Abstract: Described herein is the discovery that certain mycobacterial serine/threonine protein kinases, particularly protein kinase G (PknG), are effective therapeutic targets for the treatment of mycobacterial infections. Furthermore, the present application refers to the use of mycobacterial serine/threonine protein kinases for developing methods for detection and determination of these kinases for recognizing and monitoring diseases and for controlling therapy of diseases.

Abstract: Described are 4,5,6,7-tetrahydrobenzo[b]thiophene derivatives and pharmaceutically acceptable salts thereof, the use of these derivatives for the prophylaxis and/or treatment of mycobacteria-induced infections and opportunistic infections, as well as compositions containing at least one 4,5,6,7-tetrahydrobenzo[b]thiophene derivative and/or pharmaceutically acceptable salts thereof. Furthermore, the present application refers to the use of mycobacterial protein serine/threonine kinases for developing methods for detection and determination of these kinases for recognising and monitoring diseases and for controlling therapy of diseases.

Abstract: The invention relates to new 7H-pyrrolo[2,3-d]pyrimidine derivatives, as well as their therapeutically acceptable salts, pharmaceutical preparations containing them and process for producing the active agent. The pharmaceutical preparation is adventageously antiphlogistic and analgetic one, a preparation reducing neuropathic hyperalgesia and rheumatic arthritis, a preparation for hindering destruction of bones chondrus, being applicable for treatment of other diseases, which may be connected with other inflammatory processes e.g. asthma, eczema or psoriasis.

Abstract: The present invention relates to compounds having a naphthyridine scaffold, and stereoisomeric forms, prodrugs, solvates, hydrates and/or pharmaceutically acceptable salts of these compounds as well as pharmaceutical compositions containing at least one of these naphthyridine derivatives together with pharmaceutically acceptable carrier, excipient and/or diluents. Said naphthyridine compounds have been identified as inhibitors of the protein kinase ROCK2, also known as Rho-kinase, and are useful for the treatment of cancers (tumor growth and metastases), erectile dysfunction, cardiovascular diseases, hypertension, angina pectoris, cerebral ischaemia, cerebral vasospasm, myocardial ischaemia, coronary vasospasm, heart failure, myocardial hypertrophy, atherosclerosis, restenosis, spinal cord injuries, neuronal degeneration, thrombotic disorders, asthma, glaucoma, inflammation, anti-viral diseases (e.g. HIV), and osteoporosis.

Abstract: The present invention relates to pyrimidine derivatives, methods for their synthesis, and the use of said pyrimidine derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of cell proliferation disorders, cancer, leukemia, erectile dysfunction, cardiovascular diseases and disorders, inflammatory diseases, transplant rejection, immunological diseases, neuroimmunological diseases, autoimmune diseases, infective diseases including opportunistic infections, prion diseases and/or neuro-degeneration. Furthermore, the present invention relates to pharmaceutical compositions containing at least one pyrimidine derivative and/or pharmaceutically acceptable salts thereof as an active ingredient together with at least one pharmaceutically acceptable carrier, excipient or diluents as well as to methods for prophylaxis and/or treatment of the above-mentioned diseases and disorders.

Abstract: This invention relates to the use a pyruvate-kinase or a nucleic acid coding therefor as a target for the modulation of apoptotic processes, particularly as a target molecule for the diagnosis, prevention or treatment of apoptosis-associated disorders, such as tumours.

Abstract: Described are heterobicyclic compounds such as 4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxylic acid amides, 4,7-dihydro-5H-thieno[2,3-c]thiopyran 3-carboxylic acid amides, 4,7-dihydro-5H-thieno[2,3-c]pyran-3-carboxylic acid amides, or benzo[b]thiophene-3-carboxylic acid amides and pharmaceutically acceptable salts thereof, the use of these derivatives for the prophylaxis and/or treatment of various diseases such as infectious diseases, including mycobacteriainduced infections and opportunistic diseases, prion diseases, immunological diseases, autoimmune diseases, bipolar and clinical disorders, cardiovascular diseases, cell proliferative diseases, diabetes, inflammation, transplant rejections, erectile dysfunction, neurodegenerative diseases and stroke, as well as compositions containing at least one heterobicyclic compound and/or pharmaceutically acceptable salts thereof. Furthermore, reaction procedures for the synthesis of the heterobicyclic compound are disclosed.

Abstract: The present invention relates to a medium and a method for enriching ATP binding proteins, e.g. proteinkinases, from a pool of proteins, like a proteome. The medium of the present invention comprises specific inhibitors, e.g.

Abstract: Novel imidazole compounds particularly useful against Hepatitis C Virus infections and diseases associated therewith are described. Applications of the human cellular proteins casein kinase I alpha (?), delta (?), and epsilon (?) as targets for medical intervention against Hepatitis C Virus (HCV) infections and diseases are also described. This invention further refers to a method for identifying compounds useful for the prophylaxis and/or treatment of Hepatitis C Virus infections and diseases, methods for treating Hepatitis C Virus infections and diseases, as well as pharmaceutical compositions useful for the prophylaxis and/or treatment of Hepatitis C Virus infections and diseases. Moreover, disclosed are antibodies, oligonucleotides and specific compounds which are effective for the detection, prophylaxis and/or treatment of Hepatitis C Virus infections and diseases.

Abstract: The present invention relates to aromatic guanylhydrazone compounds and their use as pharmaceutically active agents, especially for prophylaxis and treatment of virally caused diseases and infections, including opportunistic infections. The inventive guanylhydrazone compounds are also useful as inhibitors of deoxyhypusine synthase and as inhibitors for nuclear export in infectious diseases and may be used to regulate bacterially induced TNF-? production. Furthermore, the aromatic guanylhydrazones exhibit antibacterial activity against Gram positive and Gram negative bacteria and can be regarded as a novel class of antibiotics. In addition, methods for prophylaxis and treatment of virally or bacterially induced infections and diseases are disclosed together with pharmaceutical compositions useful within said methods containing at least one aromatic guanylhydrazone of the present invention as active ingredient.

Abstract: The present invention relates to a method for generating a quantitative structure property activity relationship (QSPAR) between the structure of chemical compounds and their pharmacological activity. Said method comprises the steps of establishing at least one database containing molecular descriptors especially 2D and/or 3D biological/physical/chemical data; selecting significant descriptors according to their influence to said structure property activity relationship; providing at least a model for generating a quantitative structure property activity relationship; verifying said model by the use of at least one quality parameter; and repeating steps b, c, and d until said quality parameter reaches a predetermined value. The method is especially useful for the correlation of chemical compounds with large differences in structure.

Abstract: Described herein is the discovery that certain mycobacterial serine/threonine protein kinases, particularly protein kinase G (PknG), are effective therapeutic targets for the treatment of mycobacterial infections. Furthermore, the present application refers to the use of mycobacterial serine/threonine protein kinases for developing methods for detection and determination of these kinases for recognizing and monitoring diseases and for controlling therapy of diseases.

Abstract: The present invention relates to the use a pyruvate-kinase or a nucleic acid coding therefor as a target for the modulation of apoptotic processes, particularly as a target molecule for the diagnosis, prevention or treatment of apoptosis-associated disorders, such as tumours

Abstract: The invention relates to the use of peptide amides of formula (I) and phenylamino-oxoacetic acid derivatives of formula (II) as well as the salts of the above compounds as active substances for the preparation of pharmaceutical compositions possessing neurogenic and non-neurogenic antiinflammatory as well as analgetic effects.

Abstract: The present invention relates to aromatic guanylhydrazone compounds and their use as pharmaceutically active agents, especially for prophylaxis and treatment of virally caused diseases and infections, including opportunistic infections. The inventive guanylhydrazone compounds are also useful as inhibitors of deoxyhypusine synthase and as inhibitors for nuclear export in infectious diseases and may be used to regulate bacterially induced TNF-&agr; production. Furthermore, the aromatic guanylhydrazones exhibit antibacterial activity against Gram positive and Gram negative bacteria and can be regarded as a novel class of antibiotics. In addition, methods for prophylaxis and treatment of virally or bacterially induced infections and diseases are disclosed together with pharmaceutical compositions useful within said methods containing at least one aromatic guanylhydrazone of the present invention as active ingredient.

Abstract: The subject matter of the present invention is a cyclic or linear tetra- or pentapeptide binding to somatostatin receptors. The compounds of the invention are characterised in that they contain the radical of an amino carboxylic acid bearing a five-membered ring in the peptide backbone which may optionally contain O, S, Se, N, or P. These compounds are easy to prepare and display increased stability against peptidases.

Abstract: The invention relates to the use of peptide amides of formula (I) 1

Abstract: Method for treating a patient inflicted with a cell proliferation disorder, such as a cancer, characterized by inappropriate PDGF-R activity. The method involves the step of administering to the patient a therapeutically effective amount of a composition described in application.

Abstract: The invention relates to tumor-inhibiting heptapeptide and octapeptide amide derivatives and to a method of treating mammals, including men, suffering from tumors or from the excessive secretion of insulin, glucagon or growth hormone using these compounds.

Abstract: The compounds of the Formula (I) ##STR1## wherein R.sub.1 is a C.sub.18-24 alkenyl containing at least two double bonds, or --(CH2)n --CH(NH2)m --COOHX is 0, NH or C.sub.1-4 alkyl-N,Y is CONH.sub.2, COOH or COOMe, wherein Me is hydrogen metal, andR.sub.2 is a side chain of a any amino acid except L-GLU or L-ASP at .alpha.-position or a group of Formula--(CH.sub.2).sub.k --C.sub.6 H.sub.3 --(A).sub.2 (II),--(CH.sub.2).sub.n --X--(CH.sub.2).sub.m --X--M (III)whereink is zero or an integer of 1,n is zero or an integer of 1 to 3,m is zero or an integer of 1 to 4,A is hydroxyl or one A is hydroxyl and the other A is hydrogen.M is H or R.sub.1 --CO andX and R.sub.1 are as defined aboveand their salts having tyrosine kinase inhibitor activity can be used as antitumor agents.