US 11,684,603 B2
Neuraminidase inhibition to improve glycocalyx volume and function to ameliorate cardiovascular diseases in pathologies associated with glycocalyx damage
Luis A. Martinez-Lemus, Columbia, MO (US); Christopher A. Foote, Columbia, MO (US); and Jaume Padilla, Columbia, MO (US)
Assigned to CURATORS OF THE UNIVERSITY OF MISSOURI UNIVERSITY, Columbia, MO (US)
Appl. No. 16/754,814
Filed by The Curators Of The University Of Missouri, Columbia, MO (US)
PCT Filed Oct. 10, 2018, PCT No. PCT/US2018/055145
§ 371(c)(1), (2) Date Apr. 9, 2020,
PCT Pub. No. WO2019/075009, PCT Pub. Date Apr. 18, 2019.
Claims priority of provisional application 62/572,232, filed on Oct. 13, 2017.
Prior Publication US 2021/0186921 A1, Jun. 24, 2021
Int. Cl. A61K 31/351 (2006.01); A61K 31/215 (2006.01); A61K 31/445 (2006.01); A61K 38/47 (2006.01); A61K 31/196 (2006.01); A61P 3/10 (2006.01)
CPC A61K 31/351 (2013.01) [A61K 31/196 (2013.01); A61K 31/215 (2013.01); A61K 31/445 (2013.01); A61K 38/47 (2013.01); A61P 3/10 (2018.01)] 15 Claims
 
1. A method for ameliorating glycocalyx damage in an individual in need thereof, the method comprising: administering to the individual in need thereof a composition comprising a neuraminidase inhibitor chosen from Neu5Ac2en ((2R,3R,4S)-3-acetamido-4-hydroxy-2-[(1R,2R)-1,2,3-trihydroxypropyl]-3,4-dihydro-2H-pyran-6-carboxylic acid), a Neu5Ac2en derivative, oseltamivir (ethyl (3R,4R,5S)-5-amino-4-acetamido-3-(pentan-3-yloxy)-cyclohex-1-ene-1-carboxylate), siastatin B ((3S,4S,5R,6R)-6-acetamido-4,5-dihydroxypiperidine-3-carboxylic acid), a siastatin B analog, a siastatin B derivative, and a sialidase.
 
5. A method for treating endothelial dysfunction in an individual in need thereof, the method comprising: administering to the individual in need thereof a composition comprising a neuraminidase inhibitor chosen from Neu5Ac2en ((2R,3R,4S)-3-acetamido-4-hydroxy-2-[(1R,2R)-1,2,3-trihydroxypropyl]-3,4-dihydro-2H-pyran-6-carboxylic acid), a Neu5Ac2en derivative, oseltamivir (ethyl (3R,4R,5S)-5-amino-4-acetamido-3-(pentan-3-yloxy)-cyclohex-1-ene-1-carboxylate), siastatin B ((3S,4S,5R,6R)-6-acetamido-4,5-dihydroxypiperidine-3-carboxylic acid), a siastatin B analog, a siastatin B derivative, and a sialidase.
 
9. A method for improving flow mediated dilation in an individual in need thereof, the method comprising: administering to the individual in need thereof a composition comprising a neuraminidase inhibitor chosen from Neu5Ac2en ((2R,3R,4S)-3-acetamido-4-hydroxy-2-[(1R,2R)-1,2,3-trihydroxypropyl]-3,4-dihydro-2H-pyran-6-carboxylic acid), a Neu5Ac2en derivative, oseltamivir (ethyl (3R,4R,5S)-5-amino-4-acetamido-3-(pentan-3-yloxy)-cyclohex-1-ene-1-carboxylate), siastatin B ((3S,4S,5R,6R)-6-acetamido-4,5-dihydroxypiperidine-3-carboxylic acid), a siastatin B analog, a siastatin B derivative, and a sialidase.