45 results about "IRAK4" patented technology

The present invention provides indazole compounds of formula (I), which are therapeutically useful as kinase inhibitors, particularly IRAK4 inhibitors, wherein Z1, Z2, R1, R2, R3, ‘m’ and ‘n’ have the meanings given in the specification, and pharmaceutically acceptable salts or stereoisomers thereof that are useful in the treatment and prevention of diseases or disorders, in particular their use in diseases or disorders mediated by kinase enzyme, particularly IRAK4 enzyme. The present invention also provides pharmaceutical compositions comprising at least one of the compounds of the compound of formula (I) together with a pharmaceutically acceptable carrier, diluent or excipient.

The present invention provides bicyclic heterocyclyl kinase enzyme inhibitor compounds of formula (I), which are therapeutically useful as kinase inhibitors, particularly IRAK4 inhibitors, wherein A, Y, Z, X1, X2, R1, R3, ‘m’, ‘n’ and ‘p’ have the meanings given in the specification and pharmaceutically acceptable salt or stereoisomer thereof that are useful in the treatment and prevention of diseases or disorder, in particular their use in diseases or disorder mediated by kinase enzyme, particularly IRAK4 enzyme. The present invention also provides pharmaceutical composition comprising at least one of the compounds of compound of formula (I) together with a pharmaceutically acceptable carrier, diluent or excipient therefor.

Compounds of the formula I or II:wherein X, m, Ar, R1 and R2 are as defined herein. The subject compounds are useful for treatment of IRAK-mediated conditions.

Disclosed are compounds of Formula (I) or salts thereof, wherein HET is a heteroaryl selected from pyrrolo[2,3 b]pyridinyl, pyrrolo[2,3 d]pyrimidinyl, pyrazolo[3,4 b]pyridinyl, pyrazolo[3,4 d]pyrimidinyl, imidazolo[4,5 b]pyridinyl, and imidazolo[4,5 d]pyrimidinyl, wherein said heteroaryl is attached to the pyridinyl group in the compound of Formula (I) by a nitrogen ring atom in said heteroaryl and wherein said heteroaryl is substituted with zero to 2 Rb; A is pyrazolyl, imidazolyl, triazolyl, isoxazolyl, oxadiazolyl or dihydroisoxazolyl, each substituted with zero or 1 Ra; and R3, Ra, and Rbare 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.

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.

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.

The present invention provides methods for treating hematological disorders, such as acute myeloid leukemia, by the use of substituted heterocyclic compounds and pharmaceutically acceptable salts thereof. The compounds inhibit IRAK4 and FLT-3 kinases.

The present invention relates to a pharmaceutical composition for preventing or treating autoimmune diseases or tumors, containing, as an active ingredient, a tricyclic compound represented by the following formula 1 or a pharmaceutically acceptable salt thereof, and a health food composition for preventing or alleviating autoimmune diseases or tumors, containing the tricyclic compound as an active ingredient. [Chemical formula 1] A tricyclic compound represented by chemical formula 1 of the present invention has an excellent inhibitory activity against IRAK4, and thus can be effectively used in the prevention, treatment, or alleviation of autoimmune diseases or tumors.

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

Therapeutic combinations of an interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitor and a Bruton's tyrosine kinase (BTK) inhibitor are described. In some embodiments, the invention provides pharmaceutical compositions comprising combinations of an IRAK4 inhibitor and a BTK inhibitor, and methods of using the pharmaceutical compositions for treating a disease, in particular a cancer.

The present application relates to a novel combination product of at least two components (component A and component B) for the treatment and / or prevention of diseases: component A is an IRAK4 inhibitory compound of formula (I) as defined herein, or a diastereomer, enantiomer, metabolite, salt, solvate or solvate of a salt thereof; component B is a BTK inhibitory compound, or a pharmaceutically acceptable salt thereof; and, optionally One or more components C which are pharmaceutical products; wherein one or both of compounds A and B as defined above are optionally present in a pharmaceutical preparation intended for simultaneous, separate or sequential administration, And to its use for the manufacture of a medicament for the treatment and / or prevention of diseases, in particular for the treatment and / or prevention of endometriosis, lymphoma, macular degeneration, COPD, neoplastic disorders and psoriasis.

Therapeutic uses P2X7 inhibition and inhibition of IRAK1 and / or IRAK4, methods protecting a cell, and screening methods for identifying inhibitors are described herein.

Described herein are compounds of formula (0), formula (I) and formula (II) and methods of use as interleukin-1 receptor-associated kinase (IRAK4) inhibitors.