公开(公告)号：US20200308194A1

公开(公告)日：2020-10-01

申请号：US16902424

申请日：2020-06-16

申请人： Loxo Oncology, Inc. ,  Array BioPharma Inc.

发明人： Charles Todd EARY ,  Stacey SPENCER ,  Zack CRANE ,  Katelyn CHANDO ,  Sylvie ASSELIN ,  Weidong LIU ,  Mike WELCH ,  Adam COOK ,  Gabrielle R. KOLAKOWSKI ,  Andrew T. METCALF ,  David A. MORENO ,  Tony P. TANG

IPC分类号： C07D519/00 ,  C07D471/04

摘要： In some embodiments, provided herein is a process for preparing a compound of Formula I or a pharmaceutically acceptable salt thereof, as disclosed herein.

公开(公告)号：US20210380609A1

公开(公告)日：2021-12-09

申请号：US17401892

申请日：2021-08-13

申请人： Loxo Oncology, Inc. ,  Array BioPharma Inc.

发明人： Charles Todd EARY ,  Stacey SPENCER ,  Zack CRANE ,  Katelyn CHANDO ,  Sylvie ASSELIN ,  Weidong LIU ,  Mike WELCH ,  Adam COOK ,  Gabrielle R. KOLAKOWSKI ,  Andrew T. METCALF ,  David A. MORENO ,  Tony P. TANG

IPC分类号： C07D519/00 ,  C07D471/04

摘要： In some embodiments, provided herein is a process for preparing a compound of Formula I or a pharmaceutically acceptable salt thereof, as disclosed herein.

公开(公告)号：US20240238253A1

公开(公告)日：2024-07-18

申请号：US18440563

申请日：2024-02-13

申请人： Loxo Oncology, Inc.

发明人： Barbara J. BRANDHUBER ,  Lauren T. BRENT ,  Charles Todd EARY ,  Andrew KENNA ,  Firas KHAN ,  Vivian F.H. RENSHAW ,  Stacey Renee SPENCER

IPC分类号： A61K31/415 ,  A61K9/00 ,  A61K9/20 ,  A61K31/635 ,  A61P35/04 ,  C07K16/28

CPC分类号： A61K31/415 ,  A61K9/0053 ,  A61K9/2009 ,  A61K9/2018 ,  A61K9/2054 ,  A61K9/2059 ,  A61K31/635 ,  A61P35/04 ,  C07K16/2887 ,  C07B2200/13

摘要： A spray-dried dispersions and pharmaceutical composition of (S)-5-amino-3-(4-((5-fluoro-2-methoxybenzamido)methyl)phenyl)-1-(1,1,1-trifluoropropan-2-yl)-1H-pyrazole-4-carboxamide, pharmaceutically acceptable salts thereof, or a combination thereof and the use of the spray-dried dispersion and pharmaceutical composition in the treatment of cancer and autoimmune and inflammatory diseases are disclosed. Also provided are crystalline forms of (S)-5-amino-3-(4-((5-fluoro-2-methoxybenzamido)methyl)phenyl)-1-(1,1,1-trifluoropropan-2-yl)-1H-pyrazole-4-carboxamide also useful in the treatment of cancer and autoimmune and inflammatory diseases.

公开(公告)号：US20230322682A1

公开(公告)日：2023-10-12

申请号：US18043971

申请日：2021-09-09

申请人： LOXO ONCOLOGY, INC.

发明人： Alonso Jose ARGUELLES DELGADO ,  Charles Todd EARY ,  Jared Wade FENNELL ,  Scott Alan FRANK ,  Nicholas Andrew MAGNUS ,  Elizabeth Ann MCFADDIN ,  Roger Ryan ROTHHAAR ,  Stacey Renee SPENCER ,  Radhe Krishan VAID

IPC分类号： C07D231/38 ,  C07F5/04 ,  C07F5/02

CPC分类号： C07D231/38 ,  C07F5/04 ,  C07F5/022

摘要： The present invention provides processes and key intermediates for the synthesis of (S)-5-amino-3-(4-((5-fluoro-2-methoxybenzamido)methyl)phenyl)-1-(1,1,1-trifluoro-propane-2-yl)-1H-pyrazole-4-carboxamide:

公开(公告)号：US20220202788A1

公开(公告)日：2022-06-30

申请号：US17581219

申请日：2022-01-21

申请人： Loxo Oncology, Inc.

发明人： Mark REYNOLDS ,  Charles Todd EARY

IPC分类号： A61K31/439 ,  A61P35/00 ,  A61K47/10 ,  A61K9/16 ,  A61K31/498 ,  A61K47/26 ,  A61K9/08 ,  A61K9/20 ,  A61K47/12 ,  A61K9/00 ,  A61K47/02 ,  A61K47/38 ,  A61K9/48

摘要： 6-(2-hydroxy-2-methylpropoxy)-4-(6-(6-((6-methoxypyridin-3-yl)methyl)-3,6-diazabicyclo[3.1.1]heptan-3-yl)pyridin-3-yl)pyrazolo[1,5-a]pyridine-3-carbonitrile, or a pharmaceutically acceptable salt, amorphous form, polymorph form, or pharmaceutical composition (including solid formulations or liquid formulations) thereof and the use thereof for treating diseases and disorders which can be treated with a RET kinase inhibitor, such as RET-associated diseases and disorders, e.g., proliferative disorders such as cancers, including hematological cancers and solid tumors, and gastrointestinal disorders such as IBS are disclosed.

公开(公告)号：US20220087988A1

公开(公告)日：2022-03-24

申请号：US17530019

申请日：2021-11-18

申请人： Loxo Oncology, Inc.

发明人： Mark REYNOLDS ,  Charles Todd EARY

IPC分类号： A61K31/439 ,  A61P35/00 ,  A61K9/00 ,  A61K9/16 ,  A61K9/48 ,  A61K47/02 ,  A61K47/10 ,  A61K47/12 ,  A61K47/26 ,  A61K47/38 ,  A61K9/20 ,  A61K31/498 ,  A61K9/08

摘要： 6-(2-hydroxy-2-methylpropoxy)-4-(6-(6-((6-methoxypyridin-3-yl)methyl)-3,6-diazabicyclo[3.1.1]heptan-3-yl)pyridin-3-yl)pyrazolo[1,5-a]pyridine-3-carbonitrile, or a pharmaceutically acceptable salt, amorphous form, polymorph form, or pharmaceutical composition (including solid formulations or liquid formulations) thereof and the use thereof for treating diseases and disorders which can be treated with a RET kinase inhibitor, such as RET-associated diseases and disorders, e.g., proliferative disorders such as cancers, including hematological cancers and solid tumors, and gastrointestinal disorders such as IBS are disclosed.

公开(公告)号：US20210077474A1

公开(公告)日：2021-03-18

申请号：US17001793

申请日：2020-08-25

申请人： Loxo Oncology, Inc.

发明人： Mark REYNOLDS ,  Charles Todd EARY

IPC分类号： A61K31/439 ,  A61P35/00 ,  A61K9/00 ,  A61K9/16 ,  A61K9/48 ,  A61K47/02 ,  A61K47/10 ,  A61K47/12 ,  A61K47/26 ,  A61K47/38 ,  A61K9/20 ,  A61K31/498 ,  A61K9/08

摘要： 6-(2-hydroxy-2-methylpropoxy)-4-(6-(6-((6-methoxypyridin-3-yl)methyl)-3,6-diazabicyclo[3.1.1]heptan-3-yl)pyridin-3-yl)pyrazolo[1,5-a]pyridine-3-carbonitrile, or a pharmaceutically acceptable salt, amorphous form, polymorph form, or pharmaceutical composition (including solid formulations or liquid formulations) thereof and the use thereof for treating diseases and disorders which can be treated with a RET kinase inhibitor, such as RET-associated diseases and disorders, e.g., proliferative disorders such as cancers, including hematological cancers and solid tumors, and gastrointestinal disorders such as IBS are disclosed.