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1. 发明申请

US20080125417A1 CERTAIN PYRIMIDINES, METHOD OF MAKING, AND METHOD OF USE THEREOF 审中-公开
标题翻译：某些吡咯烷酮，其制备方法及其使用方法
公开(公告)号：US20080125417A1
公开(公告)日：2008-05-29
申请号：US11853488
申请日：2007-09-11
申请人： Kevin S. Currie , Tony Lee , James W. Darrow , Peter A. Blomgren
发明人： Kevin S. Currie , Tony Lee , James W. Darrow , Peter A. Blomgren
IPC分类号： A61K31/541 , C07D295/00 , C07D239/02 , A61K31/496 , C12Q1/48 , A61P29/00 , A61P37/00 , A61P35/00 , C12N5/00 , A61K31/505 , A61K31/5377
CPC分类号： C07D239/42 , C07D401/12 , C07D403/12 , C07D409/12 , C07D409/14
摘要： At least one chemical entity chosen from compounds of Formula 1 and pharmaceutically acceptable salts, solvates, chelates, non-covalent complexes, prodrugs, and mixtures thereof, is described herein.Pharmaceutical compositions comprising at least one chemical entity of Formula 1, together with at least one pharmaceutically acceptable vehicle chosen from carriers adjuvants, and excipients, are described.Methods of treating patients suffering from certain diseases responsive to inhibition of Btk activity and/or B-cell activity are described. Methods for determining the presence of Btk in a sample are described.
摘要翻译：本文描述了至少一种选自式1化合物的化学实体及其药学上可接受的盐，溶剂合物，螯合物，非共价复合物，前药及其混合物。描述了包含至少一种式1的化学实体的药物组合物，以及选自载体佐剂和赋形剂的至少一种药学上可接受的载体。描述了治疗患有某些对Btk活性和/或B细胞活性的抑制作出反应的某些疾病的患者的方法。描述了确定样品中Btk的存在的方法。

2. 发明授权

US08058446B2 Certain substituted amides, method of making, and method of use thereof 有权
标题翻译：某些取代的酰胺，制备方法及其使用方法
公开(公告)号：US08058446B2
公开(公告)日：2011-11-15
申请号：US11853485
申请日：2007-09-11
申请人： Peter A. Blomgren , Kevin S. Currie , Jeffrey E. Kropf , Tony Lee , James W. Darrow , Scott A. Mitchell , Jianjun Xu , Aaron C. Schmitt
发明人： Peter A. Blomgren , Kevin S. Currie , Jeffrey E. Kropf , Tony Lee , James W. Darrow , Scott A. Mitchell , Jianjun Xu , Aaron C. Schmitt
IPC分类号： C07D409/00 , A61K31/44
CPC分类号： C07D213/64 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： At least one chemical entity chosen from compounds of Formula 1 and pharmaceutically acceptable salts, solvates, chelates, non-covalent complexes, prodrugs, and mixtures thereof is described herein. Pharmaceutical compositions comprising at least one chemical entity of the invention, together with at least one pharmaceutically acceptable vehicle chosen from carriers adjuvants, and excipients, are described.Methods of treating patients suffering from certain diseases responsive to inhibition of Btk activity and/or B-cell activity are described. Methods for determining the presence of Btk in a sample are described.
摘要翻译：本文描述了至少一种选自式1化合物的化学实体及其可药用盐，溶剂合物，螯合物，非共价复合物，前药及其混合物。描述了包含本发明的至少一个化学实体的药物组合物以及选自载体佐剂和赋形剂的至少一种药学上可接受的载体。描述了治疗患有某些对Btk活性和/或B细胞活性的抑制作出反应的某些疾病的患者的方法。描述了确定样品中Btk的存在的方法。

3. 发明申请

US20080139557A1 CERTAIN SUBSTITUTED AMIDES, METHOD OF MAKING, AND METHOD OF USE THEREOF 有权
标题翻译：某些替代的制剂，制备方法及其使用方法
公开(公告)号：US20080139557A1
公开(公告)日：2008-06-12
申请号：US11853485
申请日：2007-09-11
申请人： Peter A. Blomgren , Kevin S. Currie , Jeffrey E. Kropf , Tony Lee , James W. Darrow , Scott A. Mitchell , Jianjun Xu , Aaron C. Schmitt
发明人： Peter A. Blomgren , Kevin S. Currie , Jeffrey E. Kropf , Tony Lee , James W. Darrow , Scott A. Mitchell , Jianjun Xu , Aaron C. Schmitt
IPC分类号： C07D401/02 , A61K31/4439 , A61K31/496 , C07D401/14 , C07D413/14 , A61K31/5377 , A61P37/00 , A61P35/00 , C12N5/00 , C12Q1/48
CPC分类号： C07D213/64 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： At least one chemical entity chosen from compounds of Formula 1 and pharmaceutically acceptable salts, solvates, chelates, non-covalent complexes, prodrugs, and mixtures thereof is described herein.Pharmaceutical compositions comprising at least one chemical entity of the invention, together with at least one pharmaceutically acceptable vehicle chosen from carriers adjuvants, and excipients, are described.Methods of treating patients suffering from certain diseases responsive to inhibition of Btk activity and/or B-cell activity are described. Methods for determining the presence of Btk in a sample are described.
摘要翻译：本文描述了至少一种选自式1化合物的化学实体及其可药用盐，溶剂合物，螯合物，非共价复合物，前药及其混合物。描述了包含本发明的至少一个化学实体的药物组合物以及选自载体佐剂和赋形剂的至少一种药学上可接受的载体。描述了治疗患有某些对Btk活性和/或B细胞活性的抑制作出反应的某些疾病的患者的方法。描述了确定样品中Btk的存在的方法。

4. 发明申请

US20100160292A1 Kinase Inhibitors, and Methods of Using and Identifying Kinase Inhibitors 审中-公开
标题翻译：激酶抑制剂和使用和鉴定激酶抑制剂的方法
公开(公告)号：US20100160292A1
公开(公告)日：2010-06-24
申请号：US12440695
申请日：2007-09-11
申请人： James A. Whitney , Julie Di Paolo , Mark Velleca , David R. Brittelli , Kevin S. Currie , James W. Darrow , Jeffrey E. Krope , Seung H. Lee , Steven L. Gallion , Scott A. Mitchell , Doughlas A.I. Pippen , Peter A. Blomgren , Doughlas Gregory Stafford
发明人： James A. Whitney , Julie Di Paolo , Mark Velleca , David R. Brittelli , Kevin S. Currie , James W. Darrow , Jeffrey E. Krope , Seung H. Lee , Steven L. Gallion , Scott A. Mitchell , Doughlas A.I. Pippen , Peter A. Blomgren , Doughlas Gregory Stafford
IPC分类号： A61K31/4418 , G01N33/53 , C12N9/96 , C12N5/00 , A61K31/553 , A61K31/551 , A61K31/541 , A61K31/5377 , A61K31/496 , A61K31/4965 , A61K31/4545 , C07D403/12 , C07D413/12 , C07D241/20 , C07D401/12 , C07D213/72 , A61P37/00
CPC分类号： A61K31/00 , A61K31/44 , A61K31/4965 , A61K31/497 , A61K31/4985 , A61K31/5377 , C12Q1/485 , G01N2500/04
摘要： Methods of inhibiting BTK activity by inhibiting phosphorylation of Y551 of BTK, methods of treating patients by inhibiting BTK activity by inhibiting phosphorylation of Y551 of BTK, chemical entities that bind to BTK and inhibited complexes are provided.
摘要翻译：通过抑制BTK的Y551的磷酸化抑制BTK活性的方法，提供了通过抑制BTK的Y551的磷酸化，结合BTK的化学实体和抑制复合物来抑制BTK活性来治疗患者的方法。

5. 发明授权

US07947835B2 Certain substituted amides, method of making, and method of use thereof 有权
标题翻译：某些取代的酰胺，制备方法及其使用方法
公开(公告)号：US07947835B2
公开(公告)日：2011-05-24
申请号：US11371180
申请日：2006-03-09
申请人： David R. Brittelli , Kevin S. Currie , James W. Darrow , Jeffrey E. Kropf , Seung H. Lee , Steven L. Gallion , Scott A. Mitchell , Douglas A. I. Pippin , Peter A. Blomgren , Douglas Gregory Stafford
发明人： David R. Brittelli , Kevin S. Currie , James W. Darrow , Jeffrey E. Kropf , Seung H. Lee , Steven L. Gallion , Scott A. Mitchell , Douglas A. I. Pippin , Peter A. Blomgren , Douglas Gregory Stafford
IPC分类号： C07D403/12 , C07D403/14 , C07D401/12 , C07D401/14 , A61K31/501 , A61P17/06
CPC分类号： C07D213/74 , C07D241/20 , C07D241/24 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D487/04
摘要： At least one chemical entity chosen from compounds of Formula 2 and pharmaceutically acceptable salts, solvates, chelates, non-covalent complexes, prodrugs, and mixtures thereof is described herein. Pharmaceutical compositions comprising at least one chemical entity of the invention, together with at least one pharmaceutically acceptable vehicle chosen from carriers adjuvants, and excipients, are described.Methods of treating patients suffering from certain diseases responsive to inhibition of Btk activity and/or B-cell activity are described. Methods for determining the presence of Btk in a sample are described.
摘要翻译：本文描述了至少一种选自式2化合物的化学实体及其药学上可接受的盐，溶剂合物，螯合物，非共价复合物，前药及其混合物。描述了包含本发明的至少一个化学实体的药物组合物以及选自载体佐剂和赋形剂的至少一种药学上可接受的载体。描述了治疗患有某些对Btk活性和/或B细胞活性的抑制作出反应的某些疾病的患者的方法。描述了确定样品中Btk的存在的方法。

6. 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。

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

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。

9. 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。

10. 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。

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