W0 2011/000721 A1 I||||||||||||||||||||||||||||||||||||||||||||||||||||||||| - Questel

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H wherein Q is selected from — N — , -S- or -O- and is linked to a J scaffold through a Y linker and n is 1 to 3; or wherein R 2 is -N-R 3 2 as above disclosed and M is -(O-CH 2 -CH 2 -) n -Q or -(0-CH 2 -CH 2 - CH 2 -) n -Q, wherein Q and n are as above disclosed, wherein each R 3 may be independently H , a C1-C8 linear or branched, saturated or unsaturated alkyl chain, optionally substituted with an above disclosed A group and Y is a linker selected from an amino acidic residue or a succinic acid or diglycolic acid residue. Within formula (Ib), J is a first or second or higher generation dendrimer based o n 2,2'-bis(methoxyol)propanoic acid (bis-MPA) or a poly(amidoamine) (PAMAM) based dendrimer and aJ is the functionality of the scaffold J and is comprised between 1 and 150. Within formula (Ib) above, M is preferably and the resulting X moiety has the following formula
wherein R 2 , Q and n have the same meaning as above disclosed. In particular, in a preferred embodiment, said J dendrimer based on 2,2'- bis(methoxyol)propanoic (bis-MPA) is a first or second generation or higher generation bis(methoxyol)propanoic (bis-MPA) based dendrimers (see, for instance, at Fig. 12). According to the above, a preferred compound within formula (Ib) is compound 15 below reported prepared according to the following Example 3, wherein R 1 is H, R 2 is methoxy H (-OCH 3 ), R is H, n is 1, Q is — — and it is linked to Y, which is a succinic acid residue and the J scaffold is a third generation 2,2'- bis(methoxyol)propanoic (bis-MPA) based dendrimer. Alternatively, the dendrimer scaffold J may be a poly(amidoamine) (PAMAM) based dendrimer (see, for instance, at Fig. 13). 15
Page 1 and 2: (12) INTERNATIONAL APPLICATION PUBL
Page 3 and 4: mannose disaccharide (Manα1-2Man),
Page 5 and 6: It is a forth object of the inventi
Page 7 and 8: M' is a saccharidic or pseudo-sacch
Page 9 and 10: wherein Q and n are above disclosed
Page 12 and 13: wherein R is as above disclosed,
Page 14 and 15: may be made of gold, silver, Fe 2 O
Page 16 and 17: Within the compound of formula (I)
Page 18 and 19: wherein R and R 2 are as above repo
Page 20 and 21: through the Y linker and n is 1 to
Page 22 and 23: and (12a) 12b. As per a third aspec
Page 26 and 27: According to a second object of the
Page 28 and 29: wherein aj is 32 and J is a third g
Page 30 and 31: eactions requiring anhydrous condit
Page 32 and 33: To a solution of the silylmannopyra
Page 34 and 35: 3H, CH 3 CO), 1.99 (s, 3H, CH 3 CO)
Page 36 and 37: To a solution of the compound 9 (12
Page 38 and 39: (C2 D ), 70.36 (C6 M ), 70.01 (C6 M
Page 40 and 41: EXAMPLE 2 Synthesis of compound 12a
Page 42 and 43: 13 C-NMR (100 MHz, D2 O) δ (ppm):
Page 44 and 45: (the R5 tropic laboratory-adapted s
Page 46 and 47: derived from 1 (see above); G3Man32
Page 48 and 49: CLAIMS: 1 A compound of general for
Page 50: OCH 3 ), hydroxymethyl (-CH 2 OH),
Page 53 and 54: alkyl chain, C1-C8 linear or branch
Page 55 and 56: 7 . A compound having the general f
Page 57 and 58: H wherein Q is selected from — N
Page 59: or methyl substituted 1,3-thiazole;
Page 62 and 63: wherein R 2 may be hydroxyl (-0H),
Page 64 and 65: 12. A compound according to claim 1
Page 66: or methyl substituted 1,3-thiazole;
Page 82 and 83:
INTERNATIONAL SEARCH REPORT C(Conti
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W0 2011/000721 A1 I||||||||||||||||||||||||||||||||||||||||||||||||||||||||| - Questel

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