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1. 发明授权

US07405295B2 Certain imidazo[1,2-a]pyrazin-8-ylamines and method of inhibition of Bruton's tyrosine kinase by such compounds 有权
标题翻译：某些咪唑并[1,2-a]吡嗪-8-基胺和这种化合物抑制布鲁顿酪氨酸激酶的方法
公开(公告)号：US07405295B2
公开(公告)日：2008-07-29
申请号：US10861791
申请日：2004-06-04
申请人： Kevin S. Currie , Robert W. DeSimone , Scott A. Mitchell , Douglas A. Pippin , James W. Darrow , Xiaobing Qian , Mark Velleca , Dapeng Qian
发明人： Kevin S. Currie , Robert W. DeSimone , Scott A. Mitchell , Douglas A. Pippin , James W. Darrow , Xiaobing Qian , Mark Velleca , Dapeng Qian
IPC分类号： C07D417/00 , C07D413/00 , C07D471/00 , C07D487/00 , C07D491/00 , C07D497/00
CPC分类号： C07D487/04
摘要： Compounds of Formula I-a and all pharmaceutically-acceptable forms thereof, are described herein. The variables R1, R2, R3, Z1, Q, and A shown in Formula I-a are defined herein.Pharmaceutical compositions containing one or more compounds of Formula I-a, 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-a 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.
摘要翻译：本文描述式I-a化合物及其所有药学上可接受的形式。式Ia中所示的变量R 1，R 2，R 3，Z 1，Q和A 在本文中定义。本文提供了含有一种或多种式I-a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减少疾病体征或症状的式I-a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。

2. 发明授权

US07312341B2 6-aryl-imidazo[1,2-a] pyrazin-8-ylamines, method of making, and method of use thereof 有权
标题翻译： 6-芳基 - 咪唑并[1,2-a]吡嗪-8-基胺，其制备方法及其使用方法
公开(公告)号：US07312341B2
公开(公告)日：2007-12-25
申请号：US10658121
申请日：2003-09-09
申请人： Robert W. DeSimone , Douglas A. Pippin , James W. Darrow , Scott A. Mitchell , Kevin S. Currie
发明人： Robert W. DeSimone , Douglas A. Pippin , James W. Darrow , Scott A. Mitchell , Kevin S. Currie
IPC分类号： C07D209/00 , C07D487/02
CPC分类号： C07D487/04
摘要： A novel composition comprises a compound of Formula 1 the pharmaceutically acceptable salts, hydrates, solvates, crystal forms, diastereomers, prodrugs, or mixtures thereof. The composition is of particular utility in the treatment of kinase-implicated disorders.
摘要翻译：一种新型组合物包含式1的化合物，其药学上可接受的盐，水合物，溶剂化物，晶体形式，非对映异构体，前药或其混合物。该组合物在治疗激酶介导性疾病方面特别有用。

3. 发明授权

US06919340B2 Imidazo[1,2-a]pyrazin-8-ylamines, method of making, and method of use thereof 失效
标题翻译：咪唑并[1,2-a]吡嗪-8-基胺，其制备方法及其使用方法
公开(公告)号：US06919340B2
公开(公告)日：2005-07-19
申请号：US10419682
申请日：2003-04-21
申请人： Kevin S. Currie , Robert W. DeSimone , Douglas A. Pippin , James W. Darrow , Scott A. Mitchell
发明人： Kevin S. Currie , Robert W. DeSimone , Douglas A. Pippin , James W. Darrow , Scott A. Mitchell
IPC分类号： A61K31/282 , A61K31/337 , A61K31/407 , A61K31/4985 , A61K31/704 , A61K31/7048 , A61K33/24 , A61P1/16 , A61P3/00 , A61P3/04 , A61P3/10 , A61P5/10 , A61P5/14 , A61P7/06 , A61P9/00 , A61P9/10 , A61P9/12 , A61P11/08 , A61P13/08 , A61P13/12 , A61P17/00 , A61P17/06 , A61P19/00 , A61P19/02 , A61P21/04 , A61P25/00 , A61P25/02 , A61P25/16 , A61P25/28 , A61P27/02 , A61P29/00 , A61P31/04 , A61P31/18 , A61P35/00 , A61P35/02 , A61P37/02 , A61P37/04 , A61P37/06 , A61P43/00 , C07D487/04 , A01N43/58 , A01N43/60 , A61K31/495 , A61K31/50 , C07D471/00
CPC分类号： C07D487/04
摘要： A novel composition comprises a compound of Formula 1 the pharmaceutically acceptable salts, hydrates, solvates, crystal forms, diastereomers, prodrugs, or mixtures thereof. The composition is of particular utility in the treatment of kinase-implicated disorders.
摘要翻译：一种新型组合物包含式1的化合物，其药学上可接受的盐，水合物，溶剂化物，晶体形式，非对映异构体，前药或其混合物。该组合物在治疗激酶介导性疾病方面特别有用。

4. 发明申请

US20110177011A1 CERTAIN IMIDAZO[1,2-A]PYRAZIN-8-YLAMINES AND METHOD OF INHIBITION OF BRUTON'S TYROSINE KINASE BY SUCH COMPOUNDS 审中-公开
标题翻译：某些咪唑并[1,2-A]吡嗪-8-胺和这种化合物抑制BRUTON的酪氨酸激酶的方法
公开(公告)号：US20110177011A1
公开(公告)日：2011-07-21
申请号：US12018573
申请日：2008-01-23
申请人： Kevin S. Currie , Robert W. DeSimone , Scott A. Mitchell , Douglas A. Pippin , James W. Darrow , Xiaobing Qian , Mark Velleca , Dapeng Qian
发明人： Kevin S. Currie , Robert W. DeSimone , Scott A. Mitchell , Douglas A. Pippin , James W. Darrow , Xiaobing Qian , Mark Velleca , Dapeng Qian
IPC分类号： A61K31/551 , A61K31/4985 , A61K31/5355 , A61K9/12 , A61P29/00 , A61P35/00
CPC分类号： C07D487/04
摘要： Compounds of Formula I-a and all pharmaceutically-acceptable forms thereof, are described herein.The variables R1, R2, R3, Z1, Q, and A shown in Formula I-a are defined herein.Pharmaceutical compositions containing one or more compounds of Formula I-a, 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-a 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 and domesticated companion animals, suffering from a disease responsive to inhibition of kinase activity.Methods of treatment include administering a compound of Formula I-a as a single active agent or administering a compound of Formula I-a 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-a 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：本文描述式I-a化合物及其所有药学上可接受的形式。式I-a中所示的变量R1，R2，R3，Z1，Q和A在本文中定义。本文提供了含有一种或多种式I-a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减少疾病体征或症状的式I-a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，包括患有对抑制激酶活性有响应的疾病的家畜和驯养的伴侣动物的方法。治疗方法包括施用式I-a化合物作为单一活性剂或给予式I-a的化合物与一种或多种其它治疗剂的组合。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Ia化合物或其形式接触的方法，样品中没有Btk。

5. 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。

6. 发明授权

US07189723B2 Certain 8-heteroaryl-6-phenyl-imidazo[1,2-a]pyrazines as modulators of kinase activity 有权
公开(公告)号：US07189723B2
公开(公告)日：2007-03-13
申请号：US10776002
申请日：2004-02-10
申请人： Scott A. Mitchell , Kevin S. Currie , Robert W. DeSimone , Douglas A. Pippin
发明人： Scott A. Mitchell , Kevin S. Currie , Robert W. DeSimone , Douglas A. Pippin
IPC分类号： A01N43/58 , A01N43/60 , A61K31/50 , A61K31/495 , C07D47/00
CPC分类号： C07D487/04
摘要： This invention pertains to compounds of Formula I: and all pharmaceutically-acceptable forms thereof. The variables R1, R2, R3, Z1, Z2, W, and X shown in Formula I are defined herein.The invention also provides pharmaceutical compositions containing one or more compound of Formula I, or a pharmaceutically acceptable form of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents.The invention further comprises methods of treating patients suffering from certain diseases and disorders responsive to EphB4 kinase modulation, which comprise administering to such patients an amount of a compound of Formula I effective to reduce signs or symptoms of the disease or disorder. These diseases include cancer, including of breast neoplasma, endometrial cancer, colon cancer, and neck squamous cell carcinoma. Thus methods of treatment include administering a sufficient amount of a compound or salt of the invention to decrease the symptoms or slow the progression of these diseases or disorders.The invention also encompasses methods of treating other animals, including livestock and domesticated companion animals, suffering from an disease or disorder responsive to EphB4 modulation.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.The invention also includes a method for determining the presence of EphB4 kinase in a sample, comprising contacting the sample with a compound of Formula I, or form thereof, and the detecting the amount of compound or form bound to EphB4 kinase, and therefrom determining the presence or absence of EphB4 kinase in the sample.

7. 发明授权

US07160885B2 Certain 6, 8-(heteroaryl or aryl) disubstituted imidazo[1,2-a]pyrazines as modulators of Hsp90 complex activity 有权
公开(公告)号：US07160885B2
公开(公告)日：2007-01-09
申请号：US10776631
申请日：2004-02-10
申请人： Kevin S. Currie , Robert W. DeSimone , Douglas A. Pippin , James W. Darrow , Scott A. Mitchell
发明人： Kevin S. Currie , Robert W. DeSimone , Douglas A. Pippin , James W. Darrow , Scott A. Mitchell
IPC分类号： A01N43/58 , A01N43/60 , A61K31/50 , A61K31/495 , C07D471/00
CPC分类号： C07D487/04
摘要： This invention pertains to compounds of Formula I: and the pharmaceutically-acceptable forms thereof. The variables R1, R2, R3, Z1, Z2, W, and X shown in Formula I are defined herein.The invention also provides pharmaceutical compositions containing one or more compound of Formula I, or pharmaceutically acceptable form of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents.The invention further comprises methods of treating patients suffering from certain diseases and disorders responsive to Hsp90 complex modulation, which comprise administering to such patients an amount of a compound of Formula I effective to reduce signs or symptoms of the disease or disorder. These diseases include cancer, including chronic myeloid leukemia, melanoma, breast, ovarian, brain, thyroid, colorectal, prostate, and bladder cancer, heart disease, stroke, autoimmune/inflammatory diseases, and neurodegenerative diseases. Thus methods of treatment include administering a sufficient amount of a compound of Formula I or form thereof to decrease the symptoms or slow the progression of these diseases or disorders.The invention also encompasses methods of treating non-human patients, including livestock and domesticated companion animals, suffering from a disease or disorder responsive to Hsp90 complex modulation.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.The invention also includes a method for determining the presence of certain kinases or Hsp90 complex in a sample, comprising contacting the sample with a compound of Formula I or form thereof, and detecting Hsp9O complex activity in the sample.

8. 发明授权

US07393848B2 Certain heterocyclic substituted imidazo[1,2-A]pyrazin-8-ylamines and methods of inhibition of Bruton's tyrosine kinase by such compounds 有权
标题翻译：某些杂环取代的咪唑并[1,2-A]吡嗪-8-基胺和这些化合物抑制布鲁顿酪氨酸激酶的方法
公开(公告)号：US07393848B2
公开(公告)日：2008-07-01
申请号：US10883646
申请日：2004-06-30
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： A01N43/58 , A01N43/60 , A61K31/50 , A61K31/495 , C07D471/00 , C07D487/00 , C07D491/00 , C07D495/00
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 and 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，包括患有对抑制激酶活性有响应的疾病的家畜和驯养的伴侣动物的方法。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。

9. 发明授权

US07015227B2 Certain amino-substituted monocycles as kinase modulators 有权
标题翻译：某些氨基取代的单环作为激酶调节剂
公开(公告)号：US07015227B2
公开(公告)日：2006-03-21
申请号：US10602560
申请日：2003-06-23
申请人： James W. Darrow , Robert W. DeSimone , Douglas A. Pippin , Scott A. Mitchell
发明人： James W. Darrow , Robert W. DeSimone , Douglas A. Pippin , Scott A. Mitchell
IPC分类号： A61K31/4965 , C07D241/00 , C07D241/02
CPC分类号： C07D239/26 , C07D239/42 , C07D241/20
摘要： A composition comprises a compound of Formula 1: a pharmaceutically acceptable salt, hydrate, solvate, crystal form, diastereomer, prodrug, or mixture thereof, wherein W is a nitrogen-substituted 5- or 6-membered monocyclic ring. The compounds are of utility as modulators of kinase activity.
摘要翻译：组合物包含式1的化合物：其药学上可接受的盐，水合物，溶剂合物，结晶形式，非对映异构体，前药或其混合物，其中W是氮取代的5-或6-元单环。这些化合物可用作激酶活性的调节剂。

10. 发明授权

US07259164B2 Certain substituted imidazo[1,2-a]pyrazines, as modulators of kinase activity 有权
标题翻译：某些取代的咪唑并[1,2-a]吡嗪，作为激酶活性的调节剂
公开(公告)号：US07259164B2
公开(公告)日：2007-08-21
申请号：US10915696
申请日：2004-08-11
申请人： Scott A. Mitchell , Robert W. DeSimone , James W. Darrow , Douglas A. Pippin , M. Diana Danca
发明人： Scott A. Mitchell , Robert W. DeSimone , James W. Darrow , Douglas A. Pippin , M. Diana Danca
IPC分类号： A01N43/58 , A01N43/60 , A61K31/50 , A61K31/495 , C07D471/00
CPC分类号： C07D487/04
摘要： Certain substituted imidazo[1,2-a]pyrazines and the pharmaceutically acceptable salts thereof, are provided herein. Pharmaceutical compositions containing one or more compound of Formula I, or a pharmaceutically acceptable salt of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents, are also provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to EphB4 kinase modulation, which comprise administering to such patients an amount of a compound of Formula I effective to reduce signs or symptoms of the disease or disorder are disclosed.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 agents.A method for determining the presence or absence of an angiogenic kinase in a sample comprising contacting the sample with a compound of Formula I under conditions that permit detection of activity of the angiogenic kinase, detecting a level of the activity of the angiogenic kinase, and therefrom determining the presence or absence of the angiogenic kinase in the sample.
摘要翻译：本文提供了某些取代的咪唑并[1,2-a]吡嗪及其药学上可接受的盐。本文还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盐以及一种或多种药学上可接受的载体，赋形剂或稀释剂的药物组合物。公开了治疗患有某些对EphB4激酶调节作用的疾病和病症的患者的方法，其包括给予这样的患者一定量的有效降低疾病或病症体征或症状的式I化合物。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联合给药。一种用于确定样品中血管生成激酶存在或不存在的方法，包括在允许检测血管生成激酶活性，检测血管生成激酶活性水平的条件下将样品与式I化合物接触确定样品中存在或不存在血管生成激酶。

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