Abstract: The present invention discloses a personal care composition comprising: (a) A polyvalent metal salt of pyrithione; (b) A metal complex selected from the group consisting of: wherein Y1, Y2, Z1, Z2 are selected from the following groups: —NH2, —NHR11, —NR12R12, —NHCO—R20, —SH, —OR13, —O(C?O)—, phosphate. and wherein at least one of Y1 and Z1 of compound I is —SH, and wherein at least one of Y2 and Z2 of compound II is —SH R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, can independently be H, alkyl, substituted alkyl, phenyl, aryl; R14 is —NH2, —NHCO—CH3, —NHR17, or —NR18R18 R15 is —COOH, —COOR19 R11, R12, R13 R16, R17, R18, R19 can be independently be alkyl, substituted alkyl, phenyl, aryl. and wherein the metal of the complex is selected from the group consisting of zinc, copper, and iron.

Abstract: The present invention discloses a personal care composition comprising: (a) A polyvalent metal salt of pyrithione; (b) A metal complex selected from the group consisting of: wherein Y1, Y2, Z1, Z2 are selected from the following groups: —NH2, —NHR11, —NR12R12, —NHCO—R20, —SH, —OR13, —O(C?O)—, phosphate. and wherein at least one of Y1 and Z1 of compound I is —SH, and wherein at least one of Y2 and Z2 of compound II is —SH R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, can independently be H, alkyl, substituted alkyl, phenyl, aryl; R14 is —NH2, —NHCO—CH3, —NHR17, or —NR18R18 R15 is —COOH, —COOR19 R11, R12, R13 R16, R17, R18, R19 can be independently be alkyl, substituted alkyl, phenyl, aryl. and wherein the metal of the complex is selected from the group consisting of zinc, copper, and iron.

Abstract: Methods for conjugating peptides are provided comprising i) reacting a peptide with a first compound comprising a functional group in the presence of a transglutaminase capable of incorporating said compound into the peptide to form a transaminated peptide, and ii) reacting said transaminated peptide with e.g. a functionalized polymer capable of reacting with the functional group incorporated in the peptide in the enzymatic reaction.

Abstract: Reductive amination of peptide-derived aldehydes with anilines or heteroarylamines containing a property-modifying group provides new, hydrolytically stable protein conjugates, suitable for therapy.

Abstract: Enolate salts of 4-fluoro-2-hydroxymethylene-3-oxobutyrates of formula wherein R1 is C1-10 alkyl, R2 and R3 are independently hydrogen or fluorine, M is an alkali or alkaline earth metal, and n is 1 or 2, are prepared from enolate salts of the corresponding 4-fluoro-3-oxobutyrates and carbon monoxide. The enolate salts of formula I can be alkylated or acylated to obtain the corresponding enol ethers and esters. The 4-fluoro-3-oxobutyrate starting material can be prepared from 1,1-difluoroethyl methyl ethers by SbF5-catalyzed fluoromethane elimination followed by halogen exchange with lithium chloride, reacting the thus obtained fluoroacetyl chloride with ketene and quenching with the appropriate alcohol R1—OH.

Abstract: The invention relates to methods for increasing the plasma half-life of a molecule, such as human growth hormone, comprising covalently linking the molecule to a heterocyclic carboxylic acid bioisostere.

Abstract: Certain novel benzothiazoles and benzoxazoles, e.g., 2-(piperazin-1-yl)benzothiazoles and 2-(piperazin-1-yl)benzoxazoles, optionally substituted in the 3 and/or 4 positions of the piperazine rings, having histamine H3 antagonistic activity can be used in pharmaceutical compositions.

Abstract: Enolate salts of 4-fluoro-2-hydroxymethylene-3-oxobutyrates of formula wherein R1 is C1-10 alkyl, R2 and R3 are independently hydrogen or fluorine, M is an alkali or alkaline earth metal, and n is 1 or 2, are prepared from enolate salts of the corresponding 4-fluoro-3-oxobutyrates and carbon monoxide. The enolate salts of formula I can be alkylated or acylated to obtain the corresponding enol ethers and esters. The 4-fluoro-3-oxobutyrate starting material can be prepared from 1,1-difluoroethyl methyl ethers by SbF5-catalyzed fluoromethane elimination followed by halogen exchange with lithium chloride, reacting the thus obtained fluoroacetyl chloride with ketene and quenching with the appropriate alcohol R1—OH.

Abstract: The invention relates to protracted GLP-1 compounds and therapeutic uses thereof.

Abstract: Novel polypeptide derivatives having protracted profile of action.

Abstract: The invention relates to novel compounds with formula (I) X1-X2-X3-X4-X5-(X6)n-(X7)m-Y useful as blood coagulation factor inhibitors. The compounds (I) may be used for treatment of thrombotic conditions or as stabilizers of liquid formulations of blood coagulation factors, in particular liquid formulations of FVIIa, Factor VII variants, or Factor VII derivatives.

Abstract: The invention provides derivatives of IL-21 or variants thereof, methods of producing such variants, new variants of IL-21, and various methods of using such molecules.

Abstract: Certain novel benzothiazoles and benzoxazoles, e.g., 2-(piperazin-1-yl)benzothiazoles and 2-(piperazin-1-yl)benzoxazoles, optionally substituted in the 3 and/or 4 positions of the piperazine rings, having histamine H3 antagonistic activity can be used in pharmaceutical compositions.

Abstract: Certain novel benzothiazoles and benzoxazoles, e.g., 2-(piperazin-1-yl)benzothiazoles and 2-(piperazin-1-yl)benzoxazoles, optionally substituted in the 3 and/or 4 positions of the piperazine rings,! of the general formula (1): having histamine H3 antagonistic activity can be used in pharmaceutical compositions.

Abstract: Novel polypeptide derivatives having protracted profile of action.

Abstract: Novel polypeptide derivatives having protracted profile of action.

Abstract: Protracted GLP-1 compounds and therapeutic uses thereof.

Abstract: Method for increasing half-life of compounds in plasma and novel derivatives of such compounds.

Abstract: The invention relates to novel compounds with formula (I) useful as blood coagulation factor inhibitors. The compounds (I) may be used for treatment of thrombotic conditions or as stabilizers of liquid formulations of blood coagulation factors, in particular liquid formulations of FVIIa, Factor VII variants, or Factor VII derivatives.

Abstract: Reductive amination of peptide-derived aldehydes with anilines or heteroarylamines containing a property-modifying group provides new, hydrolytically stable protein conjugates, suitable for therapy.