CY1105087T1 - Νεες αντιβακτηριακες ουσιες - Google Patents
Νεες αντιβακτηριακες ουσιεςInfo
- Publication number
- CY1105087T1 CY1105087T1 CY20061100970T CY061100970T CY1105087T1 CY 1105087 T1 CY1105087 T1 CY 1105087T1 CY 20061100970 T CY20061100970 T CY 20061100970T CY 061100970 T CY061100970 T CY 061100970T CY 1105087 T1 CY1105087 T1 CY 1105087T1
- Authority
- CY
- Cyprus
- Prior art keywords
- enzyme
- ligands
- ligand
- cell wall
- binding
- Prior art date
Links
- 239000000126 substance Substances 0.000 title abstract 4
- 230000000844 anti-bacterial effect Effects 0.000 title abstract 3
- 239000003446 ligand Substances 0.000 abstract 11
- 150000001875 compounds Chemical class 0.000 abstract 3
- 108010062010 N-Acetylmuramoyl-L-alanine Amidase Proteins 0.000 abstract 2
- 108090000279 Peptidyltransferases Proteins 0.000 abstract 2
- 230000001580 bacterial effect Effects 0.000 abstract 2
- 230000015572 biosynthetic process Effects 0.000 abstract 2
- 210000002421 cell wall Anatomy 0.000 abstract 2
- 239000000758 substrate Substances 0.000 abstract 2
- DQJCDTNMLBYVAY-ZXXIYAEKSA-N (2S,5R,10R,13R)-16-{[(2R,3S,4R,5R)-3-{[(2S,3R,4R,5S,6R)-3-acetamido-4,5-dihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy}-5-(ethylamino)-6-hydroxy-2-(hydroxymethyl)oxan-4-yl]oxy}-5-(4-aminobutyl)-10-carbamoyl-2,13-dimethyl-4,7,12,15-tetraoxo-3,6,11,14-tetraazaheptadecan-1-oic acid Chemical compound NCCCC[C@H](C(=O)N[C@@H](C)C(O)=O)NC(=O)CC[C@H](C(N)=O)NC(=O)[C@@H](C)NC(=O)C(C)O[C@@H]1[C@@H](NCC)C(O)O[C@H](CO)[C@H]1O[C@H]1[C@H](NC(C)=O)[C@@H](O)[C@H](O)[C@@H](CO)O1 DQJCDTNMLBYVAY-ZXXIYAEKSA-N 0.000 abstract 1
- 108020004256 Beta-lactamase Proteins 0.000 abstract 1
- 108090000204 Dipeptidase 1 Proteins 0.000 abstract 1
- 108090000790 Enzymes Proteins 0.000 abstract 1
- 102000004190 Enzymes Human genes 0.000 abstract 1
- 102000002068 Glycopeptides Human genes 0.000 abstract 1
- 108010015899 Glycopeptides Proteins 0.000 abstract 1
- 108700020474 Penicillin-Binding Proteins Proteins 0.000 abstract 1
- 108010087702 Penicillinase Proteins 0.000 abstract 1
- 102000006635 beta-lactamase Human genes 0.000 abstract 1
- 210000004027 cell Anatomy 0.000 abstract 1
- 230000019522 cellular metabolic process Effects 0.000 abstract 1
- 230000004060 metabolic process Effects 0.000 abstract 1
- 230000004260 plant-type cell wall biogenesis Effects 0.000 abstract 1
- 239000002243 precursor Substances 0.000 abstract 1
- 238000003786 synthesis reaction Methods 0.000 abstract 1
- 150000003952 β-lactams Chemical class 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C40—COMBINATORIAL TECHNOLOGY
- C40B—COMBINATORIAL CHEMISTRY; LIBRARIES, e.g. CHEMICAL LIBRARIES
- C40B30/00—Methods of screening libraries
- C40B30/04—Methods of screening libraries by measuring the ability to specifically bind a target molecule, e.g. antibody-antigen binding, receptor-ligand binding
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
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- A61K47/60—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
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- C07C323/12—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and singly-bound oxygen atoms bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
- C07D207/32—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
- C07D207/33—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms with substituted hydrocarbon radicals, directly attached to ring carbon atoms
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- C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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- C07D235/30—Nitrogen atoms not forming part of a nitro radical
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- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
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Abstract
Η παρούσα εφεύρεση αφορά σε νέες πολυπροσδένουσες ενώσεις (ουσίες) οι οποίες αποτελούν αντιβακτηριακές ουσίες. Οι πολυπροσδένουσες ενώσεις της εφεύρεσης περιλαμβάνουν 2-10 προσδέματα ομοιοπολικά συνδεδεμένα από έναν συνδέτη ή συνδέτες, όπου έκαστο από τα εν λόγω προσδέματα στην μονοσθενή (δηλ. ασύνδετη) κατάσταση τους διαθέτουν την ικανότητα να προσδένονται σε ένα ένζυμο το οποίο ενέχεται στην βιοσύνθεση και στο μεταβολισμό κυτταρικού τοιχώματος. Ένας πρόδρομος που χρησιμοποιείται στη σύνθεση του βακτηριακού κυτταρικού τοιχώματος και/ή της βακτηριακής κυτταρικής επιφάνειας, και κατ' αυτό τον τρόπο εμπλέκονται στη σύνθεση και ή στο μεταβολισμό του κυτταρικού τοιχώματος. Συγκεκριμένα, οι πολυπροσδένουσες ενώσεις της εφεύρεσης περιλαμβάνουν 2-10 προσδέματα ομοιοπολικά συνδεδεμένα από έναν συνδέτη ή συνδέτες, όπου έκαστο από τα εν λόγω προσδέματα διαθέτει μια περιοχή προσδέματος ικανή για πρόσδεση σε προσδένουσες πενικιλίνη πρωτεΐνες, ένα ένζυμο τρανσπεπτιδάσης, ένα υπόστρωμα ενός ενζύμου τρανσπεπτιδάσης, ένα ένζυμο β-λακταμάσης, ένα ένζυμο πενικιλινάσης, ένα ένζυμο κεφαλοσπορινάσης, ένα ένζυμο τρανσγλυκοσυλάσης ή ένα υπόστρωμα ενζύμου τρανσγλυκοσυλάσης. Κατά προτίμηση, τα προσδέματα επιλέγονται από τις τάξεις αντιβακτηριακών ουσιών της β-λακτάμης ή των γλυκοπεπτιδίων.
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1999
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- 1999-06-07 JP JP2000553117A patent/JP2004512255A/ja active Pending
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2001
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