Nitrogen-containing six-membered aromatic ring derivatives and pharmaceutical products containing the same
View Patent ↗Provided is a compound that has the ability to promote axonal outgrowth in combination with the ability to promote angiogenesis and can therefore be used to reduce central nerve injuries such as head injury and spinal cord injury, cerebral infarction, ischemic heart diseases such as myocardial infarction and organic angina, peripheral arterial occlusive diseases such as critical limb ischemia, or after-effects of these diseases. Specifically, the compound is represented by the following formula (I): in which Nx group is preferably a 6-membered aromatic ring containing two nitrogen atoms; R 0 , R 1 and R 2 are each independently a hydrogen atom, an alkyl group, an amino group or the like; E is an oxygen atom or an —NR 8 group (wherein R 8 is an alkyl group or the like); n is an integer of 0 to 5; X and Y are each a connecting bond, a cycloalkyl group, —CO— or the like; and Q is a hydrogen atom or a phenyl group.
1. A compound, wherein the compound is:
2-(5-amino-4,6-dimethylpyrimidine-2-yloxy)-N-(1-benzylpiperidine-4-yl)-N-methylacetamide.
2. A pharmaceutical preparation comprising the compound of claim 1 as an active ingredient and a pharmaceutically acceptable excipient.
3. A pharmaceutical preparation comprising the compound of claim 1 and, optionally, a filler, an expander, a binder, a moisturizer, a disintegrating agent, a surfactant, a lubricant, diluentant, excipient, or a mixture thereof.
4. A pharmaceutical preparation comprising the compound of claim 1 , wherein the pharmaceutical preparation is in the form of a tablet, a pill, a powder, a liquid, a suspension, an emulsion, a granule, a capsule, a suppository, an injection liquid, an injection suspension, an ointment, a cataplasm, or an inhalant.
5. A method of treating spinal cord injury comprising
administering to a patient in need thereof a therapeutically effective amount of the compound of claim 1 .
6. The method of claim 5 , wherein the compound is administered in the range of from about 0.1 mg/day/patient to about 1000 mg/day/patient.
7. A method for treating cerebral infarction comprising
administering to a patient in need thereof a therapeutically effective amount of the compound of claim 1 .
8. The method of claim 7 , wherein the compound is administered in the range of from about 0.1 mg/day/patient to about 1000 mg/day/patient.