Abstract: Compounds of the formula ##STR1## are described wherein R.sub.1 and R.sub.2 are each independently of the other hydrogen or a protecting group, orR.sub.1 has those definitions andR.sub.2 is a radical forming a phosphorus-containing nucleotide bridge group;B is a purine or pyrimidine radical or an analogue thereof; andR.sub.3 is a radical of formula Ia, Ib or Ic ##STR2## wherein R.sub.4 is hydrogen, C.sub.1 -C.sub.21 alkyl, C.sub.2 -C.sub.21 alkenyl, C.sub.2 -C.sub.21 alkynyl or --C(.dbd.O)-alkyl;R.sub.5 is hydrogen, C.sub.1 -C.sub.10 alkyl, --CH.sub.2 --O--R.sub.6 or a radical of formula Ib;R.sub.6 is hydrogen, C.sub.1 -C.sub.22 alkyl, C.sub.3 -C.sub.21 alkenyl, or partially or completely fluorine-substituted C.sub.1 -C.sub.10 alkyl or --[(CH.sub.2).sub.2 --O].sub.m --R.sub.7 ;R.sub.7 is hydrogen or C.sub.1 -C.sub.21 alkyl;Z is --(CH.sub.2).sub.p -- or --(CH.sub.2 --CH.sub.2 --O).sub.q --CH.sub.2 CH.sub.2 --, it being possible for Z in the case of --CH.sub.

Abstract: The invention relates to the use of certain methanebisphosphonic acid derivatives (for the manufacture of a pharmaceutical composition) for the prevention and treatment of prosthesis loosening and prosthesis migration in mammals including man.

Abstract: The invention relates to novel N-(3,5-bis-trifluoromethyl-benzoyl)-2-benzyl-4-(azanaphthoyl-amino)-piperi dines of the formula ##STR1## wherein X and Y are each independently of the other N and/or CH and the ring A is unsubstituted or mono- or poly-substituted by substituents selected from the group consisting of lower alkyl, lower alkoxy, halogen, nitro and trifluoromethyl; and the salts thereof, to the use thereof, to processes for the preparation thereof and to pharmaceutical compositions comprising a compound according to the invention or a pharmaceutically acceptable salt thereof.

Abstract: The current invention concerns the use of a receptor from the RZR/ROR receptor family or a functional fragment thereof in a test of a compound for anti-autoimmune, anti-arthritic, anti-tumor, melatonin-like and or melatonin-antagonistic activity and the production of a receptor ligand complex comprising the receptor or a functional fragment thereof and a ligand of the receptor. Also described is a method for testing compounds for said activity (screening for ligands) and the active compounds identified therewith.

Abstract: The invention relates to reshaped human monoclonal antibodies directed against isotypic determinants of immunoglobulin E (IgE), direct equivalents and derivatives of said antibodies. The molecules of the invention are useful for diagnostics, prophylaxis and treatment of allergy.

Abstract: The invention relates to novel 1-acyl-4-aliphatylaminopiperidine compounds of ##STR1## formula (I), in which R.sub.1 is a benzoyl, naphthoyl or cycloalkanoyl radical which is unsubstituted or substituted by lower alkyl, lower alkoxy, halogen and/or trifluoromethyl; R.sub.2 is cycloalkyl or a phenyl or naphthyl radical which is unsubstituted or substituted by lower alkyl, lower alkoxy, halogen, nitro, cyano and/or trifluoromethyl; R.sub.3 and R.sub.4 together are lower alkylene or aza-, oxa- or thia-lower alkylene; or R.sub.3 is lower alkyl, lower alkoxy-lower alky, di-lower alkylamino-lower alkyl or a radical of the formula --(CH.sub.2).sub.n --C(.dbd.O)--R.sub.5 (Ia); and R.sub.4 is hydrogen, lower alkyl or a radical of the formula --(CH.sub.2).sub.n --C(.dbd.O)--R.sub.5 (Ia); R.sub.

Abstract: Antiretroviral compounds (which are effective, for example, against HIV) of the formula I ##STR1## in which R.sub.

Abstract: New trityl linkers for use in solid phase synthesis comprise compounds of formula II ##STR1## wherein R.sub.4 is alkyl (e.g. C.sub.1-4 alkyl), halogen, NO.sub.2, or hydrogen;Z is a coupling group chosen from acylamido, acyloxy, amino, halogen, thiol or hydroxyl,where acyl is the residue of a carboxylic acid or a residue of formula R.sub.5 CO where R.sub.5 is an organic group;Y is H, a reactive functional group or an attachment to a solid phase;W is O when Y is H or a reactive functional group, or W is --NH--, or --NR.sub.6 --(urethane) when Y is an attachment to a solid phase,where R.sub.6 is an organic group and,each R which, may be the same or different, is C(O)NR.sub.7 R.sub.8, CF.sub.3, F or Cl wherein each R.sub.7 and R.sub.8, which may be the same or different, is H or C.sub.

Abstract: The invention relates to a novel process for the preparation of compounds of formula I ##STR1## wherein R.sub.1 is hydrogen or a suitable amino-protecting group,R.sub.2 is unsubstituted or substituted alkyl,R.sub.3 is hydrogen, aryl, heterocyclyl, unsubstituted or substituted alkyl or unsubstituted or substituted cycloalkyl,R.sub.4, independently of R.sub.1, is hydrogen or a suitable amino-protecting group andm is a number from 1 to 7; and wherein further suitable protecting groups for functional groups may be present; which compounds are antivirally active or can be used as starting materials for pharmaceutically active, especially antiviral compounds.

Abstract: A process for the preparation of nucleoside diphosphate and triphosphate sugars wherein hydroxyl protective groups are removed enzymatically, with acetylesterase and a process for the preparation of these sugars, which comprises coupling a nucleotide with a sugar-1-phosphate activated with a carbonyl bisazole and then removing the hydroxyl protective groups enzymatically with acetylesterase.

Abstract: The invention relates to the use of the compounds mentioned below in the therapeutic treatment of tumor diseases and other proliferative diseases, such as psoriasis, and to novel compounds of that type. The compounds are compounds of formula I ##STR1## wherein n is from 0 to 5 and, when n is not 0,R is one or more substituents selected from halogen, alkyl, trifluoromethyl and alkoxy; andR.sub.1 and R.sub.2 are each independently of the other alkyl, or phenyl that is unsubstituted or substituted by halogen, trifluoromethyl, alkyl or by alkoxy, it also being possible for one of the two radicals R.sub.1 and R.sub.2 to be hydrogen, or R1 and R2 together form an alkylene chain having from 2 to 5 carbon atoms that is unsubstituted or substituted by alkyl; or salts thereof. Compounds of formula I inhibit protein kinases, for example the tyrosine protein kinase of the receptor for the epidermal growth factor, EGF.

Abstract: The invention relates to purified proteins induced in human cells by interferon .alpha. or .beta., RNAs, DNAs and hybrid vectors coding for said proteins, hosts transformed with such a hybrid vector, processes for the preparation and purification of these proteins, DNAs, vectors and hosts, monoclonal antibodies specific to these proteins, monoclonal antibody derivatives, hybridoma cell lines secreting these monoclonal antibodies, the use of the monoclonal antibodies and their derivatives in the qualitative and quantitative determination of these proteins, test kits containing the monoclonal antibodies, and pharmaceutical preparations containing said proteins. A protein of the invention shows antiviral properties ascribed to interferons and may be a valuable indicator of the cell response to an interferon therapy.

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

Abstract: We have cloned and expressed the cDNA for human liver mevalonate pyrophosphate decarboxylase, an enzyme of the cholesterol synthesis pathway. This cDNA encodes a 400 amino acid protein (43 kDa) which resembles the coding sequence of an unidentified and incomplete open reading frame adjacent to the COQ2 gene of Saccharomyces cerevisiae. We also found an expression sequence tag clone made from human infant brain cDNA to be almost identical to our cDNA sequence.

Abstract: The invention concerns polypeptides with an apparent molecular weight of around 160 kD which are mediators or precursors for mediators of inflammation, derivatives thereof such as mutants and fragments, processes for their preparation, DNAs and hybrid vectors coding for the polypeptides and derivatives and host cells transformed with such hybrid vectors, polyclonal and monoclonal antibodies specific for the polypeptides or their derivatives and antibody derivatives as well as diagnostic and therapeutic methods for inflammatory conditions and Hodgkin lymphomas.

Abstract: Antiretroviral compounds (which are effective, for example, against HIV) of the formula I ##STR1## in which R.sub.

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 relates to compounds of formula ##STR1## and salts, pharmaceutical compositions, intermediates and processes of preparation thereof.

Abstract: Compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2 are each independently of the other hydrogen or a protecting group, orR.sub.1 has those meanings andR.sub.2 is a radical forming a phosphorus-containing nucleotide bridge group;B is a purine or pyrimidine radical or an analogue thereof; andR.sub.3 is OH, F or (CF.sub.2).sub.n CF.sub.3 wherein n is a number from 0 to 7, and oligonucleotides that comprise those nucleosides are described.

Abstract: The invention relates to purified proteins induced in human cells by interferon .alpha. or .beta., RNAs, DNAs and hybrid vectors coding for said proteins, hosts tranformed with such a hybrid vector, processes for the preparation and purification of these proteins, DNAs, vectors and hosts, monoclonal antibodies specific to these proteins, monoclonal antibody derivatives, hybridoma celll lines secreting these monoclonal antibodies specific to these proteins, and their derivatives in the qualitative and quantitative determination of these proteins, test kits containing the monoclonal antibodies, and pharmaceutical preparations containing said proteins. A protein of the invention shows antiviral properties ascribed to interferons and may be a valuable indicator of the cell response to an interferon therapy.