Avexxin As

Inger-Reidun Aukrust

Berit Johansen

George Kokotos

Marcel Sanderberg

Marcel Sandberg

Thomas Brimert

Geir Kildahl-Andersen

Efrosini Barbayianni

Johan Evenäs

Kildahl-Andersen Geir

A compound of formula (I) wherein X is 0, C=0 or S; Y is N or CH; Rand Rare each independently H, &#x2014;(CH)COOH, &#x2014;(CH)CON(R)or &#x2014;(CH)COOCalkyl; or Rand Rtogether form a 6-membered phenyl ring fused to the five membered ring; each Ris independently selected from H, halo (e.g. fluoro or chloro), Caryl, Carylalkyl, Calkenyl; OCalkyl, OCalkenyl or a Calkyl group; each Ris H or Calkyl; each p is 0 to 3; n is 1 to 4; or a salt, ester, solvate, N-oxide, or prodrug thereof, e.g. a salt thereof.

Anti-inflammatory and antitumor 2-oxothiazoles and 2-oxothiophenes compounds

A compound of formula (I) wherein X is O, C&#x2550;O or S;

A compound of formula (I') wherein Ris H, Calkyl, &#x2014;(CH)COOH, &#x2014;(CH)COOCalkyl, &#x2014;(CH)CONH, &#x2014;(CH)CONHCalkyl, &#x2014;(CH)CON(Calkyl), Ris as defined for R; or and Rtaken together with the atoms joining them can form a 6-membered aromatic or non aromatic, saturated or unsaturated, carbocyclic or heteroatom containing (e.g. O, N or S containing) ring optionally substituted by up to 4 groups R; each Ris defined as for Ror is oxo; Ris Calkyl Ar is a Caryl group, wherein the aryl group may be optionally substituted (preferably in the meta or para position relative to O) with one or more Rgroups; each Ris halo, OH, CN, nitro, NH, NHCalkyl, N(Calkyl), haloCalkyl, Caryl group, Carylalkyl, a Calkyl group, C-mono or multiply unsaturated alkenyl group, OCalkyl group, SCalkyl group &#x2014;OCalkyl-O&#x2014;Calkyl, &#x2014;Calkyl-O&#x2014;Calkyl, &#x2014;OC-mono or multiply unsaturated alkenyl group, OAr, O(CH)Ar, SAror S(CH)Ar; wherein Aris phenyl, optionally substituted with one or more of halo, trihalomethyl, C-alkoxy, or Calkyl; each q is 1 to 3, preferably 1; each p is 0 to 3; or a salt, ester, solvate, N-oxide, or prodrug thereof. 

2-oxothiatole compounds having activity as cPLAinhibitors for the treatment of inflammatory disorders and hyperproliferative disorders

Anti-inflammatory and antitumor 2-oxothiazoles ABD 2-oxothiophenes compounds

A process for the preparation of a polyunsaturated thiol comprising: 

Process for the preparation of a polyunsaturated ketone compound

2-oxothiatole compounds having activity as CPLA2 inhibitors for the treatment of inflammatory disorders and hyperproliferative disorders

The invention relates to the manufacture of certain polyunsaturated compounds employing a particular application of the Mitsonobu reaction in the presence of at least one anti-oxidant. We have found a method of making a pharmaceutically-acceptable polyunsaturated ester or thioester compound directly, which can ultimately be converted to the advantageous ketone compounds, in which unwanted oxidation and cis/trans isomerization are substantially reduced or eliminated using particular Mitsonobu chemistry.

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Oslo, Norway

Inger-Reidun Aukrust