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US 2006/0040934 A1Published application
Use of STAT-6 inhibitors as therapeutic agents
AssigneeThe Regents of the University of California
InventorsHoward Cottam, Lorenzo Leoni, Dennis Carson
Life of this patent
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Abstract
The present invention provides novel indole derivatives useful to inhibit cancer or sensitize cancer cells to chemotherapeutic agents, radiation or other anti-cancer treatments.
Claims2
A therapeutic method for suppressing STAT-6 activity and/or for inhibiting the IL-4/IL-13 signal transduction pathways comprising administering to a mammal subject to a pathology amenable to treatment by STAT-6 suppression an effective amount of a compound of formula (I):
- wherein R1, R2 and R3 are independently hydrogen, halo, hydroxy, cyano, N(Ra)(Rb), S(Ra), NO2, (C1-C6)alkyl, (C1-C6)alkoxy, (C2-C6)alkynyl, (C2-C6)alkenyl, (C2-C7)alkanoyl, C2-C7)alkanoyloxy, or (C3-C7)cycloalkyl or R1 and R2 taken together are benzo, optionally substituted by R1, (C3-C5)alkylene or methylene dioxy;
- wherein Ra and Rb are each independently hydrogen, (C1-C3)alkyl, (C2-C4)alkanoyl, phenyl, benzyl, or phenethyl;
- or Ra and Rb together with the nitrogen to which they are attached are a 5-6 membered heterocyclic ring, preferably a pyrrolidino, piperidino or morpholino ring;
- Ar is aryl, heteroaryl, or a 5-6 membered heterocyclic ring, preferably comprising 1-3 N(Ra), non-peroxide O or S atoms, such as a pyrrolidino, piperidino or morpholino ring, optionally substituted with 1-5, preferably 1-2, halo, CF3, hydroxy, CN, N(Ra)(Rb), (C1-C6)alkyl, (C1-C6)alkoxy, (C2-C7)alkanoyl, (C2-C7)alkanoyloxy, (C3-C7)cycloalkyl, (C2-C6)alkanoyl, (C2-C6)alkenyl, or phenyl;
- Y is oxy (—O—), S(O)0-2, Se, C(R1)(R3), N(Ra), or —P—;
- or a pharmaceutically acceptable salt thereof.
3 more elements
2-40. (canceled)
Dependencies are inferred from the claim text.