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Protein cross-linking inhibitor

Foreign code F110005822
File No. I018P010WO1
Posted date Oct 19, 2011
Country United States of America
Application number 200913058647
Gazette No. 20110212919
Gazette No. 8853424
Date of filing Aug 11, 2009
Gazette Date Sep 1, 2011
Gazette Date Oct 7, 2014
International application number JP2009064206
International publication number WO2010018837
Date of international filing Aug 11, 2009
Date of international publication Feb 18, 2010
Priority data
  • P2008-207315 (Aug 11, 2008) JP
  • 2009WO-JP64206 (Aug 11, 2009) WO
Title Protein cross-linking inhibitor
Abstract (US8853424)
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: R3―[―X―B(ZR1)―Y―B(ZR2)―W―]n―R4,  (1) R3―[―X―B(ZR1)―Y―]n―R4,  (2) R3―[―B(ZR1)―Y―B(ZR2)―W―]n―R4,  (3) R3―[―X―B(ZR1)―]n―R4,  (4) R3―[―B(ZR2)―W―]n―R4,  (5) R3―X―B(ZR1)-T[B(ZR2)―W―R4]2,  (6) R3―B(OH)2,  (7) R3―B(ZR1)―X―B(ZR2)―R4,  (8) R3―B(R1)―O―B(R2)―R4,  (9) R3―[―X―B(ZR1)―Y―B(ZR2)―]n―R4,  (10) R3―[―X―B(ZR1)―Y―B(ZR2)―W-Q-]n―R4,  (11) R3―[―P―X―B(ZR1)―Y―B(ZR2)―W―]n―R4,  (12) [R3―X―B(ZR1)―Y]2B(ZR2),  (13) wherein each symbol is as defined in the DESCRIPTION.
Scope of claims [claim1]
1. A compound of formula (8')
R3' -- B(ZR1') -- X' -- B(ZR2') -- R4' (8')
wherein B is a boron atom,
Z is O,
R1' and R2' are H, -- (CH2)m -- NH2, -- CH2R12' wherein R12' is pyrrolidinyl, -- COCH(NH2) -- (CH2)mNHCONH2, or -- COCH(NH2) -- (CH2)m -- CONH2, and m is an integer of 1 to 5,
R3' and R4' are phenyl or thienyl, and
X' is a 2,8-dibenzothiophenyl group,
or a pharmaceutically acceptable salt thereof.
[claim2]
2. The compound according to claim 1, which is any of

or a pharmaceutically acceptable salt thereof.
[claim3]
3. The compound according to claim 1 of the formula

or a pharmaceutically acceptable salt thereof.
[claim4]
4. A protein cross-linking inhibitor comprising the compound according to claim 1, or a pharmaceutically acceptable salt thereof.
[claim5]
5. The inhibitor according to claim 4, wherein the inhibition is polyglutamine aggregation inhibition.
[claim6]
6. A therapeutic drug for a disease caused by cross-linking of protein, comprising the compound according to claim 1, or a pharmaceutically acceptable salt thereof, wherein the disease is selected from Alzheimer's disease, Parkinson's disease, and mad cow disease.
[claim7]
7. A polyglutamine aggregation inhibitor comprising the compound according to claim 1, or a pharmaceutically acceptable salt thereof.
[claim8]
8. A therapeutic drug for a disease caused by polyglutamine aggregation, comprising the compound according to claim 1, or a pharmaceutically acceptable salt thereof, wherein the disease is Huntington's disease.
  • Inventor, and Inventor/Applicant
  • MIKOSHIBA KATSUHIKO
  • NUKINA NOBUYUKI
  • OZAKI SHOICHIRO
  • HAMADA KOUZO
  • GOTO JUN-ICHI
  • SUZUKI AKINOBU
  • EBISUI ETSUKO
  • TERAUCHI AKIKO
  • JAPAN SCIENCE AND TECHNOLOGY AGENCY
IPC(International Patent Classification)
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