162011-74-7

Upstream product

• 132470-25-8 1-(4-Fluorophenyl)-2-(4-(methylsulfonyl)phenyl)ethanone 
• 90536-66-6 4-(methylsulfonyl)phenylacetic acid 
• 462-06-6 fluorobenzene 
• 74426-50-9 (4-methylsulfonylphenyl)acetyl chloride 

Downstream Products

• 177754-49-3 2-benzylthio-5-(4-fluorophenyl)-4-[4-(methylsulfonyl)phenyl]imidazole 
• 177754-50-6 4-(4-fluorophenyl)-2-hydroxymethyl-5-(4-methylsulfonylphenyl)-1H-imidazole 
• 177755-44-1 5-(4-fluorophenyl)-2-hydroxymethyl-4-(4-methylthiophenyl)-1H-imidazole 
• 177755-42-9 5-(4-fluorophenyl)-4-(4-methylthiophenyl)-1-(1-methyl-1-ethoxymethyl)-1H-imidazole 
• 177755-43-0 5-(4-fluorophenyl)-4-(4-methylthiophenyl)-1H-imidazole-2-carboxaldehyde 
• 177754-42-6 5-(4-fluorophenyl)-4-(4-(methylsulfonyl)phenyl)-2-(trifluoromethyl)-1H-imidazole 
• 177560-60-0 ethyl 4-[[5-[(4-methylsulfonyl)phenyl]-4-(4-fluorophenyl)-2-thiazolyl]amino]benzoate 
• 177560-57-5 5-[(4-methylsulfonyl)phenyl]-4-(4-fluorophenyl)-2-(N-(3,5-dichlorophenyl)amino)thiazole 
• 177560-53-1 5-[(4-methylsulfonyl)phenyl]-4-(4-fluorophenyl)-2-(N-methylamino)thiazole 
• 177560-52-0 5-[(4-methylsulfonyl)phenyl]-4-(4-fluorophenyl)-2-(N-butylamino)thiazole 
• 177560-51-9 5-[(4-methylsulfonyl)phenyl]-4-(4-fluorophenyl)-2-(N-hexylamino)thiazole 
• 177560-35-9 4-(4-fluorophenyl)-5-[(4-methylsulfonyl)phenyl]-2-(1-piperidinyl)thiazole 
• 177561-25-0 2-(cyanomethyl)-4-(4-fluorophenyl)-5-(4-methylthiophenyl)-thiazole 
• 177560-58-6 2-(4-cyanophenylamino)-4-(4-fluorophenyl)-5[4-(methylsulfonyl)phenyl]thiazole 

Relevant academic research and scientific papers

2,3-Diaryl-substituted indole based COX-2 inhibitors as leads for imaging tracer development

A series of 2,3-diaryl-substituted indoles containing a fluorine or methoxy group was synthesized via Fischer indole synthesis, McMurry cyclization, or Bischler-Moehlau reaction to identify potential leads for positron emission tomography (PET) radiotracer development as well as for optical imaging. All 2,3-diaryl-substituted indoles possess autofluorescent properties with an emission maximum in a range of 443-492 nm, which is acceptable for biological studies in vitro and, in part, in vivo. The molecular structure of compounds 3a and 3j was confirmed by X-ray crystal structure analysis. COX inhibitory activity was evaluated by a fluorescence-based and enzyme immunoassay-based assay. Redox activity of all target compounds was also determined. All synthesized 2,3-diaryl-substituted indoles are inhibitors of COX-2 enzyme in the low micromolar range. Compounds 3e, 3f, 3g and 3m displayed a 30-40% inhibition of COX-2 at 0.1 μM concentration while compounds 3f and 3g also exhibited COX-1 inhibitory activity. Various compounds like 3g showed substantial antioxidative potential (RDIENE = 2.85, RHAVA = 1.98), an effect that was most measurable with methoxy-substituted compounds. With respect to PET radiotracer synthesis, OMe-containing compound 3j was selected as a promising candidate for carbon-11 labeling, and F-containing compound 3m as a lead for the development of a fluorine-18 labeled derivative. the Partner Organisations 2014.

1,2-Diaryl-1-ethanone and pyrazolo [4,3-c] quinoline-4-one as novel selective cyclooxygenase-2 inhibitors

Novel 1,2-diaryl-1-ethanone 1 and pyrazolo [4,3-c] quinoline-4-one 2, with pharmacophores different from the known COX inhibitors were identified as selective COX-2 inhibitors. The communication briefly describes SAR of both the series.

Substituted imidazo 1,2a}azines as selective inhibitors of cox-2

The invention refers to new compounds of formula (I), wherein A and B are selected from the group consisting of N and CH, with the condition that when A is N, B is N; R1is selected from the group consisting of CH3and NH2;

SUBSTITUTED IMIDAZO 1,2A]AZINES AS SELECTIVE INHIBOTORS OF COX-2

The invention refers to new compounds of formula (I), wherein A and B are selected from the group consisting of N and CH, with the condition that when A is N, B is N; R1 is selected from the group consisting of CH3 and NH2; R2 and R3 are selected from the group consisting of H, CH3, Br, Cl, COCH3 and OCH3; and R4, R5 and R6, are selected from the group consisting of H, F, Cl, Br, (C1-C3)-alkyl, trifluoromethyl, (C1-C3)-alkoxy and trifluoromethoxy. Compounds of formula (I) are prepared by reaction of a substituted aminoazine with a substituted 2-bromo-2-(4-R1-sulfonylphenyl)-1-phenylethanone in a polar solvent. These new compounds inhibit COX-2 with high selectivity over COX-1. They are useful for the treatment of inflamation and/or cyclooxygenase-mediated diseases, having the additional advantage of a reduced potencial for ulcerogenic effects.

Phenyl heterocycles as cox-2 inhibitors

The invention encompasses the novel compound of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases. STR1 The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.

Use of inhibitors of cyclooxygenase in the treatment of neurodegenerative diseases

The present invention provides a method of treating a neurodegenerative disease and in particular Alzheimers disease which comprises administering to a human in need thereof a therapeutically effective amount of a non-steroid COX-II inhibitor. Although a wide range of COX-II inhibitors may be employed but it is preferred to employ compounds of the Formula I: STR1

Benzenesulfonamide subtituted imidazolyl compounds for the treatment of inflammation

A class of imidazolyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula II STR1 wherein R1 is selected from lower alkyl, lower haloalkyl, lower hydroxyalkyl, lower aralkenyl, lower aryloxyalkyl, lower arylthioalkyl and heteroaryl; wherein R3 is selected from lower alkyl and amino; and wherein R4 is one or more radicals selected from hydrido, halo, lower alkyl and lower alkoxy; or where R4 together with the phenyl radical forms naphthyl or benzodioxolyl; provided R1 is not lower alkyl when R3 is methyl and when R4 is hydrido, methyl, methoxy or chloro; or a pharmaceutically-acceptable salt thereof.

Substituted thiazoles for the treatment of inflammation

A class of substituted thiazolyl compounds is described for use in treating inflammation disorders. Compounds are defined by Formula II STR1 wherein R1 is selected from hydrido, alkyl, haloalkyl, cyanoalkyl, alkylamino, aralkyl, arylamino, heteroarylsulfonylalkyl, heteroarylsulfonylhaloalkyl, aralkylamino, aryloxyalkyl, alkoxycarbonyl, aryl optionally substituted at a substitutable position with one or more radicals selected from halo and alkoxy, and heterocyclic optionally substituted at a substitutable position with one or more radicals selected from halo and alkyl; wherein R4 is selected from alkyl and amino; and wherein R5 is selected from aryl and heteroaryl; wherein R5 is optionally substituted at a substitutable position with one or more radicals selected from halo, alkyl and alkoxy; provided R5 is not phenyl at position 4 when R1 is α,α-bis(trifluoromethyl)methanol and R4 is methyl; or a pharmaceutically-acceptable salt thereof.

Aryl substituted 5,5 fused aromatic nitrogen compounds as anti-inflammatory agents

The invention encompasses the novel compound of Formula I as well as a method of treating cyclooxygenase-2 mediated diseases comprising administration to a patient in need of such treatment of a non-toxic therapeutically effective amount of a compound of Formula I. STR1 The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.

Phenyl heterocycles as cox-2 inhibitors

The invention encompasses the novel compound of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases, STR1 The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.