129 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 discloses a preparation method for vortioxetine. The preparation method comprises the following steps of (1) performing diazotization on a compound 4 to obtain a compound 5; (2) coupling the compound 5 and a compound 6 to obtain a compound 7; (3) deacetylating the compound 7 to obtain 1-(2-(2,4-dimethyl phenylthio)phenyl)piperazine (i.e. vortioxetine) shown in formula 8. According to the method, operation is simplified, the yield is increased, the cost is greatly reduced, and the method is more suitable for industrial expansion, and has remarkable creativity and practical application value.

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.

The invention discloses a phenyl piperazidine heterocyclic medicinal compound. The compound has high affinity to a dopamine D3 receptor, so that the compound can be used for treating addiction to and dependence on medicines such as cocaine, and a central nervous system disorder relevant to the addiction and the dependence. The compound is a 4-[4-(substituted phenyl) piperazine piperazinyl-1]-butylcarbamic acid substituted aromatic ester derivative with a structural formula as Formula (1) as shown in the specification. A synthetic method of the derivate comprises the steps that substituted aniline and 2-(beta-chloroethyl) amine hydrochloride reacts in a solvent by taking inorganic base as an acid-binding agent to form corresponding substituted phenyl piperazidine hydrochloride 1; substituted phenyl piperazidine hydrochloride 1 and N-(delta-bromobutyl) phthalimide react in acetonitrile by taking K2CO3 as an acid-binding agent and under catalysis of KI to form a reaction intermediate 2; the intermediate 2 is subjected to hydrazinolysis to form an intermediate 3; and the intermediate 3 and an intermediate 5 are condensed by taking triethylamine as an acid-binding agent and a catalyst to form a target product I. The intermediate 5 is obtained in a manner that triphosgene and substituted aromatic phenol conduct partial condensation reaction in methylene chloride.

The invention discloses phenylpiperazine derivatives and pharmaceutically acceptable salts thereof. The invention is characterized in that: the derivatives have the structure shown as a formula I; and in the formula, R1 refers to -H, -R, -OR, -COOR, halogen or -CN group, R refers to alkyl, the substitution position of R1 on a benzene ring is a para-position, ortho-position or meta-position of piperazine, m is a natural number ranging from 0 to 2, and R2 refers to a substituted or unsubstituted carboxyl group or sulfonic acid group. The phenylpiperazine derivatives and pharmaceutically acceptable salts thereof can be prepared into medicines for inhibiting tumor cell metastasis and tumor angiogenesis, medicines for treating liver cancer, breast cancer, ovarian cancer, gastric cancer, colon cancer, lung cancer or melanoma, tumor chemotherapy medicines and auxiliary medicines in surgical therapy.

The invention provides a detection method of 1-[2-(2, 4-dimethylphenylthioalkyl)phenyl]piperazine or salt thereof. The method includes the steps of: taking a methanol solution containing 1-[2-(2, 4-dimethylphenylthioalkyl)phenyl]piperazine or salt thereof as a test solution, and performing detection according to high performance liquid chromatography conditions, which specifically includes: use of pentafluorophenyl as the filler; employment of a methanol-0.02mol.L<-1> ammonium acetate buffer solution as the mobile phase A, and taking of acetonitrile as the mobile phase B; and conducting gradient elution. The detection method has the advantages of good separation degree of active components and impurities, stable baseline, and good repeatability and stability of a sample and impurities, thus being more beneficial to quality control.

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-HT1A 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 invention discloses an amide-type phenylpiperazine derivative, salt and anapplication thereof in preparing medicines for treating benign prostatic hyperplasia. The phenylpiperazine type compounds can selectively antagonize <1A>- or <1D>- adrenergic receptors. Researches indicate that an <1A> / <1D> selective antagonist has high urinary tract selectivity, and at the same time, is not liable to cause side effects of postural hypotension, exhaustion, drowsiness and the like are not . When being used as an antagonist of the <1A>- or <1D>- adrenergic receptors, the compounds, provided by the invention, can be used for treating benign prostatic hyperplasia.

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 present invention relates to certain substituted N-phenyl-piperazine derivatives of Formula: (I) that are modulators of the 5HT2c receptor. Accordingly, compounds of the present invention are useful for the prophylaxis or treatment of 5HT2c receptor associated diseases or disorders, such as, obesity, Alzheimer Disease, erectile dysfunction and related disorders.

The use of 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine in the treatment of pain and residual symptoms in depression is provided.

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.

Provided is at least one crystalline hydrate of (S)-[N-3-(3'-fluoro-4'-(4''-phenyl piperazinyl)) phenyl-2-oxo-5-oxazolidinyl] methyl acetamide, such as those with the following formula, wherein y is a number ranging from 1 / 12 to 1. Also provided are methods for the preparation of such crystalline hydrates, pharmaceutical compositions comprising such crystalline hydrates, and methods for their uses.

The invention discloses a shale intercalation inhibitor prepared from environment-friendly hyperbranched polyamino acid, and belongs to the technical field of oil and gas field drilling. The hyperbranched polyamino acid is synthesized by taking monoprimary amine amino acids with different hydrophobic chain lengths, N-phenylpiperazine and ester compounds containing diene bonds as raw materials through the following steps: S1, synthesizing amino acid methyl ester; S2, synthesizing a hyperbranched polyamino acid intermediate; and S3, synthesizing hyperbranched polyamino acid. The shale intercalation inhibitor prepared from hyperbranched polyamino acid is prepared from hyperbranched polyamino acid and water, wherein the mass ratio of hyperbranched polyamino acid in the shale intercalation inhibitor is 0.5-3%. The hyperbranched polyamino acid has good biodegradability, is safe and non-toxic, and has obviously improved inhibition performance compared with similar shale intercalation inhibitors, the raw materials are easy to obtain and low in price, and the provided synthesis method is stable and reliable, and is suitable for industrial production.

The current invention describes novel immunogens which are used in the production of novel antibodies with unique binding properties in that they cross-react with a variety of phenylpiperazine derivatives. These antibodies enable methods and kits to detect and / or determine phenylpiperazine derivatives (for example mCPP, TFMPP and MeOPP) in an in vitro sample which are advantageous over currently available analytical methods in terms of cost, ease of use, speed and sensitivity.

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 provides new therapeutic uses of 1-[2-(2,4-dimethyl-phenylsulfanyl)phenyl]-piperazine and pharmaceutically acceptable salts thereof.

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 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.