89 results about "CDK4 Inhibitor" patented technology

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 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

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.

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

This invention relates to therapies for treating mantle cell lymphoma comprising a cyclin dependent kinase 4 (CDK4) inhibitor or a pharmaceutically acceptable salt thereof, and associated methods of treatment, pharmaceutical compositions, and uses thereof.

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 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 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).

This disclosure relates to combination therapies comprising a cyclin dependent kinase 4 (CDK4) inhibitor of Formula (I) disclosed herein, and a monoclonal antibody or an antibody-drug conjugate, optionally in further combination with an endocrine therapy agent, and associated methods of treatment, pharmaceutical compositions, and uses thereof.

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

This invention relates to, in part, a method for treating cancer by administering a CDK4 inhibitor in combination with a PD-1 axis binding antagonist, and optionally an CDK2 inhibitor to a subject in need thereof.

The invention discloses a CDK4 / PARP1 double-target inhibitor and application, belongs to the technical field of medicines, and solves the problems that a single CDK4 inhibitor is poor in effect and a single PARP1 inhibitor is weak in activity, the inhibitor is a compound with a structural general formula A-Linker-B, or pharmaceutically acceptable salt, solvate, hydrate or prodrug thereof, the double-target inhibitor provided by the invention can effectively overcome the defects of poor effect of a single CDK4 inhibitor, weak activity of a single PARP1 inhibitor and the like, has a very strong inhibition effect on CDK4 and PARP1, and has a relatively good application prospect.

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.

This invention relates to crystalline and amorphous forms of 1,5-anhydro-3-({5-chloro-4-[4-fluoro-2-(2-hydroxypropan-2-yl)-1-(propan-2-yl)-1H-benzimidazol-6-yl]pyrimidin-2-yl}amino)-2,3-dideoxy-D-threo-pentitol, to pharmaceutical compositions comprising such solid forms, and to use of such solid forms and pharmaceutical compositions for the treatment of 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.