C=x Bonded Directly To The Piperidine Ring (x Is Chalcogen) Patents (Class 514/330)
  • Patent number: 8450345
    Abstract: Provided are methods of treating or preventing viral infections caused by or associated with a Dengue virus using iminosugars.
    Type: Grant
    Filed: February 22, 2010
    Date of Patent: May 28, 2013
    Assignees: The Chancellor, Masters and Scholars of the University of Oxford, United Therapeutics Corporation
    Inventors: Urban Ramstedt, Brennan Klose, Nicole Zitzmann, Raymond A. Dwek, Terry D. Butters
  • Patent number: 8449863
    Abstract: Uncoated particles of reversed cubic phase or reversed hexagonal phase material containing an active disposed within are provided. The uncoated particles have an ionic charge that is sufficient to stabilize them in dispersion in a liquid, e.g. a polar solvent. The active that is disposed within the particles may be, for example, a pharmaceutical or nutriceutical compound.
    Type: Grant
    Filed: March 25, 2010
    Date of Patent: May 28, 2013
    Assignee: Lyotropic Therapeutics, Inc.
    Inventor: David Anderson
  • Patent number: 8445515
    Abstract: Compounds are provided that are modulators of the C5a receptor. The compounds are substituted piperidines and are useful in pharmaceutical compositions, methods for the treatment of diseases and disorders involving the pathologic activation of C5a receptors.
    Type: Grant
    Filed: December 21, 2009
    Date of Patent: May 21, 2013
    Assignee: Chemocentryx, Inc.
    Inventors: Pingchen Fan, Kevin Lloyd Greenman, Manmohan Reddy Leleti, Yandong Li, Jay Powers, Hiroko Tanaka, Ju Yang, Yibin Zeng
  • Publication number: 20130109718
    Abstract: This invention relates to novel 1-cycloalkyl- or 1-heterocyclyl-hydroxyimino-3-phenyl-propanes of the formula wherein R1 to R7 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are GPBAR1 agonists and may therefore be useful as medicaments for the treatment of diseases such as type II diabetes.
    Type: Application
    Filed: October 24, 2012
    Publication date: May 2, 2013
    Applicant: Hoffmann-La Roche Inc.
    Inventor: Hoffmann-La Roche Inc.
  • Publication number: 20130109698
    Abstract: The present invention includes a method of inhibiting, suppressing or preventing retroviral infection in a subject in need thereof, comprising administering to the subject a pharmaceutical composition comprising one or more of the compounds of the invention.
    Type: Application
    Filed: April 25, 2011
    Publication date: May 2, 2013
    Inventor: Simon Cocklin
  • Publication number: 20130085162
    Abstract: Amido compounds are disclosed that have a formula represented by the following: and wherein n1, n2, R1a, R1b, R2, R3, R4, R5, and R6 are as described herein. The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, inflammatory conditions, autoimmune disorders, cancer, and graft-versus-host disease.
    Type: Application
    Filed: March 11, 2011
    Publication date: April 4, 2013
    Inventors: Dan Littman, Jun R. Huh, Wenwei Huang, Ruili Huang, Erika Elaine Englund
  • Patent number: 8410138
    Abstract: Compositions and methods for treatment and prevention of disorders and conditions characterized by reduced TGF-? signaling are described.
    Type: Grant
    Filed: December 12, 2011
    Date of Patent: April 2, 2013
    Assignees: The Board of Trustees of the Leland Stanford Junior University, SRI International
    Inventors: Anton Wyss-Coray, Mary J. Tanga
  • Patent number: 8410140
    Abstract: The present invention relates to compositions and methods use in pain reduction, including but not limited to, peripheral nerve blocks. In particular, the present invention relates to compositions and methods for the administration of perineural dexmedetomidine and ropivacaine in combination for increased antinociception in peripheral nerve blocks. In addition, this invention relates to any use of dexmedetomidine alone or in combination with other agents for the purpose of decreasing inflammation around peripheral nerves, thereby decreasing the potential for peripheral nerve injury. Further, the invention relates to the use of dexmedetomidine to reduce inflammation in the muscle to lessen or prevent muscle damage.
    Type: Grant
    Filed: June 1, 2010
    Date of Patent: April 2, 2013
    Assignee: The Regents of the University of Michigan
    Inventor: Chad M. Brummett
  • Publication number: 20130079371
    Abstract: The present invention relates to a gelling bioadhesive pharmaceutical composition comprising one or more local anaesthetics in base form and which is suitable for topical administration. The compositions have anisotropic organic phase behaviour that admits swelling at administration site with excess water.
    Type: Application
    Filed: March 31, 2011
    Publication date: March 28, 2013
    Applicant: PHARMANEST AB
    Inventors: Mark Sundberg, Arne Brodin, Jonas Gustafsson
  • Publication number: 20130079344
    Abstract: Solutions for perioperative intraocular application by continuous irrigation during ophthalmologic procedures are provided. These solutions include multiple agents that act to inhibit inflammation, inhibit pain, effect mydriasis (dilation of the pupil), and/or decrease intraocular pressure, wherein the multiple agents are selected to target multiple molecular targets to achieve multiple differing physiologic functions, and are included in dilute concentrations in a balanced salt solution carrier.
    Type: Application
    Filed: March 14, 2012
    Publication date: March 28, 2013
    Applicant: OMEROS CORPORATION
    Inventors: Gregory A. Demopulos, Pamela Pierce Palmer, Jeffrey M. Herz
  • Publication number: 20130071450
    Abstract: The present disclosure provides hydrogels that are suitable for drug delivery. In embodiments, hydrogels of the present disclosure may be used for transdermal delivery of bioactive agents, including drugs. The hydrogels of the present disclosure may also be useful as conductive compositions for use with electrodes.
    Type: Application
    Filed: November 15, 2012
    Publication date: March 21, 2013
    Applicant: COVIDIEN LP
    Inventor: Covidien LP
  • Publication number: 20130065916
    Abstract: The invention provides crystalline solid forms of (S)-4-((2S,3S)-7-carbamoyl-1,1-diethyl-3-methoxy-1,2,3,4-tetrahydronaphthalen-2-ylamino)-2-cyclohexylmethyl-butyric acid. The invention also provides pharmaceutical compositions comprising such crystalline solid forms, methods of using such crystalline solid forms to treat diseases associated with mu opioid receptor activity, and processes useful for preparing such crystalline solid forms.
    Type: Application
    Filed: October 29, 2012
    Publication date: March 14, 2013
    Applicant: THERAVANCE, INC.
    Inventors: Sean M. Dalziel, Miroslav Rapta
  • Publication number: 20130058880
    Abstract: Compositions, kits and methods of preparing a biocompatible film for cosmetic or medical uses are disclosed. The compositions or kits contain polyvinyl acetal (PVA), siloxane and a solvent. The siloxane can have a hydrophilic group. Once the solvent content is reduced, for instance, by evaporation, the mixture of PVA and siloxane is solidified, forming a film. The compositions and kits, optionally, further include one or more of an antimicrobial agent, a pigment, an anti-inflammatory agent, an anesthetic agent or a hemostatic agent. Such a film can be used, for example, in the form of an antimicrobial sealant, a liquid bandage, body paints, scar camouflage, water-proof sun block, makeup sealer, or antimicrobial wipe or spray.
    Type: Application
    Filed: May 9, 2011
    Publication date: March 7, 2013
    Inventor: Shaosheng Dong
  • Patent number: 8389730
    Abstract: Provided are small-molecule Trp-p8 modulators, including Trp-p8 agonists and Trp-p8 antagonists, and compositions comprising small-molecule Trp-p8 agonists as well as methods for identifying and characterizing novel small-molecule Trp-p8 modulators and methods for decreasing viability and/or inhibiting growth of Trp-p8 expressing cells, methods for activating Trp-p8-mediated cation influx, methods for stimulating apoptosis and/or necrosis, and related methods for the treatment of diseases, including cancers such as lung, breast, colon, and/or prostate cancers as well as other diseases, such as benign prostatic hyperplasia, that are associated with Trp-p8 expression.
    Type: Grant
    Filed: May 25, 2011
    Date of Patent: March 5, 2013
    Assignee: Dendreon Corporation
    Inventors: Sateesh K. Natarajan, Ofir Moreno, Thomas J. Graddis, David F. Duncan, Reiner Laus, Feng Chen
  • Publication number: 20130053417
    Abstract: The invention provides a compound that is a CETP activity inhibitor. The compound can increase HDL and at the same time decrease LDL through selective inhibition of CETP activity, the invention also provides for the use of the compound to prevent or treat atherosclerosis or hyperlipidemia.
    Type: Application
    Filed: March 21, 2012
    Publication date: February 28, 2013
    Applicant: JAPAN TOBACCO INC.
    Inventors: Hisashi Shinkai, Kimiya Maeda, Hiroshi Okamoto
  • Publication number: 20130053385
    Abstract: The use of a compound of formula I wherein the substituents are as defined in claim 1, or compositions containing them in controlling insects, acarines, nematodes or molluscs.
    Type: Application
    Filed: December 7, 2010
    Publication date: February 28, 2013
    Applicants: SYNGENTA LIMITED, SYNGENTA CROP PROTECTION LLC
    Inventors: Stephane Andre Marie Jeanmart, Russell Viner, John Benjamin Taylor, William Guy Whittingham, Jeffrey Steven Wailes, Sarah Margaret Targett, Christopher John Mathews, Michel Muehlebach
  • Publication number: 20130045977
    Abstract: The present invention provides a compound represented by the following formula (I) or a physiologically acceptable salt thereof, and use thereof for the prophylaxis or treatment of TGF-?-related diseases: wherein Y is a hydrogen atom and the like; R2 is and the like; R3 is —NR8—R9— and the like; R4, R5, R6 and R7 are the same or different and each is a hydrogen atom and the like; and X is and the like.
    Type: Application
    Filed: February 17, 2011
    Publication date: February 21, 2013
    Applicant: KYOTO UNIVERSITY
    Inventors: Hideaki Kakeya, Akira Hattori, Yasuaki Takasu, Nobutaka Fujii, Shinya Oishi, Soichi Kojima, Mitsuko Hara
  • Publication number: 20130040932
    Abstract: A series of substituted aryl sulfone derivatives represented by Formula I, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, calcium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, urinary incontinence, itchiness, allergic dermatitis, epilepsy, diabetic neuropathy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, sleep disorder, bipolar disorder and stroke, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds.
    Type: Application
    Filed: September 24, 2012
    Publication date: February 14, 2013
    Applicants: Neuromed Pharmaceuticals Ltd., Merck Sharp & Dohme Corp.
    Inventors: Merck Sharp & Dohme Corp., Neuromed Pharmaceuticals Ltd.
  • Publication number: 20130028843
    Abstract: The present invention relates to the crystal structure of the serine protease kallikrein 7 and to the use of this crystal structure in drug discovery. The present invention also relates to compounds binding specifically to this active site of kallikrein 7.
    Type: Application
    Filed: October 10, 2012
    Publication date: January 31, 2013
    Applicant: NOVARTIS AG
    Inventor: NOVARTIS AG
  • Publication number: 20130023527
    Abstract: The present invention relates to certain 1,2,3-trisubstituted aryl and heteroaryl derivatives of Formula (Ia) that are modulators of metabolism. Accordingly, compounds of the present invention are useful in the prophylaxis or treatment of metabolic disorders and complications thereof, such as, diabetes and obesity.
    Type: Application
    Filed: September 14, 2012
    Publication date: January 24, 2013
    Applicant: ARENA PHARMACEUTICALS, INC.
    Inventors: Robert M. Jones, Graeme Semple, Beatriz Fioravanti, Guilherme Pereira, Imelda Calderon, Jane Laguerta Uy, Kameshwari Duvvuri, Jin Sun Karoline Choi, Yifeng Xiong, Vibha Dave, Mihai D. Azimioara
  • Publication number: 20130023565
    Abstract: The present invention relates to polypeptide fragments comprising an amino-terminal fragment of the PA subunit of a viral RNA-dependent RNA polymerase possessing endonuclease activity, wherein said PA subunit is from Influenza A 2009 pan-demic H1N1 virus or is a variant thereof. This invention also relates to (i) crystals of the polypeptide fragments which are suitable for structure determination of said polypeptide fragments using X-ray crystallography and (ii) computational methods using the structural coordinates of said polypeptide to screen for and design compounds that modulate, preferably inhibit the endonucleolytically active site within the polypeptide fragment. In addition, this invention relates to methods identifying compounds that bind to the PA polypeptide fragments possessing endonuclease activity and preferably inhibit said endonucleolytic activity, preferably in a high throughput setting.
    Type: Application
    Filed: March 15, 2011
    Publication date: January 24, 2013
    Applicant: European Molecular Biology Laboratory
    Inventors: Stephen Cusack, Eva Kowalinski, Chloe Zubieta
  • Publication number: 20130023516
    Abstract: 4-(azacycloalkyl)benzene-1,3-diol compounds are described corresponding to general formula (I) below: Also described, are compositions including the same, processes for preparation thereof and uses thereof in pharmaceutical or cosmetic compositions to treat pigmentary disorders.
    Type: Application
    Filed: September 12, 2012
    Publication date: January 24, 2013
    Applicant: Galderma Research & Development
    Inventors: Jean-Guy BOITEAU, Karine Bouquet, Sandrine Talano, Corinne Millois Barbuis
  • Patent number: 8357700
    Abstract: The present invention is directed to 2,3-disubstituted piperidine amide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
    Type: Grant
    Filed: October 15, 2009
    Date of Patent: January 22, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Christopher D. Cox, Broc Flores, John D. Schreier
  • Patent number: 8343968
    Abstract: The present invention relates to piperidine-based renin inhibitor compounds having carboxylate or carboxylic acid terminal groups, and their use in treating cardiovascular events and renal insufficiency.
    Type: Grant
    Filed: May 23, 2008
    Date of Patent: January 1, 2013
    Assignee: Merck Canada Inc.
    Inventors: Tom Yao-Hsiang Wu, Helene Juteau, Michel Gallant, Daniel Dube, Patrick Roy, Renee Aspiotis, Erich I. Grimm, Sebastien Laliberte, Austin Chen
  • Publication number: 20120308519
    Abstract: Described herein are 4-methyl-piperazine-1-carbothioic acid amide derivatives and analogs, as well as compositions containing the same, for the treatment or prophylaxis of viral infections and diseases associated therewith, particularly those viral infections and associated diseases caused by hemorrhagic fever viruses, such as Arenaviruses.
    Type: Application
    Filed: December 29, 2011
    Publication date: December 6, 2012
    Applicant: Siga Technologies, Inc.
    Inventors: Sean M. Amberg, Dongcheng Dai, Tove C. Bolken, Dennis E. Hruby
  • Publication number: 20120301423
    Abstract: The present invention relates to derivatives of ?,?-disubstituted amide compounds which comprise a substituted aryl at the ? carbon such that the substituent provides a means for attachment or incorporation of the compound to or in a polymer. The provision of such a substituent on the aryl has surprisingly been found not only to permit attachment to or incorporation in a polymer but also retention of useful antifouling activity. In embodiments, the substituent is selected from hydroxyl, ethers, es ters, carboxyls, alkylsilyls and alkenyls. Experiments demonstrate that antifouling activity can be as good or better as the corresponding unsubstituted compound and that polymers functionalised so as to include or be formed from the substituted compound can be used to reduce settlement.
    Type: Application
    Filed: February 2, 2011
    Publication date: November 29, 2012
    Applicants: AGENCY FOR SCIENCE, TECHNOLOGY AND RESEARCH, MARITIME AND PORT AUTHORITY OF SINGAPORE, NATIONAL UNIVERSITY OF SINGAPORE
    Inventors: Christina Li Lin Chai, Brendan Adrian Burkett, Serena Lay Ming Teo, Daniel Rittschof, Serina Siew Chen Lee, Gary Howard Dickinson, Han Hong
  • Publication number: 20120302543
    Abstract: Provided are compounds, pharmaceutical compositions and methods of treatment or prophylaxis of certain neurologic disorders, including disorders related to NMDA receptor activation, neuropsychiatric disorders, neurodegenerative disorders and other neurologic diseases, disorders and related conditions. The compounds are of the Formulas I and Ia-Ij as described herein.
    Type: Application
    Filed: June 13, 2012
    Publication date: November 29, 2012
    Inventors: Ruppa Poornachary Kamalesh Babu, Scott James Myers
  • Publication number: 20120301517
    Abstract: The present invention is drawn to adhesive formulations, methods of drug delivery, and solidified layers for dermal delivery of a drug. The formulation can include a drug, a solvent vehicle, and a solidifying agent. The solvent vehicle can have a volatile solvent system including at least one volatile solvent, and a non-volatile solvent system including at least two non-volatile solvents. The formulation can have a viscosity suitable for application to a skin surface prior to evaporation of the volatile solvents system. When applied to the skin, the formulation can form a solidified layer after at least a portion of the volatile solvent system is evaporated.
    Type: Application
    Filed: August 3, 2012
    Publication date: November 29, 2012
    Inventors: Jie Zhang, Kevin S. Warner, Sanjay Sharma
  • Publication number: 20120294907
    Abstract: The present invention is drawn to adhesive solidifying formulations, methods of drug delivery, and solidified layers for dermal delivery of a drug. The formulation can include a drug, a solvent vehicle, and at least two solidifying agents. The solvent vehicle can include a volatile solvent system including at least one volatile solvent, and a non-volatile solvent system including at least one non-volatile solvent, wherein at least one non-volatile solvent is flux-enabling non-volatile solvent(s) capable of facilitating the delivery of the drug at therapeutically effective rates over a sustained period of time. The formulation can have a viscosity suitable for application to a skin surface prior to evaporation of the volatile solvents system. When applied to the skin, the formulation can form a solidified layer after at least a portion of the volatile solvent system is evaporated.
    Type: Application
    Filed: August 6, 2012
    Publication date: November 22, 2012
    Inventors: Jie Zhang, Kevin S. Warner, Sanjay Sharma
  • Publication number: 20120295922
    Abstract: The present invention provides methods for treating and/or preventing mucostitis with one or more compounds, or pharmaceutically acceptable salts thereof, disclosed herein, or compositions comprising the same.
    Type: Application
    Filed: May 15, 2012
    Publication date: November 22, 2012
    Applicant: POLYMEDIX, INC.
    Inventors: Richard W. Scott, Bozena Korczak
  • Publication number: 20120294926
    Abstract: The present invention is drawn to adhesive formulations and methods of drug delivery. The formulation can include a drug, a solvent vehicle, and a solidifying agent. The solvent vehicle can include a volatile solvent system including at least two volatile solvents, and a non-volatile solvent system including at least one non-volatile solvent, wherein at least one non-volatile solvent is capable of facilitating the delivery of the drug at therapeutically effective rates over a sustained period of time. The formulation can have a viscosity suitable for application to a skin surface prior to evaporation of the volatile solvents system. When applied to the skin, the formulation can form a solidified layer after at least a portion of the volatile solvent system is evaporated.
    Type: Application
    Filed: August 3, 2012
    Publication date: November 22, 2012
    Inventors: Jie Zhang, Kevin S. Warner, Sanjay Sharma
  • Patent number: 8309579
    Abstract: The present invention is related to N-hydroxyamide derivatives of Formula (I) and use thereof in particular for the treatment and/or prophylaxis of autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, cancer, respiratory diseases and fibrosis, including multiple sclerosis, arthritis, emphysema, chronic obstructive pulmonary disease, liver and pulmonary fibrosis.
    Type: Grant
    Filed: July 28, 2011
    Date of Patent: November 13, 2012
    Assignee: Merck Serono SA
    Inventors: Dominique Swinnen, Jerome Gonzalez
  • Publication number: 20120283200
    Abstract: The present invention provides a pharmaceutical composition for preventing or treating a chronic heart disease, comprising a compound of a formula (I): wherein: R1 is one independently selected from a group consisting of a hydrogen, a methyl and an ethyl; R2 is one of a hydrogen and a methyl; and R3 is one selected from a group consisting of a hydrogen, (CH2)nAr and (CH2)nArR?R?, wherein n is one of 1 and 2, R? and R? is located at C-3 and C-4 positions, respectively, R? is a hydrogen and R? is one of a hydroxy, a fluorine, a bromine and a OMe, or R?+R?=—OCH2O—; or R2+R3 is one of wherein n is one of 4 and 5.
    Type: Application
    Filed: March 27, 2012
    Publication date: November 8, 2012
    Applicants: CHINA MEDICAL UNIVERSITY, National Taiwan University
    Inventors: MING-JAI SU, YUEH-HSIUNG KUO
  • Publication number: 20120282242
    Abstract: Methods for treating ocular and periocular disorders by administration to a human patient of a therapeutically effective amount of a compound that modulates muscle action.
    Type: Application
    Filed: July 20, 2012
    Publication date: November 8, 2012
    Inventor: Marcio Marc ABREU
  • Patent number: 8304434
    Abstract: A series of substituted aryl sulfone derivatives represented by Formula I, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, calcium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, urinary incontinence, itchiness, allergic dermatitis, epilepsy, diabetic neuropathy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, sleep disorder, bipolar disorder and stroke, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds.
    Type: Grant
    Filed: September 30, 2008
    Date of Patent: November 6, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Prasun K. Chakravarty, Yanbing Ding, Joseph L. Duffy, Hassan Pajouhesh, Pengcheng Patrick Shao, Sriram Tyagarajan, Feng Ye
  • Publication number: 20120276018
    Abstract: Compounds according to formula (I) are effective for the treatment of broncho-obstructive and inflammatory diseases.
    Type: Application
    Filed: April 27, 2012
    Publication date: November 1, 2012
    Applicant: Chiesi Farmaceutici S.p.A.
    Inventors: Gabriele AMARI, Mauro Riccaboni, Daniele De Zani
  • Publication number: 20120277156
    Abstract: Described are methods of inhibiting heterotopic ossification (HO) in a subject in need thereof. The methods involve administering an effective amount of a proprioception inhibitor to the subject, whereby HO is inhibited or prevented. The present invention also relates to a method of treating a subject with bone trauma. This involves administering a proprioception inhibitor to the subject under conditions effective to treat the bone trauma, where the proprioception inhibitor prevents or inhibits HO.
    Type: Application
    Filed: July 21, 2010
    Publication date: November 1, 2012
    Applicant: UNIVERSITY OF WASHINGTON TRHOUGH IT'S CENTER FOR COMMERCIALIZATION
    Inventors: Ted Gross, Steve Bain, Sean Nork
  • Patent number: 8288417
    Abstract: The present invention relates to inhibitors of 11-? hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-? hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.
    Type: Grant
    Filed: October 24, 2011
    Date of Patent: October 16, 2012
    Assignee: Incyte Corporation
    Inventors: Wenqing Yao, Meizhong Xu, Colin Zhang, Yanlong Li, Jincong Zhuo, Brian W. Metcalf
  • Publication number: 20120252830
    Abstract: The present invention provides a compound of formula I?; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, X and n are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Application
    Filed: June 7, 2012
    Publication date: October 4, 2012
    Applicant: NOVARTIS AG
    Inventors: Gary Mark Coppola, Yuki Iwaki, Rajeshri Ganesh Karki, Toshio Kawanami, Gary Michael Ksander, Muneto Mogi, Robert Sun
  • Patent number: 8278330
    Abstract: Methods and compositions for systemically or locally administering by implantation a beneficial agent to a subject are described, and include, for example, depot gel compositions that can be injected into a desired location and which can provide controlled release of a beneficial agent over a short duration of time. The compositions include a low molecular weight biocompatible polymer, a biocompatible solvent having low water miscibility that forms a viscous gel with the polymer and limits water uptake by the implant, and a beneficial agent.
    Type: Grant
    Filed: September 27, 2010
    Date of Patent: October 2, 2012
    Assignee: Durect Corporation
    Inventors: Guohua Chen, David Priebe
  • Publication number: 20120245166
    Abstract: Methods for enhancing memory and/or learning and prevent neurodegeneration by administration of certain heterocyclic and aromatic compounds are described. The methods are particularly useful for treating patients suffering from a neurodegenerative disease such as (without limitation) Alzheimer's, Parkinsons's, Lou Gehrig's (ALS) disease or memory or learning impairment. A neuronal human cell-based assay that assess NF-kB gene up-regulation using a luciferase reporter is also provided that screens for compounds useful in methods for enhancing memory or learning.
    Type: Application
    Filed: October 14, 2010
    Publication date: September 27, 2012
    Applicant: Southern Research Institute
    Inventors: Maurizio Grimaldi, Judith Varady Hobrath, Subramaniam Ananthan, Joseph A. Maddry
  • Publication number: 20120237627
    Abstract: A pharmaceutical composition characterized in that the composition contains at least 4 wt % relative to the total weight of the composition of an active principle selected from among cetearyl octanoate and hexanoic acid, beeswax and optionally one or more pharmaceutically acceptable excipient(s), as well as to the use thereof for the treatment of cutaneous pre-burns or burns and for reducing pain following a thermal shock.
    Type: Application
    Filed: December 10, 2010
    Publication date: September 20, 2012
    Applicant: 45 SEC. LLC
    Inventor: Jean-Jacques Debetencourt
  • Patent number: 8268821
    Abstract: The present invention relates generally to the field of pain management, and in particular, the management of neuropathic or inflammatory pain including a neuropathic or inflammatory component of nociceptive pain. More particularly, the present invention provides methods and compositions which treat, alleviate, prevent, diminish or otherwise ameliorate the symptoms of neuropathic or inflammatory pain. The present invention further contemplates combination therapy involved in the treatment of pain in association with the treatment of a particular disease condition or pathology. The present invention further also provides sustained and slow release formulations, tamper-proof deliver systems and stents, catheters and other mechanical devices coated with formulations which permit sustained or slow release of active ingredients involved in pain management.
    Type: Grant
    Filed: December 1, 2010
    Date of Patent: September 18, 2012
    Assignee: Relevare Aust. Pty Ltd
    Inventors: Raymond Nadeson, Adam Paul Tucker, Colin Goodchild
  • Patent number: 8258304
    Abstract: N-aryl piperidine substituted biphenylcarboxamides compounds of formula (I) methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of hyperlipidemia, obesity and type II diabetes.
    Type: Grant
    Filed: January 9, 2009
    Date of Patent: September 4, 2012
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Lieven Meerpoel, Leo Jacobus Jozef Backx, Peter Walter Maria Roevens
  • Publication number: 20120220564
    Abstract: Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted T-type calcium channel activity are disclosed using a series of compounds containing N-acylated cyclic amines linked to an a?l ring as shown in formula (I).
    Type: Application
    Filed: September 17, 2010
    Publication date: August 30, 2012
    Applicant: Zalicus Pharmaceuticals Ltd.
    Inventors: Hassan Pajouhesh, Yongbao Zhu, Yuanxi Zhou, Michael E. Grimwood, Eric Simonson
  • Patent number: 8232265
    Abstract: Disclosed are ionic liquids and methods of preparing ionic liquid compositions of active pharmaceutical, biological, nutritional, and energetic ingredients. Also disclosed are methods of using the compositions described herein to overcome polymorphism, overcome solubility and delivery problems, to control release rates, add functionality, enhance efficacy (synergy), and improve ease of use and manufacture.
    Type: Grant
    Filed: October 10, 2006
    Date of Patent: July 31, 2012
    Assignee: Board of Trustees of the University of Alabama
    Inventors: Robin D. Rogers, Daniel T. Daly, Richard P. Swatloski, Whitney L. Hough, James Hilliard Davis, Jr., Marcin Smiglak, Juliusz Pernak, Scott K. Spear
  • Publication number: 20120184572
    Abstract: Aryl GPR119 agonists are provided. These compounds are useful for the treatment of diabetic diseases, including Type II diabetes and other diseases associated with poor glycemic control.
    Type: Application
    Filed: January 13, 2011
    Publication date: July 19, 2012
    Inventors: Jiangao Song, Jingyuan Ma, Christopher J. Rabbat, Imad Nashashibi, Xin Chen, Zuchun Zhao
  • Publication number: 20120177699
    Abstract: A preparation method of drug loaded emulsion is disclosed. The method comprises the steps of: preparing a non-self emulsifying O/W blank emulsion having no active ingredients; then, adding therapeutically effective amount of active ingredients to the 0/W blank emulsion, adjusting pH to distribute the active ingredients through the membrane to obtain the desired emulsion.
    Type: Application
    Filed: June 3, 2010
    Publication date: July 12, 2012
    Applicants: SHANGHAI HENGRUI PHARMACEUTICAL CO., LTD., JIANGSU HENGRUI MEDICINE CO., LTD.
    Inventors: Xinyong Tong, Haifeng Wang, Li Lu, Liang Chen, Yuan Shi
  • Publication number: 20120178732
    Abstract: The invention relates to substituted phenoxyacetic acids of formula (I), where the variables are as defined in claim 1, as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.
    Type: Application
    Filed: December 6, 2011
    Publication date: July 12, 2012
    Inventors: Timothy Jon Luker, Timothy Nicholas Birkinshaw, Rukhsana Tasneem Mohammed
  • Publication number: 20120172358
    Abstract: Compounds of formula (I): or pharmaceutically acceptable salts thereof, are GPCR agonists and are useful as for the treatment of obesity and diabetes.
    Type: Application
    Filed: February 14, 2012
    Publication date: July 5, 2012
    Applicant: Prosidion Limited
    Inventors: Stuart Edward Bradley, Matthew Colin Thor Fyfe, Lisa Sarah Bertram, William Gattrell, Revathy Perpetua Jeevaratnam, John Keily, Martin James Procter, Chrystelle Marie Rasamison, Philip John Rushworth, Colin Peter Sambrook-Smith, David French Stonehouse, Simon Andrew Swain, Geoffrey Martyn Williams