- Tetrahydroquinoline-Capped Histone Deacetylase 6 Inhibitor SW-101 Ameliorates Pathological Phenotypes in a Charcot-Marie-Tooth Type 2A Mouse Model
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Histone deacetylase 6 (HDAC6) is a promising therapeutic target for the treatment of neurodegenerative disorders. SW-100 (1a), a phenylhydroxamate-based HDAC6 inhibitor (HDAC6i) bearing a tetrahydroquinoline (THQ) capping group, is a highly potent and sel
- Shen, Sida,Picci, Cristina,Ustinova, Kseniya,Benoy, Veronick,Kutil, Zsófia,Zhang, Guiping,Tavares, Maurício T.,Pavlí?ek, Ji?í,Zimprich, Chad A.,Robers, Matthew B.,Van Den Bosch, Ludo,Ba?inka, Cyril,Langley, Brett,Kozikowski, Alan P.
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p. 4810 - 4840
(2021/05/07)
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- Compound for inhibiting EGFR kinase as well as preparation method and application thereof
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The invention provides a compound as shown in a general formula (I) and pharmaceutically acceptable salt thereof as well as a preparation method and application of the compound. The compound can selectively inhibit the activity of an EGFR (epidermal growt
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Paragraph 0040; 0071-0073
(2021/01/12)
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- TETRAHYDROQUINOLINE SUBSTITUTED HYDROXAMIC ACIDS AS SELECTIVE HISTONE DEACETYLASE 6 INHIBITORS
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Histone deacetylases inhibitors (HDACIs) and compositions containing the same are disclosed. Methods of treating diseases and conditions wherein inhibition of HDAC provides a benefit, like a cancer, a neurodegenerative disorder, a neurological disease, tr
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Paragraph 0183-0184
(2017/09/08)
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- Rigid: Versus flexible anilines or anilides confirm the bicyclic ring as the hydrophobic portion for optimal σ2 receptor binding and provide novel tools for the development of future σ2 receptor PET radiotracers
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Despite their uncertain identification, σ2 receptors are promising targets for the development of diagnostics and therapeutics for tumor diseases. Among the σ2 ligands developed, the class of the flexible benzamides furnished an opti
- Niso, Mauro,Pati, Maria Laura,Berardi, Francesco,Abate, Carmen
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p. 88508 - 88518
(2016/09/28)
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- Synthesis of some 1,2,4-triazoles as potential anti-tubercular agents
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A series of 5-(N-substituted carboxamidoethylthio)-3-(3'pyridyl)-4- amino-1,2,4-triazole derivatives 6a-j have been synthesized and evaluated for anti-tubercular activity. They are screened in-vitro at 10μg/mL concentration against Mycobacterium tuberculosis H37RV (ATCC 27294). All the compounds are showing antitubercular activity when compared with the standard drug Amikacin. Compounds 6e and 6h are found active as they displayed IC50 and IC90 values at 100μg/mL.
- Vijayaraghavan,Shirodkar
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p. 1149 - 1153
(2015/09/28)
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- COMPOUNDS AND COMPOSITIONS FOR THE TREATMENT OF PARASITIC DISEASES
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The present invention provides compounds of formula I: [INSERT FORMULA HERE] or a pharmaceutically acceptable salt, tautomer, or stereoisomer, thereof, wherein the variables are as defined herein. The present invention further provides pharmaceutical compositions comprising such compounds and methods of using such compounds for treating, preventing, inhibiting, ameliorating, or eradicating the pathology and/or symptomology of a disease, such as malaria, caused by a Plasmodium parasite.
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Page/Page column 140
(2014/06/11)
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- Novel cyclic amide derivatives
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Novel compounds represented by the following formula (I) that act as a ligand to sigma receptor/binding cite and a medicament comprising the same as an active ingredient: wherein X represents an alkyl group, an aryl group, a heterocyclic group or the like; Q represents a group represented by —CH2—, —CO—, —O—, —CH(OR7)— or the like wherein R7 represents a hydrogen atom, an alkyl group or the like; n represents an integer of from 0 to 5; R1 and R2 each represent a hydrogen atom, an alkyl group or the like; B represents either of the following groups: wherein R3, R4, R5, and R6 each represent a hydrogen atom, a halogen atom, an alkoxyl group or the like; m represents 1 or 2; and the ring of: represents an aromatic heterocyclic ring.
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