ECSP099377A - AMIDAS OF SELECTIVE DIAZABICICLOALCANS OF THE SUBTIPO OF THE NICOTINIC RECEIVER OF ACETILCOLINA - Google Patents

AMIDAS OF SELECTIVE DIAZABICICLOALCANS OF THE SUBTIPO OF THE NICOTINIC RECEIVER OF ACETILCOLINA

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Publication number
ECSP099377A
ECSP099377A ECSP099377A ECSP099377A EC SP099377 A ECSP099377 A EC SP099377A EC SP099377 A ECSP099377 A EC SP099377A EC SP099377 A ECSP099377 A EC SP099377A
Authority
EC
Ecuador
Prior art keywords
compounds
effects
significant
nicotinic receptors
subtipo
Prior art date
Application number
Other languages
Spanish (es)
Inventor
Anatoly Mazurov
Lan Miao
Yun-De Xiao
Philip S Hammond
Craig H Miller
Srinivisa Rao Akireddy
V Srinivasa Murthy
Regina C Whitaker
Scott R Breining
Matt S Melvin
Original Assignee
Targacept Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Targacept Inc filed Critical Targacept Inc
Publication of ECSP099377A publication Critical patent/ECSP099377A/en

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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Se describen compuestos, composiciones farmacéuticas que incluyen los compuestos, y métodos de preparación y uso de los mismos. Los compuestos son compuestos amida que se pueden preparar a partir de ciertos ácido heteoraril carboxílicos y ciertos diazabicicloalcanos. Los compuestos exhiben selectividad para, y unión con alta afinidad con, receptores nicotínicos neuronales del subtipo a4ß2 en el sistema nervioso central (SNC). Se pueden utilizar los compuestos y composiciones para tratar y/o evitar una amplia variedad de afecciones o trastornos, particularmente trastornos del SNC. Los compuestos pueden: (i) alterar el número de receptores nicotínicos colinérgicos del cerebro del paciente, (ii) exhibir efectos neuroprotectores, y (iii) cuando se emplean en cantidades efectivas, no resultan en efectos colaterales adversos apreciables (por ejemplo efectos colaterales tales como incrementos significativos en la presión sanguínea y frecuencia cardiaca, efectos negativos significativos sobre el tracto gastrointestinal, y efectos significativos sobre el sistema músculo esquelético).Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are described. The compounds are amide compounds that can be prepared from certain heteroaryl carboxylic acids and certain diazabicycloalkanes. The compounds exhibit selectivity for, and binding with high affinity with, neuronal nicotinic receptors of the a4β2 subtype in the central nervous system (CNS). The compounds and compositions can be used to treat and / or avoid a wide variety of conditions or disorders, particularly CNS disorders. The compounds may: (i) alter the number of cholinergic nicotinic receptors in the patient's brain, (ii) exhibit neuroprotective effects, and (iii) when used in effective amounts, do not result in appreciable adverse side effects (for example side effects such such as significant increases in blood pressure and heart rate, significant negative effects on the gastrointestinal tract, and significant effects on the skeletal muscle system).

ECSP099377 2006-11-02 2009-06-01 AMIDAS OF SELECTIVE DIAZABICICLOALCANS OF THE SUBTIPO OF THE NICOTINIC RECEIVER OF ACETILCOLINA ECSP099377A (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US58607906P 2006-11-02 2006-11-02

Publications (1)

Publication Number Publication Date
ECSP099377A true ECSP099377A (en) 2009-07-31

Family

ID=41087117

Family Applications (1)

Application Number Title Priority Date Filing Date
ECSP099377 ECSP099377A (en) 2006-11-02 2009-06-01 AMIDAS OF SELECTIVE DIAZABICICLOALCANS OF THE SUBTIPO OF THE NICOTINIC RECEIVER OF ACETILCOLINA

Country Status (1)

Country Link
EC (1) ECSP099377A (en)

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