1404530-92-2

Usage

Applications

a. Organic synthesis
b. Pharmaceutical applications

Chemical structure

a. Pyrazole ring with a methyl group
b. Aminophenyl ring linked to an ethanone group

Biological activities

Potential anti-inflammatory, analgesic, or antipyretic properties

Usage

a. Scaffold for developing new drugs
b. Key intermediate in the synthesis of pharmaceutical compounds
c. Reference standard in analytical chemistry and pharmacological research

Upstream product

• 5078-55-7 1-[5-methyl-1-(4-nitrophenyl)-1H-pyrazol-4-yl]ethanone 
• 1404530-79-5 ethyl 3-[5-methyl-1-(4-nitrophenyl)-1H-pyrazol-4-yl]-3-oxopropanoate 
• 260973-82-8 5-methyl-1-(4-nitrophenyl)-1H-pyrazole-4-carboxylic acid ethyl ester 
• 134653-70-6 ethyl 2-[(dimethylamino)methylene]-3-oxobutanoate 

Downstream Products

• 1404532-60-0 {3-[4-(4-acetyl-5-methyl-pyrazol-1-yl)phenylcarbamoyl]-5-chloro-indol-1-yl}acetic acid methyl ester 
• 1404532-84-8 {3-[4-(4-acetyl-5-methyl-pyrazol-1-yl)phenylcarbamoyl]-5-chloro-indol-1-yl}acetic acid 

Relevant academic research and scientific papers

N -[6-(4-Butanoyl-5-methyl-1 H -pyrazol-1-yl)pyridazin-3-yl]-5-chloro-1-[2-(4-methylpiperazin-1-yl)-2-oxoethyl]-1 H -indole-3-carboxamide (SAR216471), a Novel Intravenous and Oral, Reversible, and Directly Acting P2Y12 Antagonist

In the search of a potential backup for clopidogrel, we have initiated a HTS campaign designed to identify novel reversible P2Y12 antagonists. Starting from a hit with low micromolar binding activity, we report here the main steps of the optimization process leading to the identification of the preclinical candidate SAR216471. It is a potent, highly selective, and reversible P2Y12 receptor antagonist and by far the most potent inhibitor of ADP-induced platelet aggregation among the P2Y12 antagonists described in the literature. SAR216471 displays potent in vivo antiplatelet and antithrombotic activities and has the potential to differentiate from other antiplatelet agents.

DERIVATIVES OF N-[(1H-PYRAZOL-1-YL)ARYL]-1H-INDOLE OR 1H-INDAZOLE-3-CARBOXAMIDE, PREPARATION THEREOF AND APPLICATIONS THEREOF IN THERAPEUTICS

The present invention relates to compounds corresponding to formula (I): in which: A represents a divalent aromatic radical; X represents a —CH— group or a nitrogen atom; R1 represents a (C1-C4)alkyl or a (C1-C4)alkoxy; R2 represents a group Alk; R3 represents a hydroxyl or a group —NR7R8; R4 represents a hydrogen atom, a halogen atom, a cyano, a phenyl, a group Alk, a group OAlk or a group —NR9R10; R5 represents a hydrogen atom, a halogen atom or a group Alk; R6 represents a hydrogen atom, a halogen atom, a cyano, a group —COOAlk or a —CONH2 group.

DERIVATIVES OF N- [(1H-PYRAZOL-1-YL) ARYL] - 1H - INDOLE OR 1H - INDAZOLE - 3 - CARBOXAMIDE, THEIR PREPARATION AND THEIR USE AS P2Y12 ANTAGONISTS

The present invention relates to compounds corresponding to formula (I) and their use as P2Y12 antagonists for the treatment of cardiovascular diseases.