34385-92-7Relevant academic research and scientific papers
Compounds For The Treatment Of Neuromuscular Disorders
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Paragraph 1145; 1147; 1202, (2019/07/03)
The present invention relates to compounds suitable for treating, ameliorating and/or preventing neuromuscular disorders, including the reversal of drug-induced neuromuscular blockade. The compounds as defined herein preferably inhibit the ClC-1 ion channel. The compounds include phenoxy propanoic acid, phenoxy propanoate, and phenoxy butanoate compounds.
COMPOUNDS FOR USE IN TREATING NEUROMUSCULAR DISORDERS
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Page/Page column 103; 104, (2017/01/02)
The present invention relates to compositions comprising compounds for use in treating, ameliorating and/or preventing neuromuscular disorders. The compounds as defined herein preferably inhibit the ClC-1 ion channel. The invention further relates to methods of treating, preventing and/or ameliorating neuromuscular disorders, by administering said composition to a person in need thereof.
SUBSTITUTED AMINO TRIAZOLES, AND METHODS USING SAME
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Page/Page column 62; 68, (2015/07/07)
Disclosed are novel substituted amino triazoles of Formula (I), and pharmaceutically acceptable salts thereof. The compounds of Formula (I) are inhibitors of Acidic mammalian chitinase (AMCase) and are useful, in a non-limiting example, for treating asthma. Also provided are pharmaceutical compositions containing at least one compound of the present invention, or a pharmaceutically acceptable salt, hydrate or solvate thereof, and at least one pharmaceutically acceptable carrier, solvent, adjuvant or diluent, and methods of using such compounds and/or compositions to treat asthma and/or to monitor asthma treatment.
2-(4-R-Phenoxy/phenylthio)alkanoic esters of l-lupinine
Sparatore, Anna,Sparatore, Fabio
, p. 169 - 174 (2007/10/03)
Considering the great pharmacological interest in phenoxy/phenylthioalkanoic esters of open-chain or cyclic aminoalcohols, a set of ten such esters of lupinine was prepared. Initially, their ability to displace [3H]QNB from rat brain preparation was investigated. With the exception of two, all the prepared esters exhibited good affinity to muscarinic receptors (on a non-selective basis), with pKi in the range 6.67-7.68.
Presynaptic cholinergic modulators as potent cognition enhancers and analgesic drugs. 2. 2-Phenoxy-, 2-(phenylthio)-, and 2-(phenylamino)alkanoic acid esters
Gualtieri,Bottalico,Calandrella,Dei,Giovannoni,Mealli,Romanelli,Scapecchi,Teodori,Galeotti,Ghelardini,Giotti,Bartolini
, p. 1712 - 1719 (2007/10/02)
Further modifications of the leads ((R)-(+)-hyoscyamine and (p- chlorophenyl)propionic acid α-tropanyl ester), which show analgesic and nootropic activities as a consequence of increased central presynaptic ACh release, are reported. 2-Phenoxy- and 2-(phenylthio)alkanoic acid esters showed the best results. Several members of these classes possess analgesic properties which are comparable to that of morphine and at the same time are able to reverse dicyclomine-induced amnesia. Confirmation was found that the mechanism of action is due to an increase in ACh release at central muscarinic synapses and that both auto- and heteroreceptors controlling ACh release are very likely involved. According to the results obtained with (R)- (+)-hyoscyamine, analgesic activity is stereochemistry dependent, since the R-(+)-enantiomers are always more efficacious than the corresponding S-(-)- ones. On the basis of their potency and acute toxicity, compounds (±)-28 (SM21) and (±)-42 (SM32) were selected for further study.
Stereospecificity of the Chloride Ion Channel: The Action of Chiral Clofibric Acid Analogues
Bettoni, Giancarlo,Loiodice, Fulvio,Tortorella, Vincenzo,Conte-Camerino, Diana,Mambrini, Mercede,et al.
, p. 1267 - 1270 (2007/10/02)
2-(p-Chlorophenoxy)isobutyric acid (clofibric acid (1) or CPIB) is a drug known to block chloride membrane conductance (GCl) in rat striated muscle.In the present study chiral analogues of CPIB (2-(p-chlorophenoxy)propionic acid (2) and 2-(p-chlorophenoxy)butyric acid (3)) have been tested to evaluate the influence of chirality on Cl ion flux in the channel.The results showed that the chloride channel conductance strongly depends on the absolute configuration: in fact, the S-(-) isomers of the tested compounds strongly decreased the GCl of skeletal muscle membrane, whereas the R-(+) isomers were virtually ineffective.These data allow the hypothesis that, like other ion channels present in various biological systems, the chloride channel of skeletal muscle membrane could also have a stereospecific binding site (or receptor) regulating chloride ion flux.
