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

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hydroxyalkyl, such as hydroxymethyl (-CH 2 OH), amino (-NH 2 ), thiol (-SH), πitro (-NO 2 ), carboxy (-COOH), wherein preferred A groups are cyclopropane, cyclopentane, cyclohexane, phenyl, thiazole, imidazole, oxazole; or wherein R 3 may be any of the A groups above disclosed; and wherein M is -(O-CH 2 -CH 2 -) n -Q o r -(O-CH 2 -CH 2 -CH 2 -) n -Q, wherein Q is H selected from , -S- or -O- or Q is an heterocycle which is bound to the Z scaffold through the Y linker and n is 1 to 3 , so that the resulting X moiety may have any of the following general formulas: wherein R 2 , n and Q have the above defined meanings; or wherein M is of formula K—(O-CH 2 -CH 2 -) π -Q or K-(O-CH 2 -CH 2 -CH 2 -) π -Q, wherein K is a saccharidic residue selected from the group comprising a mannose, glucose, fructose, ribose, xylose or a galactose residue and Q and n are as above disclosed. In a preferred embodiment, within formula (I), K is a mannose residue, thus M results any of the following:
wherein Q and n are above disclosed and the resulting X moiety thus has any of the following formula: wherein R 2 , Q and n have the same meaning as above disclosed. Within formula (I), Y is a bifunctional linker, which is capable of binding the X moiety to one end and the Z scaffold to the other end; in particular, it can be a single bond, so that the scaffold Z is directly linked to each X moiety or Y may be an heteroatom, an amino acidic residue selected from a glycine, an alanine, a valine, a cysteine, a threonine, a serine, a proline, a methionine or a lysine residue or Y is a succinic acid or a diglycolic acid residue. In the above disclosure and within the present invention, unless otherwise provided, the term heteroatom refer to any atom other than carbon or hydrogen and preferable refers to nitrogen, oxygen or sulphur; accordingly, heterocycle,
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: M' is a saccharidic or pseudo-sacch
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 24 and 25: H wherein Q is selected from — N
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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