Nitrogen Attached Directly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 514/352)
Plural acyclic nitrogens bonded directly to the same carbon or bonded directly to each other (Class 514/353)
  • Heteroaryl hydroxamic acid derivatives and their use in the treatment, amelioration or prevention of a viral disease
    Publication number: 20130102600
    Abstract: The present invention relates to a compound having the general formula I, optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, prodrug, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, which is useful in treating, ameliorating or preventing a viral disease. Furthermore, specific combination therapies are disclosed.
    Type: Application
    Filed: October 18, 2012
    Publication date: April 25, 2013
    Applicants: F. HOFFMANN-LA ROCHE LTD, EUROPEAN MOLECULAR BIOLOGY LABORATORY (EMBL), SAVIRA PHARMACEUTICALS GMBH
    Inventors: F. HOFFMANN-LA ROCHE LTD, SAVIRA PHARMACEUTICALS GMBH, EUROPEAN MOLECULAR BIOLOGY LABORAT
  • METHOD FOR THE PREPARATION OF CIS-1,2-DIOLS IN THE KILOGRAM SCALE
    Publication number: 20130102640
    Abstract: The present invention relates to the scale up of the preparation of cis-1,2-diols of formula I from the gram to the kilogram scale.
    Type: Application
    Filed: June 3, 2011
    Publication date: April 25, 2013
    Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNG
    Inventors: Werner Mederski, Georg Stoehr, Andreas Werner
  • Substituted 4-phenyl pyridines having anti-emetic effect
    Patent number: 8426450
    Abstract: Disclosed are compounds, compositions and methods for the prevention and/or treatment of diseases which are pathophysiologically mediated by the neurokinin (NK1) receptor.
    Type: Grant
    Filed: May 23, 2012
    Date of Patent: April 23, 2013
    Assignee: Helsinn Healthcare SA
    Inventors: Luca Fadini, Peter Manini, Claudio Pietra, Claudio Giuliano, Emanuela Lovati, Roberta Cannella, Alessio Venturini, Valentino J. Stella
  • ETHYNYL DERIVATIVES
    Publication number: 20130090347
    Abstract: The present invention relates to ethynyl derivatives of formula I wherein U, V, W, Y, R, R1, R2, R3 and R3? are as described herein. It has been found that the compounds of general formula I are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).
    Type: Application
    Filed: September 27, 2012
    Publication date: April 11, 2013
    Applicant: Hoffmann-La Roche Inc.
    Inventor: Hoffmann-La Roche Inc.
  • Inhibitor of plasminogen activator inhibitor-1
    Patent number: 8415479
    Abstract: The present invention relates to a novel compound having plasminogen activator inhibitor-1 (PAI-1) inhibitory activity, and a PAI-1 inhibitor comprising the compound as an active ingredient. The present invention further relates to a pharmaceutical composition that has an inhibitory action on PAI-1 activity and is useful in the prevention and treatment of various diseases whose onset is associated with PAI-1 activity. The novel compound is represented by the following general formula. Each symbol is defined as those in the specification.
    Type: Grant
    Filed: March 31, 2009
    Date of Patent: April 9, 2013
    Assignee: Renascience Co., Ltd.
    Inventors: Toshio Miyata, Nagahisa Yamaoka, Hidehiko Kodama, Kenji Murano
  • Reducing myocardial reperfusion injury by the combination therapy of protein kinase A activation and B1-adrenergic receptor blockade
    Patent number: 8415384
    Abstract: Embodiments of the invention are directed to methods of treating reperfusion or resuscitation injury in an individual in need of such treatment, comprising the step of administering to the individual who has had, having, or is at immediate risk of having an ischemic event an amount of a composition comprising a protein kinase A (PKA) activator and a ?1-adrenergic receptor antagonist sufficient to reduce reperfusion injury to an ischemic tissue.
    Type: Grant
    Filed: June 12, 2009
    Date of Patent: April 9, 2013
    Assignee: The Board of Regents of the University of Texas System
    Inventors: Ming-He Huang, Kenichi Fujise, Barry F. Uretsky
  • METHODS FOR TREATING A STROKE-RELATED SENSORIMOTOR IMPAIRMENT USING AMINOPYRIDINES
    Publication number: 20130085167
    Abstract: Disclosed herein are methods and compositions related to therapeutic use of aminopyridines in patients with a stroke-related impairment, in particular, in patients with a stroke-related sensorimotor impairment.
    Type: Application
    Filed: October 4, 2012
    Publication date: April 4, 2013
    Applicant: Acorda Therapeutics, Inc.
    Inventor: Acorda Therapeutics, Inc.
  • FORMULATIONS AND USES OF RETINOIC ACID RECEPTOR SELECTIVE AGONISTS
    Publication number: 20130085166
    Abstract: The invention provides retinoic acid receptor (RAR) selective agonists and formulations thereof for the treatment of disease or for inducing a medically beneficial effect.
    Type: Application
    Filed: October 4, 2011
    Publication date: April 4, 2013
    Inventor: Ferenc Makra
  • Amine Substituted Methanesulfonamide Derivatives as Vanilloid Receptor Ligands
    Publication number: 20130079320
    Abstract: The invention relates to amine substituted methanesulfonamide derivatives as vanilloid receptor ligands, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
    Type: Application
    Filed: September 25, 2012
    Publication date: March 28, 2013
    Applicant: Gruenenthal GmbH
    Inventor: Gruenenthal GmbH
  • Unit dose formulations and methods of treating thrombosis with an oral factor Xa inhibitor
    Patent number: 8404724
    Abstract: Unit doses of factor Xa inhibitor compounds and methods of using these compounds for inhibiting blood coagulation in a human patient are taught herein. The unit dose of the factor Xa inhibitor compounds disclosed herein required to inhibit coagulation in a primate is lower than the unit dose required to obtain similar levels of coagulation inhibition in other animal models, such as rodents. Also taught are in vitro assays useful in predicting in vivo antithrombotic activity in humans.
    Type: Grant
    Filed: December 7, 2007
    Date of Patent: March 26, 2013
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Uma Sinha, Stanley J. Hollenbach, Keith Abe
  • Kinase modulating compounds and uses thereof for treatment of cancer
    Patent number: 8404669
    Abstract: The invention relates to protein binding inhibitor compounds and methods of identifying and using them. The invention further relates to pharmaceutical compositions and methods for treating a variety of diseases and disorders, including cell proliferative disorders, especially cancer.
    Type: Grant
    Filed: September 15, 2008
    Date of Patent: March 26, 2013
    Assignee: University of Florida Research Foundation, Inc.
    Inventors: William G. Cance, Elena Kurenova, Vita Golubovskaya, David A. Ostrov
  • Phenylamino isonicotinamide compounds
    Patent number: 8404725
    Abstract: The invention provides novel substituted phenylamino isonicotinamide compounds (I), pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein X, R1, R2, R3, R4, R5 and R6 are as defined in the specification. Said compounds are MEK inhibitors useful in the treatment of hyperproliferative diseases related to the hyperactivity of MEK, such as restenosis, as well as diseases modulated by the MEK cascade, such as cancer and inflammation. Also disclosed is the use of such compounds in the treatment of hyperproliferative diseases in mammals, especially humans, and pharmaceutical compositions containing such compounds.
    Type: Grant
    Filed: July 27, 2009
    Date of Patent: March 26, 2013
    Assignee: Merck Patent GmbH
    Inventors: Andreas Goutopoulos, Henry Yu, Benny C. Askew, Jr., Lesley Liu-Bujalski
  • PROPHYLACTIC OR THERAPEUTIC AGENT FOR DIABETES OR OBESITY
    Publication number: 20130072491
    Abstract: An object is to provide a CaSR agonist agent that has excellent CaSR agonist effects, and particularly, a pharmaceutical product that can prevent or remedy diabetes or obesity by the effect of CaSR activation. The aforementioned object is achieved by a composition that contains a compound represented by the following General Formula (I) or a salt thereof (refer to the Description for the definitions of the symbols used in the formula).
    Type: Application
    Filed: August 31, 2012
    Publication date: March 21, 2013
    Applicant: Ajinomoto Co., Inc.
    Inventors: Reiko YASUDA, Yuzuru Eto, Yoshiro Kitahara
  • METHODS OF USING SUSTAINED RELEASE AMINOPYRIDINE COMPOSITIONS
    Publication number: 20130072527
    Abstract: Disclosed herein are methods and compositions related to use of aminopyridines, such as fampridine, to improve impairments of patients with a demyelinating condition, such as MS.
    Type: Application
    Filed: July 5, 2012
    Publication date: March 21, 2013
    Applicant: Acorda Therapeutics, Inc.
    Inventors: Andrew R. Blight, Ron Cohen
  • CONTRACEPTIVE METHODS AND COMPOSITIONS
    Publication number: 20130065853
    Abstract: The invention encompasses compositions and methods for use in preventing pregnancy.
    Type: Application
    Filed: March 30, 2012
    Publication date: March 14, 2013
    Applicant: THE WASHINGTON UNIVERSITY
    Inventors: Kelle H. Moley, Antonina I. Frolova
  • NOVEL PHARMACEUTICAL SALTS AND POLYMORPHS OF A FACTOR XA INHIBITOR
    Publication number: 20130064806
    Abstract: The present invention provides for salts comprising a compound of Formula I and an acid that has activity against mammalian factor Xa. The present invention is also directed to methods of making the compound of Formula I.
    Type: Application
    Filed: September 12, 2012
    Publication date: March 14, 2013
    Inventors: Craig Grant, James P. Kanter, Graeme Langlands
  • BIOMARKERS FOR PI3K-DRIVEN CANCER
    Publication number: 20130065928
    Abstract: Disclosed is the discovery that the mTORC2 complex plays a role in the regulation of PKN3 phosphorylation at the turn motif threonine; and the use of the phosphorylation status of the turn motif threonine of PKN3 as a biomarker. In some embodiments, the phosphorylation status of the turn motif threonine of PKN3 is determined using an antibody that specifically binds to the turn motif threonine of a PKN3 protein, such as an anti-phosphoT860 antibody. In some embodiments, the invention relates to methods for screening compounds that have cancer therapeutic potential, methods for diagnosing cancer, methods for determining the prognosis of a patient suffering from cancer, methods for stratifying patients in a clinical trial, methods for treating a patient suffering from cancer, and methods for determining the effectiveness of a particular treatment regimen.
    Type: Application
    Filed: April 2, 2011
    Publication date: March 14, 2013
    Applicant: WYETH LLC
    Inventors: Anke Klippel-Giese, Keziban Unsal-Kacmaz
  • Optical enantiomers of phenyramidol and process for chiral synthesis
    Patent number: 8389551
    Abstract: The present invention discloses optically pure (R) and (S) Phenyramidol enantiomers and their pharmaceutically acceptable salts, a process for synthesizing such enantiomers by means of a styrene oxide based synthesis, and also a clinical evaluation of (R) and (S) enantiomers of Phenyramidol, their salts and compositions thereof for enhanced/newer therapeutic benefits.
    Type: Grant
    Filed: February 16, 2010
    Date of Patent: March 5, 2013
    Assignee: Fermenta Biotech (UK) Limited
    Inventors: Anupama Datla, Pramod Abaji Walavalker, Ashok Konda, Sreenath Babunath Trivikram
  • Use of 4-Aminopyridine to Improve Neuro-Cognitive and/or Neuro-Psychiatric Impairment in Patients With Demyelinating and Other Nervous System Conditions
    Publication number: 20130053420
    Abstract: Disclosed herein are methods and compositions related to use of aminopyridines, such as 4-aminopyridine, to improve the neuro-cognitive impairments and related neuro-psychiatric impairments of patients with a demyelinating condition such as MS, traumatic brain injury, cerebral palsy, post-radiation encephalopathy.
    Type: Application
    Filed: August 11, 2010
    Publication date: February 28, 2013
    Inventors: Thomas C. Wessel, Andrew R. Blight
  • PPAR-SPARING THIAZOLIDINEDIONES AND COMBINATIONS FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES
    Publication number: 20130053350
    Abstract: The present invention relates to thiazolidinedione analogues and pharmaceutical compositions that are useful for treating and/or preventing neurodegenerative disorders.
    Type: Application
    Filed: December 15, 2010
    Publication date: February 28, 2013
    Applicant: Metabolic Solutions Development Company, LLC
    Inventors: Gerard R. Colca, Rolf F. Kletzien, Steve P. Tanis, Scott D. Larsen
  • Aryl pyridine as aldosterone synthase inhibitors
    Patent number: 8383827
    Abstract: The present invention provides a compound of formula I; 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: Grant
    Filed: May 14, 2010
    Date of Patent: February 26, 2013
    Assignee: Novartis AG
    Inventors: Sylvie Chamoin, Qi-Ying Hu, Julien Papillon
  • RHO KINASE INHIBITORS FOR TREATMENT OF MASTOCYTOSIS AND ACUTE MYELOID LEUKEMIA
    Publication number: 20130046009
    Abstract: The disclosure is directed to methods of treating hematologic malignancies. More particularly, the disclosure is directed to methods of treating hematologic malignancies using Rho kinase (ROCK) inhibitors and myosin light chain-specific inhibitory RNA molecules. The disclosure is further directed to methods of identifying drug candidates for inhibiting ROCK in hematologic malignancies.
    Type: Application
    Filed: August 15, 2012
    Publication date: February 21, 2013
    Inventor: Reuben Kapur
  • SUSTAINED RELEASE AMINOPYRIDINE COMPOSITION
    Publication number: 20130045276
    Abstract: A pharmaceutical composition which comprises a therapeutically effective amount of a aminopyridine dispersed in a release matrix, including, for example, a composition that can be formulated into a stable, sustained-release oral dosage formulation, such as a tablet which provides, upon administration to a patient, a therapeutically effective plasma level of the aminopyridine for a period of at least 12 hours, preferably 24 hours or more and the use of the composition to treat various neurological diseases.
    Type: Application
    Filed: August 14, 2012
    Publication date: February 21, 2013
    Applicant: Alkermes Pharma Ireland Limited
    Inventors: Sean Cunningham, Seamus Mulligan, Michael Myers
  • Targeted, NIR imaging agents for therapy efficacy monitoring, deep tissue disease demarcation and deep tissue imaging
    Patent number: 8372868
    Abstract: Compounds and methods related to NIR molecular imaging, in-vitro and in-vivo functional imaging, therapy/efficacy monitoring, and cancer and metastatic activity imaging. Compounds and methods demonstrated pertain to the field of peripheral benzodiazepine receptor imaging, metabolic imaging, cellular respiration imaging, cellular proliferation imaging as targeted agents that incorporate signaling agents.
    Type: Grant
    Filed: July 13, 2010
    Date of Patent: February 12, 2013
    Assignee: Vanderbilt University
    Inventors: Darryl J. Bornhop, H. Charles Manning, Mingfeng Bai, Shelby K. Wyatt
  • Bis Aromatic Compounds for Use as LTC4 Synthase Inhibitors
    Publication number: 20130035358
    Abstract: There is provided compounds of formula I, wherein E1, E2a, E2b, E2c, E4, D1, D2, D3, L1, Y1, L2 and Y2 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of leukotriene C4 synthase is desired and/or required, and particularly in the treatment of a respiratory disorder and/or inflammation.
    Type: Application
    Filed: March 14, 2011
    Publication date: February 7, 2013
    Inventors: Peter Nilsson, Benjamin Pelcman, Martins Katkevics, Robert Ronn, Christian Krog-Jensen
  • ARYL PYRIDINE AS ALDOSTERONE SYNTHASE INHIBITORS
    Publication number: 20130035354
    Abstract: The present invention provides a compound of formula I; 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: September 14, 2012
    Publication date: February 7, 2013
    Applicant: NOVARTIS AG
    Inventors: Sylvie Chamoin, Qi-Ying Hu, Julien Papillon
  • Carbamate compounds which inhibit leukocyte adhesion mediated by VLA-4
    Patent number: 8367688
    Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.
    Type: Grant
    Filed: April 13, 2010
    Date of Patent: February 5, 2013
    Assignees: Elan Pharmaceuticals, Inc., Wyeth
    Inventors: Christopher Michael Semko, Ying-zi Xu, Frank Stappenbeck, Jenifer Lea Smith, Kassandra Inez Rossiter, Juri Y. Fukuda, Andrei W. Konradi
  • USE OF POTASSIUM CHANNEL BLOCKERS TO TREAT CEREBRAL PALSY
    Publication number: 20130030025
    Abstract: Disclosed herein is the use of aminopyridines, such as 3-aminopyridine, 4-aminopyridine or 3,4-diaminopyridine, in the management and treatment of cerebral palsy patients of all ages.
    Type: Application
    Filed: January 27, 2012
    Publication date: January 31, 2013
    Inventors: Thomas C. Wessel, Adrian L. Rabinowicz, Herbert R. Henney, III, Jacob D. Runyan, Anthony Caggiano, Andrew Blight
  • Compositions to effect neuronal growth
    Patent number: 8362262
    Abstract: Compositions containing neurogenic agents for inhibition of neuron death and inducing proliferation of neural cells are disclosed.
    Type: Grant
    Filed: October 7, 2011
    Date of Patent: January 29, 2013
    Assignee: Neuralstem, Inc.
    Inventors: Judith Kelleher-Andersson, Karl K. Johe
  • NEW COMPOUNDS
    Publication number: 20130018054
    Abstract: The present invention provides organic compounds of the following structure; A-L1-B—C-D-L2-E that are useful for treating or preventing conditions or disorders associated with DGAT1 activity in animals, particularly humans.
    Type: Application
    Filed: September 13, 2012
    Publication date: January 17, 2013
    Applicant: NOVARTIS AG
    Inventors: Michael H. SERRANO-WU, Young-shin KWAK, Wenming Liu
  • Method of using sustained release aminopyridine compositions
    Patent number: 8354437
    Abstract: A pharmaceutical composition which comprises a therapeutically effective amount of a aminopyridine dispersed in a release matrix, including, for example, a composition that can be formulated into a stable, sustained-release oral dosage formulation, such as a tablet which provides, upon administration to a patient, a therapeutically effective plasma level of the aminopyridine for a period of at about 12 hours and the use of the composition to treat various neurological diseases, including multiple sclerosis. A method of selecting individuals based on responsiveness to a treatment, including, for example, identifying individuals who responded to treatment with a sustained release fampridine composition.
    Type: Grant
    Filed: April 8, 2005
    Date of Patent: January 15, 2013
    Assignee: Acorda Therapeutics, Inc.
    Inventors: Andrew R. Blight, Ron Cohen
  • New Positive allosteric modulators of nicotinic acetylcholine receptor
    Publication number: 20130012530
    Abstract: The present invention relates to compounds useful in therapy, to compositions comprising said compounds, and to methods of treating diseases comprising administration of said compounds. The compounds referred to are positive allosteric modulators (PAMs) of the nicotinic acetylcholine ?7 receptor.
    Type: Application
    Filed: July 6, 2012
    Publication date: January 10, 2013
    Applicant: H. Lundbeck A/S
    Inventors: Jørgen Eskildsen, Anette Graven Sams, Ask Püschl
  • Fungicidal compositions
    Patent number: 8349345
    Abstract: A composition for control of diseases on useful plants or on propagation material thereof caused by phytopathogens, that, in addition to customary inert formulation adjuvants, comprises as active ingredient a mixture of component (A) and a synergistically effective amount of component (B), wherein component (A) is Cyprodinil; and component (B) a compound selected from compounds known for their fungicidal activity, is particularly effective in controlling or preventing fungal diseases of useful plants.
    Type: Grant
    Filed: September 27, 2006
    Date of Patent: January 8, 2013
    Assignee: Syngenta Crop Protection LLC
    Inventors: Birgit Forster, Duncan McKenzie, Jeremy Godwin
  • URETHANES, UREAS, AMIDINES AND RELATED INHIBITORS OF FACTOR XA
    Publication number: 20130005778
    Abstract: The invention relates to a new class of compounds, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions that are effective as selective inhibitors of factor Xa, both in the isolated state and in a complex with other proteins. The compounds of the invention can be used for treating and preventing diseases, such as acute coronary syndrome, myocardial infarction, unstable angina, refractory angina, thromboses caused by post-thrombolytic therapy or coronary angioplasty, acute ischemia mediated cerebrovascular syndrome, embolic stroke, thrombotic stroke, and other diseases in humans and other mammals associated with blood coagulation problems.
    Type: Application
    Filed: August 30, 2012
    Publication date: January 3, 2013
    Inventors: Dmitry Gennadievich TOVBIN, Dmitry Nikolaevich TARASOV, Dimitry Viktorovich MALAKHOV
  • COMPOUNDS AND THERAPEUTIC USES THEREOF
    Publication number: 20120329786
    Abstract: The invention relates to compounds, pharmaceutical compositions and methods useful for treating cancer, systemic or chronic inflammation, rheumatoid arthritis, diabetes, obesity, T-cell mediated autoimmune disease, ischemia, and other complications associated with these diseases and disorders.
    Type: Application
    Filed: August 31, 2012
    Publication date: December 27, 2012
    Applicant: Myrexis, Inc.
    Inventors: J. Adam Willardsen, Jeffrey W. Lockman, Brett R. Murphy, Weston R. Judd, In Chul Kim, Se-Ho Kim, Daniel Feodore Zigar, Kraig M. Yager, Tracey C. Fleischer, Ryan T. Terry-Lorenzo, J. Jay Boniface, Daniel P. Parker, Ian A. McAlexander, Matthew Gregory Bursavich, David M. Dastrup
  • Opioid receptor antagonists
    Patent number: 8338611
    Abstract: A compound of the formula (I) wherein the variables X1, X2, B, D, R1 to R7 including R3?, p, y, q, and z, are as defined or a pharmaceutically acceptable salt, solvate, enantiomer, racemate, diastereomer or mixtures thereof, useful for the treatment, prevention or amelioration of obesity and Related Diseases is disclosed.
    Type: Grant
    Filed: January 6, 2011
    Date of Patent: December 25, 2012
    Assignee: Eli Lilly and Company
    Inventors: Charles Howard Mitch, Steven James Quimby
  • HETEROCYCLIC AMIDES AS ROCK INHIBITORS
    Publication number: 20120322801
    Abstract: The present invention relates to new kinase inhibitors, more specifically ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In particular, the present invention relates to new ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In addition, the invention relates to methods of treatment and use of said compounds in the manufacture of a medicament for the application to a number of therapeutic indications including sexual dysfunction, inflammatory diseases, ophthalmic diseases and Respiratory diseases.
    Type: Application
    Filed: March 4, 2011
    Publication date: December 20, 2012
    Applicant: Amakem NV
    Inventors: Dirk Leysen, Olivier Defert, Nadzeya Kaval, Petra Blom, Sandro Boland
  • COMPOUNDS THAT MODULATE INTRACELLULAR CALCIUM
    Publication number: 20120316182
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.
    Type: Application
    Filed: June 8, 2012
    Publication date: December 13, 2012
    Applicant: CalciMedica, Inc.
    Inventors: Jeffrey P. WHITTEN, Jonathan Grey, Jianguo Cao, Zhijun Wang, Evan Rogers
  • 2-ARYL-PROPIONAMIDE DERIVATIVES USEFUL AS BRADYKININ RECEPTOR ANTAGONISTS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
    Publication number: 20120316169
    Abstract: (R,S) 2-aryl-propionamide derivatives, or their single enantiomers (R) and (S) are disclosed useful in the treatment or prevention of symptoms and disorders such as pain and inflammation associated with the bradykinin B1 pathway.
    Type: Application
    Filed: October 28, 2010
    Publication date: December 13, 2012
    Applicant: DOMPÉ S.P.A.
    Inventors: Andrea Beccari, Andrea Aramini, Gianluca Bianchini, Alessio Moriconi
  • Tryptophan Hydroxylase Inhibitors for the Treatment of Cancer
    Publication number: 20120316171
    Abstract: Methods and compositions for the treatment and/or management of cancer are disclosed, which comprise the use of tryptophan hydroxylase inhibitors.
    Type: Application
    Filed: November 4, 2010
    Publication date: December 13, 2012
    Inventor: Tamas Oravecz
  • HETEROCYCLIC SULFONAMIDE DERIVATIVES
    Publication number: 20120316149
    Abstract: The present invention relates to compounds: and pharmaceutically acceptable salts thereof. The compounds have been demonstrated as inhibitors of MEK and therefore may be useful in the treatment of hyperproliferative diseases like cancer and inflammation.
    Type: Application
    Filed: June 7, 2012
    Publication date: December 13, 2012
    Inventors: Ramulu PODDUTOORI, Can WANG, Xianglin ZHAO
  • NOVEL PYRIDINE DERIVATIVES
    Publication number: 20120316147
    Abstract: The invention relates to a compound of formula (I) wherein R1 to R4 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.
    Type: Application
    Filed: June 1, 2012
    Publication date: December 13, 2012
    Inventors: Caterina Bissantz, Uwe Grether, Paul Hebeisen, Atsushi Kimbara, Qingping Liu, Matthias Nettekoven, Marco Prunotto, Stephan Roever, Mark Rogers-Evans, Tanja Schulz-Gasch, Christoph Ullmer, Zhiwei Wang, Wulun Yang
  • INTERFERON-INDUCING COMPOUNDS AND USES THEREOF
    Publication number: 20120308608
    Abstract: Provided herein are Compounds that induce interferon production and methods for identifying such Compounds. Also provided herein are compositions comprising such Compounds and methods of using such Compounds to treat interferon-sensitive diseases such as viral infections, cancer, and multiple sclerosis.
    Type: Application
    Filed: January 31, 2011
    Publication date: December 6, 2012
    Inventors: Megan Shaw, Mila Ortigoza, Adolfo Garcia-Sastre, Peter Palese
  • USE OF METABOTROPIC GLUTAMATE RECEPTORS
    Publication number: 20120309742
    Abstract: The invention concerns the use an mGluR modulator, e.g. an mGluR5 modulator, for the treatment, prevention or delay of progression of cognitive dysfunction.
    Type: Application
    Filed: August 8, 2012
    Publication date: December 6, 2012
    Inventors: Ralf GLATTHAR, Donald JOHNS, Daniel UMBRICHT
  • Modulators of ATP-binding cassette transporters
    Patent number: 8324207
    Abstract: Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
    Type: Grant
    Filed: March 23, 2011
    Date of Patent: December 4, 2012
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Sara S. Hadida Ruah, Matthew Hamilton, Mark Miller, Peter D. J. Grootenhuis, Brian Bear, Jason McCartney, Jinglan Zhou, Fredrick van Goor
  • G-protein-conjugated receptor agonist
    Patent number: 8318781
    Abstract: Disclosed is a novel aralkyl carboxylic acid compound which has an agonistic activity on GPR-120 and/or GPR-40, particularly GPR-120, and is therefore useful as an appetite regulator, an anti-obesity agent, a therapeutic agent for diabetes, a pancreatic beta differentiating cell growth enhancer, a therapeutic agent for metabolic syndrome, a therapeutic agent for a gastrointestinal disease, a therapeutic agent for a neuropathy, a therapeutic agent for a mental disorder, a therapeutic agent for a pulmonary disease, a therapeutic agent for a pituitary hormone secretion disorder or a lipid flavoring/seasoning agent. The aralkyl carboxylic acid compound is represented by the general formula (I).
    Type: Grant
    Filed: April 25, 2008
    Date of Patent: November 27, 2012
    Assignees: Japan Science and Technology Agency, Kyoto University, Nagoya City University
    Inventors: Gozoh Tsujimoto, Akira Hirasawa, Naoki Miyata, Takayoshi Suzuki, Yoshiyuki Takahara, Masaji Ishiguro, Mie Hata
  • NEW ANTI-MALARIAL AGENTS
    Publication number: 20120295905
    Abstract: The present invention is related to a use of aminopyridine derivatives in the manufacture of a medicament for preventing or treating malaria. Specifically, the present invention is related to aminopyridine derivatives useful for the preparation of a pharmaceutical formulation for the inhibition of malaria parasite proliferation.
    Type: Application
    Filed: January 17, 2011
    Publication date: November 22, 2012
    Applicant: MMV MEDICINES FOR MALARIA VENTURE
    Inventors: Michael John Witty, David Hardick
  • 3-Arylamino Pyridine Derivatives
    Publication number: 20120295889
    Abstract: The invention provides novel, substituted 3-arylamino pyridine compounds pharmaceutically acceptable salts, solvates and prodrug compounds thereof, wherein W, R1, R2, R9, R10, R11, R12, R13, R14 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer, restenosis and inflammation. Also disclosed is the use of such compounds in the treatment of hyperproliferative diseases in mammals, especially humans, and pharmaceutical compositions containing such compounds.
    Type: Application
    Filed: May 16, 2012
    Publication date: November 22, 2012
    Applicant: Merck Serono S.A.
    Inventors: Ulrich Abel, Holger Deppe, Achim Feurer, Ulrich Grädler, Kerstin Otte, Renate Sekul, Meinolf Thiemann, Andreas Goutopoulos, Matthias Schwarz, Xuliang Jiang
  • NOVEL PROCESS FOR THE PREPARATION OF ROFLUMILAST
    Publication number: 20120294942
    Abstract: The invention relates to novel processes for the preparation of high-purity roflumilast.
    Type: Application
    Filed: July 12, 2012
    Publication date: November 22, 2012
    Applicant: NYCOMED GMBH
    Inventors: Bernhard KOHL, Bernd MUELLER, Walter PALOSCH
  • AMINO NICOTINIC AND ISONICOTINIC ACID DERIVATIVES AS DHODH INHIBITORS
    Publication number: 20120294854
    Abstract: The present disclosure relates to compounds of formula (I): or a pharmaceutically acceptable salt or N-oxide thereof. The present disclosure also relates to pharmaceutical compositions comprising the compounds of formula (I), and to their methods of use in therapy.
    Type: Application
    Filed: August 6, 2012
    Publication date: November 22, 2012
    Inventors: Julio Cesar CASTRO PALOMINO LARIA, Montserrat ERRA SOLA, Maria Estrella LOZOYA TORIBIO, Eloisa NAVARRO ROMERO