Patents Represented by Attorney, Agent or Law Firm Mark R. Daniel
  • Renin inhibitors containing phenylalanyl-histidine replacements
    Patent number: 5037807
    Abstract: Peptides of the formula: ##STR1## which comprise novel elements replacing the Phe(8)-His(9) sequence in renin-inhibitory peptides based on substrate analogy, which inhibit the substrate-cleaving action of renin and have improved bioavailability; compositions containing these renin-inhibitory peptides, optionally with other antihypertensive agents; and methods of treating hypertension or congestive heart failure or of establishing renin as a causative factor in these problems which employ the novel peptides.
    Type: Grant
    Filed: March 8, 1989
    Date of Patent: August 6, 1991
    Assignee: Merck & Co., Inc.
    Inventors: Arthur A. Patchett, William J. Greenlee, William H. Parsons, Prasun K. Chakravarty
  • Di- or tripeptide renin inhibitors containing lactam conformational restriction in achpa
    Patent number: 5006511
    Abstract: Enzyme di- or tripeptides of the formula: ##STR1## and analogs thereof which inhibit renin and are useful for treating various forms of renin-associated hypertension, hyperaldosteronism and congestive heart failure; compositions containing these renin-inhibitory peptides, optionally with other antihypertensive agents; and methods of treating hypertension, hyperaldosteronism or congestive heart failure or of establishing renin as a causative factor in these problems which employ these novel peptides.
    Type: Grant
    Filed: August 26, 1988
    Date of Patent: April 9, 1991
    Assignee: Merck & Co., Inc.
    Inventors: William J. Greenlee, Daniel F. Veber, Peter D. Williams
  • Di- or tripeptide renin inhibitors containing lactam conformational restriction in ACHPA
    Patent number: 5001113
    Abstract: Enzyme di- or tripeptides of the formula: ##STR1## and analogs thereof which inhibit renin and are useful for treating various forms of renin-associated hypertension, hyperaldosteronism and congestive heart failure; compositions containing these renin-inhibitory peptides, optionally with other antihypertensive agents; and methods of treating hypertension, hyperaldosteronism or congestive heart failure or of establishing renin as a causative factor in these problems which employ these novel peptides.
    Type: Grant
    Filed: March 7, 1990
    Date of Patent: March 19, 1991
    Assignee: Merck & Co., Inc.
    Inventors: Peter D. Williams, Daniel E. Veber
  • Parathyroid hormone antagonists with enhanced metabolic properties
    Patent number: 5001223
    Abstract: The present invention relates to the use of peptide hormone analogues as inhibitors of their respective naturally occurring peptide hormone. The structure of the peptide hormone analogues is exemplified by parathyroid hormone wherein Phe.sup.7 is substituted by NMePhe, D-Phe, desamino Phe, or Met.sup.8 is substituted by NMeMet.
    Type: Grant
    Filed: March 2, 1989
    Date of Patent: March 19, 1991
    Assignee: Merck & Co., Inc.
    Inventors: Michael Rosenblatt, Lynn H. Caporale, Michael Chorev
  • Renin-inhibitory pepstatin phenyl derivatives
    Patent number: 4980283
    Abstract: A phenyl derivative of pepstatin A, which is much more potent than pepstatin in inhibiting renin enzyme activity and has significantly greater selectivity for renin over pepsin inhibition than does pepstatin, which is useful in treating hypertension and congestive heart failure.
    Type: Grant
    Filed: June 2, 1989
    Date of Patent: December 25, 1990
    Assignee: Merck & Co., Inc.
    Inventors: Leeyuan Huang, Joseph Dunn, Jr., Lawrence Koupal, Jerrold Liesch, Otto Hensens, H. Boyd Woodruff
  • Parathyroid hormone antagonists
    Patent number: 4968669
    Abstract: The present invention relates to the use of peptide hormone analogues as inhibitors of their respective naturally occurring peptide hormone. The structure of the peptide hormone analogues is exemplified by parathyroid hormone wherein Gly.sup.12 is substituted by D-Trp, L-Trp, L- or D- alpha- or beta-naphthylalanine, or D- or L- alpha-MeTrp.
    Type: Grant
    Filed: April 21, 1989
    Date of Patent: November 6, 1990
    Assignee: Merck & Co., Inc.
    Inventors: Michael Rosenblatt, Michael Chorev
  • L-654,040, antibacterial agent
    Patent number: 4963569
    Abstract: L-654,040 of the structure: ##STR1## is a novel antibacterial and isolated from the novel organism Streptoverticillium synroense, strain MA6011, deposited at the ATCC.
    Type: Grant
    Filed: June 9, 1989
    Date of Patent: October 16, 1990
    Assignee: Merck & Co., Inc.
    Inventors: Sara A. Currie, Thomas W. Miller, Eugene L. Dulaney, James P. Springer, Mary E. Valiant, Sagrario Mochales del Val, Sheldon B. Zimmerman
  • Process for producing L-654,040, antibacterial agent
    Patent number: 4960698
    Abstract: L-654,040 of the structure: ##STR1## is a novel antibacterial and isolated from the novel organism Streptoverticillium synroense, strain MA6011, deposited at the ATCC.
    Type: Grant
    Filed: May 9, 1989
    Date of Patent: October 2, 1990
    Assignee: Merck & Co., Inc.
    Inventors: Sara A. Currie, Thomas W. Miller, Eugene L. Dulaney, James P. Springer, Mary E. Valiant, Sagrario M. del Val, Sheldon B. Zimmerman
  • Culture of Streptoverticillium synroense for producing an antibacterial
    Patent number: 4956294
    Abstract: The novel organism Streptoverticillium synroense, strain MA6011, deposited at the ATCC under Accession No.
    Type: Grant
    Filed: May 9, 1989
    Date of Patent: September 11, 1990
    Assignee: Merck & Co., Inc.
    Inventors: Sara A. Currie, Thomas W. Miller, Eugene L. Dulaney, James P. Springer, Mary E. Valiant, Sheldon B. Zimmerman, Sagrario M. Del Val
  • Chimeric cloning vectors for use in streptomyces and E. Coli
    Patent number: 4752574
    Abstract: The present invention discloses chimeric plasmid SCP2 and SCP2* cloning vectors that are useful in Streptomyces and E. coli. The invention further discloses transformants and a method for detecting transformants of the aforementioned vectors.
    Type: Grant
    Filed: April 30, 1987
    Date of Patent: June 21, 1988
    Assignee: Eli Lilly and Company
    Inventors: Charles L. Hershberger, Jeffrey L. Larson
  • Method, vectors and transformants for high expression of heterologous polypeptides in yeast
    Patent number: 4745057
    Abstract: Disclosed are a novel method for inducing the high expression of a nucleotide sequence which is under the transcriptional and translational control of the yeast YG100 gene and the novel vectors, transformants and selectable DNA for the practice thereof.
    Type: Grant
    Filed: August 13, 1984
    Date of Patent: May 17, 1988
    Assignee: Eli Lilly and Company
    Inventors: Cheryl A. Beckage, Thomas D. Ingolia
  • Transcription terminators
    Patent number: 4710464
    Abstract: The present transcription terminators are DNA sequences characterized by their ability to terminate the transcription of DNA sequences. The present sequences are portable, have a variety of restriction endonuclease sites and are useful in controlling the expression in hosts of DNA sequences coding for prokaryotic, eukaryotic and viral proteins and polypeptides.
    Type: Grant
    Filed: September 27, 1984
    Date of Patent: December 1, 1987
    Assignee: Eli Lilly and Company
    Inventors: Ramamoorthy Belagaje, Stuart A. Kuhstoss, R. Nagaraja Rao
  • Des-proline-N-methylarginine vasopressins
    Patent number: 4687758
    Abstract: Peptides having vasopressin antagonist activity are prepared by a peptide synthesizer to insert a N-methylarginine at the 7-position of the structure. An example of this series of compounds is [1-(.beta.-mercapto-.beta.,.beta.-cyclopentamethylenepropionic acid)-2-(O-ethyl-D-tyrosine)-4-valine-7-desproline-8-N-methylarginine-9-de sglycine]-vasopressin.
    Type: Grant
    Filed: November 19, 1985
    Date of Patent: August 18, 1987
    Assignee: SmithKline Beckman Corporation
    Inventors: Fadia E. Ali, William F. Huffman, Garland R. Marshall, Michael L. Moore
  • Polypeptide intermediates
    Patent number: 4684716
    Abstract: 2- or 3-.beta.-Indolylalanyl and .beta.-indolylglycyl vasopressins are prepared by standard peptide synthetic methods. These 2- or 3-TRP vasopressins have vasopressin antagonist activity.
    Type: Grant
    Filed: April 16, 1986
    Date of Patent: August 4, 1987
    Assignee: SmithKline Beckman Corporation
    Inventor: Nelson C. Yim
  • Compositions and methods for producing vasodilation and antioxytocic activity
    Patent number: 4684622
    Abstract: Vasopressin derivatives having V.sub.1 and oxytocin antagonist activity whose structures are characterized by a Mpa unit at position 1 and a des-Pro unit at position 7 are prepared by standard peptide synthetic methods also using an oxidative cyclization of a dimercaptan. Representative species are [1-deaminopenicillamine-2-(O-methyl)-tyrosine-7-desproline-8-arginine-9-de sglycine]vasopressin or [1-.beta.-mercaptopropionic acid-2-D-(O-ethyl)tyrosine-3-isoleucine-4-threonine-7-desproline-8-arginin e-9-desglycine]-vasopressin.
    Type: Grant
    Filed: April 18, 1986
    Date of Patent: August 4, 1987
    Assignee: SmithKline Beckman Corporation
    Inventors: Fadia E. Ali, William F. Huffman
  • Methods of producing vasodilation or antioxytocic activity
    Patent number: 4684621
    Abstract: Certain vasopressin-like peptides, which have an acyclic unit at position 1 and which have an .omega.-amino- or guanidinoalkyl substituent attached to the cysteine in the 6-position of the ring, have V.sub.1 -vasopressin and oxytocin antagonist activity. A species of this series of new compounds is [1-desaminopenicillamine-2-(O-ethyl-D-tyrosine)-8-(1,4-diaminobutane)-9-de sglycinamide]-vasopressin.
    Type: Grant
    Filed: April 16, 1986
    Date of Patent: August 4, 1987
    Assignee: SmithKline Beckman Corporation
    Inventors: James F. Callahan, William F. Huffman, Michael L. Moore, Nelson C. Yim
  • Feed compositions containing 2-(.alpha.-pyridyl)-.DELTA..sup.2 -heterocyclic compounds
    Patent number: 4680304
    Abstract: Selected 2-(.alpha.-pyridyl)-.DELTA..sup.2 -heterocyclic compounds are used as active ingredients in animal feed compositions and in methods for increasing the growth or feed efficiency of monogastric animals. An active ingredient for use in this invention is 3,4-dihydro-4-hydroxy-5-(3-hydroxy)-2-pyridinyl)-4-methyl-2H-pyrrole-5-car boxamide.
    Type: Grant
    Filed: March 12, 1985
    Date of Patent: July 14, 1987
    Assignee: SmithKline Beckman Corporation
    Inventors: Govind K. Menon, Winfred J. Sanders
  • Chemical process
    Patent number: 4677228
    Abstract: This invention relates to a Friedel-Crafts acylation process using trichlorobenzene as solvent.
    Type: Grant
    Filed: February 7, 1986
    Date of Patent: June 30, 1987
    Assignee: Smith Kline & French Laboratories, Ltd.
    Inventor: Brian M. Adger
  • Heterocyclic compounds having inotropic activity
    Patent number: 4657906
    Abstract: This invention relates to 5-(phenyl)-2(1H)-pyrazinones substituted in the 4-position of the phenyl ring by an amino or acylamino group. These compounds has inotropic activity. One specific compound is 5-(4-acetamidophenyl)-2(1H)-pyrazinone.
    Type: Grant
    Filed: September 19, 1985
    Date of Patent: April 14, 1987
    Assignee: Smith Kline & French Laboratories Ltd.
    Inventors: John C. Emmett, Robert A. Slater, Brian H. Warrington
  • 6-(cyanoguanidinophenyl)pyridazinones as cardiac stimulants
    Patent number: 4654342
    Abstract: This invention relates to cyanoguanidine derivatives that have utility in the treatment of congestive heart failure. A specific compound of this invention is 6-[4-(N.sup.3 -methyl-N.sup.2 -cyanoguanidino)phenyl]-5-methyl-4,5-dihydro-3(2H)-pyridazinone.
    Type: Grant
    Filed: January 14, 1985
    Date of Patent: March 31, 1987
    Assignee: Smith Kline & French Laboratories Ltd.
    Inventor: Robert A. Slater