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US 12,630,506 B2Granted
Direct thrombin inhibitors and methods of use thereof
AssigneeBaylor College of Medicine
InventorsMartin Matzuk, Surendra Dawadi, Melek Ucisik, John Faver, Kurt Bohren, Feng Li
Life of this patent
Estimating the term…
Abstract
Novel direct thrombin inhibitors are provided herein, along with methods for their use as anticoagulants. The direct thrombin inhibitors described herein are useful in treating and/or preventing thromboembolism and bleeding or clotting disorders. Also provided herein are methods for inhibiting thrombin in a cell using the compounds and compositions described herein.
Claims20
A compound of the following formula:
- or a pharmaceutically acceptable salt or prodrug thereof, wherein:
- m and n are each independently 0, 1, or 2;
- p is 1, 2, 3, or 4;
- X is substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted cycloalkyl, or substituted or unsubstituted heterocycloalkyl;
- Y is hydroxy, alkoxy, aryloxy, substituted or unsubstituted amino, substituted or unsubstituted cycloalkyl, or substituted or unsubstituted heterocycloalkyl;
- each R1 is independently selected from the group consisting of hydrogen, halogen, cyano, trifluoromethyl, alkoxy, aryloxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted heteroalkenyl, substituted or unsubstituted heteroalkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted cycloalkyl, and substituted or unsubstituted heterocycloalkyl;
- and
- R2, R3, R4, and R5 are each independently selected from the group consisting of hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted heteroalkenyl, substituted or unsubstituted heteroalkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted cycloalkyl, and substituted or unsubstituted heterocycloalkyl.
5 more elements
Dependencies are inferred from the claim text.