45 results about "IRAK4" patented technology

Compounds within the scope of the present invention have a Formula 1

or a salt or prodrug thereof, where ring A is selected from cycloaliphatic; ring B is aryl; R¹ is selected from (C1-C10)alkyl, (C3-C10)cycloalkyl, halo, aryl, and heteroaryl; and R² and R³ are independently selected from hydrogen and (C1-C6)alkyl. Disclosed compounds may have an IRAK4 IC₅₀ of from 0.003 μM to 3.7 μM; a TAK1 IC₅₀ of from 0.008 μM to 132 μM; and/or an IRAK4/TAK1 selectivity of from 1 to 450. Particular compounds may have an IRAK4/TAK1 selectivity of from 100 to 500. Disclosed compositions may be formulated as pharmaceutical compositions. A method for using the compounds and/or compositions also are disclosed. The method may comprise administering to a subject an effective amount of a compound within the scope of the present invention, particularly to selectively inhibit IRAK 1 and/or IRAK4 over TAK1.

The present invention relates to antibodies that bind phosphorylated forms of IRAK4, methods of using such antibodies to detect IRAK4 biological activity, and methods for the detection, diagnosis, and prognostication of pathological conditions related to IRAK4 biological activity. ERAK4 is one member of a small family of highly conserved cytoplasmic signal transduction proteins characterized by the presence of an N-terminal “death domain” and a C-terminal serine-threonine kinase domain. IRAK4 functions in cytoplasmic signal transduction pathways by interacting with membrane spanning proteins which play, inter alia, critical roles in vertebrate immune system function.

The present application relates to novel combinations of at least two components, component A and component B: component A is an IRAK4-inhibiting compound of the formula (I) as defined herein, or a diastereomer, an enantiomer, a metabolite, a salt, a solvate or a solvate of a salt thereof; component B is a BTK-inhibiting compound, or a pharmaceutically acceptable salt thereof; and, optionally, oneor more components C which are pharmaceutical products; in which one or two of the above-defined compounds A and B are optionally present in pharmaceutical formulations ready for simultaneous, separate or sequential administration, for treatment and/or prophylaxis of diseases, and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially for treatment and/or prophylaxis of endometriosis, lymphoma, macular degeneration, COPD, neoplastic disorders and psoriasis.

The invention relates to an imidazopyridine derivative represented by a general formula (I) or a pharmaceutically acceptable salt thereof, and a preparation method thereof, uses of the imidazopyridinederivative or the pharmaceutically acceptable salt thereof as treatment agents, especially as IRAK4 kinase inhibitors. According to the invention, R1, R2, R3 and R4 in the general formula (I) are defined in the specification.

Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula Ia, as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

Compounds, tautomers and pharmaceutically acceptable salts of the compounds of Formula (Ia) are disclosed which are inhibitors of Interleukin-1 receptor associated kinase (IRAK4). Methods of treatment, methods of synthesis, and intermediates are also disclosed as defined in the specification.

Disclosed are compounds of Formula (I) or salts thereof, wherein: HET is a heteroaryl selected from pyrazolyl, indolyl, pyrrolo[2,3-b]pyridinyl, pyrrolo[2,3-d]pyrimidinyl, pyrazolo[3,4-b]pyridinyl, pyrazolo[3,4-d]pyrimidinyl, 2,3-dihydro-1H-pyrrolo[2,3-b]pyridinyl, imidazo[4,5-b] pyridinyl, and purinyl, wherein said heteroaryl is substituted with Ra and Rb; and R1 and R2 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.

Disclosed are compounds of Formula (I) or salts thereof, wherein: HET is a heteroaryl selected from imidazo[1,2-b]pyridazinyl and pyrazolo[1,5-a]pyrimidinyl, wherein said heteroaryl is attached to thepyridinyl group in the compound of Formula (I) by a carbon ring atom in the heteroaryl and wherein said heteroaryl is substituted with zero to 2 Rb; A is pyrazolyl, imidazolyl, or triazolyl, each substituted with zero or 1 Ra; and R3, Ra, and Rb 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 invention provides a compound represented by a general formula I, and a pharmaceutically acceptable salt, a stereoisomer, an ester, a prodrug, a solvate and a deuterated compound thereof,and the compound is an IRAK4 kinase inhibitor, and can be used for prevention and/or treatment of IRAK4 related diseases, such as autoimmune diseases, inflammatory diseases, cancers, heteroimmune diseases, thromboembolism, atherosclerosis, myocardial infarction and metabolic syndrome.

The invention provides a compound with a general formula I, and pharmaceutically acceptable salts, stereoisomers, esters, prodrugs, solvates and deuterated compounds thereof, the compound is an IRAK4 kinase inhibitor, and can be used for preventing and/or treating IRAK4 related diseases. Such as autoimmune diseases, inflammatory diseases, cancers, heteroimmune diseases, thromboembolism, atherosclerosis, myocardial infarction and metabolic syndrome.

Compounds of Formula 0, and stereoisomers and pharmaceutically acceptable salts thereof, as well as methods of use as Interleukin-1 Receptor Associated Kinase (IRAK4) inhibitors are described herein.

The invention relates to the technical field of biological medicine, in particular to a sulfinyl imide substituted indazole compound, or an isomer and pharmaceutically acceptable salt thereof, and the structure of the sulfinyl imide substituted indazole compound is shown as a formula I. Compared with the prior art, the novel aryl(hetero) sulfoximide substituted indazole compound and the pharmaceutically acceptable salt thereof provided by the invention have better IRAK4 inhibitory activity and better safety, and the preferable compound disclosed by the invention shows good pharmacokinetic properties and has the potential of being developed into a selective IRAK4 inhibitor.

The invention provides an IRAK4 kinase inhibitor as well as preparation and application thereof, and particularly provides a compound shown as a formula (I) in the specification, a stereoisomer, a geometrical isomer, a tautomer, pharmaceutically acceptable salt, a prodrug, a hydrate or a solvate of the compound, and a preparation method and application of the compound. Compared with an IRAK4 inhibitor in the prior art, the compound of the invention has the advantage that the activity of the compound is obviously improved, so the compound can be used for preparing drugs used for preventing and/or treating IRAK4-mediated related diseases such as cancer, inflammatory diseases and autoimmune diseases.

The invention belongs to the field of medicines, and particularly relates to a novel application of an IRAK4 small-molecule inhibitor in preparation of medicines for treating or preventing acute lung injury or acute respiratory distress syndrome and related diseases thereof. Experiments prove that the IRAK4 small-molecule inhibitor can obviously reduce the generation of inflammatory factors and prevent infiltration of eosinophilic granulocytes, neutrophil granulocytes and lymphocytes, has good prevention and treatment effects on LPS-induced acute lung injury or acute respiratory distress syndrome, and can be used for preparing medicines for preventing and treating acute lung injury or acute respiratory distress syndrome. The IRAK4 inhibitor is expected to become a new generation of medicine for treating acute lung injury and acute respiratory distress syndrome.

A compound of Formula (I), pharmaceutically acceptable salts thereof, deuterated analogs thereof, compositions thereof, and methods of treating disease by using a compound thereof are disclosed.

Compounds of Formula I and methods of use as Interleukin-1 Receptor Associated Kinase 4 (IRAK4) inhibitors are described herein.

A compound related to inhibiting IRAK4 kinase activity, pharmaceutical composition thereof, use thereof in pharmacy, method for inhibiting IRAK4 kinase activity thereof and use thereof to treat and/or prevent IRAK4 kinase-mediated method of disease or disease. The compound has the structural formula I.

Provided are a class of multi-targeted inhibitors of IRAK4 and BTK, and the use thereof in preparing a drug for treating IRAK4- and BTK-related diseases. The present invention specifically relates to the compounds represented by formula (II), isomers thereof or pharmaceutically acceptable salts thereof.