Patent Number: 6,251,363

Title: Diagnostic and therapeutic alkylenediamine compounds and process

Abstract: Diamine compounds useful for treating neurodegenerated diseases characterized by the lack of dopamine neurons activity or for imaging the dopamine neurons are provided. The diamine compounds or serotonin are characterized by the formula: ##STR1## l, m and n can be the same or different and are an integer of 1 to 6; X, Y and Z can be the same or different and are hydrogen, halo, haloalkyl, (C.sub.1 -C.sub.6) alkyl, aryl, (C.sub.1 -C.sub.6) alkoxy, N-alkyl, (C.sub.2 -C.sub.6) acyloxy, N-alkylene, --SH or --SR, wherein R is from the same group as R.sub.1 and R.sub.2 and can be the same or different than R.sub.1 and R.sub.2, amino, nitro, cyano, hydroxy, --C(.dbd.O) OR.sub.6, --C(.dbd.O) NR.sub.5 R.sub.4, NR.sub.3 R.sub.2, or S(.dbd.O).sub.k R.sub.i wherein .sub.k is 1 or 2, and R.sub.4 to R.sub.6 are independently hydrogen or (C.sub.1 -C.sub.6) alkyl; R.sub.1, and R.sub.2 can be the same or different and are hydrogen, (C.sub.1 -C.sub.6) alkyl, hydroxyalkyl or mercaptoalkyl, --C(.dbd.O) OR.sub.1, cyano, (C.sub.1 -C.sub.6) alkenyl, (C.sub.2 -C.sub.6) alkynyl or 1, 2, 4-oxadiazol-5-yl optionally substituted at he 3-position by W wherein any (C.sub.1 -C.sub.6) alky, (C.sub.1 -C.sub.6) alkanoly, (C.sub.2 -C.sub.6) alkenyl or (C.sub.2 -C.sub.6) alkynyl (C.sub.1 -C.sub.6) alkyl, hydroxy (C.sub.1 -C.sub.6) alkyl or mercapto (C.sub.1 -C.sub.6) alkyl and optionally can be substituted by 1, 2 or 3 Z; W is (C.sub.1 -C.sub.6) alkyl or phenyl, optionally substituted by 1, 2 or 3 Z. .PHI. is phenyl, naphthyl, thienyl or pyridinyl.

Inventors: Elmaleh; David R. (Newton, MA), Hanson; Robert N. (Newton, MA), Sung-Woon; Choi (Norwood, MA)

Assignee: The General Hospital

International Classification: C07C 217/48 (20060101); C07C 233/78 (20060101); C07C 217/00 (20060101); C07C 233/00 (20060101); C07B 59/00 (20060101); C07D 241/00 (20060101); C07D 241/08 (20060101); C07D 211/00 (20060101); C07D 211/26 (20060101); C07D 211/58 (20060101); A61K 051/00 (); A61M 036/14 ()

Expiration Date: 06/26/2018