33 results about "CDK inhibitor" patented technology

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 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.

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.

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).

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 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.

The disclosure is in part directed to crystalline forms of (3R,5R)-5-(5-(3-(2,2-difluoroethoxy)-1-methyl-1H-pyrazole-5-carboxamido)-1H-pyrazol-3-yl)tetrahydrofuran-3-yl bicyclo[1.1.1]pentan-1-ylcarbamate, its solvates, its cocrystals, and variants thereof.

The invention relates to a method for improving the infection efficiency of AAV (adeno-associated virus) infected cells, which comprises the following steps: the cells to be infected are contacted with a DNA replication inhibitor, and the DNA replication inhibitor comprises a cell cycle non-specific drug and / or a CDK inhibitor. According to the method disclosed by the invention, the infection efficiency of the AAV infected cells can be remarkably improved.

Provided are a pharmaceutical combination and a pharmaceutical composition comprising a compound of formula (I) or a pharmaceutically acceptable form thereof and at least one other anticancer agent, and use thereof in the preparation of a medicine for treating a malignant tumor disease. The other anticancer agent is a CDK inhibitor or a pharmaceutically acceptable salt thereof (such as palbociclib), lenvatinib or a pharmaceutically acceptable salt thereof, sorafenib or a pharmaceutically acceptable salt thereof, or any combination of the above.

The present invention provides a pharmaceutical comprising a HER2 inhibitor or a CDK inhibitor that inhibits CDK4 and / or CDK6. The present invention further provides the use of a HER2 inhibitor in combination with a CDK inhibitor for treating tumors, and their use in preparing a medicament for treating tumors. The combination of the present invention significantly enhances tumor inhibition.

The present invention relates to a method of determining the therapy for treating a subject afflicted from breast cancer comprising determining the P27 T2871099G SNP in a sample of said subject and administering only endocrine therapy if the polymorphism is other than T2871099G, and administering endocrine therapy in combination with at least one CDK4 / 6 inhibitor if the polymorphism is homozygous T2871099G.

The present invention relates to a CDK kinase inhibitor and its pharmaceutical use. In particular, the present invention relates to a CDK inhibitor having the structure of formula (I) and its pharmaceutical composition, and its use as a CDK inhibitor and its use in the manufacture of a medicament for treating a cancer or a tumor at least partially associated with CDK. Wherein each substituent of formula (I) is the same as defined in the specification.

Provided herein are methods related to detecting rearrangements in the B-cell lymphoma 6 (BCL6) corepressor (BCOR) or BCL6 corepressor-like protein I (BCORL1) gene, as well as methods of treatment, uses, and kits related thereto. As demonstrated herein, detection of BCOR rearrangements can be used to identify individuals that may benefit from treatment with a targeted therapeutic, such as a CDK inhibitor, an MDM2 inhibitor, a tyrosine kinase inhibitor, a MEK inhibitor, an mTOR inhibitor, or a Hh inhibitor. In some embodiments, the BCOR rearrangement is a fusion gene between BCOR and L3MBTL2, EP300, NUTM2G, MAP7D2, RALGPS1 RGAG1, CREBBP, ING3, NUGGC, or KMT 2D.

Disclosed herein are compounds of Formula (I) useful as cyclin dependent kinase inhibitors for the treatment of cancer.

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

The present disclosure belongs to the field of medicinal chemistry, relates to a tricyclic compound as a CDK inhibitor and the use thereof, and specifically relates to a compound represented by formula (I), an isomer thereof or a pharmaceutically acceptable salt thereof.

The present invention relates to pyrazolo[1,5-a][1,3,5]triazine and pyrazolo[1,5-a]pyrimidine derivatives having Formula I:and / or pharmaceutically acceptable salts thereof, the use of these derivatives 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 at least one of the pyrazolo[1,5-a][1,3,5]triazine and pyrazolo[1,5-a]pyrimidine derivatives and / or pharmaceutically acceptable salts thereof.

The disclosure herein provides combination therapies for the treatment of cancers such as Leukemia, lymphoma and triple negative breast cancer. The disclosure provides combination therapies of CDK inhibitors, e.g., a CDK inhibitor represented by Formula I:or a pharmaceutically acceptable salt thereof together with a BCL-2 inhibitor or proteasome inhibitor for the treatment of cancer.

The present disclosure relates to a pharmaceutical combination comprising (1) a first agent which is a CDK inhibitor or a pharmaceutically acceptable salt thereof and (2) a second agent which is an anti-hormonal agent or a pharmaceutically acceptable salt thereof. The present disclosure also relates to a pharmaceutical combination comprising (1) a first agent which is a CDK inhibitor or a pharmaceutically acceptable salt thereof, (2) a second agent which is an anti-hormonal agent or a pharmaceutically acceptable salt thereof, and (3) a third agent which is an agent that regulates the PI3K / Akt / mTOR pathway or a pharmaceutically acceptable salt thereof.

To provide pyrido[2,3-d]pyrimidin-7(8H)-one compounds, pharmaceutically acceptable salts, solvates, prodrugs and active metabolites, which can be strong CDK2, CDK4, and CDK6 inhibitors.SOLUTION: Pyrido[2,3-d]pyrimidin-7(8H)-ones of a formula (1) and pharmaceutical compositions containing compounds of the formula (1) as CDK inhibitors are disclosed herein. Methods and uses of compounds of the formula 1 in the treatment of cancer and manufacturing are also disclosed.SELECTED DRAWING: None