公开(公告)号：US08691809B2

公开(公告)日：2014-04-08

申请号：US12859178

申请日：2010-08-18

Applicant: James Jeffry Howbert ,  Gregory Dietsch ,  Robert Hershberg ,  Laurence E. Burgess ,  Joseph P. Lyssikatos ,  Brad Newhouse ,  Hong Woon Yang

Inventor： James Jeffry Howbert ,  Gregory Dietsch ,  Robert Hershberg ,  Laurence E. Burgess ,  Joseph P. Lyssikatos ,  Brad Newhouse ,  Hong Woon Yang

IPC: A61K31/55 ,  C07D223/16 ,  A61P11/06 ,  A61P37/02 ,  A61P35/00

CPC classification number: A61K31/55 ,  C07D223/14 ,  C07D223/16 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/10 ,  C07D405/04 ,  C07D405/10

Abstract: Provided are compositions and methods useful for modulation of signaling through the Toll-like receptors TLR7 and/or TLR8. The compositions and methods have use in treating or preventing disease, including cancer, autoimmune disease, infectious disease, inflammatory disorder, graft rejection, and graft-verses-host disease.

Abstract translation: 提供了可用于通过Toll样受体TLR7和/或TLR8调节信号传导的组合物和方法。 组合物和方法可用于治疗或预防疾病，包括癌症，自身免疫性疾病，感染性疾病，炎性疾病，移植物排斥反应和移植物宿主病。

公开(公告)号：US08680114B2

公开(公告)日：2014-03-25

申请号：US12567258

申请日：2009-09-25

Applicant: Ian S. Mitchell ,  Keith L. Spencer ,  Peter Stengel ,  Yongxin Han ,  Nicholas C. Kallan ,  Mark Munson ,  Guy P. A. Vigers ,  James Blake ,  Anthony Piscopio ,  John Josey ,  Scott Miller ,  Dengming Xiao ,  Rui Xu ,  Chang Rao ,  Bing Wang ,  April L. Bernacki

Inventor： Ian S. Mitchell ,  Keith L. Spencer ,  Peter Stengel ,  Yongxin Han ,  Nicholas C. Kallan ,  Mark Munson ,  Guy P. A. Vigers ,  James Blake ,  Anthony Piscopio ,  John Josey ,  Scott Miller ,  Dengming Xiao ,  Rui Xu ,  Chang Rao ,  Bing Wang ,  April L. Bernacki

IPC: A61K31/47 ,  A01N43/42 ,  C07D215/00

CPC classification number: C07D239/94 ,  B41M3/008 ,  B44F1/10 ,  C07D231/56 ,  C07D237/28 ,  C07D239/42 ,  C07D239/47 ,  C07D239/48 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D409/04 ,  C07D409/12 ,  C07D471/04 ,  C07D487/04 ,  C07D491/048 ,  C07D495/04 ,  G09F13/16 ,  Y10T428/24802 ,  Y10T428/24851 ,  Y10T428/25 ,  Y10T428/31507 ,  Y10T428/31551 ,  Y10T428/31786 ,  Y10T428/31855

Abstract: The present invention provides compounds, including resolved enantiomers, diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula: A-L-CR where CR is a cyclical core group, L is a linking group and A is as defined herein. Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.

Abstract translation: 本发明提供包括分解对映异构体，非对映异构体，溶剂化物和药学上可接受的盐的化合物，其包含式为：A-L-CR，其中CR为环状核心基团，L为连接基团，A如本文所定义。 还提供了使用本发明化合物作为AKT蛋白激酶抑制剂和治疗过度增殖性疾病如癌症的方法。

公开(公告)号：US20140045817A1

公开(公告)日：2014-02-13

申请号：US14057882

申请日：2013-10-18

Applicant: Array BioPharma Inc.

Inventor： Shelley Allen ,  Laura L. Celeste ,  T. Gregg Davis ,  Robert Kirk DeLisle ,  Julie Marie Hicks ,  Stefan D. Gross ,  Erik James Hicken ,  Leila J. Jackson ,  Nicholas C. Kallan ,  Joseph P. Lyssikatos ,  Fredrik P. Marmsater ,  Mark C. Munson ,  Jed Pheneger ,  Bryson Rast ,  John E. Robinson ,  Stephen T. Schlachter ,  George T. Topalov ,  A. Dale Wright ,  Qian Zhao

IPC: C07D471/04 ,  C07D451/06

CPC classification number: C07D471/04 ,  A61K31/437 ,  C07D451/06 ,  C07D519/00

Abstract: Provided herein is a method of treating a PIM-1 and/or PIM-2 and/or PIM-3 kinase-mediated condition in a mammal, which comprises administering to said mammal a therapeutically effective amount of a compound of Formula I: in which A, B, R1, R1a, R2, R3, R4, R5, R6, and R7 have the meanings given in the specification.

Abstract translation: 本文提供了一种在哺乳动物中治疗PIM-1和/或PIM-3和/或PIM-3激酶介导的病症的方法，其包括向所述哺乳动物施用治疗有效量的式I化合物：其中 A，B，R1，R1a，R2，R3，R4，R5，R6和R7具有说明书中给出的含义。

公开(公告)号：US08648087B2

公开(公告)日：2014-02-11

申请号：US12085048

申请日：2006-11-15

Applicant: Joseph P. Lyssikatos ,  Julie Marie Greschuk ,  Fredrik P. Marmsäter ,  Qian Zhao ,  D. David Hennings ,  Weidong Liu

Inventor： Joseph P. Lyssikatos ,  Julie Marie Greschuk ,  Fredrik P. Marmsäter ,  Qian Zhao ,  D. David Hennings ,  Weidong Liu

IPC: A01N43/54 ,  A61K31/517 ,  C07D239/72 ,  C07D401/00

CPC classification number: A61K31/337 ,  A61K31/513 ,  A61K31/517 ,  A61K39/3955 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D495/04 ,  C07D519/00

Abstract: This invention provides compounds of Formula I wherein B, G, A, E, R1, R2, R3, m and n are as defined herein, which are useful as type I receptor tyrosine kinase inhibitors, and methods of use thereof in the treatment of hyperproliferative disorders in mammals.

Abstract translation: 本发明提供式I化合物，其中B，G，A，E，R 1，R 2，R 3，m和n如本文所定义，其可用作I型受体酪氨酸激酶抑制剂，及其用于治疗 哺乳动物过度增生性疾病。

公开(公告)号：US20140005418A1

公开(公告)日：2014-01-02

申请号：US14013898

申请日：2013-08-29

Applicant: ARRAY BIOPHARMA INC.

Inventor： Laurence E. Burgess ,  Christopher T. Clark ,  Adam Cook ,  Christopher P. Corrette ,  Robert Kirk DeLisle ,  George A. Doherty ,  Kevin W. Hunt ,  Todd T. Romoff ,  Ganghyeok Kim

IPC: C07D311/58

CPC classification number: C07D311/58 ,  C07D311/04 ,  C07D405/12 ,  C07D407/12

Abstract: A compound having the formula: is useful in the preparation of compounds of Formula I.

Abstract translation: 具有下式的化合物可用于制备式I化合物。

公开(公告)号：US08557809B2

公开(公告)日：2013-10-15

申请号：US13059881

申请日：2009-08-18

Applicant: Shelley Allen ,  Robert Kirk DeLisle ,  Julie Marie Greschuk ,  Erik James Hicken ,  Joseph P. Lyssikatos ,  Fredrik P. Marmsater ,  Mark C. Munson ,  John E. Robinson ,  Qian Zhao

Inventor： Shelley Allen ,  Robert Kirk DeLisle ,  Julie Marie Greschuk ,  Erik James Hicken ,  Joseph P. Lyssikatos ,  Fredrik P. Marmsater ,  Mark C. Munson ,  John E. Robinson ,  Qian Zhao

IPC: A61K31/5377 ,  A61K31/496 ,  A61K31/4709 ,  C07D471/04 ,  A61P35/02 ,  A61P29/00

CPC classification number: C07D471/04

Abstract: Compounds of Formula (I): I in which B, R1, R1a, R2, R3, R4, R5, R6, R7, R10 and R11 have the meanings given in the specification, are receptor tyrosine inhibitors useful in the treatment of diseases mediated by PIM-1 and/or PIM-2 and/or PIM-3 kinases.

Abstract translation: 式（I）的化合物：其中B，R1，R1a，R2，R3，R4，R5，R6，R7，R10和R11具有本说明书中给出的含义的I是可用于治疗疾病介导的受体酪氨酸抑制剂 通过PIM-1和/或PIM-2和/或PIM-3激酶。

公开(公告)号：US08518983B2

公开(公告)日：2013-08-27

申请号：US12364330

申请日：2009-02-02

Applicant: Mark Munson ,  David A. Mareska ,  Youngboo Kim ,  Robert D. Gronenberg ,  James P. Rizzi ,  Martha Rodriguez ,  Ganghyeok Kim ,  Guy Vigers ,  Chang Rao ,  Devan Balachari ,  Darren Harvey

Inventor： Mark Munson ,  David A. Mareska ,  Youngboo Kim ,  Robert D. Gronenberg ,  James P. Rizzi ,  Martha Rodriguez ,  Ganghyeok Kim ,  Guy Vigers ,  Chang Rao ,  Devan Balachari ,  Darren Harvey

IPC: A61K31/415 ,  C07D231/56

CPC classification number: C07D401/14 ,  C07D231/56 ,  C07D261/20 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D471/04

Abstract: This invention relates to inhibitors of p38 and methods of utilizing the inhibitors and pharmaceutical compositions thereof in the treatment and prevention of various disorders mediated by p38.

Abstract translation: 本发明涉及p38的抑制剂和利用该抑制剂及其药物组合物治疗和预防由p38介导的各种疾病的方法。

公开(公告)号：US08513263B2

公开(公告)日：2013-08-20

申请号：US13125263

申请日：2009-10-21

Applicant: Julia Haas ,  Steven W. Andrews ,  Yutong Jiang ,  Gan Zhang

Inventor： Julia Haas ,  Steven W. Andrews ,  Yutong Jiang ,  Gan Zhang

IPC: A01N43/90 ,  A61K31/519 ,  C07D487/00

CPC classification number: C07D487/04 ,  A61K9/0053 ,  A61K31/519 ,  A61K31/5377 ,  A61K45/06 ,  A61P29/00 ,  C07D471/04 ,  C07D519/00

Abstract: Compounds of Formula (I) in which R1, R2, R3, R4, X, Y and n have the meanings given in the specification, are inhibitors of Trk kinases and are useful in the treatment of diseases which can be treated with a Trk kinase inhibitor.

Abstract translation: 其中R1，R2，R3，R4，X，Y和n具有本说明书中给出的含义的式（I）化合物是Trk激酶的抑制剂，可用于治疗可用Trk激酶治疗的疾病 抑制剂。

公开(公告)号：US08501956B2

公开(公告)日：2013-08-06

申请号：US13229491

申请日：2011-09-09

Applicant: John Demattei ,  Sagar Shakya ,  Anthony D. Piscopio ,  Bruno P. Hache ,  Matthew Charles Evans ,  James Gair Ford ,  Simon Mark Pointon ,  Koen Peeters ,  Timothy John Lilley ,  John Leonard

Inventor： John Demattei ,  Sagar Shakya ,  Anthony D. Piscopio ,  Bruno P. Hache ,  Matthew Charles Evans ,  James Gair Ford ,  Simon Mark Pointon ,  Koen Peeters ,  Timothy John Lilley ,  John Leonard

IPC: C07D235/06 ,  C07D235/08 ,  C07D403/04 ,  C07D403/06

CPC classification number: C07D235/06 ,  C07C201/08 ,  C07C205/58 ,  C07C227/04 ,  C07C227/08 ,  C07C227/18 ,  C07C229/60

Abstract: Provided are compounds having Formula VIIIa-1: wherein Z, X5, R2, R2a and R10 are as defined herein. Compounds of Formula VIIIa-1 can be used to prepare heterocyclic derivatives such as benzimidazole derivatives.

Abstract translation: 提供具有式VIIIa-1的化合物：其中Z，X5，R2，R2a和R10如本文所定义。 式VIIIa-1的化合物可用于制备杂环衍生物如苯并咪唑衍生物。

公开(公告)号：US08450322B2

公开(公告)日：2013-05-28

申请号：US13063894

申请日：2009-09-21

Applicant: Steven D. Andrews ,  Julia Haas ,  Yutong Jiang ,  Gan Zhang

Inventor： Steven D. Andrews ,  Julia Haas ,  Yutong Jiang ,  Gan Zhang

IPC: A01N43/58 ,  A01N43/60 ,  A61K31/495 ,  C07D487/00

CPC classification number: C07D487/04 ,  A61K31/5025 ,  A61K31/5377 ,  A61K31/541 ,  C07C51/412 ,  C07C53/18 ,  C07D471/04 ,  C07D519/00

Abstract: Compounds of Formula (I): in which R1, R2, R3, R4, X, Y and n have the meanings given in the specification, are inhibitors of Trk kinases and are useful in the treatment of diseases which can be treated with a Trk kinase inhibitor.

Abstract translation: 式（I）化合物：其中R1，R2，R3，R4，X，Y和n具有说​​明书中给出的含义，是Trk激酶的抑制剂，可用于治疗可用Trk 激酶抑制剂。