Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Carbohydrate doai
Patent
1998-10-09
2000-08-01
Fonda, Kathleen K.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Carbohydrate doai
536 72, 536 74, A61K 3170
Patent
active
060967145
DESCRIPTION:
BRIEF SUMMARY
The present invention relates to new erythromycin derivatives, their preparation process and their use as medicaments.
A subject of the invention is the compounds of formula (I): ##STR2## in which: X represents a CH.sub.2 or SO.sub.2 radical or an oxygen atom, Y represents a (CH.sub.2)m--(CH.dbd.CH).sub.n (CH.sub.2).sub.o radical, with m+n+o.ltoreq.8, n=0 or 1, ##STR3## in which R" represents an alkyl radical containing up to 8 carbon atoms or an optionally substituted aryl radical, addition salts with acids.
Among the addition salts with acids, there can be can mentioned the salts formed with the following acids: acetic, propionic, trifluoroacetic, maleic, tartaric, methanesulphonic, benzenesulphonic, p-toluenesulphonic, and in particular stearic, ethylsuccinic or laurylsulphonic.
The aryl radical can be a phenyl or naphthyl radical.
The aryl radical can also be a substituted or non-substituted heterocyclic radical such as the thienyl, furyl, pyrolyl, thiazolyl, oxazolyl, imidazolyl, thiadiazolyl, pyrazolyl or isopyrazolyl radical, a pyridyl, pyrimidyl, pyridazinyl or pyrazinyl radical, or also an indolyl benzofurannyl, benzothiazyl or quinolinyl radical.
These aryl radicals can contain one or more groups chosen from the group constituted by hydroxyl radicals, halogen atoms, NO.sub.2 radicals, C.tbd.N radicals, alkyl, alkenyl or alkynyl, O-alkyl, O-alkenyl or O-alkynyl, S-alkyl, S-alkenyl or S-alkynyl and N-alkyl, N-alkenyl or N-alkynyl radicals, containing up to 12 carbon atoms optionally substituted by one or more halogen atoms, the ##STR4## R.sub.a and R.sub.b, identical or different, representing a hydrogen atom or an alkyl radical containing up to 12 carbon atoms, the ##STR5## R.sub.3 representing an alkyl radical containing up to 12 carbon atoms, or an optionally substituted aryl or heteroaryl radical, the following radicals: carboxylic aryl, O-aryl or S-aryl or heterocyclic aryl, O-aryl or S-aryl with 5 or 6 members containing one or more heteroatoms, optionally substituted by one or more of the substituents mentioned hereafter.
As preferred heterocycle, there can be mentioned among others: ##STR6## and the heterocyclic radicals envisaged in the European Patent Applications 487411, 596802, 676409 and 680967. These preferred heterocyclic radicals can be substituted by one or more functional groups.
A more particular subject of the invention is the compounds of formula (I) in which Z represents a hydrogen atom, those in which W represents a hydrogen atom, those in which X represents a CH.sub.2 radical, those in which Y represents a (CH.sub.2).sub.3, (CH.sub.2).sub.4 or (CH.sub.2).sub.5 radical.
Among the preferred compounds of the invention, there can be mentioned the compounds of formula (I), in which Ar represents a heterocyclic aryl radical, such as for example those in which Ar represents a 4-quinolinyl radical optionally mono- or polysubstituted on one and/or the other of the 2 quinoline rings, and quite particularly the compounds of formula (I) in which Ar represents a non-substituted 4-quinolinyl radical, or also for example the compounds of formula (I), in which Ar represents an optionally substituted: ##STR7##
Among the preferred compounds of the invention, there can naturally be mentioned the products whose preparation is given hereafter in the experimental part.
The products of general formula (I) have a very good antibiotic activity on gram.sup.+ bacteria such as staphylococci, streptococci, pneumococci.
The compounds of the invention can therefore be used as medicaments in the treatment of infections caused by susceptible germs and in particular, in that of staphylococcal infections, such as staphylococcal septicemias, malignant staphylococcal infections of the face or skin, pyodermatitis, septic or suppurating sores, boils, anthrax, phlegmons, erysipelas and acne, staphylococcia such as acute primary or post-influenzal angina, bronchopneumonia, pulmonary suppuration, streptococcal infections such as acute anginas, otitis, sinusitis, scarlet fever, pneumococcal infections such as pneumon
REFERENCES:
patent: 5444051 (1995-08-01), Agouridas et al.
LeMahieu et al. J. Med. Chem. 1974, 17(9), 953-956.
Agouridas Constantin
Chantot Jean-Francois
Fonda Kathleen K.
Hoechst Marion Roussel
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