http://rdf.ncbi.nlm.nih.gov/pubchem/patent/BR-PI0715095-B1

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classificationCPCAdditional http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K38-00
classificationCPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07K7-62
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filingDate 2007-08-10-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_a210500c15c26699ee35724eb35c649a
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_ccbd44572ba60c44b7d3688afbb33307
publicationDate 2018-08-07-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber BR-PI0715095-B1
titleOfInvention POLYMIXIN DERIVATIVE OF GENERAL FORMULA (I); COMBINATION PRODUCT; PHARMACEUTICAL COMPOSITION; Method for Sensitizing Gram-Negative Bacteria to an Antibacterial Agent; METHOD FOR DEVELOPING ANTIBIOTICS; METHOD FOR REDUCING THE TOXICITY OF POLYMIXINES, NATURAL OCTAPEPTINS AND THEIR DERIVATIVES DURING APPLICATION OF THE SAME IN THE TREATMENT OF INFECTIONS IN AN INDIVIDUAL; METHOD FOR IMPROVING PHARMACOKINETIC PROPERTIES OF POLYMIXINS, NATURAL OCTAPEPTINS AND THEIR DERIVATIVES; METHOD FOR SENSITIZING GRAM-NEGATIVE BACTERIA CLINICALLY IMPORTANT TO A DEFENSE MECHANISM COMPLEMENT IN SERUM; USE OF A DERIVATIVE; AND PROCESS FOR THE PREPARATION OF A FORMULA POLYMIXIN DERIVATIVE (I).
abstract polymyxin derivative of the general formula (i); combination product; pharmaceutical composition; method for treating, relieving or ameliorating an infection in a patient caused by a gram-negative bacterium; method for sensitizing gram negative bacteria to an antibacterial agent; method for developing novel antibiotics; method for reducing the toxicity of polymyxins, natural octapeptins and their derivatives during their application in the treatment of infections in an individual; method for improving pharmacokinetic properties, and natural polymyxins, octapeptins and derivatives thereof; method for sensitizing clinically important gran-negative bacteria to a defense mechanism complement present in serum; use of a derivative and process for the preparation of a polymyxin derivative of formula (i). The present invention relates to a polymyxin derivative in r1, r2 and r3 are optional and r1, r2, r3, r5, r8, r9 are selected cationic or neutral amino acid residues such that the total number of positive charges at a physiological ph is at least two, but not above three; and to a combination product comprising at least two such derivatives. The invention further relates to a method for treating, alleviating or ameliorating an infection in a patient caused by a gram-negative bacterium by administering a therapeutically effective amount of a derivative according to the present invention; a method for sensitizing gram-negative bacteria to an antibacterial agent by administering, simultaneously or sequentially, in any order, a therapeutically effective amount of the antibacterial agent and a derivative according to the present invention to the patient; methods for developing novel antibiotics to reduce nephrotoxicity, to improve the pharmacokinetic properties of natural polymyxins and octapeptins; and for sensitization of clinically important bacteria to a complement of host defense mechanism present in serum. Finally, the present invention relates to a process for the preparation of such polymyxin derivatives.
priorityDate 2006-08-11-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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