7-Amino-benzothiazole derivatives

A method of treating a disease mediated by the adenosine receptor comprising administering to a patient in need of such treatment, an effective amount of a compound of the formula I

• 15
• wherein
• R1 and R2 are independently selected from the group consisting of hydrogen, lower alkyl, C3-6-cycloalkyl, tetrahydropyran-2,3 or 4-yl, piperidin-4-yl, piperidin-4-yl substituted by lower alkyl, —(CH2)n—O-lower alkyl, —(CH2)n—NR′R″, —C(O)-lower alkyl, —(CH2)n—C(O)-lower alkyl, —(CH2)n—C(O)—C3-6-cycloalkyl, —(CH2)n—C(O)—NR′R″, —(CH2)n-phenyl, —(CH2)n-phenyl substituted by lower alkyl, lower alkoxy or NR′R″, —(CH2)n-pyridinyl, —(CH2)n-pyridinyl substituted by lower alkyl, lower alkoxy or NR′R″, —(CH2)n-morpholinyl, —(CH2)n-tetrahydropyran-2,3 or 4-yl, —(CH2)n-piperidin-1 or 4-yl, —(CH2)n-piperidin-1 or 4-yl substituted by lower alkyl, —C(O)—C5,6-cycloalkyl, —C(O)-tetrahydropyran-2,3 or 4-yl, —C(O)-morpholinyl, —C(O)-piperidin-1-yl
• and —C(O)-pyrrolidin-1-yl, or
• R1 and R2 form together with the N atom to which they are attached the ring 2-oxa-5-aza-bicyclo[2.2.1]hept-5-yl, an azetidinyl ring, or an azetidinyl ring substituted by lower alkyl or lower alkoxy;
• R3 is lower alkoxy, phenyl, phenyl substituted by halogen, —(CH2)n-halogen, or —(CH2)n—N(R′)—(CH2)n—O-lower alkyl, pyridinyl, pyridinyl substituted by lower alkyl, halogen or morpholinyl, morpholinyl, piperidin-1-yl disubstituted in the 4 position by lower alkyl and —(CH2)n—OH, or 2-aza-bicyclo[2.2.2]octane;
• n is 1 or 2;
• R′ and R″ are each independently selected from hydrogen or lower alkyl or together may form with the N atom an azetidinyl-, pyrrolidinyl- or piperidinyl group;
• and pharmaceutically acceptable acid addition salts thereof.

A pharmaceutical composition comprising a pharmaceutically effective amount of a compound of the formula I

• 16
• wherein
• R1 and R2 are independently selected from the group consisting of hydrogen, lower alkyl, C3-6-cycloalkyl, tetrahydropyran-2,3 or 4-yl, piperidin-4-yl, piperidin-4-yl substituted by lower alkyl, —(CH2)n—O-lower alkyl, —(CH2)n—NR′R″, —C(O)-lower alkyl, —(CH2)n—C(O)-lower alkyl, —(CH2)n—C(O)—C3-6-cycloalkyl, —(CH2)n—C(O)—NR′R″, —(CH2)n-phenyl, —(CH2)n-phenyl substituted by lower alkyl, lower alkoxy or NR′R″—(CH2)n-pyridinyl, —(CH2)n-pyridinyl substituted by lower alkyl, lower alkoxy or NR′R″, —(CH2)n-morpholinyl, —(CH2)n-tetrahydropyran-2,3 or 4-yl, —-(CH2)n-piperidin-1 or 4-yl, —(CH2),-piperidin-1 or 4-yl substituted by lower alkyl, —C(O)—C5,6-cycloalkyl, —C(O)-tetrahydropyran-2,3 or 4-yl, —C(O)-morpholinyl, —C(O)-piperidin-1-yl
• and —C(O)-pyrrolidin-1-yl, or
• R1 and R2 form together with the N atom to which they are attached the ring 2-oxa-5-aza-bicyclo[2.2.1]hept-5-yl, an azetidinyl ring, or an azetidinyl ring substituted by lower alkyl or lower alkoxy;
• R3 is lower alkoxy, phenyl, phenyl substituted by halogen, —(CH2),-halogen, or —(CH2)n—N(R′)—(CH2)n+1—O-lower alkyl, pyridinyl, pyridinyl substituted by lower alkyl, halogen or morpholinyl, morpholinyl, piperidin-1-yl disubstituted in the 4 position by lower alkyl and —(CH2)n—OH, or 2-aza-bicyclo[2.2.2]octane;
• n is 1 or 2;
• R′ and R″ are each independently selected from hydrogen or lower alkyl or together may form with the N atom an azetidinyl-, pyrrolidinyl- or piperidinyl group;
• and pharmaceutically acceptable acid addition salts thereof;
• and
• a pharmaceutically acceptable carrier.