Abstract: The present invention concerns a novel DNA sequence coding for an Aspergillus aspartic protease, an Aspergillus aspartic protease per se and a method for the preparation thereof. The invention further concerns a novel Aspergillus mutant strain defective in a protease of the aspartic proteinase-type, which is useful for the expression of heterologous protein, and a method for the preparation of such a mutant strain.

Abstract: The invention pertains to the field of thrombin inhibitors and describes the production of modified desulphatohirudins, particularly desulphatohirudins, with the aid of genetic engineering. The present invention is also directed to a method for the denaturation and renaturation of a modified desulphatohirudin to a biologically active thrombin inhibitor and the combination of two or more of desulphatohirudins to form higher molecular weight thrombin inhibitors.

Abstract: The invention relates to a novel advantageous dosage form for sparingly soluble staurosporin derivatives, especially N-benzoyl-staurosporin. The dosage form is administrable intravenously in the form of a nanoemulsion and comprises as solubilisers a combination of phospholipids, triglycerides and partial fatty acid esters of polyoxyethylene sorbitan.

Abstract: Compounds of formula I ##STR1## wherein R.sub.1 is an aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, aromatic or heteroaromatic radical, a hydroxy group that is aliphatically, araliphatically or heteroarylaliphatically etherified or protected by a hydroxy-protecting group, or an aliphatically etherified mercapto group, andR.sub.2 is an aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, araliphatic or heteroarylaliphatic radical, orR.sub.1 and R.sub.2 together form a divalent aliphatic radical,R.sub.3 is free or aliphatically, araliphatically or aromatically esterified carboxy, formyl or hydroxymethyl,R.sub.4 is hydrogen, an aliphatic or araliphatic radical or an amino-protecting group, andR.sub.5 is hydrogen or an aliphatic radical,and the salts thereof can be used as intermediates in the preparation of medicinal active ingredients.

Abstract: .delta.-Amino-.gamma.-hydroxy-.omega.-aryl-alkanoic acid amides of formula I ##STR1## and the salts thereof, have renin-inhibiting properties and can be used as antihypertensive medicinal active ingredients.

Abstract: A method of producing compounds of formula I ##STR1## wherein one of R.sub.1 and R.sub.2 is selected from --OH, --SH, and --NHR.sub.7 ; and the other of R.sub.1 and R.sub.2 is selected from H, --OH, --SH, --NHR.sub.7, and R.sub.8 ; R.sub.3 and R.sub.4 are each independently selected from R.sub.8 ; n and m are each independently 3; and each R.sub.5 and each R.sub.6 is independently selected from --OH, --SH, --NHR.sub.7, and R.sub.8 ; and R.sub.8 is as detailed in the specification;in enantiomerically enriched form, comprising reducing a compound of formula II ##STR2## wherein R.sub.1 -R.sub.6 are defined as in formula I, in the presence of B-haloisopinocampheylborane.

Abstract: .delta.-Amino-.gamma.-hydroxy-.omega.

Abstract: The invention concerns proteins having glycosyltransferase activity, recombinant DNA molecules encoding proteins having glycosyltransferase activity, hybrid vectors comprising such recombinant DNA molecules, transformed hosts suitable for the multiplication and/or expression of the recombinant DNA molecules, and processes for the preparation of the proteins, DNA molecules and hosts.

Abstract: The invention relates to nucleosides, nucleotides and oligonucleotides carrying in their basic structure a primary hydroxyl group protected by tris-4,4',4"-tert-butylphenylmethyl, to processes for the preparation of said nucleosides and nucleotides, to a process for the preparation of oligonucleotides, and to the use of said protected nucleosides, nucleotides and oligonucleotides.

Abstract: Compounds of formula I ##STR1## wherein A, X, Z and R.sub.1 -R.sub.5 are as defined in the description, and their salts have valuable pharmaceutical properties and are effective especially against tumours. They are prepared in a manner known per se.

Abstract: The invention relates to novel substituted oxazolidines of formula (I) wherein R.sub.1 and R.sub.2 are simultaneously hydrogen or both together are the identical lower alkyl radical, and to the salts thereof in racemic and chiral form, to a process for the preparation of said compounds, to pharmaceutical compositions containing them, and to the use thereof as medicaments. The compounds have a stimulating effect on beta-adrenergic receptors and can be used, inter alia, for the treatment of diseases associated with reversible obstruction of the respiratory tract, typically asthma and chronic bronchitis, and also for inflammation of different origin.

Abstract: .delta.-Amino-.gamma.-hydroxy-.omega.-aryl-alkanoic acid amides of formula I ##STR1## and the salts thereof, have renin-inhibiting properties and can be used as antihypertensive medicinal active ingredients.

Abstract: The invention relates to a novel process for the manufacture of 4-acetoxy-3-hydroxyethyl-azetidinone of the formula ##STR1## especially 4(R)-acetoxy-3(R)-(1'(R)-hydroxyethyl)-2-azetidinone, from enantiomerically pure compounds of the formula ##STR2## in which R.sup.1 represents lower alkyl and Z.sup.1 represents amino, arylmethylamino, acylamino or azido, by reduction of the C.dbd.C double bond and optionally of the arylmethylamino or azido group with hydrogen, opening of the lactone ring, cyclisation to the .beta.-lactam, optionally after hydrolysis of the acylamino group, and oxidative decarboxylation of the original lactone carboxy group in the presence of an acetate-yielding agent. Compounds of the formula I can be used as starting materials for the manufacture of .beta.-lactam antibiotics. The invention also relates to novel intermediates and starting materials.

Abstract: The invention relates to N-acyl-N-heterocyclylalkylamino acids of the formula ##STR1## wherein Y.sub.1 is O, S or N(R) and R is hydrogen or C.sub.1 -C.sub.7 alkyl;X.sub.1 is --CO-- or --S(O).sub.m -- and the index m is 0, 1 or 2;one of the variables X.sub.2 and X.sub.4 is C.sub.1 -C.sub.4 alkylene and the other of the variables X.sub.2 and X.sub.4 is a bond; or each of the variables X.sub.2 and X.sub.4 is a bond;X.sub.3 is C.sub.3 -C.sub.7 cycloalkylidene or the structural element --C(X.sub.a)(X.sub.b)-- and X.sub.a is hydrogen or C.sub.1 -C.sub.7 alkyl and X.sub.b is C.sub.1 -C.sub.7 alkyl;and the rings A, B and C, with the exception of the substituents indicated in the formula, and also aromatic substituents are, independently of one another, unsubstituted or mono- or poly-substituted by substituents selected from the group consisting of halogen, C.sub.1 -C.sub.7 alkyl, C.sub.1 -C.sub.7 alkoxy, C.sub.2 -C.sub.7 alkenyloxy, phenoxy, benzyloxy, trifluoromethyl and S(O).sub.

Abstract: A topically administrable pharmaceutical composition comprising (A) zinc phthalocyanine complex, (B) as carrier for the complex, (i) a N-alkylpyrrolidone together with a pharmaceutically acceptable co-solvent for the complex, (ii) dimethyl sulphoxide or a mixture thereof with a pharmaceutically acceptable co-solvent for the complex, (iii) a liposome, or (iv) a N,N-dialkylbenzamide or a mixture thereof with a pharmaceutically acceptable co-solvent for the complex, and (C) a gelling agent.

Abstract: The invention relates to substituted 3-amino-1-arylalkyl-benzazepin-2-ones of the general formula ##STR1## wherein Ar is aryl;X is --O-- or --S(O).sub.n -- and n is 0, 1 or 2;X.sub.1 is C.sub.1 -C.sub.2 alkylene or a direct bond;R.sub.1 is hydrogen, lower alkyl, aryl-lower alkyl or acyl;R.sub.2 is lower alkyl, hydroxy-lower alkyl, lower alkoxy-lower alkyl, aryl-lower alkoxy-lower alkyl, aryl-lower alkyl or C.sub.3 -C.sub.7 cycloalkyl-lower alkyl;R.sub.3 is carboxy; lower alkoxycarbonyl; lower alkoxy-lower alkoxycarbonyl; aryl-lower alkoxycarbonyl; aryloxycarbonyl; carbamoyl; carbamoyl that (i) is monosubstituted by hydroxy, lower alkanesulfonyl, halo-lower alkanesulfonyl or by arylsulfonyl, (ii) is monosubstituted or disubstituted, the substituents being independent of one another, by lower alkyl, lower alkenyl, lower alkynyl or by phenyl-lower alkyl or (iii) is disubstituted by lower alkylene or by lower alkylene-Z.sub.1 -lower alkylene, Z.sub.1 being O, S or NH; 5-tetrazolyl; PO.sub.2 H.sub.2 ; PO.sub.3 H.

Abstract: Compounds of formula (I) in which (a) four of the radicals R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are hydrogen and the others independently of one another are in each case C.sub.1 -C.sub.2 alkyl, these groups being bonded to the same carbon atom or to two different carbon atoms, or (b) five of the radicals R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are hydrogen and the other radical is C.sub.1 -C.sub.2 alkyl or hydroxymethyl, or salts thereof, are described. The compounds of formula (I) and their salts are ornithine decarboxylase inhibitors.

Abstract: Compounds of formula I ##STR1## wherein R.sub.1 is free or esterified carboxy, hydroxymethyl or formyl,R.sub.2 and R.sub.4 are each independently of the other aliphatic, cycloaliphatic-aliphatic, araliphatic or heteroarylaliphatic radicals andR.sub.3 is azido, or amino that is aliphatically or araliphatically substituted and/or protected by an amino-protecting group,and the salts thereof, are valuable intermediates in the preparation of medicinal active ingredients, for example of compounds of formula II ##STR2## wherein R.sub.A is an aromatic or heteroaromatic radical,R.sub.2 and R.sub.4 are each independently of the other aliphatic, cycloaliphatic, cycloaliphaticaliphatic or araliphatic radicals,R.sub.3 is unsubstituted or N-mono- or N,N-di-lower alkylated or N-lower alkanoylated amino, andR.sub.B is an aliphatically, cycloaliphatically or heteroaromatically-aliphatically substituted amino group,and the salts thereof, which can be used, for example, as antihypertensives.

Abstract: Compounds of formula I ##STR1## wherein rings A and B are as defined in the specification, have valuable pharmacological properties and are particularly effective as NK1 antagonists and substance P antagonists. Said compounds are prepared in a manner known per se.

Abstract: There is disclosed a human macrophage inflammatory protein-1 .gamma. (MIP-1 .gamma.) polypeptide and DNA(RNA) encoding such polypeptide. There is also provided a procedure for producing such polypeptide by recombinant techniques and for producing an antibody against such polypeptide. Another aspect of the invention provides a combination of the polypeptide of the present invention and a suitable pharmaceutical carrier for providing a therapeutically effective amount of the polypeptide for the treatment of various associated diseases.