Plural Chalcogens Bonded Directly To The Five-membered Hetero Ring By Nonionic Bonding Patents (Class 514/425)
  • Patent number: 11091434
    Abstract: The present invention relates to compounds that inhibit the activity of Type III deiodinase (DIO3). The present invention further relates to methods for treating or preventing depression, depression associated with other psychiatric or general medical diseases or conditions, condition amenable to treatment with known anti-depressants and cancer, particularly by using the compounds of the invention.
    Type: Grant
    Filed: August 28, 2019
    Date of Patent: August 17, 2021
    Assignees: HADASIT MEDICAL RESEARCH SERVICES AND DEVELOPMENT LTD., INDIAN INSTITUTE OF SCIENCE
    Inventors: Bernard Lerer, Mugesh Govindasamy, Tzuri Lifschytz
  • Patent number: 10987430
    Abstract: Provided in the present invention are a di-substituted maleic amide linker conjugated to an antibody and a preparation method and use thereof. In particular, the present invention conjugates a strongly cytotoxic active substance to a biomacromolecule through a class of new linkers. The class of linkers can selectively act simultaneously with disulphide chains, so as to greatly improve the substance homogeneity of a conjugate. The conjugate prepared by the linker of the present invention has a high inhibitory activity on a cell strain expressing the corresponding antigen. Also provided is a method for preparing the above-mentioned conjugate and the use.
    Type: Grant
    Filed: November 24, 2017
    Date of Patent: April 27, 2021
    Assignees: Mabwell (Shanghai) Bioscience Co., Ltd., Jiangsu Mabwell Health Pharmaceutical R&D Co., Ltd.
    Inventors: Jingkang Shen, Tao Meng, Lanping Ma, Xin Wang, Hongli Peng, Yongliang Zhang, Ting Yu, Lin Chen, Zhiyan Du, Ying Wang
  • Patent number: 10654864
    Abstract: The present disclosure generally provides compounds useful for treating cancer. In some aspects, the disclosure provides small-molecule cytotoxins that are chemically modified to include one or more moieties that include hydrophobic portions. In some embodiments, the disclosure provides small-molecule cytotoxins that are chemically modified with fatty acid-containing moieties. In some aspects, the disclosure provides compositions, such as pharmaceutical compositions, that include such modified small-molecule cytotoxins and a protein. In some embodiments, the protein is albumin or an albumin mimetic. Further, the disclosure provides various uses of these compounds and compositions.
    Type: Grant
    Filed: April 4, 2018
    Date of Patent: May 19, 2020
    Assignees: The Regents of the University of California, Elevance Renewable Sciences, Inc.
    Inventors: Cassandra E. Callmann, Matthew P. Thompson, Nathan C. Gianneschi, Clare L. M. LeGuyader, Paul A. Bertin
  • Patent number: 10603290
    Abstract: Drug combinations and their use are disclosed. A first drug is administered in combination with a second drug. The first drug such as fenfluramine is characterized by the formation of a metabolite including 5-HT2B agonists such as norfenfluramine with known adverse side effects. The second drug is in the form of a CYP inhibitor such as cannabidiol which modulates the formation of metabolite down thereby making the first drug safer.
    Type: Grant
    Filed: November 16, 2018
    Date of Patent: March 31, 2020
    Assignee: ZOGENIX INTERNATIONAL LIMITED
    Inventors: Stephen J. Farr, Brooks Boyd
  • Patent number: 10213411
    Abstract: Methods and pharmaceutical compositions comprising one or more prodrugs (e.g., aminoalkyl prodrugs) of monomethyl fumarate (MMF) thereof are provided herein for the treatment of a heart failure disease, including heart failure with preserved ejection fraction. The compounds of the present disclosure are configured to be converted in vivo, upon oral administration, to monomethyl fumarate. Upon conversion, the active moiety (i.e., monomethyl fumarate) of various embodiments is effective in treating subjects suffering from a heart failure disease, including heart failure with preserved ejection fraction.
    Type: Grant
    Filed: August 29, 2016
    Date of Patent: February 26, 2019
    Inventor: Vijaykumar Rajasekhar
  • Patent number: 9896421
    Abstract: Provided are a novel compound having skin-whitening, anti-oxidizing and PPAR activities and a medical use thereof, and the compound has skin-whitening activities for the suppression of tyrosinase, and accordingly, is useful for use in skin-whitening pharmaceutical composition or cosmetic products; has anti-oxidant activities, and accordingly, is useful for the prevention and treatment of skin-aging; and has PPAR activities, and in particular, PPAR? and PPAR? activities, and accordingly, is useful for use in pharmaceutical compositions or health foods which are effective for the prevention and treatment of obesity, metabolic disease, or cardiovascular disease.
    Type: Grant
    Filed: December 18, 2015
    Date of Patent: February 20, 2018
    Assignee: Pusan National University Industry-University Cooperation Foundation
    Inventors: Hae Young Chung, Hyung Ryong Moon, Min Hi Park, Young Mi Ha, Yun Jung Park, Ji Young Park, Jin Ah Kim, Ji Yeon Lee, Kyung Jin Lee
  • Patent number: 9572760
    Abstract: The present invention relates to novel uses of compounds from Antrodia cinnamomea mycelia and mixtures comprising the compounds. The novel uses comprise whitening skin, combating skin ageing, reducing scar formation, inducing or enhancing liver regeneration, or treating fibrosis or a fibrosis-associated disorder in a subject in need thereof. The compounds have the formula and preferably are selected from 3-isobutyl-4-[4-(3-methyl-2-butenyloxy)phenyl]furan-2,5-dione, 3-isobutyl-4-[4-(3-methyl-2-butenyloxy)phenyl]-1H-pyrrol-2,5-dione, 3-isobutyl-4-[4-(3-methyl-2-butenyloxy)phenyl]-1H-pyrrol-1-ol-2,5-dione, 3R*,4S*-1-hydroxy-3-isobutyl-4-[4-(3-methyl-2-butenyloxy)phenyl]pyrrolidine-2,5-dione, and 3R*,4R*-1-hydroxy-3-isobutyl-4-[4-(3-methyl-2-butenyloxy)phenyl]pyrrolidine-2,5-dione.
    Type: Grant
    Filed: October 22, 2014
    Date of Patent: February 21, 2017
    Assignee: Simpson Biotech Co., Ltd.
    Inventors: Kai-Wen Huang, Chia-Chin Sheu
  • Patent number: 9090558
    Abstract: The present invention provides compounds of formula (I), wherein: R1 is unsubstituted C1-C6 alkyl; La is substituted or unsubstituted C1-C6 alkyl linker, substituted or unsubstituted C3-C10 carbocycle, substituted or unsubstituted heterocycle comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S, or substituted or unsubstituted heteroaryl comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S; and R2 and R3 are each, independently, H, substituted or unsubstituted C1-C6 alkyl, or substituted or unsubstituted C6-C10 aryl; or alternatively, R2 and R3, together with the nitrogen atom to which they are attached, form a substituted or unsubstituted heteroaryl comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S or a substituted or unsubstituted heterocycle comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S.
    Type: Grant
    Filed: February 14, 2014
    Date of Patent: July 28, 2015
    Assignee: Alkermes Pharma Ireland Limited
    Inventors: Tarek A. Zeidan, Scott Duncan, Christopher P. Hencken, Thomas Andrew Wynn, Carlos N. Sanrame
  • Publication number: 20150148359
    Abstract: Uses of a compound of any of Formulas I-VI as a cytotoxic inhibitor of undifferentiated cells are disclosed herein, as well as pharmaceutical compositions comprising a compound of any of Formulas I-VI, and methods for identifying a lead candidate for inhibiting undifferentiated cells. Further disclosed are uses of an SCD-1 inhibitor as a cytotoxic inhibitor of undifferentiated cells.
    Type: Application
    Filed: May 22, 2013
    Publication date: May 28, 2015
    Inventors: Uri Ben-David, Nissim Benvenisty, Payal Arora, Qing-Fen Gan, Ralph J. Garippa
  • Publication number: 20150119442
    Abstract: The present invention relates to biodegradable biocide agents against marine woodborers. In particular, the present invention relates to novel slow releasing biocide impregnating solutions against marine woodborers, and methods of creating anti marine woodborer environments.
    Type: Application
    Filed: May 22, 2014
    Publication date: April 30, 2015
    Applicant: Teredo Marine Protection ApS
    Inventor: Michael Igelso Hvidt
  • Publication number: 20150110726
    Abstract: The present invention relates to novel uses of compounds from Antrodia cinnamomea mycelia and mixtures comprising the compounds. The novel uses comprise whitening skin, combating skin ageing, reducing scar formation, inducing or enhancing liver regeneration, or treating fibrosis or a fibrosis-associated disorder in a subject in need thereof. The compounds have the formula and preferably are selected from 3-isobutyl-4-[4-(3-methyl-2-butenyloxy)phenyl]furan-2,5-dione, 3-isobutyl-4-[4-(3-methyl-2-butenyloxy)phenyl]-1H-pyrrol-2,5-dione, 3-isobutyl-4-[4-(3-methyl-2-butenyloxy)phenyl]-1H-pyrrol-1-ol-2,5-dione, 3R*,4S*-1-hydroxy-3-isobutyl-4-[4-(3-methyl-2-butenyloxy)phenyl]pyrrolidine-2,5-dione, and 3R*,4R*-1-hydroxy-3-isobutyl-4-[4-(3-methyl-2-butenyloxy)phenyl]pyrrolidine-2,5-dione.
    Type: Application
    Filed: October 22, 2014
    Publication date: April 23, 2015
    Applicant: Simpson Biotech Co., Ltd.
    Inventors: Kai-Wen Huang, Chia-Chin Sheu
  • Publication number: 20150093370
    Abstract: The present invention provides albumin-binding probes capable of reversibly linking to short-lived amino-containing drugs and non-covalently associating with albumin in-vivo, thereby converting said drugs into inactive reactivable prodrugs having prolonged lifetime in-vivo. The invention further provides conjugates of said probes with amino-containing drugs, as well as pharmaceutical compositions and uses thereof.
    Type: Application
    Filed: December 9, 2014
    Publication date: April 2, 2015
    Inventors: Yoram SHECHTER, Matityahu FRIDKIN
  • Publication number: 20150087688
    Abstract: The present invention relates to a prodrug or a pharmaceutically acceptable salt thereof comprising a biologically active moiety-linker conjugate D-L, wherein D is a hydroxyl-comprising biologically active moiety; and L is a promoiety comprising a moiety L1 represented by formula (I) and wherein L1 is substituted with one to four groups L2-Z and optionally further substituted, provided that the hydrogen marked with the asterisk in formula (I) is not replaced by a substituent; wherein L2 is a single chemical bond or a spacer and Z is a carrier group. The invention also relates to pharmaceutical compositions comprising said prodrugs and their use as medicaments.
    Type: Application
    Filed: April 24, 2013
    Publication date: March 26, 2015
    Inventors: Ulrich Hersel, Torben Lebmann, Harald Rau
  • Publication number: 20150080364
    Abstract: Provided herein are carbamate compounds which may be useful in the treatment of for example, pain, solid tumors and/or obesity.
    Type: Application
    Filed: March 15, 2013
    Publication date: March 19, 2015
    Applicants: Abide Therapeutics, Inc., The Scripps Research Insititute
    Inventors: Justin S. Cisar, Cheryl A. Grice, Todd K. Jones, Dong-Hui Wang, Olivia Weber, Benjamin F. Cravatt, Micah J. Niphakis, Armand Cognetta, Jae Won Chang
  • Patent number: 8980321
    Abstract: A drug in a solubility-improved form is combined with a concentration-enhancing polymer in a sufficient amount so that the combination provides substantially enhanced drug concentration in a use environment relative to a control comprising the same amount of the same solubility-improved form of drug without the concentration-enhancing polymer.
    Type: Grant
    Filed: July 14, 2014
    Date of Patent: March 17, 2015
    Assignee: Bend Research, Inc.
    Inventors: William J. Curatolo, Ravi M. Shanker, Walter C. Babcock, Dwayne T. Friesen, James A. S. Nightingale, Douglas A. Lorenz
  • Publication number: 20150073004
    Abstract: The present invention relates to compounds of formula 1 that are useful for the preventive and/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: November 18, 2014
    Publication date: March 12, 2015
    Inventors: Imre BATA, Veronika BARTONE BODOR, Attila VASAS, Peter BUZDER-LANTOS, Gyorgy FERENCZY, Zsuzsanna TOMOSKOZI, Gabor SZELECZKY, Zsuzsanna SZAMOSVOLGYI
  • Publication number: 20150065534
    Abstract: The invention relates to compounds of formula (I), wherein R1, R2, and n are defined in the detailed description and claims. In particular, the present invention relates to the compounds of formula I for use in the manufacture and delivery of conjugated moieties such as small molecules, peptides, nucleic acids, fluorescent moieties, and polymers which are linked to LFA-1 integrin antagonists to target cells expressing LFA-1.
    Type: Application
    Filed: January 24, 2013
    Publication date: March 5, 2015
    Inventors: Robert Alan Goodnow, Jr., Matthew Michael Hamilton, Agnieszka Kowalczyk, Achyutharao Sidduri
  • Patent number: 8969354
    Abstract: The invention relates to Fatty Acid Fumarate Derivatives; compositions comprising an effective amount of a Fatty Acid Fumarate Derivative; and methods for treating or preventing cancer, a metabolic disorder or neurodegenerative disorder comprising the administration of an effective amount of a Fatty Acid Fumarate Derivative.
    Type: Grant
    Filed: November 9, 2012
    Date of Patent: March 3, 2015
    Assignee: Catabasis Pharmaceuticals, Inc.
    Inventors: Jill C. Milne, Michael R. Jirousek, Jean E. Bemis, Chi B. Vu
  • Patent number: 8957106
    Abstract: A proliferation of cells can be reduced by contacting the cells with a compound having formula (I) where R and R? are each alkyl groups, R? is hydrogen or an alkyl group and X3, X4 and X5 are each independently selected from the group consisting of hydrogen, benzyl, t-butyldimethylsiloxy radical and triphenylmethyl. Accordingly, compounds of formula (I) can be used for treatment of tumors including melanoma. Also a secretion of a matrix metalloproteinase (MMP) enzyme by cells can be reduced by contacting the cells with the compound having formula (I). Accordingly, compounds of formula (I) can be used for treatment physiological conditions associated with an elevated MMP level, such as tumors.
    Type: Grant
    Filed: April 18, 2008
    Date of Patent: February 17, 2015
    Assignee: The Chancellor, Masters and Scholars of the University of Oxford
    Inventors: Raymond Dwek, Wanda Buzgariu, Anca Hirtopeanu, Robert Moriarty, Gabriela Negroiu, Norica Nichita, Livia Zdrentu, Nicole Zitzmann
  • Publication number: 20150038523
    Abstract: The invention relates to compounds of formula (I): wherein R1, R2, and n are defined in the detailed description and claims. In particular, the present invention relates to the compounds of formula (I) for use in the manufacture and delivery of conjugated moieties such as small molecules, peptides, nucleic acids, fluorescent moieties, and polymers which are linked to alpha-V-beta-integrin antagonists to target cells expressing alpha-V-beta-3.
    Type: Application
    Filed: January 22, 2013
    Publication date: February 5, 2015
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Robert Alan Goodnow, Jr., Matthew Michael Hamilton, Agnieszka Kowalczyk, Achyutharao Sidduri
  • Publication number: 20150031715
    Abstract: The invention relates to compounds of formula I: wherein R1, R2, and n are defined in the detailed description and claims. In particular, the present invention relates to the compounds of formula I for use in the manufacture and delivery of conjugated moieties such as small molecules, peptides, nucleic acids, fluorescent moieties, and polymers which are linked to VLA-4 integrin antagonists to target cells expressing VLA-4.
    Type: Application
    Filed: January 24, 2013
    Publication date: January 29, 2015
    Inventors: Robert Alan Goodnow, JR., Matthew Michael Hamilton, Achyutharao Sidduri
  • Patent number: 8937187
    Abstract: The invention relates to compounds of formula (I): The invention likewise relates to a cosmetic method for depigmenting, lightening and/or whitening keratin materials, more particularly the skin, that utilizes these compounds.
    Type: Grant
    Filed: November 23, 2011
    Date of Patent: January 20, 2015
    Assignee: L'Oreal
    Inventor: Xavier Marat
  • Patent number: 8921577
    Abstract: The present invention relates to novel 5-hydroxy-5-aryl-pyrrol-2-ones, their preparation and their use as non-peptide CCK ligands, particularly in pharmaceutical formulations thereof.
    Type: Grant
    Filed: July 2, 2012
    Date of Patent: December 30, 2014
    Assignee: PNB Vesper Life Sciences Pvt. Ltd.
    Inventors: Padijarethakkal N Balaram, Pornthip Lattmann
  • Patent number: 8901038
    Abstract: The invention relates to novel compounds of the formula (I) in which W, X, Y, Z, and CKE have the meanings given above, to a plurality of processes and intermediates for their preparation and to their use as pesticides and/or herbicides and/or fungicides. Moreover, the invention relates to selectively herbicidal compositions comprising, firstly, the biphenyl-substituted cyclic ketoenols and, secondly, a crop plant compatibility-improving compound. The present invention furthermore relates to the boosting of the action of crop protection compositions comprising in particular biphenyl-substituted cyclic ketoenols through the addition of ammonium or phosphium salts and optionally penetrants, to the corresponding compositions, to processes for their preparation and to their use in crop protection as insecticides and/or nematicides and/or acaricides and/or fungicides and/or for preventing unwanted plant growth.
    Type: Grant
    Filed: February 10, 2011
    Date of Patent: December 2, 2014
    Assignee: Bayer CropScience AG
    Inventors: Reiner Fischer, Stefan Lehr, Isolde Häuser-Hahn, Christopher Hugh Rosinger, Chieko Ueno, Arnd Voerste, Elmar Gatzweiler, Ines Heinemann, Ulrich Görgens
  • Publication number: 20140343117
    Abstract: Described herein are methods of diagnosing and/or classifying heatiness, a syndrome recognized in traditional Chinese Medicine, comprising assessing a patient by checking for selected symptoms, and assigning a score to the patient based on the symptoms exhibited. The invention further provides methods of treatment and the use of oral care compositions to treat heatiness.
    Type: Application
    Filed: December 21, 2011
    Publication date: November 20, 2014
    Applicant: COLGATE-PALMOLIVE COMPANY
    Inventors: David Lungpao Chang, Zheng Yang, ZhaoSheng Huang, SiJun Liu
  • 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: 20140319059
    Abstract: Provided herein is a method for reducing down-time in a recreational body of water having a water filtering system and water recirculation system after a potential release of Cryptospridium oocyst and/or Giardia cysts. Also described is a kit for practicing the method for reducing down-time in a recreational body of water that may have a potential release of Cryptospridium oocyst and/or Giardia cysts.
    Type: Application
    Filed: April 25, 2014
    Publication date: October 30, 2014
    Inventor: Michael Joseph Unhoch
  • Publication number: 20140322325
    Abstract: A drug in a solubility-improved form is combined with a concentration-enhancing polymer in a sufficient amount so that the combination provides substantially enhanced drug concentration in a use environment relative to a control comprising the same amount of the same solubility-improved form of drug without the concentration-enhancing polymer.
    Type: Application
    Filed: July 14, 2014
    Publication date: October 30, 2014
    Applicant: Bend Research, Inc.
    Inventors: William J. Curatolo, Ravi M. Shanker, Walter C. Babcock, Dwayne T. Friesen, James A. S. Nightingale, Douglas A. Lorenz
  • Publication number: 20140314882
    Abstract: Combinations of compounds are provided that produce a synergistic effect when administered.
    Type: Application
    Filed: June 27, 2014
    Publication date: October 23, 2014
    Inventors: Frederick P. ROTH, Murat COKOL, Hon Nian CHUA
  • Publication number: 20140308325
    Abstract: The present invention provides a hemostatic porous composite sponge comprising i) a matrix of a biomaterial and ii) one hydrophilic polymeric component comprising reactive groups wherein i) and ii) are associated with each other so that the reactivity of the polymeric component is retained, wherein associated means that said polymeric component is coated onto a surface of said matrix of a biomaterial, or said matrix is impregnated with said polymeric material, or both.
    Type: Application
    Filed: February 19, 2014
    Publication date: October 16, 2014
    Inventors: Hans Christian Hedrich, Joris Hoefinghoff
  • Patent number: 8853257
    Abstract: The present invention provides methods and pharmaceutical compositions for treating ocular disorders associated with elevated intraocular pressure, such as glaucoma, by administering anti-epileptic or anti-convulsant compounds of the succinimide family, in particular compounds of formula I and/or II as defined herein.
    Type: Grant
    Filed: September 6, 2011
    Date of Patent: October 7, 2014
    Inventor: Mordechai Sharir
  • Publication number: 20140296150
    Abstract: The present invention relates to prodrugs or a pharmaceutically acceptable salt thereof comprising a covalent treprostinil carrier conjugate as well as pharmaceutical composition comprising said compounds. The compounds may be used as medicaments, especially for diseases or disorders which can be treated by treprostinil, such as pulmonary arterial hypertension (PAH).
    Type: Application
    Filed: August 10, 2012
    Publication date: October 2, 2014
    Applicant: Ascendis Pharma A/S
    Inventors: Ulrich Hersel, Harald Rau, Torben Lessmann, Nicola Bisek, Guillaume Maitro, Kennett Sprogøe, Thomas Wegge, Oliver Keil, Joachim Zettler
  • 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: 20140275048
    Abstract: The present invention provides compounds of formula (I), and pharmaceutical compositions thereof.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Applicant: Alkermes Pharma Ireland Limited
    Inventors: Tarek A. Zeidan, Scott Duncan, Christopher P. Hencken, Thomas Andrew Wynn, Carlos N. Sanrame
  • Publication number: 20140275203
    Abstract: The present invention is for method of treating metabolic bone disease, new compounds and pharmaceutical compositions comprising the active ingredients having inhibition effects on osteoclast differentiation. The pharmaceutical composition comprising new compounds according to the present invention can be used as medicines for treating metabolic bone diseases such as bone metastatic cancer, solid cancer bone metastasis, musculoskeletal complication by solid cancer bone metastasis, hypercalcemia by malignant tumor, multiple myeloma, primary bone tumor, osteoporosis, rheumatoid arthritis, osteoarthritis, periodontal disease, inflammatory resorption of alveolar bone, inflammatory resorption of bone, and Paget's disease.
    Type: Application
    Filed: June 2, 2014
    Publication date: September 18, 2014
    Applicant: Metacine, Inc.
    Inventors: Bae Keun PARK, Sung-Hwa YOON, Ju-Young PARK, Sung Hoon PARK
  • Publication number: 20140275206
    Abstract: The present invention is to provide uses of the L-oxiracetam in preparation of medicines for preventing or treating coma. Experimental results show that L-oxiracetam wake-promoting effects of alcoholism-induced coma is obvious, and D-oxiracetam has basically no effect. The effect of the above wake-promoting effects of L-oxiracetam is 2 times greater than racemic oxiracetam. The wake-promoting effects of L-oxiracetam on trauma or anesthesia-induced coma are both significant.
    Type: Application
    Filed: April 24, 2012
    Publication date: September 18, 2014
    Applicant: Chongqing Runze Pharmaceutical Company Limited
    Inventor: Lei Ye
  • Publication number: 20140275205
    Abstract: The present invention provides compounds of formula (I), wherein: R1 is unsubstituted C1-C6 alkyl; La is substituted or unsubstituted C1-C6 alkyl linker, substituted or unsubstituted C3-C10 carbocycle, substituted or unsubstituted heterocycle comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S, or substituted or unsubstituted heteroaryl comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S; and R2 and R3 are each, independently, H, substituted or unsubstituted C1-C6 alkyl, or substituted or unsubstituted C6-C10 aryl; or alternatively, R2 and R3, together with the nitrogen atom to which they are attached, form a substituted or unsubstituted heteroaryl comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S or a substituted or unsubstituted heterocycle comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S.
    Type: Application
    Filed: February 14, 2014
    Publication date: September 18, 2014
    Inventors: Tarek A. Zeidan, Scott Duncan, Christopher P. Hencken, Thomas Andrew Wynn, Carlos N. Sanrame
  • Patent number: 8791102
    Abstract: This disclosure relates to sphingosine-1-phosphate (S1P) receptor antagonists, compositions comprising the S1P receptor antagonists and methods for using and processes for making the S1P receptor antagonists. In particular, this disclosure relates to sphingosine-1-phosphate 1 (S1P1) receptor antagonists, compositions comprising the S1P1 receptor antagonist and methods for using the S1P1 receptor antagonist, such as in the treatment of cancer, and processes for making the S1P1 receptor antagonists.
    Type: Grant
    Filed: October 16, 2009
    Date of Patent: July 29, 2014
    Assignee: Exelixis, Inc.
    Inventors: Mohamed Abdulkader Ibrahim, Joon Won Jeong, Henry William Beecroft Johnson, Patrick Kearney, James W. Leahy, Gary L. Lewis, Robin Tammie Noguchi, John M. Nuss
  • Patent number: 8772329
    Abstract: The present invention relates to compounds from mycelium of Antrodia cinnamomea. The present invention also relates to a composition and a method for treating or prophylaxis of hepatitis C virus (HCV) infection.
    Type: Grant
    Filed: January 28, 2008
    Date of Patent: July 8, 2014
    Assignee: Simpson Biotech Co., Ltd.
    Inventors: Chia-Chin Sheu, Masao Hattori
  • Publication number: 20140179665
    Abstract: The present invention includes a method of inhibiting, suppressing or preventing HBV infection in an individual in need thereof, comprising administering to the individual a therapeutically effective amount of at least one compound of the invention.
    Type: Application
    Filed: December 9, 2013
    Publication date: June 26, 2014
    Inventors: George D. Hartman, Osvaldo A. Flores
  • Publication number: 20140179753
    Abstract: The present invention relates to compounds from Antrodia cinnamomea. The present invention also relates to a composition and a method for treating or prophylaxis of hepatitis C virus (HCV) or human immunodeficiency virus (HIV) infection.
    Type: Application
    Filed: March 5, 2014
    Publication date: June 26, 2014
    Applicant: Simpson Biotech Co., Ltd.
    Inventors: Masao HATTORI, Ali EL-HALAWANY, Megumi MIZUNO, Chia-Chin SHEU
  • Publication number: 20140171444
    Abstract: The present invention provides aryl- or heteroaryl-diketo acid compounds effective to inhibit an activity of a Mycobacterial malate synthase enzyme or to inhibit a malate synthase activity in other bacteria having the enzyme. The compounds may be phenyl- naphthyl-, or thienyl-substituted diketo acids and carboxylate derivatives thereof. Also provided are methods of treating tuberculosis or other pathophysiological conditions associated with a malate synthase enzyme with the inhibitory compounds and methods of in silico design of the inhibitory compounds. In addition, the present invention provides the inhibitory compounds designed by this method. Furthermore, three-dimensional X-ray crystal structures of the Mycobacterial malate synthase complexed with the inhibitory compounds are provided. Further still a method for stabilizing an aromatic or heteroaromatic diketo acid or its prodrug or close analog in solution by derivatizing at least the ortho position on the aromatic ring is provided.
    Type: Application
    Filed: March 3, 2014
    Publication date: June 19, 2014
    Applicant: THE TEXAS A&M UNIVERSITY SYSTEM
    Inventors: Joel S. Freundlich, James C. Sacchettini, Inna V. Kriger, Thomas R. Ioerger, Vijay Gawandi
  • Publication number: 20140155457
    Abstract: Provided is a method of relieving, improving, preventing or treating xerostomia including applying an oral cavity composition including a polyethylene glycol (PEG) derivative whose reactor is modified to form a covalent bond with an epithelial cell of the oral cavity. An oral moisturizing effect and moisture persistency are increased and the method is effective against xerostomia due to aging or disease.
    Type: Application
    Filed: October 4, 2013
    Publication date: June 5, 2014
    Inventors: KWANG NHO, Min Jung AHN, Byung Hee SOHN, Chang Min HYUN, Jung Hun LEE
  • Publication number: 20140155456
    Abstract: The invention relates to the use of cannabidiol (CBD), at a dose of greater than 300 mg/day, in combination with a standard anti-epileptic drug (SAED) which acts via sodium or calcium channels, for use in the treatment of epilepsy. The SAED is preferably one which•modifies low-threshold or transient neuronal calcium currents,or•reduces high-frequency neuronal firing and sodium-dependent action potentials and enhances GABA effects. Preferred SAEDs are ethosuximide and valproate.
    Type: Application
    Filed: January 3, 2012
    Publication date: June 5, 2014
    Applicants: Otsuka Pharmaceutical Co., Limited, GW Pharma Limited
    Inventors: Ben Whalley, Claire Williams, Gary Stephens
  • Publication number: 20140128446
    Abstract: Compounds of Formula (I) are disclosed herein and their use in inhibiting quorum sensing in bacteria.
    Type: Application
    Filed: June 18, 2012
    Publication date: May 8, 2014
    Applicant: THE FLORIDA INTERNATIONAL UNIVERSITY BOARD OF TRUSTEES
    Inventors: Venkata L. Malladi, Lisa Schneper, Adam J. Sobczak, Kalai Mathee, Stanislaw F. Wnuk
  • Patent number: 8703165
    Abstract: Compounds of the formula (I) wherein the substituents are as defined in claim 1, are useful as pesticides.
    Type: Grant
    Filed: November 30, 2010
    Date of Patent: April 22, 2014
    Assignee: Syngenta Crop Protection, Inc.
    Inventors: Thomas Pitterna, Michel Muehlebach, Jurgen Harry Schaetzer
  • Patent number: 8703968
    Abstract: The present invention relates to compounds from Antrodia cinnamomea. The present invention also relates to a composition and a method for treating or prophylaxis of hepatitis C virus (HCV) or human immunodeficiency virus (HIV) infection.
    Type: Grant
    Filed: October 17, 2012
    Date of Patent: April 22, 2014
    Assignee: Simpson Biotech Co., Ltd.
    Inventors: Masao Hattori, Ali El-Halawany, Megumi Mizuno, Chia-Chin Sheu
  • Publication number: 20140099333
    Abstract: The present invention relates to pyrrolidinone derivatives. The pyrrolidinone derivatives are GPR119 modulators and useful for the prevention and/or treatment of diabetes, obesity, dyslipidemia and related disorders. The invention furthermore relates to the use of pyrrolidinone derivatives as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.
    Type: Application
    Filed: October 8, 2013
    Publication date: April 10, 2014
    Applicant: SANOFI
    Inventors: Lothar SCHWINK, Martin BOSSART, Heiner GLOMBIK, Matthias GOSSEL, Dieter KADEREIT, Thomas KLABUNDE, Thomas MAIER, Siegfried STENGELIN
  • Patent number: 8669281
    Abstract: The present invention provides compounds of formula (I), wherein: R1 is unsubstituted C1-C6 alkyl; La is substituted or unsubstituted C1-C6 alkyl linker, substituted or unsubstituted C3-C10 carbocycle, substituted or unsubstituted heterocycle comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S, or substituted or unsubstituted heteroaryl comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S; and R2 and R3 are each, independently, H, substituted or unsubstituted C1-C6 alkyl, or substituted or unsubstituted C6-C10 aryl; or alternatively, R2 and R3, together with the nitrogen atom to which they are attached, form a substituted or unsubstituted heteroaryl comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S or a substituted or unsubstituted heterocycle comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S.
    Type: Grant
    Filed: September 20, 2013
    Date of Patent: March 11, 2014
    Assignee: Alkermes Pharma Ireland Limited
    Inventors: Tarek A. Zeidan, Scott Duncan, Christopher P. Hencken, Thomas Andrew Wynn, Carlos N. Sanrame
  • Patent number: 8664255
    Abstract: The present invention provides aryl- or heteroaryl-diketo acid compounds effective to inhibit an activity of a Mycobacterial malate synthase enzyme or to inhibit a malate synthase activity in other bacteria having the enzyme. The compounds may be phenyl- naphthyl-, or thienyl-substituted diketo acids and carboxylate derivatives thereof. Also provided are methods of treating tuberculosis or other pathophysiological conditions associated with a malate synthase enzyme with the inhibitory compounds and methods of in silico design of the inhibitory compounds. In addition, the present invention provides the inhibitory compounds designed by this method. Furthermore, three-dimensional X-ray crystal structures of the Mycobacterial malate synthase complexed with the inhibitory compounds are provided. Further still a method for stabilizing an aromatic or heteroaromatic diketo acid or its prodrug or close analog in solution by derivatizing at least the ortho position on the aromatic ring is provided.
    Type: Grant
    Filed: October 20, 2009
    Date of Patent: March 4, 2014
    Assignee: The Texas A&M University System
    Inventors: Joel S. Freundlich, James C. Sacchettini, Inna V. Kriger, Thomas R. Ioerger, Vijay Gawandi