107 results about "Piperazinedione" patented technology

Provided herein are compounds of Formula (I), and salts thereof, wherein each instance of RL is independently optionally substituted C6-C40 alkenyl. Further provided are compositions comprising a compound of Formula (I) and an agent. Further provided are methods and kits using the compositions for delivering an agent to a subject or cell and for treating and / or preventing a range of diseases. Further provided are methods of preparing compounds of Formula (I) and precursors thereof.

The present invention relates to crystalline forms of (3R,6R)-3-(2,3-dihydro-1H-inden-2-yl)-1-[(1R)-1-(2,6-dimethyl-3-pyridinyl)-2-(4-morpholinyl)-2-oxoethyl]-6-[(1S)-1-methylpropyl]-2,5-piperazinedione benzenesulfonate salt and pharmaceutical compositions thereof. Also disclosed are processes for the preparation the above compounds and methods for use thereof.

The invention provides polymorphism of a deuterium-substituted plinabulin compound and a preparation method and application of the polymorphism, specifically polymorphism of (3Z,6Z)-3-benzylidene-6-((5-tert-butyl-1H-imidazole-4-yl) deuterium-substituted methylene)piperazidine-2,5-diketone and preparation method and application of the polymorphism. Based on (3Z,6Z)-3-benzylidene-6-((5-tert-butyl-1H-imidazole-4-yl) deuterium-substituted methylene)piperazidine-2,5-diketone, the polymorphism of (3Z,6Z)-3-benzylidene-6-((5-tert-butyl-1H-imidazole-4-yl) deuterium-substituted methylene)piperazidine-2,5-diketone is researched, and alpha, beta, gamma, delta, and epsilon crystal forms are found. The polymorphism and preparation method and application are of great significance on research of pharmaceutical polymorphism and screening of a crystal form with excellent pharmaceutical effect, and alpha, beta, gamma, delta, and epsilon crystal forms are fully developed and applied with respect to curative effect and dosage form selection of antitumor drugs.

The invention discloses a method for preparing a piperazine diketone type compound and specifically relates to a method for preparing a compound shown as a formula (I) by cyclization after substitution. The method takes (S)-1,2-diaminopropane tartrate, haloacetic acid and low-carbon alcohol as raw materials to prepare the compound shown as the formula (I). Compared with the prior art, a pluralityof disadvantages are improved and overcome by the preparation method; the preparation method has the advantages of simple steps, low cost, convenience for post-treatment, cleanness, high yield and purity, low toxicity and less pollution, and industrial production is facilitated.

The invention discloses modified oligochitosan for aquaculture and a preparation method thereof. The preparation method includes: adopting piperazinedione acid to graft C2-NH2 on oligochitosan high in antibacterial performance; grafting quaternary ammonium salt with C6-OH on oligochitosan modified by piperazinedione acid to prepare and synthesize the modified oligochitosan. The preparation method is simple to operate and safe in operation environment, and both antibacterial performance and dissolubility of an oligochitosan derivative obtained are improved obviously.

A polycrystalline form of a dehydrophenylahistin-like compound, and a manufacturing and purification method and application thereof A (3Z,6Z)-3-benzylidene-6-[(5-tert-butyl-1H-imidazol-4-yl)deuteromethylene]piperazine-2,5-dione monohydrate crystal and a (3Z,6Z)-3-benzylidene-6-[(5-tert-butyl-1H-imidazol-4-yl)methylene]piperazine-2,5-dione monohydrate crystal are more competitive crystalline forms with stable quality. The manufacturing and purification method is simple and easy to operate, and can effectively control the generation of a trans-isomer contaminant to obtain a high purity product. The polycrystalline form of the dehydrophenylahistin-like compound has a certain value in an application for manufacturing an antitumor pharmaceutical product.

The present invention discloses 9-(CH of the following formula 2 CO-Arg-Gly-Asp-AA)-tetrahydro-β-carboline[3:4]piperazine-2,5-diketopiperidine[4:5]imidazole (where AA is a Ser residue base, Phe residue and Val residue). Their preparation method is disclosed, and their application in the preparation of antitumor drugs is disclosed.

The present invention provides an A crystal form of (3Z,6Z)-3-[((E)-3-(5-tert-butyl)-1H-imidazol-4-yl)methylene]-6-((E)-3-(3-fluorophenyl)-2-propenylidene)piperazine-2,5-dione (VDA-1). The A crystal form has a stable morphology, a definite melting point, and good chemical stability and is high-temperature resistant and suitable for pharmaceutical uses. The A crystal form can be used to treat a hyperproliferative disease.

The invention discloses (2'S,5'S)-tetrahydropyrazine[1',2':1,6]bis[1S,1R-(1-ethyl-Pro-Ala-Lys)-2, 3,4,9-tetrahydro-1H-pyridin[3,4-b]indole]-1',4'-dione discloses its preparation method, discloses its thrombolytic activity, discloses Its antithrombotic activity also discloses that it remains effective for 24 hours after the onset of ischemic stroke. Therefore, the present invention discloses its application in the preparation of thrombolytic drugs, its application in the preparation of antithrombotic drugs, its application in the preparation of drugs that are still effective for ischemic stroke for 24 hours, and its application in the preparation of antithrombotic drugs. Its application in the preparation of a drug with triple effects of thrombolysis, antithrombosis and ischemic stroke still effective for 24 hours.

The present invention discloses (3R,6S)-3-(Lys-amino n-hexanoylamino n-butyl)-6-(indole-3-methyl)-piperazine-2,5-dione of the following formula. Its preparation method, its anti-tumor metastasis activity and its anti-inflammation activity are disclosed, so the present invention discloses its application in the preparation of anti-tumor metastasis medicine and anti-inflammation medicine.

The invention discloses a method for simultaneously detecting genotoxic impurities including methyl trifluoromethanesulfonate and ethyl trifluoromethanesulfonate in tubulin inhibitor bulk drugs, and the bulk drugs are (3Z, 6Z)-3-[(E)-3-(5-tert-butyl)-1H-imidazolyl-4-yl) methylene]-6-((E)-3-(3-fluorophenyl)-2-propylene subunit)piperazine-2, 5-diketone. The method comprises the following steps: (1) taking a test sample of the raw material medicine, adding isopropanol, uniformly shaking, carrying out ultrasonic treatment, filtering, taking the subsequent filtrate, and introducing a sample to determine trifluoromethanesulfonic acid methyl ester and trifluoromethanesulfonic acid ethyl ester; wherein methyl trifluoromethanesulfonate reacts in isopropanol to generate methyl isopropyl ether, and ethyl trifluoromethanesulfonate reacts in isopropanol to generate ethyl isopropyl ether; and (2) detection conditions: taking polyethylene glycol modified by nitro terephthalic acid as a capillary column of a stationary phase, and determining by adopting a gas chromatograph-mass spectrometer. According to the method, the methyl trifluoromethanesulfonate and the ethyl trifluoromethanesulfonate in the tubulin inhibitor bulk drug can be qualitatively and quantitatively detected simply, quickly and efficiently at the same time.

The present invention relates to a 3,4-methylenedioxyphenyl substituted tetrahydro-beta-carboline piperazine dione derivative and uses thereof, and specifically discloses a compound represented by a formula I, or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, wherein each group is defined in the specification. According to the present invention, the compound has dual inhibitory activity on acetylcholinesterase and phosphodiesterase 5, and has good blood-brain barrier permeability, such that the compound can be used for preparing drugs for treatment and / or prevention ofAlzheimer's diseases. The formula I is defined in the specification.