摘要:
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.
摘要:
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.
摘要:
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.
摘要:
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.
摘要:
A novel class of substituted piperidines, pharmaceutical compositions comprising them and use thereof in the treatment of diseases and disorders related to the histamine H3 receptor. More particularly, the compounds are useful for the treatment of diseases and disorders in which an interaction with the histamine H3 receptor is beneficial.
摘要:
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.
摘要:
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.
摘要:
The present invention is directed to liquid, aqueous pharmaceutical compositions stabilised against chemical and/or physical degradation containing Factor VII polypeptides, and methods for preparing and using such compositions, as well as vials containing such compositions, and the use of such compositions in the treatment of a Factor VII-responsive syndrome. The main embodiment is represented by a liquid, aqueous pharmaceutical composition comprising at least 0.01 mg/mL of a Factor VII polypeptide (i); a buffering agent (ii) suitable for keeping pH in the range of from about 4.0 to about 9.0; and at least one stabilising agent (iii) comprising a R—CHO motif, e.g. Benzaldehyde, 3-hydroxybenzaldehyde, 4-hydroxybenzaldehyde, or 5-formyl-4-methylimidazole.
摘要:
Disclosed is a novel class of substituted imidazole compounds, pharmaceutical compositions containing them and uses of these compounds in the treatment and/or prevention of diseases and disorders related to the histamine H3 receptor. More particularly, these compounds are useful for the treatment and/or prevention of diseases and disorders in which an interaction with the histamine H3 receptor is beneficial. These imidazoles compounds have the formula I wherein R1, R2, R3, R4, R5, R6, A, X, Y and Z are as defined in the specification.