02-01-2014 дата публикации
Номер: US20140005141A1
Принадлежит:
Disclosed are chemically modified hyaluronic acid (HA) derivatives containing hydrazido groups directly linked to the glucuronic acid residues of HA. Said hydrazido groups are used to obtain crosslinked and labeled HA derivatives. The invention further relates to methods of preparation of said HA derivatives. 1. A hyaluronic acid (hereinafter HA) derivative or a salt thereof , said derivative having a part of the carboxy groups of the D-glucuronic residues converted directly into hydrazido groups.2. The hyaluronic acid derivative according to claim 1 , wherein said hyaluronic acid derivative is an uncross-linked compound represented by the formula:{'br': None, 'HA-CO—NR1—NHR2'}{'sub': 1', '20', '2', '20', '2', '10', '6', '14', '3', '2', '2', '1', '20', '2', '20', '2', '10', '1', '20', '2', '20', '6', '14, 'sup': '+', 'wherein R1and R2, the same or different, each is H, C-Calkyl, C-Calkenyl, C-Calkynyl, C-Caryl, alkaryl or heterocyclyl optionally substituted by one or more radicals selected from the group consisting of halogen, hydroxy, alkoxy, thioalkyl, nitro, cyano, CF, CONH, and —NH—NH, and/or each of the C-Calkyl, C-Calkenyl, C-Calkynyl may be interrupted by O or S or by a group NR3R4, wherein R3 and R4, the same or different; each is H, C-Calkyl, C-Calkenyl, C-Caryl.'}3. The hyaluronic acid derivative according to claim 2 , wherein said hyaluronic acid derivative is an uncross-linked claim 2 , water-soluble compound represented by the formula HA-CO-NH-NH.4. The hyaluronic acid derivative according to claim 3 , wherein said uncross-linked claim 3 , water-soluble compound further contains N-acylurea groups.5. The hyaluronic acid derivative according to claim 1 , wherein said hyaluronic acid derivative is a cross-linked compound formed by reaction of a part of the hydrazido groups of the D-glucuronic residues with a part of the carboxy groups of the D-glucuronic residues claim 1 , said carboxy groups being activated by a carbodiimide claim 1 , thus resulting in a ...
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