Charge-balanced chemoselective linkers

Details Charge-balanced chemoselective linkers Charge-balanced chemoselective linkers

C - Chemistry, Metallurgy

07

D

C07D 333/52 (2006.01) A61K 39/00 (2006.01) A61K 47/48 (2006.01) A61L 15/20 (2006.01) A61L 31/00 (2006.01) B01D 61/28 (2006.01) B01D 67/00 (2006.01) C07C 39/06 (2006.01) C07C 39/14 (2006.01) C07C 43/23 (2006.01) C07C 47/54 (2006.01) C07C 59/74 (2006.01) C07C 65/30 (2006.01) C07D 307/12 (2006.01) C07D 307/78 (2006.01) C07D 307/80 (2006.01) C07D 333/16 (2006.01) C07K 7/06 (2006.01) G01N 21/25 (2006.01) G01N 21/64 (2006.01) G01N 33/53 (2006.01) G01N 33/543 (2006.01)

Patent

CA 2481996

Compounds according to general formulae (Ia to Ie) wherein: X = O or S; Y is O, S or CH2, CHR, CRR, where R is C1-7 alkyl; Z is O or S; R1 is H or C1-7 alkyl; R2 is H or C1-7 alkyl; R4 is H or C1-7 alkyl at any vacant position on the aromatic ring; R3 is C1-7 alkyl-L1-R5-L2- R6-COOH, C3-10 cycloalkyl-L1-R5- L2- R6-COOH or Ar-C0-7 alkyl-L1-R5-L2- R6-COOH; each of L1 and L2 is absent or a suitable linker such as an amide CONH; or an ether -O-, or a thioether -S- or a sulphone -S02-; R5 is C1-7 alkyl, C3-1O cycloalkyl or Ar-C0-7 alkyl each of which is substituted with either NR8R9, where the nitrogen atom is capable of being protonated in solution to give N+HR8R9; or a quaternary nitrogen atom N+R8R9R10, such that R5 contains a positive charge; each of R8, R9 and R10 is independently C1-7 alkyl, C3-10 cycloalkyl or Ar-C0-7 alkyl, or any two or more of R8, R9 and R10 together form an alicyclic or arylalicyclic ring system; R6 is C1-7 alkyl, C3-10 cycloalkyl or Ar-C0-7 alkyl; and their salts, hydrates, solvates, complexes or prodrugs are of use as linkers for conjugating an epitope to a carrier protein.

L'invention porte sur des composés des formules générales (Ia à Ie) dans lesquelles: X = O ou S; Y représente O, S ou CH¿2?, CHR, CRR, R représentant alkyle C¿1-7?; Z représente O ou S; R¿1? représente H ou alkyle C¿1-7?; R¿2? représente H ou alkyle C¿1-7?; R¿4? représente H ou alkyle C¿1-7? à n'importe quelle position vacante sur le noyau aromatique; R¿3? représente C¿1-7? alkyl-L¿1?-R¿5?-L¿2?- R¿6?-COOH, C¿3-10? cycloalkyl-L¿1?-R¿5?-L¿2?- R¿6?-COOH ou Ar-C<SB>O-7</SB> alkyl-L¿1?-R¿5?-L¿2?- R¿6?-COOH; chacun de L¿1? et L¿2? est absent ou est un lieur approprié tel qu'un amide CONH ou un éther -O-, ou un thioéther -S- ou un sulfone -S0¿2?-; R¿5? représente alkyle C¿1-7?, cycloalkyle C¿3-1O? ou Ar-C¿0-7? alkyle, chacun d'eux étant substitué soit par NR¿8?R¿9?, l'atome d'azote pouvant être protoné en solution pour donner N?+¿HR¿8?R¿9?; soit par un atome d'azote quaternaire N?+¿R¿8?R¿9?R¿10?, de sorte que R¿5? renferme une charge positive; chacun de R¿8?, R¿9? et R¿10? représente indépendamment alkyle C¿1-7?, cycloalkyle C¿3-10? ou Ar-C¿0-7? alkyle, ou deux quelconques ou plus de R¿8?, R¿9? et R¿10?, réunis, forment un système de noyau alicyclique ou arylalicyclique; R¿6? représente alkyle C¿1-7?, cycloalkyle C¿3-10? ou Ar-C¿0-7? alkyle. L'invention porte également sur les sels, les hydrates, les solvates, les complexes ou les promédicaments de ces composés qui sont utiles comme lieurs pour conjuguer un épitope à une protéine de transport.

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