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1.发明授权Belactosin derivatives as therapeutic agents/biological probes and their synthesis 失效贝米松星衍生物作为治疗剂/生物探针及其合成公开(公告)号：US08119653B2
公开(公告)日：2012-02-21
申请号：US11775154
申请日：2007-07-09
IPC分类号： A61K31/436 , C07D221/18
CPC分类号： C07D407/12 , C07D305/12
摘要： Derivatives of belactosin and their synthesis are disclosed. In certain embodiments, compounds of the present invention exhibit anti-cancer, antiviral, antibiotic, and/or auto-immune therapeutic abilities. In general, methods of synthesis disclosed herein allow for introduction of a variety of substituents at numerous positions as well as the facile introduction of a beta-lactone ring moiety. The synthetic steps comprise, in preferred embodiments, a tandem Mukaiyama aldol lactonization reaction. Data demonstrating the utility of some of the derivatives as proteasome inhibitors is also disclosed.
摘要翻译： 披露了双乳糖蛋白衍生物及其合成。 在某些实施方案中，本发明的化合物表现出抗癌，抗病毒，抗生素和/或自身免疫治疗能力。 通常，本文公开的合成方法允许在多个位置引入各种取代基以及容易地引入β-内酯环部分。 在优选实施方案中，合成步骤包括串联的Mukaiyama醛醇内酯反应。 还公开了证明一些衍生物作为蛋白酶体抑制剂的效用的数据。
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2.发明申请NOVEL BELACTOSIN DERIVATIVES AS THERAPEUTIC AGENTS/BIOLOGICAL PROBES AND THEIR SYNTHESIS 失效新型BELACTOSIN衍生物作为治疗药物/生物探针及其合成公开(公告)号：US20090042922A1
公开(公告)日：2009-02-12
申请号：US11775154
申请日：2007-07-09
IPC分类号： A61K31/365 , C07D305/08 , A61K31/4375 , A61P35/00 , C07D491/16
CPC分类号： C07D407/12 , C07D305/12
摘要： Derivatives of belactosin and their synthesis are disclosed. In certain embodiments, compounds of the present invention exhibit anti-cancer, antiviral, antibiotic, and/or auto-immune therapeutic abilities. In general, methods of synthesis disclosed herein allow for introduction of a variety of substituents at numerous positions as well as the facile introduction of a beta-lactone ring moiety. The synthetic steps comprise, in preferred embodiments, a tandem Mukaiyama aldol lactonization reaction. Data demonstrating the utility of some of the derivatives as proteasome inhibitors is also disclosed.
摘要翻译： 披露了双乳糖蛋白衍生物及其合成。 在某些实施方案中，本发明的化合物表现出抗癌，抗病毒，抗生素和/或自身免疫治疗能力。 通常，本文公开的合成方法允许在多个位置引入各种取代基以及容易地引入β-内酯环部分。 在优选实施方案中，合成步骤包括串联的Mukaiyama醛醇内酯反应。 还公开了证明一些衍生物作为蛋白酶体抑制剂的效用的数据。
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公开(公告)号：US20100305121A1
公开(公告)日：2010-12-02
申请号：US12778944
申请日：2010-05-12
IPC分类号： A61K31/515 , C07D405/06 , C07D413/06 , A61K31/5377 , C12N5/00 , G01N33/68 , A61P35/00 , A61P3/04 , A61P19/02 , A61P17/06
CPC分类号： C07D405/06 , C07D239/62 , C07D239/74 , C07D471/04
摘要： The present invention provides for compounds of formula (I)-(XIII), as well as pharmaceutically acceptable salts thereof, metabolites thereof, pro-drugs thereof, and pharmaceutical kits that include such compounds. The present invention also provides for the compounds of formula (I)-(XIII) for use in medical therapy or diagnosis. The present invention also provides for the use of the compounds of formula (I)-(XIII) in treating cancer in mammals (e.g., humans), as well inhibiting tumor cell growth in such mammals. The present invention also provides for methods of inhibiting FAS. The methods include contacting FAS with an effective amount of a compound of formula (I)-(XIII). The present invention also provides for methods of inhibiting the TE domain of the FAS. The methods include contacting the thioesterase TE domain of the FAS with an effective amount of a compound of formula (I)-(XIII). The present invention also provides for methods of treating cancer in mammals, as well as methods of inhibiting tumor cell growth in such mammals. The methods include administering a compound of formula (I)-(XIII) to a mammal in need of such treatment.
摘要翻译： 本发明提供式（I） - （XIII）化合物及其药学上可接受的盐，其代谢物，其前药和包括这些化合物的药物试剂盒。 本发明还提供用于药物治疗或诊断的式（I） - （XIII）化合物。 本发明还提供式（I） - （XIII）化合物在哺乳动物（例如人）中治疗癌症中的用途，以及抑制这些哺乳动物的肿瘤细胞生长。 本发明还提供了抑制FAS的方法。 所述方法包括使FAS与有效量的式（I） - （XIII）化合物接触。 本发明还提供了抑制FAS的TE结构域的方法。 所述方法包括使FAS的硫酯酶TE结构域与有效量的式（I） - （XIII）化合物接触。 本发明还提供了治疗哺乳动物癌症的方法，以及抑制这些哺乳动物肿瘤细胞生长的方法。 所述方法包括向需要这种治疗的哺乳动物施用式（I） - （XIII）化合物。
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公开(公告)号：US08258321B2
公开(公告)日：2012-09-04
申请号：US12262101
申请日：2008-10-30
申请人： Jeffrey W. Smith , Daniel Romo , Gil Ma , Manuel Zancanella
发明人： Jeffrey W. Smith , Daniel Romo , Gil Ma , Manuel Zancanella
IPC分类号： C07D305/12
CPC分类号： C07D305/12
摘要： The present invention provides compounds having the general structure A, or a pharmaceutically acceptable derivatives thereof: wherein R is an alkyl group, and R1 comprises at least one moiety selected from a group consisting of an alkyl, an alkenyl, an aryl, a heterocycle, hydroxyl, ester, amido, aldehyde, and a halogen.
摘要翻译： 本发明提供具有通式结构A的化合物或其药学上可接受的衍生物：其中R是烷基，R 1包含至少一个选自烷基，烯基，芳基，杂环， 羟基，酯，酰氨基，醛和卤素。
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5.发明申请公开(公告)号：US20100173982A1
公开(公告)日：2010-07-08
申请号：US12620412
申请日：2009-11-17
申请人： Jeffrey W. Smith , Fumiko Axelrod , Steven J. Kridel , Daniel Romo , Vikram Purohit , Gil Ma
发明人： Jeffrey W. Smith , Fumiko Axelrod , Steven J. Kridel , Daniel Romo , Vikram Purohit , Gil Ma
IPC分类号： A61K31/335 , C07D305/12
CPC分类号： A61K31/336 , A61K31/335 , A61K31/337 , A61K31/365 , A61K31/40 , A61K31/42 , A61K31/425 , A61K31/445 , A61K31/585 , G01N33/5011 , G01N2333/91057
摘要： The present invention features methods of treating a cancer in a subject by administering an effective amount of a beta-lactone to the subject. The invention also features methods of inhibiting angiogenesis in a subject by administering an effective amount of an inhibitor of fatty acid synthase to the subject. These methods can be used to treat a variety of cancers and other diseases and conditions. The invention also features methods of identifying beta-lactones and other compounds that can be used in the methods of the invention for the treatment of tumors, inhibition of angiogenesis, and the treatment of diseases and conditions that involve pathological angiogenesis. The invention also features methods of synthesizing beta-lactones and features novel beta-lactone compounds.
摘要翻译： 本发明的特征在于通过向受试者施用有效量的β-内酯来治疗受试者的癌症的方法。 本发明还具有通过向受试者施用有效量的脂肪酸合酶抑制剂来抑制受试者血管生成的方法。 这些方法可用于治疗各种癌症和其他疾病和病症。 本发明还涉及鉴定可用于本发明治疗肿瘤，抑制血管发生以及涉及病理性血管生成的疾病和病症的治疗的β-内酯和其它化合物的方法。 本发明还具有合成β-内酯并具有新型β-内酯化合物特征的方法。
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公开(公告)号：US20090124681A1
公开(公告)日：2009-05-14
申请号：US12262101
申请日：2008-10-30
申请人： Jeffrey W. Smith , Daniel Romo , Gil Ma , Manuel Zancanella
发明人： Jeffrey W. Smith , Daniel Romo , Gil Ma , Manuel Zancanella
IPC分类号： A61K31/4164 , C07D305/12 , A61K31/337 , A61P29/00 , A61P31/00 , A61P37/00 , A61P35/00 , C07D233/54
CPC分类号： C07D305/12
摘要： The present invention provides compounds having the general structure A, or a pharmaceutically acceptable derivatives thereof: wherein R is an alkyl group, and R1 comprises at least one moiety selected from a group consisting of an alkyl, an alkenyl, an aryl, a heterocycle, hydroxyl, ester, amido, aldehyde, and a halogen.
摘要翻译： 本发明提供具有通式结构A的化合物或其药学上可接受的衍生物：其中R是烷基，R 1包含至少一个选自烷基，烯基，芳基，杂环， 羟基，酯，酰氨基，醛和卤素。
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公开(公告)号：US08124794B2
公开(公告)日：2012-02-28
申请号：US12620412
申请日：2009-11-17
申请人： Jeffrey W. Smith , Fumiko Axelrod , Steven J. Kridel , Daniel Romo , Vikram Purohit , Gil Ma
发明人： Jeffrey W. Smith , Fumiko Axelrod , Steven J. Kridel , Daniel Romo , Vikram Purohit , Gil Ma
IPC分类号： C07D305/00
CPC分类号： A61K31/336 , A61K31/335 , A61K31/337 , A61K31/365 , A61K31/40 , A61K31/42 , A61K31/425 , A61K31/445 , A61K31/585 , G01N33/5011 , G01N2333/91057
摘要： The present invention features methods of treating a cancer in a subject by administering an effective amount of a beta-lactone to the subject. The invention also features methods of inhibiting angiogenesis in a subject by administering an effective amount of an inhibitor of fatty acid synthase to the subject. These methods can be used to treat a variety of cancers and other diseases and conditions. The invention also features methods of identifying beta-lactones and other compounds that can be used in the methods of the invention for the treatment of tumors, inhibition of angiogenesis, and the treatment of diseases and conditions that involve pathological angiogenesis. The invention also features methods of synthesizing beta-lactones and features novel beta-lactone compounds.
摘要翻译： 本发明的特征在于通过向受试者施用有效量的β-内酯来治疗受试者的癌症的方法。 本发明还具有通过向受试者施用有效量的脂肪酸合酶抑制剂来抑制受试者血管生成的方法。 这些方法可用于治疗各种癌症和其他疾病和病症。 本发明还涉及鉴定可用于本发明治疗肿瘤，抑制血管发生以及涉及病理性血管生成的疾病和病症的治疗的β-内酯和其它化合物的方法。 本发明还具有合成β-内酯并具有新型β-内酯化合物特征的方法。
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公开(公告)号：US07728153B2
公开(公告)日：2010-06-01
申请号：US11378961
申请日：2006-03-16
申请人： Jeffrey W. Smith , Fumiko Axelrod , Steven J. Kridel , Daniel Romo , Vikram Purohit , Gil Ma
发明人： Jeffrey W. Smith , Fumiko Axelrod , Steven J. Kridel , Daniel Romo , Vikram Purohit , Gil Ma
IPC分类号： C07D305/00
CPC分类号： A61K31/336 , A61K31/335 , A61K31/337 , A61K31/365 , A61K31/40 , A61K31/42 , A61K31/425 , A61K31/445 , A61K31/585 , G01N33/5011 , G01N2333/91057
摘要： The present invention features methods of treating a cancer in a subject by administering an effective amount of a beta-lactone to the subject. The invention also features methods of inhibiting angiogenesis in a subject by administering an effective amount of an inhibitor of fatty acid synthase to the subject. These methods can be used to treat a variety of cancers and other diseases and conditions. The invention also features methods of identifying beta-lactones and other compounds that can be used in the methods of the invention for the treatment of tumors, inhibition of angiogenesis, and the treatment of diseases and conditions that involve pathological angiogenesis. The invention also features methods of synthesizing beta-lactones and features novel beta-lactone compounds.
摘要翻译： 本发明的特征在于通过向受试者施用有效量的β-内酯来治疗受试者的癌症的方法。 本发明还具有通过向受试者施用有效量的脂肪酸合酶抑制剂来抑制受试者血管生成的方法。 这些方法可用于治疗各种癌症和其他疾病和病症。 本发明还涉及鉴定可用于本发明治疗肿瘤，抑制血管发生以及涉及病理性血管生成的疾病和病症的治疗的β-内酯和其它化合物的方法。 本发明还具有合成β-内酯并具有新型β-内酯化合物特征的方法。
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公开(公告)号：US08563248B2
公开(公告)日：2013-10-22
申请号：US12959349
申请日：2010-12-02
申请人： Jeffrey W. Smith , Changming Fang
发明人： Jeffrey W. Smith , Changming Fang
CPC分类号： C12Q1/6886 , C12Q2600/106
摘要： We have identified a new variant of ileal bile acid binding protein (IBABP), designated IBABP-L, which is a biomarker for colorectal cancer. The transcript for IBABP-L arises from an alternative start site and includes three exons that are absent in IBABP. IBABP-L also shares part of a fourth exon with IBABP. The protein encoded by IBABP-L contains a deduced 49 residue N-terminal sequence that is not found in the IBABP protein. The present invention provides methods for diagnosing colorectal cancer and other compositions and methods based on this discovery.
摘要翻译： 我们已经确定了回肠胆汁酸结合蛋白（IBABP）的新变体，称为IBABP-L，其是结肠直肠癌的生物标志物。 IBABP-L的成绩单来自替代起始位点，并且包括IBABP中缺少的三个外显子。 IBABP-L还与IBABP共享第四外显子的一部分。 由IBABP-L编码的蛋白质含有在IBABP蛋白中未发现的49个残基的N-末端序列。 本发明提供了用于诊断结肠直肠癌的方法以及基于该发现的其它组合物和方法。
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10.发明授权Inhibition of fatty acid synthase by beta-lactones and other compounds for inhibition of cellular proliferation 失效通过β-内酯和其他化合物抑制脂肪酸合酶抑制细胞增殖公开(公告)号：US07799826B2
公开(公告)日：2010-09-21
申请号：US10418513
申请日：2003-04-16
IPC分类号： A61K31/335
CPC分类号： A61K31/337 , A61K31/335 , A61K31/336 , A61K31/365 , A61K31/40 , A61K31/42 , A61K31/425 , A61K31/445 , A61K31/585 , G01N33/5011 , G01N2333/91057
摘要： The present invention features methods of treating a cancer in a subject by administering an effective amount of a beta-lactone to the subject. The invention also features methods of inhibiting angiogenesis in a subject by administering an effective amount of an inhibitor of fatty acid synthase to the subject. These methods can be used to treat a variety of cancers and other diseases and conditions. The invention also features methods of identifying beta-lactones and other compounds that can be used in the methods of the invention for the treatment of tumors, inhibition of angiogenesis, and the treatment of diseases and conditions that involve pathological angiogenesis.
摘要翻译： 本发明的特征在于通过向受试者施用有效量的β-内酯来治疗受试者的癌症的方法。 本发明还具有通过向受试者施用有效量的脂肪酸合酶抑制剂来抑制受试者血管生成的方法。 这些方法可用于治疗各种癌症和其他疾病和病症。 本发明还涉及鉴定可用于本发明治疗肿瘤，抑制血管发生以及涉及病理性血管生成的疾病和病症的治疗的β-内酯和其它化合物的方法。
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