DERIVADOS DE 2,5-DIHIDRO-3-H-PIRAZOLO[4,3-C]PIRIDAZIN-3-ONA SUSTITUIDOS COMO ANTAGONISTAS DE LOS RECEPTORES CB1

SE REFIERE A DERIVADOS DE 2,5-DIHIDRO-3-H-PIRAZOLO[4,3-C]PIRIDAZIN-3-ONA SUSTITUIDOS DE FORMULA (I), EN DONDE R1 ES UN ALQUILO(C1-C12), CARBOCICLO NO AROMATICO(C3-C12), FENILO, PIRROLILO, ENTRE OTROS; R2 Y R3 SON INDEPENDIENTEMENTE FENILO SUSTITUIDO O NO POR HALOGENO, HIDROXI, -O(CH2)mR5, ENTRE OTRO...

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Hauptverfasser: DOS SANTOS VICTOR, ROUQUETTE ARNAUD, RINALDI-CARMONA MURIELLE, CONGY CHRISTIAN, VAN BROECK DIDIER
Format: Patent
Sprache:spa
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Zusammenfassung:SE REFIERE A DERIVADOS DE 2,5-DIHIDRO-3-H-PIRAZOLO[4,3-C]PIRIDAZIN-3-ONA SUSTITUIDOS DE FORMULA (I), EN DONDE R1 ES UN ALQUILO(C1-C12), CARBOCICLO NO AROMATICO(C3-C12), FENILO, PIRROLILO, ENTRE OTROS; R2 Y R3 SON INDEPENDIENTEMENTE FENILO SUSTITUIDO O NO POR HALOGENO, HIDROXI, -O(CH2)mR5, ENTRE OTROS; R4 ES H, ALQUILO(C1-C4), ALCOXI(C1-C4) O HIDROXI; R5 ES -NR7R8 O -SAlk. SON SELECCIONADOS: 5-(4-CLOROFENIL)-6-(2,4-DICLOROFENIL)-2-(4-ISOPROPILBENCIL)-2,5-DIHIDRO-3H-PIRAZOLO[4,3-c]PIRIDAZIN-3-ONA, N-{2-[(3-CLORO-4-{5-[4-(METILTIO)FENIL]-3-OXO-2-[4-(TRIFLUORO-METIL)BENCIL]-3,5-DIHIDRO-2H-PIRAZOLO[4,3-c]PIRIDAZIN-6-IL}FENIL)TIO]ETIL}CICLO-PROPANOCARBOXAMIDA, ENTRE OTROS. SE REFIERE TAMBIEN A UN PROCEDIMIENTO DE PREPARACION Y COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON UTILES EN EL TRATAMIENTO O PREVENCION DE ENFERMEDADES LIGADAS A LOS RECEPTORES DE CANNABINOIDES CB1, TALES COMO TRASTORNOS DE PSIQUIATRICOS Y/O NEURODEGENERATIVOS Pyrazolopyridazinone compounds (I), and their addition salts, hydrates and solvates are new. Pyrazolopyridazinone compounds of formula (I), and their addition salts, hydrates and solvates are new. R 11-12C alkyl (optionally substituted by F), non-aromatic 3-12C carbocyclic (optionally substituted by 1-4C alkyl, 1-4C alkoxy, F, OH, CF 3, OCF 3 or 1-4C alkylthio), phenyl (optionally substituted by halo, OH, Alk, -OAlk, methylenedioxy, -CH 2-NHAlk, -CH 2N(Alk) 2, CN, NO 2, S(O) nAlk, OS(O) nAlk, 1-4C alkylcarbonyl, 1-4C alkoxycarbonyl or phenyl, phenoxy, pyrrolyl, imidazolyl, pyridyl, pyrazolyl, oxazolyl, thiazolyl, triazolyl or thiadiazolyl, optionally substituted by 1-4C alkyl), benzyl (optionally substituted on phenyl by halo, Alk, OH, OAlk, methylenedioxy, S(O) nAlk or -OS(O) nAlk), phenethyl (optionally substituted on phenyl by halo, 1-4C alkyl, 1-4C alkoxy, CF 3 or OCF 3), benzhydryl, benzhydrylmethyl, heterocyclic aromatic comprising pyrrolyl, imidazolyl, furyl, thienyl, pyrazolyl, oxazolyl, pyridyl, indolyl, benzothienyl or thieno[3,2-b]thienyl, optionally substituted by halo, Alk, OAlk, CN, NO 2 or -S(O) nAlk; R 2phenyl (optionally substituted by halo, OH, Alk, OAlk, -S(O) nAlk or -OS(O) nAlk); R 3phenyl (optionally substituted by halo, OH, Alk, OAlk, -S(O) nAlk or OS(O) nAlk); R 4H, 1-4C alkyl, 1-4C alkoxy or OH; n : 0-2; and Alk : 1-4C alkyl (optionally substituted by F). Independent claims are included for: (1) the preparation of (I); and (2) pyrazolopyridazinone compound of formula (II). ACTIVITY : Neuroleptic; Nootropic;