16440-97-4Relevant articles and documents
The identification of indacaterol as an ultralong-acting inhaled β2-adrenoceptor agonist
Baur, Fran?ois,Beattie, David,Beer, David,Bentley, David,Bradley, Michelle,Bruce, Ian,Charlton, Steven J.,Cuenoud, Bernard,Ernst, Roland,Fairhurst, Robin A.,Faller, Bernard,Farr, David,Keller, Thomas,Fozard, John R.,Fullerton, Joe,Garman, Sheila,Hatto, Julia,Hayden, Claire,He, Handan,Howes, Colin,Janus, Diana,Jiang, Zhengjin,Lewis, Christine,Loeuillet-Ritzler, Frederique,Moser, Heinz,Reilly, John,Steward, Alan,Sykes, David,Tedaldi, Lauren,Trifilieff, Alexandre,Tweed, Morris,Watson, Simon,Wissler, Elke,Wyss, Daniel
, p. 3675 - 3684 (2010)
Following a lipophilicity-based hypothesis, an 8-hydroxyquinolinone 2-aminoindan derived series of β2-adrenoceptor agonists have been prepared and evaluated for their potential as inhaled ultralong-acting bronchodilators. Determination of their activities at the human β2-adrenoceptor receptor showed symmetrical substitution of the 2-aminoindan moiety at the 5- and 6-positions delivered the targeted intermediate potency and intrinsic-efficacy profiles relative to a series of clinical reference β2-adrenoceptor agonists. Further assessment with an in vitro superfused electrically stimulated guinea-pig tracheal-strip assay established the onset and duration of action time courses, which could be rationalized by considering the lipophilicity, potency, and intrinsic efficacy of the compounds. From these studies the 5,6-diethylindan analogue indacaterol 1c was shown to possess a unique profile of combining a rapid onset of action with a long duration of action. Further in vivo profiling of 1c supported the long duration of action and a wide therapeutic index following administration to the lung, which led to the compound being selected as a development candidate.
TRANSITION METAL COMPOUND AND METHOD FOR PRODUCING OLEFIN POLYMER
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Paragraph 0072, (2018/11/27)
PROBLEM TO BE SOLVED: To provide a transition metal compound catalyst that makes it possible to synthesize an olefin polymer that is soft and has improved catalytic activity and reduced stereoregularity, and a method for producing an olefin polymer. SOLUTION: The present invention provides a compound represented by formula (IV) (X is a σ-binding or π-binding ligand; Y is a Lewis base; Y may be crosslinked to other Y and X; q is an integer of 1-5 and [(valence of M)-2]; r is an integer of 0-3; R1 and R2 independently represent H or halogen, alkyl or the like; R3-R10 are alkyl groups. M is metal elements of groups 3-10 or lanthanoid series in the periodic table; A1-A4 independently represent a crosslinking group composed of group 14 (C, Si, Ge, Sn)). SELECTED DRAWING: None COPYRIGHT: (C)2018,JPOandINPIT
METALLOCENE COMPLEX AND METHOD FOR PRODUCING OLEFIN POLYMER
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Paragraph 0130, (2016/10/07)
PROBLEM TO BE SOLVED: To provide a metallocene complex which, in homopolymerization of propylene, can produce homopolypropylene having a high melting point, and a method for producing an olefin polymer using the same. SOLUTION: Provided is a metallocene complex crosslinked by Si, such as dichlorosilacyclobutylenebis[2-(5-methyl-2-furyl)-4-phenyl-1,5,6,7-tetrahydro-s-indacen-1-yl]zirconium and dichlorosilacyclopentylenebis[2-(5-methyl-2-furyl)-4-phenyl-1,5,6,7-tetrahydro-s-indacen-1-yl]zirconium. Also provided is a catalyst for polymerizing an olefin such as propylene, comprising the complex, a compound which forms an ion pair by reacting with the complex or an ion-exchanging phyllosilicate, and an organoaluminum compound. COPYRIGHT: (C)2016,JPOandINPIT