Beigene, Ltd.

Purdue Research Foundation

Bo Ren

Changyou Zhou

Hexiang Wang

Zhiwei Wang

Yunhang Guo

Guoliang Zhang

Tong Zhang

Kang Li

Jing Song

Min Wei

Lai Wang

Zhiyu Tang

Lusong Luo

Jianxin Ma

Xianzhao Kuang

Jingbo Duan

Xutong Wang

Rhizobial infection is the key process for initiating symbiotic nitrogen-fixing root nodules in legumes, which requires specific recognition of signal molecules produced by the bacteria and their hosts. Here, it is established that rhizobial tRNA-derived small RNA fragments (tRFs) are crucial signal molecules modulating host nodulation, which uncovers a bacterial small RNA-mediated mechanism for prokaryote-eukaryote interaction. Transgenic plants are also provided that express a construct encoding rhizobial-derived tRNA, which is subsequently cleaved to produce artificial tRFs. Constructs and methods of producing the same are also provided, as well as modifications for repressing a mechanism for the negative regulation of nodulation present within plants.

Rhizobial tRNA-derived small RNAs and uses thereof for regulating plant nodulation

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 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.

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Beijing, China

Bo Ren