- METHODS FOR TREATING CHRONIC FATIGUE SYNDROME AND MYALGIC ENCEPHALOMYELITIS
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In one aspect the invention relates to a method of treatment selected from the group consisting of: (a) treating a symptom such as pain in a subject identified or diagnosed as having Myalgic Encephalomyelitis/Chronic Fatigue Syndrome (ME/CFS); (b) treating a symptom such as pain in a subject having dysfunctional TRPM3 ion channel activity; (c) restoring NK cell function in a subject having dysfunctional TRPM3 ion channel activity; and (d) restoring calcium homeostasis in a subject having dysfunctional TRPM3 ion channel activity. The method comprises the step of administering to the subject a therapeutically effective amount of at least one therapeutic compound selected from the group consisting of: (i) an opioid receptor antagonist; (ii) an opioid antagonist; and (iii) a therapeutic compound that restores TRPM3 ion channel activity. In some embodiments the therapeutic compound is naltrexone hydrochloride.
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- Lomerizine hydrochloride synthesizing method
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The invention belongs to the technical field of drug preparation and relates to a lomerizine hydrochloride synthesizing method. The lomerizine hydrochloride synthesizing method specifically comprisesthe steps of 1) heating 2, 3, 4-trimethoxybenzyl chloride and 1-Boc-piperazine under alkaline conditions for reaction at 40 DEG C for 4 h, and then adding in hydrochloric acid to obtain 1-(2, 3, 4-trimethoxybenzyl)piperazine; 2) subjecting the 1-(2, 3, 4-thrimethoxybenzyl)piperazine and 4, 4'-difluorodiphenylmethyl chloride to reaction in triethylamine to obtain 1-(di(4-fluorophenyl)methyl)-4-(2,3, 4-thrimethoxylbenzyl)piperazine; 3) recrystallizing the 1-(di(4-fluorophenyl)methyl)-4-(2, 3, 4-thrimethoxylbenzyl)piperazine in hydrochloric acid with ethanol and methyl tertiary butyl ether to obtain lomerizine hydrochloride. Compared with the prior art, the lomerizine hydrochloride synthesizing method is low in price of raw materials, extensive in resources, mild in condition, high in yieldand chemical purity, simple in treatment and free from refining treatment.
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Paragraph 0016; 0018; 0022; 0024; 0030; 0031
(2019/05/02)
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- 1-(2,3,4-tri-methoxybenzyl)-4[bis(4-fluorophenyl)methyl] piperazines are useful for treating cerebrovascular disease
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A 1-benzyl-4-benzhydrylpiperazine derivative represented by the following general formula (I) STR1 wherein R1 represents a hydrogen atom or a methoxy group, and R2 represents a hydrogen or fluorine atom, or a pharmaceutically acceptable acid addition salt thereof. The 1-benzyl-4-benzhydrylpiperazine derivative or an acid addition salt thereof is prepared by reductively condensing a benzaldehyde derivative with a fluorobenzhydrylpiperazine, or condensing a benzyl halide derivative with a fluorobenzhydrylpiperazine optionally in the presence of an acid acceptor, or condensing a benzylpiperazine with a fluorobenzhydryl halide derivative and, optionally converting the product to its acid addition salt. The 1-benzyl-4-benzhydrylpiperazine derivative is useful for improving a cerebrovascular disease.
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