195447-69-9Relevant academic research and scientific papers
Biphenylsulfonamide endothelin receptor antagonists. 4. Discovery of N-[[2′-[[(4,5-dimethyl-3-isoxazolyl)amino]sulfonyl]-4- (2-oxazolyl)[1,1′-biphenyl]-2-yl]methyl]-N,3,3-trimethylbutanamide (BMS-207940), a highly potent and orally active ETA s
Murugesan, Natesan,Gu, Zhengxiang,Spergel, Steven,Young, Marian,Chen, Ping,Mathur, Arvind,Leith, Leslie,Hermsmeier, Mark,Liu, Eddie C.-K.,Zhang, Rongan,Bird, Eileen,Waldron, Tom,Marino, Anthony,Koplowitz, Barry,Humphreys, W. Griffith,Chong, Saeho,Morrison, Richard A.,Webb, Maria L.,Moreland, Suzanne,Trippodo, Nick,Barrish, Joel C.
, p. 125 - 137 (2007/10/03)
We have previously disclosed the selective ETA receptor antagonist N-(3,4-dimethyl-5-isoxazolyl)-4′-(2-oxazolyl)[1,1′- biphenyl]-2-sulfonamide (1, BMS-193884) as a clinical development candidate. Additional SAR studies at the 2′-position of 1 l
Substituted biphenyl isoxazole sulfonamides
-
, (2008/06/13)
Compounds of the formula STR1 inhibit the activity of endothelin. The symbols are defined as follows: R1, R2, R3 and R4 are each directly bonded to a ring carbon and are each independently (a) hydrogen; (b) alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, cycloalkylalkyl, cycloalkenyl, cycloalkenylalkyl, aryl, aryloxy, aralkyl or aralkoxy, any of which may be substituted with Z1, Z2 and Z3 ; (c) halo; (d) hydroxyl; (e) cyano; (f) nitro; (g) --C(O)H or --C(O)R5 ; (h) --CO2 H or --CO2 R5 ; (i) --Z4 --NR6 R7 ; (j) --Z4 --N(R10)--Z5 --NR8 R9 ; or (k) R3 and R4 together may also be alkylene or alkenylene, either of which may be substituted with Z1, Z2 and Z3, completing a 4- to 8-membered saturated, unsaturated or aromatic ring together with the carbon atoms to which they are attached; and the remaining symbols are as defined in the specification.
