公开(公告)号：US20140256756A1

公开(公告)日：2014-09-11

申请号：US14355804

申请日：2012-10-30

Applicant: Array BioPharma Inc.

Inventor： Thomas Daniel Aicher ,  Josef Roland Benscik ,  Steven Armen Boyd ,  Kevin Ronald Condroski ,  Jay Bradford Fell ,  John Peter Fischer ,  Ronald Jay Hinklin ,  Scott Pratt ,  Ajay Singh ,  Timothy M. Turner

IPC: C07D417/14 ,  C07D413/14

CPC classification number: C07D417/14 ,  C07D413/14

Abstract: Compounds of Formula (I) and pharmaceutically acceptable salts thereof in which X1, X2, X3, L, R3, R4, R5, R7 and n have the meanings given in the specification, are modulators of GPR119 and are useful in the treatment or prevention of diseases such as, but not limited to, type 2 diabetes, diabetic complications, symptoms of diabetes, metabolic syndrome, obesity, dyslipidemia, and related conditions.

Abstract translation: 其中X1，X2，X3，L，R3，R4，R5，R7和n具有本说明书中给出的含义的式（I）化合物及其药学上可接受的盐是GPR119的调节剂，可用于治疗或预防 的疾病，例如但不限于2型糖尿病，糖尿病并发症，糖尿病症状，代谢综合征，肥胖症，血脂异常和相关病症。

公开(公告)号：US20140249127A1

公开(公告)日：2014-09-04

申请号：US14181418

申请日：2014-02-14

Applicant: Genentech, Inc. ,  Array BioPharma 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: C07D417/14 ,  C07D409/14 ,  C07D401/14 ,  C07D413/14 ,  C07D405/14 ,  C07D401/04

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：US20140243361A1

公开(公告)日：2014-08-28

申请号：US14351835

申请日：2012-10-12

Applicant: Array BioPharma Inc.

Inventor： Donald T. Corson ,  Christopher M. Lindemann ,  Daniel J. Watson

IPC: A61K31/517 ,  A61K45/06 ,  C07D471/04

CPC classification number: A61K31/517 ,  A61K31/437 ,  A61K45/06 ,  A61P35/00 ,  C07D471/04

Abstract: Polymorphs of N4-(4-([1,2,4]triazolo[1,5-a]pyridin-7-yloxy)-3-methylphenyl)-N6-(4,4-dimethyl-4,5-dihydrooxazol-2-yl)quinazoline-4,6-diamine are provided herein. Processes for preparing the polymorphs and pharmaceutical composition comprising the polymorphs are also disclosed.

Abstract translation: N 4 - （4 - （[1,2,4]三唑并[1,5-a]吡啶-7-基氧基）-3-甲基苯基）-N6-（4,4-二甲基-4,5-二氢恶唑-2-基） 吡啶-2-基）喹唑啉-4,6-二胺。 还公开了制备多晶型物的方法和包含多晶型物的药物组合物。

公开(公告)号：US08716498B2

公开(公告)日：2014-05-06

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：US08697715B2

公开(公告)日：2014-04-15

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: A01N43/54 ,  A61K31/505

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：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：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。