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147 results about "CDK4 Inhibitor" patented technology

The US FDA approved the first drug of this type, palbociclib (Ibrance), a CDK4/6 inhibitor, in Feb 2015, for use in postmenopausal women with breast cancer that is estrogen receptor positive and HER2 negative.

Combinations of signal transduction inhibitors

The present invention relates to methods for treating cancer comprising utilizing a combination of signal transduction inhibitors. More specifically, the present invention relates to combinations of so called cell cycle inhibitors with mitogen stimulated kinase signal transduction inhibitors, more specifically combinations of CDK inhibitors with mitogen stimulated kinase signal transduction inhibitors, more preferably MEK inhibitors. Other embodiments of the invention relate to additional combinations of the aforesaid combinations with standard anti-cancer agents such as cytotoxic agents, palliatives and antiangiogenics. Most specifically this invention relates to combinations of 6-acetyl-8-cyclopentyl-5-methyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-8H-pyrido[2,3-d]pyrimidin-7-one including salt forms, which is a selective cyclin-dependent kinase 4 (CDK4) inhibitor, in combination with one or more MEK inhibitors, most preferably N-[(R)-2,3-dihydroxy-propoxy]-3,4-difluoro-2-(2-fluoro-4-iodo-phenylamino)-benzamide. The aforementioned combinations are useful for treating inflammation and cell proliferative diseases such as cancer and restenosis.
Owner:PFIZER INC

Dominant negative mutant krp protein protection of active cyclin-cdk complex inhibition by wild-type krp

Disclosed are mutant CDK inhibitor (CKI) polypeptides having dominant negative antagonist activity against wild-type CKI proteins, as well as related compositions, including nucleic acids and vectors encoding the mutant CKI polypeptides and transformed host cells and transgenic plants comprising such nucleic acids and vectors. Also disclosed are related methods for using the mutant proteins to modulate cell division in cells, particularly plant cells.
Owner:TARGETED GROWTH

Combination of a purine-based cdk inhibitor with a tyrosine kinase inhibitor and use thereof in the treatment of proliferative disorders

The present invention relates to combination comprising (i) an ErbB inhibitor; and (ii) a CDK inhibitor, or a pharmaceutically acceptable salt thereof, selected from: (a) roscovitine; (b) 3-{9-isopropyl-6-[(pyridin-3-ylmethyl)-amino]-9H-purin-2-ylamino}-2-methyl-pentan-2-ol; (c) 3-{9-isopropyl-6-[(pyridin-3-ylmethyl)-amino]-9H-purin-2-ylamino}-pentan-2-ol; and (d) (2R,3S-3-(6-((4,6-dimethylpyridin-3-ylmethylamino)-9-isopropyl-9H-purin-2-ylamino)pentan-2-ol.Further aspects of the invention relate to pharmaceutical products and pharmaceutical compositions comprising combinations according to the invention, and methods of treatment using the same.
Owner:CYCLACEL

Novel synthesis method of CDK4 (cyclin-dependent kinase 4) inhibitor

The invention relates to a novel synthesis method of a CDK4 (cyclin-dependent kinase 4) inhibitor. A reaction of 2-chloro-8-cyclopentyl-5-methylpyrido[2,3-d]pyrimidin-7(8H)-one with acetylchloride is taken as an initial reaction, consequent reactions are performed, and the CDK4 inhibitor is prepared; the preparation method is simple and easy to implement, the yield is high, the quality is high, and industrial production is facilitated.
Owner:BEIJING KANG LISHENG PHARMA TECH DEV

Cdk inhibitors containing a zinc binding moiety

InactiveUS20090093507A1Enhanced and unexpected propertyEffective for treating diseaseBiocideOrganic chemistryZinc bindingHDAC inhibitor
The present invention relates to CDK inhibitors and their use in the treatment of cell proliferative diseases such as cancer. The compounds of the invention may further act as HDAC inhibitors.
Owner:CURIS INC

1,3-Oxazole compounds for the treatment of cancer

Oxazole derivatives, which are useful as VEGFR2, CDK2, and CDK4 inhibitors are described herein. The described invention also includes methods of making such oxazole derivatives as well as methods of using the same in the treatment of hyperproliferative diseases.
Owner:SMITHKLINE BECKMAN CORP

Pyrazolo[1,5-a][1,3,5]triazine and pyrazolo[1,5-a]pyrimidine derivatives as CDK inhibitors

The present invention provides substituted pyrazolo[1,5-a][1,3,5]triazine and pyrazolo[1,5-a]pyrimidine derivatives of formula (I), which are therapeutically useful, particularly as selective transcriptional CDK inhibitors including CDK7, CDK9, CDK12, CDK13 and CDK18, more particularly transcriptional CDK7 inhibitors wherein X, ring A, ring B, L1, L2, R1, R2, R3, R4, R6, m, n and p have the meanings given in the specification and pharmaceutically acceptable salts thereof that are useful in the treatment and prevention of diseases or disorder associated with selective transcriptional CDKs in amammal. The present invention also provides preparation of the compounds and pharmaceutical formulations comprising at least one of the substituted pyrazolo[1,5-a][1,3,5]triazine and pyrazolo[1,5-a]pyrimidine derivatives of formula (I) or a pharmaceutically acceptable salt thereof or a stereoisomer thereof.
Owner:奥瑞基尼肿瘤学有限公司

Treating cancer with a combination of a pd-1 antagonist and dinaciclib

The present disclosure describes combination therapies comprising an antagonist of Programmed Death 1 receptor (PD-1) and the CDK inhibitor dincaciclib, and the use of the combination therapies for the treatment of cancer, and in particular for treating cancers that express PD-L1.
Owner:MERCK SHARP & DOHME LLC

Pyridopyrimidinone derivatives for treatment of neurodegenerative disease

This invention provides a method for treating neurodegenerative diseases in mammals comprising administering an effective amount of a cyclin-dependent kinase inhibitor. A preferred method uses cdk inhibitors of Formula (I) and Formula (II) where W is NH, S, SO, or SO2, R<1> includes phenyl and substituted phenyl, R<2> includes alkyl and cycloalkyl, R<3> includes alkyl and hydrogen, R<8> and R<9> include hydrogen and alkyl, and Z is carboxy.
Owner:WARNER-LAMBERT CO

Pharmaceutical combination 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.
Owner:PIRAMAL ENTERPRISES LTD

Companion diagnostic for cdk4 inhibitors

The present invention relates to the use of one or more biomarkers to evaluate the likelihood that a CDK4 inhibitor would produce an anti-cancer effect in a subject. It is based, at least in part, on the discovery that cancer treatment with a CDK4 inhibitor is more effective where treated cancer cells undergo cellular senescence rather than a transient cell cycle arrest, where cellular senescence is associated with decreased MDM2 protein level. Accordingly, in non-limiting embodiments, the present invention provides for methods, compositions, and kits for a companion diagnostic for CDK4 inhibitors, and in particular, to the use of MDM2 expression as a biomarker for the likelihood that a cancer can be successfully treated by CDK4 inhibition.
Owner:MEMORIAL SLOAN KETTERING CANCER CENT

Fascaplysin derivative as well as preparation method and application

The invention discloses a fascaplysin derivative as well as a preparation method and application thereof to a drug. A general formula of the fascaplysin derivative disclosed by the invention is shownas a formula (I) and the formula (I) is shown in the description. The compound disclosed by the invention can be applied to preparation of drugs for preventing or treating diseases related to a cyclin-dependent kinase CDK4 inhibitor and anti-tumor drugs. The fascaplysin derivative keeps a pharmacodynamics effect of the CDK4 inhibitor; the compound has a high yield, is relatively stable in the air,has relatively good water solubility and is simple to operate; and the compound has the advantages of easiness for obtaining raw materials, low price, short preparation route, simple preparation method and low production cost.
Owner:南通杏睿生物科技有限公司

Combination Therapy for the Treatment of Cancer

InactiveUS20160184311A1BiocideAnimal repellantsMedicinePI3K/AKT/mTOR pathway
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.
Owner:NOVARTIS AG

Pyrrolidine-substituted flavones as radio-sensitizers for use in the treatment of cancer

The present invention relates to a combination for the treatment of cancer wherein the combination exhibits a synergistic effect. The combination comprises radiation and at least one cyclin dependent kinase (CDK) inhibitor selected from the compounds of formula I or a pharmaceutically acceptable salt or a solvate thereof. The present invention also relates to a method for the treatment of cancer, which method comprises administering to a patient in need of such a treatment, a therapeutically effective amount of the combination. The present invention also relates to the use of a CDK inhibitor selected from the compounds of formula I as a radiosensitizer that enhances the efficacy of radiotherapy for the treatment of cancer, particularly head and neck cancer.
Owner:PIRAMAL ENTERPRISES LTD

Companion diagnostic for CDK4 inhibitors

The present invention relates to the use of one or more biomarkers to evaluate the likelihood that a CDK4 inhibitor would produce an anti-cancer effect in a subject. It is based, at least in part, on the discovery that cancer treatment with a CDK4 inhibitor is more effective where treated cancer cells undergo cellular senescence rather than a transient cell cycle arrest, where cellular senescence is associated with decreased MDM2 protein level. Accordingly, in non-limiting embodiments, the present invention provides for methods, compositions, and kits for a companion diagnostic for CDK4 inhibitors, and in particular, to the use of MDM2 expression as a biomarker for the likelihood that a cancer can be successfully treated by CDK4 inhibition.
Owner:MEMORIAL SLOAN KETTERING CANCER CENT

Use of cdk inhibitor for the treatment of glioma

The invention provides a low molecular weight ATP-competitive CDK inhibitor able to cross the blood brain barrier for use in the treatment of malignant glioma and, in particular, of glioblastoma. The compound can be administered together with one or more agents selected from the group consisting of cytotoxic or cytostatic agents and ionizing radiation.
Owner:NERVIANO MEDICAL SERVICES SRL

Assay for inhibitors of CIP/KIP protein degradation

An assay and system compatible with high throughput screening (HTS) that is capable of identifying inhibitors, such as small-molecule inhibitors, of the degradation of the Cdk inhibitor p21, are described. The assay is based on the use of fusion protein comprising (i) a p2 polypeptide; and (i) a reporter protein linked to the C-terminal of said p21 polypeptide, wherein the fusion protein has a half-life that is similar to that of the p21 polypeptide. Inhibitors identified by this assay may be useful to inhibit the proliferation of tumor cells, and thus for the treatment of cancers.
Owner:UNIV DE MONTREAL

Pyrrolidine-substituted flavones as radio-sensitizers for use in the treatment of cancer

The present invention relates to a combination for the treatment of cancer wherein the combination exhibits a synergistic effect. The combination comprises radiation and at least one cyclin dependent kinase (CDK) inhibitor selected from the compounds of formula I or a pharmaceutically acceptable salt or a solvate thereof. The present invention also relates to a method for the treatment of cancer, which method comprises administering to a patient in need of such a treatment, a therapeutically effective amount of the combination. The present invention also relates to the use of a CDK inhibitor selected from the compounds of formula I as a radiosensitizer that enhances the efficacy of radiotherapy for the treatment of cancer, particularly head and neck cancer.
Owner:PIRAMAL ENTERPRISES LTD

Co-crystals of CDK inhibitor and MEK inhibitor and preparation method of co-crystals

The invention relates to co-crystals of a CDK inhibitor and an MEK inhibitor and a preparation method of the co-crystals, and particularly provides hydrate or anhydride crystal forms which are named as the crystal form I, the crystal form II and the crystal form III.The co-crystals are good in stability, low in hygroscopicity and higher in solubility and have the important value on future optimization and development of the drugs.
Owner:CRYSTAL PHARMA CO LTD
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