Ring Nitrogen In The Bicyclo Ring System Patents (Class 514/235.2)
  • Patent number: 10370333
    Abstract: Described herein are compounds that modulate the activity of TNAP. In some embodiments, the compounds described herein inhibit TNAP. In certain embodiments, the compounds described herein are useful in the treatment of conditions associated with hyper-mineralization.
    Type: Grant
    Filed: February 5, 2018
    Date of Patent: August 6, 2019
    Assignee: SANFORD-BURNHAM PREBYS MEDICAL DISCOVERY INSTITUTE
    Inventors: Anthony B. Pinkerton, Russell Dahl, Nicholas D. P. Cosford, Jose Luis Millan
  • Patent number: 10358443
    Abstract: The present invention relates to certain heteroaryl amide compounds, pharmaceutical compositions containing them, and methods of using them, including methods for preventing, reversing, slowing, or inhibiting protein aggregation, and methods of treating diseases that are associated with protein aggregation, including neurodegenerative diseases such as Parkinson's disease, Alzheimer's disease, Lewy body disease, Parkinson's disease with dementia, fronto-temporal dementia, Huntington's Disease, amyotrophic lateral sclerosis, and multiple system atrophy, and cancer and melanoma.
    Type: Grant
    Filed: August 1, 2017
    Date of Patent: July 23, 2019
    Assignee: UCB Biopharma SPRL
    Inventors: Wolfgang Wrasidlo, Emily M. Stocking
  • Patent number: 10343991
    Abstract: The present invention describes the C5,C6 Substituted and/or fused oxindole compounds useful as anti-cancer agents and process for preparation thereof. Particularly the present invention relates to C5,C6 Substituted and/or fused oxindole compounds of formula I.
    Type: Grant
    Filed: November 2, 2017
    Date of Patent: July 9, 2019
    Assignee: Council of Scientific & Industrial Research
    Inventors: Raji Reddy Chada, Srigiridhar Kotamraju, Santosh Karnewar, Nagendra Babu Bathini, Nagarsenkar Atulya, Anuradha Singampalli
  • Patent number: 10344026
    Abstract: Compounds and compositions are presented that inhibit K-Ras, and especially mutant K-Ras. Certain compounds preferentially or even selectively inhibit specific forms of mutant K-Ras, and particularly the G12D mutant form.
    Type: Grant
    Filed: January 18, 2018
    Date of Patent: July 9, 2019
    Assignee: NantBio, Inc.
    Inventors: Chunlin Tao, Laxman Nallan, David G. Ho, Qinwei Wang, Paul Weingarten, Anna B. Juncker-Jensen
  • Patent number: 10300073
    Abstract: Provided are methods for the combined use of cyclin-dependent kinase 9 (CDK9) inhibitors and bromodomain containing 4 (BRD4) inhibitors to reduce, inhibit and/or prevent cartilage degradation and systemic traumatic inflammation. A combination of CDK9 inhibitors and BRD4 inhibitors can be used to reduce, inhibit and/or prevent cartilage degradation and loss of cartilage viability during allograft storage. A combination of CDK9 inhibitors and BRD4 inhibitors can be used as a post-injury intervention treatment to reduce, inhibit and/or prevent the acute cellular responses that lead to future cartilage degradation and osteoarthritis.
    Type: Grant
    Filed: October 13, 2015
    Date of Patent: May 28, 2019
    Assignee: The Regents of the University of California
    Inventors: Dominik Haudenschild, Jasper Yik
  • Patent number: 10245270
    Abstract: 3-[(3-{[4-(4-morpholinylmethyl)-1H-pyrrol-2-yl]methylene}-2-oxo-2,3-dihydro-1H-indol-5-yl)methyl]-1,3-thiazolidine-2,4-dione methanesulphonate of formula (II): Medicinal products containing the same which are useful in treating cancer.
    Type: Grant
    Filed: September 4, 2018
    Date of Patent: April 2, 2019
    Assignee: LES LABORATOIRES SERVIER
    Inventors: Alexandre Le Flohic, Jérôme Guidotti, Philippe Letellier
  • Patent number: 10246457
    Abstract: The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula (I), or pharmaceutically acceptable salts thereof, wherein X1, X2, R1, R7, R8 and R9 are as herein described. The present invention also provides pharmaceutical compositions comprising these compounds and methods for their use in therapy. In particular, the present invention relates to the use of Btk inhibitor compounds of Formula (I) in the treatment of Btk mediated disorders.
    Type: Grant
    Filed: April 4, 2016
    Date of Patent: April 2, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Tony Siu, Michael D. Altman, Brian M. Andresen, Jian Liu, Joseph Kozlowski, Sobhana Babu Boga, Younong Yu, Rajan Anand, Jiaqiang Cai, Dahai Wang, Shilan Liu
  • Patent number: 10245266
    Abstract: Provided herein are methods of using compounds and compositions for treating, managing, and/or preventing systemic lupus erythematosus (SLE). Pharmaceutical compositions and dosing regimens for use in the methods are also provided herein.
    Type: Grant
    Filed: May 18, 2015
    Date of Patent: April 2, 2019
    Assignee: Celgene Corporation
    Inventors: Peter H. Schafer, Lei Wu, Ying Ye
  • Patent number: 10220041
    Abstract: The present invention relates to methods of inducing the self-renewal of stem/progenitor supporting cells, including inducing the stem/progenitor cells to proliferate while maintaining, in the daughter cells, the capacity to differentiate into hair cells. Specifically, the invention relates to methods of using compounds comprising a 3-(pyridin-2-yl)-1H-indol-2-ol containing moiety having a Formula I: and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: April 10, 2018
    Date of Patent: March 5, 2019
    Assignee: Frequency Therapeutics, Inc.
    Inventors: Christopher Loose, Will McLean, Melissa Hill-Drzewi
  • Patent number: 10214502
    Abstract: This invention offers an effective method of decreasing expression of apolipoprotein E and increasing expression of at least one of either LDL-receptor protein or AbcA1 protein including selecting mammalian cells expressing apoE and at least one of either LDL-receptor protein or AbcA1 protein, contacting the mammalian cell with an effective amount of a compound having general formula (I) or general formula (II) in an amount sufficient to decrease expression of the apoE and increase expression of at least one of the LDL-receptor protein or the AbcA1 protein in the mammalian cell.
    Type: Grant
    Filed: October 4, 2016
    Date of Patent: February 26, 2019
    Assignees: Mayo Foundation for Medical Education and Research, California State University, Fresno
    Inventors: Santanu Maitra, Jungsu Kim
  • Patent number: 10201547
    Abstract: The invention comprises a method of treatment of aggression and similar behavioral syndromes, such as impulsivity and irritability, by a pharmaceutical agent exhibiting combined D2 and D5 antagonistic activity.
    Type: Grant
    Filed: July 26, 2018
    Date of Patent: February 12, 2019
    Assignee: Supernus Pharmaceuticals, Inc.
    Inventor: Christopher D. Breder
  • Patent number: 10155001
    Abstract: The invention relates to a Rac1 inhibitor for use as bronchodilator in a patient in need thereof. The invention provides a Rac1 inhibitor for use in a method for inducing bronchodilation in a patient in need thereof. The invention also relates to a Rac1 inhibitor for use in a method for reducing AHR in a patient in need thereof.
    Type: Grant
    Filed: June 13, 2014
    Date of Patent: December 18, 2018
    Assignees: INSERM (Institut National de la Sante et de la Recherche Medicale), Centre National de la Recherche Scientifique (CNRS), Universite de Nantes, Centre Hospitalier Universitaire de Nantes
    Inventors: Vincent Sauzeau, Gwennan Andre, Gervaise Loirand, Antoine Magnan, David Lair
  • Patent number: 10092567
    Abstract: The invention provides combinations comprising a) compound of formula I: or a pharmaceutically acceptable salt thereof wherein R1, R2, R5, R10, and A have any of the values defined in the specification; and b) one or more agents selected from 5-FU, a platinum agent, leucovorin, irinotecan, docetaxel, doxorubicin, gemcitabine, SN-38, capecitabine, temozolomide, paclitaxel, bevacizumab, pertuzumab, tamoxifen, rapamycin and lapatinib. The combinations are particularly useful for treating hyperproliferative disorders, such as cancer.
    Type: Grant
    Filed: February 21, 2017
    Date of Patent: October 9, 2018
    Assignee: GENENTECH, INC.
    Inventors: Kui Lin, Michelle Nannini, Elizabeth Punnoose, Deepak Sampath, Jeffrey Wallin, Premal Patel
  • Patent number: 10071089
    Abstract: The present invention is concerned with an oral pharmaceutical dosage form comprising oxycodone or a pharmaceutically acceptable salt thereof and naloxone or a pharmaceutically acceptable salt thereof for use in the treatment of pain in patients suffering from i) pain and at least one further disease ii), wherein said at least one further disease ii) results in intestinal dysbiosis, or for use in the treatment of pain in patients suffering from i) pain and at least one further disease iii), wherein said at least one further disease iii) increases the risk for intestinal bacterial translocation and thus for peritonitis, SIRS and/or sepsis.
    Type: Grant
    Filed: July 23, 2014
    Date of Patent: September 11, 2018
    Assignee: Euro-Celtique S.A.
    Inventors: Yvonne Von Coburg, Karen Reimer, Alexander Oksche, Peter Holzer
  • Patent number: 10058556
    Abstract: The invention comprises a method of treatment of aggression and similar behavioral syndromes, such as impulsivity and irritability, by a pharmaceutical agent exhibiting combined D2 and D5 antagonistic activity.
    Type: Grant
    Filed: October 12, 2017
    Date of Patent: August 28, 2018
    Assignee: SUPERNUS PHARMACEUTICALS, INC.
    Inventor: Christopher D. Breder
  • Patent number: 9968615
    Abstract: The present invention relates to methods of inducing the self-renewal of stem/progenitor supporting cells, including inducing the stem/progenitor cells to proliferate while maintaining, in the daughter cells, the capacity to differentiate into hair cells. Specifically, the invention relates to methods of using compounds comprising a 3-(pyridin-2-yl)-1H-indol-2-ol containing moiety having a Formula I: and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: March 2, 2017
    Date of Patent: May 15, 2018
    Assignee: Frequency Therapeutics, Inc.
    Inventors: Christopher Loose, Will McLean, Melissa Hill-Drzewi
  • Patent number: 9956202
    Abstract: The present invention relates to novel use of indolyl and indolinyl hydroxamates. Particularly, the invention relates to use of indolyl and indolinyl hydroxamates in the manufacturing a medicament or a pharmaceutical composition for treating a ischemic and hemorrhagic stroke, spinal cord injury, cranial nerve injury, peripheral nerve injury and a neurodegenerative disorder or cognitive deficit.
    Type: Grant
    Filed: November 24, 2014
    Date of Patent: May 1, 2018
    Assignee: Taipei Medical University
    Inventor: Kuo Sheng Hung
  • Patent number: 9925195
    Abstract: 3-[3-{[4-(4-morpholinylmethyl)-1H-pyrrol-2-yl]methylene}-2-oxo-2,3-dihydro-1H-indol-5-yl)methyl]-1,3-thiazolidine-2,4-dione methanesulphonate of formula (II): Medicinal products containing the same which are useful in treating cancer.
    Type: Grant
    Filed: July 11, 2014
    Date of Patent: March 27, 2018
    Assignee: LES LABORATOIRES SERVIER
    Inventors: Alexandre Le Flohic, Jérôme Guidotti, Philippe Letellier
  • Patent number: 9884826
    Abstract: Described herein are compounds that modulate the activity of TNAP. In some embodiments, the compounds described herein inhibit TNAP. In certain embodiments, the compounds described herein are useful in the treatment of conditions associated with hyper-mineralization.
    Type: Grant
    Filed: August 19, 2016
    Date of Patent: February 6, 2018
    Assignee: SANFORD-BURNHAM MEDICAL RESEARCH INSTITUTE
    Inventors: Anthony B. Pinkerton, Russell Dahl, Nicholas D. P. Cosford, Jose Luis Millan
  • Patent number: 9884062
    Abstract: Salts and solid forms of 3-(4-((4-(morpholinomethyl)benzyl)oxy)-1-oxoisoindolin-2-yl)piperidine-2,6-dione, or a stereoisomer thereof, are disclosed. Compositions comprising and methods of using the salts and solid forms are also disclosed.
    Type: Grant
    Filed: February 28, 2017
    Date of Patent: February 6, 2018
    Assignee: Celgene Corporation
    Inventors: Benjamin M. Cohen, John F. Traverse, Jean Xu, Ying Li
  • Patent number: 9878993
    Abstract: The present invention relates to compounds useful as inhibitors of DNA-PK. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
    Type: Grant
    Filed: May 19, 2016
    Date of Patent: January 30, 2018
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Paul S. Charifson, Kevin Michael Cottrell, Hongbo Deng, John P. Duffy, Huai Gao, Simon Giroux, Jeremy Green, Katrina Lee Jackson, Joseph M. Kennedy, David J. Lauffer, Mark Willem Ledeboer, Pan Li, John Patrick Maxwell, Mark A. Morris, Albert Charles Pierce, Nathan D. Waal, Jinwang Xu
  • Patent number: 9801887
    Abstract: The invention comprises a method of treatment of aggression and similar behavioral syndromes, such as impulsivity and irritability, by a pharmaceutical agent exhibiting combined D2 and D5 antagonistic activity.
    Type: Grant
    Filed: July 26, 2013
    Date of Patent: October 31, 2017
    Assignee: Supernus Pharmaceuticals, Inc.
    Inventor: Christopher D. Breder
  • Patent number: 9790180
    Abstract: Provided herein are compounds, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat diseases or disorders associated with HDAC1 and/or HDAC2 activity.
    Type: Grant
    Filed: December 11, 2015
    Date of Patent: October 17, 2017
    Assignee: REGENACY PHARMACEUTICALS, LLC
    Inventors: John H. van Duzer, Ralph Mazitschek
  • Patent number: 9765056
    Abstract: Compounds of formula (I): wherein Ra, Rb, Rc, Rd, R3, R4, R5, A1, A2, T and W are as defined in the description. Medicinal products containing the same which are useful in treating pathologies involving a deficit in apoptosis, such as cancer, auto-immune diseases, and diseases of the immune system.
    Type: Grant
    Filed: July 22, 2014
    Date of Patent: September 19, 2017
    Assignees: LES LABORATOIRES SERVIER, VERNALIS (R&D) LTD
    Inventors: Patrick Casara, Thierry Le Diguarher, Jean-Michel Henlin, Jéröme-Benoit Starck, Arnaud Le Tiran, Guillaume De Nanteuil, Olivier Geneste, James Edward Paul Davidson, James Brooke Murray, I-Jen Chen, Claire Walmsley, Christopher John Graham, Stuart Ray, Daniel Maddox, Simon Bedford
  • Patent number: 9737585
    Abstract: Pre-implantation factor (PIF) may be used to treat intracellular damage. Aspects of the invention are directed to a method of treating intracellular damage comprising administering PIF to a subject in need thereof. Some aspects may be directed to methods of increasing cytokine secretion in response to intracellular damage comprising administering PIF to a subject in need thereof. The intracellular damage may be a result of a disease such as Listeria monocytogenes infection, malaria, Lyme disease, cardiovascular disease, duodenal peptic ulcer, atherosclerosis, peritonitis or tuberculosis. In some aspects, a method of treating tuberculosis is disclosed, comprising administering PIF to a subject in need thereof. In some aspects, a method of treating atherosclerosis is disclosed, comprising administering PIF to a subject in need thereof. In some aspects, a method of treating peritonitis is disclosed, comprising administering PIF to a subject in need thereof.
    Type: Grant
    Filed: March 2, 2012
    Date of Patent: August 22, 2017
    Inventor: Eytan R. Barnea
  • Patent number: 9738635
    Abstract: The present invention relates to certain heteroaryl amide compounds, pharmaceutical compositions containing them, and methods of using them, including methods for preventing, reversing, slowing, or inhibiting protein aggregation, and methods of treating diseases that are associated with protein aggregation, including neurodegenerative diseases such as Parkinson's disease, Alzheimer's disease, Lewy body disease, Parkinson's disease with dementia, fronto-temporal dementia, Huntington's Disease, amyotrophic lateral sclerosis, and multiple system atrophy, and cancer and melanoma.
    Type: Grant
    Filed: December 29, 2015
    Date of Patent: August 22, 2017
    Assignee: NEUROPORE THERAPIES, INC.
    Inventors: Wolfgang Wrasidlo, Emily M. Stocking
  • Patent number: 9724381
    Abstract: The invention provides methods for treatment, prevention or management of obesity, obesity related disorders, diabetes mellitus, and metabolic syndrome in a subject by administering a ghrelin O-acyltransferase (GOAT) inhibitor and/or a ghrelin receptor antagonist to the subject. The invention also provides ghrelin receptor antagonists of formula (VII): A11-A12-A13-Gly-Ser-A14-Phe-Leu-A15-A16-A17-A18, wherein each of A11, A12, and A13 is independently absent, an amino acid, or an amino protecting group; each of A15, A16, A17, and A18 is independently absent or an amino acid; and A14 is a serine conjugated with a —C(O)C1-C20alky or a diaminopropionic acid conjugated with a —C(O)C1-C20alkyl group, provided that at least one of A11, A12, or A13 is present.
    Type: Grant
    Filed: October 2, 2014
    Date of Patent: August 8, 2017
    Assignees: THE ADMINISTRATORS OF THE TULANE EDUCATIONAL FUND, MCGILL UNIVERSITY
    Inventors: Cyril Y. Bowers, David H. Coy, Gloria S. Tannenbaum
  • Patent number: 9682082
    Abstract: The invention provides combinations comprising a) compound of formula I: (formula I), or a pharmaceutically acceptable salt thereof; and another agent selected from GDC-0973, PD-0325901, or a pharmaceutically acceptable salt thereof. The combinations are particularly useful for treating hyperproliferative disorders, such as cancer.
    Type: Grant
    Filed: March 30, 2012
    Date of Patent: June 20, 2017
    Assignee: GENENTECH, INC.
    Inventors: Brian Lee, Kui Lin, Michelle Nannini, Elizabeth Punnoose, Deepak Sampath
  • Patent number: 9650375
    Abstract: Novel compounds of the structural formula (I) are activators of AMP-protein kinase and may be useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention may be useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.
    Type: Grant
    Filed: March 10, 2014
    Date of Patent: May 16, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: John J. Acton, III, Rajan Anand, Ashok Arasappan, Qun Dang, Iyassu Sebhat, Zhifa Pu, Takao Suzuki
  • Patent number: 9629849
    Abstract: Salts and solid forms of 3-(4-((4-(morpholinomethyl)benzyl)oxy)-1-oxoisoindolin-2-yl)piperidine-2,6-dione, or a stereoisomer thereof, are disclosed. Compositions comprising and methods of using the salts and solid forms are also disclosed.
    Type: Grant
    Filed: November 18, 2015
    Date of Patent: April 25, 2017
    Assignee: Celgene Corporation
    Inventors: Benjamin M. Cohen, John F. Traverse, Jean Xu, Ying Li
  • Patent number: 9624225
    Abstract: The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating ROR?t activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.
    Type: Grant
    Filed: October 14, 2014
    Date of Patent: April 18, 2017
    Assignee: Janssen Pharmaceutica NV
    Inventors: Kristi A. Leonard, Kent Barbay, James P. Edwards, Kevin D. Kreutter, David A. Kummer, Umar Maharoof, Rachel Nishimura, Maud Urbanski, Hariharan Venkatesan, Aihua Wang, Ronald L. Wolin, Craig R. Woods, Xiaohua Xue, Maxwell D. Cummings, Kelly McClure, Virginia Tanis
  • Patent number: 9617244
    Abstract: The present invention relates to novel substituted quinoline derivatives according to the general Formula (Ia) or Formula (Ib): including any stereochemically isomeric form thereof, a pharmaceutically acceptable salt thereof, a N-oxide form thereof or a solvate thereof. The claimed compounds are useful for the treatment of a bacterial infection. Also claimed is a composition comprising a pharmaceutically acceptable carrier and, as active ingredient, a therapeutically effective amount of the claimed compounds, the use of the claimed compounds or compositions for the manufacture of a medicament for the treatment of a bacterial infection and a process for preparing the claimed compounds.
    Type: Grant
    Filed: April 26, 2013
    Date of Patent: April 11, 2017
    Assignee: Janssen Pharmaceutica NV
    Inventors: Jerome Emile Georges Guillemont, Magali Madeleine Simone Motte, David Francis Alain Lancois, Sebastein Robert Gaston Thomas, Wendy Mia Albert Balemans
  • Patent number: 9499531
    Abstract: The compounds of the present invention are represented by the chemical structure found in Formula (I): wherein: the carbon atom designated * is in the R or S configuration; and X is a fused bicyclic carbocycle or heterocycle selected from the group consisting of benzofuranyl, benzo[b]thiophenyl, benzoisothiazolyl, benzoisoxazolyl, indazolyl, indolyl, isoindolyl, indolizinyl, benzoimidazolyl, benzooxazolyl, benzothiazolyl, benzotriazolyl, imidazo[1,2-a]pyridinyl, pyrazolo[1,5-a]pyridinyl, [1,2,4]triazolo[4,3-a]pyridinyl, thieno[2,3-b]pyridinyl, thieno[3,2-b]pyridinyl, 1H-pyrrolo[2,3-b]pyridinyl, indenyl, indanyl, dihydrobenzocycloheptenyl, tetrahydrobenzocycloheptenyl, dihydrobenzothiophenyl, dihydrobenzofuranyl, indolinyl, naphthyl, tetrahydronaphthyl, quinolinyl, isoquinolinyl, 4H-quinolizinyl, 9aH-quinolizinyl, quinazolinyl, cinnolinyl, phthalazinyl, quinoxalinyl, benzo[1,2,3]triazinyl, benzo[1,2,4]triazinyl, 2H-chromenyl, 4H-chromenyl, and a fused bicyclic carbocycle or fused bicyclic heterocycle opti
    Type: Grant
    Filed: June 12, 2015
    Date of Patent: November 22, 2016
    Assignee: Albany Molecular Research, Inc.
    Inventors: Bruce F. Molino, Shuang Liu, Peter R. Guzzo, James P. Beck
  • Patent number: 9435006
    Abstract: The present invention extracts precious metals from an acidic solution containing precious metals in an early and highly efficient manner. Provided is an extraction agent for precious metals that is represented by the general formula below. In the formula, R1 and R2 each represent the same alkyl group or different alkyl groups, R3 represents a hydrogen atom or an alkyl group, and R4 represents a hydrogen atom or a discretionary group that is not an amino group and that bonds to ? carbon as an amino acid. By subjecting an acidic solution containing precious metals to solvent extraction using the extraction agent for precious metals, a plurality of precious metals can be recovered all at once from a solution containing a large amount of various impurities.
    Type: Grant
    Filed: April 8, 2014
    Date of Patent: September 6, 2016
    Assignees: Kyushu University, National University Corporation, SUMITOMO METAL MINING CO., LTD.
    Inventors: Masahiro Goto, Fukiko Kubota, Yuzo Baba
  • Patent number: 9428439
    Abstract: The invention provides an acid addition salt of a compound of the formula (1). Also provided by the invention are processes for preparing the compound of formula (1) and alkyl analogs thereof, novel intermediates for use in the process and methods for preparing the intermediates. The invention also provides new medical uses of compounds of the formula (1) and its ethyl analog.
    Type: Grant
    Filed: January 7, 2014
    Date of Patent: August 30, 2016
    Assignee: ASTEX THERAPEUTICS LTD.
    Inventors: Martyn Frederickson, John Francis Lyons, Neil Thomas Thompson, Mladen Vinkovic, Brian John Williams, Andrew James Woodhead, Alison Jo-Anne Woolford
  • Patent number: 9422243
    Abstract: There are provided substituted 3-phenyl-isoquinolin-1(2H)-one derivatives which selectively inhibit the activity of poly(ADP-ribose) polymerase PARP-1 with respect to poly(ADP-ribose) polymerase PARP-2. The compounds of the present invention are therefore useful in treating diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds.
    Type: Grant
    Filed: November 20, 2012
    Date of Patent: August 23, 2016
    Assignee: NERVIANO MEDICAL SCIENCES S.R.L. a corporation
    Inventors: Gianluca Mariano Enrico Papeo, Alessandra Cirla, Matteo D'Anello, Alessandra Scolaro, Fabio Zuccotto
  • Patent number: 9376734
    Abstract: Provided are an extraction agent and extraction method that selectively extract and, at a low cost, recover indium from an acidic solution containing indium and zinc. The indium extraction agent comprises an amide derivative represented by general formula (I). In the formula, R1 and R2 each indicate the same or different alkyl group, R3 indicates a hydrogen atom or an alkyl group, and R4 indicates a hydrogen atom or any given group, other than an amino group, bound to the ?-carbon as an amino acid. The general formula preferably has a glycine unit, a histidine unit, a lysine unit, an aspartic acid unit, or an N-methylglycine unit. By extracting indium from an acidic solution containing indium and zinc by means of solvent extraction using the extraction agent, it is possible to selectively extract indium.
    Type: Grant
    Filed: April 26, 2013
    Date of Patent: June 28, 2016
    Assignees: Kyushu University, National University Corporation, SUMITOMO METAL MINING CO., LTD.
    Inventors: Masahiro Goto, Fukiko Kubota, Yuzo Baba
  • Patent number: 9371281
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of histone deacetylase 8 (HDAC8). Also described herein are methods of using such HDAC8 inhibitors, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of HDAC8 activity.
    Type: Grant
    Filed: October 29, 2014
    Date of Patent: June 21, 2016
    Assignee: Pharmacyclics LLC
    Inventors: Joseph J. Buggy, Sriram Balasubramanian, Erik Verner, Vincent W. F. Tai, Chang-Sun Lee
  • Patent number: 9326962
    Abstract: The present invention provides methods, compositions, and kits for treating intestinal hyperpermeability in a subject in need thereof, including conditions such as hyperglycemia and underlying diseases such as diabetes, autism, fibromyalgia, inflammatory bowel disease (IBD), graft versus host disease (GVHD), HIV/AIDS, multiple organ dysfunction syndrome, irritable bowel syndrome (IBS), celiac disease, eczema, psoriasis, acute pancreatitis, Parkinson's disease, depression, chronic fatigue syndrome, asthma, multiple sclerosis, arthritis, ankylosing spondylitis, nonalcoholic fatty liver disease, alcoholic cirrhosis, environmental enteropathy, or kwashiorkor.
    Type: Grant
    Filed: October 21, 2014
    Date of Patent: May 3, 2016
    Inventor: Steven Hoffman
  • Patent number: 9321756
    Abstract: The invention relates to bicyclic compounds of formulas I and Ia, and salts thereof. In some embodiments, the invention relates to inhibitors or modulators of Pim-1 and/or Pim-2, and/or Pim-3 protein kinase activity or enzyme function. In still further embodiments, the invention relates to pharmaceutical compositions comprising compounds disclosed herein, and their use in the prevention and treatment of Pim kinase related conditions and diseases, preferably cancer.
    Type: Grant
    Filed: March 21, 2012
    Date of Patent: April 26, 2016
    Assignee: AMGEN INC.
    Inventors: Hui-Ling Wang, Victor J. Cee, Bradley J. Herberich, Claire L. M. Jackson, Brian Alan Lanman, Thomas Nixey, Liping H. Pettus, Anthony B. Reed, Bin Wu, Ryan Wurz, Andrew Tasker
  • Patent number: 9271941
    Abstract: Disclosed are novel pharmaceutical compositions containing N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl-2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide dimethyl sulfoxide solvate, methods of using the compositions in therapy and processes for preparing the same.
    Type: Grant
    Filed: October 2, 2013
    Date of Patent: March 1, 2016
    Assignee: Novartis AG
    Inventors: Douglas J. DeMarini, Francisco Henriquez, Ngocdiep T. Le, Lihong Wang
  • Patent number: 9248196
    Abstract: New rebamipide complexes and new rebamipide cocrystals are disclosed, specifically a 1:1 rebamipide nicotinamide complex, a 1:1 rebamipide nicotinamide cocrystal, a 1:1 rebamipide 2,4-dihydroxybenzolc acid complex, and a 1:1 rebamipide 2,4-dihydroxybenzoic acid cocrystal. Pharmaceutical compositions containing a rebamipide complex or cocrystal of the invention and a pharmaceutically acceptable carrier and methods of treatment are also disclosed.
    Type: Grant
    Filed: February 24, 2012
    Date of Patent: February 2, 2016
    Assignee: NUFORMIX LIMITED
    Inventors: Joanne Holland, Daniel Gooding, Alan Chorlton
  • Patent number: 9206128
    Abstract: Agents for modulating methyl modifying enzymes, compositions and uses thereof are provided herein.
    Type: Grant
    Filed: November 19, 2012
    Date of Patent: December 8, 2015
    Assignee: Constellation Pharmaceuticals, Inc.
    Inventors: Brian K. Albrecht, James Edmund Audia, Andrew S. Cook, Alexandre Gagnon, Jean-Christophe Harmange, Christopher G. Nasveschuk
  • Patent number: 9193686
    Abstract: The invention provides a process for the preparation of a carboxylic acid of formula (IV) (which is useful as a safener for herbicides): wherein R1 is hydrogen or chlorine, comprising the steps of: (i) subjecting a compound of formula (V) wherein: R1 is as defined above; and R2 is C1-C18 alkyl; C1-C6 alkoxyC1-C8 alkyl-; optionally substituted phenyl; or optionally substituted benzyl; to hydrolysis under acidic conditions to give a solution of a quinolinium salt; and (ii) adding base to the solution obtained in step (i) to give the free carboxylic acid (IV). The invention also provides a solid (e.g. particulate) form of one quinoline carboxylic acid compound within formula (IV) defined by R1 being chlorine; and novel intermediates useable in the above process.
    Type: Grant
    Filed: November 14, 2012
    Date of Patent: November 24, 2015
    Assignee: Syngenta Participations AG
    Inventors: Jean-Jacques Roger Gollut, Arnaud Jean Albert Gayet
  • Patent number: 9193707
    Abstract: Tetrahydroisoquinolin-2-yl-(quinazolin-4-yl)methanone derivatives represented by formula (I), pharmacologically acceptable salts thereof, and compositions containing such compounds are described. Methods for treating hyperproliferative disorders by administering the compounds are also described. 1,2,3,4-tetrahydroisoquinoline derivatives for making tetrahydroisoquinolin-2-yl-(quinazolin-4-yl)methanone compounds are also described.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: November 24, 2015
    Assignee: Rexahn Pharmaceuticals, Inc.
    Inventors: Young Bok Lee, Jae Min Kim, Deog Joong Kim, Chang-Ho Ahn
  • Patent number: 9162981
    Abstract: Compounds, compositions, kits and methods for treating conditions related to neurodegeneration or ocular disease, are disclosed.
    Type: Grant
    Filed: March 23, 2011
    Date of Patent: October 20, 2015
    Assignee: THE JOHNS HOPKINS UNIVERSITY
    Inventors: Donald J. Zack, Thomas Bannister, Tomas Vojkovsky, Zhiyong Yang, Cynthia Berlinicke
  • Patent number: 9133162
    Abstract: The present invention provides novel substituted quinoline compounds, pharmaceutical acceptable salts and formulations thereof useful in modulating the protein tyrosine kinase activity, and in modulating cellular activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.
    Type: Grant
    Filed: February 21, 2012
    Date of Patent: September 15, 2015
    Assignees: SUNSHINE LAKE PHARMA CO., LTD., CALITOR SCIENCES, LLC
    Inventor: Ning Xi
  • Patent number: 9108953
    Abstract: This application relates to chemical compounds which may act as inhibitors of, or which may otherwise modulate the activity of, a bromodomain-containing protein, including bromodomain-containing protein 4 (BRD4), and to compositions and formulations containing such compounds, and methods of using and making such compounds. Compounds include compounds of Formula I wherein R1, R2, R3, R4, R7, W, X, and Z are as described herein.
    Type: Grant
    Filed: November 21, 2014
    Date of Patent: August 18, 2015
    Assignee: Gilead Sciences, Inc.
    Inventors: Kerim Babaoglu, Britton K. Corkey, Robert H. Jiang, David Sperandio, Hai Yang
  • Patent number: 9085531
    Abstract: The compounds of the present invention are represented by the chemical structure found in Formula (I): wherein: the carbon atom designated * is in the R or S configuration; and X is a fused bicyclic carbocycle or heterocycle selected from the group consisting of benzofuranyl, benzo[b]thiophenyl, benzoisothiazolyl, benzoisoxazolyl, indazolyl, indolyl, isoindolyl, indolizinyl, benzoimidazolyl, benzooxazolyl, benzothiazolyl, benzotriazolyl, imidazo[1,2-a]pyridinyl, pyrazolo[1,5-a]pyridinyl, [1,2,4]triazolo[4,3-a]pyridinyl, thieno[2,3-b]pyridinyl, thieno[3,2-b]pyridinyl, 1H-pyrrolo[2,3-b]pyridinyl, indenyl, indanyl, dihydrobenzocycloheptenyl, tetrahydrobenzocycloheptenyl, dihydrobenzothiophenyl, dihydrobenzofuranyl, indolinyl, naphthyl, tetrahydronaphthyl, quinolinyl, isoquinolinyl, 4H-quinolizinyl, 9aH-quinolizinyl, quinazolinyl, cinnolinyl, phthalazinyl, quinoxalinyl, benzo[1,2,3]triazinyl, benzo[1,2,4]triazinyl, 2H-chromenyl, 4H-chromenyl, and a fused bicyclic carbocycle or fused bicyclic heterocycle optio
    Type: Grant
    Filed: May 2, 2014
    Date of Patent: July 21, 2015
    Assignees: Albany Molecular Research, Inc., Bristol-Myers Squibb Company
    Inventors: Bruce F. Molino, Shuang Liu, Peter R. Guzzo, James P. Beck
  • Publication number: 20150148344
    Abstract: This application relates to chemical compounds which may act as inhibitors of, or which may otherwise modulate the activity of, a bromodomain-containing protein, including bromodomain-containing protein 4 (BRD4), and to compositions and formulations containing such compounds, and methods of using and making such compounds. Compounds include compounds of Formula I wherein R1, R2, R3, R4, R7, W, X, and Z are as described herein.
    Type: Application
    Filed: November 21, 2014
    Publication date: May 28, 2015
    Inventors: Kerim Babaoglu, Britton K. Corkey, Robert H. Jiang, David Sperandio, Hai Yang