.

    发明人： SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH

    IPC分类号： A61K31/47

    CPC分类号： C07D491/08 ,  A61K47/6803 ,  A61K47/6809

    摘要： A quinone imine enediyne possessing cytotoxic activity towards cancer cells having general structure (I) wherein R1, R2 and R3 are independently the same or different and are H, Br, Cl, F, NH2, CO2H, OH, linear or branched alkyl, etc.; wherein R4 is H, OH or linear or branched alkoxy, linear or branched alkoxycarbonyl, etc.; wherein R5 is H, Br, Cl, F, O=, OH or S-SR, or linear or branched alkyl, etc.; wherein R6 is H, Br, Cl, F, CO2H, OH or S-SR', or linear or branched alkyl, etc.; wherein R7 is H, OH or S-SR", or linear or branched alkyl, linear or branched alkoxycarbonyl, linear or branched alkoxy or linear or branched hydroxyalkyl; and wherein R, R' and R" are independently the same or different and are linear or branched alkyl, linear or branched acyl or linear or branched alkoxyalkyl. Also provided are conjugates of the compound with cleavable peptides, enzymes, carbohydrates and monoclonal antibodies immunoreactive with cancer cells, as well as compositions comprising the analogues and conjugates, and methods of synthesis and treatment of tumors.

    摘要翻译： 对具有通式（I）的具有通式结构（I）的癌细胞具有细胞毒性活性的醌亚胺enediyne，其中R 1，R 2和R 3独立地相同或不同，为H，Br，Cl，F，NH 2，CO 2 H，OH，直链或支链烷基等 。 其中R4是H，OH或直链或支链烷氧基，直链或支链烷氧基羰基等; 其中R 5为H，Br，Cl，F，O =，OH或S-SR，或直链或支链烷基等; 其中R6是H，Br，Cl，F，CO2H，OH或S-SR'，或直链或支链烷基等; 其中R 7是H，OH或S-SR“，或直链或支链烷基，直链或支链烷氧基羰基，直链或支链烷氧基或直链或支链羟烷基;其中R，R'和R”独立地相同或不同， 直链或支链烷基，直链或支链酰基或直链或支链烷氧基烷基。 还提供了化合物与可切割肽，酶，碳水化合物和与癌细胞免疫反应的单克隆抗体的缀合物，以及包含类似物和缀合物的组合物，以及合成和治疗肿瘤的方法。

    OSW-1 ANALOGS AND CONJUGATES, AND USES THEREOF
    7.
    发明申请
    OSW-1 ANALOGS AND CONJUGATES, AND USES THEREOF 审中-公开
    OSW-1模拟和结合及其用途

    公开(公告)号：WO2012159027A3

    公开(公告)日：2013-03-28

    申请号：PCT/US2012038562

    申请日：2012-05-18

    申请人： HARVARD COLLEGE ,  SHAIR MATTHEW D

    发明人： SHAIR MATTHEW D

    IPC分类号： C07J9/00 ,  C07C13/66

    CPC分类号： C07J17/005 ,  A61K47/48384 ,  A61K47/48561 ,  A61K47/6803 ,  A61K47/6849 ,  A61K47/6851 ,  C07H15/24 ,  C07J41/0055 ,  C07J43/003 ,  C07J51/00

    摘要： Provided are a number of compounds structurally related to OSW-1, a natural compound that binds OSBPs. Also provided are pharmaceutical compositions comprising the OSW-1 analogs, as well as methods for use of these OSW-1 analogs, or pharmaceutically acceptable salts, enantiomers, or stereoisomers thereof, in the treatment of atherosclerosis, Alzheimer's disease, and cancer, including p21 -deficient cancer. Conjugates of OSW-1 analogs with monoclonal antibodies, including monoclonal antibodies targeted to cancer cells, are also provided. Also provided are pharmaceutical compositions comprising the conjugates, as well as methods for use of these conjugates, in the treatment of cancer, including p21 -deficient cancer.

    摘要翻译： 提供了许多与OSW-1结合相关的化合物，OSW-1是结合OSBPs的天然化合物。 还提供了包含OSW-1类似物的药物组合物，以及用于治疗动脉粥样硬化，阿尔茨海默病和癌症的这些OSW-1类似物或其药学上可接受的盐，对映体或立体异构体的方法，包括p21 缺乏癌症。 还提供了OSW-1类似物与单克隆抗体的缀合物，包括靶向癌细胞的单克隆抗体。 还提供了包含缀合物的药物组合物以及用于这些缀合物的方法用于治疗癌症，包括缺乏p21的癌症。

    HYPERFORIN ANALOGS, METHODS OF SYNTHESIS, AND USES THEREOF
    8.
    发明申请
    HYPERFORIN ANALOGS, METHODS OF SYNTHESIS, AND USES THEREOF 审中-公开
    HYPERFORIN ANALOGS，合成方法及其用途

    公开(公告)号：WO2012167021A2

    公开(公告)日：2012-12-06

    申请号：PCT/US2012/040379

    申请日：2012-06-01

    申请人： PRESIDENT AND FELLOWS OF HARVARD COLLEGE ,  SHAIR, Matthew, D. ,  SPARLING, Brian, A. ,  MOEBIUS, David

    发明人： SHAIR, Matthew, D. ,  SPARLING, Brian, A. ,  MOEBIUS, David

    IPC分类号： C07C49/733 ,  C07C49/743

    CPC分类号： C07C49/753 ,  C07C45/29 ,  C07C49/733 ,  C07C49/743 ,  C07D493/08 ,  C07F7/0818 ,  C07F7/0834 ,  C07F7/1836

    摘要： The present invention provides a novel 11-step enantioselective approach to the natural product hyperforin, which enables access to a wide variety of hyperforin analogs. The present invention also provides pharmaceutical compositions comprising inventive hyperforin analogs. Hyperforin analogs synthesized using the present synthetic method are envisionsed useful in the treatment of various conditions, including, but not limited to, depression and conditions characterized by depression, inflammatory skin conditions, diabetes, asthma, chronic obstructive pulmonary disease (COPD), kidney disorders, and ischemic brain damage.

    摘要翻译： 本发明提供了对天然产物hyperforin的新型11步对映选择性方法，其能够接近各种各样的hyperforin类似物。 本发明还提供包含本发明的高福林类似物的药物组合物。 使用本合成方法合成的Hyperforin类似物被设想用于治疗各种病症，包括但不限于以抑郁症，炎性皮肤病症，糖尿病，哮喘，慢性阻塞性肺病（COPD），肾脏疾病为特征的抑郁症和病症 ，和缺血性脑损伤。

    OSW-1 ANALOGS AND CONJUGATES, AND USES THEREOF
    9.
    发明申请
    OSW-1 ANALOGS AND CONJUGATES, AND USES THEREOF 审中-公开
    OSW-1模拟和结合及其用途

    公开(公告)号：WO2012159027A2

    公开(公告)日：2012-11-22

    申请号：PCT/US2012/038562

    申请日：2012-05-18

    申请人： PRESIDENT AND FELLOWS OF HARVARD COLLEGE ,  SHAIR, Matthew, D.

    发明人： SHAIR, Matthew, D.

    CPC分类号： C07J17/005 ,  A61K47/6803 ,  A61K47/6849 ,  A61K47/6851 ,  C07H15/24 ,  C07J41/0055 ,  C07J43/003 ,  C07J51/00

    摘要： Provided are a number of compounds structurally related to OSW-1, a natural compound that binds OSBPs. Also provided are pharmaceutical compositions comprising the OSW-1 analogs, as well as methods for use of these OSW-1 analogs, or pharmaceutically acceptable salts, enantiomers, or stereoisomers thereof, in the treatment of atherosclerosis, Alzheimer's disease, and cancer, including p21 -deficient cancer. Conjugates of OSW-1 analogs with monoclonal antibodies, including monoclonal antibodies targeted to cancer cells, are also provided. Also provided are pharmaceutical compositions comprising the conjugates, as well as methods for use of these conjugates, in the treatment of cancer, including p21 -deficient cancer.

    摘要翻译： 提供了许多与OSW-1结合相关的化合物，OSW-1是结合OSBPs的天然化合物。 还提供了包含OSW-1类似物的药物组合物，以及用于治疗动脉粥样硬化，阿尔茨海默病和癌症的这些OSW-1类似物或其药学上可接受的盐，对映体或立体异构体的方法，包括p21 缺乏癌症。 还提供了OSW-1类似物与单克隆抗体的缀合物，包括靶向癌细胞的单克隆抗体。 还提供了包含缀合物的药物组合物以及用于这些缀合物的方法用于治疗癌症，包括缺乏p21的癌症。