1198412-88-2Relevant academic research and scientific papers
SUBSTITUTED 1,1'-BIPHENYL COMPOUNDS AND METHODS USING SAME
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Page/Page column 366-367, (2021/08/13)
The present invention includes substituted 1,1'-biphenyl compounds, analogues thereof, and compositions comprising the same. In one aspect, the compounds contemplated in the invention can be used to treat, ameliorate, or prevent hepatitis B virus (HBV) and/or hepatitis D virus (HDV) infections in a patient. In another aspect, the compounds contemplated in the invention can be used to treat, ameliorate, and/or prevent cancer in a patient.
HETEROCYCLIC COMPOUNDS AND METHODS OF USE
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Paragraph 000328, (2020/02/06)
The present invention discloses compounds useful in treatment of conditions associated with excessive activity of transforming growth factor beta (TGF-β), particularly type 1 or activin-like kinase 5 (ALK 5). Specifically the present invention discloses compound of formula (I) which exhibit inhibitory activity against ALK 5. Method of treating conditions associated with excessive activity (ALK 5) with such compound is disclosed. Uses thereof, pharmaceutical composition, and kits are also disclosed.
Discovery of novel positive allosteric modulators of the metabotropic glutamate receptor 5 (mGlu5)
Varnes, Jeffrey G.,Marcus, Andrew P.,Mauger, Russell C.,Throner, Scott R.,Hoesch, Valerie,King, Megan M.,Wang, Xia,Sygowski, Linda A.,Spear, Nathan,Gadient, Reto,Brown, Dean G.,Campbell, James B.
supporting information; experimental part, p. 1402 - 1406 (2011/04/16)
Novel in vitro mGlu5 positive allosteric modulators with good potency, solubility, and low lipophilicity are described. Compounds were identified which did not rely on the phenylacetylene and carbonyl functionalities previously observed to be required for in vitro activity. Investigation of the allosteric binding requirements of a series of dihydroquinolinone analogs led to phenylacetylene azachromanone 4 (EC 50 11.5 nM). Because of risks associated with potential metabolic and toxicological liabilities of the phenylacetylene, this moiety was successfully replaced with a phenoxymethyl group (27; EC50 156.3 nM). Derivation of a second-generation of mGlu5 PAMs lacking a ketone carbonyl resulted in azaindoline (33), azabenzimidazole (36), and N-methyl 8-azaoxazine (39) phenylacetylenes. By scoping nitrogen substituents and phenylacetylene replacements in 39, we identified phenoxymethyl 8-azaoxazine 47 (EC50 50.1 nM) as a potent and soluble mGlu5 PAM devoid of both undesirable phenylacetylene and carbonyl functionalities.
Synthesis of halogenated 4H-pyrido[1,2-a]pyrimidin-4-ones
Molnar, Annamaria,Faigl, Ferenc,Podanyi, Benjamin,Finta, Zoltan,Balazs, Laszlo,Hermecza, Istvan
experimental part, p. 2477 - 2488 (2010/04/29)
Halogenated 4H-pyrido[l,2-a]pyrimidin-4-one were synthesized by thermal cyclization and decarboxylation of isopropylidene (2-pyridylamino)methylenemalonates, prepared from 2-aminopyridines and isopropylidene methoxymethylenemalonate formed in situ. Instead of 4H-pyrido[l,2-a]pyrimidin-4-ones, the 6-chloro and 6-bromo derivatives afforded mixtures of 7-halo-l,4-dihydro-l,8-naphthyridin-4-ones and 1-(6-halo-2-pyridyl)-3-[(6-halo-2-pyridylamino)methylene]-1,2,3,4-tetrahydropyridine-2,4-diones. The latters formed from N-(2-pyridyl)iminoketenes, the common intermediates of 4H-pyrido[l,2-a]pyrimidin-4-one and l,8-naphthyridin-4-ones, via a "head-to-tail" [4+2] cycloaddition. 3-Halo-4H-pyrido[l,2-a]pyrimidin-4-ones were obtained from 4H-pyrido[1,2-a]pyrimidin-4-one with N-halosuccinimides. The structures of the new compounds were characterized by means of 1H NMR and 13C NMR examinations.
