Agents for treating neurodegenerative disorders

a neurodegenerative disorder and agent technology, applied in the field of chemical compounds in medicine, can solve the problems of tacrine side effects, death, and ineffective treatment with tacrine, and achieve the effects of reducing the number of patients

Inactive Publication Date: 2006-06-29
ZEFIROV N S +10
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the treatment with tacrine is not always effective.
Besides, tacrine tends to cause undesirable side-effects.
As a result, the glutamate mediator at concentrations that are nontoxic under normal conditions becomes toxic for neurones under conditions of the developing β-amyloid dose and causes their death.
The main disadvantage of AP5 compound a side neurotoxic effect (such as the disturbance of coordination of movement and a sedative effect) which becomes apparent when AP5 is used in the doses in which it produces anti-NMDA effect (ED50=190 mg / kg) (Grigoriev et al., Chim. Pharm. Journal, 1988, No. 3, p.
However, to date such agents have not been available in clinics.

Method used

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  • Agents for treating neurodegenerative disorders
  • Agents for treating neurodegenerative disorders
  • Agents for treating neurodegenerative disorders

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examples

I. Anti-NMDA Activity of the Compounds Provided by the Present Invention

[0060] The experiment was conducted in white non-inbred male mice of 20-24 g of weight. A solution of the test agent in 0.2 ml of 5% aqueous dimethylsulfoxide was injected intraperitoneally 40 minutes before the injection of NMDA into the lateral vehicle of the brain. For the mice that had been prepared beforehand for the experiment a skin flap on the head of each mouse was removed under ether anestesia and a hole was bored in the skull by a fine drill. NMDA (0.1 μg) in a volume of 1.4 μl was injected with a microsyringe. The microsyringe needle was immersed to a depth of 2.5 mm. After the operation, the wound was treated with a 2% novocaine solution. After recovery from the anestesia, the mice showed signs of pain disturbance. The accuracy of NMDA injection was monitored by injection of methylene blue. Two to 4 hours after the operation, the mice were used for a pharmacological experiment.

[0061] The animals ...

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Abstract

Compounds and methods of using these compounds to treat neurodegenerative diseases, especially Alzheimer's disease, are provided. The compounds that are provided for the treatment of neurodegenerative diseases can be represented by a general formula (I): wherein R1 is Me, Et or PhCH2; R2 is H, PhCH2 or 6-Me-3-Py-(CH2)2; and R3 is H, Me or Br. The solid line accompanied by the dotted line i.e. represents a single or double bond and salts thereof with pharmacologically acceptable acids and quaternary derivatives.

Description

BACKGROUND OF THE INVENTION [0001] 1. Field of the Invention [0002] The present invention relates to the use of chemical compounds in medicine, more specifically, to the use of the compounds selected from hydrogenated pyrido[4,3-b]indoles for the treatment of neurodegenerative diseases, and especially Alzheimer's disease (AD), due to the discovery of new properties intrinsic to these compounds. [0003] 2. Description of the Related Art [0004] Alzheimer's disease is currently one of the severest and widely spread neurodegenerative diseases. The most traditional approach to the treatment of this disease is compensatory therapy based on the compensation of the cholinergic system functions which are reduced in Alzheimer's disease. One of the therapeutic agents used in the alleged method of treatment is tacrine hydrochloride (hereinafter referred to as tacrine) which is 9-amino-1,2,3,4-tetrahydroacridine hydrochloride represented by the formula (A): [0005] The mechanism of action of the ...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K49/00A61K31/437A61P25/28
CPCA61K31/437A61K49/006A61P25/28
Inventor ZEFIROV, NIKOLAI S.AFANASIEV, ANDREI Z.AFANASIEVA, SVETLANA V.BACHURIN, SERGEI O.TKACHENKO, SERGEI E.GRIGORIEV, VLADIMIR V.JUROVSKAYA, MARINA A.CHETVERIKOV, VALERY P.BUKATINA, ELIZAVETA E.GRIGORIEVA, IRINA V.
Owner ZEFIROV N S
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