Chalcogen In The Six-membered Hetero Ring Patents (Class 514/90)
  • Patent number: 10308940
    Abstract: The present invention is directed to antisense oligomeric compounds that may be used in the treatment Pompe disease as well as method for modulating the splicing of the GAA gene and method to treat Pompe disease. Also pharmaceutical compositions comprising the antisense oligomeric compounds are part of the invention.
    Type: Grant
    Filed: June 10, 2015
    Date of Patent: June 4, 2019
    Assignee: ERASMUS UNIVERSITY MEDICAL CENTER ROTTERDAM
    Inventors: Atze Jacobus Bergsma, Erik van der Wal, Wilhelmus Wenceslaus Matthias Pijnappel, Antje Tjitske van der Ploeg, Arnoldus Reuser
  • Patent number: 10195220
    Abstract: The application describes Hydrogen Sulphide (H2S), or a (H2S) generating compound or compound capable of stimulating H2S production in a pregnant subject, for use in the treatment of pre-eclampsia (PE) or fetal growth restriction.
    Type: Grant
    Filed: March 3, 2014
    Date of Patent: February 5, 2019
    Assignee: ASTON UNIVERSITY
    Inventors: Asif Ahmed, Keqing Wang
  • Patent number: 10172839
    Abstract: A method of alleviating or treating symptoms of cancer and/or effects of chemotherapy or of kinase inhibitors includes a step of identifying a subject having cancer. A reduced caloric diet is administered to the subject for a first time period, the reduced caloric diet providing at most 1000 kcal per day. A kinase inhibitor is administered to the subject.
    Type: Grant
    Filed: March 27, 2015
    Date of Patent: January 8, 2019
    Assignee: UNIVERSITY OF SOUTHERN CALIFORNIA
    Inventors: Valter D. Longo, Stefano Di Biase
  • Patent number: 9850267
    Abstract: The present invention provides dicyclohexylamine salt of fosaprepitant (fosaprepitant DCHA), a process for preparing fosaprepitant DCHA, and a use of fosaprepitant DCHA in the preparation of pharmaceutically acceptable fosaprepitant dimeglumine with high purity. Fosaprepitant dimeglumine is prepared by treating fosaprepitant DCHA with an acid to form fosaprepitant, followed by adding N-methyl-D-glucamine to fosaprepitant.
    Type: Grant
    Filed: May 26, 2016
    Date of Patent: December 26, 2017
    Assignee: Navinta, LLC
    Inventors: Jigneshkumar Jasubhai Patel, Raja Jeyakumar John Muthiah
  • Patent number: 9616076
    Abstract: Certain embodiments are directed to methods of treating respiratory infection by administering an H2S donor.
    Type: Grant
    Filed: June 2, 2015
    Date of Patent: April 11, 2017
    Assignee: THE BOARD OF REGENTS OF THE UNIVERSITY OF TEXAS SYSTEMS
    Inventors: Antonella Casola, Roberto P. Garofalo
  • Patent number: 9504701
    Abstract: Certain embodiments are directed to methods of treating respiratory infection by administering an H2S donor.
    Type: Grant
    Filed: November 13, 2015
    Date of Patent: November 29, 2016
    Assignee: THE BOARD OF REGENTS OF THE UNIVERSITY OF TEXAS SYSTEM
    Inventors: Antonella Casola, Olivier Escaffre, Alexander N. Freiberg, Roberto P. Garofalo
  • Publication number: 20150004158
    Abstract: The present invention relates to compositions, kits, and methods for detecting, characterizing, preventing, and treating cancer (e.g., hematological malignancies in humans). A variety of biomarker chromosomal number alterations (CNAs) and biomarkers corresponding thereto, are provided, wherein alterations in the copy number of one or more of the biomarker CNAs and/or alterations in the amount, structure, and/or activity of one or more of the biomarkers comprised within the CNAs is associated with cancer status.
    Type: Application
    Filed: February 28, 2013
    Publication date: January 1, 2015
    Inventors: Margaret A. Shipp, Stefano Monti, Bjoern Chapuy, Scott J. Rodig, Todd R. Golub
  • Publication number: 20140357599
    Abstract: The present application discloses compounds of formula (I) wherein X is ?O, ?S, ?NH, ?NOH and ?NO-Me; A is —C(?O)—, —S(?O)2—, —C(?S)— and P(?O)(R5)—; B is, —O—, —(CH2)3-6—, and O—(CH2)2-5—; D is, —O—, —CR7R8— and —NR9; m is 0-12, n is 0-12, m+n is 1-20; p is 0-4; R1 is opt.sub. heteroaryl; and pharmaceutically acceptable salts thereof, and prodrugs thereof. The application also discloses the compound for use as a medicament for the treatment of a disease or a condition caused by an elevated level of nicotinamide phosphoribosyltransferase (NAMPRT), e.g. inflammatory and tissue repair disorders; dermatosis; autoimmune diseases, Alzheimers disease, stroke, athersclerosis, restenosis, diabetes, glomerulonephritis, cancer, cachexia, inflammation associated with infection and certain viral infections, including Acquired Immune Deficiency Syndrome (AIDS), adult respiratory distress syndrome, ataxia telengiectasia.
    Type: Application
    Filed: August 18, 2014
    Publication date: December 4, 2014
    Inventors: Mette Knak CHRISTENSEN, Fredrik BJORKLING
  • Patent number: 8871747
    Abstract: The present application discloses compounds of formula (I) wherein X is ?O, ?S, ?NH, ?NOH and ?NO-Me; A is —C(?O)—, —S(?O)2—, —C(?S)— and P(?O)(R5)—; B is, —O—, —(CH2)3-6—, and O—(CH2)2-5—; D is, —O—, —CR7R8— and —NR9; m is 0-12, n is 0-12, m+n is 1-20; p is 0-4; R1 is opt. sub. heteroaryl; and pharmaceutically acceptable salts thereof, and prodrugs thereof. The application also discloses the compound for use as a medicament for the treatment of a disease or a condition caused by an elevated level of nicotinamide phosphoribosyltransferase (NAMPRT), e.g. inflammatory and tissue repair disorders; dermatosis; autoimmune diseases, Alzheimer's disease, stroke, athersclerosis, restenosis, diabetes, glomerulonephritis, cancer, cachexia, inflammation associated with infection and certain viral infections, including Acquired Immune Deficiency Syndrome (AIDS), adult respiratory distress syndrome, ataxia telengiectasia.
    Type: Grant
    Filed: August 31, 2009
    Date of Patent: October 28, 2014
    Assignee: Topotarget A/S
    Inventors: Mette Knak Christensen, Fredrik Bjorkling
  • Patent number: 8865684
    Abstract: The invention is directed to a method of administering hydrogen sulfide (H2S) slowly and sustainably to an individual in need thereof comprising administering an effective amount of a compound represented by the following structural formula: or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: August 15, 2013
    Date of Patent: October 21, 2014
    Assignee: National University of Singapore
    Inventors: Philip Keith Moore, Choon-Hong Tan, Ling Li, Yan Yi Guan
  • Publication number: 20140296186
    Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.
    Type: Application
    Filed: May 23, 2014
    Publication date: October 2, 2014
    Inventors: Weiwen Ying, Lijun Sun, Keizo Koya, Dinesh U. Chimmanamada, Shijie Zhang, Teresa Kowalcyzk-Przewloka, Hao Li
  • Patent number: 8822435
    Abstract: Novel bisphosphonate cyclic acetal compounds are disclosed, as well as methods of preparing the compounds, pharmaceutical compositions including the compounds, and administration of the compounds in methods of treating bone metabolism disorders, such as abnormal calcium and phosphate metabolism.
    Type: Grant
    Filed: March 12, 2014
    Date of Patent: September 2, 2014
    Assignee: Warner Chilcott Company, LLC
    Inventors: Frank Hallock Ebetino, Adam Wieslaw Mazur, Roy Lee Martin Dobson
  • Publication number: 20140221316
    Abstract: This disclosure relates to novel compounds containing an H2S releasing moiety and a nitric oxide (NO) releasing moiety covalently linked with a core (e.g., a salicylic acid moiety) and the use of such compounds in treating inflammatory diseases, including cancers. Therapeutic potency of these compounds is significantly higher than NSAIDs containing a H2S-releasing moiety alone (HS-NSAIDs) and NSAID containing a NO-releasing moiety alone (NO-NSAIDs). The compounds, in addition, exhibit reduced side effect, e.g., reduced stomach ulcers, upon administration.
    Type: Application
    Filed: August 15, 2012
    Publication date: August 7, 2014
    Applicant: RESEARCH FOUNDATION OF THE CITY UNIVERSITY OF NEW YORK
    Inventors: Khosrow Kashfi, Ravinder Kodela
  • Patent number: 8779128
    Abstract: Oligonucleotide analogues comprising modified intersubunit linkages and/or modified 3? and/or 5?-end groups are provided. The disclosed compounds are useful for the treatment of diseases where inhibition of protein expression or correction of aberrant mRNA splice products produces beneficial therapeutic effects.
    Type: Grant
    Filed: May 27, 2011
    Date of Patent: July 15, 2014
    Assignee: Sarepta Therapeutics, Inc.
    Inventors: Gunnar J. Hanson, Charles Rudolph, Bao Zhong Cai, Ming Zhou, Dwight D. Weller
  • Patent number: 8759324
    Abstract: The present invention provides a method of hydroxylating or oxidizing a compound of interest in a subject (e.g., a cytotoxic oxazaphosphorine prodrug), by administering the compound of interest to the subject; and concurrently administering the subject a metalloporphyrin in an amount effective to hydroxylate or oxidize the compound of interest in the subject.
    Type: Grant
    Filed: February 8, 2013
    Date of Patent: June 24, 2014
    Assignee: Duke University
    Inventors: Ivan Spasojevic, Michael O. Colvin, Ines Batinic-Haberle, Susan M. Ludeman, Michael P. Gamcsik
  • Patent number: 8673321
    Abstract: The present invention relates to methods of treating a cancer and in particular, a B-cell derived cancer, using a lymphocytotoxic but hematopoeitic cell sparing high-dose pulsed amount of an oxazaphosphorine drug in combination with immune therapeutics such as, for example, an autologous idiotypic vaccine and monoclonal antibodies that selectively bind B-cell specific antigens.
    Type: Grant
    Filed: September 12, 2011
    Date of Patent: March 18, 2014
    Assignees: The Johns Hopkins University, Accentia Biopharmaceuticals, Inc.
    Inventors: Robert A. Brodsky, Richard J. Jones, Francis E. O'Donnell, Jr., Susan Bonitz, Carlos Santos
  • Patent number: 8623844
    Abstract: The present invention generally relates to a process for the preparation of fosaprepitant dimeglumine intermediate and its use in the preparation of fosaprepitant dimeglumine; to a neutral form of fosaprepitant in a solid state and processes for the preparation thereof; and to a stable amorphous fosaprepitant dimeglumine, having a stability at temperatures of about 2° C. to about 8° C. and at a relative humidity below at least 60%; and a process for the preparation thereof.
    Type: Grant
    Filed: July 17, 2009
    Date of Patent: January 7, 2014
    Inventors: Navin Ganesh Bhatt, Nikhil Rasiklal Trivedi, Mahesh Khedekar, Sukumar Sinha, Mubeen Ahmed Khan, Ramjilal Yadav
  • Publication number: 20140005148
    Abstract: Described are stable liquid formulations of nitrogen mustards. The nitrogen mustard includes mechlorethamine, cyclophosphamide, ifosfamide, melphalan, chlorambucil, uramustine, thiotepa and combinations thereof. The formulation includes a non-aqueous liquid having at least a first solvent either individually or in combination with one or more additional solvents. The formulation further includes an antioxidant, an organic acid, and a source of chloride ions.
    Type: Application
    Filed: June 28, 2013
    Publication date: January 2, 2014
    Inventors: Sundar Neelakantan, Eric W. Smart, Charles Reichel
  • Publication number: 20130345161
    Abstract: The application describes methods for screening subjects with breast cancer to determine if the breast cancer will be responsive to a breast cancer therapy including a taxane or a taxane derivative. The application also describes methods for treating subjects with breast cancer by screening them for the likelihood of the effectiveness of treating the cancer with a therapy including a taxane or a taxane derivative and administering the therapy in subjects when it is found that a taxane or a taxane derivative is likely to be effective.
    Type: Application
    Filed: November 30, 2012
    Publication date: December 26, 2013
    Inventors: Charles M. Perou, Philip S. Bernard, Torsten O. Nielsen, Matthew J. Ellis, Joel S. Parker, Miguel Martin, Eva Carrasco, Rosalia Caballero
  • Publication number: 20130331360
    Abstract: The invention is directed to a method of administering hydrogen sulfide (H2S) slowly and sustainably to an individual in need thereof comprising administering an effective amount of a compound represented by the following structural formula: or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: August 15, 2013
    Publication date: December 12, 2013
    Applicant: National University of Singapore
    Inventors: Philip Keith Moore, Choon-Hong Tan, Ling Li, Yan Yi Guan
  • Publication number: 20130323300
    Abstract: The present invention is directed to compositions and methods for treating an animal diagnosed with Glioblastoma multiforme (GBM).
    Type: Application
    Filed: October 25, 2011
    Publication date: December 5, 2013
    Applicant: Regents of the University of Minnesota
    Inventor: Karen H. Ohlfest
  • Publication number: 20130310344
    Abstract: The present invention relates to compounds of Formula (I): and to their salts, pharmaceutical compositions, methods of use, and methods for their preparation. These compounds inhibit Bcl-2 and/or Bcl-XL activities and may be used for the treatment of cancer.
    Type: Application
    Filed: August 5, 2011
    Publication date: November 21, 2013
    Applicant: ASTRAZENECA AB
    Inventors: Robert Bruce Diebold, Thomas Gero, Paul Grover, Shan Huang, Stephanos Ioannidis, Claude Afona Ogoe, Jamal Carlos Saeh, Jeffrey Gilbert Varnes
  • Patent number: 8541396
    Abstract: The invention is directed to a method of administering hydrogen sulfide (H2S) slowly and sustainably to an individual in need thereof comprising administering an effective amount of a compound represented by the following structural formula: or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: April 24, 2009
    Date of Patent: September 24, 2013
    Assignee: National University of Singapore
    Inventors: Philip Keith Moore, Choon-Hong Tan, Ling Li, Yan Yi Guan
  • Patent number: 8518913
    Abstract: The present invention relates to novel phosphorous derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.
    Type: Grant
    Filed: December 9, 2011
    Date of Patent: August 27, 2013
    Assignee: Allergan, Inc.
    Inventors: Haiqing Yuan, Richard I. Beard, Xiaoxia Liu, John E. Donello, Veena Viswanath, Michael E. Garst
  • Publication number: 20130157983
    Abstract: Pharmaceutical compositions comprise a first compound of Formula I or a physiologically acceptable salt thereof, and a cyto-protective amount of a manganese chelate of N,N?-dipyridoxyl ethylenedianiine-N,N?-diacetic acid (MnPLED): wherein R1, R2, R3, R4 and X are defined in the specification.
    Type: Application
    Filed: February 16, 2013
    Publication date: June 20, 2013
    Applicant: PledPharma AB
    Inventor: PledPharma AB
  • Patent number: 8399434
    Abstract: The present invention provides a method of hydroxylating or oxidizing a compound of interest in a subject (e.g., a cytotoxic oxazaphosphorine prodrug), by administering the compound of interest to the subject; and concurrently administering the subject a metalloporphyrin in an amount effective to hydroxylate or oxidize the compound of interest in the subject.
    Type: Grant
    Filed: November 6, 2007
    Date of Patent: March 19, 2013
    Assignee: Duke University
    Inventors: Ivan Spasojevic, Michael O. Colvin, Ines Batinic-Haberle, Susan M. Ludeman, Michael P. Gamcsik
  • Patent number: 8362027
    Abstract: The present invention is to provide means to treat breast cancer and/or mastitis by topically administering a non-steroidal antiinflammatory analgetic agent and/or an anticancer agent and allowing them efficiently to arrive into the mammary gland. The present invention provides an iontophoretic preparation for treating breast cancer and/or mastitis which contains a non-steroidal antiinflammatory analgetic agent and/or an anticancer agent as an active ingredient and has a donor to be applied on a nipple part for topical administration of the active ingredient from the nipple part to the mammary gland by application of electric potential.
    Type: Grant
    Filed: August 8, 2011
    Date of Patent: January 29, 2013
    Assignees: Kowa Co., Ltd., Tokyo University of Science Educational Foundation Administrative Organization
    Inventors: Toshio Inagi, Makoto Kanebako, Hiroshi Terada, Kimiko Makino, Masakazu Toi
  • Publication number: 20120329712
    Abstract: This invention relates to methods of inducing differential stress resistance in a subject with cancer by starving the subject for a short term, administering a cell growth inhibitor to the subject, or reducing the caloric or glucose intake by the subject. The induced differential stress resistance results in improved resistance to cytotoxicity in normal cells, which, in turn, reduces cytotoxic side-effects due to chemotherapy, as well as improved effectiveness of chemotherapeutic agents.
    Type: Application
    Filed: June 5, 2012
    Publication date: December 27, 2012
    Applicant: University of Southern California
    Inventor: Valter Longo
  • Publication number: 20120321594
    Abstract: One aspect of the present invention relates to a method of controlling axon or dendrite development in a neuronal cell population. This method involves providing a neuronal cell population and contacting the neuronal cell population with a modulator of R-type Ca2+ channel expression or activity in controlling the neuronal cell population to induce either axon or dendrite development. Another aspect of the present invention relates to a method of treating neuronal injury in a subject. This method involves selecting a subject with neuronal injury mediated by R-type Ca2+ channel expression or activity and administering to the selected subject an inhibitor of R-type Ca2+ channel expression or activity to induce neuronal axon development under conditions effective to treat the neuronal injury in the subject. Yet another aspect of the present invention relates to a method of screening for agents that modulate R-type Ca2+ channel expression or activity.
    Type: Application
    Filed: May 7, 2012
    Publication date: December 20, 2012
    Applicant: NEW YORK UNIVERSITY
    Inventors: Kyonsoo HONG, Makoto NISHIYAMA, Kazunobu TOGASHI, Melanie J. von Schimmelmann
  • Publication number: 20120315320
    Abstract: Disclosed are methods of increasing the chemosensitivity of normal and/or chemoresistant tumor or cancer cells using thyroid hormone analogs and/or nanoparticulate or polymeric forms thereof. Also disclosed are methods of increasing radiosensitivity of normal and/or radioresistant tumor or cancer cells using thyroid hormone analogs and/or nanoparticulate or polymeric forms thereof.
    Type: Application
    Filed: January 6, 2012
    Publication date: December 13, 2012
    Inventors: Paul J. Davis, Shaker A. Mousa
  • Publication number: 20120316135
    Abstract: The invention features compounds, pharmaceutical compositions and methods for treating patients who have an EGFR-driven cancer of formula I: wherein the variables are as defined herein.
    Type: Application
    Filed: May 4, 2012
    Publication date: December 13, 2012
    Applicant: ARIAD Pharmaceuticals, Inc.
    Inventors: David C. Dalgarno, Wei-Sheng Huang, William C. Shakespeare, Yihan Wang, Xiaotian Zhu
  • Patent number: 8314081
    Abstract: Novel bisphosphonate cyclic acetal compounds are disclosed, as well as methods of preparing the compounds, pharmaceutical compositions including the compounds, and administration of the compounds in methods of treating bone metabolism disorders, such as abnormal calcium and phosphate metabolism.
    Type: Grant
    Filed: October 26, 2010
    Date of Patent: November 20, 2012
    Assignee: Warner Chilcott Company, LLC
    Inventors: Frank Hallock Ebetino, Adam Wieslaw Mazur, Roy Lee Martin Dobson
  • Publication number: 20120245128
    Abstract: The present disclosure in general relates to methods, systems, and apparatus for identifying modification of a medicinal compound exposed to a sample for use in determining which treatment to provide to a subject in need thereof.
    Type: Application
    Filed: March 26, 2012
    Publication date: September 27, 2012
    Applicant: The Board of Regents of the University of Texas System
    Inventors: Anthony M. Haag, Norbert K. Herzog, David W. Niesel
  • Publication number: 20120225062
    Abstract: The present invention provides compounds of Formula I: and related compounds as further described herein, and pharmaceutical compositions comprising these compounds. The invention further provides methods to use these compounds and compositions for treating disorders associated with undesired levels of Pim kinase activity, including cancers and autoimmune disorders.
    Type: Application
    Filed: March 2, 2012
    Publication date: September 6, 2012
    Inventors: Matthew Burger, Gisele Nishiguchi, Timothy D. Machajewski, Alice Rico, Robert Lowell Simmons, Aaron R. Smith, Victoriano Tamez, JR., Huw Tanner, Lifeng Wan
  • Publication number: 20120225847
    Abstract: The present application discloses novel squaric acid derivatives of the formula A: from —C(?O)—, —S(?O)2—, —C(?S)— and —P(?O)(R5)—; B: -, —O—, —NR6— and —C(?O)—NR6—; D: -, —O—, —CR7R8— and —NR9; m=0-12; n=0-12; m+n=1-20; p=0-2; R1: heteroaryl, aryl; R2: H, C1-12-alkyl, C3-12-cycloalkyl, —[CH2CH2O]1-10—(C1-6-alkyl), C1-12-alkenyl, aryl, heterocyclyl, heteroaryl; R3: C1-12-alkyl, C3-12-cycloalkyl, —[CH2CH2O]1-10—(C1-6-alkyl), C1-12-alkenyl, aryl, heterocyclyl, heteroaryl; or R2 and R3: N-containing heterocyclic/heteroaromatic ring; R4 and R4*: H, C1-12-alkyl, C1-12-alkenyl; and pharmaceutically acceptable salts and prodrugs thereof, and their use in the treatment of diseases/conditions caused by an elevated level of NAMPRT (inflammatory and tissue repair disorders, particularly rheumatoid arthritis, inflammatory bowel disease, asthma and CPOD, osteoarthritis, osteoporosis and fibrotic diseases; dermatosis; autoimmune diseases including systemic lupus erythematosis, multiple sclerosis, psoriatic arthritis, ankyl
    Type: Application
    Filed: June 24, 2009
    Publication date: September 6, 2012
    Inventors: Mette Knak Christensen, Fredrik Bjorkling
  • Publication number: 20120220552
    Abstract: The present disclosure relates to (thio)morpholine derivatives of the formula (I) wherein R1 is selected from cyano, (2-4C)alkynyl, (1-4C)alkyl, (3-6C)cycloalkyl, (4-6C)cycloalkenyl, (6-8C)bicycloalkyl, (8-10C)bicyclic group, each optionally substituted with (1-4C)alkyl, phenyl, biphenyl, naphthyl, each optionally substituted with one or more substituents independently selected from halogen, (1-4C)alkyl optionally substituted with one or more fluoro atoms, (2-4C)alkynyl, (1-4C)alkoxy optionally substituted with one or more fluoro atoms, amino, di(1-4C)alkylamino, —SO2-(1-4C)alkyl, —CO-(1-4C)alkyl, —CO—O-(1-4C)alkyl, —NH—CO-(1-4C)alkyl and (3-6C)cycloalkyl, phenyl substituted with phenoxy, benzyl, benzyloxy, phenylethyl or monocyclic heterocycle, each optionally substituted with (1-4C)alkyl, monocyclic heterocycle optionally substituted with halogen, (1-4C)alkyl or with phenyl optionally substituted with (1-4C)alkyl, and bicyclic heterocycle optionally substituted with (1-4C)alkyl; A is selected from —
    Type: Application
    Filed: August 27, 2010
    Publication date: August 30, 2012
    Inventors: Wouter I. Iwema Bakker, Hein K.A.C. Coolen, Axel Stoit, Harmen Mons, Eric Ronken, Elizabeth Van Der Kam, Jurjen Frankena
  • Publication number: 20120202776
    Abstract: The invention features compounds of the general formula (I) in which the variable groups are as defined herein, and to their preparation and use.
    Type: Application
    Filed: May 21, 2009
    Publication date: August 9, 2012
    Applicant: ARIAD Pharmaceuticals, Inc.
    Inventors: Yihan Wang, Wei-Sheng Huang, Shuangying Liu, William C. Shakespeare, R. Mathew Thomas, Jiwei Qi, Feng Li, Xiaotian Zhu, Anna Kohlmann, David C. Dalgarno, Jan Antoinette C. Romero, Dong Zou
  • Publication number: 20120157413
    Abstract: The present invention relates to novel phosphorous derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.
    Type: Application
    Filed: December 9, 2011
    Publication date: June 21, 2012
    Applicant: ALLERGAN, INC.
    Inventors: Haiqing Yuan, Richard I. Beard, Xiaoxia Liu, John E. Donello, Veena Viswanath, Michael E. Garst
  • Publication number: 20120149760
    Abstract: Provided herein are methods of treating lysosomal storage disease, for instance Pompe disease, through inhibition of autophagy. Optionally, treatment is administered as an adjunct to enzyme replacement therapy (ERT).
    Type: Application
    Filed: September 2, 2010
    Publication date: June 14, 2012
    Inventors: Nina N. Raben, Cynthia Schreiner, Rebecca Baum, Shoichi Takikita, Tao Xie, Paul H. Plotz
  • Publication number: 20120122819
    Abstract: The present invention includes novel compounds and pharmaceutically acceptable formulations of said compounds which exhibit antibiotic activity against microorganisms bearing a guanine riboswitch that controls the expression of the guaA gene, including organisms which are resistant to certain antibiotic families, and which are useful as antibacterial agents for treatment or prophylaxis of bacterial infections in animals or in humans, in particular but not limited to infections of the mammary gland, or their use as antiseptics, agents for sterilization or disinfection.
    Type: Application
    Filed: June 14, 2010
    Publication date: May 17, 2012
    Applicant: SOCPRA - SCIENCES ET GENIE S.E.C.
    Inventors: Jérôme Mulhbacher, Daniel Lafontaine, François Malouin, Marianne Allard, Eric Marsault
  • Publication number: 20120077782
    Abstract: The present invention provides a method of hydroxylating or oxidizing a compound of interest in a subject (e.g., a cytotoxic oxazaphosphorine prodrug), by administering the compound of interest to the subject; and concurrently administering the subject a metalloporphyrin in an amount effective to hydroxylate or oxidize the compound of interest in the subject.
    Type: Application
    Filed: November 6, 2007
    Publication date: March 29, 2012
    Applicant: DUKE UNIVERSITY
    Inventors: Ivan Spasojevic, Michael O. Colvin, Ines Batinic-Haberle, Susan M. Ludeman, Michael P. Gamcsik
  • Publication number: 20120053139
    Abstract: The present invention provides methods for improving the pharmacokinetics of protease inhibitors and protease inhibitor precursors and pharmaceutical composition comprising protease inhibitors or protease inhibitor precursors of formula I and a cytochrome P450 monooxigenase inhibitor; when the compound of formula I comprises an amino group, pharmaceutically acceptable ammonium salts thereof, wherein R1 may be, for example, (HO)2P(O)—, (NaO)2P(O)—, alkyl-CO— or cycloalkyl-CO—, wherein X may be, for example, F, Cl, and Br, and wherein R2 and R3 are as defined herein.
    Type: Application
    Filed: August 24, 2011
    Publication date: March 1, 2012
    Applicant: Ambrilia Biopharma Inc.
    Inventors: Jinzi Jason Wu, Brent Richard Stranix, Michael Ge, Guy Milot, Marco Petrella, Chandra J. Panchal
  • Patent number: 8124650
    Abstract: Antitumor combinations comprising a taxane and at least one epidophllotoxin for treating neoplastic diseases are described.
    Type: Grant
    Filed: December 30, 2003
    Date of Patent: February 28, 2012
    Assignee: Aventis Pharma S.A.
    Inventor: Marie-Christine Bissery
  • Publication number: 20120035136
    Abstract: The present invention provides antisense antiviral compounds, compositions, and methods of their use and production, mainly for inhibiting the replication of viruses of the Filoviridae family, including Ebola and Marburg viruses. The compounds, compositions, and methods also relate to the treatment of viral infections in mammals including primates by Ebola and Marburg viruses. The antisense antiviral compounds include phosphorodiamidate morpholino oligonucleotides (PMOplus) having a nuclease resistant backbone, about 15-40 nucleotide bases, at least two but typically no more than half piperazine-containing intersubunit linkages, and a targeting sequence that is targeted against the AUG start site region of Ebola virus VP35, Ebola virus VP24, Marburg virus VP24, or Marburg virus NP, including combinations and mixtures thereof.
    Type: Application
    Filed: August 9, 2010
    Publication date: February 9, 2012
    Applicant: AVI BIOPHARMA, INC.
    Inventors: Patrick L. Iversen, Dwight D. Weller
  • Patent number: 8101652
    Abstract: Antitumor combinations comprising a taxane and at least one antimetabolite for treating neoplastic diseases are described.
    Type: Grant
    Filed: December 30, 2003
    Date of Patent: January 24, 2012
    Assignee: Aventis Pharma S.A.
    Inventor: Marie-Christine Bissery
  • Publication number: 20120010172
    Abstract: The present application discloses compounds of formula (I) wherein X is ?O, ?S, ?NH, ?NOH and ?NO-Me; A is —C(?O)—, —S(?O)2—, —C(?S)— and P(?O)(R5)—; B is, —O—, —(CH2)3-6—, and O—(CH2)2-5—; D is, —O—, —CR7R8— and —NR9; m is 0-12, n is 0-12, m+n is 1-20; p is 0-4; R1 is opt.sub. heteroaryl; and pharmaceutically acceptable salts thereof, and prodrugs thereof. The application also discloses the compound for use as a medicament for the treatment of a disease or a condition caused by an elevated level of nicotinamide phosphoribosyltransferase (NAMPRT), e.g. inflammatory and tissue repair disorders; dermatosis; autoimmune diseases, Alzheimers disease, stroke, athersclerosis, restenosis, diabetes, glomerulonephritis, cancer, cachexia, inflammation associated with infection and certain viral infections, including Acquired Immune Deficiency Syndrome (AIDS), adult respiratory distress syndrome, ataxia telengiectasia.
    Type: Application
    Filed: August 31, 2009
    Publication date: January 12, 2012
    Applicant: McDERMOTT WILL & EMERY LLP
    Inventors: Mette Knak Christensen, Fredrik Bjorkling
  • Publication number: 20110288053
    Abstract: The invention is related to phosphorus substituted compounds with antiviral activity, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.
    Type: Application
    Filed: July 20, 2011
    Publication date: November 24, 2011
    Applicant: Gilead Sciences, Inc.
    Inventors: Constantine G. Boojamra, Carina Cannizzaro, James M. Chen, Xiaowu Chen, Aesop Cho, Lee S. Chong, Maria Fardis, Heolun Jin, Ralph F. Hirschmann, Alan X. Huang, Choung U. Kim, Thorsten Kirschberg, Christopher P. Lee, William A. Lee, Richard L. Mackman, David Y. Markevitch, David A. Oare, Vidya K. Prasad, Hyung-Jung Pyun, Adrian S. Ray, Rosemarie Sherlock, Sundaramoothi Swaninathan, William J. Watkins, Jenneifer Zhang
  • Patent number: 8034824
    Abstract: The present invention is to provide means to treat breast cancer and/or mastitis by topically administering a non-steroidal antiinflammatory analgetic agent and/or an anticancer agent and allowing them efficiently to arrive into the mammary gland. The present invention provides an iontophoretic preparation for treating breast cancer and/or mastitis which contains a non-steroidal antiinflammatory analgetic agent and/or an anticancer agent as an active ingredient and has a donor to be applied on a nipple part for topical administration of the active ingredient from the nipple part to the mammary gland by application of electric potential.
    Type: Grant
    Filed: October 11, 2006
    Date of Patent: October 11, 2011
    Assignees: Kowa Co., Ltd., Tokyo University of Science Educational Foundation Administrative Organization
    Inventors: Toshio Inagi, Makoto Kanebako, Hiroshi Terada, Kimiko Makino, Masakazu Toi
  • Patent number: 8008297
    Abstract: The present invention provides lysine based compounds of the formula; and when the compound of formula I comprises an amino group, pharmaceutically acceptable ammonium salts thereof, wherein R1 may be, for example, (HO)2P(O)—, (NaO)2P(O)—, alkyl-CO— or cycloalkyl-CO—, wherein X may be, for example, F, Cl, and Br, and wherein R2 and R3 are as defined herein.
    Type: Grant
    Filed: April 4, 2008
    Date of Patent: August 30, 2011
    Assignee: Ambrilia Biopharma Inc.
    Inventors: Brent Richard Stranix, Valerie Perron
  • Publication number: 20110206661
    Abstract: The present invention relates to new trimethoxyphenyl inhibitors of tyrosine kinase, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Application
    Filed: February 18, 2011
    Publication date: August 25, 2011
    Applicant: AUSPEX PHARMACEUTICALS, INC.
    Inventors: Chengzhi Zhang, Andreas Sommer