摘要:
Therapeutically active compounds of formula (I) or (II), in which R1 is hydrogen, alkyl, alkenyl, aryl, arylalkyl, hydroxyalkyl, halogenalkyl, alkoxy, COR10, CONR10R11, OR10, S(O)mR10, NR10COR11 or NR10R11, where R10 is hydrogen, alkyl, alkenyl, aryl, arylalkyl, hydroxyalkyl, halogenalkyl, alkoxy or hydroxy and R11 is hydrogen, alkyl, aryl, arylalkyl, alkoxy, aryloxy, hydroxy or acyl, or in case where X is NR11, R1 can also be carboxylalkyl; R6 is hydrogen, alkyl, alkenyl, aryl, arylalkyl; R2 and R7 mean hydrogen, alkyl, aryl, arylalkyl, alkenyl, COR10, CONR10R11, halogen, trifluoromethyl, nitro or cyano, where R10 and R11 are defined as above; R3 is hydrogen, alkyl, aryl or arylalkyl; A means alkyl or substituted alkyl, m is 0-2 and n is 1-3; Y means O, NR11 or S, where R11 is the same as above; X means O, NR11 or S, where R11 is the same as above, R4, R5, R8 and R9 mean independently one of the following groups (a), (b), (c), (d), (e), (f), (g), or in case where X is NR11, R4, R5, R8 and R9 can also independently mean HOOC-, R12OOC-, H2NCO- or HOHNCO-, wherein R12 means alkyl, arylalkyl or aryl, and wherein each aryl residue defined above by itself or as part of another group may be substituted, and pharmaceutically acceptable salts and esters thereof. The compounds have phospholamban inhibiting activity and are useful for treating heart failure.
摘要:
An ultrasonic processing method by which polymer/drug composites can be quickly and efficiently molded to form matrix-type drug delivery systems is disclosed. The advantages of the method include speed and good control of the process. Il also causes less degradation in polymers and/or drugs than most conventional processing methods.
摘要:
Aminoterminal propeptide of type I procollagen exists in serum in two forms: classical type I procollagen which is a heterotrimer containing two pro α1-chains and one pro α2-chain of type I procollagen, and an α1-homotrimer type I procollagen containing three identical pro α1-chains. These intact, trimeric aminoterminal propeptides may be isolated without the use of proteolytic enzymes and the resultant propeptides may be used to prepare antibodies specific for the intact trimeric propeptide, having no affinity for the monomeric form of the propeptide. Such antibodies are useful in methods of assaying intact trimeric aminoterminal propeptide of type I procollagen in serum, without false information resulting from inadvertent assay of the monomeric form of the propeptide.
摘要:
The invention provides a binding assay reagent comprising a backbone polypeptide comprising glutamic acid residues and lysine residues is proportions such that the backbone polypeptide has a net positive charge, said backbone polypeptide having a molecular mass of ≧ 2.0 x 10⁵ Daltons; an optical dye label covalently bound to the backbone polypeptide, a specific binding molecule covalently bound to the backbone polypeptide, and an enhancing peptide associated with the backbone polypeptide, said enhancing peptide being comprised of a mixture of a) acidic and basic amino acid monomer residues having opposite stereochemical configurations or b) mixtures of homopolymers of acidic amino acids and basic amino acids wherein the homopolymers may be of the same or different stereochemical configurations, and wherein said enhancing peptide is electrically neutral or has a net negative charge. The binding assay reagents exhibit enhanced binding activity over that of the dye labelled polypeptides alone and also enhance the sensitivity of the binding assay by providing increased amounts of optical label.
摘要:
The invention relates to free nano-sized particles of active agents e.g. therapeutic, cosmetic or diagnostic agents, and to a method for the preparation of such particles. The method comprises providing a liquid feed stock comprising an active agent or combination of two or more active agents, atomising the liquid feed stock, suspending the droplets in a carrier gas, and passing the carrier gas and droplets through a heated tube flow reactor under predetermined residence time and temperature history, and collecting the particles produced. Nano-sized crystalline spherical uncharged particles with narrow aerodynamic particle size distribution and rough surfaces, are obtained. The particles show improved dissolution rate in-vitro and bioavailability in-vivo, dispersibility and stability.
摘要:
Aminoterminal propeptide of type I procollagen exists in serum in two forms: classical type I procollagen which is a heterotrimer containing two pro α1-chains and one pro α2-chain of type I procollagen, and an α1-homotrimer type I procollagen containing three identical pro α1-chains. These intact, trimeric aminoterminal propeptides may be isolated without the use of proteolytic enzymes and the resultant propeptides may be used to prepare antibodies specific for the intact trimeric propeptide, having no affinity for the monomeric form of the propeptide. Such antibodies are useful in methods of assaying intact trimeric aminoterminal propeptide of type I procollagen in serum, without false information resulting from inadvertent assay of the monomeric form of the propeptide.
摘要:
The present invention is concerned with controllably dissolvable silica-xerogels prepared via sol-gel process and their use. Specifically, the invention is concerned with a delivery device comprising controllably dissolvable silica-xerogel into which structure a biologically active agent is incorporated. The invention is further concerned with pharmaceutical preparations comprising said delivery device. Further, the invention is directed to medical devices for orthopedic and surgical purposes comprising controllably dissolvable silica-xerogels, which may further comprise a biologically active agent.
摘要:
Products containing a nonsteroidal anti-estrogen or a pharmaceutically acceptable salt thereof and a glucocorticoid are disclosed as a combined preparation for concomitant use in treatment of auto-immune diseases.