39 results about "Benzylpiperazine" patented technology

The invention discloses a novel 4-(2-(pyrrolidine/piperidine-1-yl)benzyl)-piperazine urea type TRPV1 antagonist and a preparation method and application thereof. The invention relates to a compound ina general formula (I) and a pharmaceutically acceptable salt thereof, in the formula, n is equal to 1 or 2, R is H, F, Cl, Br, I, CF3, CH3 or OH, and Ar is phenyl or aromatic heterocyclic group. Thecompounds have a strong analgesic effect, the activity of part of the compounds is far higher than that of a TRPV1 receptor antagonist BCTC, almost no body temperature rise side effect exists, and theinvention further relates to the preparation method of the compounds and pharmaceutical preparations containing the compounds.

The invention belongs to the technical field of pharmacy, particularly discloses a benzylpiperazine urea TRPV1 antagonistic and MOR agonistic double-target drug as well as a preparation method and application thereof, and particularly relates to a compound in a general formula (I) and pharmaceutically acceptable salts thereof, and the drug can be used for preventing and/or treating diseases related to TRPV1 and/or MOR activity, such as pain, inflammation, immune dysfunction, neurological and psychiatric disorders, respiratory diseases, urinary and reproductive disorders. the invention also relates to a preparation method of the compounds and a pharmaceutical preparation containing the compounds.

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 method for preparing saturated potassium azacyclo-trifluoroborates, which comprises the following steps: 1. reacting pyrrolidine and piperidine used as initial raw materials and tert-butyl carbonic anhydride to generate N-tert-butyl carbonyl pyrrolidine and N-tert-butyl carbonyl piperidine, and performing heating reflux on the N-tert-butyl carbonyl piperazine used as an initial raw material and benzyl chloride to generate N-tert-butyl carbonyl-4-benzyl piperazine; and 2. by means of the orientation effect of the N-tert-butyl carbonyl, in a nitrogen protective atmosphere, reacting with sec-butyl lithium at low temperature, then reacting with trimethylborate to generate saturated o-boric acid, adding a saturated KHF2 solution without separating the boric acid, and performing post treatment to respectively generate a potassium N-tert-butyl carbonyl-2-pyrrolidine trifluoroborate, a potassium N-tert-butyl carbonyl-2-piperidine trifluoroborate and a potassium N-tert-butyl carbonyl-4-benzyl-2-piperazine trifluoroborate. These saturated potassium azacyclo-trifluoroborates prepared by the invention are all white solids, are stable at room temperature in an air atmosphere, belong to very important organic chemical reagents and medical intermediate compounds, and have wide application prospects. The method disclosed by the invention is simple to operate, utilizes the cheap and accessible initial raw materials, achieves high yield and favorable purity, is easy to implement scale-up production, and realizes commercialized production.

Provided herein is 4-(4-(4-(((2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-4-yl)oxy)methyl)benzyl)piperazin-1-yl)-3-fluorobenzonitrile, or an enantiomer, a mixture of enantiomers, a tautomer, or a pharmaceutically acceptable salt thereof, and methods for treating, preventing or managing multiple myeloma using such compounds. Also provided are pharmaceutical compositions comprising the compounds, and methods of use of the compositions.

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.

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.

The invention discloses a 6-phenylimidazol[2, 1-b]thiazole-3-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 hydrogen, fluorine, chlorine, bromine, methyl, methoxyl, hydroxyl, mercapto, amino, methylamino, ethylamino, morpholine, piperazine, methyl piperazine, ethyl piperazine, benzyl piperazine, p-methoxylbenzyl piperazine or p-chlorobenzyl piperazine; and n is 0 or 1 or 2. The raw materials for preparation of the derivative are easily available, the reaction is simple, and the synthesis steps are simple and are easy to operate. The compound provided in the invention has good anti-tumor activity, and has important practical value and application prospects in the field of antitumor medicine preparation. (Formula I).

Disclosed are benzylpiperazinyl-indolinylethanone compounds which are useful for the treatment and/or prevention of neuropsychological disorders including, but not limited to, schizophrenia, mania, dementia, depression, anxiety, compulsive behavior, substance abuse, Parkinson-like motor disorders and motion disorders related to the use of neuroleptic agents. Pharmaceutical compositions, including packaged pharmaceutical compositions, are further provided. Compounds of the invention are also useful as probes for the localization of GABA.sub.A receptors in tissue samples.

The invention relates to the field of medicinal chemistry, in particular to a benzylpiperazine compound (I) with anti-inflammatory activity and a preparation method thereof; pharmacodynamic tests prove that the compound provided by the invention has a COX-2, NF-[kappa]B and p38 MAPK multi-target inhibition effect, so that the compound can be used for preventing and treating inflammation-related diseases.

Disclosed is the use of a PAR-1 antagonist, in particular selected from vorapaxar, atopaxar and 3-2-(chloro-phenyl)-1-[4-(4-fluoro-benzyl)-piperazine-1-yl]propenone, for the prevention and/or treatment of a chronic inflammatory disease of the intestine and of the colon in a mammal, in particular Crohn's disease.

The invention discloses an application of a genistein benzyl piperazine derivative in the diabetes field. The molecular formula of the genistein benzyl piperazine derivative is C27H28N2O5; the molecular weight of the genistein benzyl piperazine derivative is 460.52; and the name of the genistein benzyl piperazine derivative is 8-((4-(2,4-dimethoxyphenyl)piperazine-1-yl)methyl)-5,7-dyhydroxyl-3-(4-hydroxyphenyl)-4H-benzopyran-4-one. The genistein benzyl piperazine derivative can remarkably reduce the fasting blood glucose level by activating AMPK and inhibiting the NF-kappa B pathway, so as tobe applicable to the diabetes field.

The invention discloses an application of genistein benzyl piperazine derivative compounded persimmon tannin to the respect of whitening. Research indicates that when genistein benzyl piperazine derivative and persimmon tannin are compounded for use, the whitening effect can be notably improved. The genistein benzyl piperazine derivative can reduce the content of tyrosinase and reduce the generation of melanin; the persimmon tannin has effects in the respects of inflammatory factors, oxidative stress, signal channels and the like, and restrains pigmentation to achieve the whitening effects; and when the genistein benzyl piperazine derivative and the persimmon tannin are compounded for use, the production cost can be notably reduced, and multi-way whitening effects and synergistic effects can be exerted. The persimmon tannin is produced from persimmon processing by-products or waste, so that the cost is low, the shortcomings that the genistein benzyl piperazine derivative is complex toprepare and not suitable for industrialized production can be overcome, and when the whitening effects are guaranteed, the cost of products is notably reduced.