GTPase inhibitors and use thereof for controlling platelet hyperactivity
AssigneeCincinnati Children's Hospital Medical Center
InventorsYi Zheng, Huzoor Akbar, David Williams, Wieslaw Mazur
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Abstract
The preferred embodiments generally relate to methods and compositions that affect the GTP-binding activity of members of the Rho family GTPases, preferably Rac (Rac1, Rac2 and/or Rac3), such compositions include compounds that modulate the GTP/GDP exchange activity, along with uses for the compounds including screening for compounds which recognize Rac GTPase, and methods of treating pathological conditions associated or related to a Rho family GTPase, including Rac. The preferred embodiments also relate to methods of using such compounds, or derivatives thereof, e.g., in therapeutics, diagnostics, and as research tools.
Claims12
A method for treating platelet hyperreactivity, comprising administering to a subject an effective amount of at least one compound having the formula (IIa):
- R1 to R2 are independently selected from the group consisting of H, —X-Alk, —X-Alk-X′, and —X—Y—X′;
- wherein
- X is —CR7R8;
- X′ is —CHR7R8;
- Alk is a C2-C18 substituted or unsubstituted hydrocarbon chain;
- Y is a C2-C8 substituted or unsubstituted alkylene chain;
- R6 is H or (C1-C4) alkyl;
- and
- R7 and R8 are independently selected from the group consisting of H or (C1-C4) alkyl;
- or a salt of a compound of formula (IIa).
A method for treating platelet hyperreactivity, comprising administering to a subject an effective amount of at least one compound having the formula (III):
- R10 to R12 are independently selected from the group consisting of H, halo, (C1-C4) alkyl, branched (C3-C4) alkyl, halo (C1-C4) alkyl, (C1-C4) alkoxy, NO2, and NH2;
- or a salt of a compound of formula (III).
A method for treating platelet hyperreactivity, comprising administering to a subject an effective amount of at least one compound having the formula (IV):
- or pharmaceutically acceptable salts thereof.
Dependencies are inferred from the claim text.