Tricyclo Ring System Having The Seven-membered Hetero Ring As One Of The Cyclos Patents (Class 514/220)
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Publication number: 20090215751Abstract: The invention relates to methods of and treatments for using pharmaceutical compositions from a class of compounds that directly or indirectly selectively modulates GABAA chloride channel activity to treat alcohol and/or stimulant substance abuse. The present invention also relates to methods of, and protocols for, relieving symptoms associated with alcohol and/or stimulant substance abuse in a comprehensive treatment plan. More specifically, the present invention relates to the use of a selective chloride channel modulator, such as flumazenil, to treat alcohol and/or psychostimulant dependency, the withdrawal symptoms associated therewith, and the cravings associated therewith.Type: ApplicationFiled: March 13, 2009Publication date: August 27, 2009Applicant: Hythiam, Inc.Inventor: Juan Jose Legarda Ibanez
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Publication number: 20090209525Abstract: A method developed to identify receptor modulators, involving providing a mutant receptor, wherein said mutant receptor has a mutation that alters the activity of said mutant receptor compared to a wild type receptor; contacting said mutant receptor with a candidate compound; and determining whether said candidate compound modulates the activity of said mutant receptor.Type: ApplicationFiled: December 19, 2008Publication date: August 20, 2009Inventors: Tracy A Spalding, Mark R. Brann, Robert E. Davis, Ethan S. Burstein
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Publication number: 20090209480Abstract: The present invention concerns compositions, methods and/or apparatus of central administration of various CNS-active agents. In particular embodiments, intrathecal administration is advantageous for decreasing the systemic concentrations of CNS agent, thereby decreasing side effect toxicity, while allowing more effective delivery of the agent to the site of action, simultaneously decreasing the dosage delivered to the subject. In particular embodiments, ICV delivery may be of use for patients who have previously proven to be refractory to systemic administration of CNS agents, in some cases due to systemic side effects, or for those patients whose symptoms are of sufficient severity to warrant more aggressive therapeutic intervention. ICV administration allows not only lower systemic concentration but also higher therapeutically effective concentration within the CNS.Type: ApplicationFiled: January 17, 2007Publication date: August 20, 2009Applicant: The Regents of the University of ColoradoInventors: Daniel J. Abrams, Raymond Bunch, Tom Anchordoquy, Karen E. Stevens
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Publication number: 20090203720Abstract: Cell growth is inhibited and/or cell death is induced in a cell by administering an RXR agonist and an inhibitor of casein kinase 1?. A cell or a tissue can be screened for enhanced susceptibility to cell death or interference with cell growth. Conditions characterized by uncontrolled cell growth or proliferation, such as a cancer, can be treated with inhibitors of casein kinase 1?.Type: ApplicationFiled: May 12, 2006Publication date: August 13, 2009Inventors: Yi Zhao, Roshantha A. Chandraratna
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Publication number: 20090202604Abstract: Effective treatments of pain for extended periods of time are provided. The treatments include the administration of one or more drug depots intraspinally wherein the drug depots include an effective amount of a benzodiazepine, such as midazolam, formulated within a polyorthoester. By administration of one or more drug depots, one can relieve pain caused by diverse sources, including but not limited to chronic pelvic pain syndromes, spinal disc herniation (i.e. sciatica), spondilothesis, stenosis, discongenic back pain and joint pain, as well as pain that is incidental to surgery. In some embodiments, the relief can be for at least twenty-five days, at least fifty days, at least one hundred days or at least one hundred and thirty-five days.Type: ApplicationFiled: April 17, 2009Publication date: August 13, 2009Applicant: Medtronic, Inc.Inventors: Christopher M. Hobot, Michael E. Benz, Keith R. Hildebrand, Bryant J. Pudil
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Publication number: 20090196824Abstract: In general, the invention provides methods and compositions for treating sequela of weight gain or pain insensitivity, e.g., in a subject suffering from a psychiatric disorder, such as schizophrenia. The combinations employed in the invention include a second generation antipsychotic agent and an opioid receptor antagonist.Type: ApplicationFiled: December 7, 2006Publication date: August 6, 2009Inventors: Igor Elman, David Borsook, Jan Wasley
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Publication number: 20090198145Abstract: Compositions, kits, methods, and systems to induce, maintain, monitor, and interpret a continuous, un-fragmented REM sleep state in humans, generate dreams, recover sleep, create brain neuronal plasticity and activate the brain for cognition enhancement and mood stabilization are described. If potentially combined with other medications, a platform is provided to develop new research and therapies in many fields treating the human brain. The procedure reliably and quickly generates a Continuous REM Sleep cycle of pre-determined time or indefinite duration depending on therapeutic goals, allowing the patient to experience a qualitatively superior dream sleep in a shortened period of time compared to a natural sleep cycle. Profuse positive (pleasant) dreams are produced as well. REM sleep, dreams and sleep recovery can be reliably generated, and various sleep, psychological and neurological illnesses and disorders can be treated or prevented either solely by this method or in combination with additional agents.Type: ApplicationFiled: December 8, 2008Publication date: August 6, 2009Inventor: Harrison CHOW
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Patent number: 7569561Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R6, X and Y are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or anomalous cell proliferation, as well as the use thereof for preparing a pharmaceutical composition with the above-mentioned properties.Type: GrantFiled: February 16, 2007Date of Patent: August 4, 2009Assignee: Boehringer Ingelheim International GmbHInventors: Heinz Stadtmueller, Anke Baum, Guido Boehmelt, Harald Engelhardt, Jens Juergen Quant, Flavio Solca, Martin Steegmaier, Stephan Karl Zahn
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Patent number: 7566707Abstract: The present invention relates to substituted imidazo-pyridinones and imidazo-pyridazinones of general formula wherein Y and R1 to R4 are defined as in claim 1, the tautomers, enantiomers, diastereomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).Type: GrantFiled: June 10, 2004Date of Patent: July 28, 2009Assignee: Boehringer Ingelheim International GmbHInventors: Matthias Eckhardt, Norbert Hauel, Elke Langkopf, Frank Himmelsbach, Iris Kauffmann-Hefner, Mohammad Tadayyon, Michael Mark
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Publication number: 20090186878Abstract: The present invention relates to crystalline forms of ECO-4601 and the processes for providing them. The invention further relates to pharmaceutical compositions comprising the crystalline forms and to methods of use of the crystalline forms as pharmaceuticals.Type: ApplicationFiled: January 26, 2007Publication date: July 23, 2009Applicant: THALLION PHARMACEUTICALS INC.Inventors: Patrick Morris, Faustinus Yeboah, James McAlpine, Maxime Ranger, Emmanuelle Roux, Michael Harvey
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Publication number: 20090186879Abstract: There is provided a compound of the formula (I?): wherein x is a nitrogen or CRx, Rx is a hydrogen, etc., R1 is an optionally substituted hydrocarbon group, etc., R2 is an optionally substituted hydrocarbon group, etc., ring A is 5- to 8-membered heterocyclic ring, etc., and each of Y1, Y2 and Y3 is an optionally substituted carbon or a nitrogen, etc.; or a salt thereof or a prodrug thereof, which have CRF receptor antagonistic activity and use thereof.Type: ApplicationFiled: January 21, 2009Publication date: July 23, 2009Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Kazuyoshi Aso, Katsumi Kobayashi, Takafumi Takai, Takuto Kojima, Kazuyuki Tokumaru, Michiyo Mochizuki, Yasutaka Hoashi
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Publication number: 20090186099Abstract: Buccal aerosol sprays or capsules using polar and non-polar solvent have now been developed which provide biologically active compounds for rapid absorption through the oral mucosa, resulting in fast onset of effect. The buccal polar compositions of the invention comprise formulation I: aqueous polar solvent, active compound, and optional flavoring agent; formulation II: aqueous polar solvent, active compound, optionally flavoring agent, and propellant; formulation III: non-polar solvent, active compound, and optional flavoring agent; and formulation IV: non-polar solvent, active compound, optional flavoring agent, and propellant.Type: ApplicationFiled: January 9, 2009Publication date: July 23, 2009Inventor: Harry A. Dugger, III
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Patent number: 7560454Abstract: This invention provides novel compounds according to general formula (1) wherein A is a bicyclic or tricyclic azepine derivative, V1 and V2 are both H, OMe or F, or one of V1 and V2 is Br, Cl, F, OH, OMe, OBn, OPh, O-acyl, N3, NH2, NHBn or NH-acyl and the other is H, or V1 and V2 together are ?O, —O(CH2)pO— or —S(CH2)pS—; W1 is either O or S; X1 and X2 are both H, or together are ?O or ?S; Y is OR5 or NR6R7; R1, R2, R3 and R4 are independently selected from H, lower alkyl, lower alkyloxy, F, Cl and Br; R5 is selected from H and lower alkyl; R6 and R7 are independently selected from H and lower alkyl, or together are —(CH2)n—; n=3, 4, 5, 6; and p is 2 or 3. The compounds are agonists at the vasopressin V2 receptor and are useful as antidiuretics and procoagulants. The invention further comprises pharmaceutical compositions incorporating these vasopressin agonists, which compositions are particularly useful in the treatment of central diabetes insipidus, nocturnal enuresis and nocturia.Type: GrantFiled: March 9, 2006Date of Patent: July 14, 2009Assignee: Vantia LimitedInventors: Doreen Mary Ashworth, Gary Robert William Pitt, Peter Hudson, Christopher Martyn Yea, Richard Jeremy Franklin
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Patent number: 7557099Abstract: Compounds and a method of synthesis of compounds of formula (Ia) or (Ib): and salts, solvates, and chemically protected forms thereof, wherein the dotted lines indicate the optional presence of a double bond between C1 and C2 or C2 and C3; R2 and R3 are independently selected from —H, ?O, ?CH2, —CN, —R, OR, halo, ?CH—R, O—SO2—R, CO2R and COR; R10 is a carbamate-based nitrogen protecting group; and R11 is an oxygen protecting group.Type: GrantFiled: March 1, 2005Date of Patent: July 7, 2009Assignee: Spirogen LimitedInventors: Philip Wilson Howard, Gyoung-Dong Kang
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Publication number: 20090170837Abstract: The invention relates to the discovery that the dibenzodiazepinone analogues have growth inhibiting activities on tumorigenic cells that are driven by expression of RAS or mutated RAS. Thus the invention includes methods for inhibiting the activity of RAS using dibenzodiazepinone analogues; methods for inhibiting the growth of a RAS driven cancer cell using dibenzodiazepinone analogues; methods for inhibiting the growth of a RAS driven cancer using dibenzodiazepinone analogues; and methods for treating a subject having a RAS driven cancer using dibenzodiazepinone analogues.Type: ApplicationFiled: October 24, 2008Publication date: July 2, 2009Applicant: THALLION PHARMACEUTICALS INC.Inventors: Henriette GOURDEAU, Pierre FALARDEAU, Nadia BOUFAIED, Paul Michael CAMPBELL, James John FIORDALISI, Adrienne Deich COX, Channing Joseph DER
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Publication number: 20090163451Abstract: The invention features methods of treating visceral pain in humans by administering an effective amount of a 5HT1B or 5HT1D receptor agonist, (e.g., a triptan). These methods can be used, for example, to treat a human suffering from visceral pain secondary to an underlying disease of a visceral organ, such as pancreatitis. Visceral pain treatable by the methods of the invention may also be secondary to a disease of the liver, kidney, ovary, uterus, bladder, bowel, stomach, esophagus, duodenum, intestine, colon, spleen, pancreas, appendix, heart, or peritoneum.Type: ApplicationFiled: November 17, 2008Publication date: June 25, 2009Inventors: Frank Porreca, Louis P. Vera-Portocarrero
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Publication number: 20090155331Abstract: Described are injectable formulations of particulate olanzapine that produce a prolonged duration of action upon administration, and methods of making and using such formulations. The injectable formulations comprise particulate olanzapine.Type: ApplicationFiled: December 11, 2008Publication date: June 18, 2009Applicant: Elan Pharma International LimitedInventors: Stephen B. Ruddy, David Czekai, Gary Liversidge, Scott A. Jenkins, Elaine M. Liversidge
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Publication number: 20090156562Abstract: The invention is directed to pharmaceutical compositions comprising colored solutions, colored emulsions, or colored powders of injectable pharmaceuticals wherein said pharmaceuticals are selected from the group consisting of muscle relaxants, hypnotics, induction agents, and anticholinergics. The formulations of the present invention may all be colored using fluorescein. Different colors may be achieved by either varying the concentration of fluorescein, or by combining fluorescein with another dye. The invention is also directed to methods involving the use of said pharmaceutical compositions.Type: ApplicationFiled: November 13, 2006Publication date: June 18, 2009Inventor: Peter D. Winch
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Publication number: 20090156583Abstract: The present invention relates to compounds of formula I wherein A, G, r and R1 to R5 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.Type: ApplicationFiled: February 20, 2009Publication date: June 18, 2009Inventors: Matthias Nettekoven, Jean-Marc Plancher, Hans Richter, Olivier Roche, Sven Taylor
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Publication number: 20090156578Abstract: In part, the present invention is directed towards compounds with FabI inhibiting properties. Such compounds may also inhibit other enzymes, including those similar to FabI either structurally or functionally, for example, Fab K. Kits and compositions that include the disclosed compounds are also provided. Methods of treating a subject with a bacterial illness is also disclosed.Type: ApplicationFiled: December 1, 2006Publication date: June 18, 2009Inventors: Henry Pauls, Judd M. Berman
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Patent number: 7547705Abstract: The invention relates to a dihydrospiro-[cycloalkylamine]-pyrimidone derivative represented by formula (I) or a salt thereof: wherein: X, Y, R1, R2, R3, R4, o, m, 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 disease.Type: GrantFiled: October 3, 2007Date of Patent: June 16, 2009Assignees: Sanofi-Aventis, Mitsubishi Pharma CorporationInventors: Nathalie Chereze, Alistair Lochead, Mourad Saady, Franck Slowinski, Philippe Yaiche
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Publication number: 20090149449Abstract: Disclosed are compounds of Formula I wherein X, Y, R1-R7, T1, T2, Z, and p are as described herein; a pharmaceutical composition comprising a compound of Formula I and a carrier; a method of inhibiting growth of a cell, which method comprises administering in an amount effective to inhibit growth a compound of Formula I; a method of treating cancer in a mammal, which method comprises administering in an amount effective to treat cancer a compound of Formula I; a method of treating a viral, parasitic, or bacterial infection of a cell, which method comprises administering in an amount effective to treat a viral, parasitic, or bacterial infection a compound of Formula I; and a method of preparing a compound of Formula I as described herein.Type: ApplicationFiled: February 13, 2009Publication date: June 11, 2009Applicants: The United States of America, as represented by the Secretary, Dept. of Health and Human Service, Starks Associates, Inc., Midwest Research Institute, Spirogen, Ltd.Inventors: Paul S. Liu, B. Rao Vishnuvajjala, Kenneth M. Snader, David E. Thurston, Philip W. Howard, Luke Y. Hsiao, Gregory Turner
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Publication number: 20090143356Abstract: Is to provide a novel compound having an anti-viral activity, particularly a HIV integrase inhibitory activity, and a pharmaceutical composition, particularly an anti-HIV agent. (wherein R1 is hydrogen or lower alkyl; X is lower alkylene etc.; R2 is optionally substituted aryl; R3 is hydrogen, halogen, hydroxy, optionally substituted lower alkyl etc.; R4 is hydrogen, optionally substituted lower alkyl, optionally substituted cycloalkyl, optionally substituted cycloalkyl lower alkyl, optionally substituted aryl, optionally substituted aryl lower alkyl, optionally substituted heterocyclic group, optionally substituted heterocyclic lower alkyl etc.; A broken line indicates the presence or absence of a bond; B1 and B2 are such that any one of them is CR20R21, and the other is NR22 and, in this case, there is no broken line.Type: ApplicationFiled: October 26, 2006Publication date: June 4, 2009Inventors: Hiroshi Yoshida, Takashi Kawasuji, Teruhiko Taishi, Yoshiyuki Taoda
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Publication number: 20090137563Abstract: The invention relates to a process for the preparation of 2-methyl-4-(4-methylpiperazin-1-yl)-10H-thieno-[2,3-b][1,5]benzodiazepine (olanzapine) of the formula (I) by reacting 4-amino-2-methyl-10H-thieno [2,3-b][1/5]benzodiazepine hydrochloride of the formula (II) with N-methylpiperazine in an organic solvent, which comprises carrying out the reaction in the mixture of toluene and 1,3-dimethyl-2-imidazolidinone. The invention also encompasses new 2-methyl-4-(4-methylpiperazin-1-yl)-10H-thieno [2,3-b][1,5]benzodiazepine dihydrochloride trihydrate of the formula (IB), the preparation thereof and pharmaceutical compositions comprising said new compound.Type: ApplicationFiled: November 10, 2006Publication date: May 28, 2009Inventors: Gyorgyi Kovanyine Lax, Gabor Nemeth, Gyorgy Krasznay, Norbert Mesterhazy, Kalman Nagy, Gyorgyi Vereczkeyne Donath, Zsuzsanna Szent-Kirallyi
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Publication number: 20090137564Abstract: The present invention relates to compounds of formula I, processes for their production and their use as anti-inflammatory agents.Type: ApplicationFiled: November 21, 2008Publication date: May 28, 2009Inventors: Markus Berger, Hartmut Rehwinkel, Thomas Zollner, Ekkehard May, Jorna Hassfeld, Heike Schacke
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Publication number: 20090130216Abstract: Multimodal particulate formulations of medicaments and methods for their use, e.g. by nasal or pulmonary administration for the treatment of various medical conditions, are provided.Type: ApplicationFiled: November 6, 2008Publication date: May 21, 2009Inventors: Steve Cartt, David Medeiros
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Publication number: 20090131363Abstract: This invention relates to novel compounds that are hydroxyethylamino sulfonamide derivatives and pharmaceutically acceptable salts thereof. More specifically, this invention relates to novel hydroxyethylamino sulfonamide derivatives that are derivatives of darunavir. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering a human immunodeficiency virus (HIV) protease inhibitor, such as darunavir.Type: ApplicationFiled: October 24, 2008Publication date: May 21, 2009Inventor: Scott L. Harbeson
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Publication number: 20090124607Abstract: Compounds of formula (I): or a pharmaceutically acceptable salt thereof; compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating the glucocorticoid receptor in a warm blooded animal).Type: ApplicationFiled: October 18, 2006Publication date: May 14, 2009Inventors: Hakan Bladh, Jan Dahmen, Thomas Hansson, Krister Henriksson, Matti Lepisto, Stinabritt Nilsson
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Publication number: 20090124606Abstract: New pharmaceutical combination providing to decrease or eliminate the extrapyramidal side effects of antipsychotic active ingredients by combination of deramciclane with a classic antipsychotic agent (e.g. haloperidol, chloroprozamine or levoprozamin) or an atypical antipsychotic agent (e.g. risperidone, iloperidone or olanzapine).Type: ApplicationFiled: July 12, 2006Publication date: May 14, 2009Inventors: Istvan Gacsalyi, Gyorgy Levay
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Patent number: 7531530Abstract: The invention relates to trycyclic lactam indole derivatives and triacyclic lactam benzimodole derivatives and their use in inhibiting the activity of PARP enzyme. The invention also relates to the use of these compounds in the preparation of medicaments.Type: GrantFiled: July 23, 2004Date of Patent: May 12, 2009Assignees: Cancer Research Technology Limited, PfizerInventors: Thomas Helleday, Nicola Curtin
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Publication number: 20090118170Abstract: Buccal aerosol sprays or capsule using polar and non-polar solvent have now been developed which provide biologically active compounds for rapid absorption through the oral mucosa, resulting in fast onset of effect. The buccal polar compositions of the invention comprises formulation I: polar solvent 37-98.58%, active compound 0.005-55%, optionally containing flavoring agent 0.1-10%.Type: ApplicationFiled: January 8, 2009Publication date: May 7, 2009Inventor: Harry A. Dugger, III
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Patent number: 7528126Abstract: A compound of formula (I) and salts and solvates thereof, wherein: R10 is a nitrogen protecting group and R11 is either OH or O—R12, wherein R12 is an oxygen protecting group, or R10 and R11 together form a double bond between N10 and C11; and R10? and R11? are selected from the same options as R10 and R11 respectively.Type: GrantFiled: March 9, 2005Date of Patent: May 5, 2009Assignee: Spirogen LimitedInventors: Philip Wilson Howard, Stephen John Gregson, Peter William Taylor, David Edwin Thurston, Tsveta Stefanova Hadjivassileva
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Patent number: 7528127Abstract: It has now been found that compounds of the present invention as described in Benzodiazepine derivatives of Formula (I) containing a carboxylic ester moiety and thereby capable of being inactivated by nonspecific tissue esterases in an organ-independent elimination mechanism and thereby providing a more predictable and reproducible pharmacodynamic profile. The compounds of the present invention are suitable for therapeutic purposes, including sedative-hypnotic, anxiolytic, muscle relaxant and anticonvulsant purposes and are useful to be administered intravenously in the following clinical settings: preoperative sedation, anxiolysis, and amnestic use for perioperative events; conscious sedation during short diagnostic, operative or endoscopic procedures; as a component for the induction and maintenance of general anesthesia, prior and/or concomitant to the administration of other anesthetic agents; ICU sedation.Type: GrantFiled: January 5, 2007Date of Patent: May 5, 2009Assignee: CeNes LimitedInventors: Paul L. Feldman, David Kendall Jung, Istvan Kaldor, Gregory J. Pacofsky, Jeffrey A. Stafford, Jeffrey H. Tidwell
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Patent number: 7528128Abstract: The present invention provides a compound of general formula 5, useful as potential antitumour agents against human cancer cell lines. The present invention further provides a process for the preparation of pyrrolo[2,1-c][1,4]benzodiazepine hybrids of general formula 5 wherein, X1, X2, X3 is selected from H or Cl or CH3, Y is selected from O or NH, Z is selected from C?O or CH2 and n=1 to 4.Type: GrantFiled: August 13, 2007Date of Patent: May 5, 2009Assignee: Council of Scientific & Industrial ResearchInventors: Kamal Ahmed, Rajendra Prasad Bandari
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Patent number: 7524840Abstract: The present invention provides compounds of formula I wherein R1, R2, R3, R4, and R5are described herein. The invention also provides syntheses for preparation of such compounds and pharmaceutical compositions containing them. The invention further provides methods for inhibiting kinases, in particular CDK2, for inhibiting angiogenesis, and for treating cancers, in particular breast, colon, prostate, and lung cancer.Type: GrantFiled: October 5, 2005Date of Patent: April 28, 2009Assignee: Hoffmann-La Roche Inc.Inventors: Jin-Jun Liu, Kin-Chun Luk, Giacomo Pizzolato, Yi Ren, Kshitij Chhabilbhai Thakkar, Peter Michael Wovkulich, Zhuming Zhang
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Publication number: 20090105229Abstract: The present invention provides kinase inhibitors of Formula I.Type: ApplicationFiled: December 12, 2008Publication date: April 23, 2009Inventors: Thomas Albert Engler, Timothy Paul Burkholder, Joshua Ryan Clayton, Clive Gideon Diefenbacher, Kelly Wayne Furness, James Robert Henry, Yihong Li, Sushant Malhotra, Angela Lynn Marquart, Johnathan Alexander McLean, David Mendel, Jon Kevin Reel
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Publication number: 20090105187Abstract: The present invention provides methods of identifying agents that reduce a level of active APOBEC3C in a cell. The present invention provides agents that reduce a level of active APOBEC3C in a cell; and compositions comprising the agents. The present invention further provides methods of reducing the mutation rate of a lentivirus in a cell; and methods of reducing the emergence of drug-resistant strains of lentivirus. The present invention further provides methods for treating lentivirus infections.Type: ApplicationFiled: October 31, 2005Publication date: April 23, 2009Inventors: Robert M. Grant, Khaoula Bourara
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Publication number: 20090105228Abstract: Compounds of formula I: (where variables R2, R7, D, W, X, Y and Z are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.Type: ApplicationFiled: July 25, 2006Publication date: April 23, 2009Inventor: Theresa M. Williams
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Publication number: 20090093466Abstract: The invention encompasses compounds of Formula I, including pharmaceutically acceptable salts, their pharmaceutical compositions, and their use in treating CNS disorders.Type: ApplicationFiled: September 29, 2008Publication date: April 9, 2009Inventor: Ronald J. Mattson
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Patent number: 7511037Abstract: The invention encompasses a series of bicyclic pyrimidinone compounds of Formula I which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV.Type: GrantFiled: August 16, 2006Date of Patent: March 31, 2009Assignee: Bristol-Myers Squibb CompanyInventors: B. Narasimhulu Naidu, Jacques Banville, Francis Beaulieu, Timothy P. Connolly, Mark R. Krystal, John D. Matiskella, Carl Ouellet, Serge Plamondon, Roger Remillard, Margaret E. Sorenson, Yasutsugu Ueda, Michael A. Walker
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Patent number: 7511032Abstract: Disclosed are compounds of Formula (I) wherein X, Y, Ri-R7, T1, T2, Z, and p are as described herein; a pharmaceutical composition comprising a compound of Formula (I) and a carrier; a method of inhibiting growth of a cell, which method comprises administering in an amount effective to inhibit growth a compound of Formula (I); a method of treating cancer in a mammal, which method comprises administering in an amount effective to treat cancer a compound of Formula (I); a method of treating a viral, parasitic, or bacterial infection of a cell, which method comprises administering in an amount effective to treat a viral, parasitic, or bacterial infection a compound of Formula (I); and a method of preparing a compound of Formula (I) as described herein.Type: GrantFiled: October 22, 2004Date of Patent: March 31, 2009Assignees: The United States of America as represented by the Secretary, Department of Health and Human Services, Starks Associates, Inc., Midwest Research Institute, Spirogen, Ltd.Inventors: Paul S Liu, B. Rao Vishnuvajjala, Kenneth M Snader, David E Thurston, Philip W Howard, Luke Y Hsiao, Gregory Turner
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Patent number: 7507397Abstract: The present invention relates to the delivery of muscle relaxants through an inhalation route. Specifically, it relates to aerosols containing muscle relaxants that are used in inhalation therapy. In a method aspect of the present invention, a muscle relaxant is delivered to a patient through an inhalation route. The method comprises: a) heating a coating of a muscle relaxant, on a solid support, to form a vapor; and, b) passing air through the heated vapor to produce aerosol particles having less than 5% muscle relaxant degradation products. In a kit aspect of the present invention, a kit for delivering a muscle relaxant through an inhalation route is provided which comprises: a) a coating of a muscle relaxant and b) a device for dispensing said coating a muscle relaxant as a condensation aerosol.Type: GrantFiled: September 19, 2006Date of Patent: March 24, 2009Assignee: Alexza Pharmaceuticals, Inc.Inventors: Joshua D. Rabinowitz, Alejandro C. Zaffaroni
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Publication number: 20090069267Abstract: The present invention concerns compositions, methods and/or apparatus of central administration of various CNS-active agents. In particular embodiments, intrathecal administration is advantageous for decreasing the systemic concentrations of CNS agent, thereby decreasing side effect toxicity, while allowing more effective delivery of the agent to the site of action, simultaneously decreasing the dosage delivered to the subject. In particular embodiments, ICV delivery may be of use for patients who have previously proven to be refractory to systemic administration of CNS agents, in some cases due to systemic side effects, or for those patients whose symptoms are of sufficient severity to warrant more aggressive therapeutic intervention. ICV administration allows not only lower systemic concentration but also higher therapeutically effective concentration within the CNS.Type: ApplicationFiled: July 25, 2008Publication date: March 12, 2009Inventors: Daniel J. Abrams, Raymond Bunch, Tom Anchordoquy, Karen E. Stevens
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Publication number: 20090069306Abstract: Provided is a process for producing highly pure midazolam and salts thereof, and a pharmaceutical composition containing the highly pure midazolam and/or a salt thereof.Type: ApplicationFiled: September 11, 2007Publication date: March 12, 2009Applicant: CHEMAGIS LTD.Inventors: Sonia KRIVONOS, Yana SERY
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Publication number: 20090062262Abstract: The present invention relates to compounds having general Formula (I) or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: February 14, 2006Publication date: March 5, 2009Applicant: N.V. ORGANONInventors: Ralf Plate, Guido Jenny Rudolf Zaman, Pedro Harold Han Hermkens, Christiaan Gerardus Johannes Maria Jans, Rogier Christian Buijsman, Adrianus Petrus Antonius De Man, Paolo Giovanni Martino Conti, Scott James Lusher, Willem Hendrik Abraham Dokter
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Publication number: 20090060871Abstract: A method for reducing psychological opioid dependence includes selecting a patient addicted to an opioid and administering to the patient an opioid agonist-antagonist for at least 14 days, thereby reducing craving for the opioid in the patient. An opioid agonist-antagonist is administered in a patient needing an average adherence to a treatment protocol of at least 95 percent. A non-injectable formulation containing an agonist-antagonist also is disclosed.Type: ApplicationFiled: October 24, 2008Publication date: March 5, 2009Inventors: Michael Victor VORONKOV, Efim David NEZHINSKY, Levon Gevorkovich ISAKULYAN, Daria Alexandrovna OCHERET
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Patent number: 7498334Abstract: Pyrrolopyrimidine derivatives of the formula I in which R3, R4, R5, R6 and X are as defined in claim 1, act as phosphodiesterase VII inhibitors and can be employed for the treatment of osteoporosis, tumours, cachexia, atherosclerosis, rheumatoid arthritis, multiple sclerosis, diabetes mellitus, inflammatory processes, allergies, asthma, autoimmune diseases, myocardial diseases and AIDS.Type: GrantFiled: November 8, 2002Date of Patent: March 3, 2009Assignee: Merck Patent GmbHInventors: Hans-Michael Eggenweiler, Michael Wolf
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Publication number: 20090054399Abstract: Tricyclic compounds of Formula (I) are inhibitors of HIV integrase and inhibitors of HIV replication: wherein bond a, ring A, R1, R2 and R3 are defined herein. The compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset 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: ApplicationFiled: May 5, 2006Publication date: February 26, 2009Inventors: Joseph P. Vacca, John S. Wai, Linda S. Payne, Richard C.A. Isaacs, Wei Han, Melissa Egbertson, Richard Pracitto
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Publication number: 20090054412Abstract: A method for treating various types of insomnia is provided using 7-chloro-3-(5-dimethylaminomethyl-[1,2,4]oxadiazol-3-yl)-5methyl-4,5-dihydro-imidazol[1,5,-a][1,4]benzodiazepine-6-one or its pharmaceutically acceptable salt.Type: ApplicationFiled: August 20, 2007Publication date: February 26, 2009Inventors: John Alan Kemp, Ian Michael Hunneyball, Timothy Tasker
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Patent number: 7494984Abstract: The invention encompasses a series of bicyclic heterocyclic compounds of Formula I which are inhibitors of HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV.Type: GrantFiled: August 29, 2006Date of Patent: February 24, 2009Assignee: Bristol-Myers Squibb CompanyInventors: Jacques Banville, Roger Remillard, Serge Plamondon