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1. 发明申请

US20100022516A1 4,5-Disubstituted-2-aryl pyrimidines 失效
标题翻译： 4,5-二取代-2-芳基嘧啶
公开(公告)号：US20100022516A1
公开(公告)日：2010-01-28
申请号：US12320539
申请日：2009-01-26
申请人： George D. MAYNARD , Manuka GHOSH , Jun YUAN , Kevin S. CURRIE , Scott MITCHELL , Qin GUO , He ZHAO
发明人： George D. MAYNARD , Manuka GHOSH , Jun YUAN , Kevin S. CURRIE , Scott MITCHELL , Qin GUO , He ZHAO
IPC分类号： A61K31/55 , A61K31/513 , A61K31/506 , C07D403/02
CPC分类号： A61K31/505 , C07D239/26 , C07D239/28 , C07D239/34 , C07D239/42 , C07D239/47 , C07D239/48 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12 , C07D417/04 , C07D471/04 , C07D498/04
摘要： 4,5-disubstituted-2-arypyrimidines of Formula I and Formula II are provided: wherein R1, R2, R3, R8, R9, A and Ar are defined herein. Such compounds are ligands of C5a receptors. Preferred compounds of Formula I and II bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. The present invention also relates to pharmaceutical compositions comprising such compounds, and to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. In addition, the present invention provides labeled 4,5-disubstituted-2-arylpyrimidines, which are useful as probes for the localization of C5a receptors.
摘要翻译：提供式I和式II的4,5-二取代-2-丙嘧啶：其中R1，R2，R3，R8，R9，A和Ar如本文所定义。这些化合物是C5a受体的配体。优选的式I和II化合物以高亲和力结合C5a受体，并在C5a受体上呈现中性拮抗剂或反向激动剂活性。本发明还涉及包含这些化合物的药物组合物，以及这些化合物在治疗各种炎性，心血管和免疫系统疾病中的用途。此外，本发明提供标记的4,5-二取代-2-芳基嘧啶，其可用作C5a受体定位的探针。

2. 发明申请

US20130023499A1 CERTAIN SUBSTITUTED AMIDES, METHOD OF MAKING, AND METHOD OF USE THEREOF 有权
公开(公告)号：US20130023499A1
公开(公告)日：2013-01-24
申请号：US13343624
申请日：2012-01-04
申请人： Scott A. MITCHELL , Kevin S. CURRIE , Peter A. BLOMGREN , David M. ARMISTEAD , Joseph RAKER
发明人： Scott A. MITCHELL , Kevin S. CURRIE , Peter A. BLOMGREN , David M. ARMISTEAD , Joseph RAKER
IPC分类号： A61K31/4985 , A61K31/625 , A61K31/5377 , A61K31/551 , A61K31/501 , A61P37/06 , A61P29/00 , A61P37/08 , A61P35/00 , A61P35/02 , A61P11/06 , A61P11/00 , A61P25/00 , A61K31/538 , C12N5/071 , C12N5/0781 , G01N33/573 , C07D487/04
CPC分类号： C07D487/04
摘要： Certain chemical entities chosen from compounds represented by Formula I and pharmaceutically acceptable salts and mixtures thereof, are provided herein. Pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include cancer (e.g., B-cell lymphoma and leukemia), autoimmune diseases, inflammatory diseases, acute inflammatory reactions, and allergic disorders. Methods of treatment include administering at least one chemical entity as a single active agent or administering at least one chemical entity in combination with one or more other therapeutic agents. Also provided are methods for determining the presence or absence of Syk kinase in a sample.

3. 发明申请

US20120220582A1 IMIDAZOPYRAZINE SYK INHIBITORS 有权
标题翻译：咪唑吡嗪SYK抑制剂
公开(公告)号：US20120220582A1
公开(公告)日：2012-08-30
申请号：US13441441
申请日：2012-04-06
申请人： Scott A. MITCHELL , Kevin S. CURRIE
发明人： Scott A. MITCHELL , Kevin S. CURRIE
IPC分类号： A61K31/5377 , A61P35/00 , A61P37/08 , A61P29/00 , A61P37/00 , A61P35/02 , A61P19/02 , A61P11/02 , A61P11/00 , A61P25/00 , A61P1/00 , A61P1/04 , A61P19/04 , A61P13/12 , C12Q1/48 , C07D487/04
CPC分类号： C07D471/04 , C07D487/04 , C07D491/107 , C07D498/04 , C07D498/08 , C07D519/00
摘要： Certain imidazopyrazines and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.
摘要翻译：本文提供了某些咪唑并嗪及其药物组合物。治疗患有某些对抑制Syk活性有作用的疾病和病症的患者的方法，其包括给予这些患者一定量的至少一种有效减少疾病或病症体征或症状的化学实体。还提供了用于确定样品中Syk激酶的存在或不存在的方法。

4. 发明申请

US20080182849A1 Certain Heterocyclic Substituted Imidazo[1,2-A]Pyrazin-8-Ylamines And Methods Of Inhibition Of Bruton's Tyrosine Kinase By Such Compounds 审中-公开
标题翻译：某些杂环取代的咪唑并[1,2-A]吡嗪-8-胺和这些化合物抑制布鲁特酪氨酸激酶的方法
公开(公告)号：US20080182849A1
公开(公告)日：2008-07-31
申请号：US12055514
申请日：2008-03-26
申请人： Kevin S. CURRIE , Robert W. DeSimone , Scott A. Mitchell , Douglas A. Pippin
发明人： Kevin S. CURRIE , Robert W. DeSimone , Scott A. Mitchell , Douglas A. Pippin
IPC分类号： A61K31/4985
CPC分类号： C07D487/04
摘要： Compounds of Formula I and all pharmaceutically acceptable forms thereof, are described herein.The variables R1, R2, R3, Z2, and Q, shown in Formula I are defined herein.Pharmaceutical compositions containing one or more compounds of Formula I, or a pharmaceutically acceptable form of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents are provided herein.Methods of treating patients suffering from certain diseases responsive to inhibition of tyrosine kinase activity are also given. In certain embodiments the diseases are responsive to inhibition of Btk activity and/or B-cell proliferation. Such methods comprise administering to such patients an amount of a compound of Formula I effective to reduce signs or symptoms of the disease. These diseases include cancer, an autoimmune and/or inflammatory disease, or an acute inflammatory reaction. Thus methods of treatment include administering a sufficient amount of a compound or salt as provided herein to decrease the symptoms or slow the progression of these diseases.Other embodiments include methods of treating other animals, including livestock aid domesticated companion animals, suffering from a disease responsive to inhibition of kinase activity.Methods of treatment include administering a compound of Formula I as a single active agent or administering a compound of Formula I in combination with one or more other therapeutic agent.A method for determining the presence of Btk in a sample, comprising contacting the sample with a compound or form thereof of Formula I under conditions that permit detection of Btk activity, detecting a level of Btk activity in the sample, and therefrom determining the presence or absence of Btk in the sample.
摘要翻译：本文描述了式I化合物及其所有药学上可接受的形式。式I中所示的R 1，R 2，R 3，R 3，Z 2和Q的变量是本文定义。本文提供了含有一种或多种式I化合物或这些化合物的药学上可接受的形式的药物组合物和一种或多种药学上可接受的载体，赋形剂或稀释剂。还给出了治疗患有某些对抑制酪氨酸激酶活性有响应的疾病的患者的方法。在某些实施方案中，疾病对Btk活性和/或B细胞增殖的抑制有反应。这样的方法包括向这样的患者施用一定量的有效降低疾病体征或症状的式I化合物。这些疾病包括癌症，自身免疫和/或炎性疾病或急性炎症反应。因此，治疗方法包括施用足够量的本文提供的化合物或盐以减少症状或减缓这些疾病的进展。其他实施方案包括治疗其它动物的方法，包括家畜帮助驯化的伴侣动物，患有对抑制激酶活性有反应作用的疾病。治疗方法包括给予式I化合物作为单一活性剂或将一种式I化合物与一种或多种其它治疗剂组合施用。一种用于确定样品中Btk的存在的方法，包括在允许检测Btk活性，检测样品中Btk活性水平的条件下使样品与式I化合物或其形式接触的方法，样品中没有Btk。

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