- SULPHAMOYLARYL DERIVATIVES AND USE THEREOF AS MEDICAMENTS FOR THE TREATMENT OF LIVER FIBROSIS
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Potent 5-HT2B antagonist of Formula (A), including stereochemically isomeric forms, and salts, hydrates, solvates thereof and their use wherein R1 to R4 and Ar have the meaning as defined herein. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them, alone or in combination with other drugs, in fibrosis and/or cirrhosis prevention or therapy.
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Page/Page column 13; 14
(2018/09/08)
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- Arylsulfonyl]-1H-indoles: Synthesis, SAR and biological evaluation as a novel class of 5-HT6 Receptor Antagonists
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In continuation to our efforts to develop better treatment options for cognitive decline, we have been focussing on 5-HT6 receptor (5-HT6R) antagonists, which are known to be involved in improving cognitive function in numerous animal models. In this paper, we report a novel series of [3-[(1-Methylpiperidin-4-yl) methyl] arylsulfonyl]-1H-indole derivatives as potent and selective 5-HT6R antagonists. The lead compound from this series shows potent in vitro binding affinity, functional antagonistic activity at 5-HT6R, good pharmacokinetic profile, excellent selectivity and no Cytochrome P450 liabilities. [Figure not available: see fulltext.]
- Nirogi, Ramakrishna V.S.,Badange, Rajesh Kumar,Kandukuri, Kiran Kumar,Khagga, Mukkanti
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p. 439 - 445
(2015/05/13)
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- 1-arylsulfonyl-2-(Pyridylmethylsulfinyl) benzimidazoles as new proton pump inhibitor prodrugs
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New arylsulfonyl proton pump inhibitor (PPI) prodrug forms were synthesized. These prodrugs provided longer residence time of an effective PPI plasma concentration, resulting in better gastric acid inhibition.
- Shin, Jai Moo,Sachs, George,Cho, Young-Moon,Garst, Michael
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experimental part
p. 5247 - 5280
(2010/03/30)
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- ANTIBACTERIAL AGENTS
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The present invention relates to antibacterial agents that are useful for sterilization, sanitation, antisepsis, and disinfection.
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- PRODRUGS OF PROTON PUMP INHIBITORS
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Prodrugs of proton pump inhibitors of Formulas 1 through 4, (I-IV), where the symbols are as defined in the specification, and the R group includes at least one acidic group or its pharmaceutically acceptable salt, have improved aqueous solubility and bioavailability.
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- Synthesis and D2 Dopaminergic Activity of Pyrrolidinium, Tetrahydrothiophenium, and Tetrahydrothiophene Analogues of Sulpiride
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All of the existing dopamine receptor models recognize the amine nitrogen of agonist and antagonist drugs as playing a crucial role in receptor interactions.However, there has been some controversy as to which molecular form of the amine, charged or uncharged, is most important in these interactions.We have synthesized and examined the biological activity of permanently charged and permanently uncharged analogues of the dopaminergic antagonist, sulpiride.Sulpiride and the permanently charged pyrrolidinium (6,7) and tetrahydrothiophenium (9) analogues were able to antagonize the inhibitory effect of apomorphine on the K+-induced release of acetylcholine from striatal slices.In contrast, the permanently uncharged tetrahydrothiophene analogue 8 was inactive at concentrations up to 100 μM.Additionally, both sulpiride and the tetrahydrothiophenium analogue were able to displace spiperone from D2 binding sites, while the tetrahydrothiophene analogue was unable to produce any significant displacement.These results are consistent with our previous observations on permanently charged chlorpromazine analogues and provide further evidence that dopaminergic antagonists bind in their charged molecular forms to anionic sites on the D2 receptor.
- Harrold, Marc W.,Wallace, Raye Ann,Farooqui, Tahira,Wallace, Lane J.,Uretsky, Norman,Miller, Duane D.
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p. 874 - 880
(2007/10/02)
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- Disubstituted azabicycloalkanes
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Disubstituted azabicycloalkanes of the formula SPC1 Wherein: n is 0, 1 or 2 R is saturated or unsaturated straight or branched (C1 -C5) aliphatic hydrocarbon, and X1, x2, x3, x4, x5, which are the same or different, are hydrogen, halogen, hydroxy, lower alkyl, lower alkoxy, trifluoromethyl, nitro, amino or sulfamoyl. These compounds are used as medicine especially in the treatment of gastroduodenal ulcers, gastric hypersecretion, nauseous syndromes of central origin and hypertension.
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