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1. 发明申请

WO2004062609A3 PYRIMIDINE DERIVATIVES AS IL-8 RECEPTOR ANTAGONISTS 审中-公开
标题翻译：吡嗪衍生物作为IL-8受体拮抗剂
公开(公告)号：WO2004062609A3
公开(公告)日：2004-11-25
申请号：PCT/US2004000584
申请日：2004-01-09
申请人： PHARMACOPEIA INC , ERICKSON SHAWN DAVID , BALDWIN JOHN J , DOLLE RONALD E III , INGLESE JAMES , OHLMEYER MICHAEL H J , HO KOC-KAN , BOHNSTEDT ADOLPH C , KULTGEN STEVEN G , WEBB MARIA L , AULD DOUGLAS S , ROUGHTON ANDREW LAIRD , CONTI PAOLO GIOVANNI MARTINO C , LEYSEN DIRK , VAN DER LOUW JAAP , AKZO NOBEL NV
发明人： ERICKSON SHAWN DAVID , BALDWIN JOHN J , DOLLE RONALD E III , INGLESE JAMES , OHLMEYER MICHAEL H J , HO KOC-KAN , BOHNSTEDT ADOLPH C , KULTGEN STEVEN G , WEBB MARIA L , AULD DOUGLAS S , ROUGHTON ANDREW LAIRD , CONTI PAOLO GIOVANNI MARTINO C , LEYSEN DIRK , VAN DER LOUW JAAP
IPC分类号： A61P35/00 , C07D239/42 , C07D239/46 , C07D401/04 , C07D403/04 , C07D405/04 , C07D405/12 , C07D521/00 , A61K31/505 , A61K31/506 , C07D239/47 , C07D405/14
CPC分类号： C07D239/42 , C07D231/12 , C07D233/56 , C07D239/47 , C07D249/08 , C07D401/04 , C07D403/04 , C07D405/04 , C07D405/12
摘要： Compounds containing the pyrimidine nucleus and their use to treat diseases and conditions related to inappropriate Interleukin-8 receptor activity are disclosed. The compounds are of the formula (I). In these compounds, Q is preferably unsubstituted and substituted heterocyclyl; U is usually hydrogen or fluorine; and V is preferably hydrogen, halogen, alkyl, -O-alkyl or -S-alkyl. A representative example is formula (X).
摘要翻译：公开了含有嘧啶核的化合物及其用于治疗与不适当的白细胞介素-8受体活性有关的疾病和病症的用途。该化合物具有式（I）。在这些化合物中，Q优选为未取代的和取代的杂环基; U通常是氢或氟; 且V优选为氢，卤素，烷基，-O-烷基或-S-烷基。一个代表性的例子是公式（X）。

2. 发明申请

WO2005114198A3 PROTEIN PHOSPHORYLATION ASSAY 审中-公开
标题翻译：蛋白质磷酸化测定
公开(公告)号：WO2005114198A3
公开(公告)日：2006-05-26
申请号：PCT/US2005017711
申请日：2005-05-19
申请人： PHARMACOPEIA INC , AULD DOUGLAS S
发明人： AULD DOUGLAS S
IPC分类号： C12N9/12 , C12Q1/42 , C12Q1/48 , G01N33/573
CPC分类号： C12Q1/42 , C12Q1/485 , G01N2500/00
摘要： The present invention provides methods for assaying the activity of protein kinases or phosphatases that involve reacting the enzymes with substrate, at least a portion of which is fluorescently labeled; allowing phosphorylated substrate to bind to a solid support coated with a phosphate-binding material; and measuring the fluorescence produced by bound, labeled substrate. The invention also provides methods for identifying substances that modulate the activity of protein kinases and phosphatases that comprise reacting the enzymes with a substrate, at least a portion of which is fluorescently labeled, in the presence and absence of test compounds, allowing phosphorylated substrate to bind to a solid support coated with a phosphate-binding material, measuring the fluorescence produced by bound, labeled substrate, and comparing the fluorescence from reactions carried out in the presence and absence of test compounds.
摘要翻译：本发明提供了用于测定蛋白激酶或磷酸酶的活性的方法，其涉及使酶与底物反应，其中至少一部分被荧光标记; 允许磷酸化底物结合涂覆有磷酸盐结合材料的固体支持物; 并测量由结合的标记底物产生的荧光。本发明还提供了用于鉴定调节蛋白激酶和磷酸酶的活性的物质的方法，其包括在存在和不存在测试化合物的情况下使酶与底物反应，其中至少一部分被荧光标记，允许磷酸化底物结合包被磷酸盐结合材料的固体支持物，测量由结合的标记底物产生的荧光，并比较在存在和不存在测试化合物的情况下进行的反应的荧光。

3. 发明申请

WO2010042867A2 ACTIVATORS OF HUMAN PYRUVATE KINASE 审中-公开
标题翻译：人类激素激酶的激活剂
公开(公告)号：WO2010042867A2
公开(公告)日：2010-04-15
申请号：PCT/US2009060237
申请日：2009-10-09
申请人： US HEALTH , THOMAS CRAIG J , AULD DOUGLAS S , INGLESE JAMES , SKOUMBOURDIS AMANDA P , JIANG JIAN-KANG , BOXER MATTHEW
发明人： THOMAS CRAIG J , AULD DOUGLAS S , INGLESE JAMES , SKOUMBOURDIS AMANDA P , JIANG JIAN-KANG , BOXER MATTHEW
IPC分类号： C07D209/08 , A61K31/18 , A61P35/00 , C07D211/54 , C07D215/36 , C07D265/36 , C07D277/64 , C07D295/26 , C07D311/70 , C07D317/62 , C07D319/18 , C07D321/10 , C07D401/12 , C07D403/12 , C07D495/14
CPC分类号： A61K31/496 , A61K31/445 , A61K31/495 , A61K31/5025 , C07D295/26 , C07D319/18 , C07D495/14
摘要： Disclosed are pyruvate kinase M2 activators, which are, bis sulfonamide piperazinyl compounds of Formula (I) and 2,4-disubstituted 4H-thieno[3,2-b]pyrrole-2-(substituted benzyl)pyridazin-3(2H)ones of Formula (II), wherein L and R1 to R16 are as defined herein, that are useful in treating a number of diseases that are treatable by the activation of PKM2, for example, cancer and anemia, Formulas (I); (II).
摘要翻译：公开了丙酮酸激酶M2活化剂，其为式（I）的双磺酰胺哌嗪基化合物和2,4-二取代的4H-噻吩并[3,2-b]吡咯-2-（取代的苄基）哒嗪-3（2H）式（II）的化合物，其中L和R 1至R 16如本文所定义，其可用于治疗可通过PKM2的活化治疗的许多疾病，例如癌症和贫血，式（I）; （II）。

4. 发明专利

AU6489401A Orthologues of human receptors and methods of use 未知
公开(公告)号：AU6489401A
公开(公告)日：2001-12-03
申请号：AU6489401
申请日：2001-05-22
申请人： PHARMACOPEIA INC
发明人： HORLICK ROBERT , ZHAO JIUQUAO , SWANSON ROBERT , WEBB MARIA , STROHL BARBARA , BALDWIN JOHN J , AULD DOUGLAS S
IPC分类号： C07K14/705 , C07H21/04 , C12Q1/68
摘要： Methods for identifying modulators of receptor activity using orthologues of human receptors are described. Additionally, a method for identifying an animal model useful in the screening of potential therapeutic agents is provided. The genes for bradykinin B 1 receptors from five mammalian species, vervet monkey, rhesus macaque, tree shrew, dog and pig, as well as the genes for CXCR2 receptors from chimpanzee, gorilla, orangutan, rhesus, vervet and baboon have been cloned and characterized and are described herein.

5. 发明专利

CA2410394A1 ORTHOLOGUES OF HUMAN RECEPTORS AND METHODS OF USE 未知
公开(公告)号：CA2410394A1
公开(公告)日：2001-11-29
申请号：CA2410394
申请日：2001-05-22
申请人： PHARMACOPEIA INC
发明人： HORLICK ROBERT , ZHAO JIUQUAO , AULD DOUGLAS S , SWANSON ROBERT , BALDWIN JOHN J , STROHL BARBARA , WEBB MARIA
IPC分类号： C07K14/705 , C12N15/12 , C07H21/04 , C12N15/63 , C12N15/66 , C12Q1/68
摘要： Methods for identifying modulators of receptor activity using orthologues of human receptors are described. Additionally, a method for identifying an animal model useful in the screening of potential therapeutic agents is provided. The genes for bradykinin B 1 receptors from five mammalian species, vervet monkey, rhesus macaque, tree shrew, dog and pig, as well as the genes for CXCR2 receptors from chimpanzee, gorilla, orangutan, rhesus, vervet and baboon have been cloned and characterized and are described herein.

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