249292-35-1

Upstream product

• 78329-47-2 5-chloro-1-(phenylsulfonyl)-1H-indole 
• 98-09-9 benzenesulfonyl chloride 
• 1394431-60-7 lithium 5-chloro-1-(phenylsulfonyl)-1H-indole-2-sulfinate 
• 1073-69-4 N-4-chlorophenylhydrazine 
• 17422-32-1 5-chloro-1H-indole 

Downstream Products

• 259808-17-8 1-[(5-chloro-1-phenylsulfonylindol-2-yl)sulfonyl]-3-(2-methylpropyl)piperazine 
• 249292-02-2 1-(5-chloroindol-2-ylsulfonyl)4-[4-(pyridin-4-yl)benzoyl]piperazine 
• 259802-91-0 1-[(5-chloroindol-1-phenylsulfonyl-2-yl)sulfonyl]-4-[4-(4-pyridyl)benzoyl]piperazine 
• 249292-36-2 1-(1-Benzenesulphonyl-5-chloroindol-2-ylsulphonyl)piperazine 
• 1394431-63-0 5-chloro-N-((2',4'-difluorobiphenyl-4-yl)methyl)-1H-indole-2-sulfonamide 
• 1394431-80-1 5-chloro-N-((4'-(methylsulfonyl)biphenyl-4-yl)methyl)-1H-indole-2-sulfonamide 
• 1394431-69-6 5-chloro-N-((3,4'-difluorobiphenyl-4-yl)methyl)-1H-indole-2-sulfonamide 
• 1394431-72-1 5-chloro-N-((4'-fluoro-3-methylbiphenyl-4-yl)methyl)-1H-indole-2-sulfonamide 
• 1394431-61-8 N-(4-bromobenzyl)-5-chloro-1-(phenylsulfonyl)-1H-indole-2-sulfonamide 
• 1394431-68-5 5-chloro-N-((3,4'-difluorobiphenyl-4-yl)methyl)-1-(phenylsulfonyl)-1H-indole-2-sulfonamide 

Relevant academic research and scientific papers

Development of indole sulfonamides as cannabinoid receptor negative allosteric modulators

Existing CB1 negative allosteric modulators (NAMs) fall into a limited range of structural classes. In spite of the theoretical potential of CB1 NAMs, published in vivo studies have generally not been able to demonstrate the expected therapeutically-relevant CB1-mediated effects. Thus, a greater range of molecular tools are required to allow definitive elucidation of the effects of CB1 allosteric modulation. In this study, we show a novel series of indole sulfonamides. Compounds 5e and 6c (ABD1075) had potencies of 4 and 3?nM respectively, and showed good oral exposure and CNS penetration, making them highly versatile tools for investigating the therapeutic potential of allosteric modulation of the cannabinoid system.

N- (ARYLALKYL) - 1H- INDOLE- 2 - SULFONIC ACID AMIDE COMPOUNDS AND THEIR THERAPEUTIC USE AS CANNABINOID ALLOSTERIC MODULATORS

The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain /V-(arylalkyl)-1 H-indole- 2-sulfonic acid amide compounds that, inter alia, inhibit cannabinoid receptor signalling. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit cannabinoid receptor signalling; to treat disorders that are ameliorated by the inhibition of cannabinoid receptor signalling; to treat metabolic syndrome, type-2 diabetes, dyslipidaemia, obesity, eating disorders, cardiovascular diseases and disorders, and other conditions as described herein.

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.

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.