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Aminoindan derivatives

a technology of aminoindan and derivatives, applied in the field of compounds, can solve the problem of weak active compound only

Inactive Publication Date: 2007-05-08
YISSUM RES DEV CO OF THE HEBREWUNIVERSITY OF JERUSALEM LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Furthermore, the compound is only very weakly active as a MAO-A inhibitor.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

example 1

Acetylcholinesterase Inhibition in Mice

[0090]1.1 In vitro measurement of Acetylcholinesterase (AChE) Inhibition

[0091]Human erythrocyte acetylcholinesterase (type XIII, Sigma Israel), was prepared in a stock solution of 1 U / ml, containing Triton (1%) and bovine serum albumin (0.05%) in phosphate buffer (pH 8). The enzyme (0.05U) was incubated with 3-5 different concentrations of test compound (in triplicate) for periods of from 15 to 60 minutes at 37° C. The substrate acetylthiocholine (0.075M) and 5,5′-dithiobis-(2-nitrobenzoic acid) (DTNB, 0.01M) were then added and the rate of hydrolysis of the substrate which yields a yellow product monitored spectrophotomerically at 412 nM (Ellman et al., Biochem Pharmacol. (1961) 7: 88-95). The percentage inhibition of AChE by each concentration of drug is calculated by comparison with that of enzyme in the absence of drug. The concentration of each drug that inhibits AChE by 50% (IC50) at the time of peak activity was calculated and is given i...

example 2

[0096]2.1 Inhibition of MAC activity in vitro

[0097]The MAO enzyme source was a homogenate of rat brain in 0.3M sucrose, which was centrifuged at 600 g for 15 minutes. The supernatant was diluted appropriately in 0.05M phosphate buffer, and pre-incubated with serial dilutions of test compounds for 20 minutes at 37° C. 14C-Labeled substrates (2-phenylethylamine, hereinafter PEA; 5-hydroxytryptamine, hereinafter 5-HT) were then added, and the incubation continued for a further 20 minutes (PEA), or 30-45 minutes (5-HT). Substrate concentrations used were 50 μM (PEA) and 1 mM (5-HT). In the case of PEA, enzyme concentration was chosen so that not more than 10% of the substrate was metabolized during the course of the reaction. Deaminated products were extracted into toluene-ethyl acetate (1:1 v / v) containing 0.6% (w / v) 2,5-diphenyloxazole (ppo) prior to determination by liquid scintillation counting. Radioactivity n the eluate indicates the production of neutral and acidic metabolites fo...

example 3

Effect of Drug Treatment Following Closed Head Injury (CHI) in Mice

[0105]The procedure for closed head injury followed was as described for rats in Shohami, et al. (J Neurotrauma (1993) 10 (2): 109-119) with changes as described.

[0106]Animals: Male Sabra mice (Hebrew University strain) weighing 34-40 g were used. They were housed in groups of 10 per cage, in a 12 hr:12 hr light:dark cycle. Food and water were provided ad libitium.

[0107]Trauma was induced under ether anesthesia. A longitudinal incision was performed in the skin covering the skull and the skin retracted to expose the skull. The head was fixed manually at the lower plane of the impact apparatus. A weight of 333 g was delivered by an electric device from a distance of 3 cm to the left hemisphere, 1-2 mm lateral to the midline in the midcoronal plane. Test compounds were injected sub-cutaneously at a dosage corresponding to the ED50 acetylcholinesterase, once 15 min. after CHI.

[0108]3.1 Assessment of Motor Function

[0109]...

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Abstract

This invention is directed to compounds of the following formula: wherein when a is 0, b is 1 or 2; when a is 1, b is 1, m is from 0-3, X is O or S, Y is halogeno, R1 is hydrogen C1-4 alkyl, R2 is hydrogen, C1-4 alkyl, or optionally substituted propargyl and R3 and R4 are each independently hydrogen, C1-6 alkyl, C6-12 aryl, C6-12 aralkyl each optionally substituted.This invention is also directed to the use of these compounds for treating depression, Attention Deficit Disorder (ADD), Attention Deficit and Hyperactivity Disorder (ADHD), Tourette's Syndrome, Alzheimer's Disease and other dementia's such as senile dementia, dementia of the Parkinson's type, vascular dementia and Lewy body dementia.This invention is further directed to a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.

Description

[0001]This application is a continuation of U.S. Ser. No. 09 / 336,493, filed Jun. 18, 1999, a continuation of PCT International Application No. PCT / US97 / 24155, filed Dec. 18, 1997, designating the United States of America and claiming priority of Israeli Patent Application Nos. 119853, filed Dec. 18, 1996 and 120510, filed Mar. 24, 1997, the contents of which are hereby incorporated by reference.FIELD OF INVENTION[0002]The present invention relates to novel compounds, pharmaceutical compositions containing said compounds and their use in the treatment of various CNS disorders.BACKGROUND OF THE INVENTION[0003]Dementia exists in several forms including static dementia, Alzheimer's-type dementia, senile dementia, pre-senile dementia and progressive dementia. One of the common pathological features of several types of dementia is the lack of the neurotransmitter acetylcholine. This has led to the development of acetylcholine esterase inhibitors for use in the treatment of dementias such ...

Claims

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Application Information

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Patent Type & Authority Patents(United States)
IPC IPC(8): A61K31/27A61P25/28A01N47/10A61K31/325A61P25/00C07C261/00C07C271/24C07C271/42C07C271/44C07C271/56C07C271/58C07C333/04C07C333/06C07C333/08
CPCC07C271/24C07C271/44C07C271/56C07C271/58C07C333/04C07C2601/14C07C2602/08C07C2602/10A61P25/00A61P25/28
Inventor CHOREV, MICHAELGOREN, TAMARHERZIG, YACOVSTERLING, JEFFREYWEINSTOCK-ROSIN, MARTAYOUDIM, MOUSSA B. H.
Owner YISSUM RES DEV CO OF THE HEBREWUNIVERSITY OF JERUSALEM LTD
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