36 results about "Methyldopa" patented technology

A sympatholytic cardiovascular agent delivered by a drug delivery pump to a central nervous system site to alleviate symptoms and otherwise treat heart failure (HF) and pathologies associated with HF. The drug delivery pump can be external or implantable infusion pump (IIP) coupled with a drug infusion catheter extending to the site. A patient activator can command delivery of a dosage and / or an implantable heart monitor (IHM) coupled with a sensor can detect physiologic parameters associated with HF (or pathologies associated with HF) and trigger dosage delivery. The IIP and IHM can be combined into a single implantable medical device (IMD) or can constitute separate IMDs that communicate by any of known communication mechanisms. The sympatholytic cardiovascular agent is one of the group consisting of an alpha-adrenergic agonist and an alpha2-adrenergic agonist, e.g., clonidine, p-aminoclonidine, guanabenz, lidamidine, tizanidine, moxonidine, methyldopa, xylazine, guanfacine, detomidine, medetomidine, and dexmedetomidine.

The present disclosure relates to methods of reducing the number of abnormal PBMC cells in a leukemia patient. The methods may include administering an effective amount of a drug, which may not be indicated for leukemia, or an antibody-drug conjugate. The antibody-drug conjugate includes an antibody selected from the group consisting of an anti-α2-adrenoreceptor antibody, an anti-β adrenoceptor antibody, an anti-trace amine-associated receptor 1 antibody, an anti-dopamine receptor antibody, and an anti-serotonin receptor antibody; a drug selected from the group consisting of isoproterenol, methyldopa, olanzapine, and a derivative thereof; and a linker that conjugates the antibody and the drug.

The invention belongs to the technical field of one of key steps of chemical synthesis of medicine methyldopa [alpha-methyl-(3,4-dihydroxyphenyl]-alpha-alanine] or synthesis of chiral medicine L-methyldopa [L-alpha-methyl-(3,4-dihydroxyphenyl]-alpha-alanine]: reaction for preparing methyldopa by hydrolyzing 5-methyl-5-(3,4-dimethoxybenzyl)hydantoin. The invention relates to a method for preparing methyldopa or L-methyldopa by directly hydrolyzing 5-methyl-5-(3,4-dimethoxybenzyl)hydantoin with acid at appropriate temperature. When disacidification is carried out under reduced pressure after the reaction finishes, N2 is introduced to protect the product from easy oxidative stain and accelerate the disacidification. In order to protect the product from deterioration, the vacuum drying temperature of the product is generally carried out at 50 DEG C for 5 hours.

The invention discloses a recycling method and application of an L-methyldopa intermediate. The recycling method comprises the following steps: hydrolyzing L-3-(3,4-dimethoxy phenyl)-2-amino-2-methyl propionitrile hydrochloride by utilizing hydrochloric acid, and filtering to obtaining L-3-(3,4-dimethoxy phenyl)-2-methyl alanine hydrochloride and mother liquor, adding haloid salt or ammonium salt into the mother liquor, carrying out vacuum distillation, concentrating until volume is less than or equal to 1 / 3 of the original volume, and filtering, wherein a filter cake is namely the recycled 3-(3,4-dimethoxy phenyl)-2-methyl alanine hydrochloride solid. The recycling method disclosed by the invention has the advantages that L-methyldopa can be recycled from 3-(3,4-dimethoxy phenyl)-2-methyl alanine hydrochloride production waste liquor, and ammonia nitrogen and COD in wastewater can also be reduced, so that the recycling method accords with the green chemistry concept.

The invention belongs to the technical field of one critical step in microwave nitrile hydrolysis and demethylation hydrolysis of chemical synthesis medicine methyldopa [alpha-methyl-(3,4-dyhydroxy phenyl)-alpha-aminopropionic acid, similarly hereinafter] or synthetic chiral medicine L-methyldopa [L-alpha-methyl-(3,4-dyhydroxy phenyl)-alpha-aminopropionic acid, similarly hereinafter], i.e. the chemical reaction for preparing methyldopa or L-methyldopa from alpha-methyl-(3,4-dimethoxy phenyl)-alpha-aminopropionitrile or L-alpha-methyl-(3,4-dimethoxy phenyl)-alpha-aminopropionitrile through microwave nitrile hydrolysis and demethylation hydrolysis. The microwave hydrolysis uses low-concentration hydrochloric acid or hydrobromic acid, so the energy sources and the economic cost are reduced, the acid wastewater discharge is reduced, by-products are reduced, and the purity and the yield of products are improved.

The invention relates to a method for preparing methyldopa or L-methyldopa through microwave basic hydrolysis 5-methyl-5-(3,4-dimethoxy benzyl) hydantoin. Various alkaline aqueous solutions with different concentrations are adopted to hydrolyze 5-methyl-5-(3,4-dimethoxy benzyl) hydantoin under different microwave power and radiation times to prepare DL-alpha-methyl-(3,4-dimethoxy benzyl)-alpha-aminopropionic acid salt which is hydrolyzed in an acid aqueous solution to prepare methyldopa[DL-alpha-methyl-(3,4-dimethoxy benzyl)-alpha-aminopropionic acid] or L-methyldopa[L-alpha-methyl-(3,4-dimethoxy benzyl)-alpha-aminopropionic acid]. When the method is used for hydrolyzing DL-alpha-methyl-(3,4-dimethoxy benzyl)-alpha-aminopropionic acid (or L-alpha-methyl-(3,4-dimethoxy benzyl)-alpha-aminopropionic acid), the molar ratio of a substrate and hydrogen bromide (Hbr) is 1:10-20, and the molar ratio of the substrate and chlorine hydride (HCl) is 1:10-30. The hydrolysis reaction is smooth when acid using amount is big, and disacidify pressure after the hydrolysis reaction is reduced when the acid using amount is small.

The invention belongs to the technical field of nitrile group hydrolysis and demethylation hydrolysis reaction which is one of the key steps for chemical synthesis of a methyldopa drug or a chiral drug of L-methyldopa [L-alpha-methyl-(3,4-dimethoxyphenyl)-alpha-aminopropionitrile, the same below], that is, a reaction for preparing alpha-methyl-(3,4-dimethoxyphenyl)-alpha-aminopropionitrile or L-alpha-methyl-(3,4-dimethoxyphenyl)-alpha-aminopropionitrile by nitrile group hydrolysis and demethylation hydrolysis. Under an acidic condition, the preparation of methyldopa by nitrile group hydrolysis and demethylation hydrolysis of alpha-methyl-(3,4-dimethoxyphenyl)-alpha-aminopropionitrile (or hydrochloride) requires a long period, a large material using amount, and heating hydrolysis of high-concentration acids (and the long-time heating of the high-concentration acids allows the acids to volatilize, so continuous acid addition is required during hydrolysis); however, the long-time high-concentration acid heating hydrolysis can cause unknown change of certain compound structures of alpha-methyl-(3,4-dimethoxyphenyl)-alpha-aminopropionitrile (or hydrochloride), and thus by-products are increased, and the purity and yield are decreased. Therefore, improvement of the hydrolysis technology is necessary.

The invention belongs to the field of chemical synthesis, and in particular relates to a method for synthesizing carbidopa. The method is characterized by comprising the following steps of: reacting oxaziridine with methyldopa ester to obtain methyldopa imido ester, and hydrolyzing to obtain the carbidopa. The method has the advantages that the carbidopa is prepared by a brand-new process, the used raw materials are favorable for synthesizing a medicine, and the prepared carbidopa is high in yield and quality.

The present invention provides: a pharmaceutical composition that is to be intraocularly or orally administered for preventing or treating a retinal disease (e.g., age-related macular degeneration) of a patient who needs to be treated, or inhibiting the progression of the disease, and that contains a pharmaceutically-acceptable carrier and an effective amount of at least one compound selected from the group consisting of apomorphine, eseroline, ethoxyquin, methyldopa, olanzapine, indapamide, and the like; and a method.

The invention discloses a method for refining carbidopa, which comprises the following steps: diluting a crude carbidopa product with water, regulating the pH value to below 6.5 with acid, and heating to 50-110 DEG C under the nitrogen protection or / and reducer addition condition, thereby obtaining a crude product system; adding a decolorant into the crude product system to decolorize at 50-110 DEG C for 5-60 minutes; after decolorizing, filtering while the crude product system is hot to obtain a filtrate, stirring and cooling the filtrate to 0-30 DEG C, and continuing stirring at 0-30 DEG C for 0.5-5 hours to obtain a refined system; and filtering the refined system, washing the filter cake with water, and carrying out vacuum drying to obtain the finished carbidopa product. The method disclosed by the invention has the advantages of simple preparation method, favorable controllability, strong operability, high methyldopa (impurity) removal rate, high yield and low production cost, can easily implement industrial production, has high economic benefit in the industrial production, can be easily popularized, and has wide application prospects.

The invention relates to a methyldopa-silicon dioxide-stearyl alcohol pharmaceutical composition and a preparation method thereof. The pharmaceutical composition is mainly applied to the preparation of methyldopa tablets. The pharmaceutical composition is prepared by carrying out polymerization on methyldopa, stearyl alcohol and colloidal silicon dioxide by using a spray drying technology; the Hausner ratio range of particles is 1.10-1.18, and the Carr index range of the particles is 10-15%; the pharmaceutical composition has good fluidity and compressibility, so that the compressibility and the tablet formation property are improved; furthermore, the medicine part is prevented from being oxidized and discoloring after being combined with water, so that the storage stability of the preparation is obviously improved.