- Synthesis and biological evaluation of GABA derivatives able to cross the blood-Brain barrier in rats
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Two new GABA derivatives, 1 and 2, were synthesized and tested for their capacity to display CNS activity, which was assessed by determining the effects on the duration of pentobarbital-induced hypnosis in rats. Compound 1, peripherally injected, significantly prolonged the hypnosis time, a typical GABA-mimetic effect, while both intracerebroventricular and intravenous administration of compound 2 surprisingly shortened the hypnotic effect in an atropine-sensitive way. The study was extended also to compounds 1a, 1b and 2a, putative oxidative/hydrolytic metabolites of 1 and 2.
- Carelli, Vincenzo,Liberatore, Felice,Scipione, Luigi,Giorgioni, Gianfabio,Di Stefano, Antonio,Impicciatore, Mariannina,Ballabeni, Vigilio,Calcina, Francesco,Magnanini, Francesca,Barocelli, Elisabetta
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- COMPOSITIONS AND METHODS FOR THE TREATMENT MIGRAINE AND NEUROLOGIC DISEASES
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The invention relates to the compounds of formula I or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, and methods for the treatment of migraine and neurologic diseases may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of epilepsy, migraine, Post Herpetic Neuralgia, Acute and Chronic Pain, Alzheimer's disease, Creutzfeld Disease, familial amyloid polyneuropathy, parkinson's disease, fibromyalgia syndrome.
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Paragraph 0111; 0114; 0115
(2015/06/10)
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- PRODRUGS OF GABA ANALOGS
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The disclosures herein provide compounds of formula ?, formula II, formula 111 and formula IV or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers, and hydrates thereof. These salts may be formulated as pharmaceutical compositions. The pharmaceutical compositions may be formulated for oral administration, transdermal administration, transmucosal, syrups, topical, extended or sustained release, or injection. Such compositions may be used to treatment of neurological disease and conditions such as neuropathic pain, diabetic neuropathic pain, epilepsy, restless leg syndrome, and other diseases related sub-chronic and chronic pain or its associated complications.
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- COMPOSITIONS AND METHODS FOR THE TREATMENT OF NEUROPATHIC PAIN
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The invention relates to the compounds of formula (I), formula (II), formula (III) and formula (IV) or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula (I), formula (II), formula (III) or formula (IV) and methods for the treatment of neuropathic pain may he formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of neuralgia, severe pain, chronic pain, chemotherapy induced pain, neuropathic pain, post herpetic neuralgia, neuralgia, motor neurone disease, diabetic neuropathy, postherpetic neuralgia, injury, post-operative pain, osteoarthritis, rheumatoid arthritis, multiple sclerosis, spinal cord injury, migraine, HIV related neuropathic pain, cancer pain and lower back pain.
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- NOVEL COMPOSITIONS FOR REDUCING A? 42 PRODUCTION AND THEIR USE IN TREATING ALZHEIMER'S DISEASE (AD)
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Novel small molecule compounds for reduction of A? 42 production and for treatment of Alzheimer's Disease and other neurodegenerative disorders, methods of making them and pharmaceutical compositions containing them are described.
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Page/Page column 52; 53
(2011/08/08)
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- Synthesis of GABA-valproic acid derivatives and evaluation of their anticonvulsant and antioxidant activity
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The synthesis and the anticonvulsant activity of a number of GABA and valproic acid derivatives are reported. The lipophilicity of these compunds and their inhibitory effect on lipid peroxidation were also investigated, in an effort to correlate the anticonvulsant activity with lipophilicity and inhibitory effect on lipid peroxidation. The synthetized compounds exhibited anticonvulsant effects which were stronger for the more lipophilic derivatives. One of the active anticonvulsants showed appreciable antioxidant properties. Finally, a good correlation was found between the experimentally derived (R(M)) and calculated (Σf and log P(SK)) lipophilicity for this series of compounds.
- Rekatas, George V.,Tani, Ekaterini,Demopoulos, Vassilis J.,Kourounakis, Panos N.
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p. 393 - 398
(2007/10/03)
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- Composition containing a penem or carbapenem antibiotic and the use of the same
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Administration of an N-acylated amino acid in association with a penem or carbapenem antibiotic relieves or eliminates the renal problems associated with administration of the antibiotic alone. The amino acid derivative and antibiotic may be formulated together as a composition or administered separately, either simultaneously or sequentially.
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- Composition containing a penem or carbapenem antibiotic
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Administration of an N-acylated amino acid in association with a penem or carbapenem antibiotic relieves or eliminates the renal problems associated with administration of the antibiotic alone. The amino acid derivative and antibiotic may be formulated together as a composition or administered separately, either simultaneously or sequentially. The composition may be prepared by simple mixing.
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