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1. 发明专利

TW200510328A 以5員雜環為主之p38激抑制劑 5-MEMBERED HETEROCYCLE-BASED P38 KINASE INHIBITORS 失效
简体标题：以5员杂环为主之p38激抑制剂 5-MEMBERED HETEROCYCLE-BASED P38 KINASE INHIBITORS
公开(公告)号：TW200510328A
公开(公告)日：2005-03-16
申请号：TW093118259
申请日：2004-06-24
申请人：三合一治療公司 TRIAD THERAPEUTICS, INC.
发明人：歐加M 富萊茲曼 FRYSZMAN, OLGA M. , 郎恒元 LANG, HENGYUAN , 藍炯 LAN, JIONG , 章懿勤 CHANG, EDCON , 房云峰 FANG, YUNFENG
IPC分类号： C07D , A61K
CPC分类号： C07D413/12 , C07D231/38 , C07D231/44 , C07D231/52 , C07D233/88 , C07D401/06 , C07D401/10 , C07D401/12 , C07D403/10 , C07D403/12 , C07D405/06 , C07D405/10 , C07D413/10
摘要：所提供的是以5員雜環為主之p38激抑制劑。進一步提供的是以唑和咪唑為主之p38激抑制劑，包括p38α和p38β激的抑制劑。亦提供含該化合物的醫藥組成物。亦提供使用該化合物和組成物的方法，包括治療、預防或改善一或多種由p38激所媒介疾病與失調(包括但不限於發炎疾病和失調)之症狀的方法。093118259-p01.bmp
简体摘要：所提供的是以5员杂环为主之p38激抑制剂。进一步提供的是以唑和咪唑为主之p38激抑制剂，包括p38α和p38β激的抑制剂。亦提供含该化合物的医药组成物。亦提供使用该化合物和组成物的方法，包括治疗、预防或改善一或多种由p38激所媒介疾病与失调(包括但不限于发炎疾病和失调)之症状的方法。093118259-p01.bmp

2. 发明申请

WO2004083814A3 NUCLEAR MAGNETIC RESONANCE ASSEMBLY OF CHEMICAL ENTITIES USING ADVANCED ANTENNA PROBES 审中-公开
标题翻译：使用高级天线探针的化学实验的核磁共振组装
公开(公告)号：WO2004083814A3
公开(公告)日：2009-04-30
申请号：PCT/US2004007471
申请日：2004-03-12
申请人： TRIAD THERAPEUTICS INC , KELLY MARK , VILLAR HUGO O , WANG JIANQIANG , LEE MIN S , QIN YONG , SEM DANIEL S
发明人： KELLY MARK , VILLAR HUGO O , WANG JIANQIANG , LEE MIN S , QIN YONG , SEM DANIEL S
IPC分类号： G01N33/53 , C12Q1/70 , G01N24/08 , G01N33/542 , G01R33/46 , G01R33/465
CPC分类号： G01N24/088 , G01N24/08 , G01N33/542 , G01R33/4608 , G01R33/465
摘要： The invention provides a method for identifying a ligand that binds to a macromolecular target. The methods involve (a) attaching an antenna moiety to a first ligand, wherein the ligand binds specifically to a macromolecular target; (b) providing a sample comprising the macromolecular target, the first ligand and a candidate second ligand under conditions wherein the first ligand and the macromolecular target form a bound complex; (c) detecting a subset of magnetization transfer signals between the antenna moiety of the first ligand and the second candidate Iigand, wherein the signals are obtained from an isotope edited NOFSY spectrum of the sample; thereby determining that the two ligands are proximal in a bound complex, and identifying a second ligand that binds to the macromolecular target.
摘要翻译：本发明提供了鉴定与大分子靶标结合的配体的方法。所述方法包括（a）将天线部分连接到第一配体，其中所述配体特异性结合于大分子靶; （b）在第一配体和大分子靶形成结合复合物的条件下提供包含大分子靶，第一配体和候选第二配体的样品; （c）检测所述第一配体的天线部分和所述第二候选配体之间的磁化传递信号的子集，其中所述信号是从所述样品的同位素编辑的NOFSY光谱获得的; 从而确定两个配体在结合的复合物中是近端的，并鉴定结合大分子靶标的第二配体。

3. 发明申请

WO2005000298A3 5-MEMBERED HETEROCYCLE-BASED P-38 INHIBITORS 审中-公开
标题翻译：基于5员杂环的P-38抑制剂
公开(公告)号：WO2005000298A3
公开(公告)日：2005-03-03
申请号：PCT/US2004017580
申请日：2004-06-02
申请人： TRIAD THERAPEUTICS INC , DONG QING , PIERRE FABRICE , WANG JIANQIANG
发明人： DONG QING , PIERRE FABRICE , WANG JIANQIANG
IPC分类号： A61P29/00 , C07D249/14 , C07D263/48 , C07D271/06 , C07D271/07 , C07D277/38 , C07D277/42 , C07D277/56 , C07D285/08 , C07D417/04 , C07D417/10 , C07D417/12 , A61K31/426 , C07D285/12 , C07D417/14
CPC分类号： C07D271/07 , C07D249/14 , C07D263/48 , C07D277/42 , C07D277/56 , C07D285/08 , C07D417/04 , C07D417/10 , C07D417/12
摘要： Provided are aminoaryl substituted 5-membered heterocycle-based p38 kinase, including p38alfa and p38beta. Pharmaceutical compositions containing the compounds are also provided. Method of use of the compounds and compositions are also provided, including methods of treatment, prevention, or amelioration of one or more symptoms of p38 kinase mediated diseases and disorders, including, but not limited to, inflammatory diseases and disorders.
摘要翻译：提供了氨基芳基取代的基于5元杂环的p38激酶，包括p38alfa和p38beta。还提供了含有这些化合物的药物组合物。还提供了化合物和组合物的使用方法，包括治疗，预防或改善p38激酶介导的疾病和病症（包括但不限于炎性疾病和病症）的一种或多种症状的方法。

4. 发明申请

WO2003083063A3 COMMON LIGAND MIMICS: NAPHTOATES 审中-公开
公开(公告)号：WO2003083063A3
公开(公告)日：2003-10-09
申请号：PCT/US2003/009086
申请日：2003-03-21
申请人： TRIAD THERAPEUTICS, INC. , LANG, Hengyuan , CHANG, Edcon , CEFALO, Dustin , FRYSZMAN, Olga , YU, Lin
发明人： LANG, Hengyuan , CHANG, Edcon , CEFALO, Dustin , FRYSZMAN, Olga , YU, Lin
IPC分类号： C07C39/12
摘要： The present invention provides common ligand mimics that act as common ligands for a receptor family. The present invention also provides bi-ligands containing these common ligand mimics. Bi-ligands of the invention provide enhanced affinity and/or selectivity of ligand binding to a receptor or receptor family through the synergistic action of the common ligand mimic and specificity ligand which compose the bi-ligand. The present invention also provides combinatorial libraries containing the common ligand mimics and bi-ligands of the invention. Further, the present invention provides methods for manufacturing the common ligand mimics and bi-ligands of the invention and methods for assaying the combinatorial libraries of the invention.

5. 发明申请

WO2003083063A2 COMMON LIGAND MIMICS: NAPHTOATES 审中-公开
标题翻译：通用配体MIMICS：NAPHTOATES
公开(公告)号：WO2003083063A2
公开(公告)日：2003-10-09
申请号：PCT/US2003/009086
申请日：2003-03-21
申请人： TRIAD THERAPEUTICS, INC. , LANG, Hengyuan , CHANG, Edcon , CEFALO, Dustin , FRYSZMAN, Olga , YU, Lin
发明人： LANG, Hengyuan , CHANG, Edcon , CEFALO, Dustin , FRYSZMAN, Olga , YU, Lin
IPC分类号： C12N
CPC分类号： C40B40/04 , C07C65/11 , C07C69/94 , C07C205/59 , C07C229/18 , C07C229/56 , C07C235/66 , C07C311/29 , C07D209/14 , C07D213/79 , C07D233/54 , C07D249/12 , C07D257/04 , C07D309/30 , C07D319/06 , C40B50/14 , G01N33/5735
摘要： The present invention provides common ligand mimics that act as common ligands for a receptor family. The present invention also provides bi-ligands containing these common ligand mimics. Bi-ligands of the invention provide enhanced affinity and/or selectivity of ligand binding to a receptor or receptor family through the synergistic action of the common ligand mimic and specificity ligand which compose the bi-ligand. The present invention also provides combinatorial libraries containing the common ligand mimics and bi-ligands of the invention. Further, the present invention provides methods for manufacturing the common ligand mimics and bi-ligands of the invention and methods for assaying the combinatorial libraries of the invention.
摘要翻译：本发明提供了作为受体家族的共同配体的常见配体模拟物。本发明还提供含有这些共同配体模拟物的双配体。本发明的双配体通过构成双配体的共同配体模拟物和特异性配体的协同作用，提供配体与受体或受体家族结合的增强的亲和力和/或选择性。本发明还提供了包含本发明的共同配体模拟物和双配位体的组合文库。此外，本发明提供了制备本发明的共同配体模拟物和双配位体的方法以及用于测定本发明的组合文库的方法。

6. 发明申请

WO2005012241A3 p-38 KINASE INHIBITORS 审中-公开
标题翻译：激酶抑制剂
公开(公告)号：WO2005012241A3
公开(公告)日：2005-04-14
申请号：PCT/US2004023726
申请日：2004-07-23
申请人： TRIAD THERAPEUTICS INC , LANG HENGYUAN , LAN JIONG , FANG YUNFENG
发明人： LANG HENGYUAN , LAN JIONG , FANG YUNFENG
IPC分类号： C07D213/82 , C07D239/42 , C07D239/74 , C07D239/82 , C07D239/88 , C07D249/08 , C07D271/10 , C07D413/04
CPC分类号： A61K31/538 , A61K31/165 , A61K31/4245 , A61K31/4439 , A61K31/4965 , A61K31/517 , C07C237/38 , C07C237/42 , C07C2601/02 , C07D213/82 , C07D239/42 , C07D239/74 , C07D239/82 , C07D239/88 , C07D249/08 , C07D271/10 , C07D413/04
摘要： Compounds and compositions for modulating the activity of p38 kinases are provided, including p38alpha, and p38beta kinase. Methods for treating, preventing or ameliorating one or more symptoms of a p38 kinase mediated disease or disorder are also provided.
摘要翻译：提供了用于调节p38激酶活性的化合物和组合物，包括p38α和p38β激酶。还提供了用于治疗，预防或改善p38激酶介导的疾病或病症的一种或多种症状的方法。

7. 发明申请

WO2004083814A2 NUCLEAR MAGNETIC RESONANCE ASSEMBLY OF CHEMICAL ENTITIES USING ADVANCED ANTENNA PROBES 审中-公开
标题翻译：使用高级天线探针的化学实验的核磁共振组件
公开(公告)号：WO2004083814A2
公开(公告)日：2004-09-30
申请号：PCT/US2004/007471
申请日：2004-03-12
申请人： TRIAD THERAPEUTICS, INC. , KELLY, Mark , VILLAR, Hugo, O. , WANG, Jianqiang , LEE, Min, S. , QIN, Yong , SEM, Daniel, S.
发明人： KELLY, Mark , VILLAR, Hugo, O. , WANG, Jianqiang , LEE, Min, S. , QIN, Yong , SEM, Daniel, S.
IPC分类号： G01N
CPC分类号： G01N24/088 , G01N24/08 , G01N33/542 , G01R33/4608 , G01R33/465
摘要： The invention provides a method for identifying a ligand that binds to a macromolecular target. The methods involve (a) attaching an antenna moiety to a first ligand, wherein the ligand binds specifically to a macromolecular target; (b) providing a sample comprising the macromolecular target, the first ligand and a candidate second ligand under conditions wherein the first ligand and the macromolecular target form a bound complex; (c) detecting a subset of magnetization transfer signals between the antenna moiety of the first ligand and the second candidate Iigand, wherein the signals are obtained from an isotope edited NOFSY spectrum of the sample; thereby determining that the two ligands are proximal in a bound complex, and identifying a second ligand that binds to the macromolecular target.
摘要翻译：本发明提供了鉴定与大分子靶标结合的配体的方法。所述方法包括（a）将天线部分连接到第一配体，其中所述配体特异性结合于大分子靶; （b）在其中所述第一配体和所述大分子靶形成结合复合物的条件下提供包含所述大分子靶，所述第一配体和候选第二配体的样品; （c）检测第一配体的天线部分和第二候选配体之间的磁化转移信号的子集，其中所述信号是从样品的同位素编辑的NOFSY光谱获得的; 从而确定两个配体在结合复合物中是近端的，并鉴定结合大分子靶标的第二配体。

8. 发明申请

WO2003100078A3 COMMON LIGAND UNIVERSAL ENZYME AND COMPOSITIONS FOR USE THEREIN 审中-公开
公开(公告)号：WO2003100078A3
公开(公告)日：2003-12-04
申请号：PCT/US2003/016053
申请日：2003-05-23
申请人： TRIAD THERAPEUTICS, INC. , QIN, Yong , YU, Lin , HANSEN, Mark, R. , SERGIENKO, Eduard , BERTOLAET, Bonnie , SEM, Daniel, S.
发明人： QIN, Yong , YU, Lin , HANSEN, Mark, R. , SERGIENKO, Eduard , BERTOLAET, Bonnie , SEM, Daniel, S.
IPC分类号： C12Q1/26
摘要： The present invention provides compositions containing a common ligand linked to a detectable moiety and provides methods for the preparation of such compositions. The present invention also provides methods for screening candidate ligands for binding to a NAD binding receptor, which include contacting a receptor with a candidate ligand and a composition of the invention followed by evaluation of receptor binding. The screening method of the present invention has broad applicability and can be used to screen large numbers of a wide variety of ligands. The present invention further provides methods for detecting the binding activity of a putative receptor, which include combining the putative receptor with a composition of the invention and evaluating the level of detectable moiety. The invention also provides kits useful for detection of receptors having NAD binding activity and for screening of candidate ligands that bind to a NAD binding receptor.

9. 发明申请

WO02056236A3 CLASSIFICATION OF POLYPEPTIDES BY LIGAND GEOMETRY AND RELATED METHODS 审中-公开
标题翻译：通过几何几何分析聚合物和相关方法
公开(公告)号：WO02056236A3
公开(公告)日：2004-02-26
申请号：PCT/US0150608
申请日：2001-12-19
申请人： TRIAD THERAPEUTICS INC , SEM DANIEL S , HANSEN MARK
发明人： SEM DANIEL S , HANSEN MARK
IPC分类号： G01N33/68 , G06F19/16 , G06F19/00 , G06F17/50
CPC分类号： G01N33/6803 , G06F19/16
摘要： The invention provides a method for identifying a pharmacocluster. The method includes a the steps of (a) determining bound conformations of a ligand bound to different polypeptides, and (b) clustering two or more bound conformations of the ligand having substantially the same bound conformation, thereby identifying a pharmacocluster. The invention also provides a method for identifying a member of a pharmacocluster. The invention also provides a method for identifying a polypeptide pharmacofamily. The method includes the steps of (a) determining bound conformations of a ligand bound to different polypeptides of a polypeptide family, and (b) identifying two or more bound conformations of the ligand having substantially different bound conformations, thereby identifying at least two polypeptide pharmacofamilies exhibiting binding specificity for the two or more substantially different bound conformations of the ligand.
摘要翻译：本发明提供了鉴定药物团簇的方法。该方法包括以下步骤：（a）确定与不同多肽结合的配体的结合构象，和（b）聚集具有基本上相同结合构象的配体的两个或更多个结合构象，从而鉴定药物团簇。本发明还提供了用于鉴定药物团簇成员的方法。本发明还提供了一种用于鉴定多肽药代动力学的方法。该方法包括以下步骤：（a）确定与多肽家族的不同多肽结合的配体的结合构象，和（b）鉴定具有基本上不同的结合构象的配体的两个或更多个结合构象，由此鉴定至少两个多肽药物对配体的两个或更多个基本不同的结合构象表现出结合特异性。

10. 发明申请

WO02059715A8 PREDICTION OF FUNCTIONAL AND STRUCTURAL PROPERTIES OF POLYPEPTIDES 审中-公开
标题翻译：预测多肽的功能和结构性质
公开(公告)号：WO02059715A8
公开(公告)日：2003-11-13
申请号：PCT/US0150756
申请日：2001-12-28
申请人： TRIAD THERAPEUTICS INC , SEM DANIEL S , BAKER BRIAN , HANSEN MARK R
发明人： SEM DANIEL S , BAKER BRIAN , HANSEN MARK R
IPC分类号： G06F19/16 , G01N33/68 , G06F19/00
CPC分类号： G06F19/16
摘要： The invention provides a method for identifying a polypeptide that binds a ligand. The method includes the steps of (a) comparing a sequence of a polypeptide to a sequence model for polypeptides that bind a ligand, wherein the sequence model comprises representations of amino acids consisting of a subset of amino acids, the subset of amino acids having one or more atom within a selected distance from a bound ligand in the polypeptides that bind the ligand; and (b) determining a relationship between the sequence and the sequence model, wherein a correspondence between the sequence and the sequence model identifies the polypeptide as a polypeptide that binds the ligand.
摘要翻译：本发明提供了鉴定结合配体的多肽的方法。该方法包括以下步骤：（a）将多肽的序列与结合配体的多肽的序列模型进行比较，其中所述序列模型包括由氨基酸亚组组成的氨基酸的表示，所述氨基酸的子集具有一个或多于在与配体结合的多肽中的结合配体的选定距离内的原子; 和（b）确定序列和序列模型之间的关系，其中序列和序列模型之间的对应性将多肽识别为结合配体的多肽。

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