5, 6-diaryl-pyrazine-2-amide derivatives as CB.sub.1 antagonists

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United States of America Patent

PATENT NO 7342019
APP PUB NO 20050032808A1
SERIAL NO

10499054

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ATTORNEY / AGENT: (SPONSORED)

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Abstract

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The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts, prodrugs, solvates and crystalline forms thereof, in which R.sup.1 and R.sup.2 independently represent: a C.sub.1-6alkyl group; an optionally substituted (amino)C.sub.1-4alkyl-group; an optionally substituted non-aromatic C.sub.3-15carbocyclic group; a (C.sub.3-12cycloalkyl)C.sub.1-3alkyl-group; a group --(CH.sub.2).sub.r(phenyl).sub.s in which r is 0, 1, 2, 3 or 4, s is 1 when r is 0 otherwise s is 1 or 2 and the phenyl groups are optionally independently substituted by Z; naphthyl; anthracenyl; an optionally substituted saturated 5 to 8 membered heterocyclic group containing one nitrogen and optionally one of the following: oxygen, sulphur or an additional nitrogen; 1-adamantylmethyl; a group --(CH.sub.2).sub.t Het in which t is 0, 1, 2, 3 or 4, and the alkylene chain is optionally substituted and Het represents an optionally substituted aromatic heterocycle; or R.sup.1 represents H and R.sup.2 is as defined above; or R.sup.1 and R.sup.2 together with the nitrogen atom to which they are attached represent a saturated optionally substituted 5 to 8 membered heterocyclic group as defined above; X is CO or SO.sub.2; Y is absent or represents NH optionally substitututed by a C.sub.1-3alkyl group; R.sup.3 and R.sup.4 independently represent phenyl, thienyl or pyridyl substituted by Z; Z represents a C.sub.1-3alkyl group, a C.sub.1-3alkoxy group, hydroxy, halo, trifluoromethyl, trifluoromethylthio, trifluoromethoxy, trifluoromethylsulphonyl, nitro, amino, mono or di C.sub.1-3alkylamino, mono or di C.sub.1-3alkylamido, C.sub.1-3alkylsulphonyl, C.sub.1-3alkoxycarbonyl, carboxy, cyano, carbamoyl, mono or di C.sub.1-3alkyl carbamoyl, sulphamoyl and acetyl; and R.sup.5 is H, a C.sub.1-3alkyl group, a C.sub.1-3alkoxymethyl group, trifluoromethyl, a hydroxyC.sub.1-3alkyl group, C.sub.1-3alkoxycarbonyl, carboxy, cyano, carbamoyl, mono or di C.sub.1-3alkylcarbamoyl, acetyl, or hydrazinocarbonyl of formula --CONHNR.sup.aR.sup.b; with the provisos; and processes for preparing such compounds, their use in the treatment of obesity, psychiatric and neurological disorders, to methods for their therapeutic use and to pharmaceutical compositions containing them.

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Patent Owner(s)

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ASTRAZENECA ABSE-151 85 SÖDERTÄLJE SWEDEN

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Berggren, Anna Ingrid Kristina Molndal, SE 8 3
Bostrom, Stig Jonas Molndal, SE 5 222
Elebring, Stig Thomas Molndal, SE 4 4
Greasley, Peter Molndal, SE 12 7
Terricabras, Emma Molndal, SE 2 2
Wilstermann, Johan Michael Molndal, SE 3 2

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