- 2,3-DIHYDROQUINAZOLIN COMPOUNDS AS NAV1.8 INHIBITORS
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The present invention relates to Nav1.8 Inhibitor 2,3-dihydroquinazolin compounds of Formula (X); wherein Y', X', B', R1', R2', R3', R5', R6', R7', and z1 are as defined herein; or pharmaceutically acceptable salts or tautomer forms thereof, corresponding pharmaceutical compositions or formulations, methods or processes of compound preparation, methods, compounds for use in, uses for and/or combination therapies for treating pain and/or pain-related or associated disease(s), disorder(s) or condition(s), respectively.
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Page/Page column 161; 173-174
(2021/01/23)
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- RE[N(SiMe3)2]3-Catalyzed Guanylation/Cyclization of Amino Acid Esters and Carbodiimides
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The example of rare-earth metal-catalyzed guanylation/cyclization of amino acid esters and carbodiimides is well-established, forming 4(3H)-2-alkylaminoquinazolinones in 65-96% yields. The rare-earth metal amides RE[N(TMS)2]3 (RE = Y, Yb, Nd, Sm, La; TMS = SiMe3) showed high activities, and La[N(TMS)2]3 performed best for a wide scope of the substrates.
- Lu, Chengrong,Gong, Chao,Zhao, Bei,Hu, Lijuan,Yao, Yingming
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p. 1154 - 1159
(2018/02/10)
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- Design, synthesis and biological characterization of a new class of osteogenic (1H)-quinolone derivatives
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Smoothened (Smo) is the signal transducer of the Hedgehog (Hh) pathway and its stimulation is considered a potential powerful tool in regenerative medicine to treat severe tissue injuries. Starting from GSA-10, a recently reported Hh activator acting on Smo, we have designed and synthesized a new class of quinolone-based compounds. Modification and decoration of three different portions of the original scaffold led to compounds able to induce differentiation of multipotent mesenchymal cells into osteoblasts. The submicromolar activity of several of these new quinolones (0.4–0.9?μM) is comparable to or better than that of SAG and purmorphamine, two reference Smo agonists. Structure-activity relationships allow identification of several molecular determinants important for the activity of these compounds.
- Manetti, Fabrizio,Petricci, Elena,Gabrielli, Annalisa,Mann, Andrè,Faure, Hélène,Gorojankina, Tatiana,Brasseur, Laurent,Hoch, Lucile,Ruat, Martial,Taddei, Maurizio
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supporting information
p. 747 - 757
(2016/07/21)
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- Synthesis, biological evaluation, and structure-activity relationships of 2-[2-(benzoylamino)benzoylamino]benzoic acid analogues as inhibitors of adenovirus replication
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2-[2-Benzoylamino)benzoylamino]benzoic acid (1) was previously identified as a potent and nontoxic antiadenoviral compound (Antimicrob. Agents Chemother. 2010, 54, 3871). Here, the potency of 1 was improved over three generations of compounds. We found that the ortho, ortho substituent pattern and the presence of the carboxylic acid of 1 are favorable for this class of compounds and that the direction of the amide bonds (as in 1) is obligatory. Some variability in the N-terminal moiety was tolerated, but benzamides appear to be preferred. The substituents on the middle and C-terminal rings were varied, resulting in two potent inhibitors, 35g and 35j, with EC50 = 0.6 μM and low cell toxicity.
- ?berg, Christopher T.,Strand, M?rten,Andersson, Emma K.,Edlund, Karin,Tran, Nam Phuong Nguyen,Mei, Ya-Fang,Wadell, G?ran,Elofsson, Mikael
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experimental part
p. 3170 - 3181
(2012/06/04)
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- NEW ANTIVIRAL COMPOUNDS
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The present invention provides new antiviral compounds and pharmacological compositions comprising these new compounds and their use in the prophylaxis, prevention and treatment of viral infections, particularly adenovirus and herpes virus infections.
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Page/Page column 45; 57
(2012/01/05)
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- A facile synthesis of 9-dialkylamino-9H-pyrrolo[1,2-a]indoles via iminium salts generated from 2-(pyrrol-1-yl)benzaldehydes and secondary amine hydrochlorides in the presence of NaI/TMSCl/Et3N
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The NaI/TMSCl/Et3N-mediated condensation between 2-(pyrrol-1-yl)benzaldehydes and secondary amine hydrochlorides followed by intramolecular trapping of the resulting iminium carbon by the 2-position of the pyrrole ring afforded corresponding 9-
- Kobayashi, Kazuhiro,Takanohashi, Atsushi,Hashimoto, Kenichi,Morikawa, Osamu,Konishi, Hisatoshi
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p. 3158 - 3161
(2007/10/03)
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- Substituted imidazo [1,5-a] pyrimido [5,4-d] [1] benzazepine derivatives
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The present invention is a compound of formula wherein R1 is halogen or lower alkyl; R2 is hydrogen, lower alkyl, cycloalkyl, —(CH2)m-phenyl, wherein the phenyl ring may be substituted by lower alkoxy, or is —(CH2)m-indolyl; R3 is —C(O)O-lower alkyl, —C(O)OH, or a five membered heteroaromatic group, which rings may be substituted by lower alkyl or cycloalkyl; n is 0, 1 or 2; m is 0, 1 or 2; or a pharmaceutically acceptable acid addition salt thereof. Compound I shows high affinity and selectivity for GALA A α5 receptor binding sites.
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