362656-11-9Relevant articles and documents
HETEROCYCLIC COMPOUNDS AS KINASE INHIBITORS
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Paragraph 0600; 0603, (2021/01/23)
Heterocyclic compounds as CDK4 or CDK6 or other CDK inhibitors are provided. The compounds may find use as therapeutic agents for the treatment of diseases and may find particular use in oncology.
PYRIDO[2,3-D]PYRIMIDIN-7(8H)-ONES AS CDK INHIBITORS
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Page/Page column 41; 51; 53, (2021/09/17)
The pyrido[2,3-d]pyrimidin-7(8H)-ones of Formula (1) and pharmaceutical compositions containing compounds of Formula (1) as CDK inhibitors are disclosed herein. Methods and use of a compound of Formula 1 in the treatment of cancer and manufacture are also disclosed.
Preparation method for 1-(4-cyclopentylamine-2-methylmercapto-pyrimidine-5-)ethyl ketone
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Paragraph 0057; 0058; 0059; 0065; 0066, (2017/08/28)
The invention discloses a preparation method for 1-(4-cyclopentylamine-2-methylmercapto-pyrimidine-5-)ethyl ketone. The method comprises the following steps of: (a) adding 4-cyclopentylamine-2-methylmercapto-pyrimidine-5-ethyl formate disclosed by a formula (1) and alkali into organic solvent to react to obtain 4-cyclopentylamine-2-methylmercapto-pyrimidine-5-methanoic acid disclosed in a formula (2); (b) carrying out condensation reaction on the 4-cyclopentylamine-2-methylmercapto-pyrimidine-5-methanoic acid disclosed in the formula (2) and N,O-dimethylhydroxylamine hydrochloride disclosed in a formula (3) to obtain a 4-cyclopentylamine-N-methoxyl-N-methyl-2-methylmercapto-pyrimidine-5-formamide disclosed in a formula (4); and (c) enabling the 4-cyclopentylamine-N-methoxyl-N-methyl-2-methylmercapto-pyrimidine-5-formamide disclosed in the formula (4) to react with methyl magnesium bromide to obtain the1-(4-cyclopentylamine-2-methylmercapto-pyrimidine-5-)ethyl ketone disclosed in a formula (5). The preparation method disclosed by the invention has the advantages of being low in cost and convenient and safe in operation and is easy in large-scale industrial production, and column chromatography isolation purification is not required during postprocessing.
Protection of renal tissues from ischemia through inhibition of the proliferative kinases CDK4 and CDK6
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, (2017/11/27)
The presently disclosed subject matter relates to methods and compositions for protecting cells and or tissues from damage due to ischemia. In particular, the presently disclosed subject matter relates to the protective action of cyclin dependent kinase 4/6 (CDK4/6) inhibitors administered to subjects that have been exposed to, or that are at risk of, ischemia.
Novel important intermediate for anticancer drug palbociclib and compounding process
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Paragraph 0036-0038, (2017/08/29)
The invention discloses a compounding process for a novel important intermediate for anticancer drug palbociclib. The compounding process includes allowing a compound 1 and a compound 2 to react with each other at a time with high yield under the action of Grignard reagents to obtain a compound 3, and allowing the compound 3 to react with R7CH2COOR3 to obtain a compound 4. The compounding process has a short path, and only two reaction steps, from the initial raw material 1 to the key intermediate pyridino-pyrimidine-7-ketone derivative 4, are needed; raw materials are cheap, reaction process is harmless to the environment, overall yield is high, and the compounding process is suitable for mass production.
CYCLIN DEPENDENT KINASE INHIBITORS AND METHODS OF USE
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Paragraph 127-129, (2016/02/29)
The presently disclosed subject matter relates to methods and compositions for protecting healthy cells from damage due to DNA damaging agents. In particular, the presently disclosed subject matter relates to the protective action of selective cyclin dependent kinase 4/6 (CDK4/6) inhibitors administered to subjects that have been exposed to or that are at risk of exposure to DNA damage.
Pyrimidine or pyridine pyridine ketone compound and its preparation method and application (by machine translation)
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Paragraph 0153, (2016/10/09)
The invention discloses a kind of type I of the pyrimidine or pyridine pyridine ketone compound and its preparation and application, which belongs to the technical field of pharmaceutical preparation. The compounds have high-efficient and selectively inhibit the cell cycle dependent kinases (Cdks) CDK4 and CDK6 active, and then by inhibiting CDK4/CDK6 prevent tumor cell division. Therefore, the compounds of this invention can be used for CDK4 and CDK6 the involved in cell cycle control disorders result in various diseases, especially suitable for the treatment of malignant tumors. (by machine translation)
Pyrido[2,3-d]pyrimidin-7-ones as specific inhibitors of cyclin-dependent kinase 4
VanderWel, Scott N.,Harvey, Patricia J.,McNamara, Dennis J.,Repine, Joseph T.,Keller, Paul R.,Quin III, John,Booth, R. John,Elliott, William L.,Dobrusin, Ellen M.,Fry, David W.,Toogood, Peter L.
, p. 2371 - 2387 (2007/10/03)
Inhibition of the cell cycle kinase, cyclin-dependent kinase-4 (Cdk4), is expected to provide an effective method for the treatment of proliferative diseases such as cancer. The pyrido[2,3-d]-pyrimidin-7-one template has been identified previously as a privileged structure for the inhibition of ATP-dependent kinases, and good potency against Cdks has been reported for representative examples. Obtaining selectivity for individual Cdk enzymes, particularly Cdk4, has been challenging. Here, we report that the introduction of a methyl substituent at the C-5 position of the pyrido[2,3-d]pvrimidin-7-one template is sufficient to confer excellent selectivity for Cdk4 vs other Cdks and representative tyrosine kinases. Further optimization led to the identification of highly potent and selective inhibitors of Cdk4 that exhibit potent antiproliferative activity against human tumor cells in vitro. The most selective Cdk4 inhibitors were evaluated for antitumor activity against MDA-MB-435 human breast carcinoma xenografts in mice.
