187 results about "Cell Cycle Protein" patented technology

The present disclosure provides a compound represented by structural Formula (I): Formula (I), or a pharmaceutically acceptable salt thereof. Compounds of the disclosure are useful for degrading cyclin-dependent kinases (CDKs) and for treating diseases and disorders mediated by CDKs.

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.

This invention is in the area of improved therapeutic combinations for and methods of treating selected retinoblastoma (Rb)-negative cancers and Rb-negative abnormal cellular proliferative disorders using particular topoisomerase inhibitors and specific cyclin-dependent kinase 4 / 6 (CDK4 / 6) inhibitors. In one aspect, the improved treatment of select Rb-negative cancers is disclosed using specific compounds disclosed herein in combination with a topoisomerase I inhibitor.

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 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.

Provided herein are certain aminoheteroaryl compounds with tricyclic structure moiety, pharmaceutical compositions, and methods of use related to cyclin dependent kinases (CDKs). The compounds provided herein are typically CDK4 inhibitors, which can be used for treating a variety of diseases or disorders, such as cancer.

A pharmaceutical composition comprising protein arginine methyltransferase 5 (PRMT5) and cyclin-dependent kinase 4 and 6 (CDK4 / 6) inhibitors. The pharmaceutical composition can be used for treating various cancers, comprising solid tumors. The combined product can be used for treating any number of diseases associated with PRMT5 and / or CDK4 / 6.

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.

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

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.

Disclosed herein are compounds of Formula I and methods of making the same. Also described herein are the use of such compounds, compositions for the treatment of diseases and conditions mediated, at least in part, by one or more cyclin proteins, including cancer, and intermediates useful in the preparation of these compounds. # imgabs0 #

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.

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 compound used as a CDK2 / 4 protein kinase inhibitor and application thereof. Specifically, the invention discloses a compound shown as a formula I, or pharmaceutically acceptable salt, stereoisomer, tautomer, hydrate, solvate, isotope compound or prodrug thereof, and the definitions of all groups and substituent groups are described in the specification. The compound provided by the invention can be used as an inhibitor of cyclin dependent kinase (CDK), and is used for preventing or treating cell proliferative diseases and symptoms including various cancers, in particular for regulating and / or treating related diseases caused by overexpression and / or abnormal activity of the cyclin dependent kinase CDK2 / 4. # imgabs0 #

The present invention discloses a class of pyrimidopyrimidone compounds and applications thereof. The compounds have excellent inhibitory activity on cyclin-dependent kinases 2 / 4 / 6 (CDK2 / 4 / 6), can be used as CDK2 / 4 / 6 inhibitors, and are used to prepare drugs for preventing and / or treating diseases related to CDK2 / 4 / 6 overexpression in organisms and drugs for diseases related to angiogenesis or cancer metastasis.

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.