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1. 发明申请

US20100190231A1 METHODS FOR CRYSTALLIZING ERK2 POLYPEPTIDES 审中-公开
标题翻译：用于结晶ERK2多聚体的方法
公开(公告)号：US20100190231A1
公开(公告)日：2010-07-29
申请号：US12754029
申请日：2010-04-05
申请人： JESSIE M. ENGLISH , Thierry Oliver Fischmann , Thomas Hesson , Alan William Hruza , Weihong Jin , Paul Reichert , Catherine Smith , Shahriar Shane Taremi
发明人： JESSIE M. ENGLISH , Thierry Oliver Fischmann , Thomas Hesson , Alan William Hruza , Weihong Jin , Paul Reichert , Catherine Smith , Shahriar Shane Taremi
IPC分类号： C12N9/12 , G06F17/50
CPC分类号： C12N9/1205 , C07K2299/00
摘要： The present invention relates to crystals of the ERK2 polypeptide and complexes thereof which are useful, inter alia, for structure assisted drug design.
摘要翻译：本发明涉及ERK2多肽的结晶及其复合物，其特别用于结构辅助药物设计。

2. 发明授权

US07722718B2 Methods for crystallizing ERK2 polypeptides 有权
标题翻译：使ERK2多肽结晶的方法
公开(公告)号：US07722718B2
公开(公告)日：2010-05-25
申请号：US11873831
申请日：2007-10-17
申请人： Jessie English , Thierry Oliver Fischmann , Thomas Hesson , Alan William Hruza , Weihong Jin , Paul Reichert , Catherine Smith , Shahriar Shane Taremi
发明人： Jessie English , Thierry Oliver Fischmann , Thomas Hesson , Alan William Hruza , Weihong Jin , Paul Reichert , Catherine Smith , Shahriar Shane Taremi
IPC分类号： C30B27/02 , C12N9/12
CPC分类号： C12N9/1205 , C07K2299/00
摘要： The present invention relates to crystals of the ERK2 polypeptide and complexes thereof which are useful, inter alia, for structure assisted drug design.
摘要翻译：本发明涉及ERK2多肽的结晶及其复合物，其特别用于结构辅助药物设计。

3. 发明授权

US07312061B2 ERK2 crystals 失效
标题翻译： ERK2晶体
公开(公告)号：US07312061B2
公开(公告)日：2007-12-25
申请号：US11233581
申请日：2005-09-23
申请人： Jessie English , Thierry Oliver Fischmann , Thomas Hesson , Alan William Hruza , Weihong Jin , Paul Reichert , Catherine Smith , Shahriar Shane Taremi
发明人： Jessie English , Thierry Oliver Fischmann , Thomas Hesson , Alan William Hruza , Weihong Jin , Paul Reichert , Catherine Smith , Shahriar Shane Taremi
IPC分类号： C12N9/12
CPC分类号： C12N9/1205 , C07K2299/00
摘要： The present invention relates to crystals of the ERK2 polypeptide and complexes thereof which are useful, inter alia, for structure assisted drug design.
摘要翻译：本发明涉及ERK2多肽的结晶及其复合物，其特别用于结构辅助药物设计。

4. 发明申请

US20080081360A1 ERK2 CRYSTALS 有权
标题翻译： ERK2水晶
公开(公告)号：US20080081360A1
公开(公告)日：2008-04-03
申请号：US11873831
申请日：2007-10-17
申请人： Jessie English , Thierry Fischmann , Thomas Hesson , Alan Hruza , Weihong Jin , Paul Reichert , Catherine Smith , Shahriar Taremi
发明人： Jessie English , Thierry Fischmann , Thomas Hesson , Alan Hruza , Weihong Jin , Paul Reichert , Catherine Smith , Shahriar Taremi
IPC分类号： C12N9/12 , G06F19/00
CPC分类号： C12N9/1205 , C07K2299/00
摘要： The present invention relates to crystals of the ERK2 polypeptide and complexes thereof which are useful, inter alia, for structure assisted drug design.
摘要翻译：本发明涉及ERK2多肽的结晶及其复合物，其特别用于结构辅助药物设计。

5. 发明申请

US20060088924A1 ERK2 crystals 失效
标题翻译： ERK2晶体
公开(公告)号：US20060088924A1
公开(公告)日：2006-04-27
申请号：US11233581
申请日：2005-09-23
申请人： Jessie English , Thierry Fischmann , Thomas Hesson , Alan Hruza , Weihong Jin , Paul Reichert , Catherine Smith , Shahriar Taremi
发明人： Jessie English , Thierry Fischmann , Thomas Hesson , Alan Hruza , Weihong Jin , Paul Reichert , Catherine Smith , Shahriar Taremi
IPC分类号： G06F19/00 , C12N9/12
CPC分类号： C12N9/1205 , C07K2299/00
摘要： The present invention relates to crystals of the ERK2 polypeptide and complexes thereof which are useful, inter alia, for structure assisted drug design.
摘要翻译：本发明涉及ERK2多肽的结晶及其复合物，其特别用于结构辅助药物设计。

6. 发明授权

US08440443B1 MEK1 polypeptides 失效
标题翻译： MEK1多肽
公开(公告)号：US08440443B1
公开(公告)日：2013-05-14
申请号：US11749550
申请日：2007-05-16
申请人： Thierry O. Fischmann , Hung V. Le , Vincent S. Madison , Anthony F. Mannarino , Todd W. Mayhood , Paul Reichert , Catherine Smith , Tin-Yau Chan
发明人： Thierry O. Fischmann , Hung V. Le , Vincent S. Madison , Anthony F. Mannarino , Todd W. Mayhood , Paul Reichert , Catherine Smith , Tin-Yau Chan
IPC分类号： C12N9/12
CPC分类号： C12N9/1205 , C07K2299/00 , C07K2319/40
摘要： The present invention provides, inter alia, crystals of the MEK1 polypeptide which are particularly useful for structure based drug design as well as methods of use thereof.
摘要翻译：本发明特别提供了特别可用于基于结构的药物设计的MEK1多肽的晶体及其使用方法。

7. 发明申请

US20050038001A1 Transdiscal administration of cycline compounds 有权
标题翻译：跨周期给药的细胞周期素化合物
公开(公告)号：US20050038001A1
公开(公告)日：2005-02-17
申请号：US10640412
申请日：2003-08-13
申请人： Mohamed Attawia , Thomas DiMauro , Hassan Serhan , Melissa Grace , Sudhakar Kadiyala , David Urbahns , Scott Bruder , Gregory Collins , Laura Brown , Jeff Geesin , Pamela Plouhar , Catherine Smith , John Siekierka
发明人： Mohamed Attawia , Thomas DiMauro , Hassan Serhan , Melissa Grace , Sudhakar Kadiyala , David Urbahns , Scott Bruder , Gregory Collins , Laura Brown , Jeff Geesin , Pamela Plouhar , Catherine Smith , John Siekierka
IPC分类号： A61K31/65
CPC分类号： A61K31/65 , A61K38/20 , A61K45/06 , A61K2300/00
摘要： The present invention relates to injecting a cycline compound into a diseased intervertebral disc.
摘要翻译：本发明涉及将环状化合物注射到患病的椎间盘中。

8. 发明申请

US20050186561A1 Methods of diagnosing tissue fibrosis 有权
标题翻译：诊断组织纤维化的方法
公开(公告)号：US20050186561A1
公开(公告)日：2005-08-25
申请号：US10971195
申请日：2004-10-22
申请人： Esther Oh , Catherine Smith
发明人： Esther Oh , Catherine Smith
IPC分类号： A61B20060101 , C12Q1/68 , C12Q1/70 , G01N33/53 , G01N33/567 , G01N33/68
CPC分类号： C12Q1/6883 , C12Q2600/112 , C12Q2600/158 , G01N33/6893 , G01N2800/52
摘要： The present invention provides a method of diagnosing the presence or severity of tissue fibrosis in an individual by detecting α2-macroglobulin (α2-MG) in a sample from the individual; detecting hyaluronic acid (HA) in a sample from the individual; detecting tissue inhibitor of metalloproteinases-1 (TIMP-1) in a sample from the individual; and diagnosing the presence or severity of tissue fibrosis in the individual based on the presence or level of α2-MG, HA and TIMP-1.
摘要翻译：本发明提供一种通过检测来自个体的样品中的α2-巨球蛋白（α2-MG）来诊断个体中组织纤维化的存在或严重性的方法; 检测来自个体的样品中的透明质酸（HA）; 检测来自个体的样品中金属蛋白酶-1（TIMP-1）的组织抑制剂; 并基于α2-MG，HA和TIMP-1的存在或水平诊断个体中组织纤维化的存在或严重程度。

9. 发明授权

US08361467B2 Trans-capsular administration of high specificity cytokine inhibitors into orthopedic joints 有权
标题翻译：将高特异性细胞因子抑制剂的跨荚膜施用于矫形关节
公开(公告)号：US08361467B2
公开(公告)日：2013-01-29
申请号：US10630227
申请日：2003-07-30
申请人： Thomas M. DiMauro , Mohamed Attawia , Hassan Serhan , Martin A. Reynolds , Melissa Grace , Sudhakar Kadiyala , David Urbahns , Scott Bruder , Gregory Collins , Laura J. Brown , Jeff Geesin , Pamela L. Plouhar , Catherine Smith , John Siekierka
发明人： Thomas M. DiMauro , Mohamed Attawia , Hassan Serhan , Martin A. Reynolds , Melissa Grace , Sudhakar Kadiyala , David Urbahns , Scott Bruder , Gregory Collins , Laura J. Brown , Jeff Geesin , Pamela L. Plouhar , Catherine Smith , John Siekierka
IPC分类号： A61K39/395 , A61K39/00 , A61K38/18
CPC分类号： A61K38/30 , A61K31/198 , A61K31/436 , A61K38/1816 , A61K2039/505
摘要： The present invention relates to trans-capsularly administering into a diseased joint a high specificity antagonist selected from the group consisting of: i) an inhibitor of a pro-inflammatory interleukin; ii) an inhibitor of TNF-α synthesis; iii) an inhibitor of membrane-bound TNF-α; iv) an inhibitor of a natural receptor of TNF-α; v) an inhibitor of NO synthase, vi) an inhibitor of PLA2 enzyme; vii) an anti-proliferative agent; viii) an anti-oxidant; ix) an apoptosis inhibitor selected from the group consisting of EPO mimetic peptides, EPO mimetibodies, IGF-I, IGF-II, and caspase inhibitors, and x) an inhibitor of MMPs; and xi) an inhibitor of p38 kinase.
摘要翻译：本发明涉及向患病关节中透射施用高特异性拮抗剂，所述高特异性拮抗剂选自：i）促炎白细胞介素的抑制剂; ii）TNF-α合成抑制剂; iii）膜结合TNF-α的抑制剂; iv）TNF-α的天然受体的抑制剂; v）NO合酶抑制剂，vi）PLA2酶抑制剂; vii）抗增殖剂; viii）抗氧化剂; ix）选自EPO模拟肽，EPO模拟物，IGF-I，IGF-II和胱天蛋白酶抑制剂的细胞凋亡抑制剂，和x）MMP的抑制剂; 和xi）p38激酶的抑制剂。

10. 发明申请

US20070179315A1 Methods of amination 失效
标题翻译：胺化方法
公开(公告)号：US20070179315A1
公开(公告)日：2007-08-02
申请号：US10593212
申请日：2005-03-18
申请人： Andrew Holmes , Catherine Smith , Melanie Tsang , Theresa Early , Richard Shute
发明人： Andrew Holmes , Catherine Smith , Melanie Tsang , Theresa Early , Richard Shute
IPC分类号： C07C209/00
CPC分类号： C07C227/08 , C07C209/10 , C07C213/02 , C07D207/325 , C07D207/327 , C07C211/55 , C07C217/92 , C07C229/60
摘要： A method of synthesizing a compound of formula I: comprising the step of reacting a moiety of formula II: with a moiety of formula III: in compressed carbon dioxide in the presence of a transition metal catalyst and a base, wherein L is a labile leaving group; RN1 is optionally substituted C5-20 aryl; RN2 is selected from optionally substituted C5-20aryl, optionally substituted C3-20 heterocyclyl, optionally substituted C3-7 alkyl, and optionally substituted sulfonyl; RN3 is selected from H and optionally substituted C1-7 alkyl, C3-20 heterocyclyl and C5-20 aryl; or RN2 and RN3 together with the nitrogen atom to which they are attached form optionally substituted nitrogen-containing C3-20 heterocylyl or C5-20 heteroaryl; and R1 R2 and R3 are independently selected from optionally substituted C1-7 alkyl, C5-20 aryl, C3-20 heterocyclyl, hydroxy, halo, amino and C1-7 alkoxy, or two of R1, R2 and R3, together with the silicon atom to which they are attached, may form a silicon containing C5-7 heterocyclyl group.
摘要翻译：合成式I化合物的方法：包括使式II部分与式III部分反应的步骤：在过渡金属催化剂和碱的存在下，在压缩二氧化碳中，其中L是不稳定的离去组; R 01是任选取代的C 5-20芳基; R N2选自任选取代的C 5-20芳基，任选取代的C 3-20杂环基，任选取代的C 3-8芳基， 7烷基和任选取代的磺酰基; R N 3选自H和任选取代的C 1-7 - 烷基，C 3-20 - 杂环基和C 5-20杂环基， / SUB>芳基; 或R N2和R N3与它们所连接的氮原子一起形成任选取代的含氮C 3-20异氰酸酯或C 5-20杂芳基; R 1和R 3独立地选自任选取代的C 1-7烷基，C 1 -C 6烷基，羟基，卤素，氨基和C 1-7 - 烷氧基，或者R 1，R 2，R 2， 1，R 2和R 3与它们所连接的硅原子一起可以形成含有C 5-7的硅， / SO 2杂环基。

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