Abstract: The present technology provides methods of generating the peptides, and pharmaceutically acceptable salts of the peptides and intermediates thereof. In some embodiments, the peptide is D-Arg-2?6?-Dmt-Lys-Phe-NH2.

Abstract: The present invention relates to an ionic liquid based support of Formula-I: wherein: X+ is a heteroatom containing cationic part; W is a halogen containing polymeric solid support; n is an integer in the range of 2 to 8; Y is a hydrophobic anion; R is selected from CO—Z or Z; Z is selected from the group consisting of —Cl, —Br, —OH, —O-Alkyl and combinations thereof. The present invention also relates to a process for preparation of said ionic liquid based support used for di, oligo or polypeptide manufacture.

Abstract: We describe methods that allow either carbodiimides or other carboxyl-reactive substances to be mixed with solutions of carboxylic acids or phosphates or amines or combinations thereof, so as to form a homogeneous mixture which is then dried, preferably in a freeze drying process. The mixture is then contacted with an entity, which preferably involves the dissolution of the mixture with a buffered solution of the entity, so as to initiate a conjugation reaction between the entity and a component in the mixture.

Abstract: Peptides may be produced by using (A) a first amino acid or peptide, which is converted into its ionic liquid form through the formation of an ionic bond, as a substance serving as both a reaction solvent and a reaction starting material; and reacting the first amino acid or peptide with (B) an ester of second amino acid or peptide, in the absence of any peptide hydrolase or any condensation agent, in the presence of water in an amount of not more than 20% by mass relative to the total mass of the reaction system to form a peptide bond between the first amino acid or peptide and the second amino acid or peptide. By means of this process, it is possible to synthesize a peptide at a high concentration and at a high yield, and this method is excellent for producing peptides on an industrial scale.

Abstract: A subject of the invention is the use of a salt with a dedicated task of formula (I): A+-L-R—OY, X? as soluble support for peptide synthesis, in which: X? represents a functional or non-functional anion, Y represents either a hydrogen atom, or a —COOR1 group, R1 representing in particular an alkyl group comprising 1 to 20 carbon atoms, A+ represents a cationic entity, L represents an arm, in particular an alkyl group of 3 to 20 carbon atoms, R represents in particular a group of formula —C(Ra)(Rb)—, Ra and Rb representing independently of one another in particular a hydrogen or an alkyl group, comprising 1 to 20 carbon atoms.

Abstract: The invention relates to novel luminescent compositions of matter containing two fluorophores (sensitizers), synthetic methods for making the compositions, macromolecular conjugates of the compositions, and the use of the compositions and their conjugates in various methods of detection. The invention also provides kits containing the compositions and their conjugates for use in the methods of detection.

Abstract: A catalytically active peptide comprising an imidazole function in position i flanked by at least one functional group to be amidated in position i+3+4k, where k is an integer equal to or higher than ?1 or in position i?4?4n, wherein n is an integer equal to or higher than 0, characterized in that it also comprises at least one activating group in position i+4+4n or i?3?4n, respectively, wherein n is as above.

Abstract: A method for preparing a solid support material for carrying out a chemical reaction, said method comprising the following steps: (i) reacting an amino functionalised solid material with a carboxylic acid having at least two similarly protected amino groups to form amide bonds between them, (ii) removing protecting groups in a single step, (iii) optionally repeating steps (i) and (ii) one or more times using the product of the preceding step as the amino functionalised solid material, and (iv) connecting a linkage agent to at least some of the free NH2 groups of the product. The method increases the loading capacity of the solid support material. It is particularly useful in connection with peptide synthesis.

Abstract: The present invention relates to a process for forming an N-&agr;-amino protected amino acid fluoride in situ by reacting an N-&agr;-amino protected amino acid with an ionic fluoride salt in the presence of a peptide coupling agent. It is also directed to the use of the amino acid fluoride thus formed in peptide synthesis.

Abstract: Novel alkoxythiocarbonylimidazoles provide new reagents for the N-terminal sequencing of small polypeptide samples. These reagents form an alkoxy thiourea derivative which is cleaved with acid to remove the N-terminal amino acid as a stable thiazolinone which does not rearrange to a thiohydantoin. This thiazolinone may be derivatized to provide a detectable group such as a fluorescent group or ionizable group detectable by mass spectrometry.

Abstract: The present invention is drawn to a process for forming an amide bond linkage comprising reacting a carboxylic acid and an amine in a two-phase mixture of water and an organic solvent selected from an oxygenated organic solvent or an aromatic solvent in the presence of a coupling reagent and an additive. This process is useful for making ubiquitous amides and polypeptides having various biological activities.

Abstract: A process is disclosed for the manufacture of amides, including peptides, in which a carboxylic acid is reacted with a primary or secondary amine in the presence of a carbodiimide and a catalytic amount of N-hydroxy compound.

Abstract: This invention relates to a process for forming an amide or an ester from a reaction between an amine or an alcohol, respectively and an acylating derivative of a carboxylic acid, in the presence of an effective amount of a compound having the formula: ##STR1## and N-oxides thereof and salts thereof.

Abstract: A process for producing peptide derivatives of formula (1) or salts thereof: ##STR1## which comprises condensation of peptide derivative of formula (2): ##STR2## with carboxylic acid of formula (3): ##STR3## or condensation of a peptide derivative of formula (4): ##STR4## with a protected amino acid of formula (5'): ##STR5## wherein R.sup.1 and R.sup.2 are a lower alkyl group or hydrogen atom, R.sup.3 is a lower alkyl group, X is a methylthiomethyl, methanesulfonylmethyl, carbamoylmethyl, or a lower alkyl group, Ar is an aryl or heteroaryl group, and A.sup.4 is Ar--O--CH.sub.2 --CO. The peptide derivatives and salts thereof are useful as the human immunodeficiency virus (HIV) protease inhibitors.

Abstract: A process for the manufacture of amides, including peptides, by reacting a carboxylic acid with a primary or secondary amine in the presence of a carbodiimide and a catalytic amount of a N-hydroxy compound.

Abstract: A liquid phase peptide synthetic method which uses (1) Fmoc as the protecting group for the non-side chain amino functionality, (2) ammonia, a primary or secondary amine to remove the Fmoc protecting group, and (3) substituted carbodiimide as the coupling agent for the C to N synthesis of peptides or peptide derivatives in a proper organic solvent.

Abstract: The present invention is drawn to a process for forming an amide bond linkage comprising reacting a carboxylic acid and an amine in a two-phase mixture of water and an organic solvent selected from an oxygenated organic solvent or an aromatic solvent in the presence of a coupling reagent and an additive. This process is useful for making ubiquitous amides and polypeptides having various biological activities.

Abstract: Activated carboxylic acid modified polyethylene membranes useful in the C-terminal sequencing of a peptide are disclosed. The membranes comprise activated carboxylic acid modified polyethylene having a linker coupled to an amide linkage to the surface carboxyl radicals of the membrane. Activation is accomplished by reaction of the carboxylic acid modified polyethylene membrane with DCC, CDI, EDC, BOP, DICD or 2-fluoro-1-methyl pyridine.

Abstract: This invention relates to a process for forming an amide or an ester from a reaction between an amine or an alcohol, respectively and an acylating derivative of a carboxylic acid, in the presence of an effective amount of a compound having the formula: and N-oxides thereof and salts thereof.

Abstract: This invention relates to a process for forming an amide or an ester from a reaction between an amine or an alcohol, respectively and an acylating derivative of a carboxylic acid, in the presence of an effective amount of a compound having the formula: and N-oxides thereof and salts thereof.