229646-37-1

Upstream product

• 102153-63-9 6-chloronaphth-2-ylsulfonyl chloride 
• 229647-14-7 1-[[1-(4-pyridinyl)-4-piperidinyl]methyl]piperazinone 
• 239073-00-8 4-Benzyloxycarbonyl-1,2,3,4-tetrahydropyrazin-2-one 
• 239074-30-7 1-(pyridin-4-yl)-4-methylsulfonyloxymethylpiperidine 
• 7440-05-3 palladium 
• 229647-08-9 1-(4-pyridinyl)-4-piperidinecarboxaldehyde 
• 130658-67-2 4-hydroxymethyl-1-(pyridin-4-yl)piperidine 

Relevant academic research and scientific papers

Sulfonamide derivatives, processes for producing the same and utilization thereof

The present invention is to provide a compound or a salt thereof represented by the formula: wherein R1is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, the ring A is an optionally substituted divalent nitrogen-containing heterocyclic group, X′ is an optionally substituted alkylene chain, Y is an optionally substituted divalent cyclic group, X is a chemical bond or an optionally substituted alkylene chain, and Z is (1) an optionally substituted amino group, (2) an optionally substituted imidoyl group or (3) an optionally substituted nitrogen-containing heterocyclic group, or a pro-drug thereof, which have activated coagulation factor X inhibitory activity and which are useful as anti-coagulants.

Synthesis and evaluation of 1-arylsulfonyl-3-piperazinone derivatives as factor Xa inhibitor

Intravascular clot formation is an important factor in a number of cardiovascular diseases. Therefore, the prevention of blood coagulation has become a major target for new therapeutic agents. One attractive approach is the inhibition of factor Xa (FXa), which is a key enzyme in coagulation cascade responsible for the generation of thrombin by limited proteolysis of its zymogen, prothrombin. We have investigated 1-arylsulfonyl-3-piperazinone derivatives, containing a 4-(piperidino)pyridine group in place of guanidino and/or amidino groups, and discovered compound M55113 (30a: 4-[(6-Chloro-2-naphthalenyl)sulfonyl]-1-[[1-(4-pyridinyl)-4-piperidinyl]- methyl]piperazinone), as a potent inhibitor of FXa (IC50=0.06 μM) with high selectivity for FXa over trypsin and thrombin.

AROMATIC COMPOUNDS HAVING CYCLIC AMINO OR SALTS THEREOF

Compounds represented by general formula (I) or salts thereof which specifically inhibit FXa, exert a potent anticoagulant effect and thus are useful as medicinal compositions, wherein G1 to G4, X and Y represent each CH or N; Z1 represents -SO2- or -CH2 -; Q represents aryl or heteroaryl; and R1 to R9 represent each hydrogen or a substituent.