Abstract: A solid phase method for the synthesis of a plurality of differently substituted thiophenes with a wide variety of side-chain substituents as compounds of potential therapeutic interest is disclosed. The thiophenes are prepared by acylation of a substrate-bound primary or secondary amine with cyanoacetic acid and reaction of the resulting cyanoacetamide with an isothiocyanate in the presence of a base. Alkylation with an appropriate alkyl halide, followed by Thorpe-Ziegier-cyclization yields differently substituted, support-bound 3-aminothiophenes. These may be screened on the substrate or cleaved from the substrate and then screened in solution. Alternatively, the resin-bound 3-amino thiophenes or the synthetic intermediates can be subjected to further synthetic transformations (N-acylation, reduction) on the support, which permits the preparation of further therapeutically interesting compounds.

Abstract: The present invention relates to enzyme-containing granules comprising (a) an enzyme and (b) a core which intrinsically is capable of absorbing at least 5% w/w (based on the weight of the core) of water and to processes for the production of such granules comprises (a) contacting absorbent cores, capable of absorbing at least 5% w/w (based on the weight of the core) of water, with a liquid medium, such as an aqueous medium, containing an enzyme in dissolved and/or dispersed form, the amount of the liquid medium employed being such that substantially no attendant agglomeration of the resulting product occurs; and (b) at least partially removing volatile components of the liquid medium from the resulting product.

Abstract: The present invention relates to a method for the production of saccharide preparations, i.e., syrups, by saccharifying a liquefied starch solution, which method comprises a saccharification step during which step one or more enzymatic saccharification stages takes place, and the subsequent steps of one or more high temperature membrane separation steps, and re-circulation of the saccharification enzyme, in which method the membrane separation steps are carried out as an integral part of the saccharification step. In another specific aspect, the invention provides a method of producing a saccharide preparation, which method comprises an enzymatic saccharification step, and the subsequent steps of one or more high temperature membrane separation steps and re-circulation of the saccharification enzyme.

Abstract: The present invention relates to a storage-stable liquid formulation comprising a laccase comprising (i) a laccase, (ii) at least one polyalcohol, which formulation has a pH which is more alkaline than the pH optimum of the laccase. It is also an object of the invention to provide a method for improving the storage-stability of liquid formulations comprising a laccase and the use of said liquid formulations for a personal care application or for bleaching or for textile applications such as dyeing of fabrics.

Abstract: The present invention relates to 1,4-disubstituted piperazines of the general formula ##STR1## wherein X, Y, Z, R.sup.1, R.sup.2 and r are as defined in the detailed part of the present description or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation as well as their use for the treatment of indications caused by or related to the secretion and circulation of insulin antagonising peptides, e.g. non-insulin-dependent diabetes mellitus (NIDDM) and ageing-associated obesity.

Abstract: The present invention relates to a method for the production of saccharide preparations, i.e., syrups, by saccharifying a liquefied starch solution, which method comprises a saccharification step during which step one or more enzymatic saccharification stages takes place, and the subsequent steps of one or more high temperature membrane separation steps, and recirculation of the saccharification enzyme, in which method the membrane separation steps are carried out as an integral part of the saccharification step.

Abstract: Novel peptide derivatives, compositions containing them, and their use for treating medical disorders resulting from a deficiency in growth hormone are disclosed. The peptides have the formula (I): ##STR1## wherein a, b, A, R.sup.1, L.sup.1, D, R.sup.3, R.sup.4, R.sup.2, L.sup.2, E and G are as defined in the specification. These peptides exhibit improved resistance to proteolytic degradation, and hence, improved bioavailability.

Abstract: An acidic phospholipase is obtained from a strain of the genus Hyphozyma. It is able to hydrolyze both fatty acyl groups in intact phospholipid. Advantageously, it has no lipase activity and is active at very low pH; these properties make it very suitable for use in oil degumming, as enzymatic and alkaline hydrolysis (saponification) of the oil can both be suppressed. The phospholipase is not membrane bound, making it suitable for commercial production and purification.

Abstract: Compounds of the general formula I ##STR1## compositions containing them, and their use for treating medical disorders resulting from a deficiency in growth hormone are described.

Abstract: Compounds of peptide mimetic nature having the general formula I ##STR1## wherein a and b are independently 1 or 2, R.sup.1 and R.sup.2 are independently H or C.sub.1-6 alkyl, G and J are independently, inter alia, aromats, and D and E are independently several different groups are growth hormone secretagogous with improved bioavailability.

Abstract: A plastic adaptor top for adapting to a chosen syringe a standard cartridge of the kind having a neck with a flange and being closed by a rubber membrane sealingly secured against the flange by a metal cover having its edge beaded behind the flange. This plastic top has a bore for receiving the neck part of the cartridge, which bore has a diameter making it fit over the metal cover and is provided with protrusions gripping behind the edge of the metal cover when the neck part is inserted in the bore. The outer contour of the adaptor top is provided with threads coaxial with the bore to receive a needle hub in a way causing the needle to penetrate the membrane of the cartridge when the hub is mounted on the thread of the plastic top.

Abstract: The present invention relates to compounds, compositions containing them, and their use for treating medical disorders related to binding to human somatostatin receptor subtypes.

Abstract: A method for continuously biopolishing cellulose-containing fabrics is disclosed. This method involves (a) contacting the fabric with a cellulase having low affinity for cellulose and (b) subjecting the contacted fabric to high temperature. Treatment of the cellulose-containing material may be carried out as an additional step or a combined step with chemical preparation, dyeing, printing and finishing. This treatment results in excellent pilling performance, minimal loss in fabric strength and weight, and better wettability.

Abstract: Insulin preparations of superior physical stability, comprising dissolved and/or precipitated human insulin or an analogue or derivative thereof, and a water-soluble reduced or non-reducing carbohydrate containing at least 4 carbon atoms in the main carbohydrate structure, or a water-soluble non-reducing ester and/or ether derivative of a carbohydrate or reduced carbohydrate containing at least 4 carbon atoms in the main carbohydrate structure, or mixtures thereof are disclosed.

Abstract: The present invention relates to microbial pectate lyases, more specifically to microbial enzymes exhibiting pectate lyase activity as their major enzymatic activity in the neutral and alkaline pH ranges, to a method of producing such enzymes, and to methods for using such enzymes in the textile, detergent and cellulose fiber processing industries.

Abstract: The present invention relates to variants of a Family 7 cellulase comprising one or more mutations of the amino acid sequence of the cellulase in which each mutation is independently a substitution of an amino acid residue with another amino acid or an insertion of at least one amino acid residues, wherein the variant has a modified H-bonding potential and hydrophobic interaction relative to the cellulase. The present invention also relates to the use of the cellulase variants in detergent compositions, especially for soil removal or color clarification or preventing backstaining; in fabric softeners; for bio-polishing of textiles; for drainage improvement of paper pulp; for deinking of old paper; for plant degradation.

Abstract: Divalent cation crystals of human growth factor (hGH) or derivatives thereof, and pharmaceutical preparations comprising divalent cation crystals of hGH. In specific embodiments, the divalent cation is Zn++ and the molar ration Zn++ and hGH is about 0.2 to about 10.

Abstract: The present invention relates to novel affinity ligand-matrix conjugates comprising a ligand with the general formula (a) ##STR1## which ligand is attached to a support matrix in position (A), optionally through a spacer arm interposed between the matrix and ligand. The invention furthermore relates to these novel affinity ligand-matrix conjugates and the preparation and use thereof in the purification of proteinaceous materials such as e.g. immunoglobulins, insulins, Factor VII, or human Growth Hormone or analogues, derivatives and fragments thereof and precursors.

Abstract: The present invention relates to novel N-substituted azaheterocyclic compounds of the general formula ##STR1## wherein X, Y, Z, R.sup.1, R.sup.2 and r are as defined in the detailed part of the present description, or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neuragenic pain or inflammation as well as their use for treatment of indications caused by or related to the secretion and circulation of insulin antagonising peptides, e.g. non-insulin-dependent diabetes mellitus (NIDDM) and ageing-associated obesity.

Abstract: The invention relates to modified polypeptides with reduced allergenicity comprising a parent polypeptide with a molecular weight from between 10 kDa and 100 kDa conjugated to a polymer with a molecular weight (M.sub.r) in the range of 1 kDa and 60 kDa. The modified polypeptide are produced using a process including the step of conjugating from 1 to 30 polymer molecules with the parent polypeptide. Further the invention relates to compositions comprising said polypeptides and further ingredients normally used in e.g. detergents, including dishwashing detergents and soap bars, household article, agrochemicals, personal care products, cosmetics, toiletries, oral and dermal pharmaceuticals, composition for treating textiles, and compositions used for manufacturing food and feed. Finally the invention is directed to uses of polypeptides with reduced allergenicity or compositions thereof for reducing the allergenicity of products for a vast number of industrial applications.