Beigene, Ltd.

Tsinghua University

Beone Medicines I Gmbh

Hexiang Wang

Changyou Zhou

Bo Ren

Zhiwei Wang

Yunhang Guo

Guoliang Zhang

Xianzhao Kuang

Tong Zhang

Kang Li

Jing Song

Min Wei

Lai Wang

Tiantian Zhang

Zhiyu Tang

Boyu Zhang

Lusong Luo

Huaqing Liu

Changxin Huo

Ruipeng Qi

Hongen Liao

Disclosed herein are novel bifunctional compounds formed by conjugating BTK inhibitor moieties with E3 ligase Ligand moieties, which function to recruit targeted proteins to E3 ubiquitin ligase for degradation, and methods of preparation and uses thereof.

Degradation of bruton's tyrosine kinase (BTK) by conjugation of BTK inhibitors with E3 ligase ligand and methods of use

Disclosed is a self-propelled soft robot body, including a tube which is internally and axially provided with a tube cavity, and at least one propelling structure, comprising a first driving unit, a second driving unit and a third driving unit, which are evenly fixed on a peripheral wall of the tube cavity, relative to an axis thereof, and along the axis of the tube; and the first driving unit, the second driving unit and the third driving unit are respectively telescopic along the axis of the tube; at least two support structures, with each two adjacent support structures having at least one propelling structure arranged therebetween, the support structures are fixedly connected with the propelling structure and arranged on the peripheral wall of the tube cavity.

Self-propelled soft robot body

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 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 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

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

Disclosed are substituted 5-(3,5-dimethylisoxazol-4-yl)indoline-2-one compounds, pharmaceutical compositions comprising at least one such 4 substituted 5-(3,5-dimethylisoxazol-4-yl)indoline-2-one compound processes for the preparation thereof, and the use thereof for inhibiting BET family of bromodomains and for treating disorders mediated thereby, such as certain cancers.

Substituted 5-(3,5-dimethylisoxazol-4-yl)indoline-2-ones

The present invention provides a compound of Formula (I):  wherein the variables Z, n, Y and p are as defined herein, and pharmaceutically acceptable salts thereof, which can inhibit the activity of poly (ADP-ribose)polymerases, and pharmaceutical compositions comprising the same.

Growing community of inventors

Beijing, China

Hexiang Wang