- A nitric oxide donor nature of the benzofuran compounds (by machine translation)
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The invention discloses a benzofuran compound with nitrous oxide donor property. The benzofuran compound is a compound shown by a general formula (I) or a pharmaceutically acceptable salt thereof, wherein in the formula, R1 or R2 represents independent hy
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Paragraph 0211-0212
(2017/04/20)
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- Novel and highly potent histamine H3 receptor ligands. Part 3: An alcohol function to improve the pharmacokinetic profile
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Synthesis and biological evaluation of potent histamine H3 receptor antagonists incorporating a hydroxyl function are described. Compounds in this series exhibited nanomolar binding affinities for human receptor, illustrating a new possible component for the H3 pharmacophore. As demonstrated with compound BP1.4160 (cyclohexanol 19), the introduction of an alcohol function counter-intuitively allowed to reach high in vivo efficiency and favorable pharmacokinetic profile with reduced half-life.
- Labeeuw, Olivier,Levoin, Nicolas,Poupardin-Olivier, Olivia,Calmels, Thierry,Ligneau, Xavier,Berrebi-Bertrand, Isabelle,Robert, Philippe,Lecomte, Jeanne-Marie,Schwartz, Jean-Charles,Capet, Marc
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p. 2548 - 2554
(2013/06/27)
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- Process for preparing dronedarone
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The present invention relates to a process for preparing dronedarone and in particular for preparing an intermediate useful in the preparation of dronedarone. Furthermore, the present invention relates to a process for preparing crystalline dronedarone hydrochloride as well as pharmaceutical compositions comprising this salt.
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Page/Page column 9
(2011/10/13)
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- Novel and highly potent histamine H3 receptor ligands. Part 1: Withdrawing of hERG activity
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Pre-clinical investigation of some aryl-piperidinyl ether histamine H3 receptor antagonists revealed a strong hERG binding. To overcome this issue, we have developed a QSAR model specially dedicated to H3 receptor ligands. This model was designed to be di
- Levoin, Nicolas,Labeeuw, Olivier,Calmels, Thierry,Poupardin-Olivier, Olivia,Berrebi-Bertrand, Isabelle,Lecomte, Jeanne-Marie,Schwartz, Jean-Charles,Capet, Marc
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scheme or table
p. 5378 - 5383
(2011/10/12)
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- NPY ANTAGONISTS, PREPARATION AND USES
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The present invention concerns novel compounds, their preparation and their uses, therapeutic uses in particular. More specifically it concerns derivative compounds having at least two aromatic cycles, their preparation and their uses, in particular in the area of human or animal health. These compounds have an affinity for the biological receptors of neuropeptide Y, NPY, present in the central and peripheral nervous systems. The compounds of the invention are preferably NPY antagonists, and more particularly antagonists of sub-type NPY Y1, and can therefore be used for the therapeutic or prophylactic treatment of any disorder involving NPY. The present invention also concerns pharmaceutical compositions containing said compounds, their preparation and their uses, as well as treatment methods using said compounds.
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Page/Page column 57
(2009/09/28)
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- Phenoxypropylpiperidines and -pyrrolidines and their use as histamine H3-receptor ligands
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The present patent application concerns compounds of formula (I), with R1 and R2 taken together with the nitrogen atom to which they are attached, form a mono or bicyclic saturated nitrogen-containing ring; their preparation and their use as a H3 receptor ligand for treating e.g. CNS disorders like Alzheimer's disease.
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Page/Page column 13; 21; 24
(2008/06/13)
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- Fibrinogen receptor antagonists
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Novel fibrinogen receptor antagonists of the formula: are provided in which the claimed compounds exhibit fibrinogen receptor antagonist activity, inhibit platelet aggregation and are therefore useful in modulating thrombus formation.
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- Arylalkylheterocyclic amines,N-substituted by aryloxyalkyl group in a method for allergy treatment
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A method of inhibiting Type 1 allergic responses in a living animal body with substituted heterocyclic amines is disclosed wherein the active agents are expressed generally by the formula which includes certain known and certain known compounds: STR1 wherein P is zero, one or two; m is one to six inclusive; A is selected from hydrogen, hydroxy or cyano; d is zero or one; Q is --CH--, CH2 -- or STR2 n is zero or one and when Q is --CH-- and n is one, a double bond is formed with one of the adjacent carbons but not both at the same time, and when n and d are zero at the same time, a double bond is formed between the α carbon and a carbon of the central heterocyclic amine ring; Ar, D and R are selected from phenyl, substituted phenyl, pyridinyl, thienyl, furanyl or naphthyl and in addition, R may have the values benzyl, substituted benzyl, cycloalkyl or loweralkyl and D may additionally have the values: 2H-1-benzopyran-2-one,4-oxo-4H-1-benzopyran-2-carboxylic acid loweralkyl ester, 2,3-dihydro-4H-1-benzopyran-4-one, 1,4-benzodioxanloweralkyl-2-yl or 1,1'-biphenyl-4-yl and the pharmaceutically acceptable salts thereof.
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- Synthesis and Antiallergy Activity of 4-(Diarylhydroxymethyl)-1-piperidines and Structurally Related Compounds
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A series of 4-(diarylhydroxymethyl)-1-piperidines was synthesized and evaluated for antiallergy activity.Several analogues had potent activity in the passive foot anaphylaxis (PFA) assay, an IgE-mediated model useful in the detection of compounds possessing antiallergic activity.In particular 1--1-piperidinyl>propoxy>-3-methoxyphenyl>ethanone (1, AHR-5333) was more potent than oxatomide and terfenadine in this assay.
- Walsh, David A.,Franzyshen, Stephen K.,Yanni, John M.
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p. 105 - 118
(2007/10/02)
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