The present invention relates to the compound (E,Z)-ajoene of formula (1) for use in treatment of bacterial infections. Another aspect of the present invention is a composition comprising (E,Z)-ajoene of formula (1) and at least one antibiotic. Yet another aspect of the invention relates to a method for manufacturing (E,Z) ajoene of formula (1) wherein the conformation of the internal CC bond can be either E or Z or a mixture thereof, said method comprising reacting allicin of formula (3) with an acid in the presence of a solvent to provide (E,Z ajoene) of formula (1) as defined above. Yet another aspect of the invention is (E,Z)-ajoene of formula 1 obtainable by the method described above.

The present invention relates to the compound (E,Z)-ajoene of formula (1) for use in treatment of bacterial infections. Another aspect of the present invention is a composition comprising (E,Z)-ajoene of formula (1) and at least one antibiotic. Yet another aspect of the invention relates to a method for manufacturing (E,Z) ajoene of formula (1) wherein the conformation of the internal CC bond can be either E or Z or a mixture thereof, said method comprising reacting allicin of formula (3) with an acid in the presence of a solvent to provide (E,Z ajoene) of formula (1) as defined above. Yet another aspect of the invention is (E,Z)-ajoene of formula 1 obtainable by the method described above.

A process for the preparation of 2-alkyl-4-trifluoromethyl-3-alkylsulfonylbenzoic acids of the formula (I) is described.

##STR00001##

Herein, the substituents are radicals such as alkyl and substituted phenyl.

A process for the preparation of 2-alkyl-4-trifluoromethyl-3-alkylsulfonylbenzoic acids of the formula (I) is described.

##STR00001##

Herein, the substituents are radicals such as alkyl and substituted phenyl.

A process for the preparation of 2-alkyl-4-trifluoromethyl-3-alkylsulfonylbenzoic acids of the formula (I) is described.

##STR00001##

Herein, the substituents are radicals such as alkyl and substituted phenyl.

The present invention relates to a process for producing ajoene from allicin via a polymeric substrate, comprising the steps of heating allicin or an allicin solution at a predetermined temperature range such that at least a portion of the allicin is converted to ajoene to form an ajoene solution; and separating the ajoene from the ajoene solution; wherein at least one of the heating or separating steps is conducted via a polymeric substrate. The process for producing ajoene from allicin via a polymeric substrate further comprises a step of retaining the allicin or the allicin solution on the polymeric substrate before the heating step is conducted within or out of the polymeric substrate. The present invention also relates to ajoene or a composition comprising ajoene obtained by the process thereof.

The present invention relates to a process for producing ajoene from allicin via a polymeric substrate, comprising the steps of heating allicin or an allicin solution at a predetermined temperature range such that at least a portion of the allicin is converted to ajoene to form an ajoene solution; and separating the ajoene from the ajoene solution; wherein at least one of the heating or separating steps is conducted via a polymeric substrate. The process for producing ajoene from allicin via a polymeric substrate further comprises a step of retaining the allicin or the allicin solution on the polymeric substrate before the heating step is conducted within or out of the polymeric substrate. The present invention also relates to ajoene or a composition comprising ajoene obtained by the process thereof.

Aromatic entities that modulate HIF-2 activity, pharmaceutical compositions containing the aromatic entities, and methods of using these chemical entities for treating proliferative diseases and conditions associated with HIF-2 activity are described herein.

Aromatic entities that modulate HIF-2 activity, pharmaceutical compositions containing the aromatic entities, and methods of using these chemical entities for treating proliferative diseases and conditions associated with HIF-2 activity are described herein.

The present disclosure is generally directed to compositions and methods for treating diseases that are ameliorated by the inhibition of CYP26 mediated retinoic acid metabolism. The compositions comprise compounds of formula (I). A repreid50000060307390 IB/345 nullsents aryl optionally substituted with one, two, three, or four groups that are each independently halogen, cyano, nitro, C.sub.1-6 alkyl, C.sub.1-6 haloalkyl, NH.sub.2, NH(C.sub.1-C.sub.6 alkyl), N(C.sub.1-C.sub.6 alkyl).sub.2, OH, C.sub.1-C.sub.6 alkoxy, and C.sub.1-C.sub.6 haloalkoxy; X is a bond, CH.sub.2, CHR.sup.5, CCHR.sup.4, NR.sup.4, NOR.sup.4, O, S, SO, SO.sub.2, C(O), or C(NR.sup.4), or X is of formula (a), (b) or (c), wherein each n is independently 1, 2, or 3; each R.sup.4 is independently hydrogen or C.sub.1-6 alkyl; R.sup.5 is independently hydrogen, C.sub.1-6 alkyl, or OR.sup.6, where R.sup.6 is selected from the group consisting of hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyL C.sub.3-12 cycloalkyl, heterocyclyl, aryl, arylC.sub.1-6 alkyl, heteroaryl, or heteroarylC.sub.1-6 alkyl; Y is C.sub.1-6 alkylene, C.sub.2-6 alkenylene, or C.sub.2-6 alkylylene moiety. ##STR00001##