Patent ID: 11944690
Assignee: BAYER AKTIENGESELLSCHAFT
Field: Pharmaceuticals (Chemistry)
Classification: CPC A | IPC A

Claim 0:
1. A liquid pharmaceutical formulation comprising a DO3A -derived tetra-chelate of general formula (I):, wherein
R1 represents a group selected from:, wherein group * indicates the point of attachment of the group with the rest of the molecule,
R2, R3, and R4 independently of each other represents a hydrogen atom or a group selected from: C1-C6-alkyl, C3-C6-cycloalkyl, (C1-C2-alkoxy)-(C2-C3-alkyl)-, and phenyl,
wherein the C1-C6-alkyl group is optionally substituted, identically or differently, with a phenyl substituent, wherein the phenyl substituent is optionally substituted, one, two or three times, identically or differently, with a group selected from a halogen atom, C1-C3-alkyl, C1-C3-haloalkyl, and C1-C3-alkoxy, and
wherein the phenyl group is optionally substituted, one, two or three times, identically or differently, with a group selected from a halogen atom, C1-C3-alkyl, C1-C3-haloalkyl, and C1-C3-alkoxy,

R5 represents a group selected from:
C1-C6-alkyl, C3-C6-cycloalkyl, (C1-C2-alkoxy)-(C2-C3-alkyl)- and phenyl,
wherein the C1-C6-alkyl group is optionally substituted, identically or differently, with a phenyl substituent, wherein the phenyl substituent is optionally substituted, one, two or three times, identically or differently, with a group selected from a halogen atom, C1-C3-alkyl, C1-C3-haloalkyl, and C1-C3-alkoxy, and
wherein the phenyl group is optionally substituted, one, two, or three times, identically or differently, with a group selected from a halogen atom, C1-C3-alkyl, C1-C3-haloalkyl, and C1-C3-alkoxy,

X represents a group C(═O)OH or C(═O)O−, and
M represents Gd3+,
or a stereoisomer, a tautomer or a salt thereof, or a mixture of same,
wherein the formulation further comprises a pharmaceutically acceptable solvent; and
at least one compound capable of forming a chelate with a free paramagnetic metal ion M, wherein the at least one compound is Ca-BT-DO3A (Calcobutrol) in a concentration range of 0.002% to 5% mol/mol (inclusive), measured as a proportion relative to a total concentration of the Gd3− ion in the formulation,
wherein the DO3A-derived tetra-chelate has a concentration in the formulation in a range of 60 to 750 mmol paramagnetic Gd3−/L (inclusive).