91331-85-0Relevant academic research and scientific papers
One-pot, telescoped synthesis of N-aryl-5-aminopyrazoles from anilines in environmentally benign conditions
Marinozzi, Maura,Marcelli, Gloria,Carotti, Andrea,Natalini, Benedetto
, p. 7019 - 7023 (2014/02/14)
An efficient synthetic approach to synthesize N-aryl-5-aminopyrazoles from anilines via a one-pot, telescoped reaction performed in entirely aqueous conditions has been developed. This protocol provides a rapid, convenient method to prepare N-aryl-5-aminopyrazoles, useful building blocks for the synthesis of several bicyclic nitrogen heterocycles, by avoiding the isolation of the toxic intermediate arylhydrazines and the use of a metallic reductant. The Royal Society of Chemistry 2014.
NEW POSITIVE ALLOSTERIC MODULATORS OF NICOTINIC ACETYLCHOLINE RECEPTOR
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Page/Page column 13, (2013/02/28)
The present invention relates to compounds useful in therapy, to compositions comprising said compounds, and to methods of treating diseases comprising administration of said compounds. The compounds referred to are positive allosteric modulators (PAMs) of the nicotinic acetylcholine alpha7 receptor.
PYRAZOLOPYRIDINES USEFUL IN THE TREATMENT OF DISORDERS OF THE CENTRAL NERVOUS SYSTEM
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Page/Page column 31, (2013/03/26)
The present invention relates to compounds useful in therapy, to compositions comprising said compounds, and to methods of treating diseases comprising administration of said com- pounds. The compounds referred to are positive allosteric modulators (PAMs) of the nicotinic acetylcholine α7 receptor.
Pyrazole[3,4-e][1,4]thiazepin-7-one derivatives as a novel class of Farnesoid X Receptor (FXR) agonists
Marinozzi, Maura,Carotti, Andrea,Sansone, Emanuele,MacChiarulo, Antonio,Rosatelli, Emiliano,Sardella, Roccaldo,Natalini, Benedetto,Rizzo, Giovanni,Adorini, Luciano,Passeri, Daniela,De Franco, Francesca,Pruzanski, Mark,Pellicciari, Roberto
supporting information; experimental part, p. 3429 - 3445 (2012/07/30)
A virtual screening procedure was applied to the discovery of structurally diverse non-steroidal Farnesoid X Receptor (FXR) agonists. From 117 compounds selected by virtual screening, a total of 47 compounds were found to be FXR agonists, with 34 of them showing activity below a concentration of 20 μM. 1H-Pyrazole[3,4-e][1,4]thiazepin-7-one-based hit compound 7 was chosen for hit-to-lead optimization. A large number of 1H-pyrazole[3,4-e][1,4]thiazepin-7- one derivatives was designed, synthesized, and evaluated by a cell-based luciferase transactivation assay for their agonistic activity against FXR. Most of them exhibited low micromolar range of potency and very high efficacy.
SUBSTITUTED 5-AMINOPYRAZOLES AND USE THEREOF
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Page/Page column 89, (2010/04/03)
The present application relates to novel substituted 5-aminopyrazoles, methods of production thereof, use thereof alone or in combinations for the treatment and/or prophylaxis of diseases and use thereof for the production of medicinal products for the treatment and/or prophylaxis of diseases.
Discovery of new orally active phosphodiesterase (PDE4) inhibitors
Ochiai, Hiroshi,Ishida, Akiharu,Ohtani, Tazumi,Kusumi, Kensuke,Kishikawa, Katuya,Yamamoto, Susumu,Takeda, Hiroshi,Obata, Takaaki,Nakai, Hisao,Toda, Masaaki
, p. 1098 - 1104 (2007/10/03)
A series of 4-anilinopyrazolopyridine derivatives were synthesized and biologically evaluated as inhibitors of phosphodiesterase (PDE4). Chemical modification of 3, a structurally new chemical lead that was found in our in-house library, was focused on 1- and 3-substituents. Full details of the discovery of a new orally active chemical lead 5 are presented. Structure-activity relationship data, pharmacological evaluation, and the subtype selectivity study are also presented.
