Back to results
US 11,957,735 B2Granted
Releasable GLP-1 conjugates
AssigneeQuiaPEG Pharmaceuticals AB
InventorsMarek Kwiatkowski, Christian Sund
Life of this patent
Estimating the term…
Abstract
The present application provides compounds of Formula (I): or pharmaceutically acceptable salts thereof, wherein D is a residue of a GLP-polypeptide or an analog thereof, which underdo hydrolysis under physiological conditions to release the GLP-polypeptide or analog thereof and which are useful in the treatment of disorders that could be beneficially treated with the GLP-polypeptide or analog thereof.
Claims20
A compound of Formula (I):
- or a pharmaceutically acceptable salt thereof, wherein:
- the aliphatic moiety is a polyethylene glycol having an average molecular weight from about 500 Da to about 40,000 Da;
- D is a residue of a GLP-1 polypeptide or an analog thereof;
- Z1 is selected from O, S, and N(RN);
- Z3 is selected from O and N(RN), or Z3 is absent;
- A is O or N, wherein when A is O then R3 is absent;
- RN is selected from H and optionally substituted C1-6 alkyl;
- R3 is selected from H and C1-6 alkyl, or
- R3 and R1, together with A and the carbon atom to which R1 is attached, form an optionally substituted 4 to 7 membered aliphatic heterocyclic ring;
- or
- R3 and R2, together with A, the carbon atom to which R1 is attached, and the carbon atom to which R2 is attached, form an optionally substituted 4 to 8 membered aliphatic heterocyclic ring;
- MA is a self-immolative group having any one of formulae (a)-(i):
- wherein x denotes a point of attachment to Z1 and y denotes a point of attachment to Z3;
- R1 and R2 are independently selected from the group consisting of hydrogen, optionally substituted C1-6 alkyl, optionally substituted C6-10 aryl and optionally substituted 5- to 14-membered heteroaryl;
- or R1 and R2 are joined together with the carbon atoms to which they are attached to form an optionally substituted C3-7 cycloalkyl ring, an optionally substituted 4 to 7 membered aliphatic heterocyclic ring, an optionally substituted C6-10 aryl or an optionally substituted 5-to 14-membered heteroaryl;
- or R1 and R2 are joined together to form a ribose ring system;
- R7 and R8 are independently selected from H and C1-6 alkyl;
- and
- E is a cleavable moiety.
16 more elements
Dependencies are inferred from the claim text.