38 results about "Diphenylmethylpiperazine" patented technology

A pharmaceutical composition comprising a therapeutically effective amount of a mixture consisting essentially of(i) pseudoephedrine, an individual optical isomer or a pharmaceutically acceptable salt thereof, and(ii) at least one compound selected from 2-[4-(diphenylmethyl)-1-piperazinyl]-acetic acid or amide derivatives, an individual optical isomer or a pharmaceutically acceptable salt thereof.

Stable and palatable taste masked pharmaceutical compositions of substituted benzhydrylpiperazines and processes for preparing them.

The invention relates to a class of inhibitors of non-peptidic SARS coronavirus 3CL protease and uses thereof. The inhibitor is a benzhydryl piperazine derivative, and its inhibition mechanism lies in the volume occupation and the hydrophobic interaction with 3CL protease. Utilize reversed-phase high-pressure liquid chromatography method and substrate pNA-labeled enzyme activity system to test the influence of the inhibitor on SARS coronavirus 3CL protease activity, confirm that it has inhibitory effect on 3CL protease, and cell experiments also confirm its effect on cell culture SARS coronavirus has inhibitory effect and can be used for treating and preventing SARS virus infection.

The invention discloses a preparation process of optically pure manidipine hydrochloride for treating hypertension. The preparation process comprises the following steps: a) preparing 2-(4-benzhydryl-1-piperazinyl) ethyl acetoacetate Ester, m-nitrobenzaldehyde, 3-aminocrotonate methyl ester, (S)-BINAP, ferric iron compound and reaction solvent are added in reaction vessel and react to obtain (S)-manidipine; b) gaining (S) )-manidipine and hydrogen chloride solution are added in the reactor to react, and the reaction is completed, concentrated under reduced pressure, recrystallized, and dried to obtain optically pure (S)-manidipine hydrochloride. The target product (S)-manidipine of the preparation process provided by the present invention has higher yield and ee value, and the method of the present invention is simple to operate, has short reaction time, and is suitable for industrial production.

Synthesis of levo-citilitrin chloride is carried out by taking mono-p-chlorophenacyl ketone as raw material, synthesizing mixed active mono-p-chlorobenzhydrylamine, resoluting to obtain levo-mono-p-chlorobenzhydrylamine by levo-o-chloromandelic acid, synthesizing levo-1-N-mono-p-chlorodiphenyl-methyl-4-N-toluene-p-sulfonyl-piperazine, removing protection to obtain levo-N-mono-p-chlorodiphenyl-methyl-piperazine, reacting with ethylene chlohydrin to synthesize levo-1-N-mono-p-diphenyl-methyl-4-N-piperaethanol, reacting with sodium acetate chloride, and adding into hydrochloride to obtain final product. It costs low and is simple and can be used for industrial production.

The present invention is directed to compositions of taste-masked microparticles comprising a substituted benzhydrylpiperazine coated and a taste-masking layer comprising a water-insoluble polymer and a gastrosoluble polymer, and methods of making such taste-masked microparticles. The present invention is also directed to stable orally disintegrating compositions comprising taste-masked microparticles of a substituted benzhydrylpiperazine and rapidly dispersing granules, and methods of making such orally disintegrating compositions.

The present invention relates to the preparation process of diphenyl ofloxacin and its application in preparing medicine for treating cardiac and cerebral vascular diseases. The preparation process includes the following steps: A) preparing gamma-chloro-4-fluorobenzene-1-butanone through the reaction between gamma-butyrolactone and sulfoxide chloride to obtain gamma-butyryl chloride and the subsequent reaction in mixed solvent with catalyst; B) preparing benzhydryl piperazine through the reaction between diphenylcaabinol and concentrated hydrochloric acid to obtain diphenyl chloromethane, the subsequent reaction in mixed solvent with catalyst and filtering; and C) preparing the product diphenyl ofloxacin with proper amount of benzhydryl piperazine, gamma-chloro-4-fluorobenzene-1-butanone, solvent methyl isobutyl ketone and catalyst potassium iodide and potassium carbonate, and through mixing and reaction.

The present invention provides: a novel compound which has a useful pharmacological action for treating heart failure or shock without increasing heart rate; and a pharmaceutical composition using the same. The present invention relates to a diphenylmethyl piperazine derivative represented by general formula (I)(In the formula, R1 is a hydrogen atom or a hydroxy group. R2 is a hydrogen atom, a halogen atom, a hydroxy group, an alkyl group having one to five carbon atoms, or an alkoxyl group having one to five carbon atoms, excluding the case where R1 is a hydroxy group and R2 is a chlorine atom.) or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing the same.

The invention relates to a substituted benzhydryl piperazine derivative and a preparation method and an application of the substituted benzhydryl piperazine derivative. The substituted benzhydryl piperazine derivative has a compound in structural formula (I): FORMULA. A part of compound provided by the invention is administrated preventively to prolong the survival time of mice suffering from acute cerebral ischemia so that the derivative has a certain neuroprotective effect of preventing cerebral ischemia. Thus, the compound provided by the invention can be used to prepare medicines for treating cerebral arterial thrombosis.

The invention belongs to the technical field of medicine, and relates to 2-[(pyridyl-2-yl methyl)thio]-1H-benzimidazole compounds, a preparation method thereof and application of the compounds in preparation of drugs for antitumor diseases. The structural general formula of the 2-[(pyridyl-2-yl methyl)thio]-1H-benzimidazole compounds and prodrugs, pharmaceutically active metabolites and pharmaceutically acceptable salts of the 2-[(pyridyl-2-yl methyl)thio]-1H-benzimidazole compounds are shown in the description, wherein R1 and R2 are the same or different, and are selected from hydrogen, C3-C6cycloalkyl groups, phenyl groups, halogen-substituted phenyl groups, C1-C4 alkoxy-substituted phenyl groups, phenyl groups with simultaneous substitution of halogen and C1-C4 alkoxy groups and benzylgroups, or substituted or unsubstituted phenylpiperazinyl, benzylpiperazinyl or diphenylmethylpiperazinyl groups are formed by R1, R2 and nitrogen atoms attached to R1 and R2; and the substituent groups comprise C1-C4 alkyl groups, C1-C4 alkoxy groups and halogen, and R3 and R5 can be selected from H and C1-C4 alkyl groups. The synthesis method of the compounds is simple and convenient, and is suitable for industrial production, and it is shown by biological activity tests that the compounds have antitumor activity, and are novel antitumor drugs.

The invention belongs to the technical field of medicine, and relates to 2-[(pyridin-2-ylmethyl)thio]-1H-benzimidazole compounds and their preparation methods and applications. The general formula of described 2-[(pyridin-2-ylmethyl)thio]-1H-benzimidazoles and pharmaceutically acceptable salts is as follows: R 1 , R 2 Same or different, selected from hydrogen, C1‑C8 alkyl, C3‑C6 cycloalkyl, phenyl, halogen substituted phenyl, C1‑C4 alkyl substituted phenyl, C1‑C4 alkoxy substituted phenyl , phenyl substituted with halogen and C1‑C4 alkoxy, phenyl substituted with halogen and C1‑C4 alkoxy, phenyl substituted with halogen substituted C1‑C4 alkyl, benzyl, 4‑benzyloxy Phenyl; or R 1 , R 2 Together with the nitrogen atoms connected to them, they form substituted or unsubstituted morpholinyl, phenylpiperazine or benzhydrylpiperazine; the substituents are C1-C4 alkoxy, C1-C4 alkyl, halogen; R 3 , R 5 Can be selected from H, C1-C4 alkyl. The synthesis method of the compound of the invention is simple and convenient, suitable for industrial production, and has obvious antitumor activity.