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1. WO1997030027 - BETA-THIOPROPIONYL-AMINOACID DERIVATIVES AND THEIR USE AS BETA-LACTAMASE INHIBITORS

Publication Number WO/1997/030027
Publication Date 21.08.1997
International Application No. PCT/EP1997/000516
International Filing Date 03.02.1997
Chapter 2 Demand Filed 30.08.1997
IPC
A61K 45/06 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
45Medicinal preparations containing active ingredients not provided for in groups A61K31/-A61K41/132
06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
C07C 323/60 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
323Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
50containing thio groups and carboxyl groups bound to the same carbon skeleton
51having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton
60with the carbon atom of at least one of the carboxyl groups bound to nitrogen atoms
C07D 209/20 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
209Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
02condensed with one carbocyclic ring
04Indoles; Hydrogenated indoles
10with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
18Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
20substituted additionally by nitrogen atoms, e.g. tryptophane
C07D 215/14 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
215Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
02having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
12with substituted hydrocarbon radicals attached to ring carbon atoms
14Radicals substituted by oxygen atoms
C07D 231/12 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
231Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
02not condensed with other rings
10having two or three double bonds between ring members or between ring members and non-ring members
12with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 233/96 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
233Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
96having three double bonds between ring members or between ring members and non-ring members
CPC
A61K 45/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
45Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61P 31/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
A61P 31/04
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
04Antibacterial agents
A61P 43/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
43Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
C07C 2601/02
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
2601Systems containing only non-condensed rings
02with a three-membered ring
C07C 323/60
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
323Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
50containing thio groups and carboxyl groups bound to the same carbon skeleton
51having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton
60with the carbon atom of at least one of the carboxyl groups bound to nitrogen atoms
Applicants
  • SMITHKLINE BEECHAM PLC [GB]/[GB] (AllExceptUS)
  • BATESON, John, Hargreaves [GB]/[GB] (UsOnly)
  • WITTY, David, R. [GB]/[GB] (UsOnly)
  • GASSON, Brian, Charles [GB]/[GB] (UsOnly)
  • BEST, Desmond, John [GB]/[GB] (UsOnly)
  • PAYNE, David, John [GB]/[US] (UsOnly)
Inventors
  • BATESON, John, Hargreaves
  • WITTY, David, R.
  • GASSON, Brian, Charles
  • BEST, Desmond, John
  • PAYNE, David, John
Agents
  • VALENTINE, Jill, Barbara
  • GIDDINGS, Peter, John
Priority Data
9602860.013.02.1996GB
9610907.924.05.1996GB
9619147.313.09.1996GB
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) BETA-THIOPROPIONYL-AMINOACID DERIVATIVES AND THEIR USE AS BETA-LACTAMASE INHIBITORS
(FR) DERIVES D'ACIDES BETA-THIOPROPIONYLE AMINES ET LEUR UTILISATION EN TANT QU'INHIBITEURS DE BETA-LACTAMASE
Abstract
(EN)
A method of treatment of bacterial infections in humans or animals which comprises administering, in combination with a $g(b)-lactam antibiotic, a therapeutically effective amount of an amino acid derivative of Formula (I) or a pharmaceutically acceptable salt, solvate or $i(in vivo) hydrolysable ester thereof, wherein: R is hydrogen, a salt forming cation or an $i(in vivo) hydrolysable ester-forming group; R1 is hydrogen, (C1-6)alkyl optionally substituted by up to three halogen atoms or by a mercapto, (C1-6)alkoxy, hydroxy, amino, nitro, carboxy, (C1-6)alkylcarbonyloxy, (C1-6)alkoxycarbonyl, formyl or (C1-6)alkylcarbonyl group, (C3-7)cycloalkyl, (C3-7)cycloalkyl(C2-6)alkyl, (C2-6)alkenyl, (C2-6)alkynyl, aryl, aryl(C1-6)alkyl, heterocyclyl or heterocyclyl(C1-6)alkyl; R2 is hydrogen, (C1-6)alkyl or aryl(C1-6)alkyl; R3 is hydrogen, (C1-6)alkyl optionally substituted by up to three halogen atoms, (C3-7)cycloalkyl, fused aryl(C3-7)cycloalkyl, (C3-7)cycloalkyl(C2-6)alkyl, (C2-6)alkenyl, (C2-6)alkynyl, aryl, aryl-(CHR10)m-X-(CHR11)n, heterocyclyl or heterocyclyl-(CHR10)m-X-(CHR11)n, where m is 0 to 3, n is 1 to 3, each R10 and R11 is independently hydrogen or (C1-4)alkyl and X is O, S(O)x where x is 0-2, or a bond; R4 is hydrogen, or an $i(in vivo) hydrolysable acyl group; and R5 and R6 are independently hydrogen and (C1-6)alkyl or together represent (CH2)p where p is 2 to 5. Some compounds are claimed per se.
(FR)
Procédé de traitement d'infections bactériennes chez l'homme ou chez l'animal, consistant à administrer, combiné à un antibiotique de $g(b)-lactame, une quantité efficace sur le plan thérapeutique d'un dérivé d'acide aminé de Formule (I) ou d'un de ses sels, solvates ou esters hydrolysables $i(in vivo), acceptables sur le plan pharmaceutique, formule dans laquelle R représente hydrogène, un cation formant un sel ou un groupe formant un ester hydrolysable in vivo; R1 représente hydrogène, alkyle C1-C6 éventuellement substitué par trois atomes d'halogène au maximum ou par un groupe mercapto, alcoxy C1-C6,hydroxy, amino, nitro, carboxy, alkylcarbonyloxy C1-C6, alcoxycarbonyle C1-C6, formyle ou alkylcarbonyle C1-C6, cycloalkyle C3-C7, cycloalkyle C3-C7 alkyle C2-C6, alkényle C2-C6, alkynyle C2-C6, aryle, arylalkyle C1-C6, hétérocyclyle ou hétérocyclyle alkyle C1-C6; R2 représente hydrogène, alkyle C1-C6 ou aryle alkyle C1-C6; R3 représente hydrogène, alkyle C1-C6 éventuellement substitué par trois atomes d'halogène au maximum, cycloalkyle C3-C7, aryl fusionné cycoalkyle C3-C7, cycloalkyle C3-C7 alkyle C2-C6, alkényle C2-C6, alkynyle C2-C6, aryle-(CHR10)m-X-(CHR11)n, hétérocyclyle ou hétérocyclyle-(CHR10)m-X (CHR11)n dans laquelle m est 0 à 3, n est 1 à 3, chaque R10 et R11 représente indépendamment hydrogène ou alkyle C1-C4 et X représente 0-2 ou une liaison; R4 représente hydrogène ou un groupe acyle hydrolysable $i(in vivo); R5 et R6 représentent indépendamment hydrogène et alkyle C1-C6 ou représentent ensemble (CH2)n dans laquelle p est 2 à 5. On revendique certains composés.
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