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
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.
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
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
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.
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
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.
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
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.
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.
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.
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
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.
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.
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
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
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.
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.
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