Bicyclo Ring System Having The Seven-membered Hetero Ring As One Of The Cyclos Patents (Class 514/221)
  • Publication number: 20150118301
    Abstract: Described are oral dosage forms that contain abuse-deterrent features and that contain core-shell polymers that include an active pharmaceutical ingredient, with particular examples including immediate release dosage forms that contain a drug that is commonly susceptible to abuse.
    Type: Application
    Filed: September 4, 2014
    Publication date: April 30, 2015
    Inventors: Dinesh K. Haswani, Derek V. Moe, Victoria A. O'Neill, Manuel A. Vega Zepeda
  • Publication number: 20150110874
    Abstract: A pharmaceutical composition for delivering lorazepam in a prolonged fashion is achieved with prolonged release lorazepam pharmaceutical beads. The composition typically contains sustained release lorazepam beads and delayed sustained release lorazepam beads. The composition can provide once daily dosing that maintains 24 hour therapeutic effect under steady state conditions.
    Type: Application
    Filed: January 8, 2014
    Publication date: April 23, 2015
    Inventors: Douglas A. Saltel, Michael Vachon
  • Publication number: 20150105378
    Abstract: The present invention provides compounds of Formula (I) or Formula (III): as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.
    Type: Application
    Filed: December 18, 2014
    Publication date: April 16, 2015
    Inventors: Lynn Abell, Leonard Adam, Cullen L. Cavallaro, Heather Finlay, Todd J. Friends, Jon J. Hangeland, Ji Jiang, R. Michael Lawrence, John Lloyd, Zulan Pi, George O. Tora, Jennifer X. Qiao, Carol Hui Hu, Tammy C. Wang
  • Publication number: 20150105375
    Abstract: This invention relates to 2-Aza-bicyclo[2.2.1]heptane-3-carboxylic acid (benzyl-cyano-methyl)-amides of formula 1 and their use as inhibitors of Cathepsin C, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of diseases connected with dipeptidyl peptidase I activity, e.g. respiratory diseases.
    Type: Application
    Filed: December 18, 2014
    Publication date: April 16, 2015
    Inventors: Ralf ANDERSKEWITZ, Florian BINDER, Matthias GRAUERT, Marc GRUNDL, Peter Wilhelm HAEBEL, Thorsten OOST, Alexander PAUTSCH, Stefan PETERS, Viktor VINTONYAK
  • 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: 20150099737
    Abstract: The invention is directed to novel pyrrolopyrimidine compounds of formula (1) wherein R1, R2y, R4, R8-R11, A and L are defined herein and to salts, including pharmaceutically acceptable salts thereof. The compounds of the present invention are CDK4/6 inhibitors and could be useful in the treatment of diseases and disorders mediated by CDK4/6, such as cancer, including mantle cell lymphoma, liposarcoma, non small cell lung cancer, melanoma, squamous cell esophageal cancer and breast cancer. The invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting CDK4/6 activity and to the treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
    Type: Application
    Filed: December 12, 2014
    Publication date: April 9, 2015
    Applicant: NOVARTIS AG
    Inventors: Christopher Thomas BRAIN, Young Shin CHO, John William GIRALDES, Bharat LAGU, Julian Roy LEVELL, Michael Joseph LUZZIO, Lawrence Blas PEREZ, Yaping WANG, Fan YANG
  • 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: 20150080353
    Abstract: The subject invention relates to compositions and methods useful for the in vivo delivery of substantially water-insoluble drugs, like taxol. The use of specific composition and preparation conditions enables the reproducible production of unusually water-soluble formulation, which can be sterile-filtered. The particulate system produced according to the invention can be converted into a re-dispersible dry powder comprising nanoparticles of drug. The innovation is also based on the fact that complementary partner is also an active drug but may have a different mode action with respect to primary molecule of the hybrid drug. The complementary molecule has multiple properties like antioxidant, antimicrobial, anti-inflammatory, anti-allergic, cox-2 inhibitors, etc. This results in a unique delivery system, in which part of the pharmacologically active agent is readily bioavailable.
    Type: Application
    Filed: November 6, 2014
    Publication date: March 19, 2015
    Inventors: Mewa SINGH, Maninder SANDHU
  • Publication number: 20150072974
    Abstract: Provided herein are heteroaryl compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. In one embodiment, the compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as CNS disorders and neurological disorders, including, but not limited to, e.g., psychosis, schizophrenia, depression, movement disorders, and Parkinson's disease.
    Type: Application
    Filed: May 9, 2013
    Publication date: March 12, 2015
    Inventors: Phillip G. Jones, Robert Lew, Kerry L. Spear, Linghong Xie
  • Publication number: 20150065471
    Abstract: The present invention is directed to a pharmaceutically acceptable crystalline addition salt of 5-[(1R)-2-({2-[4-({4-(2,2-difluoro-2-phenylethoxy)phenyl]ethyl}amino)-1-hydroxyethyl]-8-hydroxyquinolin-2(1H)-one, and (ii) a dicarboxylic acid, a sulfonic acid or a sulfimide, or a pharmaceutically acceptable solvate thereof.
    Type: Application
    Filed: March 28, 2013
    Publication date: March 5, 2015
    Inventors: Carlos Puig Duran, Francesc Carrera Carrera, Juan Bautista Pérez Garcia, Enrique Moyes Valles, Iolanda Marchueta Hereu
  • Publication number: 20150065465
    Abstract: The invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof. The Formula (I) imidazotriazines inhibit protein kinase activity thereby making them useful as anticancer agents.
    Type: Application
    Filed: November 4, 2014
    Publication date: March 5, 2015
    Inventors: Ashok Vinayak Purandare, Brian E. Fink, Ashvinikumar V. Gavai, Walter Lewis Johnson, Amy C. Hart, Liqi He, Tram N. Huynh, Jennifer Inghrim, Harold Mastalerz, Xiaopeng Sang, Christine M. Tarby, Honghe Wan, Wayne Vaccaro, Guifen Zhang, Yufen Zhao, Kurt Zimmermann
  • Publication number: 20150065491
    Abstract: The invention relates to pharmaceutical compositions comprising one or more benzodiazepine drugs for nasal administration, methods for producing and for using such compositions.
    Type: Application
    Filed: October 29, 2014
    Publication date: March 5, 2015
    Inventors: Steve Cartt, David Medeiros, Garry Thomas Gwozdz, Andrew Loxley, Mark Mitchnick, David Hale, Edward T. Maggio
  • Publication number: 20150056308
    Abstract: Methods and compositions for the treatment of treatment-resistant depression are described. More specifically, the invention demonstrates that intranasal administration of ketamine is effective to ameliorate the symptoms of depression in a patient who has not responded to an adequate trial of one antidepressant in the current episode and has recurrent or chronic depressive symptoms (>2 years).
    Type: Application
    Filed: June 17, 2014
    Publication date: February 26, 2015
    Inventors: Dennis S. Charney, Sanjay J. Mathew, Husseini K. Manji, Carlos A. Zarate, John H. Krystal
  • Patent number: 8962614
    Abstract: The invention includes compositions and methods of treatment of cancers susceptible to treatment with nucleotide analog chemotherapeutic agent, including cancers in which nucleotide analog resistant tumors have developed, including identifying a subject having cancer susceptible to treatment with a nucleotide analog chemotherapeutic agent and a mitotic disruptor/polo-like kinase (Plk) pathway inhibitor to a subject; and monitoring the subject for a reduction or stabilization of at least one sign or symptom of cancer.
    Type: Grant
    Filed: April 17, 2008
    Date of Patent: February 24, 2015
    Assignee: The Johns Hopkins University
    Inventors: Antonio Jimeno, Manuel Medina Hidalgo
  • Patent number: 8962615
    Abstract: The described invention relates to compounds (I) which modulate cell migration, and find use in, for example, wound healing, cancer progression and angiogenesis. All definitions as in claim 1.
    Type: Grant
    Filed: June 29, 2012
    Date of Patent: February 24, 2015
    Assignee: University of Dundee
    Inventors: Ana Maria Schor, Seth Lawrence Schor, Rodolfo Marquez, David George Norman
  • Publication number: 20150050241
    Abstract: The present invention is directed to methods and compositions employing 9-(4-hydroxy-2-(hydroxymethyl)butyl)guanine (“H2G”) or derivatives or analogs thereof for the treatment of viral diseases, as well as for the treatment of other conditions, including, but not limited to, cancer, chronic fatigue syndrome, Alzheimer's disease, multiple sclerosis and Graves' disease. The H2G or derivative or analog thereof can be administered in a pharmaceutical composition and can be administered with an additional antiviral therapeutic agent or another agent for the treatment of other conditions.
    Type: Application
    Filed: October 30, 2014
    Publication date: February 19, 2015
    Inventors: Fred VOLINSKY, Steven Daniel DONG
  • Publication number: 20150038495
    Abstract: To provide a cancer pain therapeutic and/or prophylactic agent which can be administered to a patient for a long period of time from the early stage to the final stage of the cancer pain therapy, instead of conventional non-opioid analgesic agents or opioid analgesic agents. The cancer pain therapeutic and/or prophylactic agent containing, as an active ingredient, a 1,5-benzodiazepine derivative represented by formula (1): (wherein R1 represents a C1-6 alkyl group, R2 represents a phenyl group or a cyclohexyl group, and Y represents a single bond or a C1-4 an alkylene group) or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: September 24, 2014
    Publication date: February 5, 2015
    Applicant: Zeria Pharmaceutical Co., Ltd.
    Inventors: Koji YOSHINAGA, Hiroki Hamano, Takayuki Hori
  • Patent number: 8946203
    Abstract: The present invention relates to compounds of formula (I): wherein R1 to R3, A, X and n are as defined herein. The compounds of formula (I) are useful as inhibitors of leukotriene A4 hydrolase (LTA4H) and treating LTA4H related disorder. The present invention also relates to pharmaceutical compositions comprising the compounds of formula (I), methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.
    Type: Grant
    Filed: March 5, 2013
    Date of Patent: February 3, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Asitha Abeywardane, Steven Richard Brunette, Michael J. Burke, Suresh R. Kapadia, Thomas Martin Kirrane, Matthew Russell Netherton, Hossein Razavi, Sonia Rodriguez, Anjan Saha, Robert Sibley, Lana Louise Smith-Keenan, Hidenori Takahashi, Michael Robert Turner, Jiang-Ping Wu, Erick Richard Roush Young, Qiang Zhang, Qing Zhang, Renee M. Zindell
  • 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
  • Patent number: 8946209
    Abstract: Compositions and methods for the treatment of urinary calculi and fragments thereof are provided. Compositions and methods for the prevention and/or treatment of renal and urinary colic caused by urinary calculi or fragments are also provided. Such compositions and methods provide locally effective amounts of diazepam sufficient to prevent formation of and/or expel ureteral calculi and fragments thereof and thus prevent and/or treat pain associated with calculi and fragments thereof.
    Type: Grant
    Filed: April 28, 2010
    Date of Patent: February 3, 2015
    Assignee: OptMed, Inc.
    Inventor: Daniel Brookoff
  • Publication number: 20150030683
    Abstract: In certain embodiments the methods of preventing or delaying the onset of a pre-Alzheimer's condition and/or cognitive dysfunction, and/or ameliorating one or more symptoms of a pre-Alzheimer's cognitive dysfunction, and/or preventing or delaying the progression of a pre-Alzheimer's condition or cognitive dysfunction to Alzheimer's disease, and/or of promoting the processing of amyloid precursor protein (APP) by the non-amyloidogenic pathway are provided. In certain embodiments the methods involve administering, or causing to be administered, to a subject in need thereof certain formulations comprising or more active agent(s) selected from the group consisting of tropisetron disulfiram, honokiol, nimetazepam, and/or derivatives or analogs thereof.
    Type: Application
    Filed: February 15, 2013
    Publication date: January 29, 2015
    Inventors: Varghese John, Dale E. Bredesen, Stelios Tzannis
  • Publication number: 20150025064
    Abstract: The present invention relates to novel benzodiazepinone compounds of Formulae (I) wherein R1, R2, R4, R6, R7, R8, R9, and R10 are as defined herein. The invention also relates to pharmaceutical compositions containing such compounds, methods of use of such compounds and compositions, and methods for preparing the compounds and compositions. The compounds are Group II metabotropic glutamate antagonists or allosteric modulators and are useful for the treatment of a variety of CNS disorders.
    Type: Application
    Filed: August 29, 2012
    Publication date: January 22, 2015
    Applicant: Sanford-Burnham Medical Research Institute
    Inventors: John Howard Hutchinson, Leo Bleicher, Nick Cosford, Robert John Ardecky, Jiwen Zou
  • Publication number: 20150018345
    Abstract: The present invention relates to a compound according to formula (A) wherein n is 1 or 2; R1 and R2 are independently hydrogen, C1-4 alkyl, C1-4 haloalkyl, C1-4 alkoxy, CD3 or halogen; R3 is hydrogen, C(?O)OR7 or C1-4 alkyl optionally substituted with hydroxy or NR8R9; R4 is hydrogen or oxo; R5 and R6 are independently hydrogen, hydroxy, NR8R9, C(?O)R7, C(?O)OR7, C(?O)NR8R9, C1-4 alkyl, wherein said C1-4 alkyl is optionally substituted with hydroxy, NR8R9 or a 5- or 6-membered heterocyclic ring, wherein said 5- or 6-membered heterocyclic ring is optionally substituted with C1-4 alkyl or C(?O)R7; or R5 and R6, together with the carbon atom to which they are attached, form ?CH2 or a 5- or 6-membered heterocycloalkyl, wherein said heterocycloalkyl is optionally substituted with C1-4 alkyl; R7 is hydrogen or C1-4 alkyl; R8 and R9 are independently hydrogen or C1-4 alkyl, or R8 and R9, together with the nitrogen atom to which they are attached, form a 5- or 6-membered heterocyclic ring, or a pharmaceutically accep
    Type: Application
    Filed: February 20, 2013
    Publication date: January 15, 2015
    Inventors: Morten Dahl Sørensen, Romano Di Fabio, Alfonso Pozzan, Maria Pia Catalani, Haakon Bladh, Jakob Felding
  • Publication number: 20150011537
    Abstract: The present invention describes a unique antiviral screen system. The assay is based on quantitatively monitoring viral activation of host cell beta-interferon (IFN-?) gene expression in a HEK293-derived reporter cell line expressing a firefly luciferase gene under the control of a human IFN-? promoter. Unlike the traditional high throughput antiviral assays that measure either the reduction of viral components/yields or cytopathic effect, the readout of the reporter assay in the present invention is the virus-induced host cellular innate immune response. Hence, the assay allows for identification of compounds that inhibit virus infection. In addition, because induction of IFN is one of the most common attributes of viruses, the assay is applicable to all the viruses that are able to infect the reporter cell line and induce IFN-? expression.
    Type: Application
    Filed: February 22, 2013
    Publication date: January 8, 2015
    Inventors: Andrea Cuconati, Jinhong Chang, Timothy M. Block, Ju-Tao Guo
  • Patent number: 8927484
    Abstract: The present application includes novel inhibitors of HCV, compositions containing such compounds, therapeutic methods that include the administration of such compounds.
    Type: Grant
    Filed: December 1, 2010
    Date of Patent: January 6, 2015
    Assignee: Gilead Sciences, Inc.
    Inventors: Zhenhong R. Cai, Michael O'Neil Hanrahan Clarke, Edward Doerffler, Mingzhe Ji, Choung U. Kim, Hyung-jung Pyun, Xiaoning C. Sheng, Qiaoyin Wu
  • Publication number: 20150005260
    Abstract: The present invention relates to methods and kits for detecting diastolic dysfunction in subjects without clinical signs of heart failure.
    Type: Application
    Filed: January 2, 2013
    Publication date: January 1, 2015
    Inventors: Faiez Zannad, Patrick Rossignol
  • Publication number: 20140364423
    Abstract: This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.
    Type: Application
    Filed: August 26, 2014
    Publication date: December 11, 2014
    Inventors: Wei-Sheng Huang, Ranny M. Thomas
  • 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
  • Patent number: 8906913
    Abstract: The present invention relates to novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers including R and S isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The invention also relates to processes for the synthesis of novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers, polymorphs, prodrugs, metabolites, salts or solvates thereof.
    Type: Grant
    Filed: June 22, 2010
    Date of Patent: December 9, 2014
    Assignee: Panacea Biotec Limited
    Inventors: Rajesh Jain, Sanjay Trehan, Jagattaran Das, Gurmeet Kaur, Sandeep Kanwar, Nishan Singh, Gurmeet Kaur Nanda, Sitaram Kumar Magadi, Sudhir Kumar Sharma
  • Publication number: 20140357605
    Abstract: Disclosed are compounds of Formula (I) or prodrugs thereof; wherein: R1 is —CH2CF3 or —CH2CH2CF3; R2 is —CH2CF3, —CH2CH2CF3, or —CH2CH2CH2CF3; R3 is H or —CH3; each Ra is independently F, Cl, —CN, —OCH3, and/or —NHCH2CH2OCH3; and z is zero, 1, or 2. Also disclosed are methods of using such compounds to inhibit the Notch receptor, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as cancer.
    Type: Application
    Filed: July 28, 2014
    Publication date: December 4, 2014
    Inventors: Ashvinikumar V. Gavai, Claude A. Quesnelle, Soong-Hoon Kim
  • Publication number: 20140357617
    Abstract: The invention relates to novel heterocyclic acrylamide compounds (I), to the preparation of the compounds and intermediates used therein, to the use of the compounds as antibacterial medicaments and pharmaceutical compositions containing the compounds.
    Type: Application
    Filed: August 20, 2014
    Publication date: December 4, 2014
    Applicant: FAB PHARMA S.A.S.
    Inventors: Vincent Gerusz, Sonia Escaich, Mayalen Oxoby, Alexis Denis
  • 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
  • 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
  • Patent number: 8895546
    Abstract: The invention relates to pharmaceutical compositions comprising one or more benzodiazepine drugs for nasal administration, methods for producing and for using such compositions.
    Type: Grant
    Filed: June 13, 2012
    Date of Patent: November 25, 2014
    Assignee: Hale Biopharma Ventures, LLC
    Inventors: Steve Cartt, David Medeiros, Garry Thomas Gwozdz, Andrew Loxley, Mark Mitchnick, David Hale, Edward T. Maggio
  • Publication number: 20140343032
    Abstract: The invention provides novel compounds having the general formula: wherein R1, R2, R3 and R4 are as defined in the description and in the claims, as well as or pharmaceutically acceptable salts, or tautomerism isomers, or enantiomers, or diastereomers thereof. The invention also contains compositions including the compounds and methods of using the compounds.
    Type: Application
    Filed: May 16, 2014
    Publication date: November 20, 2014
    Applicant: HOFFMANN-LA ROCHE INC.
    Inventors: Lei Guo, Taishan Hu, Yimin Hu, Buelent Kocer, Buyu Kou, Gangqin Li, Xianfeng Lin, Haixia Liu, Hong Shen, Houguang Shi, Guolong Wu, Zhisen Zhang, Mingwei Zhou, Wei Zhu
  • Publication number: 20140336183
    Abstract: A method and composition for the treatment of ischemic neuronal reperfusion injury are provided. The composition may include at least a benzodiazepine class material. In another form, the composition may include at least two components selected from the group consisting of an antagonist of the type 3 ryanodine receptor, an NMDA blocker (antagonist), and a benzodiazepine class material which can be administered for ischemic neuronal reperfusion injury. In one form, all three components may be used.
    Type: Application
    Filed: May 8, 2014
    Publication date: November 13, 2014
    Inventors: Harpal S. Mangat, Pradeep K. Karla
  • Publication number: 20140336153
    Abstract: The present invention provides substituted pyridine derivatives of formula (I), which may be therapeutically useful as as anti-bacterial agents, more particularly FabI inhibitors. Formula (I) in which R1 to R5 and L have the meanings given in the specification, and pharmaceutically acceptable salts thereof that are useful in the treatment and prevention in diseases or disorder, in particular their use in diseases or disorder where there is an advantage anti-bacterial agents, more particularly FabI inhibitors. The present invention also provides methods for synthesizing and administering the FabI inhibitor compounds. The present invention also provides pharmaceutical formulations comprising at least one of the FabI inhibitor compounds together with a pharmaceutically acceptable carrier, diluent or excipient therefor.
    Type: Application
    Filed: November 29, 2012
    Publication date: November 13, 2014
    Inventors: Mohamed Takhi, Subramanya Hosahalli, Sunil Kumar Panigrahi, Muni Kumar Mahadari, Chandrashekar Reddy Kottam, Noorsaadah Abd Rahman, Rohana Yusof
  • Publication number: 20140329805
    Abstract: The present invention provides analogs and derivatives of thalidomide which inhibit cancer and angiogenesis. The present invention further provides compounds which disrupt microtubule polymerization. The present further provides methods of treating cancers comprising mutant p53.
    Type: Application
    Filed: January 28, 2014
    Publication date: November 6, 2014
    Applicant: University of Virginia Patent Foundation
    Inventor: Milton L. Brown
  • Publication number: 20140323473
    Abstract: Organophosphate (OP) nerve agents and pesticides are potent inhibitors of acetylcholinesterase (AChE). Though oxime nucleophiles can reactivate an AChE-phosphyl adduct, the adduct can undergo a reaction called aging, leading to an aged-AChE adduct. The invention provides compounds and methods that can be used to reactivate an aged-AChE adduct. Such compounds and methods are useful to counteract organophosphorus poisoning.
    Type: Application
    Filed: January 24, 2014
    Publication date: October 30, 2014
    Applicant: University of Iowa Research Foundation
    Inventors: Daniel Quinn, Joseph John Topczewski
  • Patent number: 8871756
    Abstract: A compound of formula (I) as well as pharmaceutically acceptable salt thereof, wherein R1 to R10, A, Q, X and Y are as defined in the specification and claims, and their use as a pharmaceutical for the treatment or prophylaxis of respiratory syncytial virus disease.
    Type: Grant
    Filed: July 30, 2012
    Date of Patent: October 28, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Li Chen, Lichun Feng, Song Feng, Lu Gao, Tao Guo, Mengwei Huang, Chungen Liang, Yongfu Liu, Lisha Wang, Jason Christopher Wong, Jim Zhen Wu, Xihan Wu, Hongying Yun, Xiufang Zheng
  • Publication number: 20140315881
    Abstract: The present invention relates to novel retinoid-related orphan receptor gamma (ROR?) modulators and their use in the treatment of diseases mediated by ROR?.
    Type: Application
    Filed: July 27, 2012
    Publication date: October 23, 2014
    Inventors: Erkan Baloglu, Gary J. Bohnert, Shomir GHOSH, Mercedes Lobera, Darby R. Schmidt, Leonard Sung
  • Publication number: 20140315892
    Abstract: The present invention relates to (+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane and pharmaceutically acceptable salts thereof, compositions comprising (+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane or a pharmaceutically acceptable salt thereof, and methods for treating or preventing an alcohol-related or addictive disorder. The (+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.
    Type: Application
    Filed: January 31, 2014
    Publication date: October 23, 2014
    Inventors: Anthony Alexander McKinney, Franklin Porter Bymaster
  • Patent number: 8865704
    Abstract: The present invention relates to known and novel compounds of formula (I) as herein described and pharmaceutical compositions thereof. The compounds of formula (I) have inhibitory effect on the Wnt pathway and are therefore useful in the preparation of a medicament, in particular for the treatment of cancer.
    Type: Grant
    Filed: October 6, 2010
    Date of Patent: October 21, 2014
    Assignee: Siena Biotech S.p.A.
    Inventors: Maurizio Varrone, Arianna Nencini, Joanna Margaret Quinn, Andrea Caricasole, Annette Cornelia Bakker, Giovanni Gaviraghi, Massimilano Salerno
  • Publication number: 20140309217
    Abstract: Disclosed herein are compositions and methods for the treatment of otic disorders with CNS modulating agent compositions and compositions administered locally to an individual afflicted with an otic disorder, through direct application of these compositions and compositions onto or via perfusion into the targeted auris structure(s).
    Type: Application
    Filed: June 9, 2014
    Publication date: October 16, 2014
    Inventors: Jay Lichter, Andrew M. Trammel, Fabrice Piu, Qiang Ye, Michael Christopher Scaife, Benedikt Vollrath, Sergio G. Duron, Luis A. Dellamary, Carl Lebel, Jeffrey P. Harris
  • Publication number: 20140308282
    Abstract: Benzimidazoles of formula (I): wherein: A is 5- to 12-membered aryl or 5- to 12-membered heteroaryl, each of which is unsubstituted or substituted; Y is a single bond, —(CH2)p—, —X—, —CH2—X—, or —X—CH2—; X is —O—, —S—, —N(R2)—, >C?O, >S(?O), >S(?O)2, —O—C(?O)—, —C(?O)—O—, N(R2)—C(?O)—, or —C(?O)—N(R2)—; each L is independently a single bond, C1-3alkylene, C2-3alkenylene or C2-3alkynylene; R1 is C1-6alkyl, C2-6alkenyl or C2-6alkynyl, each of which is unsubstituted or substituted; each Z is independently —N(R2)2, —OR2, —SR2, —S(?O)R2, —S(?O)2R2; each R2 is independently hydrogen, C1-6alkyl, C2-6alkenyl or C2-6 alkynyl, wherein said alkyl, alkenyl and alkynyl groups are unsubstituted or substituted; m is 0, 1, 2, or 3; n is 1, 2, or 3; and p is 1, 2, or 3; and the pharmaceutically acceptable salt thereof are inhibitors of RSV and can therefore be used to treat or prevent an RSV infection.
    Type: Application
    Filed: November 12, 2012
    Publication date: October 16, 2014
    Applicant: re: Viral Ltd
    Inventors: Stuart Cockerill, Christopher Pilkington, James Lumley, Richard Angell, Neil Mathews
  • Publication number: 20140309181
    Abstract: Small compounds that modulate the expression of and/or function of sodium channel, voltage-gated, alpha subunit (SCNxA) are presented. Pharmaceutical compositions containing such small molecules and their use in treating diseases and disorders associated with the expression of SCNxA are also presented.
    Type: Application
    Filed: August 28, 2012
    Publication date: October 16, 2014
    Applicant: CuRNA, Inc.
    Inventors: Joseph Collard, Olga Khorkova Sherman, Jane H. Hsiao
  • Patent number: 8859537
    Abstract: This invention relates to the use of a ligand of the 5-HT4 receptor or of a pharmaceutically acceptable salt of this ligand and to a nucleic acid coding for a 5-HT4 receptor or of a functionally equivalent receptor for a drug for treating and/or preventing a pathology associated with an obsessional behavior such as anorexia, bulimia and the addiction to drugs of abuse or obesity. The invention also relates to a method for identifying a compound that is biologically active in the treatment and/or the prevention of a pathology associated with an obsessional conduct or obesity including: a) placing the 5-HT4 receptor or a functionally equivalent receptor in contact with this biologically active compound, and b) the determination of whether this biologically active compound is capable of modulating the basal activity of the 5-HT4 receptor or of a functionally equivalent receptor.
    Type: Grant
    Filed: April 29, 2005
    Date of Patent: October 14, 2014
    Assignee: Centre National de la Recherche Scientifique-CNRS
    Inventor: Valerie Compan
  • Patent number: 8859538
    Abstract: The present invention provides a method of prophylaxis, treatment or inhibition of a cannabinoid receptor-associated disease, disorder or condition in a mammalian subject, the method comprising administering to the subject a compound having the structure of formula I or a pharmaceutically acceptable salt, acid salt, hydrate or stereoisomer thereof, wherein the cannabinoid receptor-associated disease, disorder or condition is pain or an inflammatory disease, disorder or condition, and wherein formula I is as follows: wherein Rb, Rc, Z, Y and m are defined in the specification.
    Type: Grant
    Filed: August 26, 2010
    Date of Patent: October 14, 2014
    Assignee: Cara Therapeutics, Inc.
    Inventors: R. Paul Beckett, Richard Foster, Christelle Henault, Janet L. Ralbovsky, Carla M. Gauss, Gary G. Gustafson, Zhiyong Luo, Ann-Marie Campbell, Tatiana E. Shelekhin
  • Publication number: 20140302141
    Abstract: This invention pertains to a multi-layered tablet for a triple combination release of active agents to an environment of use. More particularly, the invention pertains to a multi-layered tablet (1) comprising two external drug-containing layers (2 and 3) in stacked arrangement with respect to and on opposite sides of an oral dosage form (4) that provides a triple combination release of at least one active agent. In one embodiment of the invention the dosage form is an osmotic device. In another embodiment of the invention the dosage form is a gastro-resistant coated core. In yet another embodiment of the invention the dosage form is a matrix tablet. In a different embodiment the dosage form is a hard capsule.
    Type: Application
    Filed: February 24, 2014
    Publication date: October 9, 2014
    Applicant: OSMOTICA KERESKEDELMI ES SZOLGALTATO KFT
    Inventors: FERNANDO G. TONEGUZZO, GLENN A. MEYER, Marcelo A. RICCI, Marcelo A. COPPARI, ANA C. PASTINI, GUSTAVO A. FISCHBEIN
  • Patent number: 8853204
    Abstract: A pharmaceutical composition which comprises a pharmaceutically acceptable carrier or diluent and: (a) an inhibitor of the RSV fusion protein; and (b) a benzodiazepine derivative capable of inhibiting RSV replication is found to be highly active against RSV.
    Type: Grant
    Filed: March 18, 2005
    Date of Patent: October 7, 2014
    Assignee: Arrow Therapeutics Limited
    Inventors: Kenneth Powell, Richard Kelsey, Malcolm Carter, Dagmar Alber, Lara Wilson, Elisa Henderson, Phil Chambers, Debra Taylor, Stan Tyms, Verity Dowdell