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US 2004/0167069 A1Published application
Drug therapy for Celiac Sprue
AssigneeThe Board of Trustees of the Leland Stanford Junior University
InventorsChaitan Khosla, Kihang Choi
Life of this patent
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Abstract
Administering an effective dose of a tTGase inhibitor to a Celiac or dermatitis herpetiformis patient reduces the toxic effects of toxic gluten oligopeptides, thereby attenuating or eliminating the damaging effects of gluten.
Claims18
A method of treating Celiac Sprue and/or dermatitis herpetiformis, the method comprising:
- administering to a patient an effective dose of a tTGase inhibitor;
- wherein said tTGase inhibitor attenuates gluten toxicity in said patient.
A formulation for use in treatment of Celiac Sprue and/or dermatitis herpetiformis, comprising:
- an effective dose of a tTGase inhibitor and a pharmaceutically acceptable excipient.
A tTGase inhibitor of the formula:
- 17
- wherein R1 and R2 are independently selected from H, alkyl, alkenyl, cycloalkyl, aryl, heteroalkyl, heteroaryl, alkoxy, alkylthio, arakyl, aralkenyl, halo, haloalkyl, haloalkoxy, heterocyclyl, and heterocyclylalkyl groups, an amino acid, a peptide, a peptidomimetic, or a peptidic protecting group;
- wherein R2 can additionally be selected from the group consisting of LPYPQPQLPY, LPFPQPQLPF-NH2, LPYPQPQLP, LPYPQPQLPYPQPQPF, LP-X2-15, where X2-15 is a peptide consisting of any 2-15 amino acid residues followed by a C-terminal proline;
- R3 is selected from F, I, Cl, and Br;
- n is from 0 to 10;
- and X is selected from the group consisting of O and NH,
- other than {(S)-1-[(3-Bromo-4,5-dihydro-isoxazol-5-ylmethyl)-carbamoyl]-2-phenyl-ethyl}-carbamic acid benzyl ester.
4 more elements
Dependencies are inferred from the claim text.