公开(公告)号：US09278936B2

公开(公告)日：2016-03-08

申请号：US14382178

申请日：2013-02-27

Applicant: Array BioPharma Inc.

Inventor： Alisha B. Arrigo ,  Donald T. Corson ,  Coralee G. Mannila

IPC: C07D231/56 ,  A61K31/4155

CPC classification number: C07D231/56 ,  A61K31/4155 ,  Y02A50/411 ,  Y02A50/463

Abstract: Provided herein is a hydrogen chloride salt of 1-(3-/t?r/-butyl-1-p-tolyl-1H-pyrazol-5-yl)-3-(5-fluoro-2-(1-(2-hydroxyethyl)-1H-indazol-5-yloxy)benzyl)urea, crystalline forms of 1-(3-½^butyl-1^-tolyl-1H-pyrazol-5-yl)-3-(5-fluoro-2-(1-(2-hydroxyethyl)-1H-indazol-5-yloxy)benzyl)urea hydrochloride, processes for the preparation of said crystalline forms, pharmaceutical compositions containing a crystalline form of 1-(3-r

Abstract translation: 本文提供的是1-（3-叔丁基-1-叔丁基-1-对甲苯基-1H-吡唑-5-基）-3-（5-氟-2-（1-（2 - 羟基乙基）-1H-吲唑-5-基氧基）苄基）脲，1-（3 - 1/2丁基-1'-甲苯基-1H-吡唑-5-基）-3-（5-氟-2 - （1-（2-羟乙基）-1H-吲唑-5-基氧基）苄基）脲盐酸盐，制备所述结晶形式的方法，含有1-（3-r 丁基-1-对甲苯基-1H-吡唑-5-基）-3-（5-氟-2-（1-（2-羟乙基）-1H-吲唑-5-基氧基）苄基）脲盐酸盐形式B ，所述组合物的制备方法，通过所述方法制备的药物组合物，以及所述组合物在治疗各种疾病和病症中的用途。

公开(公告)号：US09242964B2

公开(公告)日：2016-01-26

申请号：US14016951

申请日：2013-09-03

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

Inventor： James Jeffry Howbert ,  Gregory Dietsch ,  Robert M. Hershberg ,  Laurence E. Burgess ,  George A. Doherty ,  C. Todd Eary ,  Robert D. Groneberg ,  Zachary Jones

IPC: A61K31/55 ,  C07D223/16 ,  C07D403/14 ,  A61K31/4025 ,  C07D401/04 ,  C07D403/04 ,  C07D403/10 ,  C07D401/14

CPC classification number: C07D223/16 ,  A61K31/4025 ,  A61K31/55 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/10 ,  C07D403/14

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.

公开(公告)号：US09238627B2

公开(公告)日：2016-01-19

申请号：US14057498

申请日：2013-10-18

Applicant: Novartis AG ,  Array BioPharma, Inc.

Inventor： Christoph Max Krell ,  Marian Misun ,  Daniel Andreas Niederer ,  Werner Heinz Pachinger ,  Marie-Christine Wolf ,  Daniel Zimmermann ,  Weidong Liu ,  Peter J. Stengel ,  Paul Nichols

IPC: C07D235/06 ,  A61K47/26 ,  A61K47/38 ,  A61K9/20

CPC classification number: A61K31/4184 ,  A61K9/0053 ,  A61K9/2009 ,  A61K9/2013 ,  A61K9/2018 ,  A61K9/2054 ,  A61K45/06 ,  A61K47/02 ,  A61K47/12 ,  A61K47/26 ,  A61K47/38 ,  C07B2200/13 ,  C07D235/06 ,  C07D235/08 ,  C30B7/08 ,  C30B29/54

Abstract: The present invention relates to processes for preparing 6-(4-bromo-2-fluorophenylamino)-7-fluoro-3-methyl-3H-benzoimidazole-5-carboxylic acid (2-hydroxyethyoxy)-amide, processes for preparing crystallized 6-(4-bromo-2-fluorophenylamino)-7-fluoro-3-methyl-3H-benzoimidazole-5-carboxylic acid (2-hydroxyethyoxy)-amide, and intermediates useful therefore. Also provided herein are pharmaceutical compositions comprising this crystallized compound.

Abstract translation: 本发明涉及制备6-（4-溴-2-氟苯基氨基）-7-氟-3-甲基-3H-苯并咪唑-5-甲酸（2-羟基乙氧基） - 酰胺的方法， （4-溴-2-氟苯基氨基）-7-氟-3-甲基-3H-苯并咪唑-5-甲酸（2-羟基乙氧基） - 酰胺，以及有用的中间体。 本文还提供包含该结晶化合物的药物组合物。

公开(公告)号：US20150232442A1

公开(公告)日：2015-08-20

申请号：US14702947

申请日：2015-05-04

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 ,  C07D407/12 ,  C07D405/12

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

Abstract: Provided herein are compounds of Formula I: in which A1, A2, W, L, G, R7a, R7b, R8, R9 and R10 have the meanings given in the specification, which are DP2 receptor modulators useful in the treatment of immunologic diseases.

Abstract translation: 本文提供了式I的化合物：其中A1，A2，W，L，G，R7a，R7b，R8，R9和R10具有本说明书中给出的含义，其是可用于治疗免疫疾病的DP2受体调节剂。

公开(公告)号：US09024040B2

公开(公告)日：2015-05-05

申请号：US13614941

申请日：2012-09-13

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: C07D235/00 ,  C07D403/02 ,  C07D235/18 ,  C07D235/06 ,  C07C205/58 ,  C07C229/60 ,  C07C201/08 ,  C07C227/04 ,  C07C227/08 ,  C07C227/18

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

Abstract: Provided are processes for the preparation of benzimidazole structures having Formula VIIIb-1: and salts and solvates thereof, wherein Z, X5, R2b, R2c and R10 are as defined herein. Compounds of Formula VIIIb-1 are useful for the preparation of benzimidazole derivatives.

Abstract translation: 提供制备具有式VIIIb-1的苯并咪唑结构的方法及其盐和溶剂化物，其中Z，X5，R2b，R2c和R10如本文所定义。 式VIIIb-1的化合物可用于制备苯并咪唑衍生物。

公开(公告)号：US08987251B2

公开(公告)日：2015-03-24

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: A61K31/437 ,  C07D471/04 ,  C07D451/06 ,  C07D519/00

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：US08883828B2

公开(公告)日：2014-11-11

申请号：US13669083

申请日：2012-11-05

Applicant: Array BioPharma Inc.

Inventor： Thomas Daniel Aicher ,  Steven Armen Boyd ,  Mark Joseph Chicarelli ,  Kevin Ronald Condroski ,  Ronald Jay Hinklin ,  Ajay Singh

IPC: A01N43/40 ,  C07D417/00 ,  C07D417/14 ,  C07D491/04 ,  C07D487/04 ,  C07D513/04 ,  C07D417/12 ,  C07D471/04 ,  C07D413/14 ,  C07D495/04

CPC classification number: C07D417/12 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D495/04 ,  C07D513/04

Abstract: Provided are compounds that are useful in the treatment and/or prevention of diseases mediated by deficient levels of glucokinase activity, such as diabetes mellitus. Also provided are methods of treating or preventing diseases and disorders characterized by underactivity of glucokinase or which can be treated by activating glucokinase.

Abstract translation: 提供了可用于治疗和/或预防由缺乏水平的葡糖激酶活性（例如糖尿病）介导的疾病的化合物。 还提供了治疗或预防以葡萄糖激酶不足活性为特征的疾病和病症的方法，或者可以通过激活葡糖激酶治疗。

公开(公告)号：US08846683B2

公开(公告)日：2014-09-30

申请号：US13753008

申请日：2013-01-29

Applicant: Array BioPharma Inc. ,  Genentech, Inc.

Inventor： Josef R. Bencsik ,  James F. Blake ,  Nicholas C. Kallan ,  Ian S. Mitchell ,  Keith L. Spencer ,  Dengming Xiao ,  Rui Xu ,  Christine Chabot ,  Jun Liang ,  Brian S. Safina

IPC: A61P35/00

CPC classification number: C07D239/70 ,  A61K31/506 ,  C07D401/12 ,  C07D403/12 ,  C07D409/12

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: 本发明提供了式I化合物，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：US08841304B2

公开(公告)日：2014-09-23

申请号：US12812447

申请日：2009-01-08

Applicant: James F. Blake ,  Indrani W. Gunawardana ,  Yvan Le Huerou ,  Peter J. Mohr ,  Eli M. Wallace ,  Bin Wang

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

IPC: C07D471/04 ,  A61K31/496

CPC classification number: C07D471/04

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：US08785445B2

公开(公告)日：2014-07-22

申请号：US13141675

申请日：2009-12-18

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

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

IPC: C07D405/12 ,  A61K31/4433 ,  C07D241/20 ,  A61K31/497 ,  A61K31/501 ,  A61P11/06 ,  A61P27/14 ,  A61P17/00 ,  A61P29/00

CPC classification number: C07D405/12 ,  C07D405/14 ,  C07D413/12 ,  C07D417/12

Abstract: Compounds of Formula I: (I) in which A, A1, R1, R7a, R7b, R8 and R10 have the meanings given in the specification, are DP2 receptor inhibitors useful in the treatment of useful in the treatment and prevention of immunologic diseases, allergic diseases such as asthma, allergic rhinitis and atopic dermatitis, and other inflammatory diseases mediated by prostaglandin D2 (PGD2). The compounds of Formula I may also be useful in treating diseases or medical conditions involving the Th2 T cell via production of IL-4, IL-5 and/or IL-13.

Abstract translation: 其中A，A1，R1，R7a，R7b，R8和R10具有本说明书中给出的含义的式I化合物：（I）是可用于治疗和预防免疫疾病的DP2受体抑制剂， 过敏性疾病如哮喘，过敏性鼻炎和特应性皮炎，以及由前列腺素D2（PGD2）介导的其他炎性疾病。 式I化合物还可用于通过产生IL-4，IL-5和/或IL-13来治疗涉及Th2T细胞的疾病或医学病症。