Conformationally restricted polyamine analogs as disease therapies for cancer, epilepsy, alzheimers, infections, grafts and others

摘要

A conformationally restricted polyamine analog of the formula: E-NH-B-A-B-NH-B-A-B-NH-B-A-B-NH-B-A-B-NH-E wherein: each A is independently selected from the group consisting of a single bond, Cl-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C6 cycloalkyl, C3-C6 cycloaryl, and C3-C6 cycloalkenyl; each B is independently selected from the group consisting of a single bond, C-C6 alkyl, and C2-C6 alkenyl; and each E is independently selected from the group consisting of H, Cl-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C6 cycloalkyl, C3-C6 cycloaryl, and C3-C6 cycloalkenyl; with the proviso that either at least one A moiety is selected from the group consisting of C2-C6 alkenyl, C2-C6 alkynyl, C3-C6 cycloalkyl, C3-C6 cycloaryl, and C3-C6 cycloalkenyl, or at least one B moiety is selected from the group consisting of C2-C6 alkenyl; and any salt or stereoisomer thereof. Such Compounds are useful in the treatment of diseases such as cancer and other diseases associated with cell proliferation, Alzheimer's disease, epilepsy, multiple sclerosis, problems associated with tissue grafts and organ transplants, psoriasis, restenosis, stomach ulcers, or tissue overgrowth after surgery, or an infection or infestation of parasites, bacteria, fungi or insects.