- Patent Title: Pentaaza macrocyclic ring complexes possessing oral bioavailability
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Application No.: US17378852Application Date: 2021-07-19
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Publication No.: US12077549B2Publication Date: 2024-09-03
- Inventor: Jeffery L. Keene , Otto F. Schall , Dennis P. Riley
- Applicant: Galera Labs, LLC
- Applicant Address: US MO Creve Coeur
- Assignee: Galera Labs, LLC
- Current Assignee: Galera Labs, LLC
- Current Assignee Address: US PA Malvern
- Agency: Bryan Cave Leighton Paisner LLP
- Main IPC: C07F13/00
- IPC: C07F13/00 ; A61K9/00 ; A61K9/28 ; A61K9/48 ; A61K31/28 ; A61K31/555 ; A61K47/14 ; A61K47/38 ; A61K47/44 ; A61P1/00 ; A61P17/00

Abstract:
Aspects of the present disclosure relate to compounds which have enhanced oral bioavailability. A transition metal complex includes a transition metal coordinated by a macrocycle comprising the pentaaza 15-membered macrocyclic ring corresponding to Formula A and two axial ligands having the formula —OC(O)X1.
each of the two axial ligands has the formula —OC(═O)X1 wherein each X1 is independently substituted or unsubstituted phenyl or —C(—X2)(—X3)(—X4);
each X2 is independently substituted or unsubstituted phenyl, or substituted or unsubstituted alkyl;
each X3 is independently hydrogen, hydroxyl, alkyl, amino, —X5C(═O)R13 where X5 is NH or O, and R13 is C1-C18 alkyl, substituted or unsubstituted aryl or C1-C18 aralkyl, or —OR14, where R14 is C1-C18 alkyl, substituted or unsubstituted aryl or C1-C18 aralkyl, or together with X4 is (═O); and
each X4 is independently hydrogen or together with X3 is (═O).
each of the two axial ligands has the formula —OC(═O)X1 wherein each X1 is independently substituted or unsubstituted phenyl or —C(—X2)(—X3)(—X4);
each X2 is independently substituted or unsubstituted phenyl, or substituted or unsubstituted alkyl;
each X3 is independently hydrogen, hydroxyl, alkyl, amino, —X5C(═O)R13 where X5 is NH or O, and R13 is C1-C18 alkyl, substituted or unsubstituted aryl or C1-C18 aralkyl, or —OR14, where R14 is C1-C18 alkyl, substituted or unsubstituted aryl or C1-C18 aralkyl, or together with X4 is (═O); and
each X4 is independently hydrogen or together with X3 is (═O).
Public/Granted literature
- US20210347796A1 PENTAAZA MACROCYCLIC RING COMPLEXES POSSESSING ORAL BIOAVAILABILITY Public/Granted day:2021-11-11
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