Benzosuberonylpiperdine compounds as analgesics

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United States of America Patent

PATENT NO 7115633
APP PUB NO 20040029917A1
SERIAL NO

10275242

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ATTORNEY / AGENT: (SPONSORED)

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Abstract

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Compounds of formula (I) or a derivative thereof, wherein; R is C.sub.1-6alkyl, C.sub.3-7cycloalkyl, C.sub.1-6alkoxy, hydroxy, halo, C.sub.1-6alkenyl, C.sub.1-6alkynyl, amino, C.sub.1-6alkylamino, di(C.sub.1-6alkyl)amino, hydroxyC.sub.1-6alkyl, C.sub.1-6alkoxyC.sub.1-6alkyl, aminoC.sub.1-6alkyl, (C.sub.1-6alkyl)aminoC.sub.1-6alkyl, di(C.sub.1-6alkyl)aminoC.sub.1-6alkyl; R.sup.1 is hydrogen or R; R.sup.2 is hydroxy, C.sub.1-6alkoxy, amino, C.sub.1-6alkylamino, di(C.sub.1-6alkyl)amino; R.sup.3 is hydrogen or C.sub.1-6alkyl; R.sup.4 and R.sup.5 are each independently selected from the list consisting of perhaloC.sub.1-6alkyl, hydrogen, halo, C.sub.1-6alkyl, C.sub.1-6alkoxy, hydroxy, amino, C.sub.1-6alkylamino, di(C.sub.1-6alkyl)amino, hydroxyC.sub.1-6alkyl, C.sub.1-6alkoxyC.sub.1-6alkyl, aminoC.sub.1-6alkyl, (C.sub.1-6alkyl)aminoC.sub.1-6alkyl, di(C.sub.1-6alkyl)aminoC.sub.1-6alkyl, aryl, and COX wherein X may be hydroxy, C.sub.1-6alkoxy, C.sub.1-6alkyl, amino, C.sub.1-6alkylamino, or di(C.sub.1-6alkyl)amino; with the proviso that, when R.sup.3 is hydrogen, then R.sup.4 and R.sup.5 are not both hydrogen; and wherein any alkyl group or the alkyl moiety of any group containing such a moiety may be substituted one or more times by halo; are ligands of the ORL-1 receptor and are useful in therapy. ##STR00001##

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Patent Owner(s)

Patent OwnerAddress
GLAXOSMITHKLINE S P AVIA ALESSANDRO FLEMING 2 VERONA 37135

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Barlocco, Daniela Milan, IT 3 19
Cignarella, Giorgio Milan, IT 10 82
Giardina, Giuseppe Milan, IT 23 89
Grugni, Mario Milan, IT 40 152
Ronzoni, Silvano Milan, IT 18 85

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