Patents Represented by Attorney, Agent or Law Firm Joan E. Switzer
  • Patent number: 8329711
    Abstract: The invention relates to compounds of general formula (I-0): wherein R1, R2, R3, R4, R5, R6, R7a, R8a, X, and Y are as defined herein. Compounds of the invention have, based on excellent Wee1 kinase-inhibitory effect, a cell growth-inhibitory effect and an additive/synergistic effect with any other anticancer agent, and are therefore useful in the field of medicine.
    Type: Grant
    Filed: October 20, 2008
    Date of Patent: December 11, 2012
    Assignee: MSD K.K.
    Inventors: Hidetomo Furuyama, Mikako Kawamura, Toshihiro Sakamoto, Fuyuki Yamamoto, Takashi Yoshizumi
  • Patent number: 8288396
    Abstract: The invention is to provide a novel anticancer agent or sensitizer for cancer chemotherapy or radiotherapy. A compound of a general formula (I): wherein A means an aryl group or a heteroaryl group, or a group of a formula (a): R1 means a —(C?O)aOb(C1-C6)alkyl group, a —(C?O)aOb(C2-C6)alkenyl group, a —(C?O)aOb(C3-C6)cycloalkyl group, an aryl group or a heteroaryl group; R2 and R3 each mean a hydrogen atom, a halogen atom, a hydroxyl group, a carboxyl group, a —(C?O)aOb(C1-C6)alkyl group or a group of —(C?O)aN(R1e)R2e; R4 means a hydrogen atom or a (C1-C6)alkyl group, and the like have an excellent Wee1-kinase-inhibitory effect, and are therefore useful in the field of medicine, especially in the field of various cancer treatments.
    Type: Grant
    Filed: February 18, 2010
    Date of Patent: October 16, 2012
    Assignee: MSDKK
    Inventors: Yasuhiro Goto, Kenji Niiyama, Satoshi Sunami, Keiji Takahashi
  • Patent number: 8242103
    Abstract: Bridged bicyclic sulphamides of formula (I) are disclosed for treatment of cancer.
    Type: Grant
    Filed: May 16, 2006
    Date of Patent: August 14, 2012
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Huw David Lewis, Timothy Harrison, Mark Steven Shearman
  • Patent number: 8198281
    Abstract: The present invention relates to the crystalline forms of 2-allyl-1-[6-(I-hydroxy-1 methylethyl)pyridin-2-yl]-6-{[4-(4-methylpiperazin-1-yl)phenyl]amino}-1,2-dihydro-3H-pyrazolo[3,4-d]pyrimidin-3-one or a salt thereof, which are useful in the field of treatment of various cancers as a kinase inhibitor, especially as a Weel kinase inhibitor.
    Type: Grant
    Filed: April 22, 2008
    Date of Patent: June 12, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Masashi Kawasaki, Hiroo Mizuno, Toshihiro Sakamoto, Kimimasa Suzuki, Arlene E. McKeown
  • Patent number: 7479372
    Abstract: The present invention provides synthetic ?-secretase peptide substrates useful in various assays for measuring ?-secretase activity. Antibodies that recognize the synthetic substrates and uses of the antibodies in various assays are disclosed. The herein disclosed peptide substrates are hydrolyzed at rates substantially faster than the attendant Swedish mutant APP from which the substrate sequences are derived.
    Type: Grant
    Filed: September 19, 2006
    Date of Patent: January 20, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Stephen F. Brady, James E. Bruce, Elizabeth Chen-Dodson, Victor Garsky, Yueming Li, Mohinder Sardana, Jules A. Shafer, Xiaoting Tang
  • Patent number: 7432414
    Abstract: The present invention provides transgenic animals having an amyloid precursor protein wherein the amino acids flanking the &bgr; secretase cleavage site are NF and EV. The invention also provides tissues and cell lines derived from such animals. The invention further provides methods of screening candidate compounds to determine whether the compounds can alter the rate of cleavage of amyloid precursor protein by &bgr; secretase.
    Type: Grant
    Filed: May 28, 2004
    Date of Patent: October 7, 2008
    Assignee: Merck & Co., Inc.
    Inventors: Richard Z. Chen, Adam J. Simon, Thomas F. Vogt
  • Patent number: 7368541
    Abstract: A trace amine receptor 1 has been isolated from the genome of Cercopithecus aethiops (African green monkey). Described is the amino acid sequence of the receptor, the nucleic acid encoding the receptor, and methods for using the receptor to identify analytes that are agonists or antagonists of the receptor.
    Type: Grant
    Filed: December 1, 2005
    Date of Patent: May 6, 2008
    Assignee: Merck & Co., Inc.
    Inventors: Mark Eben Massari, Herve Schaffhauser, Satoshi Ozaki
  • Patent number: 7276206
    Abstract: Methods of identifying activators and inhibitors of voltage-gated ion channels are provided in which the methods employ electrical field stimulation of the cells in order to manipulate the open/close state transition of the voltage-gated ion channels. This allows for more convenient, more precise experimental manipulation of these transitions, and, coupled with efficient methods of detecting the result of ion flux through the channels, provides methods that are especially suitable for high throughput screening.
    Type: Grant
    Filed: July 12, 2002
    Date of Patent: October 2, 2007
    Assignee: Merck & Co., Inc.
    Inventors: Paul R. Augustine, Randal M. Bugianesi, Gary S. Kath, Owen B. McManus, Paul B. Bennett, Tina A. Garyantes, John P. Imredy
  • Patent number: 7179620
    Abstract: The gene responsible for Stargardt-like macular dystrophy has been identified, along with its normal allelic form. The mutant gene encodes a mutant protein containing a frameshift mutation, resulting in abnormal fatty acid synthesis and transport in the retina. Also disclosed are assays for Stargardt-like macular dystrophy and therapies.
    Type: Grant
    Filed: June 28, 2006
    Date of Patent: February 20, 2007
    Assignee: Merck & Co., Inc.
    Inventors: Konstantin Petrukhin, Wen Li, Kang Zhang
  • Patent number: 7157443
    Abstract: A high molecular weight polysaccharide intracellular adhesin (SAE) antigen having the general structure of poly-1,6,?-2-amidoglucopyranoside, which is variable substituted with N-acetyl and O-succinyl substituents is described. Also, a method is given for isolating this antigen from Staphylococcus aureus. The SAE can be used in a vaccine, either alone, conjugated to an immunogenic protein, and/or with an immunogenic adjuvant.
    Type: Grant
    Filed: December 6, 2002
    Date of Patent: January 2, 2007
    Assignee: Merck & Co., Inc.
    Inventors: Joseph G. Joyce, James C. Cook, III, Chitrananda Abeygunawardana, Karen M. Grimm, Craig T. Przysiecki, Robert W. Hepler, Charlotte C. Ip, Keith Roper, Qiuwei Xu, Kathrin U. Jansen, Paul M. Keller, Leslie D. Cope
  • Patent number: 7135307
    Abstract: Gamma three protease is provided, a novel aspartyl class protease that is capable of taking part in the processing of amyloid precursor protein (APP) to A? peptide. Gamma three protease may be involved in the development and/or progression of Alzheimers disease. Methods of identifying inhibitors of gamma three protease, useful in the prevention or treatment of Alzheimers disease, are disclosed.
    Type: Grant
    Filed: August 8, 2002
    Date of Patent: November 14, 2006
    Assignee: Merck & Co., Inc.
    Inventors: Ming-Chih Crouthamel, Stephen J. Gardell, Qian Huang, Ming-Tain Lai, Yueming Li
  • Patent number: 7132401
    Abstract: The present invention provides synthetic ?-secretase peptide substrates useful in various assays for measuring ?-secretase activity. Antibodies that recognize the synthetic substrates and uses of the antibodies in various assays are disclosed. The herein disclosed peptide substrates are hydrolyzed at rates substantially faster than the attendant Swedish mutant APP from which the substrate sequences are derived.
    Type: Grant
    Filed: May 17, 2002
    Date of Patent: November 7, 2006
    Assignee: Merck & Co., Inc.
    Inventors: Stephen F. Brady, James E. Bruce, Elizabeth Chen-Dodson, Victor Garsky, Yueming Li, Mohinder Sardana, Jules A. Shafer, Xiaoting Tang
  • Patent number: 7091005
    Abstract: The gene responsible for Stargardt-like macular dystrophy has been identified, along with its normal allelic form. The mutant gene encodes a mutant protein containing a frameshift mutation, resulting in abnormal fatty acid synthesis and transport in the retina. Also disclosed are assays for Stargardt-like macular dystrophy and therapies.
    Type: Grant
    Filed: May 11, 2001
    Date of Patent: August 15, 2006
    Assignee: Merck & Co., Inc.
    Inventors: Konstantin Petrukhin, Wen Li, Kang Zhang
  • Patent number: 7029868
    Abstract: Methods of identifying inhibitors of the fusion of two types of cells, particularly when fusion is mediated by the interaction of a viral protein and such cellular proteins as CD4 and chemokine receptors, are disclosed. The methods are suitable for identifying substances that are useful for the treatment and prevention of viral diseases. Particularly preferred methods are useful for the identification of inhibitors of HIV-1 infection.
    Type: Grant
    Filed: February 13, 2001
    Date of Patent: April 18, 2006
    Assignee: Merck & Co., Inc.
    Inventors: Kathleen A. Sullivan, Diana Benincasa, Margaret A. Cascieri, Lyndon J. Mitnaul, Lin-Lin Shiao, Michael R. Tota
  • Patent number: 6641807
    Abstract: Helper dependent adenoviral vectors encoding erythropoietin (epo) provide high levels of epo to achieve a long-term therapeutically effective dosage, and allow for repeat administration to patients with disorders such as anaemia of Chronic Renal Failure (CFR), anaemias due to beta-thalassaemia, and sickle cell anaemia (SCA).
    Type: Grant
    Filed: April 23, 2001
    Date of Patent: November 4, 2003
    Assignee: Merck & Co., Inc.
    Inventors: Rocco Savino, Gennaro Ciliberto, Nicola La Monica
  • Patent number: 6605753
    Abstract: The present invention provides mice that have had their PTP-1B genes disrupted by targeted homologous recombination. The mice have no detectable PTP-1B protein, yet appear to be physiologically normal. However, in the fed state on a normal diet, the mice have half the level of circulating insulin as their wild-type littermates. In glucose and insulin tolerance tests, the mice show an increased insulin sensitivity. When fed a high fat, high carbohydrate diet, the mice show a resistance to weight gain as compared to their wild-type littermates. Methods making the mice and cell lines derived from the mice are also provided. The present invention also provides methods of identifying inhibitors of the enzymatic activity of PTP-1B as well as inhibitors identified by such methods.
    Type: Grant
    Filed: January 23, 2001
    Date of Patent: August 12, 2003
    Assignees: Merck & Co., Inc., McGill University
    Inventors: Brian Kennedy, Paul Payette, Michael Gresser, Chidambaram Ramachandran, Michel Tremblay, Mounib Elchebly
  • Patent number: 6518052
    Abstract: The present invention provides a nucleic acid and amino acid sequence of a human Pif-1 type helicase. The invention also provides methods of screening for compounds that modulate the activity of human Pif-1 type helicase, as well as methods for affecting viability of a cell by contacting the cell with a human Pif-1 helicase modulator. Such contacting specifically increases or decreases the specific activity of the human helicase in the cell, and may affect its viability, by affecting telomere length regulatory processes.
    Type: Grant
    Filed: October 22, 1999
    Date of Patent: February 11, 2003
    Assignee: Bristol-Myers Squibb Company
    Inventor: Roberto Weinmann
  • Patent number: 6472510
    Abstract: The present invention relates to a counter-receptor, termed CD40CR, for the CD40 B-cell antigen, and to soluble ligands for this receptor, including fusion molecules comprising at least a portion of CD40 protein. It is based, at least in part, on the discovery that a soluble CD40/immunoglobulin fusion protein was able to inhibit helper T-cell mediated B-cell activation by binding to a novel 39 kD protein receptor on helper T-cell membranes. The present invention provides for a substantially purified CD40CR receptor; for soluble ligands of CD40CR, including antibodies as well as fusion molecules comprising at least a portion of CD40 protein; and for methods of controlling B-cell activation which may be especially useful in the treatment of allergy or autoimmune disease.
    Type: Grant
    Filed: November 14, 1994
    Date of Patent: October 29, 2002
    Assignee: Bristol-Myers Squibb Company
    Inventors: Alejandro A. Aruffo, Jeffrey A. Ledbetter, Ivan Stamenkovic, Randolph Noelle
  • Patent number: 6465424
    Abstract: The present invention relates to compositions that inhibit the proliferation and migration of endothelial cells. The compositions contain a pre-activation domain (“PAD”) from plasminogen, or a biologically active fragment thereof, and at least one kringle region from plasminogen, or a biologically active portion thereof. The compositions are useful to treat angiogenic associated disorders.
    Type: Grant
    Filed: January 17, 2000
    Date of Patent: October 15, 2002
    Assignee: Bristol-Myers Squibb Company
    Inventors: Mohammad Eghtedarzadeh Kondri, Richard-Weidong Ji, Pamela A. Trail
  • Patent number: 6413514
    Abstract: A method for the treatment of T cell mediated disorders is described. The method involves administering to a subject a therapeutically effective amount of an anti-human CD40 antibody. Disease states suitable for treatment with this method include graft versus host disease and transplant rejection and auto immune disease such as type I diabetes, psoriasis, multiple sclerosis, rheumatoid arthritis, systemic lupus erythematosus, and myesthenia gravis.
    Type: Grant
    Filed: December 17, 1999
    Date of Patent: July 2, 2002
    Assignee: Bristol-Myers Squibb Company
    Inventors: Alejandro A. Aruffo, Diane Hollenbaugh, Anthony W. Siadak, Karen K. Berry, Linda Harris, Barbara A. Thorne, Jurgen Bajorath