121 results about "Phenylpiperazine" patented technology

The present invention relates to a novel class of substituted phenylpiperazinyl derivatives having the formula (I) wherein X, Z, Y, U,V, Alk, W, R<1> , R<2>, R<3>, R<11>, R<12>, R<13> n, m and the dotted line are as defined in the description. The compounds of the invention are dopamine D4 receptor ligands and are therefore useful for the treatment of certain psychiatric and neurologic disorders, including psychosis.

The invention provides compounds represented by the general formula I wherein the substituents are defined in the application. The compounds are useful in the treatment of an affective disorder, including depression, anxiety disorders including general anxiety disorder and panic disorder and obsessive compulsive disorder.

1-[2-(2,4-dimethylphenylsulphanyl)phenyl]piperazine exhibits potent activity on SERT, 5-HT₃ and 5-HT_1A and may as such be useful for the treatment of cognitive impairment, especially in depressed patients.

The present invention discloses a phenylpiperazine derivative, a use method and uses thereof, and particularly relates to a class of novel (2-(heteroaryloxo)phenyl)piperazine derivatives and a pharmaceutical composition containing the compound, wherein the derivatives and the composition can be used for inhibiting 5-hydroxytryptamine reuptake. The present invention further relates to a method for preparing the compounds and the pharmaceutical composition, and uses of the compounds and the pharmaceutical composition in treatment of central nervous system dysfunction, particularly affective disorders.

The invention discloses an H2S corrosion resistant ground gathering system corrosion inhibitor and a preparation method thereof. The H2S corrosion resistant ground gathering system corrosion inhibitor comprises the following ingredients in mass percent: 20-40% of main ingredient, N-benzyl-N '-phenylpiperazine and 60-80% of compound, wherein the compound comprises the following ingredients in masspercent: 5-15% of methoxy propyl amine, 5-15% of hydroxy ethylidene diphosphate, 5-20% of methylamine, 5-20% of emulsifying agent and 40-50% of solvent; the main ingredient, N-benzyl-N '-phenylpiperazine is prepared by N-phenylpiperazine and benzyl chloride. The corrosion inhibitor of the invention is a water-soluble corrosion inhibitor, so that the corrosion inhibitor can be extensively applied in the H2S corrosion and high mineralization water of pipelines in the ground gathering system to effectively control the H2S corrosion on the metallic materials in the ground gathering pipelines; besides, the corrosion inhibitor has the advantages of non pungent smell, little dosage, high corrosion inhibition efficiency, simple and convenient production, good water-soluble dispersibility, uniformand dense adsorption film, and non spot corrosion or pointed corrosion on material protection.

The present invention is directed to phenylpiperazine cycloalkanol derivatives, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromylagia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.

The invention belongs to the field of biological pharmacy, relates to a medicinal use of 4-(4-phenylpiperazino)quinazoline derivatives and especially relates to a use of the 4-(4-phenylpiperazino)quinazoline derivatives in preparation of drugs for treating nervous system diseases and especially in preparation of dopamine D3 receptor inhibitors. A result of a biological activity test shows that the 4-(4-phenylpiperazino)quinazoline derivatives have good effects of inhibiting D3 receptors. The 4-(4-phenylpiperazino)quinazoline derivatives can be used as drug lead compounds, be synthesized into dopamine D3 receptor inhibitors, and be further used for preparation of drugs for treating schizophrenia and Parkinsonism caused by dopamine system dysfunction.

The invention discloses phenylpiperazine derivatives, a using method thereof and uses of the derivatives, and particularly relates to novel (2-(heteroaryloxy) phenyl)piperazine derivatives and medicine compositions comprising the compounds, wherein the derivatives and the compositions can be used for inhibiting serotonin reuptake. The invention also relates to methods of preparing the compounds and the medicine compositions, and uses of the compounds and the medicine compositions in treatment of central nervous system dysfunction, especially affective disturbance.

The invention relates to environment-sensitive alpha1-adrenergic receptor near infrared fluorescence ligands and an application thereof. The ligands are represented by general formula (I); and in the formula (I), R1 is a pharmacophore quinazoline or phenylpiperazine, R2 is a different substituent, X is a linker (carbon chain or triazole ring) of different types, n1 represents the carbon number and is 1-6, and X2 is an iodide or bromide ion. The molecules of the fluorescence ligands have high affinity to an alpha1-adrenergic receptor, and the fluorescence does not substantially enhance with the polarity decrease or viscosity increase of surrounding environment. When the ligand molecules are combined with the alpha1-adrenergic receptor, the molecules enter hydrophobic environment and release a strong fluorescence signal, so visualization is easily realized, and the signal to noise ratio is good. The fluorescence ligands can be used in researches of the pharmacologic and physiological characteristics of the alpha1-adrenergic receptor as a tool drug. A preparation method of like compounds has the advantages of maturation, mild reaction conditions, cheap and easily available raw materials, and convenient operation and post-treatment.

The invention provides an azole antifungal compound and its pharmaceutically acceptable salt. The structural general formula of the azole antifungal compound is shown in the specification, wherein R is selected from various aliphatic primary amine or secondary amine, aromatic primary amine or secondary amine and various substituted phenylpiperazine; the substituent group on phenyl of the substituted phenylpiperazine is hydrogen, alkyl group, halogen, cyanogroup, nitro-group, amino group or alkoxy group, is arranged at ortho, meta or para position of phenyl ring, and is monosubstituted or polysubstituted; the alkyl group is the alkyl group with 1-4 carbon atoms; the halogen is selected from F, Cl, Br or I; and the alkoxy group is selected from methoxy, ethoxy and t-butyl oxygroup. The compound provided by the invention has strong antifungal activity to deep fungi. In comparison with present antifungal drugs applied in clinic, the compound provided by the invention has advantages of high efficiency, low toxicity, wide antifungal spectrum and the like. Thus, the compound can be applied to prepare antifungal drugs. A preparation method of the compound is simple and has high yield. The prepared compound has a good antifungal effect.

The invention relates to N-benzylbenzamide compounds represented by formula (I), a preparation method and a medicinal use thereof, and an anti-tuberculosis medicinal composition adopting the compounds as an effective component. The N-benzylbenzamide compounds are concretely characterized in that a substituent group in the para-position of a benzyl group of the N-benzylbenzamide compounds is a nitrogen-containing heterocyclic segment; and in the formula (I), R represents a trifluoromethyl group or a nitro group, and X represents a 4-thiomorpholinyl group, an octahydro-2H-isoindole-2-yl group, an isoindoline-2-yl group, a 4-substituted piperidine-1-yl group, a (4-substituted phenyl)piperidine-1-yl group or a (4-substituted phenyl)piperazine-1-yl group.

The invention discloses substituted phenyl piperazinyl aralkylone derivatives and application thereof to the preparation of analgesics. The derivatives of the invention may be free alkali or salts of compounds with a general structural formula. Pharmacological experiments show that the compounds of the invention are nonopioid analgesics and have high analgesic activity, relatively poorer toxic or side effect and the general structural formula.

The invention relates to a phenyl piperazine small-molecule fluorescent probe of an alpha1-adrenergic receptor and application thereof. General formulas of the small-molecule fluorescent probe are shown as a formula (I) and a formula (II) respectively, wherein R1 represents a single substituent or a multi-substituent of hydroxy, methyl, amino and halogen, and R2 and R3 represent various fluorophores. The fluorescent probe molecule can be used for marking the alpha-adrenergic receptor and be used as a tool drug for researching pharmacological and physiological characteristics of the alpha-adrenergic receptor. In addition, the preparation method of the compound has mild reaction conditions, cheap and easily available raw materials, and simple operations and post-treatments.

The invention relates to a method for preparing a medicine intermediate, namely 1-methyl-3-phenyl-piperazine. Epoxy phenylethane and N-methyl ethanolamine react for ring opening in a methylbenzene solution and further react with thionyl chloride to obtain N-(2- chloroethyl)-N-methyl-2-chloro-2-phenylethylamine hydrochloride, the hydrochloride reacts with toluene sulfonamide and sodium hydroxide in a DMF solution to obtain 1-methyl-4-p-toluenesufonyl-3-phenylpiperazine, the 1-methyl-4-p-toluenesufonyl-3-phenylpiperazine reacts with concentrated hydrochloric acid to remove sulfonyl, and a product is obtained through neutralization extraction and recrystallization. Compared with the prior art, the method for preparing the 1-methyl-3-phenyl-piperazine has the advantages of low cost of selected raw materials, cost conservation, few synthesis steps, convenient and safe operation, simple post-treatment, high reaction yield, high product purity, good quality, and suitability for industrialized application.

The invention discloses a preparation method of a posaconazole intermediate, namely 1-(4-aminophenyl)-4-(4-hydroxylphenyl)piperazine, belonging to the field of medicinal chemistry. The preparation method comprises the following steps: S1, with chlorobromobenzene and anhydrous piperazine as raw materials, generating 1,4-bis(4-chlorophenyl)piperazine under certain conditions; S2, performing single-side methylation on the product generated in the step S1 to obtain 1-(4-methoxyphenyl)-4-(4-chlorophenyl)piperazine; S3, performing ammoniation on the product in the step S2 to obtain 1-(4-methoxyphenyl)-4-(4-aminophenyl)piperazine; and S4, demethylating the product obtained in the step S3, and carrying out crystallizing and purifying to obtain the 1-(4-aminophenyl)-4-(4-hydroxylphenyl)piperazine.The raw materials used in the preparation method are very cheap; reaction conditions are relatively simple; the method is easy to implement; yield is high; and the cost of a final product can be obviously reduced.

The invention provides a novel methyl-phenyl-piperazinyl modified polysiloxane and a preparation method thereof. The methyl-phenyl-piperazinyl modified polysiloxane is synthesized through ring-opening polymerization and equilibrium condensation polymerization with otcamethylcyclotetrasiloxane (D4), methylphenyldimethoxysilane (MPDS), gamma-piperazinylpropylmethyldimethoxysilane and hexamethyldisiloxane as raw materials and potassium hydroxide (KOH) as an initiator for ring opening of D4 and a catalyst for condensation polymerization. The synthesized methyl-phenyl-piperazinyl modified polysiloxane is applicable as an oiling agent for preoxidation of a carbon fiber precursor.

The invention discloses a method for synthesizing mirtazapine. According to the method, 2-halogenated nicotinonitrile is used as an initial compound, and 2-chloronicotinamide, 2-(4-methyl-2phenyl-1-piperazinyl)nicotinamide, 2-(4-methyl-2phenyl-1-piperazinyl)nicotinic acid, 1-(3-hydroxymethylpyridyl-2-)-4-methyl-2-phenylpiperazine and other intermediate products are sequentially synthesized to prepare the mirtazapine. Against the defects in a current mirtazapine synthesizing method, the process is improved, a new synthesizing route is designed, and a preparation method which is economical and is easy for practical operation is provided to mirtazapine synthesis. The method is suitable for large-scale industrial production.

The present invention provides a process for producing 2-(4-methyl-2-phenylpiperazin-1-yl)-3-cyanopyridine which comprises reacting 1-methyl-3-phenylpiperazine with 2-chloro-3-cyanopyridine in the presence of an organic base and in the absence of alkali metal halide in an polar aprotic organic solvent.

The invention discloses a surfactant for development of a low-permeability oil reservoir and a preparation method of the surfactant. The preparation method comprises the following steps: reacting 1-(4-hydroxyphenyl)piperazine with organic acid to prepare an amidation product; reacting an amidation product with ethylene oxide and propylene oxide in sequence to prepare a nonionic product containingpolyoxyethylene and polyoxypropylene chain segments; and finally, sulfonating the non-ionic product through fuming sulfuric acid to prepare the anionic/non-ionic surfactant. The surfactant has excellent dissolving, temperature-resistant and salt-resistant properties, the adsorption, interfacial tension change, wettability adjustment and other properties of the surfactant are controllable, and theself-imbibition recovery ratio of the low-permeability oil reservoir can be remarkably increased.

The invention relates to a novel method for preparing vortioxetine. Reduction, nucleophilic substitution and coupling are conducted on a 2-nitroiodobenzene compound, and a compound of 1-[2-(2,4-dimethyl phenyl sulfanyl)-phenyl]methyl piperazine; then the obtained compound reacts with phenyl chloroformate to obtain 1-[2-(2,4-dimethyl phenyl sulfanyl)-phenyl]piperazine-1-carboxylic acid phenyl ester which generates vortioxetine after being hydrolyzed under the alkaline condition.

The invention relates to the technical field of synthetic rubber, and discloses rubber containing modified graphene, which comprises the following components: rubber, carbon black, zinc oxide, stearic acid, sulfur, an accelerant, a scorch retarder and modified graphene. The modified graphene is obtained by fully mixing and ball-milling graphite and a modifier, then adding tert-butyl nitrite and a solvent, mixing and ball-milling, fully mixing, washing and drying; and the modifying agent is one or more of amino propionyl aniline, 4-aminobenzoyl aniline, 2-amino-N-cyclohexyl-N-methyl benzene methylamine, 4-(4-isopropyl piperazine-1-yl) aniline, (4-aminobenzene)-4-(4-methoxyphenyl) piperazine, (4-(4-aminobenzyl) piperazine-1-yl) ethanone and (4-aminobenzene)-4-(4-methoxyphenyl) piperazine. Rubber formed by mixing and refining the modified graphene and other components of rubber has a better anti-aging effect.