WO1998000131A1 - Anticonvulsant derivatives useful in treating amyotrophic lateral sclerosis (als) - Google Patents
Anticonvulsant derivatives useful in treating amyotrophic lateral sclerosis (als) Download PDFInfo
- Publication number
- WO1998000131A1 WO1998000131A1 PCT/US1997/010955 US9710955W WO9800131A1 WO 1998000131 A1 WO1998000131 A1 WO 1998000131A1 US 9710955 W US9710955 W US 9710955W WO 9800131 A1 WO9800131 A1 WO 9800131A1
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- formula
- topiramate
- als
- lateral sclerosis
- amyotrophic lateral
- Prior art date
Links
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7048—Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
- A61K31/255—Esters, e.g. nitroglycerine, selenocyanates of sulfoxy acids or sulfur analogues thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/08—Antiepileptics; Anticonvulsants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
Definitions
- ALS amyotrophic lateral sclerosis
- X is O or CH2
- Ri , R2, R3, R4 and R5 are as defined hereinafter are useful in treating acute amyotrophic lateral sclerosis (ALS).
- ALS acute amyotrophic lateral sclerosis
- R2, R3, R4 and R5 are independently hydrogen or lower alkoxyl, when X is oxygen, R2 and R3 and/or R4 and R5 together may be a methylenedioxy group of the following formula (II):
- R6 and R7 are the same or different and are hydrogen, lower alkyl or are alkyl and are joined to form a cyclopentyl or cyclohexyl ring.
- R l in particular is hydrogen or alkyl of about 1 to 4 carbons, such as methyl, ethyl and iso-propyl.
- Alkyl throughout this specification includes straight and branched chain alkyl.
- Alkyl groups for R2, R3, R4- R5» R6 and R7 are of about 1 to 3 carbons and include methyl, ethyl, iso-propyl and n-propyl.
- a particular group of compounds of formula (I) are those wherein X is oxygen and both R2 and R3 t and R4 and R5 together are methylenedioxy groups of the formula (II), wherein R6 and R7 are both hydrogen, both alkyl, or combine to form a spiro cyclopentyl or cyclohexyl ring, in particular where R6 and R7 are both alkyl such as methyl.
- a second group of compounds are those wherein X is CH2 and R4 and R5 are joined to form a benzene ring.
- a third group of compounds of formula (I) are those wherein both R2 and R3 are hydrogen.
- the compounds of formula (I) may be synthesized by the following methods: (a) Reaction of an alcohol of the formula RCH2OH with a chlorosulfamate of the formula CISO2NH2 or CISO2NHR 1 in the presence of a base such as potassium a-butoxide or sodium hydride at a temperature of about -20° to 25° C and in a solvent such as toluene, THF or dimethylformamide wherein R is a moiety of the following formula (III):
- the chlorosulfate of the formula RCH2OSO2CI may then be reacted with an a ine of the formula R1 NH2 at a temperature of abut 40° to 25° C in a solvent such as methylene chloride or acetonitrile to produce a compound of formula (I).
- a solvent such as methylene chloride or acetonitrile.
- the starting materials of the formula RCH2OH may be obtained commercially or as known in the art.
- starting materials of the formula RCH2OH wherein both R2 and R3 t and R4 and R5 are identical and are of the formula (II) may be obtained by the method of R. F. Brady in Carbohydrate Research, Vol. 14, p. 35 to 40 (1970) or by reaction of the trimethylsilyl enol ether of a R6COR7 ketone or aldehyde with fructose at a temperature of about 25° C, in a solvent such a halocarbon, e.g. methylene chloride in the presence of a protic acid such as hydrochloric acid or a Lewis Acid such as zinc chloride.
- the trimethylsilyl enol ether reaction is described by G. L. Larson et al in J. Org. Chem. Vol. 38, No. 22, p. 3935 (1973).
- carboxylic acids and aldehydes of the formulae RCOOH and RCHO may be reduced to compounds of the formula RCH2OH by standard reduction techniques, e.g. reaction with lithium aluminum hydride, sodium borohydride or borane-THF complex in an inert solvent such a diglyme, THF or toluene at a temperature of about 0° to 100° C, e.g. as described by H.O. House in "Modern Synthetic Reactions", 2nd Ed., pages 45 to 144 (1972).
- the compounds of formula I: may also be made by the process disclosed US Patent: No.4,513,006, which is incorporated by reference herein.
- the compounds of formula I include the various individual isomers as well as the racemates thereof, e.g., the various alpha and beta attachments, i.e., below and above the plane of the drawing, of R2, R3, R4 and R5 on the 6-membered ring.
- the oxygens of the methylenedioxy group (II) are attached on the same side of the 6-membered ring.
- ALS amyotrophic lateral sclerosis
- Glutamate is utilized as the major excitatory neurotransmitter in the CNS. This function is served by a physiological process in which glutamate molecules are stored in vesicles within synaptic terminals of neurons. These molecules are released into the synaptic cleft when an action potential depolarizes the synaptic membrane, whereupon they activate specific receptors in the post-synaptic membrane of target neurons.
- the molecules are removed from the synaptic cleft by protein "transporters” in the membrane of the synaptic terminal of the presynaptic neuron and the surrounding glial cells (astrocytes).
- protein "transporters” in the membrane of the synaptic terminal of the presynaptic neuron and the surrounding glial cells (astrocytes).
- glial cells astrocytes
- the activity of these transport proteins apppears to be abnormally low, which can cause an abnormal increase in the concentration of glutamate within the synaptic cleft. This in turn can cause an excessive activation of glutamate receptors, which, if sufficient, can induce neuronal cell death (J.D. ROTHSTEIN, In: Pathogenesis and Therapy of Amyotrophic Lateral Sclerosis, Edited by G. Serratrice and T. Munsat, Advances in Neurology 68, 7-20, Lippincott-Raven Publishers, Philadelphia, 1995).
- topiramate antagonizes the neuronal excitatory activity kainate, an analog of glutamate that selectively activates some subtypes of glutamate receptors (J. W. GIBBS in, S. SOMBATI, R.J. DELORENZO, and D.A. COULTER, Epilepsia 37, in press, 1996; The R.W. Johnson Pharmaceutical Research Institute, Internal Research Reports, Document ID Accession Numbers A500,960 and 398533:1).
- primary cultures enriched in neurons derived from the hippocampus of fetal rats were grown in vitro for 14 to 21 days under conditions that allowed them to reach a high density and develop numerous synaptic contacts.
- Perforated whole-cell patch-clamp procedures were used to study electrical properties of the neuronal membranes.
- electrical contact between the recording electrode and the intracellular fluid is achieved by using amphotericin B to form pores in the cell membrane. This enables the cell membrane potential or current flow across the cell membrane to be recorded accurately.
- Kainate, topiramate and other test compounds were microperfused onto the neurons using a multi-barrel Teflon concentration clamp pipette. Topiramate (dissolved in DMSO at 1 M, then diluted in the medium in which the neurons were incubated) was applied at concentrations of 0.01, 0.1, 1 , 10 or 100 and kainate was applied at concentrations 0.1 or 1 mM.
- Kainate was pulsed into the bathing fluid for 3 sec at 1 min intervals, and once a baseline for the kainate-evoked current was established topiramate was applied constantly for a period ranging from a few min to 20 min. A partial block of the kainate-evoked current was evident within one min after topiramate was applied, but even at saturating concentrations the kainate-evoked current was reduced by only 20 to 40%. This effect was readily reversed if topiramate was withdrawn (washed out) within 5 min.
- topiramate directly or indirectly inhibits the ability of a protein kinase (PKA) to phosphorylate kainate-activatable receptors, which over time shifts the receptors into a dephosphorylated state in which they are desensitized (can not be activated).
- PKA protein kinase
- a compound of formula (I) may be employed at a daily dosage in the range of about 100 to 800 mg, usually two divided doses, for an average adult human.
- a unit dose would contain about 25 to 200 mg of the active ingredient.
- one or more sulfamate compounds of formula (I) are intimately admixed with a pharmaceutical carrier according to conventional pharmaceutical compounding techniques, which carrier may take a wide variety of forms depending on the form of preparation desired for administration, e.g., oral, by suppository, or parenteral.
- a pharmaceutical carrier may take a wide variety of forms depending on the form of preparation desired for administration, e.g., oral, by suppository, or parenteral.
- any of the usual pharmaceutical media may be employed.
- suitable carriers and additives include water, glycols, oils, alcohols, flavoring agents, preservatives, coloring agents and the like;
- suitable carriers and additives include starches, sugars, diluents, granulating agents, lubricants, binders, disintegrating agents and the like. Because of their ease in administration, tablets and capsules represent the most advantageous oral dosage unit form, in which case solid pharmaceutical carriers are obviously employed. If desired, tablets may be sugar coated or enteric coated by standard techniques. Suppositories may be prepared, in which case cocoa butter could be used as the carrier.
- the carrier will usually comprise sterile water, though other ingredients, for example, for purposes such as aiding solubility or for preservation, may be included.
- injectable suspensions may also be prepared in which case appropriate liquid carriers, suspending agents and the like may be employed.
- Topiramate is currently available for oral administration in round tablets containing 25 mg, 100 mg or 200 mg of active agent.
- the tablets contain the following inactive ingredients: lactose hydrous, pregelatinized starch, microcrystalline cellulose, sodium starch glycolate, magnesium stearate, purified water, carnauba wax, hydroxypropyl methylcellulose, titanium dioxide, polyethylene glycol, synthetic iron oxide, and polysorbate 80.
- compositions herein will contain, per dosage unit, e.g., tablet, capsule, powder injection, teaspoonful, suppository and the like from about 50 to about 200 mg of the active ingredient.
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Organic Chemistry (AREA)
- Epidemiology (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Molecular Biology (AREA)
- Emergency Medicine (AREA)
- Heart & Thoracic Surgery (AREA)
- Pain & Pain Management (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Cardiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
Description
Claims
Priority Applications (16)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
AU35010/97A AU725093B2 (en) | 1996-06-28 | 1997-06-24 | Anticonvulsant derivatives useful in treating amyotrophic lateral sclerosis (ALS) |
JP10504245A JP2000514426A (en) | 1996-06-28 | 1997-06-24 | Anticonvulsant derivatives useful for the treatment of amyotrophic lateral sclerosis (ALS) |
SI9730259T SI0936908T1 (en) | 1996-06-28 | 1997-06-24 | Anticonvulsant derivatives useful in treating amyotrophic lateral sclerosis (als) |
EP97931367A EP0936908B1 (en) | 1996-06-28 | 1997-06-24 | Anticonvulsant derivatives useful in treating amyotrophic lateral sclerosis (als) |
NZ333588A NZ333588A (en) | 1996-06-28 | 1997-06-24 | Sulphamates as anticonvulsant derivatives useful in treating amyotrophic lateral sclerosis (ALS) |
DE69711067T DE69711067T2 (en) | 1996-06-28 | 1997-06-24 | ANTI-CONVULSIVA FOR USE IN TREATING AMYOTROPICAL LATERAL Sclerosis |
DK97931367T DK0936908T3 (en) | 1996-06-28 | 1997-06-24 | Anti-convulsive derivatives useful in the treatment of amyotrophic lateral sclerosis (ALS) |
CA002258892A CA2258892C (en) | 1996-06-28 | 1997-06-24 | Anticonvulsant derivatives useful in treating amyotrophic lateral sclerosis (als) |
UA98126945A UA46112C2 (en) | 1996-06-28 | 1997-06-24 | METHOD OF TREATMENT OF SIDE AMYOTROPHIC SCLEROSIS |
IL12771797A IL127717A (en) | 1996-06-28 | 1997-06-24 | Anticonvulsant derivatives useful in treating amyotrophic lateral sclerosis (als) |
APAP/P/1998/001428A AP1167A (en) | 1996-06-28 | 1997-06-24 | Anticonvulsant derivatives useful in treating amyotrophic lateral sclerosis (ALS). |
BR9710993-2A BR9710993A (en) | 1996-06-28 | 1997-06-24 | Anticonvulsant derivatives useful in the treatment of amyotrophic lateral sclerosis (als) |
AT97931367T ATE214274T1 (en) | 1996-06-28 | 1997-06-24 | ANTICONVULSIVALS FOR USE IN THE TREATMENT OF AMYOTROPIC LATERAL SCLERosis |
SK1806-98A SK284331B6 (en) | 1996-06-28 | 1997-06-24 | Anticonvulsant derivatives useful in treating amyotrophic lateral sclerosis (ALS) |
CZ19984279A CZ293945B6 (en) | 1996-06-28 | 1997-06-24 | Medicament useful in treating amyotrophic lateral sclerosis |
NO19986054A NO317136B1 (en) | 1996-06-28 | 1998-12-22 | Anti-convulsant derivatives for use in the treatment of amyotrophic lateral sclerosis (ALS) |
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US2200696P | 1996-06-28 | 1996-06-28 | |
US60/022,006 | 1996-06-28 |
Publications (1)
Publication Number | Publication Date |
---|---|
WO1998000131A1 true WO1998000131A1 (en) | 1998-01-08 |
Family
ID=21807346
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PCT/US1997/010955 WO1998000131A1 (en) | 1996-06-28 | 1997-06-24 | Anticonvulsant derivatives useful in treating amyotrophic lateral sclerosis (als) |
Country Status (22)
Country | Link |
---|---|
US (1) | US5753694A (en) |
EP (1) | EP0936908B1 (en) |
JP (1) | JP2000514426A (en) |
AP (1) | AP1167A (en) |
AT (1) | ATE214274T1 (en) |
AU (1) | AU725093B2 (en) |
BR (1) | BR9710993A (en) |
CA (1) | CA2258892C (en) |
CZ (1) | CZ293945B6 (en) |
DE (1) | DE69711067T2 (en) |
DK (1) | DK0936908T3 (en) |
ES (1) | ES2176755T3 (en) |
HU (1) | HUP9904318A3 (en) |
IL (1) | IL127717A (en) |
NO (1) | NO317136B1 (en) |
NZ (1) | NZ333588A (en) |
PT (1) | PT936908E (en) |
SI (1) | SI0936908T1 (en) |
SK (1) | SK284331B6 (en) |
UA (1) | UA46112C2 (en) |
WO (1) | WO1998000131A1 (en) |
ZA (1) | ZA975764B (en) |
Cited By (13)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2000061138A1 (en) * | 1999-04-08 | 2000-10-19 | Ortho-Mcneil Pharmaceutical, Inc. | Anticonvulsant derivatives useful in treating chronic neurodegenerative disorders |
WO2002043731A3 (en) * | 2000-11-30 | 2003-02-20 | Univ Florida | Treatments for neurogenetic disorders, impulse control disorders, and wound healing |
WO2008001016A1 (en) * | 2006-06-30 | 2008-01-03 | Universite Claude Bernard Lyon 1 | Use of a carbonic anhydrase inhibitor for preparation of a drug for treating skeletal muscle degeneration |
US8084490B2 (en) | 2004-06-16 | 2011-12-27 | Janssen Pharmaceutica N.V. | Sulfamate and sulfamide derivatives useful for the treatment of epilepsy and related disorders |
US8283478B2 (en) | 2005-05-20 | 2012-10-09 | Janssen Pharmaceutica Nv | Process for preparation of sulfamide derivatives |
US8492431B2 (en) | 2005-12-19 | 2013-07-23 | Janssen Pharmaceutica, N.V. | Use of benzo-fused heterocycle sulfamide derivatives for the treatment of obesity |
US8497298B2 (en) | 2005-12-19 | 2013-07-30 | Janssen Pharmaceutica Nv | Use of benzo-fused heterocycle sulfamide derivatives for lowering lipids and lowering blood glucose levels |
US8691867B2 (en) | 2005-12-19 | 2014-04-08 | Janssen Pharmaceutica Nv | Use of benzo-fused heterocycle sulfamide derivatives for the treatment of substance abuse and addiction |
US8716231B2 (en) | 2005-12-19 | 2014-05-06 | Janssen Pharmaceutica Nv | Use of benzo-fused heterocycle sulfamide derivatives for the treatment of pain |
US8809385B2 (en) | 2008-06-23 | 2014-08-19 | Janssen Pharmaceutica Nv | Crystalline form of (2S)-(-)-N-(6-chloro-2,3-dihydro-benzo[1,4]dioxin-2-ylmethyl)-sulfamide |
US8815939B2 (en) | 2008-07-22 | 2014-08-26 | Janssen Pharmaceutica Nv | Substituted sulfamide derivatives |
US8853263B2 (en) | 2006-05-19 | 2014-10-07 | Janssen Pharmaceutica Nv | Co-therapy for the treatment of epilepsy and related disorders |
US8937096B2 (en) | 2005-12-19 | 2015-01-20 | Janssen Pharmaceutica Nv | Use of benzo-fused heterocyle sulfamide derivatives for the treatment of mania and bipolar disorder |
Families Citing this family (29)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5985930A (en) * | 1996-11-21 | 1999-11-16 | Pasinetti; Giulio M. | Treatment of neurodegenerative conditions with nimesulide |
US7674776B2 (en) | 1999-06-14 | 2010-03-09 | Vivus, Inc. | Combination therapy for effecting weight loss and treating obesity |
AU770068B2 (en) | 1999-06-14 | 2004-02-12 | Vivus, Inc. | Combination therapy for effecting weight loss and treating obesity |
US7659256B2 (en) * | 1999-06-14 | 2010-02-09 | Vivus, Inc. | Combination therapy for effecting weight loss and treating obesity |
US20080255093A1 (en) * | 1999-06-14 | 2008-10-16 | Tam Peter Y | Compositions and methods for treating obesity and related disorders |
US7056890B2 (en) | 1999-06-14 | 2006-06-06 | Vivus, Inc. | Combination therapy for effecting weight loss and treating obesity |
US20080103179A1 (en) * | 2006-10-27 | 2008-05-01 | Tam Peter Y | Combination Therapy |
US7553818B2 (en) * | 1999-06-14 | 2009-06-30 | Vivus, Inc. | Combination therapy for effecting weight loss and treating obesity |
US6191117B1 (en) * | 2000-07-10 | 2001-02-20 | Walter E. Kozachuk | Methods of producing weight loss and treatment of obesity |
WO2002064085A2 (en) * | 2001-02-02 | 2002-08-22 | Ortho-Mcneil Pharmaceutical, Inc. | Treatment of neurological dysfunction comprising fructopyranose sulfamates and erythropoietin |
JP2005514352A (en) * | 2001-11-14 | 2005-05-19 | ラルフ ライバック | Treatment of autoimmune diseases |
WO2004043444A1 (en) * | 2002-11-06 | 2004-05-27 | Mount Sinai School Of Medicine | Treatment of amyotrophic lateral sclerosis with nimesulide |
US20060041022A1 (en) * | 2002-11-06 | 2006-02-23 | Pasinetti Giulio M | Treatment of amyotrophic lateral sclerosis with nimesulide |
US20050070524A1 (en) * | 2003-06-06 | 2005-03-31 | Pharmacia Corporation | Compositions of a cyclooxygenase-2 selective inhibitor and an anticonvulsant agent for the treatment of central nervous system disorders |
AR049646A1 (en) * | 2004-06-16 | 2006-08-23 | Janssen Pharmaceutica Nv | USEFUL SULFAMATE AND SULFAMIDE DERIVATIVES FOR THE TREATMENT OF EPILEPSY AND RELATED DISORDERS |
ES2310366T3 (en) * | 2004-08-24 | 2009-01-01 | Janssen Pharmaceutica Nv | NEW DERIVATIVES OF HETEROARIL SULFONAMIDE BENZO-CONDENSED USEFUL AS ANTI-CONVERSIVE AGENTS. |
IS7748A (en) * | 2005-03-17 | 2006-09-18 | Actavis Group | Composition for tablets containing topiramate |
US20070155823A1 (en) * | 2005-12-19 | 2007-07-05 | Smith-Swintosky Virginia L | Use of benzo-fused heterocycle sulfamide derivatives as neuroprotective agents |
US20070155827A1 (en) * | 2005-12-19 | 2007-07-05 | Smith-Swintosky Virginia L | Use of benzo-fused heterocycle sulfamide derivatives for the treatment of depression |
US20070155824A1 (en) * | 2005-12-19 | 2007-07-05 | Smith-Swintosky Virginia L | Use of benzo-fused heterocycle sulfamide derivatives for disease modification / epileptogenesis |
US20070191474A1 (en) * | 2006-02-15 | 2007-08-16 | Smith-Swintosky Virginia L | Use of benzo-fused heterocyle sulfamide derivatives for the treatment of migraine |
US20070191460A1 (en) * | 2006-02-15 | 2007-08-16 | Smith-Swintosky Virginia L | Use of Benzo-Heteroaryl Sulfamide Derivatives for the Treatment of Disease Modification / Epileptogenesis |
US20070191451A1 (en) * | 2006-02-15 | 2007-08-16 | Smith-Swintosky Virginia L | Use of benzo-heteroaryl sulfamide derivatives as neuroprotective agents |
US20090247617A1 (en) * | 2008-03-26 | 2009-10-01 | Abdel-Magid Ahmed F | Process for the preparation of benzo-fused heteroaryl sulfamates |
US20090247616A1 (en) * | 2008-03-26 | 2009-10-01 | Smith-Swintosky Virginia L | Use of benzo-fused heterocyle sulfamide derivatives for the treatment of anxiety |
US20090304789A1 (en) * | 2008-06-09 | 2009-12-10 | Thomas Najarian | Novel topiramate compositions and an escalating dosing strategy for treating obesity and related disorders |
US8580298B2 (en) | 2008-06-09 | 2013-11-12 | Vivus, Inc. | Low dose topiramate/phentermine composition and methods of use thereof |
US8652527B1 (en) | 2013-03-13 | 2014-02-18 | Upsher-Smith Laboratories, Inc | Extended-release topiramate capsules |
US9101545B2 (en) | 2013-03-15 | 2015-08-11 | Upsher-Smith Laboratories, Inc. | Extended-release topiramate capsules |
Citations (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4513006A (en) * | 1983-09-26 | 1985-04-23 | Mcneil Lab., Inc. | Anticonvulsant sulfamate derivatives |
US4792569A (en) * | 1987-08-27 | 1988-12-20 | Mcneilab, Inc. | Anticonvulsant phenethyl sulfamates |
Family Cites Families (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5384327A (en) * | 1992-12-22 | 1995-01-24 | Mcneilab, Inc. | Anticonvulsant sorbopyranose sulfamates |
-
1997
- 1997-06-23 US US08/881,023 patent/US5753694A/en not_active Expired - Fee Related
- 1997-06-24 DE DE69711067T patent/DE69711067T2/en not_active Expired - Fee Related
- 1997-06-24 CA CA002258892A patent/CA2258892C/en not_active Expired - Fee Related
- 1997-06-24 ES ES97931367T patent/ES2176755T3/en not_active Expired - Lifetime
- 1997-06-24 AU AU35010/97A patent/AU725093B2/en not_active Ceased
- 1997-06-24 CZ CZ19984279A patent/CZ293945B6/en not_active IP Right Cessation
- 1997-06-24 UA UA98126945A patent/UA46112C2/en unknown
- 1997-06-24 AT AT97931367T patent/ATE214274T1/en not_active IP Right Cessation
- 1997-06-24 HU HU9904318A patent/HUP9904318A3/en unknown
- 1997-06-24 NZ NZ333588A patent/NZ333588A/en unknown
- 1997-06-24 SK SK1806-98A patent/SK284331B6/en unknown
- 1997-06-24 EP EP97931367A patent/EP0936908B1/en not_active Expired - Lifetime
- 1997-06-24 WO PCT/US1997/010955 patent/WO1998000131A1/en active IP Right Grant
- 1997-06-24 BR BR9710993-2A patent/BR9710993A/en not_active Application Discontinuation
- 1997-06-24 SI SI9730259T patent/SI0936908T1/en unknown
- 1997-06-24 AP APAP/P/1998/001428A patent/AP1167A/en active
- 1997-06-24 DK DK97931367T patent/DK0936908T3/en active
- 1997-06-24 JP JP10504245A patent/JP2000514426A/en active Pending
- 1997-06-24 IL IL12771797A patent/IL127717A/en not_active IP Right Cessation
- 1997-06-24 PT PT97931367T patent/PT936908E/en unknown
- 1997-06-27 ZA ZA975764A patent/ZA975764B/en unknown
-
1998
- 1998-12-22 NO NO19986054A patent/NO317136B1/en unknown
Patent Citations (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4513006A (en) * | 1983-09-26 | 1985-04-23 | Mcneil Lab., Inc. | Anticonvulsant sulfamate derivatives |
US4792569A (en) * | 1987-08-27 | 1988-12-20 | Mcneilab, Inc. | Anticonvulsant phenethyl sulfamates |
Cited By (18)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
AU782344C (en) * | 1999-04-08 | 2006-08-17 | Ortho-Mcneil Pharmaceutical, Inc. | Anticonvulsant derivatives useful in treating chronic neurodegenerative disorders |
WO2000061138A1 (en) * | 1999-04-08 | 2000-10-19 | Ortho-Mcneil Pharmaceutical, Inc. | Anticonvulsant derivatives useful in treating chronic neurodegenerative disorders |
US6583172B1 (en) | 1999-04-08 | 2003-06-24 | Richard P. Shank | Anticonvulsant derivatives useful in treating chronic neurodegenerative disorders |
AU782344B2 (en) * | 1999-04-08 | 2005-07-21 | Ortho-Mcneil Pharmaceutical, Inc. | Anticonvulsant derivatives useful in treating chronic neurodegenerative disorders |
US8084491B2 (en) | 2000-11-30 | 2011-12-27 | Novodermix International Limited | Treatments for wound healing |
WO2002043731A3 (en) * | 2000-11-30 | 2003-02-20 | Univ Florida | Treatments for neurogenetic disorders, impulse control disorders, and wound healing |
US8084490B2 (en) | 2004-06-16 | 2011-12-27 | Janssen Pharmaceutica N.V. | Sulfamate and sulfamide derivatives useful for the treatment of epilepsy and related disorders |
US8283478B2 (en) | 2005-05-20 | 2012-10-09 | Janssen Pharmaceutica Nv | Process for preparation of sulfamide derivatives |
US8497298B2 (en) | 2005-12-19 | 2013-07-30 | Janssen Pharmaceutica Nv | Use of benzo-fused heterocycle sulfamide derivatives for lowering lipids and lowering blood glucose levels |
US8492431B2 (en) | 2005-12-19 | 2013-07-23 | Janssen Pharmaceutica, N.V. | Use of benzo-fused heterocycle sulfamide derivatives for the treatment of obesity |
US8691867B2 (en) | 2005-12-19 | 2014-04-08 | Janssen Pharmaceutica Nv | Use of benzo-fused heterocycle sulfamide derivatives for the treatment of substance abuse and addiction |
US8716231B2 (en) | 2005-12-19 | 2014-05-06 | Janssen Pharmaceutica Nv | Use of benzo-fused heterocycle sulfamide derivatives for the treatment of pain |
US8937096B2 (en) | 2005-12-19 | 2015-01-20 | Janssen Pharmaceutica Nv | Use of benzo-fused heterocyle sulfamide derivatives for the treatment of mania and bipolar disorder |
US8853263B2 (en) | 2006-05-19 | 2014-10-07 | Janssen Pharmaceutica Nv | Co-therapy for the treatment of epilepsy and related disorders |
FR2903019A1 (en) * | 2006-06-30 | 2008-01-04 | Univ Claude Bernard Lyon I Eta | USE OF A CARBONIC ANHYDRASE INHIBITOR FOR THE PREPARATION OF A MEDICAMENT FOR TREATING SKELETAL MUSCLE DEGENERATION |
WO2008001016A1 (en) * | 2006-06-30 | 2008-01-03 | Universite Claude Bernard Lyon 1 | Use of a carbonic anhydrase inhibitor for preparation of a drug for treating skeletal muscle degeneration |
US8809385B2 (en) | 2008-06-23 | 2014-08-19 | Janssen Pharmaceutica Nv | Crystalline form of (2S)-(-)-N-(6-chloro-2,3-dihydro-benzo[1,4]dioxin-2-ylmethyl)-sulfamide |
US8815939B2 (en) | 2008-07-22 | 2014-08-26 | Janssen Pharmaceutica Nv | Substituted sulfamide derivatives |
Also Published As
Publication number | Publication date |
---|---|
ZA975764B (en) | 1998-12-28 |
ES2176755T3 (en) | 2002-12-01 |
CA2258892C (en) | 2005-08-09 |
DK0936908T3 (en) | 2002-05-27 |
NZ333588A (en) | 2000-07-28 |
NO986054L (en) | 1999-03-01 |
HUP9904318A3 (en) | 2001-02-28 |
SK284331B6 (en) | 2005-01-03 |
ATE214274T1 (en) | 2002-03-15 |
JP2000514426A (en) | 2000-10-31 |
DE69711067T2 (en) | 2002-09-19 |
EP0936908B1 (en) | 2002-03-13 |
AU725093B2 (en) | 2000-10-05 |
US5753694A (en) | 1998-05-19 |
UA46112C2 (en) | 2002-05-15 |
AP1167A (en) | 2003-06-30 |
AP9801428A0 (en) | 1998-12-31 |
CZ293945B6 (en) | 2004-08-18 |
BR9710993A (en) | 2002-02-26 |
IL127717A0 (en) | 1999-10-28 |
DE69711067D1 (en) | 2002-04-18 |
SK180698A3 (en) | 2000-07-11 |
EP0936908A1 (en) | 1999-08-25 |
NO986054D0 (en) | 1998-12-22 |
CA2258892A1 (en) | 1998-01-08 |
IL127717A (en) | 2004-09-27 |
AU3501097A (en) | 1998-01-21 |
CZ427998A3 (en) | 1999-08-11 |
HUP9904318A2 (en) | 2000-05-28 |
PT936908E (en) | 2002-08-30 |
SI0936908T1 (en) | 2002-12-31 |
NO317136B1 (en) | 2004-08-23 |
Similar Documents
Publication | Publication Date | Title |
---|---|---|
EP0936908B1 (en) | Anticonvulsant derivatives useful in treating amyotrophic lateral sclerosis (als) | |
US5760007A (en) | Anticonvulsant derivatives useful in treating neuropathic pain | |
US5935933A (en) | Anticonvulsant derivatives useful in treating neuropathic pain | |
AU739363B2 (en) | Use of topiramate or derivatives thereof for the manufacture of a medicament for the treatment of manic-depressive bipolar disorders | |
NZ514810A (en) | Anticonvulsant derivatives useful in lowering lipids | |
US20020052325A1 (en) | Anticonvulsant derivatives useful in maintaining weight loss | |
AU725570B2 (en) | Anticonvulsant derivatives useful in treating neuropathic pain | |
US5760006A (en) | Anticonvulsant derivatives useful in treating psoriasis | |
EP1143917B1 (en) | Anticonvulsant derivatives useful in treating post traumatic stress disorder | |
AU759756B2 (en) | Anticonvulsant derivatives useful in treating alcohol dependency, addiction and abuse | |
KR100496933B1 (en) | Anticonvulsive derivatives useful for the treatment of amyotrophic lateral sclerosis | |
AP1230A (en) | Anticonvulsant derivatives useful in treating psoriasis. | |
AU4685300A (en) | Anticonvulsant derivatives useful in treating cocaine dependency | |
WO1998000129A9 (en) | Anticonvulsant derivatives useful in treating psoriasis |
Legal Events
Date | Code | Title | Description |
---|---|---|---|
WWE | Wipo information: entry into national phase |
Ref document number: 97195910.2 Country of ref document: CN |
|
AK | Designated states |
Kind code of ref document: A1 Designated state(s): AL AM AT AU AZ BA BB BG BR BY CA CH CN CU CZ DE DK EE ES FI GB GE HU IL IS JP KE KG KP KR KZ LC LK LR LS LT LU LV MD MG MK MN MW MX NO NZ PL PT RO RU SD SE SG SI SK TJ TM TR TT UA UG UZ VN |
|
AL | Designated countries for regional patents |
Kind code of ref document: A1 Designated state(s): AT BE CH DE DK ES FI FR GB GR IE IT LU MC NL PT SE |
|
DFPE | Request for preliminary examination filed prior to expiration of 19th month from priority date (pct application filed before 20040101) | ||
121 | Ep: the epo has been informed by wipo that ep was designated in this application | ||
WWE | Wipo information: entry into national phase |
Ref document number: PV1998-4279 Country of ref document: CZ |
|
ENP | Entry into the national phase |
Ref document number: 2258892 Country of ref document: CA Ref document number: 2258892 Country of ref document: CA Kind code of ref document: A |
|
WWE | Wipo information: entry into national phase |
Ref document number: 333588 Country of ref document: NZ |
|
WWE | Wipo information: entry into national phase |
Ref document number: 1019980710674 Country of ref document: KR |
|
WWE | Wipo information: entry into national phase |
Ref document number: 180698 Country of ref document: SK Ref document number: 1199801090 Country of ref document: VN |
|
WWE | Wipo information: entry into national phase |
Ref document number: PA/A/1999/000179 Country of ref document: MX |
|
WWE | Wipo information: entry into national phase |
Ref document number: 1997931367 Country of ref document: EP |
|
REG | Reference to national code |
Ref country code: DE Ref legal event code: 8642 |
|
WWP | Wipo information: published in national office |
Ref document number: PV1998-4279 Country of ref document: CZ |
|
WWP | Wipo information: published in national office |
Ref document number: 1997931367 Country of ref document: EP |
|
WWP | Wipo information: published in national office |
Ref document number: 1019980710674 Country of ref document: KR |
|
WWG | Wipo information: grant in national office |
Ref document number: 1997931367 Country of ref document: EP |
|
WWG | Wipo information: grant in national office |
Ref document number: PV1998-4279 Country of ref document: CZ |
|
WWG | Wipo information: grant in national office |
Ref document number: 1019980710674 Country of ref document: KR |