38 results about "Pyrrole derivatives" patented technology

The present invention relates to a novel pyrrole derivative compound or a pharmaceutically acceptable salt thereof. In addition, the present invention relates to a pharmaceutical composition for potassium-competitive inhibition of gastric acid secretion and a pharmaceutical composition for preventing or treating diseases caused by gastric acid secretion disorder, the pharmaceutical composition containing the novel pyrrole derivative compound or a pharmaceutically acceptable salt thereof as an active component. The pyrrole derivative compound or the like according to the present invention is a potassium-competitive acid blocker (PCAB) and has an excellent H+ / K+ adenosine triphosphatase (ATPase) (proton pump) inhibition effect, and is thus widely used as a therapeutic agent for diseases caused by gastric acid secretion disorder.

The invention relates to the technical field of medicines, and discloses an atrasentan derivative as well as a preparation method and application thereof. The atrasentan derivative is a tetra-substituted pyrrole derivative designed by taking atrasentan as a pilot, and the synthesis difficulty and cost are remarkably reduced by reducing three chiral centers; the atrasentan derivative has relatively high safety to HK-2 cells, and the pathological state of fibrosis generated by TGF-beta induced HK-2 can be remarkably improved; the application has the potential of being applied to preparation of drugs for preventing and treating renal fibrosis related diseases, the synthesis bottleneck of atrasentan is broken through, and a brand new candidate drug is provided for renal fibrosis treatment.

The invention provides a composite electrolyte, a positive pole piece and an all-solid-state battery, the composite electrolyte comprises a sulfide electrolyte and a functional additive, the functional additive is selected from at least one of a benzofuran derivative, a thiophene derivative and a pyrrole derivative, based on the total mass of the composite electrolyte, the mass fraction of the functional additive is 0.1-5%, and the mass fraction of the sulfide electrolyte is 0.1-5%. When the battery is charged for the first time, the functional additive in the positive electrode is subjected to in-situ reaction under a specific potential, and a compact and stable interface layer with high ionic conductivity is generated on the surface of the positive electrode active material particles, so that the problem of interface side reaction can be solved, and the service life of the battery is prolonged. And the cycle performance and the first-circle discharge capacity of the battery are improved.

A tetraarylmethane compound possessing both indole and pyrrole skeletons and its synthetic method are disclosed. The chemical structural formula of the compound is shown in Formula 3. The synthetic method involves adding 2-indole-methanol and a pyrrole derivative as reactants to an organic solvent. Under the catalysis of Brønsted acid or Lewis acid and in the presence of molecular sieve additives, the reaction is stirred at room temperature. The reaction is monitored by TLC until complete, followed by filtration, concentration, and purification to obtain the final product. The tetraarylmethane compound possessing both indole and pyrrole skeletons synthesized in this invention exhibits high sensitivity and strong cytotoxic activity against HepG2 human liver cancer cells through bioactivity testing. The reaction conditions of this invention are relatively conventional, the reaction process is mild, simple, and low-cost, suitable for large-scale industrial production, thus broadening the applicability of this method. A variety of substrates are used as reactants, resulting in structurally diverse products with high yields.

This invention relates to the field of pharmaceutical technology, and discloses an atrasentan derivative, its preparation method, and its applications. The atrasentan derivative is a tetrasubstituted pyrrole derivative designed using atrasentan as a lead, significantly reducing the difficulty and cost of synthesis by decreasing three chiral centers. This atrasentan derivative exhibits high safety in HK-2 cells and can significantly improve the pathological state of fibrosis induced by TGF-β in HK-2 cells. It has the potential to be used in the preparation of drugs for the prevention and treatment of renal fibrosis-related diseases, breaking through the synthetic bottleneck of atrasentan and providing a novel candidate drug for the treatment of renal fibrosis.

The invention discloses a near-infrared two-region imaging material and a preparation method and application thereof, and belongs to the technical field of photoelectric functional materials. The near-infrared two-region imaging material is an aza-fluorine boron pyrrole derivative NJ1040; the preparation method comprises the following steps: dissolving 2-acetylthiophene in ethanol to obtain a mixed solution, adding a potassium hydroxide aqueous solution, stirring, adding 4-diethylaminobenzaldehyde, stirring, and extracting; drying the extracted organic phase, and performing rotary evaporation concentration and purification to obtain an intermediate I; mixing the intermediate I, diethylamine and nitromethane, reacting, extracting, drying the extracted organic phase, and performing rotary evaporation concentration and purification to obtain an intermediate II; mixing the intermediate II, ammonium acetate and ethanol for reaction, adding triethylamine and a boron trifluoride diethyl etherate complex for continuous reaction after rotary evaporation concentration, and extracting; and drying the extracted organic phase, carrying out rotary evaporation concentration, and purifying to obtain the product. NJ1040 nanoparticles are prepared by a nano coating technology, so that the problem of poor solubility of a contrast agent is solved.

The invention provides a disubstituted tetrahydropyrrole derivative as well as a preparation method and application thereof. Specifically, provided are a compound represented by formula I, a stereoisomer, an ester or a pharmaceutically acceptable salt thereof, and a use thereof in preparation of drugs for preventing or treating epinephrine beta3 receptor related diseases.

The invention discloses a photopolymerization composition of a series of aza-boron-fluorine dipyrrole derivatives, and belongs to the technical field of photocuring materials. In the composition, the aza-boron-fluorine dipyrrole derivative is used as a photosensitizer, has high molar extinction coefficient, excellent light stability and wide spectral response characteristic, and can realize efficient intersystem crossing and long triplet service life. After being compounded with tris (3-chloro-4-methylphenyl) hexyl tetrabutylammonium borate (NB), the acrylate monomer polymerization can be rapidly initiated under 365 nm ultraviolet light, the curing time is within 20 seconds, and the highest double bond conversion rate can reach 75%. Wherein the brominated aza-BODIPY derivative (ADP-Br) can also be efficiently polymerized under the irradiation of 620 nm red light, and the conversion rate of double bonds can be up to 50%. The photopolymerization system disclosed by the invention is high in initiation efficiency, high in curing speed and wide in application scene, and can be applied to the fields of photocureable coatings, adhesives, photoetching materials, 3D printing and the like.

The invention discloses a diketopiperazine tetrahydropyrrole derivative as well as a preparation method and application thereof, and belongs to the technical field of medicines. The technical problem to be solved is to provide the diketopiperazine tetrahydropyrrole derivative with a new structure and the preparation method thereof. The key points of the technical scheme are as follows: the diketopiperazine tetrahydropyrrole derivative is a compound as shown in the following formula I, an isomer, a prodrug, a stable isotope derivative, a pharmaceutically acceptable salt or a mixture of the compounds, the isomer, the prodrug, the stable isotope derivative and the pharmaceutically acceptable salt, wherein L1 and L2 are independently selected from substituted or unsubstituted alkylene; x1 and X2 are respectively and independently selected from N, O or S; and L3 is independently selected from substituted or unsubstituted heterocyclic alkyl. Formula I

The invention provides an application of a sulfonyl pyrrole derivative in preparation of a medicine for treating sepsis. The medicine can effectively block the formation of sepsis thrombosis by inhibiting the activity of FXIIa.

One embodiment of the present invention provides a semiconductor photoresist composition with excellent resolution characteristics and pattern adhesion by reducing the influence of variables during pattern formation and improving CD (critical dimension) stability. [Solution] The present invention relates to a semiconductor photoresist composition comprising an organometallic compound; a pyrrole-based compound including pyrrole, a pyrrole derivative, or a combination thereof; and a solvent, and a pattern formation method utilizing the same.

This invention discloses a method using arylmethyl ketones and 2-aryl- N This invention relates to a method for synthesizing dihydropyrrole derivatives using toluenesulfonylaziridine as a starting material, belonging to the field of organic synthetic chemistry. The method uses tris(dibenzylacetone)dipalladium (Pd2(dba)3) as a catalyst, and 2-iodobenzoic acid (IBX) and potassium persulfate (K2S2O8) as co-oxidants. N,N Using dimethylformamide (DMF) as both solvent and carbon source, the reaction is carried out in an oil bath at 100℃–120℃ for 15–24 h, followed by post-treatment to obtain dihydropyrrole derivatives. This invention utilizes readily available raw materials, is simple to operate, employs mild reaction conditions, exhibits broad functional group compatibility, provides high product selectivity, and is environmentally friendly. Yields can reach 51%–90%, making it suitable for large-scale preparation of structurally diverse dihydropyrrole derivatives. It has significant application value in drug development, natural product synthesis, and materials chemistry.

Disclosed are a semiconductor photoresist composition and a method of forming or providing a pattern using the same, the semiconductor photoresist composition including an organometallic compound, a pyrrole-based compound including pyrrole, a pyrrole derivative, or a combination thereof, and a solvent.

This invention discloses a polypyrrole derivative / black phosphorus carbon-based composite material and its preparation method, relating to the field of new energy battery materials technology. The polypyrrole derivative / black phosphorus carbon-based composite material disclosed in this invention possesses stable P-C bonds, which can stabilize the structure of black phosphorus to form a phosphorus-carbon conductive network structure. Furthermore, the polypyrrole derivative coating on its surface can effectively buffer the volume expansion of black phosphorus, effectively ensuring the cycle stability of the battery. When applied to the negative electrode of lithium-ion batteries, it can enable the battery to possess both high capacity and excellent cycle performance.

The invention discloses a synthesis method of a 2-alkynyl-3-ester pyrrole compound, which comprises the following steps: by taking a pyrrole derivative and (bromoethynyl) triisopropyl silane as raw materials, under the conditions of a silver additive and alkali, catalyzing a pyrrole C2 site direct alkynylation reaction by using a ruthenium catalyst to prepare the 2-alkynyl-3-ester pyrrole compound. The method is based on a precise C-H activation strategy of a ruthenium catalyst, and through reasonable matching of the ruthenium catalyst, a silver salt additive and an alkali system, the activity of a metal center can be effectively regulated and controlled, so that the metal center selectively recognizes a pyrrole C2 site and precise and directional introduction of alkynyl is realized, thereby overcoming challenges such as site competition and catalytic circulation blocking caused by an electronic effect. In a word, the alkynylation system established by the invention is simple and convenient to operate and good in repeatability, provides a reliable technical approach for rapid preparation of the 2-alkynyl-3-ester pyrrole compound, expands a new synthesis thought for construction of drug molecules, functional materials and organic photoelectric structural units, and has important application value and popularization prospect.

The application relates to the technical field of medicines, and discloses application of a tetra-substituted pyrrole derivative in preparation of a product for treating neurodegenerative diseases. The application provides application of the tetra-substituted pyrrole derivative or a pharmaceutically acceptable salt thereof in preparation of the product for treating neurodegenerative diseases. The tetra-substituted pyrrole derivative has high cell safety, and the neuroprotective effect on glutamic acid damage is far higher than that of atrasentan, edaravone and riluzole which are standard clinical drugs; not only can the tetra-substituted pyrrole derivative effectively correct TDP-43 nuclear and cytoplasmic mislocation, but also has the ability of removing insoluble pathological aggregates which atrasentan does not have; the tetra-substituted pyrrole derivative can more effectively inhibit the co-localization of TDP-43 and stress granule protein G3BP1, and intervene in the formation of pathological granules from the source; on a whole animal model, the tetra-substituted pyrrole derivative successfully converts the advantages at the cell level into significant survival benefits, and significantly prolongs the life span of a disease model fruit fly.

The present invention relates to: a novel 4-cyclopropyl pyrrole derivative exhibiting proton pump inhibitory activity and, more specifically, to a 4-cyclopropyl pyrrole derivative exhibiting excellent proton pump inhibitory activity or a pharmaceutically acceptable salt thereof; and a use thereof for preventing or treating gastrointestinal inflammatory diseases or gastric acid-related diseases.

The present disclosure relates generally to thioeno[3, 2-], pyrrole derivatives pharmaceutical compositions comprising said compounds, and methods of making and using said compounds and pharmaceutical compositions. The compounds and compositions provided herein may be used for the treatment or prevention of an autoimmune disease and / or inflammatory condition, including systemic lupus erythematosus and cutaneous lupus erythematosus.

The invention discloses a synthesis method of a 3-ester-5-alkynyl pyrrole compound, which comprises the following steps: by taking a pyrrole derivative and (bromoethynyl) triisopropyl silane as raw materials, under the condition of a silver additive, catalyzing a pyrrole C5 site direct alkynylation reaction by using a palladium catalyst to prepare the 3-ester-5-alkynyl pyrrole compound. According to the method, by optimizing the composition of a catalytic system and reaction conditions, the coordination interaction strength between an ester group guiding group and a palladium catalyst is effectively regulated and controlled, and regioselective inversion from a C2-site reaction to a C5-site reaction, which is more beneficial in thermodynamics and dynamics, is realized; the high regioselectivity alkynylation of the C5 site of the 3-ester pyrrole and the efficient synthesis of the 3-ester group-5-alkynyl pyrrole compound are successfully realized. The method is mild in condition, simple and convenient to operate, high in regioselectivity and good in functional group compatibility, a brand new technical path is provided for preparation of the 3-ester-5-alkynyl pyrrole compound and the derivative thereof, and powerful technical support is provided for development of related fields.

The invention relates to the technical field of medicines, and discloses an application of a tetra-substituted pyrrole derivative in preparation of a product for treating neurodegenerative diseases. According to the tetra-substituted pyrrole derivative or the pharmaceutically acceptable application of the tetra-substituted pyrrole derivative in preparation of products for treating neurodegenerative diseases, the tetra-substituted pyrrole derivative is high in cell safety, and the neuroprotective effect on glutamic acid injury is far better than that of atrasentan and clinical standard drugs edaravone and riluzole; not only can the nucleoplasm dislocation of the TDP-43 be effectively corrected, but also the capability of removing insoluble pathological aggregates, which is not possessed by the atrasentan, is achieved; the co-localization of the TDP-43 and the stress particle protein G3BP1 can be more effectively inhibited, and the formation of pathological particles is intervened from the source; on the whole animal model, the tetra-substituted pyrrole derivative successfully converts the advantage of the cellular level into remarkable survival benefit, and the life of the disease model fruit flies is remarkably prolonged.

The invention discloses a double-lock cascade activated fluorescent probe as well as a preparation method and application thereof. The probe BDP-PLN takes a BODIPY (boron dipyrromethene) derivative as a fluorophore and is integrated with a leucine peptide unit and a p-nitrobenzene glyoxylic acid unit to form a double-lock recognition module. According to the double-lock probe BDP-PLN constructed by the invention, through the ingenious AND logic gating molecular design, the sequential and cascade specific response to two pathological markers, namely peroxynitroso (ONOO-) and leucine aminopeptidase (LAP), is realized. The probe is stable under physiological conditions, and generates obvious fluorescence opening only in a pathological environment in which ONOO <-> triggers and then activates LAP, so that the problems that a single signal probe is insufficient in selectivity and is easy to generate false positive are effectively solved. Due to the high signal-to-noise ratio and cascade activation characteristic, an innovative tool is provided for early and accurate molecular imaging of oxidative stress related diseases such as acute liver injury.

The invention discloses a tetrahydropyrrole derivative for resisting breast cancer as well as a preparation method, application and a medicine of the tetrahydropyrrole derivative. The structural formula of the tetrahydropyrrole derivative is shown as a chemical formula 1. The application refers to application of the tetrahydropyrrole derivative in preparation of anti-breast cancer drugs. The drug is an anti-breast cancer drug comprising the tetrahydropyrrole derivative or a pharmaceutically acceptable salt of the tetrahydropyrrole derivative. Experiments prove that the tetrahydropyrrole derivative has an anti-breast cancer effect and can be used as a candidate active component for preparing the anti-breast cancer medicine.

Provided are a compound as represented by general formula I or a pharmaceutically acceptable salt, stereoisomer or tautomer thereof, a composition containing the compound, a preparation method thereof, an intermediate thereof, and the use thereof in the field of medicine.

The application belongs to the technical field of biological medical materials, and provides a H-aggregated pyrrole derivative, a preparation method and application thereof, the derivative has a molecule with a donor-acceptor (D-A) structure, the donor structure is an aromatic amine derivative, the bridge structure is a dithieno[3,2-b:2,3-d]pyrrole, and the acceptor structure is 2-(3-cyano-4,5,5-trimethylfuran-2(5H)-methylene)malonitrile or 2-[3-cyano-4-methyl-5-phenyl-5-trifluoromethyl-2(5H)-furyl]-malonitrile. Through the synergistic molecular design of "strong donor-large plane bridge-strong acceptor", the application successfully guides the self-assembly of the molecule to form a stable H-aggregate, realizes the "integration" and "synergistic enhancement" of the type I photodynamic and photothermal properties on a single material, and thus can synchronously trigger two kinds of efficient treatment mechanisms under single-wavelength near-infrared light irradiation.

The present invention relates to a lithium secondary battery electrolyte and a lithium secondary battery comprising same, and, more specifically, to a lithium secondary battery comprising a lithium secondary battery electrolyte, which comprises, as an additive, a monomer of a conductive polymer selected from pyrrole derivatives, wherein, during charging, the additive donates electrons to a negative electrode and is oxidized so as to form a conductive polymer coating layer on the surface of a positive electrode, thereby reducing initial irreversible capacity and improving cycle performance and rate capability.

The invention relates to a tetrahydro-beta-carboline pyrrole derivative and a preparation method of the tetrahydro-beta-carboline pyrrole derivative. The invention relates to a preparation method of a tetrahydro-beta-carboline pyrrole derivative, which comprises the following steps: carrying out cyclization reaction on substituted-3-aryl (heteroaryl)-3-chloroacrolein and tetrahydro-beta-carboline under the promotion of triethylamine, and separating and purifying a product after the reaction is completed, so as to obtain the tetrahydro-beta-carboline pyrrole derivative. According to the tetrahydro-beta-carboline-pyrrole derivative and the preparation method thereof disclosed by the invention, TEA (Tetraethyl Alcohol) is used for promoting an intermolecular tandem cyclization reaction between 3-aryl-3-chloroacrolein and tetrahydro-beta-carboline, and the reaction provides a simple, convenient and practical method for synthesizing a tetrahydro-beta-carboline-pyrrole compound; metal catalysis is avoided, and raw materials are economical and easy to obtain.

The present invention relates to compounds of general formula I or pharmaceutically acceptable salts, stereoisomers, tautomers, compositions containing said compounds, processes for their preparation, intermediates, and uses in the pharmaceutical field. JPEG2026500272000136.jpg31105

This invention relates to a novel class of cationic fused-ring conjugated pyrrole derivatives and their applications in the pharmaceutical field, characterized by having the following structures (I) and (II): Specifically, this invention relates to a class of novel cationic fused-ring conjugated pyrrole derivatives with advantages such as structural stability, low aggregation resistance, good amphiphilicity, strong absorption in the near-infrared region, high photodynamic activity, and wide applicability. These compounds can be used as photosensitizing drugs or reagents for the diagnosis and treatment of microbial infections, tumors, macular degeneration, actinic keratosis, port-wine stains, condyloma acuminata, and other diseases. They can also be used as fluorescent dyes and reagents in near-infrared fluorescence imaging, fluorescent labeling, or optoelectronic materials.

The invention discloses a preparation method and application of a column [n] arene electrochemical sensor for specific recognition of cadaverine, the electrochemical sensor comprises an electrode and a surface-modified conductive polymer with a layer of polypyrrole as a main chain and a column [n] arene unit as a side chain, the preparation method comprises the following steps: synthesis of a pyrrole derivatization modified column [n] aromatic hydrocarbon monomer py-P [n] A, electrochemical preparation of the pyrrole column [n] aromatic hydrocarbon polymer Ppy-P [n] A, and preparation of the column [n] aromatic hydrocarbon polymer electrochemical sensor. The method is used for detecting cadaverine in fresh food such as meat and fish and biological samples, and has the characteristics of low cost, convenience in detection, rapidness, time saving and high sensitivity.