157672-20-3Relevant academic research and scientific papers
INDOLE DERIVATIVES AS CRAC MODULATORS
-
Page/Page column 30-31, (2012/01/30)
Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein R1, R2, R3 and R4 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with calcium release-activated calcium channels (CRAC).
Preparation of 2-substituted oxazoles
Pandit, Chennagiri R.,Polniaszek, Richard P.,Thottathil, John K.
, p. 2427 - 2432 (2007/10/03)
A simple and economical method for 2-substituted oxazole synthesis and its scope are described.
Biphenylsulfonamide endothelin receptor antagonists. 2. Discovery of 4'-oxazolyl biphenylsulfonamides as a new class of potent, highly selective ET(A) antagonists
Murugesan,Gu,Stein,Spergel,Mathur,Leith,Liu,Zhang,Bird,Waldron,Marino,Morrison,Webb,Moreland,Barrish
, p. 3111 - 3117 (2007/10/03)
The synthesis and structure-activity relationship (SAR) studies of a series of 4'-oxazolyl-N-(3,4-dimethyl-5-isoxazolyl)[1, 1'-biphenyl]-2-sulfonamide derivatives as endothelin-A (ET(A)) receptor antagonists are described. The data reveal a remarkable improvement in potency and metabolic stability when the 4'-position of the biphenylsulfonamide is substituted with an oxazole ring. Additional 2'-substitution of an acylaminomethyl group further increased the binding activity and provided one of the first subnanomolar ET(A)-selective antagonists in the biphenylsulfonamide series (17, ET(A) K(i) = 0.2 nM). Among the compounds described, 3 (N-(3,4-dimethyl-5-isoxazolyl)-4'-(2-oxazolyl)[1,1'-biphenyl]-2-s ulfonamide; BMS-193884) had the optimum pharmacological profile and was therefore selected as a clinical candidate for studies in congestive heart failure.
SUBSTITUTED BIPHENYL ISOXAZOLE SULFONAMIDES
-
, (2008/06/13)
Compounds of the formula STR1 inhibit the activity of endothelin. The symbols are defined as follows: R 1, R 2, R 3 and R 4 are each directly bonded to a ring carbon and are each independently(a) hydrogen;(b) alkyl, alkenyl, alkynyl, alkoxy,
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.
SUBSTITUTED BIPHENYL ISOXAZOLE SULFONAMIDES
-
, (2008/06/13)
Compounds of the formula STR1 inhibit the activity of endothelin. The symbols are defined as follows: R 1, R 2, R 3 and R 4 are each directly bonded to a ring carbon and are each independently(a) hydrogen;(b) alkyl, alkenyl, alkynyl, alkoxy,
