Patents Examined by Celia Chang
  • Patent number: 9687480
    Abstract: Chiral 1-(4-methylphenylmethyl)-5-oxo-{N-[(3-t-butoxycarbonyl-aminomethyl)]-piperidin-1-yl}-pyrrolidine-2-carboxamides as inhibitors of collagen induced platelet activation and adhesion. The present invention provides chiral (2S)-1-(4-methylphenylmethyl)-5-oxo-(3S)-{N-[(3-t-butoxycarbonyl aminomethyl)]-piperidin-1-yl}-pyrrolidine-2-carboxamide, and (2S)-1-(4-methylphenylmethyl)-5-oxo-(3R)-{N-[(3-t-butoxycarbonyl amino methyl)]-piperidin-1-yl}-pyrrolidine-2-carboxamide of formula 6 and 7 respectively. The present invention also relates to use of these moieties as inhibitors of collagen induced platelet adhesion and aggregation mediated through collagen receptors. The present invention provides a process for preparation of chiral carboxamides of formula 6 and 7 using the process which has advantage to avoid any racemization at the a-carboxylic center, during N-alkylation. The reagent LiHMDS is used at low temperatures to furnish methyl N-(p-methylphenylmethyl)1pyroglutamate in good chiral purity.
    Type: Grant
    Filed: November 5, 2015
    Date of Patent: June 27, 2017
    Assignee: Council of Scientific & Industrial Research
    Inventors: Dinesh Kumar Dikshit, Madhu Dikshit, Tanveer Irshad Siddiqui, Anil Kumar, Rabi Sankar Bhatta, Girish Kumar Jain, Manoj Kumar Barthwal, Ankita Misra, Vivek Khanna, Prem Prakash, Manish Jain, Vishal Singh, Varsha Gupta, Anil Kumar Dwivedi
  • Patent number: 9675599
    Abstract: The invention relates to compounds of formula I: where a, R1, and R3-6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin and norepinephrine reuptake inhibitors. The invention also relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Grant
    Filed: September 9, 2015
    Date of Patent: June 13, 2017
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Lori Jean Patterson, Eric L. Stangeland
  • Patent number: 9669015
    Abstract: This invention is directed to derivatives of piperidine-2,6-dione, or their organic or inorganic salts thereof, a methods of synthesis of these derivatives, and their application as active pharmaceutical ingredient as inhibitors of TNF? releasing in cells, the derivative of piperidine-2,6-dione being of the general formula (I): wherein n represents 1, 2, 3, 4, 5 or 6; R1 represents from one to four of the same or different substituents selected from F, Cl, Br, C1-4 alkyl, OH, OC1-4 alkyl, NO2, NHC(O)C1-4 alkyl, NH2, NH(C1-4 alkyl), N(C1-4 alkyl)2; R2 represents OR3, NR3R4, N(R3)COR4, O2CR5; R3 and R4 represent independently and at each occurrence H or C1-4 alkyl; R5 represents CHR6NR7R8, CHR6NR9C(O)CHR10NR7R8, a heterocycle W or CHR6NR9C(O)W; R6, R9, R10 represent independently and at each occurrence H, or C1-4 alkyl; R7 and R8 represent independently and at each occurrence H, C1-4 alkyl, or R7 and R8 taken together represent 1,3-propylene, 1,4-butylene, 1,5-pentylene, or 1,6-hexylene; W represents four-m
    Type: Grant
    Filed: June 16, 2015
    Date of Patent: June 6, 2017
    Assignee: Tianjin Hemay Bio-Tech Co., Ltd.
    Inventor: Hesheng Zhang
  • Patent number: 9670487
    Abstract: The instant invention provides for novel cationic lipids that can be used in combination with other lipid components such as cholesterol and PEG-lipids to form lipid nanoparticles with oligonucleotides. It is an object of the instant invention to provide a cationic lipid scaffold that is susceptible to hydrolytic instability that may translate into reduced liver residence times and reduced hepatocellular toxicity. The present invention employs acetals and ketals to provide a low pH sensitive chemical handle for degradation.
    Type: Grant
    Filed: January 19, 2011
    Date of Patent: June 6, 2017
    Assignee: SIRNA THERAPEUTICS, INC.
    Inventors: Steven L. Colletti, Zhengwu James Deng, Matthew G. Stanton, Weimin Wang, Ivory Hills
  • Patent number: 9656946
    Abstract: A method for preparing 1-adamantyltrimethylammonium methylcarbonate or N,N-dimethyl-3,5-dimethylpiperidinium methylcarbonate is disclosed. The method comprises reacting dimethyl carbonate and 3,5-dimethylpiperidine or a 1-adamantylamine compound and in the presence of water in a sealed vessel at a temperature of from 80 to 200° C. The 1-adamantylamine compound is 1-adamantylamine, 1-adamantylmethylamine, or mixtures thereof.
    Type: Grant
    Filed: March 4, 2016
    Date of Patent: May 23, 2017
    Assignee: Johnson Matthey Public Limited Company
    Inventor: Richard Charles Bryan
  • Patent number: 9656993
    Abstract: The invention provides crystalline forms of biphenyl-2-ylcarbamic acid 1-(2-{[4-(4-carbamoylpiperidin-1-ylmethyl)benzoyl]methylamino}ethyl)piperidin-4-yl ester, and pharmaceutically acceptable solvates thereof. The crystalline form can be a freebase, or a salt such as a diphosphate, monosulfate or dioxalate salt. The invention also provides pharmaceutical compositions comprising these crystalline compounds or prepared using these compounds; processes and intermediates for preparing the crystalline compounds; and methods of using these compounds to treat a pulmonary disorder.
    Type: Grant
    Filed: December 18, 2015
    Date of Patent: May 23, 2017
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Sabine Axt, Timothy J. Church
  • Patent number: 9650337
    Abstract: A method is described for the synthesis of 4-piperidin-4-yl-benzene-1,3-diol of the following formula (I): and the pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: February 14, 2014
    Date of Patent: May 16, 2017
    Assignee: GALDERMA RESEARCH & DEVELOPMENT
    Inventors: Jean-Guy Boiteau, Branislav Musicki
  • Patent number: 9643950
    Abstract: The invention in one embodiment is directed to solid forms of {S-3-(4-Amino-1-oxo-isoindolin-2-yl)(piperidine-3,4,4,5,5-d5)-2,6-dione}, including an anhydrous crystalline form, two hydrates, and an amorphous form. The invention in one embodiment is directed to methods of preparation of the solid forms.
    Type: Grant
    Filed: October 21, 2013
    Date of Patent: May 9, 2017
    Assignee: Concert Pharmaceuticals, Inc.
    Inventors: Joanna A. Bis, David H. Igo
  • Patent number: 9643952
    Abstract: The invention provides a pyridone compound represented by the following formula (I) [wherein, R1 represents cycloalkyl optionally having substituent(s) and the like, R2 represents a hydrogen atom and the like, R3 represents hydroxy and the like, and R4A represents the following formula (R4A-1) (wherein, R4 and R5 are the same or different and each represents a hydrogen atom and the like), and the like], or a pharmaceutically acceptable salt thereof, which is useful as a prophylactic and/or therapeutic agent for skin diseases, and the like.
    Type: Grant
    Filed: December 6, 2013
    Date of Patent: May 9, 2017
    Assignee: Kyowa Hakko Kirin Co., Ltd.
    Inventors: Rina Nakamura, Seiji Aratake, Kenji Uchida, Kimihisa Ueno, Maasa Motosawa, Takahiro Kabeya
  • Patent number: 9637471
    Abstract: The present invention relates to hydroxyindalpine derivatives of formula (I) as defined herein and pharmaceutical compositions comprising these compounds, as well as their medical use, particularly in the treatment or prevention of gastrointestinal diseases/disorders, such as constipation and functional dyspepsia.
    Type: Grant
    Filed: February 14, 2014
    Date of Patent: May 2, 2017
    Assignee: Technische Universitat Munchen
    Inventors: Arne Skerra, Michael Muller, Michael Schemann, Thomas Berger
  • Patent number: 9637454
    Abstract: The present invention relates to the field of pharmaceutical chemistry and pharmacotherapeutics, and in particular to compounds of general formula I, racemates, R-isomers, S-isomers, and pharmaceutically acceptable salts thereof and their mixtures, and the preparation methods thereof and a pharmaceutical composition containing the compounds and uses thereof as an acetylcholine esterase inhibitor.
    Type: Grant
    Filed: October 17, 2013
    Date of Patent: May 2, 2017
    Assignee: SHANGHAI INSTITUTE OF MATERIA MADICA, CHINESE ACADEMY OF SCIENCES
    Inventors: Hong Liu, Haiyan Zhang, Yu Zhou, Yan Fu, Hualiang Jiang, Xican Tang, Kaixian Chen
  • Patent number: 9637504
    Abstract: Described herein are compounds and compositions that modulate the activity of beta-lactamases. In some embodiments, the compounds described herein inhibit beta-lactamase. In certain embodiments, the compounds described herein are useful in the treatment of bacterial infections.
    Type: Grant
    Filed: May 23, 2016
    Date of Patent: May 2, 2017
    Assignee: VENATORX PHARMACEUTICALS, INC.
    Inventors: Christopher J. Burns, Denis Daigle, Bin Liu, Randy W. Jackson, Jodie Hamrick, Daniel McGarry, Daniel C. Pevear, Robert E. Lee Trout
  • Patent number: 9630929
    Abstract: This invention is directed to benzensulfonamide compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment of sodium channel-mediated diseases or conditions, such as pain.
    Type: Grant
    Filed: October 30, 2012
    Date of Patent: April 25, 2017
    Assignee: XENON PHARMACEUTICALS INC.
    Inventors: Shaoyi Sun, Alla Yurevna Zenova, Mikhail Chafeev, Qi Jia, Zaihui Zhang, Renata Marcella Oballa
  • Patent number: 9617241
    Abstract: The present invention relates to a process for the preparation of (2R,3R)-2-(2,4-difluorophenyl)-3-(4-methylene-1-piperidinyl)-1-(1H-1,2,4-triazol-1-yl)-2-butanol (Efinaconazole) and intermediates used in such process.
    Type: Grant
    Filed: March 2, 2015
    Date of Patent: April 11, 2017
    Assignee: MAPI PHARMA LTD.
    Inventors: Anna Gopin, Shai Rubnov, Galina Zats, Ehud Marom
  • 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: 9604966
    Abstract: The present invention relates to the technical field of medicine and organic synthesis, particularly to a method for preparing crizotinib. The method comprises the compound of formula b and the compound of formula e undergoing Suzuki coupling reaction to produce the compound of formula a which then was subjected to deprotection to afford (±) crizotinib.
    Type: Grant
    Filed: February 13, 2014
    Date of Patent: March 28, 2017
    Assignee: Zhejiang Jiuzhou Pharmaceutical Co., Ltd
    Inventors: Yuanqiang Li, Jianqiang Qian, Daqing Che
  • Patent number: 9586950
    Abstract: The present invention is directed to 2-pyridyloxy-3-ester-4-nitrile compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the 2-pyridyloxy-3-ester-4-nitrile compounds described herein in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
    Type: Grant
    Filed: October 14, 2013
    Date of Patent: March 7, 2017
    Assignee: MERCK SHARP & DOHME CORP.
    Inventors: Scott D. Kuduk, Jason W. Skudlarek
  • Patent number: 9573897
    Abstract: Compounds are provided that are modulators of the C5a receptor. The compounds are substituted piperidines and are useful in pharmaceutical compositions, methods for the treatment of diseases and disorders involving the pathologic activation of C5a receptors.
    Type: Grant
    Filed: September 4, 2015
    Date of Patent: February 21, 2017
    Assignee: CHEMOCENTRYX, INC.
    Inventors: Pingchen Fan, Kevin Lloyd Greenman, Manmohan Reddy Leleti, Yandong Li, Jay Powers, Hiroko Tanaka, Ju Yang, Yibin Zeng
  • Patent number: 9556118
    Abstract: The present invention relates to novel heterocyclic derivatives which are allosteric modulators of cannabinoid receptor 1 (CB1) and which are useful for the treatment or prevention of neurological and psychiatric disorders associated with endocannabinoid dysfunction and diseases in which the CB1 subtype of cannabinoid receptor is involved; to processes for their preparation; to pharmaceutical compositions comprising them; and to methods of using them.
    Type: Grant
    Filed: July 3, 2014
    Date of Patent: January 31, 2017
    Assignee: Northeastern University
    Inventors: Ganeshsingh A. Thakur, Pushkar M. Kulkarni
  • Patent number: 9546152
    Abstract: The present invention is directed to 2-pyridyloxy-3-substituted-4-nitrile compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the 2-pyridyloxy-3-substituted-4-nitrile compounds described herein in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
    Type: Grant
    Filed: October 21, 2013
    Date of Patent: January 17, 2017
    Assignee: MERCK SHARP & DOHME CORP.
    Inventors: Scott D. Kuduk, Jason W. Skudlarek