Additional Hetero Ring Is Attached Directly Or Indirectly To The Bicyclo Ring System By Nonionic Bonding Patents (Class 514/259.41)
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Publication number: 20080306043Abstract: The invention relates to the use of sabcomeline or a pharmaceutically acceptable salt thereof in monotherapy for the treatment of bipolar disorder or mania or and to adjunctive and simultaneous combination therapies for the treatment of bipolar disorder or mania in which sabcomeline or a pharmaceutically acceptable salt thereof and at least one other mood stabilizing or antimanic agent are administered adjunctively or simultaneously. The invention provides methods of treatment of bipolar disorder or mania utilizing such monotherapy and such adjunctive or simultaneous therapeutic combination therapies, therapeutic combinations for use therein and pharmaceutical compositions comprising them.Type: ApplicationFiled: December 23, 2005Publication date: December 11, 2008Inventors: Carol Routledge, James Joseph Hagan, Stuart Paul Cuffe
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Publication number: 20080287464Abstract: Disclosed are formulations and related methods that comprise a non-polymeric, non-water soluble high viscosity liquid carrier material having a viscosity of at least 5,000 cP at 37° C. that does not crystallize neat under ambient or physiological conditions; a specified linear polymer comprising lactide repeat units; and one or more solvents that have a solvent capacity.Type: ApplicationFiled: May 16, 2008Publication date: November 20, 2008Inventors: Jeremy C. Wright, Felix Theeuwes, John W. Gibson, Keith E. Branham, Stefania Sjobeck
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Publication number: 20080286234Abstract: A method for treating demyelinating diseases such as MS comprised of administering to an individual afflicted with a demyelinating disease a medicament that induces prolactin secretion. Prolactin secretion stimulates oligodendrocyte precurser cells, which remyelinate demyelinated nerve cells. The medicament is administered at a dosage sufficient to induce prolactin secretion resulting in a hyperprolactinemia. Estrogen, estradiol, estriol, histamine H2-receptor antagonists such as cimetidine, and vitamin D can be administered in conjunction with the prolactin-inducing medicament to further promote the remyelination of the nerve cells.Type: ApplicationFiled: May 14, 2008Publication date: November 20, 2008Inventor: Daniel A. Eyink
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Publication number: 20080269257Abstract: The invention relates to use of a pyrimidone derivative represented by formula (I) or a salt thereof as therapeutic agents: Wherein m, n, p, X, Y, R1, R2, R3, R4 R5, are as defined herein. The invention specifically relates to a medicament comprising the said derivative or a salt thereof as an active ingredient which is used for preventive and/or therapeutic treatment of a neurodegenerative disease caused by abnormal activity of GSK3? or GSK3? and cdk5/p25, such as Alzheimer disease.Type: ApplicationFiled: May 14, 2008Publication date: October 30, 2008Applicants: SANOFI-AVENTIS, MITSUBISHI PHARMA CORPORATIONInventors: Thierry Gallet, Patrick Lardenois, Alistair Lochead, Severine Marguerie, Alain Nedelec, Mourad Saady, Franck Slowinski, Philippe Yaiche
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Publication number: 20080269105Abstract: Formulations of drugs and crystalline side chain polymers to provide controlled and/or sustained release drug formulations.Type: ApplicationFiled: December 4, 2007Publication date: October 30, 2008Inventors: David Taft, Steven Bitler, Qiang Zheng, Adam Bell, Stelios Tzannis
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Publication number: 20080268067Abstract: This invention relates to methods of inhibiting a Cav3 calcium channel in a cell using a C2-C10 alkyl alcohol, or mixtures thereof. This invention further relates to methods of treating a thalamocortical dysrhythmia disorder in a mammal and for treating a neurological disorder in a mammal associated with the thalamocortical dysrhythmia using a C2-C10 alkyl alcohol, a lipophilic molecule with a partition coefficient substantially similar to that of a C2-C10 alkyl alcohol, or mixtures thereof, or a pharmaceutical composition comprising the same.Type: ApplicationFiled: March 10, 2008Publication date: October 30, 2008Inventors: Rodolfo R. Llinas, Mutsuyuki Sugimori, Francisco Urbano
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Publication number: 20080248123Abstract: Described are controlled release nanoparticulate formulations comprising a nanoparticulate agent to be administered and a rate-controlling polymer which functions to prolong the release of the agent following administration. The novel compositions release the agent following administration for a time period ranging from about 2 to about 24 hours or longer.Type: ApplicationFiled: March 26, 2008Publication date: October 9, 2008Inventors: Jon Swanson, Rajeev A. Jain, Robert Hontz, John G. Devane, Kenneth Iain Cumming, Maurice Joseph Anthony Clancy, Janet Elizabeth Codd, Gary Liversidge
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Publication number: 20080249082Abstract: The present invention relates to the treatment of compulsive, impulsive and pervasive developmental disorders. More particularly, the methods described herein comprise administration of memantine to an individual suffering from such a disorder in an amount effective to relieve one or more symptoms of said disorder.Type: ApplicationFiled: September 19, 2005Publication date: October 9, 2008Applicant: Mount Sinai School of MedicineInventor: Eric Hollander
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Patent number: 7420056Abstract: Substituted bicyclic imidazo-3-yl-amine compounds are provided, as well as processes for the production thereof and pharmaceutical formulations containing these compounds. The use of these compounds for the production of pharmaceutical formulations and related methods of treatment are also provided.Type: GrantFiled: March 14, 2007Date of Patent: September 2, 2008Assignee: Gruenenthal GmbHInventors: Sven Kuehnert, Stefan Oberboersch, Corinna Sundermann, Michael Haurand, Ruth Jostock, Klaus Schiene, Thomas Tzschentke, Thomas Christoph, Dagmar Kaulartz, Saskia Zemolka
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Patent number: 7414045Abstract: Tetrahydro-4H-pyrido[1,2-a]pyrimidines and related compounds of Formula (A): are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein n is an integer equal to zero, 1, 2 or 3, and R1, R3, R4, R12, R14, R16, R30, R32, R34 and R36 are defined herein. These compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: GrantFiled: December 18, 2003Date of Patent: August 19, 2008Assignee: Istituto di Ricerche di Biologia Molecolare P. Angeletti S.p.A.Inventors: Benedetta Crescenzi, Olaf Kinzel, Ester Muraglia, Federica Orvieto, Giovanna Pescatore, Michael Rowley, Vincenzo Summa
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Publication number: 20080188464Abstract: Methods of treating and or preventing substance abuse/dependence, and alcohol abuse/dependence in particular. Combinations of medications are also disclosed.Type: ApplicationFiled: February 1, 2008Publication date: August 7, 2008Inventors: Alan I. Green, David Chau
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Publication number: 20080166406Abstract: A rapidly disintegrating dosage form containing magnesium carbonate heavy is described, which disintegrates upon contact with moisture. The dosage forms can be either dispersible or orodispersible tablets and can accommodate widely different active principles. The magnesium carbonate heavy is found to be an excellent dispersant under basic and neutral conditions, and gives the tablets a smooth mouth-feel.Type: ApplicationFiled: March 2, 2006Publication date: July 10, 2008Inventor: Torfi E. Kristjansson
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Patent number: 7393853Abstract: The invention relates to use of a substituted-pyrimidone derivative represented by formula (I) or a salt thereof: wherein X, Y, R1, R2, R3, R4, R5, n, p and q are as described herein for treating a variety of disease states. More specifically, the invention relates to a medicament comprising the said derivative or a salt thereof as an active ingredient which is used for preventive and/or therapeutic treatment of a disease caused by abnormal activity of GSK3?, such as Pick's disease.Type: GrantFiled: April 4, 2007Date of Patent: July 1, 2008Assignees: Sanofi Aventis, Mitsubishi Pharma Corp.Inventors: Alistair Lochead, Mourad Saady, Franck Slowinski, Philippe Yaiche
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Publication number: 20080146541Abstract: A method for treating or preventing symptoms of hormonal variation includes administering an effective amount of a receptor antagonist to a subject having one or more symptoms of hormonal variations, wherein the receptor antagonist binds to at least one selected from the group consisting of a serotonin type 2A (5-HT2A) and a dopamine type 2 (D2) receptors.Type: ApplicationFiled: December 13, 2006Publication date: June 19, 2008Inventor: Hung-Ming Wu
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Publication number: 20080131513Abstract: Provided, among other things, are compositions and methods for making sustained-release microspheres, as well as a microsphere delivery system for the sustained release of an active agent. The microsphere delivery system comprises a homogeneous mixture of biodegradable polymer, active agent, and a so-called release-modifying agent (including a pH-stabilizing agent), and provides protected and sustained release of active agents from the microsphere delivery system. According to the invention, the microspheres preferably are produced by an oil-in-water emulsion method that involves the production of a homogeneous oil phase prepared by mixing active agent and a release-modifying agent, such as arginine, with biodegradable polymer, each dissolved in organic solvent.Type: ApplicationFiled: April 29, 2005Publication date: June 5, 2008Inventors: Byung Ho Woo, Sumeet H. Dagar, Kang Yong Yang
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Publication number: 20080108602Abstract: O-(3-piperidino-2-hydroxypropyl)-nicotinic amidoxime or a pharmaceutically suitable acid addition salt thereof (BGP-15) can be used for the prevention or reduction of weight gain or obesity in a patient treated with an antipsychotic drug or an antidepressant drug or an antiepileptic drug.Type: ApplicationFiled: March 19, 2007Publication date: May 8, 2008Inventors: Peter Literati Nagy, Jesse Roth, Zoltan Szilvassy, Kalman Tory, Mike Brownstein, Kalman Takacs, Laszlo Vigh, Jozsef Mandi, Balazs Sumegi, Sandor Bernath, Attila Kolonics, Gabor Balogh, Janos Egri
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Publication number: 20080096870Abstract: The subject invention pertains to methods of treating mental illnesses or conditions characterized by a decreased function of NMDA receptors and/or excessively enhanced glutamate release and activity of non-NMDA receptors (AMPA and/or kainate). Specifically disclosed are methods utilizing BrPhe, or isomers of analogs thereof, for treating or preventing mental illness or conditions such as schizophrenia.Type: ApplicationFiled: July 18, 2005Publication date: April 24, 2008Inventors: Anatoly E. Martynyuk, Donn M. Dennis, Nikolaus Gravenstein, Alexander V. Glushakov, Viktor Yarotskyy, Colin Sumners, Christoph Seubert
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Publication number: 20080081806Abstract: A new treatment methodology and pharmacological composition for the treatment and remission of Parkinson's Disease and other neurological diseases are provided. The medication and treatment are based on the use of a combination of a phosphodiesterase inhibitor medication, commonly used to treat male erectile dysfunction, and a high-dose of serotonergic synaptic reuptake inhibitor medication, commonly used to treat depression, anxiety disorders, obsessive compulsive disorder and various panic phobias. The treatment regime is based upon the discovery that the primary cause of PD and various other related neurological conditions is dysfunction in the serotonergic pathways involving the brainstem, nucleus of Raphe, and various projecting serotonergic fibers.Type: ApplicationFiled: October 2, 2006Publication date: April 3, 2008Inventor: Jerry M. Held
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Patent number: 7326711Abstract: Pyridin[1,2-a]pyrimidinyl compounds, pharmaceutically acceptable salts, and prodrugs thereof; compositions that include a pharmaceutically acceptable carrier and one or more of the pyridino[1,2-a]pyrimidinyl compounds, either alone or in combination with at least one additional therapeutic agent. Methods of using the pyridino[1,2-a]pyrimidinyl compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of proliferative diseases.Type: GrantFiled: June 17, 2004Date of Patent: February 5, 2008Assignee: Chiron CorporationInventors: Weibo Wang, Ryan N. Constantine, Liana Marie Lagniton, Sabina Pecchi, Matthew T. Burger, Manoj C. Desai
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Publication number: 20080026081Abstract: The present invention relates to methods of treatment using the compound (+)-isopropyl 2-methoxyethyl 4-(2-chloro-3-cyano-phenyl)-1,4-dihydro-2,6-dimethyl-pyridine-3,5-dicarboxylate, as a sole active agent or in combination with other pharmacological agents.Type: ApplicationFiled: November 19, 2004Publication date: January 31, 2008Inventors: Axel Unterbeck, Michael De Vivo, Gregory M. Rose
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Patent number: 7256195Abstract: The present invention is directed to the novel forms of risperidone, designated Form A, Form B and Form E. Methods for their preparation are also disclosed. The present invention also relates to processes for making risperidone. Pharmaceutical compositions containing the new forms of risperidone and methods of using them are also disclosed.Type: GrantFiled: September 23, 2003Date of Patent: August 14, 2007Assignee: Teva Pharmaceutical Industries Ltd.Inventors: Barnaba Krochmal, Dov Diller, Ben-Zion Dolitzky, Judith Aronhime
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Patent number: 7247638Abstract: The invention relates to substituted-pyrimidone derivatives represented by formula (I) or a salt thereof: wherein X, Y, R1, R2, R3, R4, R5, n, p and q are as defined herein. The invention relates also to a medicament comprising the said derivative or a salt thereof as an active ingredient which is used for preventive and/or therapeutic treatment of a neurodegenerative disease caused by abnormal activity of GSK3?, such as Alzheimer's disease.Type: GrantFiled: September 13, 2005Date of Patent: July 24, 2007Assignees: Sanofi-Aventis, Mitsubishi Pharma CorporationInventors: Alistair Lochead, Mourad Saady, Franck Slowinski, Philippe Yaiche
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Patent number: 7232827Abstract: The invention relates to a pyrimidone derivative represented by formula (I) or a salt thereof wherein: (I) X represents two hydrogen atoms, a sulphur atom, an oxygen atom or a C1-2 alkyl group and a hydrogen atom; Y represents a bond, an ethenylene group, an ethynylene group or a methylene group optionally substituted; R1 represents a 2, 3 or 4-pyridine ring or a 2, 4 or 5-pyrimidine ring optionally substituted; R2 represents a heterocyclic bicyclic rings, having 1–4 heteroatoms selected from an oxygen atom, a sulfur atom and a nitrogen atom and having 5–9 carbon atoms, of formula (II) R3 represents a hydrogen atom, a C1-6 alkyl group, a hydroxy group, a C1-4 alkoxy group or a halogen atom; R4 represents a hydrogen atom, a C1-6 alkyl group, a C1-4 alkoxy group or a halogen atom.Type: GrantFiled: February 26, 2003Date of Patent: June 19, 2007Assignees: Sanofi-Aventis, Mitsubishi Pharma CorporationInventors: Alistair Lochead, Alain Nedelec, Mourad Saady, Philippe Yaiche
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Patent number: 7230103Abstract: Substituted 3,4-dihydropyrido[1,2-a]pyrimidines of formula I and processes for the production thereof Also disclosed are substance libraries and pharmaceutical compositions containing the compound, and methods of treatment for pain, urinary incontinence, pruritus, tinnitus and/or diarrhoea using the pharmaceutical composition.Type: GrantFiled: April 11, 2003Date of Patent: June 12, 2007Assignee: Gruenenthal GmbHInventors: Matthias Gerlach, Corinna Maul, Utz-Peter Jagusch
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Patent number: 7217715Abstract: The invention relates to a substituted-pyrimidone derivative represented by formula (I) or a salt thereof: wherein X, Y, R1, R2, R3, R4, R5, n, p and q are as described herein. The invention relates also to a medicament comprising the said derivative or a salt thereof as an active ingredient which is used for preventive and/or therapeutic treatment of a neurodegenerative disease caused by abnormal activity of GSK3?, such as Alzheimer disease.Type: GrantFiled: September 13, 2005Date of Patent: May 15, 2007Assignees: Sanofi-Aventis, Mitsubishi Pharma CorporationInventors: Alistair Lochead, Mourad Saady, Franck Slowinski, Philippe Yaiche
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Patent number: 7214682Abstract: The invention relates to a pyrimidone derivative represented by formula (I) or a salt thereof wherein X represents two hydrogen atoms, a sulfur atom, an oxygen atom or a C1-2 alkyl group and a hydrogen atom; Y represents a bond, an ethenylene group, an ethynylene group an oxygen atom, a sulfur atom, a sulfonyl group, a sulfoxide group, a carbonyl group, a hydroxyiminomethylene group, a dioxolan group, a nitrogen atom being optionally substituted; or a methylene group optionally substituted; or a methylene group optionally substituted; R1 represents a 2, 3 or 4-pyridine ring optionally substituted; R2 may represent a C1-6 alkyl group optionally; a C3-6 cycloalkyl group, a C1-4 alkythio group, a C1-4 alkoxy group, a C1-2 perhalogenated alkyl group, a C1-3 halogenated alkyl group, a phenylthio group, a benzyl group, a benzene ring, an indan ring, a 5,6,7,8-tetrahydronaphthalene ring, a naphthalene ring, a pyridine ring, a pyrrole ring, a thiophene ring, a furan ring or an imidazole ring; R3 and R4 represent, eacType: GrantFiled: September 19, 2002Date of Patent: May 8, 2007Assignees: Sanofi-aventis, Mitsubishi Pharma CorporationInventors: Thierry Gallet, Patrick Lardenois, Alistair Lochead, Séverine Marguerie, Alain Nedelec, Mourad Saady, Franck Slowinski, Philippe Yaiche
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Patent number: 7118763Abstract: Sustained-release microparticle composition. The microparticle composition can be formulated to provide multi-phasic release. In one aspect, the composition includes microparticles having more than one rate of release. In another aspect, the composition includes microparticles that exhibit diffusional release and microparticles that exhibit biodegradation release.Type: GrantFiled: August 18, 2004Date of Patent: October 10, 2006Assignees: Alkermes Controlled Therapeutics, Inc. II, Janssen PharmaceuticaInventors: Jean Mesens, Michael E. Rickey, Thomas J. Atkins
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Patent number: 6974819Abstract: Imidazo[1,2-?]pyrimidinones and pyrimido[1,2-?]pyrimidinones useful for preventive and/or therapeutic treatment of neurodegenerative diseases, such as Alzheimer's disease, caused by abnormal GSK3? activity.Type: GrantFiled: August 31, 2001Date of Patent: December 13, 2005Assignees: Sanofi-Aventis, Mitsubishi Pharma CorporationInventors: Antonio Almario Garcia, Thierry Gallet, Adrien Tak Li, Alistair Lochead, Séverine Marguerie, Alain Nedelec, Mourad Saady, Philippe Yaiche
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Patent number: 6964962Abstract: A composition comprising: (a) a pharmaceutically effective amount of reboxetine; and selected from the group consisting of clozapine, olanzapine, risperidone and mixtures thereof (b) a pharmaceutically effective amount of one or more neuroleptic agents or a pharmaceutically effective salt thereof is provided.Type: GrantFiled: December 28, 2001Date of Patent: November 15, 2005Assignee: Pharmacia & Upjohn CompanyInventors: Erik Ho Fong Wong, Christopher C. Gallen, Torgny Svensson
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Patent number: 6887870Abstract: Heterocyclic are provided which are sodium/proton exchange (NHE) inhibitors which have the structure wherein n is 1 to 5; X is N or C—R5 wherein R5 is H, halo, alkenyl, alkynyl, alkoxy, alkyl, aryl or heteroaryl; Z is a heteroaryl gorup, R1, R2, R3 and R4 are as defined herein, and where X is N. R1 is preferably aryl or heteroaryl, and are useful as antianginal and cardioprotective agents. In addition, a method is provided for preventing or treating angina pectoris, cardiac dysfunction, myocardial necrosis, and arrhythmia employing the above heterocyclic derivatives.Type: GrantFiled: September 25, 2000Date of Patent: May 3, 2005Assignee: Bristol-Myers Squibb CompanyInventors: Saleem Ahmad, Shung C. Wu, Steven V. O'Neil, Khehyong Ngu, Karnail S. Atwal, David S. Weinstein
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Patent number: 6875771Abstract: Novel pyridopyrimidine derivatives which have a binding affinity for the human 5-HT6 receptor and, therefore, are useful in treating disorders responsive to antagonism of the 5-HT6 receptor such as psychosis, schizophrenia, manic depression, depression, neurological disorder, memory disorder, Parkinson's disease, amyotrophic lateral sclerosis, Alzheimer's disease and Huntington's chorea.Type: GrantFiled: July 15, 2003Date of Patent: April 5, 2005Assignee: Bristol-Myers Squibb CompanyInventors: Yong-Jin Wu, Shuanghua Hu, Paul M. Scola, Yazhong Huang, Katharine A. Grant-Young
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Patent number: 6864259Abstract: The present invention provides compounds of Formula (I): wherein R1-R6 and K have any of the values defined in the specification, and pharmaceutically acceptable salt thereof, that are useful as antibacterial agents. Also disclosed are pharmaceutical compositions comprising one or more compounds of Formula I, processes for preparing compounds of Formula I, and intermediates useful for preparing compounds of Formula I.Type: GrantFiled: May 29, 2002Date of Patent: March 8, 2005Assignee: Warner-Lambert CompanyInventors: Edmund Lee Ellsworth, Kim Marie Hutchings, Dai Nguyen, Rajeshwar Singh, Howard Daniel Hollis Showalter
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Publication number: 20040266791Abstract: Salts of risperidone are provided including solid state salts and water soluble salts. The salts are useful in making pharmaceutical compositions.Type: ApplicationFiled: April 16, 2004Publication date: December 30, 2004Inventors: Reinerus G. Gieling, Desiree Laurant
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Publication number: 20040266790Abstract: Monohydrochloride salts of risperidone have been found to have useful properties. A preferred form is crystalline risperidone monohydrochloride hemipentahydrate. The monohydrochloride salts can be used in pharmaceutical compositions and methods such as for use in treating psychotic disorders.Type: ApplicationFiled: April 16, 2004Publication date: December 30, 2004Inventors: Jiri Bartl, Reinerus G. Gieling
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Publication number: 20040266792Abstract: Methods and compositions utilizing compounds represented by Formula III, 1Type: ApplicationFiled: July 13, 2004Publication date: December 30, 2004Applicant: Sepracor Inc.Inventor: William E. Yelle
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Publication number: 20040209898Abstract: The present invention is directed to a process for the preparation of the EPCRS form of Risperidone. The present invention also embodies a process for the preparation of EPCRS crystalline form of Risperidone which comprises, heating the Risperidone in an organic solvent(s) followed by subsequent cooling and isolation to get desired polymorph of Risperidone (Formula I).Type: ApplicationFiled: January 21, 2004Publication date: October 21, 2004Applicants: DR. REDDY'S LABORATORIES LIMITED, DR. REDDY'S LABORATORIES, INC.Inventors: Reguri Buchi Reddy, Chakka Ramesh, Tamma Ranga Reddy, Kandirelli Venkata Kiran Kumar
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Publication number: 20040204401Abstract: The present invention relates to a new method of treatment for persons meeting diagnoses for major depressive disorder, or other unipolar (non-bipolar, non-psychotic and non-treatment resistant) depression. The method comprises administering a combination of two categories of drugs, antipsychotics or dopamine system stabilizers, in combination with a newer antidepressant such as a selective serotonin reuptake inhibitor, as initial treatment or as soon as possible. The method targets the prevention of suicide, and provides other benefits including preventing disease progression development of tolerance toward the antidepressants. Another aspect of the invention relates to using the method for alleviating cognitive distortion and related functional impairment or health risks, and/or using the method for smoking cessation or nicotine withdrawal.Type: ApplicationFiled: July 25, 2003Publication date: October 14, 2004Inventor: Peter Migaly
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Patent number: 6800639Abstract: In accordance with the present invention there is provided a pharmaceutical combination useful for the treatment of cancer comprising at least one active compound of formula (I): and at least one further therapeutic agent chosen from a nucleoside analogue and/or a chemotherapeutic agents; and, a method of treating a patient having cancer comprising at least one active compound of formula (I), as defined above, and at least one further therapeutic agent chosen from a nucleoside analogue and/or a chemotherapeutic agents.Type: GrantFiled: March 25, 2002Date of Patent: October 5, 2004Assignee: Shire BioChem Inc.Inventors: Francis Giles, Hagpop Kantarjian, Jacques Jolivet
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Publication number: 20040167125Abstract: The present invention relates to the combination of cyamemazine and an atypical neuroleptic, or a pharmaceutically acceptable salt thereof, and to the use thereof in the treatment of schizophrenia, and in particular of acute episodes of schizophrenia.Type: ApplicationFiled: February 20, 2004Publication date: August 26, 2004Applicant: Aventis Pharma S.A.Inventors: Michel Dib, Cyrille Leperlier
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Publication number: 20040152711Abstract: The present invention is related to crystalline forms of ziprasidone and its hydrochloride salt and an amorphous form of ziprasidone hydrochloride and the process for the preparation thereof. The crystalline forms and amorphous form of the invention are suitable for pharmaceutical purposes in the treatment of psychosis. The processes of the invention are simple, non-hazardous and commercially suitable.Type: ApplicationFiled: December 4, 2003Publication date: August 5, 2004Applicants: DR. REDDY'S LABORATORIES LIMITED, DR. REDDY'S LABORATORIES, INC.Inventors: Manne Satyanarayana Reddy, Thirumalai Rajan Srinivasan, Venka Bhaskara Rao Uppala, Mummadi Venkatesh, Akundi Surya Prabhakar
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Publication number: 20040147532Abstract: A liquid phase conjugate formed of a bioactive agent such as a drug compound, e.g. ziprasidone, and a liquid polymer of requisite functionality is disclosed.Type: ApplicationFiled: October 24, 2003Publication date: July 29, 2004Applicant: Pfizer IncInventors: Shalaby W. Shalaby, Jaymin C. Shah
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Publication number: 20040142039Abstract: Aqueous solubility of drugs including insoluble or poorly soluble drugs such as ziprasidone is improved using a functional polymer to form an ionic conjugate with said drug.Type: ApplicationFiled: October 24, 2003Publication date: July 22, 2004Applicant: Pfizer IncInventors: Shalaby W. Shalaby, Jaymin C. Shah, Joel T. Corbett
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Publication number: 20040138237Abstract: An injectable depot formulation that is viscous, or becomes viscous in situ, comprising a solubilized aryl-heterocyclic pharmaceutical compound, such as ziprasidone, is provided.Type: ApplicationFiled: October 21, 2003Publication date: July 15, 2004Applicant: Pfizer IncInventor: Jaymin C. Shah
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Patent number: 6762181Abstract: This invention provides a quinolone derivative having potent antibacterial activity against various bacteria including drug-resistant strains which is a compound of the following formula wherein R1 is an optionally substituted aromatic group, a salt of the same or a hydrate of both.Type: GrantFiled: September 7, 2001Date of Patent: July 13, 2004Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Makoto Takemura, Hisashi Takahashi, Katsuhiro Kawakami, Toshiyuki Takeda, Rie Miyauchi
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Publication number: 20040127489Abstract: The present invention provides novel antipsychotic therapies and compositions useful therein and provides methods for identifying new candidate molecules for the treatment of psychosis based on the proportional binding affinities for &agr;2 adrenergic and D2 dopamine receptors.Type: ApplicationFiled: July 28, 2003Publication date: July 1, 2004Inventors: David Pickar, Torgny Svensson, Marie-Louise Wadenberg
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Patent number: 6747032Abstract: Compound of formula (I): wherein: R1, R2, R3 and R4, which may be the same or different, each represent a hydrogen atom, a halogen atom or a group selected from alkyl, alkoxy, polyhaloalkyl, hydroxy, cyano, nitro and amino, or R1 with R2, R2 with R3, or R3 with R4, together with the carbon atoms carrying them, form an optionally substituted benzene ring or an optionally substituted heteroaromatic ring, X represents an oxygen atom or a methylene group, A represents an alkylene chain, represents an optionally substituted, unsaturated, nitrogen-containing heterocycle and R5 represents an alkyl group, its enantiomers and diastereoisomers, and addition salts thereof with a pharmaceutically acceptable acid, a medicinal products containing the same are useful as a double &agr;2/5-HT2c antagonist.Type: GrantFiled: April 18, 2002Date of Patent: June 8, 2004Assignee: Les Laboratoires ServierInventors: Gilbert Lavielle, Thierry Dubuffet, Olivier Muller, Mark Millan, Anne Dekeyne, Mauricette Brocco
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Publication number: 20040097523Abstract: The formation of risperidone is enhanced by the use of enriched Z-isomer oxime intermediate(s) of formula (3) or (7).Type: ApplicationFiled: November 13, 2003Publication date: May 20, 2004Inventors: Pavel Slanina, Jiri Bartl
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Publication number: 20040092534Abstract: Dosage forms and methods for providing a substantially ascending rate of release of paliperidone are provided. The sustained release dosage forms provide therapeutically effective average steady-state plasma paliperidone concentrations when administered once per day. This once-a-day dosing regimen results in only one peak plasma paliperidone concentration occurrence in each 24 hour period. In addition, the peak plasma paliperidone concentration occurs at a later time following dose administration and exhibits a lesser magnitude than the peak plasma paliperidone concentration that occurs following administration of paliperidone in an immediate-release dosage form.Type: ApplicationFiled: July 28, 2003Publication date: May 13, 2004Inventors: Nyomi V. Yam, Iran Reyes, Nipun Davar, Atul D. Ayer, Julie Lee
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Publication number: 20040092508Abstract: This invention relates to use of the combined action of a nicotinic acetylcholine receptor agonist and a monoaminergic substance for the treatment of affective disorders, as well as to pharmaceutical compositions comprising these substances and chemical substances for use according to the invention.Type: ApplicationFiled: March 17, 2003Publication date: May 13, 2004Inventors: Gunnar M Olsen, Dan Peters, Elsebet Nielsen
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Publication number: 20040038975Abstract: Compounds of the following formula: 1Type: ApplicationFiled: June 16, 2003Publication date: February 26, 2004Applicant: The Procter & Gamble CompanyInventors: Benoit Ledoussal, Xiufeng Eric Hu, Ji-In Kim Almstead, Jeffrey Lyle Gray