61results about How to "Novel chemical structure" patented technology

It is intended to provide novel amine compounds which are efficacious against diseases such as infection with HIV virus, rheumatism and cancer metastasis. Namely, amine compounds represented by the following general formula (1): In a typical case, A1 and A2 represent each an optionally substituted monocyclic or polycyclic aromatic heterocycle; W represents cyclic C3-10 alkylene, an optionally substituted monocyclic or polycyclic aromatic heterocycle, a monocyclic or polycyclic aromatic ring or a partly saturated polycyclic aromatic ring; X represents O, CH2, C(═O) or NR11; and D is a group represented by the following general formula (4) or (6). In the formula (6), Q represents a single bond, S, O or NR12; and Y is a group represented by the following general formula (7). z represents an optionally substituted monocyclic or polycyclic aromatic ring. In the formula (6), B represents NR25R26. In the above formulae, R1 to R26 each represents hydrogen, alkyl, alkenyl or alkynyl.

The invention relates to a bridged dipyrene-3,4,6,7-12, 13, 15, 16-octcarboxylic acid tetraimide compound containing sulphur atoms or selenium atoms and a preparation method thereof. 1,6, 7,12-tetrahalogenated pyrene-3,4-9,10-tetracarboxylic acid diimide compound or 1,9,10,18-tetrahalogenated dipyrene-3,4,6,7-12, 13, 15, 16-octcarboxylic acid tetraimide compound, sodium sulfide or sodium selenide, a catalyst, an amino acid ligand and inorganic base are mixed; then an organic solvent is added; the reaction is carried out under the protection of inert gas; the product is dissolved in the solvent, is washed in sodium chloride aqueous solution, and is dried and filtrated; then the solvent is distilled to dryness; and the bridged dipyrene-3,4,6,7-12, 13, 15, 16-octcarboxylic acid tetraimide compound containing sulphur atoms or selenium atoms in the lateral position showed by formula(I) or (II) is obtained through column chromatography separation. The yield after purification is 10 to 40 percent.

The invention belongs to the technical field of medicines, and discloses indoline compounds having a general formula I in which substitutes R1, R2, R3, R4 and R5 are defined in the specification and apreparing method and application thereof. The indoline compounds, stereisomers thereof, pharmaceutically acceptable salts thereof and pharmaceutical compositions containing the compounds can be usedfor preparing medicines treating diseases related to PD-1 / PD-L1 protein / protein interactions, such as cancer and virus infection.

A polyglycolized derivative of thymopeptide-5, which can be used to prepaer the medicines for preventing and treating rheumatoid arthritis, allergic dermatisis, tumor, viral infection, and the diseases associated with immune deficiency and hypoimmunofunction, is disclosed. Said derivative features that the polyglycol, polyglycol modified amino acid, cysteine, maleamido glycol, vinyl glycol, or iodoacetylglycol is introduced or coupled to the N or C terminal of thymopeptide-5.

The invention relates to a vancomycin derivative as shown in the formula (I) and a stereisomer, pharmaceutically acceptable salts, a preparation method of the vancomycin derivative and its application in treating and / or preventing diseases or symptoms related to gram negative bacterial infections.

The invention discloses an N-substituted polybenzimidazole amide compound and a preparation method thereof. The preparation method disclosed by the invention comprises the following steps that: (1) bis(benzimidazole) compounds with different structures are obtained in the catalysis of a polyphosphoric acid system based on aromatic dicarboxylic acids with different structures and o-phenylenediamine (the molar ratio is 1:2.2) as monomers; (2) difluorinated amido compounds with different structures are obtained in the catalysis of triethylamine based on aromatic diamines with different structures and 4-fluorobenzoyl chloride (the molar ratio is 1:5) as the monomers; and (3) the N-substituted polybenzimidazole amide compound is obtained by taking bis(benzimidazole) intermediate and the difluorinated amido compound (the molar ratio is 1:1) as the monomers, sulfolane as a solvent, chlorobenzene as a dewatering agent and calcium carbonate as a fluorinion removing agent in the catalysis of anhydrous potassium carbonate. The preparation method disclosed by the invention is simple in synthesis process and low in cost, and the compound disclosed by the invention is high in yield.

The invention discloses polyaryletherketone containing an indole group and a preparation method of polyaryletherketone. The polyaryletherketone is shown in formula (I). The preparation method includes the following steps: under the protection of nitrogen, adding 4-hydroxyindole, a keto-group-containing difluoro monomer, a bisphenol monomer, a salt-forming agent, a solvent and methylbenzene in a reactor; stirring the mixture evenly, and conducting heating to increase the temperature to 130-140 DEG C for reaction for 3-4 hours; distilling off methylbenzene, and then increasing the temperature to 160-190 DEG C for continuous reaction for 4-6 hours; cooling the materials obtained after the reaction to room temperature, and pouring the materials in deionized water for sedimentation; conducting suction filtration to obtain a solid product, conducting extraction with methyl alcohol, and drying the solid product obtained by suction filtration to obtain polyaryletherketone containing the indole group. The polyaryletherketone containing the indole group is good in thermal stability, relatively high in glass transition temperature, good in solubility and unique in optical property, and can be used in battery diaphragms, optoelectronic devices, electrode materials, inertial confinement fusion film targets and other fields. Please see the formula in the specification.

The invention discloses substituted xanthine compounds, a preparation method and applications thereof, and specifically relates to compounds represented by the formula (I), stereo isomers and pharmaceutically acceptable salts thereof, wherein the R1 and R2 are defined in the description. The invention also relates to a pharmaceutical composition containing the compounds, an application of the pharmaceutical composition in preparation of drugs for treating diseases or symptoms caused by high activity of DPP-IV or overexpression of DPP-IV, and a method using the pharmaceutical composition to treat related diseases. The provided compounds can effectively inhibit the activity of DPP-IV.

A red light fluorescent material adapted for being excited by a first light to emit a red light is provided. The red light fluorescent material has the chemical formula (1) presented below,A2Eu(MO4)(PO4)  (1),in which A represents Li, Na, K, Rb, Cs, or Ag, and M represents Mo, W, or a combination thereof (MoxW(1-x)). The red light fluorescent material can provide a red light with high luminance and good color purity. Moreover, since the composition of the red light fluorescent material includes oxides, the red light fluorescent material has high chemical stability and long lifetime.

The invention discloses a benzo-azepine type derivative and a preparation method and purposes thereof. The benzo-azepine type derivative has the structure of a general formula I, wherein in the formula I, R1 is any one among hydrogen, halogen, or halogen substituted C1-C4 alkyl, R2 is oxygen or hydroxyl, and R3 is any one among hydrogen, C1-C4 alkyl, C1-C4 alkoxy, halogen or hydroxyl. According to the invention, compounds or pharmaceutically acceptable salts having the structure of the formula I are novel in chemical constitution, and have an obvious restraining effect, the same as fluorouracil generally used in clinical trials, for tumors, in particular to human lung adenocarcinoma cells, human breast cancer cells and human gastric carcinoma cells.

The present invention discloses a five-membered-aromatic-heterocycte-containing substituted xanthine compound and a preparation method and use thereof. More specifically, the present invention relates to a compound of formula (I) and stereoisomers and pharmaceutically acceptable salts thereof which are as described in specification. The present invention also relates to a pharmaceutical composition comprising the compound, use of the compound in the manufacture of drugs for treatment and / or prevention of diseases or disorders related to too high DPP-IV activity or DPP-IV overexpression, and a method for using the compound for treatment of the related diseases. The compound has efficient DPP-IV inhibitory activity.

A kind of antineoplastic antibiotic compound, chinikornycin A and B, for suppressing the cells of lung cancer, breast cancer, melanoma, renal cancer and uterine cancer is prepared from Streptomyces sp. through fermenting and chromatography by silica gel column.

The invention relates to a pyridine-ion-containing vinyl cephalosporin derivative of structural formula I as shown in the specification, a pharmaceutically acceptable salt of the vinyl cephalosporin derivative, a preparation method of the derivative, and application of the derivative in preparing medicines for preventing and / or treating diseases, symptoms and the like related to bacterial infection.

The invention belongs to the technical field of a medicine, and relates to a phloroglucinolo abietane diterpenoid compound, a preparation method of the compound and a medicinal application, particularly, an application to preparation of a protein-tyrosine-phosphatase 1B inhibitor. The novel phloroglucinolo abietane diterpenoid compound (having a structural formula shown in the description) capable of inhibiting activity of protein-tyrosine-phosphatase 1B (PTP1B) is extracted and separated from entire herbs or roots of chloranthus oldhami, which is a plant in chloranthus genus of the chloranthaceae family. In the structural formula, R1 and R2 are methyl or hydroxymethyl, and R3 is a long-chain alkene. An in-vitro biological activity test shows that the compound has obvious inhibition activity of PTP1B, and can be used for preparing medicines for preventing, delaying, or treating diabetes, obesity, and complication thereof, and other medicines mediated by PTP1B.

The invention discloses a nitrogen-containing heterocyclic substituted pyrrolidine formyl thiomorpholin DPP-IV inhibitor, a preparation method therefor and use thereof. Specifically, the invention relates to a compound shown in a formula (I), a stereisomer thereof and pharmaceutically acceptable salt thereof mentioned in the description. The invention further relates to a pharmaceutical composition comprising the compound, use of the compound in preparing drugs for treating and / or preventing diseases or illnesses associated with DDP-IV excessive activity or DPP-IV overexpression and a method of treating associated diseases by using the compound. The compound disclosed by the invention has the effect of effectively inhibiting the activity of DDP-IV. The FORMULA is shown in the description.

The invention belongs to the technical field of medicinal chemical industry, and discloses an oxygen-substituted phenylimidazole XOR / URAT1 dual inhibitor, preparation and applications thereof, whereinthe oxygen-substituted phenylimidazole XOR / URAT1 dual inhibitor has a structure represented by a formula (A), R1 represents C1-C7 alkyl, R2 is -COOH or -COOC2H5, and R3 is -H or -CH3. According to the present invention, the oxygen-substituted phenylimidazole XOR / URAT1 dual inhibitor has the chemical structure different from the known XOR / URAT1 dual inhibitor, has excellent effects on both key targets of XOR and URAT1 related to gout, and can be used for preparing anti-hyperuricemia or anti-gout drugs.

The invention discloses a preparation method of a monoterpenoid indole alkaloid compound with a novel chemical structure from ochrosia borbonica and a medical application of the compound in preparation of a targeted anti-tumor drug by employing protein tyrosine kinase as a target. The compound is a novel monoterpenoid indole alkaloid compound. The compound has significant anti-tumor activity, has protein tyrosine kinase-inhibition activity equivalent to a positive control drug, and has the prospect of being developed into the targeted anti-tumor drug by employing the protein tyrosine kinase as the target.

The invention relates to a micromolecular reversible BTK inhibitor for treating rheumatoid arthritis, and specifically provides a compound. The compound is the compound as shown in a formula I, or a stereisomer, a geometrical isomer and a tautomer thereof, nitric oxide, aquo-complex, a solvate, a metabolite and pharmaceutically acceptable salts and prodrugs. The inventor finds that polysubstitutedquinolone compound or derivate thereof as shown in formula I can be used as the BTK inhibitor and is high in activity during treating rheumatoid arthritis.

The invention discloses bisbenzylisoquinoline betaine with anti-tumor activity and a preparation method thereof. The compound has the following structural general formula shown in the specification. The preparation method comprises the steps of taking bisbenzylisoquinoline compounds as raw materials, dissolving into a certain solvent, adding a catalyst and a reactant Y, mixing, performing reaction for 0.1-72 hours at -20 DEG C to 300 DEG C, performing hydrolysis and neutralization reaction on the materials after reaction, and then separating and purifying to obtain an objective product. According to the preparation method disclosed by the invention, the prepared bisbenzylisoquinoline betaine has a relatively good inhibiting effect on proliferation of the human liver cancer cell strain HepG2 and leukemia K562 cells, and can be used for preparing anti-tumor medicaments.

The invention provides an N-substituted polybenzimidazole pyridine compound (the general formula is I) and a preparation method thereof. The preparation method sequentially comprises steps of (1) by taking 2, 6-dual (terephthaloyl chloride) pyridine and fluorobenzene as monomers, under the condition of existence of anhydrous aluminum chloride, obtaining a 2,6-dual (4-fluorobenzene formyl) pyridine compound; (2) by taking the 2,6-dual (4-fluorobenzene formyl) pyridine compound and dual (benzimidazole) of different structures as the monomers, sulfolane as the solvent, chlorobenzene as the dewatering agent, calcium carbonate as the fluorinion removing agent, under the condition of catalysis of anhydrous potassium carbonate, preparing the N-substituted polybenzimidazole pyridine compound. The preparation method has a simple synthetic process, and has low cost and high productivity.

The invention discloses a poly(aryl ketone)imidazole and a preparation method thereof, wherein the poly(aryl ketone)imidazole has a structural general formula shown as below. The invention also relates to a preparation method of the poly(aryl ketone)imidazole. The method comprises the steps that aromatic diacids with different structures and o-phenylenediamine are used as monomers to prepare bis(benzimidazole) intermediates with different structures under catalysis of a polyphosphoric acid and phosphoric acid system; monomers of difluoride aromatic ketone and bis(benzimidazole) intermediates,a solvent of sulfolane and a water-removal additive of chlorobenzene are used to prepare poly(aryl ketone)imidazole under catalysis of anhydrous potassium carbonate. The poly(aryl ketone)imidazole prepared by the invention has high glass-transition temperature, high decomposition temperature, excellent mechanical properties, and is prepared through a simple technical operation at low costs.

The invention belongs to the field of pharmaceutical chemistry, and relates to C20 site epimerization salinomycin and acylated derivatives thereof, and a preparation method and an anti-tumor use thereof, especially a use in preparation of drugs for resisting lung cancer, colon cancer and liver cancer.

The invention belongs to the technical field of medicine and relates to a triazolopyridine compound and a preparation method and application thereof, in particular to a triazolopyridine compound having the structure of general formula I and its stereoisomers and pharmaceutically acceptable salts, wherein R1, R2, R3 and R4 are described as in the claims and the description. All the triazolopyridinecompound, its stereoisomers and pharmaceutically acceptable salts, and a composition containing the triazolopyridine compound can evidently inhibit interaction of PD-1 / PD-L1 protein / protein, are suitable for treating the various diseases, such as cancers and viral infections, and therefore, are applicable to the preparation of drugs to prevent and / or treat diseases associated with PD-1 / PD-L1 signal pathway.

The invention relates to a triterpenoid compound as shown below and a preparation method and use thereof. It is shown through several in vitro immunosuppressive activity tests that the compound has anobvious effect on inhibiting lymphocyte proliferation in mice and are expected to be used in the preparation of immunosuppressive drugs. The triterpenoid compound and the preparation method and use thereof can provide lead compounds for the development of new drugs for the treatment of autoimmune diseases and organ transplant rejection.

The invention discloses a 4-substituted pyrrolidine formyl thiomorpholine DPP-IV (Dipeptidyl Peptidase IV) inhibitor and a preparation method therefor and use thereof. Specifically, the invention relates to a compound represented by a formula (I) shown in the description, a stereoisomer thereof and pharmaceutically-acceptable salts thereof, wherein R1 and R2 are as defined in the description. The invention also relates to a pharmaceutical composition containing the compound disclosed by the invention, use of the compound disclosed by the invention in preparation of drugs for methods for treating and / or preventing too-high DPP-IV activity or DPP-IV overexpression related diseases or disease symptoms, and a method for treating related diseases by using the compound disclosed by the invention. The compound disclosed by the invention has effective DPP-IV inhibiting activity.

The invention relates to a benzophenone bisamide bridged diquaternary ammonium salt type light-induced synergistic antibacterial agent and a preparation method thereof. The preparation method comprises the following steps: taking 3,3',4,4'-benzophenonetetracarboxylic dianhydride and an N,N-dimethyl fatty amine compound as raw materials, and performing a condensation reaction to obtain a benzophenonetetracarboxylic diamide compound intermediate; performing a quaternization reaction to obtain the benzophenone bisamide bridged diquaternary ammonium salt type light-induced synergistic antibacterial agent. The antibacterial agent involved in the invention has synergistic efficient antibacterial properties of a light-induced quaternary ammonium salt unit and a benzophenone bisamide unit, and has the advantages of mild reaction conditions, simple preparation process and the like at the same time.