Patents Examined by Rebecca Anderson
  • Spiro-oxindole compounds and their use as therapeutic agents
    Patent number: 9458178
    Abstract: This invention is directed to spiro-oxindole compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.
    Type: Grant
    Filed: November 14, 2014
    Date of Patent: October 4, 2016
    Assignee: Xenon Pharmaceuticals Inc.
    Inventors: Mikhail Chafeev, Sultan Chowdhury, Lauren Fraser, Jianmin Fu, Jonathan Langille, Shifeng Liu, Jianyu Sun, Shaoyi Sun, Serguei Sviridov, Mark Wood, Alla Yurevna Zenova, Qi Jia, Jean-Jacques Alexandre Cadieux, Simon J. Gauthier, Amy Frances Douglas, Tom Hsieh, Nagasree Chakka, Zoran Cikojevic
  • Heterocyclic derivatives
    Patent number: 9458163
    Abstract: The invention relates to novel heterocyclic compounds of the formula in which all of the variables are as defined in the specification, to their preparation, to their medical use, in particular to their use in the treatment of cancer and neurodegenerative disorders, and to medicaments comprising them.
    Type: Grant
    Filed: March 11, 2015
    Date of Patent: October 4, 2016
    Assignee: Novartis AG
    Inventors: Branko Radetich, Bing Yu, Yanyi Zhu
  • Manufacturing process for pyrimidine derivatives
    Patent number: 9452994
    Abstract: The invention relates to processes for manufacturing a compound of formula 5, or a stereoisomer, tautomer or a salt thereof, wherein the substituents are as defined in the specification. The invention further relates to new manufacturing processes for specific solid forms of Compound A and its salts, to such solid forms and to use of such solid forms for the therapeutic treatment of warm-blooded animals.
    Type: Grant
    Filed: May 6, 2016
    Date of Patent: September 27, 2016
    Assignee: Novartis AG
    Inventors: Dietmar Flubacher, Pascal Michel, Maria Caterina Testa, Rasmus Mose
  • Method for decarboxylation of amino acids via imine formation
    Patent number: 9452954
    Abstract: The present application provides methods for decarboxylation of amino acids via imine formation with a catalyst under pressurized and superheated conditions in either a microwave or oil bath.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: September 27, 2016
    Inventors: Richard W. Morrison, Douglas Michael Jackson
  • Solid forms of curcumin
    Patent number: 9447050
    Abstract: The present invention provides forms of curcumin and the pharmaceutical compositions thereof. The forms of curcumin disclosed herein are curcumin polymorph Form III, curcumin-2-aminobenzimidazole co-crystal, and curcumin-L-lysine co-crystal. Further, the invention provides methods inhibiting cancer cells and HSV-1 using these curcumin novel solid forms.
    Type: Grant
    Filed: April 5, 2012
    Date of Patent: September 20, 2016
    Assignees: THE TRANSLATIONAL GENOMICS RESEARCH INSTITUTE, VAN ANDEL RESEARCH INSTITUTE
    Inventors: Stephen T. Gately, Steven J. Triezenberg, Tong Wang
  • Inauhzin analogues that induce P53, inhibit cell growth, and have antitumor activity
    Patent number: 9447103
    Abstract: Inauhzin (INZ) was identified as a novel p53 activator, which selectively and efficiently suppressing tumor growth without displaying genotoxicity and with little toxicity to normal cells. A panel of INZ analogs were synthesized and evaluated their ability to induce cellular p53 and to inhibit cell growth in cell-based assays. As described, this leads to the discovery of INZ analog 37, a molecule that exhibits much better potency than INZ in both of p53 activation and cell growth inhibition in several human cancer cell lines including H460 and HCT116+/+ cells. This INZ analog exhibited a much lower effect on p53-null H1299 cells and importantly no toxicity towards normal human p53-containing WI-38 cells. Those results also reveal key chemical features for INZ activity, and identify the newly synthesized INZ analog 37 as a better small molecule for further development of anti-cancer therapies.
    Type: Grant
    Filed: July 27, 2013
    Date of Patent: September 20, 2016
    Assignee: Indiana University Research & Technology Corporation
    Inventors: Hau Lu, Shelya Zeng, Qi Zhang, Qizhuang Ye, Derong Ding
  • Imidazopyridine compounds
    Patent number: 9447090
    Abstract: An excellent drug for treating or preventing cardiovascular diseases, based on cGMP production enhancing action due to soluble guanylate cyclase activating action, is provided. It was found that imidazopyridine compounds having a carbamoyl group at the 3-position and a substituent bonded at the 8-position via an oxygen atom in an imidazo[1,2-a]pyridine skeleton exhibits a cGMP production enhancing action by a potent soluble guanylate cyclase activating action, and is useful as a drug for treating or preventing various soluble guanylate cyclase-related cardiovascular diseases, thereby completing the present invention.
    Type: Grant
    Filed: November 26, 2013
    Date of Patent: September 20, 2016
    Assignee: Astellas Pharma Inc.
    Inventors: Yuji Koga, Kyoichi Maeno, Ippei Sato, Yoshimasa Imamura, Takeshi Hanazawa, Maiko Iida, Kazuhiko Ohne, Kenichiro Imamura, Tsubasa Watanabe, Eisuke Nozawa, Hiroshi Shibata
  • Substituted 2,3-dihydro-1H-inden-1-one retinoic acid-related orphan nuclear receptor antagonists for treating multiple sclerosis
    Patent number: 9446047
    Abstract: The present invention is directed to compounds, their synthesis, and their use as antagonists, inverse agonists, modulators and or inhibitors of the Retinoic acid-related orphan nuclear receptor ?t (ROR?t)/ROR?. The compounds of the present invention are useful for modulating ROR?t)/ROR? activity and for treating diseases or conditions mediated by ROR?t)/ROR? such as for example, disease states associated with immunopathology of human autoimmune diseases such as Multiple Sclerosis (MS), Rheumatoid Arthritis (RA), Inflammatory Colitis, Psoriasis, COPD, Pain, Obesity, Diabetes, Dyslipidemia, Osteoporosis, Asthma, Neurodegenerative diseases and Cancer.
    Type: Grant
    Filed: March 31, 2016
    Date of Patent: September 20, 2016
    Assignee: Arrien Pharmaceuticals LLC
    Inventors: Hariprasad Vankayalapati, Venkatakrishnareddy Yerramreddy
  • Triazolone compounds as mPGES-1 inhibitors
    Patent number: 9439890
    Abstract: The present disclosure is directed to compounds of formula (I), and pharmaceutically acceptable salts thereof, as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases.
    Type: Grant
    Filed: June 19, 2015
    Date of Patent: September 13, 2016
    Assignee: GLENMARK PHARMACEUTICALS S.A.
    Inventors: Laxmikant A. Gharat, Nagarajan Muthukaman, Neelima Khairatkar-Joshi, Vidya G. Kattige
  • Process for the synthesis of benzothiadiazole compounds
    Patent number: 9440965
    Abstract: The invention relates to a significantly improved process for the preparation of benzothiadxazole compounds which can be used in the production of Luminescent Solar Concentrators, (LSC). In particular, the synthesis process of the present invention is oriented towards the preparation of 4,-di-2-thienyl-2,1,3-benzo-thiadiazole.
    Type: Grant
    Filed: July 13, 2011
    Date of Patent: September 13, 2016
    Assignee: ENI S.P.A.
    Inventors: Samuele Santarelli, Marco Ricci, Roberto Fusco
  • Form-III crystal of 2-{4-[N-(5,6-diphenylpyrazin-2-yl)-N-isopropylamino]butyloxy}-N-(methylsulfonyl)acetamide and use thereof
    Patent number: 9440931
    Abstract: Form-III crystal of 2-{4-[N-(5,6-diphenylpyrazin-2-yl)-N-isopropylamino]butyloxy}-N-(methylsulfonyl)acetamide and a method of producing the crystal are provided. The Form-III crystal exhibits diffraction peaks in its X-ray powder diffraction spectrum at least at the following angles of diffraction 2? when the spectrum is obtained by using Cu K? radiation: 9.3 degrees, 9.7 degrees, 16.8 degrees, 20.6 degrees, and 23.5 degrees. The Form-III crystal can be produced by crystallizing the subject compound from an ester solvent or an aromatic hydrocarbon solvent. The crystal may be administered as an active ingredient to a subject for the purpose of treating or preventing certain diseases, disorders, and symptoms, or for promoting angiogenesis or gene therapy.
    Type: Grant
    Filed: June 9, 2015
    Date of Patent: September 13, 2016
    Assignee: NIPPON SHINYAKU CO., LTD.
    Inventors: Koji Nakamichi, Takashi Tosaka
  • Acrylamide compounds and use thereof for inhibiting apoptosis
    Patent number: 9439881
    Abstract: The present invention relates to a compound of Formula I, or an isomer, pharmaceutically acceptable salt and solvate of the compound, and to a composition comprising the compound of Formula I, or the isomer, pharmaceutically acceptable salt and solvate thereof, and a pharmaceutically acceptable carrier, excipient or diluents. The present invention also relates to use of the compound of Formula I, or the isomer, pharmaceutically acceptable salt and solvate thereof for combating apoptosis, preventing or treating a disease or disorder associated with apoptosis; and especially use for protecting cardiomyocyte, and for preventing or treating a disease or disorder associated with cardiomyocyte apoptosis.
    Type: Grant
    Filed: October 26, 2015
    Date of Patent: September 13, 2016
    Assignee: CHINESE PLA GENERAL HOSPITAL
    Inventors: Kunlun He, Song Li, Wu Zhong, Juan Liu, Lili Wang, Xin Li, Guoliang Hu, Jie Wang, Long Long, Junhai Xiao, Zhibing Zheng, Wei Li, Ruijun Li, Chunlei Liu, Jie Tang
  • Compounds inhibiting leucine-rich repeat kinase enzyme activity
    Patent number: 9440952
    Abstract: The present invention is directed to indazole compounds which are potent inhibitors of LRRK2 kinase and useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which LRRK-2 kinase is involved.
    Type: Grant
    Filed: February 27, 2014
    Date of Patent: September 13, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michael Miller, Kallol Basu, Duane DeMong, Jack Scott, Hong Liu, Xing Dai, Joel M. Harris, Bernard Neustadt, Andrew Stamford, Marc Poirier, John A. McCauley, Thomas Greshock, Heather Stevenson, John Sanders, Jonathan Kern
  • Sulfide scavengers, methods for making and methods for using
    Patent number: 9440909
    Abstract: Methods for making sulfide scavenging compositions are provided. The method comprises reacting at least one secondary amine with at least one aldehyde and solvent in the presence of a catalyst to form a reaction composition, wherein a reaction temperature is less than or equal to 90° C. Sulfide scavengers using the above method are also disclosed. Methods for removing sulfides from fluid streams are also provided. The methods include adding the above sulfide scavengers to fluid streams.
    Type: Grant
    Filed: June 30, 2015
    Date of Patent: September 13, 2016
    Assignee: General Electric Company
    Inventor: Gregory Kaplan
  • Pyrrolo[2, 1-F] [1,2,4]triazine derivative and use thereof for treating tumors
    Patent number: 9440981
    Abstract: Disclosed are a pyrrolo[2,1-f][1,2,4]triazine derivative of Formula (I) and use thereof for treating tumors. The compound has remarkable antiproliferative activity for a variety of human tumor cell lines, and is useful for treating cancers, especially solid tumors such as gastric cancer, lung cancer, liver cancer, breast cancer, colon cancer, prostatic cancer, and oral cancer.
    Type: Grant
    Filed: May 17, 2013
    Date of Patent: September 13, 2016
    Assignee: PHARMABLOCK (NANJING) R&D CO. LTD
    Inventors: Xihan Wu, Minmin Yang, Qingning Shu, Chunrui Zhu
  • Substituted pyrazoloquinazolinones and pyrroloquinazolinones as allosteric modulators of group II metabotropic glutamate receptors
    Patent number: 9434734
    Abstract: The present invention relates to the pyrazoloquinazolinone and pyrroloquinazolinone derivatives of the general formula (I), as well as pharmaceutical compositions containing them, and their use in the treatment and/or prophylaxis of conditions associated with altered glutamatergic signalling and/or functions, and/or conditions which can be affected by alteration of glutamate level or signalling in mammals, in particular their use in the treatment and/or prophylaxis of acute and chronic neurological and/or psychiatric disorders.
    Type: Grant
    Filed: May 21, 2013
    Date of Patent: September 6, 2016
    Assignee: DOMAIN THERAPEUTICS
    Inventors: Stanislas Mayer, Stephan Schann
  • Modified creatine compounds
    Patent number: 9434753
    Abstract: The invention discloses creatine derivatives that are represented by Formula (I), Formula (II), and Formula (III); wherein Z is a functional group; Y is a mitochondrial targeting agent, a cationic ammonium group, or a polypeptide containing at least one positively charged amino acid residue; each R1 is independently hydrogen, alkyl, or a phosphate group; R2 a linker; R3 is a spacer group; R4 is hydrogen, alkyl, aryl, or heterocyclic; or R4 and R1, or R4 and R3, together with the nitrogen atoms to which they are attached form a heterocyclic ring, and W is hydrogen or alkyl.
    Type: Grant
    Filed: September 18, 2012
    Date of Patent: September 6, 2016
    Assignee: Gencia Corporation
    Inventors: Shaharyar M. Khan, Robert Gadwood, Arthur Glenn Romero
  • Cystine diamide analogs for the prevention of cystine stone formation in cystinuria
    Patent number: 9428453
    Abstract: Cystine analogs that improve the solubility of L-cystine in urine for treatment of cystinuria and which have the structure: and pharmaceutically acceptable salts, solvates and prodrugs thereof, wherein each R and R? pair are independently selected from (i) or (ii); (i) R and R? are independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alcohol, substituted or unsubstituted aryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocyclic, and substituted or unsubstituted heteroaryl, or (ii) R and R? together form a substituted or unsubstituted heterocyclic ring structure, or a substituted or unsubstituted heteroaryl ring structure; X is hydrogen, or an alkyl; and Y is O or S.
    Type: Grant
    Filed: January 2, 2014
    Date of Patent: August 30, 2016
    Assignee: RUTGERS, THE STATE UNIVERSITY OF NEW JERSEY
    Inventors: Longqin Hu, Amrik Sahota
  • Selectively substituted quinoline compounds
    Patent number: 9428495
    Abstract: Embodiments of the disclosure relate to selectively substituted quinoline compounds that act as antagonists or inhibitors for Toll-like receptors 7 and/or 8, and their use in pharmaceutical compositions effective for treatment of systemic lupus erythematosus (SLE) and lupus nephritis.
    Type: Grant
    Filed: October 14, 2014
    Date of Patent: August 30, 2016
    Assignee: EISAI R&D MANAGEMENT CO., LTD.
    Inventors: Eric Carlson, Hans Hansen, Lynn Hawkins, Sally Ishizaka, Matthew Mackey, Shawn Schiller, Chikako Ogawa, Heather Davis, Atsushi Endo
  • Triazolopyrazine
    Patent number: 9428513
    Abstract: The present invention encompasses compounds of general formula (I) wherein the groups R1 to R3, X3 to X6 have the meanings given in the claims and in the specification. The compounds of the invention are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation pharmaceutical preparations containing such compounds and their uses as a medicament.
    Type: Grant
    Filed: November 4, 2014
    Date of Patent: August 30, 2016
    Assignee: Boehringer Ingelheim International GmbH
    Inventor: Harald Engelhardt