Polycyclo Ring System Having The Five-membered Hetero Ring As One Of The Cyclos Patents (Class 548/113)
  • Patent number: 9700557
    Abstract: A pharmaceutical combination comprising (a) CDK4/6 inhibitor (b) a B-Raf inhibitor, and optionally (c) a MEK 1/2 inhibitor; combined preparations and pharmaceutical compositions thereof; the uses of such combination in the treatment of proliferative diseases; and methods of treating a subject suffering from a proliferative disease comprising administering a therapeutically effective amount of such combination.
    Type: Grant
    Filed: July 25, 2013
    Date of Patent: July 11, 2017
    Assignee: NOVARTIS AG
    Inventors: Giordano Caponigro, Darrin Stuart, Sunkyu Kim, Alice Loo, Scott Delach
  • Patent number: 9643923
    Abstract: The present invention relates to a new class of indole derivatives, having a particular MKlp2 inhibition profile and useful as a therapeutic agent, in particular for the treatment of cancer, viral infections and lung diseases.
    Type: Grant
    Filed: December 6, 2013
    Date of Patent: May 9, 2017
    Assignees: BIOKINESIS, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE
    Inventors: Cécile Bougeret, Catherine Guillou, Julien Rouleau, Julie Rivollier, Denis Carniato
  • Publication number: 20150065463
    Abstract: Benzothiazole phosphonate analogs and methods of using the same to inhibit the activity of Amyloid Binding Alcohol Dehydrogenase and in the amelioration or treatment of Alzheimer's disease are provided.
    Type: Application
    Filed: November 12, 2014
    Publication date: March 5, 2015
    Applicant: University of Kansas
    Inventors: ShiDu Yan, Koteswara Rao Valasani
  • Publication number: 20140341851
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Application
    Filed: April 4, 2014
    Publication date: November 20, 2014
    Applicant: ENANTA PHARMACEUTICALS, INC.
    Inventors: YAO-LING QIU, Ce Wang, Xiaowen Peng, Hui Cao, Lu Ying, Xuri Gao, Bin Wang, Yat Sun Or
  • Publication number: 20140296177
    Abstract: A new class of biotin protein ligase (BPL) inhibitors that have antibacterial activity against multiple Staphylococcus aureus isolates, including clinically important methicillin-resistant S. aureus (MRSA) are disclosed that are non-toxic.
    Type: Application
    Filed: September 21, 2012
    Publication date: October 2, 2014
    Inventors: Andrew Abel, Steven Polyak, Grant Booker, John Wallace, Tatiana Soares Da Costa, Angie Jarrad, William Tieu, Kelly Lee Keeling, Daniel Sejer Pederson, Nicole Pendini, Matthew Wilce, Min Yin Yap
  • Publication number: 20140290748
    Abstract: The present invention relates to an organic colorant corresponding to one of the following structures (I) or (II): eD-pi-conjugated chromophore-L-A??(I) A-L-pi-conjugated chromophore-eD??(II) in which eD represents an electron donor segment; L represents a covalent bond or a spacer segment; A represents an electron attractor segment able to form a covalent bond with a semi-conductor; the pi-conjugated chromophore comprising at least two aromatic rings, at least one of which is a thiophene, selenophene or furan type ring. The present invention relates to the use thereof as photosensitizer in a photovoltaic device and said photovoltaic device.
    Type: Application
    Filed: November 12, 2012
    Publication date: October 2, 2014
    Applicant: COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES
    Inventors: Renaud Demadrille, Yann Kervella
  • Patent number: 8846941
    Abstract: This document relates to functionalized (e.g., mono- or bi-functional) polymers (e.g., polyethylene glycol and related polymers) as well as methods and materials for making and using such functionalized polymers.
    Type: Grant
    Filed: December 13, 2011
    Date of Patent: September 30, 2014
    Assignee: QuiaPEG AB
    Inventor: Marek Kwiatkowski
  • Publication number: 20140243288
    Abstract: The present invention relates to a fused ring-containing oxazolidinone compound shown by general formula (I), a pharmaceutically acceptable salt thereof and a stereoisomer thereof, wherein R1, R2, R3, R4, R5, R6, A, B and C are as defined in the description. The present invention further relates to a method for preparing the compound, a pharmaceutical composition and a pharmaceutical formulation comprising the compound, and a use of the compound for the manufacture of a medicament for the treatment and/or prevention of infectious diseases and a use for the treatment and/or prevention of infectious diseases.
    Type: Application
    Filed: September 29, 2012
    Publication date: August 28, 2014
    Inventors: Hui Zhang, Aichen Wang
  • Publication number: 20140243287
    Abstract: The present invention relates to pyrazole derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: February 24, 2014
    Publication date: August 28, 2014
    Applicant: Allergan, Inc.
    Inventors: Janet A. Takeuchi, Ling Li, Wha Bin Im, Ken Chow
  • Publication number: 20140193363
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Application
    Filed: January 15, 2014
    Publication date: July 10, 2014
    Applicant: ENANTA PHARMACEUTICALS, INC.
    Inventors: Yao-Ling Qiu, Ce Wang, Xiaowen Peng, Lu Ying, Yat Sun Or
  • Publication number: 20140171392
    Abstract: The present invention relates to a method of treating a disease or disorder characterised by increased stress hormone levels and/or decreased androgen hormone levels in a subject, comprising administering to the subject a therapeutically effective amount of a compound represented by formula (I): wherein n is 1 or 3; R is hydrogen or —C(O)N(Ra)(Rb) wherein Ra and Rb are independently —(C1-C4) alkyl, or —(C1-C4) alkyl-(C5-C7) aryl, wherein each of Ra and Rb is optionally substituted by —(C1-C4) alkoxy; R1, R2, and R3, are independently hydrogen, halogen, cyano or —(C6-C10) aryl, wherein said —(C6-C10) aryl is optionally substituted by halogen, with the proviso that no more than one of R1, R2, and R3 is hydrogen; and R4 and R5 are hydrogen; or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: November 13, 2013
    Publication date: June 19, 2014
    Applicant: Novartis AG
    Inventors: Qi-Ying Hu, Gary Michael Ksander, Erik Meredith, Lauren G. Monovich, Julien Papillon, Christoph Schumacher
  • Publication number: 20140100194
    Abstract: The invention is directed to TRPM8 antagonists of Formula (I). More specifically, the present invention relates to certain novel compounds, methods for preparing compounds, compositions, intermediates and derivatives thereof and methods for treating TRPM8-mediated disorders. Pharmaceutical and veterinary compositions and methods of treating pain and various other disease states or conditions using compounds of the invention are also described.
    Type: Application
    Filed: December 5, 2013
    Publication date: April 10, 2014
    Applicant: Janssen Pharmaceutica, NV
    Inventors: Raymond W Colburn, Scott L. Dax, Christopher M. Flores, Jay M. Matthews
  • Publication number: 20140018320
    Abstract: There are disclosed compound of Formula (1): A1, A2, A3 and A4 which may be the same or different, represent N or CR1, X is a divalent group selected from O, S(O)n, C?W, NR4, NC(?O)R5 and CR6R7, W is O, S, NR20, Y is N or CR8, one of R4, R5, R6, R8, R9 and NR20 represents -L-R3, in which L is a single bond or a linker group, additionally, R1, R3-R9, which may be the same or different, independently represent hydrogen or a substituent and R20 represents hydrogen, hydroxyl, alkyl optionally substituted by aryl, alkoxy optionally substituted by aryl, aryl, CN, optionally substituted alkoxy, optionally substituted aryloxy, optionally substitute alkanoyl, optionally substituted aroyl, NO2, NR30R31, in which R30 and R31, which may be the same or different, represent hydrogen, optionally substituted alkyl or optionally substituted aryl; additionally, one of R30 and R31 may represent optionally substituted alkanoyl or optionally substituted aroyl, n represents an integer from 0 to 2, in addition, when an adjacent pai
    Type: Application
    Filed: July 11, 2013
    Publication date: January 16, 2014
    Applicant: Summit Corporation PLC
    Inventors: GRAHAM MICHAEL WYNNE, STEPHEN PAUL WREN, PETER DAVID JOHNSON, PAUL DAMIEN PRICE, OLIVIER DE MOOR, GARY NUGENT, RICHARD STORER, RICHARD JOSEPH PYE, COLIN RICHARD DORGAN
  • Patent number: 8629281
    Abstract: The invention is directed to TRPM8 antagonists of Formula (I). More specifically, the present invention relates to certain novel compounds, methods for preparing compounds, compositions, intermediates and derivatives thereof and methods for treating TRPM8-mediated disorders. Pharmaceutical and veterinary compositions and methods of treating pain and various other disease states or conditions using compounds of the invention are also described.
    Type: Grant
    Filed: January 14, 2011
    Date of Patent: January 14, 2014
    Assignee: Janssen Pharmaceutica, NV
    Inventors: Raymond W. Colburn, Scott L. Dax, Christopher Flores, Jay Matthews, Ning Qin, Laura Reany, Christopher Teleha, Mark A. Youngman
  • Patent number: 8552205
    Abstract: Derivatives of 6,7-dihydro-5H-imidazo[1,2-?]imidazole-3-carboxylic acid amide exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease.
    Type: Grant
    Filed: November 20, 2008
    Date of Patent: October 8, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Antonio Jose del Moral Barbosa, Jr., Joerg Martin Bentzien, Steven Richard Brunette, Zhidong Chen, Derek Cogan, Donghong A. Gao, Alexander Heim-Riether, Joshua Courtney Horan, Jennifer A. Kowalski, Michael David Lawlor, Rene Marc Lemieux, Weimin Liu, Bryan McKibben, Craig Andrew Miller, Neil Moss, Matt Aaron Tschantz, Zhaoming Xiong, Hui Yu, Yang Yu
  • Patent number: 8513219
    Abstract: The invention relates to novel and known substituted phosphonates for use in ameliorating amyloid aggregates, particularly for use in the treatment of Alzheimer's disease.
    Type: Grant
    Filed: May 2, 2008
    Date of Patent: August 20, 2013
    Assignee: Queen Mary & Westfield College, University of London
    Inventors: Alice Sullivan, Adina Michael-Titus, Lesley Robson
  • Publication number: 20130211097
    Abstract: The present disclosure relates to a new diphosphonate compound, and the method to prepare the above new diphosphonate compound. The new diphosphonate compound exhibits an activity in inhibiting osteoclast equivalent to alendronate sodium, and a higher activity in affecting the proliferation of osteoplast than the positive control compounds, but the positive control exhibits a weaker effect on osteoblast proliferation. In experimental examples, an administration schedule for the diphosphonate compound is provided.
    Type: Application
    Filed: August 24, 2011
    Publication date: August 15, 2013
    Inventors: Mingqi Li, Han Wang, Qimin Deng, Zuoyong Cheng, Maoliang Li, Yonglong Zeng, Xue Jiang, Yuchun Duan, Sanping Zhu, Dezhong Wen
  • Patent number: 8501713
    Abstract: Combinations comprising (or consisting essentially of) one or more compounds of formula (1) with one or more ancillary agents, to processes for preparing the combinations, and to various therapeutic uses of the combinations. Also provided are pharmaceutical compositions containing the combinations as well as a method of treatment of Duchenne muscular dystrophy, Becker muscular dystrophy or cachexia using the combinations.
    Type: Grant
    Filed: August 1, 2008
    Date of Patent: August 6, 2013
    Assignee: Summit Corporation PLC
    Inventors: Graham Michael Wynne, Stephen Paul Wren, Peter David Johnson, Paul Damien Price, Olivier De Moor, Gary Nugent, Richard Storer, Richard Joseph Pye, Colin Richard Dorgan
  • Publication number: 20130130289
    Abstract: The present invention provides compounds and methods for assaying redox state of metabolically active cells and methods for assaying enzyme activity and/or metabolite level by coupling to redox defining co-factor NAD(P)/NAD(P)H measurement.
    Type: Application
    Filed: August 31, 2012
    Publication date: May 23, 2013
    Applicant: PROMEGA CORPORATION
    Inventors: Helene A. BENINK, James J. CALI, Sarah DUELLMAN, Dieter KLAUBERT, Donna LEIPPE, Martha O'BRIEN, John SHULTZ, Jolanta VIDUGIRIENE, Wenhui ZHOU, Mary SOBOL
  • Publication number: 20130023495
    Abstract: The present invention relates to the use of a DGAT1 inhibitor, or a pharmaceutically acceptable salt or ester thereof, for the prevention, delay of progression or treatment of a disease or condition which is selected from chylomicronemia syndrome, familial chylomicronemia syndrome and Type V hyperlipoproteinemia. The present invention further relates to the use of a pharmaceutical composition comprising a DGAT1 inhibitor, or a pharmaceutically acceptable salt or ester thereof, for the prevention, delay of progression or treatment of a disease or condition which is selected from chylomicronemia syndrome, familial chylomicronemia syndrome and Type V hyperlipoproteinemia.
    Type: Application
    Filed: March 29, 2011
    Publication date: January 24, 2013
    Applicant: Novartis AG
    Inventors: Charles Meyers, Michael H. Serrano-Wu, Tom Thuren
  • Patent number: 8357801
    Abstract: The present invention provides dyes, reactive dyes and labeled reagents that may be used in the detection or quantification of desirable target molecules, such as proteins, nucleic acids and cellular organelles. Dyes are provided that may be used free in solution where the binding of the dye to the target molecule provides signal generation. Dyes are also provided that comprise reactive groups that may be used to attach the dyes to probes that will bind to desirable target molecules. The novel dyes of the present invention have been modified to provide beneficial properties.
    Type: Grant
    Filed: December 4, 2008
    Date of Patent: January 22, 2013
    Assignee: Enzo Life Sciences, Inc.
    Inventors: Praveen Pande, Zaiguo Li, Maciej Szczepanik, Wayne F. Patton
  • Patent number: 8329914
    Abstract: Novel compounds of the structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention are useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.
    Type: Grant
    Filed: October 22, 2009
    Date of Patent: December 11, 2012
    Assignees: Merck Sharp & Dohme Corp, Metabasas Therapeutics, Inc.
    Inventors: Jianming Bao, Ping Lan, Huagang Lu, Gergely M. Makara, F. Anthony Romero, Iyassu Sebhat, Dariusz Wodka, Qun Dang, De Michael Chung, Tony S. Gibson, Hongjian Jiang, Daniel K. Cashion
  • Publication number: 20120277190
    Abstract: Compounds of formula (I) wherein A, R1, R2, and R3 are defined in the specification, and which are useful as therapeutic compounds particularly for treating disorders or conditions associated with inflammation, pain, bladder overactivity, urinary incontinence, and other disorders caused by or exacerbated by TRPV1.
    Type: Application
    Filed: July 9, 2012
    Publication date: November 1, 2012
    Inventors: Arthur R. Gomtsyan, Erol K. Bayburt, John R. Koenig, Kennan C. Marsh, Robert G. Schmidt, JR., Chih-Hung Lee, Weili Wang, Jerome F. Daanen, Brian S. Brown
  • Publication number: 20120225846
    Abstract: Disclosed herein are new heterocyclic compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus.
    Type: Application
    Filed: March 2, 2012
    Publication date: September 6, 2012
    Applicant: BIOENERGENIX
    Inventors: John M. McCall, Donna L. Romero, Michael Clare
  • Publication number: 20120214767
    Abstract: Disclosed are compounds of Formula (I) or stereoisomers or salts thereof, wherein: X1, X2, X3, W, Q1, Q2, and G2 are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
    Type: Application
    Filed: October 29, 2010
    Publication date: August 23, 2012
    Inventors: T.G. Murali Dhar, Hai-Yun Xiao, Scott Hunter Watterson, Soo S. Ko, Alaric J. Dyckman, Charles M. Langevine, Jagabandhu Das
  • Patent number: 8221737
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Grant
    Filed: June 15, 2010
    Date of Patent: July 17, 2012
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventors: Yat Sun Or, Xiaowen Peng, Lu Ying, Ce Wang, Yao-Ling Qiu
  • Publication number: 20120178940
    Abstract: This document relates to functionalized (e.g., mono- or bi-functional) polymers (e.g., polyethylene glycol and related polymers) as well as methods and materials for making and using such functionalized polymers.
    Type: Application
    Filed: December 13, 2011
    Publication date: July 12, 2012
    Inventor: Marek Kwiatkowski
  • Patent number: 8212049
    Abstract: Disclosed is a new class of chiral bidentate ligands capable of performing asymmetric hydrogenation. Also disclosed are processes of performing asymmetric hydrogenation the chiral bidentate ligands.
    Type: Grant
    Filed: June 28, 2011
    Date of Patent: July 3, 2012
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Carl Alan Busacca, Jon Charles Lorenz
  • Publication number: 20120156691
    Abstract: Alternative methods for the detection and measurement of proteases in biological samples and compounds which allow for such detection are required to allow for rapid and selective identification of these enzymes. Compounds which allow for selective identification of these enzymes are provided with assays and kits for their use.
    Type: Application
    Filed: August 26, 2010
    Publication date: June 21, 2012
    Inventors: Stella Lorraine Martin, Brian Walker
  • Publication number: 20120129811
    Abstract: This invention relates to tricycle I and its therapeutic and prophylactic uses, wherein the variables C1, C2, Z1, Z2, Q, J, R1, and R3 are defined in the specification. Disorders treated and/or prevented include rheumatoid arthritis.
    Type: Application
    Filed: November 16, 2011
    Publication date: May 24, 2012
    Inventors: Aihua WANG, Yan Zhang, Kristi Anne Leonard, Michael Hawkins, Brett Andrew Tounge, Umar S.M. Maharoof, Joseph Kent Barbay
  • Patent number: 8163911
    Abstract: The invention relates to substituted arylsulphonylaminomethylphosphonic acid derivatives of general formula (I) wherein the groups Ra to Rf, A and Z are defined as mentioned in the specification and claims, which are suitable for preparing a medicament for the treatment of metabolic disorders, particularly type 1 or type 2 diabetes mellitus.
    Type: Grant
    Filed: September 4, 2008
    Date of Patent: April 24, 2012
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Elke Langkopf, Alexander Pautsch, Corinna Schoelch, Annette Schuler-Metz, Ruediger Streicher, Holger Wagner
  • Patent number: 8148516
    Abstract: The present invention provides compounds, methods and systems for sequencing nucleic acid using single molecule detection. Using labeled NPs that exhibit charge-switching behavior, single-molecule DNA sequencing in a microchannel sorting system is realized. In operation, sequencing products are detected enabling real-time sequencing as successive detectable moieties flow through a detection channel. By electrically sorting charged molecules, the cleaved product molecules are detected in isolation without interference from unincorporated NPs and without illuminating the polymerase-DNA complex.
    Type: Grant
    Filed: August 10, 2010
    Date of Patent: April 3, 2012
    Assignee: Pacific Biosciences of California, Inc.
    Inventors: John G. K. Williams, Gregory R Bashford, Jiyan Chen, Dan Draney, Nara Narayanan, Bambi L. Reynolds, Pamela Sheaff
  • Publication number: 20120076756
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Application
    Filed: October 4, 2011
    Publication date: March 29, 2012
    Inventors: Yao-Ling Qiu, Ce Wang, Xiaowen Peng, Lu Ying, Yat Sun Or
  • Patent number: 8134146
    Abstract: The present invention relates to heterocyclic radicals or diradicals, the dimers, oligomers, polymers, dispiro compounds and polycycles thereof, to the use thereof to organic semiconductive materials and to electronic and optoelectronic components.
    Type: Grant
    Filed: March 20, 2007
    Date of Patent: March 13, 2012
    Assignee: Novaled AG
    Inventors: Michael Limmert, Olaf Zeika, Martin Ammann, Horst Hartmann, Ansgar Werner
  • Publication number: 20120053347
    Abstract: The invention is directed to TRPM8 antagonists of Formula (I). More specifically, the present invention relates to certain novel compounds, methods for preparing compounds, compositions, intermediates and derivatives thereof and methods for treating TRPM8-mediated disorders. Pharmaceutical and veterinary compositions and methods of treating pain and various other disease states or conditions using compounds of the invention are also described.
    Type: Application
    Filed: August 31, 2010
    Publication date: March 1, 2012
    Inventors: Raymond W. Colburn, Scott L. Dax, Christopher Flores, Jay Matthews
  • Publication number: 20110294758
    Abstract: The present invention provides for novel compounds of Formulas I and II and pharmaceutically acceptable salts and co-crystals thereof which have glucokinsae activator activity. The present invention further provides for pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucokinase activator is indicated, including Type 1 and 2 diabetes, impaired glucose tolerance, insulin resistance and hyperglycemia. The present invention also provides for processes of making the compounds of Formulas I and II, including salts and co-crystals thereof, and pharmaceutical compositions comprising the same.
    Type: Application
    Filed: May 25, 2011
    Publication date: December 1, 2011
    Applicant: Metabasis Therapeutics, Inc.
    Inventors: Feng Tian, Qun Dang, G. Sridhar Prasad, Wenyu Li, Brett C. Bookser, Nicholas Brian Raffaele, Mark D. Erion
  • Publication number: 20110287031
    Abstract: Improved methods for the production, selection and inhibition of catalytic antibodies are disclosed.
    Type: Application
    Filed: April 27, 2009
    Publication date: November 24, 2011
    Inventors: Sudhir Paul, Yasuhiro Nishiyama
  • Publication number: 20110263533
    Abstract: Novel compounds of the structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention are useful in the treatment of Type 2 diabetes, hyperglycemia, Metabolic Syndrome, obesity, hypercholesterolemia, and hypertension.
    Type: Application
    Filed: October 12, 2009
    Publication date: October 27, 2011
    Inventors: Qun Dang, Tony S. Gibson, Hongjian Jiang, De Michael Chung, Jianming Bao, Jinlong Jiang, Andy Kassick, Ahmet Kekec, Ping Lan, Huagang Lu, Gergely M. Makara, F. Anthony Romero, Iyassu Sebhat, David Wilson, Dariusz Wodka, Brett C. Bookser
  • Patent number: 8026388
    Abstract: Synthesis of biphosphonate compounds can be advantageously carried out in a solvent/diluent comprising a compound of formula (3) wherein R is hydrogen or a C1-C6 alkyl group; each of R1 is a C1-C6 alkyl group or both R1 groups are linked to form a C1-C3 alkylene group; and R2 is hydrogen, a C1-C6 alkyl group, a C1-C6 alkoxy group, or is linked together with R to form a C3-C7 carbon ring.
    Type: Grant
    Filed: July 10, 2009
    Date of Patent: September 27, 2011
    Assignee: Synthon BV
    Inventor: Jiri Bartl
  • Publication number: 20110223093
    Abstract: This invention relates to sulfur functionalized ionic liquid compounds that are useful in methods of carbon dioxide or sulfur dioxide removal to which they may be applied.
    Type: Application
    Filed: March 11, 2011
    Publication date: September 15, 2011
    Applicant: E.I. DU PONT DE NEMOURS AND COMAPNY
    Inventor: MARK A. SCIALDONE
  • Publication number: 20110218174
    Abstract: Novel compounds of the structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention are useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.
    Type: Application
    Filed: October 22, 2009
    Publication date: September 8, 2011
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Jianming Bao, Ping Lan, Huagang Lu, Gergely M. Makara, F. Anthony Romero, Iyassu Sebhat, Dariusz Wodka, Qun Dang, De Michael Chung, Tony S. Gibson, Hongjian Jiang, Daniel K. Cashion
  • Publication number: 20110212923
    Abstract: The present invention relates to phosphate derivatives of estrogen receptor beta agonists, compositions thereof, preparations thereof, and uses thereof. Formula (I).
    Type: Application
    Filed: February 6, 2009
    Publication date: September 1, 2011
    Inventors: Reinhardt Baudy, Eugene J. Trybulski, Ronald Magolda, Diane Schneider, Gulnaz Khafizova, Mahdi B. Fawzi, Cuijian Yang
  • Publication number: 20110195934
    Abstract: The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable faints thereof according to wherein all of the variables are defined herein.
    Type: Application
    Filed: October 8, 2009
    Publication date: August 11, 2011
    Inventors: Pratik Devasthale, Wliiam N. Washburn, Wei Wang, Andres Hernandez, Saleem Ahmad, Guohua Zhao
  • Publication number: 20110195932
    Abstract: Combinations comprising (or consisting essentially of) one or more compounds of formula (1) with one or more ancillary agents, to processes for preparing the combinations, and to various therapeutic uses of the combinations. Also provided are pharmaceutical compositions containing the combinations as well as a method of treatment of Duchenne muscular dystrophy, Becker muscular dystrophy or cachexia using the combinations.
    Type: Application
    Filed: August 1, 2008
    Publication date: August 11, 2011
    Inventors: Graham Michael Wynne, Stephen Paul Wren, Peter David Johnson, Paul Damien Price, Olivier De Moor, Gary Nugent, Richard Storer, Richard Joseph Pye, Colin Richard Dorgan
  • Patent number: 7994335
    Abstract: Disclosed is a new class of chiral bidentate ligands capable of performing asymmetric hydrogenation. Also disclosed are processes of performing asymmetric hydrogenation the chiral bidentate ligands.
    Type: Grant
    Filed: November 20, 2007
    Date of Patent: August 9, 2011
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Carl Alan Busacca, Jon Charles Lorenz
  • Publication number: 20110077389
    Abstract: Novel CE-phosphoramidites and CPG reagents have been synthesized from a serinol backbone. These reagents are useful to introduce functional groups or directly label oligonucleotides. The versatile serinol scaffold allows for labeling at any position (5? or 3? termini, or any internal position) during automated DNA synthesis. Multiple labels or functional groups can be achieved by repetitive coupling cycles. Optimal spacer arms and protected label moieties have been specially designed. Further, the natural 3-carbon atom internucleotide phosphate distance is retained when inserted internally.
    Type: Application
    Filed: September 28, 2010
    Publication date: March 31, 2011
    Applicants: Nelson Biotechnologies, Inc., Glen Research Corporation
    Inventors: Paul S. Nelson, Hugh Mackie, Andrew Murphy
  • Patent number: 7897781
    Abstract: The invention is directed to TRPM8 antagonists of Formula (I). More specifically, the present invention relates to certain novel compounds, methods for preparing compounds, compositions, intermediates and derivatives thereof and methods for treating TRPM8-mediated disorders. Pharmaceutical and veterinary compositions and methods of treating pain and various other disease states or conditions using compounds of the invention are also described.
    Type: Grant
    Filed: May 9, 2007
    Date of Patent: March 1, 2011
    Assignee: Janssen Pharmaceutica NV
    Inventors: Raymond W. Colburn, Scott L. Dax, Christopher Flores, Jay Matthews, Ning Qin, Laura Reany, Christopher Teleha, Mark A. Youngman
  • Patent number: 7893271
    Abstract: This invention relates to benzimidazole carbamates and (thio)carbamates corresponding to Formula I: Here, X1 and X2 are independently O or S, wherein at least one of X1 and X2 is O; Y1 and Y2 are independently O or S, wherein at least one of Y1 and Y2 is O; R1 is alkyl having from 1-4 carbon atoms; R2, R3, and R4 are independently hydrogen or a cation; R5 and R6 are independently hydrogen, halogen, alkyl (having from 1-8 carbon atoms), —OR7, —SR8, —CO—R9, —OSO2—Ar, or —S(O)R10; R7 is alkyl having from 1-8 carbon atoms; R8 is alkyl (having from 1-8 carbon atoms) or aryl; R9 is alkyl (having from 1-8 carbon atoms), cycloalkyl (having from 3-6 carbon atoms), or aryl; Ar is aryl; and R10 is alkyl (having from 1-8 carbon atoms) or aryl. The compounds generally are soluble and stable in water, and have antiparasitic (particularly anthelmintic) activity in vivo that is comparable to known water-insoluble benzimidazole carbamates (e.g., albendazole and fenbendazole).
    Type: Grant
    Filed: July 18, 2006
    Date of Patent: February 22, 2011
    Assignee: Intervet International B.V.
    Inventor: Christophe Pierre Alain Chassaing
  • Publication number: 20100316607
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Application
    Filed: June 15, 2010
    Publication date: December 16, 2010
    Inventors: Yat Sun Or, Xiaowen Peng, Lu Ying, Ce Wang, Yao-Ling Qiu
  • Publication number: 20100279983
    Abstract: This invention provides novel ?-lactamase inhibitors of the aryl- and heteroarylsulfonamidomethylphosphonate monoester class having nitrogen-based cations or quarternary ammonium groups. The compounds inhibit three classes of ?-lactamases and synergize the antibacterial effects of ?-lactam antibiotics (e.g., imipenem and ceftazidime) against those micro-organisms normally resistant to the ?-lactam antibiotics as a result of the presence of the ?-lactamases. Formula (I) or pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: May 21, 2007
    Publication date: November 4, 2010
    Inventors: Frank Dininno, Milton L. Hammond, Kevin Dykstra, Seongkon Kim, Qiang Tan, Katherine Young, Jeffrey Donald Hermes, Helen Chen, Stephane Raeppel, Michael Mannion, Frederic Gaudette, Arkadii Vaisburg, Jubrail Rahil, Nafsika Georgopapadakou, Nancy Z. Zhou