11 results about "Imidazoquinoline" patented technology

The present invention provides novel drug-linker conjugates and antibody-drug conjugates of imidazo quinoline amine derivatives, which have agonistic activity against Toll-like receptors (TLRs), in particular TLR7 and / or TLR8, also provided are pharmaceutical compositions and methods of treatment against certain diseases or conditions mediated by or associated with TLR7 and / or TLR8 (e.g., graft rejection, autoimmunity, inflammation, allergy, asthma, infection, sepsis, cancer, and immunodeficiency).

The invention provides a photoacid generator, a preparation method of the photoacid generator, a chemical amplification type photoresist and a preparation method of the chemical amplification type photoresist, and relates to the field of photoresist. The structural formula of the photoacid generator provided by the invention is shown in the specification, and the photoacid generator is sulfonium salt taking 5-tert-butyl-3-methyl-4-methylimidazo [1, 5-a] quinoline-3, 5-dicarboxylate as an acidic unstable group. The acidic unstable group is decomposed into an acid under high-energy radiation, the acidic unstable group is effectively decomposed into a carboxylic acid derivative and an imidazo [1, 5-a] quinoline derivative under the action of the acid and PDB (photolysis alkali), and the imidazo [1, 5-a] quinoline derivative can inhibit the diffusion rate of photoacid in the resist, so that the resistance of the resist is improved. Therefore, the dissolution rate of the photoresist in the developing solution after exposure is changed, and the problem of top loss after exposure and development of the photoresist is further solved.

Provided herein are lipidated imidazoquinoline compounds and compositions comprising such compounds. The lipidated imidazoquinoline compounds may be used as an adjuvant to enhance to immune response elicited by an antigen of interest. Accordingly, also provided herein are methods for enhancing the immune response of an antigen of interest in a subject, comprising administering to the subject an antigen of interest with a lipidated imidazoquinoline compound described herein in an immunogenic composition, or administering to the subject a composition comprising a lipidated imidazoquinoline compound described herein in combination with (e.g., prior to, concurrently, or subsequently) the administration of an immunogenic composition comprising an antigen of interest to the subject.

Imidazo[4,5-c]quinoline compounds having a substituent that is attached at the N-1 position by a branched group, single enantiomers of the compounds, pharmaceutical compositions containing the compounds, and methods of making the compounds are disclosed. Methods of use of the compounds as immune response modifiers, for inducing cytokine biosynthesis in humans and animals, and in the treatment of diseases including infectious and neoplastic diseases are also disclosed.

The application discloses a CDK8 hydrophobic tag degrading agent and a preparation method and application thereof. The CDK8 hydrophobic tag degrading agent is a 7,8-dibromo-9-methyl-2-(piperazine-1-yl)-5,6-dihydro-4H-imidazo[4,5,1-iJ]quinoline derivative, and has excellent CDK8 degrading activity and antitumor activity.

The invention discloses an imidazo [4, 5-C] quinoline-2-ketone derivative for preparing an ATM kinase inhibitor, and belongs to the field of chemical medicines. The invention provides an imidazo [4, 5-C] quinoline-2-ketone derivative shown as a general formula (I) or a pharmaceutically acceptable salt thereof, and the compound has an excellent ATM inhibition effect and can be used as a medicine for treating or preventing ATM-mediated diseases (including cancers).

Provided are an imidazoquinoline or benzoindazolone compound or a pharmaceutically acceptable salt, hydrate, solvate, enantiomer, diastereomer, tautomer or precursor drug thereof; a use thereof for preventing and treating an inflammatory disease; and an intermediate for preparing same, where the compound is used as a substrate of NQO1 to activate the oxidation-reduction of NQO1, thus making it possible to prevent the expression and activity of inflammatory cytokines, and as such, can be used for preventing or treating diseases associated with NQO1 activity.

This application relates to the field of chemical pharmaceutical technology, and more particularly to an imidazoquinoline compound having an alkylthio or alkyldithio group, its preparation method, and its application. The imidazoquinoline compound of this application includes the imidazoquinoline compound shown in Formula I and its pharmaceutically acceptable salt. This imidazoquinoline compound can activate TLR7 and TLR8 receptors, and after local injection, the level of the inflammatory factor IL6 in the blood is further reduced compared to the prototype molecule 78A1. While achieving local immunostimulation, it minimizes the non-specific immunotoxicity caused by cytokine storms, thus significantly improving safety. Therefore, the imidazoquinoline compound provided in this application can be used more safely for local immune activation, such as for tumor treatment or as an immunostimulatory adjuvant for vaccines.

4-amino-imidazoquinoline compounds and uses thereof are disclosed. The compounds of the present invention are Toll-like receptor 7 (TLR7) and TLR8 dual agonists and exhibit the activity of inducing the expression of IL-12 and IP-10 without excessively inducing IL-6. TLR7 / 8 dual agonists may be useful pharmaceuticals as immune response modifiers. Use of the compounds of the present invention or salts thereof in the manufacture of a medicament for treating a disease or condition in a subject in need thereof in which activation of TLR7 and / or TLR8 would be beneficial is disclosed. Compounds or pharmaceutical compositions for use in treating viral infections, cancers, and / or allergic diseases in a subject in need thereof, or for activating an effective immune response against viral infections, tumors, and / or allergic diseases, are also disclosed.

The application provides a kind of double stimulus responsive polythioic acid polymer, nano delivery system and its preparation method and application.The double stimulus responsive polythioic acid polymer described in the application includes glutathione responsive polythioic acid, and the carboxyl position of the glutathione responsive polythioic acid is grafted with polyethylene glycol group and tissue protease B responsive peptide chain covalent connection TLR7 / 8 agonist imidazoquinoline.The application takes PTA with good biocompatibility and glutathione degradability as skeleton, side chain is covalently connected with TLR7 / 8 agonist IMDQ through tissue protease B responsive peptide chain, self-assembled to form nanoparticle, can be accumulated in injection site and effectively drained to lymph node, responds to release IMDQ in antigen presenting cell (APC), realizes the accurate delivery and efficient release of IMDQ.

The application relates to the technical field of medicines, and particularly discloses a novel immune stimulant, a preparation method and application thereof. The immune stimulant comprises an alpha-mannose modified imidazoquinoline derivative, an N-acetyl cysteine modified cytosine-guanine dinucleotide, a glycyrrhetinic acid-polyethylene glycol derivative, a phytic acid-glycine oligomer, a medicinal excipient and water for injection, three modified active ingredients are bridged by the phytic acid-glycine oligomer as a bridging unit, and a ternary coordination complex is formed through dynamic non-covalent coordination. The preparation method comprises the following steps: after raw materials are pretreated, the active ingredients are premixed, dissolved and solvent is recovered, then dynamic coordination reaction, ultrafiltration purification and concentration are carried out, and finally, a finished product is obtained through double-cavity preparation forming. The immune stimulant can be used for preparing a tumor immunotherapy, an anti-infection treatment, an immune deficiency disease auxiliary treatment drug or a vaccine adjuvant, and has the advantages of high active ingredient stability, good in-vivo delivery efficiency and outstanding synergistic effect.