242 results about "IRAK4" patented technology

The present disclosure relates generally to various salt forms and compositions thereof useful for the modulation of interleukin-1 receptor-associated kinase 4 ("IRAK4") via ubiquitination and / or degradation and uses of the same in the treatment various diseases.

The present invention provides compounds, compositions thereof, and methods of using the same to treat IRAK4-mediated disorder, disease, or condition in a patient.

The present disclosure relates generally to processes for preparing compounds that are inhibitors of the kinase IRAK4 and the synthetic intermediates prepared thereby.

The present invention relates to the technical field of chemical pharmacy, and in particular to a compound for degradation of a targeted interleukin-1 receptor-associated kinase 4 (IRAK4), and a pharmaceutically acceptable salt of the compound. The compound can be used for treating or preventing IRAK4-mediated immune diseases, inflammatory diseases, and cancers.

Disclosed are compounds of Formula (I) or a salt or prodrug thereof, wherein: X1 and X2 are independently C or N, provided that zero or one of X1 and X2 is N; Ring A represented by the structure is: or; and Q, R1, R2, R3, R4, R6, and p are define herein. Also disclosed are methods of using such compounds as modulators of IRAK4, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing inflammatory and autoimmune diseases, or in the treatment of cancer.

The present disclosure relates to methods of treating certain diseases and disorders (e.g., cancer) with a combination of an IRAK4 inhibitor, a BCL-2 inhibitor, and a nucleoside analog.

A nanoparticle for delivering an interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitor to a subject and methods for treating inflamed tissue in a subject using the nanoparticle.

Disclosed in the present invention are a five-membered ring-fused six-membered ring compound, a preparation method therefor, and a pharmaceutical composition and the use thereof. Provided in the present invention is a compound as represented by formula (I), or a pharmaceutically acceptable salt or an isotope compound thereof. The compound of the present invention has an inhibition and / or degradation effect on IRAK4.

Disclosed herein are novel bifunctional compounds formed by conjugating an IRAK4 inhibitor moiety to an E3 ligase ligand moiety, the function of these bifunctional compounds being to recruit a target protein to an E3 ubiquitin ligase for degradation, as well as methods of making and uses thereof.

The present disclosure provides bifunctional compounds as IRAK4 degraders via ubiquitin proteasome pathway, and method for treating diseases modulated by IRAK4.

The present application relates to a proteolysis targeting chimera compound represented by formula (A) for degrading IRAK4 and a preparation method therefor, a pharmaceutical composition comprising said compound, and a use of the pharmaceutical composition for treating diseases, disorders or conditions associated with the kinase protein IRAK4.

The present disclosure relates generally to processes for preparing compounds that are inhibitors of the kinase IRAK4 and the synthetic intermediates prepared thereby.

Disclosed in the present invention are a five-membered ring-fused six-membered compound, a preparation method therefor, and a pharmaceutical composition and the use thereof. Provided in the present invention is a compound as represented by formula (I), or a pharmaceutically acceptable salt or an isotope compound thereof. The compound of the present invention has an inhibition and / or degradation effect on IRAK4.

A five-membered-fused six-membered compound, a preparation method, a pharmaceutical composition, and the use. The penta-fused hexa-heterocyclic compound is a compound represented by formula (II) or (III). The compound has an inhibition or / and degradation effect on IRAK4.

Disclosed are compounds of Formula (I) or a salt or prodrug thereof, wherein: X is C or N; Y is C or N; Z is CR4 or N; provided that when: (i) X is N, then Y is C; and (ii) X is C, then Y is N and Z is N; and wherein R1, R2, R3, and R4 are define herein. Also disclosed are methods of using such compounds as modulators of IRAK4, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing inflammatory and autoimmune diseases, or in the treatment of cancer.

The invention provides a polysubstituted aromatic amine compound (as shown in a general formula I) as well as a preparation method, a pharmaceutical composition and application thereof, and particularly provides a compound with a structure as shown in the general formula I as well as an optical isomer, a medicinal salt or a mixture of the compound and the optical isomer. The compound has good IRAK4 inhibitory activity, so that the compound can be used for treating, preventing and relieving IRAK4 target related diseases, especially for treating autoimmune diseases such as arthritis, inflammatory bowel disease and the like, malignant tumors such as leukemia and the like or other related diseases.

The invention relates to an IRAK4 degradation agent and application thereof, in particular to a bifunctional compound shown in the following formula (I), an isomer, a deuterated substance or pharmaceutically acceptable salt of the bifunctional compound, and application of the compound in treating IRAK4-mediated related diseases. # imgabs0 #

The present invention discloses a 5-membered condensed 6-membered compound, a preparation method, a pharmaceutical composition, and an application. The 5-membered condensed 6-membered compound disclosed in the present invention is a compound represented by formula I, formula II, or formula III. The compound according to the present invention has an inhibitory effect on FLT3 and / or IRAK4. [Formula 1] TIFF2025501618000478.tif31170

Disclosed are compounds of Formula (I) or a salt or prodrug thereof, wherein R1, R2, and R3 are defined herein. Also disclosed are methods of using such compounds as modulators of IRAK4, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing inflammatory and autoimmune diseases, or in the treatment of cancer.

The invention discloses a compound synthesized based on a PROTAC technology and a synthesis method and application thereof.The compound is shown in the formula I. IRAK4 serves as a core of a MyD88 dependent signal channel, is an effective target for inhibiting a TLR / IL-R signal channel, can be used for treating various skin diseases including atopic dermatitis (AD) and has potential patent medicine prospects. # imgabs0 #

The present disclosure relates to salts and solid forms of a compound that are inhibitors of the kinase IRAK4 and their uses as therapeutic agents for treating diseases, disorders, or conditions modulated by IRAK4, such as inflammatory bowel disease (IBD), systemic lupus erythematosus (SLE), psoriasis, or rheumatoid arthritis.

The present disclosure provides bifunctional compounds as IRAK4 degraders via ubiquitin proteasome pathway, and method for treating diseases modulated by IRAK4.

Provided herein are methods of enhancing gene therapy in an individual by administering an IRAK modulator (e.g., an IRAK-4 degrading agent) with a gene therapy to inhibit innate immunity to the gene therapy. In some embodiments, the gene therapy uses an adeno-associated virus (AAV) vector, an adenoviral vector, a lentiviral vector, a herpes simplex virus (HSV) vector, or lipid nanoparticles. Also provided herein are methods for selecting an individual for treatment with an IRAK modulator in combination with a gene therapeutic agent.

The invention provides a preparation method of an IRAK4 targeted protein degradation agent key intermediate, and belongs to the field of drug synthesis. According to the invention, 2-pyrrolidone and a benzimidazolone compound are used as raw materials to prepare a key intermediate of the IRAK4 targeted protein degradation agent, a protecting group is introduced to 2-pyrrolidone, and a reaction route is optimized, so that generation of a by-product 3-bromo-1-(3-methyl-2-oxo-2, 3-dihydro-1H-benzo [D] imidazole-4-yl) piperidine-2, 6-diketone is avoided, and the yield of the IRAK4 targeted protein degradation agent is improved. The product yield is obviously improved, the product is easier to purify, and the method has a wide application prospect and is convenient for industrialization.