Patents Represented by Attorney, Agent or Law Firm Mark R. Daniel
  • Inhibitors of prenyl-protein transferase
    Patent number: 6380228
    Abstract: The present invention is directed to peptidomimetic 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: April 6, 2001
    Date of Patent: April 30, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Craig A. Stump, Theresa M. Williams
  • Angiogenesis inhibitors
    Patent number: 6380203
    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 tyrosine kinase-dependent diseases/conditions such as angiogenesis, cancer, atherosclerosis, diabetic retinopathy or autoimmune diseases, in mammals.
    Type: Grant
    Filed: November 18, 1999
    Date of Patent: April 30, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Mark T. Bilodeau, Mark E. Fraley, Randall W. Hungate, Richard L. Kendall, Ruth Rutledge, Kenneth A. Thomas, Jr., Robert Rubino
  • DNA encoding monkey gonadotropin releasing hormone receptor
    Patent number: 6380375
    Abstract: The monkey GnRH receptor has been isolated, cloned and sequenced. The monkey GnRH receptor may be used to screen and identify compounds which bind to the GnRH receptor. Such identified compounds may be used in the treatment of sex hormone related conditions such as endometriosis, uterine fibroids, polycystic ovarian disease, hirsutism, precocious puberty, gonadal steroid-dependent neoplasias such as cancers of the prostate, breast and ovary, gonadotrophe pituitary adenomas, sleep apnea, irritable bowel syndrome, premenstrual syndrome and benign prostatic hypertrophy. The receptor proteins and polypeptides, nucleic acids, cells and assays of this invention are useful in drug screening and development, diagnosis and therapeutic applications.
    Type: Grant
    Filed: February 10, 2000
    Date of Patent: April 30, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Jisong Cui, Jane-Ling Lo, George R. Mount
  • Inhibitors of prenyl-protein transferase
    Patent number: 6376496
    Abstract: The present invention comprises piperazine-containing compounds which inhibit prenyl-protein transferases, including farnesyl-protein transferase and geranylgeranyl-protein transferase type I. Such therapeutic compounds are useful in the treatment of cancer.
    Type: Grant
    Filed: March 1, 2000
    Date of Patent: April 23, 2002
    Assignee: Merck & Co., Inc.
    Inventors: George D. Hartman, William C. Lumma, Jr., John T. Sisko, Anthony M. Smith, Thomas J. Tucker, Jeffrey M. Bergman
  • Inhibitors of prenyl-protein transferase
    Patent number: 6358985
    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: March 19, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Neville J. Anthony, Ian M. Bell, Douglas C. Beshore, Terrence M. Ciccarone, S. Jane de Solms, Christopher J. Dinsmore, Gerald E. Stokker
  • Inhibitors of prenyl-protein transferase
    Patent number: 6358956
    Abstract: The present invention comprises piperazine-containing compounds which inhibit prenyl-protein transferases, including-farnesyl-protein transferase and geranylgeranyl-protein transferase type I. Such therapeutic compounds are useful in the treatment of cancer.
    Type: Grant
    Filed: March 1, 2000
    Date of Patent: March 19, 2002
    Assignee: Merck & Co., Inc.
    Inventors: George D. Hartman, William C. Lumma, Jr., John T. Sisko, Anthony M. Smith, Thomas J. Tucker, Gerald E. Stokker
  • Salt form of a conjugate useful in the treatment of prostate cancer
    Patent number: 6355611
    Abstract: The present invention is directed to the sodium salt of formula 5: which may be useful in the treatment of prostate cancer and benign prostatic hyperplasia. Also described are lyophilized formulations that comprise the sodium salt 5 or the corresponding free acid.
    Type: Grant
    Filed: October 27, 2000
    Date of Patent: March 12, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Shyam B. Karki, Mark Cameron, David R. Lieberman, Joseph E. Lynch, Michael A. Robbins, Yao-Jun Shi, Örn Almarsson, Michael J. Kaufman, Maneesh J. Nerurkar
  • Inhibitors of prenyl-protein transferase
    Patent number: 6355643
    Abstract: The present invention comprises unsubstituted and substituted piperazine-containing compounds having alkanoyl, alkylsulfonyl, alkylamido or alkoxycarbonyl substituents, and having the formula A, which inhibit prenyl-protein transferases. In particular, the invention relates to prenyl-protein transferase inhibitors which are efficacious in vivo as inhibitors of geranylgeranyl-protein transferase type I (GGTase-I) and that inhibit the cellular processing of both the H-Ras protein and the K4B-Ras protein. Such therapeutic compounds are useful in the treatment of cancer.
    Type: Grant
    Filed: March 1, 2000
    Date of Patent: March 12, 2002
    Assignee: Merck & Co., Inc.
    Inventors: William C. Lumma, John T. Sisko, Anthony M. Smith, Thomas J. Tucker, Christopher J. Dinsmore, Jeffrey M. Bergman
  • Asymmetric conjugate addition reaction
    Patent number: 6353110
    Abstract: This invention relates to a key intermediate in the synthesis of an endothelin antagonist the synthesis of this key intermediate via an asymmetric conjugate addition reaction.
    Type: Grant
    Filed: November 24, 1999
    Date of Patent: March 5, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Paul N. Devine, Richard D. Tillyer, Richard M. Heid, Jr., David M. Tschaen
  • Synthesis of substituted prolines
    Patent number: 6350882
    Abstract: The instant invention is directed to a process for synthesizing substituted prolines, in particular, optically pure substituted prolines, which comprises the steps of: a) adding an unsubstituted or substituted proline alkali salt and an alkali halide to a solution of dialkylacylamidomalonate; and b) adding &agr;, &bgr; unsaturated aldehyde to produce an adduct.
    Type: Grant
    Filed: May 5, 2000
    Date of Patent: February 26, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Khateeta Emerson, Guo-Jie Ho
  • Inhibitors of prenyl-protein transferase
    Patent number: 6350755
    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: January 9, 2001
    Date of Patent: February 26, 2002
    Assignee: Merck & Co., Inc.
    Inventors: S. Jane deSolms, Anthony W. Shaw
  • Catechols as antimicrobial agents
    Patent number: 6348482
    Abstract: Compounds, pharmaceutically acceptable salts, and compositions thereof of the general formula: wherein Ar is aryl and heteroaryl; R1, R2, R3, and R4 are hydrido, alkyl, cyano, heteroaryl, hydroxy, amino, acylamino, halo, alkoxy, aryloxy, carboxyamido, alkenyl, cycloalkyl, heterocyclyl, acyl, acyloxy, carboalkoxy, carboxy, thio, sulfinyl, sulfonyl and sulfoxy, R5, R6, R7, and R8 are hydrido and lower alkyl; and Het is a nitrogen-containing heterocyclic ring.
    Type: Grant
    Filed: May 5, 2000
    Date of Patent: February 19, 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, Jason Hill, Dennis Keith
  • Carbapenem antibacterial compounds, compositions containing such compounds and methods of treatment
    Patent number: 6346525
    Abstract: Compounds of formula I: as well as pharmaceutically acceptable salts thereof and compositions useful as carbapenem antibacterial agents are disclosed.
    Type: Grant
    Filed: June 23, 1999
    Date of Patent: February 12, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Timothy A. Blizzard, Ronald W. Ratcliffe, Sherman T. Waddell, Jerry D. Morgan, II
  • Crystalline 2-hydroxymethyl carbapenem intermediate compounds and process for synthesis thereof
    Patent number: 6346617
    Abstract: A process for preparation of a compound of formula I: wherein: R1 represents CH3 or H; and P represents a protecting group; comprising reacting a compound of formula IV:  wherein R1 and P and are defined above and R4 represents triflate or SO2F; in the presence of a catalyst and (R3)3SnCH2OP″, wherein each R3 represents C1-4 lower alkyl, and P″ represents H or a protecting group, to yield the compound of formula I.
    Type: Grant
    Filed: June 16, 1999
    Date of Patent: February 12, 2002
    Assignee: Merck & Co., Inc.
    Inventors: John Y. Chung, Nobuyoshi Yasuda, Johnnie L. Leazer, Jr., Mark S. Jensen, Kenneth M. Wells, Chunhua Yang
  • Carbapenem antibacterial compounds, compositions containing such compounds and methods of treatment
    Patent number: 6346526
    Abstract: Compounds of formula I: as well as pharmaceutically acceptable salts thereof useful as carbapenem antibacterial agents are disclosed wherein X is CH2 or C═O.
    Type: Grant
    Filed: June 23, 1999
    Date of Patent: February 12, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Timothy A. Blizzard, Kevin D. Dykstra, Ronald W. Ratcliffe
  • Inhibitors of prenyl-protein transferase
    Patent number: 6335343
    Abstract: The present invention comprises piperazine/piperazinone-containing compounds having multicyclic ring system substituents on one of the piperazine/piperazinone nitrogens, which inhibit prenyl-protein transferases, including farnesyl-protein transferase and geranylgeranyl-protein transferase type I. Such therapeutic compounds are useful in the treatment of cancer.
    Type: Grant
    Filed: March 1, 2000
    Date of Patent: January 1, 2002
    Assignee: Merck & Co., Inc.
    Inventors: William C. Lumma, Jr., Anthony M. Smith, John T. Sisko
  • Prolines as antimicrobial agents
    Patent number: 6333344
    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: May 5, 2000
    Date of Patent: December 25, 2001
    Assignees: Merck & Co., 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
  • Process of synthesizing binaphthyl derivatives
    Patent number: 6333435
    Abstract: A process of synthesizing a compound of the formula 1: is disclosed, which comprises reacting a compound of the formula 2: with diphenylphosphine in the presence of an amine base and a nickel catalyst to produce a compound of formula 1.
    Type: Grant
    Filed: May 18, 1995
    Date of Patent: December 25, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Dongwei Cai, David L. Hughes, Sylvain Levac, Thomas R. Verhoeven
  • Phenyl-protein transferase inhibitors
    Patent number: 6333335
    Abstract: The present invention is directed to tetrahydro-imidazopyridinyl 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 30, 2000
    Date of Patent: December 25, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Christopher J. Dinsmore, Samuel L. Graham, Theresa M. Williams
  • Inhibitors of prenyl-protein transferase
    Patent number: 6329376
    Abstract: The present invention is directed to peptidomimetic piperazine-containing macrocyclic compounds which inhibit a prenyl-protein transferase (FTase) 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: October 26, 1999
    Date of Patent: December 11, 2001
    Assignee: Merck & Co., Inc.
    Inventor: Jeffrey M. Bergman