Shionogi Company Limited

Kiyoshi Nagata

Teruo Yamamori

Natsuki Ishizuka

Katsunori Sakai

Kunio Hayashi

Compounds having an activity to enhance the expression of apoAI are provided. Compounds of formula (I): in which Arand Arare independently a phenyl, naphthyl, or monocyclic or bicyclic aromatic heterocyclic group, which may be optionally substituted; &#x2014;X&#x2014; is &#x2014;N&#x2550;CZ&#x2014;, &#x2014;CY&#x2550;CZ&#x2014;, &#x2014;CYY&#x2014;CHZ&#x2014;, &#x2014;S&#x2014;, &#x2014;O&#x2014;, or the like; Y, Y, Y, Zand Zare independently a hydrogen, a halogen, a lower alkyl, a phenyl, or the like; Zand Zmay be independently a linker group that may combine with Arand Arto form a condensed ring; m is 0 or 1, and n is 0 to 2; a prodrug thereof, a pharmaceutically acceptable salt or solvate thereof; are disclosed.

Method of enhancing the expression of apolipoprotein AI using olefin derivatives

Compounds having an activity to enhance the expression of apoAI are provided, which are used as medicaments. Compounds of formula (I): in which ring A and Arare independently a monocyclic or bicyclic aromatic carbocyclic group or aromatic heterocyclic group, each of which may be optionally substituted, or the like; R is a hydrogen or the like; Z is oxygen or the like; Yand Yare a hydrogen, a lower alkyl, or the like; n is an integer of 0 to 2; the broken line is the presence or absence of a bond; and the wavy line represents a cis- or trans-geometrical isomerism with respect to the double bond; are disclosed.

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Osaka, Japan

Kiyoshi Nagata