RU2003101405A - MEDICINES FOR THE PREVENTION AND TREATMENT OF NEURODEGENERATIVE DISEASES - Google Patents

Claims (10)

1. A drug for the prevention and treatment of schizophrenia, which contains a derivative of 5-substituted-3-oxadiazolyl-1,6-naphthyridin-2 (1H) -one of the following formula (I):

in which Het represents an oxadiazolyl group; R ¹ represents a hydrogen atom, a lower alkyl group, a lower cycloalkyl group, a trifluoromethyl group, a lower alkenyl group, a lower alkynyl group, a lower alkoxyl group, a lower alkoxysilane alkyl group, a lower hydroxyalkyl group, a substituted or unsubstituted aryl group, a substituted or unsubstituted heteroaryl group ; R ² represents a hydrogen atom, a lower alkyl group, a lower cycloalkyl group, a lower cycloalkylmethyl group, a lower alkenyl group, a lower cycloalkenyl group, a lower alkynyl group, a substituted or unsubstituted aryl group, and a substituted or unsubstituted heteroaryl group, or a physiologically acceptable acid addition salt thereof. 2. The medicament for the prevention and treatment of schizophrenia according to claim 1, wherein R ¹ is a C ₁ -C ₃ alkyl group, a C ₃ -C ₄ cycloalkyl group or a C ₂ -C ₃ alkenyl group, and R ² is a hydrogen atom , an alkyl group C ₁ -C ₄ , a cycloalkyl group C ₃ -C ₆ , a substituted or unsubstituted aryl group, and a substituted or unsubstituted heteroaryl group. 3. The medicament for the prevention and treatment of schizophrenia according to claim 2, where R ¹ represents a C ₁ -C ₃ alkyl group or a C ₃ -C ₄ cycloalkyl group, and R ² represents a hydrogen atom, a C ₁ -C ₃ alkyl group a cycloalkyl group C ₃ -C ₄ , a substituted or unsubstituted phenyl group, and a substituted or unsubstituted heteroaryl group. 4. A medicament for the prevention and treatment of schizophrenia, which contains a 5-substituted-3-oxadiazolyl-1,6-naphthyridin-2 (1H) -one derivative selected from 3- (5-ethyl-1,2,4-oxadiazol-3-yl) -5- (2-methylcyclopropyl) -1,6-naphthyridin-2 (1H) -one, 3- (5-methyl-1,2,4-oxadiazol-3-yl) -5- (2-methylphenyl) -1,6-naphthyridin-2 (1H) -one, 3- (5-methyl-1,2,4-oxadiazol-3-yl) -5- (4-methoxyphenyl) -1,6-naphthyridin-2 (1H) -one, 3- (5-ethyl-1,2,4-oxadiazol-3-yl) -5- (2-thienyl) -1,6-naphthyridin-2 (1H) -one, 3- (5-methyl-1,2,4-oxadiazol-3-yl) -5- (4-pyridyl) -1,6-naphthyridin-2 (1H) -one, 3- (3-ethyl-1,2,4-oxadiazol-5-yl) -5-methyl-1,6-naphthyridin-2 (1H) -one, 3- (3-ethyl-1,2,4-oxadiazol-5-yl) -5- (3-fluorophenyl) -1,6-naphthyridin-2 (1H) -one, 3- (3-methyl-1,2,4-oxadiazol-5-yl) -5- (3-methylphenyl) -1,6-naphthyridin-2 (1H) -one, 3- (3-methyl-1,2,4-oxadiazol-5-yl) -5- (3-methoxyphenyl) -1,6-naphthyridin-2 (1H) -one, 3- (3-ethyl-1,2,4-oxadiazol-5-yl) -5- (4-methoxyphenyl) -1,6-naphthyridin-2 (1H) -one, 3- (3-ethyl-1,2,4-oxadiazol-5-yl) -5- (4-pyridyl) -1,6-naphthyridin-2 (1H) -one and 3- (3-cyclopropyl-1,2,4-oxadiazol-5-yl) -5- (3-thienyl) -1,6-naphthyridin-2 (1H) -one, or their physiologically acceptable acid addition salts. 5. A medicament for the prevention and treatment of schizophrenia, which contains 3- (5-methyl-1,2,4-oxadiazol-3-yl) -5- (3-methoxyphenyl) -1,6-naphthyridin-2 (1H) -one, or a physiologically acceptable acid addition salt thereof. 6. The use of a compound according to any one of claims 1 to 4 for the manufacture of a medicament for the prevention and treatment of schizophrenia. 7. The use of a compound according to claim 5 for the manufacture of a medicament for the prevention and treatment of schizophrenia. 8. A method for preventing and / or treating schizophrenia in mammals, which comprises administering an effective amount of a compound according to any one of claims 1 to 4 to a mammal in need of such prevention and / or treatment of schizophrenia. 9. A method for preventing and / or treating schizophrenia in mammals, which comprises administering an effective amount of a compound according to claim 5 to said mammal in need of such prevention and / or treatment of schizophrenia. 10. The method of prevention and / or treatment of claim 8 or 9, in which the mammal is a human.