Tricyclo Ring System Having The Seven-membered Hetero Ring As One Of The Cyclos Patents (Class 514/220)
  • Publication number: 20150119383
    Abstract: Embodiments disclosed herein generally relate to acamprosate formulations, methods of use of the formulations, to methods of using the formulations in combination with at least one other medication, and to combination products and compositions comprising the formulations and at least one other medication, such as neuroleptic (antipsychotic) and/or antidepressant drugs.
    Type: Application
    Filed: June 5, 2014
    Publication date: April 30, 2015
    Inventors: Barry S. Fogel, William D. Kerns, Kei-Lai Fong, San-Laung Chow, Edward Lin, David Wong
  • Patent number: 9018202
    Abstract: Disclosed herein is a method of treating disorders of the retina comprising administering to a patient in need of such treatment a compound selected from the group consisting of olanzapine, certain of its metabolites, clozapine, and n-desmethyl clozapine.
    Type: Grant
    Filed: November 16, 2011
    Date of Patent: April 28, 2015
    Assignee: Allergan, Inc.
    Inventors: Jyotirmoy Kusari, Sheila X. Zhou, Mingting Tian, Edwin U. Padillo, Sandhya S. Rao, Daniel W. Gil, Larry A. Wheeler
  • Patent number: 9017735
    Abstract: Disclosed herein are compositions and methods for treating a psychiatric disorder or symptoms thereof in a patient. The compositions comprise a compound that modulates KCNQ (Kv7) potassium channel activity and the methods include administering an effective amount of the compound that modulates KCNQ (Kv7) potassium channel activity.
    Type: Grant
    Filed: June 3, 2010
    Date of Patent: April 28, 2015
    Assignee: Marquette University
    Inventor: Mohammadhossein Behnam Ghasemzadeh
  • Publication number: 20150111880
    Abstract: A compound with the formula I: wherein: R2 is of formula II: where A is a C5-7 aryl group, X is selected from the group comprising: OH, SH, CO2H, COH, N?C?O, NHRN, wherein RN is selected from the group comprising H and C1-4 alkyl, and (OC2H4)mOCH3, where m is 1 to 3, and either: (i) Q1 is a single bond, and Q2 is selected from a single bond and —Z—(CH2)n—, where Z is selected from a single bond, O, S and NH and is from 1 to 3; or (ii) Q1 is —CH?CH—, and Q2 is a single bond; R12 is a C5-10 aryl group, optionally substituted by one or more substituents selected from the group comprising: halo, nitro, cyano, ether, C1-7 alkyl, C3-7 heterocyclyl and bis-oxy-C1-3 alkylene; R6 and R9 are independently selected from H, R, OH, OR, SH, SR, NH2, NHR, NRR?, nitro, Me3Sn and halo; where R and R? are independently selected from optionally substituted C1-12 alkyl, C3-20 heterocyclyl and C5-20 aryl groups; R7 is selected from H, R, OH, OR, SH, SR, NH2, NHR, NHRR?, nitro, Me3Sn and halo; either: (a) R10 is H, and R
    Type: Application
    Filed: December 22, 2014
    Publication date: April 23, 2015
    Inventors: Philip Wilson Howard, Stephen John Gregson, Luke Masterson
  • Patent number: 9011912
    Abstract: Oral dosage forms for poorly soluble amine drugs are provided. Such dosage forms include an ionizable compound such as an organic acid, an amphiphilic polymer and a release rate-controlling membrane. Such dosage forms allow for the consistent release of the active agent in both gastric pH conditions and in the intestine. Methods of making such dosage forms are also provided.
    Type: Grant
    Filed: October 7, 2010
    Date of Patent: April 21, 2015
    Assignee: Abon Pharmaceuticals, LLC
    Inventors: Yanming Zu, Sudhir Gorukanti, Salah Uddin Ahmed
  • Publication number: 20150105351
    Abstract: The present invention is directed to novel nanomolar and picomolar inhibitors of HIV reverse transcriptase, pharmaceutical compositions therefrom and methods for inhibiting reverse transcriptase and treating HIV infections, especially included drug resistant strains of HIV-1 and HIV-2 and/or secondary disease states and/or conditions which occur as a consequence of HIV infection.
    Type: Application
    Filed: October 8, 2014
    Publication date: April 16, 2015
    Inventors: William L. Jorgensen, Karen S. Anderson
  • Patent number: 9006233
    Abstract: Described herein are ?3 or ?2 or ?2/?3 GABAergic receptor subtype selective ligands, pharmaceutical compositions, and methods of use of such ligands and compositions in treatment of anxiety disorders, epilepsy and schizophrenia with reduced sedative and ataxic side effects. In embodiments, such as ?3 or ?2 or ?2/?3 GABAergic receptor subtype selective ligands lack ester linkages and may be thus relatively insensitive to hydrolysis by esterases.
    Type: Grant
    Filed: April 27, 2012
    Date of Patent: April 14, 2015
    Assignee: UWM Research Foundation, Inc.
    Inventors: James M. Cook, Terry S. Clayton, Hiteshkumar D. Jain, Sundari K. Rallipalli, Yun Teng Johnson, Jie Yang, Michael Ming-jin Poe, Ojas A. Namjoshi, Zhi-jian Wang
  • Publication number: 20150099742
    Abstract: The present invention relates to a substance for the treatment of the phantom phenomena of tinnitus and/or phantom pain, a method for the diagnosis and for the treatment of these phantom phenomena.
    Type: Application
    Filed: December 16, 2014
    Publication date: April 9, 2015
    Applicant: OTOLANUM AG
    Inventors: Marlies KNIPPER-BREER, Lukas Rüttiger
  • Publication number: 20150099741
    Abstract: Disclosed are methods and kits for diagnosing, prognosing, and treating patients having psychiatric disorders. The methods may include assessing whether a patient has a treatment resistant psychiatric disorder or assessing whether the patient is likely to develop a treatment resistant psychiatric disorder. The methods may include detecting genetic markers such as the single nucleotide polymorphism (SNP) in genes present in a genomic nucleic acid sample from the patient, and/or receiving, as a caregiver, the results of tests indicating whether the genetic markers are present in the genomic nucleic acid sample from the patient. The methods may include administering treatment to the patient, for example, based on the detected genetic markers, and administering treatment may include administering new antipsychotic drugs (APDs) that are trace amine-associated receptor 1 (TAAR1) agonists.
    Type: Application
    Filed: October 3, 2014
    Publication date: April 9, 2015
    Applicant: Northwestern University
    Inventors: Jiang Li, Herbert Y. Meltzer
  • Publication number: 20150099015
    Abstract: Methods and compositions are provided for treating neuropsychiatric disorders such as schizophrenia, depression, attention deficit disorder, mild cognitive impairment, dementia, and bipolar disorder. The methods entail administering to a patient diagnosed as having a neuropsychiatric disorder (e.g., schizophrenia, depression, attention deficit disorder, mild cognitive impairment, dementia bipolar disorder, etc.) or as at risk for a neuropsychiatric disorder a benzoic acid, benzoic acid salt, and/or benzoic acid derivative, and/or a sorbic acid, sorbic acid salt, and/or sorbic acid derivative, in combination with a neuropharmacological agent (e.g., an antipsychotic, an antidepressant, medications for attention deficit and hyperactivity disorder, cognitive impairment, or dementia, etc.) where the benzoic acid, benzoic acid salt, or benzoic acid derivative, and/or a sorbic acid, sorbic acid salt, and/or sorbic acid derivative, is in an amount sufficient to increase the efficacy of the neuropharmacological agent.
    Type: Application
    Filed: November 24, 2014
    Publication date: April 9, 2015
    Inventor: Guochuan Emil TSAI
  • Publication number: 20150087512
    Abstract: The subject invention is directed toward antimicrobial agents and methods of treating and preventing infection by pathogenic microorganisms and endophytic microorganisms in a plant through the use of SecA inhibitors.
    Type: Application
    Filed: September 26, 2014
    Publication date: March 26, 2015
    Inventors: Nian WANG, Nagaraju AKULA
  • Publication number: 20150087636
    Abstract: The use of BETi as a potential treatment for FSHD is provided. Specifically, the use of BETi, and particularly selective BETi for BRD4, are shown to inhibit DUX4 expression which is expected to result in a decrease in the severity of symptoms of FSHD. Further, the treatments are shown to work when pulsed as opposed to continuous. This allows for a BETi to be supplied to a human in a pulse, and then allows the human to not need any additional treatment for a window at least as long as the one of the treatment pulse.
    Type: Application
    Filed: September 19, 2014
    Publication date: March 26, 2015
    Inventor: Francis M. Sverdrup
  • Publication number: 20150080325
    Abstract: This disclosure relates to compounds for the inhibition of histone deacetylase and treatment of a cognitive disorder or deficit. More particularly, the disclosure provides for compounds of formula (I) wherein (I), Q, J, L and Z are as defined in the specification.
    Type: Application
    Filed: April 1, 2014
    Publication date: March 19, 2015
    Applicant: EnVivo Pharmaceuticals, Inc.
    Inventors: Kathryn Rogers, Holger Patzke
  • Publication number: 20150080384
    Abstract: Effective methods and compositions to deter abuse of pharmaceutical products (e.g., orally administered pharmaceutical products) including but not limited to immediate release, sustained or extended release and delayed release formulations for drugs subject to abuse comprising at least 10% by weight hydroxypropylcellulose; polyethylene oxide; and a disintegrant selected from the group consisting of crospovidone, sodium starch glycolate and croscarmellose sodium; wherein the ratio of hydroxypropylcellulose to polyethylene oxide on a weight basis is between about 10:1 and 1:10.
    Type: Application
    Filed: November 24, 2014
    Publication date: March 19, 2015
    Applicant: ACURA PHARMACEUTICALS, INC.
    Inventors: Ronald L. LEECH, Rachelle L. HALL YUNG, Albert W. BRZECZKO
  • Patent number: 8981083
    Abstract: The invention features compositions and methods for treating or preventing a neoplasia. More specifically, the invention provides compositions and methods for disrupting the interaction of a BET family polypeptide comprising a bromodomain with chromatin (e.g., disrupting a bromodomain interaction with an acetyl-lysine modification present on a histone N-terminal tail).
    Type: Grant
    Filed: May 16, 2011
    Date of Patent: March 17, 2015
    Assignee: Dana Farber Cancer Institute, Inc.
    Inventors: James Elliott Bradner, Jun Qi
  • Patent number: 8980882
    Abstract: The invention relates to a pharmaceutical preparation for applying a pharmaceutical agent. According to the invention, the preparation contains: a) a pharmaceutical agent which has an aromatic group or an aromatic part and the molecule of which has a maximum diameter of ?2 nm; b) a permethylated cyclodextrin having a degree of substitution of 3 methyl groups per glucopyranose unit. The permethylated cyclodextrin and the pharmaceutical agent form a complex.
    Type: Grant
    Filed: April 1, 2009
    Date of Patent: March 17, 2015
    Inventors: Norbert Roewer, Jens Broscheit
  • Publication number: 20150072964
    Abstract: Use of particular substituted heterocycle fused gamma-carboline compounds as pharmaceuticals for the treatment of agitation, aggressive behaviors, posttraumatic stress disorder or impulse control disorders.
    Type: Application
    Filed: April 14, 2013
    Publication date: March 12, 2015
    Inventors: Sharon Mates, Robert Davis, Kimberly Vanover, Lawrence Wennogle
  • Publication number: 20150064118
    Abstract: The present invention relates to pre-formulations comprising low viscosity, non-liquid crystalline, mixtures of: a) at least one neutral diacyl lipid and/or at least one tocopherol; b) at least one phospholipid; c) at least one biocompatible, oxygen containing, low viscosity organic solvent; wherein at least one bioactive agent is dissolved or dispersed in the low viscosity mixture and wherein the pre-formulation forms, or is capable of forming, at least one liquid crystalline phase structure upon contact with an aqueous fluid. The preformulations are suitable for generating parenteral, non-parenteral and topical depot compositions for sustained release of active agents. The invention additionally relates to a method of delivery of an active agent comprising administration of a preformulation of the invention, a method of treatment comprising administration of a preformulation of the invention and the use of a preformulation of the invention in a method for the manufacture of a medicament.
    Type: Application
    Filed: September 15, 2014
    Publication date: March 5, 2015
    Inventors: Krister THURESSON, Fredrik TIBERG, Markus JOHANSSON, Ian HARWIGSSON, Fredrik JOABSSON, Markus JOHNSSON
  • Publication number: 20150065485
    Abstract: This invention provides compounds having antiviral activities especially inhibiting activity for influenza virus, more preferably provides substituted 3-hydroxy-4-pyridone derivatives having cap-dependent endonuclease inhibitory activity.
    Type: Application
    Filed: November 7, 2014
    Publication date: March 5, 2015
    Inventors: Toshiyuki Akiyama, Kenji Takaya, Makoto Kawai, Yoshiyuki Taoda, Minako Mikamiyama, Kenji Morimoto, Chika Kageyama, Kenji Tomita, Hidenori Mikamiyama, Naoyuki Suzuki
  • Patent number: 8969371
    Abstract: The present disclosure relates to compositions, kits, uses, systems and methods related to naltrexone plus bupropion for treating an overweight or obese subject at increased risk of adverse cardiovascular outcomes. Preferably, the subject has had type-two diabetes for a period of less than 6 years or is a current smoker, optionally that does not have type-two diabetes.
    Type: Grant
    Filed: July 2, 2014
    Date of Patent: March 3, 2015
    Assignee: Orexigen Therapeutics, Inc.
    Inventors: Preston Klassen, Kristin Taylor
  • Patent number: 8969337
    Abstract: The present invention relates to compounds of Formula I:
    Type: Grant
    Filed: December 14, 2012
    Date of Patent: March 3, 2015
    Assignee: Alkermes Pharma Ireland Limited
    Inventors: Laura Cook Blumberg, John A. Lowe, Orn Almarsson, Juan Alvarez, Tarek A. Zeidan
  • Publication number: 20150056192
    Abstract: The invention provides for compositions for treating a cancer or an inflammatory disorder comprising a combination of agents in a pharmaceutically acceptable carrier, wherein said agents comprise: (i) a non-covalent DNA binding agent; and (ii) an anti-cancer or anti-inflammatory agent.
    Type: Application
    Filed: February 28, 2013
    Publication date: February 26, 2015
    Inventors: Pravin R. Chaturvedi, Palaniyandi Manivasakam, Steven Grossman, Sharon Cantor
  • Patent number: 8962018
    Abstract: 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: Grant
    Filed: December 19, 2006
    Date of Patent: February 24, 2015
    Assignee: Laboratorios Lesvi, S.L.
    Inventors: Ignacio Diez Martin, Carmen Ubeda Perez, Pablo Pablo Alba
  • Patent number: 8962613
    Abstract: A diazepine derivative having the following formula (III) or a pharmacologically acceptable salt thereof is used as A P2X4 receptor antagonist: wherein each of R21 and R22 is hydrogen, a C1-8 alkyl group or the like; R23 is hydrogen, a C1-8 alkyl group or the like; each of R24 and R25 is hydrogen, a C1-8 alkyl group or the like; R26 is hydrogen, a C1-8 alkyl group, a halogen atom, hydroxyl, nitro, cyano, phenyl optionally having one or more substituents, or a heterocyclic group optionally having one or more substituents or the like; and p is 0 or 1.
    Type: Grant
    Filed: July 13, 2011
    Date of Patent: February 24, 2015
    Assignee: Nippon Chemiphar Co., Ltd.
    Inventors: Shogo Sakuma, Masahiko Arai, Kunio Kobayashi, Yoshikazu Watanabe, Toshiyasu Imai, Kazuhide Inoue
  • Publication number: 20150045352
    Abstract: 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: Application
    Filed: October 24, 2014
    Publication date: February 12, 2015
    Inventors: Kazuyoshi SAGARA, Tomoyuki OMURA, Hirofumi SAMEMOTO, Hirotsugu KOMATSU
  • Patent number: 8946208
    Abstract: A composition for intranasal delivery of a drug comprising: includes: (i) the drug; and (ii) a non-aqueous vehicle containing (a) propylene glycol and at least one additional solvent selected from N-methylpyrrolidone, propylene carbonate, dimethyl sulfoxide and at least one propylene glycol fatty acid ester; (b) from about 40 to 100% by volume of N-methylpyrrolidone; or (c) from about 40 to 100% by volume of dimethyl sulfoxide (DMSO).
    Type: Grant
    Filed: August 29, 2008
    Date of Patent: February 3, 2015
    Assignee: Archimedes Development Limited
    Inventors: Jonathan Castile, Alan Smith, Yu-Hui Cheng, Peter James Watts
  • Publication number: 20150030616
    Abstract: The invention relates to novel benzodiazepine derivatives with antiproliferative activity and more specifically to novel benzodiazepines of formula (I) and (II), in which the diazepine ring (B) is fused with a heterocyclic ring (CD), wherein the heterocyclic ring is bicyclic or a compound of formula (III), in which the diazepine ring (B) is fused with a heterocyclic ring (C), wherein the heterocyclic ring is monocyclic. The invention provides cytotoxic dimers of these compounds. The invention also provides conjugates of the monomers and the dimers. The invention further provides compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention. The invention further relates to methods of using the compounds or conjugates for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.
    Type: Application
    Filed: June 26, 2014
    Publication date: January 29, 2015
    Inventors: Wei Li, Nathan Elliott Fishkin, Robert Yongxin Zhao, Michael Louis Miller, Ravi V.J. Chari
  • Publication number: 20150030704
    Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R1 and R2 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Application
    Filed: August 21, 2012
    Publication date: January 29, 2015
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: William Farnaby, Charlotte Fieldhouse, Katherine Hazel, Catrina Kerr, Natasha Kinsella, David Livermore, Kevin Merchant, David Miller
  • Publication number: 20150031652
    Abstract: Disclosed are compounds of the following formula: in which R1, R2, R3, R4, R5, R6, R7, X, and t are defined in the specification. Also disclosed are pharmaceutical compositions, kits, and articles of manufacture, which contain the compounds, methods and intermediates useful for making the compounds, and methods of using the compounds to treat diseases, disorders, and conditions related to PARP activity.
    Type: Application
    Filed: August 1, 2014
    Publication date: January 29, 2015
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Anthony R. Gangloff, Andrew John Jennings, Benjamin Jones, Andre A. Kiryanov
  • Publication number: 20150031677
    Abstract: Monomeric and dimeric trioxane thioacetals and methods of their use for treating subjects infected with malaria or other parasitic infectious diseases including, but not limited to, toxoplasmic infection; subjects afflicted with psychiatric conditions associated with toxoplasmic infection; and subjects afflicted with cancer.
    Type: Application
    Filed: February 28, 2013
    Publication date: January 29, 2015
    Applicant: THE JOHNS HOPKINS UNIVERSITY
    Inventors: Gary H. Posner, Alexander M. Jacobine, Rachel D. Slack, Jennifer R. Mazzone
  • Publication number: 20150031655
    Abstract: The disclosure provides a method of treating a mammal afflicted with an age-related disorder, comprising administering to the mammal a combination of liver X receptor (LXR) modulator and estrogen receptor (ER) modulator, in an amount effective to treat the mammal. Further disclosed are the LXR modulators and ER modulators used in the combination therapy.
    Type: Application
    Filed: April 10, 2012
    Publication date: January 29, 2015
    Applicant: UNIVERSITY OF NORTH DAKOTA
    Inventor: Othman Ghribi
  • Patent number: 8940733
    Abstract: The present invention is directed to novel pyrrolobenzodiazepine dimers and methods of using the dimers in the treatment of proliferative diseases.
    Type: Grant
    Filed: November 13, 2013
    Date of Patent: January 27, 2015
    Assignee: Spirogen SARL
    Inventors: Philip Wilson Howard, Stephen John Gregson, Luke Masterson
  • Patent number: 8940732
    Abstract: The invention relates to methods for diagnosis and treatment of autism spectrum disorders, particularly for autism spectrum disorders characterized by increased head size (circumference) and deficits in social behavior.
    Type: Grant
    Filed: January 15, 2010
    Date of Patent: January 27, 2015
    Assignee: Massachusetts Institute of Technology
    Inventors: Damon Theron Page, Mriganka Sur
  • Patent number: 8940315
    Abstract: 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: Grant
    Filed: April 17, 2009
    Date of Patent: January 27, 2015
    Assignee: Medtronic, Inc.
    Inventors: Christopher M. Hobot, Michael E. Benz, Keith R. Hildebrand, Bryant J. Pudil
  • Publication number: 20150025061
    Abstract: The present invention is directed to a method of enhancing visual acuity in a subject, comprising intravitreally administering to the subject in need of such enhancement, a therapeutically effective amount of an extrasynaptic GABAA receptor antagonist. The present invention is also directed to an ocular implant comprising a therapeutically effective amount of the extrasynaptic GABAA receptor antagonist.
    Type: Application
    Filed: July 10, 2014
    Publication date: January 22, 2015
    Inventor: Movses H. Karakossian
  • Publication number: 20150023950
    Abstract: The present invention relates to 2,6-diaminopyridine compounds that can be employed in the treatment of a group of disorders and abnormalities associated with amyloid protein and of diseases or conditions associated with amyloid-like proteins. The compounds of the present invention can also be used in the treatment of ocular diseases associated with pathological abnormalities/changes in the tissues of the visual system.
    Type: Application
    Filed: September 30, 2014
    Publication date: January 22, 2015
    Inventors: Heiko Kroth, Wolfgang Froestl, Andrea Pfeifer, Andreas Muhs
  • Publication number: 20150011536
    Abstract: The present invention relates to the field of pharmaceutical chemistry, and particularly to an aza-benzo[f]azulen derivative (I) and an antitumor effect thereof Pharmacological tests show that the compound of the present invention has in vitro and in vivo antitumor activities, and can be developed into clinical drugs for treating or controlling diseases such as stomach cancer, lung cancer, liver cancer, breast cancer, colon cancer, prostate cancer, and oral cancer.
    Type: Application
    Filed: January 24, 2013
    Publication date: January 8, 2015
    Inventors: Xihan Wu, Liwu Fu, Dongmei Zhang, Yurong Wang
  • Publication number: 20150010549
    Abstract: The present invention relates to use of DHA analogs and their pharmaceutical compositions for treating ALS, by administering these compounds or pharmaceutical compositions to subjects in need thereof.
    Type: Application
    Filed: February 15, 2013
    Publication date: January 8, 2015
    Applicant: ANIDA PHARMA INC.
    Inventor: Per Gjorstrup
  • Patent number: 8927538
    Abstract: The present invention provides a compound of general formulae A 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 formulae 6a-g, 10a-o, 14a-g and 18a-o.
    Type: Grant
    Filed: December 3, 2010
    Date of Patent: January 6, 2015
    Assignee: Council of Scientific & Industrial Research
    Inventors: Ahmed Kamal, Rajesh V. C. R. N. C Shetti, Srinivasa K. Reddy, Adla Malla Reddy
  • Patent number: 8927537
    Abstract: The present invention is drawn to transdermal drug formulations, transdermal patches incorporating such formulations, as well as associated methods. The formulations can include about 0.3 wt % to about 5 wt % of a drug, such as alprazolam, about 4 wt % to about 30 wt % water, about 10 wt % to about 40 wt % glycerol, about 0.5 wt % to about 6 wt % oleyl alcohol. Other co-solvents and/or additives can be present to achieve a 100 wt % formulation.
    Type: Grant
    Filed: December 19, 2008
    Date of Patent: January 6, 2015
    Assignee: Nuvo Research Inc.
    Inventors: Sanjay Sharma, Kevin S. Warner, Jie Zhang, Guang Yan
  • Publication number: 20140378443
    Abstract: The present invention includes novel compositions useful for preventing or treating an HIV-1 infection in a subject in need thereof. The present invention further includes a novel method of preventing or treating an HIV-1 infection in a subject in need thereof, the method comprising administering to the subject an effective amount of a compound of the invention. In one embodiment, the subject is further administered at least one additional therapeutic agent.
    Type: Application
    Filed: June 20, 2014
    Publication date: December 25, 2014
    Inventors: William L. Jorgensen, Karen S. Anderson
  • Publication number: 20140371210
    Abstract: A method of rapid transbuccal delivery of an active agent into the bloodstream is provided. The method can include providing a pharmaceutical composition comprising the active agent, resin and a volatile solvent and, optionally, water. In some embodiments, the method achieves a Tmax 60 minutes or less, an onset of therapeutic effect of 60 minutes or less, and/or achieves therapeutic serum levels of the active agent within 60 minutes or less. Related compositions also are provided.
    Type: Application
    Filed: October 12, 2012
    Publication date: December 18, 2014
    Applicant: Jaleva Pharmaceuticals, LLC
    Inventor: Alex Battaglia
  • Publication number: 20140371157
    Abstract: Disclosed herein are novel methods and compositions useful for inhibiting interaction between a bromodomain protein and an immunoglobulin (Ig) regulatory element. The methods and compositions are particularly useful for downregulating expression of an oncogene translocated with an Ig locus, as well as for treating a cancer (e.g., hematological malignancy) characterized by increased expression of an oncogene which is translocated with an Ig locus.
    Type: Application
    Filed: August 30, 2012
    Publication date: December 18, 2014
    Applicants: DANA-FARBER CANCER INSTITUTE, INC., WHITEHEAD INSTITUTE FOR BIOMEDICAL RESEARCH
    Inventors: Richard A. Young, Peter B. Rahl, James Bradner
  • Patent number: 8906867
    Abstract: The production method prepares a solid preparation by dissolving water-insoluble and/or water indissolvable alkaline active pharmaceutical ingredient in an acidifier-containing acid solution to obtain medicated acid liquid; homogeneously mixing alkalizer, adjuvants and the medicated acid liquid, and carrying out wet granulation. The alkalizer is a reagent to reduce the acidity of the mixture of the alkalizer and the medicated acid liquid relative to the acidity of the medicated acid liquid. The preparation method avoids the problems in mechanical pulverization, such as environmental pollution, great loss and serious security risks. This method is simply operated, has high safety coefficient and is convenient for industrialized production. Also disclosed is the solid preparation produced by the method. The solid preparation produced by the method has better dissolution performance than that produced by prior art, and has better or at least equivalent stability and content uniformity with prior art.
    Type: Grant
    Filed: December 28, 2010
    Date of Patent: December 9, 2014
    Assignees: Shanghai Zhongxi Pharmaceutical Company, Shanghai Zhongxi Sunve Pharmaceutical Co., Ltd.
    Inventors: Siji Zheng, Bo Tan
  • Publication number: 20140357625
    Abstract: The invention relates to compound of the formula I or a salt thereof, wherein the substituents are as defined in the specification; to its preparation, to its use as medicament and to medicaments comprising it.
    Type: Application
    Filed: August 19, 2014
    Publication date: December 4, 2014
    Applicant: NOVARTIS AG
    Inventors: Dirk BEHNKE, David CARCACHE, Peter ERTL, Manuel KOLLER, David ORAIN
  • Publication number: 20140357586
    Abstract: The present invention provides solid pharmaceutical compositions for improved delivery of a wide variety of pharmaceutical active ingredients contained therein or separately administered. In one embodiment, the solid pharmaceutical composition includes a solid carrier, the solid carrier including a substrate and an encapsulation coat on the substrate. The encapsulation coat can include different combinations of pharmaceutical active ingredients, hydrophilic surfactant, lipophilic surfactants and triglycerides. In another embodiment, the solid pharmaceutical composition includes a solid carrier, the solid carrier being formed of different combinations of pharmaceutical active ingredients, hydrophilic surfactants, lipophilic surfactants and triglycerides. The compositions of the present invention can be used for improved delivery of hydrophilic or hydrophobic pharmaceutical active ingredients, such as drugs, nutritional agents, cosmeceuticals and diagnostic agents.
    Type: Application
    Filed: August 14, 2014
    Publication date: December 4, 2014
    Inventor: Mahesh V. Patel
  • Publication number: 20140356292
    Abstract: A method of evaluating memory/learning functions with the use of a model with glutamic acid N-methyl-D-aspartate (NMDA) type receptor hypofunction as an animal model for schizophrenia and with the use of reference memory task, wherein there has been found concrete means for detecting any differences in activity between typical anti-psychosis drugs and atypical anti-psychosis drugs is found. An in vivo animal model for screening of a therapeutic agent for improving cognitive dysfunction by schizophrenia is provided.
    Type: Application
    Filed: August 14, 2014
    Publication date: December 4, 2014
    Applicant: Sumitomo Dainippon Pharma Co., Ltd.
    Inventor: Takeo ISHIYAMA
  • Patent number: 8901113
    Abstract: Effective methods and compositions to deter abuse of pharmaceutical products (e.g., orally administered pharmaceutical products) including but not limited to immediate release, sustained or extended release and delayed release formulations for drugs subject to abuse comprising at least 10% by weight hydroxypropylcellulose; polyethylene oxide; and a disintegrant selected from the group consisting of crospovidone, sodium starch glycolate and croscarmellose sodium; wherein the ratio of hydroxypropylcellulose to polyethylene oxide on a weight basis is between about 10:1 and 1:10.
    Type: Grant
    Filed: September 29, 2010
    Date of Patent: December 2, 2014
    Assignee: Acura Pharmaceuticals, Inc.
    Inventors: Ronald L. Leech, Rachelle L. Hall Yung, Albert W. Brzeczko
  • Publication number: 20140349999
    Abstract: The present invention relates to the discovery of a novel opioid modulator effective in reducing pharmacologically induced weight gain associated with atypical antipsychotic use. The present invention provides methods of reducing antipsychotic induced weight gain, methods for suppressing food intake and reducing ghrelin levels induced by atypical antipsychotic medications in a patient.
    Type: Application
    Filed: June 5, 2014
    Publication date: November 27, 2014
    Inventors: Daniel Deaver, Mark Todtenkopf
  • Patent number: 8895545
    Abstract: In part, the present invention is directed to antibacterial compounds.
    Type: Grant
    Filed: October 4, 2012
    Date of Patent: November 25, 2014
    Assignee: Debiopharm International SA
    Inventors: Heinz W. Pauls, Jailall Ramnauth, Peter Sampson, Andras Toro