Patents Examined by Golam M M Shameem
  • Xanthine derivative
    Patent number: 9255098
    Abstract: The present invention discloses a xanthine derivative having the structure of the following general formula (I) or a pharmaceutically acceptable salt thereof; further discloses a preparation method for the xanthine derivative or a pharmaceutically acceptable salt thereof; and further discloses the use of the xanthine derivative or a pharmaceutically acceptable salt thereof. Through experiments of DPP-IV activity inhibition experiments in vitro, impact on glucose tolerance in normal mice and impact on blood glucose in spontaneous diabetic mice, it proves that the compounds and pharmaceutically acceptable salts thereof show good DPP-IV inhibition activity, can be applied to prepare medicines for treating dipeptidyl peptidase IV-related diseases, and more particularly, can be applied to the use of medicines for treating type II diabetes or diseases of abnormal glucose tolerance.
    Type: Grant
    Filed: May 15, 2013
    Date of Patent: February 9, 2016
    Assignee: Chengdu Easton Pharmaceutical Co., Ltd.
    Inventors: Ying Wang, Yongzhe Xiang, Guodong Cen, Long Huang, Jian Liu, Ning Zhou, Jibing Zhang
  • Purifying crude furan 2,5-dicarboxylic acid by hydrogenation
    Patent number: 9249118
    Abstract: A process for purifying a crude furan 2,5-dicarboxylic acid composition (cFDCA) by hydrogenation of a FDCA composition dissolved in a hydrogenation solvent such as water, and hydrogenating under mild conditions, such as at a temperature within a range of 130° C. to 225° C. by contacting the solvated FDCA composition with hydrogen in the presence of a hydrogenation catalyst under a hydrogen partial pressure within a range of 10 psi to 900 psi. A product FDCA composition is produced having a low amount of tetrahydrofuran dicarboxylic acid, a low b*, and a low amount of 5-formyl furan-2-carboxylic acid (FFCA).
    Type: Grant
    Filed: June 19, 2014
    Date of Patent: February 2, 2016
    Assignee: Eastman Chemical Company
    Inventors: Mesfin Ejerssa Janka, Charles Edwan Sumner, Jr., Shane Kipley Kirk, Ashfaq Shahanawaz Shaikh, Kenny Randolph Parker
  • Process for the preparation of dronedarone by oxidation of a sulphenyl group
    Patent number: 9249119
    Abstract: The invention relates to a novel process for the preparation of dronedarone (I) and pharmaceutically acceptable salts thereof which comprises oxidizing a compound of formula (IV) or a salt thereof with an oxidizing agent in an organic or inorganic solvent or solvent mixture, and isolating the obtained product and, if desired, converting it into a pharmaceutically acceptable salt thereof. Further aspects of the invention include the novel intermediary compound of formula (IV), and a process for the preparation thereof.
    Type: Grant
    Filed: February 1, 2013
    Date of Patent: February 2, 2016
    Assignee: SANOFI
    Inventors: Csaba Huszár, Adrienn Hegedus, Zsolt Dombrády
  • Xanthanodien for the treatment of cancer
    Patent number: 9238022
    Abstract: The present invention relates to a method for the treatment or prophylaxis of a disease associated with hyperproliferative cellular division, comprising administering to a subject in need thereof a therapeutically effective dosage of the pharmaceutical composition comprising xanthanodien, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: July 6, 2011
    Date of Patent: January 19, 2016
    Inventor: Caroline Van Haaften
  • Inhibitors of cholesterol ester transfer protein
    Patent number: 9233938
    Abstract: The invention relates to novel oxazolidinones their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering cholesterol ester transfer protein inhibitors.
    Type: Grant
    Filed: May 6, 2014
    Date of Patent: January 12, 2016
    Assignee: CoNCERT Pharmaceuticals, Inc.
    Inventor: Roger D. Tung
  • Method for preparing meropenem using zinc powder
    Patent number: 9233963
    Abstract: The present invention relates to an improved method for synthesizing meropenem trihydrate[(1R,5S,6S)-2-[((2?S,4?S)-2?-dimethylaminocarbozyl)pyrrolidin-4?-ylthio]-6-[(R)-1-hydroxyethyl]-1-methylcarbapen-2-em-3-carboxylic acid, trihydrate], which is a novel carbapenem antibiotic.
    Type: Grant
    Filed: March 11, 2010
    Date of Patent: January 12, 2016
    Assignees: DAEWOONG PHARMACEUTICAL CO., LTD., DAEWOONG BIO, INC.
    Inventors: Yoon Seok Song, Sung Woo Park, Yeon Jung Yoon, Hee Kyoon Yoon, Seong Cheol Moon, Byung Goo Lee, Soo Jin Choi, Sun Ah Jun
  • Purine derivatives for use in the treatment of allergic, inflammatory and infectious diseases
    Patent number: 9233962
    Abstract: The present invention relates to compounds of formula (I): wherein R1 is C1-6alkylamino, C1-6alkoxy, or C3-7cycloalkyloxy; m is an integer having a value of 3 to 6; n is an integer having a value of 0 to 4; and salts thereof are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, the treatment of infectious diseases and cancer, and may also be useful as vaccine adjuvants.
    Type: Grant
    Filed: May 16, 2014
    Date of Patent: January 12, 2016
    Assignee: GlaxoSmithKline LLC
    Inventors: Keith Biggadike, Diane Mary Coe, Xiao Qing Lewell, Charlotte Jane Mitchell, Stephen Allan Smith, Naimisha Trivedi
  • Covalent inhibitors of Kras G12C
    Patent number: 9227978
    Abstract: Irreversible inhibitors of G12C mutant K-Ras protein are provided. Also disclosed are methods to modulate the activity of G12C mutant K-Ras protein and methods of treatment of disorders mediated by G12C mutant K-Ras protein.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: January 5, 2016
    Assignee: Araxes Pharma LLC
    Inventors: Pingda Ren, Yi Liu, Liansheng Li, Jun Feng, Tao Wu
  • Pyrrolidine derivatives
    Patent number: 9226916
    Abstract: The present invention relates to compounds of formula wherein R1, R2, R3, R4, Z, and n are as defined herein or to a pharmaceutically active salt thereof. Compounds of the invention are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).
    Type: Grant
    Filed: February 28, 2013
    Date of Patent: January 5, 2016
    Assignee: HOFFMANN-LA ROCHE INC.
    Inventors: Henner Knust, Andreas Koblet, Matthias Nettekoven, Hasane Ratni, Claus Riemer, Walter Vifian
  • Method for producing a pi-electron conjugated compound
    Patent number: 9224959
    Abstract: A leaving substituent-containing compound including a partial structure represented by the following General Formula (I): where a pair of X1 and X2 or a pair of Y1 and Y2 each represent a hydrogen atom; the other pair each represent a group selected from the group consisting of a halogen atom and a substituted or unsubstituted acyloxy group having one or more carbon atoms; a pair of the acyloxy groups represented by the pair of X1 and X2 or the pair of Y1 and Y2 may be identical or different, or may be bonded together to form a ring; R1 to R4 each represent a hydrogen atom or a substituent; and Q1 and Q2 each represent a hydrogen atom, a halogen atom or a monovalent organic group, and may be bonded together to form a ring.
    Type: Grant
    Filed: February 4, 2014
    Date of Patent: December 29, 2015
    Assignee: Ricoh Company, Ltd.
    Inventors: Daisuke Goto, Satoshi Yamamoto, Toshiya Sagisaka, Takuji Kato, Takashi Okada, Masato Shinoda, Shinji Matsumoto, Masataka Mohri, Keiichiro Yutani
  • Thiazolopyrimidine modulators as immunosuppressive agents
    Patent number: 9221822
    Abstract: The present invention relates to compound of formula I, II, III, or IV, and/or a pharmaceutical acceptable addition salt thereof and/or a stereoisomer thereof and/or a solvate thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R11, and R12 are as defined in the claim 1. The present invention also relates to a method for their preparation, as well as to pharmaceutical compositions thereof. The present invention further relates to the use of said compounds as biologically active ingredients, more specifically as medicaments for the treatment of disorders and pathologic conditions such as, but not limited to, immune and auto-immune disorders, organ and cells transplant rejections.
    Type: Grant
    Filed: October 20, 2014
    Date of Patent: December 29, 2015
    Assignee: Katholieke Universiteit Leuven, K. U. Leuven R&D
    Inventors: Piet Herdewijn, Steven De Jonghe, Ling-Jie Gao, Mi-Yeon Jang, Bart Vanderhoydonck, Mark Jozef Albert Waer, Yuan Lin, Jean Ferdinand Herman, Thierry Andre Michel Louat
  • Crystal form of pyrrolidylthiocarbapenem derivative
    Patent number: 9221823
    Abstract: Novel crystals of a pyrrolidylthiocarbapenem derivative having excellent stability is provided. According to the present invention, a crystal of (+)-(4R,5S,6S)-6-[(1R)-1-hydroxyethyl]-4-methyl-7-oxo-3[[(3S,5S)-5-(sulfamoylaminomethyl)pyrrolidin-3-yl]thio]-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid having a diffraction pattern in powder X-ray diffraction having main peaks at diffraction angles (2?) of about 6.62, 13.04, 15.44, 16.58, 17.64, 20.88, 23.26, 25.02 and 25.52 (degrees) are provided.
    Type: Grant
    Filed: February 21, 2014
    Date of Patent: December 29, 2015
    Assignee: SHIONOGI & CO., LTD.
    Inventors: Izumi Saitoh, Masayuki Takahira, Toshio Kawakita, Yasuyuki Yoshioka
  • Process for preparation of dronedarone by the use of dibutylaminopropanol reagent
    Patent number: 9221777
    Abstract: The invention relates to a novel process for preparation of dronedarone of formula (I) and pharmaceutically acceptable salts thereof, characterized in that a compound of formula (II)—where L is leaving group—is reacted with compound of formula (III) and the obtained product is isolated and, if desired, converted into a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: March 1, 2013
    Date of Patent: December 29, 2015
    Assignee: SANOFI
    Inventor: Antal Friesz
  • Antimicrobial compounds and methods of making and using the same
    Patent number: 9221827
    Abstract: The present invention relates generally to the field of antimicrobial compounds and to methods of making and using them. These compounds are useful for treating, preventing, and reducing the risk of microbial infections in humans and animals.
    Type: Grant
    Filed: April 11, 2012
    Date of Patent: December 29, 2015
    Assignee: Melinta Therapeutics, Inc.
    Inventors: Erin M. Duffy, Ashoke Bhattacharjee, Shili Chen, Zoltan F. Kanyo, Matthew H. Scheideman, Yuanqing Tang
  • Rhodamine compounds and their use as fluorescent labels
    Patent number: 9222131
    Abstract: The present invention relates to new rhodamine compounds and their use as fluorescent labels. The compounds may be used as fluorescent labels for nucleotides in nucleic acid sequencing applications.
    Type: Grant
    Filed: May 2, 2014
    Date of Patent: December 29, 2015
    Assignee: Illumina Cambridge Limited
    Inventors: Nikolai Nikolaevich Romanov, Xiaohai Liu
  • Use of 6-substituted 9-halogenalkyl purines for regulation of growth and development of whole plants, plant cells and plant organs; novel 6-substituted 9-halogenalkyl purines
    Patent number: 9220269
    Abstract: The invention relates to 6-substituted 9-halogenalkyl purine derivatives of the general formula I wherein R6 is selected from the group comprising —NH-furfuryl, —NH-(4-hydroxy-3-methylbut-2-en-1-yl), —NH-(3-methylbut-2-en-1-yl), —NH-(4-hydroxy-3-methylbutyl), —NH-(4-hydroxy-1,3-dimethylbut-2-en-1-yl), —NH-(4-hydroxy-1,3-dimethylbutyl), —NH-benzyl, —NH-phenyl, wherein benzyl, furfuryl and phenyl can be unsubstituted or optionally substituted with 1 to 3 substituents selected from the group comprising hydroxy, halogen, methyl and methoxy, and R9 is selected from the group comprising C1-C3 alkyl or C1-C3 alkenyl wherein each of the groups is substituted with one or more halogen atoms, for use in the regulation of growth and development of plant cells, organs and/or whole plants. The invention also relates to preparations containing these derivatives and to novel to 6-substituted 9-halogenalkyl purines.
    Type: Grant
    Filed: September 2, 2011
    Date of Patent: December 29, 2015
    Assignee: UNIVERZITA PALACKEHO V OLOMOUCI
    Inventors: Vaclav Mik, Lucie Szucova, Karel Dolezal, Lukas Spichal, Petr Galuszka, Miroslav Strnad, Jiri Gruz
  • 2,3-fluorinated glycosides as neuraminidase inhibitors and their use as anti-virals
    Patent number: 9221859
    Abstract: Compounds having a structure of Formula I and compositions comprising these compounds are provided. Uses of such compounds and compositions are provided for treatment or prophylaxis of viral infection. In particular, compounds and compositions may be for use in the treatment or prophylaxis of viral influenza.
    Type: Grant
    Filed: July 14, 2014
    Date of Patent: December 29, 2015
    Assignee: The University of British Columbia
    Inventors: Stephen Withers, Andrew Graham Watts, Jin Hyo Kim, Tom Wennekes
  • Process for preparation of dronedarone by removal of hydroxyl group
    Patent number: 9221778
    Abstract: The invention relates to a process for preparation of dronedarone of formula (I) and pharmaceutically acceptable salts thereof characterized in that from the compound of formula (II). The hydroxyl group is removed, and the obtained product is isolated and, if desired, converted into a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: February 1, 2013
    Date of Patent: December 29, 2015
    Assignee: SANOFI
    Inventors: Antal Friesz, Zsolt Dombrády
  • Inhibition of leukemic stem cells by PP2A activating agents
    Patent number: 9220706
    Abstract: A method of inhibiting the growth of leukemic hematopoietic stem cells in a subject with leukemia is described. The method includes administering a therapeutically effective amount of a composition including a compound of formula I: I wherein R1 is independently selected from hydrogen and methyl; R2 is selected from the group consisting of 4,8-dimethyl-non-1-enyl, 4,8-dimethyl-nonyl, non-1-enyl, and nonanyl groups; X is a carboxyl, phosphonic, or sulfonic moiety, and n is an integer from 1 to 6, or a compound of Formula II: II wherein R1 is a C6-C12 alkyl or C6-C12 alkoxy group; R2 is independently selected from the group consisting of hydrogen, methoxy, and hydroxyl; and R3 is an alkyl or cycloalkyl group; or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: May 31, 2013
    Date of Patent: December 29, 2015
    Assignees: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), THE UNITED STATES OF AMERICA NIH DIVISION OF EXTRAMURAL INVENTIONS AND TECHNOLOGY RESOURCES (DEITR)
    Inventors: Danilo Perrotti, Paolo Neviani
  • Purinylpyridinylamino-2,4-difluorophenyl sulfonamide derivative, pharmaceutically acceptable salt thereof, preparation method thereof, and pharmaceutical composition with inhibitory activity against Raf kinase, containing same as active ingredient
    Patent number: 9216981
    Abstract: A novel purinylpyridinylamino-2,4-difluorophenyl sulfonamide derivative, a pharmaceutically acceptable salt thereof, a preparation method thereof, and a pharmaceutical composition with an inhibitory activity against Raf kinase, containing the same as an active ingredient are provided. The purinylpyridinylamino-2,4-difluorophenyl sulfonamide derivative of the present invention effectively regulates the activity of B-Raf kinase, and thus may be useful for preventing or treating cancers induced by the over-activation of Raf kinase, especially various melanoma, colorectal cancer, prostate cancer, thyroid cancer, ovarian cancer and the like.
    Type: Grant
    Filed: November 25, 2011
    Date of Patent: December 22, 2015
    Assignee: Medpacto, Inc.
    Inventors: Eun Kyong Shim, Nam Doo Kim, Tae Bo Shim, Seung Yong Kim