173 results about "Btk inhibitors" patented technology

The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula I

or a pharmaceutically acceptable salt thereof or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of Btk inhibitor compounds in the treatment of Btk mediated disorders.

The invention relates to HDAC inhibitors, or combinations comprising an HDAC inhibitor and a BTK inhibitor for the treatment of non-hodgkin's lymphoma in a subject in need thereof. Also provided herein are methods for treating non-hodgkin's lymphoma in a subject in need thereof comprising administering to the subject a therapeutically effective amount of an HDAC inhibitor, or a combination comprising an HDAC inhibitor and a BTK inhibitor.

Provided are 6-5 membered fused pyridine ring compounds according to Formula (I) or pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising these compounds and their use in therapy. In particular, provided is the use of membered fused pyridine ring compounds in the treatment of Bruton's Tyrosine Kinase (Btk) mediated disorders.

The present invention is directed to the combination therapy of an anti-CD20 antibody with a BTK inhibitor for the treatment of cancer, especially to the combination therapy of CD20 expressing cancers with a type I anti-CD20 antibody or an afucosylated humanized B-Ly1 antibody and a BTK inhibitor.

The invention discloses a Bruton tyrosine kinase inhibitor with spiro or endo structure and a preparation method thereof. The inhibitor comprises Formula (I). The inhibitor has an obvious inhibiting action on BTK activity, and the inhibition activity for DOHH2 cells is enhanced by approximately 8 times. The spiro or endo compound can be used as a BTK inhibitor, and has wide application prospects in resisting malignant tumors.

The present invention relates to 6-5 membered fused pyridine ring compounds of formula (I) or a pharmaceutically acceptable salt thereof or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of 6-5 membered fused pyridine ring compounds in the treatment of Bruton's Tyrosine Kinase (Btk) mediated disorders.

Described herein are combination therapies for cancer (such as lymphoid malignancies) and immune diseases (such as autoimmune diseases and inflammatory diseases). The therapies comprise the combined use of inhibitors of BTK, mTOR kinase, and Bcl-2 or their signaling pathways, and immunomodulatory drugs. Also described are pharmaceutical compositions and kits comprising these inhibitors.

The invention belongs to the field of medical chemistry, relates to a novel pyridazinone BTK inhibitor as well as preparation and application thereof, in particular to a pyridazinone BTK inhibitor, apreparation method thereof, a pharmaceutical composition containing the same, and application thereof to treatment of Bruton's tyrosine kinase-related diseases.

The invention relates to the field of medicinal chemistry, relates to pyridazinone BTK inhibitors and an application thereof, and concretely relates to pyridazinone BTK inhibitors represented by formula (I), a preparation method thereof, a medicinal composition containing the compounds, and a use of the compounds or the medicinal composition in the treatment of Bruton's tyrosine kinase-related diseases.

In certain embodiments, the invention includes therapeutic methods of using a BTK inhibitor to treat solid tumor cancers by modulation of the tumor microenvironment, including macrophages, monocytes, mast cells, helper T cells, cytotoxic T cells, regulatory T cells, natural killer cells, myeloid-derived suppressor cells, regulatory B cells, neutrophils, dendritic cells, and fibroblasts.

The present invention provides a BTK inhibitor compound (having s structure represented by a formula (I)) and uses of the BTK inhibitor compound in medicines. According to the present invention, the compound and the pharmaceutical composition can be used for treatment of diffuse large B-cell lymphoma, follicular lymphoma or chronic lymphocytic leukemia. The formula (I) is defined in the specification.

The present application describes therapies for the effective treatment of colon and colorectal carcinomas. The present invention relates to a pharmaceutical kit, comprising combinations of a BTK inhibitor and fluorouracil, for the treatment of colon and colorectal carcinomas also in the case in which such carcinomas are drug resistant and therefore allows to overcome cancer drug resistance.

The present disclosure provides compounds of Formula (II)

as disclosed herein, and/or pharmaceutically acceptable salts thereof that are tyrosine kinase inhibitors, in particular BTK inhibitors, and are potentially useful for the treatment of diseases treatable by inhibition of tyrosine kinases such as cancer, inflammatory diseases such as arthritis, and the like. Also provided are pharmaceutical compositions containing such compounds and/or pharmaceutically acceptable salts thereof and processes for preparing such compounds and pharmaceutically acceptable salts thereof.

In some embodiments, the invention includes a therapeutic combination of a phosphoinositide 3-kinase (PI3K) inhibitor, including PI3K inhibitors selective for the γ- and δ-isoforms and selective for both γ- and δ-isoforms, and a Bruton's tyrosine kinase (BTK) inhibitor. In some embodiments, the invention includes therapeutic methods of using a BTK inhibitor and a PI3K-δ inhibitor to treat solid tumor cancers by modulation of the tumor microenvironment, including macrophages, monocytes, mast cells, helper T cells, cytotoxic T cells, regulatory T cells, natural killer cells, myeloid-derived suppressor cells, regulatory B cells, neutrophils, dendritic cells, and fibroblasts.

The present disclosure provides methods of treating with a BTK inhibitor a blistering disease, in particular pemphigus vulgaris or pemphigus folliaceous in a mammal, use of a BTK inhibitor as a replacement therapy for corticosteroid therapy for diseases treatable with a corticosteroid, such as autoimmune or inflammatory disease and in particular where corticosteroids are used as first or second line therapy, and pharmaceutical formulations comprising the same.

In certain embodiments, the invention includes therapeutic methods of using a BTK inhibitor to treat dermatoses, such as psoriasis, atopic dermatitis, contact dermatitis, scleroderma, and cutaneous lupus erythematosus. In other embodiments, the methods of the invention further comprise the step of administering a therapeutically effective dose of an anti-inflammatory agent.

Therapeutic methods of treating chronic lymphocytic leukemia (CLL) and small lymphocytic leukemia (SLL) are described. In certain embodiments, the invention includes therapeutic methods of treating CLL and SLL using a BTK inhibitor. In certain embodiments, the invention includes therapeutic methods of treating subtypes of CLL and SLL using a BTK inhibitor, including subtypes of CLL in patients sensitive to thrombosis and subtypes of CLL that increase monocytes and NK cells in peripheral blood after treatment with a BTK inhibitor. In certain embodiments, the invention includes therapeutic methods of treating CLL and SLL using a combination of a BTK inhibitor and an anti-CD20 antibody.

The invention relates to a crystal form of a bruton tyrosine kinase (BTK) inhibitor key intermediate and a preparation method of the crystal form, and belongs to the technical field of medicine. The crystal form is a (R)-1-(1-(tert-butyloxyl)pyrrolidine-3-yl)-3-cyano-4-(4-(2,6-difluorophenoxyl)phenyl)-1H-pyrrole-2-ethyl formate crystal form II. The obtained (R)-1-(1-(tert-butyloxyl)pyrrolidine-3-yl)-3-cyano-4-(4-(2,6-difluorophenoxyl)phenyl)-1H-pyrrole-2-ethyl formate crystal form II has good chemical stability and crystal form stability, storage and transportation are facilitated, meanwhile,the intermediate can be highly purified, a sample with the purity being 99.7% is obtained, and the crystal form has important significance to quality control over BTK inhibitor (R)-4-amino-1-(1-(butyl-2-alkynyl)pyrrolidine-3-yl)-3-(4-(2,6-difluorophenoxyl)phenyl)-1,6-dihydro-7H-pyrrolo[2,3-d]pyridazin-7-one, and is simple in preparation process and suitable for industrial scale production.