44 results about "TLR7" patented technology

Provided in the present invention are an anti-TLR7 antibody or an antigen-binding fragment thereof, and a pharmaceutical composition thereof. The antibody or the antigen-binding fragment thereof can specifically bind to a human or simian TLR7 antigen and does not bind to murine TLR7, exhibits significant TLR7 antigen-binding activity, and can effectively inhibit various inflammatory cytokines produced upon TLR7 activation. The anti-TLR7 antibody or the antigen-binding fragment thereof can be used, either as a monotherapy or in combination with other drugs, for treating and / or preventing diseases pathologically associated with the TLR7 target, including immune inflammation-related diseases, allergic diseases, infectious diseases, cancers, etc.

The invention provides an anti-TLR7 antibody or an antigen binding fragment and a pharmaceutical composition thereof, the antibody or the antigen binding fragment thereof can be specifically bound with a human or monkey TLR7 antigen and is not bound with mouse TLR7, has remarkable TLR7 antigen binding activity, and can effectively inhibit various inflammatory cytokines generated by TLR7 activation. The anti-TLR7 antibody or the antigen binding fragment thereof can be used as a single agent or a drug combination and can be used for treating and / or preventing diseases related to TLR7 target pathology, including immune inflammation related diseases, allergic diseases, infectious diseases or cancers and the like.

The present application relates to a compound of Formula I or a pharmaceutically acceptable salt thereof, as a Toll-like Receptor 7 (TLR7) agonist, for use in the treatment of lung cancer, a pharmaceutical combination of a TLR7 agonist and a tyrosine kinase inhibitor for use in the treatment of lung cancer, and the use of a compound of Formula I or a pharmaceutically acceptable salt thereof in the pharmaceutical combination in the treatment of lung cancer.

The present disclosure provides methods of treating or inhibiting cancer, reducing its severity, reducing its risk, or inhibiting its metastasis in an individual with a radiation-activated N-oxide TLR7 / 8 agonist.

Lipidized oxoadenines of formula (I) are TLR7 / 8 receptor ligands useful for modulating immune responses. These compounds may have therapeutic applications in the treatment of cancer, infectious diseases, allergies, or autoimmune disorders (SEE FORMULA).

Lipidated oxoadenines of formula (I) are TLR7 / 8 receptor ligands useful for modulating immune responses. The compounds may have therapeutic application in the treatment of cancer, infectious diseases, allergy, or autoimmune disorders.

The present invention provides a method for activating an N-oxide TLR7 / 8 agonist using radiation and a method for treating or inhibiting cancer, reducing its severity, lowering its risk, or inhibiting metastasis.

This invention discloses a photoactivated nanoparticle-based drug delivery material for immunoadjuvants, its preparation method, and its applications. The drug delivery material is constructed from photosensitizer monomers, crosslinking monomers, and immunoadjuvant prodrug monomers within a confined space of a nanoemulsion via a copper-free click polymerization reaction to form crosslinked polymer nanoparticles. The nanoparticle size is controllable, and the composition is precisely defined. Under physiological conditions, the drug delivery material exhibits good colloidal stability and high drug loading. Upon near-infrared light irradiation, the generated ROS can cleave the thioketone bonds, causing the nanoparticles to depolymerize and achieving photo-triggered, controllable release of the immunoadjuvant. Under photodynamic action, this drug delivery material efficiently generates reactive oxygen species to induce immunogenic cell death in tumor cells. Simultaneously, the released immunoadjuvant activates the TLR7 / 8 pathway, promotes dendritic cell maturation, and enhances the systemic anti-tumor immune response, thereby inhibiting the growth of tumors in situ and at distant sites, and reducing the risk of metastasis and recurrence.

An imidazo [2,1-f] [1,2,4] triazin-4-amine derivative or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof which are used as a TLR7 agonist in the treatment of cancer are provided. Pharmaceutical compositions comprising the imidazo [2,1-f] [1,2,4] triazin-4-amine derivative or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof are also provided.

The present invention relates to compounds of formula (I) and pharmaceutically acceptable compositions thereof useful as toll-like receptor 7 / 8 (TLR7 / 8) antagonists.SOLUTION: In Formula (I), ring A is aryl or heteroaryl; ring B is aryl or heteroaryl; and X is C (R4) 2, O, NR4, S, S (R4), or S (R4) 2.SELECTED DRAWING: None

The invention relates to a compound as shown in a formula (I) and an isotope form, a stereoisomer, a tautomer, pharmaceutically acceptable salt, pharmaceutically acceptable solvate, hydrate, prodrug and polymorphic substance thereof, the compound as shown in the formula (I) can be used as a TLR inhibitor, effectively inhibits the expression level of TLR, especially double inhibition on TLR7 / 8, and can be used for preparing a TLR inhibitor. The compound has a good application prospect in the aspect of preparing medicines for treating TLR activity mediated diseases.

The present disclosure describes methods, compositions, and kits related to the combination of a TLR7 modulating compound and an HIV vaccine. The combination can be used in a method of treating or preventing an HIV infection in a human.

A compound of Chemical Formula 1 or a pharmaceutically acceptable salt thereof is disclosed. The compound inhibits a toll-like receptor (TLR) signaling pathway. A composition containing the compound and uses thereof are disclosed. The novel compound blocks the TNF-α secretion by inhibiting the expression and activation of NF-κB- and MAPK-related proinflammatory genes, and thus can be utilized as a therapeutic agent for many autoimmune diseases, such as systemic lupus erythematosus, psoriasis and psoriatic arthritis, associated with a hyperactivity of a nucleic acid:

The application discloses an injection containing a compound as shown in formula (I) or a pharmaceutically acceptable salt thereof, and a preparation method of the injection. The preparation method of the injection is simple, the quality of the injection is stable, the injection is convenient for clinical administration, and the injection meets the requirements of subsequent clinical tests.

A method to enhance an immune response in a mammal, and a composition comprising liposomes, a TLR4 agonist and a TLR7 agonist, are provided.

Provided are a pharmaceutically acceptable salt, a crystal form and a preparation method of a TLR7 / 8 agonist compound of formula I, a pharmaceutical composition containing the pharmaceutically acceptable salt, and a medical use of the pharmaceutically acceptable salt, which can be used for preparing drugs for preventing or treating Toll-like receptor 7 / 8 (TLR7 / 8) related diseases, such as a new therapeutic agent for human immunodeficiency virus (HIV) infection, hepatitis B virus (HBV) infection, hepatitis C virus (HCV) infection and cancer.

The present invention provides a pharmaceutical composition comprising solid particles comprising at least one toll-like receptor 4 (TLR4) agonist and micelles comprising at least one toll-like receptor 7 (TLR7) agonistfor use as a medicament or for use in the treatment of cancer, an antibiotic resistance, an inflammatory condition or disease, an autoimmune disease or an infectious disease and at least one amphiphilic micelle-forming agent. Also provided is a method of preparing the pharmaceutical composition and a kit or kit of parts comprising the pharmaceutical composition for use.

Use of artemisia oil in a medicament for treating a side effect-related condition caused by the administration of a TLR7 / 8 agonist, in particular use of artemisia oil in the manufacture of a medicament for preventing, treating or ameliorating skin microflora imbalance caused by the administration of a TLR7 / 8 agonist on the body surface.

Compound having a structure represented by one or more of the formulas I-a1 and I-c1: or a pharmaceutically acceptable salt, solvate, hydrate, crystal form, tautomer or diastereomer thereof, wherein: A is a tumor-directed unit with a molecular weight of 3000 Da or less and is a PSMA-binding unit; B is a spacer; C is a splittable or non-splittable left; D is a self-destructing spacer; c and d can each be 0 or an integer of 1 or more; preferably 0, 1, 2 or 3; wherein each occurrence of B, C and D may be in any order; and wherein each of E-a1 and E-c1 is a TLR7 agonist unit which is a structure of the formula E-a1 or E-c1 respectively. This includes: where Z a1 C3-Alkynyl is; U 1 -W 1Selected from: and R is selected from H, C 1-3 -Alkyl, C 1-3 -Haloalkyl and C 1-3 -Heteroalkyl; and R 1 selected from C 1-8 -Alkyl, C 2-8 -Cycloalkyl, (C 3-6 -Cycloalkyl) C 1-3 -alkyl, C 1-7 -Heteroalkyl, C 2-7 -Cycloheteroalkyl, -C (=O) NH (C 1-3 -alkyl), -C 1-3 -Alkyl (C=O) OME, -C(=O)NH (C 2-8 -Cycloalkyl), (C 2-7 -Cycloheteroaryl) C 1-3 -alkyl and (C 6-10 -Aryl) C 1-3 -alkyl; each optionally substituted with one or more substituents, preferably selected from OH, CH3, OMe, CN, -C(=O)Me, F2CH, SO2Me and halogen.

The disclosure relates to compounds of Formula (I)and pharmaceutically acceptable salts thereof, wherein X1, X2, and Y are as defined in the description; to their use in medicine; to compositions containing them; to processes for their preparation; and to intermediates used in such processes. The compounds of Formula (I) may modulate the activity of antigens of interest and may be useful in inducing or enhancing an immune response against diseases, disorders and conditions mediated by antigens of interest. In a particular embodiment, the compounds of Formula (I) may be useful as a component of a liposomal adjuvant formulation.

The invention relates to the technical field of vaccine adjuvants, and discloses a TLR7 / 8-Lipo + AL freeze-dried vaccine adjuvant as well as a preparation method and application thereof, and the freeze-dried vaccine adjuvant comprises a TLR7 / 8-coupling-Lipo compound, a TLR7 / 8-Lipo + AL freeze-dried vaccine adjuvant, a TLR7 / 8-Lipo + AL freeze-dried vaccine adjuvant and a TLR7 / 8-Lipo + AL freeze-dried vaccine adjuvant, an aluminum salt adjuvant; sucrose at a concentration of 2.0% to 3.0%; the invention provides a Lipo-AL compound freeze-drying agent and a preparation method thereof, the Lipo-AL compound freeze-drying agent comprises sucrose and glycine, the concentration of the sucrose is 1.0-2.0%, the sucrose and the glycine are specifically combined for use, the problems of particle aggregation and structure collapse caused by freeze-drying stress in the Lipo-AL compound freeze-drying process are synergistically solved, the invention also provides a preparation method, and the preparation method comprises the following steps: preparing a Lipo compound, adsorbing with an aluminum salt adjuvant, adding the sucrose and the glycine, and preparing the Lipo-AL compound freeze-drying agent. And finally, carrying out freeze drying. The freeze-drying adjuvant prepared by the invention has the characteristics of complete form, quick redissolution and uniform particle size after redissolution, and can still keep high biological activity after long-term storage.

The present invention belongs to the technical field of cancer immunotherapy and specifically relates to a combination-therapy drug and composition of a cholesterolylated TLR7 liposome and a TLR9 agonist and use thereof. Toll-like receptor agonists have poor targeting capability and significant side effects in anti-tumor treatment, and, as monotherapy in anti-tumor treatment, have limited efficacy. To address the described issues, the present invention provides the cholesterolylated TLR7 liposome, which is prepared from the cholesterol-modified 1V209 molecule 1V209-Cho, a lipid component, and cholesterol, and uses the liposome in combination with the TLR9 agonist to treat tumors. Animal results show that the combination of the liposome and the TLR9 agonist, when administered as nasal drops or by means of intramuscular injection, can significantly inhibit pulmonary metastasis of cervical cancer cells and melanoma cells, indicating that using the cholesterolylated liposome 1V209-Cho-Lip in combination with the TLR9 agonist to treat tumors is a strategy with great potential.

The invention relates to a fused heteroaryl compound, a preparation method thereof and application of the fused heteroaryl compound in medicine. Specifically, the invention relates to a fused heteroaryl compound as shown in a general formula (I), a preparation method thereof, a pharmaceutical composition containing the compound and application of the compound as a therapeutic agent, especially application of the compound as a TLR7 / 8 / 9 inhibitor and application of the compound in preparation of drugs for treating and / or preventing inflammatory and autoimmune diseases.

Disclosed in the present invention are a use of a combination of an anti-PD-L1 nanobody and a TLR7 small molecule agonist in anti-tumor treatment, and a PD-L1 and TLR7 double-targeting nanobody coupling drug, a preparation method therefor, and a use thereof. Specifically, disclosed in the present invention are a use and solution of a combination of an anti-PD-L1 nanobody and a derived protein thereof as well as a TLR7 small molecule agonist and a derived compound thereof in anti-tumor treatment. Meanwhile, disclosed in the present invention are design, preparation, and identification solutions for a novel PD-L1 and TLR7 double-targeting-nanobody drug conjugate and a derived molecule thereof, and an effect of the novel PD-Ll and TLR7 double-targeting nanobody drug conjugate in anti-tumor treatment. The PD-L1 and TLR7 double-targeting nanobody drug conjugate of the present invention can yield a significant antineoplastic efficacy in various transplantation tumor models.

The invention provides a multi-antigen loaded, active lymph node targeting and ultrasonic response senescence nano vaccine based on artificial vesicles as well as a preparation method and application of the senescence nano vaccine, and belongs to the technical field of vaccines. The invention relates to a modular two-component senescence nano vaccine based on click chemistry, which comprises DSPE-PEG-DBCO and azide functionalized senescence cell-derived artificial nano vesicles (N3-SCAVH / R) co-carrying a sound sensitive agent and a TLR7 / 8 receptor agonist, and the N3-SCAVH / R carries abundant SAAs. According to the vaccine, a DBCO target is pre-marked on a lymph node through subcutaneous injection of DSPE-PEG-DBCO, and N3-SCAVH / R which is continuously delivered can be anchored to the lymph node through a click chemical reaction; and then ultrasonically irradiating the lymph node to activate the sound-sensitive agent to assist the antigen in escaping from the endosome and enhance DC cross presentation. The nano vaccine can effectively remove plaque senescence cells and delay disease progression, and is good in safety.

This provides a combination of pharmaceuticals for treating hepatitis B virus infection. [Solution] A therapeutic oligonucleotide and formula (I) or (II): TIFF2026069791000108.tif48137 Alternatively, pharmaceutical combinations comprising or comprising a pharmaceutically acceptable salt, enantiomer, or diastereomer of TLR7 agonist thereof are provided.