22348-44-3Relevant academic research and scientific papers
BTK INHIBITOR
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Paragraph 0356-0358, (2017/11/16)
Provided are a series of BTK inhibitors, and specifically disclosed are a compound, pharmaceutically acceptable salt thereof, tautomer thereof or prodrug thereof represented by formula (I), (II), (III) or (IV).
New cyclohexylamine derivatives having beta2 adrenergic agonist and M3 muscarinic antagonist activities
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Paragraph 0129, (2013/05/23)
The present invention relates to novel compounds having β2 adrenergic agonist and M3 muscarinic antagonist dual activity, to pharmaceutical compositions containing them, to the process for their preparation and to their use in respiratory therapies.
NEW CYCLOHEXYLAMINE DERIVATIVES HAVING β2 ADRENERGIC AGONIST AND M3 MUSCARINIC ANTAGONIST ACTIVITIES
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Page/Page column 39, (2013/05/23)
The present invention relates to novel compounds having β2 adrenergic agonist and M3 muscarinic antagonist dual activity, to pharmaceutical compositions containing them, to the process for their preparation and to their use in respiratory therapies.
New cyclohexylamine derivatives having beta2 adrenergic agonist and m3 muscarinic antagonist activities
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Paragraph 0074, (2013/03/26)
The present invention relates to novel compounds having β2 adrenergic agonist and M3 muscarinic antagonist dual activity, to pharmaceutical compositions containing them, to the process for their preparation and to their use in respiratory therapies.
DI-SUBSTITUTED AMIDES FOR ENHANCING GLUTAMATERGIC SYNAPTIC RESPONSES
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Example 51, (2009/01/20)
This invention relates to compounds, pharmaceutical compositions and methods for use in the prevention and treatment of cerebral insufficiency, including enhancement of receptor functioning in synapses in brain networks responsible for basic and higher order behaviors. These brain networks, which are involved in regulation of breathing, and cognitive abilities related to memory impairment, such as is observed in a variety of dementias, in imbalances in neuronal activity between different brain regions, as is suggested in disorders such as Parkinson's disease, schizophrenia, respiratory depression, sleep apneas, attention deficit hyperactivity disorder and affective or mood disorders, and in disorders wherein a deficiency in neurotrophic factors is implicated, as well as in disorders of respiration such as overdose of an alcohol, an opiate, an opioid, a barbiturate, an anesthetic, or a nerve toxin, or where the respiratory depression results form a medical condition such as central sleep apnea, stroke- induced central sleep apnea, obstructive sleep apnea, congenital hypoventilation syndrome, obesity hypoventilation syndrome, sudden infant death syndrome, Rett syndrome, spinal cord injury, traumatic brain injury, Cheney-Stokes respiration, Ondines curse, Prader-Willi's syndrome and drowning. In a particular aspect, the invention relates to compounds useful for treatment of such conditions, and methods of using these compounds for such treatment.
Oxidosqualene cyclase (OSC) inhibitors for the treatment of dyslipidemia
Dehmlow, Henrietta,Ackermann, Jean,Aebi, Johannes,Blum-Kaelin, Denise,Chucholowski, Alexander,Coassolo, Philippe,Hartman, Peter,Kansy, Manfred,Maerki, Hans Peter,Morand, Olivier,Von Der Mark, Elisabeth,Panday, Narendra,Ruf, Armin,Thoma, Ralf,Schulz-Gasch, Tanja
, p. 72 - 76 (2007/10/03)
Novel inhibitors of oxidosqualene cyclase (OSC) for the treatment of dyslipidemia are reported. Starting point for the chemistry program was a set of compounds derived from a fungicide project which, in addition to high affinity for OSC from Candida albicans, also showed high affinity for the human enzyme (hOSC). Here the evaluation process of different scaffolds is outlined for two representative series, the phenyl substituted benzo[d]isothiazoles and the aminocyclohexanes. The most promising compounds derived from the latter series were further profiled in vivo and showed promising properties with respect to modulation of lipid parameters. Schweizerische Chemische Gesellschaft.
Inhibitors of Cyclic AMP Phosphodiesterase. 2. Structural Variations of N-Cyclohexyl-N-methyl-4-quinazolin-7-yl)oxy>butyramide (RS-82856)
Venuti, Michael C.,Jones, Gordon H.,Alvarez, Robert,Bruno, John J.
, p. 303 - 318 (2007/10/02)
A series of analogues of the cyclic AMP phosphodiesterase (PDE) inhibitor N-cyclohexyl-N-methyl-4-quinazolin-7-yl)oxy>butyramide (RS-82856, 1) was prepared by systematic variation of the side-chain substituent, length, position, connecting atom, and the parent heterocycle itself.The compounds were evaluated as inhibitors of cyclic AMP phosphodiesterase from both human platelets and rat or dog heart tissue and as inhibitors of ADP-induced platelet aggregation.Structure-activity correlations for the analogue series revealed significant limitations on the steric bulk of substituents on the 1,2,3,5-tetrahydroimidazoquinaazolin-2-one heterocycle and the position and length of the side-chain.As inhibitors of cyclic AMP phosphodiesterase (PDE), potency steadily increased with increasingly lipophilic side chains.In platelet aggregation inhibition studies, however, a maximum in activity was reached with 1, while more lipophilic compounds were significantly less active.Major changes in the heterocycle itself, represented by isomeric and other carbonyl variations, also decreased activity.The molecular features defined by this series of analogues of 1 correlate to a high degree with current understanding of thr chemical and topographical requirements of the active site of the FIII (type IV) form of cyclic AMP PDE.Selective inhibition of this enzyme has been proposed as the principal component of the positive inotropic action of a number of cardiotonic agents.
