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:
Indole derivatives (I), their enantiomers, diastereomers and their acid/base addition salts are new. Indole derivatives of formula (I), their enantiomers, diastereomers and their acid/base addition salts are new. R 11-6C alkyl, 3-8C cycloalkyl or 3-8C cycloalkyl-1-6C alkyl, preferably methyl; R 21-6C alkyl, preferably methyl, ethyl or propyl; and n : 1-6, preferably 2. An independent claim is included for the preparation of (I). [Image] ACTIVITY : Hypnotic; Tranquilizer; Antidepressant; Cardiovascular-Gen; Gastrointestinal-Gen; Neuroleptic; Anorectic; Anticonvulsant; Antidiabetic; Antiparkinsonian; Nootropic; Antimigraine; Neuroprotective; Endocrine-Gen; Contraceptive; Immunomodulator; Cytostatic. MECHANISM OF ACTION : Melatonin receptor binder. The affinity of (I) to bind with melatonin receptors MT1 and MT2 was tested using 2-[ 1> 2> 5>I]-iodomelatonin as reference radioligand. The results showed that (I) exhibited an inhibition constant value of less than 1 mu M.
Abstract:
Indole derivatives (I), their enantiomers, diastereomers and their acid/base addition salts are new. Indole derivatives of formula (I), their enantiomers, diastereomers and their acid/base addition salts are new. R 11-6C alkyl, 3-8C cycloalkyl or 3-8C cycloalkyl-1-6C alkyl, preferably methyl; R 21-6C alkyl, preferably methyl, ethyl or propyl; and n : 1-6, preferably 2. An independent claim is included for the preparation of (I). [Image] ACTIVITY : Hypnotic; Tranquilizer; Antidepressant; Cardiovascular-Gen; Gastrointestinal-Gen; Neuroleptic; Anorectic; Anticonvulsant; Antidiabetic; Antiparkinsonian; Nootropic; Antimigraine; Neuroprotective; Endocrine-Gen; Contraceptive; Immunomodulator; Cytostatic. MECHANISM OF ACTION : Melatonin receptor binder. The affinity of (I) to bind with melatonin receptors MT1 and MT2 was tested using 2-[ 1> 2> 5>I]-iodomelatonin as reference radioligand. The results showed that (I) exhibited an inhibition constant value of less than 1 mu M.
Abstract:
Indole derivatives (I), their enantiomers, diastereomers and their acid/base addition salts are new. Indole derivatives of formula (I), their enantiomers, diastereomers and their acid/base addition salts are new. R 11-6C alkyl, 3-8C cycloalkyl or 3-8C cycloalkyl-1-6C alkyl, preferably methyl; R 21-6C alkyl, preferably methyl, ethyl or propyl; and n : 1-6, preferably 2. An independent claim is included for the preparation of (I). [Image] ACTIVITY : Hypnotic; Tranquilizer; Antidepressant; Cardiovascular-Gen; Gastrointestinal-Gen; Neuroleptic; Anorectic; Anticonvulsant; Antidiabetic; Antiparkinsonian; Nootropic; Antimigraine; Neuroprotective; Endocrine-Gen; Contraceptive; Immunomodulator; Cytostatic. MECHANISM OF ACTION : Melatonin receptor binder. The affinity of (I) to bind with melatonin receptors MT1 and MT2 was tested using 2-[ 1> 2> 5>I]-iodomelatonin as reference radioligand. The results showed that (I) exhibited an inhibition constant value of less than 1 mu M.
Abstract:
Composés de formule (I), dans laquelle R1 représente un groupement alkyle , cycloalkyle, ou cycloalkylalkyle; R2 représente un groupement alkyle (C1-C 6) linéaire ou ramifié; et n représente 1 à 6, et leur utilisation pour trai ter les troubles du système mélatoninergique tels que les troubles du sommei l, le stress, l'anxiété, les pathologies cardiovasculaires, etc.