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1.发明授权公开(公告)号：US07566708B2
公开(公告)日：2009-07-28
申请号：US11509115
申请日：2006-08-23
申请人： Nidhi Arora , Roland Joseph Billedeau , Nolan James Dewdney , Tobias Gabriel , David Michael Goldstein , Counde O'Yang , Michael Soth , Teresa Alejandra Trejo-Martin
发明人： Nidhi Arora , Roland Joseph Billedeau , Nolan James Dewdney , Tobias Gabriel , David Michael Goldstein , Counde O'Yang , Michael Soth , Teresa Alejandra Trejo-Martin
IPC分类号： C07D487/04 , A61K31/519 , A61P31/18 , A61P31/22 , A61P37/08 , A61P31/16
CPC分类号： C07D471/04 , C07D487/04
摘要： Compounds effective as p38 MAP kinase inhibitors, methods of making the compounds, and methods of using the compounds for treatment of p38 MAP kinase-mediated diseases.
摘要翻译： 作为p38 MAP激酶抑制剂有效的化合物，制备化合物的方法，以及使用该化合物治疗p38 MAP激酶介导的疾病的方法。
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![Substituted pyrazolo [3,4-d] pyrimidines and methods of using the same](/abs-image/US/2008/11/18/US07452880B2/abs.jpg.150x150.jpg)
2.发明授权公开(公告)号：US07452880B2
公开(公告)日：2008-11-18
申请号：US11065890
申请日：2005-02-25
申请人： Nidhi Arora , Roland Joseph Billedeau , Nolan James Dewdney , Tobias Gabriel , David Michael Goldstein , Teresa Alejandra Trejo-Martin
发明人： Nidhi Arora , Roland Joseph Billedeau , Nolan James Dewdney , Tobias Gabriel , David Michael Goldstein , Teresa Alejandra Trejo-Martin
IPC分类号： C07D487/04 , C07D413/04 , A61K31/519 , A61K31/5355 , A61K31/497 , A61P19/02 , A61P11/04 , C07D471/02 , A61K31/4985 , A61K31/437
CPC分类号： C07D471/04 , C07D487/04
摘要： Compounds of the formula I: where A, B, X, Y, Z, k, R1, R2 and R3 are those defined herein, and compositions comprising the same. The present invention also provides methods for preparing compounds of formula I and using the same in treating p38 mediated disorders in a patient.
摘要翻译： 式I化合物：其中A，B，X，Y，Z，k，R 1，R 2和R 3是那些 和包含其的组合物。 本发明还提供了制备式I化合物的方法，并且使用它们来治疗患者中p38介导的病症。
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![Substituted pyrazolo[3,4-d]pyrimadines and methods of using the same](/abs-image/US/2008/10/14/US07435731B2/abs.jpg.150x150.jpg)
3.发明授权公开(公告)号：US07435731B2
公开(公告)日：2008-10-14
申请号：US11067336
申请日：2005-02-25
申请人： Nidhi Arora , Roland Joseph Billedeau , Nolan James Dewdney , Tobias Gabriel , David Michael Goldstein , Counde O'Yang , Michael Soth
发明人： Nidhi Arora , Roland Joseph Billedeau , Nolan James Dewdney , Tobias Gabriel , David Michael Goldstein , Counde O'Yang , Michael Soth
IPC分类号： C07D487/04 , C07D413/04 , C07D413/12 , A61K31/519 , A61K31/541 , A61K31/5355 , C07D471/04 , A61K31/437 , A61P19/02 , A61P11/16
CPC分类号： C07D487/04 , C07D471/04
摘要： Compounds of the formula Ia or Ib: wherein A, B, X, Y, Z, W, k, R1, R2, R3, R4 and R5 are those defined herein, and compositions comprising the same. The present invention also provides methods for preparing compounds of formula I and using the same in treating p38 mediated disorders in a subject.
摘要翻译： 式Ia或Ib化合物：其中A，B，X，Y，Z，W，k，R 1，R 2，R 3， SUP，R 4和R 5是本文定义的那些，以及包含它们的组合物。 本发明还提供了制备式I化合物的方法，并且使用它们来治疗受试者中p38介导的病症。
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公开(公告)号：US07495015B2
公开(公告)日：2009-02-24
申请号：US11065979
申请日：2005-02-25
IPC分类号： A61K31/4439
CPC分类号： C07D231/56
摘要： Compounds of the formula I: or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein m, k, B, R1, R2 and R3 are those defined herein, and compositions comprising the same. Also provided are methods for preparing compounds of formula I and using the same in treating p38 mediated disorders in a patient.
摘要翻译： 式I化合物或其药学上可接受的盐，溶剂合物或前药，其中m，k，B，R 1，R 2和R 3是本文定义的那些，以及包含其的组合物。 还提供了制备式I化合物的方法，并将其用于治疗患者中p38介导的病症。
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![Substituted pyrazolo[3,4-D]pyrimidines as p38 map kinase inhibitors](/abs-image/US/2009/07/21/US07563799B2/abs.jpg.150x150.jpg)
5.发明授权公开(公告)号：US07563799B2
公开(公告)日：2009-07-21
申请号：US11509422
申请日：2006-08-23
IPC分类号： C07D487/04 , A61K31/519 , A61P11/04 , A61P19/02
CPC分类号： C07D487/04
摘要： Compounds of the formula Ia or Ib: wherein X and Y are N or one of X and Y is N and the other is CRg, and A, D, E, G, W, R1, R2, R3, R4 and R5 are as defined herein. Also disclosed are methods of making the subject compounds and methods of using the compounds for treatment of p38 MAP kinase-mediated diseases.
摘要翻译： 式Ia或Ib化合物：其中X和Y为N或X和Y中的一个为N，另一个为CRg，A，D，E，G，W，R 1，R 2，R 3，R 4和R 5为 本文定义。 还公开了制备本发明化合物的方法和使用该化合物治疗p38MAP激酶介导的疾病的方法。
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![Substituted pyrazolo[3,4-d]pyrimidines as p38 MAP kinase inhibitors](/abs-image/US/2009/10/13/US07601726B2/abs.jpg.150x150.jpg)
6.发明授权Substituted pyrazolo[3,4-d]pyrimidines as p38 MAP kinase inhibitors 失效取代的吡唑并[3,4-d]嘧啶作为p38 MAP激酶抑制剂公开(公告)号：US07601726B2
公开(公告)日：2009-10-13
申请号：US11509240
申请日：2006-08-23
IPC分类号： C07D487/04 , A61K31/519 , A61P11/04 , A61P19/02
CPC分类号： C07D471/04 , C07D231/56 , C07D413/12 , C07D487/04
摘要： Compounds of formula Ia or Ib: wherein A, W, X, Y, R1, R2, R3 and R4 are as defined herein. Also disclosed are methods of making the compounds and methods of using the compounds for treatment of p38 MAP kinase-mediated diseases.
摘要翻译： 式Ia或Ib化合物：其中A，W，X，Y，R 1，R 2，R 3和R 4如本文所定义。 还公开了制备化合物的方法和使用该化合物治疗p38MAP激酶介导的疾病的方法。
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![Substituted pyrazolo[3,4-D]pyrimidines as p38 MAP kinase inhibitors](/abs-image/US/2009/10/27/US07608603B2/abs.jpg.150x150.jpg)
7.发明授权Substituted pyrazolo[3,4-D]pyrimidines as p38 MAP kinase inhibitors 失效取代的吡唑并[3,4-D]嘧啶作为p38 MAP激酶抑制剂公开(公告)号：US07608603B2
公开(公告)日：2009-10-27
申请号：US11509121
申请日：2006-08-23
IPC分类号： C07F9/09 , C07D487/04 , A61K31/519 , A61K31/661 , A61P11/16 , A61P19/02
CPC分类号： C07D487/04
摘要： Compounds of formula Ia, Ib, Ic, Id, Ie, If, Ig or Ih: wherein X and Y are nitrogen or one of X and Y is nitrogen and the other is CRg, and W, D, E, R4, R5, R6 and Rg are as defined herein. Also disclosed are methods of making the subject compounds and methods of using the compounds in the treatment of p38 MAP kinase-mediated diseases.
摘要翻译： 式Ia，Ib，Ic，Id，Ie，If，Ig或Ih的化合物：其中X和Y是氮或X和Y中的一个是氮，另一个是CR 1，W，D，E，R 4，R 5， R6和Rg如本文所定义。 还公开了制备本发明化合物的方法和使用该化合物治疗p38 MAP激酶介导的疾病的方法。
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公开(公告)号：US07943618B2
公开(公告)日：2011-05-17
申请号：US12288730
申请日：2008-10-23
申请人： Nolan James Dewdney , Rama K. Kondru , Yan Lou , Michael Soth , Tobias Gabriel
发明人： Nolan James Dewdney , Rama K. Kondru , Yan Lou , Michael Soth , Tobias Gabriel
IPC分类号： A61K31/50
CPC分类号： C07D213/63 , C07D401/12 , C07D401/14 , C07D403/14 , C07D409/12 , C07D413/12 , C07D413/14
摘要： This application discloses pyridine and pyrimidine compounds according to formula I wherein R1, R2, R3, R4, R5, X1 and A are as described herein which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of formula I and at least one carrier, diluent or excipient.
摘要翻译： 本申请公开了根据式I的吡啶和嘧啶化合物，其中R 1，R 2，R 3，R 4，R 5，X 1和A如本文所述抑制Btk。 本文公开的化合物可用于调节Btk的活性并治疗与过量Btk活性相关的疾病。 该化合物还可用于治疗与异常B细胞增殖相关的炎症和自身免疫疾病，例如类风湿性关节炎。 还公开了含有式I化合物和至少一种载体，稀释剂或赋形剂的组合物。
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公开(公告)号：US20090105209A1
公开(公告)日：2009-04-23
申请号：US12288730
申请日：2008-10-23
申请人： Nolan James Dewdney , Rama K. Kondru , Yan Lou , Michael Soth , Tobias Gabriel
发明人： Nolan James Dewdney , Rama K. Kondru , Yan Lou , Michael Soth , Tobias Gabriel
IPC分类号： A61K31/5377 , C07D403/14 , C07D417/14 , A61K31/501
CPC分类号： C07D213/63 , C07D401/12 , C07D401/14 , C07D403/14 , C07D409/12 , C07D413/12 , C07D413/14
摘要： This application discloses pyridine and pyrimidine compounds according to formula I wherein R1, R2, R3, R4, R5, X1 and A are as described herein which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of formula I and at least one carrier, diluent or excipient.
摘要翻译： 本申请公开了根据式I的吡啶和嘧啶化合物，其中R 1，R 2，R 3，R 4，R 5，X 1和A如本文所述抑制Btk。 本文公开的化合物可用于调节Btk的活性并治疗与过量Btk活性相关的疾病。 该化合物还可用于治疗与异常B细胞增殖相关的炎症和自身免疫疾病，例如类风湿性关节炎。 还公开了含有式I化合物和至少一种载体，稀释剂或赋形剂的组合物。
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10.发明申请公开(公告)号：US20050203091A1
公开(公告)日：2005-09-15
申请号：US11065890
申请日：2005-02-25
申请人： Nidhi Arora , Roland Billedeau , Nolan Dewdney , Tobias Gabriel , David Goldstein , Kristen McCaleb , Michael Soth , Teresa Trejo-Martin
发明人： Nidhi Arora , Roland Billedeau , Nolan Dewdney , Tobias Gabriel , David Goldstein , Kristen McCaleb , Michael Soth , Teresa Trejo-Martin
IPC分类号： A61K31/519 , A61K31/5377 , C07D471/04 , C07D487/02 , C07D487/04
CPC分类号： C07D471/04 , C07D487/04
摘要： Compounds of the formula I: where A, B, X, Y, Z, k, R1, R2 and R3 are those defined herein, and compositions comprising the same. The present invention also provides methods for preparing compounds of formula I and using the same in treating p38 mediated disorders in a patient.
摘要翻译： 式I化合物：其中A，B，X，Y，Z，k，R 1，R 2和R 3是那些 和包含其的组合物。 本发明还提供了制备式I化合物的方法，并且使用它们来治疗患者中p38介导的病症。
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