Chalcogen Bonded Directly To Ring Carbon Of The Oxazole Ring Patents (Class 514/376)
  • Patent number: 10300046
    Abstract: The present invention relates to pharmaceutical compositions useful for administration for treating, preventing, or reducing the risk of microbial infections.
    Type: Grant
    Filed: September 9, 2016
    Date of Patent: May 28, 2019
    Assignee: MELINTA SUBSIDIARY CORP.
    Inventor: Danping Li
  • Patent number: 10035775
    Abstract: The present invention relates to novel compounds and their use in the prophylactic and/or therapeutic treatment of fibrosis and fibrosis-related conditions.
    Type: Grant
    Filed: March 18, 2016
    Date of Patent: July 31, 2018
    Assignee: VECTUS BIOSYSTEMS LIMITED
    Inventor: Karen Annette Duggan
  • Patent number: 9539218
    Abstract: The present invention relates to the field of blood coagulation, more specifically it relates to a method of treating a thromboembolic disorder by administering once daily a direct factor Xa inhibitor in oral dosage form to a patient in need thereof, wherein the factor Xa inhibitor has a plasma concentration half life indicative of a bid or tid administration interval, e.g. of 10 hours or less.
    Type: Grant
    Filed: January 19, 2006
    Date of Patent: January 10, 2017
    Assignee: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Frank Misselwitz, Dagmar Kubitza, Son-Mi Park, Klaus Wehling
  • Patent number: 9394228
    Abstract: Methods are disclosed to treat or prevent at least one disease or condition in a subject in need thereof comprising administering a compound of Formula (I): or a pharmaceutically acceptable salt, or ester thereof, wherein R1 and R2 are independently chosen from a hydrogen atom or linear, branched, and/or cyclic C1-C6 alkyl groups, with the proviso that R1 and R2 are not both hydrogen or a pharmaceutically acceptable salt or ester thereof. Such diseases or conditions may relate to coronary heart disease (CHD), for example atherosclerosis; metabolic syndrome/insulin resistance; and/or a dyslipidemic condition such as hypertriglyceridemia (HTG), elevated LDL-cholesterol, elevated total-cholesterol, elevated Apo B and low HDL-cholesterol. The present disclosure further provides for a method of reducing atherosclerosis development. Pharmaceutical compositions comprising a compound of Formula (I) are also disclosed.
    Type: Grant
    Filed: November 3, 2011
    Date of Patent: July 19, 2016
    Assignee: PRONOVA BIOPHARMA NORGE AS
    Inventors: Ragnar Hovland, Tore Skjæret, David Fraser
  • Patent number: 9376400
    Abstract: The present invention relates to processes for the preparation of triazoles. These compounds are useful as anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents.
    Type: Grant
    Filed: July 7, 2014
    Date of Patent: June 28, 2016
    Assignee: MELINTA THERAPEUTICS, INC.
    Inventors: Shili Chen, Rongliang Lou, Yusheng Wu, Jiacheng Zhou, Roger Hanselmann
  • Patent number: 9365482
    Abstract: Methods for the efficient synthesis of fatty acid derivatives and their intermediates are provided.
    Type: Grant
    Filed: February 27, 2014
    Date of Patent: June 14, 2016
    Assignee: Pronova Biopharma Norge AS
    Inventors: Tore Skjæret, Ragnar Hovland
  • Patent number: 9359341
    Abstract: The present invention relates to the prodrug of 5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxo-morpholin-4-yl)phenyl]-1,3-oxazolidin-5-yl}methyl)thiophene-2-carboxamide, rivaroxaban per se; processes for their preparation, and the application in treatment and/or prophylaxis of diseases, especially of thromboembolic disorders. The prodrug of a compound of formula (B) is chemically designated as 5-chloro-N-formyl-N-({(5S)-2-oxo-3-[4-(3-oxomorpholin-4-yl)phenyl]-1,3-oxazolidin-5-yl}methyl)thiophene-2-carboxamide.
    Type: Grant
    Filed: December 24, 2013
    Date of Patent: June 7, 2016
    Assignee: WANBURY LTD.
    Inventors: Nitin Sharadchandra Pradhan, Nilesh Sudhir Patil, Rajesh Ramchandra Walavalkar, Nilesh Subhas Kulkarni, Sandip Babanrao Pawar, Tarak Sambhaji Pawar
  • Patent number: 9345681
    Abstract: The present invention provides an agent for preventing the increase in a body weight (or for decreasing a body weight) or an anti-obesity agent each comprising at least one component selected from the group consisting of EPA and pharmaceutically acceptable salts, esters and derivatives thereof as an active ingredient for obesity in which the increase in the formation of hepatic lipid or the occurrence of fatty liver is mild, preferably the increase in the formation of hepatic lipid or the occurrence of fatty liver is not observed.
    Type: Grant
    Filed: July 6, 2012
    Date of Patent: May 24, 2016
    Assignee: MOCHIDA PHARMACEUTICAL CO., LTD.
    Inventors: Takayuki Ishida, Hiroyuki Kawano
  • Patent number: 9255066
    Abstract: A pharmaceutical composition, comprising a therapeutically effective amount of an active pharmaceutical ingredient (API) compound represented by the following structural formula at least one acidifying agent; and a vehicle base comprising at least one pharmaceutically acceptable non-aqueous solvent. Values and preferred values of the variables in structural formula (I) are defined herein.
    Type: Grant
    Filed: October 13, 2011
    Date of Patent: February 9, 2016
    Assignee: TetraLogic Shape UK Ltd
    Inventors: Todd W. Chappell, Keith A. Johnson
  • Patent number: 9180120
    Abstract: The present application relates to novel substituted N-phenethyltriazoloneacetamides, to processes for preparing them, to their use alone or in combinations for the treatment and/or prevention of diseases and also to their use for the production of medicaments for the treatment and/or prevention of diseases, more particularly for the treatment and/or prevention of cardiovascular disorders.
    Type: Grant
    Filed: August 31, 2011
    Date of Patent: November 10, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Chantal Fürstner, Joerg Keldenich, Martina Delbeck, Peter Kolkhof, Axel Kretschmer, Elisabeth Pook, Carsten Schmeck, Hubert Trübel
  • Publication number: 20150148386
    Abstract: The present invention relates to oxazolidinone compounds represented by Chemical Formula 1, pharmaceutically acceptable salts thereof or hydrates, a method of preparing the same, and a pharmaceutical composition for preventing or treating Hepatitis C infection: Wherein R1, R7 and X are defined in the detailed description.
    Type: Application
    Filed: November 12, 2014
    Publication date: May 28, 2015
    Applicants: POSTECH ACADEMY-INDUSTRY FOUNDATION, KOREA INSTITITE OF SCIENCE AND TECHNOLOGY
    Inventors: Sung Key JANG, GYO CHANG KEUM, Eunice Eun-Kyeong KIM, Soon Bang KANG, Suyeon YEOM, Juhyeon LEE, SeongGi LEE, HEE SUN KIM
  • Publication number: 20150133431
    Abstract: This invention relates to geranylgeranyl acetone (GGA) derivatives, pharmaceutical compositions comprising GGA derivatives and the use of GGA derivatives.
    Type: Application
    Filed: July 10, 2014
    Publication date: May 14, 2015
    Applicant: COYOTE PHARMACEUTICALS, INC.
    Inventor: Gary C. Look
  • Publication number: 20150119431
    Abstract: (R)-Nifuratel is disclosed together with its use as bactericide and bacteriostatic agent as well as the pharmaceutical compositions containing the same; (R)-nifuratel has been surprisingly found to possess a better antimicrobial profile than either nifuratel racemate or (S)-nifuratel. A new procedure for the synthesis of both (R)-Nifuratel and (S)-Nifuratel is also disclosed.
    Type: Application
    Filed: March 13, 2013
    Publication date: April 30, 2015
    Inventors: Stefania Gagliardi, Alessandra Consonni, Federico Mailland, Anna Bulgheroni
  • Publication number: 20150119376
    Abstract: The present invention relates to cycloalkenyl aryl derivatives, isomers thereof, pharmaceutically acceptable salts thereof, hydrates thereof, or solvates thereof; a method for preparing the derivatives; and pharmaceutical compositions containing the same. The compounds of the present invention show the effect of CETP activity inhibition. It means that the compounds can increase HDL-cholesterol and decrease LDL-cholesterol.
    Type: Application
    Filed: April 12, 2012
    Publication date: April 30, 2015
    Applicant: CHONG KUN DANG PHARMACEUTICAL CORP.
    Inventors: SeoHee LEE, JungTaek OH, JaeKwang LEE, JaeWon LEE, Suyeal BAE, Nina HA, Sera LEE
  • Publication number: 20150099696
    Abstract: The present invention relates to compounds of the general formula (I), their tautomeric forms, their stereoisomers, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, methods for their preparation, use of these compounds in medicine and the intermediates involved in their preparation. The present invention is directed to compounds suitable for the treatment of Disease conditions such as hyperlipidemia.
    Type: Application
    Filed: June 26, 2012
    Publication date: April 9, 2015
    Applicant: Cadila Healthcare Limited
    Inventors: Harikishore Pingali, Pankaj Makadia, Vrajesh Pandya, Sairam V.V.M. Kalapatapu
  • Patent number: 8987256
    Abstract: The present application relates to novel carboxylic acid derivatives having an oxo-substituted azaheterocyclic partial structure, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for producing medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prevention of cardiovascular disorders.
    Type: Grant
    Filed: April 6, 2009
    Date of Patent: March 24, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Michael Hahn, Eva-Maria Becker, Andreas Knorr, Dirk Schneider, Johannes-Peter Stasch, Karl-Heinz Schlemmer, Frank Wunder, Friederike Stoll, Stefan Heitmeier, Klaus Münter, Nils Griebenow, Thomas Lampe, Sherif El Sheikh, Volkhart Min-Jian Li
  • Publication number: 20150080442
    Abstract: Disclosed are preparations and formulations of high thermodynamic activity lipophilic associations (LA), in which there is pairing between an ionizable pharmaceutical agent and a lipophilic species having ionic characteristics opposite to that of the pharmaceutical agent. Such lipophilic associations manifest high thermodynamic activity, as evidenced by their being predominantly in a liquid phase at room temperature or solvated in a lower-than-water dielectric solvent. Further the pharmaceutical agent being solubilized means that dissolution is not rate limiting to transmucosal absorption. This LA or LA-solvate is formulated into a low dielectric dosage form, from whence, upon the dosage form's hydration, the pharmaceutical agent is driven through the mucosal tissue and into systemic circulation. The invention therefore provides an enhanced transmucosal drug delivery system for ionizable pharmaceutical agents at or near physiological pH.
    Type: Application
    Filed: March 10, 2014
    Publication date: March 19, 2015
    Inventor: John McCarty
  • Publication number: 20150072970
    Abstract: The present invention relates generally to the field of anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. More particularly, the invention relates to a family of compounds having both a biaryl moiety and at least one heterocylic moiety that are useful as such agents.
    Type: Application
    Filed: May 19, 2014
    Publication date: March 12, 2015
    Applicant: MELINTA THERAPEUTICS, INC.
    Inventors: Jiacheng Zhou, Ashoke Bhattacharjee, Shili Chen, Yi Chen, Jay J. Farmer, Joel A. Goldberg, Roger Hanselmann, Rongliang Lou, Alia Orbin, Adegboyega K. Oyelere, Joseph M. Salvino, Dane M. Springer, Jennifer Tran, Deping Wang, Yusheng Wu
  • Publication number: 20150056164
    Abstract: This invention relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.
    Type: Application
    Filed: April 24, 2014
    Publication date: February 26, 2015
    Applicant: AbbVie Inc.
    Inventors: David A. Betebenner, John K. Pratt, David A. DeGoey, Pamela L. Donner, Charles A. Flentge, Douglas K. Hutchinson, Warren M. Kati, Allan C. Krueger, Kenton L. Longenecker, Clarence J. Maring, John T. Randolph, Todd W. Rockway, Michael D. Tufano, Rolf Wagner, Dachun Liu
  • Publication number: 20150057301
    Abstract: This invention relates generally to stimulating neurogenesis (e.g., post-natal neurogenesis, e.g., post-natal hippocampal neurogenesis) and protectiong from neuron cell death.
    Type: Application
    Filed: July 24, 2014
    Publication date: February 26, 2015
    Inventors: Steven L. McKnight, Joseph M. Ready, Andew A. Pieper, Jef K. De Brabander
  • Publication number: 20150038501
    Abstract: Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C.
    Type: Application
    Filed: October 20, 2014
    Publication date: February 5, 2015
    Inventors: Leping LI, Min ZHONG
  • Publication number: 20150031685
    Abstract: The present invention relates to a series of substituted compounds having the general formula (I), including their stereoisomers and/or their pharmaceutically acceptable salts, wherein R1, R2, R3, R4, R5, and R6 are as defined herein. This invention also relates to methods of making these compounds including intermediates. The compounds of this invention are effective at the kappa (?) opioid receptor (KOR) site. Therefore, the compounds of this invention are useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of central nervous system disorders (CNS), including but not limited to acute and chronic pain, and associated disorders, particularly functioning peripherally at the CNS.
    Type: Application
    Filed: March 5, 2013
    Publication date: January 29, 2015
    Applicant: Dr. Reeddy's Laboratories Ltd.
    Inventors: Pradip Kumar Sasmal, Chintakunta Vamseekrishna, Vijay Potluri, Ashok Tehim, Yonghua Gai, Hang Zhang
  • Publication number: 20150033373
    Abstract: A novel canola variety designated VR 9561 GS and seed, plants and plant parts thereof, produced by crossing Pioneer Hi-Bred International, Inc. proprietary inbred canola varieties. Methods for producing a canola plant that comprises crossing canola variety VR 9561 GS with another canola plant. Methods for producing a canola plant containing in its genetic material one or more traits introgressed into VR 9561 GS through backcross conversion and/or transformation, and to the canola seed, plant and plant part produced thereby. This discovery relates to the canola variety VR 9561 GS, the seed, the plant produced from the seed, and variants, mutants, and minor modifications of canola variety VR 9561 GS. This discovery further relates to methods for producing canola varieties derived from canola variety VR 9561 GS.
    Type: Application
    Filed: July 23, 2013
    Publication date: January 29, 2015
    Applicant: PIONEER HI BRED INTERNATIONAL INC
    Inventors: Jayantilal Devabhai Patel, Igor Falak, Winnifred Marie Mcnabb
  • Patent number: 8937056
    Abstract: The present invention provides compounds, pharmaceutical compositions and methods for the treatment of specific cancers. Such compositions may generally comprise a compound of formula (I): wherein R1-R3 are as defined herein, or pharmaceutically acceptable salts or esters thereof; and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: March 11, 2013
    Date of Patent: January 20, 2015
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Sergei Agoulnik, Bruce Decosta, Hong Du, Yimin Jiang, Xiang-Yi Li, Kenichi Nomoto, John (Yuan) Wang, Huiming Zhang
  • Publication number: 20150011595
    Abstract: The invention relates to novel oxazolidinones their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering cholesterol ester transfer protein inhibitors.
    Type: Application
    Filed: May 6, 2014
    Publication date: January 8, 2015
    Applicant: Concert Pharmaceuticals, Inc.
    Inventor: Roger D. Tung
  • Publication number: 20150010619
    Abstract: The present invention generally relates to the transdermal delivery of various compounds. In some aspects, transdermal delivery may be facilitated by the use of a hostile biophysical environment. One set of embodiments provides a composition for topical delivery comprising ergopeptines, triptans, and other compounds, including salts and derivatives of these, and optionally, a hostile biophysical environment and/or a nitric oxide donor. In some cases, the composition may be stabilized using a combination of a stabilization polymer (such as xanthan gum, KELTROL® BT and/or KELTROL® RD), propylene glycol, and a polysorbate surfactant such as Polysorbate 20, which combination unexpectedly provides temperature stability to the composition, e.g., at elevated temperatures such as at least 40° C. (at least about 104° F.), as compared to compositions lacking one or more of these.
    Type: Application
    Filed: September 26, 2014
    Publication date: January 8, 2015
    Applicant: Strategic Science & Technologies, LLC
    Inventor: Eric T. Fossel
  • Patent number: 8927585
    Abstract: The present invention relates to spirocarbamate analogs, pharmaceutical compositions containing them and their use as TRPV4 antagonists.
    Type: Grant
    Filed: June 15, 2012
    Date of Patent: January 6, 2015
    Assignee: GlaxoSmithKline Intellectual Property (NO.2) Limited
    Inventors: Carl Brooks, Mui Cheung, Krista B. Goodman, Marlys Hammond
  • Publication number: 20140371210
    Abstract: A method of rapid transbuccal delivery of an active agent into the bloodstream is provided. The method can include providing a pharmaceutical composition comprising the active agent, resin and a volatile solvent and, optionally, water. In some embodiments, the method achieves a Tmax 60 minutes or less, an onset of therapeutic effect of 60 minutes or less, and/or achieves therapeutic serum levels of the active agent within 60 minutes or less. Related compositions also are provided.
    Type: Application
    Filed: October 12, 2012
    Publication date: December 18, 2014
    Applicant: Jaleva Pharmaceuticals, LLC
    Inventor: Alex Battaglia
  • Publication number: 20140364398
    Abstract: The present invention is directed to a new class of hydroxamic acid derivatives, their use as LpxC inhibitors, and more specifically their use to treat bacterial infections.
    Type: Application
    Filed: August 27, 2014
    Publication date: December 11, 2014
    Applicant: PFIZER INC.
    Inventors: Matthew Frank Brown, Anthony Marfat, Michael Joseph Melnick, Usa Reilly
  • Patent number: 8906949
    Abstract: Silicon dioxide free orally disintegrating tablet formulations of zolmitriptan or a pharmaceutically acceptable salt thereof having magnesium carbonate heavy and sodium stearyl fumarate with one or more pharmaceutically acceptable excipients and a process for preparing such a formulation and its use in the treatment of migraines.
    Type: Grant
    Filed: May 20, 2011
    Date of Patent: December 9, 2014
    Assignee: Sanovel Ilac Sanayi Ve Ticaret Anonim Sirketi
    Inventors: Umit Cifter, Ali Turkyilmaz, Gulay Yelken
  • Patent number: 8906913
    Abstract: The present invention relates to novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers including R and S isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The invention also relates to processes for the synthesis of novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers, polymorphs, prodrugs, metabolites, salts or solvates thereof.
    Type: Grant
    Filed: June 22, 2010
    Date of Patent: December 9, 2014
    Assignee: Panacea Biotec Limited
    Inventors: Rajesh Jain, Sanjay Trehan, Jagattaran Das, Gurmeet Kaur, Sandeep Kanwar, Nishan Singh, Gurmeet Kaur Nanda, Sitaram Kumar Magadi, Sudhir Kumar Sharma
  • Publication number: 20140350059
    Abstract: The present invention relates to novel derivatives of oxazolidinone, a method thereof and pharmaceutical compositions comprising the derivatives for use in an antibiotic. The oxazolidinone derivatives of the present invention show inhibitory activity against a broad spectrum of bacteria and lower toxicity. The prodrugs, prepared by reacting the compound having hydroxyl group with amino acid or phosphate, have an excellent efficiency on solubility thereof against water. Further, the derivatives of the present invention may exert potent antibacterial activity versus various human and animal pathogens, including Gram-positive bacteria such as Staphylococi, Enterococci and Streptococi, anaerobic microorganisms such as Bacteroides and Clostridia, and acid-resistant microorganisms such as Mycobacterium tuberculosis and Mycobacterium avium. Accordingly, the compositions comprising the oxazolidinone are used in an antibiotic.
    Type: Application
    Filed: August 13, 2014
    Publication date: November 27, 2014
    Inventors: Jae Keol RHEE, Weon Bin IM, Chong Hwan CHO, Sung Hak CHOI, Tae Ho LEE
  • Patent number: 8894979
    Abstract: The present invention relates to a composition including at least one C7 sugar, or derivative from esterification of said sugar, and a pharmaceutically acceptable carrier for treating alopecia. The present invention also relates to a method for cosmetically treating hair and nails, said method being intended to stimulate the growth thereof and/or slow the loss thereof. According to said method, a cosmetic composition including at least one C7 sugar, or derivative from esterification of said sugar, is administered. The present invention finally relates to a method for cosmetic care of hair and/or eyelashes and/or nails.
    Type: Grant
    Filed: December 15, 2010
    Date of Patent: November 25, 2014
    Assignee: Laboratoires Expanscience
    Inventors: Caroline Baudouin, Philippe Msika
  • Publication number: 20140343018
    Abstract: This technology relates generally to compounds and methods for stimulating neurogenesis (e.g., post-natal neurogenesis, including post-natal hippocampal and hypothalamic neurogenesis) and/or protecting neuronal cell from cell death. Various compounds are disclosed herein. In vivo activity tests suggest that these compounds may have therapeutic benefits in neuropsychiatric and/or neurodegenerative diseases such as schizophrenia, major depression, bipolar disorder, normal aging, epilepsy, traumatic brain injury, post-traumatic stress disorder, Parkinson's disease, Alzheimer's disease, Down syndrome, spinocerebellar ataxia, amyotrophic lateral sclerosis, Huntington's disease, stroke, radiation therapy, chronic stress, abuse of a neuro-active drug, retinal degeneration, spinal cord injury, peripheral nerve injury, physiological weight loss associated with various conditions, as well as cognitive decline associated with normal aging, chemotherapy, and the like.
    Type: Application
    Filed: July 24, 2014
    Publication date: November 20, 2014
    Inventors: Steven L. McKnight, Andew A. Pieper, Joseph M. Ready, Jef K. De Brabander, Jeffrey M. Zigman
  • Publication number: 20140336228
    Abstract: Provided is a pharmaceutical composition for preventing or treating hyperlipidemia comprising (4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-3-({2-[4-fluoro-2-methoxy-5-(propan-2-yl)phenyl]-5-(trifluoromethyl)phenyl}methyl)-4-methyl-1,3-oxazolidin-2-one or its pharmaceutically acceptable salt; and a calcium channel blocker or a fibrate as active ingredients.
    Type: Application
    Filed: November 28, 2012
    Publication date: November 13, 2014
    Applicant: DAEWOONG PHARMACEUTICAL CO., LTD.
    Inventors: Jong-Wook Lee, Sang-Ho Lee, Taek-Joo Lim, Eun-Ji Koh
  • Publication number: 20140336229
    Abstract: Provided is a pharmaceutical composition for preventing or treating hyperlipidemia comprising (4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-3-({2-[4-fluoro-2-methoxy-5-(propan-2-yl)phenyl]-5-(trifluoromethyl)phenyl}methyl)-4-methyl-1,3-oxazolidin-2-one or its pharmaceutically acceptable salt; and an angiotensin II receptor blocker as active ingredients.
    Type: Application
    Filed: November 28, 2012
    Publication date: November 13, 2014
    Applicant: DAEWOONG PHARMACEUTICAL CO., LTD.
    Inventors: Jong-Wook Lee, Sang-Ho Lee, Taek-Joo Lim, Eun-Ji Koh
  • Publication number: 20140329849
    Abstract: The disclosure relates to diseases in the peripheral nervous system, particularly hereditary neuropathies, such as Charcot-Marie-Tooth (CMT) disease. It is shown that this disease is associated with decreased acetylated tubulin levels, which can be overcome by inhibition of histone deacetylases (HDACs). Using HDAC inhibitors, it is shown herein that the symptoms of the CMT phenotype can be overcome both in vitro and in vivo. Also provided herein are two different mouse models of CMT disease.
    Type: Application
    Filed: July 18, 2014
    Publication date: November 6, 2014
    Inventors: Ludo Van Den Bosch, Constantin Van Outryve d'Ydewalle, Wim Robberecht
  • Publication number: 20140329835
    Abstract: Oral dosage forms as a biodegradable, water soluble film for delivering pharmaceutically active agents, to patients through insertion into the mouth of patient and methods for administering pharmaceutically active agents to patients by insertion into the mouth to provide selective uptake of said agents through the mucosa and thus avoiding the gastrointestinal tract.
    Type: Application
    Filed: June 19, 2014
    Publication date: November 6, 2014
    Inventors: Je Phil Ryoo, Chun Kwong Chu, Zheng Wang
  • Publication number: 20140323519
    Abstract: This invention relates to novel heterocyclic compounds that are useful for treating cancer and other cellular proliferative diseases and/or disorders associated with B-Raf activity. The compounds of the invention may be illustrated by the Formula (I).
    Type: Application
    Filed: April 20, 2012
    Publication date: October 30, 2014
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: M. Arshad Siddiqui, Lianyun Zhao, Amit K. Mandal
  • Patent number: 8871793
    Abstract: The invention relates to improvements of the physiochemical and/or the pharmaceutical properties of metaxalone. Disclosed herein are several new cocrystals of metaxalone, including: a 1:1 metaxalone adipic acid cocrystal, a 1:0.5 metaxalone fumaric acid cocrystal, a 1:1 metaxalone salicyclic acid cocrystal, a 1:0.5 metaxalone succinic acid cocrystal, and a 1:0.5 metaxalone maleic acid cocrystal. The therapeutic uses of these metaxalone cocrystals are described as well as therapeutic compositions containing them.
    Type: Grant
    Filed: December 22, 2010
    Date of Patent: October 28, 2014
    Assignee: Nuformix Limited
    Inventors: Joanne Holland, Christopher Frampton, Alan Chorlton, Daniel Gooding
  • Publication number: 20140315953
    Abstract: A method for treating migraines is disclosed. The method utilizes a rapid drug delivery system which prevents deactivation or degradation of the active agent, including small molecules and peptides being administered to a patient in need of treatment. In particular, the drug delivery system is designed for inhalation for delivery of drugs to the pulmonary circulation in a rapid and therapeutically effective manner.
    Type: Application
    Filed: June 16, 2014
    Publication date: October 23, 2014
    Inventors: Andrea Leone-Bay, Grayson W. Stowell, Joseph J. Guarneri, Dawn M. Carlson, Marshall Grant, Chad C. Smutney
  • Publication number: 20140315808
    Abstract: A method of treating a disease or condition in which up-regulating GAGs is therapeutically beneficial is disclosed. The method comprises locally administering to a subject a therapeutically effective amount of an agent capable of down-regulating activity or expression of a component of the renin-angiotensin system.
    Type: Application
    Filed: June 30, 2014
    Publication date: October 23, 2014
    Inventors: Talia WEINSTEIN, Uzi GAFTER, Zvi NEVO, Dror ROBINSON, Zoharia EVRON
  • Publication number: 20140302127
    Abstract: The present invention relates to methods for producing particles of metaxalone using dry milling processes as well as compositions comprising metaxalone, medicaments produced using metaxalone in particulate form and/or compositions, and to methods of treatment of an animal, including man, using a therapeutically effective amount of metaxalone administered by way of said medicaments.
    Type: Application
    Filed: April 10, 2014
    Publication date: October 9, 2014
    Applicant: ICEUTICA PTY LTD.
    Inventors: Aaron DODD, Felix MEISER, Marck NORRET, Adrian RUSSELL, H. William BOSCH
  • Publication number: 20140303198
    Abstract: Provided is an agent for treating and/or preventing obesity. An agent for suppressing expression of NPC1L1 (Niemann-Pick disease, type C1, gene-like 1) and/or LIPG (Lipase, endothelial) mRNA, and an agent for preventing and/or treating obesity, each comprising, as an active ingredient, a compound having CETP inhibitory activity, or a salt thereof, or a solvate thereof.
    Type: Application
    Filed: November 28, 2012
    Publication date: October 9, 2014
    Applicant: KOWA COMPANY, LTD.
    Inventors: Takeshi Murakami, Kentaro Murakami, Tadaaki Ohgiya, Kimiyuki Shibuya
  • Patent number: 8846667
    Abstract: The application describes an assay for the identification of small molecule modulators of integrin CD11b/CD18 and small molecules capable of modulating activity of this receptor. Such compounds may be used in certain embodiments for treating a disease or condition selected from inflammation, immune-related disorders, cancer, ischemia-reperfusion injury, stroke, neointimal thickening associated with vascular injury, bullous pemphigoid, neonatal obstructive nephropathy, and cardiovascular disease, or in other embodiments for the treatment of a disease or condition selected from immune deficiency, acquired immune deficiency syndrome (AIDS), myeloperoxidase deficiency, Wiskott-Aldrich syndrome, chronic granulomatous disease, hyper-IgM syndromes, leukocyte adhesion deficiency, Chediak-Higashi syndrome, and severe combined immunodeficiency.
    Type: Grant
    Filed: September 13, 2012
    Date of Patent: September 30, 2014
    Assignee: The General Hospital Corporation
    Inventors: Vineet Gupta, M. Amin Arnaout
  • Patent number: 8846746
    Abstract: The present invention provides a pyrazole compound of the following general Formula [Ib] having SGLT1 inhibitory activity, or a pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising the same, and its pharmaceutical use: wherein each symbol is the same as defined in the description.
    Type: Grant
    Filed: August 30, 2012
    Date of Patent: September 30, 2014
    Assignee: Japan Tobacco Inc.
    Inventors: Tomoya Miura, Yosuke Ogoshi, Kazuhito Ueyama, Dai Motoda, Toshihiko Iwayama, Koichi Suzawa, Hironobu Nagamori, Hiroshi Ueno, Akihiko Takahashi, Kazuyuki Sugimoto
  • Publication number: 20140288106
    Abstract: The present invention relates to compounds of formula 1 that are useful for the preventive or therapeutic treatment of diseases caused by abnormal activation of CXCR3 chemokines. The invention relates furthermore to a process for the preparation of said compounds, to pharmaceutical compositions containing said compounds and to novel intermediates used in the preparation of said compounds.
    Type: Application
    Filed: June 3, 2014
    Publication date: September 25, 2014
    Applicant: Sanofi
    Inventors: Imre BATA, Peter BUZDER-LANTOS, Attila VASAS, Veronika BARTANE BODOR, Gyorgy FERENCZY, Zsuzsanna TOMOSKOZI, Gabor SZELECZKY, Sandor BATORI, Martin SMRCINA, Marcel PATEK, Aleksandra WEICHSEL, David Squire Thorpe
  • Publication number: 20140275133
    Abstract: The present invention is directed to compounds of the Formula (I) as well as pharmaceutically acceptable salts thereof that are possible useful for treating aldosterone-mediated diseases. The invention furthermore relates to processes for preparing compounds of the Formula (I), to their possible use for the treatment of the above mentioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical compositions which comprise compounds of the Formula (I).
    Type: Application
    Filed: October 8, 2012
    Publication date: September 18, 2014
    Inventors: Hong Shen, Jason M. Cox, Hong Dong Chu
  • Patent number: 8835426
    Abstract: This invention relates to novel compounds of the Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11?-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds of the Formula (I) and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.
    Type: Grant
    Filed: February 26, 2008
    Date of Patent: September 16, 2014
    Assignee: Vitae Pharmaceuticals, Inc.
    Inventors: David A. Claremon, Gerard McGeehan, Suresh B. Singh, Colin M. Tice, Yuanjie Ye, Wei Zhao
  • Publication number: 20140255466
    Abstract: The present invention relates to a composition for enhancing transdermal absorption of a drug, containing a polyvalent alcohol having 3 to 8 carbon atoms, an organic acid having 2 to 20 carbon atoms, and a higher alcohol having 12 to 20 carbon atoms, and a patch preparation containing a support and a drug-containing adhesive layer containing the composition on one surface of the support.
    Type: Application
    Filed: March 10, 2014
    Publication date: September 11, 2014
    Applicant: Nitto Denko Corporation
    Inventors: Tsuyoshi MUKOBATA, Arimichi OKAZAKI, Akinori HANATANI, Sachiko SAKAMOTO