126 results about "Btk inhibitors" patented technology

Disclosed are a pyrrolopyrimidine compound and a use thereof in preparing a medicine for diseases related to a BTK protein kinase inhibitor. Specially, disclosed are a compound as shown in formula (III) and a pharmaceutically acceptable salt thereof.

Described herein are pharmaceutical formulations of Bruton's tyrosine kinase (Btk) inhibitor 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo [3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one. Also disclosed are methods of using the Btk inhibitor, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.

Methods related to inhibiting CLEC-2 and treating venous thrombosis with certain BTK inhibitors and / or pharmaceutically acceptable salts thereof are provided.

Provided herein are BTK inhibitors containing piperidine modified at the 3-position. Further disclosed are methods of making and using said BTK inhibitors.

The invention relates to a polycyclic compound, a preparation method thereof and application of the polycyclic compound in medicine. Specifically, the invention relates to a polycyclic compound as shown in a general formula (I), a preparation method of the polycyclic compound, a pharmaceutical composition containing the polycyclic compound and application of the polycyclic compound as a therapeutic agent, especially application of the polycyclic compound as a BTK inhibitor or degradation agent and application of the polycyclic compound in preparation of drugs for treating and / or preventing BTK-mediated or dependent diseases or symptoms. Wherein each group in the general formula (I) is defined in the specification.

Methods for treating Sickle Cell Disease (SCD) comprising administering a BTKi, such as at least one compound chosen from (R)-2-[3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile (rilzabrutinib) and pharmaceutically acceptable salts thereof, are disclosed.

The present application relates to a heteroaryl compound, a preparation method therefor, and the pharmaceutical use thereof. Specifically, the present application relates to a heteroaryl compound as shown in general formula (I), a preparation method therefor, a pharmaceutical composition containing the heteroaryl compound, the use thereof as a therapeutic agent, particularly as a BTK inhibitor or degrader, and the use thereof in the preparation of a drug for treating and / or preventing BTK-mediated or dependent diseases or conditions. Each group in general formula (I) is as defined in the description.

The application relates to a preparation method of a BTK inhibitor intermediate. In particular, the application relates to a preparation method of a compound as shown in formula (A'K), which comprises the following steps: a step of preparing a compound as shown in formula (IIK) from a compound as shown in formula (IIIK), and a step of preparing a compound as shown in formula (A'K) from a compound as shown in formula (IIK). The method has high yield and mild reaction conditions, and is suitable for industrial production.

The invention belongs to the technical field of biological medicine, and particularly relates to a pharmaceutical composition of an HDAC6 inhibitor and a BTK inhibitor and application of the pharmaceutical composition. According to the present invention, the BTK inhibitor and the HDAC6 inhibitor are combined for use to provide the synergistic effect, such that the tumor inhibition effect is significantly enhanced, the medication dosage and the medication period can be improved, the side effect of the drug can be easily reduced, and the compliance of the patient on the drug can be easily improved.

The present disclosure provides methods of treating multiple sclerosis (MS) using Compound 1 represented by the following structure, or a pharmaceutically acceptable salt thereof, in combination with dihydroxymethyl fumarate (DRF).

This disclosure relates to pharmaceutical combinations for treating and / or preventing cancer and methods and uses thereof. More particularly, provided are pharmaceutical combination comprising a PRMT5 Inhibitor and a cellular activity modulator selected from an EGFR inhibitor, a KRAS inhibitor, a KRAS-G12C inhibitor, a MEK inhibitor, a Bcl-2 inhibitor, a SOS1 inhibitor, a PARP inhibitor, a RAF inhibitor, a ERK inhibitor, a CDK4 / 6 inhibitor, a MALT1 inhibitor, a BTK inhibitor, MAT2A inhibitor, a PI3K inhibitor, a AKT inhibitor, a FGFR inhibitor, a Type I PRMT inhibitor, a STING agonist, or an immune checkpoint inhibitor / modulator.

The invention relates to the technical field of pharmaceutical preparations, in particular to a BTK inhibitor solid tablet and a preparation method thereof.The BTK inhibitor solid tablet is prepared from, by weight, 4.5-5.5% of a compound shown in the formula I, 80-90% of filler, 1-5% of adhesive, 3-10% of disintegrating agent and 0.1-5% of lubricant, and the particle size of the compound shown in the formula I is D90lt; the dissolution rate of the solid tablet of the compound shown in the formula I in a medium with the pH value of 1.0 for 15 min is larger than 85%, the dissolution rate after acceleration is not remarkably changed, and the preparation is simple in process, capable of guaranteeing the stability, convenient to transport and store and suitable for large-scale production.

To provide: compounds inhibiting ErbBs (e.g., EGFR or Her 2), especially mutant forms of ErbBs, and BTK; pharmaceutically acceptable salts, hydrates, solvates or stereoisomers thereof; and pharmaceutical compositions comprising the compounds.SOLUTION: The invention provides compounds represented by the formula (I), pharmaceutically acceptable salts, esters, hydrates, solvates or stereoisomers thereof.SELECTED DRAWING: None

The present disclosure provides methods of treating multiple sclerosis (MS) using Compound 1 represented by the following structure or a pharmaceutically acceptable salt thereof.

The invention discloses application of a BTK inhibitor in preparation of a medicine for treating acute kidney injury and complications thereof. The invention provides a new strategy for treating acute kidney injury and complications thereof by using a BTK inhibitor, and particularly relates to application of the BTK inhibitor as an acute kidney injury medicine. The invention finds that serum creatinine and urea nitrogen levels can be effectively reduced by knocking out mouse BTK, and kidney injury is relieved and conversion from AKI to CKD is delayed or prevented by recovering kidney pathological structure and reducing apoptotic cell generation, which indicates that BTK is an effective target for treating acute kidney injury. Meanwhile, through treatment of an acute renal ischemia-reperfusion model, it is found that the BTK inhibitor such as ibrutinib can relieve ischemia-reperfusion induced renal function impairment and improve the renal function of a mouse, and it is indicated that the BTK inhibitor can serve as a treatment scheme for acute renal injury.

The present invention relates to efficient synthetic processes useful in the preparation of Compound A, a BTK inhibitor of Formula (I): or a pharmaceutically acceptable salt thereof, including the preparation of intermediates used to make Compound A or a pharmaceutically acceptable salt thereof.

The invention relates to a polycyclic compound, a preparation method thereof and application of the polycyclic compound in medicine. Specifically, the invention relates to a polycyclic compound as shown in a general formula (I), a preparation method of the polycyclic compound, a pharmaceutical composition containing the polycyclic compound and application of the polycyclic compound as a therapeutic agent, especially application of the polycyclic compound as a BTK inhibitor or degradation agent and application of the polycyclic compound in preparation of drugs for treating and / or preventing BTK-mediated or dependent diseases or symptoms. Wherein each group in the general formula (I) is defined in the specification.

The invention relates to a pyrrolopyrimidine compound, a preparation method thereof and application of the pyrrolopyrimidine compound in medicine. Specifically, the invention relates to a pyrrolopyrimidine compound as shown in a general formula (I), a preparation method thereof, a pharmaceutical composition containing the pyrrolopyrimidine compound and application of the pyrrolopyrimidine compound as a therapeutic agent, the invention also relates to a use thereof, in particular as a BTK inhibitor or degradation agent and in the preparation of a medicament for the treatment and / or prevention of BTK-mediated or dependent diseases or conditions. Wherein each group in the general formula (I) is defined in the specification.

The application discloses a PROTAC compound for targeted degradation of PRMT5 and application thereof, and relates to a compound shown in the following formula, a related analogue of the compound or a pharmaceutically acceptable salt, metabolite or prodrug thereof: wherein X represents a ligand combined to a PRMT5 protein, Z represents a ligand of an E3 ubiquitin ligase, and Y represents a connecting group connecting X and Z; the application takes CRBN as the E3 ligase, and a series of PROTAC degradation compounds for targeting PRMT5 are designed and synthesized. The compound can effectively induce degradation of PRMT5, significantly inhibit proliferation, growth, migration, infiltration, clonal formation and metastasis of tumor cells, promote apoptosis of cancer cells, promote autophagy of tumor cells, prevent or overcome BTK inhibitor drug resistance, and / or prolong the survival period of tumor patients, and has a wide application prospect.

Provided is use of a compound represented by Formula (I), or a stereoisomer, tautomer, solvate or pharmaceutically acceptable salt of the compound represented by Formula (I) in the manufacture of a medicament for treating and / or preventing an immune system disease.

The present invention relates to compounds and methods useful for dual inhibition of C-X-C receptor type 4 (CXCR4) and Bruton's tyrosine kinase (BTK). The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders.

The invention relates to a medicine for treating myasthenia gravis and application thereof, and belongs to the technical field of medical biology. The invention relates to a medicament for treating myasthenia gravis (MG), which is characterized in that the medicament contains a Bruton's tyrosine kinase (BTK) inhibitor Pirtobrutinib, and the medicament can be used for treating myasthenia gravis (MG). The Pirtobrutinib is a third generation of BTK (brutinib) inhibitor with high selectivity and a non-covalent (reversible) binding mode. The Pirtobrutinib can be used for effectively treating the MG, and meanwhile, the serious safety defect of similar medicines in the prior art can be avoided.

The invention relates to a pharmaceutical formula of a Bruton's tyrosine kinase inhibitor. Described herein are pharmaceutical formulations of the Bruton's tyrosine kinase (Btk) inhibitor 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo [3, 4-d] pyrimidin-1-yl) piperidin-1-yl) prop-2-en-1-one. Also disclosed are methods of using Btk inhibitors, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.

The invention discloses a gene marker panel for diagnosing PCNSL based on cerebrospinal fluid ctDNA, and relates to the technical field of gene detection, the technical key point is that the gene marker panel comprises MYD88, PIM1, CD79B, GNA13, IRF4, DTX1, KMT2D and B2M genes, and PCNSL diagnosis and prognosis evaluation are realized through targeted capture sequencing and a machine learning model. The specificity of the kit in MYD88 wild type PCNSL cases reaches 100%, the BTK inhibitor treatment response and the total lifetime of patients can be predicted, tiny residual focuses can be detected, and recurrence can be warned in advance. The invention further provides a detection kit, a prognosis evaluation system and online webpage application, the quantity demanded of samples is small, the detection sensitivity is high, the specificity is high, and a powerful tool is provided for PCNSL diagnosis and treatment.

This disclosure provides methods for treating a disease chosen from membranous nephropathy (MN), IgG4-related diseases, and antiphospholipid syndrome (APS) in a mammal using, for example, a therapeutically effective amount of the BTK inhibitor 2-[(3R)-3-[4-amino-3-(2-fluoro-4-phenoxyphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile or a pharmaceutically acceptable salt thereof.