Patents Represented by Attorney, Agent or Law Firm Mark R. Daniel
  • Angiogenesis assay
    Patent number: 6468735
    Abstract: The present invention relates to assays and kits using porcine carotid arteries for screening compounds to identify modulators of angiogenesis. In particular, an assay for rapidly screening compounds that inhibit angiogenesis is provided.
    Type: Grant
    Filed: February 26, 2001
    Date of Patent: October 22, 2002
    Assignee: Merck & Co., Inc.
    Inventor: Janet Stiffey-Wilusz
  • Angiogenesis inhibitors
    Patent number: 6465484
    Abstract: The present invention relates to compounds which inhibit tyrosine kinase enzymes, compositions which contain tyrosine kinase inhibiting compounds and methods of using tyrosine kinase inhibitors to treat tryrosine kinase-dependent diseases/conditions such as angiogenenesis, cancer, atherosclerosis, diabetic retinopathy or autoimmune diseases, in mammals.
    Type: Grant
    Filed: February 28, 2001
    Date of Patent: October 15, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Mark T. Bilodeau, Randall W. Hungate, April M. Cunningham, Timothy J. Koester
  • Method for inhibiting bone resorption
    Patent number: 6465443
    Abstract: Disclosed are methods for inhibiting bone resorption in mammals while minimizing the occurrence of or potential for adverse gastrointestinal effects. Also disclosed are pharmaceutical compositions and kits for carrying out the therapeutic methods disclosed herein.
    Type: Grant
    Filed: March 20, 2001
    Date of Patent: October 15, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Anastasia G. Daifotis, Arthur C. Santora, II, A. John Yates
  • Cannula operated pinch valve
    Patent number: 6461345
    Abstract: There is disclosed a pinch valve for allowing access to a sterile reaction vessel using a cannula. The valve remains closed until a cannula is inserted. Upon removal of the cannula, the valve automatically closes maintaining the sterile or otherwise controlled conditions of the reaction vessel.
    Type: Grant
    Filed: November 9, 1999
    Date of Patent: October 8, 2002
    Assignee: Merck & Co., Inc.
    Inventor: Gary S. Kath
  • Radiolabeled farnesyl-protein transferase inhibitors
    Patent number: 6458935
    Abstract: The present invention is directed toward radiolabeled farnesyl-protein transferase inhibitor compounds which are useful to label FPTase in assays, whether cell-based, tissue-based or in whole animal. The tracers can also be used in competitive binding assays to obtain information on the interaction of unlabeled FTIs with FPTase.
    Type: Grant
    Filed: June 12, 2000
    Date of Patent: October 1, 2002
    Assignee: Merck & Co., Inc.
    Inventors: H. Donald Burns, Terence G. Hamill, Raymond E. Gibson
  • Estrogen receptor
    Patent number: 6458551
    Abstract: This invention relates to a novel estrogen receptor and to the polynucleotide sequences encoding this receptor. This invention also relates to methods for identifying ligands which bind to this receptor, to the ligands so identified, and to pharmaceutical compositions comprising such ligands. This invention also relates to pharmaceutical compositions useful for treating or preventing estrogen receptor mediated diseases or conditions, such as abnormal bone resorption, cardiovascular diseases, cancer, or central nervous system disorders.
    Type: Grant
    Filed: April 26, 2000
    Date of Patent: October 1, 2002
    Assignee: Merck & Co., Inc.
    Inventor: Hilary Wilkinson
  • Apparatus for gripping microplates
    Patent number: 6449827
    Abstract: An apparatus suitable for securely gripping and holding a microplate or other containers during robotic de-lidding operations. A microplate placed on the apparatus is held by a vacuum drawn through the base thereof, allowing the lid of the microplate to be removed without movement of the plate. Afterwards, the vacuum can be discontinued and the plate removed from the apparatus.
    Type: Grant
    Filed: October 10, 2000
    Date of Patent: September 17, 2002
    Assignee: Merck & Co., Inc
    Inventors: Glenn A. Clarke, Marc N. Feiglin, Gary S. Kath, Gregory W. King
  • Method for inhibiting bone resorption
    Patent number: 6432932
    Abstract: Disclosed are methods for inhibiting bone resorption in mammals while minimizing the occurrence of or potential for adverse gastrointestinal effects. Also disclosed are pharmaceutical compositions and kits for carrying out the therapeutic methods disclosed herein.
    Type: Grant
    Filed: September 2, 1999
    Date of Patent: August 13, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Anastasia G. Daifotis, Arthur C. Santora, II, A. John Yates
  • Tyrosine kinase inhibitors
    Patent number: 6420382
    Abstract: The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, inflammatory diseases, and the like in mammals.
    Type: Grant
    Filed: February 20, 2001
    Date of Patent: July 16, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Mark E. Fraley, George D. Hartman, Randall W. Hungate
  • Methods of identifying modulators of kinases responsive to stress
    Patent number: 6416964
    Abstract: The present invention relates to methods of identifying compounds useful as modulators of certain stress responsive kinases. More particularly, the compounds so identified are useful for treating or preventing diseases or conditions that are mediated by, for example, abnormal bone resorption or angiogenesis. These compounds are useful for treating or preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, and tumor growth.
    Type: Grant
    Filed: January 27, 1999
    Date of Patent: July 9, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Alfred A. Reszka, Gideon A. Rodan
  • Prolines as antimicrobial agents
    Patent number: 6417217
    Abstract: Transfer ribonucleic acid (tRNA) synthetase inhibitors, salts, and pharmaceutically acceptable compositions thereof of the general formula: wherein Ar is aryl and heteroaryl; L is —C(O)N(Q)CH2—, or —CR10R11OCR12R13—; Q is hydrido, —(CH2)mCO2H and —(CH2)mCO2CH3, m is 1, 2, 3, and 4; R1, R2, R9, R10, R11, R12 and R13 are hydrido or lower alkyl; wherein Het is a heterocyclic moiety, the inhibitors are suitable for use as antimicrobial agents.
    Type: Grant
    Filed: August 22, 2001
    Date of Patent: July 9, 2002
    Assignees: Merck & Co., Inc., Cubist Pharmaceuticals, Inc.
    Inventors: Milton L. Hammond, Aaron H. Leeman, Milana Maletic, Gina M. Santorelli, Sherman T. Waddell, John Finn, Michael Morytko, Siya Ram, Dennis Keith
  • Inhibitors of prenyl-protein transferase
    Patent number: 6413964
    Abstract: The present invention is directed to peptidomimetic macrocyclic compounds of the formula A: wherein W is a heterocycle, V is a heterocycle or aryl moiety and Z1 is a suitably substituted aryl or heterocycle moiety. The instant compounds inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.
    Type: Grant
    Filed: January 9, 2001
    Date of Patent: July 2, 2002
    Inventors: S. Jane deSolms, Suzanne C. MacTough, Anthony W. Shaw
  • Methods for inhibiting bone resorption
    Patent number: 6414006
    Abstract: The present invention relates to methods for inhibiting bone resorption in a mammal comprising administering to a mammal in need thereof a therapeutically effective amount of an EP4 receptor subtype antagonist.
    Type: Grant
    Filed: October 13, 1999
    Date of Patent: July 2, 2002
    Assignees: Merck Frosst Canada & Co., Merck & Co., Inc.
    Inventors: Shun-ichi Harada, Gideon A. Rodan, Mohamed Machwate, Marc LaBelle, Kathleen Metters, Robert N. Young
  • Inhibitors of prenyl-protein transferase
    Patent number: 6410534
    Abstract: The present invention is directed to peptidomimetic macrocyclic compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.
    Type: Grant
    Filed: June 29, 1999
    Date of Patent: June 25, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Christopher J. Dinsmore, Ian M. Bell, Douglas C. Beshore, Theresa M. Williams
  • Dry mix formulation for bisphosphonic acids
    Patent number: 6406714
    Abstract: Pharmaceutical compositions of bisphosphonic acids, and salts thereof, are prepared by direct compression/dry mix tablet formulation. These pharmaceutical compositions are useful in the treatment of disturbances involving calcium or phosphate metabolism, in particular, the treatment and prevention of diseases involving bone resorption, especially osteoporosis, Paget's disease, malignant hypercalcemia, and metastatic bone disease.
    Type: Grant
    Filed: October 17, 2000
    Date of Patent: June 18, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Simon R. Bechard, Kenneth A. Kramer, Ashok V. Katdare
  • Bishphosphonate/estrogen synergistic therapy for treating and preventing bone loss
    Patent number: 6399592
    Abstract: Disclosed is a combination therapy for treating and for preventing bone loss by the use of estrogen and a bisphosphonate selected from: alendronate, clodronate, tiludronate, YM175, BM 210995, or mixture thereof. Also described is a pharmaceutical composition of the above for carrying out the therapeutic method.
    Type: Grant
    Filed: June 23, 1997
    Date of Patent: June 4, 2002
    Assignee: Merck & Co., Inc.
    Inventor: Donna T. Whiteford
  • 1,8-naphthosultamylmethyl carbapenem antibacterial compounds, compositions containing such compounds and methods treatment
    Patent number: 6399597
    Abstract: Compounds of formula I are disclosed. as well as pharmaceutically acceptable salts thereof. The naphthosultam is substituted with various substituent groups including at least one cationic group —A—Q—L—B. The carbapenems of the invention are effective against susceptible bacterial organisms, including methicillin resistant Staphylococcus aureus (MRSA), methicillin resistant Staphylococcus epidermidis (MRSE), and methicillin resistant coagulase negative Staphylococci (MRCNS).
    Type: Grant
    Filed: March 20, 2000
    Date of Patent: June 4, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Lovji D. Cama, Ronald W. Ratcliffe, Robert R. Wilkening, Kenneth J. Wildonger, Wanying Sun
  • Process for the synthesis of carbapenem intermidiates, and compounds produced
    Patent number: 6395894
    Abstract: A process of synthesizing a compound of structural formula 6 is disclosed wherein R1 represents H or a suitable protecting group for an alcohol; R2 represents a benzyl, C1-6 alkyl or aryl; Y represents C1-3 alkyl, O, NH or S; X represents O, NH, or S and R5 represents a carboxy protecting group, comprising reacting a compound of formula 5: wherein R1, R2, R5, X and Y are as previously described with a phosphite or phosphonite reagent to produce a compound of formula 6. Further disclosed is an efficient method for the synthesis of a compound of formula 2: which comprises reacting a 4-acyl-2-azetidinone with a titanium, zirconium or hafnium enolate of a 1-hydroxy-2-butanone derivative.
    Type: Grant
    Filed: April 15, 1999
    Date of Patent: May 28, 2002
    Inventors: Philip J. Pye, Paul J. Reider, Kai Rossen, Ralph P. Volante
  • Conjugates useful in the treatment of prostate cancer
    Patent number: 6391305
    Abstract: Chemical conjugates which comprise oligopeptides, having amino acid sequences that are selectively proteolytically cleaved by free prostate specific antigen (PSA), hydrophilic oligopeptide blocking groups and known cytotoxic agents are disclosed. Such conjugates are useful in the treatment of prostatic cancer and benign prostatic hypertrophy (BPH).
    Type: Grant
    Filed: June 28, 1999
    Date of Patent: May 21, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Dong-Mei Feng, Victor M. Garsky, Raymond E. Jones, Allen I. Oliff, Jenny M. Wai
  • Inhibitors of prenyl-protein transferase
    Patent number: 6387903
    Abstract: The present invention is directed to compounds which inhibit prenyl-protein transferases, farnesyl-protein transferase and geranylgeranyl-protein transferase type I, and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and geranylgeranyl-protein transferase type I and the prenylation of the oncogene protein RAS.
    Type: Grant
    Filed: February 1, 2000
    Date of Patent: May 14, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Christopher J Dinsmore, John H. Hutchinson, Theresa M. Williams