936901-72-3

Usage

Uses

Used in Pharmaceutical Industry:
3-(1-chloroH-pyrrolo[1,2-a]pyrazin-6-yl)cyclobutanone is used as a chemical intermediate for the development of novel drugs, leveraging its unique structure to target specific biological pathways and address various disease conditions. Its potential applications in drug discovery make it a valuable asset in the pharmaceutical field, warranting further research and exploration to fully understand its capabilities and optimize its use in medicinal chemistry.

Upstream product

• 23761-23-1 3-oxocyclobutanecarboxylic acid 
• 939412-81-4 3-oxocyclobutanecarboxylic acid 2,5-dioxopyrrolidin-1-yl ester 
• 939412-84-7 N-[(2-chlorophenyl(methyl))]-3-oxocyclobutanecarboxamide 
• 939412-86-9 C-(3-chloropyrazin-2-yl)-methylamine hydrochloride salt 

Relevant academic research and scientific papers

CYCLOALKYLIDENE CARBOXYLIC ACIDS AND DERIVATIVES AS BTK INHIBITORS

The present invention relates to novel cycloalkylidene carboxylic acids and derivatives thereof useful as Bruton tyrosine kinase (BTK) inhibitors. The present disclosure also relates to processes for their preparation, pharmaceutical compositions containing one or more such compounds, and to the use of such compounds and pharmaceutical compositions for the treatment of disorders involving mediation of BTK in humans (Formula I).

PROTEIN KINASE INHIBITORS

The present invention relates to a novel family of protein kinase inhibitors, more specifically the present invention is directed to inhibitors of the Tec or Src protein kinase families. The present invention also relates to the processes of preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative, inflammatory, autoimmune or infectious diseases, disorders, or conditions in which protein kinase activity is implicated.

Discovery of novel insulin-like growth factor-1 receptor inhibitors with unique time-dependent binding kinetics

This letter describes a series of small molecule inhibitors of IGF-1R with unique time-dependent binding kinetics and slow off-rates. Structure-activity and structure-kinetic relationships were elucidated and guided further optimizations within the series

Process to prepare substituted imidazopyrazine compounds

A method of preparing wherein, X=Cl, Br, I, comprises the step of treating with N-chloro-, N-bromo-, or N-iodosuccinimide in a compatible solvent such as dimethylformamide (DMF) at 0-60° C. followed by halogenation.

Combined treatment with an EGFR kinase inhibitor and an agent that sensitizes tumor cells to the effects of EGFR kinase inhibitors

The present invention provides a method for treating NSCL, pancreatic, colon or breast cancer tumors or tumor metastases in a patient, comprising administering to the patient simultaneously or sequentially a therapeutically effective amount of a combination of an EGFR kinase inhibitor and an agent that sensitizes tumor cells to the effects of EGFR kinase inhibitors, wherein the agent is an mTOR inhibitor, with or without additional agents or treatments, such as other anti-cancer drugs or radiation therapy. The present invention also provides a method for treating tumors or tumor metastases in a patient, comprising administering to said patient simultaneously or sequentially a therapeutically effective amount of a combination of an EGFR kinase inhibitor and an agent that sensitizes tumor cells to the effects of EGFR kinase inhibitors, wherein said agent is an mTOR inhibitor that binds to and directly inhibits both mTORC1 and mTORC2 kinases. The present invention also provides a pharmaceutical composition comprising an EGFR kinase inhibitor and an mTOR inhibitor that binds to and directly inhibits both mTORC1 and mTORC2 kinases, in a pharmaceutically acceptable carrier. A preferred example of an EGFR kinase inhibitor that can be used in practicing the methods of this invention is the compound erlotinib HCl (also known as TARCEVA?).