54127-30-9Relevant academic research and scientific papers
BENZODIAZEPINE DERIVATIVES AS RSV INHIBITORS
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Page/Page column 77, (2020/10/09)
The present invention discloses compounds of Formula (I), or pharmaceuticall acceptable salts, esters, or prodrugs thereof: which inhibit Respiratory Syncytial Virus (RSV). The present invention further relates to pharmaceutical compositions comprising th
NEW SUBSTITUTED BIPHENYL ANALOGUES AS DUAL INHIBITORS OF AROMATASE AND SULFATASE
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Page/Page column 51, (2015/07/16)
Provided are new biphenyl derivatives of formula (Ia). These compounds act as aromatase and sulfatase inhibitors. They are particularly useful for treating pathological conditions or diseases in which aromatase and sulfatase are involved. Moreover, provided are processes for the preparation of these compounds and pharmaceutical compositions containing said products and their use for the preparation of a medicament, in particular for the treatment of diseases characterized by aromatase and sulfatase activity such as hormone-dependent cancers.
Tetrahydronaphthyridine and dihydronaphthyridinone ethers as positive allosteric modulators of the metabotropic glutamate receptor 5 (mGlu 5)
Turlington, Mark,Malosh, Chrysa,Jacobs, Jon,Manka, Jason T.,Noetzel, Meredith J.,Vinson, Paige N.,Jadhav, Satyawan,Herman, Elizabeth J.,Lavreysen, Hilde,Mackie, Claire,Bartolomé-Nebreda, José M.,Conde-Ceide, Susana,Martín-Martín, M. Luz,Tong, Han Min,López, Silvia,Macdonald, Gregor J.,Steckler, Thomas,Daniels, J. Scott,Weaver, C. David,Niswender, Colleen M.,Jones, Carrie K.,Conn, P. Jeffrey,Lindsley, Craig W.,Stauffer, Shaun R.
supporting information, p. 5620 - 5637 (2014/08/05)
Positive allosteric modulators (PAMs) of metabotropic glutamate receptor 5 (mGlu5) represent a promising therapeutic strategy for the treatment of schizophrenia. Starting from an acetylene-based lead from high throughput screening, an evolved bicyclic dihydronaphthyridinone was identified. We describe further refinements leading to both dihydronaphthyridinone and tetrahydronaphthyridine mGlu5 PAMs containing an alkoxy-based linkage as an acetylene replacement. Exploration of several structural features including western pyridine ring isomers, positional amides, linker connectivity/position, and combinations thereof, reveal that these bicyclic modulators generally exhibit steep SAR and within specific subseries display a propensity for pharmacological mode switching at mGlu5 as well as antagonist activity at mGlu3. Structure-activity relationships within a dihydronaphthyridinone subseries uncovered 12c (VU0405372), a selective mGlu5 PAM with good in vitro potency, low glutamate fold-shift, acceptable DMPK properties, and in vivo efficacy in an amphetamine-based model of psychosis.
NOVEL COMPOUNDS FOR MODULATION OF ROR-GAMMA ACTIVITY
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Paragraph 00314; 00370, (2014/03/22)
The present invention relates to aryl sulfones and related compounds that are modulators of ROR-gamma receptors. The invention also provides pharmaceutical compositions comprising these modulators, and methods of modulating ROR-gamma receptors using them. Also provided are methods of using aryl sulfones and related compounds as modulators of ROR-gamma to treat ROR-gamma mediated diseases
NAPHTHYRIDINONE ANALOGS AS MGLUR5 POSITIVE ALLOSTERIC MODULATORS
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Page/Page column 82, (2012/07/14)
In one aspect, the invention relates to naphthyridinone analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
N'-Cyano-N-Halogenalkylimidamide Derivatives
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Page/Page column 25, (2010/03/31)
The present application relates to novel substituted N′-cyano-N-halogenalkylimidamide derivatives, to processes for their preparation and to their use for controlling animal pests, especially arthropods, in particular insects.
SUBSTITUTED ENAMINOCARBONYL COMPOUNDS USED AS INSECTICIDES
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, (2010/10/03)
The present application relates to novel substituted enaminocarbonyl compounds, to processes for their preparation and to their use for controlling animal pests, especially arthropods, in particular insects.
BICYCLIC ENAMINO(THIO)CARBONYL COMPOUNDS
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Page/Page column 39, (2009/07/25)
The present invention relates to novel bicyclic enamino(thio)carbonyl compounds, to processes for their preparation and to their use for controlling animal pests, especially arthropods, in particular insects.
SUBSTITUTED ENAMINOCARBONYL COMPOUNDS
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Page/Page column 27, (2009/10/06)
The present invention relates to novel substituted enaminocarbonyl compounds, to processes for their preparation and to their use for controlling animal pests, especially arthropods, in particular insects.
Multi-substituted pyridyl sulfoximines and their use as insecticides
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Page/Page column 7, (2008/12/04)
Multi-substituted pyridyl sulfoximines are useful as insecticides.
