40 results about "Benzylpiperazine" patented technology

Although it is known that certain benzylpiperazine-aminopyridines or open chain forms thereof are effective in stimulating neural growth in in vitro tests, it has now been surprisingly found that administering these compounds in a dosage range of 10 mg / day-130 mg / day over 25-35 days is effective in treating Major Depressive Disorder (MDD) such that statistically significant results can be obtained with samples of only six subjects.

Disclosed is a benzylpiperizine compound represented by formula (1) or a pharmaceutically acceptable salt thereof, which is useful as a medicinal agent such as an antidepressant agent. (In the formula (1), R1 represents a hydrogen atom or a methyl group; R2 is a group bound in a p- or m-position relative to a methylene group and represents a chlorine atom bound in a p-position, a bromine atom bound in a p-position, a methyl group bound in a p-position, a chlorine atom bound in a m-position or a bromine atom bound to in a m-position; X represents a methylene or an oxygen atom; and n represents an integer of 1 to 3.)

The invention discloses a camptothecin sulfonyl amidine compound and a preparation method and application thereof. The camptothecin sulfonyl amidine compound is shown in the formula 1, wherein in the formula, R1 is any one of methyl, ethyl, p-chlorophenyl, p-nitrophenyl, p-methylphenyl, p-fluorophenyl, phenyl, thienyl, pyridyl and naphthyl; R2 is any one of hydrogen, fluorine and methoxy. The preparation method of the camptothecin sulfonyl amidine compound includes the steps that 7-benzylpiperazine-camptothecin trifluoroacetate is dissolved into methylene dichloride, a catalyst (triethylamine) is added for stirring to clarify a solvent, then a sulfonyl azide and alkyne are sequentially added, finally, copper iodide is added for a catalytic reaction, after completion, methylene dichloride is used for a quenching reaction, then the solvent is removed, and a crude product of the target product is obtained. The camptothecin sulfonyl amidine compound can be applied to preparation of medicine for treating all kinds of cancers.

The invention relates to the detection and quantification of 1-benzylpiperazine and its metabolites. The invention is underpinned by novel polyclonal antibodies with unique binding properties which enable immunoassay methods and kits for various applications.

The invention discloses a substitutive (S)-benaldehyde sulfonyl pyrrolidine-3-amino derivative, and a preparation method and application thereof. The structure of the compound is shown in an equation I. The preparation method includes: different substitutive alpha-toluenesulfonyl chloride and (S)-3-tert-butoxycarbonyl amino pyrrolidine are reacted, deprotection of a reaction product is performed so that an important intermediate is generated; and another intermediate can be prepared from different substitutive benzylpiperazine via 2-chloromethylation. The two intermediates are reacted in tetrahydrofuran in a backflow manner overnight, and the structure as shown in the equation I can be obtained by thin layer chromatography. A compound has an excellent tumor activity inhibiting effect, and has important practical value and application prospect in the field of preparation of anti-tumor medicines.

The invention discloses the application of a genistein benzylpiperazine derivative in the field of diabetes, wherein the molecular formula of the genistein benzylpiperazine derivative is: C 27 h 28 N 2 o 5 ; Molecular weight: 460.52; Name: 8‑((4‑(2,4‑dimethoxyphenyl)piperazin‑1‑yl)methyl)‑5,7‑dihydroxy‑3‑(4‑hydroxy phenyl)-4H-benzopyran-4-one. It has the effect of significantly reducing fasting blood sugar by activating AMPK and inhibiting NF-κB pathway, so this derivative can be used in the field of diabetes.

Disclosed are compounds of the formula:or the pharmaceutically acceptable addition salts thereof wherein:R1 is halogen or C1–C4 alkyl; andR2 and R3 are the same or different and represent hydrogen, halogen, C1–C4 alkyl, C1–C4 alkoxy, alkylthio, hydroxy, amino, mono(C1–C4)alkylamino, di(C1–C4)alkylamino, orR2 and R3 together represent a 4 carbon alkenylene moiety that together with the phenyl ring to which they are attached form a naphthyl moiety,which compounds are useful in the treatment of neuropsycological diseases such as schizophrenia, psychotic depression and mania.

The invention discloses a 2-aminothiazole-amide derivative, its preparation method and application. The structural formula of the compound is shown as formula I, wherein R1 is H, or one or more of the following mono-substituted or multi-substituted groups on a benzene ring: fluorine, chlorine, bromine, methyl, methoxyl, hydroxyl, nitro, amino, trifluoromethyl and cyano; R2 is -CH2-, -CO-, -NHCO- or -S02-; R3 is C or N; R4 is C, N, O or S; R5 is C or N; R6 is hydrogen, fluorine, chlorine, bromine, methyl, methoxyl, hydroxyl, mercapto, amino, methylamino, ethylamino, morpholine, piperazine, methyl piperazine, ethyl piperazine, benzyl piperazine, p-methoxyl benzyl piperazine or p-chlorobenzyl piperazine; R7 is -H, -F, -Cl, -Br, -COOCH3, -COOCH2CH3, -CONH2, -CONHCH3 or -CONHCH2CH3; and n is 0 or 1 or 2. The compound provided in the invention has very good anti-tumor activity, and has important practical value and application prospects in the antitumor medicine preparation field. (Formula I).

The invention belongs to the technical field of fluorescent probes, and particularly relates to a 1, 8-naphthalimide derivative and application. The invention discloses application of 3-[6-(4-benzyl piperazine-1-yl)-1, 3-dioxo-1H-benzo [iso] quinoline-2 (3H)-yl] propionic acid in preparation of a fluorescent probe for detecting intracellular pH, and application in cell imaging. The derivative is excited at 402nm in an aqueous solution, and has maximum emission at 526nm. In a phosphate buffer system, the fluorescence intensity at 526nm is gradually enhanced along with the reduction of the pH value from 9.00 to 4.00. The pKa value is 6.69, and the pH linear range is 6.40 to 8.00. Besides, the probe has good selectivity, water solubility and low toxicity, is suitable for detecting the pH change of a water environment, and can be used for detecting the pH change in cells by utilizing a laser confocal microscopy imaging technology.

The preparation method of N-benzylpiperazine is that piperazine and benzyl halide react under catalyst conditions to generate N-benzylpiperazine, piperazine is dissolved in a solvent, and nitrogen-containing amine salt is dropped into as a catalyst, at 0-100 Add dropwise benzyl halide and piperazine at ℃ to react, keep warm for 0.5-24 hours after the reaction, evaporate the solvent under reduced pressure, add lye to strong alkalinity, extract with extractant, and then distill and rectify to obtain the finished product. The invention has the advantages of minimizing the post-treatment procedure after the reaction, simple operation, high purity of the target product, which can reach more than 99%, and the yield can reach more than 95%.

The invention belongs to the field of medicines and particularly relates to the use of 1-erucic acyl-4-(3'-chloro-)benzylpiperazine in medicine of inhibition of vascular endothelial cell oxidative stress, inflammation and adhesion. The concrete structure of the compound is shown in the description. 1-erucic acyl-4-(3'-chloro-)benzylpiperazine has obvious effects on inhibiting oxidant stress generated by vascular endothelial cells and monocyte and adhering action and inflammation generating effect of the vascular endothelial cells, and can be used for preparing medicines for treating vascular diseases.

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 discloses a preparation method of an imatinib impurity. The preparation method comprises: using 1,4-bi(4-carboxybenzyl)piperazine as a raw material, and at presence of N,N- diisopropylcarbodiimide, 1-hydroxy benzotriazole and N,N-diisopropylethylamine, reacting with imaamine to obtain the imatinib impurity 1,4-bi[4-[4-methyl-3-[[4-(pyridine-3-group)pyrimidyl-2group]amino]phenyl]carbamoyl radical]benzyl piperazine. The preparation method provided by the invention is simple, low in requirement on reaction conditions, high in product purity, high in yield, and suitable for industrial production. The synthesized impurity can be used for qualitative and quantitative analysis of the impurity, thus improving drug safety of the imatinib.