Analgesic and nootropic drugs

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

Patent

Rate now

  [ 0.00 ] – not rated yet Voters 0   Comments 0

Details

546124, 546127, 546128, 546129, 546130, A61K 3144, C07D45102

Patent

active

055831427

ABSTRACT:
Compounds of general formula: ##STR1## where: Ar=phenyl or beta-naphtyl, or aromatic heterocyclic 6-membered ring containing one or two nitrogen atoms;
R.sub.1 =one or more substituents of the Ar nucleus, preferably in para position, and selected out of the group consisting of H, CH.sub.3, CH.sub.2 --CH--(CH.sub.3).sub.2, O--CH.sub.3, Cl, F, Br, CF.sub.3, NH.sub.2, S--CH.sub.3, CN, NO.sub.2 R.sub.2 =H, CH.sub.3, C.sub.2 H.sub.5, CH(CH.sub.3).sub.2 ;
R.sub.3 = ##STR2## Where R.sub.4 =H, CH.sub.3, C.sub.2 H.sub.5 R.sub.5 =H, CH.sub.3
X=none O, S, NH, NCH.sub.3, --CH=CH--, --C.ident.C--
Y=O, NH,
both in the racemic Form and in the isomeric enantiomeric forms,
which produce a nootropic effect, i.e. memory enhancement and learning facilitation, as well as an analgesic effect.

REFERENCES:
W. Schultz et al. Eine Neue Methode Zur Technischen Darstellung von Tertiaren etc., Arzneimittel Forschung. Drug Research vol. 26, No. 5A, 1976 Aulendorf De pp. 960-974.
Louis S. Harris et al., Narcotic-Antagonist Analgesics: Interactions With Cholinergic Systems, May 9, 1969, The Journal of Pharmacology and Experimental Therapeutics, vol. 1969, No. 1, pp. 17-22.
A. Bartolini, et al., Antinociception Induced By Systemic Administration of Local Anaesthetics Depends On a Central Cholinergic Mechanism., Br. J. Pharmac (1987), 92, 711-721.
A. Bartolini, et al., Role of Muscarinic Receptor Subtypes in Central Antinociception, Br. J. Pharmacol. (1992) 105, 77-82.
Von W. Schulz, et al., Eine Neue Methode zur technischen Darstellung von tertiaren and quartaren d,1-Tropasaureenstern einiger N-substituieter Northropan-bzw Granatan 3-ole, Arzeneim-Forsch (Drug. Res.) 26, Nr. 5a (1976), 960-974.
J. C. Szerb et al., Release of [.sup.3 H] Acetylcholine From Rat Hippocampal Slices: Effect of Septal Lesion and of Graded Concentrations of Muscarinic Agonists and Antagonists, Brain Resarch, 128 (1977) 285-291.
Roman Pohorecki et al., Effects of Selected Muscarinic Cholinergic Antagonists on [.sup.3 H] Acetylcholine Release From Rat Hippocampal Slices, 1987, The Journal of Pharmacoclogy and Experimental Therapeutics, 1987, vol. 244, No. 1, 213-217.
Paul A. Lapchak, et al., Binding sites for [.sup.3 H] 116 and effect of AF-DX 116 on endogenous acetylcholine release from rat brain slices, Brain Research, 496 (1989) 285-294).
Torocsik et al., Presynaptic Effects Of Methoctramine On Release Of Acetylcholine, 1991, Neuropharmacology, vol. 30, No. 3 pp. 293-298.
J. de Belleroche et al., Dopamine Inhibition of the Release of Endogenous Acetylcholine from Corpus Striatumane Cerebral Cortex In Tissue Sliceds and Synaptosomes: A Presynaptic Response?, 1982, J. Neurochem., vol. 39, No. 1, pp. 217-222.
D. Fage et al., Opposing effects of D-1 and D-2 receptor antagonists on acetylcholine levels in the rat striatum, 1986, European Journal of Pharmacology, 129, pp. 359-362.
D. H. Thor, et al., Social Memory of the Male Laboratory Rat, Journal of Comparative and Physiological Psychology, vol. 96, No. 6, 1000-1006, 1982.
O. Vainio et al., Sedative and analgesic effects of medetomidine in dogs, 1989, J. Vet. Pharmacol Ther. 12, 225-231 (1989).
J. L. Vaught, et al., A Comparison of the Antinociceptive Responses to the Gaba-Receptor Agonists Thip and Baclofen, Neuropharmacology, vol. 24, No. 3, pp. 211-216, 1985.
Daniela Parolaro, et al., Effect of Intracerebroventricular Administration of Morphine Upon Intestinal Motility in Rat and its Antagonism with Naloxone, European Journal of Pharmacology, 46, 1977, 329-338.
L. F. Berhenke, et al., Some Aryloxyaliphatic Acids, 1952, Journal Am. Chem. Soc., 73, 4458.
C. H. Fawcett, et al., Ann Appl. Biol. 43, 342-354 (1955).
D. C. Abbott, et al., Addition and Substitution with the Bromine Cation in Aqueous Solution, J. Chem. Soc. 2934, 1952.
C. A. Bischoff, et al., Berichte, 1900, 33, 1386.
Berndt Sjoberg, Arkiv Kemi 15, 397-401 (1960).
Giancarlo Bettoni, et al., Stereospecificity of the Chloride Ion Channel: The Action of Chiral Clofibric Acid Analogues, J. Med. Chem., 1987, 30, 1267-1270.
A. Berthold, et al., Arnzneim Forsch., 17, 719 (1967).
Friedrich Nerdel, et al., Chem. Ber., 87, 217, 1954.
Bartolini, et al., i.c.v. AFDX-116 induces analgesia only when administered at very low doses, TIPPS Suppl. IV 99 (1989).
Gualtieri, et al., Muscarinic M.sub.1 contrary to M.sub.2 antagonists do not induce analgesia, TIPPS Supp. IV 99 (1989).
C. Ghelardini, et al., Investigation into atropine-induced antinociception, Br. J. Pharmacol. (1990), 101, 49-54.

LandOfFree

Say what you really think

Search LandOfFree.com for the USA inventors and patents. Rate them and share your experience with other people.

Rating

Analgesic and nootropic drugs does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Analgesic and nootropic drugs, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Analgesic and nootropic drugs will most certainly appreciate the feedback.

Rate now

     

Profile ID: LFUS-PAI-O-424452

  Search
All data on this website is collected from public sources. Our data reflects the most accurate information available at the time of publication.