Tricyclo Ring System Having The Seven-membered Hetero Ring As One Of The Cyclos Patents (Class 514/220)
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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
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Publication number: 20090048234Abstract: The present invention provides compositions and methods for preventing, treating or reversing neuronal dysfunction in a mammal resulting from exposure to organophosphate nerve agents, organophosphate insecticides and incapacitating agents of the central nervous system (CNS); CNS injury, including traumatic brain injury, neurologic complications of cardiac surgery, perinatal asphyxia, and stroke, spinal cord injury, and peripheral nerve injury; and neuronal disorders associated with the loss of motor function including post-polio syndrome, amyotrophic lateral sclerosis, myasthenia gravis, Parkinson's disease and Rett syndrome; neurodegenerative disorders including Alzheimer's disease, mild cognitive impairment and schizophrenia; and cognitive impairment associated with aging.Type: ApplicationFiled: September 17, 2004Publication date: February 19, 2009Inventor: Franklin Volvovitz
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Publication number: 20090047347Abstract: The present invention provides compositions and methods and for speeding the onset of drug action and reducing the first-pass effect drug metabolism in fast-dispersing drug formulations.Type: ApplicationFiled: August 20, 2008Publication date: February 19, 2009Applicant: AEGIS THERAPEUTICS, INC.Inventor: Edward T. Maggio
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Patent number: 7491716Abstract: The present invention provides kinase inhibitors of Formula I.Type: GrantFiled: March 4, 2003Date of Patent: February 17, 2009Assignee: Eli Lilly and CompanyInventor: Thomas Albert Engler
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Publication number: 20090042861Abstract: The present invention provides a prophylactic or therapeutic agent for depression or anxiety disorders, comprising (S)-N-[2-(1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-yl)ethyl]propionamide.Type: ApplicationFiled: April 3, 2006Publication date: February 12, 2009Applicant: Takeda Pharmaceutical Company LimitedInventors: Keisuke Hirai, Masaomi Miyamoto
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Publication number: 20090036431Abstract: The present invention is related to new tomaymycin derivatives, their process of preparation and their therapeutic uses.Type: ApplicationFiled: July 16, 2008Publication date: February 5, 2009Applicant: SANOFI-AVENTISInventors: Laurence GAUZY, Herve BOUCHARD, Ravi V.J. CHARI, Alain COMMERCON, Robert ZHAO, Yonghong DENG, Wei LI
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Patent number: 7485635Abstract: The present invention provides a compound of formula (I): wherein all variables are as defined herein, pharmaceutical formulations containing the same, processes for preparing the same and their use therapy.Type: GrantFiled: December 5, 2006Date of Patent: February 3, 2009Assignee: CeNes LimitedInventors: Paul L. Feldman, David Kendall Jung, Istvan Kaldor, Gregory J. Pacofsky, Jeffrey A. Stafford, Jeffrey H. Tidwell
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Publication number: 20090029972Abstract: The invention relates to biologically active dibenzodiazepinone analogs represented by Formula I, to methods of producing them, and their use in the preparation of medicaments for the treatment of neoplastic conditionsType: ApplicationFiled: September 26, 2005Publication date: January 29, 2009Applicant: Ecopia BioSciences IncInventors: James B. McAlpine, Arjun H. Banskota
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Publication number: 20090029965Abstract: The present invention concerns compounds inter alia according to general formula 1a. Compounds according to the invention are vasopressin V1a receptor antagonists. Pharmaceutical compositions of the compounds are useful as treatment of dysmenorrhoea.Type: ApplicationFiled: August 24, 2005Publication date: January 29, 2009Applicant: Ferring B.V.Inventors: Andrzej Roman Batt, Martin Lee Stockley, Michael Bryan Roe, Celine Marguerite Simone Heeney, Andrew John Baxter, Peter Hudson, Rachel Handy
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Publication number: 20090029967Abstract: There is disclosed a method for the treatment or prevention of Extra Pyramidal syndrome (EPS), dystonia, restless leg syndrome (RLS) or periodic leg movement in sleep (PLMS) comprising the administration of an adenosine A2a receptor antagonist, alone or in combination with other agents useful for treating EPS, dystonia, RLS or PLMS.Type: ApplicationFiled: July 29, 2008Publication date: January 29, 2009Inventors: Michael Grzelak, John Hunter, Annamarie Pond, Geoffrey Vaity
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Publication number: 20090029973Abstract: The present invention relates to a compound represented by the formula: wherein W is C(R1) or N, each A is an optionally substituted aryl group or a heteroaryl group, X1 is —NR3—Y1—, —O—, —S—, —SO—, —SO2— or —CHR3— wherein R3 is a hydrogen atom or an optionally substituted aliphatic hydrocarbon group, or R3 is optionally bonded to A to form an optionally substituted ring structure, R1 is a hydrogen atom or an optionally substituted group bonded via a carbon atom, a nitrogen atom or an oxygen atom, R2 is a hydrogen atom or optionally substituted group bonded via a carbon atom or a sulfur atom, or R1 and R2, or R2 and R3 are optionally bonded to form an optionally substituted ring structure, or a salt thereof, and a tyrosine kinase inhibitor or an agent for the prophylaxis or treatment of cancer, which contains this compound or a prodrug thereof.Type: ApplicationFiled: July 14, 2008Publication date: January 29, 2009Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Tomoyasu ISHIKAWA, Takahiko TANIGUCHI, Hiroshi BANNO, Masaki SETO
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Publication number: 20090028948Abstract: The present invention relates to improved therapeutically active nanocomposite microstructure compositions, including nanoparticle compositions and nanoparticle preparations. Preferred embodiments include nanoparticle compositions comprising nanoparticles of a therapeutically active agent dispersed in a carrier matrix. The invention also relates to a method for preparing said compositions and preparations using solid-state mechanochemical synthesis. Further, it relates to therapeutic products produced using said compositions and to methods of treatment using the compositions.Type: ApplicationFiled: December 30, 2005Publication date: January 29, 2009Applicant: ICEUTICA PTY LTDInventors: Trevor Payne, Felix Meiser, Almar Postma, Raffaele Cammarano, James Williams, Paul McCormick, Aaron Dodd, Frank Caruso
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Publication number: 20090023712Abstract: The invention relates to new pharmaceutical compositions for the treatment of Attention Deficit Hyperactivity Disorder (ADHD) and methods for the preparation thereof. In a preferred embodiment, the instant invention is directed to pharmaceutical combinations comprising flibanserin as one active ingredient in combination with at least one additional active ingredient for the treatment ADHD and methods for the preparation thereof.Type: ApplicationFiled: February 15, 2007Publication date: January 22, 2009Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Boris Ferger, Angelo Ceci
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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: 20090018119Abstract: Disclosed herein is a method to treat neuropsychiatric diseases including psychosis, affective disorders, dementia, neuropathic pain, and glaucoma. Treatment is carried out by administering a therapeutically effective amount of N-desmethylclozapine to a patient suffering from a neuropsychiatric disease.Type: ApplicationFiled: September 22, 2008Publication date: January 15, 2009Applicant: ACADIA PHARMACEUTICALS, INC.Inventors: David M. Weiner, Mark R. Brann
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Patent number: 7476664Abstract: The present invention provides a novel bis 2-difluoro pyrrolo[2,1-c][1,4]benzodiazepine of formula VII wherein, n is 3 to 10. novel bis 2-difluoro pyrrolo[2,1-c][1,4]benzodiazepine of formula VII exhibits biding affinity with calf thymus (CT) DNA at a molar ratio of 1:5 in aqueous sodium phosphate buffer at pH of about 7.00. The present invention further provides a process for the preparation of novel bis 2-difluoro pyrrolo[2,1-c][1,4]benzodiazepine of formula VII.Type: GrantFiled: March 7, 2007Date of Patent: January 13, 2009Inventors: Ahmed Kamal, Depatla Rajasekhar Reddy, Rajendar Rajendar
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Publication number: 20090010992Abstract: Improved compositions, methods and systems for oral transmucosal administration of small volume bioadhesive drug dosage forms to pediatric subjects are provided. The drug dosage form is easily administered and may be delivered using a single dose applicator or a device.Type: ApplicationFiled: October 11, 2007Publication date: January 8, 2009Applicant: AceIRx Pharmaceuticals, Inc.Inventors: Pamela Palmer, Thomas Schreck, Stelios Tzannis, Larry Hamel, Andrew I. Poutiatine
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Publication number: 20090012064Abstract: The present invention provides a composition controlling a pH range of release and/or a release rate, which contains (i) a thienotriazolodiazepine compound of the formula (I) and (ii) at least one kind of ingredient selected from the group consisting of a water-soluble polymer, an enteric polymer, a water-insoluble polymer and a porous polymer and/or a surfactant, as well as a production method thereof.Type: ApplicationFiled: August 5, 2008Publication date: January 8, 2009Inventors: Kazuyoshi Sagara, Tomoyuki Omura, Hirofumi Samemoto, Hirotsugu Komatsu
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Patent number: 7473689Abstract: The present invention provides a compound of formula (I): wherein all variables are as defined herein, pharmaceutical formulations containing the same, processes for preparing the same and their use therapy.Type: GrantFiled: January 5, 2007Date of Patent: January 6, 2009Assignee: CeNes LimitedInventors: Paul L. Feldman, David Kendall Jung, Istvan Kaldor, Gregory J. Pacofsky, Jeffrey A. Stafford, Jeffrey H. Tidwell
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Publication number: 20090005366Abstract: The present application describes deuterium-enriched olanzapine, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: June 19, 2007Publication date: January 1, 2009Applicant: PROTIA, LLCInventor: Anthony W. Czarnik
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Publication number: 20090005367Abstract: Disclosed are pharmaceutical compositions comprising a benzodiazepine, an alcohol aversive agent, and an abuse aversive agent, and methods of use in preventing alcohol or cocaine abuse.Type: ApplicationFiled: September 7, 2007Publication date: January 1, 2009Inventor: Murray James Propes
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Publication number: 20090005357Abstract: The present invention relates generally to pharmacological methods for the prevention of amelioration of sleep-related breathing disorders via administration of agents or combinations of agents that possess serotonin-related pharmacological activity.Type: ApplicationFiled: September 11, 2008Publication date: January 1, 2009Applicant: THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOISInventors: Miodrag Radulovacki, David W. Carley
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Publication number: 20080317853Abstract: Disclosed herein is a orally disintegrating and/or dissolving oral pharmaceutical composition, comprising one or more active pharmaceutical ingredients, one or more fillers having particle size of 100 microns or above, a high and desirable amount of silicon dioxide, one or more disintegrating agents, optionally effervescent couple, wherein said composition has good organoleptic properties like desired mouth feel and fast oral disintegration time.Type: ApplicationFiled: August 30, 2006Publication date: December 25, 2008Applicant: Jubilant Organosys Ltd.Inventors: Namdev Kashid, Gour Mukherji
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Publication number: 20080318934Abstract: The invention relates to compounds of the formula (I), to the preparation and use thereof for the preparation of a medicament for the treatment of diseases, in particular tumours and/or diseases in the development or course of which kinases are involved.Type: ApplicationFiled: November 28, 2006Publication date: December 25, 2008Inventors: Melanie Schultz, Lars Thore Burgdorf, Dirk Finsinger, Andree Blaukat, Hartmut Greiner, Christina Esdar
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Publication number: 20080311203Abstract: The invention relates to a solid formulation for the oral administration of olanzapine that comprises a core of anhydrous olanzapine Form I or a pharmaceutically acceptable salt thereof and, optionally, pharmaceutically acceptable excipients, said core being coated with a functional polymer that acts as filmogenic agent. The method for obtaining it comprises: i) providing anhydrous olanzapine Form I or a salt thereof and, optionally, pharmaceutically acceptable excipients in solid form; ii) providing a functional polymer that acts as filmogenic agent; iii) preparing a dispersion of said functional polymer in an aqueous medium,—and applying the dispersion obtained in step iii) onto the solid form of step i).Type: ApplicationFiled: December 19, 2006Publication date: December 18, 2008Applicant: Laboratories Lesvi, S. I.Inventors: Ignacio Diez Martin, Carmen Ubeda Perez, Pablo Pablo Alba
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Publication number: 20080311193Abstract: The present invention is directed towards the preparation of extended release Alprazolam formulation. The formulation thus obtained provides an efficient mode of delivery of Alprazolam in a continuous manner.Type: ApplicationFiled: July 20, 2006Publication date: December 18, 2008Inventors: Manjusha Joshi, Ganesh Vinayak Gat, Satish Ramanlal Mehta
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Patent number: 7465722Abstract: A compound of the formulae (I) or (II): wherein: Y is a moiety selected from NR or —(CH2)n; wherein R is hydrogen or (C1-C6) lower alkyl, and n is 1; represents: (1) a phenyl ring optionally substituted with one or two substituents selected, independently, from the group comprising hydrogen, (C1-C6) lower alkyl, halogen, cyano, CF3, hydroxy, (C1-C6) lower alkoxy, (C1-C6) lower alkoxy carbonyl, carboxy, —CONH2, —CONH[(C1-C6) lower alkyl], —CON[(C1-C6) lower alkyl]2; or (2) a 6-membered aromatic (unsaturated) heterocyclic ring having one nitrogen atom, optionally substituted by (C1-C6) lower alkyl, halogen or (C1-C6) lower alkoxy; represents: (1) a phenyl ring optionally substituted with one or two substituents selected, independently, from the group comprising hydrogen, (C1-C6) lower alkyl, halogen, cyano, CF3, hydroxy, (C1-C6) lower alkoxy, or (C1-C6) lower alkoxy carbonyl, carboxy, —CONH2, —CONH[(C1-C6) lower alkyl], —CON[(C1-C6) lower alkyl]2; or (2) a 5-membered aromatic (unsaturatedType: GrantFiled: August 11, 2006Date of Patent: December 16, 2008Assignee: WyethInventors: Amedeo A. Failli, John P. Dusza, Thomas J. Caggiano, Jay S. Shumsky, Kevin A. Memoli, Eugene J. Trybulski
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Patent number: 7465724Abstract: The present invention provides novel bis-pyrrolo[2,1-c][1,4]benzodiazepine-anthraquinone conjugates of general formula V, useful as potential antitumour agents against human cancer cell lines. The present invention further provides a process for the preparation of novel bis-pyrrolo[2,1 -c][1,4]benzodiazepine-anthraquinone conjugates of general formula V. wherein n=3, 4, or 5.Type: GrantFiled: February 12, 2007Date of Patent: December 16, 2008Assignee: Council of Scientific and Industrial ResearchInventors: Ahmed Kamal, Rondla Ramu, Gollapalli Bhasker Ramesh Khanna
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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: 20080306042Abstract: Novel triazole derivatives are inhibitors of TGF-beta receptor I kinase, and can be employed, inter alia, for the treatment of tumours.Type: ApplicationFiled: November 24, 2006Publication date: December 11, 2008Inventors: Bertram Cezanne, Christiane Amendt, Hartmut Greiner, Ulrich Graedler, Guenter Hoelzemann
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Publication number: 20080306019Abstract: Provided herein is a method of protecting a neuron from dysfunction induced by an HIV neurotoxin, comprising contacting the cell with a therapeutically effective dose of a dopamine D1 receptor agonist. Also provided is a method of treating or preventing HIV-1 associated dementia (HAD) in a subject in need of such treatment or prevention, comprising administering to the subject a therapeutically effective dose of a dopamine D1 receptor agonist and estrogenic compound.Type: ApplicationFiled: May 3, 2006Publication date: December 11, 2008Inventors: Rosemarie M. Booze, Charles Mactutus
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Patent number: 7459449Abstract: Several salts of olanzapine, including olanzapine malonate, olanzapine glycolate, olanzapine maleate, and olanzapine benzoate, have been found to have favorable solid state characteristics.Type: GrantFiled: January 27, 2005Date of Patent: December 2, 2008Inventor: Rolf Keltjens
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Publication number: 20080293699Abstract: Methods for screening for inhibitors of endoplasmic reticulum (ER) stress are provided. These methods involve the addition of thapsigargin, which induces ER stress, and a test agent to mammalian cells in multi-well plates. Cell survival can be readily monitored by measuring intracellular ATP content using a bioluminescent reagent. Screening a commercially available library of 50,000 compounds led to the identification of 93 hit compounds that were subjected to secondary assays to confirm their ability to rescue cells from thapsigargin-induced cell death.Type: ApplicationFiled: May 23, 2008Publication date: November 27, 2008Applicant: BURNHAM INSTITUTE FOR MEDICAL RESEARCHInventors: John C. Reed, In-Ki Kim
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Publication number: 20080293664Abstract: Compounds of formula I, wherein R1, R2, R3, R4, Ra, X, X1, and Y are as defined herein or pharmaceutically acceptable salts thereof, inhibit HIV-1 reverse transcriptase and afford a method for prevention and treatment of HIV-1 infections and the treatment of AIDS and/or ARC. The present invention also relates to compositions containing compounds of formula I useful for the prevention and treatment of HIV-1 infections and the treatment of AIDS and/or ARC.Type: ApplicationFiled: April 8, 2008Publication date: November 27, 2008Inventors: Roland Joseph Billedeau, Wylie Solang Palmer, Zachary Kevin Sweeney, Jeffrey Wu
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Publication number: 20080293698Abstract: The invention provides dilute and concentrated, aqueous, pharmaceutical compositions comprising gamma-hydroxybutyric acid or pharmaceutically acceptable salts thereof; gamma-butyryl lactone; 1,4-butanediol; 4-hydroxyl pentanoic acid or pharmaceutically acceptable salts thereof; 4-hydroxyl pentanoic acid lactone, or combinations thereof, and a coloring agent and/or flavoring agent that is useful in preventing sexual assault or date rape. Methods of treating conditions responsive to the administration of gamma-hydroxyl butyric acid and/or its pharmaceutically acceptable salts; gamma-butyryl lactone; 1,4-butanediol; 4-hydroxyl pentanoic acid and/or its pharmaceutically acceptable salts; and 4-hydroxyl pentanoic acid lactone are also described. The invention provides methods for treating patients with acquired resistance to GABAnergic agents.Type: ApplicationFiled: May 12, 2006Publication date: November 27, 2008Inventor: Joseph Johnson
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Patent number: 7456170Abstract: Compounds of formula (I), or pharmaceutically acceptable derivatives thereof, wherein R represents H, C1-6 alkyl, SO2R1, SO2NR1R2, or COR1; R1 and R2 independently represent C1-6 alkyl; and Ring A represents a phenyl ring or a pyridinyl ring; may be useful in the treatment of anxiety, cardiovascular disease (including angina, atherosclerosis, hypertension, heart failure, edema, hypernatremia), dysmenorrhoea (primary and secondary), endometriosis, emesis (including motion sickness), intrauterine growth retardation, inflammation (including rheumatoid arthritis), mittlesmerchz, preclampsia, premature ejaculation, premature (preterm) labor and Raynaud's disease.Type: GrantFiled: August 12, 2005Date of Patent: November 25, 2008Assignee: Pfizer Inc.Inventor: Patrick S. Johnson
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Patent number: 7456169Abstract: Compounds having the formula are useful for inhibiting protein kinases. Also disclosed are methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.Type: GrantFiled: August 23, 2006Date of Patent: November 25, 2008Assignee: Abbott Laboratories Inc.Inventors: Lisa A. Hasvold, Laura Hexamer, Gaoquan Li, Nan-Horng Lin, Hing Sham, Thomas J. Sowin, Gerard M. Sullivan, Le Wang, Ping Xia
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Publication number: 20080287390Abstract: The invention provides the use of an optionally hydroxyl-protected 4-hydroxy or hydroperoxy-3,5-dioxopyrazolidine or an equivalent wherein a pyrazolidine ring attached oxygen is replaced by a sulphur, or a physiologically acceptable salt thereof, for the manufacture of a medicament for use in drug therapy or prophylaxis. Additionally, the invention provides a method of combating HIV infection which comprises administering to an HIV-infected patient a T-lymphocyte growth suppressing agent, preferably a pyrazolidinol, in an amount sufficient to suppress T-lymphocyte growth in said patient for a period sufficient to reduce the T-lymphocyte concentration in lymph nodes in said patient.Type: ApplicationFiled: January 14, 2008Publication date: November 20, 2008Applicant: A-Viral ASInventors: Enok Tjotta, Jo Klaveness
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Publication number: 20080280884Abstract: Said mixed solvate is a solvate of olanzapine/water/tetrahydrofuran in the proportion 1:1:1/2 (I). The method for preparing said solvate comprises treating a crude anhydrous olanzapine with a mixture of tetrahydrofuran/water. The method for preparing Form I of olanzapine includes desolvating the mixed solvate of formula I, by means of drying, in vacuo and under temperature-controlled conditions.Type: ApplicationFiled: July 7, 2005Publication date: November 13, 2008Applicant: Inke, S.A.Inventors: Pere Dalmases Barjoan, Jordi Bessa Bellmunt
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Publication number: 20080280886Abstract: Disclosed herein are urea-based 5-HT receptor modulators, pharmaceutically acceptable salts and prodrugs thereof, the chemical synthesis thereof, and medical use of such compounds for the treatment and/or management of 5-HT receptor-mediated disorders.Type: ApplicationFiled: May 8, 2008Publication date: November 13, 2008Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Thomas G. Gant, Sepehr Sarshar
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Publication number: 20080280885Abstract: The present invention relates to methods of and compositions for treating and relieving symptoms and disease associated with indications caused by a physiological drive to alleviate a sensation of anxiety. In one treatment method, methods of, and compositions for, modulating the expression of certain GABAA receptor subunits are used to treat anxiety-related disorders and depressive disorders associated with physiological tolerance to endogenous neurosteroids.Type: ApplicationFiled: April 7, 2006Publication date: November 13, 2008Applicant: Hythiam, INC.Inventors: Sanjay Sabnani, Donald Wesson
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Publication number: 20080279784Abstract: Particulate formulations of benzodiazepines, such as diazepam, are used for nasal administration of diazepine drugs to patients. Multimodal particulate formulations of benzodiazepines and methods for their use, e.g. by nasal administration for the treatment of seizure, are also provided.Type: ApplicationFiled: May 7, 2008Publication date: November 13, 2008Applicant: QUESTCOR PHARMACEUTICALS, INC.Inventors: Steve Cartt, David Medeiros
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Publication number: 20080280849Abstract: The invention relates to a combination comprising a quinoline compound or its sail, according to general formula (I) and at least one HIV infection therapeutic agent selected from the group consisting of entry inhibitors, reverse-transcriptase inhibitors, strand-transfer inhibitors, protease inhibitors, and maturation inhibitors. Said combination has therapeutic synergy in the treatment of an HIV infection compared with the quinoline compound, or HIV infection therapeutic agent alone.Type: ApplicationFiled: June 1, 2005Publication date: November 13, 2008Inventors: Herve Leh, Fatima Zouhiri, Jean-Francois Mouscadet, Claire-Marie Thomas, Elisabeth Dam, Dominique Costantini
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Publication number: 20080275023Abstract: New N-hydroxyamides of n-alkyl carboxylic acids omega substituted with suitable tricyclic systems characterised by a central 7-membered ring, having activity as inhibitors of histone deacetylase (HDAC).Type: ApplicationFiled: March 13, 2006Publication date: November 6, 2008Inventors: Antonio Guidi, Tula Dimoulas, Danilo Giannotti, Nicholas Harmat
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Publication number: 20080275030Abstract: The present invention provides a liquid pharmaceutical composition comprising a therapeutic agent and an alkoxy-polyethylene glycol, for example, methoxy-polyethylene glycol, for administration of the therapeutic agent to the mammal. The compositions can be applied to a membrane, for example, a nasal membrane during intranasal administration. The invention also provides methods of administering such compositions to a mammal.Type: ApplicationFiled: January 18, 2008Publication date: November 6, 2008Inventors: Sveinbjorn Gizurarson, James Arp, Raouf Ghaderi, Michael E. Lusty, Gregory G. Plucinski, Mehdi Yazdi
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Publication number: 20080275026Abstract: Novel compounds according to general formula 1, wherein G1 is NR5R6 or a fused polycyclic group that are specific OT receptor agonists and/or V1a receptor antagonists. Pharmaceutical compositions comprising such compounds are useful in the treatment of, inter alia, primary dysmenorrhoea.Type: ApplicationFiled: June 20, 2008Publication date: November 6, 2008Inventors: Peter Hudson, Andrzej Roman Batt, Celine Marguerite Simone Heeney, Andrew John Baxter, Michael Bryan Roe, Peter Andrew Robson
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Publication number: 20080269161Abstract: Provided is a method of protecting a neuron from dysfunction induced by an HIV neurotoxin comprising contacting the cell with a therapeutically effective dose of an inhibitor of mitochondrial hyperpolarization.Type: ApplicationFiled: January 19, 2006Publication date: October 30, 2008Inventors: Seth Perry, John Phillip Norman, Stephen Dewhurst, Harris A. Gelbard
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Publication number: 20080268071Abstract: Disclosed herein are substituted cyclohexanone-based NMDA receptor modulators of Formula I, process of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: April 25, 2008Publication date: October 30, 2008Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Thomas G. Gant, Sepehr Sarshar
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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: 20080261951Abstract: 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)S—; 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: ApplicationFiled: June 23, 2008Publication date: October 23, 2008Inventors: Doreen Mary Ashworth, Gary Robert William Pitt, Peter Hudson, Christopher Martyn Yea, Richard Jeremy Franklin