Chalcogen Bonded Directly To Ring Carbon Of The Piperidine Ring Patents (Class 514/327)
  • Patent number: 11945779
    Abstract: The present invention relates to a pharmaceutical composition for preventing or treating cancer metastasis, a health functional food, and a method for preventing or treating cancer metastasis using the same, containing a novel compound for inhibiting migration and invasion of cancer cells or a pharmaceutically acceptable salt thereof as an active ingredient.
    Type: Grant
    Filed: May 2, 2019
    Date of Patent: April 2, 2024
    Assignee: VSPHARMTECH
    Inventors: Byoung-Mog Kwon, Dong Cho Han, Yae Jin Yoon, Yu Jin Lee, Jiyoun Choi, Sangku Lee
  • Patent number: 11786522
    Abstract: The present invention belongs to the field of pharmaceutical formulation, and particularly relates to an aripiprazole injectable suspension formulation having prolonged shelf life, and methods of using the formulation in treating schizophrenia and related diseases. In another aspect, the present invention also relates to a method of prolonging shelf life of an aripiprazole injectable suspension formulation.
    Type: Grant
    Filed: March 16, 2016
    Date of Patent: October 17, 2023
    Assignee: Nanjing Noratech Pharmaceuticals Co., LTD
    Inventors: Yunzhe Sun, Qi Peng, Cheng-Gang Lin, Li Gui, Zhihui Liu, Fei Liu
  • Patent number: 11708329
    Abstract: The present disclosure relates to compounds that are capable of modulating the WNT/Beta-Catenin pathway. The disclosure further relates to methods of treating colorectal cancer and other WNT/Beta-Catenin mediated cancers.
    Type: Grant
    Filed: January 30, 2019
    Date of Patent: July 25, 2023
    Assignee: The Regents of the University of California
    Inventors: Michael E. Jung, Xiaohong Chen, Cun-Yu Wang, Jiong Li, Jie Zheng
  • Patent number: 11642335
    Abstract: A method of synthesizing a clopidogrel metabolite is provided. A piperidone intermediate is formed from a mandelate. An asymmetric ketone reduction of the piperidone intermediate is performed. A mercapto installation is performed on the piperidone intermediate to form a clopidogrel metabolite that includes a 4-carbon chiral center having an (R) configuration.
    Type: Grant
    Filed: September 28, 2020
    Date of Patent: May 9, 2023
    Assignee: Board of Regents, The University of Texas System
    Inventor: Yaoqiu Zhu
  • Patent number: 11338010
    Abstract: Systems, methods, and kits for treating, preventing, and diagnosing viral infection using an androgen mediated pathway are described. Additionally, methods and kits for guiding treatment of viral respiratory disease are described by a method for testing for polymorphisms in the androgen receptor gene. Further, systems and methods for treatment of viral respiratory disease with various anti-androgens is detailed. Finally, systems, methods, and kits for treating, preventing, and diagnosing SARS-CoV-2 (COVID-19) are presented.
    Type: Grant
    Filed: May 21, 2020
    Date of Patent: May 24, 2022
    Assignee: SUZHOU KINTOR PHARMACEUTICALS, INC.
    Inventors: Ofer A. Goren, John McCoy
  • Patent number: 11273152
    Abstract: This invention relates to the finding that Piperlongumine compounds, such as Piperlongumine and analogues, derivatives and prodrugs thereof, are reversible, allosteric antagonists of transient receptor potential vanilloid 2 channel (TRPV2). Methods of treatment of conditions that are characterised by TRPV2 expression using Piperlongumine compounds and Piperlongumine compounds for use in such treatments are provided.
    Type: Grant
    Filed: September 14, 2018
    Date of Patent: March 15, 2022
    Assignee: Instituto de Medicina Molecular João Lobo Antunes
    Inventors: Goncalo Bernardes, Tiago Rodrigues, João Conde, Charlotte Baker
  • Patent number: 11053245
    Abstract: Use of particular substituted heterocycle fused gamma-carboline compounds as pharmaceuticals for the treatment of agitation, aggressive behaviors, posttraumatic stress disorder or impulse control disorders.
    Type: Grant
    Filed: April 14, 2013
    Date of Patent: July 6, 2021
    Assignee: INTRA-CELLULAR THERAPIES, INC.
    Inventors: Sharon Mates, Robert Davis, Kimberly Vanover
  • Patent number: 11033554
    Abstract: Disclosed herein are methods of treating disorders of the retina (e.g., macular degeneration, retinitis pigmentosa, etc.) comprising administering to a subject in need of such treatment a therapeutically effective amount of a compound (for example, an antipsychotic drug) that blocks or diminishes agonist-mediated responses upon binding to either dopamine D2-like receptors or serotonin 5-HT2 receptors.
    Type: Grant
    Filed: July 25, 2016
    Date of Patent: June 15, 2021
    Assignee: UNITED STATES GOVERNMENT AS REPRESENTED BY THE DEPARTMENT OF VETERANS AFFAIRS
    Inventor: Ralph Jensen
  • Patent number: 10925851
    Abstract: The invention provides methods and compositions for producing analgesia in an animal.
    Type: Grant
    Filed: March 14, 2019
    Date of Patent: February 23, 2021
    Assignee: Regents of the University of Minnesota
    Inventors: Robert Vince, Rohit Singh, Swati Sudhakar More
  • Patent number: 10881648
    Abstract: The present invention provides combination therapy that includes an MDM2 inhibitor and one or more additional pharmaceutically active agents, particularly for the treatment of cancers. The invention also relates to pharmaceutical compositions that contain an MDM2 inhibitor and one or more additional pharmaceutically active agents for the treatment of cancers.
    Type: Grant
    Filed: December 21, 2018
    Date of Patent: January 5, 2021
    Assignee: AMGEN INC.
    Inventors: Sean Caenepeel, Jude Canon, Paul Hughes, Jonathan D. Oliner, Richard J. Rickles, Anne Y. Saiki
  • Patent number: 10696656
    Abstract: The invention relates to benzimidazole-carboxamide 5-HT4 receptor agonist compounds of formula (I) wherein R1 and X are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The invention also relates to pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds.
    Type: Grant
    Filed: January 29, 2019
    Date of Patent: June 30, 2020
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventor: Robert Murray McKinnell
  • Patent number: 10350204
    Abstract: Provided herein are methods of treating a cognitive deficit, including cognitive deficits associated with a Fmr1 genetic defect. More particularly, provided herein are methods in which an effective amount of a MDM2-p53 pathway inhibitor is administered to a subject afflicted with at least one cognitive deficit, whereby administration of the inhibitor improves, enhances, or rescues at least one cognitive deficit in the subject.
    Type: Grant
    Filed: March 8, 2018
    Date of Patent: July 16, 2019
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Xinyu Zhao, Yue Li
  • Patent number: 10335378
    Abstract: Pharmaceutical compositions and methods of use therefor for reducing the desire to engage in smoking are disclosed. More specifically, the pharmaceutical composition utilizes an active ingredient to reduce the side effects of smoking cessation and to limit the molecular feedback caused by nicotine-mediated activation of acetylcholine receptors.
    Type: Grant
    Filed: March 13, 2014
    Date of Patent: July 2, 2019
    Assignee: Altria Client Services LLC
    Inventors: Gerd Kobal, Justin Heynekamp, Peter Reeh, Munmaya K. Mishra, Tetyana Kichko
  • Patent number: 10010538
    Abstract: This invention is directed to compounds and salts that are generally useful as agents to treat an infection with Dirofilaria immitis. This invention also is directed to treatments comprising the administration of the compounds and salts to animals in need of the treatments.
    Type: Grant
    Filed: July 10, 2015
    Date of Patent: July 3, 2018
    Assignee: Intervet Inc.
    Inventors: Christophe Pierre Alain Chassaing, Jurgen Lutz, Anja Regina Heckeroth
  • Patent number: 9962380
    Abstract: Provided herein are methods of treating a cognitive deficit, including cognitive deficits associated with a Fmr1 genetic defect. More particularly, provided herein are methods in which an effective amount of a MDM2-p53 pathway inhibitor is administered to a subject afflicted with at least one cognitive deficit, whereby administration of the inhibitor improves, enhances, or rescues at least one cognitive deficit in the subject.
    Type: Grant
    Filed: September 23, 2016
    Date of Patent: May 8, 2018
    Inventors: Xinyu Zhao, Yue Li
  • Patent number: 9943687
    Abstract: The present invention relates, in general, to movement disorders and, in particular, to a method of treating movement disorders, including Parkinson's Disease.
    Type: Grant
    Filed: September 26, 2008
    Date of Patent: April 17, 2018
    Assignee: Duke University
    Inventors: Miguel A. L. Nicolelis, Romulo A. Fuentes
  • Patent number: 9850227
    Abstract: The present invention provides a diaminopyrimidine derivative or its pharmaceutically acceptable salt, a process for the preparation thereof, a pharmaceutical composition comprising the same, and a use thereof. The diaminopyrimidine derivative or its pharmaceutically acceptable salt functions as a 5-HT4 receptor agonist, and therefore can be usefully applied for preventing or treating dysfunction in gastrointestinal motility, one of the gastrointestinal diseases, such as gastroesophageal reflux disease (GERD), constipation, irritable bowel syndrome (IBS), dyspepsia, post-operative ileus, delayed gastric emptying, gastroparesis, intestinal pseudo-obstruction, drug-induced delayed transit, or diabetic gastric atony.
    Type: Grant
    Filed: February 24, 2012
    Date of Patent: December 26, 2017
    Assignee: YUHAN CORPORATION
    Inventors: Hyun-Joo Lee, Dong-Hoon Kim, Tae-Kyun Kim, Young-Ae Yoon, Jae-Young Sim, Myung-Hun Cha, Eun-Jung Jung, Kyoung-Kyu Ahn, Tai-Au Lee
  • Patent number: 9776965
    Abstract: The N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is 1 or 2; L represents a C1-3alkyl linker optionally substituted with one or two substituents selected from C1-4alkyl, C1-3alkyloxy-C1-4alkyl-, hydroxy-C1-4alkyl, hydroxy, C1-3alkyloxy- or phenyl-C1-4alkyl; M represents a direct bond or a C1-3alkyl linker optionally substituted with one or two substituents selected from hydroxy, C1-4alkyl or C1-4alkyloxy; R1 and R2 each independently represent hydrogen, halo, cyano, hydroxy, C1-4alkyl optionally substituted with halo, C1-4alkyloxy- optionally substituted with one or where possible two or three substituents selected from hydroxy, Ar1 and halo; or R1 and R2 taken together with the phenyl ring to which they are attached form naphtyl or 1,3-benzodioxolyl, wherein said naphtyl or 1,3-benzodioxolyl are optionally substituted with halo; R3 represents hydrogen, halo, C1-4alkyl, C1-4alkyloxy-, cyano or hydroxy; R4 represents hydrogen, halo,
    Type: Grant
    Filed: February 24, 2016
    Date of Patent: October 3, 2017
    Assignee: JANSSEN PHARMACEUTICA NV
    Inventors: Libuse Jaroskova, Joannes Theodorus Maria Linders, Christophe Francis Robert Nestor Buyck, Louis Jozef Elisabeth Van Der Veken, Vladimir Dimtchev Dimitrov, Theo Teofanov Nikiforov
  • Patent number: 9718778
    Abstract: This invention is in the field of medicinal chemistry. In particular, the invention relates to mixed disulfide conjugates of thienopyridine compounds, and their use as therapeutics for the treatment, amelioration, and prevention of cardiovascular diseases.
    Type: Grant
    Filed: January 6, 2014
    Date of Patent: August 1, 2017
    Assignee: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: Haoming Zhang, Paul Hollenberg
  • Patent number: 9579299
    Abstract: The present invention is directed to CNS pharmaceutical compositions and methods of use. The pharmaceutical compositions comprise a CNS active agent and preferably at least two vagal neuromodulators, one of which is a mechanoreceptor stimulator. The vagal neuromodulators are preferably in an amount sufficient to reduce a somnolence side-effect of the CNS active agent without changing its therapeutic efficacy/activity. The invention further encompasses a method of reducing CNS active agent side-effects. The method typically comprises oral administration of at least one CNS active agent to a patient at the conventionally accepted dose; and administration of at least two vagal neuromodulators to the patient so that at least one neuromodulator is administered or released from dosage form after the CNS active agent is administered and/or released.
    Type: Grant
    Filed: May 19, 2014
    Date of Patent: February 28, 2017
    Assignee: Targia Pharmaceuticals
    Inventor: Sabina Glozman
  • Patent number: 9527830
    Abstract: This invention relates to compounds having structural Formula I: and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir1.1). The compounds of Formula I are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.
    Type: Grant
    Filed: September 10, 2012
    Date of Patent: December 27, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Shawn Walsh, Alexander Pasternak, Brian Cato, Paul E. Finke, Jessica Frie, Qinghong Fu, Dooseop Kim, Barbara Pio, Aurash Shahripour, Zhi-Cai Shi, Haifeng Tang
  • Patent number: 9487509
    Abstract: The present invention relates to wherein each symbol is as defined in the specification. The compound of the present invention has a superior RBP4-lowering action, and is useful as a medicament for the prophylaxis or treatment of disease and condition mediated by increased RBP4.
    Type: Grant
    Filed: October 16, 2013
    Date of Patent: November 8, 2016
    Assignee: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Shizuo Kasai, Tomohiro Kaku, Masahiro Kamaura
  • Patent number: 9272996
    Abstract: A compound for use in treating polycystic kidney disease is represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of treating polycystic kidney disease in a subject in need thereof comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. Methods of treating in polycystic kidney disease in a subject in need thereof respectively comprise administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: August 27, 2012
    Date of Patent: March 1, 2016
    Assignee: Genzyme Corporation
    Inventors: Craig Siegel, Cecilia M. Bastos, David J. Harris, Angeles Dios, Edward Lee, Richard Silva, Lisa M. Cuff, Mikaela Levine, Cassandra A. Celatka, Thomas H. Jozefiak, Frederic Vinick, Yibin Xiang, John Kane, Junkai Liao
  • Patent number: 9200268
    Abstract: Disclosed herein are compounds, compositions, methods and kits for purifying a serine protease and serine proteases purified with the compounds, compositions and methods.
    Type: Grant
    Filed: March 14, 2013
    Date of Patent: December 1, 2015
    Assignee: Portola Pharmaceuticals, Inc.
    Inventors: Anjali Pandey, Jack W. Rose
  • Publication number: 20150126554
    Abstract: Methods of preventing and treating gastrointestinal dysfunction, particularly postoperative ileus and post-partum ileus, in a patient undergoing surgery or other biological stress by administering 4-aryl-piperidine derivatives are disclosed.
    Type: Application
    Filed: January 15, 2015
    Publication date: May 7, 2015
    Inventors: David D. Christ, Bruce A. Wallin, Deanne D. Garver, William K. Schmidt, David Jackson
  • Publication number: 20150126486
    Abstract: The compound represented by the formula (I-1): wherein all the symbols have the same meanings as described in the specification, has two cyclic groups, particularly phenoxy groups at specific substitution positions and thus has high human S1P2 antagonistic activity. The compound may therefore be used as a therapeutic agent for S1P2-mediated diseases such as diseases resulting from vascular constriction, fibrosis and respiratory diseases.
    Type: Application
    Filed: January 8, 2015
    Publication date: May 7, 2015
    Applicant: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Atsushi NAGANAWA, Kensuke KUSUMI, Kazuhiro OTSUKI, Tetsuya SEKIGUCHI, Akito KAKUUCHI, Koji SHINOZAKI, Hiroshi YAMAMOTO, Shigeyuki NONAKA
  • Publication number: 20150126518
    Abstract: The present invention relates to biguanide compounds and use thereof, more particularly, to biguanide derivatives exhibiting excellent effects for inhibition of cancer cell proliferation and inhibition of cancer metastasis and recurrence, a method for preparing the same, a pharmaceutical composition containing the same as an active ingredient, and a method of prevention or treatment of cancer comprising the step of administering an effective amount of the composition to a subject in need thereof.
    Type: Application
    Filed: October 30, 2014
    Publication date: May 7, 2015
    Applicant: HANALL BIOPHARMA CO., LTD.
    Inventors: Hong Woo KIM, Ji Sun LEE, Hye Jin HEO, Hong Bum LEE, Jae Kap JEONG, Ji Hyun PARK, Seo-il KIM, Young Woo LEE
  • Publication number: 20150119422
    Abstract: The present invention relates to solid pharmaceutical formulations based on simethicone and calcium phosphate and mannitol.
    Type: Application
    Filed: December 11, 2012
    Publication date: April 30, 2015
    Inventors: José Luis Velada, Hiteshkumar Anilkant Doshi, Anjali Rajesh Tendulkar, Vicky Shinde
  • Publication number: 20150119383
    Abstract: Embodiments disclosed herein generally relate to acamprosate formulations, methods of use of the formulations, to methods of using the formulations in combination with at least one other medication, and to combination products and compositions comprising the formulations and at least one other medication, such as neuroleptic (antipsychotic) and/or antidepressant drugs.
    Type: Application
    Filed: June 5, 2014
    Publication date: April 30, 2015
    Inventors: Barry S. Fogel, William D. Kerns, Kei-Lai Fong, San-Laung Chow, Edward Lin, David Wong
  • Patent number: 9018232
    Abstract: Disclosed herein are methods of administering deuterated pirfenidone and kits thereof.
    Type: Grant
    Filed: March 6, 2012
    Date of Patent: April 28, 2015
    Assignee: Auspex Pharmaceuticals, Inc.
    Inventor: Chengzhi Zhang
  • Patent number: 9017735
    Abstract: Disclosed herein are compositions and methods for treating a psychiatric disorder or symptoms thereof in a patient. The compositions comprise a compound that modulates KCNQ (Kv7) potassium channel activity and the methods include administering an effective amount of the compound that modulates KCNQ (Kv7) potassium channel activity.
    Type: Grant
    Filed: June 3, 2010
    Date of Patent: April 28, 2015
    Assignee: Marquette University
    Inventor: Mohammadhossein Behnam Ghasemzadeh
  • Patent number: 9018206
    Abstract: The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula I in which R1, R2, R3a, R3b, R4, Q, Y, A and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula Ia and Ib in which R1, r, R2b, R3a, R3b, R4, Y and X have the meanings mentioned in the claims, including the tautomers thereof and the pharmaceutically suitable salts thereof.
    Type: Grant
    Filed: September 12, 2012
    Date of Patent: April 28, 2015
    Assignees: AbbVie Deutschland GmbH & Co. KG, AbbVie Inc.
    Inventors: Helmut Mack, Andreas Kling, Katja Jantos, Achim Moeller, Wilfried Hornberger, Charles W. Hutchins
  • Publication number: 20150099786
    Abstract: The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula I in which R1, R2, R3a, R3b, R4, Q, Y, A and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula Ia and Ib in which R1, r, R2b, R3a, R3b, R4, Y and X have the meanings mentioned in the claims, including the tautomers thereof and the pharmaceutically suitable salts thereof.
    Type: Application
    Filed: December 15, 2014
    Publication date: April 9, 2015
    Inventors: Helmut Mack, Andreas Kling, Katja Jantos, Achim Moeller, Wilfried Hornberger, Charles W. Hutchins
  • Patent number: 8987306
    Abstract: Novel compounds inhibiting the integrin ?2?1/GPIa-IIa receptor are disclosed. Also disclosed are pharmaceutical compositions containing the compounds, as well as methods of their therapeutic use. The compounds disclosed are useful, inter alia, as inhibitors of integrin ?2?1/GPIa-IIa-mediated activity.
    Type: Grant
    Filed: September 24, 2009
    Date of Patent: March 24, 2015
    Assignee: The Trustees Of The University of Pennsylvania
    Inventors: William F. DeGrado, Meredith W. Miller, Sandeep Basra, Joel S. Bennett, Sungwook Choi
  • 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
  • Patent number: 8980923
    Abstract: The present invention concerns methods for treating or preventing neurological disorders characterized by dysfunction of nicotinic acetylcholine receptors by administering 2,2,6,6-tetramethylpiperidin-4-yl heptanoate (TMPH), or a pharmaceutically acceptable salt thereof, to the patient. In another aspect, the present invention pertains to pharmaceutical compositions containing TMPH, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier. In another aspect, the present invention pertains to methods for selectively inhibiting nicotinic acetylcholine receptors that lack an ?5, ?6, or ?3 subunit by contacting an effective amount of TMPH, or a pharmaceutically acceptable salt thereof, to the receptor. The method for selectively inhibiting nicotinic acethylcholine receptors that lack an ?5 subunit can be carried out in vivo or in vitro.
    Type: Grant
    Filed: June 18, 2012
    Date of Patent: March 17, 2015
    Assignee: University of Florida Research Foundation, Inc.
    Inventors: Roger L. Papke, Nicole A. Horenstein, Michael M. Francis, Kyung Il Choi
  • Publication number: 20150051144
    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 towards compounds which can be used to treat diseases such as hyperlipidemia and also have a beneficial effect on cholesterol.
    Type: Application
    Filed: September 26, 2012
    Publication date: February 19, 2015
    Inventors: Harikishore Pingali, Vrajesh Pandya
  • Publication number: 20150051247
    Abstract: Compounds and methods for treating or preventing cancer associated with binding to the urokinase receptor are provided. Biological processes affected by the compounds include cell migration, cell growth, cell adhesion, angiogenesis, cancer cell invasion, apoptosis, tumor formation, tumor progression, metastasis, degradation of the extracellular matrix, pericellular proteolysis, activation of plasminogen, changes in the levels of an extracellular protease, and changes in the levels of a VEGF receptor.
    Type: Application
    Filed: August 16, 2012
    Publication date: February 19, 2015
    Inventor: Samy O. Meroueh
  • Publication number: 20150051250
    Abstract: An object to be solved by the present invention is to provide a superior prophylactic agent and/or therapeutic agent for stress urinary incontinence. The present invention provides a prophylactic agent and/or a therapeutic agent for stress urinary incontinence comprising an effective amount of 4-piperidyl diphenylpropoxyacetate or a salt thereof, and a pharmaceutical carrier.
    Type: Application
    Filed: May 14, 2013
    Publication date: February 19, 2015
    Applicant: Taiho Pharmaceutical Co., Ltd.
    Inventors: Masato Nanri, Fukumitsu Sakakibara
  • Patent number: 8952036
    Abstract: The present invention provides a MDM2 inhibitor compound, or a pharmaceutically acceptable salt thereof, which compound is useful as a therapeutic agent, particularly for the treatment of cancers. The present invention also relates to pharmaceutical compositions that contains the MDM2 inhibitor.
    Type: Grant
    Filed: February 27, 2014
    Date of Patent: February 10, 2015
    Assignee: Amgen Inc.
    Inventor: Yosup Rew
  • Publication number: 20150031677
    Abstract: Monomeric and dimeric trioxane thioacetals and methods of their use for treating subjects infected with malaria or other parasitic infectious diseases including, but not limited to, toxoplasmic infection; subjects afflicted with psychiatric conditions associated with toxoplasmic infection; and subjects afflicted with cancer.
    Type: Application
    Filed: February 28, 2013
    Publication date: January 29, 2015
    Applicant: THE JOHNS HOPKINS UNIVERSITY
    Inventors: Gary H. Posner, Alexander M. Jacobine, Rachel D. Slack, Jennifer R. Mazzone
  • Publication number: 20150031670
    Abstract: Compounds of the formula (I), in which R1, R3, R5, R6, R7, R, X and Y have the meanings indicated in Claim 1, are inhibitors of methionine aminopeptidase and can be employed for the treatment of tumours.
    Type: Application
    Filed: March 21, 2013
    Publication date: January 29, 2015
    Applicant: MERCK PATENT GmbH
    Inventors: Timo Heinrich, Frank Zenke, Mireille Krier, Manja Friese-Hamim, Jeyaprakashnarayanan Seenisamy
  • Publication number: 20150025110
    Abstract: This invention relates to novel 1-cycloalkyl- or 1-heterocyclyl-hydroxyimino-3-phenyl-propanes of the formula wherein R1 to R7 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are GPBAR1 agonists and may therefore be useful as medicaments for the treatment of diseases such as type II diabetes.
    Type: Application
    Filed: October 9, 2014
    Publication date: January 22, 2015
    Inventors: Henrietta Dehmlow, Rainer E. Martin, Patrizio Mattei, Ulrike Obst Sander, Hans Richter
  • Publication number: 20150010638
    Abstract: It is an object of the present invention to provide a method for improving the solubility of a poorly-soluble substance, which is capable of increasing the solubility of substantially all poorly-soluble substances. This is a method comprising coating the surface of a poorly-soluble substance particle with microparticles of a calcium compound such as calcium phosphate or calcium carbonate, and at least one selected from a pH adjuster and a surfactant, by applying mechanical energy thereto.
    Type: Application
    Filed: February 21, 2013
    Publication date: January 8, 2015
    Inventors: Shuji Sakuma, Keiichiro Kikukawa, Ryosuke Miyasaka
  • Patent number: 8927533
    Abstract: The present invention relates to novel amide compounds of Formula (I), and their use as anti-tumoral and pro-apoptotic agents. The invention includes the use of such compounds in medicine, in relation to cancer disease as well as other diseases where an inhibition of HDAC is responsive, and the pharmaceutical composition containing such compounds.
    Type: Grant
    Filed: September 17, 2012
    Date of Patent: January 6, 2015
    Assignee: SIGMA-TAU Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Giuseppe Giannini, Walter Cabri, Gianfranco Battistuzzi, Davide Vignola, Nicola Fanto', Claudio Pisano, Loredana Vesci
  • Publication number: 20140377328
    Abstract: Provided is an intraoral soluble-type film preparation in which an unpleasant taste of a drug is masked. The intraoral soluble-type film preparation comprises a drug layer containing: a drug having a bitter taste and/or an astringent taste; an alkyl sulfate at a content of ¾ mol or more with respect to 1 mol of the drug; and a water-soluble polymer.
    Type: Application
    Filed: December 12, 2012
    Publication date: December 25, 2014
    Applicant: KYUKYU PHARMACEUTICAL CO., LTD.
    Inventors: Akihiro Ishise, Hisanobu Nishikawa
  • Publication number: 20140371269
    Abstract: The present invention provides compounds of Formula I or a pharmaceutical salt thereof, where the variables for R1, R2, and R3 are as described herein; methods of treating a condition such as hypertriglyceridemia; and processes for preparing the compounds.
    Type: Application
    Filed: January 16, 2013
    Publication date: December 18, 2014
    Applicant: Eli Lilly and Company
    Inventors: Maria Carmen Fernandez, Maria Rosario Gonzalez-Garcia, Bin Liu, Lance Allen Pfeifer
  • Publication number: 20140371270
    Abstract: An acetic acid ester compound represented by the following formula (I) or a salt thereof, wherein R represents optionally substituted deuterated lower alkyl, is disclosed.
    Type: Application
    Filed: January 25, 2013
    Publication date: December 18, 2014
    Applicant: Taiho Pharmaceutical Co., Ltd.
    Inventors: Masato Nanri, Yoshikazu Iwasawa, Fukumitsu Sakakibara, Shinichi Aoki
  • Publication number: 20140371177
    Abstract: A method of treating cancer, inflammatory disease, and autoimmune disease by administering to a subject in need thereof an effective amount of one or more 1,5-dipenylpenta-1,4-dien-3-one compounds. The compounds feature either or both of the phenyl rings being substituted with hydroxyl, diethyl(2-alkoxyethyl)amine, 1-(2-alkoxyethyl)piperidine, sulfonate, phosphinate, or phosphate.
    Type: Application
    Filed: August 28, 2014
    Publication date: December 18, 2014
    Inventors: Charles C-Y Shih, Toshio Kitamura, Qian Shi, Toshiyuki Kawashima, Hui-Kang Wang
  • Patent number: 8912219
    Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, p, q, r, A, X1, X2, X3, X4, X5, X6, Y, Z, G, R1a, R2a, R1b, R2b, R3, R4, R5 and R6 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: December 16, 2014
    Assignee: Genentech, Inc.
    Inventors: Benjamin Fauber, Olivier Rene, Monique Bodil van Niel, Stuart Ward