Search Results - "DELCANALE, Maurizio"
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Novel Class of Benzoic Acid Ester Derivatives as Potent PDE4 Inhibitors for Inhaled Administration in the Treatment of Respiratory Diseases
Published in Journal of medicinal chemistry (13-02-2014)“…The first steps in the selection process of a new anti-inflammatory drug for the inhaled treatment of asthma and chronic obstructive pulmonary disease are…”
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Pharmacological actions of a novel, potent, tissue-selective benzopyran estrogen
Published in The Journal of pharmacology and experimental therapeutics (01-10-2002)“…We have identified a new benzopyran derivative, 3-(4-methoxy) phenyl-4-[[4-[2-(1-piperidinyl)ethoxy]phenyl]methyl]-2H-1-benzopyran-7-ol hydrochloride (CHF…”
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Effects of 3-phenyl-4-[[4-[2-(1-piperidinyl)ethoxy]phenyl]methyl]- 2H-1-benzopyran-7-ol (CHF 4056), a novel nonsteroidal estrogen agonist/antagonist, on reproductive and nonreproductive tissue
Published in The Journal of pharmacology and experimental therapeutics (01-03-2002)“…We have discovered a new, nonsteroidal, estrogen agonist/antagonist, 3-phenyl-4-[[4-[2-(1-piperidinyl)ethoxy]phenyl] methyl]-2H-1-benzopyran-7-ol (CHF 4056)…”
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Optimization of M3 Antagonist–PDE4 Inhibitor (MAPI) Dual Pharmacology Molecules for the Treatment of COPD
Published in Journal of medicinal chemistry (24-08-2023)“…Aiming at the inhaled treatment of pulmonary diseases, the optimization process of the previously reported MAPI compound 92a is herein described. The project…”
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Discovery of a Potent, Selective, and Orally Bioavailable Tool Compound for Probing the Role of Lysophosphatidic Acid Type 2 Receptor Antagonists in Fibrotic Disorders
Published in Journal of medicinal chemistry (27-04-2023)“…Idiopathic pulmonary fibrosis (IPF) is a progressive and fatal disease characterized by lung fibrosis leading to an irreversible decline of lung function…”
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Optimization of M 3 Antagonist-PDE4 Inhibitor (MAPI) Dual Pharmacology Molecules for the Treatment of COPD
Published in Journal of medicinal chemistry (24-08-2023)“…Aiming at the inhaled treatment of pulmonary diseases, the optimization process of the previously reported MAPI compound is herein described. The project was…”
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Discovery of a novel class of inhaled dual pharmacology muscarinic antagonist and β 2 agonist (MABA) for the treatment of chronic obstructive pulmonary disease (COPD)
Published in Bioorganic & medicinal chemistry letters (01-06-2021)“…The targeting of both the muscarinic and β-adrenergic pathways is a well validated therapeutic approach for the treatment of chronic obstructive pulmonary…”
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Discovery of a novel class of inhaled dual pharmacology muscarinic antagonist and β2 agonist (MABA) for the treatment of chronic obstructive pulmonary disease (COPD)
Published in Bioorganic & medicinal chemistry letters (01-06-2021)“…[Display omitted] The targeting of both the muscarinic and β-adrenergic pathways is a well validated therapeutic approach for the treatment of chronic…”
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Discovery of Clinical Candidate CHF-6366: A Novel Super-soft Dual Pharmacology Muscarinic Antagonist and β2 Agonist (MABA) for the Inhaled Treatment of Respiratory Diseases
Published in Journal of medicinal chemistry (11-08-2022)“…The development of molecules embedding two distinct pharmacophores acting as muscarinic antagonists and β2 agonists (MABAs) promises to be an excellent…”
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Discovery of M 3 Antagonist-PDE4 Inhibitor Dual Pharmacology Molecules for the Treatment of Chronic Obstructive Pulmonary Disease
Published in Journal of medicinal chemistry (08-07-2021)Get full text
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CHF6001 I: a novel highly potent and selective phosphodiesterase 4 inhibitor with robust anti-inflammatory activity and suitable for topical pulmonary administration
Published in The Journal of pharmacology and experimental therapeutics (01-03-2015)“…This study examined the pharmacologic characterization of CHF6001…”
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Design, Synthesis, and Biological Characterization of Inhaled p38α/β MAPK Inhibitors for the Treatment of Lung Inflammatory Diseases
Published in Journal of medicinal chemistry (26-05-2022)“…The identification of novel inhaled p38α/β mitogen-activated protein kinases (MAPK) (MAPK14/11) inhibitors suitable for the treatment of pulmonary inflammatory…”
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Discovery of M3 Antagonist-PDE4 Inhibitor Dual Pharmacology Molecules for the Treatment of Chronic Obstructive Pulmonary Disease
Published in Journal of medicinal chemistry (08-07-2021)“…In this paper, we report the discovery of dual M3 antagonist-PDE4 inhibitor (MAPI) compounds for the inhaled treatment of pulmonary diseases. The…”
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Discovery and Optimization of Thiazolidinyl and Pyrrolidinyl Derivatives as Inhaled PDE4 Inhibitors for Respiratory Diseases
Published in Journal of medicinal chemistry (28-12-2017)“…Phosphodiesterase 4 (PDE4) is a key cAMP-metabolizing enzyme involved in the pathogenesis of inflammatory disease, and its pharmacological inhibition has been…”
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Erythroid differentiation ability of butyric acid analogues: Identification of basal chemical structures of new inducers of foetal haemoglobin
Published in European journal of pharmacology (05-04-2015)“…Several investigations have demonstrated a mild clinical status in patients with β-globin disorders and congenital high persistence of foetal haemoglobin. This…”
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Solution- and solid-state structures of the (-)-n-heptylcarbamate of geneseroline and its hydrochloride salt
Published in Journal of pharmaceutical sciences (01-09-1995)“…The solid state structures of the (-)-n-heptylcarbamate of geneseroline and its hydrochloride salt were determined by single crystal X-ray diffraction…”
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Structural Determinants of Torpedo californica Acetylcholinesterase Inhibition by the Novel and Orally Active Carbamate Based Anti-Alzheimer Drug Ganstigmine (CHF-2819)
Published in Journal of medicinal chemistry (24-08-2006)“…Ganstigmine is an orally active, geneserine derived, carbamate-based acetylcholinesterase inhibitor developed for the treatment of Alzheimer's disease. The…”
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Functionalized pyrazoles and pyrazolo[3,4- d]pyridazinones: Synthesis and evaluation of their phosphodiesterase 4 inhibitory activity
Published in Bioorganic & medicinal chemistry (15-05-2010)“…A series of pyrazoles and pyrazolo[3,4- d]pyridazinones were synthesized and evaluated for their PDE4 inhibitory activity. All the pyrazoles were found devoid…”
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Discovery of Diaryl Imidazolidin-2-one Derivatives, a Novel Class of Muscarinic M3 Selective Antagonists (Part 1)
Published in Journal of medicinal chemistry (05-04-2007)“…Pharmacophore-based structural identification, synthesis, and structure−activity relationships of a new class of muscarinic M3 receptor antagonists, the diaryl…”
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