Abstract:
Compounds of formula (I): in which: R 1 is an alkyl, cycloalkyl or cycloalkylalkyl group, R 2 and R 3 form, together with the nitrogen atom which bears them, a heterocycle comprising from 5 to 8 ring members, and n is 2 to 6; medicaments.
Abstract:
Compounds of formula (I): in which: R1 is an alkyl, cycloalkyl or cycloalkylalkyl group, R2 and R3 form, together with the nitrogen atom which bears them, a heterocycle comprising from 5 to 8 ring members, and n is 2 to 6; medicaments.
Abstract:
The invention relates to compounds of formula (I), in which: R is an alkyl, cycloalkyl or cycloalkylalkyl group, R is a linear or branched (C 1 -C 6 ) alkyl group, and n is 1 to 6, and to the use thereof for the treatment of disorders in the melatoninergic system, such as sleep disorders, stress, anxiety, cardiovascular pathologies, etc..
Abstract:
COMPOSÉS DE FORMULE (I), DANS LAQUELLE R1 REPRÉSENTE UN GROUPEMENT ALKYLE, CYCLOALKYLE, OU CYCLOALKYLALKYLE; R2 REPRÉSENTE UN GROUPEMENT ALKYLE (C1-C6) LINÉAIRE OU RAMIFIÉ; ET N REPRÉSENTE 1 À 6, ET LEUR UTILISATION POUR TRAITER LES TROUBLES DU SYSTÈME MÉLATONINERGIQUE TELS QUE LES TROUBLES DU SOMMEIL, LE STRESS, L'ANXIÉTÉ, LES PATHOLOGIES CARDIOVASCULAIRES, ETC.
Abstract:
Naphthalenic derivatives (I) and their enantiomers, diastereoisomer or additive salts of acid or base, are new. Naphthalenic derivatives of formula (I) and their enantiomers, diastereoisomer or additive salts of acid or base, are new. R 1R 4or NHR 4; R 41-6C (halo)alkyl, 1-6C alkenyl, polyhalo(1-6C)alkyl, 3-8C cycloalkyl, 3-8C cycloalkyl(1-6C)alkyl, aryl, aryl(1-6C)alkyl, heteroaryl or heteroaryl(1-6C)alkyl; R 21-6C alkyl substituted 1-6C alkoxy, OH, OSO 2CH 3, N 3, NRR1a, NHCOR1b or NHSO 2R1b; either R, R1a : H or 1-6C alkyl, 3-8C cycloalkyl, aryl or aryl(1-6C)alkyl; or NRR1a : 5-6 membered ring having another heteroatom e.g. N, O or S; R1b : R; and R 3H, halo, 1-6C alkyl or 1-6C alkenyl. Provided that: when R 1is methyl and R 2is hydroxymethyl, then R 3is not hydrogen; the aryl is phenyl, naphthyl or biphenyl; and the heteroaryl is mono or bicyclic heteroaryl with 1-3 heteroatoms e.g. oxygen, sulfur and nitrogen. An independent claim is included for the preparation of (I). [Image] ACTIVITY : Hypnotic; Tranquilizer; Antidepressant; Cardiovascular-Gen; Gastrointestinal-Gen; Muscular-Gen; CNS-Gen; Neuroleptic; Anorectic; Anticonvulsant; Antidiabetic; Antiparkinsonian; Nootropic; Dermatological; Antimigraine; Neuroprotective; Cytostatic; Cerebroprotective; Endocrine-Gen.; Contraceptive. MECHANISM OF ACTION : Melatoninergic receptor agonist. The melatoninergic receptor inhibiting activity of N-[3-methoxy-2-(7-methoxy-1-naphtyl)propyl]acetamide was tested. The result showed that the compound had an inhibition constant (Ki) value of 4.9 mu M.
Abstract:
Described is a compound of formula (I): wherein n is l, 2 or 3, A represents a group -NR-C(=Z)-R', -C(=Z)-N(R)-R', or a group -NR-C(=Z)-N(R')-R", wherein: Z represents a S or O; R and R", which may be identical or different, each represents a H or alkyl group; R' represents an alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkyl-alkyl, aryl, aryl-alkyl, heteroaryl or heteroaryl-alkyl group; X represents N or N-R1 wherein R1 represents a H or alkyl, cycloalkyl, cycloalkyl-alkyl, aryl, aroyl, aryl-alkyl, heteroaryl, heteroaroyl or heteroaryl-alkyl group; R2 represents an alkoxy, cycloalkoxy or cycloalkyl-alkoxy group Provided are processes for the preparation of compounds if the formula (I) and descriptions of their use in the preparation of medicaments for treatment of disorders of the melatoninergic system.
Abstract:
N - ARIL PIPERIDINAS DE FORMULA I: DONDE M = 1-5; N = 1,2; R REPRESENTA UN ATOMO DE HIDROGENO, UN RADICAL ALQUILO O ARALQUILO; E REPRESENTA UN ATOMO DE HIDROGENO O UN RADICAL METILO; AR REPRESENTA: A REPRESENTA: Y X, X 1 , X 2 , X 3 Y X 4 REPRESENTAN UN ATOMO DE HIDROGENO O CIERTOS SUSTITUTIVOS. ESTOS COMPUESTOS SON LIGANDOS DEL RECEPTOR 5 - HT 1 B Y RESULTAN UTILES PARA EL TRATAMIENTO DE ENFERMEDADES EN LAS QUE ESTE IMPLICADO EL SISTEMA SEROTONINERGICO.