Abstract: Molecular structures of .beta.-adrenergic antagonists are modified to produce biologically active compounds. The .beta.-antagonists are modified to form molecules of the general structure: ##STR1## wherein R is most generally R"--OCH.sub.2 --, and in some instances is R"--, and R"=an aryl or substituted aryl moiety; R'=--H, --CH.sub.3, or a short chain alkyl moiety; and Y=--OH, or more usually, --OAX or --NHAX, where A=an alkyl, aryl, or aralkyl moiety, and X=a terminal grouping, such as --CH.sub.3, --CF.sub.3 or --(CH.sub.2).sub.n COOH; or AX may be a carrier moiety consisting of a defined peptide or protein.
Type:
Grant
Filed:
August 13, 1987
Date of Patent:
June 6, 1989
Assignee:
The Regents of the University of California
Inventors:
Murray Goodman, Debra Marr-Leisy, Roberto P. Rosenkranz, Kenneth L. Melmon, Michael S. Verlander
Abstract: Somatostatin derivatives of general Formula I ##STR1## wherein at least one of the residues X represents a moiety, bound to the free amino group of alanine or lysine, of Formula II ##STR2## with R meaning an alkyl group containing 7-23 carbon atoms, and the residues X which may remain mean hydrogen atoms, are pharmacologically active compounds.
Abstract: A composition containing a tissue Plasminogen Activator (tPA) which comprises a partial hydrolyzate of gelatin cross-linked to a diisocyanate as an essential ingredient; or alternatively a partial hydrolyzate of gelatin cross-linked to a diisocyanate and one or more of a basic amino acid or salt thereof. The composition enhances the solubility of the tPA in water, thereby making the tPA further available in the treatment of circulatory diseases caused by thrombi.
Abstract: Production of human relaxin or novel human relaxin analogs by combination of a human relaxin A-chain and B-chain comprises combining the reduced form of the human relaxin A-chain and the reduced form of the human relaxin B-chain in an aqueous medium having a pH of about 7.0 to 12 at room temperature, under conditions that are mildly denaturing for the relaxin B-chain such that the human relaxin or novel human relaxin analog can be formed.
Abstract: The antagonistic effect of the releasing hormone of LH and FSH or of one of its synthetic analogues selected from the group(pyro) Glu-His-Trp-Ser-Tyr-D-Trp-Leu-Arg-Pro-Gly-NH.sub.2(pyro) Glu-His-Trp-Ser-Tyr-D-Phe-Leu-Arg-Pro-Gly-NH.sub.2and(pyro) Glu-His-Trp-D-Ser-Tyr-D-Leu-Leu-Arg-Pro-NHR.sup.1(R.sup.1 being an alkyl group). On hormone-dependent diseases can be increased by coating such compounds by micro-encapsulation or by matrix formation with a copolymer of a lactide and a glycolide. The initial stimulating effect of the above-mentioned compounds is increased by this coating, with about 23 to 50% of the active principle of the analog being released within about 1-5 days after injection to a human, with the remainder released over a period of between about 3 weeks and two months.
Type:
Grant
Filed:
May 19, 1987
Date of Patent:
May 30, 1989
Assignee:
Debiopharm S.A.
Inventors:
Thomas R. Tice, Piero Orsolini, Andrew V. Schally
Abstract: A method of linking primary aromatic amine- or nitro-compounds to carrier proteins by photochemical reactions in order to produce antibodies against the haptens.
Abstract: A 16.7 kilodalton membrane protein which is produced in mature, but no early-stage, T cells has been discovered. The protein has four distinct amphipathic domains, each having an amino acid composition which is predictive of an alpha helical structure that would be stable in a lipid bilayer. Each of these regions is flanked by a relatively polar domain whose amino acid sequence is predictive of .beta. pleat peptide regions. An antibody specific against one of the polar domains can be used to discriminate mature T-cells in a mixed-cell sample.
Abstract: A unique class of tissue kallikrein inhibitors is provided which are specific for tissue kallikreins and do not substantially cross-react with plasma kallikreins or other serine proteases in-vivo. These inhibitors are substrate analogues of low molecular weight kininogens but are highly inhibitory, stable and resistant to enzymatic hydrolysis, and release non-toxic degradation products.
Abstract: The peptides of the formula ##STR1## together with their pharmacologically acceptable salts, which have been described as exhibiting analgesic, antidiarrhoeal and antitussive activity, are effective in reversing neuronally-mediated bronchoconstriction in mammals. The said compounds have application in the palliation of conditions characterized by such a state, in particular asthma in human beings.
Type:
Grant
Filed:
September 11, 1987
Date of Patent:
May 23, 1989
Assignee:
Burroughs Wellcome Co.
Inventors:
Geoffrey Allan, John J. Adcock, Terence W. Smith
Abstract: A novel colony stimulating factor (CSF) that has the ability to promote the differentiation and proliferation of human bone marrow cells to neutrophiles, and a method for obtaining the same are disclosed. This CSF is produced from a novel cell line which has been established from tumor cells in patients with oral cancer.This CSF has the potential for use only as a curative for leukopenia but also as a reagent for clinical testing and research studies.
Abstract: The present invention provides synthetic peptides and fragments and analogs thereof complementary to growth hormone releasing hormone, and antibodies raised against such peptides. The present invention also includes methods of using such peptides and antibodies.
Abstract: A method for increasing bone mass in a human afflicted with osteoporosis or a similar disease which comprises administering to the human so afflicated an effective amount of a composition comprising a parathyroid hormone or physiologically active fragment thereof, or equivalents thereof, in combination with either (a) a hydroxylated Vitamin D compound, or a structural or functional analogue thereof, or (b) a dietary calcium supplement. Pharmaceutical compositions containing the necessary components are also disclosed.
Type:
Grant
Filed:
May 21, 1987
Date of Patent:
May 23, 1989
Assignee:
The General Hospital Corporation
Inventors:
Robert M. Neer, John T. Potts, Jr., David M. Slovik
Abstract: Novel inhibitors of angiotensin coverting enzyme having the general formula R - A - S - Z are disclosed as potent inhibitors of angiotensin converting enzyme and are useful anti-hypertensive agents.
Abstract: Polydisperse native Pseudomonas flagellar (H) antigens (FAg) and methods of producing them are described, wherein each monomeric component contains certain amino acids, has a certain N-terminal amino acid sequence and a certain molecular weight and is free from pyrogenic substances. The ratio of the individual amino acids in the flagellar antigen of the individual H-serotypes is stated.For producing the polydisperse native Pseudomonas flagellar (H) antigens (FAg) methods are indicated, wherein Pseudomonas aeruginosa bacterial cultures or fractions thereof are treated with a detergent and the flagellar antigens are separated from the cultures. Prior to treatment or in the presence of the detergent, the bacterial culture is subjected to a shearing procedure, i.e. exposed to shearing forces. Thereafter, the flagellar antigens separated from the bacterial mass are isolated by a chromatographic treatment.
Abstract: This invention relates to new chemical compounds having valuable pharmaceutical activity. It particularly relates to stereoisomeric compounds possessing hypotensive activity, i.e., angiotensin converting enzyme inhibitory (ACEI) activity and having the structure ##STR1## wherein R and R.sub.9 are independently hydroxy, lower alkoxy, lower alkenoxy, di(lower alkyl)amino-lower alkoxy, hydroxy-lower alkoxy, acylamino-lower alkoxy, acryloxy-lower alkoxy, aryloxy, aryloxyl-lower alkoxy, amino, lower alkylamino, di-lower alkylamino, hydroxyamino, or aryl-lower alkylamino;R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.7 and R.sub.8 are independently hydrogen, alkyl, alkenyl or alkynyl containing up to 20 carbon atoms, aryl or aryl-lower alkyl having from 7 to 12 carbon atoms, heterocyclic or heterocyclic-lower alkyl having from 6 to 12 carbon atoms, cycloalkyl or cycloalkyl-alkyl containing up to 20 carbon atoms in the cycloalkyl group, provided that each of R.sub.1 and R.sub.2 and R.sub.4 and R.sub.
Type:
Grant
Filed:
February 14, 1983
Date of Patent:
May 16, 1989
Assignee:
Rorer Pharmaceutical Corporation
Inventors:
Raymond D. Youssefyeh, Jerry W. Skiles, John T. Suh, Howard Jones
Abstract: New aminoacid derivatives of the formula IX--Z--NR.sup.2 --CHR.sup.3 --CR.sup.4 --(CHR.sup.5).sub.n --CO--E--NR.sup.6 --(CHR.sup.7).sub.s --D Iwherein X, Z, R.sup.2, R.sup.3, R.sup.4, R.sup.5, E, R.sup.6, R.sup.7, D, n and s have the meanings defined herein and their salts, inhibit the activity of human plasma renin.
Type:
Grant
Filed:
July 31, 1987
Date of Patent:
May 9, 1989
Assignee:
Merck Patent Gesellschaft Mit Beschrankter Haftung
Inventors:
Peter Raddatz, Joachim Gante, Claus J. Schmitges, Klaus Otto Minck, Johannes Sombroek, Gunter Holzemann
Abstract: Novel analogs of biologically active vasopressin and its synthetic analogs having improved activity are represented by the structural formula: ##STR1## wherein A hydrogen; is hydroxy or lower alkoxy, especially methoxy, B is the peptide residue of phenylalanine (Phe) or isoleucine, Gln represents the peptide residue of glutamine Asn represents the peptide residue of asparagine, E represents the peptide residue of proline (Pro), 4-thioproline (4-thioPro) or 3,4-dehydroproline (3,4-dehydroPro), FNH represents an N-substituted peptide residue of L- or D-lysine (Lys) L or D homolysine (h Lys) or L- or D-orntihine (Orn), X represents a side peptide chain consisting of one or more of Gly, L-Ala, L-Val, L-Leu, or L-Phe, Gly represents the peptide residue of glycine, and G is disulfide (--S--S--) or thioether (--CH.sub.2 S-- or --SCH.sub.2 --).
Abstract: Synthetic polypeptides are disclosed which exhibit potent serine protease inhibition. Methods and compositions useful for treating conditions caused by unwanted serine protease activity are also disclosed.
Type:
Grant
Filed:
May 8, 1987
Date of Patent:
May 9, 1989
Assignee:
Monsanto Company
Inventors:
George I. Glover, Charles A. McWherter, Charles S. Schasteen