Abstract: Compounds of the formula: as well as pharmaceutically usable salts and esters thereof, wherein R.sup.1, R.sup.2 and R.sup.3 have the significance ascribed herein, inhibit binding of adhesive proteins to the surface of different types of cell and accordingly influence cell--cell and cell-matrix interactions. These compounds can be used in the form of pharmaceutical preparations for the control or prevention of neoplasms, tumor metastasing, tumor growth, osteoporosis, Paget's disease, diabetic retinopathy, macular degeneration, restenosis following vascular intervention, psoriasis, arthritis, fibrosis, kidney failure, as well as infection caused by viruses, bacteria or fungi.

Abstract: A method for the determination of factor IXa in a sample solution using a measurable factor IXa substrate and a water-miscible alcohol and measuring the cleavage of the factor IXa substrate as a measure for factor IXa activity is suitable for the direct determination of factor IXa.

Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is lower-alkyl, cycloalkyl or phenyl,R.sup.2 is H, OH or C(O)O-A, wherein A is lower-alkyl, cycloalkyl or phenyl, andR.sup.3, R.sup.4 and R.sup.5 are either methyl or R.sup.3 is H and R.sup.4 and R.sup.5 taken together are trimethyleneas well as hydrates or solvates and physiologically usable salts thereof can be used for the production of medicaments for the treatment or prophylaxis of illnesses which are caused by thrombin-induced platelet aggregation or fibrinogen clotting in blood plasma.

Abstract: This invention relates to a novel process for the synthesis of vasoactive intestinal peptide analog Ac(1-31)--NH.sub.2 from four protected peptide fragments.

Abstract: A novel process for the manufacture of compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 independently represent aroyl. The present invention also concerns novel intermediates used in the novel process for making compounds of formula I.

Abstract: The invention provides hydroxylamine derivatives of formula (I) wherein A, R.sup.1, R.sup.2 and R.sup.3 have the significance given in the description, which are matrix metalloproteinase inhibitors and which also prevent TNF release. They are therefore useful for the control or prevention of degenerative joints diseases such as rheumatoid arthritis and osteoarthritis or for the treatment of invasive tumours, atherosclerosis or multiple sclerosis. They can be manufactured according to generally known methods.

Abstract: The present invention relates to the discovery of novel genes and proteins, which function in pathways involved in brain pathogenesis. In particular, the novel genes and proteins relate to inflammatory tissue responses caused by brain injuries such trauma, ischemia or autoimmune-inflammation or other diseases or processes related to neuroinflammation. The compounds disclosed in the present invention are useful as therapeutics, diagnostics and in screening assays.

Abstract: Novel piperidine derivatives, their manufacture and use as medicaments, are disclosed. The invention is concerned with the novel piperidine derivatives of general formula I ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, Q, X, Z, m and n are as described herein.

Abstract: This disclosure relates to novel antibodies specific to the recently discovered receptor to human interleukin 12 (IL-12R). The antibodies to IL-12R, most preferably, the monoclonal antibodies to that protein, are useful in determining the status of the human immune system and as diagnostic reagents or potential therapeutic reagents for conditions involving imbalances in IL-12 levels or cell types sensitive to IL-12 activation.Further aspects of the disclosure relate to methods of producing and purifying such novel antibodies and hybridoma cell lines capable of their production. Another aspect of the disclosure relates to an immunoprecipitation assay for the detection of solubilized IL-12R which employs, in a preferred embodiment, monoclonal antibodies to the receptor of the present invention covalently bound to Protein G-Sepharose resin.

Abstract: A novel delivery system for targeting drugs to the colon is herein described. The system is a tablet comprised of three parts: 1) an outer enteric coating, 2) an inner semi-permeable polymer membrane containing a plasticizer and 3) a central core comprising swelling excipients and an active ingredient. The novel dosage form described herein will release the drug consistently in the colon by a time-dependent explosion mechanism.This delivery system is particularly suitable for delivering viral protease inhibitors to the colon.

Abstract: Novel, chiral diarsine compounds, which are present in the (R)- or (S)- or (rac)-form, of the formula ##STR1## wherein R signifies an optionally substituted aryl from the group of phenyI, naphthyl, furyl and thienyl; C.sub.3-8 -cycloalkyl or C.sub.1-8 -alkyl;R.sup.1, R.sup.2, R.sup.3 each independently signify C.sub.1-8 -alkyl, C.sub.1-8 -alkoxy, aryloxy, F or Cl,R.sup.2 and R.sup.3 each independently also signify hydrogen orR.sup.1 and R.sup.2 together signify tetramethylene or a benzo or benzofuro system or dioxymethylene on the respective benzene ring; orR.sup.2 and R.sup.3 together signify dioxymethylene,and the manufacture of the diarsine compounds of formula I, as well as complexes of the compounds of formula I with Group VIII metal and their use for enantioselective reactions.

Abstract: Tertiary amines of the formula ##STR1## wherein A.sup.1, A.sup.2, A.sup.3, A.sup.4, L, M, p, T, and Q are as defined herein, have antimycotic and cholesterol-lowering activity.

Abstract: A process manufactures of a compound of formula: ##STR1## and unique intermediates.

Abstract: The invention relates to conjugates of lipids and basic, membrane disturbing peptides, particularly compounds of the formula(R--CONH).sub.n --R.sup.3 (I)and(R--S--S).sub.n --R.sup.3 (II)wherein R is the hydrocarbyl moiety of a straight-chain or branched-chain, saturated or unsaturated aliphatic carboxylic acid, or a phospholipid moiety having a free valence bond; R.sup.3 is a basic membrane disturbing peptide having a free valence bond at one or two carbon atom(s); and n is 1 or 2. These conjugates can be used as a vector for transfecting a cell with a polynucleotide or any other anionic macromolecule.

Abstract: The present invention provides orally administrable pharmaceutical compositions containing an inhibitor of gastrointestinal lipase, and at least one compound selected from the group consisting of chitosan, its derivatives and salts thereof. Methods are provided for preventing and treating anal leakage of oil in a patient to whom a composition containing an inhibitor of gastrointestinal lipase is orally administered.

Abstract: Polyethylene and polypropylene protein conjugates which modulate body weight of ani is and humans for the treatment, prevention and control obesity and associated diseases or conditions, and the recombinant expression of these biologically active proteins in purified and homogeneous forms.

Abstract: Polyethylene and polypropylene protein conjugates which modulate body weight of animals and humans for the treatment, prevention and control of obesity and associated diseases or conditions, and the recombinant expression of these biologically active proteins in purified and homogeneous forms.

Abstract: The invention provides amino acid derivatives of the formula ##STR1## wherein E represents CHO or B(OH).sub.2 ;R.sup.1 represents lower alkyl (optionally substituted by halo, cyano, lower alkylthio, aryl-lower alkylthio, aryl or heteroaryl), lower alkenyl or lower alkynyl;R.sup.2 represents lower alkyl optionally substituted by hydroxy, carboxy, aryl, aminocarbonyl or lower cycloalkyl; andR.sup.3 represents hydrogen or lower alkyl; orR.sup.2 and R.sup.3 together represent di- or trimethylene optionally substituted by hydroxy;R.sup.4 represents lower alkyl (optionally substituted by hydroxy, lower cycloalkyl, carboxy, aryl, lower alkylthio, cyano-lower alkylthio or aryl-lower alkylthio), lower alkenyl, aryl or lower cycloalkyl;R.sup.5 represents lower alkyl (optionally substituted by hydroxy, lower alkylthio, aryl, aryl-lower alkylthio or cyano-lower alkylthio) or lower cycloalkyl;R.sup.6 represents hydrogen or lower alkyl;R.sup.

Abstract: The invention provides an immunogenic polypeptide having the amino acid sequenceM A K S M L S G I V F A G L V A A A A A - S S A N S A A N V S V L E S G P A V Q E - V P A R T V T A R L A K P L L L L S A L - A A T L A A A F L V L Q C F N I I S S N - N Q Q T S V R R L A A G G A C G D E E D - A D E G T S Q Q A S R R R R K P D T P A - A D K Y D F V G G T P V S V T E P N V D - E V L I Q I R N K Q I F L K N P W T G Q - E E Q V L V L E R Q S E E P I L I V A R - T R Q T L E G Y L G S Q A L A Q D G K T - A K E E K V E G G K T H R R Y K V K S S - D P G Y G F P Y T T V L D G V P V G T D - E D G Y V V E V L M K T G P H G G V D M - M T S T A S Q G K F C G V L M D D G K G - N L V D G Q G R K I T A V I G M L T Q P - D T E F R S G P G D D E D D E (SEQ ID NO:1)and fragments thereof,which polypeptides are capable of inducing an immune response against Eimeria parasites, and the DNA encoding such polypeptides, as well as recombinant vectors and recombinant viruses containing the said DNA or fragments thereof and transformed micr

Abstract: Product containing tetrahydrolipstatin as the active ingredient and pharmaceutically acceptable excipients, characterized in that it is in the form of particles with a diameter of 0.25 to 2 mm; and pharmaceutical preparation s or compositions for oral administration containing the product.