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Antiproliferative 1,2,3-thiadiazole compounds

, : Antiproliferative 1,2,3-thiadiazole compounds. Official Gazette of the United States Patent & Trademark Office Patents 1260(3), July 16

Pharmaceutical compositions and compounds are provided. The compounds of the invention have anti-proliferative activity, and may promote apoptosis in cells lacking normal regulation of cell cycle and death. In one embodiment of the invention, formulations of the compounds in combination with a physiologically acceptable carrier are provided. The pharmaceutical formulations are useful in the treatment of hyperproliferative disorders, which disorders include tumor growth, lymphoproliferative diseases, angiogenesis. The compounds of the invention are 1,2,3-thiadiazoles having the structure: ##STR1## and including stereoisomers, solvates, and pharmaceutically acceptable salts thereof, wherein each of R1, R2, R3 and R4 is independently selected from hydrogen, R5, R6, and R7 ; R5 is selected from alkyl, heteroalkyl, aryl and heteroaryl; R6 is selected from (R5)n -alkylene, (R5)n -heteroalkylene, (R5)n -arylene and (R5)n -heteroarylene; R7 is selected from (R6)n -alkylene, (R6)n -heteroalkylene, (R6)n -arylene, and (R6)n -heteroarylene; and n is selected from 0, 1, 2, 3, 4 and 5, where R1 and R2 may together form a heterocyclic structure including the nitrogen to which they are both attached, and R3 and R4 may together form a heterocyclic structure including the nitrogen to which they are both attached; and each of L1 and L2 is independently selected from --A1--A2--A3-- where each of A1, A2, and A3 is independently selected from a direct bond, alkylene, heteroalkylene, arylene and heteroarylene.


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