公开(公告)号：US20160304504A1

公开(公告)日：2016-10-20

申请号：US15101373

申请日：2014-11-25

Applicant: AMGEN INC.

Inventor： Mary CHAVES ,  Matthew BIO ,  Matthew PETERSON

IPC: C07D409/14 ,  C07C309/30 ,  C07C309/04

CPC classification number: C07D409/14 ,  C07B2200/13 ,  C07C309/04 ,  C07C309/30

Abstract: The present invention relates to crystalline forms and co-crystal forms of pharmaceutically acceptable salts of the compound, N-(4-((3-(2-amino-4-pyrimidinyl)-2-pyridinyl)oxy)phenyl)-4-(4-methyl-2-thienyl)-1-phthalazinamine (AMG 900, and pharmaceutical compositions comprising said crystalline and co-crystal forms thereof. The invention further provides uses of the crystalline forms and compositions, to treat cancer, including various types of solid tumors and hematologic cancer including myeloma and leukemia.

Abstract translation: 本发明涉及化合物N-（4 - （（3-（2-氨基-4-嘧啶基）-2-吡啶基）氧基）苯基）-4-甲基苯甲酸的药学上可接受的盐的结晶形式和共晶形式， （4-甲基-2-噻吩基）-1-酞嗪胺（AMG 900和包含其结晶和共晶形式的药物组合物）本发明还提供了结晶形式和组合物用于治疗癌症的用途，包括各种类型 实体肿瘤和血液癌，包括骨髓瘤和白血病。

公开(公告)号：US20160289243A1

公开(公告)日：2016-10-06

申请号：US15175805

申请日：2016-06-07

Applicant: AMGEN INC.

Inventor： Matthew BIO ,  Sebastien CAILLE ,  Yuanqing FANG ,  Brian M. FOX ,  Brian S. LUCAS ,  Lawrence R. McGEE ,  Sean H. WIEDEMANN

IPC: C07D498/04 ,  C07C309/35

CPC classification number: A61K31/451 ,  C07B2200/13 ,  C07C309/04 ,  C07C309/25 ,  C07C309/35 ,  C07C313/02 ,  C07D211/76 ,  C07D211/94 ,  C07D491/048 ,  C07D498/04

Abstract: The present invention provides processes for making 2-((3R,5R,6S)-5-(3-chlorophenyl)-6-(4-chlorophenyl)-1-((S)-1-(isopropylsulfonyl)-3-methylbutan-2-yl)-3-methyl-2-oxopiperidin-3-yl)acetic acid as well as intermediates and processes for making the intermediates. Also provided are crystalline forms of the compound and the intermediates.

公开(公告)号：US20140364455A1

公开(公告)日：2014-12-11

申请号：US14301087

申请日：2014-06-10

Applicant: AMGEN INC.

Inventor： Matthew BIO ,  Sebastien CAILLE ,  Brian COCHRAN ,  Yuanqing FANG ,  Brian M. FOX ,  Brian S. LUCAS ,  Lawrence R. McGEE ,  Filisaty VOUNATSOS ,  Sean WIEDEMANN ,  Sarah WORTMAN

IPC: C07D211/94 ,  C07C309/25 ,  C07C309/04 ,  C07D491/048

CPC classification number: A61K31/451 ,  C07B2200/13 ,  C07C309/04 ,  C07C309/25 ,  C07C309/35 ,  C07C313/02 ,  C07D211/76 ,  C07D211/94 ,  C07D491/048 ,  C07D498/04

Abstract: The present invention provides processes for making 2-((3R,5R,6S)-5-(3-chlorophenyl)-6-(4-chlorophenyl)-1-((S)-1-(isopropylsulfonyl)-3-methylbutan-2-yl)-3-methyl-2-oxopiperidin-3-yl)acetic acid as well as intermediates and processes for making the intermediates. Also provided are crystalline forms of the compound and the intermediates.

Abstract translation: 本发明提供了制备2 - （（3R，5R，6S）-5-（3-氯苯基）-6-（4-氯苯基）-1 - （（S）-1-（异丙基磺酰基）-3-甲基丁基 -2-基）-3-甲基-2-氧代哌啶-3-基）乙酸，以及制备中间体的中间体和方法。 还提供了化合物和中间体的晶型。