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Compounds capable of activating cholinergic receptors

a technology compounds, which is applied in the direction of heterocyclic compound active ingredients, drug compositions, biocides, etc., can solve the problems of not providing significant side effects, and achieve the effects of increasing the number of nicotinic cholinergic receptors of the brain of the patient, preventing and suppressing symptoms, and increasing blood pressure and heart ra

Inactive Publication Date: 2010-06-24
TARGACEPT INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

"The present invention relates to new compounds called aryl substituted olefinic amine compounds, which can be used to treat various conditions and disorders involving dysfunction of nicotinic cholinergic neurotransmission. These compounds can interact with relevant nicotinic receptor sites and exhibit nicotinic pharmacology, elicit neurotransmitter secretion, and have the potential to increase the number of nicotinic cholinergic receptors of the brain. The pharmaceutical compositions of the present invention are safe and effective with regards to prevention and treatment of a wide variety of conditions and disorders."

Problems solved by technology

It would be highly beneficial to provide individuals suffering from certain disorders (e.g., CNS diseases) with interruption of the symptoms of those disorders by the administration of a pharmaceutical composition containing an active ingredient having nicotinic pharmacology and which has a beneficial effect (e.g., upon the functioning of the CNS), but which does not provide any significant associated side effects.

Method used

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  • Compounds capable of activating cholinergic receptors
  • Compounds capable of activating cholinergic receptors
  • Compounds capable of activating cholinergic receptors

Examples

Experimental program
Comparison scheme
Effect test

example 1

Determination of Log P Value

[0038]Log P values, which have been used to assess the relative abilities of compounds to pass across the blood-brain barrier (Hansch, et al., J. Med. Chem. ii:1 (1968)), were calculated using the Cerius2 software package Version 3.5 by Molecular Simulations, Inc.

example 2

Determination of Binding to Relevant Receptor Sites

[0039]Binding of the compounds to relevant receptor sites was determined in accordance with the techniques described in U.S. Pat. No. 5,597,919 to Dull et al. Inhibition constants (Ki values), reported in nM, were calculated from the IC50 values using the method of Cheng et al., Biochem, Pharmacol. 22:3099 (1973).

example 3

Determination of Dopamine Release

[0040]Dopamine release was measured using the techniques described in U.S. Pat. No. 5,597,919 to Dull et al. Release is expressed as a percentage of release obtained with a concentration of (S)-(−)-nicotine resulting in maximal effects. Reported EC50 values are expressed in nM, and Emax values represent the amount released relative to (S)-(−)-nicotine on a percentage basis.

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PUM

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Abstract

Compounds incorporating aryl substituted olefinic amine are provided. Representative compounds are (4E)-N-methyl-5-(3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-pyrimidinyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-methoxy-3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(6-amino-5-methyl-3-pyridyl)-4-penten-2-amine, (2R)-(4E)-N-methyl-5-(3-pyridyl)-4-penten-2-amine, (2R)-(4E)-N-methyl-5-(5-isopropoxy-3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-bromo-3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-ethoxy-3-pyridyl)-4-penten-2-amine, (2S)-(4E)-N-methyl-5-(3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-isopropoxy-3-pyridyl)-4-penten-2-amine and (2S)-(4E)-N-methyl-5-(5-isopropoxy-3-pyridyl)-4-penten-2-amine.

Description

RELATED APPLICATIONS[0001]This application is a continuation of U.S. application Ser. No. 11 / 932,895, filed Oct. 31, 2007; which is a continuation of U.S. application Ser. No. 11 / 379,443, filed Apr. 20, 2006 (now U.S. Pat. No. 7,307,092); which is a continuation of U.S. application Ser. No. 11 / 181,055, filed Jul. 14, 2005 (now U.S. Pat. No. 7,060,826); which is a continuation of U.S. application Ser. No. 11 / 048,212, filed Feb. 1, 2005 (abandoned); which is a continuation of U.S. application Ser. No. 09 / 522,117 filed Mar. 9, 2000 (abandoned); which is a continuation of U.S. application Ser. No. 09 / 098,285, filed Jun. 16, 1998 (abandoned), the disclosures of which are incorporated herein by reference in their entirety.BACKGROUND OF THE INVENTION[0002]The present invention relates to compounds capable of activating nicotinic cholinergic receptors, for example, as agonists of specific nicotinic receptor subtypes.[0003]Nicotine has been proposed to have a number of pharmacological effect...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/44C07D213/24C07D213/63A61P25/28A61K31/505C07D213/38C07D213/61C07D213/65C07D213/73C07D239/26
CPCA61K31/44A61K31/505C07D213/38C07D239/26C07D213/65C07D213/73C07D213/61A61P25/00A61P25/14A61P25/16A61P25/18A61P25/28
Inventor CALDWELL, WILLIAM SCOTTDULL, GARY MAURICEBHATTI, BALWINDER SINGHHADIMANI, SRISHAILKUMAR B.PARK, HAEILWAGNER, JARED MILLERCROOKS, PETER ANTHONY
Owner TARGACEPT INC
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