Patents Examined by Lester L. Lee
  • 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
  • Patent number: 5036054
    Abstract: The invention concerns novel renin-inhibitory peptides which contain novel amino acids having an .alpha.-heteroatom attached to the backbone of the amino acid. These novel amino acids are positioned at the P.sub.2 position of the peptide. These are useful for treating renin-associated hypertension, hyperaldosteronism, and congestive heart failure. Processes for preparing the peptides, compositions containing them and methods of using them are included. Novel intermediates are also disclosed. Also included is a diagnostic method which uses the compounds to determine the presence of renin-associated hypertension or hyperaldosteronism.
    Type: Grant
    Filed: June 6, 1988
    Date of Patent: July 30, 1991
    Assignee: Warner-Lambert Company
    Inventors: James S. Kaltenbronn, Joseph T. Repine
  • Patent number: 5036053
    Abstract: The invention concerns novel renin-inhibitory peptides which are useful for treating renin-associated hypertension, congestive heart failure, hyperaldosteronism, and diseases caused by retroviruses including HTLV-I and -III. Processes for preparing the peptides, composition containing them, and methods of using them are included. Also included is a diagnostic method which uses the compounds to determine the presence of renin-associated hypertensions, or hyperaldosteronism.
    Type: Grant
    Filed: March 15, 1989
    Date of Patent: July 30, 1991
    Assignee: Warner-Lambert Company
    Inventors: Richard Himmelsbach, John C. Hodges, James S. Kaltenbronn, William C. Patt, Joseph T. Repine, Ila Sircar
  • Patent number: 5034376
    Abstract: Polypeptides and derivatives thereof containing nor-statine and nor-cyclostatine are useful for inhibiting the angiotensinogen-cleaving action of the enzyme renin.
    Type: Grant
    Filed: March 21, 1990
    Date of Patent: July 23, 1991
    Assignee: Pfizer Inc.
    Inventors: Dennis J. Hoover, Robert L. Rosati, Ronald T. Wester
  • Patent number: 5034227
    Abstract: A process for preparing products from legumes which comprises preparing an aqueous suspension containing finely ground seed from peas or beans, at a pH within the range of about 2.0 to 10.0, subjecting the suspension to one or more centrifugation operations and isolating therefrom at least one product containing essentially the protein content of the seed and another product containing essentially the starch content of the seed. A good quality fibrous by-product may also be isolated. The products are useful in the food industry.
    Type: Grant
    Filed: June 3, 1988
    Date of Patent: July 23, 1991
    Assignee: James Richardson & Sons Limited
    Inventor: Gary B. Nickel
  • Patent number: 5034512
    Abstract: The invention concerns a novel series of renin-inhibitory branched-backbone peptides which are useful for treating renin associated hypertension, congestive heart failure, and hyperaldosteronism. Processes for preparing the peptides, compositions containing them and methods of using them are included. Also included is a diagnostic test using the compounds to determine the presence of renin-associated hypertension, congestive heart failure, or hyperaldosteronism.
    Type: Grant
    Filed: August 3, 1988
    Date of Patent: July 23, 1991
    Assignee: Warner-Lambert Company
    Inventors: James P. Hudspeth, James S. Kaltenbronn, Joseph T. Repine, Ila Sircar
  • Patent number: 5032578
    Abstract: A method is provided for inhibiting onset of or treating depression by administering an ACE inhibitor, such as captopril, fosinopril, zofenopril or ceranapril in combination with a drug that acts at serotonin receptors such as zacopride, over a prolonged period of treatment.
    Type: Grant
    Filed: September 17, 1990
    Date of Patent: July 16, 1991
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Zola P. Horovitz
  • Patent number: 5032577
    Abstract: A renin inhibiting compound of the formula: ##STR1## wherein A is a substituent; W is C.dbd.O or CHOH; U is CH.sub.2 or NR.sub.2, provided that when W is CHOH then U is CH.sub.2 ; R.sub.1 is loweralkyl, cycloalkylmethyl, benzyl, 4-methoxybenzyl, halobenzyl, (1-naphthyl)methyl, (2-naphthyl)methyl, (4-imidazoyl)methyl, (alpha,alpha)-dimethylbenzyl, 1-benzyloxyethyl, phenethyl, phenoxy, thiophenoxy or anilino; R.sub.2 is hydrogen or loweralkyl; R.sub.3 is loweralkenyl, [(alkoxy)alkoxy]alkyl, (thioalkoxy)alkyl, lowerakenyl, benzyl or heterocyclic ring substituted methyl; R.sub.4 is loweralkyl, cycloalkylmethyl or benzyl; R.sub.5 is vinyl, formyl, hydroxymethyl or hydrogen; R.sub.7 is hydrogen or loweralkyl; R.sub.8 and R.sub.9 are independently selected from OH and NH.sub.2 ; and R.sub.6 is hydrogen, loweralkyl, vinyl or arylalkyl; provided that when R.sub.5 and R.sub.7 are both hydrogen and R.sub.8 and R.sub.9 are OH, the carbon bearing R.sub.5 is of the "R" configuration and the carbon bearing R.sub.
    Type: Grant
    Filed: December 18, 1987
    Date of Patent: July 16, 1991
    Assignee: Abbott Laboratories
    Inventors: Anthony K. L. Fung, Dale J. Kempf, Jay R. Luly, Saul H. Rosenberg, Jacob J. Plattner
  • Patent number: 5030619
    Abstract: A fungicidal composition comprising a nikkomycin and an echinocandin B. Method of treating a fungal infection comprising administering therapeutically effective amounts of a combination of the nikkomycin and the echinocandin B. Composition and method are especially useful in treating infections of filamentous fungi. Combination of nikkomycin Z and cilofungin found to be synergistic against aspergillosis.
    Type: Grant
    Filed: April 16, 1990
    Date of Patent: July 9, 1991
    Assignee: Miles Inc.
    Inventor: Richard F. Hector
  • Patent number: 5028592
    Abstract: An antipyretic tripeptide, having the amino acid sequence lysine-proline-valine, and a method for utilizing the tripeptide to reduce fever and inflammation in mammals are disclosed. The tripeptide can either be isolated from natural sources or chemically synthesized. A "protected" tripeptide having greater antipyretic potency and duration of action is also disclosed. The "protected" tripeptide contains an acyl group, such as an acetyl or a dibenzyl oxy carboxyl group, at its amino terminals and is amidated or esterified at its carboxyl terminals. Further, improved antipyretic potency and direction of action can be achieved through the co-administration of copper salts with the tripeptide.
    Type: Grant
    Filed: August 5, 1988
    Date of Patent: July 2, 1991
    Inventor: James M. Lipton
  • Patent number: 5028420
    Abstract: A novel physiologically active polypeptide having antitumor activity obtained by improving human tumor necrosis factor (TNF). The amino acid sequence of the polypeptide essentially corresponds to that of human tumor necrosis factor, except that ten amino acids Nos. 1 to 10 are deleted and (Met).sub.n -Arg-Lys-Arg are added to the amino (NH.sub.2)-terminus, where n is 0 or 1. Other amino acid modifications can also be made to the polypeptide while retaining high antitumor activity. The novel polypeptide has less side effects that the natural-type TNF, particularly with respect to cytotoxicity. A a DNA fragment encoding the polypeptide, a recombinant plasmid containing the DNA fragment, a recombinant microorganism cell transformed with the plasmid, a method of producing a novel physiologically active polypeptide using the microorganism cell, and a pharmaceutical composition comprising the polypeptide as an active ingredient are also provided.
    Type: Grant
    Filed: July 26, 1988
    Date of Patent: July 2, 1991
    Assignee: Teijin Limited
    Inventors: Tsukio Masegi, Satoshi Nakamura, Kazuo Kitai, Masami Fukuoka, Kenji Yone, Arata Kato, Jun Suzuki, Noriyuki Tsunekawa, Yataro Ichikawa
  • Patent number: 5028626
    Abstract: Compounds of formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, and n have the meanings reported in the specification, processes for their preparation and pharmaceutical compositions containing them as active ingredient are described. The compounds of formula I are inhibitors of enzymatic systems and they are useful in pharmaceutical field.
    Type: Grant
    Filed: March 15, 1989
    Date of Patent: July 2, 1991
    Assignee: Zambon Group S.p.A.
    Inventors: Dario Chiarino, Angelo Carenzi, Davide Della Bella, Franco Pellacini
  • Patent number: 5028593
    Abstract: The tuftsin analog Thr-Lys-Leu-Lys has been found to have biological activity superior to that of tuftsin itself.
    Type: Grant
    Filed: August 15, 1989
    Date of Patent: July 2, 1991
    Assignee: Board of Regents, The University of Texas System
    Inventor: Kenji Nishioka
  • Patent number: 5026825
    Abstract: Disclosed are intranasal formulations comprising calcitonin and .sup..DELTA. -aminolevulinic acid in a pharmaceutically acceptable excipient.
    Type: Grant
    Filed: September 8, 1988
    Date of Patent: June 25, 1991
    Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.
    Inventors: Peter E. Grebow, Herschel H. Li, Lewis J. Klunk, Jr.
  • Patent number: 5026686
    Abstract: Novel antiviral peptides are disclosed which have a sequence of about 4 to 10 amino acids and which are substantially identical to a small portion of the cytoplasmic domain of a glycoprotein in a virus that contains a lipid-bilayer in its structure.
    Type: Grant
    Filed: February 1, 1989
    Date of Patent: June 25, 1991
    Assignee: Washington University
    Inventors: Milton J. Schlesinger, Steven P. Adams
  • Patent number: 5024994
    Abstract: The invention concerns novel renin-inhibitory peptides which are useful for treating renin-assocated hypertension, hyperaldosteronism, and congestive heart failure. Processes for preparing the peptides, compositions containing them and methods of using them are included. Also included is a diagnostic method which uses the compounds to determine the presence of renin-associated hypertension or hyperaldosteronism.
    Type: Grant
    Filed: August 17, 1988
    Date of Patent: June 18, 1991
    Assignee: Warner-Lambert Company
    Inventors: Annette M. Doherty, James P. Hudspeth, James S. Kaltenbronn, Joseph T. Repine, William H. Roark, Ila Sircar, Francis J. Tinney
  • Patent number: 5023235
    Abstract: An antioxidant system comprises at least one ascorbyl ester stabilized with at least one complexing agent and at least one thiol. The antioxidant system is usefully employed in fatty body containing compositions such as cosmetic or alimentary compositions.
    Type: Grant
    Filed: February 8, 1988
    Date of Patent: June 11, 1991
    Assignee: L'Oreal
    Inventors: Quang L. N'Guyen, Jacqueline Griat, Francois Millecamps
  • Patent number: 5023237
    Abstract: A variety of compositions suitable for use with methods for (a) reducing the formation of stomach ulcers in warm-blooded animals, (b) reducing the secretion of stomach acid in warm-blooded animals, (c) increasing the secretion of cytoprotective mucous in the stomach of warm-blooded animals, and (d) healing established stomach or intestinal ulcers in warm-blooded animals are disclosed. The compositions include glycyl-L-histidyl-L-lysine, L-lysyl-L-histidyl-glycine, L-lysyl-L-histidyl-glycine:copper(II), glycyl-L-histidyl-L-lysine:copper(II), and derivatives thereof.
    Type: Grant
    Filed: August 30, 1989
    Date of Patent: June 11, 1991
    Assignee: ProCyte Corporation
    Inventor: Loren R. Pickart
  • Patent number: 5023234
    Abstract: A method of treatment of breast cancer in susceptible male animals whose testicular hormonal secretions are blocked by surgical or chemical means, e.g., by use of an LH-RH agonist, e.g., [D-Trp.sup.6, des-Gly-NH.sub.2.sup.10 ]LH-RH ethylamide which comprises administering an antiandrogen, e.g., flutamide and optionally at least one inhibitor of sex steroid biosynthesis, e.g., aminoglutethimide and/or ketoconazole. Pharmaceutical compositions useful for such treatment are also disclosed.
    Type: Grant
    Filed: February 8, 1985
    Date of Patent: June 11, 1991
    Inventor: Fernand Labrie
  • Patent number: 5023233
    Abstract: A fibrinogen receptor antagonist of the formula: ##STR1## wherein A, B, C, D, E, R, R.sup.1 and X-Y are preferably defined as follows:A is acylamido;R and R.sup.1 are H;X-Y is S--S;B is L-asparagine;C is proline or thioproline or .beta., .beta.-dimethylthroprolineD is arginine; andE is COOH.
    Type: Grant
    Filed: July 28, 1989
    Date of Patent: June 11, 1991
    Assignee: Merck & Co., Inc.
    Inventors: Ruth F. Nutt, Stephen F. Brady, Daniel F. Veber