公开(公告)号：US08889704B2

公开(公告)日：2014-11-18

申请号：US14001657

申请日：2012-02-24

Applicant: James F. Blake ,  Robert Kirk Delisle ,  Lisa A. De Meese ,  James M. Graham ,  Yvan Le Huerou ,  Michael Lyon ,  John E. Robinson ,  Eli M. Wallace ,  Bin Wang ,  Rui Xu

Inventor： James F. Blake ,  Robert Kirk Delisle ,  Lisa A. De Meese ,  James M. Graham ,  Yvan Le Huerou ,  Michael Lyon ,  John E. Robinson ,  Eli M. Wallace ,  Bin Wang ,  Rui Xu

IPC: C07D471/04 ,  C07D487/04 ,  C07D487/10 ,  C07D491/048 ,  C07D401/06 ,  C07D519/00

CPC classification number: C07D471/04 ,  C07D401/06 ,  C07D487/04 ,  C07D487/10 ,  C07D491/048 ,  C07D519/00

Abstract: Compounds of Formula I: in which R1, R2, R3, R4 and R10 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: R 1，R 2，R 3，R 4和R 10具有本说明书中给出的含义的式I化合物是可用于治疗由PIM-1和/或PIM-2和/或PIM-2介导的疾病的受体酪氨酸抑制剂， 3激酶。

公开(公告)号：US08853409B2

公开(公告)日：2014-10-07

申请号：US13493616

申请日：2012-06-11

Applicant: Thomas Daniel Aicher ,  Steven Armen Boyd ,  Mark Joseph Chicarelli ,  Kevin Ronald Condroski ,  Jay Bradford Fell ,  John P. Fischer ,  Indrani W. Gunawardana ,  Ronald Jay Hinklin ,  Ajay Singh ,  Timothy M. Turner ,  Eli M. Wallace

Inventor： Thomas Daniel Aicher ,  Steven Armen Boyd ,  Mark Joseph Chicarelli ,  Kevin Ronald Condroski ,  Jay Bradford Fell ,  John P. Fischer ,  Indrani W. Gunawardana ,  Ronald Jay Hinklin ,  Ajay Singh ,  Timothy M. Turner ,  Eli M. Wallace

IPC: A61K31/44 ,  C07D417/00 ,  C07D417/14 ,  C07D417/12 ,  C07D213/75

CPC classification number: C07D401/14 ,  C07D213/75 ,  C07D401/12 ,  C07D417/12 ,  C07D417/14

Abstract: Provided are compounds of Formula (I): wherein R2, R3, R13, L and D2 are as defined in the specification, which are useful in the treatment and/or prevention of diseases or disorders mediated by deficient levels of glucokinase activity or which can be treated by activating glucokinase including, but not limited to, diabetes mellitus, impaired glucose tolerance, IFG (impaired fasting glucose) and IFG (impaired fasting glycemia), as well as other diseases and disorders such as those discussed herein.

Abstract translation: 提供式（I）的化合物：其中R2，R3，R13，L和D2如说明书中所定义，其可用于治疗和/或预防由缺乏葡萄糖激酶水平的活性介导的疾病或病症，或可以 通过激活葡糖激酶，包括但不限于糖尿病，葡萄糖耐量降低，IFG（空腹血糖受损）和IFG（空腹血糖受损））以及其它疾病和病症如本文讨论的疾病和病症。

公开(公告)号：US08853199B2

公开(公告)日：2014-10-07

申请号：US13272079

申请日：2011-10-12

Applicant: Ian S. Mitchell ,  James F. Blake ,  Rui Xu ,  Nicholas C. Kallan ,  Dengming Xiao ,  Keith Lee Spencer ,  Josef R. Bencsik ,  Eli M. Wallace ,  Stephen T. Schlachter ,  Anna L. Banka ,  Jun Liang ,  Brian Safina ,  Birong Zhang ,  Christine Chabot ,  Steven Do

Inventor： Ian S. Mitchell ,  James F. Blake ,  Rui Xu ,  Nicholas C. Kallan ,  Dengming Xiao ,  Keith Lee Spencer ,  Josef R. Bencsik ,  Eli M. Wallace ,  Stephen T. Schlachter ,  Anna L. Banka ,  Jun Liang ,  Brian Safina ,  Birong Zhang ,  Christine Chabot ,  Steven Do

IPC: C07D409/12 ,  C07D409/14 ,  C07D403/12 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12 ,  A61K31/496 ,  A61P35/00 ,  A61P29/00 ,  A61P25/28 ,  C07D239/70

CPC classification number: A61K31/517 ,  C07D239/70 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D407/12 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12

Abstract: The present invention provides compounds, including resolved enantiomers, resolved diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula I: 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: 本发明提供了包含分解的对映异构体，分解的非对映异构体，溶剂合物和其药学上可接受的盐的化合物，其包含式I：还提供了使用本发明化合物作为AKT蛋白激酶抑制剂和用于治疗过度增殖性疾病 癌症。

公开(公告)号：US20140234376A1

公开(公告)日：2014-08-21

申请号：US14180939

申请日：2014-02-14

Applicant: Array BioPharma, Inc. ,  VentiRx Pharmaceuticals, Inc.

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

IPC: C07D223/16 ,  C07D405/04 ,  C07D401/04 ,  C07D405/10 ,  C07D401/12 ,  C07D403/10

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：US08758830B2

公开(公告)日：2014-06-24

申请号：US13974895

申请日：2013-08-23

Applicant: Array BioPharma Inc.

Inventor： Yvan Le Huerou ,  James F. Blake ,  Indrani W. Gunawardana ,  Peter J. Mohr ,  Eli M. Wallace ,  Bin Wang ,  Mark Joseph Chicarelli ,  Michael Lyon

IPC: A61K31/4545 ,  A61K31/437 ,  A61K31/497 ,  A61K31/506 ,  A61K31/513 ,  A61K31/444 ,  A61K31/501 ,  A61K35/00 ,  A61K33/24

CPC classification number: C07D471/04 ,  C07D401/06 ,  C07D519/00

Abstract: Compounds of Formula I are useful for inhibition of CHK1 and/or CHK2. Methods of using compounds of Formula I and stereoisomers and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.

Abstract translation: 式I的化合物可用于抑制CHK1和/或CHK2。 公开了使用式I化合物及其立体异构体及其药学上可接受的盐在体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种病症的方法。

公开(公告)号：US20140100369A1

公开(公告)日：2014-04-10

申请号：US13974895

申请日：2013-08-23

Applicant: Array BioPharma Inc.

Inventor： Yvan Le Huerou ,  James F. Blake ,  Indrani W. Gunawardana ,  Peter J. Mohr ,  Eli M. Wallace ,  Bin Wang ,  Mark Joseph Chicarelli ,  Michael Lyon

IPC: C07D471/04

CPC classification number: C07D471/04 ,  C07D401/06 ,  C07D519/00

Abstract: Compounds of Formula I are useful for inhibition of CHK1 and/or CHK2. Methods of using compounds of Formula I and stereoisomers and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.

公开(公告)号：US08618097B2

公开(公告)日：2013-12-31

申请号：US12667848

申请日：2008-07-03

Applicant: Josef Bencsik ,  James F. Blake ,  James M. Graham ,  Martin F. Hentemann ,  Nicholas C. Kallan ,  Ian S. Mitchell ,  Stephen T. Schlachter ,  Keith L. Spencer ,  Dengming Xiao ,  Rui Xu ,  Mike Welch ,  Jun Liang ,  Brian S. Safina

Inventor： Josef Bencsik ,  James F. Blake ,  James M. Graham ,  Martin F. Hentemann ,  Nicholas C. Kallan ,  Ian S. Mitchell ,  Stephen T. Schlachter ,  Keith L. Spencer ,  Dengming Xiao ,  Rui Xu ,  Mike Welch ,  Jun Liang ,  Brian S. Safina

IPC: A61K31/5377 ,  A61K31/496 ,  C07D413/14 ,  C07D239/70 ,  A61P25/28 ,  A61P35/00 ,  A61P29/00 ,  A61P9/00

CPC classification number: C07D403/12 ,  C07D401/12

Abstract: The present invention provides compounds of Formula (I), including tautomers, resolved enantiomers, diastereomers, solvates, metabolites, salts and pharmaceutically acceptable prodrugs thereof. 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: 本发明提供式（I）化合物，其包括互变异构体，拆分的对映异构体，非对映异构体，溶剂合物，代谢物，盐和药学上可接受的前药。 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：US20130252934A1

公开(公告)日：2013-09-26

申请号：US13782513

申请日：2013-03-01

Applicant: ARRAY BIOPHARMA INC. ,  GENENTECH, INC.

Inventor： James F. Blake ,  Mark Joseph Chicarelli ,  Rustam Ferdinand Garrey ,  John Gaudino ,  Jonas Grina ,  David A. Moreno ,  Peter J. Mohr ,  Li Ren ,  Jacob Schwarz ,  Huifen Chen ,  Kirk Robarge ,  Aihe Zhou

IPC: A61K31/506 ,  C07D401/04 ,  A61K45/06 ,  C07D413/14 ,  C07D409/14 ,  C07D417/14 ,  C07D405/14 ,  C07D401/14

CPC classification number: C07D401/04 ,  A61K31/444 ,  A61K31/506 ,  A61K31/513 ,  A61K31/53 ,  A61K45/06 ,  C07D401/14 ,  C07D403/04 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07F9/65586

Abstract: Compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of hyperproliferative, pain and inflammatory diseases. Methods of using compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.

Abstract translation: 提供式I化合物或其立体异构体，互变异构体，前药或其药学上可接受的盐，其可用于治疗过度增生，疼痛和炎性疾病。 公开了使用式I化合物或其立体异构体，互变异构体，前药或其药学上可接受的盐在体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种病症的方法。

公开(公告)号：US08513293B2

公开(公告)日：2013-08-20

申请号：US13463487

申请日：2012-05-03

Applicant: Eli M. Wallace ,  Joseph P. Lyssikatos ,  Allison L. Marlow ,  T. Brian Hurley

Inventor： Eli M. Wallace ,  Joseph P. Lyssikatos ,  Allison L. Marlow ,  T. Brian Hurley

IPC: A61K31/4184 ,  C07D235/06

CPC classification number: C07D235/06 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D405/06 ,  C07D413/04 ,  C07D413/06 ,  C07D417/06 ,  C07D417/12

Abstract: Disclosed are methods for inhibiting abnormal cell growth or treating hyperproliferative diseases in mammals, comprising administering to a mammal in heed thereof a pharmaceutical composition comprising 6-(4-bromo-2-fluorophenylamino)-7-fluoro-3-methyl-3H-benzoimidazole-5-carboxylic acid (2-hydroxy-ethoxy)-amide, or a pharmaceutically acceptable salt thereof, in combination with an effective amount of an anti-tumor agent or in combination with radiation therapy.

Abstract translation: 公开了抑制哺乳动物异常细胞生长或治疗过度增殖性疾病的方法，包括向哺乳动物施用包含6-（4-溴-2-氟苯基氨基）-7-氟-3-甲基-3H-苯并咪唑的药物组合物 -5-羧酸（2-羟基 - 乙氧基） - 酰胺或其药学上可接受的盐与有效量的抗肿瘤剂组合或与放射治疗组合。

公开(公告)号：US08492437B2

公开(公告)日：2013-07-23

申请号：US13448689

申请日：2012-04-17

Applicant: George A. Doherty ,  Adam Cook

Inventor： George A. Doherty ,  Adam Cook

IPC: C07D211/22 ,  C07D211/84 ,  C07D333/22 ,  C07D233/00 ,  C07C229/00 ,  A01N37/12 ,  A01N37/44

CPC classification number: C07C311/19 ,  C07C233/75 ,  C07C233/87 ,  C07C235/46 ,  C07C255/57 ,  C07C271/22 ,  C07C307/06 ,  C07C311/06 ,  C07C317/46 ,  C07C2601/02 ,  C07C2601/14 ,  C07C2602/10 ,  C07D213/71 ,  C07D213/81 ,  C07D213/82 ,  C07D233/42 ,  C07D333/16 ,  Y02P20/55

Abstract: Compounds of formula (I): in which R1, R2, R7, R8, R9, R10 and A have the meanings given in the specification, are DP2 receptor modulators useful in the treatment of immunologic diseases.

Abstract translation: 其中R1，R2，R7，R8，R9，R10和A具有本说明书中给出的含义的式（I）化合物是可用于治疗免疫疾病的DP2受体调节剂。