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Anti-epileptogenic agents

A technology of epilepsy and compounds, applied in the field of anti-epileptic agents, can solve problems such as no epilepsy

Inactive Publication Date: 2006-05-17
QUEENS UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Thus, while many drugs are available for the treatment of epilepsy (i.e., by inhibiting the convulsive effects associated with seizures), there is no universally accepted drug for the treatment of the pathological changes that characterize epilepsy
There is also no generally accepted method of inhibiting the epileptogenic process and no drugs recognized as anti-epileptogenic

Method used

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preparation example Construction

[0237] The preparation method of III.β-amino anion compound

[0238] The invention also provides a preparation method of the β-amino anion compound.

[0239] In one embodiment, the present invention includes a process for the preparation of a β-amino anionic compound represented by the following formula (Formula VI):

[0240] or

[0241] Formula VI

[0242] Wherein the dashed line represents an optional single / double bond (E- or Z-configuration); R 2 and R 3 each independently hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, alkylcarbonyl, arylcarbonyl, alkoxycarbonyl, or aryloxycarbonyl; or R 2 and R 3 Joined with the attached nitrogen to form an unsubstituted or substituted heterocyclic ring with 3-7 atoms in the heterocyclic ring; R 4 and R 5 each independently hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, alkylcarbonyl, arylcarbonyl, alkoxycarbonyl, aryloxycarbonyl, amino, hydroxyl, cyano, alkoxy, aryl Oxy, carboxy, alkoxyca...

Embodiment 1

[0279] Example 1: Identification of Compounds Based on Pharmacophore Models

[0280] A pharmacophore model was developed incorporating the structural parameters and properties of two different classes of compounds: (1) GABA uptake receptor inhibitors, and (2) NMDA receptor co-antagonists.

[0281] Previous models (Murali Dhar et al. (1994) J. Med. Hem. 37: 2334, Falch and Krogsgaard-Larson (1991) Eur. J. Med. Chem. 26: 69, N'Goka (1991) J. Med.Chem 34:2547) suggests that GABA absorption inhibitors should include:

[0282] i) Amine functionality (preferably secondary amine)

[0283] ii) Carboxyl functional group

[0284] iii) lipophilic groups, preferably aromatic

[0285] iv) Electron-rich functional group (double bond or oxygen) located between amine and lipophilic group

[0286] v) Two-carbon chain length between amine functional group and double bond or oxygen atom

[0287] Other previous models for antagonists of the glycine co-agonist site of the NMDA receptor comple...

Embodiment 2

[0302] Example 2: In vivo evaluation of the pharmacological efficacy of candidate compounds for inhibiting epileptogenesis

[0303] The anti-seizure activity and neurotoxicity of two sets of candidate analogs were tested in vivo. A seizure model was established using adult male Sprague-Dawley rats following the guidelines of the Canada Council on Animal Care and under the supervision of the Queen's University Animal Ethics Committee. This protocol has been adopted from previous work by Turski et al. (1984) Brain Res. 321:237. Test compounds were administered by intraperitoneal (i.p.) injection at a dose of 100 mg / kg. Seizures were induced 20 minutes after i.p. administration of pilocarpine hydrochloride (350 mg / kg). Protection was defined as the absence of chronic convulsions during the 30-minute observation period following pilocarpine administration. Using this assay, compounds 1, 2, 3, 5, 8, 10, 11, 13, A1, A4, A5, A11, A13, A14, A15, A16, A21, A26, A28, A29 and A31 exhi...

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Abstract

Methods and compounds useful for inhibiting convulsive disorders, including epilepsy, are disclosed. The methods and compounds of the invention inhibit or prevent seizure onset and / or epileptogenesis. The present invention also describes processes for the preparation of the compounds of the invention.

Description

[0001] related application [0002] The application to which this application claims priority is U.S. Patent Application No. 60 / 275,618, filed March 13, 2001; Other material is referred to and disclosed in addition to US Patent Application No. 6,306,909, now US Patent No. 6,306,909, both of which are fully incorporated herein by reference. Background of the invention [0003] Epilepsy is a serious neurological disorder associated with seizures that affects hundreds of thousands of people worldwide. Clinically, seizures are caused by sudden discharges of collections of neurons in the brain. The resulting nerve cell activity manifests itself in symptoms such as uncontrolled movements. [0004] A seizure is a single discrete clinical event resulting from the excessive firing of clusters of neurons through a process known as "ictogengsis." Therefore, seizures are only a symptom of epilepsy. Epilepsy is a dynamic, often progressive process characterized by an underlying continu...

Claims

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Application Information

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IPC IPC(8): G01N33/566A61K31/165G01N33/68A61K31/195A61K31/196A61K31/197A61K31/215A61K31/216A61K31/22A61K31/277A61K45/00A61P9/00A61P9/10A61P21/02A61P25/00A61P25/02A61P25/08A61P25/14A61P25/18A61P25/22A61P25/28A61P29/00A61P31/18A61P35/00A61P37/04A61P43/00C07D239/54C07D239/553C07D239/557C07D239/96C07D405/04C07D473/06C07D491/04C07K5/06G01N33/58G01N33/94
CPCA61K31/195C07D239/54C07D239/553C07D239/557C07D239/96C07D405/04C07D473/06C07D491/04G01N33/6896G01N33/9406G01N2500/00A61P21/02A61P25/00A61P25/02A61P25/08A61P25/14A61P25/18A61P25/22A61P25/28A61P29/00A61P31/18A61P35/00A61P37/04A61P43/00A61P9/00A61P9/10
Inventor D·F·韦弗C·Y·K·谭S·T·金X·孔L·魏J·R·卡兰
Owner QUEENS UNIV
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