Abstract: The present invention relates to novel "pseudo" nonapeptide and decapeptide derivatives of LHRH. More particularly the present invention relates to derivatives of LHRH wherein the nitrogen atom of at least one of the amide bonds has been alkylated.

Abstract: The subject of the invention is a procedure for the preparation of water-soluble macromolecular conjugates of hemoglobin, characterized in that:in the first step, Z sites are bound to a polymer P, the Z sites containing, on the one hand, at least one negative charge borne for example by sulfate groups and intended to lead to the formation of an ionic linkage with hemoglobin, and containing, on the other hand, at least one carboxylic group for example intended to lead to the formation of a covalent linkage with hemoglobin,then in the second step, the polymer P containing the Z site(s) is made to react with hemoglobin in the oxygenated form in order to form, on the one hand, at least one ionic linkage between at least one of the Z sites borne by the polymer and hemoglobin and, on the other hand, at least one covalent linkage between the same Z site mentioned above borne by the polymer and hemoglobin.

Abstract: Synthesis and use of novel oligopeptides are described, many of which peptides contain one or several unnatural amino acids. These short linear peptide derivatives are characterized by the presence of a free sulfhydryl function. These compounds have a high affinity for the Atrial Natriuretic Peptide (ANP) receptor coupled to particulate guanylate cyclase. Such peptides are full agonists at the ANP receptor as demonstrated by the ability of the peptides to stimulate the production of cGMP and to relax smooth muscles in vitro. In accord with these observations, the compounds of the invention lower blood pressure in mammals. Preferred peptides are the following:Cys-Cha-Gly-Gly-Arg-Ile-Asp-Arg-Ile-GlyNH.sub.2 ; D-Cys-Cha-Gly-Gly-Arg-Ile-Asp-Arg-Ile-GlyNH.sub.2 ; L-Pen-Cha-Gly-Gly-Arg-Ile-Asp-Arg-Ile-GlyNH.sub.2 ; and Cys-Cha-Gly-Gly-Arg-Ile-Asp-Arg-IleNH.sub.2.

Abstract: Various specific human SP-18 and human SP-5 derived peptides have alveolar surfactant protein (ASP) activity. These peptides are prepared using synthetic methods or by recombinant techniques. The peptides of the invention include surfactant proteins having serine replacements for the cysteines.

Abstract: The subject of the invention is peptide derivatives corresponding to formulaX.sup.1 - X.sup.2 - Gly - Asp-X.sup.3 - X.sup.4 (I)in which:X.sup.1 represents a hydrogen atom, a N-protecting group, an amino acid residue or a N-protected amino acid residue,X.sup.2 represents a residue of L-Arg or D-Arg, L-Orn or D-Orn, N-aminocarbonyl -L-Orn or N-aminocarbonyl-D-Orn, or L-Lys, or D-Lys,X.sup.3 represents a residue of L-Trp, D-Trp, L-Leu, D-Leu, L-Ile, D-Ile, L-Phe, D-Phe or a chain of 2 or 3 of these residues, andX.sup.4 represents a -OH group, -NH.sub.2 group, -OR.sup.1 group in which R.sup.1 represents an alkyl radical of C.sub.1 to C.sub.4, a NHR.sup.2 group in which R.sup.2 represents an alkyl radical of C.sub.1 to C.sub.4, or an amino acid residue.These derivatives are useful in therapy on account of their platelet aggregation inhibiting activity.

Abstract: Disclosed herein are derivatives of atrial natriuretic peptides which are characterized by having (at position 124 or at positions 106 and 124) a phenylalanyl residue bearing a fluoro or trifluoromethyl substituent on the aromatic portion thereof. Optionally, the exocyclic N-terminal peptide segment and the first cystienyl residue (at position 105) are replaced by an optionally substituted thioalkanoyl residue. The derivatives possess useful diuretic, natriuretic and antihypertensive activities.

Abstract: Analogs of the 17-membered ring portion of ANF wherein the cysteine moiety is replaced with dipeptidyl moieties, specifically, Phe-Pro, NMP-Pro, Pro-Pro, Val-Pro, Lys-Pro, Ile-Pro, Arg-Pro, HAr-Pro, Dly-Pro, Arg-Pro, Lys-BAr, Arg-Pro, CyA-CyA, Cys-Cys, or with .alpha.-aminoheptanoic acid result in analogs of ANF having increased potencies and metabolic stability.

Abstract: The present invention is a process for preparing a pharmaceutical composition comprising a biologically active conjugated protein. It comprises a polyethylene glycol or a polyoxyethylated polyol conjugated to IL-2. This protein is conjugated to reduce its immunogenicity, and increase its solubility, and increase its circulating in vivo half-life.

Abstract: The subject of the invention is a water-soluble macromolecular conjugate of hemoglobin characterized in that it is constitutedon the one hand, by hemoglobin,on the other, by a water-soluble polymer P containing polar groups, this macromolecular conjugate contains Z sites, bound to the polymer P and containing at least one negative charge carried for example by sulfate groups, the polymer P being bound to hemoglobinon the one hand, through the intermediary of at least one linkage established between at least one of the Z sites contained in the polymer and hemoglobin,and, on the other, through the intermediary of at least one covalent linkage established between the polymer and hemoglobin, or between at least one of the Z sites contained in the polymer and hemoglobin.The macromolecular conjugates according to the invention exhibit a lower affinity for oxygen than that of free hemoglobin.

Abstract: The present invention relates to a process for preparing peptide synthons in which the optical purity of each of the peptides to be condensed is retained.According to this process, a silyl derivative of an amino acid or peptide, which is activated by a complex chloroimmonium salt, a complex coordinated phosphorus halide, oxyhalide salt or a complex oxalyl halide salt, is prepared. The activated peptide is then condensed with an N-silyl amino acid or peptide in which the acid group is protected.

Abstract: A novel peptide possessing excellent antihypertensive activity is disclosed. The peptide has the formula:Pro-Thr-His-Ile-Lys-Trp-Gly-Asp (I)and can be prepared by purifying a fluid extracted from fish tissues or by combining constituting amino acids by a peptide synthesis method. It exhibits excellent ACE inhibitory activity, low toxicity, and good stability, and is thus an extremely useful and effective antihypertensive substance.

Abstract: Insulin preparations with improved properties for parenteral administration can be prepared at pH values of about 3 to 8.5 by presence of magnesium ions in concentration of about 0.005 to 0.5M, a preferred range is 0.02M to 0.5M.

Abstract: A novel and convenient process is described for providing protected amino acids and activating agents for solid phase synthesis which drastically reduces the capital costs of equipment required for the preparation of peptides. The two normally very reactive reagents, when mixed as anhydrous powders are shelf stable and yet form an active compound rapidly when mixed together in solution. This invention presents a method for combining these highly reactive dry solids in a manner which makes them unreactive and shelf stable at room temperature for extended periods of time. Once the solids are dissolved in solvent, a highly reactive amino acid ester that can readily be used in solid phase peptide synthesis is formed. This method of delivery of reagents to an automated peptide synthesizer allowers a very simplified instrument to be constructed using fewer and less expensive components and significantly reducing the associated software required.

Abstract: The present invention relates to methods of treating mental disorders and memory deficits not caused by HIV infection. The methods involve administration of a thymoleptic effective amount of defined linear peptides to patients. The peptides can be administered for example, as a powder or a solution obtained by dissolving a powder in a pharmaceutically acceptable solvent.

Abstract: An atrial natriuretic peptide having profound natriuretic, diuretic and hypotensive effects, characterized by a 45 amino acid residue sequence: ##STR1## having a disulphide bond between the cysteine residues which may be extracted from mammalian heart atria is described. A synthetic peptide comprising the above sequence of 45 amino acids and a synthetic 29 amino acid residue peptide corresponding to residues 17-45 of the above sequence both containing a disulfide linkage between the cysteine residues have also been prepared and shown to have similar biological activity as the native peptides. A synthetic 23 amino acid residue peptide corresponding to residues 23-29, which is the disulphide bonded ring portion of the above sequences, has been shown to have biological activity.

Abstract: Novel peptides having potent natriuretic activity are disclosed with the following amino acid sequence: ##STR1## wherein X is L-Ile, D-Ile, D-allo-Ile, L-Met or D-Met, Y is Gly, L-Ala or D-Ala, A is optionally absent or is Ser, Ser-Ser, Arg-Ser-Ser, Arg-Arg-Ser-Ser, Leu-Arg-Arg-Ser-Ser or Ser-Leu-Arg-Arg-Ser-Ser and B is optionally absent or is Asn, Asn-Ser, Asn-Ser-Phe, Asn-Ser-Phe-Arg, or Asn-Ser-Phe-Arg-Tyr, provided that at least one of Y.sup.10, Y.sup.16, Y.sup.20 or Y.sup.22 is Ala or D-Ala, and the amides, lower alkyl esters and the physiologically acceptable metal salts and acid addition salts thereof.

Abstract: The present invention relates to a renal growth promoter based on the finding that luteinizing hormone or an isoform thereof has an effect of promoting renal growth.It was previnsly unknown that luteinizing hormone or an isoform thereof has an effect of promoting renal growth.With the present invention, it is expected that kidneys suffering from a decreased in the number of renal cells or a lowering in the renal function may be activated by administering luteinizing hormone or an isoform thereof.

Abstract: The invention is directed to a method for purifying sequentially synthesized peptides and oligonucleotides by immunoaffinity techniques. Selected products are lapped with an antigenic capping agent and are conjugated with antibodies that are specific for the capping agent.

Abstract: Process for the production of peptides of general formula R.sup.1 CO--NHR.sup.2 (1), where R.sup.1 CO-is the carboxy component and R.sup.2 NH-is the amino component of a peptide building block. The process is characterized in that a carboxylic acid of general formula R.sup.1 COOH (II), where R.sup.1 CO- has the above meaning, is made to react with a carboxylic acid imide choloride of general formula (III), wherein X is a hydrogen atom, an alkyl group with a maximum of 4 carbon atoms, a fluorine atom, a cholorine atom or a nitro group, Y is a fluorine atom, a chlorine atom or a nitro group and Z has the same meaning as Y or is a hydrogen atom, and the diacylamine of general formula (IV), where R.sup.1, C, Y and Z have the above meaning, is bound to an amine of general formula R.sup.2 NH.sup.2 (V), where R.sup.2 NH- have the above-mentioned meaning.

Abstract: Compounds and compositions comprising synthetic analogs of Atrial Natriuretic Peptides are provided, together with methods for their production and use as natriuretics, diuretics and/or vasodilators, or as intermediates for or modulators of such useful compounds or of native Atrial Natriuretic Peptides.