JP2013227299A5

JP2013227299A5 -

Info

Publication number: JP2013227299A5
Application number: JP2013068344A
Authority: JP
Filing date: 2013-03-28
Publication date: 2015-02-19
Anticipated expiration: 2033-03-28

Claims

Formula (1A)

[In the formula (1A),
R ¹ represents C _1-5 alkyl;
R ² represents hydrogen;
R ^a represents a hydrogen atom or C _1-5 alkyl;
R ³ is aryl or heteroaryl (the aryl or heteroaryl is a group consisting of C _1-5 alkoxy, C _1-5 alkyl, halogen atom, trifluoromethyl, trifluoromethoxy, cyano, hydroxy, and difluoromethoxy. Or may be substituted with 1 to 2 groups selected from
R ⁴ and R ⁵ together with the adjacent nitrogen atom, a 6-membered saturated heterocyclic ring that may contain one or more oxygen atoms in addition to the nitrogen atom in the ring (the 6-membered saturated heterocyclic ring is The 6-membered saturated heterocycle may be bridged with C _1-5 alkylene between two different carbon atoms in the ring ). Or 2-oxa-6-azaspiro [3.3] hept-6-yl;
A represents the formulas (2) to (4);

X represents a single bond;
n is an integer of 1. ]
1,2,4-triazolone derivative represented by the above, or a pharmaceutically acceptable salt thereof as an active ingredient , and one or more pharmaceutically acceptable carriers, excipients or diluents Including mood disorders, anxiety disorders, schizophrenia, Alzheimer's disease, Parkinson's disease, Huntington's disease, eating disorders, hypertension, digestive disorders, drug addiction, epilepsy, cerebral infarction, cerebral ischemia, brain edema, head An oral or parenteral preparation for use in the treatment or prevention of trauma, inflammation, immune-related diseases, and alopecia .

The oral or parenteral preparation according to claim 1, wherein the dose of the 1,2,4-triazolone derivative or a pharmaceutically acceptable salt thereof contained as an active ingredient is 0.001 to 500 mg per day.

The active ingredient is 2- [3- (3-chlorophenyl) -1- {4- [2- (morpholin-4-yl) ethyl] phenyl} -5-oxo-1,5-dihydro-4H-1,2 , 4-Triazol-4-yl] -N- (propan-2-yl) acetamide, or a pharmaceutically acceptable salt thereof, The oral or parenteral preparation according to claim 1 or 2.

The active ingredient is 2- [3- (3-chlorophenyl) -1- {5- [2- (3-oxa-8-azabicyclo [3.2.1] oct-8-yl) ethyl] pyridine-2- IL} -5-oxo-1,5-dihydro-4H-1,2,4-triazol-4-yl] -N- (propan-2-yl) acetamide, or a pharmaceutically acceptable salt thereof Item 3. Oral or parenteral preparation according to item 1 or 2.

The active ingredient is 2- [3- (3-chlorophenyl) -1- {5- [2- (morpholin-4-yl) propyl] pyridin-2-yl} -5-oxo-1,5-dihydro-4H The oral or parenteral preparation according to claim 1 or 2, which is -1,2,4-triazol-4-yl] -N- (propan-2-yl) acetamide, or a pharmaceutically acceptable salt thereof. .

The active ingredient is N-tert-butyl-2- [3- (3-chlorophenyl) -1- {5- [2- (morpholin-4-yl) ethyl] pyridin-2-yl} -5-oxo-1 , 5-dihydro-4H-1,2,4-triazol-4-yl] acetamide, or a pharmaceutically acceptable salt thereof, The oral or parenteral preparation according to claim 1 or 2.

The active ingredient is 2- [3- (3-chloro-4-fluorophenyl) -1- {4- [2- (morpholin-4-yl) ethyl] phenyl} -5-oxo-1,5-dihydro- 4H-1,2,4-triazol-4-yl] -N- (propan-2-yl) acetamide, or a pharmaceutically acceptable salt thereof, orally or parenterally according to claim 1 or 2. Formulation.

The active ingredient is 2- [3- (3-chloro-4-fluorophenyl) -5-oxo-1- {5- [2- (piperidin-1-yl) ethyl] pyridin-2-yl} -1, The oral use according to claim 1 or 2, which is 5-dihydro-4H-1,2,4-triazol-4-yl] -N- (propan-2-yl) acetamide, or a pharmaceutically acceptable salt thereof. Or parenteral preparation.

The active ingredient is 2- [3- (3-chloro-4-fluorophenyl) -1- {5- [2- (morpholin-4-yl) ethyl] pyridin-2-yl} -5-oxo-1, The oral use according to claim 1 or 2, which is 5-dihydro-4H-1,2,4-triazol-4-yl] -N- (propan-2-yl) acetamide, or a pharmaceutically acceptable salt thereof. Or parenteral preparation.