New 1,5-diamino-pentan-3-ol derivatives, useful e.g. for the treatment of arrhythmia, emesis, migraine, narcolepsy, obesity, diarrhea, inflammation, asthma, glaucoma, depression or especially pain

摘要

N,N,N',N'-Tetrasubstituted 1,5-diamino-pentan-3-ol derivatives (I) are new. Diaminopentanols of formula (I), in the form of diastereomers, enantiomers or their mixtures (including racemates) and bases, salts or solvates, are new. R<1>, R<2> = linear or branched, saturated or unsaturated aliphatic residue; R<1>+R<2> = (CH2)n; n = 3 or more; R<3> = linear or branched, saturated or unsaturated aliphatic residue, saturated or unsaturated cycloaliphatic residue, aryl or heteroaryl (where the ring systems are optionally substituted and optionally bonded via a linear or branched, saturated or unsaturated aliphatic bridge, the aryl or heteroaryl residues optionally being part of a polycyclic system); R<4>, R<5> = linear or branched, saturated or unsaturated aliphatic residue or aryl (optionally bonded via a linear or branched, saturated or unsaturated aliphatic bridge); R<4>+R<5> = (CH2)m; m = integer; R<6>, R<7> = linear or branched, saturated or unsaturated aliphatic residue or aryl (optionally bonded via a linear or branched, saturated or unsaturated aliphatic bridge); R<6>+R<7> = (CH2)p; p = integer; and R<8> = H; or aryl or heteroaryl (both optionally substituted); the following compounds (I') are excluded: 1,5-bis-(N,N-dimethylamino)-2,4-dimethyl-3-pyridin-2-yl-pentan-3-ol, 2,6-bis-(N,N-dimethylaminomethyl)-1-phenylcyclohexanol, 2,6-bis-(N,N-dimethylaminomethyl)-1-pyridin-2-ylcyclohexanol and 2,7-bis-(N,N-dimethylaminomethyl)-1-pyridin-2-ylcycloheptanol. Independent claims are also included for: (1) Medicaments containing (I) or (I') as active agents, optionally together with auxiliaries; and (2) Preparation of compounds of formula (I).