Granted Patent
B2
US 8,470,782 · App. 12/064,800 · Granted Jun 25, 2013
Transglutaminase inhibitors and methods of use thereof
Inventors:
Chaitan Khosla (Palo Alto, CA); Richard Edward Watts (Lindale, TX); Matthew John Siegel (San Mateo, CA); Daniel M. Pinkas (Menlo Park, CA); Kihang Choi (Seoul, KR); Keith M. Rich (St. Louis, MO)
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Abstract
Transglutaminase inhibitors and methods of use thereof are provided.
Claims (5)
1. A pharmaceutical formulation comprising:
an effective dose of a tTGase inhibitor, wherein said tTGase inhibitory moiety is:
wherein R 1 is quinolin-3-ylmethyl ester and R 2 is selected from the group consisting of 5-fluoro-1H-indol-3-yl, (S)-Bn, (S)—CO 2 Me, (S)-Me, (R)-Bn, (S)—CH 2 CONHBn, (S)-(1H-inol-yl)-methyl, (S)-(4-hydroxy-phenyl)-methyl, OMe, OtBu, Gly, Gly-NH 2 , LPY, LPF—NH 2 ;
R 3 is selected from Cl, and Br; n is 0; and X is selected from the group consisting of O and NH.
2. The formulation of claim 1 , wherein R 2 is 5-fluoro-1H-indol-3-yl.
Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST
Recorded Feb 14, 2012
From: KHOSLA, CHAITAN; WATTS, RICHARD EDWARD; SIEGEL, MATTHEW JOHN; PINKAS, DANIEL M.; CHOI, KINHANG; RICH, KEITH M.
To: THE BOARD OF TRUSTEES OF THE LELAND STANFORD JUNIOR UNIVERSITY
Reel/Frame 027703/0836 →
CONFIRMATORY LICENSE
Recorded Feb 11, 2009
From: STANFORD UNIVERSITY
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 022241/0728 →
Continuity (2)