236 results about "Cyclin" 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.

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.

The invention relates to the technical field of biology, in particular to application of active polypeptide in maintaining dryness of umbilical cord mesenchymal stem cells. The active polypeptide disclosed by the invention is PNC-27, and the amino acid sequence of the PNC-27 is as shown in SEQ ID NO: 1. Experiments find that the PCN-27 polypeptide can effectively promote proliferation of the umbilical cord mesenchymal stem cells by regulating expression of periodic proteins Cyclin-D1 and CDK1, and can also effectively maintain dryness of the umbilical cord mesenchymal stem cells by promoting expression of dry gene Oct-4 protein in the umbilical cord mesenchymal stem cells. Experiments fully prove that the PCN-27 polypeptide can effectively maintain the dryness of the umbilical cord mesenchymal stem cells and stimulate the potential application value of the umbilical cord mesenchymal stem cells in the fields of cell culture, biomedicine and the like.

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 invention discloses an application of a phellinus igniarius extract in preparation of a lung cancer H1299 cell inhibitor, the active ingredient of the inhibitor comprises the phellinus igniarius extract, and the inhibitor at least has the following functions: a, inhibiting proliferation and clone formation of lung cancer H1299 cells; b, inhibiting the invasion and metastasis capability of lung cancer H1299 cells; c, arresting the cell cycle of the lung cancer H1299 in the S period; and d, the lung cancer H1299 cyclin Cyclind1 is down-regulated, the pro-apoptotic protein Bax is up-regulated, and the expression of p-AKT and Bcl-2 proteins is inhibited. The phellinus igniarius extract is phellinus igniarius extract powder or phellinus igniarius extract liquid, and the concentration of the phellinus igniarius extract liquid is 0.1-1.0 mg / ml. According to the application of the phellinus igniarius extract in preparation of the lung cancer H1299 cell inhibitor, a new thought is provided for preparation and / or screening of lung cancer drugs, a good working foundation is laid, and a new strategy is provided for clinical application.

The present invention relates to compounds having cyclin-dependent kinase (CDK)-inhibitory functions and / or pharmaceutically acceptable salts thereof, the use of these compounds as pharmaceutically active agents, especially for the prophylaxis and / or treatment of cell proliferative diseases, inflammatory diseases, immunological diseases, cardiovascular diseases and infectious diseases. Furthermore, the present invention is directed towards pharmaceutical compositions containing such compounds.

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 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 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.

Phospholamban (PLN) is a critical regulator of calcium cyclin and contractility in the heart. The deletion of Arginine 14 of the phospholamban gene (R14del) is associated with the pathogenesis of an inherited form of cardiomyopathy with prominent arrhythmias. Although the genetic etiology is well defined, there are currently no therapies for this rare disease. This disclosure provides an allele-specific silencing approach by interfering RNA (RNAi) to reduce the expression levels of the R14del allele of the PLN gene.

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 invention relates to a degradation agent containing monocyclic aryl substituted CDK12 / 13 as well as a preparation method, a pharmaceutical composition and application of the degradation agent. The degradation agent for cell cycle-dependent protein kinase 12 / 13 (CDK12 / 13) has a structure as shown in a formula (I), and the compound can be used as a protein kinase degradation agent, can effectively degrade CDK12 / 13 protein with high selectivity, and can inhibit proliferation, migration and invasion of various tumor cells. # imgabs0 #

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 invention belongs to the technical field of biological medicines, and particularly relates to application of CDK9 as a target spot in preparation of a medicine for preventing and treating oral leukoplakia canceration. The invention proves that the phenomenon of transcriptional activity increase and the characteristic of transcription addiction exist in the oral leukoplakia canceration process, and a driving factor cyclin-dependent kinase 9 (CDK9) closely related to oral leukoplakia transcriptional disorder is screened out. Moreover, a molecular mechanism of CDK9 driving oral leukoplakia transcription addiction is further clarified, an important role of CDK9 in an oral leukoplakia canceration process is clarified, and transcription addiction of oral leukoplakia cells can be effectively inhibited through targeted intervention of activity or expression level of CDK9, so that canceration potential of oral leukoplakia can be effectively prevented and treated.

The invention relates to compounds that have been identified as CDK4 (cyclin-dependent kinase enzyme) inhibitors for the first time, for use as a medication, in particular, for the treatment of cancers e.g. those with overexpression of the enzyme CDK4, and to pharmaceutical compositions comprising same. Said compounds target the interaction interface between CDK4 and its activating cyclin, whereas those drugs already approved for the treatment of cancers with overexpression of the enzyme CDK4 target the ATP-binding site.

Disclosed herein are methods of treating cancer by administering plinabulin and a cyclin-dependent kinase inhibitor, such as abamecril, in combination.