摘要:
A 3,5-dioxo-(2H,4H)-1,2,4-triazine compounds of formula I ##STR1## in which: R.sub.1 and R.sub.2, which are identical or different, represent hydrogen or C.sub.1 -C.sub.6 alkyl, n is 2 to 6, inclusive,A represents aryl piperazino II ##STR2## the Ar grouping representing phenyl, naphthyl, pyrimidyl, or pyridyl, unsubstituted or substituted by C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy, hydroxy, trifluoromethyl, or halogen, or III benzodioxanyl-methyl-amino or pyridodioxanyl-methyl-amino ##STR3## in which R represents hydrogen or C.sub.1 -C.sub.3 alkyl and X represents a nitrogen or carbon atom, therapeutically-acceptable salts and enantiomers thereof, pharmaceutical compositions thereof, and method for treatment of diseases requiring a 5HT.sub.1A receptor agonist therewith.
摘要:
The invention concerns novel 3-oxo-(2H)-1,2,4-triazine derivatives of general formula (I) in which R1 represents: hydrogen, when A is an optionally substituted nitrogen atom; a linear or branched 1-C4 alkyl group; a C1-C4phenyl alkyl group, the phenyl ring being optionally substituted by one or several groups such as C1-C4 alkyl, C1-C3 alkoxy, halogen, trifluoromethyl. R2 represents: hydrogen; a linear or branched C1-C4 alkyl radical; a C1-C4 phenyl or phenylalkyl group, the phenyl ring being optionally substituted by one or several groups such as C1-C4 alkyl, C1-C3 alkoxy, halogen, trifluoromethyl. A represents an oxygen atom or a nitrogen atom optionally NR3 substituted. R3 represents hydrogen or a methyl group. B represents a group such as (IIa) in which Ar itself represents an aromatic structure such as phenyl, pyridyl or pyrimidyl, optionally substituted by one or several groups such as C1-C3 alkyl, C1-C3 alkoxy, hydroxy, trifluoromethyl or halogen and n can be whole numbers ranging between 3 and 5; (IIb) in which Ar is as defined in formula (IIa) and m can be a whole number ranging between 1 and 2; (IIc) in which R4 represents hydrogen or a C1-C3 alkyl group and n can be whole numbers ranging between 3 and 5.
摘要:
The invention concerns 3,5-dioxo-(2H,4H)-1,2,4-triazine derivatives of general formula (I), wherein: R1 and R2, identical or different, represent a branched or linear C1-C7 alkyl or alkenyl radical, a C1-C6 alkyl radical substituted by groups such as trifluoromethyl, C5-C6 cycloalkyl, nitrile, C1-C4 alkoxycarbonylvinyl, hydroxycarbonylvinyl, C1-C4 alkoxycarbonyl, carboxylate, benzyloxy or phenyl (for which the phenyl ring is optionally substituted by one or more groups such as C1-C4 alkoyl, C1-C4 alkoxy, nitro, halogen, trifluoromethyl); YR3 represents oxygen or NR3 for which R3 represents hydrogen, a linear or branched C1-C7 alkyl or alkenyl radical, a C1-C6 alkyl radical substituted by groups such as trifluoromethyl or phenyl (for which the phenyl ring is optionally substituted by one or more groups such as C1-C4 alkoyl, C1-C4 alkoxy, nitro, halogen, trifluoromethyl); Z represents an oxygen atom or a carbon atom capable of being bound to the ortho, meta or para positions of the phenyl group of formula I; n can be 0 to 5 when Z=C or 2 to 4 when Z=O; X represents oxygen or sulphur; R4, R5, R6, R7 and R8 represent hydrogen or fluorine; R9, R10 and R11 represent hydrogen or a linear or branched C1-C5 alkyl group as well as the pharmaceutically acceptable base addition salts, and the various enantiomers of compounds having asymmetric carbons, and their mixtures in all proportions including in particular the racemic mixtures.
摘要:
The invention concerns novel cyclohexane derivatives difunctionalised in 1.4 of general formula (1) in which A represents a group such as (IIa) in which Ar itself represents an aromatic structure such as phenyl or pyrimidinyl optionally substituted by one or several groups such as C1-C3 alkyl, C1-C3 alkoxy, trifluoromethyl or halogen (IIb); B represents a heterocyclic group such as: 3,5-dioxo-(2H,4H)-1,2,4 triazine substituted in position 2 (IIIa); 3-oxo-(2H)-1,2,4 triazine substituted in position 5 (IIIb); 3,5-dioxo-6-amino-(2H,4H)-1,2,4-triazine (IIIc) in which R represents a C1-C3 alkyl group. The invention also concerns the salts of compounds of general formula I with pharmaceutically acceptable acids. It also concerns the various “cis” and “trans” isomers and the various enantiomers with asymmetric carbons.
摘要:
Novel 3,5-dioxo-(2H,4H-triazine derivatives of general formula (I): wherein R.sub.1 is hydrogen, a C.sub.1 -C.sub.4 alkyl radical, phenyl C.sub.1 -C.sub.4 alkyl or phenyl, the phenyl ring being optionally substituted by one or more groupings such as (C.sub.1 -C.sub.3) alkyl, hydroxyl, trifluoromethyl or halogen: R.sub.2 is hydrogen or a (C.sub.1 -C.sub.4) alkyl radical, n can be an integer from 2 to 6; A is a grouping of the aryl piperazino or benzodioxanyl-methylamino or pyridodioxanyl-methylamino type. The invention also concerns a method of preparing said derivatives and pharmaceutical compositions comprising at least one of the compounds of general formula (I) as the active ingredient: ##STR1##
摘要:
The present invention relates to the docosahexaenoatepanthenyl of the following formula: It also relates to a method for preparing same and to a pharmaceutical composition comprising same and to the use of same in the treatment or the prevention of cardiovascular diseases, in particular atrial fibrillation.
摘要:
The present invention relates to diarylpyridazinone derivatives that block the potassium Kv channels (specifically the Kv1.5, Kv4.3, and Kv11.1 channels) and to the use thereof for the treatment of humans. Said compounds have the general formula (I), where R1 and R2 are simultaneously or independently one or more groupings such as: halogen, such as F, Br, Cl, a straight or branched C1-C4 alkyl, hydroxy, a straight or branched C1-C4 alkoxy, arylsulfonamido, in which the aryl is optionally replaced with a straight or branched C1-C4 alkyl, or nitrile, as well as the various enantiomers and the mixtures thereof in any proportion, and the pharmaceutically acceptable salts thereof.
摘要:
The present invention relates to derivatives of general formula I wherein: —W represents nitrogen, —R1 represents: •a hydrogen or a linear or branched C1-C5 alkyl radical or, •a C1-C3 alkyl radical substituted with groups such as trifluoromethyl, nitrile, hydroxy, C1-C3 alcoxy, C3-C6 alkoxyalkoxy, indolyl, thiophenyl, oxothiophenyl, C1-C3 N-alkylcarbamoyl groups or, •a phenyl or pyridyl or naphthyl, or thiophenyl group optionally substituted with one or more groups such as halogen atoms, nitro, nitrile, trifluoromethyl, vinyl, methylsulfanyl, linear branched C1-C4 alkyl, linear or branched C1-C3 alkoxy groups, •a C6 2-oxocycloalkyl radical—R2 represents a methyl or heptyl, —m, n are equal to 1, —V represents CH2, —X—Y represents —N— (C═O)—, —CH—O—, —Z represents a phenyl group substituted with one or more trifluoromethyl groups, halogen atoms or linear C1-C4 alkyl groups.
摘要:
The present invention relates to derivatives of general formula I wherein: —W represents nitrogen, —R1 represents: •a hydrogen or a linear or branched C1-C5 alkyl radical or, •a C1-C3 alkyl radical substituted with groups such as trifluoromethyl, nitrile, hydroxy, C1-C3 alcoxy, C3-C6 alkoxyalkoxy, indolyl, thiophenyl, oxothiophenyl, C1-C3 N-alkylcarbamoyl groups or, •a phenyl or pyridyl or naphthyl, or thiophenyl group optionally substituted with one or more groups such as halogen atoms, nitro, nitrile, trifluoromethyl, vinyl, methylsulfanyl, linear branched C1-C4 alkyl, linear or branched C1-C3 alkoxy groups, •a C6 2-oxocycloalkyl radical—R2 represents a methyl or heptyl, -m, n are equal to 1, —V represents CH2, —X—Y represents —N— (C═O)—, —CH—O—, —Z represents a phenyl group substituted with one or more trifluoromethyl groups, halogen atoms or linear C1-C4 alkyl groups.
摘要:
The present invention concerns derivatives of heteroarylsulfonamides, notably as blockers of Kv potassium channels, and more particularly of channels Kv1.5, Kv4.3 or Kv11.1, their application in clinical therapy and their preparation methods. These compounds correspond to the following general formula (I): where R1 represents one or more substituents of the phenyl core X such as: hydrogen, halogen, trifluoromethyl, trifluoromethoxy, linear or branched C1-C4 alkyl, or linear or branched C1-C4 alkoxy, A represents oxygen or sulphur, B represents nitrogen when n=1 or 2 and D represents —C(═O)—, or B represents CH when n=0 and D represents —CH2O— or when n=1 and D represents —O—, R2 represents a hydrogen, a methyl, a fluorine or chlorine atom or a methoxy, HetAr represents a pyridyl or quinolyl group, possibly substituted by a group such as a linear or branched C1-C4 alkyl, a linear or branched C1-C4 alkoxy, a halogen, or a trifluoromethyl, and to their pharmaceutically acceptable salts.