- A comparative study of the recent most potent small-molecule PD-L1 inhibitors: what can we learn?
-
Immune checkpoint inhibitors targeting the PD-1/PD-L1 pathway have become a “game-changer” in the cancer treatment. However, none of the small molecular inhibitors has been approved yet. To explore the advantages and disadvantages of various scaffolds, di
- Liu, Mei,Zhang, Yu,Guo, Yu,Gao, Jian,Huang, Wenhai,Dong, Xiaowu
-
-
Read Online
- Mn(III)-Mediated Cascade Cyclization of 3-Isocyano-[1,1′-biphenyl]-2-carbonitrile with Arylboronic Acid: Construction of Pyrrolopyridine Derivatives
-
A Mn(III) mediated cascade cyclization of new designed multifunctionalized 3-isocyano-[1,1′-biphenyl]-2-carbonitrile with arylboronic acid to construct pyrrolopyridine derivatives is developed. A series of pyrroloporidine compounds have been constructed through the formation of two new C-C bonds and one C-N bond via a radical pathway.
- Xu, Pei,Zhu, Yi-Ming,Wang, Fei,Wang, Shun-Yi,Ji, Shun-Jun
-
-
Read Online
- TBPB-initiated cascade cyclization of 3-arylethynyl-[1,1′-biphenyl]-2-carbonitriles with sulfinic acids: Access to sulfone-containing cyclopenta[: Gh] phenanthridines
-
A novel TBPB-initiated cascade cyclization of 3-arylethynyl-[1,1′-biphenyl]-2-carbonitriles with sulfinic acids via C-S, C-C and C-N bond formation for the synthesis of 3-sulfonated cyclopenta[gh]phenanthridines under metal-free conditions has been developed. This protocol features mild conditions, good functional group tolerance and a broad substrate scope. By using this protocol, a variety of potentially bioactive 3-sulfonated cyclopenta[gh]phenanthridines were facilely synthesized via direct annulation.
- Wu, Meixia,Zhang, Man,Zhou, Nengneng,Zhou, Wei,Zhou, Xiaoqiang
-
-
Read Online
- Triazolopyridine compound and preparation method and application thereof
-
The invention belongs to the technical field of medicine and relates to a triazolopyridine compound and a preparation method and application thereof, in particular to a triazolopyridine compound having the structure of general formula I and its stereoisomers and pharmaceutically acceptable salts, wherein R1, R2, R3 and R4 are described as in the claims and the description. All the triazolopyridinecompound, its stereoisomers and pharmaceutically acceptable salts, and a composition containing the triazolopyridine compound can evidently inhibit interaction of PD-1/PD-L1 protein/protein, are suitable for treating the various diseases, such as cancers and viral infections, and therefore, are applicable to the preparation of drugs to prevent and/or treat diseases associated with PD-1/PD-L1 signal pathway.
- -
-
Paragraph 0114; 0116-0118
(2019/07/11)
-
- HETEROCYCLIC COMPOUNDS AS IMMUNOMODULATORS
-
Disclosed are compounds of Formula (I′), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.
- -
-
-
- N-PHENYL-PYRIDINE-2-CARBOXAMIDE DERIVATIVES AND THEIR USE AS PD-1/PD-L1 PROTEIN/PROTEIN INTERACTION MODULATORS
-
Disclosed are compounds of Formula (I), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.
- -
-
Page/Page column 74; 81
(2017/07/06)
-
- QUINAZOLINES AS POTASSIUM ION CHANNEL INHIBITORS
-
A compound of formula (I) wherein A, X, Y, Z, R1 and R24 are described herein. The compounds are useful as inhibitors of potassium channel function and in the treatment and prevention of arrhythmia, IKur-associated disorders, and other disorders mediated by ion channel function.
- -
-
Page/Page column 218-219
(2011/04/14)
-