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filingDate 2004-10-07-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_73a326ebaa26768377d908b398975b6e
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_ad0dd991d74d965662381a2fbec240e3
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publicationDate 2005-11-23-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber AR-046056-A1
titleOfInvention DERIVATIVES OF THIOPHEN-2-CARBOXAMIDE AND ITS USE AS ANTAGONISTS OF CB1 CANABINOID RECEPTORS
abstract This refers to thiophene-2-carboxamide derivatives and their use as antagonists of CB1 cannabinoid receptors. Procedure for preparation and therapeutic application. Claim 1: Compound that responds to formula (1) in which R 1 represents H or a C 1-4 alkyl; R2 represents a C4-10 alkyl group, a C3-12 non-aromatic carbocyclic radical, not substituted once or several times by a C1-4 alkyl, C1-4 alkoxy or hydroxyl group; a 1,2,3,4-tetrahydronaphthyl-1- or -2; a monooxygenated or mono-sulfur, saturated heterocyclic radical of 5 to 7 atoms, unsubstituted or substituted once or several times by a C1-4 alkyl group; a mononitrogenated, saturated heterocyclic radical of 5 to 7 atoms, where the N atom is substituted by a C1-4 alkyl, phenyl, benzyl, C1-4 alkoxycarbonyl or C1-4 alkanoyl group; a C1-3 alkylene group bearing a C3-10 non-aromatic carbocyclic radical unsubstituted or substituted once or several times by a C1-4 alkyl group; a phenylalkylene group in which the alkylene is C1-3, unsubstituted or substituted in the alkylene by one or more methyl groups, and / or substituted in the phenyl by one or more identical or different substituents chosen from a halogen atom or a C1-4 alkyl group, trifluoromethyl, C1-4 alkoxy, trifluoromethoxy; a methylene substituted by a benzothienyl, benzofuryl, thienyl, or furyl radical, and said radicals are unsubstituted or substituted by one or more C1-4 alkyl groups; an NR9R10 group; or R1 and R2 together with the N atom to which they are attached constitute either a piperazin-1-yl or 1,4-diazepan-1-yl radical substituted in 4- by a phenyl or benzyl group, or a radical piperidin-1-yl or pyrrolidin-1-yl mono- or gem- substituted by a phenyl, benzyl, C1-4 alkyl, hydroxy, C1-4 alkoxy, cyano, C1-3 alkanoyl, C1-4 alkoxycarbonylamino, C1 alkanoylamino -3; the phenyl or benzyl groups are unsubstituted or substituted once or several times by a halogen atom and / or a C1-4 alkyl and / or C1-4 alkoxy group, and / or trifluoromethyl; R3, R4, R5, R6, R7, R8 each independently represent each other an H or halogen atom, a C1-6 alkyl group, C1-6 alkoxy, trifluoromethyl or an S (O) nAlk group; R9 represents an H atom or a methyl group; R10 represents a 1-6 alkyl, phenyl or C3-10 cycloalkyl group, and the phenyl and cycloalkyl groups are unsubstituted or substituted by one or more halogen atoms and / or C1-4 alkyl groups; or R9 and R10 together with the N atom to which they are attached, constitute a heterocyclic radical, saturated or unsaturated, of 5 to 11 atoms, bridged or not, which comprises or not a spherical C and that contains, or not, a second heteroatom chosen from O or N, and said radical is unsubstituted or substituted by a hydroxyl or phenyl group or once or several times by a C1-4 alkyl and / or C1-4 alkoxy group; R11 represents an H atom, a C1-4 alkyl or C3-7 cycloalkyl group; n represents 0, 1 or 2; Alk represents a C1-4 alkyl group; in a state of base or of addition salts with an acid, as well as in a state of hydrate or solvate.
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