Publication number: 20030166581
Abstract: The invention encompasses novel salts of topiramate, and pharmaceutically acceptable polymorphs, solvates, hydrates, dehydrates, co-crystals, anhydrous, or amorphous forms thereof, as well as pharmaceutical compositions and pharmaceutical unit dosage forms containing the same. In particular, the invention encompasses pharmaceutically acceptable salts of topiramate, including without limitation topiramate sodium, topiramate lithium, topiramate potassium, or polymorphs, solvates, hydrates, dehydrates, co-crystals, anhydrous, and amorphous forms thereof. The invention further encompasses novel co-crystals or complexes of topiramate, as well as pharmaceutical compositions comprising them. The invention also encompasses methods of treating or preventing a variety of diseases and conditions including, but not limited to, seizures, epileptic conditions, tremors, cerebral function disorders, obesity, neuropathic pain, affective disorders, tobacco cessation, migraines, and cluster headache.
Type:
Application
Filed:
November 18, 2002
Publication date:
September 4, 2003
Inventors:
Orn Almarsson, Julius Remenar, Matthew L. Peterson
Patent number: 6294541
Abstract: A compound of the formula:
wherein
R3 represent a C1-8 alkyl which is unbranched or branched and unsubstituted or substituted with OH, alkoxy, CO2H, ═NOH, ═NOCONH2, or ═O; C3-8 cycloalkyl which is unsubstituted or substituted with OH, alkoxy, CO2H, ═NOH, ═NOCONH2, or ═O; C4-8 cycloalkylalkyl wherein the cycloalkyl portion is unsubstituted or substituted with OH, alkoxy, CO2H, ═NOH, ═NOCONH2, or ═O; aryl which is unsubstituted or substituted with Cl, NH2, alkylamino, dialkylamino, amido, C1-C8 alkylamido, C1-C3 dialkylamido, OH, alkoxy, HC═NOH, HC═NOCONH2, C1-C3 alkyl, phenyl or benzyl; aralkyl (C1-4); heterocyclyl; heterocyclylalkyl (C1-C4); and heteroaryl;
R8 represents H or a C1-8 alkyl which is unbranched or branched and unsubstituted or substituted with OH, alkoxy, CO2H, ═NOH, ═NOCONH2, or ═O; C3-8 cycloalkyl which is unsubstituted or substituted with OH, alkoxy, CO2H, ═NOH, ═NOCONH2, or ═O; C4-8 cyclo
Type:
Grant
Filed:
October 14, 1999
Date of Patent:
September 25, 2001
Assignee:
Euro-Celtique S.A.
Inventors:
David J. Cavalla, Mark Chasin, Peter Hofer, Andre Gehrig, Peter Wintergerst
Patent number: 6248746
Abstract: With the above and other objects in view, the present invention comprises compounds having the general formula (I):
wherein:
R1 is a C2-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, C3-8 cycloalkyl, C3-8 cycloalkenyl or cycloalkynyl, wherein said alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl or cycloalkynyl is optionally substituted with hydroxy, C1-5 alkoxy, C3-5 cycloalkoxy, halogen, oxo, carbamido, hydroxycarbamido, oximido, C1-5 alkyloximido, C3-5 cycloalkyloximido, C1-5 acyloximido or C3-5 cycloacyloximido;
Q is methylene or ethylene;
R3 is aryl or heteroaryl wherein said aryl or heteroaryl has one to three substituents selected from the group consisting of C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-6 cycloalkyl, C3-6 cycloalkenyl, cycloalkynyl, C3-5 alkylene, C3-5 cycloalkylene, haloC1-6 alkyl, haloC1-6 cycloalkyl, hydroxy, C1-5 alkoxy, C3-5 cycloalkoxy, C1-2 alkylenedioxy, C1-6 acyl, C3-6 cycloacyl, C1-6 acyloxy, C3-6 cycloacyloxy, halogen, nitro or cyano;
R8 is C1-5 alkyl or C3-5 cycl
Type:
Grant
Filed:
January 7, 1999
Date of Patent:
June 19, 2001
Assignee:
Euro-Celtique S.A.
Inventors:
Mark Chasin, David J. Cavalla, Peter Hofer
Patent number: 6133274
Abstract: Disclosed are therapeutic compounds having the formula:(R)j-(core moiety),including resolved enantiomers, diastereomers, hydrates, salts, solvates and mixtures thereof. j is an integer from one to three, the core moiety is either non-cyclic or comprises at least one five- to seven-membered ring structure, R may be selected from the group consisting of hydrogen, halogen, hydroxyl, amino, substituted or unsubstituted benzyl, C.sub.1-6 alkyl or C.sub.1-6 alkenyl, and at least one R has the formula I: ##STR1## n is an integer from seven to twenty and at least one of X or Y is --OH. The other of X or Y, which is not --OH, is hydrogen, CH.sub.3 --, CH.sub.3 --CH.sub.2 --, CH.sub.3 --(CH.sub.2).sub.2 -- or (CH.sub.3).sub.2 --CH.sub.2 --, and each W.sub.1, W.sub.2, and W.sub.3 is independently hydrogen, CH.sub.3 --, CH.sub.3 --CH.sub.2 --, CH.sub.3 --(CH.sub.2).sub.2 -- or (CH.sub.3).sub.2 --CH.sub.2 --. The X, Y, W.sub.1, W.sub.2, or W.sub.
Type:
Grant
Filed:
November 26, 1996
Date of Patent:
October 17, 2000
Assignee:
Cell Therapeutics, Inc.
Inventors:
Gail E. Underiner, David Porubek, J. Peter Klein, Paul Woodson
Patent number: 6020337
Abstract: Therapeutic compounds, including resolved enantiomers and/or diastereomers, hydrates, salts, solvates and mixtures thereof, having a formula: ##STR1## wherein R.sub.0 is selected from the group consisting of hydrogen, halo, hydroxyl, amino, substituted or unsubstituted C.sub.(1-10) alkyl, C.sub.(2-10) alkenyl, cyclic or heterocyclic groups, wherein the substituents of substituted C.sub.(1-10) alkyl, C.sub.(2-10) alkenyl are other than halo; n is an integer from one to sixteen; R.sub.1, R.sub.2, and R.sub.3 are independently selected from the group consisting of a halo; haloacetoxy; hydrogen; hydroxy; oxo; --N.dbd.C.dbd.S; --N.dbd.C.dbd.O; --0--C.tbd.N; --C.tbd.N; --N.dbd.N.dbd.N; and --C--(R.sub.5).sub.3, R.sub.5 being independently a halo or hydrogen, at least one R.sub.5 being halo, at least one of R.sub.1, R.sub.2, and R.sub.3 being halo, cyano, isocyano, isothiocyano, azide or haloacetoxy group; R.sub.4 is hydrogen, C.sub.(1-6) alkyl, C.sub.(1-6) alkenyl, cyclo C.sub.
Type:
Grant
Filed:
September 16, 1997
Date of Patent:
February 1, 2000
Assignee:
Cell Therapeutics, Inc.
Inventors:
Alistair J. Leigh, John Michnick, Anil M. Kumar, J. Peter Klein, Gail Underiner