Abstract: The disclosure relates to macrocyclic peptides and pharmaceutical compositions thereof. The disclosure further relates to pharmaceutical compositions for modulating opioid receptor activity. The macrocyclic tetrapeptides provided herein are useful in treating diseases or disorders relating to the activity of one or more opioid receptors, such as neurological disorders.

Abstract: The present invention is directed to novel aminooxy-cyclodextrin derivatives of the formula (1): CD—(X—Y—ONH2)n, wherein CD is mono- or polydeoxy ?-, ?-, or ?-cyclodextrin, carrying in its 6-, 3- and/or 2-position a group containing the aminooxy group, and optionally carrying substituents different from (X—Y—ONH2). Y is a linker group between the aminooxy group and the mono- or polydeoxy-CD group, X is a functional group or an atom necessary to connect the linker Y and the deoxy CD group, or Y is a direct bond when X is a direct bond, and n is ?1, but ?24, 21 and 18 for ?-, ?- or ?-cyclodextrin, respectively, the protected aminooxy derivatives thereof, as well the methods for their preparation and use.