46049-49-4Relevant academic research and scientific papers
SUBSTITUTED FUSED PYRIMIDINE COMPOUNDS AND USES THERE
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Paragraph 00142; 00143; 00149, (2019/02/15)
Disclosed are new small molecules having a substituted pyrimidine or substituted fused pyrimidine core structure and the uses thereof for modulating glucocerebrosidase activity. Also disclosed are pharmaceutical compositions comprising the small molecules
Orally active ghrelin receptor inverse agonists and their actions on a rat obesity model
Takahashi, Bitoku,Funami, Hideaki,Iwaki, Takehiko,Maruoka, Hiroshi,Shibata, Makoto,Koyama, Makoto,Nagahira, Asako,Kamiide, Yoshiyuki,Kanki, Satomi,Igawa, Yoshiyuki,Muto, Tsuyoshi
, p. 4792 - 4803 (2015/08/03)
A series of 2-alkylamino nicotinamide analogs was prepared as orally active ghrelin receptor (ghrelinR) inverse agonists. Starting from compound 1, oral bioavailability was improved by modifying metabolically unstable sites and reducing molecular weight. Brain-permeable compound 33 and compound 24 with low brain permeability were tested in rat models of obesity; 30 mg/kg of compound 33 suppressed weight gain. PK/PD analysis revealed that the anti-obesity effect of ghrelinR inverse agonists depends on their brain concentrations.
Diastereomeric 2-aminomethyl-1,4-benzodioxane mandelates: Phase diagrams and resolution
Bolchi, Cristiano,Pallavicini, Marco,Fumagalli, Laura,Ruggeri, Paola,Valoti, Ermanno
, p. 796 - 800 (2013/08/23)
The diastereomeric salts of (R)- and (S)-2-aminomethyl-1,4-benzodioxane with unichiral mandelic acid form a simple eutectic, whose binary phase melting point diagram shows the unique eutectic at 0.35 M ratio of the less soluble diastereomer. Such an eutectic composition, near to 0.5, is consistent with the modest efficiency previously reported for their separation via crystallization from ethanol/ethyl acetate. However, the ternary solubility phase diagram, obtained from solubility measurements in methanol, shifts the eutectic to a lower molar ratio (0.10) of the less soluble diastereomer, thus indicating an optimal resolvability of the diastereomeric mandelates. This was confirmed by the highly efficient resolution of racemic 2-aminomethyl-1,4-benzodioxane with (R)-mandelic acid via a single crystallization from methanol. The ready availability of both the racemic substrate and the resolving acid makes this simple and efficient resolution procedure very attractive to obtain the enantiomers of 2-aminomethyl-1,4-benzodioxane, which are important synthetic intermediates.
Novel, broad-spectrum anticonvulsants containing a sulfamide group: Pharmacological properties of (S)- N -[(6-chloro-2,3-dihydrobenzo[1,4]dioxin-2- yl)methyl]sulfamide (JNJ-26489112)
McComsey, David F.,Smith-Swintosky, Virginia L.,Parker, Michael H.,Brenneman, Douglas E.,Malatynska, Ewa,White, H. Steve,Klein, Brian D.,Wilcox, Karen S.,Milewski, Michael E.,Herb, Mark,Finley, Michael F. A.,Liu, Yi,Lubin, Mary Lou,Qin, Ning,Reitz, Allen B.,Maryanoff, Bruce E.
, p. 9019 - 9030 (2014/01/06)
Broad-spectrum anticonvulsants are of considerable interest as antiepileptic drugs, especially because of their potential for treating refractory patients. Such "neurostabilizers" have also been used to treat other neurological disorders, including migraine, bipolar disorder, and neuropathic pain. We synthesized a series of sulfamide derivatives (4-9, 10a-i, 11a, 11b, 12) and evaluated their anticonvulsant activity. Thus, we identified promising sulfamide 4 (JNJ-26489112) and explored its pharmacological properties. Compound 4 exhibited excellent anticonvulsant activity in rodents against audiogenic, electrically induced, and chemically induced seizures. Mechanistically, 4 inhibited voltage-gated Na+ channels and N-type Ca2+ channels and was effective as a K+ channel opener. The anticonvulsant profile of 4 suggests that it may be useful for treating multiple forms of epilepsy (generalized tonic-clonic, complex partial, absence seizures), including refractory (or pharmacoresistant) epilepsy, at dose levels that confer a good safety margin. On the basis of its pharmacology and other favorable characteristics, 4 was advanced into human clinical studies.
COMPOSITIONS AND METHODS FOR CYCLOFRUCTANS AS SEPARATION AGENTS
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Page/Page column 45-49; 64, (2010/12/31)
The present invention relates to derivatized cyclofructan compounds, compositions comprising derivatized cyclofructan compounds, and methods of using compositions comprising derivatized cyclofructan compounds for chromatographic separations of chemical species, including enantiomers. Said compositions may comprise a solid support and/or polymers comprising derivatized cyclofructan compounds.
USE OF BENZO-FUSED HETEROCYLE SULFAMIDE DERIVATIVES FOR THE TREATMENT OF ANXIETY
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Page/Page column 15, (2009/10/06)
The present invention is a method for the treatment of anxiety and related disorders comprising administering to a subject in need thereof a therapeutically effective amount of one or more novel benzo-fused heterocycle sulfamide derivatives of formula (I)
USE OF BENZO-FUSED HETEROCYCLE SULFAMIDE DERIVATIVES FOR DISEASE MODIFICATION / EPILEPTOGENESIS
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Page/Page column 20, (2008/06/13)
The present invention is a method for treating, preventing, reversing, arresting or inhibiting the occurrence, development and maturation of seizures or seizure-related disorders. More specifically, the present invention is directed to methods for the use
USE OF BENZO-FUSED HETEROCYCLE SULFAMIDE DERIVATIVES FOR LOWERING LIPIDS AND LOWERING BLOOD GLUCOSE LEVELS
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Page/Page column 16, (2010/11/27)
The present invention is a method for the glucose related disorders and lipid related disorders comprising administering to a subject in need thereof a therapeutically effective amount of one or more novel benzo-fused heterocycle sulfamide derivatives of
USE OF BENZO-FUSED HETEROCYCLE SULFAMIDE DERIVATIVES AS NEUROPROTECTIVE AGENTS
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Page/Page column 13, (2010/11/27)
The present invention is a methods for neuroprotection, for treating an acute neurodegenerative disorder, for treating a chronic neurodegenerative disorder and/or for preventing neuron death or damage following brain, head and/or spinal cord trauma or inj
USE OF BENZO-FUSED HETEROCYCLE SULFAMIDE DERIVATIVES FOR THE TREATMENT OF DEPRESSION
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Page/Page column 14-15, (2010/11/27)
The present invention is a method for the treatment of depression comprising administering to a subject in need thereof a therapeutically effective amount of one or more novel benzo-fused heterocycle sulfamide derivatives of formula (I) and formula (II) a
