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US 2025/0017888 A1Published application
Compounds for treating diseases associated with hyaluronan overproduction
AssigneeThe Royal Veterinary College
InventorsPeter PREHM, Behzad JAVAHERI, Andrew PITSILLIDES
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Abstract
There are provided compounds of formula (I): [hyaluronan production inhibitor]-[labile linker]-X (I), which compounds are useful in the treatment of diseases associated with hyaluronan overproduction.
Claims23
A compound of Formula Ia:
- [hyaluronan production inhibitor]-[labile linker]-X (Ia),
- or a pharmaceutically acceptable salt thereof,
- wherein the hyaluronan production inhibitor fragment is of:
- formula A
- wherein Y is a group selected from the group consisting of:
- RA1, RA2, and RA4 are each independently selected from the group consisting of —OH, —ORA5, halo, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, which C1-6 alkyl, C2-6 alkenyl and C2-6 alkynyl groups are optionally substituted by one or more groups selected from halo, —OH and —OMe;
- and one RA1, RA2 or RA4 group is
- n is 0 to 5;
- m is 0 to 5;
- and
- RA5 is C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, which three groups are optionally substituted by one or more groups selected from halo, —OH and —OMe;
- formula B
- wherein RB1, RB2, and RB3 are each independently selected from the group consisting of —OH, —ORB4, halo, C1-6 alkyl, C2-6 alkenyl, and C2-6 alkynyl, which C1-6 alkyl, C2-6 alkenyl and C2-6 alkynyl groups are optionally substituted with one or more groups selected from halo, —OH and —OMe;
- and one RB2 or RB3 group is
- n is 0 to 4;
- m is 0 to 5;
- RB4 is C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, which three groups are optionally substituted by one or more groups selected from halo, —OH and —OMe;
- formula C
- wherein the wavy line represents the point of attachment to the labile linker fragment;
- formula D
- wherein the wavy line represents the point of attachment to the labile linker fragment;
- or
- formula E
- wherein the wavy line represents the point of attachment to the labile linker fragment;
- the labile linker fragment is —OC(O)RL1—;
- wherein RL1 is selected from C1-6 alkylene, C2-6 alkenylene, C2-6 alkynylene, arylene, or heteroarylene, which five groups are optionally substituted with one or more groups independently selected from halo, —ORL2 or ═O;
- RL2 represents H or C1-6 alkyl;
- X is selected from the group consisting of quaternary ammonium, quaternary phosphonium, pyridinium and thiazolium salts;
- or
- X is
- wherein R5 is C1-6 alkyl.
28 more elements
(canceled)
-33. (canceled)
A method of treatment according to claim 37, wherein the diseased characterised by hyaluronan overproduction is cancer, optionally wherein the cancer is sarcoma, or chondrosarcoma.
Dependencies are inferred from the claim text.