Benzylideneguanidine derivatives and therapeutic use for the treatment of protein misfolding diseases

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United States of America Patent

PATENT NO 9682943
SERIAL NO

14760350

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ATTORNEY / AGENT: (SPONSORED)

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Abstract

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The present invention relates to a compound of formula (I), or a tautomer and/or a pharmaceutically acceptable salt thereof, wherein: R1 is alkyl, Cl, F or Br; R2 is H or F; R3 is selected from H and alkyl; R4 is selected from H and C(O)R6; R5 is H; or R4 and R5 are linked to form a heterocyclic group which is optionally substituted with one or more R10 groups; R6 is selected from R7, OR7 and NR8R9; R7, R8 and R9 are each independently selected from alkyl, cycloalkyl, aralkyl, cycloalkenyl, heterocyclyl and aryl, each of which is optionally substituted with one or more R10 groups; each R10 is independently selected from halogen, OH, CN, NO2, COO-alkyl, aralkyl, SO2-alkyl, SO2-aryl, COOH, CO-alkyl, CO-aryl, NH2, NH-alkyl, N(alkyl)2, CF3, alkyl and alkoxy; X and Z are each independently CR11, and Y is selected from CR11 and N; and R11 is H or F; for use in treating a disorder associated with protein misfolding stress and in particular associated with accumulation of misfolded proteins.

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Patent Owner(s)

Patent OwnerAddress
UNITED KINGDOM RESEARCH AND INNOVATIONPOLARIS HOUSE NORTH STAR AVENUE SWINDON SN2 1FL

International Classification(s)

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  • 2014 Application Filing Year
  • A61K Class
  • 14144 Applications Filed
  • 11600 Patents Issued To-Date
  • 82.02 % Issued To-Date
Click to zoom InYear of Issuance% of Matters IssuedCumulative IssuancesYearly Issuances2014201520162017201820192020202120222023202420250255075100

Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Bertolotti, Anne Cambridge, GB 13 28
Guedat, Philippe Montenois, FR 26 45

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Patent Citation Ranking

  • 4 Citation Count
  • A61K Class
  • 45.09 % this patent is cited more than
  • 8 Age
Citation count rangeNumber of patents cited in rangeNumber of patents cited in various citation count ranges763281956782001332911183139501 - 1011 - 2021 - 3031 - 4041 - 5051 - 6061 - 7071 - 8081 - 9091 - 100100 +050010001500200025003000350040004500500055006000650070007500800085009000

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