Chugai Seiyaku Kabushiki Kaisha

Denki Kagaku Kogyo Kabushiki Kaisha

Akie Honma

Haruhiko Sato

Takashi Emura

Takuya Shiraishi

Takenori Ishizawa

Hitoshi Yoshino

Masateru Ohta

Mitsuaki Nakamura

Kazutaka Tachibana

Koichi Takahashi

Etsuro Onuma

Hiromitsu Kawata

Tadashi Morikawa

Noriyuki Izutani

Kenji Taniguchi

Hitoshi Ikeya

Akira Okamachi

Yoshinobu Higuchi

Tatsuya Tamura

Tatsuya Kato

An imidazole derivative represented by formula (I): wherein Q is: A is hydrogen, halogen, or a substituted or unsubstituted Calkyl group; E is independently selected from a Calkyl group; Rand Rare independently selected from Calkyls; Xand Xare independently selected from O and S; Y is selected from a substituted or unsubstituted arylene group and a substituted or unsubstituted divalent 5- or 6-membered monocyclic or 8- to 10-membered condensed heterocyclic group; Z is &#x2014;CON(&#x2014;Ra)&#x2014;, &#x2014;CO&#x2014;, &#x2014;OOO&#x2014;, &#x2014;NRa&#x2014;C(&#x2550;NH)NRb&#x2014;, &#x2014;NRa&#x2014;C(&#x2550;N&#x2014;CN)NRb&#x2014;, &#x2014;N(&#x2014;Ra)COO&#x2014;, &#x2014;C(&#x2550;NH)&#x2014;, &#x2014;SO&#x2014;, &#x2014;SON(&#x2014;Ra)&#x2014;, &#x2014;SONR&#x2014;, &#x2014;N(&#x2014;Ra)CO&#x2014;, &#x2014;N(&#x2014;Ra)CON(&#x2014;Rb)&#x2014;, &#x2014;N(COR)CO&#x2014;, &#x2014;N(&#x2014;Ra)SO&#x2014;, &#x2014;N(SOR)SO&#x2014;, &#x2014;N(&#x2014;Ra)&#x2014; or &#x2014;N(&#x2014;Ra)SON(&#x2014;Rb)&#x2014;; Ris independently a hydrogen atom, a hydroxyl group, or substituted or unsubstituted group selected from Calkyl group, heterocyclic group, aryl group, Ccycloalkyl group and Ccycloalkenyl group; or salt or prodrug thereof.

Imidazolidine derivative and use thereof

An object of the present invention is to provide a hyaluronic acid-methotrexate conjugate useful as a therapeutic drug for joint disorders. There is provided a hyaluronic acid-methotrexate conjugate useful for the treatment of joint disorders, wherein methotrexate is conjugated with a hydroxy group of hyaluronic acid through a linker containing a peptide chain consisting of 1 to 8 amino acids, and the linker is conjugated with the hyaluronic acid through a carbamate group.

Hyaluronic acid-methotrexate conjugate

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Gotenba, Japan

Akie Honma