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US 8,895,563 B2Granted
Human protein tyrosine phosphatase inhibitors and methods of use
AssigneeAerpio Therapeutics Inc.
InventorsJeffrey Lyle Gray, Kande K. D. Amarasinghe, Cynthia Monesa Clark, Ryan Matthew Nichols, Matthew B. Maier
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Abstract
The present disclosure relates to compounds effective as human protein tyrosine phosphatase beta (HPTP-β) inhibitors thereby regulating angiogenesis. The present disclosure further relates to compositions comprising said human protein tyrosine phosphatase beta (HPTP-β) inhibitors, and to methods for regulating angiogenesis.
Claims27
A method for controlling an angiogenesis regulated disease or disorder comprising, contacting a subject with an effective amount of a compound having the formula:
- wherein R is a substituted or unsubstituted thiazolyl unit having the formula:
- R4 and R5 are each independently chosen from:
- i) hydrogen;
- ii) substituted or unsubstituted C1-C6 linear, C3-C6 branched, or C3-C6 cyclic alkyl;
- iii) substituted or unsubstituted phenyl;
- iv) substituted or unsubstituted heteroaryl;
- or
- R4 and R5 can be taken together to form a saturated or unsaturated ring having from 5 to 7 atoms;
- said substitutions are independently chosen from one or more C1-C6 linear, C3-C6 branched, or C3-C6 cyclic alkyl, halogen, hydroxyl, or cyano units;
- R6 is a unit chosen from:
- i) hydrogen;
- ii) substituted or unsubstituted C1-C6 linear, C3-C6 branched, or C3-C6 cyclic alkyl;
- iii) substituted or unsubstituted phenyl;
- and
- iv) substituted or unsubstituted heteroaryl;
- R1 is chosen from:
- i) hydrogen;
- ii) C1-C6 linear or C3-C6 branched alkyl;
- iii) substituted or unsubstituted phenyl;
- or
- iv) substituted or unsubstituted benzyl;
- R2 is chosen from:
- i) C1-C6 linear or C3-C6 branched alkyl;
- or
- ii) C1-C6 linear or C3-C6 branched alkoxy;
- R3 is hydrogen or C1-C4 linear or C3-C4 branched alkyl;
- or
- a pharmaceutically acceptable salt thereof;
- wherein the angiogenesis regulated disease or disorder is chosen from skeletal muscle and myocardial ischemia, stroke, coronary artery disease, or peripheral vascular disease.
26 more elements
Dependencies are inferred from the claim text.