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    • 21. 发明授权
    • Integrin ligand dissociators
    • 整合素配体解离子
    • US06184206B2
    • 2001-02-06
    • US09146503
    • 1998-09-02
    • Jeffrey W. SmithDana D. Hu
    • Jeffrey W. SmithDana D. Hu
    • A61K3800
    • C07K16/2848A61K38/08A61K38/363C07K14/75
    • The invention provides a method of disaggregating a ligand:integrin receptor complex. Specifically, the invention provides a method of disaggregating an existing platelet thrombus in a blood vessel in a subject, comprising administering to the subject a compound which dissociates fibrinogen bound to a first site on platelet glycoprotein IIB-IIIa, by binding a second interacting site on the platelet glycoprotein IIB-IIIa, thereby disaggregating the platelet thrombus. The present invention also provides a method of screening compounds for the ability to dissociate a ligand from its integrin receptor by binding an interacting second site, comprising contacting the compound with an existing ligand:integrin receptor complex and determining if the complex dissociates.
    • 本发明提供了分解配体:整联蛋白受体复合物的方法。 具体地说,本发明提供了一种分解受试者血管中的现有血小板血栓的方法,其包括通过将第二相互作用位点结合到受试者上来解离与血小板糖蛋白IIB-IIIa上的第一部位结合的纤维蛋白原的化合物 血小板糖蛋白IIB-IIIa,从而分解血小板血栓。 本发明还提供了一种筛选化合物以通过结合相互作用的第二位点将配体从其整联蛋白受体解离的能力的方法,包括使化合物与现有的配体:整联蛋白受体复合物接触并确定复合物是否解离。
    • 26. 发明申请
    • NOVEL ANTAGONISTS OF THE HUMAN FATTY ACID SYNTHASE THIOESTERASE
    • 人类脂肪酸合成酶的新型拮抗剂
    • US20100305121A1
    • 2010-12-02
    • US12778944
    • 2010-05-12
    • Jeffrey W. SmithRobyn D. Richardson
    • Jeffrey W. SmithRobyn D. Richardson
    • A61K31/515C07D405/06C07D413/06A61K31/5377C12N5/00G01N33/68A61P35/00A61P3/04A61P19/02A61P17/06
    • C07D405/06C07D239/62C07D239/74C07D471/04
    • 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.
    • 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。
    • 28. 发明申请
    • SELECTIVE SUBSTRATES FOR MATRIX METALLOPROTEINASES
    • 基质金属选择性基体
    • US20090253896A1
    • 2009-10-08
    • US12252160
    • 2008-10-15
    • Jeffrey W. SmithEmily I. ChenSteven J. Kridel
    • Jeffrey W. SmithEmily I. ChenSteven J. Kridel
    • C07K7/06
    • A61K49/0021A61K47/64A61K49/0056C07K5/0806C07K5/0808C07K5/081C07K5/0812C07K5/0815C07K5/0821C07K5/0823C07K5/1008C07K5/101C07K5/1013C07K5/1016C07K5/1019C07K5/1024C07K7/06C07K7/08C12Q1/37
    • 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.
    • 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。
    • 29. 发明授权
    • Selective substrates for matrix metalloproteinases
    • 基质金属蛋白酶的选择性底物
    • US07439319B2
    • 2008-10-21
    • US10243613
    • 2002-09-13
    • Jeffrey W. SmithEmily I. ChenSteven J. Kridel
    • Jeffrey W. SmithEmily I. ChenSteven J. Kridel
    • A61K38/00C07K16/00
    • A61K49/0021A61K47/64A61K49/0056C07K5/0806C07K5/0808C07K5/081C07K5/0812C07K5/0815C07K5/0821C07K5/0823C07K5/1008C07K5/101C07K5/1013C07K5/1016C07K5/1019C07K5/1024C07K7/06C07K7/08C12Q1/37
    • 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.
    • 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。
    • 30. 发明授权
    • Portable multi-purpose workstation assembly
    • 便携式多用途工作站总成
    • US06581920B1
    • 2003-06-24
    • US10134758
    • 2002-04-30
    • Jeffrey W. SmithDwayne Hoffman
    • Jeffrey W. SmithDwayne Hoffman
    • B25B100
    • B25H1/0007B25H3/02B25H5/00
    • A portable multi-purpose workstation assembly for allowing users to mount two engines side-by-side and to easily transfer parts from one engine to the other engine. The portable multi-purpose workstation assembly includes a base assembly including a plurality of elongate base members, and also including base connecting members interconnecting and supporting the elongate base members, and further including wheel assemblies upon which the elongate base members and the base connecting members are supported; and also includes a support assembly being adjustably mounted upon the base assembly, and including sleeve members being disposed about one of the elongate base members, and also including post members being attached to the sleeve members, and further including bracket assemblies being mounted upon the post members.
    • 一种便携式多用途工作站组件,用于允许用户并排安装两台发动机并且容易地将部件从一个发动机传递到另一个发动机。 该便携式多用途工作站组件包括一个底座组件,该基座组件包括多个细长的底座部件,并且还包括互连并支撑细长底座部件的底座连接件,并且还包括轮组件,细长底座部件和底座连接部件 支持的; 并且还包括可调节地安装在基座组件上的支撑组件,并且包括围绕细长基部构件中的一个设置的套筒构件,并且还包括附接到套筒构件的柱构件,并且还包括安装在柱上的支架组件 会员