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US 8,802,716 B2Granted
IAP binding compounds
AssigneeTetralogic Pharmaceuticals Corporation
InventorsStephen M. Condon, Matthew G. LaPorte, Yijun Deng, Susan R. Rippin
Life of this patent
Estimating the term…
Abstract
IAP binding molecules and compositions including these are disclosed. The IAP binding molecules interact with IAPB (inhibitor of apoptosis proteins) in cells and may be used to modify apoptosis in cells treated with such molecules. Embodiments of these compounds have a Kd of less than 0.1 micromolar. Methods of using these IAP binding molecules for therapeutic, diagnostic, and assay purposed are also disclosed.
Claims26
A compound of formula (5)
- or a pharmaceutically acceptable salt thereof
- where A1 is H, or lower alkyl, or A1 and R1b together form a ring of 3-5 atoms;
- R1a is H;
- R1b is lower alkyl, or together with A1 forms a ring of 3 to 5 atoms;
- Y is an alkyl group, an alkynyl group, a cycloalkyl group of 3 to 7 carbon atoms, optionally substituted versions of these groups, or Y together with Z1a, Z1b, or R10 forms a carbocyclic ring, or a heterocyclic ring containing 1 to 5 heteroatoms, where Y is linked to Z1a, Z1b, or R10;
- Z1a and Z1b are independently an H, hydroxy, amino, alkylamino, diakylamino, alkoxy, aryloxy, or heteroaryloxy;
- or Z1a, Z1b, together with Y or R10 form a carbocyclic ring, or a heterocyclic ring containing 1 to 5 heteroatoms, where Z1a or Z1b, is linked to Y or R10;
- M is an optionally-substituted alkylene of 1 to 5 carbon atoms;
- G is a bond, a heteroatom, —(C═O)—;
- —NR18—;
- —NCOR18—;
- or —NS(O)xR18— where x=0, 1, or 2, and R18 is lower alkyl, or an optionally-substituted lower alkyl;
- and
- R10 is heteroaryl.
11 more elements
A compound of formula (3):
- or a pharmaceutically acceptable salt thereof
- where A1 is H, lower alkyl, or optionally-substituted lower alkyl;
- R1a and R1b are separately H, lower alkyl, optionally-substituted lower alkyl, or A1 together with either R1a or R1b form an optionally substituted heterocycloalkyl of 3 to 6 atoms;
- Y is H, alkyl, alkynyl, cycloalkyl of 3 to 7 carbon atoms, aryl, heteroaryl, or arylalkyl;
- Z is H, alkyl, hydroxy, amino, alkylamino, diakylamino, alkoxy, cycloalkyl, cycloalkyloxy, aryl, heteroaryl, aryloxy, or heteroaryloxy;
- M is an optionally-substituted alkylene, alkenylene, or alkynylene of 1 to 5 carbon atoms;
- G is a bond, a heteroatom, —(C═O)—;
- —S(O)t— where t=0, 1, or 2;
- —NR18—;
- —NCOR18—;
- or —NS(O)xR18— where x=0, 1, or 2, and R18 is lower alkyl, or cycloalkyl or R18 is contained within a carbocyclic, or heterocyclic ring containing 1 to 5 heteroatoms, where R18 is linked to Z, M, or R10;
- and
- R10 is heteroaryl.
10 more elements
Dependencies are inferred from the claim text.