766556-54-1Relevant articles and documents
Benzimidazole derivatives as well as preparation method and application thereof
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Paragraph 0124-0127, (2020/08/26)
The invention discloses a benzimidazole compound as well as a preparation method and application thereof. The compound has a structure as shown in a formula (I); wherein the X and Y are each independently C or N, R1, R2, R3, R4, A and B are different substituents. The compound is novel in structure and has excellent inhibition effect on the phosphodiesterase 10 type, can effectively selectively suppress the phosphodiesterase 10 type and is free of or is very weak in inhibition effect on other subtype phosphodiesterase; therefore, the compound disclosed by the invention can be used as a phosphodiesterase 10 type inhibitor to be prepared into a medicine for treating and/or preventing related diseases caused by phosphodiesterase 10 type, such as pulmonary hypertension, pulmonary fibrosis, schizophrenia and the like; meanwhile, the benzimidazole compound or the pharmaceutically acceptable salt thereof can be used as a fluorescent probe; for example, the benzimidazole compound or the pharmaceutically acceptable salt thereof can be applied to the aspects of cell imaging, tissue imaging, living body imaging and the like.
LACTAM-CONTAINING COMPOUNDS AND DERIVATIVES THEREOF AS FACTOR XA INHIBITORS
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, (2017/04/28)
The present application describes lactam-containing compounds and derivatives thereof of Formula I: P4—P-M-M4??I or pharmaceutically acceptable salt forms thereof, wherein ring P, if present is a 5-7 membered carbocycle or heterocycle and ring M is a 5-7 membered carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.
Structure-activity relationships of anthranilamide-based factor Xa inhibitors containing piperidinone and pyridinone P4 moieties
Corte, James R.,Fang, Tianan,Pinto, Donald J.P.,Han, Wei,Hu, Zilun,Jiang, Xiang-Jun,Li, Yun-Long,Gauuan, Jolicia F.,Hadden, Mark,Orton, Darren,Rendina, Alan R.,Luettgen, Joseph M.,Wong, Pancras C.,He, Kan,Morin, Paul E.,Chang, Chong-Hwan,Cheney, Daniel L.,Knabb, Robert M.,Wexler, Ruth R.,Lam, Patrick Y.S.
, p. 2845 - 2849 (2008/12/21)
Introduction of the phenyl piperidinone and phenyl pyridinone P4 moieties in the anthranilamide scaffold led to potent, selective, and orally bioavailable inhibitors of factor Xa. Anthranilamide 28 displayed comparable efficacy to apixaban in the rabbit a