公开(公告)号：US20240058338A1

公开(公告)日：2024-02-22

申请号：US18450638

申请日：2023-08-16

申请人： DAY ONE BIOPHARMACEUTICALS, INC.

发明人： Samuel C. BLACKMAN ,  Eleni VENETSANAKOS

IPC分类号： A61K31/506 ,  A61K31/44 ,  A61P35/00

CPC分类号： A61K31/506 ,  A61K31/44 ,  A61P35/00

摘要： Described herein are methods and compositions for treating subjects suffering from cancer. In some aspects, herein is described a method of treating a patient suffering from cancer comprising administering to the subject: (i) (R)-2-(1-(6-amino-5-chloropyrimidine-4-carboxamido)ethyl)-N-(5-chloro-4-(trifluoromethyppyridin-2-yl)thiazole-5-carboxamide (Compound A) or a pharmaceutically acceptable salt thereof; and (ii) a MEK inhibitor as provided herein. In some aspects, the method of treating a subject suffering from cancer comprises: identifying a subject suffering from cancer, wherein the cancer has one or more of: a RAF alteration, a RAS mutation, an NF-1 mutation, or a genomic alteration that results in a dependence on signaling through the MAPK pathway; administering to a subject: (i) (R)-2-(1-(6-amino-5-chloropyrimidine-4-carboxamido)ethyl)-N-(5-chloro-4-(trifluoromethyppyridin-2-yl)thiazole-5-carboxamide (Compound A) or a pharmaceutically acceptable salt thereof; and (ii) a MEK inhibitor as provided herein.

公开(公告)号：US12129249B2

公开(公告)日：2024-10-29

申请号：US17180127

申请日：2021-02-19

申请人： DAY ONE BIOPHARMACEUTICALS, INC.

发明人： Sayuri Hirano ,  Yoshiyuki Takeda ,  Koji Nakamoto ,  Motoki Ikeuchi ,  Masato Kitayama ,  Masatoshi Yamada ,  Jun-ichi Kawakami

IPC分类号： C07D417/12 ,  C07D417/14

CPC分类号： C07D417/14 ,  C07D417/12

摘要： The aim of the present invention is to provide a method capable of producing an optically active pyrimidinamide derivative on an industrial scale.
Compound (I) or a salt thereof is subjected to an asymmetric reduction reaction, the obtained compound (II) or a salt thereof is subjected to a deprotection reaction, and the obtained compound (III) or a salt thereof is reacted with compound (VI) or a salt thereof to obtain compound (V) or a salt thereof.






wherein each symbol is as defined in the specification.

公开(公告)号：US20230355618A1

公开(公告)日：2023-11-09

申请号：US18035478

申请日：2021-11-05

申请人： Day One Biopharmaceuticals, Inc. ,  The Brigham and Women's Hospital, Inc. ,  Dana-Farber Cancer Institute Inc.

发明人： Karen D. WRIGHT ,  Daphne Adele HAAS-KOGAN ,  Samuel c. BLACKMAN

IPC分类号： A61K31/506 ,  A61K45/06 ,  A61P35/00

CPC分类号： A61K31/506 ,  A61K45/06 ,  A61P35/00

摘要： Described herein are methods and compositions for treating gliomas such as pediatric low grade glioma. In some embodiments, a herein described method of treating pediatric low grade glioma comprises administering to a subject in need thereof (R)-2-(1-(6-amino-5-chloropyrimidine-4-carboxamido)ethyl)-N-(5-chloro-4-(trifluoromethyl)pyridin-2-yl)thiazole-5-carboxamide (Compound A), or a pharmaceutically acceptable salt thereof. In some embodiments, Compound A or a pharmaceutically acceptable salt thereof is administered in an amount that is equivalent to about 400 mg/m2 to about 600 mg/m2 of Compound A per week. In some embodiments, the subject is less than 20 years of age.

公开(公告)号：US20240041765A1

公开(公告)日：2024-02-08

申请号：US18332906

申请日：2023-06-12

申请人： DAY ONE BIOPHARMACEUTICALS, INC.

发明人： Donald T. CORSON ,  Michael PREIGH ,  Dan SMITHEY ,  Randy WALD ,  Erica B. SCHLESINGER

IPC分类号： A61K9/10 ,  A61K47/32 ,  A61K47/38 ,  A61K47/26 ,  A61K47/20 ,  A61K47/34 ,  A61K47/02 ,  A61K31/506 ,  A61K9/00 ,  A61K9/19

CPC分类号： A61K9/10 ,  A61K47/32 ,  A61K47/38 ,  A61K47/26 ,  A61K47/20 ,  A61K47/34 ,  A61K47/02 ,  A61K31/506 ,  A61K9/0053 ,  A61K9/19

摘要： Disclosed herein are solid formulations of (R)-2-(1-(6-amino-5-chloropyrimidine-4-carboxamido)ethyl)-N-(5-chloro-4-(trifluoromethyl)pyridin-2-yl)thiazole-5-carboxamide (Compound A) or a pharmaceutically acceptable salt thereof for preparing liquid suspensions. In another aspect, the instant application provides methods of preparation of liquid suspensions and kits of solid formulations comprising Compound A. In another aspect, the instant application provides methods of treating cancer with formulations of Compound A. Additionally, the instant disclosure provides methods of treating pediatric cancer patients by the administration of formulations of Compound A.

公开(公告)号：US20220401369A1

公开(公告)日：2022-12-22

申请号：US17824237

申请日：2022-05-25

申请人： DAY ONE BIOPHARMACEUTICALS, INC.

发明人： Yuki KODONO ,  Yasushi SHONO ,  Hirohisa TAKEUCHI

IPC分类号： A61K9/20

摘要： The present disclosure provides a pharmaceutical composition comprising a solid dispersion having a mass median diameter of about 75 μm to about 400 μm, and one or more pharmaceutically acceptable excipients, wherein the solid dispersion comprises (R)-2-(1-(6-amino-5-chloropyrimidine-4-carboxamido)ethyl)-N-(5-chloro-4-(trifluoromethyl)pyridin-2-yl)thiazole-5-carboxamide, or a pharmaceutically acceptable salt thereof, and a vinylpyrrolidone-vinyl acetate copolymer.