1834-27-1Relevant articles and documents
Optimization and Synthesis of Pyridazinone Derivatives as Novel Inhibitors of Hepatitis B Virus by Inducing Genome-free Capsid Formation
Lu, Dong,Liu, Feifei,Xing, Weiqiang,Tong, Xiankun,Wang, Lang,Wang, Yajuan,Zeng, Limin,Feng, Chunlan,Yang, Li,Zuo, Jianping,Hu, Youhong
, p. 199 - 205 (2017)
The capsid of hepatitis B virus (HBV) plays a vital role in virus DNA replication. Targeting nucleocapsid function has been demonstrated as an effective approach for anti-HBV drug development. A high-throughput screening and mechanism study revealed the h
Discovery of the S1P2 Antagonist GLPG2938 (1-[2-Ethoxy-6-(trifluoromethyl)-4-pyridyl]-3-[[5-methyl-6-[1-methyl-3-(trifluoromethyl)pyrazol-4-yl]pyridazin-3-yl]methyl]urea), a Preclinical Candidate for the Treatment of Idiopathic Pulmonary Fibrosis
Mammoliti, Oscar,Palisse, Adeline,Joannesse, Caroline,El Bkassiny, Sandy,Allart, Brigitte,Jaunet, Alex,Menet, Christel,Coornaert, Beatrice,Sonck, Kathleen,Duys, Inge,Clément-Lacroix, Philippe,Oste, Line,Borgonovi, Monica,Wakselman, Emanuelle,Christophe, Thierry,Houvenaghel, Nicolas,Jans, Mia,Heckmann, Bertrand,Sanière, Laurent,Brys, Reginald
, p. 6037 - 6058 (2021/06/01)
Mounting evidence from the literature suggests that blocking S1P2 receptor (S1PR2) signaling could be effective for the treatment of idiopathic pulmonary fibrosis (IPF). However, only a few antagonists have been so far disclosed. A chemical enablement strategy led to the discovery of a pyridine series with good antagonist activity. A pyridazine series with improved lipophilic efficiency and with no CYP inhibition liability was identified by scaffold hopping. Further optimization led to the discovery of 40 (GLPG2938), a compound with exquisite potency on a phenotypic IL8 release assay, good pharmacokinetics, and good activity in a bleomycin-induced model of pulmonary fibrosis.
NOVEL COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS THEREOF FOR THE TREATMENT OF FIBROSIS
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Paragraph 0307, (2017/09/15)
The present invention discloses compounds according to Formula I, wherein R1a, R1b, R2a, R2b, R3, R4, R5, R6a, X, Cy1, Cy2, and the subscript n and m are as defined herein. The present invention relates to antagonists compounds of sphingosine 1-phosphate (SIP) receptor, methods for their production, pharmaceutical compositions comprising the same, and methods of treatment using the same, for the prophylaxis and/or treatment of diseases involving fibrotic diseases, inflammatory diseases, autoimmune diseases, metabolic diseases, cardiovascular diseases, and/or proliferative diseases by administering the compound of the invention.