Abstract: During the preparation of 6-(substituted methylene)-2-penem compounds (which are known for their anti-bacterial and .beta.-lactamase inhibitory properties) mixtures of the E-isomer and the Z-isomer may be formed. The Z-isomer is, however generally preferred, and the present invention provides a process whereby the E-isomer may be converted into the Z-isomer by reaction with an aromatic heterocyclic thiol in the presence of a base.

Abstract: A method for the treatment and/or prophylaxis of disorders associated with pulmonary hypertension and/or disorders associated with right heart failure, in mammals, such as humans, which method comprises administering to the mammal in need of such treatment and/or prophylaxis an effective and/or prophylactic amount of pinacidil; or a pharmaceutically acceptable salt thereof or a pharmaceutically acceptable solvate thereof.

Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein X is CO and Y is NH;Z is NR.sub.3 wherein R.sub.3 is hydrogen, C.sub.1-6 alkyl, C.sub.3-7 alkenyl-methyl, phenyl or phenyl C.sub.1-4 alkyl either of which phenyl moieties may be substituted by one or two of halogen, CF.sub.3, C.sub.1-6 alkoxy or C.sub.1-6 alkyl; and R.sub.a is not present; orZ is N and R.sub.a is as defined for R.sub.3 above;R.sub.b is present when X-Y-R.sub.2 is attached at the phenyl ring and is selected from hydrogen, halogen, CF.sub.3, hydroxy, C.sub.1-6 alkoxy or C.sub.1-6 alkyl;R.sub.1 is hydrogen, halogen, CF.sub.3, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, C.sub.1-7 acyl, C.sub.1-7 acylamino, C.sub.1-6 alkylsulphonylamino, N(C.sub.1-6 alkylsulphonyl)-N-C.sub.1-4 alkylamino, C.sub.1-6 alkylsulphinyl, hydroxy, nitro or amino, aminocarbonyl, aminosulphonyl, aminosulphonylamino or N-(aminosulphonyl)-C.sub.1-4 alkylamino optionally N-substituted by one or two groups selected from C.sub.

Abstract: Compounds of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein: j is 0 or 1;q is 0, 1 or 2;p is 0 and r is 2 or 3, orp is 1 and r is 2;X is O, S, SO or NR where R is hydrogen, C.sub.1-6 alkyl or C.sub.1-10 carboxylic acyl;Y is NH; or O when R.sub.1 is hydrogen;either R.sub.1-6 alkoxy and one of R.sub.2, R.sub.3 and R.sub.4 is hydrogen and the other two are selected from hydrogen, halogen, CF.sub.3, C.sub.1-6 alkylithio, C.sub.1-7 acyl, C.sub.1-10 carboxylic acylamino, C.sub.1-6 alkyl S(O)n wherein n is 0, 1 or 2, nitro or amino, aminocarbonyl or aminosulphonyl optionally substituted by one or two groups selected from C.sub.1-6 alkyl, C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkyl C.sub.1-4 alkyl or phenyl C.sub.1-4 alkyl groups any of which phenyl moieties may be substituted by one or two groups selected from halogen, CF.sub.3, C.sub.1-6 alkyl or C.sub.1-6 alkoxy; or R.sub.1 is hydrogen and R.sub.2, R.sub.3 and R.sub.4 are independently selected from hydrogen, C.sub.

Abstract: Compounds of formula (I), or a pharmaceutically acceptable salt thereof:Y-CO-L-Z (I)whereinL is NH or O; Y is a group of formula (a), (b) or (c): ##STR1## wherein R.sub.1 and R.sub.2, R.sub.5 and R.sub.6, R.sub.9 and R.sub.10, are independently selected from hydrogen or halogen;X is N or CR.sub.3whereinR.sub.3 is hydrogen or C.sub.1-6 alkoxy;R.sub.4 is hydrogen, halogen, CH.sub.3, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, C.sub.1-6 alkylsulphonyl, C.sub.1-6 alkylsulphinyl, C.sub.1-7 acyl, cyano, C.sub.1-6 alkoxycarbonyl, C.sub.1-7 acylamino, hydroxy, nitro or amino, aminocarbonyl, or aminosulphonyl, optionally N-substituted by one or two groups selected from C.sub.1-6 alkyl, C.sub.3-8 cycloalkyl, and C.sub.3-8 cycloalkyl C.sub.1-4 alkyl or disubstituted by C.sub.4 or C.sub.5 polymethylene; phenyl or phenyl C.sub.1-4 alkyl group optionally substituted in the phenyl ring by one or two of halogen, C.sub.1-6 alkoxy or C.sub.1-6 alkyl groups;one of R.sub.7 and R.sub.8 is C.sub.

Abstract: A method for treating livestock to decrease birth mortality rate and to increase post-natal survival rate by administering ethanolamine derivatives is disclosed.

Abstract: A hybrid protein which comprises plasmin A-chain linked to urokinase B-chain, the catalytic site of which is blocked by a removable blocking group.

Abstract: Pharmacuetical compositions for topical application to the skin are disclosed comprising the hydrated crystalline calcium salt of mupirocin and a corticosteriod intimately mixed therewith. The compositions are useful for the treatment of skin disorders in humans and domestic animals.

Abstract: .beta.-Lactam antibiotics having an .alpha.-formamido substituent on the carbon atom adjacent to the carbonyl group of the .beta.-lactam ring and in particular bicyclic compounds having the partial structure: ##STR1## Intermediates and processes for the preparation of the compounds are further disclosed.

Abstract: Injectable pharmaceutical compositions are provided which comprise fine particles of amoxycillin trihydrate coated with a dispersing agent, the ratio of amoxycillin trihydrate to dispersing agent being from 1000:1 to 20:1. A preferred dispersing agent is a mixture of polyvinylpyrrolidone and lecithin. Such compositions give surprising prolonged blood levels of amoxycillin after administration. The compositions can be used in the treatment of both humans and domestic animals.

Abstract: A method for increasing the weight gain and/or improving the feed utilization efficiency of livestock is described which comprises the oral or non-oral administration to livestock of an effective, non-toxic amount of a compound of formula (XX): ##STR1## or a salt thereof, in which W is phenyl optionally substituted by halogen or trifluoromethyl, or a benzofuran-2-yl group, R.sup.1x is hydrogen or methyl, R.sup.2x is carboxyl or a group O--Z.sup.4 --CO.sub.2 H or an ester or amide thereof; a group O--E.sup.1 --NR.sup.3x R.sup.4x or a group O--E.sup.1 --OR.sup.5x, wherein R.sup.3x, R.sup.4x and R.sup.5x each represents hydrogen or C.sub.1-6 alkyl, Z.sup.4 is a C.sub.1-6 straight or branched alkylene chain, x is 1 or 2, y is 2 or 3, and E.sup.1 is C.sub.2-7 straight or branched alkylene chain with at least two carbon atoms separating the two heteroatoms in the group R.sup.2x.

Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof; ##STR1## wherein L is NH or O;X and Y are independently selected from hydrogen or C.sub.1-4 alkyl, or together are a bond;R.sub.1 and R.sub.2 are independently selected from hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl-C.sub.1-4 alkyl, or together are C.sub.2-4 polymethylene;R.sub.3 and R.sub.4 are independently selected from hydrogen, halogen, CF.sub.3, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, C.sub.1-7 acyl, C.sub.1-7 acylamino, C.sub.1-6 alkylsulphonylamino, N-(C.sub.1-6 alkylsulphonyl)-N-C.sub.1-4 alkylamino, C.sub.1-6 alkylsulphinyl), hydroxy, nitro or amino, aminocarbonyl, aminosulphonyl, aminosulphonylamino or N-(aminosulphonyl)-C.sub.1-4 alkylamino optionally N-substituted by one or two groups selected from C.sub.1-6 alkyl, C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkyl C.sub.1-4 alkyl, phenyl or phenyl C.sub.1-4 alkyl groups or optionally N-disubstituted by C.sub.

Abstract: A compound of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## in which A represents a bond or --CH.sub.2 -- and B represents hydrogen, or A and B together with the carbon atom to which they are both attached represents a group ##STR2## R represents R.sub.1 OOC-- in which R.sub.1 is C.sub.1-4 alkyl, C.sub.2-4 alkenyl or C.sub.2-4 alkynyl; R.sub.2 O-- in which R.sub.2 is C.sub.1-3 alkyl, C.sub.1-2 alkylcarbonyl or aminocarbonyl optionally substituted by one or two methyl groups; or R.sub.3 CH.sub.2 - in which R.sub.3 is C.sub.1-2 alkoxy; and p represents an integer of 2 to 4, and wherein compounds of formula (I) where B is hydrogen have the stereochemical configuration in which the group R and the methylene bridge are both on the same side of the plane of the molecule which contains both bridge head atoms and the ring carbon atom bonded to the group R.

Abstract: Peptides comprising, in sequence, units selected from the amino acid residues 17 to 24 of VIP, and consisting at least of the amino acid residues 18 to 23, or an analogue thereof wherein one or more of the amino acid residues is replaced by an equivalent other amino acid; having anti-ulcer activity, a process for their preparation and their use as pharmaceuticals.

Abstract: A compound of formula (I): ##STR1## in which R is optionally substituted phenyl; C.sub.3-8 cycloalkyl; C.sub.5-8 cycloalkenyl; C.sub.1-8 alkyl which may be straight or branched; C.sub.2-8 alkenyl which may be straight or branched; 5- or 6-membered heterocyclyl; or optionally substituted phenyl C.sub.1-4 alkyl, each of Y and Z, which may be the same or different, is oxygen or sulphur; and X is --CH.sub.2 -- or oxygen, a process for the preparation of such compounds and their use in human and veterinary medicine.

Abstract: A compound of formula (I): ##STR1## or a pharmaceutically acceptable salt, ester or amide thereof, wherein: Z represents a residue of a substituted or unsubstituted aryl group,X represents O or NR.sup.o wherein R.sup.o represents a hydrogen atom, a substituted or unsubstituted alkyl group, a substituted or unsubstituted aryl group, an alkanoyl group substituted or unsubstituted in the alkyl moiety, or an arylalkyl moiety substituted or unsubstituted in the aryl moiety.n represents an integer 1 or 2,m represents an integer 1 or 2,p represents an integer 2 or 3, andq represents an integer in the range of from 1 to 12; pharmaceutical compositions containing such compounds and the use of such compounds and compositions in medicine.

Abstract: Crystalline anhydrous amoxycillin is prepared by removing bound solvent molecules from a crystalline solvate (other than the trihydrate) of amoxycillin. A preferred crystalline solvate is the monomethanolate.

Abstract: Compounds of formula (I): ##STR1## wherein ##STR2## is a 5-membered heterocyclic group having a 6-.pi.electron system, the five ring atoms being either(a) one carbon atom and four atoms selected from carbon and nitrogen,(b) two carbon atoms, two nitrogen atoms and one atom selected from oxygen and sulphur, or(c) four carbon atoms and one atom selected from oxygen and sulphurand R.sup.1 is a substituent on a carbon or nitrogen of ##STR3## selected from C.sub.1-20 alkyl, C.sub.2-8 alkenyl aryl, aralkyl and heterocyclyl, each of which may optionally be substituted; hydrogen and C.sub.3-7 cycloalkyl,and, where appropriate, R.sup.2 is a substituent on a carbon or nitrogen of ##STR4## and when present is the same or different to R.sup.1 and is selected from C.sub.1-20 alkyl, C.sub.2-8 alkenyl, aryl, aralkyl and heterocyclyl each of which may optionally be substituted; hydrogen and C.sub.3-7 cycloalkyl, have antibacterial and antimycoplasmal activity.

Abstract: A compound of formula (I): ##STR1## or a pharmaceutically acceptable acid addition salt and/or a pharmaceutically acceptable solvate thereof, wherein A represents a residue of a benzene ring optionally having up to four substituents selected from the group consisting of halogen, C.sub.1-6 alkyl aNd C.sub.1-6 alkoxy; R.sup.1 and R.sup.2 each independently represent a hydrogen atom or a C.sub.1-6 alkyl group; X represents a bond or a moiety CHR.sup.1 wherein R.sup.1 is as defined above; and Z represents O, NH or S.

Abstract: A process is disclosed for the preparation of a compound of formula (I): ##STR1## where Ar is aryl or substituted aryl and R.sup.3 and R.sup.4 are the same or different and each is alkyl, which process comprises hydrognating a compound of formula (II): ##STR2## wherein Ar, R.sup.3 and R.sup.4 are as defined with respect to formula (I) and Hal is a halogen atom.Compounds of formula (I) are useful as chemical intermediates.