Abstract: Substituted C-cyclohexylmethylamine derivatives, methods for the production thereof, pharmaceuticals containing said compounds, the use of substituted C-cyclohexylmethylamine derivatives for producing pharmaceuticals, and method of pain treatment using the pharmaceuticals.
Type:
Application
Filed:
March 31, 2003
Publication date:
December 18, 2003
Applicant:
GRUENENTHAL GmbH
Inventors:
Bernd Sundermann, Corinna Maul, Helmut Buschmann, Michael Finkam, Babette-Yvonne Koegel
Abstract: The invention relates to O-substituted 6-methyl-tramadol derivatives, to methods for producing them, to medicaments containing these compounds, to the use of O-substituted 6-methyl-tramadol derivatives for producing medicaments for treating pain and other symptoms or diseases, and to methods of treatment using the medicaments.
Type:
Application
Filed:
March 31, 2003
Publication date:
November 27, 2003
Applicant:
GRUENENTHAL GMBH
Inventors:
Helmut Buschmann, Babette-Yvonne Koegel, Elmar Friderichs, Dagmar Kaulartz
Abstract: The present invention relates to pharmaceutical preparations in the form of aqueous solutions for the production of propellant-free aerosols.
Abstract: The use of a compound of formula (I): wherein R1, R2, R3, R4, R5 and R6 are independently selected from hydrogen, alkyl, aryl and non-aromatic heterocyclic groups, or each of one or more pair(s) of the substituent groups R1 to R6 may together form a 3, 4, 5, 6, 7 or 8-membered ring containing 0, 1 or 2 heteroatom(s); R7 is selected from alkyl, aryl and non-aromatic heterocyclic groups, and R8 is selected from hydrogen, halogen, alkyl, aryl and non-aromatic heterocyclic groups; and pharmaceutically acceptable salts and prodrugs thereof, in the manufacture of a medicament for use in the treatment of a condition generally associated with abnormalities in glutamatergic transmission; novel compounds of formula (1) per se and for use in therapy.
Type:
Application
Filed:
March 31, 2003
Publication date:
November 6, 2003
Inventors:
Michael Frederick Snape, Roger John Gillespie, Claire Elizabeth Dawson, Steven Michael McAteer, Suneel Gaur
Abstract: The present invention provides enantiomers of N-Desmethyl venlafaxine, as well as their use in pharmaceutical compositions and medically useful treatments, particularly including central nervous system uses.
Abstract: Methods are disclosed for the treatment and prevention of disorders and conditions including, but are not limited to, erectile dysfunction, affective disorders, weight gain, cerebral functional disorders, pain, obsessive-compulsive disorder, substance abuse, chronic disorders, anxiety, eating disorders, migraines, and incontinence. The methods comprise the administration of a dopamine reuptake inhibitor and optionally an additional pharmacologically active compound. Pharmaceutical compositions and dosage forms are also disclosed that comprise a dopamine reuptake inhibitor and optionally an additional pharmacologically active compound. Preferred dopamine reuptake inhibitors are racemic or optically pure sibutrarnine metabolites and pharmaceutically acceptable salts, solvates, and clathrates thereof. Preferred additional pharmacologically active compounds include drugs that affect the central nervous system, such as 5-HT3 antagonists.
Type:
Application
Filed:
March 25, 2003
Publication date:
October 16, 2003
Applicant:
Sepracor Inc.
Inventors:
Thomas P. Jerussi, Chrisantha H. Senanayake, Qun K. Fang
Abstract: Methods and pharmaceutical compositions for using desmethylselegiline. In particular, the present invention provides novel compositions and methods for using desmethylselegiline for selegiline-responsive diseases and conditions. Diseases and conditions responsive to selegiline include those produced by neuronal degeneration or neuronal trauma and those due to immune system dysfunction. Desmethylselegiline is the R-(−) enantiomer of N-methyl-N-(prop-2-ynyl)-2-aminophenylpropane. Claimed compositions include both the R-(−) isomer and mixtures of the R-(−) and S(+) isomers. Pharmaceutically acceptable acid addition salts may also be used. Effective dosages are a daily dose of at least about 0.015 mg/kg of body weight.
Abstract: The application is directed to the treatment of neoplastic diseases or conditions by administering R(−) desmethylselegiline, S(+) desmethylselegiline, or a combination of the two. Neoplastic diseases and conditions responsive to R(−) desmethylselegiline and/or S(+) desmethylselegiline include both malignant and benign neoplasms.
Abstract: The present disclosure is directed to methods for alleviating the symptoms associated with peripheral neuropathy by administering R(−)-desmethylselegiline, S(+) desmethylselegiline, or a combination of the two. The neuropathy may be the result of a genetically inherited condition, a systemic disease, or exposure to a toxic agent. The disclosure is also directed to a method for treating patients with cancer by administering a chemotherapeutic agent known to have a toxic affect on peripheral nerves together with R(−)-desmethylselegiline, S(+) desmethylselegiline, or a mixture of the two.
Abstract: The present invention is directed to methods for alleviating the symptoms associated with peripheral neuropathy. The neuropathy may be the result of a genetically inherited condition, systemic disease or exposure to a toxic agent. A reduction or elimination of symptoms is obtained by administering the drug selegiline. The invention is also directed to a method for treating patients with cancer by administering a chemotherapeutic agent known to have a toxic affect on peripheral nerves together with selegiline.
Abstract: The invention relates to high purity (1R,2S,4R)-(−)-2-[(2′-{N,N-dimethylamino}-ethoxy)]-2-[phenyl]-1,7,7-tri-[methyl]-bicyclo[2.2.1]heptane and pharmaceutically acceptable acid addition salts thereof containing not more than 0.2% of (1R,3S,4R)-3-[(2′-{N,N-dimethylamino}-ethyl)]-1,7,7-tri-[methyl]-bicyclo[2.2.1]heptane-2-one and/or of a pharmaceutically acceptable acid addition salt thereof.
Furthermore the invention is concerned with a process for the preparation of these compounds.
Moreover the invention relates to medicaments containing 1 or more of these compounds and their use.
Type:
Grant
Filed:
October 30, 2001
Date of Patent:
September 23, 2003
Assignee:
Orion Corporation
Inventors:
Gyula Lukács, Gyula Simig, Tibor Mezei, Zoltán Budai, Márta Porcs-Makkay, György Krasznai, Kálmán Nagy, Györgyi Donáth Vereczkey, Tibor Szabó, Norbert Németh, János Szulágyi
Abstract: The invention solves a controlled release pharmaceutical composition containing tramadol hydrochloride, characterized in that it contains 100 to 200 mg of the active ingredient in admixture with micronized esters of glycerol with higher fatty acids, alkali salts of phosphoric acid, non-ionic vinylpyrrolidone polymers, substances from the group of salts of higher fatty acids with alkaline earth metals and silicon oxides and a method for the preparation of this composition.
Type:
Application
Filed:
May 5, 2003
Publication date:
September 18, 2003
Inventors:
L?apos;uboslav Razus, Helena Sedlarova, Ivan Varga, Ondrej Gattnar, Marian Zemanek
Abstract: Squaric acid Derivatives of formula (1) are described: 1
Type:
Application
Filed:
December 13, 2002
Publication date:
August 28, 2003
Inventors:
Barry John Langham, Rikki Peter Alexander, John Clifford Head, Janeen Marsha Linsley, John Robert Porter, Sarah Catherine Archibald, Graham John Warrellow
Abstract: The invention relates to a method of producing an agglomerate of drug and solid binder. The process involves producing individual agglomerate particles and then converting the convertible amorphous content of same, following agglomeration, by the application of, for example, moisture. Agglomerates capable of conversion as well as the finished agglomerates and oral and nasal dosing systems including same are also contemplated. The process produces agglomerates which are rugged but which will produce an acceptable fine particle fraction during dosing.
Abstract: Disclosed are a compound of tramadol and a sugar substitute, pharmaceutical compositions and sustained-release formulations comprising the compound, and methods of treatment using the compound. The tramadol compound according to the present invention has reduced bitter taste of tramadol and is more acceptable to the patient.
Abstract: This invention provides pharmaceutically active enantiomers of the venlafaxine metabolite O-Desmethyl venlafaxine, R(−)-4-[2-(Dimethylamino-1-(1-hydroxycyclo-hexyl)ethyl]phenol or R(−)1-[2-(dimethylamino)-1-(4-hydroxyphenyl)ethyl]cyclo-hexanol, and S(+)-1-[2-(Dimethylamino)-1-(4-hydroxycyclohexyl)ethyl]cyclohexanol or S(+)-4-[2-(Dimethylamino)-1-(1-hydroxcyclohexyl)ethyl]phenol,or one one or more pharmaceutically acceptable salts or salt hydrates thereof, as well as pharmaceutical compositions utilizing these enantiomers and methods of using the enantiomers to treat, inhibit or control central nervous system disorders.
Abstract: A compound of the formula
wherein X, Y, Z, R2 and R3 are as defined above, useful in treating or preventing migraine, depression and other disorders for which a 5-HT1, agonist or antagonist is indicated.
Abstract: This invention relates to the use of a CYP2D6 inhibitor in combination with a drug having CYP2D6 catalyzed metabolism, wherein the drug and the CYP2D6 inhibitor are not the same compound; and pharmaceutical compositions for said use.
Abstract: This invention relates to aerosol formulations of use for the administration of medicaments by inhalation, in particular a pharmaceutical aerosol formulation which comprises particulate salbutamol and physiologically acceptable salts and solvates thereof and a fluorocarbon or hydrogen-containing chlorofluorocarbon propellant, which formulation is substantially free of surfactant. A method of treating respiratory disorders which comprises administration by inhalation of an effective amount of a pharmaceutical aerosol formulation as defined is also described.
Type:
Application
Filed:
March 11, 2003
Publication date:
July 31, 2003
Applicant:
Glaxo Group Limited
Inventors:
Rachel Ann Akehurst, Anthony James Taylor, David Andrew Wyatt
Abstract: The present invention provides a method for improving respiratory function and inhibiting muscular degeneration (e.g., dystrophy and atrophy). Alternative embodiments of the invention provide a method of inhibiting motor neuron apoptosis and the subsequent muscular degeneration associated with the denervation of muscular tissue resulting from neuron death.
Type:
Application
Filed:
September 13, 2002
Publication date:
July 24, 2003
Applicant:
The Children's Medical Center Corporation
Abstract: The present invention relates to compounds of formula I:
and to their pharmaceutically acceptable salts. Compounds of formula I exhibit activity as serotonin, norepinephrine, and dopamine reuptake inhibitors and can be used in the treatment of central nervous system and other disorders.
Abstract: Methods and compositions are disclosed for the intravaginal or rectal delivery of selected serotonin reuptake inhibitors (SSRIs) to the systemic circulation. Such methods and compositions are useful in the treatment of depression, migraine headaches, chronic pain, psychoactive substance abuse disorders, pre-menstrual dysphoric disorder (PMDD) and obsessive compulsive disorders. The compositions may be formulated for the immediate release or controlled release of SSRIs over an extended period of time. A preferred SSRI is fluoxetine.
Type:
Application
Filed:
March 12, 2002
Publication date:
July 17, 2003
Inventors:
Anu Mahashabde, Martha Francine Kay, Brian Glazer, Junxiong Zhang
Abstract: Powdery pharmaceutical compositions including an active ingredient and carrier particles containing only a small amount of lubricant, 0.05-0.5% by weight, are used to prepare dry powder inhalers in order to increase the fine particle dose. A process for coating the surface of the carrier particles with such little amount of lubricant is also provided. Use of limited amount of lubricant is safe and provides ordered stable mixtures without segregation of the active particles during handling and before use.
Type:
Application
Filed:
February 5, 2003
Publication date:
July 17, 2003
Applicant:
Chiesi Farmaceutici S.p.A.
Inventors:
Rossella Musa, Paolo Ventura, Paolo Chiesi
Abstract: Dosage forms of sertraline encapsulated in a water-immiscible vehicle shorten Tmax and/or reduce side effects and/or decrease sertraline precipitation in chloride ion-containing use environments such as the gastrointestinal tract.
Type:
Application
Filed:
December 5, 2002
Publication date:
July 17, 2003
Inventors:
William John Curatolo, Ravi Mysore Shanker
Abstract: The present invention provides a method of treating and preventing obesity and related co-morbid conditions comprising the administration of a therapeutically effective amount of one or more monoamine reuptake inhibitors which are serotonin reuptake inhibitors and/or noradrenaline reuptake inhibitors and a 5-HT1A agonist to a patient in need thereof.
Type:
Application
Filed:
November 12, 2002
Publication date:
July 10, 2003
Inventors:
David John Heal, Sharon Crawford Cheetham
Abstract: The present invention is concerned with pharmaceutical formulations comprising a combination of salmeterol and budesonide and the use of such formulations in medicine, particularly in the prophylaxis and treatment of respiratory diseases.
Abstract: Tramadol or a pharmaceutically acceptable salt thereof is used in the manufacture of a pharmaceutical preparation for the treatment of functional gastrointestinal disorders such as irritable bowel syndrome.
Abstract: The present invention is concerned with pharmaceutical formulations comprising a combination of salmeterol and mometasone and the use of such formulations in medicine, particularly in the prophylaxis and treatment of respiratory diseases.
Type:
Application
Filed:
October 15, 2002
Publication date:
June 19, 2003
Inventors:
Brian Charles Gavin, Ronique Nichele Garrett, Trevor Charles Roche
Abstract: Disclosed are multibinding compounds which are &bgr;2 adrenergic receptor agonists and are useful in the treatment and prevention of respiratory diseases such as asthma and bronchitis. They are also useful in the treatment of nervous system injury and premature labor.
Type:
Grant
Filed:
August 14, 2000
Date of Patent:
June 10, 2003
Assignee:
Theravance, Inc.
Inventors:
Edmund J. Moran, John H. Griffin, Seok-Ki Choi
Abstract: Crystalline forms of Venlafaxine hydrochloride were found, referred to hereinafter as polymorphic Forms A, B and D. Furthermore, the present invention is directed to processes for the preparation of these crystalline forms and pharmaceutical compositions comprising the crystalline forms.
Type:
Application
Filed:
October 1, 2002
Publication date:
June 5, 2003
Inventors:
Paul Adriaan Van Der Schaaf, Claudia Marcolli, Martin Szelagiewicz, Beat Freiermuth
Abstract: Methods are disclosed for the treatment and prevention of disorders and conditions such as, but are not limited to: eating disorders; weight gain; obesity; irritable bowel syndrome; obsessive-compulsive disorders; platelet adhesion; apnea; affective disorders such as attention deficit disorders, depression, and anxiety; male and female sexual function disorders; restless leg syndrome; osteoarthritis; substance abuse including nicotine and cocaine addiction; narcolepsy; pain such as neuropathic pain, diabetic neuropathy, and chronic pain; migraines; cerebral function disorders; chronic disorders such as premenstrual syndrome; and incontinence.
Type:
Application
Filed:
October 23, 2002
Publication date:
May 22, 2003
Applicant:
Sepracor, Inc.
Inventors:
Thomas P. Jerussi, Chrisantha H. Senanayake, Qun K. Fang
Abstract: The present invention is concerned with pharmaceutical formulations comprising a combination of salmeterol and rofleponide and the use of such formulations in medicine, particularly in the prophylaxis and treatment of respiratory diseases.
Abstract: A process for separating a mixture of trans (RR, SS) and cis (RS, SR) tramadol comprises a classical salt resolution using a chiral resolving agent selected from tartaric acid and derivatives thereof, and mandelic acid, provided that the resolving agent is not substantially single enantiomer di-O,O-toluoyltartaric acid.
Abstract: The present invention comprises an improved method of treatment of AIDS-associated non-Hodgkin's lymphoma by administering gallium nitrate in a pharmaceutically acceptable vehicle.
Abstract: The invention is directed, in part, to racemic and stereomerically pure 2-hydroxy derivatives of sibutramine and its metabolites, and 2-hydroxy derivatives of desmethylsibutramine and didesmethylsibutramine in particular. The invention is further directed to novel methods of preparing these derivatives are also disclosed.
Type:
Application
Filed:
September 11, 2002
Publication date:
May 8, 2003
Inventors:
Chris H. Senanayake, Thomas P. Jerussi, Mark G. Currie, Qun K. Fang, Bob Hsu
Abstract: An intradermal patch having a permeable backing coated with a polyvinylpyrrolidone-based hydrogel and containing one or more local anesthetics. The patch is breathable, non-irritating upon application and removal, soothing, and sterile. The patch is useful for treating the pain associated with non-intact skin indications.
Abstract: This invention encompasses methods for the treatment and prevention of disorders that include, but are not limited to, eating disorders; weight gain; obesity; irritable bowel syndrome; obsessive-compulsive disorders; platelet adhesion; apnea; affective disorders such as attention deficit disorders, depression, and anxiety; male and female sexual function disorders; restless leg syndrome; osteoarthritis; substance abuse including nicotine and cocaine addiction; narcolepsy; pain such as neuropathic pain, diabetic neuropathy, and chronic pain; migraines; cerebral function disorders; chronic disorders such as premenstrual syndrome; and incontinence.
Abstract: The present invention is a method of treating an mammal selected from the group consisting of humans and horses who has asthma, COPD or allergic rhinitis and is in need of such treatment by inhaling an anti-asthma, anti-COPD anti-allergic rhinitis effective amount, respectively, of a compound selected from the group consisting of tolterodine
hydroxytolterodine and 2-(diisopropylamino)ethyl-1-phenylcyclopentanecarboxylate and pharmaceutically acceptable salts thereof.
Type:
Grant
Filed:
October 23, 2001
Date of Patent:
March 25, 2003
Assignee:
Pharmacia & Upjohn Company
Inventors:
Per-Goran Gillberg, Staffan Sundquist, Sue K. Cammarata
Abstract: A class of substituted benzylnaphthylene compounds of the structure
where R1 and R2 are independently hydrogen, alkyl of one to six carbon atoms, acyl of two to six carbon atoms, or phenacyl; X is —(CH2)1-6; Y is absent or is selected from 1,4-piperazinylene; ureido; N-(lower alkyl)ureido; N′-(lower alkyl)ureido; or N, N′-(di-lower alkyl ureido; and Z is 1-, 2- or 3-pyrrolidinyl; 1-, 2-, or 3-[1-(lower alkyl) pyrrolidinyl]; 1- 2-, 3- or 4-piperidinyl; 1-, 2-, 3- or 4-[1-lower alkyl)piperidinyl]; N,N-dialkyl; 1-azepinyl; 1- or 2-naphthylamino, 4-morpholinyl, dimethyl-4-morpholinyl, 3-azaspiro[5.
Type:
Grant
Filed:
August 4, 1998
Date of Patent:
January 21, 2003
Assignee:
Eli Lilly and Company
Inventors:
Jeffrey Alan Dodge, Andrew Lawrence Glasebrook, Charles Willis Lugar, III
Abstract: Phenylamino benzoic acid, benzamides, and benzyl alcohol derivatives of the formula
where R1, R2, R3, R4, R5, and R6 are hydrogen or substituent groups such as alkyl, and where R7 is hydrogen or an organic radical, and Z is COOR7, tetrazolyl, CONR6R7, or CH2OR7, are potent inhibitors of MEK and, as such, are effective in treating cancer and other proliferative diseases such as inflammation, psoriasis and restenosis, as well as stroke, heart failure, and immunodeficiency disorders.
Type:
Grant
Filed:
August 16, 2001
Date of Patent:
December 10, 2002
Assignee:
Warner-Lambert Company
Inventors:
Stephen Douglas Barrett, Alexander James Bridges, Donna Reynolds Cody, Annette Marian Doherty, David Thomas Dudley, Alan Robert Saltiel, Mel Conrad Schroeder, Haile Tecle
Abstract: The invention concerns compounds of formula (I) wherein A, X, Y, n, R1, R2 and R3 are as defined in claim 1. Said compounds are specifically binding to sigma receptors particularly those of the peripheral nervous system.
Type:
Grant
Filed:
February 27, 2002
Date of Patent:
November 19, 2002
Assignee:
Sanofi-Synthelabo
Inventors:
Robert Boigegrain, Bernard Bourrie, Martine Bourrie, Pierre Casellas, Jean Marc Herbert, Pierre Lair, Dino Nisato, Raymond Paul, Jean Claude Vernieres
Abstract: Controlled cessation of heart beat during coronary bypass surgery and other cardiac surgeries on a beating heart improves surgical technique, and is achieved typically by electrical stimulation of the vagus nerve and administration of a combination of drugs.
Abstract: The present invention provides enantiomers of N-Desmethyl venlafaxine, as well as their use in pharmaceutical compositions and medically useful treatments, particularly including central nervous system uses.