Ring Chalcogen In The Additional Hetero Ring Patents (Class 544/374)
  • Patent number: 9637590
    Abstract: A method for synthesizing polylactide (PLA). The method employs RCOOCG, a nontoxic carboxylate of cyclic guanidine (CG), as a catalyst and non-toxic organic alcohol R?OH as an initiator to catalyze/initiate a living ring-opening polymerization of lactide (LA). The method includes: 1) adding monomer LA, the catalyst RCOOCG, and the initiator R?OH to a reaction still, where an initial molar ratio of the monomer to the catalyst is [LA]0/[RCOOCG]0=1000-1500:1, an initial molar amount [R?OH]0 of the initiator R?OH is determined by a number average molecular weight (Mn) of a target product PLA; 2) removing air in the reaction still, sealing the reaction still after a pressure in the reaction still is constant at between 1.0 and 0.1 torr; stirring and heating the reaction still in 30 to 40 minutes to a temperature between 95 and 96° C.; and allowing reactants in the reaction still to polymerization.
    Type: Grant
    Filed: September 19, 2016
    Date of Patent: May 2, 2017
    Assignee: NANJING UNIVERSITY
    Inventors: Hong Li, Quanxing Zhang, Wei Huang, Jiaye Sheng, Aimin Li
  • Patent number: 9028874
    Abstract: The present invention is directed to multiple a-lipoic acid-containing hydrophobic compounds (mALAs) capable of acting as scavengers of free radicals, metals and reactive oxygen species (ROS). Methods of synthesizing novel antioxidant mALAs, spontaneous emulsification or nanoprecipitaion thereof to produce antioxidant nanospheres and their use in preventing or treating diseases or conditions caused by oxidative stress and other free radical mediated conditions are also described. Another aspect of this invention is the use of these antioxidant nanospheres for the preparation of antioxidant particulate delivery system of therapeutic agents.
    Type: Grant
    Filed: December 30, 2008
    Date of Patent: May 12, 2015
    Assignee: Cedars-Sinai Medical Center
    Inventors: John S. Yu, Bong Seop Lee
  • Publication number: 20150105397
    Abstract: The present inventions relate to substituted piperazine derivatives of general formula (I) and to the manufacture of said compounds, pharmaceutical compositions comprising a compound according to general formula (I), and the use of said compounds for the treatment of various medical conditions related to glycine transporter-1 (GlyT1).
    Type: Application
    Filed: October 14, 2014
    Publication date: April 16, 2015
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Christoph HOENKE, Riccardo GIOVANNINI, Uta LESSEL, Holger ROSENBROCK, Bernhard SCHMID
  • Patent number: 8969559
    Abstract: Disclosed herein are ketal amide compounds. The ketal amide compounds are synthesized by the reaction of ketal acids or ketal esters with amine functional compounds. Also disclosed are methodologies useful to make the ketal amide compounds. Also disclosed herein are formulations and articles containing the ketal amide compounds.
    Type: Grant
    Filed: February 10, 2012
    Date of Patent: March 3, 2015
    Assignee: Segetis, Inc.
    Inventors: Sergey Selifonov, Adam E. Goetz, Marc D. Scholten, Ning Zhou
  • Publication number: 20140336375
    Abstract: The disclosure is directed to compounds identified as allosteric modulators of 5-HT 2CR, as well as pharmaceutical compositions and methods using the same. Certain embodiments also include methods of identifying and methods of synthesizing the compounds. Optimization and development of allosteric 5-HT 2CR modulators that bind sites other than the primary ligand binding site generate novel, highly selective, and potent ligands of 5-HT2CR. Such molecules can be used as small molecule probes for the nervous system and as effective therapeutics for a variety of diseases.
    Type: Application
    Filed: December 7, 2012
    Publication date: November 13, 2014
    Applicant: The Board of Regents of the University of Texas system
    Inventors: Jia Zhou, Chunyong Ding, Kathryn A. Cunningham
  • Publication number: 20140309192
    Abstract: The present invention relates to compounds of Formula (I) and pharmaceutically acceptable salts, solvates, and hydrates thereof: that are useful in methods of treatment and alleviation of diseases and disorders of the heart, brain, kidney, immune, and reproductive system resulting from ischemia, or reperfusion subsequent to ischemia, and any downstream complication(s) related thereto. The present invention further relates to methods of treatment and alleviation of diseases and disorders of the vasculature resulting from vasoconstriction or hypertension and any downstream complication(s) resulting from elevated blood pressure and/or reduced tissue perfusion.
    Type: Application
    Filed: November 7, 2012
    Publication date: October 16, 2014
    Inventors: Thuy-Anh Tran, Anthony C. Blackburn, Bryan A. Kramer, Maiko Nagura, Carleton R. Sage, Young-Jun Shin, Ning Zou
  • Publication number: 20140275010
    Abstract: The present invention provides quaternary salts, such as those of Formula I: as well as the use thereof in methods of treatment for cancer.
    Type: Application
    Filed: March 11, 2014
    Publication date: September 18, 2014
    Inventors: Guo Zhu Zheng, Yuan Wang, Gregg F. Keany, Kenzo Arai, Kazunobu Kira, Xiang Liu, Nick Gearhart, Baudouin Gerard
  • Patent number: 8835419
    Abstract: Aniline compounds are provided which bind to CCR(4) and are useful for the treatment of diseases such as allergic diseases, autoimmune diseases, graft rejection and cancer.
    Type: Grant
    Filed: November 30, 2012
    Date of Patent: September 16, 2014
    Assignee: ChemoCentryx, Inc.
    Inventors: Trevor T. Charvat, Junfa Fan, Christopher W. Lange, Manmohan Reddy Leleti, Yandong Li, Venkat Reddy Mali, Jeffrey P. MacMahon, Jay Powers, Sreenivas Punna, Ju Yang
  • Publication number: 20140235650
    Abstract: The invention relates to a compound of formula (I), where R1, R2, R7, m, n, and L1 are as defined in claim 1, and to the methods for preparing same, to the pharmaceutical compositions containing same, and to the uses thereof in the treatment of diseases associated with insulin resistance syndrome.
    Type: Application
    Filed: June 22, 2012
    Publication date: August 21, 2014
    Applicant: Metabolys
    Inventors: Gerard Moinet, Gabriel Baverel, Remi Nazaret, Bernard Ferrier
  • Publication number: 20140194422
    Abstract: The disclosure relates to piperazine derivatives, compositions, and methods related thereto. In certain embodiments, the disclosure relates to inhibitors of NADPH-oxidase.
    Type: Application
    Filed: June 12, 2012
    Publication date: July 10, 2014
    Applicant: EMORY UNIVERSITY
    Inventors: Thota Ganesh, Aiming Sun, Susane M. Smith, John David Lambeth
  • Publication number: 20140107119
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 or Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which are expressed anti-apoptotic Bcl-2 protein.
    Type: Application
    Filed: November 15, 2013
    Publication date: April 17, 2014
    Applicant: AbbVie Inc.
    Inventors: Milan Bruncko, Hong Ding, George A. Doherty, Steven W. Elmore, Lisa Hasvold, Laura A. Hexamer, Aaron R. Kunzer, Robert A. Mantei, William J. McClellan, Chang H. Park, Cheol-Min Park, Andrew M. Petros, Xiaohong Song, Andrew J. Souers, Gerard M. Sullivan, Zhi-fu Tao, Gary T. Wang, Le Wang, Xilu Wang, Michael D. Wendt, Todd M. Hansen
  • Publication number: 20140088106
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.
    Type: Application
    Filed: October 14, 2013
    Publication date: March 27, 2014
    Applicant: AbbVie Inc.
    Inventors: Milan Bruncko, Yujia Dai, Hong Ding, George A. Doherty, Steven W. Elmore, Lisa Hasvold, Laura A. Hexamer, Aaron R. Kunzer, Robert A. Mantei, William J. McClellan, Chang H. Park, Cheol-Min Park, Andrew M. Petros, Xiaohong Song, Andrew J. Souers, Gerard M. Sullivan, Zhi-Fu Tao, Gary T. Wang, Le Wang, Xilu Wang, Michael D. Wendt, Todd M. Hansen
  • Publication number: 20140088077
    Abstract: The invention relates to substituted tetrahydronaphthalenes and derivatives thereof, and also to the physiologically compatible salts and physiologically functional derivatives thereof, to preparation thereof, to medicaments comprising at least one inventive substituted tetrahydronaphthalene or derivative thereof, and to the use of the inventive substituted tetrahydronaphthalenes and derivatives thereof as medicaments.
    Type: Application
    Filed: December 3, 2013
    Publication date: March 27, 2014
    Applicant: SANOFI
    Inventors: Lothar Schwink, Siegfried Stengelin, Matthias Gossel, Torsten Haack, Petra Lennig
  • Patent number: 8673904
    Abstract: Provided herein are novel epoxide inhibitors of cysteine proteases, compositions comprising the epoxide inhibitors, and packaged pharmaceuticals. Also provided are methods of inhibiting a papain-family cysteine protease and methods of treating or preventing a disease by administering a composition containing an epoxide inhibitor of the invention. The compositions may be administered in combination with another therapeutic agent.
    Type: Grant
    Filed: June 13, 2007
    Date of Patent: March 18, 2014
    Assignee: The Board of Trustees of the Leland Stanford Junior University
    Inventors: Matthew S. Bogyo, Amir M. Sadaghiani, Steven Verhelst
  • Patent number: 8669260
    Abstract: The application discloses ketoconazole derivatives that are antagonists of the human pregnane X receptor (PXR), methods of preparing the derivatives, uses of the derivatives with drug therapy, and methods of inhibiting tumor cell proliferation and multidrug resistance using inhibitors of PXR.
    Type: Grant
    Filed: January 27, 2009
    Date of Patent: March 11, 2014
    Assignee: Albert Einstein College of Medicine of Yeshiva University
    Inventors: Sridhar Mani, Bhaskar C. Das
  • Publication number: 20140066621
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.
    Type: Application
    Filed: July 26, 2013
    Publication date: March 6, 2014
    Applicants: The Walter and Eliza Hall Institute of Medical Research, AbbVie Inc.
    Inventors: Milan Bruncko, Yujia Dai, Hong Ding, George A. Doherty, Steven W. Elmore, Lisa Hasvold, Laura Hexamer, Aaron R. Kunzer, Robert A. Mantei, Chang H. Park, Cheol-Min Park, Andrew M. Petros, Xiahong Song, Andrew J. Souers, Gerard M. Sullivan, Zhi-Fu Tao, Gary T. Wang, Le Wang, Xilu Wang, Michael D. Wendt, Peter Edward Czabotar, Guillaume Laurent Lessene, Peter Malcolm Colman, William J. McClellan
  • Publication number: 20140057889
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 or Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which are expressed anti-apoptotic Bcl-2 protein.
    Type: Application
    Filed: October 18, 2013
    Publication date: February 27, 2014
    Applicant: AbbVie Inc.
    Inventors: Milan Bruncko, Hong Ding, George A. Doherty, Steven W. Elmore, Lisa Hasvold, Laura A. Hexamer, Aaron R. Kunzer, Robert A. Mantei, William J. McClellan, Chang H. Park, Cheol-Min Park, Andrew M. Petros, Xiaohong Song, Andrew J. Souers, Gerard M. Sullivan, Zhi-Fu Tao, Gary T. Wang, Le Wang, Xilu Wang, Michael D. Wendt
  • Publication number: 20140057890
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 or Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which are expressed anti-apoptotic Bcl-2 protein.
    Type: Application
    Filed: October 18, 2013
    Publication date: February 27, 2014
    Applicant: AbbVie Inc.
    Inventors: Milan Bruncko, Hong Ding, George A. Doherty, Steven W. Elmore, Lisa Hasvold, Laura A. Hexamer, Aaron R. Kunzer, Robert A. Mantei, William J. McClellan, Chang H. Park, Cheol-Min Park, Andrew M. Petros, Xiaohong Song, Andrew J. Souers, Gerard M. Sullivan, Zhi-Fu Tao, Gary T. Wang, Le Wang, Xilu Wang, Michael D. Wendt
  • Patent number: 8623859
    Abstract: The invention relates to compounds of formula (I) wherein R1, R1a, R1b, R2, R3 and X, X1, X2, X3 have the meaning as cited in the description and the claims. Said compounds are useful as Bradykinin B1 antagonists. The invention also relates to pharmaceutical compositions, the preparation of such compounds as well as the production and use as medicament.
    Type: Grant
    Filed: August 10, 2009
    Date of Patent: January 7, 2014
    Assignee: Evotec AG
    Inventors: James Madden, David James Hallett, Alastair Parkes, Ali Raoof, Xiaolu Wang
  • Publication number: 20140005181
    Abstract: The present disclosure relates to compounds and methods for treating a disease mediated by apelin.
    Type: Application
    Filed: June 20, 2013
    Publication date: January 2, 2014
    Applicant: Sanford-Burnham Medical Research Institute
    Inventors: Layton Smith, Anthony B. Pinkerton
  • Patent number: 8614211
    Abstract: Chemical entities that are arctigenin derivatives, pharmaceutical compositions and methods of treatment of cancer are described.
    Type: Grant
    Filed: August 10, 2012
    Date of Patent: December 24, 2013
    Assignee: NeuPharma, Inc.
    Inventors: Xiangping Qian, Yong-Liang Zhu
  • Publication number: 20130323777
    Abstract: A ligand design allows compact nanoparticle materials, such as quantum dots (QDs), with excellent colloidal stability over a wide range of pH and under high salt concentrations. Self-assembled biomolecular conjugates with QDs can be obtained which are stable in biological environments. Energy transfer with these ligands is maximized by minimizing distances between QDs/nanoparticles and donors/acceptors directly attached to the ligands or assembled on their surfaces.
    Type: Application
    Filed: July 16, 2013
    Publication date: December 5, 2013
    Applicant: Naval Research Laboratory
    Inventors: Igor L. Medintz, Kimihiro Susumu, Michael H. Stewart
  • Patent number: 8552188
    Abstract: The present invention provides a novel intermediate for manufacturing a 2,3-dihydroimidazo[2,1-b]oxazole compound with a high yield and a high purity, and a manufacturing method of the intermediate. The present invention provides an epoxy compound represented by the general formula (2): wherein, R1 represents a hydrogen or a lower alkyl group; and R2 represents a piperidyl group represented by the general formula (A1): (wherein, R3 represents a phenoxy group having a halogen-substituted lower alkoxy group substituted on a phenyl group, and the like) and the like; and n represents an integer of 1 to 6, a manufacturing method of the epoxy compound, and a manufacturing method of an oxazole compound using the epoxy method.
    Type: Grant
    Filed: November 15, 2012
    Date of Patent: October 8, 2013
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Hidetsugu Tsubouchi, Yoshikazu Haraguchi, Satoshi Hayakawa, Naoto Utsumi, Shinichi Taira, Yoshihisa Tanada, Nobuhisa Fujita, Koichi Shinhama, Kimiyoshi Annaka, Takuya Furuta
  • Patent number: 8541601
    Abstract: The present invention relates to piperazine dithioctate, a novel addition salt of thioctic acid with a base and a pharmaceutical composition comprising the same. The piperazine dithioctate according to the present invention has good thermal and moisture stability and high water-solubility as well as dosage increase lower than other addition salts, thereby being effectively used for preparing a pharmaceutical composition for antioxidation or for preventing or treating diabetic polyneuropathy, etc.
    Type: Grant
    Filed: June 18, 2010
    Date of Patent: September 24, 2013
    Assignees: Celltrion Chemical Research Institute, Celltrion Pharm, Inc.
    Inventors: Kyoung Soo Kim, Young Jun Park, Hyun-Nam Song, In Suk Lee, Joon Woo Kim
  • Publication number: 20130190288
    Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, A, X1, X2, X3, X4, R1, R2, R3a, R3b, R4a and R4b are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.
    Type: Application
    Filed: December 18, 2012
    Publication date: July 25, 2013
    Applicant: GENENTECH, INC.
    Inventor: Genentech, Inc.
  • Publication number: 20130190488
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic protein family members, compositions containing the compounds and uses of the compounds for preparing medicaments for treating diseases during which occurs expression one or more than one of an anti-apoptotic protein family member.
    Type: Application
    Filed: December 12, 2012
    Publication date: July 25, 2013
    Applicant: Abbott Laboratories
    Inventor: Abbott Laboratories
  • Publication number: 20130172315
    Abstract: Aniline compounds are provided which bind to CCR(4) and are useful for the treatment of diseases such as allergic diseases, autoimmune diseases, graft rejection and cancer.
    Type: Application
    Filed: November 30, 2012
    Publication date: July 4, 2013
    Applicant: ChemoCentryx, Inc.
    Inventor: ChemoCentryx, Inc.
  • Publication number: 20130158046
    Abstract: Fumagillin analog polymer conjugates, methods of making fumagillin analog polymer conjugates, compositions comprising a polymer conjugate of a fumagillin analog, and methods for treating cancer, or treating angiogenic diseases comprising administering to a subject in need thereof an effective amount of a polymer conjugate of a fumagillin analog, are described. Also described are novel fumagillin analogs, methods of making fumagillin analogs, compositions comprising at least one fumagillin analog, and methods for treating cancer, or treating angiogenic diseases comprising administering to a subject in need thereof an effective amount of a fumagillin analog.
    Type: Application
    Filed: February 15, 2013
    Publication date: June 20, 2013
    Applicant: Mersana Therapeutics, Inc
    Inventors: Laura C. Akullian, Russell C. Petter, John J. Kane, Charles E. Hammond, Mao Yin, Aleksandr Yurkovetskiy, Cheri A. Stevenson
  • Publication number: 20130072683
    Abstract: The present invention provides a novel intermediate for manufacturing a 2,3-dihydroimidazo[2,1-b]oxazole compound with a high yield and a high purity, and a manufacturing method of the intermediate. The present invention provides an epoxy compound represented by the general formula (2): wherein, R1 represents a hydrogen or a lower alkyl group; and R2 represents a piperidyl group represented by the general formula (A1): (wherein, R3 represents a phenoxy group having a halogen-substituted lower alkoxy group substituted on a phenyl group, and the like) and the like; and n represents an integer of 1 to 6, a manufacturing method of the epoxy compound, and a manufacturing method of an oxazole compound using the epoxy method.
    Type: Application
    Filed: November 15, 2012
    Publication date: March 21, 2013
    Applicant: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventor: Otsuka Pharmaceutical Co., Ltd.
  • Publication number: 20130053564
    Abstract: Disclosed herein are ketal amide compounds. The ketal amide compounds are synthesized by the reaction of ketal acids or ketal esters with amine functional compounds. Also disclosed are methodologies useful to make the ketal amide compounds. Also disclosed herein are formulations and articles containing the ketal amide compounds.
    Type: Application
    Filed: February 10, 2012
    Publication date: February 28, 2013
    Applicant: SEGETIS, INC.
    Inventors: Sergey SELIFONOV, Adam E. GOETZ, Marc D. SCHOLTEN, Ning ZHOU
  • Publication number: 20130045499
    Abstract: A ligand design allows compact nanoparticle materials, such as quantum dots (QDs), with excellent colloidal stability over a wide range of pH and under high salt concentrations. Self-assembled biomolecular conjugates with QDs can be obtained which are stable in biological environments. Energy transfer with these ligands is maximized by minimizing distances between QDs/nanoparticles and donors/acceptors directly attached to the ligands or assembled on their surfaces.
    Type: Application
    Filed: August 15, 2011
    Publication date: February 21, 2013
    Applicant: The Government of the United States of America, as represented by the Secretary of the Navy
    Inventors: Igor L. Medintz, Kimihiro Susumu, Michael H. Stewart
  • Patent number: 8343963
    Abstract: The present invention relates to novel sulfamoyl-phenyl-ureido compounds having the formula (I) or a physiologically acceptable salt or derivative thereof which are suitable for the therapy of infections caused by protozoa and in particular uncomplicated or severe malaria caused by plasmodia.
    Type: Grant
    Filed: January 29, 2010
    Date of Patent: January 1, 2013
    Assignee: 4SC AG
    Inventor: Stefano Pegoraro
  • Publication number: 20120329775
    Abstract: The present invention provides compounds of formula (I) in which y, m, n, R1, R2 and Q are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Application
    Filed: June 4, 2012
    Publication date: December 27, 2012
    Inventors: Rhonan Ford, Andrew Mather, Antonio Mete, Ian Millichip
  • Patent number: 8299067
    Abstract: Provided herein are 5-demethoxyfumagillol and its derivatives. Also provided herein are methods of making the 5-demethoxyfumagillol and derivatives. Also provided herein are biological activities of the 5-demethoxyfumagillol and derivatives and methods of using same for treating diseases.
    Type: Grant
    Filed: March 25, 2009
    Date of Patent: October 30, 2012
    Assignees: Versitech Limited, Morningside Ventures Limited
    Inventors: Dan Yang, Chengyong Li, Shiwu Chen
  • Patent number: 8288389
    Abstract: The present invention relates to 1-(1-methylethyl)-4-{[4-(tetrahydro-2H-pyran-4-yloxy)phenyl]carbonyl}piperazine or a pharmaceutically acceptable salt thereof, in particular the hydrochloride salt thereof and crystalline forms of the hydrochloride salt; to processes for the preparation of the compound or its salt; to compositions containing it; and to its use in the treatment or prophylaxis of neurological or psychiatric diseases, such as cognitive impairment, fatigue or a sleep disorder, for example in a mammal such as a human. The compound or a salt thereof has affinity for and is an antagonist and/or inverse agonist of the histamine H3 receptor.
    Type: Grant
    Filed: September 4, 2008
    Date of Patent: October 16, 2012
    Assignee: Glaxo Group Limited
    Inventors: Desmond John Best, Sing Yeung Mak, Barry Sidney Orlek, Geracimos Rassias, Pamela Joan Theobald
  • Publication number: 20120245183
    Abstract: The present invention provides compounds represented by formula (1): wherein, R1, R2, R3 and R4 are as defined in the specification, in all their stereoisomeric and tautomeric forms and mixtures thereof in all ratios, and their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, pharmaceutically acceptable polymorphs and prodrugs. The invention also relates to processes for the manufacture of compounds of formula (1) and pharmaceutical compositions containing them. The compounds and the pharmaceutical compositions of the present invention are useful for the treatment of cancer. The present invention further provides a method of treatment of cancer by administering a therapeutically effective amount of the said compound of formula (1) or its pharmaceutical composition, to a mammal in need thereof.
    Type: Application
    Filed: November 15, 2010
    Publication date: September 27, 2012
    Applicants: ONCOTEST GMBH, PIRAMAL LIFE SCIENCES LIMITED
    Inventors: Prabhu Dutt Mishra, Shafee Mohammed Abdul, Ram Vishwakarma, Heinz-Herbert Fiebig, Gerhard Kelter
  • Publication number: 20120237874
    Abstract: According to one embodiment, an actinic-ray- or radiation-sensitive resin composition includes any of the compounds (A) of general formula (I) below that when exposed to actinic rays or radiation, generates an acid and a resin (B) whose rate of dissolution into an alkali developer is increased by the action of an acid. (The characters used in general formula (I) have the meanings mentioned in the description.
    Type: Application
    Filed: May 31, 2012
    Publication date: September 20, 2012
    Applicant: FUJIFILM CORPORATION
    Inventors: Shuhei Yamaguchi, Akinori Shibuya
  • Publication number: 20120183498
    Abstract: Compounds, compositions and methods are provided for the prophylaxis and treatment of infections caused by viruses of the Pneumovirinae subfamily of Paramyxoviridae and diseases associated with such infection.
    Type: Application
    Filed: March 22, 2012
    Publication date: July 19, 2012
    Inventors: Theodore J. Nitz, Janet A. Gaboury, Christopher J. Burns, Sylvie Laguerre, Daniel C. Pevear, Thomas A. Lessen, David J. Rys
  • Patent number: 8198280
    Abstract: The present invention is related to N-hydroxyamide derivatives of Formula (I) and use thereof in particular for the treatment and/or prophylaxis of autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, cancer, respiratory diseases and fibrosis, including multiple sclerosis, arthritis, emphysema, chronic obstructive pulmonary disease, liver and pulmonary fibrosis.
    Type: Grant
    Filed: December 16, 2010
    Date of Patent: June 12, 2012
    Assignee: Merck Serono SA
    Inventors: Dominique Swinnen, Jerome Gonzalez
  • Publication number: 20120128640
    Abstract: An expansion agent for hematopoietic stem cells and/or hematopoietic progenitor cells useful for improvement in the efficiency of gene transfer into hematopoietic stem cells for gene therapy useful for treatment of various disorders is provided. An expansion agent for hematopoietic stem cells and/or hematopoietic progenitor cells containing a compound represented by the formula (I) (wherein X, Y, Z, Ar1, R1, R2, R3, R4, R5, R6 and R7 are as defined in the description), a tautomer, prodrug or pharmaceutically acceptable salt of the compound or a solvate thereof, which can expand hematopoietic stem cells and/or hematopoietic progenitor cells.
    Type: Application
    Filed: June 4, 2010
    Publication date: May 24, 2012
    Applicant: NISSAN CHEMICAL INDUSTRIES LTD.
    Inventors: Taito Nishino, Shunsuke Iwamoto, Katsuaki Miyaji
  • Publication number: 20120129870
    Abstract: The present invention is directed to piperidinyl and piperazinyl derivatives of formula (II) useful as inhibitors of the NPY Y2 receptor, pharmaceutical compositions comprising said compounds, processes for the preparation of said compounds and the use of said compounds for the treatment and/or prevention of disorders, diseases and conditions mediated by the NPY Y2 receptor.
    Type: Application
    Filed: December 17, 2008
    Publication date: May 24, 2012
    Inventors: Wenying Chai, Jill A. Jablonowski, Dale A. Rudolph, Chandravadan R. Shah, Devin M. Swanson, Victoria D. Wong
  • Patent number: 8183239
    Abstract: The invention provides novel non-peptidic NPY Y2 receptor inhibitors useful in treating or preventing: anxiolytic disorders or depression; injured mammalian nerve tissue; conditions responsive to treatment through administration of a neurotrophic factor; neurological disorders; bone loss; substance related disorders; sleep/wake disorders; cardiovascular disease; obesity; or an obesity-related disorder. Compounds of the invention are also useful in modulating endocrine functions, particularly endocrine functions controlled by the pituitary and hypothalamic glands, and are therefore useful in the treatment or prevention of inovulation and infertility.
    Type: Grant
    Filed: October 27, 2006
    Date of Patent: May 22, 2012
    Assignee: Janssen Pharmaceutica NV
    Inventors: Pascal Bonaventure, Nicholas I. Carruthers, Wenying Chai, Curt A. Dvorak, Jill A. Jablonowski, Dale A. Rudolph, Mark Seierstad, Chandravadan R. Shah, Devin M. Swanson, Victoria D. Wong
  • Publication number: 20120101107
    Abstract: The present invention relates to piperazine dithioctate, a novel addition salt of thioctic acid with a base and a pharmaceutical composition comprising the same. The piperazine dithioctate according to the present invention has good thermal and moisture stability and high water-solubility as well as dosage increase lower than other addition salts, thereby being effectively used for preparing a pharmaceutical composition for antioxidation or for preventing or treating diabetic polyneuropathy, etc.
    Type: Application
    Filed: June 18, 2010
    Publication date: April 26, 2012
    Applicants: CELLTRION PHARM, INC., CELLTRION CHEMICAL RESEARCH INSTITUTE
    Inventors: Kyoung Soo Kim, Young Jun Park, Hyun-Nam Song, In Suk Lee, Joon Woo Kim
  • Publication number: 20120095020
    Abstract: The present invention provides a compound of Formula (I): or a pharmaceutically acceptable salt thereof. Also, the present invention provides a pharmaceutical composition comprising a compound of Formula (I) or a pharmaceutically acceptable salt thereof with a pharmaceutically acceptable diluent or carrier. The present invention further provides methods for treating abdominal aortic aneurysm, plaque instability, atherosclerosis, or autoimmune disorders such as rheumatoid arthritis, psoriasis, and lupus comprising administering a therapeutically effective amount of a compound of Formula (I) or a pharmaceutically acceptable salt thereof or a pharmaceutical composition comprising a compound of Formula (I) or pharmaceutically acceptable salt thereof and a pharmaceutically acceptable diluent or carrier.
    Type: Application
    Filed: October 14, 2011
    Publication date: April 19, 2012
    Applicant: Eli Lilly and Company
    Inventors: Gary G. DENG, Konstantinos GAVARDINAS, Prabhakar Kondaji JADHAV, Euibong Jemes KIM, Matthew Allen SCHIFFLER
  • Publication number: 20120071489
    Abstract: The present invention relates to a compound represented by the formula wherein each symbol is as defined in the present specification, which has a superior RBP4-lowering action and is useful as a pharmaceutical composition for the prophylaxis or treatment of a disease or condition mediated by an increase in RBP4.
    Type: Application
    Filed: April 16, 2010
    Publication date: March 22, 2012
    Inventors: Shizuo Kasai, Kevin Francis McGee, JR.
  • Patent number: 8106190
    Abstract: To provide a novel and excellent agent for treating or preventing nociceptive pain, neuropathic pain, cancer pain, headache, bladder function disorder and the like, based on the inhibitory action on the capsaicin receptor VR1 activation. The present invention was accomplished by confirming that a benzamide derivative characterized by the possession of a benzene ring in which a single ring is condensed on the nitrogen atom of amido group and possession of a lower alkylamino or an amino group substituted with a ring group at the neighboring position of said amido group has a strong inhibitory action on VR1 activation and excellent pharmacological actions based on this and by finding that it can become an excellent agent for treating or preventing VR1-involved diseases such as nociceptive pain, neuropathic pain, cancer pain, headache, bladder function disorder and the like.
    Type: Grant
    Filed: November 29, 2006
    Date of Patent: January 31, 2012
    Assignee: Astellas Pharma Inc.
    Inventors: Takahiro Kuramochi, Ryoji Hirabayashi, Yohei Koganemaru, Ryosuke Munakata, Koichi Yonezawa, Tetsuo Kiso
  • Publication number: 20110312931
    Abstract: The compounds of the present invention are represented by the following formula (I): wherein the substituents R1, R2, R3, R4, (R5)m, R6, A, X, and Y are as defined herein. The compounds are useful in methods of treating a disorder which is created by or is dependent upon inhibiting GlyT-1.
    Type: Application
    Filed: June 2, 2011
    Publication date: December 22, 2011
    Applicant: ALBANY MOLECULAR RESEARCH, INC.
    Inventors: Christopher L. CIOFFI, Mark A. WOLF, Peter R. GUZZO, Shuang LIU, Kashinath SADALAPURE, Visweswaran PARTHASARATHY, Jun-Ho MAENG
  • Patent number: 8067620
    Abstract: A means and method for treating malaria, schistosomiasis, and cancer using a spiro or dispiro 1,2,4-trioxolane is described. The preferred 1,2,4-trioxolanes include a spiroadamantane group on one side of the trioxolane group, and a spirocyclohexyl on the other side of the trioxolane group. In comparison to artemisinin semisynthetic derivatives, the compounds of this invention are structurally simple, easy to synthesize, non-toxic, and potent against malarial parasites. The compounds of the invention unexpectedly provide a single-dose cure for malaria, as well as prophylactic activity against the same. The compounds are also active against schistosomiasis and cancer.
    Type: Grant
    Filed: October 31, 2007
    Date of Patent: November 29, 2011
    Assignee: Medicines for Malaria Venture MMV
    Inventors: Jonathan L. Vennerstrom, Yuxiang Dong, Susan A. Charman, Sergio Wittlin, Jacques Chollet, Darren J. Creek, Xiaofang Wang, Kamaraj Spiraghavan, Lin Zhou, Hugues Matile, William N. Charman
  • Publication number: 20110256175
    Abstract: The present invention provides superior compositions and methods for the delivery of therapeutic agents to cells. In particular, these include novel lipids and nucleic acid-lipid particles that provide efficient encapsulation of nucleic acids and efficient delivery of the encapsulated nucleic acid to cells in vivo. The compositions of the present invention are highly potent, thereby allowing effective knock-down of specific target proteins at relatively low doses. In addition, the compositions and methods of the present invention are less toxic and provide a greater therapeutic index compared to compositions and methods previously known in the art.
    Type: Application
    Filed: October 9, 2009
    Publication date: October 20, 2011
    Applicants: THE UNIVERSITY OF BRITISH COLUMBIA, TEKMIRA PHARMACEUTICALS CORPORATION
    Inventors: Michael J. Hope, Sean C. Semple, Jianxin Chen, Thomas D. Madden, Pieter R. Cullis, Marco A. Ciufolini, Barbara Low Shoud Mui
  • Publication number: 20110237566
    Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain macrolide compounds (for convenience, collectively referred to herein as “MC compounds”), which, inter alia, are useful in treatment of cancer. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to treat proliferative conditions such as cancer, and in the treatment of diseases and conditions that are mediated by the regulation (e.g. inhibition) of cell proliferation, optionally in combination with another agent.
    Type: Application
    Filed: November 24, 2009
    Publication date: September 29, 2011
    Applicant: MERLION PHARMACEUTICALS PTE LTD
    Inventors: Rustum S. Boyce, Muhammad Sofian Asi Sihombing, Hiroki Sone