926256-60-2Relevant articles and documents
HETEROCYCLIC COMPOUNDS AND METHODS FOR THEIR USE
-
Page/Page column 59; 60, (2016/09/26)
The present invention relates to heterocyclic compounds useful for antagonising angiotensin II Type 2 (AT2) receptor. More particularly the invention relates to compounds of formula (I), as described herein, compositions containing them and their use in methods of treating or preventing disorders or diseases associated with AT2 receptor function including neuropathic pain, inflammatory pain, conditions associated with neuronal hypersensitivity, impaired nerve conduction velocity, cell proliferation disorders, disorders associated with an imbalance between bone resorption and bone formation and disorders associated with aberrant nerve regeneration.
Synthesis, determination of absolute configuration, and biological evaluation of spiro-fused thiadiazoline inhibitors of kinesin spindle protein (KSP)
Angeles, Angie R.,Yang, Liping,Dai, Chaoyang,Brunskill, Andrew,Basso, Andrea D.,Siddiqui, M. Arshad
supporting information; experimental part, p. 6236 - 6239 (2011/01/12)
A facile and highly convergent synthesis of biologically active spiro-fused thiadiazoline KSP inhibitors is reported. The highlights of the synthesis include the Michael reaction and cyclization of thiosemicarbazone to 1,3,4-thiadiazoline. This chemistry lends itself to the preparation of (+)-2, a potent and orally bioavailable anti-cancer agent, and to the development of a structure-activity relationship program.