Abstract: The present invention relates to compounds of formula (I): or pharmaceutically acceptable salts, solvates, hydrates or pharmaceutically acceptable formulations thereof. Those compounds can be used in inhibiting factor Xa and in the prevention and/or treatment of thrombolytic conditions.

Abstract: The present invention relates to compounds of the Formula (I) that are useful antimicrobial agents and effective against a variety of multi-drug resistant bacteria:

Abstract: The present invention describes novel anti-bacterial compounds of formula (I). Q-A-R3??(I) These compounds are, amongst others, of interest as inhibitors of DNA gyrase.

Abstract: The present invention relates to compounds of the Formula or a pharmaceutically acceptable salt, solvate, hydrate or formulation thereof. These compounds can be used for the inhibition of Factor Xa and for the treatment and/or prevention of diseases that are mediated by Factor Xa activity.

Abstract: The present invention relates to the use of compounds, in which the pharmacophores of quinolone and oxazolidinone are chemically linked together through a linker that is stable under physiological conditions, for the treatment of anthrax and other infections.

Abstract: The present invention describes novel anti-bacterial compounds of formula (I).

Abstract: The present invention relates to novel bioisosteres of the antibiotic actinonin of the general formula (I). The novel compounds are of particular interest as inhibitors of metalloproteinases.

Abstract: The present invention describes intermediates (ZP) for a novel and efficient synthesis of compounds in which the pharmacophores of quinolone and oxazolidinone are linked to one another by way of a chemically stable linker.

Abstract: The present invention describes novel anti-bacterial compounds of formula (I). These compounds are, amongst others, of interest as inhibitors of Topoisomerase IV (Topo IV) as well as of DNA gyrase.

Abstract: The present invention relates to compounds of formula (I): or a pharmaceutically acceptable salt, solvate, hydrate or pharmaceutically acceptable formulation thereof. Those compounds can be used in inhibiting factor Xa and in the prevention and/or treatment of thromboembolic conditions.

Abstract: This invention relates to novel compounds, compositions containing the compounds, that inhibit dipeptidyl peptidase (especially DPP-IV) and neprilysin (NEP, neutral endopeptidase) as well as dipeptidyl peptidase (especially DPP-IV) and angiotensin converting enzyme (ACE) and/or dipeptidyl Peptidase (especially DPP-IV) and vasopeptidases (especially ACE and NEP). These compounds and pharmaceutical compositions thereof are useful for the treatment as well as the prevention of type 2 diabetes mellitus.

Abstract: The present invention is directed to novel acyloins, their derivatives, methods for their production and their use for the production of novel epothilones and their derivatives. In addition, the invention is directed to the building blocks for epothilone synthesis, methods for their production and the use of synthetic building blocks for the production of epothilones and their derivatives.

Abstract: The present invention relates to compounds of formula (I): or a pharmaceutically acceptable salt, solvate, hydrate or a pharmaceutically acceptable formulation thereof. Those compounds can be used for inhibiting factor Xa and for the prevention and/or treatment of thromboembolic conditions.

Abstract: The invention relates to a process for the preparation of heterocycles, characterised in that the following components: i) a propargyl derivative of the general structural formula I  a wherein Het is an optionally substituted hetero atom and A is a substituted or unsubstituted aromatic entity, a substituted or unsubstituted aromatic heterocycle, a substituted or unsubstituted vinyl arene and/or a derivative thereof, an olefin, an alkyne, an acceptor group or a nitrile; (ii) a compound of the general structural formula II, B—X  II,  wherein B is an electron-deficient substituted or unsubstituted aromatic entity with or without an acceptor group, an electron-deficient substituted or unsubstituted heteroaromatic entity with or without an acceptor group, an electron-deficient olefin and/or alkyne, a metal complex, and X is a leaving group; (iii) a nucleophile of the general structural formula III, Y—Cn—Z  III,  wherein Y and/or Z, each

Abstract: The present invention relates to the use of compounds, in which the pharmacophores of quinolone and oxazolidinone are chemically linked together through a linker that is stable under physiological conditions, for the treatment of bacterial infections in acidic environments (pH<7.0). The activity of these compounds is strongly increased at even slightly acidic conditions what makes them especially interesting for the treatment of infections in abscesses or inflamed tissues.

Abstract: The present invention relates to 3-pyrroloimidazole derivatives of the general formula (I) wherein the imidazole radical is an optionally substituted imidazole ring, X, Y, A and B are, each independently of the others, carbon or nitrogen atoms, the radicals Z denote, each independently of the others, a hydrogen atom, a halogen atom, a pseudohalogen, an optionally substituted alkyl, alkenyl, alkynyl, aralkyl, aralkenyl, aralkynyl, cycloalkyl, cycloalkenyl, cycloalkynyl, cycloaralkyl, cycloaralkenyl, cycloaralkynyl, aryl or alkoxy radical or an optionally substituted ring, to which one or two further, optionally substituted rings may be fused, and/or at least two of the radicals Z may be part of an optionally substituted ring, to which one or two further, optionally substituted rings may be fused, and to pharmaceutical compositions comprising at least one of the above-mentioned compounds, optionally in combination with carriers and/or adjuvants and/or excipients customary per se.

Abstract: The present invention relates to novel yeast cells with increased permeability to compounds, such as small organic compounds. In particular, the invention provides genetically modified yeast cells carrying functional, preferably conditionally regulated, copies of HXT9 and HXT11 genes integrated in the chromosome at the PDR1 and PDR3 loci, thereby disrupting the PDR1 and PDR3 gene activity. The invention further relates to methods and compositions for the use of these hyperpermeable yeast cells for screening for compounds that modulate macromolecular interactions. The invention is exemplified by the use of the hyperpermeable yeast cells in such a screening system. In addition, the invention further provides methods of producing the yeast cells of the invention, as well as polynucleotides, vectors, and kits for use of the hyperpermeable yeast cells and the screening methods of the invention.

Abstract: The present invention relates to compounds of the Formula 1

Abstract: A process for the preparation of polymers having nucleobases as side groups by means of multicomponent reactions, especially the Ugi reaction, is described. Because of the multicomponent nature of preparation, the properties of the polymers can be varied substantially better than has hitherto been possible and can be adapted to requirements for use as an antisense or antigen therapeutic agent or as a diagnostic agent.

Abstract: The present invention relates to methods and compositions for the identification and modulation of protein-protein interactions. Specifically, the invention relates to methods and compositions for efficient, sensitive, high-throughput CadC-based screens for the identification of peptides involved in protein-protein interactions, including, but not limited to, peptides comprising amino acid sequences involved in receptor dimerization. The invention further relates to methods and compositions for efficient, sensitive, high-throughput CadC-based screens for compounds which modulate protein-protein interactions, such as, for example, modulation of interactions between protein sequences involved in receptor interactions, e.g., dimerization.