[EN] INDAZOLOPYRIMIDINONES AS FIBRINOLYSIS INHIBITORS<br/>[FR] INDAZOLOPYRIMIDINONES COMME INHIBITEURS DE LA FIBRINOLYSE
申请人:BAYER PHARMA AG
公开号:WO2016173948A1
公开(公告)日:2016-11-03
The present application relates to novel substituted indazolopyrimidinones, to processes for their preparation, the compounds for use alone or in combinations in a method for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of acute and recurrent bleeding in patients with or without underlying hereditary or acquired hemostatic disorders, wherein the bleeding is associated with a disease or medical intervention selected from the group consisting of heavy menstrual bleeding, postpartum hemorrhage, hemorrhagic shock, trauma, surgery, transplantation, stroke, liver diseases, hereditary angioedema, nosebleed, and synovitis and cartilage damage following hemarthrosis.
Hamamelitannin Analogues that Modulate Quorum Sensing as Potentiators of Antibiotics against <i>Staphylococcus aureus</i>
作者:Arno Vermote、Gilles Brackman、Martijn D. P. Risseeuw、Bieke Vanhoutte、Paul Cos、Kristof Van Hecke、Koen Breyne、Evelyne Meyer、Tom Coenye、Serge Van Calenbergh
DOI:10.1002/anie.201601973
日期:2016.5.23
drugs is a promising alternative to the development of novel antibiotics. In the present study, we synthesized 58 analogues of hamamelitannin (HAM), a quorumsensing inhibitor and antimicrobial potentiator. These efforts resulted in the identification of an analogue that increases the susceptibility of Staphylococcusaureus towards antibiotics in vitro, in Caenorhabditis elegans, and in a mouse mammary
series of pyridine‐, pyridazine‐, and pyrazine‐derived carboxamides bearing at the ring N‐atom an alkyl side‐chain with a terminal carboxylic group (7–11) or with a terminal acetylamino malonic ester moiety (13–17, 19–23) is described. Two desaza‐pyridazomycin derivatives (24, 26) and homologs thereof (25, 27) were synthesised. The novel compounds which are structurallyrelated to the antifungal antibiotic