PENTAAZA MACROCYCLIC RING COMPLEXES POSSESSING ORAL BIOAVAILABILITY

    公开(公告)号:US20210347796A1

    公开(公告)日:2021-11-11

    申请号:US17378852

    申请日:2021-07-19

    申请人: Galera Labs, LLC

    摘要: 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).

    RHENIUM COMPLEXES AND METHODS OF USE FOR TREATING CANCER

    公开(公告)号:US20210317151A1

    公开(公告)日:2021-10-14

    申请号:US17267687

    申请日:2019-08-16

    IPC分类号: C07F13/00 A61P35/00

    摘要: A composition comprising the following structure: (1) wherein Re represents a rhenium ion having a +1 charge; (I) represents an uncharged bidentate ligand containing at least one ring containing a ring nitrogen atom bound to the rhenium (Re), and the bidentate ligand containing another nitrogen atom, either in a ring or not in a ring, bound to the rhenium (Re); and L1, L2, L3, and L4 are neutral ligands with at least one neutral ligand being an isonitrile ligand of the formula —CN—R, wherein R is an aliphatic or aromatic hydrocarbon group containing 1-20 carbon atoms; and X− represents a non-coordinating monovalent anion; wherein the bidentate ligand and R are optionally substituted by one or more groups selected from (i)-(xi) as further discussed above. Methods for treating a condition that benefits from ER stress induction, such as cancer, by administering the above rhenium complex are also disclosed.