123762-06-1Relevant articles and documents
DIHYDROPYRIMIDINE DERIVATIVES AND USES THEREOF IN THE TREATMENT OF HBV INFECTION OR OF HBV-INDUCED DISEASES
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, (2020/01/24)
The application describes dihydropyrimidine derivatives which are useful in the treatment or prevention of HBV infection or of HBV-induced diseases, more particularly of HBV chronic infection or of diseases induced by HBV chronic infection, as well as pharmaceutical or medical applications thereof.
Tetraoxanes as inhibitors of apicomplexan parasites Plasmodium falciparum and Toxoplasma gondii growth and anti-cancer molecules
Opsenica, Dejan M.,Radivojevic, Jelena,Matic, Ivana Z.,?tajner, Tijana,Kne?evic-U?aj, Slavica,Djurkovic-Djakovic, Olgica,?olaja, Bogdan A.
, p. 1339 - 1359 (2016/02/18)
New cyclohexylidene 1,2,4,5-tetraoxanes with polar guanidine and urea based groups were synthesized and evaluated for their antimalarial activity against chloroquine resistant and susceptible Plasmodium falciparum strains. The derivatives showed moderate, nM range antimalarial activities and low cytotoxicity. The N-phenylurea derivative 24 exhibited the best resistance indices (RIW2 = 0.44, RITM91C235 = 0.80) and was not toxic against human normal peripheral blood mononuclear cells (IC50 > 200 μM). Seven derivatives were tested in vitro against four human cancer cell lines and they demonstrated high selectivity toward leukaemia K562 cells. One compound, derivative 21 with a primary amino group, was the first tetraoxane tested in vivo against Toxoplasma gondii as another apicomplexan parasite. Subcutaneous administration at a dose of 10 mg kg-1 day-1 for 8 days allowed the survival of 20 % of infected mice, thus demonstrating the high potential of tetraoxanes for the treatment of apicomplexan parasites.
l-HYDROXYCYCLOALKANECARBOXAMIDE DERIVATIVES AS BRADYKININ ANTAGONISTS
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Page/Page column 35-36, (2008/06/13)
α-Hydroxycycloalkanecarboxamide derivatives of formula (I) or a pharmaceutically acceptable salt thereof, wherein formula (a) is a single or double bond; Rl, R2 and R3 are each independently selected from H, halogen and OH; or Rl and R2 attached to the same carbon atom together represent oxo; R4 is H or methyl; R5 is Cl or F; R6 is selected from -CO2-C1-4alkyl, -O-C1-4alkyl, -O- C1-4haloalkyl, 2-methyltetrazol-5-yl, 5-methyl l,2,4-oxadiazol-3-yl, 3-methyl-1,2,4-oxadiazol-5-yl, 5-halomethyl-l,2,4-oxadiazol-3-yl, 3-halomethyl- l,2,4-oxadiazol-5-yl, tetrazol-5-yl, 5-halomethyl-l,2,3-triazolyl, and 5-methyl-l ,2,3-triazolyl; R7 and R8 are each independently Cl or F; and n is 0 or 1, are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway.