909712-01-2

Usage

Uses

Used in Pharmaceutical Industry:
(5-bromopyridin-2-yl)(4-methylpiperazin-1-yl)methanone is used as a building block for the synthesis of novel bioactive molecules due to its versatile chemical structure and potential reactivity with biological systems. The presence of bromopyridine and methylpiperazine groups, which are commonly found in pharmaceuticals, indicates its potential for creating new drugs with various biological activities.
Used in Drug Discovery and Development:
(5-bromopyridin-2-yl)(4-methylpiperazin-1-yl)methanone serves as a key component in the development of new drugs, leveraging its compatibility with different biological systems and the known biological activities of its constituent groups. Its potential applications in medicinal chemistry make it a promising candidate for further research and development in the pharmaceutical field.

Upstream product

• 109-01-3 1-methyl-piperazine 
• 30766-11-1 5-bromoisonicotinic acid 
• 137178-88-2 5-bromopyridine-2-carbonyl chloride 

Relevant academic research and scientific papers

Identification of 2-Aminopyrimidine Derivatives as FLT3 Kinase Inhibitors with High Selectivity over c-KIT

Herein, we report two promising compounds 30 and 36 possessing nanomolar FLT3 inhibitory activities (IC50 = 1.5-7.2 nM), high selectivity over c-KIT (>1000-fold), and excellent anti-AML activity (MV4-11 IC50 = 0.8-3.2 nM). Furthermore, these two compounds efficiently inhibited the growth of multiple mutant BaF3 cells expressing FLT3-ITD, FLT3-D835V/F, FLT3-F691L, FLT3-ITD-F691L, and FLT3-ITD-D835Y. Oral administration of 30 and 36 at 6 mg/kg/d could significantly suppress tumor growth in the MV4-11 cell-inoculated xenograft model, exhibiting tumor growth inhibitory rates of 83.5% and 95.1%, respectively. Importantly, 36 could prolong the mouse survival time in the FLT3-ITD-TKD dual mutation syngeneic mouse model (BaF3-FLT3-ITD-D835Y) at a dose of 6 mg/kg p.o. bid/4W. No clear myelosuppression was observed in the treated group of 36 in the MPO strain of zebrafish, even at 10 μM. In summary, our data demonstrated that 36 may represent a promising candidate for the treatment of FLT3 mutant AML.

N2-carbamylaryl-2-aminopyrimidine derivative and medical application thereof

The invention provides an N2-carbamylaryl-2-aminopyrimidine derivative and a medical application thereof. The N2-carbamylaryl-2-aminopyrimidine derivative provided by the invention comprises an optical isomer of the N2-carbamylaryl-2-aminopyrimidine derivative and pharmaceutically acceptable salt thereof. Pharmacodynamic research shows that the traditional Chinese medicine composition has no toxicor side effect, the compound has an FLT3 inhibitory activity. The proliferation inhibition activity is realized on various leukemia cell strains; a medium inhibition effect is achieved on breast cancer cells; moreover, the polypeptide is effective for multiple mutations of AML, such as internal tandem repeat mutation of a near-membrane structural domain and D835 point mutation of an activated ring in a kinase structural domain, almost has no inhibition effect on c-KIT, can overcome drug resistance brought by clinical point mutation, can reduce toxic and side effects of bone marrow inhibition,and can be applied to preparation of antitumor drugs. The structures of the general formulas Ia and Ib of the N2-carbamylaryl-2-aminopyrimidine derivative are shown in the specification,

1,5,7-TRISUBSTITUTED ISOQUINOLINE DERIVATIVES, PREPARATION THEREOF, AND USE THEREOF IN MEDICINES

The present disclosure relates to 1,5,7-trisubstituted isoquinoline derivatives, their preparation and pharmaceutical use. In particular, the present disclosure discloses a compound of formula (I) or a pharmaceutically acceptable salt, stereoisomer, solvate or prodrug thereof, and a preparation method and use thereof. The definitions of the groups in the formula can be found in the specification and claims.

A thiophene and pyrimidine derivatives, its preparation process and its use in medicine

The invention discloses thiophene miazines derivates as well as a preparation method and a medical application thereof. The thiophene miazines derivates are compounds with a general formula I, a general formula II or a general formula III, wherein in the general formulae, Ar is any one of phenyl, halogen-substituted phenyl, C1-6 alkyl-substituted phenyl, biphenylyl, halogen-substituted biphenylyl, naphthyl, pyridyl, thienyl, halogen-substituted thienyl, C1-3 alkyl-substituted thienyl, furyl, halogen-substituted furyl and C1-3 alkyl-substituted furyl, A, D and E are respectively carbon atoms or nitrogen atoms but are not carbon atoms at the same time, and R is R1-NH-. The thiophene miazines derivates provided by the invention can be used for obviously restraining the activity of an EGFR (Epidermal Growth Factor Receptor) and the activity of A431 cells, are expected to be developed as a tyrosine kinase inhibitor, and are extensive in application prospect and medicinal value.

Modification of a dihydropyrrolopyrimidine phosphoinositide 3-kinase (PI3K) inhibitor to improve oral bioavailability

Phosphoinositide 3-kinase (PI3K) is activated in various human cancer cells and well known as a cancer therapy target. We previously reported a dihydropyrrolopyrimidine derivative as a highly potent PI3K inhibitor that has strong tumor growth inhibition in a xenograft model. In this report, we describe further optimization to improve its bioavailability.

3-ARYL-5-SUBSTITUTED-ISOQUINOLIN-1-ONE COMPOUNDS AND THEIR THERAPEUTIC USE

The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain 3-aryl-5-substituted-2H-isoquinolin-1-one compounds that, inter alia, inhibit PARP (e.g., PARP1, TNKS1, TNKS2, etc.

NEW COMPOUNDS 384

The present invention relates to a compound of formula (I) as a free base or a pharmaceutically acceptable salt thereof. The present invention also relates to pharmaceutical formulations containing said compound and to the use of said compound in therapy.

(IMIDAZOLO-5-YL)-2-ANILO-PYRIMIDINES AS AGENTS FOR THE INHIBITION OF CELL PROLIFERATION

Compounds of the formula (I): wherein variable groups are as defined within and a pharmaceutically acceptable salts and in vivo hydrolysable esters are described. Also described are processes for their preparation and their use as medicaments, particularly medicaments for producing a cell cycle inhibitory (anti cell proliferation) effect in a warm blooded animal, such as man.