60 results about "CDK inhibitor" patented technology

Described herein are compositions comprising a lanthanide (III) modified fatty acid and methods of treating cancer with the composition. In particular, the application includes a lanthanide (III) modified fatty acid is a 9-R′, 10-R″ tri octadecanoate compound. This lanthanide (III) modified fatty acid can be combined with additional therapeutic agents, such as chemotherapeutic agents, radiopharmaceuticals, hormone therapies, CDK inhibitors, epigenetic modulators, selective estrogen receptor modulators, selective estrogen receptor degraders, aromatase inhibitors, phosphatidyl inositol-3-posphate kinase inhibitors, ATP-adenosine axis-targeting agents, signal transduction inhibitors, RAS signaling inhibitors, PI3K inhibitors, arginase inhibitors, HIF inhibitors, AXL inhibitors, PAK4 inhibitors, immunotherapeutic agents, immune checkpoint inhibitors, and agonists of stimulatory or co-stimulatory immune checkpoints.

The invention provides a compound represented by represented by the following strutural formula:or a pharmaceutically acceptable salt, or a stereoisomer thereof useful for treating cancer.

To provide methods and compositions for controlling sucker growth in tobacco by altering the expression of different target genes.SOLUTION: A modified tobacco plant comprises a mutation in an endogenous gene encoding polypeptide selected from the group consisting of cyclin, cyclin-dependent kinase (CDK), a CDK inhibitor, MYB, and a WRKY transcription factor, wherein the mutation is not present in the endogenous gene in a control tobacco plant of the same variety, and wherein the modified tobacco plant comprises no suckers or reduced suckers after topping as compared to the control tobacco plant when grown under comparable growth conditions.SELECTED DRAWING: None

Various salt forms and free bases of compound (I) represented by the following chemical formula are disclosed (I).

Disclosed herein are bicyclic compound derivatives used as inhibitors of cyclin-dependent kinases. Disclosed herein is the use of these inhibitors for inhibiting cyclin-dependent kinases, and the use of such compounds for treating cancer.

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.

The present invention relates to a CDK inhibitor and the pharmaceutical uses thereof. In particular, the present invention relates to a CDK inhibitor having a structure of formula (I), a pharmaceutical composition thereof, the use thereof as a CDK inhibitor, and the use thereof in the preparation of a drug for treating at least part of CDK-related cancers or tumors, each substituent in formula (I) being as defined in the description.

Provided herein are CDK inhibitor compounds having a fused 6-6 bicyclic heteroaryl core, such as naphthyridine, quinazoline, pyridopyrimidine or a further substituted associated electron isosteric core structure. The core structure may be substituted with an amino group, wherein the amino group is further substituted with a cyclic group having an additional hydrophilic group. Also provided herein are compositions comprising the subject CDK inhibitor compounds. In some embodiments, the CDK inhibitor compound is a CDK2 inhibitor or a CDK4 inhibitor. Methods of using the compositions of the present disclosure in research or as therapeutic agents are also provided.

The application provides a polymorph of a compound of formula (A) (N-(1-((4-((3S,5S)-3,5-dimethylpiperazin-1-yl)phenyl)sulfonyl)piperidin-4-yl)-4-((S)-tetrahydrofuran-3-yl)oxy)-5-(trifluoromethyl)pyrimidin-2-amine) and a polymorph of a phosphate salt of the compound of formula (A). The crystal form provided by the application has good chemical stability, physical stability and low hygroscopicity, is less affected by temperature, humidity and light, and is convenient to store and develop into a preparation.

The present disclosure relates to novel compounds and pharmaceutical compositions thereof and methods of inhibiting the activity of CDK enzyme using the compounds and compositions of the present disclosure. The present disclosure further relates to, but is not limited to, methods of treating disorders associated with CDK signaling using the compounds and compositions of the present disclosure.

Provided herein are CDK inhibitors, e.g., a compound of Formula (I), and pharmaceutical compositions thereof. Also provide herein is a method of their use for treating, preventing, or ameliorating a chemotherapy-induced gastrointestinal side effect.

Provided herein are methods of treating diseases, disorders, or conditions including cancers, where the methods comprise administration of Compound 1, or a pharmaceutically acceptable salt thereof, in combination with a CDK inhibitor or a selective estrogen receptor degrader (SERB), as described herein. Such methods may comprise the treatment of cancer, such as breast cancer.

Disclosed herein are bicyclic compound derivatives useful as cyclin dependent kinase inhibitors. Disclosed herein are the use of these inhibitors for inhibiting cyclin-dependent kinases, and the use of these compounds for the treatment of cancer.

The invention relates to a CDK inhibitor with a structure as shown in a formula (I) and a pharmaceutical composition thereof, and application of the CDK inhibitor as the CDK inhibitor and application of the CDK inhibitor in preparation of drugs for treating at least part of cancers or tumors related to CDK. Wherein each substituent in the formula (I) is as defined in the specification.

Disclosed herein are compounds used as inhibitors of cyclin-dependent kinases. Disclosed herein is the use of these inhibitors for inhibiting cyclin-dependent kinases, and the use of such compounds for treating cancer.

Disclosed are various salt forms and the free base of Compound (I) represented by the following formula. (I).

Various salt forms and free base of Compound (I) represented by the following formula are disclosed.

The invention relates to cancer, and in particular, to novel conjugates, compositions, therapies and methods for treating, preventing or ameliorating cancer. The invention is especially concerned with conjugates comprising a targeting moiety and a CDK inhibitor, and compositions comprising such conjugates, and methods of making the compositions. The invention relates particularly, although not exclusively, to immunoconjugates, such as, antibody drug conjugates (ADC) comprising an antibody or an antigen-binding fragment thereof conjugated to a CDK inhibitor. The invention extends to the use of such conjugates in treating, preventing or ameliorating cancer.

The present invention relates to a pharmaceutical combination comprising a CDK inhibitor and at least one antioxidant enzyme inhibitor for use in the treatment of cancer. The present invention also relates to a method for the treatment of cancer comprising administering to a subject in need thereof, a therapeutically effective amount of a CDK inhibitor and a therapeutically effective amount of at least one antioxidant enzyme inhibitor. The pharmaceutical combination of the present invention exhibits synergistic effect when used in the treatment of cancer.

The present disclosure relates to a CDK4 inhibitor compound represented by formula (Z) or a pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising same, and use thereof in the preparation of a medicament for preventing or treating a CDK4-mediated disease.

The present invention provides methods of treating cancer, for example, one or more hematological malignancies, in a subject in need thereof, by administering to the subject a therapeutically effective amount of a compound of Formula I either alone or in combination with a BTK inhibitor.

Provided herein are CDK inhibitors, e.g., a compound of Formula (I), and pharmaceutical compositions thereof. Also provide herein is a method of their use for treating, preventing, or ameliorating a chemotherapy-induced gastrointestinal side effect.

strutural formula: F N N N N N N N N N cancer. 20 26 20 09 99 11 F eb 2 02 6 A B S T R A C T 2 0 2 6 2 0 0 9 9 9 1 1 F e b 2 0 2 6 F N N N N N N N N c a n c e r . A B S T R A C T 2 0 2 6 2 0 0 9 9 9 1 1 F e b 2 0 2 6 F N N N N N N N N c a n c e r .

The present disclosure provides, inter alia, methods for treating or delaying progression of cancer in an individual, or increasing sensitivity of a cancer to treatment, comprising administering to the individual an effective amount of a protein kinase A (PKA) activator; and a cyclin-dependent kinase 9 (CDK9) or cyclin-dependent kinase 12 (CDK12) inhibitor, or a salt thereof. Kits, compositions, and uses related thereto are also provided.

The present invention relates generally to the field of therapeutic compounds. More specifically, the present invention relates to certain substituted pyrazolo[1,5-a]pyrimidin-7-amine compounds PPA that specifically inhibit cyclin-dependent protein kinases (CDKs), particularly CDK12 and / or CDK13, e.g., selective for CDK12 and / or CDK13 over CDK7. In addition to selectively inhibiting CDK12 and / or CDK13, the compounds also act as selective cyclin K degraders, thereby removing key cofactors required for CDK12 and / or CDK13 activation. This provides additional cellular potency and selectivity. The present invention also relates to methods for inhibiting CDKs, particularly CDK12 and / or CDK13; and to disorders associated with CDKs, particularly CDK12 and / or CDK13, disorders resulting from inappropriate activity of CDKs, particularly CDK12 and / or CDK13, disorders associated with CDK mutations, particularly CDK12 mutations and / or CDK13 mutations, disorders associated with CDK overexpression, particularly CDK12 and / or CDK13 overexpression, disorders associated with pathway activation upstream of CDKs, particularly CDK12 and / or CDK13, The present invention relates to pharmaceutical compositions comprising such compounds, and to the use of such compounds and compositions, both in vitro and in vivo, for treating disorders that are ameliorated by inhibition of CDK12 and / or CDK13, including proliferative disorders; cancer; viral infections (including HIV); neurodegenerative disorders (including Alzheimer's disease and Parkinson's disease); ischemia; kidney disease; cardiovascular disorders (including atherosclerosis); autoimmune disorders (including rheumatoid arthritis), and disorders caused by dysfunction of translation in cells (including muscular dystrophies). Optionally, the treatment further comprises treatment (e.g., simultaneous or sequential treatment) with additional active agents, such as DNA repair inhibitors, immune checkpoint inhibitors, immune system stimulants, cell cycle checkpoint inhibitors, Her2 blockers, transcription inhibitors, cytotoxic chemotherapeutic agents, and the like.