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Inhibitor of protein crosslinking and use of the same

Foreign code F170009213
File No. I018P012WO
Posted date Sep 12, 2017
Country United States of America
Application number 201013508247
Gazette No. 20120277423
Gazette No. 8937091
Date of filing May 19, 2010
Gazette Date Nov 1, 2012
Gazette Date Jan 20, 2015
International application number JP2010058411
International publication number WO2011055561
Date of international filing May 19, 2010
Date of international publication May 12, 2011
Priority data
  • P2009-015978 (Jan 27, 2009) JP
  • P2009-255518 (Nov 6, 2009) JP
  • 2010WO-JP58411 (May 19, 2010) WO
Title Inhibitor of protein crosslinking and use of the same
Abstract (US8937091)
The present invention relates to: a ketone compound having transglutaminase-inhibiting activity, which is represented by the following Formula 1, 2, or 3: wherein R1 is a substituted or unsubstituted aryl or heterocyclyl group, R2, R3, and R4 are hydrogen atoms, n is 2, X is halogen, R5 and R6 independently represent a hydrogen atom or a substituted or unsubstituted C1-C10 alkyl, aryl, or aralkyl group, wherein R5 and R6 are not hydrogen atoms at the same time, or R5 and R6 may 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.
Scope of claims [claim1]
1. A compound represented by the following Formula (3):

wherein: R1 is pyridyl, which is optionally substituted with C1-C4 alkyl or halogen;
R2, R3, and R4 are hydrogen atoms;
R5 is benzyl; and
R6 is hydrogen, C1-C4 alkyl, or hydroxyl C1-C4 alkyl.
[claim2]
2. The compound according to claim 1, wherein the compound is selected from the group consisting of:
[claim3]
3. A pharmaceutical composition, comprising at least one of the compounds of claim 1 and a pharmaceutically acceptable carrier.
  • Inventor, and Inventor/Applicant
  • MIKOSHIBA KATSUHIKO
  • HAMADA KOZO
  • TERAUCHI AKIKO
  • OZAKI SHOUICHIROU
  • GOTO JUN-ICHI
  • EBISUI ETSUKO
  • SUZUKI AKINOBU
  • JAPAN SCIENCE AND TECHNOLOGY AGENCY
IPC(International Patent Classification)
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