Back to results
US 2014/0371272 A1Published application
Therapeutic compounds
AssigneeRegents of the University of Minnesota
InventorsVenkatram R. Mereddy, Lester R. Drewes, Mohammed Abrar Alam, Sravan K. Jonnalagadda, Shirisha Gurrapu
Life of this patent
Estimating the term…
Abstract
The invention provides compounds of formula (I) or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula (I), processes for preparing compounds of formula (I), intermediates useful for preparing compounds of formula (I) and therapeutic methods for treating cancer or treating autoimmune diseases or preventing transplant rejection using compounds of formula (I).
Claims23
A compound of formula I:
- wherein:
- X is CN, Y is R5 and the dashed bond is absent;
- or
- X is —C(═O)—, Y is O and the dashed bond is a single bond;
- R1 is H or (C1-C6)alkyl;
- R2 is H, (C1-C6)alkyl, (C1-C6)alkoxy, halo(C1-C6)alkyl, halo, —OH, —CN, —NO2, —CO2Ra, —C(═O)Ra, —NRa(C═O)Rb, —C(═O)NRcRd or —NRcRd;
- R3 is H, (C1-C6)alkyl, (C1-C6)alkoxy, halo(C1-C6)alkyl, halo, —OH, —CN, —NO2, —CO2Ra, —C(═O)Ra, —NRa(C═O)Rb, —C(═O)NRcRd or —NRcRd;
- R4 is H, (C1-C6)alkyl, (C1-C6)alkoxy, halo(C1-C6)alkyl, halo, —OH, —CN, —NO2, —CO2Ra, —C(═O)Ra, —NRa(C═O)Rb, —C(═O)NRcRd or —NRcRd;
- R5 is H, (C1-C6)alkyl, (C1-C6)alkoxy, halo(C1-C6)alkyl, halo, —OH, —CN, —NO2, —CO2Ra, —C(═O)Ra, —NRa(C═O)Rb, —C(═O)NRcRd or —NRcRd;
- R6a and R6b are each independently H, (C1-C7)alkyl, (C2-C7)alkenyl, (C2-C7)alkynyl, aryl(C1-C6)alkyl-, heteroaryl(C1-C6)alkyl-, heterocycle(C1-C6)alkyl-, aryl, heterocycle or hetereoaryl, wherein any (C1-C7)alkyl, (C2-C7)alkenyl, (C2-C7)alkynyl, aryl(C1-C6)alkyl-, heteroaryl(C1-C6)alkyl-, heterocycle(C1-C6)alkyl-, aryl, heterocycle or hetereoaryl of R6a and R6b is optionally substituted with one or more Z1 groups;
- or R6a and R6b together with the nitrogen to which they are attached form a heterocycle, wherein the heterocycle is optionally substituted with one or more Z1 groups;
- each Ra is independently H, (C1-C6)alkyl, aryl(C1-C6)alkyl- or aryl;
- each Rb is independently (C1-C6)alkyl, aryl(C1-C6)alkyl- or aryl;
- Rc and Rd are each independently H, (C1-C6)alkyl, aryl(C1-C6)alkyl- or aryl;
- or Rc and Rd together with the nitrogen to which they are attached form a pyrrolidino, piperidino, piperazino, azetidino, morpholino, or thiomorpholino;
- each Z1 is independently (C1-C6)alkyl, (C1-C6)alkoxy, halo(C1-C6)alkyl, halo, —OH, —CN, —NO2, —CO2Re, —C(═O)Re, —NRe(C═O)Rf, —C(═O)NRgRh or —NRgRh;
- each Re is independently H, (C1-C6)alkyl, aryl(C1-C6)alkyl- or aryl;
- each Rf is independently (C1-C6)alkyl, aryl(C1-C6)alkyl- or aryl;
- and
- Rg and Rh are each independently H, (C1-C6)alkyl, aryl(C1-C6)alkyl- or aryl;
- or Rg and Rh together with the nitrogen to which they are attached form a pyrrolidino, piperidino, piperazino, azetidino, morpholino, or thiomorpholino;
- or a pharmaceutically acceptable salt thereof, for use in medical therapy.
19 more elements
23-32. (canceled)
Dependencies are inferred from the claim text.