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US 8,507,672 B2Granted
Substituted pyrrolo[2,3-d]pyrimidines as LIM kinase 2 inhibitors
AssigneeLexicon Pharmaceuticals, Inc.
InventorsBryce Alden Harrison, Spencer David Kimball, Ross Mabon, David Brent Rawlins, Dennis S. Rice, Michael Victor Voronkov, Yulian Zhang
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Abstract
Substituted pyrrolo[2,3-d]pyrimidine-based compounds useful as inhibitors of LIM kinase 2 are disclosed. Also disclosed are pharmaceutical compositions comprising the compounds and methods of their use to treat, manage and prevent inflammatory diseases and disorders, cancer, and diseases and disorders of the eye.
Claims12
A compound of formula I:
- or a pharmaceutically acceptable salt thereof, wherein:
- X is O;
- Y is O or NRB;
- A is aryl;
- R1 is hydrogen, ORB, N(RB)2, SRB, or optionally substituted alkyl, aryl, or heterocycle;
- R2 is optionally substituted lower alkyl;
- each R3 is independently halogen or optionally substituted alkyl, and/or two R3s may be taken together with the ring to which they are attached to provide an optionally substituted cycloalkyl or heterocyclyl;
- each R4 is cyano, halogen, hydroxy, nitro, RC, ORC, N(RC)2, NHC(O)RC, C(O)RC, C(O)N(RC)2, or SO2RC;
- each RB is independently hydrogen or optionally substituted alkyl;
- each RC is independently hydrogen or optionally substituted alkyl, heteroalkyl, aryl, heterocyclyl, alkylaryl, or alkylheterocycle;
- n is 0-8;
- and
- m is 0-4.
10 more elements
A compound of formula II:
- or a pharmaceutically acceptable salt thereof, wherein:
- X is O or NRA;
- Y is O, NRB, or C(RB)2;
- A is cycloalkyl, aryl or heterocyclyl;
- R1 is hydrogen, ORB, N(RB)2, SRB, or optionally substituted alkyl, aryl, or heterocyclyl;
- R2 is hydrogen, halogen, cyano, ORB, N(RB)2, SRB, or optionally substituted alkyl, aryl, or heterocyclyl;
- each R3 is independently halogen or optionally substituted alkyl, and/or two R3s may be taken together with the ring to which they are attached to provide an optionally substituted cycloalkyl or heterocyclyl;
- each R4 is cyano, halogen, hydroxy, nitro, RC, ORC, N(RC)2, NHC(O)RC, C(O)RC, C(O)N(RC)2, or SO2RC;
- R5 is oxo;
- RA is hydrogen, cyano, nitro, RA1, SO2RA1, SO2NRA1, or SO2N(RA1)2;
- each RA1 is independently hydrogen or optionally substituted alkyl, heteroalkyl, aryl, heterocyclyl, alkylaryl, or alkylheterocycle;
- each RB is independently hydrogen or optionally substituted alkyl;
- each RC is independently hydrogen or optionally substituted alkyl, heteroalkyl, aryl, heterocyclyl, alkylaryl, or alkylheterocycle;
- m is 0-4;
- p is 0-3;
- and
- q is 0-2.
14 more elements
Dependencies are inferred from the claim text.