802541-48-6

Usage

Uses

Used in Pharmaceutical Research:
1,4,4-Trimethyl-7-oxo-4,5,6,7-tetrahydro-1H-indazole-3-carboxylic acid ethyl ester is used as a research compound for the development of new pharmaceuticals, particularly due to its potential as an antifungal and antibacterial agent. Its unique chemical structure allows for the exploration of its therapeutic properties and the creation of novel drug candidates.
Used in Organic Synthesis:
In the field of organic synthesis, 1,4,4-Trimethyl-7-oxo-4,5,6,7-tetrahydro-1H-indazole-3-carboxylic acid ethyl ester is used as a key intermediate or building block. Its reactivity and functional groups make it suitable for the synthesis of complex organic molecules, including those with potential pharmaceutical applications.
Used in Drug Development:
1,4,4-Trimethyl-7-oxo-4,5,6,7-tetrahydro-1H-indazole-3-carboxylic acid ethyl ester is used as a precursor in the development of new drugs. Its derivatives have shown promise in combating fungal and bacterial infections, making it a valuable component in the creation of innovative treatments for various diseases.
Used in Chemical Compound Libraries:
This ester derivative is also utilized in the construction of chemical compound libraries, which are essential for high-throughput screening and the identification of new bioactive molecules. Its inclusion in such libraries aids researchers in discovering new leads and optimizing drug candidates for further development.

Upstream product

• 802541-47-5 ethyl (3-methoxy-6,6-dimethyl-2-oxocyclohex-3-en-1-yl)(oxo)acetate 
• 60-34-4 methylhydrazine 

Relevant academic research and scientific papers

Identification of N,1,4,4-tetramethyl-8-{[4-(4-methylpiperazin-1-yl)phenyl] amino}-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide (PHA-848125), a potent, orally available cyclin dependent kinase inhibitor

The discovery of a novel class of inhibitors of cyclin dependent kinases (CDKs) is described. Starting from compound 1, showing good potency as inhibitor of CDKs but being poorly selective against a panel of serine-threonine and tyrosine kinases, new analogues were synthesized. Enhancement in selectivity, antiproliferative activity against A2780 human ovarian carcinoma cells, and optimization of the physical properties and pharmacokinetic profile led to the identification of highly potent and orally available compounds. Compound 28 (PHA-848125), which in the preclinical xenograft A2780 human ovarian carcinoma model showed good efficacy and was well tolerated upon repeated daily treatments, was identified as a drug candidate for further development. Compound 28 is currently undergoing phase I and phase II clinical trials.

PYRAZOLO-QUINAZOLINE DERIVATIVES,PROCESS FOR THEIR PREPARATION AND THEIR USE AS KINASE INHIBITORS

Pyrazolo-quinazoline derivatives of formula (Ia) or (Ib) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.