216 results about "Inflammasome" patented technology

The invention relates to a probiotic preparation for improving Parkinson's disease and an application of the probiotic preparation. The bacterial strains in the probiotic preparation comprise an Ackermania muciniphila Akk11 bacterial strain and a Bifidobacterium breve BBr60 bacterial strain. The invention further relates to a preparation method of the probiotic preparation for improving the Parkinson's disease and an application of the probiotic preparation for improving the Parkinson's disease, wherein the bacterial strains in the probiotic preparation comprise the Ackermania muciniphila Akk11 bacterial strain and the Bifidobacterium breve BBr60 bacterial strain. The invention develops a brand-new probiotic compounding mode and a brand-new probiotic intervention strategy for improving the Parkinson's disease, that is, the Akk11 strain and the BBr60 strain are compounded, and the two strains are found to have potential interaction and can be matched with each other, so that a synergistic effect is achieved on the aspect of improving the Parkinson's disease, and the effect of improving the Parkinson's disease is achieved. Specifically, the traditional Chinese medicine composition synergistically improves dyskinesia caused by Parkinson's disease, reduces expression of related inflammatory factors in nigra, promotes generation of anti-inflammatory factors to relieve neurological inflammation, inhibits activation of inflammasome NLPR3 in nigra, and further inhibits brain inflammation.

The present invention relates to a compound of formula (I) wherein R1 is a hydrogen atom, halogen or -(C1-C2)alkyl, R2 is -halo(C1-C2)alkoxy, and R3 and R4 form together with N to which they are attached an optionally substituted 5-7 membered monocyclic heterocycloalkyl ring or an optionally substituted 8-11 membered bicyclic heterocycloalkyl ring. The present invention also relates to a medicament and a pharmaceutical composition comprising said compound of formula (I), as well as their therapeutic uses, in particular as inhibitor of NOD-like receptor protein 3 inflammasome for preventing and / or treating Parkinson's disease, frontotemporal Dementia, Multiple System Atrophy, Alzheimer's disease, Multiple Sclerosis, Amyotrophic Lateral Sclerosis or brain injury.

This specification generally relates to compounds of formula (I), formula (II), and formula (VI), and pharmaceutically acceptable salts thereof. Such compounds are useful for inhibiting NLRP3 inflammasome activity and may be useful as therapeutic agents. This specification also relates to the use of such compounds for treating or preventing diseases and conditions involving the NLRP3 inflammasome. This specification further relates to compositions comprising such compounds. (Formula (I), Formula (II), Formula (VI)) [Formula 1] JPEG2026503239000288.jpg82128

The invention discloses an NLRP3 inhibitor as well as a preparation method and application thereof. Specifically, the invention relates to a compound shown as a formula (NLRP3i-3) or a pharmaceutically acceptable salt thereof, the formula (I) is COCCNc1nc2c (c (= O) n (C) c (= O) n2C) n1Cc1cc (OC) ccc1N, and the chemical name is 8-((4-amino-2-methoxybenzyl)-7, 9-dimethyl-7, 9-dihydro-8H-purine-6, 8-diketone. The invention also provides a preparation method of the compound, a pharmaceutical composition containing the compound, and application of the compound in preparation of drugs for preventing and / or treating NLRP3-mediated diseases. The disease is preferably myocardial ischemia reperfusion injury. Experimental results show that the compound provided by the invention has excellent NLRP3 inhibitory activity (IC50lt, 100nM), and has high selectivity to NLRP3 inflammasomes; good pharmacokinetic characteristics are achieved in a rat body, and the bioavailability is high; in myocardial ischemia reperfusion injury models of mice and rats, the composition can significantly reduce myocardial infarction area, reduce myocardial enzyme level, alleviate inflammatory response and improve heart function; preliminary toxicological evaluation shows that the safety is good. Therefore, the compound disclosed by the invention is expected to be developed into a novel medicine for treating NLRP3 related diseases such as myocardial ischemia-reperfusion injury.

Disclosed herein are methods, compounds, and compositions for treating or preventing an inflammasome-mediated disease or condition, including an inflammasome-mediated pulmonary disease or condition.

To provide methods for detecting inflammasome proteins as biomarkers of neurological disorders.SOLUTION: The present invention provides compositions and methods for detecting components of the inflammasome in a sample from a subject as markers for brain injuries such as multiple sclerosis, stroke or traumatic brain injury. Methods of using such inflammasome markers to determine prognosis, direct treatment and monitor response to treatment for the subject with a brain injury such as multiple sclerosis, stroke, mild cognitive impairment or traumatic brain injury are also described. Presented herein are inflammasome components useful as biomarkers with high sensitivity and specificity for various neurological or psychiatric conditions and methods of their use.SELECTED DRAWING: None

The invention provides medical application of a licochalcone B derivative CTG12 in preparation of an NLRP3 inflammasome inhibitor, and belongs to the technical field of biological medicine. The invention provides application of a licochalcone B derivative CTG12 in preparation of an NLRP3 inflammasome inhibitor. The invention also discloses application of the compound in preparation of drugs for preventing or treating diseases related to abnormal activation of NLRP3 inflammasomes. The synthesized compound CTG12 has the remarkable activity of inhibiting caspase-1 generated by BMDM cells, the effect is improved by about eight times compared with licochalcone B, and the compound CTG12 has the broad-spectrum and specific inhibiting effect and can effectively inhibit activation of NLRP3 inflammasomes.

This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt thereof) that degrade and / or otherwise modulate (e.g., inhibit) NIMA Related Kinase 7 (NEK7). Said chemical entities are useful, e.g., for treating a subject (e.g., a human subject) having one or more disorders or diseases associated with NLRP3 inflammasome activation. Said disorders or diseases include but are not limited to, autoinflammatory and autoimmune disorders (e.g., gout, inflammatory bowel disease, rheumatoid arthritis, multiple sclerosis), neurodegenerative diseases (e.g., Alzheimer's disease, Parkinson's disease), cardiovascular and metabolic disorders (eg. pericarditis, atherosclerosis, Type 2 diabetes, obesity, and metabolic syndrome), fibrotic disorders (e.g. interstitial lung disease, chronic kidney disease), hematology (eg, anemia of inflammation) and eye disorders (eg. macular degeneration). In embodiments, and while not wishing to be bound by theory, it is believed that the chemical entities described herein directly target (e.g., directly bind to) NEK7, thereby altering (e.g., attenuating) the inflammatory response modulated by the NLRP3 inflammasome. This disclosure also features compositions containing the same as well as methods of using and making the same.

Compounds useful as inhibitors of the NLRP3 inflammasome pathway are provided wherein such compounds are as defined by a compound of formula (I) and wherein the radicals R1, R2, R3, R4, L and A are defined in the description, and wherein the compounds are useful as medicaments, for example, for use in the treatment of diseases or conditions associated with NLRP3 inflammasome activity.

The invention belongs to the technical field of gene editing and disease model construction, and particularly relates to a construction method and application of a Wilson disease animal model. Aiming at a large fragment deletion mutation type which exists clinically in Wilson disease but lacks a corresponding animal model, a CRISPR / Cas9 gene editing technology is utilized, a pair of sgRNAs is specifically designed, an eighth exon region of a mouse Atp7b gene is precisely cut and deleted, and a WD mouse model with deletion mutation (c.2333340delGACGGTGG) of eight basic groups of the eighth exon of the Atp7b gene is successfully constructed. The method can be used for research on pathogenesis of WD, screening of novel diagnostic markers and evaluation of curative effect of therapeutic drugs, is particularly suitable for preclinical evaluation of gene therapy strategies and development of adjuvant therapeutic drugs of targeted NLRP3 inflammasomes, and has great scientific research value and clinical transformation prospect.

The present invention relates to novel compounds of formula (I): wherein each of ring A, R1, R2, X, Y and Z is as defined herein, which inhibit NOD-like receptor protein 3 (NLRP3) inflammasome activity. The invention also relates to a preparation method of the compound, a pharmaceutical composition and a medicament containing the compound, and application of the compound and the pharmaceutical composition and the medicament in treatment of NLRP3 mediated diseases and symptoms.

The invention relates to an NEK7 inhibitor, a pharmaceutical composition and application of the NEK7 inhibitor. The NEK7 inhibitor has a structural formula as shown in a formula (I). The compound disclosed by the invention has good NEK7 inhibitory activity, and can be used for treating or preventing a plurality of inflammatory pathological diseases (Alzheimer's disease, Parkinson's disease, amyotrophic lateral sclerosis, multiple sclerosis, atopic dermatitis, ulcerative colitis, Crohn's disease, cancer, osteoarthritis, gout and the like) regulated by NLRP3 inflammasome.

The present disclosure relates to compounds that act as inhibitors of the NLRP3 inflammasome, pharmaceutical compositions containing the compounds, and methods for treating inflammation and inflammation-aging-related disorders, including neurosensory disorders and other diseases associated with aging.

This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt thereof) that degrade and / or otherwise modulate (e.g., inhibit) NIMA Related Kinase 7 (NEK7). Said chemical entities are useful, e.g., for treating a subject (e.g., a human subject) having one or more disorders or diseases associated with NLRP3 inflammasome activation. Said disorders or diseases include but are not limited to, autoinflammatory and autoimmune disorders (e.g., gout, inflammatory bowel disease, rheumatoid arthritis, multiple sclerosis), neurodegenerative diseases (e.g., Alzheimer's disease, Parkinson's disease), cardiovascular and metabolic disorders (eg. pericarditis, atherosclerosis, Type 2 diabetes, obesity, and metabolic syndrome), fibrotic disorders (e.g. interstitial lung disease, chronic kidney disease), hematology (eg. anemia of inflammation) and eye disorders (eg. macular degeneration). In embodiments, and while not wishing to be bound by theory, it is believed that the chemical entities described herein directly target (e.g., directly bind to) NEK7, thereby altering (e.g., attenuating) the inflammatory response modulated by the NLRP3 inflammasome. This disclosure also features compositions containing the same as well as methods of using and making the same.

The present invention provides novel markers of the severity of a central nervous system injury, such as spinal cord injury or traumatic brain injury, in a patient. In particular, protein components of inflammasomes in the cerebrospinal fluid that can be used to assess the severity of central nervous system injury in a patient are disclosed. Methods of using such protein biomarkers to determine a prognosis, direct treatment and rehabilitation efforts, and monitor response to treatment for a patient with a central nervous system injury are also described.

The present disclosure relates to compounds of Formula (I):and to their pharmaceutically acceptable salts, pharmaceutical compositions, methods of use, and methods for their preparation. The compounds disclosed herein are useful for inhibiting the maturation of cytokines of the IL-1 family by inhibiting inflammasomes and may be used in the treatment of disorders in which inflammasome activity is implicated, such as inflammatory, autoinflammatory and autoimmune diseases and cancers.

Described herein are methods of treating a hematological malignancy, including minimal residual disease in hematological malignancies, and methods of preventing relapse of hematological malignancies, the methods comprising administering an inflammasome modulator. In some embodiments the method of treatment comprises administering a compound of formula (I) or a pharmaceutically acceptable salt or solvate thereof, wherein the variables are as defined herein.

The present invention relates to methods, compositions, and combinations for inhibiting the NLRP3 inflammasome and / or LON protease as well as methods, compositions, and combinations for treating cancer, particularly blood cancer or brain cancer. In certain aspects, the compositions and combinations include a synthetic triterpenoid, such as 1-[2-Cyano-3,12-dioxooleana-1,9(11)-dien-28-oyl]-4(-pyridin-2-yl)-1H-imidazole (“CDDO-2P-Im”) and 1-[2-Cyano-3,12-dioxooleana-1,9(11)-dien-28-oyl]-4(-pyridin-3-yl)-1H-imidazole (“CDDO-3P-Im”).

The invention relates to the technical field of medicines, in particular to application of AV-412. The invention relates to an application of AV-412 in preparation of an NLRP3 inflammasome inhibitor. The invention discloses application of AV-412 in preparation of a medicine for treating infectious shock. The invention discloses application of AV-412 in preparation of a medicine for treating acute liver injury. The invention discloses application of AV-412 in preparation of a medicine for treating acute peritonitis. The invention provides a new choice for medicines for preventing or treating NLRP3 inflammasome related diseases, and also provides a new medicine with treatment potential for infectious shock, acute liver injury and acute peritonitis.

Compounds for use as inhibitors of the NLRP3 inflammasome pathway are provided, such compounds being as defined by the compounds of formula (I) and containing a group R 1 , R 2 , R 3 , R 4 , and R 5 is defined herein, and the compounds may be useful, for example, as pharmaceutical agents for use in the treatment of diseases or disorders associated with NLRP3 inflammasome activity. [Formula 1] TIFF2026504424000139.tif33128

The invention relates to the technical field of medicines, in particular to application of garcinia cambogia ketone C. The invention relates to an application of gamboge C in preparation of an NLRP3 inflammasome inhibitor. The invention relates to an application of garcinia cambogia ketone C in preparation of a medicine for treating infectious shock. The invention relates to an application of garcinia flavone C in preparation of a medicine for treating acute liver injury. The invention relates to an application of garcinia flavone C in preparation of a medicine for treating acute peritonitis. The invention provides a new choice for medicines for preventing or treating NLRP3 inflammasome related diseases, and also provides a new medicine with treatment potential for infectious shock, acute liver injury and acute peritonitis.

The present disclosure relates to compounds that act as inhibitors of NLRP3 inflammasomes; pharmaceutical compositions comprising the compounds; and methods of treating cancer and disorders associated with inflammation and inflammaging.

The inventions relate to compounds and compositions comprising connexin hemichannel modulators, inflammasome modulators, and / or pannexin channel modulators and methods for the treatment of post-acute infection disorders, including long COVID, long flu, and post-treatment Lyme disease syndrome.

The present disclosure relates to compounds that act as inhibitors of NLRP3 inflammasomes; pharmaceutical compositions comprising the compounds; and methods of treating disorders associated with inflammation and inflammaging, including hearing loss and other diseases associated with aging; wherein the inhibitors of NLRP3 inflammasomes are compounds of Formula VII:or a pharmaceutically acceptable salt thereof.

The invention discloses a 1, 10-split ring type guaiane sesquiterpene lactone quasi-natural product as well as a preparation method and application of the 1, 10-split ring type guaiane sesquiterpene lactone quasi-natural product. The quasi-natural product and the derivative thereof are prepared by taking (R)-Carvone as a raw material through a chemical synthesis method. Experiments show that the 1, 10-split ring type guaiane sesquiterpene lactone compound prepared by the invention has the effect of inhibiting red blood cell hemolysis, can be used as a candidate drug molecule for preventing and / or treating NLRP3 inflammasome related diseases, and has the potential of being developed into related anti-inflammatory drugs.

The invention belongs to the technical field of medicines, and relates to an NLRP3 inflammasome inhibitor and application thereof. Specifically, the invention relates to a compound represented by a general formula (I), or a deuterated compound thereof, or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, and the definition of each group is as defined in the specification. Researches show that the compound represented by the general formula (I), or a deuterated compound thereof, or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof has high biological activity on NLRP3 inflammasomes, and has important clinical development value Y-W-R3 (I) for treating NLRP3 related diseases.

Described herein are NOD-like receptor protein 3 (NLRP3) inflammasome inhibitors and pharmaceutical compositions comprising the inhibitors. The subject compounds and compositions are useful for the treatment of diseases or disorders associated with the NLRP3 inflammasome pathway.

The present invention relates to the production of a polyketide compound with NLRP3 inflammasome inhibitory activity using the Antarctic fungus Pseudogymnoascus sp. HDN17-895 (Deposit Number: CCTCC M20211640), and also relates to the use of such a compound in preventing or treating NLRP3 inflammasome-related diseases. The structural formula is: #imgabs0#. The fermentation product containing such a compound can be obtained by fermenting and culturing the fungus Pseudogymnoascus sp. HDN17-895, and then separated and purified by methods such as normal phase silica gel column chromatography, Sephadex LH20 gel column chromatography, medium pressure MPLC, and semi-preparative HPLC. The present invention aims to provide a novel polyketide compound with NLRP3 inflammasome inhibitory activity from a secondary metabolite derived from the fungus, as well as a preparation method and use thereof.

The present disclosure relates to methods of preparing 2-methylpyrimidine salt from 4,6-dichloro-2-methylpyrimidine. The present disclosure also relates to compounds being prepared by the methods, the pharmaceutical compositions comprising the compounds, and the use thereof, e.g., in the treatment of disorders (e.g., in which inflammasome activity is implicated).