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1. 发明授权

US08119653B2 Belactosin derivatives as therapeutic agents/biological probes and their synthesis 失效
标题翻译：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
申请人： Daniel Romo , Sung Wook Cho , Jeffrey W. Smith , Robyn D. Richardson
发明人： Daniel Romo , Sung Wook Cho , Jeffrey W. Smith , Robyn D. Richardson
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。

2. 发明申请

US20090042922A1 NOVEL BELACTOSIN DERIVATIVES AS THERAPEUTIC AGENTS/BIOLOGICAL PROBES AND THEIR SYNTHESIS 失效
标题翻译：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
申请人： Daniel Romo , Sung Wook Cho , Jeffrey W. Smith , Robyn D. Richardson
发明人： Daniel Romo , Sung Wook Cho , Jeffrey W. Smith , Robyn D. Richardson
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。

3. 发明申请

US20100305121A1 NOVEL ANTAGONISTS OF THE HUMAN FATTY ACID SYNTHASE THIOESTERASE 审中-公开
标题翻译：人类脂肪酸合成酶的新型拮抗剂
公开(公告)号：US20100305121A1
公开(公告)日：2010-12-02
申请号：US12778944
申请日：2010-05-12
申请人： Jeffrey W. Smith , Robyn D. Richardson
发明人： Jeffrey W. Smith , Robyn D. Richardson
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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