6026-73-9Relevant articles and documents
Production of [...] (by machine translation)
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Paragraph 0032, (2017/05/23)
Useful as an intermediate for the production of a horticultural [to] acaricidal agent can provide an industrially advantageous method for producing 3 - [...]. [Solution] nitro bromobenzene isobutene and the like, a palladium catalyst, a phosphine-based coordination, bases, solvents, and the auxiliary agent in the presence of reaction, isobutene was added to compound, the additional compound is isolated or not isolated, hydrogenation (catalytic reduction) by the production method 3 - [...] or salts thereof. [Drawing] no (by machine translation)
Discovery of olodaterol, a novel inhaled β2-adrenoceptor agonist with a 24 h bronchodilatory efficacy
Bouyssou, Thierry,Hoenke, Christoph,Rudolf, Klaus,Lustenberger, Philipp,Pestel, Sabine,Sieger, Peter,Lotz, Ralf,Heine, Claudia,Büttner, Frank H.,Schnapp, Andreas,Konetzki, Ingo
scheme or table, p. 1410 - 1414 (2010/07/10)
Compound 4p was identified from a series of 6-hydroxy-4H-benzo[1,4]oxazin-3-ones as potent agonist of the human β2-adrenoceptor with a high β1/β2-selectivity. A complete reversal of acetylcholine-induced bronchoconstrictio
Biphenylsulfonamide endothelin antagonists: Structure-activity relationships of a series of mono- and disubstituted analogues and pharmacology of the orally active endothelin antagonist 2'-amino-N-(3,4- dimethyl-5-isoxazolyl)-4'-(2-methylpropyl)[1,1'-biphenyl]-2-sulfonamide (BMS- 187308)
Murugesan, Natesan,Gu, Zhengxiang,Stein, Philip D.,Bisaha, Sharon,Spergel, Steve,Girotra, Ravi,Lee, Ving G.,Lloyd, John,Misra, Raj N.,Schmidt, Joan,Mathur, Arvind,Stratton, Leslie,Kelly, Yolanda F.,Bird, Eileen,Waldron, Tom,Liu, Eddie C.-K.,Zhang, Rongan,Lee, Helen,Serafino, Randy,Abboa-Offei, Benoni,Mathers, Parker,Giancarli, Mary,Seymour, Andrea Ann,Webb, Maria L.,Moreland, Suzanne,Barrish, Joel C.,Hunt, John T.
, p. 5198 - 5218 (2007/10/03)
Substitution at the ortho position of N-(3,4-dimethyl-5-isoxazolyl) benzenesulfonamide led to the identification of the biphenylsulfonamides as a novel series of endothelin-A (ETA) selective antagonists. Appropriate substitutions on the pendant phenyl ring led to improved binding as well as functional activity. A hydrophobic group such as isobutyl or isopropoxyl was found to be optimal at the 4'-position. Introduction of an amino group at the 2'-position also led to improved analogues. Combination of the optimal 4'- isobutyl substituent with the 2'-amino function afforded an analogue (20, BMS-187308) with improved ET(A) binding affinity and functional activity. Compound 20 also has good oral activity in inhibiting the pressor effect caused by an ET-1 infusion in rats. Doses of 10 and 30 μmol/kg iv 20 attenuated the pressor responses due to the administration of exogenous ET-1 to conscious monkeys, indicating that the compound inhibits the in vivo activity of endothelin-1 in nonhuman primates.