Beigene Switzerland Gmbh

Beigene, Ltd.

Lai Wang

Yang Liu

Kang Li

Tong Zhang

Zhiwei Wang

Yunhang Guo

Jing Song

Min Wei

Lusong Luo

Changyou Zhou

Gongyin Shi

Zhiyu Tang

Guoliang Zhang

Nan Hu

Hexiang Wang

Bo Ren

Zhirong Shen

Hui Yao

Qinzhou Qi

Jeannie Hou

Zhong Wu

Xinfeng Hou

Haiyi Guo

Weige Wang

Yiling Yu

The present invention relates to a crystalline form of (S)-7-(1-acryloylpiperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetr a-hydropyrazolo[1,5-a]pyrimi dine-3-carboxamide for inhibiting Btk, methods of preparation thereof and pharmaceutical compositions, and use of the crystalline form above in the treatment of a disease, or in the manufacturing of a medicament for the treatment of a disease.

Crystalline form of (s)-7-(1-acryloylpiperidin-4-yl)- 2-(4-phenoxyphenyl)-4,5,6,7-tetra- hydropyrazolo[1,5-a]pyrimidine-3-carboxamide, preparation, and uses thereof

The present invention relates to a crystalline form of (S)-7-(1-acryloylpiperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetra-hydropyrazolo[1,5-a]pyrimidine-3-carboxamide for inhibiting Btk, methods of preparation thereof and pharmaceutical compositions, and use of the crystalline form above in the treatment of a disease, or in the manufacturing of a medicament for the treatment of a disease.

Crystalline form of (S)-7-(1-acryloylpiperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetra- hydropyrazolo[1,5-a]pyrimidine-3-carboxamide, preparation, and uses thereof

Disclosed herein is a method for the prevention, delay of progression or treatment of cancer in a subject, comprising administering to the subject in need thereof a Btk inhibitor, particularly, (S)-7-(1-acryloylpiperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetra-hydropyrazolo[1,5-a]pyrimidine-3-carboxamide or a pharmaceutically acceptable salt thereof, in combination with an immune checkpoint inhibitor or a targeted therapy agent. Also, disclosed a pharmaceutical combination comprising a Btk inhibitor, particularly, (S)-7-(1-acryloylpiperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetra-hydropyrazolo[1,5-a]pyrimidine-3-carboxamide or a pharmaceutically acceptable salt thereof, in combination with an immune checkpoint inhibitor, or a targeted therapy agent and the use thereof.

Treatment of B cell cancers using a combination comprising Btk inhibitors

Disclosed herein is method for the prevention, delay of progression or treatment of hepatocellular carcinoma in a subject, comprising administering to the subject in need thereof a therapeutically effective amount of an anti-PD-1 antibody, which is an antibody or a fragment antigen binding thereof, specifically binding to human PD-1.

Immunotherapy for hepatocellular carcinoma

Disclosed herein is a pharmaceutical combination for use in the prevention, delay of progression or treatment of cancer, wherein the pharmaceutical combination exhibits a synergistic efficacy. The pharmaceutical combination comprises a humanized antagonist monoclonal antibody against PD- and a RAF inhibitor. Also disclosed herein is a combination for use in the prevention, delay of progression or treatment of cancer in a subject, comprising administering to the subject a therapeutically effective amount of a humanized antagonist monoclonal antibody against PD-1 and a therapeutically effective amount of a RAF inhibitor.

Combination of a PD-1 antagonist and a RAF inhibitor for treating cancer

Disclosed herein is a method for the prevention, delay of progression or treatment of cancer in a subject, comprising administering to the subject in need thereof a PARP inhibitor, particularly, (R)-2-fluoro-10a-methyl-7,8,9,10,10a,11-hexahydro-5,6,7a,11-tetraazacyclohepta[def]cyclopenta[a]fluoren-4(5H)-one, a sesqui-hydrate thereof, or a pharmaceutically acceptable salt thereof, in combination with an immune checkpoint inhibitor or a chemotherapeutic agent. Also, disclosed a pharmaceutical combination comprising a PARP inhibitor, particularly, (R)-2-fluoro-10a-methyl-7,8,9,10,10a,11-hexahydro-5,6,7a,11-tetraazacyclohepta[def]cyclopenta[a]fluoren-4(5H)-one, a sesqui-hydrate thereof, or a pharmaceutically acceptable salt thereof, in combination with an immune checkpoint inhibitor, or a chemotherapeutic agent and the use thereof.

Treatment cancers using a combination comprising PARP inhibitors

Growing community of inventors

Beijing, China

Lai Wang