Therapeutic agent for cerebral infarction
AssigneeMitsubishi Tanabe Pharma Corporation
InventorsHaruto NAKAGAWA, Naoko ANDO
Life of this patent
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Abstract
The present invention provides a novel therapeutic drug for cerebral infarction, which contains a piperazine compound as an active ingredient. The compound of the present invention can be provided as a novel therapeutic drug for cerebral infarction having an effect of suppressing brain injury volume or improving neurological deficit, since it suppresses production of plural inflammatory cytokines and chemokines present in the brain such as TNF-β, IL-1β, IL-6 and MCP-1 and the like.
Claims10
(canceled)
A piperazine compound represented by formula <2>
- wherein
- R1 and R2 are the same or different and each is hydrogen, halogen, lower alkyl, lower alkoxy, amino, nitro, hydroxyl, cyano or amino which is mono- or di-substituted by at least one functional group selected from the group consisting of lower alkyl and lower acyl,
- R3, R4 and R5 are the same or different and each is hydrogen, halogen, lower alkyl, lower alkoxy, nitro, amino, hydrocyano or amino which is mono- or di-substituted by at least one functional group selected from the group consisting of lower alkyl and lower acyl,
- R6 and R7 are the same or different and each is hydrogen, lower alkyl, lower alkyl substituted by 1 to 3 halogens, aralkyl, acyl or lower acyl substituted by 1 to 3 halogens,
- R8 and R9 are the same or different and each is hydrogen or lower alkyl,
- Ra-Rd are the same or different and each is hydrogen, lower alkyl, aralkyl or hydroxy lower alkyl, or any two of Ra-Rd are bonded to each other to form alkylene having a carbon number of 1-2,
- Y is a group represented by formula
- wherein
- R10 and R11 are the same or different and each is hydrogen or lower alkyl,
- R12 and R13 are the same or different and each is hydrogen or lower alkyl, or R12 and R13 are groups that form alkylene in combination,
- R14 and R15 are the same or different and each is hydrogen or lower alkyl,
- m is an integer of 0-2, n is an integer of 0-2, and 0≦m+n≦2,
- ring A is phenyl, pyrimidyl, thiazolyl, pyridyl, pyrazinyl or imidazolyl, and
- ring B1 is pyridyl or thienyl,
- or a pharmaceutically acceptable salt thereof.
A method of treating a cerebral infarction, the method comprising:
- administering to a subject in need thereof an effective amount of a piperazine compound represented by formula <1>
- wherein
- R1 and R2 are the same or different and each is hydrogen, halogen, lower alkyl, lower alkoxy, amino, nitro, hydroxyl, cyano or amino which is mono- or di-substituted by at least one functional group selected from the group consisting of lower alkyl and lower acyl,
- R3, R4 and R5 are the same or different and each is hydrogen, halogen, lower alkyl, lower alkoxy, nitro, amino, hydroxyl, cyano or amino which is mono- or di-substituted by at least one functional group selected from the group consisting of lower alkyl and lower acyl,
- R6 and R7 are the same or different and each is hydrogen, lower alkyl, lower alkyl substituted by 1 to 3 halogens, aralkyl, acyl or lower acyl substituted by 1 to 3 halogens,
- R8, R9 are the same or different and each is hydrogen or lower alkyl,
- Ra-Rd are the same or different and each is hydrogen, lower alkyl, aralkyl or hydroxy lower alkyl, or any two of Ra-Rd are bonded to each other to form alkylene having a carbon number of 1 or 2,
- Y is a group represented by the formula
- wherein
- R10 and R11 are the same or different and each is hydrogen or lower alkyl,
- R12 and R13 are the same or different and each is hydrogen or lower alkyl, or R12 and R13 are groups that form alkylene in combination,
- R14 and R15 are the same or different and each is hydrogen or lower alkyl, and
- m is an integer of 0-2, n is an integer of 0-2 and 0≦m+n≦2,
- ring A is phenyl, pyrimidyl, thiazolyl, pyridyl, pyrazinyl or imidazolyl, and
- ring B is pyridyl or thienyl,
- or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.