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Heterobifunctional pan-selectin inhibitors
专利权人:
GlycoMimetics; Inc.
发明人:
Magnani, John L.,Patton, John T.,Sarkar, Arun K.,Svarovsky, Sergei A.,Ernst, Beat
申请号:
ES10011660
公开号:
ES2651929T3
申请日:
2006.09.01
申请国别(地区):
ES
年份:
2018
代理人:
摘要:
Compound or physiologically acceptable salt thereof, which has the formula: ** Formula ** in which R1>; = ** Formula ** or in which n>; = 0-2, and when n>; = 2, each occurrence of R8 is independently selected; R2>; = - [C (>; = O) NH (CH2) nNHC (>; = O)] m (L) mZ, where n>; = 0-30, m>; = 0-1, L is a group of union and Z is a benzyl aminosulfonic acid, a benzyl aminocarboxylic acid, or a polyethylene glycol; R310>; = ** Formula ** -OC (>; = O) -X, -NH2, -NH-C (>; = O) -NHX or -NH-C (>; = O) -X where n>; = 0-2 and X are independently selected from C1-C8 alkanyl, C2-C8 alkenyl, C2-C8 alkynyl, ** Formula ** and in which n>; = 0-10, and any of the above ring compounds may be substituted with one to three substituents independently selected from Cl, F, C1-C8 alkynyl, C2-C8 alkenyl, C2-C8 alkynyl, C6-C14 aryl, or OY wherein Y is independently selected from H, C1-C8 alkanyl , C2-C8 alkenyl, C2-C8 alkynyl or C6-C14 aryl; R4>; = ** Formula ** 6 'sulfated GlcNAc, 6' carboxylated GlcNAc, 6 'sulfated GalNAc, 6' sulfated galactose, 6 'carboxylated galactose or ** Formula ** in which R9 is aryl, heteroaryl, cyclohexane, t -butane, adamantane or triazole, and any of R9 may be substituted with one to three substituents independently selected from Cl, F, C1-C8 alkynyl, C2-C8 alkenyl, C2-C8 alkynyl and OY in which Y is H, C1-C8 alkanyl, C2-C8 alkenyl, C2-C8 alkynyl or C6-C14 aryl; ** Formula ** R5>; = H, or R4 and R5 are taken together to form ** Formula ** in which R10 is aryl , 5 heteroaryl, ** Formula ** in which n>; = 0-10, and any one of the above ring compounds may be substituted with one to three substituents independently selected from Cl, F, C1-C8 alkanyl, alkenyl C2-C8, C2-C8 alkynyl and OY in which Y is H, C1-C8 alkynyl, C2-C8 alkenyl, C2-C8 alkynyl; ** Formula ** R6>; = H, fucose, mannose, arabinose, galactose or polyol; R7>; = H, C1-C8 alkynyl, C2-C8 alkenyl, C2-C8 alkynyl or ** Formula ** R8>; = H, C1-C8 alkynyl, C2-C8 alkenyl, C2-
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