Abstract: Thrombin inhibitors from the hirudin family which differ from the previously known hirudins by mutation in the protein chain, and a process for their preparation are described. The novel hirudins are distinguished by a high specific activity, high stability and good pharmacokinetics.
Type:
Grant
Filed:
March 22, 1993
Date of Patent:
June 21, 1994
Assignee:
Hoechst Aktiengesellschaft
Inventors:
Dominique Tripier, Peter Crause, Paul Habermann, Martin Kramer, Joachim Engels, Matthias Scharf
Abstract: A composition of crystalline TGF-.beta.2 is described. The tertiary structure of the protein homodimer determined by X-ray crystallography to 2.1 angstrom resolution is shown. This structure provides data useful in the rational design of drugs to mimic the physiologic properties of proteins of the TGF-.beta. family.
Type:
Grant
Filed:
May 7, 1992
Date of Patent:
June 21, 1994
Assignee:
The United States of America as represented by the Secretary of the Department of Health and Human Services
Inventors:
David R. Davies, Sun Daopin, Yasushi Ogawa, Karl Piez
Abstract: Hemoglobin-containing solutions containing polyalkylene oxide-conjugated hemoglobin having a molecular weight greater than about 85,000 daltons and a degree of substitution of at least five polyalkylene oxide conjugates per hemoglobin molecule are described that are not associated with hemoglobinuria in mammals. A method of simultaneously fractionating and purifying polyalkylene oxide-conjugated hemoglobins is also disclosed.
Type:
Grant
Filed:
October 13, 1992
Date of Patent:
May 17, 1994
Assignee:
Enzon, Inc.
Inventors:
Robert G. L. Shorr, Myung-Ok P. Cho, Kwang Nho
Abstract: A multi-functional physiologically active substance can be obtained from the residue of saccharified malt which is worthless other than feed for cattle. The isolation of the active substance is performed by an extraction of the residue with water or an aqueous solvent and removal of a low molecular weight fraction from the extract.
Abstract: A novel peptide derivative having the formula: ##STR1## wherein A between Pro and Q.sup.2 is Arg or Lys: Q.sup.1 is pGlu or H; Q.sup.2 is --Gly--OH or OH; Y.sup.1 is H or --CO--T and Y.sup.2 is OH or T; wherein T is a thiamine derivative group is disclosed. The peptide derivative shows a remarkable nootropic effect.
Abstract: Synthetic polypeptides corresponding to the B lymphocyte CR2 receptor binding site present on an interferon alpha-related CR2 ligand are disclosed together with polypeptide aggregates, compositions, anti-polypeptide antibodies and methods of preparing and using the polypeptides and antibodies.
Type:
Grant
Filed:
April 20, 1990
Date of Patent:
May 10, 1994
Assignee:
California Institute of Biological Research
Abstract: Antifungal and antiparasital lipopeptide compounds stable in aqueous media are described. Stability in aqueous media render lipopeptides more useful for compositions for therapeutic applications.
Abstract: A cyclohexapeptide base which is the nucleus of closely related antibiotics obtained by culturing Zalerion arboricola and its salts are described. They are useful intermediates for the preparation of new semisynthetic compounds having antimicrobial activity.
Type:
Grant
Filed:
March 12, 1990
Date of Patent:
May 10, 1994
Assignee:
Merck & Co., Inc.
Inventors:
Dennis M. Schmatz, Jan S. Tkacz, Robert E. Schwartz, Mervyn Turner
Abstract: A freeze-dried pharmaceutical composition for parenteral administration which includes a therapeutically effective amount of a calcitonin, as the active ingredient, and human albumin.The injectable solution which is obtained by dissolving the freeze-dried composition in a physiologically acceptable solvent is also described.
Abstract: Crandell feline kidney cells infected with a Rickard isolate of FeLV, i.e., FeLV-A.sub.R1, are provided, the infected cells being capable of producing viral materials in amounts sufficient for formulating FeLV vaccines. Processes for producing viral material and FeLV vaccines utilizing the viral material thus prepared also are provided.
Abstract: An antimicrobial peptide containing at least the following amino acid sequence (a), (b), (c) or (d), an antimicrobial agent containing the said antimicrobial peptide as active components at a concentration of at least 5 ppm (weight), an antimicrobial composition the said antimicrobial peptide and a method for processing products which uses the antimicrobial agent containing the said antimicrobial peptide.
Type:
Grant
Filed:
September 5, 1991
Date of Patent:
April 19, 1994
Assignee:
Morinaga Milk Industry Co., Ltd.
Inventors:
Mamoru Tomita, Kohzo Kawase, Mitsunori Takase, Wayne R. Bellamy, Kohji Yamauchi, Hiroyuki Wakabayashi
Abstract: New bactericidal and/or bacteriostatic, thermostable peptides which are isolated from hemolymph of immune honeybees and which are distinct from lysozymes, attacins, cecropins, diptericins and magainins. The peptides feature at least the 10 C-terminal amino acids of the following peptide:H.sub.2 N-Gly-Asn-Asn-Arg-Pro-X-Tyr-Ile-Pro-Gln-Pro-Arg-Pro-Pro-His-Pro-Arg-Z-OHin whichX is a valyl or isoleucyl residue andZ is a leucyl or isoleucyl residue.
Type:
Grant
Filed:
November 14, 1991
Date of Patent:
April 5, 1994
Assignee:
Plant Genetic Systems, N.V.
Inventors:
Peter Casteels, Paul Tempst, Frans Jacobs, Mark Vaeck
Abstract: Novel diamino acid derivative dual inhibitors of neutral endopeptidase and angiotensin converting enzyme of the formula ##STR1## wherein: Z is amino, lower alkylamino, di-(lower alkyl)amino R.sup.9 C(O)NH-- or an optionally substituted guanidino group;R.sup.1 is hydrogen or R.sup.7 R.sup.8 N--;R.sup.2 is hydrogen, lower alkyl, cyclolower alkyl, aryllower alkyl or heteroaryllower alkyl; and R.sup.3 is hydrogen, lower alkyl or cyclolower alkyl; or R.sup.2 and R.sup.3, together with the carbon to which they are attached, comprise a 3-7 membered carboxyclic ring;R.sup.4 is hydrogen, lower alkyl, aryl lower alkyl or heteroaryllower alkyl;R.sup.5 and R.sup.6 are independently hydroxy, lower alkoxy, amino, aryllower alkoxy, lower alkylamino and di-(lower alkyl)amino;R.sup.7 is R.sup.9 C(O)-- or R.sup.10 SO.sub.2 --; and R.sup.8 is hydrogen, lower alkyl, aryllower alkyl or aryl; or R.sup.7 and R.sup.8, together with the nitrogen to which they are attached, comprise a 5-7 membered ring;R.sup.
Type:
Grant
Filed:
August 4, 1992
Date of Patent:
March 29, 1994
Assignee:
Schering Corporation
Inventors:
Bernard R. Neustadt, Elizabeth M. Smith, Deen Tulshian
Abstract: Peptides which include unnatural amino acids and which either inhibit or promote the secretion of gonadotropins by the pituitary gland and inhibit the release of steroids by the gonads. Administration of an effective amount of such peptides that are GnRH antagonists prevents ovulation of female mammalian eggs and/or the release of steroids by the gonads. The antagonists may be used to treat steroid-dependent tumors, such as prostatic and mammary tumors. The peptides are analogs of the decapeptide GnRH wherein there is at least one residue of an unnatural amino acid in the 3-, 5-, 6- and/or 8-positions. Such unnatural amino acids are useful in the synthesis of peptides and have the formula U.sup.* : ##STR1## where W is (CH.sub.2).sub.n or ##STR2## n is an integer from 1 to 6; and j=1, 2 or 3. Preferably, either Y is N--CN, X is NH and R.sub.2 is alkyl, modified alkyl, alkenyl, alkynyl, aryl or methyl pridyl or ##STR3## where R.sub.11 is H or acyl.
Type:
Grant
Filed:
January 21, 1993
Date of Patent:
March 22, 1994
Assignee:
The Salk Institute for Biological Studies
Inventors:
Carl A. Hoeger, Jean E. F. Rivier, Paula G. Theobald, John S. Porter, Catherine L. Rivier, Wylie W. Vale, Jr.
Abstract: The present invention provides a method of treating ocular diseases by the administration of cyclosporine A or G by periocular injection in a pharmaceutically acceptable carrier.
Type:
Grant
Filed:
December 20, 1989
Date of Patent:
March 15, 1994
Assignee:
The Government of the United States of America as represented by the Secretary of the Department of Health and Human Services
Inventors:
Robert B. Nussenblatt, Alan G. Palestine
Abstract: Administration into fish of gonadotropin releasing hormone (GnRH), luteinising releasing hormone (LHRH) and their analogs in a polymer based sustained release delivery system was found to induce a prolonged elevation in the fish's plasma level of gonadotropin (GtH), which leads to ovulation and spawning. Such induction of ovulation and spawning was found to occur both within the natural spawning season and outside this season. Such administration thus enables for the first time an effective means for manipulating reproduction in fish, which is a very important factor in the economic management of fish farming.
Type:
Grant
Filed:
October 6, 1989
Date of Patent:
February 22, 1994
Assignee:
Israel Oceanographic & Limnological Research Ltd.
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, novel intermediates useful in the preparation thereof, 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, congestive heart failure, or hyperaldosteronism.
Type:
Grant
Filed:
August 4, 1992
Date of Patent:
February 22, 1994
Assignee:
Warner-Lambert Company
Inventors:
Annette M. Doherty, Harriet W. Hamilton, John C. Hodges, Joseph T. Repine, Ila Sircar
Abstract: Affinity chromatography matrices are disclosed which are useful in purifying interleukin-1.beta. converting enzyme (ICE) from crude or partially purified cell lysate preparations. The chromatographic matrices comprise a specific ICE inhibitor of Formula I which is attached to an affinity column support by means of a bifunctional spacer.
Abstract: Polypeptides derived from domain VI of the amino terminal globule of the A chain of laminin and having sequences of at least about 5 amino acids, and which exhibit cell adhesion and cell spreading capacity are described.Medical devices such as prosthetic implants, percutaneous devices and cell culture substrates coated wGOVERNMENT SUPPORTThis invention was made with government support under contract No. CA-29995 by the U.S. National Institutes of Health. The government has certain rights in the invention.
Abstract: The present invention relates to analgesic enkephalin derivatives represented by the following formula:Tyr-A.sub.1 -A.sub.2 -A.sub.3 -A.sub.4 SEQ ID NO:5 (1)and the acid salts thereof, wherein Tyr is L-tyrosine, A.sub.1 or A.sub.2 is a glycine, and that which is not a glycine is an optically active trifluoro amino acid of the formula: ##STR1## wherein n is an integer from 1-3 and m is 1 or 2; A.sub.3 is L-Phenylalanine, or N-methyl-(L)-phenylalanine, and A.sub.4 is L-Methionine, L-Met-OH, L-Met-ol or L-Met-NH.sub.2.
Type:
Grant
Filed:
December 18, 1990
Date of Patent:
January 4, 1994
Assignee:
The Research Foundation of State University of New York