249292-02-2

Upstream product

• 249292-34-0 1-(5-chloroindol-2-ylsulphonyl)-piperazine 
• 4385-76-6 4-(4-pyridinyl)benzoic acid 
• 78329-47-2 5-chloro-1-(phenylsulfonyl)-1H-indole 
• 17422-32-1 5-chloro-1H-indole 
• 259807-33-5 1-(tert-butoxycarbonyl)-4-[(5-chloro-1-phenylsulfonylindol-2-yl)sulfonyl]piperazine 
• 249292-35-1 5-chloro-1-phenyl-sulfonylindole-2-sulfonyl chloride 
• 259802-91-0 1-[(5-chloroindol-1-phenylsulfonyl-2-yl)sulfonyl]-4-[4-(4-pyridyl)benzoyl]piperazine 

Relevant academic research and scientific papers

Design, synthesis, and biological activity of non-basic compounds as factor Xa inhibitors: SAR study of S1 and aryl binding sites

Compound 7 was identified as the active metabolite of 6 by HPLC and mass spectral analysis. Modification of lead compound 7 by transformation of its N-oxide 6-6 biaryl ring system and fused aromatics produced a series of non-basic fXa inhibitors with excellent potency in anti-fXa and anticoagulant assays. The optimized compounds 73b and 75b showed sub to one digit micromolar anticoagulant activity (PTCT2). Particularly, anti-fXa activity was detected in plasma of rats orally administered with 1 mg/kg of compound 75b.

Heterocyclic derivatives which inhibit factor Xa

The invention relates to heterocyclic derivatives of formula (I), or pharmaceutically-acceptable salts thereof, which possess antithrombotic and anticoagulant properties and are accordingly useful in methods of treatment of humans or animals. The invention also relates to processes for the preparation of the heterocyclic derivatives, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments for use in the production of an antithrombotic or anticoagulant effect.

NOVEL SULFONYL DERIVATIVES

Sulfonyl derivatives represented by the following general formula (I): Q1-Q2-T1-Q3-SO2-QA and drugs containing the same (wherein Q1 is an optionally substituted, saturated or unsaturated, five- or six-membered cyclic hydrocarbon group, a five- or six-membered heterocyclic group, or the like; Q2 is a single band, oxygen, sulfur, C1-C6 alkylene or the like; QA is optionally substituted arylalkenyl, heteroarylalkenyl or the like; and T1 is carbonyl or the like). These compounds have potent FXa-inhibitory effects and promptly exert satisfactory and persistent antithrombotic effects through oral administration, thus being useful as anticoagulant agents little accompanied with side effects.