189 results about "Cyclin" patented technology

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.

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.

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.

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.

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 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.

The invention provides a purine compound as well as a preparation method and application thereof. Specifically, the invention provides a compound as shown in a formula I or pharmaceutically acceptable salts, enantiomers, diastereoisomers, atropisomers, polymorphs, solvates, isotope labeled compounds or racemes thereof. The definition of each substituent group is described in the specification and claims. The purine compound can be used for preparing a CDK12-cyclin K inhibitor and a CDK12-cyclin K degradation agent, and can be used for preparing medicines for treating diseases or symptoms caused by dysfunction of the CDK12-cyclin K. # imgabs0 #

The present disclosure provides combination therapies for treating a cancer having a BRAF mutation, the combination therapies comprising administering to a subject an effective amount of (a) an epidermal growth factor receptor (EGFR) inhibitor; (b) a mitogen-activated protein kinase (MEK) 1 / 2 inhibitor; (c) a cyclin-dependent kinase (CDK) 4 / 6 inhibitor. Also provided are compositions and kits related to the combination therapies.

Use of a pyrimidine-based selective cyclin-dependent kinase 2 (CDK2) of structure: (Compound I), or a pharmaceutically acceptable salt thereof or morphic form described herein for the treatment of disorders characterized by aberrant cellular division having amplified cyclin E activation and / or expression or aberrant cellular division disorders, CDK4 / 6 resistance, and / or endocrine therapy resistance, including but not limited to the treatment of tumors and cancers.

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.

Disclosed is an application of a protein kinase inhibitor in preparation of a medicine for inhibiting uterine leiomyosarcoma, wherein the protein kinase inhibitor can effectively inhibit tumor growth in vitro and in vivo, and has better efficacy and safety compared with traditional chemotherapy. The protein kinase is one of the following: Wee1-like protein kinase, cyclin-dependent kinase 1, serine / threonine protein kinase 1 and serine / threonine protein kinase ATR.

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 #

A Cyclin K degrader drug and an antibody conjugate thereof, as well as preparation methods therefor and use thereof.

This invention is in the area of cell cycle inhibiting compounds for the treatment of disorders involving abnormal cellular proliferation, and include selective CDK2 inhibitors for medical therapy and their pharmaceutically acceptable salts and compositions. The inhibitors are pyrimidine-based N-heterocyclic compounds of formula: