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Protein cross-linking inhibitor

外国特許コード F110005822
整理番号 I018P010WO1
掲載日 2011年10月19日
出願国 アメリカ合衆国
出願番号 200913058647
公報番号 20110212919
公報番号 8853424
出願日 平成21年8月11日(2009.8.11)
公報発行日 平成23年9月1日(2011.9.1)
公報発行日 平成26年10月7日(2014.10.7)
国際出願番号 JP2009064206
国際公開番号 WO2010018837
国際出願日 平成21年8月11日(2009.8.11)
国際公開日 平成22年2月18日(2010.2.18)
優先権データ
  • 特願2008-207315 (2008.8.11) JP
  • 2009JP064206 (2009.8.11) WO
発明の名称 (英語) Protein cross-linking inhibitor
発明の概要(英語) 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.
特許請求の範囲(英語) [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.
  • 発明者/出願人(英語)
  • MIKOSHIBA KATSUHIKO
  • NUKINA NOBUYUKI
  • OZAKI SHOICHIRO
  • HAMADA KOUZO
  • GOTO JUN-ICHI
  • SUZUKI AKINOBU
  • EBISUI ETSUKO
  • TERAUCHI AKIKO
  • JAPAN SCIENCE AND TECHNOLOGY AGENCY
国際特許分類(IPC)
米国特許分類/主・副
  • 549/4
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