Jeffrey I Krieger

US Patent:

57391696, Apr 14, 1998

Filed:

May 31, 1996

Appl. No.:

8/656468

Inventors:

Timothy D. Ocain - Framingham MA
Huai Gao - Groton MA
Jeffrey I. Krieger - Newton MA
Theresa M. Sampo - Boston MA

Assignee:

Procept, Incorporated - Cambridge MA

International Classification:

A61K 31135
A01N 3302
C07C22900

US Classification:

514658

Abstract:

Novel compounds ##STR1## wherein R. sup. 1 to R. sup. 13 are independently selected from C. sub. 2 -C. sub. 4 linear and branched alkyls, H, NH. sub. 2, CH. sub. 3, OR. sup. 14, fluorine, chlorine, iodine, NO. sub. 2, CF. sub. 3, NHCOCH. sub. 3, NHCOOtBu, NHR. sup. 15, NR. sup. 16 R. sup. 17 and phenyl, for use as immunosuppressive agents to prevent or significantly reduce graft rejection in organ and bone marrow transplantation are described. The novel compounds can also be used as an immunosuppressant drug for T-lymphocyte mediated autoimmune diseases, such as diabetes, and may be useful in alleviating psoriasis and contact dermatitis. Additionally, the novel compounds can be used for antiproliferation and gene therapy.