337519-98-9

Upstream product

• 98116-49-5 3-cyano-1-(2-formylethenyl)benzene 
• 138227-63-1 tert-butyl 4-(4-aminophenoxy)piperidine-1-carboxylate 
• 123-30-8 4-amino-phenol 
• 109384-19-2 t-butyl 4-hydroxy piperidine-1-carboxylate 
• 100-02-7 4-nitro-phenol 
• 24964-64-5 3-Cyanobenzaldehyde 
• 138227-62-0 tert-butyl 4-(4-nitrophenoxy)piperidine-1-carboxylate 
• 141-78-6 ethyl acetate 
• 475504-76-8 C₂₆H₂₉N₃O₃ 

Downstream Products

• 337520-11-3 3-[3-[N-[4-(1-t-butoxycarbonylpiperidin-4-yloxy)phenyl]-N-(2-hydroxyethyl)amino]-1-(E)-propenyl]benzonitrile 
• 337520-04-4 N-{4-[1-(t-butoxycarbonyl)piperidin-4-yloxy]phenyl}-N-[(E)-3-(3-cyanophenyl)-2-propenyl]-2-hydroxyacetamide 
• 337520-00-0 3-[3-[N-[4-(1-t-Butoxycarbonylpiperidin-4-yloxy)phenyl]-N-ethylamino]-1-(E)-propenyl]benzonitrile 
• 337520-05-5 Ethyl 2-[N-[4-(1-t-butoxycarbonylpiperidin-4-yloxy)phenyl]-N-[3-(3-cyanophenyl)-2-(E)-propenyl]amino]acetate 
• 337520-06-6 Ethyl 2-[N-[4-(1-t-butoxycarbonylpiperidin-4-yloxy)phenyl]-N-[3-(3-cyanophenyl)-2-(E)-propenyl]amino]propionate 
• 337520-03-3 N-{4-[1-(t-butoxycarbonyl)piperidin-4-yloxy]phenyl}-N-[(E)-3-(3-cyanophenyl)-2-propenyl]acetamide 
• 337519-99-0 3-[(E)-3-(N-{4-[1-(t-butoxycarbonyl)piperidin-4-yloxy]phenyl}-N-methylamino)-1-propenyl]benzonitrile 
• 337520-01-1 3-[3-[N-[4-(1-t-butoxycarbonylpiperidin-4-yloxy)phenyl]-N-isopropylamino]-1-(E)-propenyl]benzonitrile 
• 475504-77-9 C₃₀H₃₅N₃O₆ 
• 454437-24-2 3-(3-{4-[(1-tert-butoxycarbonyl-4-piperidyl)oxy]anilino}propyl)benzonitrile 

Relevant academic research and scientific papers

Cinnamyl derivatives: Synthesis and factor Xa (FXa) inhibitory activities

To develop a potent and oral anticoagulant, a series of compounds with cinnamyl moiety was synthesized and their factor Xa (FXa) inhibitory activities were examined. As a result, some cinnamyl derivatives showed potent FXa inhibitory activities in vitro. Among them, compounds with substituent at the 3-position on the central benzene ring represented by (N-{4-[1-(acetimidoyl) piperidin-4-yloxy]-3-chlorophenyl}-N-[(E)-3-(3-amidinophenyl)-2-propenyl] sulfamoyl)acetic acid dihydrochloride (45b) and (N-{4-[1-(acetimidoyl)piperidin- 4-yloxy]-3-carbamoylphenyl}-N-[(E)-3-(3-amidinophenyl)-2-propenyl]sulfamoyl) acetic acid dihydrochloride (45j) exhibited potent FXa inhibitory activities with IC50 values of less than 10 nM in vitro. These compounds also showed potent anticoagulant activities both in vitro and ex vivo. Furthermore, these compounds exhibited no lethal toxicity (30 mg/kg, i.v.).

BENZAMIDINE DERIVATIVES

Benzamidine derivatives of formula (I) or pharmaceutically acceptable salts thereof exhibit excellent inhibitory activity against factor Xa and are useful for treating or preventing blood coagulation disorders: wherein R 1represents a hydrogen atom, a halogen atom, an alkyl group or a hydroxyl group; R 2represents a hydrogen atom, a halogen atom or an alkyl group, R 3represents a hydrogen atom, an optionally substituted alkyl group, an aralkyl group, an optionally substituted alkanoyl group or an optionally substituted alkylsulfonyl group, R 4and R 5 are the same as or different from each other and each represent a hydrogen atom, a halogen atom, an optionally substituted alkyl group, an alkoxy group, a carboxyl group, an alkoxycarbonyl group or an optionally substituted carbamoyl group, and R 6represents a substituted pyrrolidine group or substituted piperidine group.

The discovery of YM-60828: a potent, selective and orally-bioavailable factor Xa inhibitor.

Since Factor Xa (FXa) is well known to play a central role in thrombosis and hemostasis, inhibition of FXa is an attractive target for antithrombotic strategies. As a part of our investigation of a non-peptide, orally available FXa inhibitor, we found tha

Design and synthesis of aminophenol-based factor Xa inhibitors

A novel potent and selective aminophenol scaffold for fXa inhibitors was developed from a previously reported benzimidazole-based naphthylamidine template. The aminophenol template is more synthetically accessible than the benzimidazole template, which si