Abstract: This invention relates to stable non-aqueous protic formulations of peptide compounds. These stable formulations comprise peptide in non-aqueous protic solvent. They may be stored at elevated temperatures for long periods of time and are especially useful in implantable delivery devices for long term delivery of drug.
Type:
Grant
Filed:
June 13, 1997
Date of Patent:
November 9, 1999
Assignee:
Alza Corporation
Inventors:
Cynthia L. Stevenson, Sally A. Tao, Steven J. Prestrelski, James B. Eckenhoff, deceased, Jeremy C. Wright, John J. Leonard, Jr.
Abstract: Novel synthetic Arg-Gly-Asp containing peptides which have high affinity and specificity for their receptors by virtue of restrictions on their stereochemical conformation. Such restrictions can be provided by cyclization, by inclusion into a constraining conformational structure such as a helix, by providing an additional chemical structure such as an amide or an enantiomer of a naturally occurring amino acid, or by other methods. In particular, there are provided cyclic peptides having increased affinity and selectivity for the certain receptors over that of linear, Arg-Gly-Asp-containing synthetic peptides.
Type:
Grant
Filed:
June 2, 1995
Date of Patent:
November 9, 1999
Assignee:
La Jolla Cancer Research Foundation
Inventors:
Michael D. Pierschbacher, Erkki I. Ruoslahti
Abstract: A process for isolating insulin which entails performing high-pressure liquid chromatography with pressure-stable acidic cation exchange material under a pressure of from 1.1 MPa to 40 MPa.
Type:
Grant
Filed:
December 17, 1997
Date of Patent:
November 2, 1999
Assignee:
Hoechst Aktiengesellschaft
Inventors:
Rainer Obermeier, Jurgen Ludwig, Walter Sabel
Abstract: A prodrug of the formula (I): ##STR1## where R.sup.1 is a group such that the compound R.sup.1 NH.sub.2 represents actinomycin D, doxorubicin, mitomycin C, or a nitrogen mustard of the formula (IV): ##STR2## a prodrug of the formula (II): ##STR3## where R.sup.2 is a group such that the compound R.sup.2 OH is a phenolic nitrogen mustard; and processes whereby the prodrugs shown above are made in which a prodrug precursor compound is reacted with 4-nitrobenzyl chloroformate under anhydrous conditions.
Type:
Grant
Filed:
June 1, 1998
Date of Patent:
November 2, 1999
Assignee:
Cancer Research Campaign Technology Limited
Inventors:
Gillian Anlezark, Roger Melton, Roger Sherwood, Thomas Connors, Frank Friedlos, Michael Jarman, Richard Knox, Anthony Mauger, Caroline Joy Springer
Abstract: An inhibiting agent against the proliferation of tumor cells comprises a lower condensation polymer or oligomer of an .alpha.-hydroxy acid, an oligopeptide containing at least one pyroglutamic acid residue, and a stabilizer. The lower condensate and the lower polymer of an .alpha.-hydroxy acid comprise mainly compounds formed by condensing and polymerizing 2 to 10 molecules of an .alpha.-hydroxy acid and their metal salts. The weight ratio of the components is such that the ratio of the lower condensate and the lower polymer of an .alpha.-hydroxy acid is 10, the ratio of the oligopeptide containing at least one pyroglutamic acid residue is 1 to 4, and the ratio of the stabilizer a saccharide or a sugaralcohol comprising is 1 to 3.
Abstract: Vascular disease including asymptomatic atherosclerosis can be diagnosed by administering a synthetic peptide or peptide analog having an affinity for, and propensity to accumulate at, a site of vascular injury to a patient, and then detecting the location of the peptide or peptide analog within the patient's vascular system. The synthetic peptide or peptide analog may include an amino acid sequence sufficiently duplicative of the amino acid sequence of a region of either the apolipoprotein B, apolipoprotein A-I, or elastin proteins such that the peptide or peptide analog accumulates at a site of vascular injury.
Type:
Grant
Filed:
February 28, 1995
Date of Patent:
October 26, 1999
Assignee:
New England Deaconess Hospital Corporation
Inventors:
Robert S. Lees, Ann M. Lees, Allan Fischman, Ing-Lung Shih, Mark A. Findeis
Abstract: The isolated and purified PAI from several active snake venoms is described and characterized. In addition, PAIs lacking the Arg-Gly-Asp (RGD) adhesion sequence but containing K* -(G/Sar)-D wherein K* is a modified lysyl residue of the formulaR.sup.1.sub.2 N(CH .sub.2).sub.4 CHNHCO--wherein each R.sup.1 is independently H, alkyl(1-6C) or at most one R.sup.1 is R.sup.2 --C.dbd.NR.sup.3 wherein R.sup.2 is H, alkyl(1-6C), phenyl or benzyl, or is NR.sup.4 .sub.2 in which each R.sup.4 is independently H or alkyl(1-6C) and R.sup.3 is H, alkyl(1-6C), phenyl or benzyl, or R.sup.2 --C.dbd.NR.sup.3 is a radical selected from the group consisting of: ##STR1## where m is an integer of 2-3, and each R.sup.5 is independently H or alkyl(1-6C);and wherein one or two (CH.sub.2) may be replaced by O or S provided said O or S is not adjacent to another heteroatomare prepared and shown to specifically inhibit the binding of fibrinogen or von Willebrand Factor to GP IIb-IIIa.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
October 19, 1999
Assignee:
COR Therapeutics, Inc.
Inventors:
Robert M. Scarborough, David Lawrence Wolf, Israel F. Charo
Abstract: The present invention provides a peritoneal dialysis solution that contains atrial natriuretic peptide (ANP), a derivative of ANP, an analogue of ANP, a substance that binds ANP to clearance receptors or a substance that promotes ANP synthesis, which results in an increased net ultrafiltration and increased sodium clearance experienced in peritoneal dialysis patients.
Type:
Grant
Filed:
May 23, 1997
Date of Patent:
October 12, 1999
Assignees:
Baxter International Inc., Miles G. Johnston
Inventors:
Chi J. Chen, Ty R. Shockley, Miles G. Johnston
Abstract: Disclosed are methods for inhibiting and modulating the actions of CXC intercrine molecules. The antileukinate peptides described inhibit IL-8, GRO and MIP2.beta. binding to neutrophils and neutrophil activation. The peptides are particularly advantageous as they inhibit IL-8-induced enzyme release at a 25 fold lower concentration than is required to inhibit chemotaxis, which makes them ideal for treating various inflammatory diseases and disorders including, amongst others, Adult Respiratory Distress Syndrome (ARDS), cystic fibrosis and chronic bronchitis.
Type:
Grant
Filed:
June 14, 1996
Date of Patent:
October 12, 1999
Assignee:
Board of Regents, The University of Texas System
Inventors:
Allen Barry Cohen, deceased, Edmund J. Miller, Shinichiro Hayashi, Anna K. Kurdowska, Ronald R. Tuttle
Abstract: There is provided compounds of formula I,R.sup.1 O(O)C--CH.sub.2 --(R)Cgl-Aze-Pab-R.sup.2 Iwherein R.sup.1 and R.sup.2 have meanings given in the description, which are useful as prodrugs of inhibitors of trypsin-like proteases, such as thrombin, and in particular in the treatment of conditions where inhibition of thrombin is required (eg thrombosis) or as anticoagulants.
Type:
Grant
Filed:
January 31, 1997
Date of Patent:
October 12, 1999
Assignee:
Astra AB
Inventors:
David Gustafsson, Jan-Erik Nystrom, Henrik Sorensen, Mikael Sellen
Abstract: This invention concerns peptides (I) having intracellular potassium channel modulating activity comprising the amino acid sequence shown in SEQ ID No: 2:(N terminal function) (I) Met Ile Ser Ser Val Cys Val Ser Ser 1 5} Tyr Arg Gly Arg Lys Ser Gly Asn Lys 10 15 Pro Pro Ser Lys Thr Cys Leu Lys Glu Glu 20 25 (C terminal function)in which the cysteines are optionally linked via a disulphide bridge and wherein ______________________________________ Met represents L-methionine Ile represents L-isoleucine Ser represents L-serine Val represents L-valine Cys represents L-cysteine Tyr represents L-tyrosine Arg represents L-arginine Gly represents glycine Lys represents L-lysine Asn represents L-asparagine Pro represents L-proline Thr represents L-threonine Leu represents L-leucine Glu represents L-glutamic acid ______________________________________or a variant thereof,with the proviso that excluded is the 13-Lys variant (where 13-Arg is replaced by 13-Lys) in which the cysteines are not linked via a disulphide bridge
Type:
Grant
Filed:
May 26, 1995
Date of Patent:
October 12, 1999
Assignee:
John Wyeth & Brother, Ltd.
Inventors:
Roger Crossley, Albert Opalko, David Geraint Owen, Brian Robertson
Abstract: A method of ameliorating degradation of radiolabeled peptides, especially radiolabeled proteins such as antibodies, by including povidone, also widely known as polyvinylpyrrolidone or PVP, as a radioprotectant in a composition containing a radiolabeled peptide is described. A radioprotectant composition and a stable peptide-radioisotope composition having povidone are also described. Ascorbic acid or other secondary stabilizers may also be added to the compositions to further enhance radioprotection.
Type:
Grant
Filed:
August 21, 1997
Date of Patent:
October 5, 1999
Assignee:
Coulter Pharmaceutical, Inc.
Inventors:
Dan Shochat, Albert S. K. Chan, Michael J. Buckley, David Colcher
Abstract: The present invention relates to disulphide-cyclo-?H-Cys-Glu-Gln-Tyr-Cys-OH! and salts thereof which are useful in the treatment of blood clotting disorders.
Type:
Grant
Filed:
September 10, 1997
Date of Patent:
October 5, 1999
Assignee:
Nycomed Imaging AS
Inventors:
Lars Orning, Kjell Steinar Sakariassen, Kjell Eric Agner, Peter Fischer, May Engebretsen
Abstract: The invention relates to storage-stable fibrinogen preparations for preparing concentrated fibrinogen solution for use as a tissue adhesive or for preparing fibrinogen solutions for other uses, for example, for infusion purposes. The fibrinogen preparations are characterized in that(i) the lyophilized preparation comprises a substance improving the solubility of fibrinogen such that the reconstitution time is up to 15 minutes, preferably less than 7 minutes, when dissolving with water at room temperature to a solution with a fibrinogen concentration of at least 70 mg/ml and(ii) the ready-to-use tissue adhesive solution obtained from the preparation forms fibrin clots having physiological fibrin structure after mixing with a thrombin-CaCl.sub.2 solution.
Abstract: Compositions of the invention include composites comprising a biomaterial having compounds thereon with enhanced cell binding with respect to collagen. These composites are useful for soft and hard tissue repair or reconstruction and for in vitro uses. Suitable compounds with enhanced cell binding include synthetic peptides that mimic the conformation necessary for recognition and docking of collagen binding species (such as cell surface receptors for collagen and fibronectin) and have the amino acid residues -Ile-Ala- folded in a .beta.-bend.
Type:
Grant
Filed:
May 20, 1997
Date of Patent:
September 28, 1999
Assignee:
The Regents of the University of California
Abstract: The invention is directed to lanthocin-containing tablet formulations for oral administration. The inventive formulations afford delivery of the lanthocin to the colon in amounts sufficient to treat diseases brought on by bacterial infection of the colon. Also provided is a process for preparation of the formulations.
Type:
Grant
Filed:
October 14, 1997
Date of Patent:
September 28, 1999
Assignee:
University of Cincinnati
Inventors:
Ahmed Adel Sakr, Walid Abdel-Azim Habib
Abstract: Compounds which display a surface similar to the surface presented by one of five distinct lateral domains of CD4 are disclosed. Methods of treating individuals suspected of suffering from or susceptible to conditions characterized by an undesired immune response comprising administering to the individual at least one compound which mimics a portion of the lateral surface of the CD4 glycoprotein are disclosed.
Type:
Grant
Filed:
October 11, 1996
Date of Patent:
September 28, 1999
Assignee:
Thomas Jefferson University
Inventors:
Bradford A. Jameson, James M. McDonnell, Robert Korngold
Abstract: New peptide compounds of the formula: ##STR1## wherein R.sup.1 is alkyl or aralkyl,R.sup.2 is amino(lower)alkyl or protected amino(lower)alkyl,R.sup.3 is hydroxy, protected hydroxy, amino or protected amino,R.sup.4 is hydroxy, orR.sup.3 and R.sup.4 are linked together to form --Z-- (in which --Z-- is --O-- or --NH--), andR.sup.5 is hydrogen or an amino protective group,R.sup.6 is hydroxy, orR.sup.5 and R.sup.6 are linked together to form bond,with proviso thatwhenR.sup.3 is hydroxy, protected hydroxy, amino or protected amino andR.sup.4 is hydroxy,then R.sup.5 and R.sup.6 are linked together to form bond,and a pharmaceutically acceptable salt thereof, which is useful as a medicament.
Abstract: The present invention relates to an antiviral raw material having mannose-binding type lectin bound, through a hydrophilic high-molecular chain, to a base material composed of a hydrophobic high-molecular chain. The raw material has excellent shape stability and at the same time has excellent antiviral activity so that it can be used in a wide range of fields.
Abstract: A novel homogenous alcohol free, free flowing, clear and transparent pharmaceutical composition containing Cyclosporin is disclosed. The amount of Cyclosporin is easily measurable at a wide range of temperature of 15.degree. to 45.degree. C. The composition comprises a Cyclosporin in a hydrophillic carrier medium comprising propylene glycol, a transesterification product of a natural vegetable oil triglyceride and a polyalkylene polyol and polyethylene hydrogenated castor oils.