Chalcogen Bonded Directly To Carbon Of The Hetero Ring Of The Quinoline Ring System Patents (Class 514/253.07)
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Publication number: 20090227571Abstract: Provided herein are compounds that bind to androgen receptors and modulate the activity and/or the amount of androgen receptors and to methods for making and using such compounds. Also provided are compositions including such compounds and methods for making and using such compositions.Type: ApplicationFiled: June 30, 2006Publication date: September 10, 2009Inventors: Jon C. Loren, Todd Miller, Bijan Pedram, Charlene V. Rowley, Yixing Shen, Cornelis Arjan Van Oeveren, Lin Zhi
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Publication number: 20090215793Abstract: A method for treating drug-resistant cancer, includes: administering to a patient in need thereof, a compound of formula I, a tautomer of the compound, a salt of the compound, a salt of the tautomer, a mixture thereof, or a pharmaceutical composition comprising the compound, the tautomer, the salt of the compound, the salt of the tautomer, or the mixture, wherein the patient is a cancer patient with drug-resistant cancer, wherein the compound of Formula I is as defined in the application.Type: ApplicationFiled: May 10, 2006Publication date: August 27, 2009Inventors: Glenn C. Michelson, Vivien W. Chan, Carla C. Heise, Marion Wiesmann, Timothy D. Dawes
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Publication number: 20090209551Abstract: The invention relates to an in vitro method for diagnosing essential tremor wherein a mutation of dopamine D3 receptor gene or protein is sought. The invention further relates to the use of a ligand having anti-dopamine D3 receptor activity for treatment of essential tremor.Type: ApplicationFiled: April 28, 2005Publication date: August 20, 2009Inventors: Pierre Sokoloff, Gérard Lucotte, Freddy Jeanneteau, Benoît Funalot
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Patent number: 7566785Abstract: The invention provides novel ?2 adrenergic receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with ?2 adrenergic receptor activity, and processes and intermediates useful for preparing such compounds.Type: GrantFiled: September 8, 2005Date of Patent: July 28, 2009Assignee: Theravance, Inc.Inventors: Martin S. Linsell, John R. Jacobsen, Ningning Xu
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Publication number: 20090186903Abstract: An aripiprazole formulation is provided which includes the antipsychotic agent aripiprazole in the form of an inclusion complex in a ?-cyclodextrin, preferably, sulfobutyl ether ?-cyclodextrin (SBECD), which in the form of an injectable produces reversible generally minimal to mild irritation at the intramuscular injection site. A method for minimizing or reducing irritation caused by aripiprazole at an intramuscular injection site and a method for treating schizophrenia employing the above formulation are also provided.Type: ApplicationFiled: April 2, 2009Publication date: July 23, 2009Inventors: Manoj Nerurkar, Vijay Naringrekar
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PHARMACEUTICALLY ACCEPTABLE SALTS OF QUINOLINONE COMPOUNDS HAVING IMPROVED PHARMACEUTICAL PROPERTIES
Publication number: 20090181979Abstract: A lacate salt of a compound of Formula I or a tautomer of the compound, wherein Formula I has the following structure and R1-R9 and R12-R14 are as defined hereinType: ApplicationFiled: March 4, 2009Publication date: July 16, 2009Inventors: Shaopei Cai, Joyce Chou, Eric Harwood, Timothy Machajewski, David Ryckman, Xiao Shang, Shuguang Zhu, Augustus O. Okhamafe, Marc S. Tesconi -
Publication number: 20090181978Abstract: The present invention relates to a method of treating a patient suffering from a disorder of the central nervous system associated with 5-HT1A receptor subtype, comprising as an active ingredient a carbostyril derivative or a salt thereof represented by the formula (1) wherein the carbon-carbon bond between 3- and 4-positions in the carbostyril skeleton is a single or a double bond.Type: ApplicationFiled: August 29, 2008Publication date: July 16, 2009Inventors: Shaun Jordan, Tetsuro Kikuchi, Katsura Tottori, Tsuyoshi Hirose, Yasufumi Uwahodo
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Publication number: 20090155326Abstract: The present invention is directed generally to a layered polymeric monofilament fiber drug delivery device, where each layer of the device can contain a different polymer, drug, additive, or any combination or mixture thereof. The layered nature of the current monofilament polymeric monofilament device provides the capability to modulate the release of one or more drugs and/or the mechanical properties of the fiber so that drug release and device failure can be separately tuned to provide for the tailored introduction of therapeutically effective drugs or agents to a target tissue. Moreover, the fiber may comprise more than one distinct segments along its length, each segment itself having different combinations and/or numbers of layers thereby providing even greater freedom in the design of the therapeutic delivery device. The invention is also directed to a method of manufacturing such a layered polymeric monofilament fiber drug delivery device, and methods of treatment using such devices.Type: ApplicationFiled: November 12, 2008Publication date: June 18, 2009Inventors: Brendan C. Mack, Mark E. Davis, Kenneth W. Wright
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Publication number: 20090143403Abstract: The present invention relates, in part, to the discovery that a pharmaceutical composition comprising aripiprazole and a carrier administered in a bolus injection resulted in an extended release profile similar to that obtained by the injection of a poly lactide-co-glycolide microsphere formulation containing the active agent. This surprising result suggests that pharmacologically beneficial extended release formulations without the complexities and expense associated with the manufacture microspheres.Type: ApplicationFiled: October 15, 2008Publication date: June 4, 2009Applicant: Alkermes, Inc.Inventor: Josiah Brown
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Publication number: 20090111829Abstract: The present invention provides for new salts of aripiprazole of the general formula (II) formed with dibasic organic acids, camphorsulfonic acid, phosphoric acid, and processes for their preparation. Further objects of the present invention are pharmaceutical compositions containing said new aripiprazole salts. Aripiprazole salts according to present invention can be prepared by the reaction of aripiprazole base and suitable acid compounds in a molar ratio 0.5-3 based on the molar amount of aripiprazole in a suitable organic solvent.Type: ApplicationFiled: July 11, 2006Publication date: April 30, 2009Applicant: Egis Gyógyszergyár Nyilvanosan Mukodo ReszvenytarsasagInventors: Laszlo Pongo, Gyula Simig, Andras Dancso, Gyorgy Morovjan
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Publication number: 20090099176Abstract: Compounds represented by Formula (I) or pharmaceutically acceptable salts thereof, are useful in the prophylactic or therapeutic treatment of diabetes, hyperglycemia, hypercholesterolemia, hyperinsulinemia, hyperlipidemia, hypertension, atherosclerosis or tissue ischemia e.g. myocardial ischemia, and as cardioprotectants.Type: ApplicationFiled: December 2, 2005Publication date: April 16, 2009Inventors: Thomas Martin Krulle, Robert John Rowley, Gerard Hugh Thomas
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Publication number: 20090076480Abstract: The invention relates to compositions comprising silicone elastomers and antimicrobially active substances in homogeneous distribution, a process for their production and their use in medical articles.Type: ApplicationFiled: October 22, 2005Publication date: March 19, 2009Applicant: Bayer Business Services GmbHInventors: Heinz Pudleiner, Ralf Dujardin, Reinhard Albers
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Publication number: 20090075974Abstract: Disclosed is a pharmaceutical composition for prophylaxis and treatment of pancreatitis comprising a 5-HT2A receptor antagonist as an effective component, wherein the binding activity (pKi) of the 5-HT2A receptor antagonist to a 5-HT2A receptor is higher at least by 1.0 than the binding activities to a 5-HT2B receptor and a 5-HT2C receptor. Preferably the binding activity (pKi) of the 5-HT2A receptor antagonist to the 5-HT2A receptor is at least 7.0, and more preferably at least 8.0. The present invention also provides a method of identifying a candidate substance for prophylactic and therapeutic agent for pancreatitis, comprising determining whether a test substance has a 5-HT2A receptor antagonistic activity.Type: ApplicationFiled: April 27, 2006Publication date: March 19, 2009Applicant: UMN Pharma Inc.Inventors: Isamu Yamaguchi, Kentaro Hamada, Yasunari Kashihara
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Publication number: 20090048266Abstract: Methods of utilizing biomarkers to identify patients for treatment or to monitor response to treatment are taught herein. Alterations in levels of gene expression of the biomarkers, particularly in response to FGFR3 inhibition, are measured and identifications or adjustments may be made accordingly.Type: ApplicationFiled: December 7, 2006Publication date: February 19, 2009Applicant: NOVARTS AGInventors: Carla Heise, Esther Masih-Khan, Edward Moler, Michael Rowe, Keith Stewart, Suzanne Trudel
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Publication number: 20090042881Abstract: The present invention provides compounds of formula (I), their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I) wherein n, s, R1, R2, R3, Q, X and Y have defined meanings.Type: ApplicationFiled: November 18, 2004Publication date: February 12, 2009Inventors: Dominique Jean-Pierre Mabire, Jacobus Alphonsus Josephus Van Dun, Maria Victorina Francisca Somers, Walter Boudewijn Leopold Wouters
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Publication number: 20090022823Abstract: The present invention relates, in part, to the discovery that parenterally administered extended release formulations possess an unexpected advantage in treating patients possessing active CYP 3A4. This advantage is particularly beneficial where the individual is concomitantly administering a CYP 3A4 inhibitor or is in risk of doing so. Thus, the invention relates to a method for treating individuals possessing a functional CYP3A4 gene with an active agent metabolized by CYP3A4 comprising parenterally administering the active agent in a first extended release formulation in a first administration and the formulations for use in such methods. The invention further includes a method for preventing adverse drug reactions in individuals possessing a functional CYP3A4 gene with an active agent metabolized by CYP3A4 comprising parenterally administering the active agent in a first extended release formulation in a first administration.Type: ApplicationFiled: September 30, 2008Publication date: January 22, 2009Applicant: Alkermes, Inc.Inventors: Elliot Ehrich, Trevor Mundel
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Publication number: 20090012098Abstract: The present invention relates to a method of treating a patient suffering from a disorder of the central nervous system associated with 5-HT1A receptor subtype, comprising as an active ingredient a carbostyril derivative or a salt thereof represented by the formula (1) wherein the carbon-carbon bond between 3- and 4-positions in the carbostyril skeleton is a single or a double bond.Type: ApplicationFiled: August 29, 2008Publication date: January 8, 2009Inventors: Shaun Jordan, Tetsuro Kikuchi, Katsura Tottori, Tsuyoshi Hirose, Yasufumi Uwahodo
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Publication number: 20080318972Abstract: The present invention relates to a method of treating a patient suffering from a disorder of the central nervous system associated with 5-HT1A receptor subtype, comprising as an active ingredient a carbostyril derivative or a salt thereof represented by the formula (1) wherein the carbon-carbon bond between 3- and 4-positions in the carbostyril skeleton is a single or a double bond.Type: ApplicationFiled: August 29, 2008Publication date: December 25, 2008Inventors: Shaun Jordan, Tetsuro Kikuchi, Katsura Tottori, Tsuyoshi Hirose, Yasufumi Uwahodo
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Patent number: 7468369Abstract: The invention relates to substituted sulfonylpyrrolidines of the formula I and to the physiologically tolerated salts thereof, as well as to their use as medicaments.Type: GrantFiled: June 20, 2007Date of Patent: December 23, 2008Assignee: Sanofi-AventisInventors: Stefanie Keil, Hans-Ludwig Schaefer, Maike Glien, Stefan Guessregen, Wolfgang Wendler, Marion Schneider
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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: 20080293738Abstract: A pharmaceutical formulation, comprising: a compound of formula (I), a tautomer of the compound, a salt of the compound, a salt of the tautomer, or a mixture thereof and at least one ingredient selected from the group consisting of (i) cellulose; (ii) silicon dioxide; (iii) magnesium stearate; and (iv) an ingredient selected from crospovidone, starch, or lactose.Type: ApplicationFiled: November 29, 2006Publication date: November 27, 2008Applicant: Novartis AGInventors: Joyce Chou, Augustus Okhamafe, Patricia Frech, Rampurna Gullapalli
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Patent number: 7452888Abstract: Disclosed are novel quinoline compounds of formula (I), processes for their preparation, compositions containing them and their use in the treatment of CNS disorders.Type: GrantFiled: March 25, 2003Date of Patent: November 18, 2008Assignee: Glaxo Group LimitedInventors: Mahmood Ahmed, Christopher Norbert Johnson, Martin C Jones, Gregor James Macdonald, Stephen Frederick Moss, Mervyn Thompson, Charles Edward Wade, David R Witty
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Publication number: 20080280921Abstract: Morphologically stabilized amorphous aripiprazole and process for preparing the same.Type: ApplicationFiled: June 2, 2008Publication date: November 13, 2008Applicant: Helm AGInventors: Katja Dreyer, Uwe Loeffler, Klaus Glaenzer
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Publication number: 20080275058Abstract: The present invention relates to compounds of N-substituted -1H-quinoline-2,4-diones acting as a 5HT6 receptor antagonist, a preparation method thereof, and a pharmaceutical composition containing the same for treatment of the central nervous system disorders. The compounds of N-substituted-1H-quinoline-2,4-diones according to the present invention have excellent binding affinity for the 5HT6 receptor and excellent selectivity for the 5HT6 receptor over other receptors. Also, the compounds reverse a disruption of PPI by methamphetamine and don't show rotatod deficit in mice.Type: ApplicationFiled: November 23, 2005Publication date: November 6, 2008Applicant: KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGYInventors: Churlmin Seong, Nosang Park, Jinil Choi, Wookyu Park, Jaeyang Kong, Chulmin Park
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Publication number: 20080275040Abstract: This invention relates to novel quinoline compounds having pharmacological activity, to processes for their preparation, to compositions containing them and to their use in the treatment of CNS and other disorders.Type: ApplicationFiled: August 26, 2004Publication date: November 6, 2008Applicant: GLAXO GROUP LIMITEDInventors: Christopher Norbert Johnson, Stephen Frederick Moss, Malcolm M. Tait, David R. Witty
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Patent number: 7439243Abstract: Disclosed are quinoline compounds of formula (I) having pharmacological activity, processes for their preparation, compositions containing them, and methods for the treatment of CNS and other disorders.Type: GrantFiled: September 23, 2004Date of Patent: October 21, 2008Assignee: Glaxo Group LimitedInventors: Christopher Norbert Johnson, Stephen Frederick Moss, David R Witty
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Patent number: 7439244Abstract: Disclosed are quinoline compounds of formula (I) having pharmacological activity, processes for their preparation, compositions containing them, and methods for the treatment of CNS and other disorders.Type: GrantFiled: September 9, 2004Date of Patent: October 21, 2008Assignee: Glaxo Group LimitedInventors: Christopher Norbert Johnson, David R Witty
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Publication number: 20080255116Abstract: Use of a compound for the manufacture of a medicament for the treatment of a bacterial infection provided that the bacterial infection is other than a Mycobacterial infection, said compound being a compound of Formula (Ia) or (Ib) a pharmaceutically acceptable acid or base addition salt thereof, a quaternary amine thereof, a stereochemically isomeric form thereof, a tautomeric form thereof or a N-oxide form thereof, wherein R1 is hydrogen, halo, haloalkyl, cyano, hydroxy, Ar, Het, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkylthioalkyl, Ar-alkyl or di(Ar)alkyl; p is 1, 2 or 3; R2 is hydrogen; alkyl; hydroxy; mercapto; optionally substituted alkyloxy; alkyloxyalkyloxy; alkylthio; mono or di(alkyl)amino wherein alkyl may optionally be substituted; Ar; Het or a radical of formula R3 is alkyl, Ar, Ar-alkyl, Het or Het-alkyl; q is zero, 1, 2, 3 or 4; X is a direct bond or CH2; R4 and R5 each independently are hydrogen, alkyl or benzyl; or R4 and R5 may be taken together including the N to which they areType: ApplicationFiled: July 31, 2006Publication date: October 16, 2008Inventors: Koenraad Jozef Lodewijk Marcel Andries, Anil Koul, Jerome Emile Georges Guillemont, Elisabeth Therese Jeanne Pasquier, David Francis Alain Lancois
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Patent number: 7435737Abstract: Inhibitors of MIF are provided which have utility in the treatment of a variety of disorders, including the treatment of pathological conditions associated with MIF activity. The inhibitors of MIF have the following structures: including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein n, R1, R2, R3, R4, X, Y and Z are as defined herein. Compositions containing an inhibitor of MIF in combination with a pharmaceutically acceptable carrier are also provided, as well as methods for use of the same.Type: GrantFiled: December 7, 2006Date of Patent: October 14, 2008Assignee: Avanir PharmaceutialsInventors: Federico C. A. Gaeta, Andrew Baird, Jerry Anchin, Wenbin Ying, Robert Florkiewicz, Jagadish Sircar, Sunil Kumar K. C.
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Publication number: 20080221121Abstract: A controlled release sterile freeze-dried aripiprazole formulation is provided which is formed of aripiprazole of a desired mean particle size and a vehicle therefor, which upon constitution with water and intramuscular injection releases aripiprazole over a period of at least about one week and up to about eight weeks. A method for preparing the controlled release freeze-dried aripiprazole formulation, and a method for treating schizophrenia employing the above formulation are also provided.Type: ApplicationFiled: August 17, 2007Publication date: September 11, 2008Inventors: Takakuni Matsuda, Toru Nishibayashi
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Publication number: 20080207617Abstract: An objective of the present invention is to provide compounds and pharmaceuticals useful for the treatment of disease where the inhibition of autophosphorylation of FMS-like tyrosine kinase 3(Flt3) is therapeutically effective. The present invention relates to a pharmaceutical composition for use in the treatment or prevention of diseases where the inhibition of autophosphorylation of Flt3 therapeutically or prophylactically effective, which comprises a compound represented by formula (I) or a pharmaceutically acceptable salt or solvate thereof: wherein X represents CH or N; Z represents O or S; R1, R2, and R3 represent H, OH, or optionally substituted alkoxy; R4 represents H; R5, R6, R7, and R8 represent H, Hal, alkyl or the like; and R9 represents, e.g., alkyl substituted by t-butyl or the like.Type: ApplicationFiled: October 29, 2003Publication date: August 28, 2008Applicant: KIRIN BEER KABUSHIKI KAISHAInventors: Atsushi Miwa, Tetsuya Yoshino, Mineo Kurokawa, Hisamaru Hirai, Naoko Hirai
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Publication number: 20080182856Abstract: The present invention provides novel crystalline forms of aripiprazole and aripiprazole hydrochloride, processes for their preparation and pharmaceutical compositions containing them.Type: ApplicationFiled: October 10, 2007Publication date: July 31, 2008Applicant: HETERO DRUGS LIMITEDInventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Rapolu Raji Reddy, Dasari Muralidhara Reddy, Kesireddy Subash Chander Reddy
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Patent number: 7402583Abstract: The invention provides a compound of Formula (Ia), or a pharmaceutically acceptable salt thereof, a process for t he preparation of a compound of Formula (1a) and pharmaceutical compositions of a compound of Formula (1a).Type: GrantFiled: March 14, 2006Date of Patent: July 22, 2008Assignee: AstrZenca ABInventors: Francis Thomas Boyle, Keith Hopkinson Gibson, Kevin Michael Foote
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Publication number: 20080171752Abstract: The present invention relates to a method of treating a patient suffering from a disorder of the central nervous system associated with 5-HT1A receptor subtype, comprising as an active ingredient a carbostyril derivative or a salt thereof represented by the formula (1) wherein the carbon-carbon bond between 3- and 4-positions in the carbostyril skeleton is a single or a double bond.Type: ApplicationFiled: October 31, 2007Publication date: July 17, 2008Inventors: Shaun Jordan, Tetsuro Kikuchi, Katsura Tottori, Tsuyoshi Hirose, Yasufumi Uwahodo
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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: 20080139574Abstract: The present invention relates to novel compounds of general formula (I), their tautomeric forms, their pharmaceutically acceptable salts and pharmaceutical compositions containing them. The present invention also relates to a process for preparing compounds of general formula (I), their tautomeric forms, their pharmaceutically acceptable salts and pharmaceutical compositions containing them.Type: ApplicationFiled: November 29, 2007Publication date: June 12, 2008Inventors: Brijesh Kumar Srivastava, Mukul R. Jain, Pankaj Ramanbhai Patel
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Publication number: 20080139551Abstract: treatment of a variety of disorders, including the treatment of pathological conditions associated with tumor necrosis factor alpha. The inhibitors of tumor necrosis factor alpha have the following structures: including stereoisomers, pharmaceutically acceptable salts, and solvates thereof, wherein substituents are as defined herein. Compositions containing an inhibitor of tumor necrosis factor alpha in combination with a pharmaceutically acceptable carrier are also provided, as well as methods for use of the same.Type: ApplicationFiled: August 21, 2007Publication date: June 12, 2008Applicants: AVANIR PHARMACEUTICALS, NOVARTIS PHARMA GMBHInventors: Jagadish Sircar, Sunil Kumar, Timothy James Davis, Wenbin Ying, Peter Nussbaumer, Andreas Billich
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Publication number: 20080132518Abstract: The present invention relates to novel polymorphic forms of aripiprazole and processes for producing them. It further relates to pharmaceutical compositions comprising the novel forms and to the use of the novel forms in the treatment of schizophrenia.Type: ApplicationFiled: January 27, 2006Publication date: June 5, 2008Applicant: SANDOZ AGInventors: Josef Wieser, Hannes Lengauer, Doris Braun, Ulrich Griesser, Richard Tessadri
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Patent number: 7319097Abstract: The present invention relates to substituted bis-arylsulfonamide and arylsulfonamide compounds of the general formula (I) or the formula (II), which compounds are potentially useful for the prophylaxis and treatment of medical conditions relating to obesity, type II diabetes and/or disorders of the central nervous systemType: GrantFiled: August 30, 2005Date of Patent: January 15, 2008Assignee: Biovitrum ABInventors: Ulf Bremberg, Patrizia Caldirola, Annika J. Jensen, Gary Johansson, Lori Sutin, Andrew Mott, Jan Tejbrant
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Patent number: 7312220Abstract: Inhibitors of MIF are provided which have utility in the treatment of a variety of disorders, including the treatment of pathological conditions associated with MIF activity. The inhibitors of MIF have the following structures: including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein n, R1, R2, R3, R4, X, and Z are as defined herein. Compositions containing an inhibitor of MIF in combination with a pharmaceutically acceptable carrier are also provided, as well as methods for use of the same.Type: GrantFiled: November 3, 2006Date of Patent: December 25, 2007Assignee: Avanir PharmaceuticalsInventors: Jagadish Sircar, Sunil Kumar K C, Wenbin Ying
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Patent number: 7312221Abstract: Inhibitors of MIF are provided which have utility in the treatment of a variety of disorders, including the treatment of pathological conditions associated with MIF activity. The inhibitors of MIF have the following structures: including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein n, R1, R2, R3, R4, X, and Z are as defined herein. Compositions containing an inhibitor of MIF in combination with a pharmaceutically acceptable carrier are also provided, as well as methods for use of the same.Type: GrantFiled: November 3, 2006Date of Patent: December 25, 2007Assignee: Avanir PharmaceuticalsInventors: Jagadish Sircar, Sunil Kumar K C, Wenbin Ying
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Patent number: 7304053Abstract: Substituted heterocyclic compounds for treating multidrug resistance are disclosed. Compositions and methods of use for the substituted heterocyclic compounds are disclosed.Type: GrantFiled: December 19, 2003Date of Patent: December 4, 2007Assignee: H. Lee Moffitt Cancer Center & Research Institute, Inc.Inventors: Charles Raymond Degenhardt, David Joseph Eickhoff
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Patent number: 7276508Abstract: The present invention relates to dopamine D4 ligands having the general formula I wherein R1-R10, W, X, Y1-Y4, and n are as described herein. The compounds of the invention are potent dopamine D4 receptor ligands.Type: GrantFiled: March 3, 2005Date of Patent: October 2, 2007Assignee: H. Lundbeck A/SInventors: Benny Bang-Andersen, Jakob Felding, Jan Kehler, Kim Andersen
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Patent number: 7273870Abstract: An antibacterial formulation suitable for injection into animals containing approximately 2-10% w/v difloxacin HCl, L-arginine base, propylene glycol, ethanol and/or benzyl alcohol, and water. The formulation is a solution having a pH of form 9 to 10. The formulation produces little or no tissue damage or irritation at the injection site.Type: GrantFiled: March 3, 2005Date of Patent: September 25, 2007Assignee: WyethInventor: Henderik W. Frijlink
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Patent number: 7232826Abstract: The present invention provides compounds of Formula I or II that are useful as anti-cancer agents and other diseases that can be treated by inhibiting tyrosine kinase enzymesType: GrantFiled: September 29, 2003Date of Patent: June 19, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Upender Velaparthi, Mark D. Wittman
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Patent number: 7202248Abstract: Inhibitors of MIF are provided which have utility in the treatment of a variety of disorders, including the treatment of pathological conditions associated with MIF activity. The inhibitors of MIF have the following structures: including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein n, R1, R2, R3, R4, X, Y and Z are as defined herein. Compositions containing an inhibitor of MIF in combination with a pharmaceutically acceptable carrier are also provided, as well as methods for use of the same.Type: GrantFiled: January 31, 2006Date of Patent: April 10, 2007Assignee: Avanir PharmaceuticalsInventors: Federico C. A. Gaeta, Andrew Baird, Jerry Anchin, Wenbin Ying, Robert Florkiewicz, Jagadish Sircar, Sunil Kumar K. C.
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Patent number: 7192961Abstract: Inhibitors of MIF are provided which have utility in the treatment of a variety of disorders, including the treatment of pathological conditions associated with MIF activity. The inhibitors of MIF have the following structures: including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein n, R1, R2, R3, R4, X, Y and Z are as defined herein. Compositions containing an inhibitor of MIF in combination with a pharmaceutically acceptable carrier are also provided, as well as methods for use of the same.Type: GrantFiled: May 2, 2006Date of Patent: March 20, 2007Assignee: Avanir PharmaceuticalsInventors: Federico C. A. Gaeta, Andrew Baird, Jerry Anchin, Wenbin Ying, Robert Florkiewicz, Jagadish Sircar, Sunil Kumar K. C.
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Patent number: 7176206Abstract: The invention provides compounds of the general formula: wherein X is selected from the group consisting of oxygen, sulfur and nitrogen-containing groups selected from azine, oxime, hydrazone, aromatic hydrazone, aliphatic hydrazone, semicarbazone, guanidinyl group, and aliphatic or aromatic imines; Y is selected from the group of halogens; R1 and R2 are independently selected from the group consisting of H, lower alkyl group (of C1 up to C6), lower hydroxyalkyl group (of C1 up to C6), lower O-alkyl group (of C1 up to C6), lower alkylcarbonyl group (of C2 up to C6), lower alkyloxycarbonyl group (of C1 up to C6), haloalkylcarbonyl group (of C1 up to C6), or arylsulfonyl group, and their pharmaceutically acceptable salts. The compounds are useful as active ingredients in pharmaceutical compositions. The invention relates to the use of the said compounds as a medicament, in particular as an antibiotic.Type: GrantFiled: March 20, 2002Date of Patent: February 13, 2007Assignee: Dar Al Dawa Development and Investment Co.Inventor: Farouk Hussni Al-Hajjar
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Patent number: 7173036Abstract: Inhibitors of MIF are provided which have utility in the treatment of a variety of disorders, including the treatment of pathological conditions associated with MIF activity. The inhibitors of MIF have the following structures: including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein n, R1, R2, R3, R4, X, and Z are as defined herein. Compositions containing an inhibitor of MIF in combination with a pharmaceutically acceptable carrier are also provided, as well as methods for use of the same.Type: GrantFiled: February 13, 2004Date of Patent: February 6, 2007Assignee: Avanir PharmaceuticalsInventors: Jagadish Sircar, Sunil Kumar K C, Wenbin Ying
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Patent number: 7169788Abstract: The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, inflammatory diseases, and the like in mammals.Type: GrantFiled: October 25, 2002Date of Patent: January 30, 2007Assignee: Merck & Co., Inc.Inventors: Kenneth L. Arrington, Mark E. Fraley, George D. Hartman