3990-58-7Relevant articles and documents
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.
USE OF BENZO-FUSED HETEROCYLE SULFAMIDE DERIVATIVES FOR THE TREATMENT OF ANXIETY
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Page/Page column 17, (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)
ANTAGONISTS OF THE TRPV1 RECEPTOR AND USES THEREOF
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Page/Page column 20, (2008/12/06)
The present application is directed to compounds that are TRPV1 antagonists and have formula (I) wherein variables Ar1, L1, R1, R2, R3, R4, R5, Y1, Y2, and Y3, are as defined in the description, which are useful for treating disorders caused by or exacerbated by vanilloid receptor activity.
NOVEL SULFONAMIDE SUBSTITUTED CHROMAN DERIVATIVES USEFUL AS BETA-3 ADRENORECEPTOR AGONISTS
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Page/Page column 32, (2008/12/07)
This invention relates to novel sulfonamide substituted chroman derivatives which are useful in the treatment of beta-3 receptor mediated conditions.
CHROMANE AND CHROMENE DERIVATIVES AND USES THEREOF
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, (2010/11/28)
Methods of preparing compounds of formula (I) or pharmaceutically acceptable salts thereof are provided wherein each of R1, R2, R3, R4, x, m, n, and Ar are as defined, and described in classes and subclasses herein, which are agonists or partial agonists of the 2C subtype of brain serotonin receptors. The compounds, and compositions containing the compounds, can be used to treat a variety of central nervous system disorders such as schizophrenia.
USE OF BENZO-FUSED HETEROCYCLE SULFAMIDE DERIVATIVES FOR DISEASE MODIFICATION / EPILEPTOGENESIS
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Page/Page column 22, (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
CO-THERAPY FOR THE TREATMENT OF EPILEPSY AND RELATED DISORDERS
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Page/Page column 40-41, (2008/06/13)
The present invention is directed to co-therapy for the treatment of epilepsy and related disorders comprising administering to a subject in need thereof, co-therapy with a therapeutically effective amount of a benzo-fused heterocycle sulfamide derivative
USE OF BENZO-FUSED HETEROCYLE SULFAMIDE DERIVATIVES FOR THE TREATMENT OF MANIA AND BIPOLAR DISORDER
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Page/Page column 17-18, (2010/11/27)
The present invention is a method for the treatment of mania and/or bipolar disorder 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 THE TREATMENT OF OBESITY
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Page/Page column 39, (2010/11/27)
The present invention is a method for the treatment of obesity, for promoting weight loss and / or suppressing appetite comprising administering to a subject in need thereof a therapeutically effective amount of one or more novel benzo-fused heterocycle s
SULFAMATE AND SULFAMIDE DERIVATIVES FOR THE TREATMENT OF EPILEPSY AND RELATED DISORDERS
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Page/Page column 43, (2010/02/15)
The present invention is directed to novel sulfamide and sulfamate derivatives, pharmaceutical composlons containing them and their use in the treatment of epilepsy and related disorders.
