414 results about "Pyrrole derivatives" patented technology

Compounds, compositions and methods for modulating the activity of receptors are provided. In particular compounds and compositions are provided for modulating the activity of receptors and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder directly or indirectly related to the activity of the receptors.

A process for preparing 1-hexene under existance of ethylene oligonerizing catalyst includes such steps as premixing part of ethylene gas with solvent, mixing with the components in catalyst system, including chromic compound, pyrrol derivative, alkylaluminium and improver, loading in reactor via gas distributor, directly loading the rest of ethylene gas in reactor, discharging the resultant liquid, adding catalysis stopping agent, and separating. Its advantages are high selectivity of 1-hexene and high catalytic activity.

The invention belongs to strong-fluorescence boron dipyrromethene dyes containing a carbazole structure in the technical field of organic chemical industry and fine chemical industry. Because a method for preparing the strong-fluorescence boron dipyrromethene dye containing the carbazole structure and derivatives thereof adopts boron dipyrromethene and carbazole aldehyde with substituent as raw materials, the molar ratio of the boron dipyrromethene to the carbazole aldehyde is 1:2-5, piperidine is a catalyst, a 4-angstrom molecular sieve is a dehydrating agent, and the molar ratio of the borondipyrromethene to the catalyst is 1:0.01-0.20; in an organic solvent, at the temperature of between 100 and 150 DEG C and under the protection of argon or nitrogen, the mixture reacts for 8 to 50 hours by stirring, the carbazole aldehyde and the active methylene of the boron dipyrromethene are dehydrated to generate the boron dipyrromethene derivatives; and after the carbazole structure with different substituents is introduced into the boron dipyrromethene, the optical property of the boron dipyrromethene compound is changed, the red shift of the absorption spectrum thereof is 80 nanometers, the red shift of the emission spectrum is 90 nanometers, higher fluorescence quantum yield is kept at 0.67, the laser efficiency reaches more than 30 percent, and the strong-fluorescence boron dipyrromethene derivatives containing the carbazole structure are obtained.

A photosensitive tetrapyrrole derivative having formula (I)where n stands for 1 or 2 or a pharmaceutically acceptable salt thereof is useful as an effective ingredient in an obstruent composition for photochemotherapeutically obstructing neovascular vessels. The photosensitive tetrapyrroles of the formula (I) may be administered in a photochemotherapeutic method for obstructing neovascular vessels, particularly choroidal and retinal neovascularizations.

The invention relates to near infrared fluoro-boron dipyrrole fluorescent dyes and a synthesis method of the fluorescent dyes. The dyes have the general formula shown in the specification. The fluorescent dyes are synthesized from aldehyde or imine compounds of halogenated pyrrole or isoindazole and pyrrole derivatives by a one-pot method. The emission wavelength of the fluorescent dyes is more than 600nm, and the emission spectra of the monostyryl-substituted dyes and derivatives thereof can be up to 714nm. The fluorescent dyes have excellent light, physical and chemical performances of higher fluorescent quantum yield (0.61-0.91) and better light stability and the like, and has excellent application prospects in fluorescence labeling, biological imaging and other bioanalysis fields.

A non-aqueous pigment dispersion comprising a diketopyrrolo-pyrrole pigment, a polymeric dispersant and a dispersion synergist in a non-aqueous dispersion medium characterized in that said dispersion synergist is a diketopyrrolo-pyrrole derivative according to Formula (I):whereinR1, R2 and R3 are independently selected from the group consisting of hydrogen, a halogen atom, a methyl group, an ethyl group, an tert.-butyl group, a phenyl group, a cyano group and an acid group;R4, R5 and R6 are independently selected from the group consisting of hydrogen, a halogen atom, a methyl group, an ethyl group, an tert.-butyl group, a phenyl group and a cyano group; andcharacterized in that one of R7 and R8 is a group comprising two acid functions while the other one of R7 and R8 represents hydrogen.

The invention discloses conducting polymeric hydrogel, sponge, a preparation method and an application thereof. Eigenstate conducting high-molecular polymer is used as a three-dimensional framework of the hydrogel, and the hydrogel is an organic conducting material having good mechanical strength and compression elasticity. The hydrogel can be obtained through step-by-step oxidative coupling polymerization on pyrroles and pyrrole derivatives by using an oxidizing agent and long-term secondary growth. Content of the conducting high-molecular polymer in the hydrogel is 1.5-21.5 wt%; maximum compression ratio can reach 90%; the hydrogel recovers to normal within 10 s to 5 min after compression; conductivity is 0.001-10 S / m; and the hydrogel has shape memory characteristics, and compression deformation recovery quantity is directly related to solvent volume. The sponge is obtained by drying the hydrogel. Mechanical strength, elasticity and conductivity of gel can be greatly maintained. With increasing of compression ratio, resistance value of the sponge is gradually reduced by 0-10%. The hydrogel and sponge of the invention can be widely applied in fields of dye adsorption, stress sensing, electrical switch and the like.

A conductive elastomeric foam composite is presented, comprising an elastomer foam and polypyrrole, thiophene, or aniline and derivatives thereof. The foam is manufactured by first diffusing an oxidant into the dense polymer phase of a solvent-swollen foam and then diffusing pyrrole or pyrrole derivative vapor or solution into the dried foam, resulting in an in situ chemical oxidative polymerization of pyrrole at the oxidant site. Only about 5 wt % of conductive polymer is required for observing an insulator to conductor transition. The conductivity of the composite foam can be effectively controlled between 10-7 and 10-1 S / cm by varying either the amount of oxidant used and / or the copolymer composition.

The invention discloses glycosylated boron dipyrromethene fluorophore derivatives as well as a preparation method and application of the glycosylated boron dipyrromethene fluorophore derivatives. The method comprises the following steps: by taking glucose and glucosides thereof as action targets, connecting covalent bonds of the action targets to boron dipyrromethene fluorophore derivatives for photodynamics therapy, so that a third generation photosensitizer against cancer which can be used for targeted therapy is obtained. The dipyrromethene fluorophore derivatives containing glucose and glucosides are taken as study researches, activity study of in-vitro breast cancer-resistant cells MBA-MD-231 is expanded, a prodrug suitable for molecular targeted therapy is screened, and a foundation is laid for applying the glycosylated boron dipyrromethene fluorophore derivatives to targeted therapy of cancers. Moreover, the compound synthesis method is simple, readily available in raw materials, low in cost, few in side reactions, high in yield and simple in purification, and industrial production is promoted.

The invention provides a preparation method of a long wavelength BODIPY dye and a derivative thereof, belonging to the organic chemical industry and the fine chemical industry technology field. Bromine or iodo-BODIPY and substituted alenyle boric acid are used as the raw material with the mol ratio around 1 to between 2 and 10 in the preparation method of the long wavelength BODIPY dye and the derivative thereof, palladium carbon or zero-valent palladium is used as a catalyst, the mol ratio of bromine or iodo-BODIPY to the catalyst is 1 to between 0.01 and 0.20. Allowing the bromine or iodo-BODIPY and the substituted alenyle boric as well as the catalyst to react in an organic solvent for one to seventy-two hours at a temperature of between forty and one hundred and sixty DEG C with the protection and stirring of argon or nitrogen, then the bromine or iodine on the raw material is substituted, conjugated double bond BODIPY derivative is generated and the boric acid and conjugated double bond BODIPY derivative is substituted, and after the introduction of conjugated double bond groups in different numbers, the optical property of the BODIPY is changed to absorb and emit spectrum and Einstein shift occurs.

The present invention relates to a class of new tetrahydrocyclopenta[c]pyrrole derivatives represented by a general formula (I) and a preparation method thereof, a pharmaceutical composition containing the derivative, and uses of the tetrahydrocyclopenta[c]pyrrole derivative as the treatment agent, particularly the gastric acid secretion inhibitor and the potassium ion competitive acid blocker (P-CABs). Each substituent in the general formula (I) is defined in the specification. The general formula (I) is defined in the specification.

The invention discloses erlotinib modified 4-difluoro-4-borata-3a-azonia-4a-aza-s-indacene derivatives, and a preparation method and application thereof. According to the invention, erlotinib which is a listed small-molecule inhibitor is used as a tumor target and is covalently connected to a 4-difluoro-4-borata-3a-azonia-4a-aza-s-indacene photosensitizer capable of being used for photodynamic therapy by the click reaction so as to obtain third-generation anti-tumor photosensitizers capable of being used for targeted therapy, namely, a double-erlotinib modified 4-difluoro-4-borata-3a-azonia-4a-aza-s-indacene derivative and a single-erlotinib modified 4-difluoro-4-borata-3a-azonia-4a-aza-s-indacene derivative. Meanwhile, by using the erlotinib modified 4-difluoro-4-borata-3a-azonia-4a-aza-s-indacene derivatives as research objects and respectively using human body hepatoma carcinoma cells HepG2 and HELF (Human Embryonic Lung Fibroblast) as tested cell strains, research on in vitro anti-tumor activity of the erlotinib modified 4-difluoro-4-borata-3a-azonia-4a-aza-s-indacene derivatives is developed, a prodrug suitable for molecular targeted therapy is screened out and the foundation is laid for application of the erlotinib modified 4-difluoro-4-borata-3a-azonia-4a-aza-s-indacene derivatives to targeted therapy of cancers. A synthetic method of the derivatives is simple; raw materials of the derivatives are easy to obtain and low in cost, have few side effects and high yield, are easy to purify and are beneficial to industrial production.

The invention provides a 1,2,5-triphenyl substituted pyrrole derivative with a gathering induced luminescence performance as well as a preparation method and an application thereof. Particularly, the invention provides a triphenyl pyrrole derivative with the gathering induced luminescence performance, which is represented by a general formula (I), wherein in the general formula (I), R1 represents H, an ester group or a carboxylate radical group; R2 represents H or a carboxylate radical group; and the premise is that R1 and R2 are not H at the same time. The invention also provides a preparation method of the triphenyl pyrrole derivative. The triphenyl pyrrole derivative with the gathering induced luminescence performance, provided by the invention, has very good application prospects in the aspects like organic light-emitting diodes, chemical detection, bioassay and the like.

Provided are a polymer compound which has a pyrrole derivative compound and a phenoxazine derivative compound as a repeating unit, and an organic electroluminescent (EL) device using the same for forming a hole injection layer and / or a hole transport layer. The polymer compound according to the present invention has superior electric features and a high hole-transporting capability. Thus the organic EL device using the polymer compound for forming a hole injection layer and / or a hole transport layer has superior features such as low voltage and high efficiency compared to using conventional materials.

The invention discloses an ionic liquid micro-array monomolecular-layer fluorescent sensing film, and a preparation method and application thereof. The ionic liquid micro-array monomolecular-layer fluorescent sensing film is prepared by self-assembling an amphiphilic BOPIDY derivative with a BOPIDY host molecule as a hydrophobic head group and an ether oxygen chain as a hydrophilic tail in hydrophilic ionic liquid 1-butyl-3-methylimidazole tetrafluoroborate and then transplanting the prepared monomolecular-layer fluorescent sensing film onto a gold substrate through microcontact transferring technology. The preparation method is simple to operate and has mild reaction conditions; the prepared fluorescent sensing film has good stability, long service life and high sensitivity in detection of formaldehyde gas and can be applied to sensors for detecting formaldehyde gas; and the fluorescent sensing film can also be installed on a detection apparatus used for detecting formaldehyde gas in virtue of fluorescence principles, and response of the fluorescent sensing film to formaldehyde gas is monitored in real time.

The present invention relates to compounds of the formulae I and Ia,wherein R0; R1; R3; R4; R22, Q; V, G and M have the meanings indicated in the claims. The compounds of the formulae I and Ia are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable for the therapy and prophylaxis of cardiovascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa (FXa) and / or factor VIIa (FVIIa), and can in general be applied in conditions in which an undesired activity of factor Xa and / or factor VIIa is present or for the cure or prevention of which an inhibition of factor Xa and / or factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of the formulae I and Ia, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.

The invention relates to two novel difluoro boron dipyrromethene compounds which can be used as near-infrared fluorescent dyes and a preparation method thereof and belongs to the techcnial field of fluorescent probes. 8-(4-(chloromethyl) phenyl)-4,4-difluoro-1,3,5,7-tetramethyl-4-boron-3a,4a-dipyrrole (labeled as BODIPY-C), 1,2,3,4-tetrahydro naphthalene, 5-hydroxyl isophthalate and p-anisaldehyde are used as raw materials to synthesize the two novel difluoro boron dipyrromethene (BODIPY) derivatives. The two compounds are compounds for near-infrared absorption and near-infrared fluorescence emission and can be expected to be used as fluorescent probes for imaging in cells or organisms, and background interference is reduced.

The invention discloses a preparation method and an application of a boron-dipyrromethene (BODIPY) based fluorescent probe for determining cysteine (Cys). The structural formula of the probe is shown in the specification. The preparation method of the BODIPY derivative based Cys fluorescent probe with a simple structure is provided, and the BODIPY derivative based Cys fluorescent probe is used for directly measuring Cys concentration. In the system, the fluorescent probe shows good selectivity and is not interfered with other biological thiols (Hcy and GSH) and other 19 amino acids. The probe shows quite high sensitivity to Cys, and the fluorescence intensity is enhanced by 23 times when 3 equivalents of Cys are added. When the pH is between 6.0 and 8.0, determination of Cys by the fluorescent probe is not affected by pH. The fluorescence probe and Cys act quickly, and the response time is within 6 minutes. In addition, the probe can also be used in cell imaging to detect intracellular Cys.

The invention belongs to the technical field of organic synthesis chemistry, and particularly relates to a method for preparing iron-catalyzed pyrrole and pyrrole cyclic compounds. The invention provides a method for preparing FeX3-catalyzed pyrrole and thick pyrrole derivatives. The method comprises synthesis of an omega, gamma-alkynone compound, a cyclization reaction and the like. The method develops the cyclization reaction of the FeX3-catalyzed omega, gamma-alkynone compound and a primary amine compound, and can efficiently prepare high-purity pyrrole and pyrrole cyclic compounds with high yield. Compared with the conventional Pd, Au, Ag and Cu catalysts, the FeX3 has the advantages of environment friendliness and low price. The method has the advantages of simple operation, easily obtained raw materials and reagents, mild condition, environment-friendly catalytic system and easy separation and purification of products, is suitable for synthesizing various substituted pyrrole and pyrrole cyclic compounds, and is particularly suitable for large-scale industrial production.

Compounds of the formula (I), in which X, Y, Z and Ar have the meanings indicated in claim 1, are inhibitors of Raf kinase and can be employed, inter alia, for the treatment of tumours

The present invention relates to Saroglitazar free acid of Formula (IA) or its pharmaceutically acceptable salts, pharmaceutically acceptable solvates, pharmaceutically acceptable esters, stereoisomers, tautomers, analogs and derivatives thereof. The present invention also provides an amorphous form of saroglitazar free acid and processes of preparation thereof. The present invention also provides pharmaceutical composition comprising an amorphous form saroglitazar magnesium.

The invention relates to a pharmaceutical composition comprising a pyrrole derivative of the following formula [1] or a pharmaceutically acceptable salt thereof, or a solvate of either of them, as an active ingredient.(wherein R1 represents hydrogen or alkoxycarbonylamino, R2 represents alkyl, aryl which may be substituted, aromatic heterocyclyl which may be substituted, unsubstituted amino, monoalkylamino, dialkylamino, or cyclic amino which may be substituted; R3 represents cyano or carbamoyl; R4 represents hydrogen or alkyl; E represents alkylene; q is equal to 0 or 1, A represents methyl, aryl which may be substituted, or aromatic heterocyclyl which may be substituted)The pharmaceutical composition of the invention is effective for the treatment of pollakiuria or urinary incontinence.

A transdermal delivery system for pyrrole derivatives of formula 1, metabolites thereof, enantiomers thereof, racemates thereof, and salts including acid addition salts thereof, alone or in conjunction with one or more other therapeutic agents, using vehicles selected to enhance absorption and which enable the compounds to be administered into and through the skin when topically applied.

The present invention relates to an improved process for the preparation of pyrroles derivatives having hypolipidemic and hypocholesteremic activities. In particular, the invention relates to an improved process for the preparation of 2-ethoxy-3-(4-(2-(2-methyl-5-(4-(methylthio)phenyl)-1H-pyrrol-1-yl)ethoxy)phenyl)propanoate and its pharmaceutically acceptable salts, hydrates, solvates, polymorphs or intermediates thereof. The invention also relates to an improved process for the preparation of mesylate compound (A1).

The invention belongs to the technical field of the organic chemical industry, and particularly relates to a fluorine-boron pyrrolizinone fluorochrome. The chemical structural formula of the fluorochrome is shown in the description, wherein the substituent groups R1 and R2 are hydrogen or alkyl or ester or nitryl or nitrile or alkoxy or halogen or aryl or other conjugated systems, and the positions, numbers and conjugated positions of the substituent groups are flexible. A synthesizing method comprises the steps that a 2,3,3-3-methylindole derivative and 2-formyl pyrrole derivative are subjected to a condensation and complexing reaction under the action of an organic catalyst, and a novel fluorine-boron pyrrolizinone fluorescent compound is obtained. The synthesizing method has the advantages that few steps are needed, and the yield is high, and the fluorine-boron pyrrolizinone fluorochrome is beneficial to in vivo application due to the good electronic spectrum feature.

The invention relates to a novel pyrroles derivative as well as a preparation method and pharmaceutical application thereof. Specifically, the invention relates to the novel pyrroles derivative shown as a general formula (I) as well as pharmaceutically acceptable salt thereof or a pharmaceutical composition containing the novel pyrroles derivative, and a preparation method thereof. The invention further relates to application of the pyrroles derivative and the pharmaceutically acceptable salt thereof or the pharmaceutical composition containing the novel pyrroles derivative to preparation of a treatment agent, particularly application to a gastric acid secretion inhibitor and potassium competitive acid blockers (P-CABs), wherein the definition of each substituent group in the general formula (I) is the same as that in the description. (The general formula (I) is shown in the description.).