Beigene, Ltd.

Merck + Co., Inc.

Merck Sharp + Dohme Corp.

Other

Beigene Switzerland Gmbh

Changyou Zhou

Lihu Yang

Guoliang Zhang

Hexiang Wang

Bo Ren

Alexander Pasternak

Stephen D Goble

Sander G Mills

Gabor Butora

Gregori J Morriello

Christopher Richard Moyes

Zhiwei Wang

Yunhang Guo

Shankaran Kothandaraman

Richard Jiao

Tong Zhang

Qun Dang

Kang Li

Jing Song

Min Wei

Deodialsingh Guiadeen

Lai Wang

Zhiyu Tang

Shaohui Wang

Lusong Luo

Min Ge

Cheng Tang

Wuxin Zou

Yuxia Hua

Songnian Lin

Xianzhao Kuang

Arthur A Patchett

Haifeng Tang

Liangqin Guo

Robert D Larsen

Shawn P Walsh

Dongwei Cai

Mark S Jensen

Kothandaraman Shankaran

Wenjie Li

Fred Fleitz

Eric Dean Cline

Sunita Malkani

Scott Hoerrner

Gary Javadi

Dorian Nelson

Elizabeth Szumigala

Yanping Pan

Gouliang Zhang

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 are novel benzoimidazoles and pharmaceutical compositions comprising at least one such novel benzoimidazoles, processes for the preparation thereof, and the method for using the same in therapy. In particular, disclosed herein are certain novel benzoimidazoles that are useful for inhibiting indoleamine 2, 3-dioxygenase and for treating diseases or disorders mediated thereby.

Benzoimidazoles as selective inhibitors of indoleamine 2,3-dioxygenases

Disclosed herein is a pyrazolotriazolopyrimidine derivative or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof useful as an A2A receptor antagonist, and a pharmaceutical composition comprising the same. Also disclosed herein is a method of treating cancer using the pyrazolotriazolopyrimidine derivative or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof as an A2A receptor antagonist.

Pyrazolotriazolopyrimidine derivatives as A2A receptor antagonist

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

Disclosed herein are salts of (R)-2-fluoro-10a-methyl-7,8,9,10,10a,11-hexahydro-5,6,7a,11-tetraazacyclohepta[def]cyclopenta[a]fluoren-4(5H)-one, and crystalline forms (polymorphs) thereof. Also disclosed herein are methods of preparing those crystalline forms, and methods of using at least one of those crystalline forms in treating a cancer responsive to inhibition of PARP, especially a cancer associated with BRCA1/2 mutant activities or other HR deficiencies, in a subject.

Crystalline forms of salts of fused penta-cyclic dihydrodiazepinocarbazolones, and uses thereof

Disclosed herein are 5 or 8-substituted imidazo [1, 5-a] pyridines and pharmaceutical compositions comprising at least one such 5 or 8-substituted imidazo [1, 5-a] pyridines, processes for the preparation thereof and the use thereof in therapy. Disclosed herein are certain 5 or 8-substituted imidazo [1, 5-a] pyridines that can be useful for inhibiting indoleamine 2, 3-dioxygenase and/or tryptophane 2, 3-dioxygenase and for treating diseases or disorders mediated thereby.

5 or 8-substituted imidazo [1,5-a] pyridines as selective inhibitors of indoleamine and/or tryptophane 2,3-dioxygenases

Disclosed herein are 5 or 8-substituted imidazo[1,5-a]pyridines and pharmaceutical compositions comprising at least one such 5 or 8-substituted imidazo[1,5-a]pyridines, processes for the preparation thereof, and the use thereof in therapy. Disclosed herein are certain 5 or 8-substituted imidazo[1,5-a]pyridines that can be useful for inhibiting indoleamine 2,3-dioxygenase and/or tryptophane 2,3-dioxygenase and for treating diseases or disorders mediated thereby. 

5 or 8-substituted imidazo[1,5-a]pyridines as indoleamine and/or tryptophane 2,3-dioxygenases

Provided are certain fused tricyclic compounds and salts thereof, compositions thereof, and methods of use therefor.

Fused tricyclic compounds as Raf kinase inhibitors

Provided are certain fused tricyclic urea compounds and salts thereof, compositions thereof, and methods of use therefor.

Fused tricyclic urea compounds as Raf kinase and/or Raf kinase dimer inhibitors

Provided are certain fused tetra or penta-cyclic compounds and salts thereof, compositions thereof, and methods of use thereof.

Fused tetra or penta-cyclic dihydrodiazepinocarbazolones as PARP inhibitors

Provided are a process for preparing a Parp1/2 inhibitor, i.e., (R)-2-fluoro-10a-methyl-7,8,9,10,10a,11-hexahydro-5,6,7a,11-tetraazacyclohepta[def]cyclopenta[a]fluoren-4(5H)-one (hereinafter referred to as Compound A), crystalline forms (poly-morphs) of Compound A or hydrate or solvate thereof, methods for preparing the crystalline forms, and the use thereof.

Process for preparing a PARP inhibitor, crystalline forms, and uses thereof

The invention relates to 5-(((1R,1aS,6bR)-1-(6-(trifluoromethyl)-1H-benzo [d] imidazol-2-yl)-1a,6b-dihydro-1H-cyclopropa [b] benzofuran-5-yl) oxy)-3,4-dihydro-1, 8-naphthyridin-2 (1H)-one (Compound 1) maleate salts, in particular the sesqui-maleate salt and its crystalline forms, methods of preparation, pharmaceutical compositions, and therapeutic uses for treatment of diseases or disorders mediated by BRAF or other kinases.

Maleate salts of a B-RAF kinase inhibitor, crystalline forms, methods of preparation, and uses therefore

5 or 8-substituted imidazo[1, 5-a] pyridines as indoleamine and/or tryptophane 2, 3-dioxygenases

Growing community of inventors

Princeton, NJ, United States of America

Changyou Zhou