59039-17-7

Upstream product

• 109-01-3 1-methyl-piperazine 
• 63186-59-4 10,11-dihydro-dibenzo[b,f]thiepine-3,11-diol 
• 124-63-0 methanesulfonyl chloride 
• 54533-09-4 N,N-bis(2-chloroethyl)methanesulfonamide 
• 74-89-5 methylamine 

Downstream Products

• 110417-56-6 2-((4-methylpiperazin-1-yl)sulfonyl)-1-phenylethan-1-one 
• 130178-94-8 1-Methyl-4-[2-(4-trifluoromethyl-phenyl)-ethynesulfonyl]-piperazine 
• 130178-97-1 1-Methyl-4-[2-(4-nitro-phenyl)-ethynesulfonyl]-piperazine 
• 130178-96-0 1-[2-(3,4-Dimethoxy-phenyl)-ethynesulfonyl]-4-methyl-piperazine 
• 130178-92-6 1-[2-(2,4-Dichloro-phenyl)-ethynesulfonyl]-4-methyl-piperazine 
• 130178-95-9 1-[2-(4-tert-Butyl-phenyl)-ethynesulfonyl]-4-methyl-piperazine 
• 130178-90-4 1-[2-(2-Chloro-phenyl)-ethynesulfonyl]-4-methyl-piperazine 
• 130214-76-5 1-[2-(4-Methoxy-phenyl)-ethynesulfonyl]-4-methyl-piperazine 
• 130178-91-5 1-[2-(4-Chloro-phenyl)-ethynesulfonyl]-4-methyl-piperazine 
• 130178-93-7 1-[2-(4-Fluoro-phenyl)-ethynesulfonyl]-4-methyl-piperazine 
• 130179-09-8 2-(4-Methyl-piperazine-1-sulfonyl)-1-(4-trifluoromethyl-phenyl)-ethanone 
• 130179-13-4 2-(4-Methyl-piperazine-1-sulfonyl)-1-(4-nitro-phenyl)-ethanone 
• 130179-12-3 1-(3,4-Dimethoxy-phenyl)-2-(4-methyl-piperazine-1-sulfonyl)-ethanone 
• 130179-08-7 1-(2,4-Dichloro-phenyl)-2-(4-methyl-piperazine-1-sulfonyl)-ethanone 

Relevant academic research and scientific papers

3-SUBSTITUTED CARBONYL-NAPHTHO[2,3-B]FURANE DERIVATIVE OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF

The present invention provides a compound of the following Formula (1) or a pharmaceutically acceptable salt thereof: Formule (i) wherein X is an oxygen atom and the like; Y is -CO-, -S02-and the like; R1 is an optionally- substituted C1-6 alkyl group, an optionally-substituted C1-6 alkylcarbonyl group and the like; R2 is an optionally- substituted C1-6 alkyl group, an optionally-substituted C1-6 alkoxy group, an optionally-substituted amino group, an optionally-substituted 5- to 12-membered monocyclic or polycyclic saturated heterocyclic group and the like; R3, R4, R5, and R6 are independently a hydrogen atom and the like which exhibits excellent effects in suppressing the proliferation and sphere-forming ability of cancer cells, and can be useful as an antitumor drug or cell growth inhibitor.

Hepatoselectivity of statins: Design and synthesis of 4-sulfamoyl pyrroles as HMG-CoA reductase inhibitors

4-Sulfamoyl pyrroles were designed as novel hepatoselective HMG-CoA reductase inhibitors (statins) to reduce myalgia, a statin-induced adverse effect. The compounds were prepared via a [3 + 2] cycloaddition of a Muenchnone with a sulfonamide-substituted alkyne. We identified compounds with greater selectivity for hepatocytes compared to L6-myocytes than rosuvastatin and atorvastatin. There was an inverse correlation of myocyte potencies and C log P values. A number of analogs were effective at reducing cholesterol in acute and chronic in vivo models but they lacked sufficient chronic in vivo activity to warrant further development.

CHEMICAL COMPOUNDS

Compounds of formula (I):wherein variable groups are as defined within; for use in the inhibition of 11betaHSD1 are described

4-(1-hydroxy-2-N-substituted sulfonamido) ethyl-5-hydroxy-2(5H)-furanones and 4-(N-substituted sulfonamido)-2-ethenyl-5-hydroxy-2(5H)-furanones as anti-inflammatory agents

Compounds of Formula 1, and of Formula 2, STR1 in which R1 is H or alkyl of 1 to 20 carbons, CO--R1* CO--O--R1* CO--NH--R1* or PO(OR1*)2 or PO(OR