Abstract: A compound of formula (II), named pseudomonic acid C or a salt or ester thereof: ##STR1## has antibacterial and anti-mycoplasma activity, and can be produced either by fermentation of Pseudomonas fluorescens, or by de-oxygenation of pseudomonic acid A, the compound having an epoxide in place of the double bond. The compounds are therefore useful in the treatment of human and veterinary bacterial and mycoplasma-induced infections.
Abstract: An apparatus for culturing cells is produced which comprises a vessel, a solid porous matrix within the vessel which permits the adherence of cells, a foam generator located to supply foam to at least part of the surface of the solid porous matrix and means for removing liquid from the vessel.
Abstract: Orally administrable pharmaceutical compositions for reducing the rate of gastric acid secretion and acid addition salts thereof containing an effective amount of halo-substituted 2-pyridyl thioureas and a pharmaceutical carrier and a method of treating gastric ulcers and reducing gastric acid secretion with such compositions.
Abstract: A process for the purification of pseudomonic acid, particularly suitable for isolating the compound when prepared by bacterial culture, comprises making a solution in an organic solvent of the acidic components of the crude preparation substantially free of the neutral components. The polarity of the organic solvent is adjusted so that the pseudomonic acid crystallizes. This may be achieved either by adding a non-polar diluent such as n-heptane to the solution for example in methyl iso-butyl ketone; or by employing a di-C.sub.1-6 alkyl ether in which the acidic components dissolve and then crystallize out.
Type:
Grant
Filed:
September 29, 1978
Date of Patent:
September 16, 1980
Assignee:
Beecham Group Limited
Inventors:
Peter J. O'Hanlon, Maurice C. Woodford, Norman H. Rogers
Abstract: Pharmaceutically acceptable particles comprising an anhydrous hygroscopic salt of clavulanic acid dispersed in a polymeric binder of low water vapour permeability may be used in the preparation of pharmaceutical compositions of enhanced storage stability.
Abstract: This invention provides compounds, having major tranquilizing activity, of the formula (II): ##STR1## wherein R.sub.1 is a phenyl group optionally substituted by a fluorine, chlorine or bromine atom or an alkyl or alkoxyl group of up to 3 carbon atoms; R.sub.2 is a hydrogen atom or an alkyl group of up to 4 carbon atoms; R.sub.3 is a hydrogen atom or an amino group, a nitro group or a group of the formula NHCOR.sub.4 or NHCO.sub.2 R.sub.4 where R.sub.4 is an alkyl group of up to 4 carbon atoms optionally substituted by one, two or three chlorine atoms or by three fluorine atoms attached to the same carbon atom; n is 0, 1 or 2; and X is a group of the sub-formula (a), (b), (c) or (d):--CH.sub.2 --CH.sub.2 --NR.sub.5 -- (a) ##STR2## wherein R.sub.5 is an alkyl group of up to 4 carbon atoms; or a N-oxide thereof of the nitrogen atom to which the CHR.sub.2 --(CH.sub.2).sub.n --R.sub.
Abstract: Compounds of the formula (I): ##STR1## wherein G is hydrogen, alkyl, alkenyl, substituted alkyl or substituted alkenyl, R.sub.1 is alkyl or aryl, substituted alkyl or substituted aryl, and R is an organic group such that --CO.sub.2 R is an ester group are produced. The compounds are useful as antibacterial and .beta.-lactamase inhibitory agents.
Abstract: A process for making solid sodium amoxycillin is disclosed. The process comprises freeze drying a solution containing sodium amoxycillin in a solvent system containing water and a secondary or tertiary carbinol of four or five carbon atoms which is at least 5% w/v soluble in water at 25.degree..
Abstract: The invention provides novel compounds of formula (I). ##STR1## and pharmaceutically acceptable salts thereof wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 which may be the same or different, represent hydrogen, halogen, lower alkyl, and lower alkoxy, or any adjacent two of R.sub.1 to R.sub.4 taken together represent an alkylene group containing from 3 to 5 carbon atoms or a 1,4-buta-1,3-dienylene group. The compounds are useful as anti-allergic agents.
Abstract: Peptides (6-12 amino acids) and their salts, useful in allergy desensitization compositions, particularly vaccines, have the formulaX--R--R.sub.1 --R.sub.2 --R.sub.3 --Ywhere R is optional and, if present, is a group resistant to enzyme hydrolysis; R.sub.1 is a basic amino acid residue optionally linked to basic and/or neutral nonhydrophobic amino acid residues; R.sub.2 is one or more neutral nonhydrophobic amino acid residues; R.sub.3 is one or more hydrophobic amino acid residues optionally linked to neutral nonhydrophobic amino acid residues; X is hydrogen or an N-protecting group; and Y is hydroxyl or a C-terminal protecting group. Examples are:Lys Thr Lys Gly Ser Gly Phe Phe OCH.sub.3Arg Lys Thr Lys Gly Ser Gly Phe Phe OCH.sub.3Lys Thr Lys Gly Ser Gly Phe Phe Val Phe OCH.sub.3Lys Thr Lys Gly Ser Gly Phe Phe Val Phe OHPro Arg Lys Thr Lys Gly Ser Gly Phe Phe OCH.sub.
Type:
Grant
Filed:
June 29, 1978
Date of Patent:
September 16, 1980
Assignee:
Beecham Group Limited
Inventors:
Peter Roy, Brian G. Overell, Denis R. Stanworth
Abstract: This invention provides a process for the preparation of salts of the .beta.-lactamase inhibitory antibiotics MM4550A, MM13902 and MM17880, which are the compounds of the formulae (I)-(III), respectively: ##STR1## which process comprises cultivating a strain of Streptomyces gedanensis and isolating a salt of at least one of MM4550A, MM13902 and MM17880.
Abstract: This invention provides a process for the preparation of 4-(6'-methoxy-2'naphthyl)-butan-2-one, which process comprises the hydrogenation of 4-(6' methoxy-2'-naphthyl)-4-hydroxy-but-3-en-2-one.
Abstract: Anti-inflammatory compositions are prepared which comprise a therapeutically effective effective amount of a compound of the formula ##STR1## wherein X is CO; Y is an oxygen atom; the dotted line represents a double bond which is present or absent; R.sub.1 is hydrogen or methyl; R.sub.2 is hydrogen; and R.sub.3 is phenyl unsubstituted or substituted by 1 or 2 substituents selected from the group consisting of fluorine, chlorine, bromine, methyl, ethyl, methoxyl, ethoxyl, benzyloxyl, hydroxyl, acetoxyl, trifluoromethyl, nitro, amino, acetyl, methylthiol, methylsulphonyl, methylamino and dimethylamino; in combination with a pharmaceutically acceptable carrier. Methods of treating inflammation utilizing the compounds of formula (I) are part of the present invention together with the compounds themselves of the above formula.
Type:
Grant
Filed:
February 17, 1978
Date of Patent:
August 5, 1980
Assignee:
Beecham Group Limited
Inventors:
William G. Cole, Alexander C. Goudie, Carl J. Rose
Abstract: A thiol acid and esters thereof of formula (II): ##STR1## wherein R is hydrogen, a salt forming ion or a pharmaceutically acceptable ester-forming radical, have antibacterial and antimycoplasmal activity and are therefore useful in the treatment of human and veterinary bacterial and mycoplasmal infections.
Type:
Grant
Filed:
November 22, 1978
Date of Patent:
August 5, 1980
Assignee:
Beecham Group Limited
Inventors:
John P. Clayton, Norman H. Rogers, Steven Coulton
Abstract: A class of esters of the penicillin, nafcillin have the general formula: ##STR1## wherein A is a C.sub.1 -C.sub.6 alkylene group substituted with one or two groups of formula --NR.sup.1 R.sup.2 and optionally further substituted with one or more methyl or ethyl groups, wherein R.sup.1 and R.sup.2 are the same or different and each is a C.sub.1 -C.sub.6 alkyl group or R.sup.1 and R.sup.2 together with the nitrogen atom to which they are attached form a saturated 5- or 6- membered heterocyclic ring. Upon oral administration, the esters are absorbed into the bloodstream where they are hydrolyzed to release the antibacterially active parent penicillin, nafcillin.
Abstract: This invention provides the compounds of the formula (II): ##STR1## and salts and esters thereof, wherein R.sub.1 is H and R.sub.3 is H or an aryl, aralkyl, lower alkyl or substituted lower alkyl group or R.sub.1 and R.sub.3 are joined so that the CHR.sub.1.NH.CO.R.sub.3 moiety forms a group of the sub-formula (a): ##STR2## wherein R.sub.4 is a hydrogen atom or a NH.CO.R.sub.5 group wherein R.sub.5 is a lower alkyl, lower alkoxy lower alkyl, aryl, aralkyl, aryloxyalkyl, lower alkoxy or aryloxy group.The compounds have .beta.-lactamase inhibitory and anti-bacterial properties.The invention also provides a process for their preparation, and pharmaceutical compositions containing them.
Abstract: Compounds of the formula (I), and their pharmaceutically acceptable salts: ##STR1## wherein: R.sub.1 is a C.sub.1-6 alkoxy group;R.sub.2 and R.sub.3 are the same or different and are hydrogen, halogen, CF.sub.3, hydroxy, C.sub.1-6 alkoxy, C.sub.2-7 acyl, amino, amino substituted by one or two C.sub.1-6 alkyl groups, C.sub.2-7 acylamino aminocarbonyl or aminosulphone optionally substituted by one or twoC.sub.1-6 alkyl groups, C.sub.1-6 alkylsulphone or nitro groups;X is either a nitrogen atom, in which case m+n is 3 to 5, m is 2 to 4, n is 1 to 3; or X is CH in which case m+n is 2 to 5, m is 1 to 5, and n is 0 to 4;p is 0 to 3;R.sub.4 is hydrogen, C.sub.1-6 alkyl, phenyl or phenyl-C.sub.1-6 alkyl, either of which phenyl moiety may be substituted by C.sub.1-6 alkyl, C.sub.1-6 alkoxy, CF.sub.3 or halogen, and R.sub.5 is hydrogen; or R.sub.4 and R.sub.5 are attached to two adjacent carbon atoms and form together with these two carbon atoms a fused benzene ring, which benzene ring may be substituted by C.sub.
Abstract: A class of 2-substituted benzisothiazolones carrying a nitrogen-containing heterocyclic ring are effective in inhibiting platelet aggregation and are therefore of value in the prophylactic and therapeutic treatment of thrombotic diseases.