SUMMARY OF THE INVENTION
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[0005] The invention provides u of aryl piperazine derivatives of formula (I) and pharmaceutically acceptable salts thereof alone or in combination with other analgesics in manufacturing a medicament for treating acute pain, neuropathic pain or receptive nociceptive pain in mammals, including human beings:
wherein Ar is aryl or heteroaryl which is unsubstituted or substituted by a group lected from the group consisting of halogen, C1-6 alkyl, C1-4 alkoxyl and halogenated C1-4 alkyl.
[0006] According to another aspect of the invention, there is provided a method for treating acute pain, neuropathic pain or receptive nociceptive pain in mammals, including human beings, with the compound of formula (I), including administration of a therapeutically effective amount of the compound to a subject in need of such treatment.
DETAILED DESCRIPTION OF THE EMBODIMENTS
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[0007] In the invention, halogen refers to F, Cl, Br or I, preferably F, Cl or Br.
校园规划[0008] C1-6 alkyl means a linear, branched or cyclic saturated alkyl containing 1, 2, 3, 4, 5 or 6 carbon atoms, such as methyl, ethyl, propyl, isopropyl, n-butyl, n-pentyl, and n-hexyl. Methyl is preferable.
[0009] C1-4 alkoxyl means an alkyl-O- group, wherein the alkyl is an alkyl containing 1, 2, 3 or 4 carbon atoms as defined above, such as methoxyl, ethoxyl, n-propoxyl, iso-propoxyl and n-butoxyl. Methoxyl is preferable.
[0010] Halogenated C1-4 alkyl means an alkyl containing 1, 2, 3 or 4 carbon atoms as defined above which is substituted partly or completely by halogen. Trifluoromethyl is preferable.
[0011] Aryl means an aliphatic aromatic group containing 5-14 carbon atoms, such as phenyl or naphthyl. Phenyl is preferable, particularly preferable is phenyl substituted by the above mentioned substituents.
[0012] Heteroaryl means a monocyclic or bicyclic 5-14 member aryl containing 1-4, prefer
蜜蜂做工ably 1-2 heteroatoms lected from O, N and S. Benzothiazolyl, pyridyl or pyrimidinyl is preferable.
[0013] In one embodiment of the prent invention, the aryl is mono- or di-substituted phenyl, wherein the substituent is preferably lected from F, Cl, Br, methyl, methoxyl and trifluoromethyl.
清朝女子服饰[0014] In another embodiment of the prent invention, the heteroaryl reprents benzothiazolyl, pyridyl or pyrimidinyl, and the substituted heteroaryl compris no more than two substituents lected from F, Cl, Br, methyl, methoxyl and trifluoromethyl.
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[0015] The compound of formula (I) according to the prent invention may be prepared in the form of pharmaceutically acceptable salts according to common methods known in the art. The pharmaceutically acceptable salts are tho conventionally ud in the art, such as acid addition salts. The pharmaceutically acceptable acid addition salts include inorganic acid addition salts made from inorganic acids such as hydrochloric acid, hydrobromic acid, phosphoric acid or sulfuric acid; organic acid addition salts made from
organic acids such as acetic acid, propionic acid, lactic acid, citric acid, fumaric acid, malic acid, succinic acid, salicylic acid, maleic acid, glycerophosphoric acid, acetosalicylic acid, and alkyl or aryl sulfonic acid such as methanesulfonic acid, benzene sulfonic acid or toluene sulfonic acid.
产后脱发严重
[0016] The u of the compound of formula (I) or the pharmaceutically acceptable salts in manufacturing a medicament for treating pain refers to the u as an analgesic in the clinic. The acute pain includes, but is not limited to, headache, arthralgia, muscular tension or dysmenorrheal. The neuropathic pain includes, but is not limited to, chronic backache, postherpetic neuralgia, diabetic peripheral neuralgia, fibromyalgia, cancer-related pain, phantom limb pain, labour pains and opioid analgesics resistant neuralgia. The perceptive nociceptive pain includes, but is not limited to, postoperative pain, toothache, pain from surgery, and pain from rious burns.
[0017] The compounds of formula (I) can be formulated to a pharmaceutical composition according to a common standard pharmaceutical technique for administration of the com
pounds in the treatment. For example, the compounds of formula (I) may be dissolved in oil, propylene glycol or other solvents often ud for preparing injections. Preferable carriers are, but are not limited to, a saline solution, polyethylene glycol, ethanol, vegetable oil, isopropyl myristate, and the like. For topical administration, the compounds of the invention may be formulated into the form of ointment or cream.
[0018] The compounds of formula (I) may be dissolved, suspended or emulsified in an aqueous solution such as a conventional saline solution and 5% gluco solution, or a non-aqueous solution such as synthetic fatty glyceride, high fatty acids ester and propylene glycol, and thereby an injection is formulated. The composition of the prent invention may compri conventional additives, such as a solubilizing agent, an isotonizing agent, a suspending agent, an emulsifying agent, a stabilizing agent and a prervative.
[0019] The preferable administrating do of the compound of formula (I) may vary depending on such factors as condition and weight of patients, verity of the dia, for
mulation of the medicament, as well as route and time of administration, but tho skilled in the art may determine it properly. To obtain a preferable effect, however, the daily dosage of the compounds of the prent invention may be 1-200 mg/kg (body weight), preferably 1-100 mg/kg (body weight), while the do may be administered once or in veral times.肌肉英语
