2,3-Dihydro-imidazo[2,1-b]benzothiazole compositions to treat depressions

Claim 1

A composition to treat depressions, comprising an inert carrier and, as an active ingredient, an amount, which is effective to treat depressions, of a compound selected from the group consisting of a 2,3-dihydroimidazo[2,1-b]benzothiazole which may structurally be represented by the formula ##STR42## and the pharmaceutically acceptable acid addition salts thereof, the imidazo[2,1-b]benzothiazolium salts of formula ##STR43## and metal salt complexes thereof with a transition metal salt, wherein: R 1 and R 3 are each independently selected from the group consisting of hydrogen and lower alkyl; R 2 and R 4 are each independently selected from the group consisting of hydrogen, lower alkyl, aryl, aryllower alkyl, lower alkyloxy-lower alkyl or aryloxylower alkyl; R 5 , R 6 , R 7 and R 8 are each independently selected from the group consisting of hydrogen; halo; nitro; alkyl having from 1 to 20 carbon atoms; cyclalkyl having from 3 to 6 carbon atoms; hydroxy; lower alkyloxy; aryloxy; α-hydroxy-arylmethyl; amino; mono- and dialkyl-amino; mono-, di- and trihalo-lower alkylamino; lower alkenylamino; lower alkynylamino; (aryl-lower alkyl)amino; (lower alkyloxy-lower alkyl)amino; (hydroxy-lower alkyl)amino; (aryloxy-lower alkyl)amino; [mono- and di(lower-alkyl)amino-lower alkyl]amino; lower alkanoylamino; N-(lower alkyl)lower alkanoylamino; aminocarbonylamino; (1-lower alkyl-4-piperidinyl)amino; cycloalkylamino wherein said cycloalkyl represents a mono-, bi-, tri- or tetracyclic hydrocarbon radical having from 3 to 10 carbon atoms; and a radical of the formula ##STR44## wherein R 10 is selected from the group consisting of hydrogen, lower alkyl, lower alkenyl and lower alkynyl; or, when taken together R 5 and R 6 , R 6 and R 7 , or R 7 and R 8 may form a tri- or tetramethylene bridge or complete a fused benzene nucleus; R 9 is a member selected from the group consisting of lower alkyl, lower alkenyl, lower alkynyl and aryl lower alkyl; and X is a pharmaceutically acceptable anion and n represents the valency of the anion; wherein aryl as used in the foregoing definitions is phenyl, optionally substituted with 1 to 3 substituents each independently selected from the group consisting of halo, lower alkyl, lower alkyloxy and trifluoromethyl; and aroyl is arylcarbonyl.

Claim 5

A method of treating depressions in patients, which comprises the systemic administration to said patients, in need of same, of an effective anti-depressive amount of a compound selected from the group consisting of a 2,3-dihydroimidazo[2,1-b]benzothiazole which may structurally be represented by the formula ##STR45## and the pharmaceutically acceptable acid addition salts thereof, and imidazo[2,1-b]benzothiazolium salts of formula ##STR46## and metal salt complexes thereof with a transition metal salt, wherein: R 1 and R 3 are each independently selected from the group consisting of hydrogen and lower alkyl; R 2 and R 4 are each independently selected from the group consisting of hydrogen, lower alkyl, aryl, aryl-lower alkyl, lower alkyloxy-lower alkyl or aryloxy-lower alkyl; R 5 , R 6 , R 7 and R 8 are each independently selected from the group consisting of hydrogen; halo; nitro; alkyl having from 1 to 20 carbon atoms; cycloalkyl having from 3 to 6 carbon atoms; hydroxy; lower alkyloxy; aryloxy; α-hydroxy-arylmethyl; amino; mono- and dialkyl-amino; mono-, di- and trihalo-lower alkylamino; lower alkenylamino; lower alkynylamino; (aryl-lower alkyl)amino; (lower alkyloxy-lower alkyl)amino; (hydroxy-lower alkyl)amino; (aryloxy-lower alkyl)amino; [mono- and di(lower alkyl)amino-lower alkyl]amino; lower alkanoylamino; N-(lower alkyl)lower alkanoylamino; aminocarbonylamino; (1-lower alkyl-4-piperidinyl)amino; cycloalkylamino wherein said cycloalkyl represents a mono-, bi-, tri- or tetracyclic hydrocarbon radical having from 3 to 10 carbon atoms; and a radical of the formula ##STR47## wherein R 10 is selected from the group consisting of hydrogen, lower alkyl, lower alkenyl and lower alkynyl; or, when taken together R 5 and R 6 , R 6 and R 7 , or R 7 and R 8 may form a tri- or tetramethylene bridge or complete a fused benzene nucleus; R 9 is a member selected from the group consisting of lower alkyl, lower alkenyl, lower alkynyl and aryllower alkyl; and X is a pharmaceutically acceptable anion and n represents the valency of the anion; wherein aryl as used in the foregoing definitions is phenyl, optionally substituted with 1 to 3 substituents each independently selected from the group consisting of halo, lower alkyl, lower alkyloxy and trifluoromethyl; and aroyl is arylcarbonyl.

Claim 6

A method of treating depressions in patients, which comprises the systemic administration to said patients, in need of same, of an effective anti-depressive amount of a compound selected from the group consisting of a 2,3-dihydroimidazo[2,1-b]benzothiazole which may structurally be represented by the formula ##STR45## and the pharmaceutically acceptable acid addition salts thereof, and imidazo[2,1-b]benzothiazolium salts of formula ##STR46## and metal salt complexes thereof with a transition metal salt, wherein: R 1 and R 3 are each independently selected from the group consisting of hydrogen and lower alkyl; R 2 and R 4 are each independently selected from the group consisting of hydrogen, lower alkyl, aryl, aryl-lower alkyl, lower alkyloxy-lower alkyl or aryloxy-lower alkyl; R 5 , R 6 , R 7 and R 8 are each independently selected from the group consisting of hydrogen; halo; nitro; alkyl having from 1 to 20 carbon atoms; cycloalkyl having from 3 to 6 carbon atoms; hydroxy; lower alkyloxy; aryloxy; α-hydroxy-arylmethyl; amino; mono- and dialkyl-amino; mono-, di- and trihalo-lower alkylamino; lower alkenylamino; lower alkynylamino; (aryl-lower alkyl)amino; (lower alkyloxy-lower alkyl)amino; (hydroxy-lower alkyl)amino; (aryloxy-lower alkyl)amino; [mono- and di(lower alkyl)amino-lower alkyl]amino; lower alkanoylamino; N-(lower alkyl)lower alkanoylamino; aminocarbonylamino; (1-lower alkyl-4-piperidinyl)amino; cycloalkylamino wherein said cycloalkyl represents a mono-, bi-, tri- or tetracyclic hydrocarbon radical having from 3 to 10 carbon atoms; and a radical of the formula ##STR47## wherein R 10 is selected from the group consisting of hydrogen, lower alkyl, lower alkenyl and lower alkynyl; or, when taken together R 5 and R 6 , R 6 and R 7 , or R 7 and R 8 may form a tri- or tetramethylene bridge or complete a fused benzene nucleus; R 9 is a member selected from the group consisting of lower alkyl, lower alkenyl, lower alkynyl and aryllower alkyl; and X is a pharmaceutically acceptable anion and n represents the valency of the anion; wherein aryl as used in the foregoing definitions is phenyl, optionally substituted with 1 to 3 substituents each independently selected from the group consisting of halo, lower alkyl, lower alkyloxy and trifluoromethyl; and aroyl is arylcarbonyl.