60 results about "Diketopiperazines" patented technology

Provided are treprostinil derivatives with a reduced ability to form undesired impurities in a pharmaceutical formulation, such as a dry powder formulation, further containing a carboxyl group containing inactive ingredient, such as fumaryl diketopiperazine.

The invention discloses a 2, 5-diketopiperazine compound with an anti-tumor effect and application of the 2, 5-diketopiperazine compound in preparation of a medicine for treating and / or preventing neutropenia, and the 2, 5-diketopiperazine compound is novel in structure, has good activity and water solubility, and can be used for preparing medicines for treating and / or preventing neutropenia. The defects of poor water solubility of the ponabulin, unfavorable patent medicine and difficult clinical administration can be overcome. The 2, 5-diketopiperazine compound as shown in the formula (I) or the pharmaceutically acceptable salt thereof can be used for treating and / or preventing neutropenia and improving toxic and side effects of clinical tumor treatment, and has an anti-tumor effect at the same time. The invention also discloses application of drug combination of the compound and a granulocyte colony stimulating factor (G-CSF) biological agent in drugs for treating and / or preventing neutropenia. # imgabs0 #

The present invention concerns the recovery of methionylmethionine from aqueous alkali ions containing media by intermediate formation of Bis(methionyl)-diketopiperazine.

The invention discloses a diketopiperazine heterodimer as well as a biosynthesis method and application thereof, and belongs to the technical field of bioengineering. The biosynthesis method of the diketopiperazine heterodimer comprises the following steps: S1, culturing a recombinant cell containing P450 dimerization enzyme or a mutant thereof, and performing induced expression to obtain a whole-cell culture; and S2, adding a cyclic dipeptide substrate containing tryptophan into the whole-cell culture, carrying out a catalytic reaction, and separating and purifying the obtained product to obtain the diketopiperazine heterodimer. According to the invention, the P450 dimerization enzyme or the mutant thereof is used for catalyzing the biosynthesis of the tryptophan-containing diketopiperazine into the diketopiperazine heterodimer with different regioselectivity / stereoselectivity, the biosynthesis method is green and environment-friendly, the efficiency is high, and the variety of the diketopiperazine heterodimer is greatly expanded.

The invention discloses a three-dimensional cobalt metal organic complex and a preparation method and application thereof, and belongs to the technical field of crystal materials. The three-dimensional cobalt metal organic complex with the chemical formula of [Co (DPDA) (4, 4 '-bpy)] n is prepared by selecting 2, 5-diketopiperazine-N, N'-diacetic acid, 4, 4 '-bipyridine and cobalt ions as raw materials. The three-dimensional network structure has a six-connection three-dimensional network structure of a dual-core [Co2 (COO) 2] structural unit, and the topological symbol is {312.424. 59}. Besides, the three-dimensional cobalt metal organic complex can quickly activate peroxymonosulfate to effectively degrade dyes, can degrade three dyes, namely methylene blue, malachite green and crystal violet, to 95.0% or above within 5 minutes, does not generate toxic byproducts in the degradation process, and has a relatively good reuse rate. In addition, the three-dimensional cobalt metal organic complex is mild in synthesis condition and simple in step, has excellent structural stability and good thermal stability, and has antiferromagnetism at high temperature.

A novel pesticide formulation comprising an adjuvant selected from diketopiperazines and a pesticide active substance. A concentrate suitable for forming the formulation is also provided. The diketopiperazine provides the adjuvant activity in the concentrate and the pesticide formulation. A method for making the formulation is also provided, as well as the use of the diketopiperazine as an adjuvant in a pesticide formulation. A method for forming the diketopiperazine is also described. The diketopiperazine can be used in formulations or seed coatings for treating plants to control pests.

The application discloses a steroid-indole alkaloid hybrid dimer compound, a preparation method thereof and application of the compound in preparation of an antitumor chemotherapy drug sensitizer, and first prepares the steroid-indole diketopiperazine alkaloid hybrid compound from a fungus Aspergillus sp. EGF15-0-3 rice culture medium. The compound is a new skeleton compound first discovered in nature. It is first discovered that the hybrid compound has Tdp1 inhibitory activity and can be applied as a tyrosine-DNA phosphodiesterase 1 (Tdp1) inhibitor. It is first discovered that the hybrid compound has chemotherapy sensitization activity on a tumor chemotherapy drug topotecan TPT, which provides a drug source molecule and data support for development of a new natural antitumor combination inhibitor, and has important significance for development and utilization of marine Aspergillus sp. fungus resources.

The invention discloses a preparation method and application of a 2, 5-diketopiperazine derivative, and belongs to the field of biological medicine. The preparation method comprises the following steps: by taking 1, 4-diacetyl piperazine-2, 5-diketone (II) as an initial raw material, firstly, carrying out condensation reaction on the initial raw material and isobutyraldehyde to prepare a key intermediate (III); meanwhile, 4-amino-1-butanol (IV) is converted into an intermediate (VI) through acylation and oxidation two-step reaction; and finally, carrying out condensation and elimination reaction on the intermediates (III) and VI to prepare the target compound (I). The preparation method provided by the invention has the advantages of reasonable route design, mild conditions and outstanding stereoselectivity. According to the method, on the basis of easily available raw materials, a product mainly comprising a Z configuration is efficiently constructed through a modular strategy and consistent mild base catalysis conditions. Experimental data show that the compound prepared by the invention can inhibit TG accumulation in nematode bodies and reduce nematode fat accumulation, and can be developed into efficient medicines for preventing and treating obesity.

The invention discloses an indole diketopiperazine alkaloid compound as well as a preparation method and application of the indole diketopiperazine alkaloid compound. Aspergillus sp. SYPHU504 is preserved in Guangdong Microbial Culture Collection Center on August 26, 2024, and the preservation number is GDMCC No: 65055. According to the invention, the indole diketopiperazine alkaloid compound and the pharmaceutically acceptable salt, isomer or solvate of the indole diketopiperazine alkaloid compound are separated and prepared from a fermentation culture of Aspergillus sp. SYPHU504. It is found through tests that the indole diketopiperazine alkaloid compound can remarkably inhibit proliferation of leukemia cell strains K562 and RS4: 11, and dose dependence is shown. Therefore, the compound is expected to be developed into a safe and effective novel anti-leukemia drug, and has important significance on development of Chinese marine drug resources.

The invention discloses a biphenyl-diketopiperazine indole alkaloid hybrid compound, which is separated from a fermentation product of a strain Aspergillus candidus HNNU0546, and has a skeleton molecule formed by hybridizing rare diketopiperazine indole alkaloid with biphenyl molecules through an isopentenylation branch chain, and the biphenyl compound can obviously inhibit the activity of crop disease fungi.

The invention relates in particular to a process for the preparation of DL / LD-methionine diketopiperazine (I) characterized in that a DD / LL-methionylmethionine-containing aqueous solution or suspension, which has a pH of 3 to 7, measured using a pH electrode at 20° C., is reacted at a temperature of 150 to 220° C., preferably at 170 to 210° C., until an aqueous solution or suspension has formed containing at least a proportion of 30 mol %, preferably 50 mol %, especially 60 mol % of DL / LD-methionine diketopiperazine, based on the total content of DL / LD- and DD / LL-methionine diketopiperazine in the reaction mixture. This process forms part of an overall process for the preparation of DL / LD-methionylmethionine, which is obtained by hydrolysis from the DL / LD-methionine diketopiperazine (I) produced initially.

A method, composition and kit for the treatment of interstitial lung disease are disclosed. The method utilizes a combination product for inhalation comprising a therapeutic amount of a dry powder formulation provided in an inhaler to be administered to a subject in need by oral inhalation. The composition comprise diketopiperazine particles for pulmonary inhalation.

An agrochemical formulation comprising adjuvants selected from diketopiperazines and an agrochemical active. A concentrate is also provided suitable for forming the formulation. The diketopiperazines provide adjuvancy in the concentrate and agrochemical formulations. There is also provided a method of making the formulation, and use of said diketopiperazines as adjuvants in agrochemical formulations is also provided. A method of forming the diketopiperazines is also described. The diketopiperazines may be used in a formulation for treating vegetation to control pests, or in a seed coating.

A method for the synthesis of N-protected 3,6-aminoalkyl-2,5-diketopiperazines is provided. The method includes obtaining a cyclic α-N protected active amino ester and adding it to a mixture of an amine catalyst in an organic solvent.

The invention provides a glycine separation and purification method, which can be widely applied to the technical field of preparation of diketopiperazine by glycine condensation, and solves the problem of low raw material utilization rate caused by incomplete reaction of glycine raw materials, enrichment in mother liquor and difficulty in purification in the existing process of preparing diketopiperazine from glycine. The glycine separation and purification method comprises the following steps: firstly, carrying out heating concentration pretreatment on a mother solution of diketopiperazine to remove moisture in the mother solution, then adding an inorganic copper compound, heating and stirring, concentrating and cooling, and filtering to obtain a copper diglycinate complex; and dissolving the copper diglycinate complex in the solution, adding acid, controlling the pH value, and filtering to obtain glycine. The whole process is easy to operate, the glycine recovery rate is high, the purity can reach 99.5% to the maximum, the yield can reach 98.1% to the maximum, the amplification effect is not obvious during amplification, and the method has good industrial application value.

The invention belongs to the technical field of medicinal chemistry, and discloses a 2, 5-diketopiperazine compound, a synthesis method, a composition and application. The synthesis method comprises the following steps: synthesizing or providing 2, 3, 4, 5 or 6-substituted benzaldehyde A; synthesizing or providing an intermediate 2, 5-diketopiperazine derivative B; 2, 3, 4, 5 or 6-substituted benzaldehyde A and an intermediate 2, 5-diketopiperazine derivative B are subjected to Aldol condensation to obtain the compound with the structure as shown in the formula (I). The compound is novel in structure, part of the compound has excellent anti-tumor activity and optical stability, and the compound has good development prospects.

This invention discloses a bacterial strain that degrades aspartame, a bacterial-algal symbiotic system, and its application. The strain is *Sphingosphomonas zeatus* (…). Sphingomonas zeae The specimen, NCU J1, with accession number CCTCC NO:M 20251462, was prepared using *Sphingomonas zeylans* and *Chlorella vulgaris*. Chlorella A directional symbiotic combination of *Sphingosine monocytogenes* sp. constructs a bacterial-algal symbiotic system. *Sphingosine monocytogenes* can metabolize aspartame and its degradation products, and can achieve metabolic complementarity through the bacterial-algal symbiotic interface. The bacteria preferentially promote the photohydrolysis of aspartame to generate degradation products such as diketopiperazine derivatives, while the microalgae simultaneously initiate isomerization enzymatic reactions to convert the degradation products into low-toxicity products. Compared with traditional physicochemical methods, this reduces the risk of secondary pollution by more than 40%, achieving efficient degradation of aspartame and significantly reducing the formation of its derivatives. It can be used to treat wastewater containing aspartame.

Provided in the present invention are 2,5-diketopiperazine compounds and the use thereof. The 2,5-diketopiperazine compounds are a novel series of substituted heterocyclic skeleton compounds. Specifically disclosed is a structural formula shown as formula (I). The 2,5-diketopiperazine compounds have novel structures, good water solubility and antitumor activity, and therefore can be used for preparing pharmaceutical compositions for treating tumors and also can be used as tubulin inhibitors for inhibiting tubulins, achieving wide application scenarios.

The application discloses 2,5-diketopiperazine-imidazole compounds, a preparation method and application thereof. Specifically disclosed are compounds as shown in formula (I), a tautomer thereof, a stereoisomer thereof, a pharmaceutically acceptable salt thereof, or a solvate of any one of the foregoing. The compound of the application is novel in structure and has good activity.

Synthesis of a peptide has a problem that a desired elongation reaction is prevented from proceeding by diketopiperazine and a 6-membered diamine skeleton compound formed when a protective group at the N-terminal is removed. The present inventors have found that when in production of a peptide, a peptide in which an amino group at the N-terminal is protected with a protective group having an Fmoc skeleton is treated in a specific solvent with a base having a pKa of 23 or more in acetonitrile as a conjugate acid, and a peptide chain is then elongated, it is possible to solve the problem described above.

Disclosed embodiments relate to improved methods for the synthesis of activated fumarate intermediates and their use in chemical synthesis. Disclosed embodiments describe the synthesis of activated fumarate esters including those derived from activating groups including: 4-nitrophenyl, diphenylphophoryl azide, pivaloyl chloride, chlorosulfonyl isocyanate, p-nitrophenol, MEF, trifluoroacetyl and chlorine, for example, ethyl fumaroyl chloride and the subsequent use of the activated ester in situ. Further embodiments describe the improved synthesis of substituted aminoalkyl-diketopiperazines from unisolated and unpurified intermediates allowing for improved yields and reactor throughput.

The present invention provides a method for preparing 2,5-diketopiperazine from diglycine, wherein diglycine is stirred in a solvent for reaction, and after the reaction is completed, a large amount of solids are precipitated by cooling, suction filtration, washing and drying to obtain a product. The solvent includes any one of ethylene glycol, glycerol, N-methylpyrrolidone, octanol, and octyl acetate, or a mixture of any two of them. The present invention uses diglycine as a raw material to prepare 2,5-diketopiperazine, which has the characteristics of high reaction selectivity, simple operation, less wastewater, and low processing difficulty compared with the prior art.

The invention discloses a steroid-indole alkaloid hybrid dimer compound, a preparation method of the steroid-indole alkaloid hybrid dimer compound and application of the steroid-indole alkaloid hybrid dimer compound in preparation of an anti-tumor chemotherapeutic drug sensitizer. The steroid indole diketopiperazine alkaloid hybrid compound is prepared from a fungus Aspergillus sp.EGF15-0-3 rice culture medium for the first time; the compound is a novel skeleton compound found for the first time in nature. It is found for the first time that the heterocomplex has Tdp1 inhibitory activity and can be applied as a tyrosine-DNA phosphodiesterase 1 (Tdp1) inhibitor. The chemosensitization activity of the heterocomplex on the tumor chemotherapeutic drug topotecan TPT is found for the first time, drug source molecules and data support are provided for developing a novel natural anti-tumor combined inhibitor, and the heterocomplex has important significance on development and utilization of marine aspergillus fungus resources.

This invention discloses a class of indole-diketopiramate derivatives, their preparation methods, and their applications in the preparation of cardioprotective drugs. The structural formula of the indole-diketopiramate derivative is shown in formula (I) or (II), wherein: in formula (I), R1, R2, and R3 are selected from H, ... ...

Methods for producing substituted diketopiperazines, including fumaryl substituted amino alkyl diketopiperazines, with improved purity and desirable isomer content are described herein. The methods provide substituted diketopiperazines that are useful as pharmaceutical drug delivery systems for delivery to the lungs of individuals. The resulting substituted diketopiperazines show reduced or undetectable amounts of certain impurities that are known to affect product purity and performance.

The invention belongs to the technical field of pharmaceutical chemistry, and discloses a diketopiperazine compound, a synthesis method, a pharmaceutical composition and application. The synthesis method comprises the following steps: synthesizing or providing imidazole formaldehyde C; synthesizing or providing an intermediate 2, 5-diketopiperazine derivative B; synthesizing or providing 3-substituted benzaldehyde A; 3-substituted benzaldehyde A and an intermediate 2, 5-diketopiperazine derivative B are subjected to Aldol condensation to obtain the diketopiperazine compound with the structure as shown in the formula (I). The invention also discloses application of the compound in preparation of medicines for preventing or treating cancers, especially application in preparation of medicines for treating lung cancers. The compound disclosed by the invention is novel in structure, part of the compound has excellent anti-tumor activity, all the compounds have excellent solubility, and the compound has a good development prospect.

Disclosed herein are diketopiperazine microparticles having high capacity for adsorbing a drug or active agent. In particular, the diketopiperazine microparticle are formed using fumaryl diketopiperazine and can comprise a drug in large doses for the treatment of disease or disorders by pulmonary delivery via oral inhalation.

A method, composition and kit for the treatment of fibrotic lung disease are disclosed. The method utilizes a combination product for inhalation comprising a therapeutic amount of a dry powder formulation provided in an inhaler to be administered to a subject in need by oral inhalation. The composition comprises diketopiperazine particles and a kinase inhibitor for oral inhalation.

The disclosed embodiments detail improved methods for the synthesis of diketopiperazines from amino acids. In particular improved methods for the cyclocondensation and purification of N-protected 3,6-(aminoalkyl)-2,5-diketopiperazines from N-protected amino acids. Disclosed embodiments describe methods for the synthesis of 3,6-bis-[N-protected aminoalkyl]-2,5-diketopiperazine comprising heating a mixture of an amino acid in the presence of a catalyst in an organic solvent. The catalyst is selected from the group comprising sulfuric acid, phosphoric acid, p-toluenesulfonic acid, 1-propylphosphonic acid cyclic anhydride, tributyl phosphate, phenyl phosphonic acid and phosphorous pentoxide among others. The solvent is selected from the group comprising: dimethylacetamide, N-methyl-2-pyrrolidone, diglyme, ethyl glyme, proglyme, ethyldiglyme, m-cresol, p-cresol, o-cresol, xylenes, ethylene glycol and phenol among others.