专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

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。

4. 发明授权

US08258321B2 Beta-lactone compounds 有权
标题翻译： β-内酯化合物
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。

5. 发明申请

US20100173982A1 NOVEL METHOD FOR THE ASYMMETRIC SYNTHESIS OF BETA-LACTONE COMPOUNDS 失效
标题翻译：用于不对称合成BETA-LACTONE化合物的新方法
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。

6. 发明申请

US20090124681A1 BETA-LACTONE COMPOUNDS 有权
标题翻译： BETA-LACTONE化合物
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。

7. 发明授权

US08124794B2 Method for the asymmetric synthesis of beta-lactone compounds 失效
标题翻译： β-内酯化合物的不对称合成方法
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。

8. 发明授权

US07728153B2 Method for the asymmetric synthesis of beta-lactone compounds 失效
标题翻译： β-内酯化合物的不对称合成方法
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。

9. 发明授权

US08712475B2 Method to calibrate RF paths of an FHOP adaptive base station 有权
标题翻译：校准FHOP自适应基站的RF路径的方法
公开(公告)号：US08712475B2
公开(公告)日：2014-04-29
申请号：US13350489
申请日：2012-01-13
申请人： John R. Noll , Jeffrey W. Smith , Shannon Tomarchio , Brady Gaughan
发明人： John R. Noll , Jeffrey W. Smith , Shannon Tomarchio , Brady Gaughan
IPC分类号： H04B1/38
CPC分类号： H04B7/0848 , H04B17/21
摘要： A base transceiver station including a transceiver unit is provided. A method of calibration uses a transceiver unit to receive an RF signal, measure a calibration value, and transmit the measured value. The calibration value is used to determine weighting parameters to compensate for relative RF path phase delay and amplitude variation.
摘要翻译：提供了包括收发器单元的基站收发器。校准方法使用收发器单元来接收RF信号，测量校准值并传输测量值。校准值用于确定加权参数以补偿相对RF路径相位延迟和幅度变化。

10. 发明授权

US07935785B2 Selective substrates for matrix metalloproteinases 失效
标题翻译：基质金属蛋白酶的选择性底物
公开(公告)号：US07935785B2
公开(公告)日：2011-05-03
申请号：US12252160
申请日：2008-10-15
申请人： Jeffrey W. Smith , Emily I. Chen , Steven J. Kridel
发明人： Jeffrey W. Smith , Emily I. Chen , Steven J. Kridel
IPC分类号： C07K5/00 , C07K14/00
CPC分类号： A61K49/0021 , A61K47/64 , A61K49/0056 , C07K5/0806 , C07K5/0808 , C07K5/081 , C07K5/0812 , C07K5/0815 , C07K5/0821 , C07K5/0823 , C07K5/1008 , C07K5/101 , C07K5/1013 , C07K5/1016 , C07K5/1019 , C07K5/1024 , C07K7/06 , C07K7/08 , C12Q1/37
摘要： The invention provides isolated MMP-2, MMP-9 and MT1-MMP selective substrate polypeptides or functional peptidomimetics. The selective substrate polypeptides contain the following sequences: MMP-2 selective substrate polypeptides contain SEQ ID NOS:1-27, MMP-9 selective substrate polypeptides contain SEQ ID NOS:28-35, and MT1-MMP selective substrate polypeptide contain SEQ ID NOS:36-40. In addition, the invention provides a method of preferentially directing a moiety to a site of MMP-2 activity by administering to a subject an effective amount of an isolated MMP-2 selective substrate polypeptide containing SEQ ID NOS:45-47 linked to a moiety. Also provided is a method of preferentially directing a moiety to a site of MMP-9 activity by administering to a subject an effective amount of an isolated MMP-9 selective substrate polypeptide containing SEQ ID NO:44 linked to a moiety, and preferentially directing a moiety to a site of MT1-MMP activity by administering to a subject an effective amount of an isolated MT1-MMP selective substrate polypeptide containing SEQ ID NOS:36-40 linked to a moiety.
摘要翻译：本发明提供分离的MMP-2，MMP-9和MT1-MMP选择性底物多肽或功能肽模拟物。选择性底物多肽包含以下序列：MMP-2选择性底物多肽含有SEQ ID NO：1-27，含有SEQ ID NO：28-35的MMP-9选择性底物多肽，并且含有SEQ ID NOS的MT1-MMP选择性底物多肽：36-40。此外，本发明提供了通过向受试者施用有效量的与部分连接的含有SEQ ID NO：45-47的分离的MMP-2选择性底物多肽来优先将部分定向到MMP-2活性位点的方法。还提供了通过向受试者施用有效量的与部分连接的含有SEQ ID NO：44的分离的MMP-9选择性底物多肽，优先将一部分连接至部分MMP-9活性部位的方法，通过向受试者施用有效量的与部分连接的含有SEQ ID NO：36-40的分离的MT1-MMP选择性底物多肽，从而部分到MT1-MMP活性的位点。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式