Japan Science and Technology Agency

Jun-ichi Goto

Katsuhiko Mikoshiba

Akinobu Suzuki

Akiko Terauchi

Etsuko Ebisui

Shoichiro Ozaki

Kouzo Hamada

Kozo Hamada

Shouichirou Ozaki

Nobuyuki Nukina

The present invention relates to: a ketone compound having transglutaminase-inhibiting activity, which is represented by the following Formula 1, 2, or 3: wherein Ris a substituted or unsubstituted aryl or heterocyclyl group, R, R, and Rare hydrogen atoms, n is 2, X is halogen, Rand Rindependently represent a hydrogen atom or a substituted or unsubstituted C1-C10 alkyl, aryl, or aralkyl group, wherein Rand Rare not hydrogen atoms at the same time, or Rand Rmay be taken together to form a saturated or unsaturated and substituted or unsubstituted heterocyclyl group containing a nitrogen atom (N); an inhibitor of protein crosslinking comprising the compound; and a composition for preventing or treating a protein-crosslinking causative disease, which comprises the compound or the protein crosslinking inhibitor.

Inhibitor of protein crosslinking and use of the same

The present invention provides a protein cross-linking inhibitor containing a compound represented by any of the following formulas (1)-(13), or a pharmaceutically acceptable salt thereof:R&#x2014;[&#x2014;X&#x2014;B(ZR)&#x2014;Y&#x2014;B(ZR)&#x2014;W&#x2014;]&#x2014;R,&#x2003;&#x2003;(1)R&#x2014;[&#x2014;X&#x2014;B(ZR)&#x2014;Y&#x2014;]&#x2014;R,&#x2003;&#x2003;(2)R&#x2014;[&#x2014;B(ZR)&#x2014;Y&#x2014;B(ZR)&#x2014;W&#x2014;]&#x2014;R,&#x2003;&#x2003;(3)R&#x2014;[&#x2014;X&#x2014;B(ZR)&#x2014;]&#x2014;R,&#x2003;&#x2003;(4)R&#x2014;[&#x2014;B(ZR)&#x2014;W&#x2014;]&#x2014;R,&#x2003;&#x2003;(5)R&#x2014;X&#x2014;B(ZR)-T[B(ZR)&#x2014;W&#x2014;R],&#x2003;&#x2003;(6)R&#x2014;B(OH),&#x2003;&#x2003;(7)R&#x2014;B(ZR)&#x2014;X&#x2014;B(ZR)&#x2014;R,&#x2003;&#x2003;(8)R&#x2014;B(R)&#x2014;O&#x2014;B(R)&#x2014;R,&#x2003;&#x2003;(9)R&#x2014;[&#x2014;X&#x2014;B(ZR)&#x2014;Y&#x2014;B(ZR)&#x2014;]&#x2014;R,&#x2003;&#x2003;(10)R&#x2014;[&#x2014;X&#x2014;B(ZR)&#x2014;Y&#x2014;B(ZR)&#x2014;W-Q-]&#x2014;R,&#x2003;&#x2003;(11)R&#x2014;[&#x2014;P&#x2014;X&#x2014;B(ZR)&#x2014;Y&#x2014;B(ZR)&#x2014;W&#x2014;]&#x2014;R,&#x2003;&#x2003;(12)[R&#x2014;X&#x2014;B(ZR)&#x2014;Y]B(ZR),&#x2003;&#x2003;(13)wherein each symbol is as defined in the DESCRIPTION.

Protein cross-linking inhibitor

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Saitama, Japan

Jun-ichi Goto