Abstract: A method of providing contraception for and regulation of the menstrual cycle of a gonadal female mammal by a) administering thereto about once a week throughout her menstrual cycle an amount of a GnRH-antagonist effective to block folliculogenesis and thereby achieve a contraceptive state but less than the amount thereof required to block hormonogenesis; and b) inducing menses by administering during the last half of that cycle an amount of a progestin effective to produce a secretory endometrium and then terminating the progestin administration.
Abstract: Enzyme-inhibiting urea derivatives of dipeptides, a process for the preparation thereof, agents containing these, and the use thereof.The present invention relates to compounds of the formula I ##STR1## in which A and B denote, indpendently of one another, an amino acid,X as desired can be absent or represents --O--, --S--, --CF.sub.2 --, --CO-- or --CHR.sup.8,p and q denote, independently of one another, 0, 1, 2, 3 or 4, andR.sup.1 to R.sup.4 are defined in the description, as well as the salts thereof.The invention furthermore relates to a process for the preparation of the compounds of the formula I and to the use thereof as medicines.
Type:
Grant
Filed:
December 7, 1989
Date of Patent:
May 26, 1992
Assignee:
Hoechst Aktiengesellschaft
Inventors:
Wolfgang Ruger, Hansjorg Urbach, Dieter Ruppert, Bernward Scholkens
Abstract: A novel arthropodicidally-active composition-of-matter is disclosed. Such comprises an aqueous lower alkanol solvent, a toxicant contained within the solvent, and an effective amount of an emulsifier, also contained within the solvent, for forming a foam matrix of predetermined stability. Also disclosed are methods for producing such a composition-of-matter.
Abstract: This invention is directed to an antifouling paint that contains a polymer having organosilyl groups and/or organosiloxane groups in side claims.
Abstract: Compounds represented by the following formula: ##STR1## wherein A.sub.1 and A.sub.2 each represents a specific amino acid residue, are excellent as substrates for determination of enzyme activity such as trypsin, etc.
Abstract: The present invention relates to the use of peptide analogues as inhibitors of their respective naturally occurring peptides. The structure of the peptide analogues is exemplified by an internal region of the N-terminus of humoral hypercalcemic factor hHCF, and truncations thereof: hHCF(14-34)NH.sub.2, hHCF(13-34)NH.sub.2, hHCF(12-34)NH.sub.2, hHCF(11-23)NH.sub.2, hHCF(10-34)NH.sub.2, hHCF(9-34)NH.sub.2, hHCF(8-34)NH.sub.2 and various amino acid substitutions.
Type:
Grant
Filed:
February 25, 1991
Date of Patent:
May 19, 1992
Assignee:
Merck & Co., Inc.
Inventors:
Michael Rosenblatt, Roberta L. McKee, Michael P. Caulfield, Ruth F. Nutt
Abstract: Light activated acyl-enzymes of the formula: ##STR1## are disclosed. In the compounds of Formula (III), ENZ is an enzyme, X is O or S, Y is --NR.sub.3 R.sub.4, --OR.sub.5, or --SR.sub.5, and Z is a nucleophile. m is 0 to 3 and n is 1 or 2. Y is substituted on the ring at either or both of the 4 and 6 position.R.sub.1 and R.sub.2 are each independently H, C1 to C4 alkyl, C3 to C4 unconjugated alkenyl, or C3 to C4 unconjugated alkynyl.R.sub.3 and R.sub.4 are each independently H, C1 to C4 alkyl, C3 to C4 unconjugated alkenyl, or C3 to C4 unconjugated alkynyl, except that R.sub.3 and R.sub.4 are not simultaneously both H. R.sub.5 is C1 to C4 alkyl, C3 to C4 unconjugated alkenyl, or C3 to C4 unconjugated alkynyl.Methods of using the acyl-enzymes and intermediates for making the acyl-enzymes are disclosed.
Abstract: Polycondensation silicone elastomer dosage forms adapted for the continuous and controlled release of iodine values, notably to domestic water supplies for the treatment of the various disease states attributed to iodine deficiency, are shaped from (A) at least one diorganopolysiloxane oil bearing at least two condensable or hydrolyzable groups, or a single hydroxyl group, at each end of the polymer chain; (B) a therapeutically effective amount of at least one water soluble, nontoxic, organic and/or inorganic iodine compound which is in solid or liquid state at ambient temperature and which does not inhibit curing of the composition into an elastomer; (C) a catalytically effective amount of a polycondensation catalyst; and optionally, (D) a silane containing at least three condensable or hydrolyzable groups.
Type:
Grant
Filed:
December 11, 1990
Date of Patent:
May 19, 1992
Assignee:
Rhone-Poulenc Chimie
Inventors:
Guy Cyprien, Alain Fisch, Johnny Haggiage, Huges Porte, Thierry Prazuck, Ghislaine Torres
Abstract: The invention relates to a tetrapeptide corresponding to the general formulaSer-Asp-Lys-Pro--OHand its substitution derivatives by one or several groups, identical or different, currently used in the chemistry of peptides for biological use, as well as their pharmaceutically acceptable salts, in particular the tetrapeptideSer-(N-Ac)-Asp-Lys-Pro--OHwhich can be extracted, for example, from fetal calf marrow or obtained by peptide synthesis.The peptide of the invention is particularly useful in the protection of bone marrow in the course of anti-cancer treatments by chemotherapy.
Type:
Grant
Filed:
March 17, 1989
Date of Patent:
May 19, 1992
Assignees:
Institut National De La Sante Et De La Recherche Medicale, Institut Gustave Roussy
Inventors:
Emilia Frindel, Maryse Lenfant, Martine Guigon, Johanna Bakala
Abstract: Compounds of the formula: ##STR1## which are potent inhibitors of human renin and are useful for treating various forms of renin-associated hypertension, hyperaldosteronism and congestive heart failure; compositions containing these renin-inhibitory compounds, optionally with other antihypertensive agents; and methods of treating hypertension, hyperaldosteronism or congestive heart failure or of establishing renin as a causative factor in these conditions which employ these novel compounds.
Type:
Grant
Filed:
September 9, 1991
Date of Patent:
May 19, 1992
Assignee:
Merck & Co., Inc.
Inventors:
Wallace T. Ashton, Christine L. Cantone, Richard L. Tolman
Abstract: This invention relates to novel analogs of certain peptidase substrates in which the nitrogen atom of the scissile amide bond has been replaced with a difluoromethylene moiety and in which the carbonyl moiety of its adjacent amide bond has been replaced with a terminal amine function, said novel analogs having the property of inhibiting renin and which are useful in the treatment of hypertension.
Abstract: Monomeric synthetic peptide and dimeric synthetic peptide comprising an amino acid sequence represented by the formula:X-Asn-Val-Thr-Glu-Arg-Tyr-Met-Ala-Cys-Lys-LyswhereinX represents a residue comprising 0 to 10 amino acids sequence; and Asn represents aspartic acid, Val valine, Thr threonine, Glu glutamic acid, Arg arginine, Tyr tyrosine, Met methionine, Ala alanine, Cys cysteine and Lys lysine;an assay kit of human Mn-SOD to be used in the assay method of human Mn (manganese)-SOD comprising as essential components:(a) at least one of the above monomeric and dimeric synthetic peptides; and(b) an enzyme-labelled monoclonal antibody having a very high specific immunoreactivity against at least one of the above monomeric and dimeric synthetic peptides and at the same time having a very high specific immunoreactivity against human Mn-SOD; and an assay method of human Mn-SOD, which comprises immobilizing at least one of the above monomeric and dimeric synthetic peptides on a carrier, then allowing human Mn-SOD i
Abstract: Novel polypeptides, designated hirullins, have a strong antithrombic activity and can therefore be used for the therapy and prophylaxis of thromboses. Said compounds are isolated from the leech Hirudinaria manillensis or are produced by conventional peptide synthesis or by recombinant DNA techniques.
Type:
Grant
Filed:
June 8, 1989
Date of Patent:
May 19, 1992
Assignees:
Ciba-Geigy Corporation, UCP Gen-Pharma AG
Inventors:
Reinhard Maschler, Verena Steiner, Markus G. Grutter, Fritz Raschdorf
Abstract: Amphiphilic biologically active peptides and intermediates. For example, the polypeptide comprises a chain of at least four groups of four amino acids. In each group of four amino acids, two amino acids are hydrophobic, one amino acid is basic hydrophilic, and the remaining amino acid is basic or neutral hydrophilic. A preferred amino acid sequence is Ala-Phe-Ser-Lys.
Abstract: The present invention relates to compositions useful as thickening agents for aqueous systems. More particularly, it relates to compositions comprising smectite clays and cationic polymers.
Abstract: The invention relates to peptides having the general formulaH.sub.2 N - W - Ser - Asp - Lys - X - OHwherein X represents a Pro or Lys residue or a valence bond and W represents a Thr or Pro residue or a valence bond with the proviso that if X represents a Pro residue then W also represents a Pro residue; to a process for the preparation of the same and to therapeutic compositions containing said peptides.
Type:
Grant
Filed:
March 6, 1990
Date of Patent:
May 12, 1992
Assignee:
Societe de Conseils de Recherches et d'Applications Scientifiques
Abstract: Disclosed is a novel peptide having one of the formulae: ##STR1## (A and B are the amino acids: wherein if A is D- or L-Pro, B is Har or Cit;if A is D-Pro, B is D-Arg, andif B is D- or L-Arg, A is Sar, Pip, Aze or Arg)Asn-A-L-(D-)Pro-Arg-(Gly).sub.n(A is Ser, Thr or Ala, n is 1 or 0)A-Ser-Pip-Arg(A is Pro-Asn-, Asn- or Pro-) ##STR2## (A is cyclopentylcarbonyl, Pro or pGlu; B is Gly or .beta.-Ala, W is a hydrogen atom or a group having the formula: or a peptide having the formula: ##STR3## wherein A and B have the same meanings as mentioned above, respectivelypGlu-Asn-Ser-A-B-(Gly).sub.n(A is Aze, D- or L-Pro, Pip or Sar, B is D- or L-Arg, Cit, Har, Lys or Orn, n is 1 or 0) andPro-(Asn).sub.m -Ser-L-(D-)Pro-Arg-(Gly).sub.n(m and n are independently 0 or 1)their functional derivatives, and pharmaceutically acceptable salts thereof.
Abstract: A peptide preparation from hydrolysis of whey containing peptides with a molecular weight of up to 6,000 Dalton. Such a preparation is hypoallergenic and therefore useful in food products and stimulants, such as mother's milk substitutes, edible ice, protein beverages and other products, usually containing milk or milk protein, in particular for allergics or humans with lactose malabsorption. The preparation is produced by a combination of enzymatic hydrolysis and ultra filtration.
Type:
Grant
Filed:
July 8, 1991
Date of Patent:
May 12, 1992
Inventors:
Ernst-Gunnar Samuelsson, Otto M. Poulsen
Abstract: A series of carboxyl-containing N-alkyldipeptides have been found to posess antiviral potency--specifically against herpes simplex virus--by selectively inhibiting the viral ribonucleotide reductase enzyme.
Type:
Grant
Filed:
July 28, 1989
Date of Patent:
May 5, 1992
Assignee:
Merck & Co., Inc.
Inventors:
Richard L. Tolman, Wallace T. Ashton, Mu T. Wu