Tricyclo Ring System Having The Six-membered Hetero Ring As One Of The Cyclos Patents (Class 514/290)
  • Patent number: 10730871
    Abstract: The invention provides compounds of formula I: wherein R1-R3, Ra, and Rb have any of the values defined herein, and salts thereof. The compounds have immunomodulatory properties.
    Type: Grant
    Filed: January 27, 2017
    Date of Patent: August 4, 2020
    Assignee: REGENTS OF THE UNIVERSITY OF MINNESOTA
    Inventor: David Ferguson
  • Patent number: 10619027
    Abstract: Provided an agent for suppressing an odor of a polysulfide compound. This agent for suppressing an odor of a polysulfide compound comprises, as an active ingredient, at least one selected from the group consisting, butyl 2-methylbutanoate, ?-terpinene, dipentene, cis-4-heptenal, 1,4-cineol, trimethylhexyl aldehyde, and (+)-limonene oxide, wherein the polysulfide compound is represented by the following formula (I): R1—[S]n—R2 (I) (in the formula, R1 and R2 are the same or different, and each denote a linear-chain or branched-chain alkyl or alkenyl group having 1 to 6 carbon atoms, and n denotes an integer of 2 to 5).
    Type: Grant
    Filed: June 16, 2016
    Date of Patent: April 14, 2020
    Assignee: KAO CORPORATION
    Inventors: Keiichi Yoshikawa, Naoko Saito
  • Patent number: 10463656
    Abstract: Methods for preventing feedlot bovine respiratory diseases employing an anti-inflammatory drug rupatadine are disclosed. Compositions are further disclosed. Beneficially, the methods and compositions provide safe and cost-effective management of a costly disease.
    Type: Grant
    Filed: January 5, 2018
    Date of Patent: November 5, 2019
    Assignee: Iowa State University Research Foundation, Inc.
    Inventors: Steven Alan Carlson, Timothy L. Day
  • Patent number: 10407734
    Abstract: The present invention provides compositions and methods of using transposons. In one aspect, methods are disclosed that are useful for identifying negatively selected genes in an insertional mutagenesis screen. In another aspect, compositions for reducing proliferation of a tumor cell expressing an oncogenic RAS include an activator of a WNT pathway. Pharmaceutical compositions for reducing proliferation of tumor cells in a subject in need thereof by administering an effective amount of an activator of a WNT pathway to the tumor cells of the subject are also disclosed.
    Type: Grant
    Filed: November 17, 2014
    Date of Patent: September 10, 2019
    Assignee: Yale University
    Inventors: Tian Xu, Feng Qian, Sean Landrette
  • Patent number: 10238644
    Abstract: Pharmaceutical formulations and methods for the topical or transdermal delivery of 1-isobutyl-1H-imidazo[4,5-c]-quinolin-4-amine or 1-(2-methylpropyl)-1H-imidazo[4,5-c]quinolin-4-amine, i.e., imiquimod, to treat actinic keratosis with short durations of therapy, than currently prescribed for the commercially available Aldara® 5% imiquimod cream, as now approved by the U.S. Food & Drug Administration (“FDA”), are disclosed and described. More specifically, lower dosage strength imiquimod formulations to deliver an efficacious dose of imiquimod for treating actinic keratosis with an acceptable safety profile and dosing regimens that are short and more convenient for patient use than the dosing regimen currently approved by the U.S. Food & Drug Administration (“FDA”) for Aldara® 5% imiquimod cream to treat actinic keratosis are also disclosed and described.
    Type: Grant
    Filed: June 20, 2016
    Date of Patent: March 26, 2019
    Assignee: Medicis Pharmaceutical Corporation
    Inventors: Michael T. Nordsiek, Sharon F. Levy, James Hurn-Joung Lee, James H. Kulp, Kodumudi S. Balaji, Tze-Chiang Meng, Jason J. Wu, Valyn S. Bahm, Robert Babilon
  • Patent number: 10189834
    Abstract: The specification generally relates to compounds of Formula (I): and pharmaceutically acceptable salts thereof, where Q, R1, R2, R3, R4 and R5 have any of the meanings defined herein. The specification also relates to the use of such compounds and salts thereof to treat or prevent ATM kinase mediated disease, including cancer. The specification further relates to crystalline forms of compounds of imidazo[4,5-c]quinolin-2-one compounds and pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising such compounds and salts; kits comprising such compounds and salts; methods of manufacture of such compounds and salts; intermediates useful in the manufacture of such compounds and salts; and to methods of treating ATM kinase mediated disease, including cancer, using such compounds and salts.
    Type: Grant
    Filed: October 17, 2017
    Date of Patent: January 29, 2019
    Assignee: AstraZeneca AB
    Inventors: Bernard Christophe Barlaam, Kurt Gordon Pike
  • Patent number: 9962378
    Abstract: The administration of a compound advantageously efficacious as ROS1 inhibitor and its effect on subjects with cancer includes administering a compound having certain structural components such as a quinoline moiety in the backbone and at least one tertiary amine containing moiety in a side chain as well as heteroatoms, in particular oxygen atoms, present in the backbone and the side chain for treating a subject suffering from a disease such as cancer. The presence of such structural components allows for an advantageous interaction with the ROS1 kinase domain, in particular with the hinge region. The administered compounds represent a highly promising opportunity in particular for patients bearing ROS1-dependent cancer. A method for targeting tumor cells harboring an abnormality in ROS1 gene includes contacting a cell with compounds of the present invention as well as pharmaceutical compositions comprising such compounds.
    Type: Grant
    Filed: October 30, 2015
    Date of Patent: May 8, 2018
    Assignee: Macau University of Science and Technology
    Inventors: Xiao Jun Yao, Lai Han Leung, Lian Xiang Luo, Liang Liu
  • Patent number: 9913836
    Abstract: The present invention relates to a pharmaceutical composition comprising propiverine, trospium or glycopyrrolate; and a non-anticholinergic antiemetic agent. It is also related to a pharmaceutical composition comprising a high dose of solifenacin or a pharmaceutically acceptable salts thereof; and a non-anticholinergic antiemetic agent. Pharmaceutical compositions containing high dose of nsPAChA for use for increasing the AChEI blood concentrations and for combating neurodegeneration are also described. The invention also relates to a method for inducing neuroprotection and combating neurodegeneration in a patient suffering from Alzheimer type dementia as well as to a method for increasing the blood levels of an acetyl choline esterase inhibitor (AChEI) in a human subject treated with an AChEI dose.
    Type: Grant
    Filed: December 13, 2016
    Date of Patent: March 13, 2018
    Assignee: Chase Pharmaceuticals Corporation
    Inventors: Kathleen E. Clarence-Smith, Thomas N. Chase
  • Patent number: 9884866
    Abstract: The invention provides compounds of formula I: wherein R1-R3, Ra, and Rb have any of the values defined herein, and salts thereof. The compounds have immunomodulatory properties.
    Type: Grant
    Filed: September 3, 2015
    Date of Patent: February 6, 2018
    Assignee: Regents of the University of Minnesota
    Inventors: David M. Ferguson, John Ohlfest, Courtney Aldrich
  • Patent number: 9744145
    Abstract: This invention provides a method of treating lung cancer including administering a therapeutically effective amount of a compound of 0089-0022 formula I to a subject in need thereof. The compound activates pyruvate kinase M2 isoform (PKM2) to treat the lung cancer. In one example, the lung cancer is Non-Small Cell Lung Cancer (NSCLC).
    Type: Grant
    Filed: January 16, 2017
    Date of Patent: August 29, 2017
    Assignee: Macau University of Science and Technology
    Inventors: Liang Liu, Lai-Han Elaine Leung, Xiao-Jun Yao, Run-Ze Li
  • Patent number: 9650378
    Abstract: Substituted pyridoindoles for incorporation in pharmaceutical compositions employed in the treatment of various diseases correspond to formula (I) wherein R1 is H or optionally substituted alkyl; R2, R3, R4 are each independently selected from H, —O-alkyl, —S-alkyl, alkyl, halo, —CF3, and —CN; G is —CR12R13—NR5— or —NR5—CR12R13; R5 is H, optionally substituted alkyl, optionally substituted heterocycle, —C(?O)—R6, —C(?O)—O—R7, or —C(?O)—NR19R20; R6 and R7 are each optionally substituted alkyl or optionally substituted heterocycle; R8, R9, R10, R11, R12, R13, R19 and R20 are each independently selected from H or optionally substituted alkyl; R14 and R15 are each independently H or halogen; L is —CH2—O—, —CH2CH2—, —CH?CH— or a bond; and B is aryl or heteroaryl or cycloalkyl; with the proviso that, when L is a direct bond, B cannot be unsubstituted heteroaryl or heteroaryl monosubstituted with fluorine.
    Type: Grant
    Filed: February 17, 2016
    Date of Patent: May 16, 2017
    Assignee: Albany Molecular Research, Inc.
    Inventors: Peter Guzzo, Matthew David Surman, Alan John Henderson, May Xiaowu Jiang, Mark Hadden, James Grabowski, Alexander Usyatinsky
  • Patent number: 9492682
    Abstract: This disclosure is directed to the use of sequentially applied topical therapy with a lower dosage strength imiquimod composition and photodynamic therapy for treating actinic keratosis, wherein the photodynamic therapy is administered subsequent to the topical therapy with the imiquimod composition. In some embodiments, the imiquimod composition comprises from about 1% (w/w) to about 4.25% (w/w) imiquimod.
    Type: Grant
    Filed: September 14, 2012
    Date of Patent: November 15, 2016
    Assignee: Medicis Pharmaceutical Corporation
    Inventors: Michael H. Gold, Joel L. Cohen, Girish S. Munavalli, Tze-Chiang Meng
  • Patent number: 9494597
    Abstract: The present invention provides novel, rationally designed human control antibodies for use in various in vivo and in vitro applications. The antibodies of the present invention have well characterized variable domains that have been designed to minimize or eliminate antigen binding without altering gross antibody structure. Using the antibodies of the present invention in various assays allows researchers to distinguish effects that result from specific antigen-antibody interactions from other, non-specific antibody effects.
    Type: Grant
    Filed: April 2, 2013
    Date of Patent: November 15, 2016
    Assignee: AB BIOSCIENCES, INC.
    Inventors: Hsiu-Ching Chang, Yen-Ming Hsu, Jeng-Shin Lee
  • Patent number: 9381203
    Abstract: Provided herein are combination therapies for the treatment of progeroid diseases and conditions, cellular aging, bone diseases, and cardiovascular diseases. The provided combination therapies target the aberrant farnesylation of the mutant lamin A protein progerin, and inhibit farnesyl biosynthesis, lamin A prenylation, and increase progerin clearance.
    Type: Grant
    Filed: March 13, 2014
    Date of Patent: July 5, 2016
    Inventors: Leslie B. Gordon, Mark W. Kieran, Monica E. Kleinman
  • Patent number: 9370509
    Abstract: Pharmaceutical formulations and methods for the topical or transdermal delivery of 1-isobutyl-1H-imidazo[4,5-c]-quinolin-4-amine or 1-(2-methylpropyl)-1H-imidazo[4,5-c]quinolin-4-amine, i.e., imiquimod, to treat actinic keratosis with short durations of therapy, than currently prescribed for the commercially available Aldara® 5% imiquimod cream, as now approved by the U.S. Food & Drug Administration (“FDA”), are disclosed and described. More specifically, lower dosage strength imiquimod formulations to deliver an efficacious dose of imiquimod for treating actinic keratosis with an acceptable safety profile and dosing regimens that are short and more convenient for patient use than the dosing regimen currently approved by the U.S. Food & Drug Administration (“FDA”) for Aldara® 5% imiquimod cream to treat actinic keratosis are also disclosed and described.
    Type: Grant
    Filed: August 6, 2012
    Date of Patent: June 21, 2016
    Assignee: Medicis Pharmaceutical Corporation
    Inventors: Michael T. Nordsiek, Sharon F. Levy, James H. Lee, James H. Kulp, Kodumudi S. Balaji, Tze-Chiang Meng, Jason J. Wu, Valyn S. Bahm, Robert Babilon
  • Patent number: 9290509
    Abstract: An improved, high yielding process is disclosed for making bisglycidyl ether derivatives of isosorbide, isomannide and/or isoidide, wherein up to quantitative yields overall are demonstrated. In another related aspect, a process is disclosed for making novel monoallyl, monoglycidyl ether derivatives or a combination of monoallyl, monoglycidyl ether derivatives and bisglycidyl ether derivatives via the same diallyl isohexide intermediate.
    Type: Grant
    Filed: June 10, 2013
    Date of Patent: March 22, 2016
    Assignee: Archer Daniels Midland Company
    Inventor: Kenneth Stensrud
  • Patent number: 9226891
    Abstract: Disclosed are pharmaceutical compositions having a portion of aspirin for intraoral release and another aspirin for gastrointestinal release. The compositions can further include niacin. Methods of using such compositions to treat diseases or conditions suitably treated by niacin are also provided which result in reduced flushing.
    Type: Grant
    Filed: October 24, 2012
    Date of Patent: January 5, 2016
    Assignee: Vitalis LLC
    Inventor: Joseph Habboushe
  • Patent number: 9120769
    Abstract: The present invention relates to compounds defined by formula I wherein the variables R1, R2, R3, R4, and m are defined as in claim 1, possessing valuable pharmacological activity. Particularly, the compounds are inhibitors of 11?-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity, and dyslipidemia.
    Type: Grant
    Filed: February 26, 2014
    Date of Patent: September 1, 2015
    Assignee: Boehringer-Ingelheim International GmbH
    Inventors: Matthias Eckhardt, Hans-Juergen Martin, Martin Schuehle, Sandra Sick, Bing Shiou Yang
  • Patent number: 9066940
    Abstract: The present invention relates in general to the field of modulators of the innate immune system, particularly to pharmaceutical compositions comprising imidazoquinolin(amines) and derivatives thereof, preferably suitable for local administration, such as, intravesical administration. In addition, the present invention concerns the use of imidazoquinolin(amines) and derivatives thereof for intravesical treatment of bladder diseases, such as, for example, bladder cancer and cystitis. The present invention furthermore comprises methods of treatment for these diseases as well as methods of administration of the inventive pharmaceutical compositions.
    Type: Grant
    Filed: February 5, 2010
    Date of Patent: June 30, 2015
    Assignee: TELORMEDIX, SA
    Inventors: Lorenzo Leoni, Roberto Maj, Franco Pattarino, Carlo Vecchio
  • Patent number: 9056134
    Abstract: The present invention is in the fields of medicine, pharmaceuticals, nutraceuticals, endocrinology and cardiology. The invention provides compositions comprising a statin, an inhibitor of the angiotensin converting enzyme, an antiplatelet compound and an anti-hyperglycemic compound for use in the treatment and/or prevention of cardiometabolic risk factors of Metabolic Syndrome and treatment and/or prevention of Metabolic Syndrome. The present invention provides for the use of such compositions in the manufacture of products for treatment and/or prevention of Metabolic Syndrome. The biguanide metformin of the composition could be present in extended release form allowing its use together with the other drugs in a single dosage form at low dose. This combination of drugs in a single daily dosage greatly improves compliance and adherence to treatment which is a critical factor for treating patients with Metabolic Syndrome.
    Type: Grant
    Filed: July 21, 2011
    Date of Patent: June 16, 2015
    Assignee: NUCITEC S.A. DE C.V.
    Inventors: Miguel Angel Duarte-Vazquez, Sandra Garcia Padilla, Jorge Luis Rosado
  • Publication number: 20150140093
    Abstract: Compositions, methods of making, and methods of using nanoclusters in which the nanoclusters comprise a plurality of nanoparticles having a core of nanoparticles arranged such that the surfaces of the nanoparticles contact adjacent nanoparticles, the nanoparticles comprise an active ingredient, and the nanocluster has a mass median aerodynamic diameter of from about 0.25 ?m to about 20 ?m.
    Type: Application
    Filed: November 6, 2014
    Publication date: May 21, 2015
    Inventors: Cory J. Berkland, Lianjun Shi, Nashwa El Gendy, Carl Plumley, Mark Bailey
  • Publication number: 20150132410
    Abstract: The invention provides compositions for the prevention and treatment of the symptoms of alcoholic beverage-induced hangover syndrome, related kits and methods of using the compositions and kits.
    Type: Application
    Filed: November 12, 2014
    Publication date: May 14, 2015
    Inventor: Michael M. Jacobs
  • Publication number: 20150133442
    Abstract: The invention features compositions and methods for inhibiting the Pin1 protein, and the treatment of disorders characterized by elevated Pin1 levels.
    Type: Application
    Filed: June 7, 2013
    Publication date: May 14, 2015
    Inventors: Kun Ping Lu, Matthew Brian Boxer, Mindy Irene Emily Davis, Rajan Pragani, Min Shen, Anton Momtchilov Simeonov, Shuo Wei, Xiao Zhen Zhou
  • Patent number: 9023862
    Abstract: The use of a dopamine agonist in the manufacture of a medicament for the treatment or prevention of endometriosis.
    Type: Grant
    Filed: November 17, 2014
    Date of Patent: May 5, 2015
    Assignee: Ferring International Center S.A.
    Inventors: Antonio Pellicer-Martinez, Carlos Simon-Valles, Edurne Novella-Maestre
  • Patent number: 9000005
    Abstract: The present invention relates to highly-pure pyrroloquinolinyl-pyrrole-2,5-dione and pyrroloquinolinyl-pyrrolidine-2,5-dione, for example, 3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione, 3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione, and pharmaceutically acceptable salts, solvates, and diastereomers thereof. The present invention also relates to methods for preparing highly-pure pyrroloquinolinyl-pyrrole-2,5-dione and pyrroloquinolinyl-pyrrolidine-2,5-dione, for example, 3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione, 3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione, and pharmaceutically acceptable salts, solvates, and diastereomers thereof.
    Type: Grant
    Filed: March 7, 2013
    Date of Patent: April 7, 2015
    Assignee: ArQule, Inc.
    Inventors: Yoshitaka Nakamura, Jo Ooyama
  • Patent number: 8987294
    Abstract: The present invention is directed to novel compounds that are able to inhibit the interaction of paxillin or its paralogues, including leupaxin or Hic-5, with alpha.4 integrin or its binding partners that regulate signaling events downstream of the paxillin-.alpha.4 interaction. The present invention further relates to methods for therapeutic use of such compounds and pharmaceutical compositions of such compounds for the treatment of a disease or condition.
    Type: Grant
    Filed: September 15, 2010
    Date of Patent: March 24, 2015
    Assignee: The Regents of the University of California
    Inventors: Mark Ginsberg, Christiane Kummer
  • Patent number: 8980300
    Abstract: A biocompatible plasticizer useful for forming a coating composition with a biocompatible polymer is provided. The coating composition may also include a biobeneficial polymer and/or a bioactive agent. The coating composition can form a coating on an implantable device. The implantable device can be used to treat or prevent a disorder such as atherosclerosis, thrombosis, restenosis, hemorrhage, vascular dissection or perforation, vascular aneurysm, vulnerable plaque, chronic total occlusion, claudication, anastomotic proliferation for vein and artificial grafts, bile duct obstruction, ureter obstruction, tumor obstruction, or combinations thereof.
    Type: Grant
    Filed: May 29, 2009
    Date of Patent: March 17, 2015
    Assignee: Advanced Cardiovascular Systems, Inc.
    Inventors: Stephen Dirk Pacetti, Yiwen Tang, Syed Faiyaz Ahmed Hossainy
  • Publication number: 20150073010
    Abstract: The use of a dopamine agonist in the manufacture of a medicament for the treatment or prevention of endometriosis.
    Type: Application
    Filed: November 17, 2014
    Publication date: March 12, 2015
    Inventors: Antonio Pellicer-Martinez, Carlos Simon-Valles, Edurne Novella-Maestre
  • Patent number: 8975405
    Abstract: Disclosed is a compound of formula (I) and salts thereof. Also disclosed are methods of making the compound of formula (I) and the use of the compound as an intermediate for making pharmaceutically active compounds such as 11-?-hydroxysteroid hydrogenase type 1 (11-?-HSD1) inhibitors.
    Type: Grant
    Filed: December 13, 2013
    Date of Patent: March 10, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Bo Qu, Anjan Saha, Jolaine Savoie, Xudong Wei, Nathan K. Yee
  • Patent number: 8956662
    Abstract: The invention discloses a pharmaceutical composition comprising phenylephrine or a pharmaceutically acceptable salt thereof and an erodible layer which is for oral administration wherein the composition delivers phenylephrine or a pharmaceutically acceptable salt thereof via absorption in the colon. The pharmaceutical composition comprises a core comprising phenylephrine or a pharmaceutically acceptable salt thereof and an erodible layer which is in a time-dependent, pH-dependent, or colon-specific enzyme-dependent erodible layer that degrades to expose the core to release phenylephrine in the colon. In one preferred embodiment, the erodible layer encases the core. The composition optionally further comprises phenylephrine in the erodible layer or other additional layer(s).
    Type: Grant
    Filed: June 1, 2007
    Date of Patent: February 17, 2015
    Assignee: MSD Consumer Care, Inc.
    Inventors: David Monteith, John O'Mullane, Joseph P. Reo, Robert T. Nowak, Jiansheng Wan, Mohammed A. Kabir, Malaz A. Abutarif, Glenn E. Fritz
  • Patent number: 8957108
    Abstract: The invention relates to the areas of therapeutics, pharmaceuticals, drug discovery, and immunotherapy. More specifically, the present invention relates to methods of stimulating the immune system through the administration of flavone acetic acid [FAA] analogs, and in particular, the flavone acetic acid analog, 5,6-dimethylxanthenone-4-acetic acid (DMXAA) so as to comprise an antimicrobial therapeutic agent for the treatment of viral infections of DNA and RNA viruses in humans and non-human animals. The invention is especially suitable for use in a process of treating and preventing infection by, for example, rhinoviruses, enteroviruses, and influenza viruses.
    Type: Grant
    Filed: March 14, 2011
    Date of Patent: February 17, 2015
    Assignee: University of Maryland, Baltimore
    Inventors: Stefanie N. Vogel, Zachary J. Roberts, Jorge Blanco
  • Publication number: 20150045300
    Abstract: The subject invention is directed to a pharmaceutical composition comprising an open matrix network carrying a pharmaceutically active ingredient, wherein the open matrix network comprises both the polysaccharides levan and inulin.
    Type: Application
    Filed: September 7, 2012
    Publication date: February 12, 2015
    Applicant: FERRING B.V.
    Inventors: Varinder Ahuja, Tejas Gunjikar, Balachendar Gundu
  • Publication number: 20150038438
    Abstract: The present description relates to compounds and forms and pharmaceutical compositions thereof and methods for use thereof to treat or ameliorate bacterial infections caused by wild-type and multi-drug resistant Gram-negative and Gram-positive pathogens.
    Type: Application
    Filed: August 29, 2012
    Publication date: February 5, 2015
    Inventors: Arthur Branstrom, Vara Prasad Venkata Nagendra Josyula, Michael Andrew Arnold, Aleksey I. Gerasyuto, Gary Karp, Jiashi Wang, Guangming Chen, Olya Ginzburg, Song Huang, Jana Narasimhan, Srinivasa Peddi, Sean Wesley Smith, Anthony Allan Turpoff, Matthew G. Woll, Nanjing Zhang, Xiaoyan Zhang
  • Patent number: 8946422
    Abstract: The invention provides compound and salts of Formula I and II, disclosed herein, which includes compounds of Formula A and Formula B: Such compounds possess useful antimicrobial activity. The variables R2, R3, R5, R6, R7, and R9 shown in Formula A and B are defined herein. Certain compounds of Formula I and Formula II disclosed herein are potent and/or selective inhibitors of bacterial DNA synthesis and bacterial replication. The invention also provides antimicrobial compositions, including pharmaceutical compositions, containing one or more compounds of Formula I or Formula II and one or more carriers, excipients, or diluents. Such compositions may contain a compound of Formula I or Formula II as the only active agent or may contain a combination of a compound of Formula I or Formula II and one or more other active agents. The invention also provides methods for treating microbial infections in animals.
    Type: Grant
    Filed: October 24, 2011
    Date of Patent: February 3, 2015
    Assignee: Achillion Pharmaceuticals, Inc.
    Inventors: Barton James Bradbury, Jason Allan Wiles, Qiuping Wang, Akhiro Hashimoto, Edlaine Lucien, Godwin Clarence Gilroy Pais, Milind Deshpande, Micheal John Pucci, Ha Young Kim
  • Patent number: 8946260
    Abstract: The present invention provides compounds of Formula (I), or a pharmaceutically acceptable salt thereof, where R1, R2, R3, R4, R5, R6, A and n are as defined herein. A deuteriated derivative of the compound of Formula (I) is also provided.
    Type: Grant
    Filed: September 14, 2011
    Date of Patent: February 3, 2015
    Assignee: Novartis AG
    Inventors: Mark Gary Bock, Christoph Gaul, Venkateshwar Rao Gummadi, Henrik Moebitz, Saumitra Sengupta
  • Patent number: 8946153
    Abstract: The subject invention is directed to a pharmaceutical composition comprising an open matrix network carrying a pharmaceutically active ingredient, wherein the open matrix network comprises levan.
    Type: Grant
    Filed: March 28, 2011
    Date of Patent: February 3, 2015
    Assignee: Ferring B.V.
    Inventors: Shweta Gupta, Varinder Ahuja, Tejas Gunjikar, Kristin Wannerberger
  • Patent number: 8940755
    Abstract: The present invention provides therapeutic combinations that include an immune response modifier (IRM) component and an anti-inflammatory component. The inventions further provide methods of treating a condition by administering to one having the condition a therapeutic combination that includes an IRM component and an anti-inflammatory component.
    Type: Grant
    Filed: December 2, 2004
    Date of Patent: January 27, 2015
    Assignee: 3M Innovative Properties Company
    Inventors: Mark A. Tomai, Gary W. Gullikson, David M. Hammerbeck, Elaine A. Egging, Michael J. Reiter, Christopher D. Gram, John P. Vasilakos
  • Publication number: 20150025067
    Abstract: Inhibitors of p67phox protein are provided herein, as well as pharmaceutical compositions and methods relating thereto.
    Type: Application
    Filed: February 13, 2013
    Publication date: January 22, 2015
    Applicant: CHILDREN'S HOSPITAL MEDICAL CENTER
    Inventors: Yi Zheng, Prakash Jagtap, Emily E. Bosco, Jaroslaw Meller, Marie-Dominique Filippi
  • Publication number: 20150018381
    Abstract: Although it can be farnesylated, the mutant lamin A protein expressed in Hutchinson Gilford Progeria Syndrome (HGPS) cannot be defarnesylated because the characteristic mutation causes deletion of a cleavage site necessary for binding the protease ZMPSTE24 and effecting defarnesylation. The result is an aberrant farnesylated protein (called “progerin”) that alters normal lamin A function as a dominant negative, as well as assuming its own aberrant function through its association with the nuclear membrane. The retention of farnesylation, and potentially other abnormal properties of progerin and other abnormal lamin gene protein products, produces disease. Farnesyltransferase inhibitors (FTIs) (both direct effectors and indirect inhibitors) will inhibit the formation of progerin, cause a decrease in lamin A protein, and/or an increase prelamin A protein. Decreasing the amount of aberrant protein improves cellular effects caused by and progerin expression.
    Type: Application
    Filed: July 21, 2014
    Publication date: January 15, 2015
    Inventors: Leslie B. GORDON, Francis S. COLLINS, Thomas GLOVER, Michael W. GLYNN, Brian C. CAPELL, Adrienne D. COX, Channing J. DER
  • Publication number: 20150018290
    Abstract: The present invention generally relates to compositions containing chemical compounds and compositions and pharmaceutical formulations of the compounds which increase the expression of total hemoglobin or globin protein such as embryonic or fetal globin, or the proliferation of hemoglobin expressing and other blood cells. These compositions can be used to treat or prevent the symptoms associated with anemia, sickle cell diseases, thalassemia, and other blood cell deficiencies and blood disorders. The invention also relates to methods for administering these compositions to subjects and for use as medical aids for the treatment and prevention of blood and other disorders.
    Type: Application
    Filed: December 2, 2011
    Publication date: January 15, 2015
    Applicant: Trustees of Boston University
    Inventors: Susan Perrine, Douglas V. Faller
  • Publication number: 20150018382
    Abstract: Disclosed is the use of rupatadine in the manufacture of pharmaceutical composition for preventing or treating chronic obstructive bronchitis, obstructive emphysema or chronic obstructive pulmonary disease. The new medicament, i.e. rupatadine, for treating chronic obstructive pulmonary disease is obvious in therapeutic effects, and low in toxic and side effects, and safe in use in the aspects of treating chronic obstructive bronchitis, obstructive emphysema or chronic obstructive pulmonary disease.
    Type: Application
    Filed: May 18, 2012
    Publication date: January 15, 2015
    Applicant: Beiging Weifeng Yimin Bio-Technology Limited Company
    Inventor: Zhuowei Hu
  • Publication number: 20150011525
    Abstract: A stable ternary solid dispersion composition with enhanced physical stability and/or bioavailability comprising: (a) about 1% wt. to about 50% wt. of one or more poorly soluble active pharmaceutical ingredient (API) which belongs to Biopharmaceutics Classification System (BCS) class II and/or IV; (b) about 11% wt. to about 50% wt. of at least one water-soluble polymer; and (c) about 20% wt. to about 99% wt. of crosslinked polyvinylpyrrolidone (crospovidone, a water-insoluble polymer). The solid dispersion is capable of inhibiting crystallization of API in solid state and/or aqueous gastrointestinal tract (GIT) medium. Also disclosed is a method of preparation of such solid dispersion composition by fusion or solvent or fusion-solvent method.
    Type: Application
    Filed: September 13, 2012
    Publication date: January 8, 2015
    Applicant: ISP Investments Inc.
    Inventors: Yunxia Bi, Mohammed Abdul Rahman, James David Lester
  • Patent number: 8927568
    Abstract: The use of a dopamine agonist in the manufacture of a medicament for the treatment or prevention of endometriosis.
    Type: Grant
    Filed: February 1, 2008
    Date of Patent: January 6, 2015
    Assignee: Ferring International Center S.A.
    Inventors: Antonio Pellicer-Martinez, Carlos Simon-Valles, Edurne Novella-Maestre
  • Patent number: 8927569
    Abstract: A class of macrocyclic compounds of formula (I), wherein R1, R3, R4, Ra, Rb, A, Z, Y, X, M, W, n and m are defined herein, that are useful as inhibitors of viral proteases, particularly the hepatitis C virus (HCV) NS3 protease, are provided. Also provided are processes 5 for the synthesis and use of such macrocyclic compounds for treating or preventing HCV infection.
    Type: Grant
    Filed: July 17, 2008
    Date of Patent: January 6, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Steven Harper, Vincenzo Summa, Nigel J. Liverton, John A. McCauley, John W. Butcher, Marcello Di Filippo, Maria Emilia Di Francesco, Marco Ferrara, Joseph J. Romano, Michael T. Rudd
  • Publication number: 20140378398
    Abstract: The invention relates to a pharmaceutical combination comprising the compound of formula I or pharmaceutically acceptable salts thereof in combination with at least one second therapeutic agent 2. The pharmaceutical combination of the invention is suitable in the treatment or prevention of one or more conditions selected from type 1 diabetes mellitus, type 2 diabetes mellitus, impaired glucose tolerance and hyperglycemia. In addition the present invention relates to methods for preventing or treating of metabolic disorders and related conditions.
    Type: Application
    Filed: September 5, 2014
    Publication date: December 25, 2014
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Bradford S. HAMILTON, Thomas RAUCH, Manami TSUTSUMI
  • Publication number: 20140371210
    Abstract: A method of rapid transbuccal delivery of an active agent into the bloodstream is provided. The method can include providing a pharmaceutical composition comprising the active agent, resin and a volatile solvent and, optionally, water. In some embodiments, the method achieves a Tmax 60 minutes or less, an onset of therapeutic effect of 60 minutes or less, and/or achieves therapeutic serum levels of the active agent within 60 minutes or less. Related compositions also are provided.
    Type: Application
    Filed: October 12, 2012
    Publication date: December 18, 2014
    Applicant: Jaleva Pharmaceuticals, LLC
    Inventor: Alex Battaglia
  • Patent number: 8912209
    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: Grant
    Filed: May 20, 2013
    Date of Patent: December 16, 2014
    Assignee: Amakem NV
    Inventors: Dirk Leysen, Oliver Defert, Nadzeya Kaval, Petra Blom, Sandro Boland
  • Patent number: 8901115
    Abstract: The present invention provides compounds of Formula (Ia): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
    Type: Grant
    Filed: August 6, 2012
    Date of Patent: December 2, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Patrick Y. S. Lam, Charles G. Clark, James R. Corte, William R. Ewing, Paul J. Gilligan, Yoon Jeon, Wu Yang, Leon M. Smith, II, Yufeng Wang
  • Patent number: 8895581
    Abstract: The present invention encompasses compounds of general formula (1), wherein the groups R1 to R7, Qa, Qb, L, n and m are defined as in claim 1, which are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation, pharmaceutical preparations containing such compounds and their use as medicaments.
    Type: Grant
    Filed: May 17, 2011
    Date of Patent: November 25, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Darryl McConnell, Harald Engelhardt, Christiane Kofink
  • Patent number: 8895579
    Abstract: Disclosed are heterotricyclic compounds, pharmaceutical compositions, methods of treatment, and methods for selectively antagonizing a glutamate receptor. The pharmaceutical compositions may include and the methods may utilize heterotricyclic compounds that are glutamate analogues which have specificity for AMPA receptors. The pharmaceutical compositions may be utilized to treat or prevent neurological diseases or disorders.
    Type: Grant
    Filed: March 21, 2011
    Date of Patent: November 25, 2014
    Assignee: Northwestern University
    Inventors: Geoffrey T. Swanson, Martin B. Gill, Ryuichi Sakai, Masato Oikawa