199863-76-8

Usage

Chemical Structure

It is a pyrimidine derivative.

Functional Groups

Amino group at the 2-position
Hydroxyl group at the 4-position

Pharmaceutical Applications

Studied for anti-inflammatory and anti-arthritic properties
Potential treatment for conditions like rheumatoid arthritis and autoimmune diseases

Research Focus

Investigating its role in modulating the immune response
Potential inhibition of inflammatory cytokines production

Promising Therapeutic Agent

Shows promise for treating a range of inflammatory and autoimmune conditions

Ongoing Research

Continual investigation into its therapeutic potential and mechanisms of action.

Upstream product

• 64670-14-0 methyl 3-cyclopentyl-3-oxopropanoate 
• 24922-00-7 ethyl 3-cyclopentyl-3-oxopropionate 
• 50-01-1 guanidine hydrochloride 

Downstream Products

• 199863-89-3 2-amino-4-chloro-6-cyclopentylpyrimidine 

Relevant academic research and scientific papers

Discovery and SAR of 6-alkyl-2,4-diaminopyrimidines as histamine H 4 receptor antagonists

This report discloses the discovery and SAR of a series of 6-alkyl-2-aminopyrimidine derived histamine H4 antagonists that led to the development of JNJ 39758979, which has been studied in phase II clinical trials in asthma and atopic dermatitis. Building on our SAR studies of saturated derivatives from the indole carboxamide series, typified by JNJ 7777120, and incorporating knowledge from the tricyclic pyrimidines led us to the 6-alkyl-2,4-diaminopyrimidine series. A focused medicinal chemistry effort delivered several 6-alkyl-2,4-diaminopyrimidines that behaved as antagonists at both the human and rodent H4 receptor. Further optimization led to a panel of antagonists that were profiled in animal models of inflammatory disease. On the basis of the preclinical profile and efficacy in several animal models, JNJ 39758979 was selected as a clinical candidate; however, further development was halted during phase II because of the observation of drug-induced agranulocytosis (DIAG) in two subjects.

CHEMICAL COMPOUNDS

The invention is directed to to substituted indazole derivatives. Specifically, the invention is directed to compounds according to Formula I: wherein R1 - R6 and X are defined herein. The compounds of the invention are inhibitors of PDK1 and can be useful in the treatment of disorders characterized by constitutively activated ACG kinases such as cancer and more specifically leukemia and cancers of the breast, colon, and lung. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting PDK1 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.

2-Aminopyrimidine modulators of the histamine H4 receptor

2-Aminopyrimidine compounds are described, which are useful as H4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H4 /su