13 results about "Diketopiperazines" patented technology

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 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.

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.

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.

The application discloses a compound with neuroprotective activity, a preparation method and application. A new compound of diketopiperazine alkaloids is separated from a fermentation product of Aspergillus, the compound is stable in performance, has no cytotoxicity, and has significant neuroprotective activity. The compound can improve the cell survival rate of a nerve injury in vitro model at a lower concentration, inhibit the generation of active oxygen and malondialdehyde, and obviously increase the expression amount of superoxide dismutase, and has the effects of antioxidation and anti-nerve injury, and has a wide application prospect in the preparation of medicines for preventing and treating neurodegenerative diseases.

The present invention addresses the problem of providing a novel cytotoxic substance, in particular, a novel cytotoxic substance suitable as a payload of a ligand-drug conjugate, and a ligand-drug conjugate containing the cytotoxic substance. The present invention relates to a dispirodiketopiperazine compound represented by formula (VIII), or to a novel ligand-drug conjugate represented by formula (I), which contains the compound as a payload.

A method, composition and kit for the treatment of lung diseases caused by radiation, chemicals, diseases and other conditions 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 invention discloses an acid addition salt of a 2, 5-diketopiperazine compound as well as a preparation method and application thereof, and belongs to the technical field of biological medicines, the structural formula of the acid addition salt is shown as a formula I. The preparation method comprises the following steps: dissolving a compound shown as a formula II in an organic solvent, adding an acid solution, stirring to react, separating out a solid, filtering and washing to obtain the 2, 5-diketopiperazine compound. The invention relates to an acid addition salt of a 2, 5-diketopiperazine compound. According to the present invention, the solubility of the 2, 5-diketopiperazine compound is effectively improved, and the toxicity of the 2, 5-diketopiperazine compound is substantially reduced, such that the important significance is provided for the improvement of the bioavailability of the active component of the 2, 5-diketopiperazine compound in the drug application, and the dosage form selection of the 2, 5-diketopiperazine compound in the drug application can be broadened.

This invention discloses a three-dimensional cobalt metal-organic complex, its preparation method, and its applications, belonging to the field of crystal materials technology. This invention uses 2,5-diketopiperazine-N,N'-diacetic acid and 4,4'-bipyridine as raw materials with cobalt ions to prepare a compound with the chemical formula [Co(DPDA)(4,4'-bpy)]. n A three-dimensional cobalt-organic metal complex. It has a six-connected three-dimensional network structure with dual-core [Co2(COO)2] structural units, and its topological symbol is {3 12 0.4 24 0.5 9 Furthermore, the aforementioned three-dimensional cobalt metal-organic complex can rapidly activate peroxymonosulfate to effectively degrade dyes. It can degrade methylene blue, malachite green, and crystal violet to over 95.0% within 5 minutes, without producing toxic byproducts during the degradation process, and exhibits good reusability. Additionally, the synthesis conditions of the three-dimensional cobalt metal-organic complex are mild, the steps are simple, and it possesses excellent structural stability, good thermal stability, and antiferromagnetism at high temperatures.

The invention discloses an application of marine-derived alkaloid in preparation of an anti-cholestasis medicine, and belongs to the field of natural medicines. The invention discloses an application of indolediketopiperazine alkaloid 12R, 13S-Dihydroxyfumitorgin C (DHFC) or a pharmaceutically acceptable salt of the indolediketopiperazine alkaloid in preparation of an agonist of a peroxisome proliferator-activated receptor delta (PPAR delta), and an application of the indolediketopiperazine alkaloid 12R, 13S-Dihydroxyfumitorgin C (DHFC) or the pharmaceutically acceptable salt of the indolediketopiperazine alkaloid in preparation of an anti-cholestasis medicine, and the indolediketopiperazine alkaloid 12R, 13S-Dihydroxyfumitorgin C (DHFC) or the pharmaceutically acceptable salt of the indolediketopiperazine alkaloid has a protective effect on cholestasis by activating the PPAR delta. DHFC is in high-affinity binding with an LBD region of PPAR delta, the transcriptional level of downstream genes of PPAR delta is increased, the affinity KD of DHFC to PPAR delta protein is 153nM, and the DHFC plays a synergistic treatment role in multiple links of improving bile acid homeostasis, inhibiting inflammation, relieving liver fibrosis and the like. The invention provides a new lead compound for the development of anti-cholestasis drugs, and has important significance for the development of Chinese marine-derived drugs. Formula (I)