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US 2013/0095040 A1Published application
Dye compositions and dye syntheses
AssigneeGe Healthcare Limited
InventorUmamaheshwar P. Mokkapati
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Abstract
The present invention relates to sulfonated unsymmetrical pentamethine optical dye compositions, especially dyes suitable for biological applications in vitro, and for in vivo imaging. Improved dye compositions and intermediates are provided, which enable the suppression of undesirable newly-identified impurities. Also provided is the use of the improved dye compositions in the preparation of conjugates with biological targeting molecules.
Claims13
1-14. (canceled)
A composition which comprises an unsymmetrical cyanine dye of Formula A, together with symmetrical cyanine dyes of Formula B and Formula C:
- wherein:c
- the molar ratio of A:B and also A:C in said composition is at least 46:1;
- R1 and R2 are independently H, —SO3M1 or Ra, where M1 is H or Bc, and Bc is a biocompatible cation;
- R3 is H or an Rd group;
- R4 and R5 are independently an Rd group;
- R6 to R9 are independently C1-3 alkyl or an Rc group, and are chosen such that in Formula A, at least one of R6 to R9 is Rc;
- Ra is C1-4 sulfoalkyl;
- Rb is C1-6 carboxyalkyl;
- Rc is an Ra or Rb group;
- Rd is C1-5 alkyl or an Rc group;
- with the provisos that in Formula A:
- (i) at least one of the pairs of substituents R1/R2, R4/R5, R6/R8, and R7/R9 is different;
- (ii) the cyanine dye comprises at least one Rb group and a total of 3 to 6 sulfonic acid substituents from the R1, R2, Ra and Rc groups.
10 more elements
Dependencies are inferred from the claim text.