36187-57-2

Upstream product

• 462-06-6 fluorobenzene 
• 63327-11-7 4-methylthiophenyl acetic chloride 
• 177755-36-1 2-(4-fluorophenyl)-3-(4-methylthiophenyl)propenoic acid 
• 75-65-0 tert-butyl alcohol 
• 405-51-6 4-fluorophenyl acetate 
• 7677-24-9 trimethylsilyl cyanide 
• 874-87-3 1-(chloromethyl)-4-methylthiobenzene 
• 459-57-4 4-fluorobenzaldehyde 
• 7647-01-0 hydrogenchloride 
• 100-68-5 methyl-phenyl-thioether 

Downstream Products

• 204512-50-5 (Z)-3-Chloro-3-(4-fluoro-phenyl)-2-(4-methylsulfanyl-phenyl)-propenal 
• 132470-23-6 cis,trans-3-chloro-3-(4-fluorophenyl)-2-(4-(methylthio)phenyl)propenal 
• 165252-26-6 3-amino-2-(4-fluorophenyl)-1-[4-(methylthio)phenyl]-4,4,4,-trifluoro-2-butenone 
• 132470-25-8 1-(4-Fluorophenyl)-2-(4-(methylsulfonyl)phenyl)ethanone 
• 177561-18-1 1-(4-methylthiophenyl)-2-bromo-2-(4-fluorophenyl)-1-ethanone 
• 71006-38-7 1-(4-fluorophenyl)-2-(4-methylthiophenyl)-2-bromoethanone 
• 221057-71-2 3-(4-Fluorobenzoyl)-3-(4-methylthiophenyl)propionic acid, ethyl ester 
• 140403-87-8 5-(4-fluorophenyl)-4-[4-(methylsulfonyl)phenyl]thiophene-2-sulfonic acid 
• 140402-47-7 methyl 5-(4-fluorophenyl)-4-[4-(methylsulfonyl)phenyl]thiophene-2-acetate 

Relevant academic research and scientific papers

PROSTAGLANDIN ENDOPEROXIDE H SYNTHASE BIOSYNTHESIS INHIBITORS

The present invention describes pyridazinone compounds which are cyclooxygenase (COX) inhibitors, and in particular, are selective inhibitors of cyclooxygenase-2 (COX-2). COX-2 is the inducible isoform associated with inflammation, as opposed to the constitutive isoform, cyclooxygenase-1 (COX-1) which is an important "housekeeping" enzyme in many tissues, including the gastrointestinal (GI) tract and the kidneys. The selectivity of these compounds for COX-2 minimizes the unwanted GI and renal side-effects seen with currently marketed non-steroidal anti-inflammatory drugs (NSAIDs).

CHEMICAL COMPOUNDS

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

Synthesis and biological evaluation of 2-phenylpyran-4-ones: A new class of orally active cyclooxygenase-2 inhibitors

A series of 2-phenylpyran-4-ones were prepared and evaluated for their ability to inhibit cyclooxygenase-2 (COX-2). Extensive structure-activity relationship work was carried out within this series, and a number of potent and selective COX-2 inhibitors were identified. Compounds having a p-methylsulfone group at the 2-phenyl ring showed the best COX-2 inhibitory activity. The introduction of a substituted phenoxy ring at position 3 enhanced both the in vitro and in vivo activity within the series. A selected group of 3-phenoxypyran-4-ones exhibited excellent activity in an experimental model of pyresis. The in vivo antiinflammatory activity of these compounds was confirmed with the evaluation of their antiarthritic and analgesic effectiveness. Moreover, their pharmacokinetic profile in rats is compatible with a once a day administration by oral route in humans. Within this novel series, compounds 21, 31, 34, and 35 have been selected for further preclinical and clinical evaluation.

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;

Prostaglandin endoperoxide H synthase biosynthesis inhibitors

The present invention describes pyridazione compounds having the formula (I), which are cyclooxygenase (COX) inhibitors The compounds are selective inhibitors of cyclooxygenase-2-(COX-2), which is the inducible isoform associated with inflammation, as opposed to the constitutive isoform, cyclooxygenase-1 (COX-1), which is an important “housekeeping” enzyme in many tissues, including the gastrointestinal (GI) tract and the kidneys. The selectivity of these compounds for COX-2 minimizes the unwanted GI and renal side-effects seen with currently marketed non-steroidal anti-inflammatory drugs (NSAIDS).

5-arylpyrrole derivatives

The present invention provides compounds represented by the general formula (I): and a salt thereof, and anti-inflammatory agents and antitumor agents containing the compounds as the active ingredients.

Phosphonic acids derivatives as inhibitors of protein tyrosine phosphate 1B (PTP-1B)

The invention encompasses the novel class of compounds represented by formula I which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions and methods of treating or preventing PTP-1B mediated diseases.

2,3-substituted pyridines for the treatment of inflammation

A class of substituted pyridyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula II wherein R1 is selected from hydrido, halo, alkoxy, haloalkoxy, aryl, alkylthio, alkylamino, aralkoxy, azido and alkenyloxy; wherein R2 is selected from hydrido, cyano, hydroxyalkyl, haloalkyl, aminoalkyl, alkylaminoalkyl, alkylcarbonyloxyalkyl, aminocarbonyl and alkylcarbonylaminoalkyl; and wherein R5 and R6 are one or more radicals independently selected from halo, alkylsulfonyl, aminosulfonyl, alkoxy and alkylthio; provided one of R5 and R6 is substituted with alkylsulfonyl, aminosulfonyl, or haloalkylsulfonyl; or a pharmaceutically-acceptable salt thereof.

Substituted oxazolyl compounds for the treatment of inflammation

A class of substituted oxazolyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula I: STR1 wherein R is selected from alkyl, hydroxyalkyl, haloalkyl, cycloalkyl, cycloalkylalkyl, aryl optionally substituted at a substitutable position by carboxy, alkyl, alkoxy and halo, aralkyl optionally substituted at a substitutable position on the aryl radical by carboxy, alkyl, alkoxy and halo, aryloxyalkyl optionally substituted at a substitutable position on the aryl radical with halo, carboxy, alkyl and alkoxy, aralkoxyalkyl optionally substituted at a substitutable position by alkyl, carboxy, alkoxy and halo, heteroaryloxyalkyl optionally substituted at a substitutable position with halo, carboxy, alkyl and alkoxy, alkoxycarbonylalkyl, carboxyalkyl and aminocarbonylalkyl; wherein R1 is selected from cycloalkyl, cycloalkenyl, heteroaryl and aryl optionally substituted at a substitutable position by alkyl, alkoxy and halo, and wherein R2 is alkyl; or a pharmaceutically-acceptable salt thereof; provided R1 is not phenyl when R2 is methyl and R is isopropyl or tert-butyl.

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.