149 results about "Cell Cycle Protein" patented technology

Provided are a compound of formula (I) and a pharmaceutical composition thereof. The compound of formula (I) can be used as a degradation agent for CyclinK protein, and can be used for preventing or treating diseases related to CyclinK protein.

The present disclosure provides, among other things, methods for treating cancer comprising administering an effective dose of Azenosertib to subjects selected to have a Cyclin E1 status above a predetermined threshold.

The present disclosure relates to pyrrolo-pyrimidine compounds, or pharmaceutically acceptable salts thereof, of Formula (I"): Compounds of the disclosure are useful for degrading cyclin-dependent kinase 4 (CDK4), and methods of making the same are provided.

The present application provides compounds of Formula (I):or a pharmaceutically acceptable salt thereof, that are inhibitors of cyclin-dependent kinase 4 (CDK4), as well as pharmaceutical compositions thereof, and methods of treating cancer using the same.

The present invention relates to an aryl substituent-containing degradation agent for cyclin-dependent kinase 12 / 13 (CDK12 / 13), a preparation method therefor, and a pharmaceutical composition and use thereof. The degradation agent for CDK12 / 13 of the present invention has a structure represented by formula (I). The compound can be used as a protein kinase degradation agent, and can effectively and highly selectively degrade a CDK12 / 13 protein and inhibit proliferation, migration, and invasion of various tumor cells.

Described herein are compounds that mediate the degradation of cyclin-dependent kinase 2 (CDK2) and are therefore useful in the treatment of various disorders, such as cancer.

The present disclosure provides certain bifunctional compounds that cause degradation of Cyclin-dependent kinase 2 (CDK2) via ubiquitin proteasome pathway and are therefore useful for the treatment of diseases mediated by CDK2. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

This invention relates to combination therapies comprising an inhibitor of anaplastic lymphoma kinase (ALK) and, an inhibitor of cyclin dependent kinase 4 and 6 (CDK4 / 6 inhibitor) or an inhibitor of cyclin dependent kinase 2, 4 and 6 (CDK2 / 4 / 6 inhibitor), and associated methods of treatment, combinations, pharmaceutical compositions and uses thereof.

Disclosed herein are methods for increasing sensitivity of a cancer cell to alternating electric fields by administering an AKT inhibitor, a mammalian target of rapamycin (mTOR) inhibitor, a Phosphatidylinositol 3-Kinase (PI3K) inhibitor, and / or a Glycogen synthase kinase 3β (GSK3β) inhibitor. Disclosed are methods of increasing treatment efficacy comprising applying alternating electric fields to a target site of the subject for a period of time, the alternating electric fields having a frequency and field strength, wherein the target site comprises one or more cancer cells, and administering a therapeutically effective amount of one or more of an mTOR inhibitor, AKT inhibitor, PI3K inhibitor, or GSK3β inhibitor to the subject. Disclosed are methods of reducing viability of cancer cells using alternating electric fields for a period of time, the alternating electric fields having a frequency and field strength in combination with either an mTOR inhibitor, AKT inhibitor, PI3K inhibitor, or GSK3β inhibitor and / or a composition or compound that increases cyclin D1. Disclosed are methods of increasing apoptosis of a cancer cell comprising exposing the cancer cell to alternating electric fields for a period of time, the alternating electric fields having a frequency and field strength; and exposing the cancer cell to a PI3K inhibitor.

This document provides bifunctional compounds, one part of which (e.g., lenalidomide, thalidomide) is a binder of an E3 ubiquitin ligase (e.g., Cereblon) and the other part of which is a binder of a target protein (e.g., a kinase (e.g., CDK (e.g., CDK9 and / or CDK12))) to induce the degradation of the target protein CDK9 and / or CDK12. Pharmaceutical compositions comprising bifunctional compounds are also provided, as well as methods for treating and / or preventing diseases (e.g., proliferative diseases such as cancers (e.g., ovarian cancer, breast cancer, or prostate cancer)). Methods for inducing the degradation of target proteins (e.g., kinases (e.g., CDK (e.g., CDK9 and / or CDK12))) and methods for inducing apoptosis in biological samples or subjects by administering the bifunctional compounds or compositions described herein are also provided.

The present invention relates to pyrazolo[1,5-a][1,3,5]triazine derivatives and pyrazolo[1,5-a]pyrimidine derivatives and / or pharmaceutically acceptable salts thereof, and the use of these derivatives as pharmaceutically active agents, particularly for the prevention and / or treatment of cell proliferative diseases, inflammatory diseases, immunological diseases, cardiovascular diseases, and infectious diseases. Furthermore, the present invention relates to pharmaceutical compositions comprising at least one of the pyrazolo[1,5-a][1,3,5]triazine derivatives and pyrazolo[1,5-a]pyrimidine derivatives and / or pharmaceutically acceptable salts thereof.

Provided is a 1H-imidazo[4,5-h]quinazoline compound of formula (I). The compound is a broad spectrum inhibitor having strong activity for cyclin-dependent kinase (CDK) and is applicable in treating cell proliferative disorder

The invention relates to a fused tricyclic cyclin-dependent kinase inhibitor as well as a preparation method and medical application thereof. Particularly, the structure of the fused tricyclic cyclin-dependent kinase inhibitor is shown as a formula I, and the definition of each substituent group is shown in the specification. The fused tricyclic cyclin-dependent kinase inhibitor is used for preventing and / or treating diseases related to cyclin-dependent kinase, especially cancers.

The invention relates to compounds which inhibit Cyclin-Dependent Kinases such as CDK2 (Cyclin-Dependent Kinase 2 or Cell Division protein Kinase 2) and CDK4 (Cyclin-Dependent Kinase 4 or Cell Division protein Kinase 4), and to processes for the preparation of said compounds, pharmaceutical compositions comprising said compounds, and use of said compounds in the treatment of conditions, diseases and disorders mediated by CDK2 and / or CDK4.

The present invention relates to pharmaceutical compounds of formula (I) and pharmaceutical compositions containing said compounds, processes for the preparation of said compounds, and the use of said compounds as inhibitors of cyclin-dependent kinase 7 (CDK7), and their use in the treatment of diseases, such as cancer. [Formula 1] TIFF2023554673000617.tif33128

The present invention provides novel compounds of Formula (I) and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are methods and kits involving the compounds or compositions for treating or preventing proliferative diseases in a subject, wherein the proliferative diseases include cancer, benign neoplasm, angiogenesis, inflammatory disease, autoinflammatory disease, and autoimmune disease, and the cancer includes leukemia, melanoma, multiple myeloma. Treatment of a subject having a proliferative disease with the compounds or compositions of the present invention can inhibit abnormal activity of cyclin-dependent kinase 7, thus inducing apoptosis and / or inhibiting transcription in the subject.

Disclosed herein are compounds of formula (I) and methods for their preparation. Also disclosed are the use of such compounds, compositions, and intermediates useful in the preparation of these compounds for the treatment of diseases and disorders mediated, at least in part, by one or more cyclins, including cancer. JPEG2025535351000507.jpg55134

The present invention relates to pharmaceutical compounds of Formula (I) and pharmaceutical compositions comprising said compounds, methods for preparing said compounds and the use of said compounds as Cyclin-Dependent Kinase 7 (CDK7) inhibitors and their use in the treatment of diseases, such as cancer.

The application discloses a bifunctional compound and use thereof, the bifunctional compound is a bifunctional compound with K-L-S structure, wherein: K is a targeting group of cyclin 7CDK7;S is a covalent group targeting cysteine or lysine on CDK7 protein;L is a divalent linking group chemically connecting the targeting group K and the covalent group S;The bifunctional compound or does not contain divalent linking group L, and the targeting group K is directly connected with the covalent group S.The bifunctional compound or its pharmaceutically acceptable salt, ester, hydrate, solvate or stereoisomer and the pharmaceutical composition containing the same show pharmacological activity related to degradation, inhibition of target protein CDK7, and can be used for preventing and treating CDK7 related diseases or disorders.

Disclosed herein are methods and agents for the treatment and / or prevention of cyclin-dependent kinase-like 5 (CDKL5) deficiency. In particular, disclosed herein are compounds or compositions for increasing cyclin-dependent kinase-like 2 (CDKL2) in a subject, for example, in the brain of a subject, and the use of such compounds and compositions in methods for treating CDKL5 deficiency.

The invention discloses an NKT cell, a culture medium and a culture method thereof, and relates to the technical field of cell culture, the NKT cell comprises a basal culture medium, a cell factor combination, a plant extract compound, a metabolism regulator and an antioxidant; wherein the plant extract compound is prepared from astragalus polysaccharide, ganoderic acid, tea polyphenol, asiaticoside and notoginsenoside R1, and the mass ratio of the astragalus polysaccharide to the ganoderic acid to the tea polyphenol to the asiaticoside to the notoginsenoside R1 is (3 to 5) to (1 to 2) to 1 to (0.5 to 1) to (0.5 to 1). According to the NKT cell, the culture medium and the culture method of the NKT cell, through the synergistic effect of the six-membered plant extract compound, the expression of cyclin is promoted, the G1 / S phase conversion is accelerated, and the cell amplification amount is remarkably increased; the ratio of plant extracts and high astragalus polysaccharide are dynamically adjusted, so that cell proliferation and induced differentiation of high ganoderic acid are promoted, cells are forced to turn to efficient-productivity oxidative phosphorylation metabolism in cooperation with 2-deoxyglucose, and the cell multiplication time is shortened.

The present invention provides a cyclin modulator. Specifically, the present invention provides a compound as shown in Formula (I) or a pharmaceutically acceptable salt thereof.

The invention provides a cyclin regulator. Specifically, the invention provides a compound shown as a formula (I) or pharmaceutically acceptable salt thereof. # imgabs0 #

Disclosed are purine derivatives of formulae (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods involving the inventive compounds or compositions for treating and / or preventing cell proliferative diseases including certain cancers of breast, brain, ovarian, lung, colorectal cancer, leukemias, lymphoma, melanoma, multiple myeloma, Ewing's sarcoma, osteosarcoma and inflammatory and myotonic dystrophy type 1 diseases in a mammal. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of kinases, such as a cyclin-dependent kinases (CDK) (e.g., CDK12 / 13), and therefore, induce potent antiproliferative and apoptotic effects and / or inhibit transcription in the subject.

The present invention relates to a compound of formula (I), a compound-linker construct comprising the compound, and a conjugate comprising the compound-linker and a targeting moiety. The compound of the present invention has the ability to stimulate and / or induce, particularly induce degradation of a target protein. Such a target protein may be a protein involved in diseases, like cancer, metabolic disorder, infectious disease and / or neurological disorder, namely in particular cyclin K (CCNK) and / or CDK12 and / or CDK13. The present invention also relates to the compound, the compound-linker construct and the conjugate for use as medicament, preferably for use in treating specific diseases as disclosed herein.

Provided herein are novel compounds (e.g., Formula I or II), pharmaceutical compositions, and methods of using related to cyclin dependent kinases (CDKs). The compounds herein are typically CDK inhibitors, which can be used for treating a variety of diseases or disorders, such as cancer.

This invention discloses *Bifidobacterium longum* with anti-aging functions and its applications, belonging to the field of microbial technology. The *Bifidobacterium longum* BBS 02 provided by this invention can promote cell vitality and proliferation, inhibit the high activity of β-galactosidase in senescent cells, and inhibit the high expression of the cyclin-dependent kinase inhibitor gene Cdkn1a, thereby achieving an anti-aging effect. The *Bifidobacterium longum* BBS 02 can be used to prepare edible nutrients or skin nutrients.

The present disclosure relates to a method of determining a prognostic outlook for patients having metastatic breast cancer. The method includes receiving imaging data from an image of a patient that is receiving or that is to receive cycline dependent kinase 4 and 6 (CDK 4 / 6) inhibitor therapy for hormone receptor-positive (HR+) metastatic breast cancer. Radiomic heterogeneity features are extracted from imaging data associated with a metastasis within the imaging. A prognostic marker is determined from the radiomic heterogeneity features. The prognostic marker is indicative of a response of the patient to CDK 4 / 6 inhibitor therapy for HR+ metastatic breast cancer.