Benzothiazole derivatives as adenosine receptor ligands

Details Benzothiazole derivatives as adenosine receptor ligands Benzothiazole derivatives as adenosine receptor ligands

C - Chemistry, Metallurgy

07

D

C07D 417/14 (2006.01) A61K 31/4412 (2006.01) A61P 25/16 (2006.01) A61P 25/28 (2006.01) C07D 277/82 (2006.01) C07D 417/12 (2006.01)

Patent

CA 2467551

The present invention relates to compounds of the general formula (I): wherein R is phenyl, pyridin-2-yl, -C(O)-O-lower alkyl, -C(O)-lower alkyl, -C(O)- morpholinyl, -C(O)-NR'2,-(CH2)N-NR'2or -(CH2)N-O-lower alkyl and R' may be hydrogen or lower alkyl; and to pharmaceutically acceptable acid addition salts thereof. The compounds disclosed in this application have a good affinity to the A2A receptor and therefore they may be used in the control or prevention of illnesses based on the modulation of the adenosine system, such as Alzheimer's disease, Parkinson's disease, Huntington's disease, neuroprotection, schizophrenia, anxiety, pain, respiration deficits, depression, drug addiction, such as amphetamine, cocaine, opioids, ethanol, nicotine, cannabinoids, or against asthma, allergic responses, hypoxia, ischaemia, seizure and substance abuse. Furthermore, compounds of the present invention may be useful as sedatives, muscle relaxants, antipsychotics, antiepileptics, anticonvulsants and cardiaprotective agents for disorders such as coronary artery disease and heart failure.

La présente invention concerne des composés représentés par la formule générale (I) et certains de leurs sels d'addition acides pharmaceutiquement admis. Dans cette formule, R est phényle, pyridin-2-yle, -C(O)-O-alkyle inférieur, -C(O)-alkyle inférieur, -C(O)-morpholinyle, -C(O)-NR'¿2?,-(CH¿2?)<SB>N</SB>-NR'¿2? ou -(CH¿2?)<SB>N</SB>-O-alkyle inférieur, R' pouvant être hydrogène ou alkyle inférieur. Ces composés présentent une bonne affinité pour le récepteur A¿2A?, ce qui fait qu'ils conviennent pour le traitement ou la prévention d'affections imputables à un déficit de modulation du système adénosinien. Les affections concernées ici sont essentiellement les maladies d'Alzheimer et de Parkinson, la chorée de Huntington, la neuroprotection, la schizophrénie, l'angoisse, la douleur, les déficits respiratoires, la dépression, la toxicomanie (amphétamines, cocaïne, opioïdes, éthanol, nicotine, cannabinoïdes), sans oublier l'asthme, les réactions allergiques, l'hypoxie, l'ischémie, la crise d'épilepsie et l'abus de substances psychoactives. En outre, les composés de l'invention conviennent comme sédatifs, myorelaxants, neuroleptiques, antiépileptiques, anticonvulsifs et cardioprotecteurs pour des troubles tels que la coronaropathie et l'insuffisance cardiaque.

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