BENZOTHIAZOL DERIVATIVES AS ADENOSINE RECEPTOR LIGANDS Russian patent published in 2009 - IPC C07D417/14 C07D419/10 C07D417/04 A61K31/428 A61P25/28 

FIELD: chemistry.

SUBSTANCE: invention refers to benzothiazol derivatives of general formula (I) and to their pharmaceutically acceptable acid-additive salts as adenosine receptor ligands and to based medicinal agent. In general formula (I) , R¹ represents 1,4-dioxepanyl or tetrahydropyran-4-yl; R² represents -N(R)-(CH₂)_n-5- or 6-merous nonaromatic heterocycle containing 1-2 nitrogen heteroatoms optionally substituted with one-two substitutes chosen from group, consisting of C₁-C₆alkyl or -NR₂, or represents -(CH₂)_n-5- or 6-merous nonaromatic heterocycle containing 1-2 heteroatoms chosen of N, S or O, optionally substituted with group -(CH₂)_n-OH, C₁-C₆alkyl, C₁-C₆alkoxy, or represents -(CH₂)_n-5-or 6-merous aromatic heterocycle containing 1-2 nitrogen heteroatoms optionally substituted with the following group: C₁-C₆alkyl, C₁-C₆alkoxy, halogen, halogen-(C₁-C₆alkyl), -CH₂N(R)(CH₂)₂OCH₃, -N(R)(CH₂)₂OCH₃, - CH₂-morpholinyl or -CH₂-pyrrolidinyl or represents (CH₂)_n-C₃-C₆cycloalkyl optionally substituted with group hydroxy, or represents -N(R)-C₃-C₆cycloalkyl optionally substituted with group hydroxy or C₁-C₆alkyl, or represents phenyl optionally substituted with group C₁-C₆alkoxy, halogen, halogen-(C₁-C₆alkyl), C₁-C₆alkyl, -CH₂-pyrrolidine-1-yl, CH₂N(R)(CH₂)₂OCH₃ or -CH₂-N(R)C(O)-(C₁-C₆alkyl), or represents 1,4-dioxa-8-azaspiro[4,5]decane, or 2-oxa-5-azabicyclo[2,2,1]heptane, or 1-oxa-8-azaspiro[4,5]decane, or -N(R)-7-oxabicyclo[2,2,1]hept-2-yl, or 2-azabicyclo[2,2,2]octane; R represents hydrogen or C₁-C₆alkyl; n stands for 0 or 1.

EFFECT: compounds can be applied for treatment and prevention of diseases mediated by adenosine A_2A and A₁ receptors, eg Alzheimer's disease, some depressions, toxicomania, Parkinson's disease.

8 cl, 3 dwg, 61 ex