1H-1,2,4-triazole-3-carboxamide derivatives having cannabinoid-CB1 receptor agonistic, partial agonistic, inverse agonistic or antagonistic activity

A method of treating disorders involving CB1 cannabinoid neurotransmission such as psychosis, anxiety, depression, attention deficits, memory disorders, cognitive disorders, appetite disorders, obesity, addiction, appetence, drug dependence, neurodegenerative disorders, dementia, dystonia, muscle spasticity, tremor, epilepsy, multiple sclerosis, traumatic brain injury, stroke, Parkinson's disease, Alzheimer's disease, epilepsy, Huntington's disease, Tourette's syndrome, cerebral ischaemia, cerebral apoplexy, craniocerebral trauma, stroke, spinal cord injury, neuroinflammatory disorders, plaque sclerosis, viral encephalitis, demyelinisation related disorders, as well as for the treatment of pain disorders, including neuropathic pain disorders, septic shock, glaucoma, diabetes, cancer, emesis, nausea, gastrointestinal disorders, gastric ulcers, diarrhoea and cardiovascular disorders, characterized in that for the preparation of a pharmaceutical composition for the treatment of said disorders a compound of formula (I) is used

• 6
• wherein
• R and R1 independently represent a phenyl, naphtyl, thienyl, pyridyl, pyrimidyl, pyrazinyl, pyridazinyl or triazinyl group, which groups may be substituted with 1-4 substituents X, which can be the same or different, from the group branched or unbranched (C1-3)-alkyl or alkoxy, hydroxy, halogen, trifluoromethyl, trifluoromethylthio, trifluoromethoxy, nitro, amino, mono- or dialkyl (C1-2)-amino, mono- or dialkyl (C1-2)-amido, (C1-3)-alkoxycarbonyl, trifluoromethylsulfonyl, sulfamoyl, (C1-3)-alkylsulfonyl, carboxyl, cyano, carbamoyl, (C1-3)-dialkylaminosulfonyl, (C1-3)-monoalkylamino-sulfonyl and acetyl,
• R2 represents a hydrogen atom or a branched or unbranched C1-8 alkyl or C1-8 cycloalkyl-alkyl group or a phenyl, benzyl or phenethyl group which aromatic rings may be substituted with 1-4 substituents X, wherein X has the meaning as indicated above, or R2 represents a pyridyl or thienyl group,
• R3 represents branched or unbranched C1-8 alkyl, C1-8 alkoxy, C3-8 cycloalkyl, C5-10 bicycloalkyl, C6-10 tricycloalkyl, C3-8 alkenyl, C5-8 cycloalkenyl, which groups may optionally contain one or more heteroatoms from the group (O, N, S), which groups may be substituted with a hydroxy group, an ethynyl group or 1-3 fluoro atoms, or R3 represents a phenyl, benzyl or phenethyl group which aromatic rings may be substituted with 1-4 substituents X, wherein X has the meaning as indicated above, or R3 represents a pyridyl, pyrimidyl, pyrazinyl, pyridazinyl, triazinyl or thienyl group which heteroaromatic rings may be substituted with 1-2 substituents X, wherein X has the meaning as indicated above, or R3 represents a group NR4R5 wherein
• R4 and R5, together with the nitrogen atom to which they are bonded, form a saturated or unsaturated, monocyclic or bicyclic, heterocyclic moiety having 4 to 10 ring atoms, which heterocyclic group contains one or two heteroatoms from the group N, O or S, which heteroatoms can be the same or different, which heterocyclic moiety may be substituted with a branched or unbranched C1-3 alkyl, hydroxy or trifluoromethyl group or a fluoro atom, or
• R2 and R3, together with the nitrogen atom to which they are bonded, form a saturated or unsaturated, monocyclic or bicyclic, heterocyclic moiety having 4 to 10 ring atoms, which heterocyclic group contains one or two heteroatoms from the group N, O or S, which heteroatoms can be the same or different, which heterocyclic moiety may be substituted with a branched or unbranched C1-3 alkyl, hydroxy, piperidinyl or trifluoromethyl group or a fluoro atom,
• and prodrugs, stereoisomers and salts thereof.