Plural Chalcogens Bonded Directly To Ring Carbons Of The Five-membered Hetero Ring (e.g., Phthalimide, Etc.) Patents (Class 514/417)
  • Patent number: 10682336
    Abstract: Methods of treating immune reconstitution inflammatory syndrome (IRIS) in immunodeficient patients, including HIV patients, using PDE4 modulators are described.
    Type: Grant
    Filed: October 20, 2016
    Date of Patent: June 16, 2020
    Assignee: AMGEN INC.
    Inventors: Vikram Khetani, Jerome Zeldis
  • Patent number: 10610516
    Abstract: Stereomerically pure (+)-2-[1-(3-Ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione, substantially free of its (?) isomer, and prodrugs, metabolites, polymorphs, salts, solvates, hydrates, and clathrates thereof are discussed. Also discussed are methods of using and pharmaceutical compositions comprising the (+) enantiomer of 2-[1-(3-Ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione are disclosed. The methods include methods of treating and/or preventing disorders ameliorated by the reduction of levels of TNF-? or the inhibition of PDE4.
    Type: Grant
    Filed: September 7, 2018
    Date of Patent: April 7, 2020
    Assignee: AMGEN INC.
    Inventors: George W. Muller, Peter H. Schafer, Hon-Wah Man, Chuansheng Ge
  • Patent number: 10494342
    Abstract: The present invention relates to a process for preparation of apremilast. The present invention relates to p-xylene solvate of apremilast and process for its preparation.
    Type: Grant
    Filed: August 22, 2016
    Date of Patent: December 3, 2019
    Assignee: Glenmark Life Sciences Limited
    Inventors: Shekhar Bhaskar Bhirud, Suresh Mahadev Kadam, Sachin Baban Gavhane, Sandeep Bandu Khandagale, Sunil Pandurang Nirgude, Ajit Shankar Mindhe, Rajesh Kumar Dwivedi
  • Patent number: 10399942
    Abstract: The present invention provides an improved process for the preparation of Apremilast using novel intermediates. The present invention also relates to the novel crystalline polymorphic form of Apremilast.
    Type: Grant
    Filed: July 29, 2016
    Date of Patent: September 3, 2019
    Assignee: Alembic Pharmaceuticals Limited
    Inventors: Mahender Rao Siripragada, Dinesh Panchasara, Ilesh Patel, Bhavesh Prajapati, Ankit Shah, Ananda Babu Thirunavakarasu, Pinky Parikh
  • Patent number: 10239825
    Abstract: The present invention relates to ketamine derivatives of the formula (I), pharmaceutical compositions comprising them, and methods for treating pain comprising administering them, and their use in the manufacture of medicaments for treating pain. The present invention also relates to methods for anaesthetizing and methods for sedating a subject comprising administering ketamine derivatives of the formula (II).
    Type: Grant
    Filed: March 20, 2017
    Date of Patent: March 26, 2019
    Assignee: Auckland Uniservices Limited
    Inventors: James Wallace Sleigh, William Alexander Denny, Jiney Jose, Swarnalatha Akuratiya Gamage, Martyn Gregory Harvey, Logan James Voss
  • Patent number: 10092542
    Abstract: Stereomerically pure (+)-[1-(3-Ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione, substantially free of its (?) isomer, and prodrugs, metabolites, polymorphs, salts, solvates, hydrates, and clathrates thereof are discussed. Also discussed are methods of using and pharmaceutical compositions comprising the (+) enantiomer of 2-[1-(3-Ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione are disclosed. The methods include methods of treating and/or preventing disorders ameliorated by the reduction of levels of TNF-? or the inhibition of PDE4.
    Type: Grant
    Filed: June 21, 2017
    Date of Patent: October 9, 2018
    Assignee: Celgene Corporation
    Inventors: George W. Muller, Peter H. Schafer, Hon-Wah Man, Chuansheng Ge
  • Patent number: 10092541
    Abstract: Methods of treating, managing or preventing diseases ameliorated by inhibiting PDE4 such as psoriasis, ankylosing spondylitis, Behcet's disease, rheumatoid arthritis, atopic dermatitis, Crohn's disease, and ulcerative colitis are disclosed. Specific methods encompass the administration of apremilast in specific dosage titration schedule, alone or in combination with a second active agent.
    Type: Grant
    Filed: August 13, 2015
    Date of Patent: October 9, 2018
    Assignee: Celgene Corporation
    Inventor: Robert Day
  • Patent number: 10016414
    Abstract: The instant invention is based, at least in part, on a newly-identified proteasome-independent signaling function of ubiquitinated PSD-95. Mdm2 inhibitors, Mdm4 inhibitors, PSD-95 inhibitors, and/or enantiomers and/or derivatives thereof decrease endocytosis via preventing PSD-95 ubiquitination, and thereby increase AMPAR, NMDAR, D1 dopamine receptor surface expression in response to a given stimulus (e.g., NMDA, A?). Accordingly, the invention provides methods for modulating AMPARs, NMDARs, or D1 dopamine receptors in a neuronal cell by contacting the neuronal cell with an Mdm2 and/or Mdm4 inhibitor or PSD-95 inhibitor and/or enantiomers and/or derivatives thereof. Mdm2 and/or Mdm4 inhibitors decrease the enzymatic activity of the respective proteins, and/or interactions with their respective substrates. Mdm2 and Mdm4 inhibitors and/or PSD-95 inhibitors of the invention are contemplated for use in the treatment of neurological disorders, neurodevelopmental disorders, and psychiatric disorders.
    Type: Grant
    Filed: November 14, 2011
    Date of Patent: July 10, 2018
    Assignee: UNIVERSITY OF MASSACHUSETTS
    Inventors: Maria Morabito, Michael Bianchetta
  • Patent number: 9850205
    Abstract: A stable Crystalline Form II of non-solvate of Apremilast (Formula I), methods of making Form II, pharmaceutical compositions comprising Form II, and their uses are disclosed. Also discloses are mixed crystals comprising Form Hand Form B and methods of making the same. The crystalline forms are characterized using X-ray powder diffractometry (XRPD), infrared spectroscopy (IR), differential scanning calorimetry (DSC), and thermal gravimetric analysis (TG). As compared with Forms A, B, C, D, E, F, and G reported in prior art references, Apremilast Form II of the present invention is more stable to temperature, light, and humidity, and is more suitable for long term storage; the crystallization solvents are safe and can be easily removed; the Form II has a white or off white appearance, and can be directly used in preparation processing; the preparation methods are simple and easy to reproduce, and are suitable for industrialized production.
    Type: Grant
    Filed: June 30, 2017
    Date of Patent: December 26, 2017
    Inventors: Junzhi Luo, Jing Nian, Siyuan Gao
  • Patent number: 9822093
    Abstract: The present invention provides new processes for the preparation of unsubstituted and substituted 4-amino-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione compounds which are useful, for example, for preventing or treating diseases or conditions related to an abnormally high level or activity of TNF-?. The invention can provide improved and/or efficient processes for the commercial production of unsubstituted and substituted 4-amino-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione compounds, including, but not limited to, unsubstituted 4-amino-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione.
    Type: Grant
    Filed: June 20, 2016
    Date of Patent: November 21, 2017
    Assignee: Celgene Corporation
    Inventors: Chuansheng Ge, George W. Muller, Roger Chen, Manohar Tukaram Saindane
  • Patent number: 9724330
    Abstract: Stereomerically pure (+)-2-[1-(3-Ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione, substantially free of its (?) isomer, and prodrugs, metabolites, polymorphs, salts, solvates, hydrates, and clathrates thereof are discussed. Also discussed are methods of using and pharmaceutical compositions comprising the (+) enantiomer of 2-[1-(3-Ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione are disclosed. The methods include methods of treating and/or preventing disorders ameliorated by the reduction of levels of TNF-? or the inhibition of PDE4.
    Type: Grant
    Filed: February 5, 2016
    Date of Patent: August 8, 2017
    Assignee: Celgene Corporation
    Inventors: George W. Muller, Peter H. Schafer, Hon-Wah Man, Chuansheng Ge
  • Patent number: 9480676
    Abstract: Methods of treating cystic fibrosis by administering a PDE4 inhibitor in combination with one or more cystic fibrosis transmembrane conductance regulator (CFTR) potentiators, including ivacaftor, and/or one or more CFTR correctors, including lumacaftor. Pharmaceutical compositions, dosage forms, and kits suitable for use in methods of the invention are also disclosed.
    Type: Grant
    Filed: May 14, 2015
    Date of Patent: November 1, 2016
    Assignee: Celgene Corporation
    Inventors: Peter H. Schafer, Shimon Korish
  • Patent number: 9433606
    Abstract: Solid forms comprising (+)-2-[1-(3-Ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione, compositions comprising the solid forms, methods of making the solid forms and methods of their use are disclosed. The methods include methods of treating and/or preventing disorders ameliorated by the reduction of levels of TNF-? or the inhibition of PDE4.
    Type: Grant
    Filed: March 26, 2015
    Date of Patent: September 6, 2016
    Assignee: Celgene Corporation
    Inventors: George W. Muller, Peter H. Schafer, Hon-Wah Man, Chuansheng Ge, Jean Xu
  • Patent number: 9394274
    Abstract: The present invention provides new processes for the preparation of unsubstituted and substituted 4-amino-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione compounds which are useful, for example, for preventing or treating diseases or conditions related to an abnormally high level or activity of TNF-?. The invention can provide improved and/or efficient processes for the commercial production of unsubstituted and substituted 4-amino-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione compounds, including, but not limited to, unsubstituted 4-amino-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione.
    Type: Grant
    Filed: April 29, 2014
    Date of Patent: July 19, 2016
    Assignee: Celgene Corporation
    Inventors: Chuansheng Ge, George W. Muller, Roger Chen, Manohar Tukaram Saindane
  • Patent number: 9283207
    Abstract: Stereomerically pure (+)-2-[1-(3-Ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione, substantially free of its (?) isomer, and prodrugs, metabolites, polymorphs, salts, solvates, hydrates, and clathrates thereof are discussed. Also discussed are methods of using and pharmaceutical compositions comprising the (+) enantiomer of 2-[1-(3-Ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione are disclosed. The methods include methods of treating and/or preventing disorders ameliorated by the reduction of levels of TNF-? or the inhibition of PDE4.
    Type: Grant
    Filed: June 26, 2014
    Date of Patent: March 15, 2016
    Assignee: Celgene Corporation
    Inventors: George W. Muller, Peter H. Schafer, Hon-Wah Man, Chuansheng Ge
  • Patent number: 9023886
    Abstract: Provided are compositions and methods for preparation and administration of an oral nanosuspension of a poorly soluble drug with improved bioavailability. The method is optimized through microfluidization process with water soluble polymeric excipients in the absence of surfactants.
    Type: Grant
    Filed: November 9, 2010
    Date of Patent: May 5, 2015
    Assignee: Celgene Corporation
    Inventors: Ming J. Chen, Ho-Wah Hui, Thomas Lee, Paul Kurtulik, Sekhar Surapaneni
  • Patent number: 9018243
    Abstract: Solid forms comprising (+)-2-[1-(3-Ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione, compositions comprising the solid forms, methods of making the solid forms and methods of their use are disclosed. The methods include methods of treating and/or preventing disorders ameliorated by the reduction of levels of TNF-? or the inhibition of PDE4.
    Type: Grant
    Filed: December 10, 2013
    Date of Patent: April 28, 2015
    Assignee: Celgene Corporation
    Inventors: George W. Muller, Peter H. Schafer, Hon-Wah Man, Chuansheng Ge, Jean Xu
  • Publication number: 20150105438
    Abstract: This invention relates to novel substituted isoindoline-1,3-dione derivatives and pharmaceutically acceptable salts thereof. More specifically, the invention relates to novel substituted isoindoline-1,3-dione derivatives that are analogues of apremilast. This invention also provides compositions comprising a compound of this invention and a carrier and the use of disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering apremilast.
    Type: Application
    Filed: September 19, 2014
    Publication date: April 16, 2015
    Applicant: CONCERT PHARMACEUTICALS, INC.
    Inventor: Julie F. Liu
  • Publication number: 20150094314
    Abstract: A method of modulating ribonucleotide reductase activity in a neoplastic cell includes administering to the cell an amount of a ribonucleotide reductase allosteric modulator (RRAmod), the amount being effective to inhibit neoplastic cell growth.
    Type: Application
    Filed: March 21, 2013
    Publication date: April 2, 2015
    Inventor: Chris Dealwis
  • Publication number: 20150031655
    Abstract: The disclosure provides a method of treating a mammal afflicted with an age-related disorder, comprising administering to the mammal a combination of liver X receptor (LXR) modulator and estrogen receptor (ER) modulator, in an amount effective to treat the mammal. Further disclosed are the LXR modulators and ER modulators used in the combination therapy.
    Type: Application
    Filed: April 10, 2012
    Publication date: January 29, 2015
    Applicant: UNIVERSITY OF NORTH DAKOTA
    Inventor: Othman Ghribi
  • Patent number: 8932631
    Abstract: Liquid formulations of imidoalkanepercarboxylic acids, in the form of aqueous dispersions comprising, in percentages by weight relative to the total weight of the composition: A) from ?7% to 40% and preferably from 10% to 20% of imidoalkanepercarboxylic acids having the general formula (I), the said imidoalkanepercarboxylic acids being in the ? form and having a dissolution time, determined via the test of the rate of dissolution at a temperature of 40° C. or 18° C., of not more than 5 minutes when determined at 40° C. or 15 minutes when determined at 18° C., for an amount of dissolved acid equal to 99% of the theoretical amount; B) from 0.001% to 0.9% of a nonionic surfactant; the said dispersions having a viscosity of not more than 2000 mPa·sec at 25° C. by applying a shear rate of 20 s?1; in which the dissolution time of the component A), determined via the test of the rate of dissolution at a temperature of 40° C. or 18° C., is not more than 5 minutes when determined at 40° C.
    Type: Grant
    Filed: December 23, 2004
    Date of Patent: January 13, 2015
    Assignee: Solvay Solexis S.p.A.
    Inventors: Ugo Piero Bianchi, Roberto Garaffa
  • Patent number: 8916605
    Abstract: The present application relates to the use of one or more compounds of Formula (I) or pharmaceutically acceptable solvates or prodrugs thereof, for treating cancer or for treating or preventing a viral infection.
    Type: Grant
    Filed: March 2, 2010
    Date of Patent: December 23, 2014
    Inventor: William G. Tucker
  • Publication number: 20140370092
    Abstract: Pharmaceutical compositions and single unit dosage forms of apremilast, i.e., (+)-2-[1-(3-ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione, or a pharmaceutically acceptable stereoisomer, prodrug, salt, solvate, hydrate, or clathrate, are provided herein. Also provided are methods of treating, managing, or preventing various disorders, such as diseases or disorders ameliorated by the inhibition of TNF-? production in mammals.
    Type: Application
    Filed: June 16, 2014
    Publication date: December 18, 2014
    Inventors: Darshan K. Parikh, Anil Menon, Anthony Tutino
  • Publication number: 20140371287
    Abstract: Stereomerically pure (+)-2-[1-(3-Ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione, substantially free of its (?) isomer, and prodrugs, metabolites, polymorphs, salts, solvates, hydrates, and clathrates thereof are discussed. Also discussed are methods of using and pharmaceutical compositions comprising the (+) enantiomer of 2-[1-(3-Ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione are disclosed. The methods include methods of treating and/or preventing disorders ameliorated by the reduction of levels of TNF-? or the inhibition of PDE4.
    Type: Application
    Filed: June 26, 2014
    Publication date: December 18, 2014
    Inventors: George W. Muller, Peter H. Schafer, Hon-Wah Man, Chuansheng Ge
  • Publication number: 20140336187
    Abstract: Methods are provided to inhibit proliferation of Leishmania parasites, and in particular Leshmania donovani with imido-substituted 1,4-naphthoquinones, including novel compounds. Administering an imido-substituted 1,4-naphthoquinone can used to provide prophylaxis or treatment to a patient in need of treatment against leishmaniasis disease.
    Type: Application
    Filed: November 16, 2012
    Publication date: November 13, 2014
    Inventors: Oladapo Bakare, Clarence M. Lee, Yakini Brandy, Cheu Manka
  • Publication number: 20140301980
    Abstract: Methods of treating, managing or preventing psoriatic arthritis are disclosed. Specific methods encompass the administration of apremilast, alone or in combination with a second active agent.
    Type: Application
    Filed: March 13, 2014
    Publication date: October 9, 2014
    Applicant: CELGENE CORPORATION
    Inventor: Robert DAY
  • Publication number: 20140303226
    Abstract: The present disclosure relates to methods and compositions for modulating the activity of KCNQ channels as a means for reducing the effects of aberrant KCNQ channel function associated with epilepsy, deafness and arrhythmias including but not limited to, Long-QT syndrome (“LQTS”), and atrial fibrillation. The present disclosure also relates to the discovery of certain regions of KCNQ channels that interact with various channel stimulating molecules such as, ATP, and PIP2, as well as KCNQ channel domains that effect voltage dependant channel activation. The disclosure is also directed to the use of small molecules to modulate KCNQ channel activity in a cell. Moreover, the present disclosure relates to the therapeutic effects of treating a subject with modulators of KCNQ channel activity.
    Type: Application
    Filed: March 14, 2014
    Publication date: October 9, 2014
    Applicants: WASHINGTON UNIVERSITY, Curators of the University of Missouri, The Research Foundation for The State University of New York
    Inventors: Jianmin Cui, Ira S. Cohen, Xiaoqin Zou
  • Patent number: 8853175
    Abstract: Provided are phenethyl isoindoline compounds, and pharmaceutically acceptable salts, solvates, or stereoisomers thereof. Methods of use and pharmaceutical compositions of these compounds are also disclosed.
    Type: Grant
    Filed: January 9, 2012
    Date of Patent: October 7, 2014
    Assignee: Celgene Corporation
    Inventors: Gondi Kumar, Hon-Wah Man, Roger S. C. Chen, George W. Muller, Anthony J. Frank
  • Patent number: 8853253
    Abstract: Thalidomide analogs that modulate tumor necrosis factor alpha (TNF?) activity and angiogenesis are disclosed. In particularly disclosed embodiments, the thalidomide analogs are isosteric sulfur-containing analogs. Also disclosed are methods of treating a subject with the analogs.
    Type: Grant
    Filed: October 10, 2012
    Date of Patent: October 7, 2014
    Assignee: P2D, Inc.
    Inventors: Nigel H. Greig, Harold Holloway, Tony Giordano, Qian-sheng Yu, William D. Figg
  • Publication number: 20140294957
    Abstract: The invention relates to niclosamide and derivates thereof, which effectively inhibit transcription of the S100A4 gene, resulting in inhibition and/or reduction of S100A4-induced cell motility, invasiveness, metastasis and proliferation of human cancer cells.
    Type: Application
    Filed: April 18, 2012
    Publication date: October 2, 2014
    Applicant: MAXDELBRUCK-CENTRUM FUR MOLEKULARE MEDIZIN
    Inventors: Ulrike Stein, Wolfgang Walther, Ulrike Sack, Robert Shoemaker, Dominic Scudiero, Peter M Schlag
  • Publication number: 20140294933
    Abstract: A composition for delivery of an angiogenesis inducing agent, including a temperature-sensitive liposome, a vascular cell-specific antibody, and an angiogenesis inducing agent, a tissue culture obtained using the composition, an artificial tissue including the tissue culture, and a method for preparing an artificial tissue are provided.
    Type: Application
    Filed: April 2, 2014
    Publication date: October 2, 2014
    Applicant: SAMSUNG ELECTRONICS CO., LTD.
    Inventors: Jae Min CHA, Min Sang Kim, Hyun-Ryoung Kim, Eun Sung Park
  • 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: 20140256767
    Abstract: A method of identifying compounds as direct inhibitors of Keap1-Nrf2 interaction through high-throughput screening and lead development. The direct inhibitors of Keap1-Nrf2 interaction are more specific and free of various undesirable effects than existing indirect inhibitors, and are potential drug candidates of chemopreventive and therapeutic agents for treatment of various diseases or conditions involving oxidative stress and/or inflammation, including but not limited to cancers, diabetes, Alzheimer's, and Parkinson's. Novel compounds are identified and methods of preventing or treating diseases or conditions related to Keap1-Nrf2 interaction activity by use of the novel compounds identified or compositions containing such compounds are also disclosed.
    Type: Application
    Filed: October 31, 2012
    Publication date: September 11, 2014
    Applicants: THE BROAD INSTITUTE, INC., RUTGERS, THE STATE UNIVERSITY OF NEW JERSEY
    Inventors: Longqin Hu, Sadagopan Magesh, Lin Chen, Timothy Lewis, Ben Munoz, Lili Wang
  • Publication number: 20140243348
    Abstract: Compositions and methods that are useful for the treatment of herpesvirus infection (including herpes simplex virii) are disclosed. Methods for identifying compounds useful for the treatment of herpesvirus infection are also disclosed.
    Type: Application
    Filed: January 22, 2014
    Publication date: August 28, 2014
    Applicant: PRESIDENT AND FELLOWS OF HARVARD COLLEGE
    Inventors: David M. Knipe, Kevin Bryant, David H. Dreyfus
  • Patent number: 8802717
    Abstract: Stereomerically pure (+)-2-[1-(3-Ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione, substantially free of its (?) isomer, and prodrugs, metabolites, polymorphs, salts, solvates, hydrates, and clathrates thereof are discussed. Also discussed are methods of using and pharmaceutical compositions comprising the (+) enantiomer of 2-[1-(3-Ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione are disclosed. The methods include methods of treating and/or preventing disorders ameliorated by the reduction of levels of TNF-? or the inhibition of PDE4.
    Type: Grant
    Filed: November 20, 2012
    Date of Patent: August 12, 2014
    Assignee: Celgene Corporation
    Inventors: George W. Muller, Peter H. Schafer, Hon-Wah Man, Chuansheng Ge
  • Publication number: 20140213589
    Abstract: The invention relates to hydroxyphenyl derivatives of formula (I); and uses thereof as anti-bacterial and/or anti-parasitic agents.
    Type: Application
    Filed: March 28, 2014
    Publication date: July 31, 2014
    Applicant: FAB PHARMA S.A.S.
    Inventors: Alexis DENIS, Vincent Gerusz, Yannick Bonvin
  • Publication number: 20140194486
    Abstract: A compound of formula (I) or a compound of formula (II) or pharmaceutically acceptable salts thereof, wherein R1-R7 and X are as defined in the description, and the use of these compounds in therapy, in particular in treating cancer or as an inhibitor of the interaction of the MDM2 protein with p53.
    Type: Application
    Filed: November 20, 2013
    Publication date: July 10, 2014
    Applicant: CANCER RESEARCH TECHNOLOGY LIMITED
    Inventors: Bernard Thomas GOLDING, Christiane Riedinger, Roger John Griffin, Ian Robert Hardcastle, Eric Valeur, Anna Frances Watson, Martin Noble
  • Publication number: 20140194485
    Abstract: Provided herein are isoindole derivatives, which is enriched with isotopes such as deuterium. Pharmaceutical compositions comprising the isotopes-enriched compounds, and methods of using such compounds are also provided.
    Type: Application
    Filed: January 12, 2012
    Publication date: July 10, 2014
    Applicant: Celgene Corporation
    Inventors: Hon-Wah Man, Louise Michelle Cameron, Anthony Joseph Frank
  • Publication number: 20140187599
    Abstract: Methods of treating a disease selected from dermatomyositis, prurigo nodularis, pyoderma gangrenosum, alopecia areata, hidradenitis suppurtiva, rosacea, lichen planus, giant cell arteritis, Sjogren's syndrome, gout, chronic prostatitis, posterior uveitis, vulvodynia and interstitial cystitis in a human are disclosed. Specific methods encompass the administration of (+)-2-[1-(3-ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione, cyclopropyl {2-[(15)-1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl]-3-oxoisoindolin-4-yl}carboxamide or a combination thereof, or a pharmaceutically acceptable prodrug, metabolite, polymorph, salt, solvate or clathrate thereof.
    Type: Application
    Filed: March 2, 2012
    Publication date: July 3, 2014
    Applicant: CELGENE CORPORATION
    Inventors: Peter H. Schafer, Sai Shankar
  • Publication number: 20140155261
    Abstract: The present specification discloses honeybee repellents exhibiting repellent properties similar to 2-heptanone, compositions comprising such repellents, uses to repel a honeybee from a mammal, location, plant, structure treated of such repellents, and methods of treating a mammal, location, plant, structure by applying such repellents.
    Type: Application
    Filed: May 4, 2012
    Publication date: June 5, 2014
    Applicant: INSCENT, INC.
    Inventors: Daniel F. Woods, Spiros Dimitratos, Robin W. Justice
  • Publication number: 20140155454
    Abstract: Hand wash compositions including ?-phthalimido-peroxyhexanoic acid are described herein.
    Type: Application
    Filed: July 20, 2012
    Publication date: June 5, 2014
    Applicant: Diversey, Inc.
    Inventors: Arnoud U. M. Gengler, Meredith O. Theelen, Ragna M. S. van den Heuvel
  • Publication number: 20140147691
    Abstract: The present invention relates to a preservative formulation for use in treating wood or other cellulosic materials, said formulation comprising: at least one biocidal metal compound; at least one preservative; and an aqueous carrier, wherein the preservative formulation has an uptake in the sapwood of less than about 220 l/m3 yet achieves substantially full penetration of the sapwood. Preferably, the preservative formulation is copper/tebuconazole in a ratio of about 25/1 w/w; and the wood is around 25 mm in thickness—for instance, decking timber.
    Type: Application
    Filed: June 29, 2012
    Publication date: May 29, 2014
    Applicant: ARCH WOOD PROTECTION PTY LTD
    Inventors: David Humphrey, Brett Skewes, Angelo Hrastov, Drago Bagaric, Peter Hausler, Shane McFarling, Greg Jensen, Steve Koch, Noel Koskela, Troy Justice
  • Publication number: 20140137808
    Abstract: The present invention is directed to an insect repelling device that may serve as an effective barrier against ticks. The insect repelling device may include a band of technical fabric, with the fabric being very stretchable. The insect repelling device may be worn around the ankles, wrist or head. The insect repelling device may be worn in pairs on each ankle and/or wrist. The insect repelling device may have an open, tubular design and be made of a high performance, nylon/ polyester fabric, allowing a user to easily insert the foot or hand and fit the device around the ankle or wrist area. Each insect repelling device may be pre-treated with an insecticide or insect repellant, such as Permethrin. In use, the insect repellant device may be effective at preventing biting insects, such as ticks, from crawling onto the user, for example from crawling up the legs of the user.
    Type: Application
    Filed: March 6, 2013
    Publication date: May 22, 2014
    Inventor: Simon J. WHITE
  • Publication number: 20140113012
    Abstract: The present invention provides compounds and compositions for the amelioration of arthritis and joint injuries by inducing mesenchymal stem cells into chondrocytes.
    Type: Application
    Filed: March 26, 2012
    Publication date: April 24, 2014
    Applicant: THE SCRIPPS RESEARCH INSTITUTE
    Inventors: Peter Schultz, Laure Bouchez
  • Publication number: 20140100259
    Abstract: Solid forms comprising (+)-2-[1-(3-Ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione, compositions comprising the solid forms, methods of making the solid forms and methods of their use are disclosed. The methods include methods of treating and/or preventing disorders ameliorated by the reduction of levels of TNF-? or the inhibition of PDE4.
    Type: Application
    Filed: December 10, 2013
    Publication date: April 10, 2014
    Applicant: CELGENE CORPORATION
    Inventors: George W. MULLER, Peter H. SCHAFER, Hon-Wah MAN, Chuansheng GE, Jean XU
  • Patent number: 8673959
    Abstract: A polymer comprising at least one type of repeat unit comprising at least one type of an optionally substituted indolocarbazole moiety and at least one divalent linkage.
    Type: Grant
    Filed: April 22, 2008
    Date of Patent: March 18, 2014
    Assignee: Xerox Corporation
    Inventors: Yuning Li, Beng S Ong, Yiliang Wu, Ping Liu
  • Patent number: 8673360
    Abstract: Powdery compositions for intranasal administration, which comprise non-peptide/non-protein drugs and as a carrier, crystalline cellulose aggregates having a particular cribriform particle diameter, yield rapid action and high absorbability of the drugs.
    Type: Grant
    Filed: August 5, 2005
    Date of Patent: March 18, 2014
    Assignee: Shin Nippon Biomedical Laboratories, Ltd.
    Inventors: Ryoichi Nagata, Shunji Haruta
  • Publication number: 20140073574
    Abstract: A method for enhancing glycemic control and/or insulin sensitivity in a human subject having diabetic nephropathy and/or metabolic syndrome comprises administering to the subject a selective endothelin A (ETA) receptor antagonist in a glycemic control and/or insulin sensitivity enhancing effective amount. A method for treating a complex of comorbidities in an elderly diabetic human subject comprises administering to the subject a selective ETA receptor antagonist in combination or as adjunctive therapy with at least one additional agent that is (i) other than a selective ETA receptor antagonist and (ii) effective in treatment of diabetes and/or at least one of said comorbidities other than hypertension. A therapeutic combination useful in such a method comprises a selective ETA receptor antagonist and at least one antidiabetic, anti-obesity or antidyslipidemic agent other than a selective ETA receptor antagonist.
    Type: Application
    Filed: November 13, 2013
    Publication date: March 13, 2014
    Inventors: Robert L. Roden, Richard J. Gorczynski, Michael J. Gerber
  • Publication number: 20140066408
    Abstract: This invention provides, but is not limited to, novel oleanolic acid derivatives having the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.
    Type: Application
    Filed: January 14, 2013
    Publication date: March 6, 2014
    Applicant: REATA PHARMACEUTICALS, INC.
    Inventor: REATA PHARMACEUTICALS, INC.
  • Publication number: 20140057873
    Abstract: There is provided amino acid ester compounds comprising at least one nitric oxide releasing group, pharmaceutically acceptable salts thereof and compositions thereof. These compounds involve an amino acid side-chain or an amino acid derivative thereof and a nitric oxide releasing group as depicted in the following structures: wherein R1 is either an ethyl or an amino acid side-chain group or an amino acid derivative thereof and R2 is an amino acid side-chain group or an amino acid derivative thereof and n is an integer from 1 to 10.
    Type: Application
    Filed: November 1, 2013
    Publication date: February 27, 2014
    Inventor: Michael Farber