Search results for "Amine derivatives"
showing 10 items of 22 documents
Photochemical intermediates of trans-Rh(CO)L2Cl where L=PMe3, PBu3, and i-Pr2HN and cis-Rh(CO)2(i-Pr2HN)Cl in frozen organic glasses
2002
International audience; The Nujol glass matrix photolyses of Rh(CO)(PMe3)2Cl (1), Rh(CO)(PBu3)2Cl (2), Rh(CO)2(i-Pr2HN)Cl (3), and Rh(CO)(i-Pr2HN)2Cl (4), have been examined. Phototolysis of 1 (λirr>400 nm) and 2 (350<λirr<400 nm) give new species, A, with carbonyl stretching bands slightly below the parent bands. In the case of 1 this species appears to give rise to a second product, C, upon either extended photolysis or annealing. High-energy photolysis of 1, 2, and 4, result in loss of CO and formation of an IR silent species, RhL2Cl. In the case of 1 a new carbonyl species, B, is observed upon high-energy photolysis or annealing of a matrix containing CO and Rh(PMe3)2Cl. B may be conver…
A dose-ranging study of indacaterol in obstructive airways disease, with a tiotropium comparison.
2008
This dose-ranging study assessed the bronchodilator efficacy and tolerability of indacaterol, a novel once-daily inhaled beta2-agonist, in subjects clinically diagnosed with COPD. Comparative data with tiotropium were collected. In the double-blind, core period of the study, 635 subjects with COPD (prebronchodilator FEV(1)40% of predicted and > or =1.0L; FEV1/FVC <70%) were randomized to receive indacaterol 50, 100, 200 or 400microg or placebo via multi-dose dry powder inhaler, or indacaterol 400microg via single-dose dry powder inhaler, once daily for 7 days. After completing double-blind treatment and washout, a subset of subjects from each treatment group entered an open-label extension …
Efficacy and safety of indacaterol and tiotropium in COPD patients according to dyspnoea severity.
2013
Background Guidelines for chronic obstructive pulmonary disease (COPD) recommend that treatment choices be based partly on symptoms. Methods A post-hoc analysis of pooled data from clinical studies compared the efficacy and safety of once-daily inhaled bronchodilators indacaterol (150 and 300 μg) and open-label tiotropium (18 μg) according to baseline dyspnoea severity on the modified Medical Research Council (mMRC) scale in patients with COPD (mMRC scores <2 = ‘less dyspnoea’; scores ≥2 = ‘more dyspnoea’). Outcomes were assessed after 26 weeks. Results The analysis included 3177 patients. In patients with less dyspnoea: indacaterol (both doses) improved 24-h post-dose (‘trough’) forced exp…
Blinded 12-week comparison of once-daily indacaterol and tiotropium in COPD.
2011
Two, once daily (q.d.) inhaled bronchodilators are available for the treatment of chronic obstructive pulmonary disease (COPD): the β(2)-agonist indacaterol and the anticholinergic tiotropium. This blinded study compared the efficacy of these two agents and assessed their safety and tolerability. Patients with moderate-to-severe COPD were randomised to treatment with indacaterol 150 μg q.d. (n=797) or tiotropium 18 μg q.d. (n=801) for 12 weeks. After 12 weeks, the two treatments had similar overall effects on "trough" (24 h post-dose) forced expiratory volume in 1 s. Indacaterol-treated patients had greater improvements in transition dyspnoea index (TDI) total score (least squares means 2.0…
Alternative mechanisms for tiotropium
2009
Tiotropium is commonly used in the treatment of chronic obstructive pulmonary disease. Although largely considered to be a long-acting bronchodilator, its demonstrated efficacy in reducing the frequency of exacerbations and preliminary evidence from early studies indicating that it might slow the rate of decline in lung function suggested mechanisms of action in addition to simple bronchodilation. This hypothesis was examined in the recently published UPLIFT study and, although spirometric and other clinical benefits of tiotropium treatment extended to four years, the rate of decline in lung function did not appear to be reduced by the addition of tiotropium in this study. This article summ…
Plant-growth-regulatingN-(phosphonoacetyl)amines
1994
A series of N‐(phosphonacetyl)amine derivatives were synthesized and screened for plant‐growth regulating activity on Lepidium sativum L. and Cucumis sativus L. Aromatic N‐(phosphonoacetyl)amines. which may be considered as possible analogues of N‐acylaniline herbicides obtained by replacement of their acyl group by the phosphonacetyl moiety, exhibited significant or moderate herbicidal activity. In contrast, N‐(phosphonoacetyl)amino acids and N‐(phosphonoacetyl)aminophosphonic acids promoted the growth of L. sativum and C. sativus roots.
One-Pot Three-Component Solvent-Free Syntheses of n-Alkyl-Bridged N,N,N,N-tetra(2-hydroxybenzyl)diamines and N,N-bis(2-hydroxybenzyl) amines
2010
A simple solvent-free method to prepare four N,N,N’,N’-tetra(2-hydroxy-3,5dimethylbenzyl)diaminoalkanes and four N,N,N’,N’-tetra(2-hydroxy-5-t-butyl-3-methylbenzyl)-diaminoalkanes containing a long n-alkyl-bridge (58 CH2 groups between N-atoms) is described. In addition, preparations of four dihydrochlorides of prepared n-alkyl-bridged N,N,N’,N’-tetra(2-hydroxybenzyl)diamines are described. This method was also tested in the preparation of eight previously reported N,N-bis(2-hydroxybenzyl)amine derivatives.
Studien zum Vorgang der Wasserstoffübertragung, 53. Beitrag zur Kenntnis der elektroreduktiven Spaltung von Hydroxylaminderivaten
1978
Die Elektroreduktion von 26 Hydroxylaminderivaten wird polarographisch und an 6 Beispielen praparativ untersucht. Es wurde gefunden: 1) Dreifach mit Alkyl- oder Arylgruppen substituierte Hydroxylaminderivate werden bis zu einem Potential von -2.5 V (gegen Ag/AgCl/KClges.) nicht elektroreduziert. — 2) Der Einbau von Acylgruppen erleichtert in Abhangigkeit von Art, Zahl und Verknupfungsstelle die Elektroreduktion. Acylreste mit aromatischen Gruppen verschieben das Halbstufenpotential starker nach positiven Werten als aliphatisch substituierte Acylreste (entsprechend: Phthaloyl > Benzoyl > Formyl > Acetyl > Ethoxycarbonyl). Acylgruppen am Sauerstoff des Hydroxylamins fordern die Elektroredukti…
H2-Antihistaminika, 8. Mitt. Synthese potentieller H2-Antihistaminika der Ethylendiamin-Reihe
1982
Als potentielle H2-Antihistaminika wurden die Ethylendiaminderivate 8,9 und 13 dargestellt und auf ihre H2-antihistaminische Wirksamkeit untersucht. H2-Antihistaminics, VIII: Synthesis of Potential H2-Antihistaminics with Ethylenediamine Structure As potential H2-antihistaminics, the ethylenediamine derivatives 8,9 and 13 were prepared and tested for their H2-antihistaminic activity.
Acetylcholine mediates the release of IL-8 in human bronchial epithelial cells by a NFkB/ERK-dependent mechanism
2007
Acetylcholine may play a role in cell activation and airway inflammation. We evaluated the levels of both mRNA and protein of muscarinic M(1), M(2), M(3) receptors in human bronchial epithelial cell line (16HBE). 16HBE cells were also stimulated with acetylcholine and extracellular signal-regulated kinase1/2 (ERK1/2) and NFkB pathway activation as well as the IL-8 release was assessed in the presence or absence of the inhibitor of Protein-kinase (PKC) (GF109203X), of the inhibitor of mitogenic activated protein-kinase kinase (MAPKK) (PDO9805), of the inhibitor of kinaseB-alpha phosphorilation (pIkBalpha) (BAY11-7082), and of muscarinic receptor antagonists tiotropium bromide, 4-Diphenylacet…