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176 results about "Btk inhibitors" patented technology

BTK inhibitor 1 (Compound 27) BTK inhibitor 1 (compound 27) is an inhibitor of BTK with an IC50 of 0.11 nM for Btk and inhibits B cell activation in hWB with an IC50 of 2 nM.

Btk inhibitors

The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula Ior 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.
Owner:MERCK SHARP & DOHME CORP

HDAC inhibitors, alone or in combination with btk inhibitors, for treating nonhodgkin's lymphoma

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.
Owner:MOFFITT CANCER CENT +1

Btk inhibitors

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.
Owner:MERCK SHARP & DOHME CORP +1

4-imidazopyridazin-1-yl-benzamides and 4-imidazotriazin-1-yl-benzamides as btk inhibitors

The present invention relates to 6-5 membered fused pyridine ring 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 6-5 membered fused pyridine ring compounds according to formula I in the treatment of Brutons Tyrosine Kinase (Btk) mediated disorders.
Owner:MERCK SHARP & DOHME BV

Combination therapy of an anti cd20 antibody with a btk inhibitor

InactiveUS20150125446A1Enhanced antiproliferative effectGood effectAntibody ingredientsImmunoglobulinsFucosylationOncology
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.
Owner:ONO PHARMA CO LTD +1

Bruton tyrosine kinase inhibitor with spiro or bridge ring structure and preparation method thereof

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.
Owner:CHENGDU BRILLIANT PHARMA CO LTD

4-imidazopyridazin-1-yl-benzamides and 4-imidazotriazin-1-yl-benzamides btk inhibitors

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.
Owner:MERCK SHARP & DOHME BV

Pharmaceutical compositions and their use for treatment of cancer and autoimmune diseases

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.
Owner:ZHEJIANG DTRM BIOPHARMA

Compounds containing conjugated allene structure, and pharmaceutical compositions and application thereof

The invention relates to compounds containing conjugated allene structure, and pharmaceutical compositions and application thereof, specifically to compounds as shown in a general formula (I) which are described in the specification or salts thereof, pharmaceutical compositions of the compounds, and application of the compounds as BTK inhibitors and / or B-cell activation inhibitors to prevention ortreatment of abnormal B-cell active activity or diseases related to BTK. The compounds have good lethal effect on cancer cells of lymphoma, breast cancer, liver cancer, intestinal cancer, stomach cancer, lung cancer, cervical cancer and the like, which proves that the compounds have potential of treating related cancers and autoimmune diseases.
Owner:SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI

Synthesis method of BTK inhibitor Acalabrutinib for treating chronic lymphocytic leukemia

A synthesis method of a BTK inhibitor Acalabrutinib for treating chronic lymphocytic leukemia comprises the steps as follows: preparing (S)-2-(8-aminoimidazo[1,5-a]pyrazine-3-yl)-1-pyrrolidinecarboxylic aci benzyl ester; preparing (S)-2-(8-tert-butoxycarbonylaminoimidazo[1,5-a]pyrazine-3-yl)-1-pyrrolidinecarboxylic acid benzyl ester; preparing (S)-2-(8-tert-butoxycarbonylamino-1-bromoimidazo[1,5-a]pyrazine-3-yl)-1-pyrrolidinecarboxylic acid benzyl ester; preparing (S)-2-(8-tert-butoxycarbonylamino-1-[4-(2-pyridylcarbamoyl)phenyl]imidazo[1,5-a]pyrazine-3-yl)-1-pyrrolidinecarboxylic acid benzyl ester; preparing (S)-2-(8-tert-butoxycarbonylamino-1-[4-(2-pyridylcarbamoyl)phenyl]imidazo[1,5-a]pyrazine-3-yl)pyrrolidine; preparing (S)-2-(8-tert-butoxycarbonylamino-1-[4-(2-pyridylcarbamoyl)phenyl]imidazo[1,5-a]pyrazine-3-yl)-1-(2-butynoyl)pyrrolidine; preparing Acalabrutinib. The yield is high, the process is simplified, and the synthesis method is green and environmentally friendly.
Owner:SUZHOU FUSHILAI PHARMA CO LTD +1

Novel pyridazinone BTK inhibitor as well as preparation and application thereof

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.
Owner:NANJING ADVANCED BIOLOGICAL MATERIALS & PROCESS EQUIP INST CO LTD

Pyridazinone BTK inhibitors and application thereof

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.
Owner:NANJING ADVANCED BIOLOGICAL MATERIALS & PROCESS EQUIP INST CO LTD

Polyfluorinated compounds acting as bruton tyrosine kinase inhibitors

Described herein is a novel series of multi-fluoro-substituted pyrazolopyrimidine compounds or salts thereof. These compounds are Bruton's tyrosine kinase (BTK) inhibitors. These compounds may possess better BTK inhibition selectivity and pharmacokinetic properties. Disclosed herein are the synthesis methods of these compounds. Disclosed herein are novel synthesis methods of the multi-fluoro-substituted benzophenone and substituted phenoxy benzene. Also disclosed are pharmaceutical compositions comprising the BTK inhibitors described herein. The present invention also relates to pharmaceutical formulations comprising the compounds described herein as active ingredients. The present invention also includes the therapeutic methods by administering the BTK inhibitors and their formulations to treat and inhibit autoimmune disease, hypersensitivity disease, inflammatory diseases and cancer.
Owner:ZHEJIANG DTRM BIOPHARMA

Btk inhibitors with improved dual selectivity

Disclosed herein is a tri-substituted phenyl Btk inhibitors with improved dual selectivity, a method and a composition for inhibiting Btk and treating disease associated with undesirable Btk activity (Btk-related diseases).
Owner:BEIGENE

Compound serving as protein kinase inhibitor and application of compound

The invention discloses a compound used as a protein kinase inhibitor and application of the compound, the compound has an obvious inhibition effect on protein kinase activity, can be used as a BTK inhibitor for preparing medicines for treating BTK-mediated diseases such as malignant tumors, autoimmune diseases and the like, and has wide application prospect.
Owner:CHENGDU HYPERWAY PHARM CO LTD

BTK Inhibitors to Treat Solid Tumors Through Modulation of the Tumor Microenvironment

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.
Owner:ACERTA PHARMA BV

Combinations of a btk inhibitor and fluorouracil for treating cancers

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.
Owner:BIONSIL

Substituted pyrazolo[3,4-d]pyrimidines as kinase inhibitors

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.
Owner:PRINCIPIA BIOPHARMA

Therapeutic Combination of PI3K Inhibitor and a BTK Inhibitor

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.
Owner:ACERTA PHARMA BV

Treatment of indolent or aggressive b-cell lymphomas using a combination comprising btk inhibitors

Disclosed herein is a method for the prevention, delay of progression or treatment of indolent or aggressive B-cell lymphomas in an individual in need thereof, comprising administering a Btk inhibitor (in particularly (S)-7-(1-actyloylpiperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetrahydropyrazolo-[1,5-a]pyrimidine-3-carboxamide or a pharmaceutically acceptable salt thereof) in combination with an anti-PD-1 antibody. The potent and selective BTK inhibitor in combination with the anti-PD-1 antibody have a manageable toxicity profile in patients with indolent and aggressive lymphomas.
Owner:BEIGENE SWITZERLAND GMBH

Bi-Specific Monovalent Diabodies That are Capable of Binding CD19 and CD3, and Uses Thereof

The present invention is directed to a combination therapy involving the administration of: (1) a bi-specific molecule capable of specifically binding to CD19 and to CD3 (i.e., a CD19×CD3 bi-specific molecule), and (2) a Bruton's Tyrosine Kinase (BTK) inhibitor for the treatment of disease, in particular treatment of a disease associated with or characterized by the expression of CD19. Preferably, such a CD19×CD3 bi-specific molecules are bi-specific monovalent diabodies. The invention is directed to pharmaceutical compositions that contain such a CD19×CD3 bi-specific molecule, a BTK inhibitor, or a combination of such agents. The invention is additionally directed to methods for the use of such pharmaceutical compositions in the treatment of disease, in particular, treatment of a cancer associated with or characterized by the expression of CD19.
Owner:MACROGENICS INC

Treatment of pemphigus

ActiveCN107257686ALong-term progress minimizedLittle long-term progressOrganic active ingredientsPeptide/protein ingredientsDiseaseSecond-line therapy
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.
Owner:PRINCIPIA BIOPHARMA

Methods of Using BTK Inhibitors to Treat Dermatoses

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.
Owner:ACERTA PHARMA BV

Methods of Treating Chronic Lymphocytic Leukemia and Small Lymphocytic Leukemia Using a BTK Inhibitor

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.
Owner:ACERTA PHARMA BV

Crystal form of bruton tyrosine kinase (BTK) inhibitor key intermediate and preparation method of crystal form

ActiveCN110372562AImprove stabilityMeet the requirements of production, transportation and storageOrganic chemistry methodsAntineoplastic agentsPyrrolidinePhenyl group
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.
Owner:SHANGHAI ZAIQI BIO TECH
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