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  Compounds for the modulation of the glykolysis-enzyme-and/or of the transaminase-complexUSPTO Application #: 20070238781Title: Compounds for the modulation of the glykolysis-enzyme-and/or of the transaminase-complex Abstract: The invention relates to compounds for the modulation of the glycolysis enzyme complex and of the transaminase complex, pharmaceutical compositions containing such compounds as well as uses of such compounds for preparing pharmaceutical compositions for treating various diseases. (end of abstract) Agent: Mayer Fortkort & Williams, PC - Westfield, NJ, US Inventors: Erich Eigenbrodt, Hans Scheefers, Sybille Mazurek USPTO Applicaton #: 20070238781 - Class: 514506000 (USPTO) Related Patent Categories: Drug, Bio-affecting And Body Treating Compositions, Designated Organic Active Ingredient Containing (doai), Ester Doai The Patent Description & Claims data below is from USPTO Patent Application 20070238781. Brief Patent Description - Full Patent Description - Patent Application Claims
STATEMENT OF RELATED APPLICATION [0001] This is a continuation of U.S. patent application Ser. No. 10/618,578, filed Jul. 11, 2003, entitled "Compounds For The Modulation Of The Glykolysis-Enzyme-And/Or Of The Transaminase-Complex, which is incorporated by reference herein in its entirety. FIELD OF THE INVENTION [0002] The invention relates to compounds for the modulation of the glycolysis enzyme and/or transaminase complex and thus in particular to the growth inhibition of cells and/or bacteria, pharmaceutical compositions containing such compounds as well as uses of such compounds for preparing pharmaceutical compositions for treating various diseases. BACKGROUND OF THE INVENTION [0003] Cancer is one of the most prevalent causes of death today, and the number of cancer cases in industrialized countries continues to grow. This is mainly based on the fact that malignant tumors are diseases of advanced age and due to successes in controlling infectious diseases, it is likely that more people will reach this age. [0004] In spite of much progress in the diagnostic and therapeutic fields, the odds for overcoming the most prevalent types of cancer types are seldom higher than 20%. A cancerous tumor nowadays can be destroyed or its growth inhibited. A re-conversion of a tumor cell into a normal cell is, however, not yet possible. Rather, the most important therapeutic measures, via operation and irradiation, remove cancer cells from the organism. The presently used chemotherapeutic agents for cancer, the cytostatics, also lead to the destruction or damaging of tumor cells only. In most cases, the effect is so non-specific that simultaneous heavy damage to healthy cells will occur. [0005] In general, tumor cells have a metabolism differing from healthy cells, in particular glycolysis. Thus, a change in the isoenzyme system involved in glycolysis and a change in the transport of NADH is typical for tumor cells. Among other effects, the activity of the enzymes involved in glycolysis is increased. This permits high reaction rates under the aerobic conditions typical for tumor cells. For details, reference is made to E. Eigenbrodt et al., Biochemical and Molecular Aspects of Selected Cancers, Vol. 2, p. 311 ff (1994). [0006] Various other diseases mentioned below are either characterized by an excessive metabolism by glycolysis enzyme complex and can be treated by the reduction or inhibition thereof. PRIOR ART [0007] From the document E. Eigenbrodt et al., Biochemical and Molecular Aspects of Selected Cancers, Vol. 2, p. 311 ff (1994), it is known that glucose analogs are used for inhibiting the glycolysis. Other approaches known here from are the use of inhibitors of glycolysis isoenzymes, for instance by suitable chelation or inhibition of chelations. As a result, the tumor cells are, in a manner of speaking, starved out. However, a problem with the above compounds is that many of them are genotoxic and/or not sufficiently specific for tumor cells. SUMMARY OF THE INVENTION [0008] It is the technical object of the present invention to specify active ingredients that are able to modulate or inhibit the glycolysis enzyme and transaminase complex, in particular the proliferation of cancer cells and to thus inhibit the growth of neoplastic tumors as well as defense over-reactions of the body, such as septic shock, autoimmune diseases, transplant rejections as well as acute and chronic inflammatory diseases, and that simultaneously have only slight to no cytotoxicity at all with regard to cells which have an intact glycolysis enzyme complex or other complex structures. In addition, it is intended to inhibit the growth of unicellular organisms. BRIEF DESCRIPTION OF THE DRAWINGS [0009] FIG. 1a is a graphical representation showing the migration of PGM from the glycolysis enzyme completed into the transaminase complex. [0010] FIG. 1b is a graphical representation showing the effect of aminoacetate (AOA) and hydrozylamine (HA) on the activity of the cytosolic and mitochondrial isoenzyme of the GOT in vitro. [0011] FIG. 2a is the structural formula of 5-methyl-N-[4-(trifluoromethyl)phenyl]isoxazole-4-carboxamide. [0012] FIG. 2b is the structural formula of (2Z)-2-cyano-3-hydroxy-N-[4-(trifluoromethyl)phenyl]but-2-enamide. [0013] FIG. 2c is the structural formula of N-(3,5-dihalogenophenyl)-5-methylisoxazole-4-carboxamide. [0014] FIG. 2d is the structural formula (2Z)-2-cyano-N-(3,5-dihalogenophenyl)-3-hydroxybut-2-enamide. [0015] FIG. 2e is the structural formula of 5-methyl-N-[4-(trihalogenomethoxy)phenyl]isoxazole-4-carboxamide. [0016] FIG. 2f is the structural formula of (2Z)-2-cyano-3-hydroxy-N-[4-(trihalogenomethoxy)phenyl]but-2-enamide. [0017] FIG. 2g is the structural formula of N-(3-halogenophenyl)-5-methylisoxazole-4-carboxamide. [0018] FIG. 2h is the structural formula of (2Z)-2-cyano-N-(3-halogenophenyl)-3-hydroxybut-2-enamide. Continue reading... Full patent description for Compounds for the modulation of the glykolysis-enzyme-and/or of the transaminase-complex Brief Patent Description - Full Patent Description - Patent Application Claims Click on the above for other options relating to this Compounds for the modulation of the glykolysis-enzyme-and/or of the transaminase-complex patent application. ###  How KEYWORD MONITOR works... a FREE service from FreshPatents1. Sign up (takes 30 seconds). 2. Fill in the keywords to be monitored. 3. Each week you receive an email with patent applications related to your keywords. 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