Abstract: The invention relates to novel, edible fat-containing food products adapted for human infant nutrition containing a novel fat composition. The fat composition comprises (a) palm oil; (b) an oil selected from olive oil and oleic oil; (c) an oil selected from coconut oil, babassu oil and palm kernel oil; (d) an oil selected from soybean oil, corn oil, sunflower seed oil, cotton seed oil and safflower oil, and, if desired, (e) up to 2% calculated on the weight of the fat composition, of a lecithin such as soy lecithin. The amounts of the oils are so chosen that the composition contains defined quantities of linoleic acid, oleic acid, lauric and myristic acids and palmitic and stearic acids.

Abstract: The invention provides novel silyl reagents of Formula IR.sup.b R.sup.c R.sup.d SiNCYwherein R.sup.b is a branched chain alkyl of 3-10 carbon atoms, cycloalkyl of 4-8 carbon atoms or branched chain aralkyl of 8-12 carbon atoms and R.sup.c and R.sup.d are selected from alkyl of 1-10 carbon atoms, cycloalkyl of 4-8 carbon atoms, aralkyl of 7-12 carbon atoms or aryl with the proviso that R.sup.c and R.sup.d are not the same group as R.sup.b, and Y is oxygen or sulphur. A further novel compound tri-isopropylsilyl isothiocyanate is also included. These silyl reagents are useful in preparing tetrahydroquinoline 8-nitriles, amides and thioamides as described in Ser. No. 506,279.

Abstract: The invention provides a compound of formula I ##STR1## wherein A is a C.sub.1 -C.sub.4 straight or branched alkylene chain which may be saturated or unsaturated,B is a C.sub.2 -C.sub.4 straight or branched alkylene chain which may be saturated or unsaturated,Ar is a phenyl or naphthyl group which may be substituted or unsubstituted,R.sup.1 and R.sup.2 are the same or different and are hydrogen, alkyl, alkoxy, alkoxyalkyl, hydroxyalkyl, hydroxy, halogen, nitro, carboxy, a carboxylic alkyl ester, carbamoyl, carbamoyloxy, cyano, acyl, acylamino or trifluoromethyl, or an acid addition salt thereof.The compounds are useful for the treatment of ulcers or hypersecretion in mammals. Pharmaceutical compositions containing the novel compounds and processes for their preparation are described.

Abstract: Compounds containing a cation of formula Ia ##STR1## and a pharmaceutically acceptable anion are anti-fungal agents. In formula Ia and Ib R.sub.1 is alkyl of at least 3 carbon atoms or aralkyl; R.sub.2 and R.sub.5 are hydrogen, lower alkyl, lower alkoxy, halogen or nitro; R.sub.6 and R.sub.7, when separate, are lower alkyl or aryl(lower)alkyl or, when joined together, are --(CH.sub.2).sub.2 --A--(CH.sub.2).sub.2 -- (where A is --(CH.sub.2).sub.n --, O, S or NR.sub.8 where n is O, 1 or 2 and R.sub.8 is lower alkyl) or a mono- or di-(lower alkyl) substitution product thereof.

Abstract: This invention concerns the use in the treatment or prevention of atherosclerotic disorders and/or coronary heart disease of compounds of formula ##STR1## represents a ring system of formula ##STR2## wherein R.sup.1 represents hydrogen, methyl or benzyl, R.sup.2 represents hydrogen or methyl, R.sup.3 represents hydrogen or methoxy, R.sup.5 represents phenyl, 3-indolyl, 2-furyl, diphenylmethyl, benzyloxy, or phenyl monosubstituted by chlorine, bromine, lower alkyl, carboxy, methylenedioxy, trifluoromethyl or phenyl, or represents phenyl substituted up to three times by lower alkoxy, A represents an ethylene or a 1-oxoethylene biradical, and Z is an oxo- group or, when A is ethylene and R.sup.5 is phenyl, may also represent two hydrogen atoms, and X is an anion of a pharmaceutically acceptable acid.

Abstract: The invention concerns benzoquinolizines of general formula ##STR1## or their pharmaceutically acceptable acid addition salts. In the formula R.sup.1 and R.sup.2 which may be the same or different each represent hydrogen, lower alkyl, lower alkoxy or halogen, R.sup.3 represents lower alkyl and R.sup.4 is lower alkoxy or lower alkoxy carbonyl. The compounds possess .alpha..sub.2 -adrenoceptor antagonistic activity in warm blooded animals.

Abstract: The invention concerns novel compounds of formula IIIAR.sub.x.sup.a Si(NCS).sub.4-x IIIAwherein R.sup.a is selected from electron donating substituents consisting of alkoxy of 1-10 carbon atoms, cycloalkoxy of 4-8 carbon atoms, aralkoxy of 7-12 carbon atoms, phenoxy which may be substituted by alkyl of 1-10 carbon atoms, alkoxy of 1-10 carbon atoms or trifluoromethyl, the group R.sup.b R.sup.c N-wherein R.sup.b and R.sup.c are selected from alkyl of 1-6 carbon atoms, cycloalkyl of 4-6 carbon atoms, phenyl which may be substituted by alkyl of 1-10 carbon atoms, alkoxy of 1-10 carbon atoms or trifluoromethyl, and aralkyl of 7-12 carbon atoms or R.sup.b and R.sup.

Abstract: The invention relates to the preparation of 1-bromo-2-D-alkylpropanoyl-L-proline derivatives and analogous compounds which are useful as chemical intermediates to angiotensin converting enzyme (ACE) inhibitors and to the stereospecific synthesis of such ACE inhibitors having the formula: ##STR1## wherein R.sup.1 is lower alkyl and R.sup.4 and R.sup.5 are both hydrogen or together with the carbons to which they are attached represent a benzene ring optionally substituted by defined substituents. Intermediates of formula ##STR2## are also disclosed wherein R.sup.1, R.sup.4, R.sup.5 are as defined above and B.sup.+ is a cation.

Abstract: The invention provides a compound of the formula I ##STR1## wherein Y is a heterocyclic radical of formula ##STR2## wherein R is hydrogen or lower alkyl, R.sup.1 is hydrogen, hydroxy, lower alkyl, hydroxyloweralkyl, loweralkoxyloweralkyl, loweralkoxy, halogen, formyl, phenyl, phenylalkyl, halophenyl, or acetal [CH(OR.sup.4).sub.2 where R.sup.4 is lower alkyl or two R.sup.4 radicals are joined to form a lower alkylene chain], m is 1 or 2, the dotted lines in formula V represent an optional double bond in one of the indicated positions, A is a saturated or unsaturated alkylene radical having from 1 to 6 carbon atoms, which may be substituted by lower alkyl of 1 to 6 carbon atoms, S is sulphur and R.sup.3 is lower alkyl, phenyl or aralkyl of 7 to 12 carbon atoms and Z.sup.- is an anion, and acid addition salts thereof, with the provisos that (1) when more than one R.sup.1 radical is present in the molecule then the R.sup.

Abstract: The invention provides new silyl derivatives of 5,6,7,8-tetrahydroquinolines and related compounds. The tetrahydroquinolines are substiuted at the 8-position by the group SiR.sub.3 where R may be one of various hydrocarbon groups or an electron donating substituent. The 8-position may also carry a lithium, sodium or potassium atom. The new silyl derivatives may be prepared by treating a corresponding 8-lithio, sodio or potassio tetrahydroquinoline with a silyl halide R.sub.3 SiHal followed by a metal compound R*M where M is sodium, potassium or lithium and R* is alkyl, cycloalkyl, aralkyl or aryl or an amine residue. The new silyl derivatives are useful intermediates for the preparation of known 5,6,7,8-tetrahydroquinline-8-nitriles, amides and thioamides employing an alkyl silyl isothiocyanate or cyanate. The nitriles and thioamides are anti-ulcer agents. The related compounds may be made by analogous methods.

Abstract: The invention concerns benzoquinolizines of general formula ##STR1## and their pharmaceutically acceptable acid addition salts. In the formula R.sup.1 and R.sup.2 which may be the same or different each represent hydrogen, lower alkyl, lower alkoxy or halogen, R.sup.3 represents hydrogen or lower alkyl and R.sup.4 represents a heterocyclic radical attached to the SO.sub.2 group through a carbon atom of the heterocyclic ring. The compounds possess .alpha..sub.2 -adrenoceptor antagonistic activity in warm blooded animals.

Abstract: This invention concerns compounds of formula ##STR1## and acid addition salts thereof, wherein R represents lower alkoxy, alkanoyloxy of 2 to 7 carbon atoms or hydroxy;R.sup.1 and R.sup.2 independently represent hydrogen, lower alkoxy, alkanoyloxy of 2 to 7 carbon atoms, hydroxy or lower alkyl;R.sup.3, R.sup.4 and R.sup.5 each represent hydrogen or lower alkyl with the proviso that at least one of R.sup.3, R.sup.4 and R.sup.5 is lower alkyl;and R.sup.6 and R.sup.7 each represent hydrogen or lower alkyl which possess anti-ulcer activity.

Abstract: The invention concerns novel compounds of formula IX--A--S--Y (I)wherein X is a radical selected from imidazolyl, pyridyl, quinolyl, tetrahydropyridyl or piperidyl any of which may be substituted and Y is any of the above radicals or a pyridinium radical, A is alkylene of 1-6 carbon atoms. Most of the compounds are anti-ulcer agents but some have anti-hypertensive activity, e.g. where X is quinolyl. Methods of treating ulcers and anti-ulcer compositions are also described.

Abstract: An improved process for preparing fused carbocyclic ring derivatives of pyridine especially 5,6,7,8-tetrahydroquinoline 8-nitriles, amides and thioamides is described. The nitriles and thioamides are anti-ulcer and/or anti-secretory agents. Typically a compound of formula A ##STR1## wherein M is sodium, potassium, lithium or MgHal where Hal is chlorine, bromine or iodine, is reacted with a silyl compound R.sub.x.sup.a Si(NCY).sub.4-x III, wherein R.sup.a is selected from electron donating substituents, e.g. alkoxy or dialkylamino, and hydrocarbon substituents e.g. alkyl, at least one R.sup.a being an electron donating substituent, Y is oxygen or sulphur, x has a value from 1 to 3, then subjecting the product to hydrolysis or alcoholysis to obtain the corresponding nitrile, amide or thioamide, provided that when a nitrile is desired the molar ratio of compound III to compound A is at least 2:1 and x is 3 and Y is S. The products may be isolated as acid addition salts.

Abstract: The invention concerns pharmaceutical compositions containing a novel oxazole derivative, calcium oxaprozin. The formulations may be for oral or other use. The oral formulations are more palatable than those containing oxaprozin itself.

Abstract: Fused carbocyclic ring derivatives of pyridine which contain a nitrile or thioamide group on the carbocyclic ring e.g. 8-cyano or thiocarboxamido-5,6,7,8-tetrahydroquinolines are prepared by a process in which a sodium, potassium, lithium or magnesium halide derivative of the pyridine compound is treated with a compound RaRbNCN wherein Ra and Rb are the same or different and represent alkyl, cycloalkyl, or aralkyl, or Ra and Rb are joined to form a heterocyclic ring with the nitrogen, and the product is treated with a proton source to obtain the nitrile which is optionally treated with a sulphurizing agent to form the thioamide. The nitriles or thioamides may be isolated as their acid addition salts.

Abstract: An improved process for preparing tetrahydroquinolines and related compounds especially 5,6,7,8-tetrahydroquinoline-8-nitriles, amides and thioamides is described. The nitriles and thioamides are anti-ulcer and/or anti-secretory agents. Typically a compound of formula A ##STR1## where M is sodium, potassium, lithium or MgHal where Hal is chlorine, bromine or iodine, is reacted, e.g., in an ether solvent, with a silyl compound R.sub.x.sup.a Si(NCY).sub.4-x (III) wherein R.sup.a is alkyl, cycloalkyl, aralkyl, or aryl, at least one group R.sup.a being a branched chain alkyl, cycloalkyl, aryl or branched chain aralkyl, Y is oxygen or sulphur, x has a value from 1 to 3, then subjecting the product to hydrolysis or alcoholysis, to obtain the corresponding nitrile, amide or thioamide, provided that when a nitrile is desired the molar ratio of compound III to compound A is at least 2:1 and x is 3 and Y is S. The products may be obtained as acid addition salts.Compound A may contain various substituents, e.g.

Abstract: The invention concerns benzoquinolizines of general formula ##STR1## and their pharmaceutically acceptable acid addition salts. In formula (I), R represents hydrogen or lower alkyl, R.sup.1 and R.sup.2 which may be the same or different each represent hydrogen, lower alkyl, lower alkoxy or halogen, R.sup.3 and R.sup.4 which may be the same or different each represents lower alkyl, halo(lower)alkyl or aryl and A represents a lower alkylene group having 1 to 3 carbon atoms in the chain between the two N atoms. The compounds possess .alpha..sub.2 -adrenoceptor antagonistic activity in warm blooded animals.

Abstract: The invention provides a sustained release pharmaceutical composition comprising a mixture of micronized indoramin or a pharmaceutically acceptable salt thereof, a water-channelling agent, a wetting agent and a disintegrant, the mixture being in the form of a non-compressed pellet and having an enteric coat or a sustained release coat permeable to gastrointestinal juices. Sustained release capsules are also provided comprising a plurality of the aforementioned pellets.

Abstract: The invention relates to the preparation of 1-bromo-2-D-alkylphopanoyl-L-proline derivatives and analogous compounds which are useful as chemical intermediates to angiotensin converting enzyme (ACE) inhibitors and to the stereospecific synthesis of such ACE inhibitors having the formula: ##STR1## wherein R.sup.1 is lower alkyl and R.sup.4 and R.sup.5 are both hydrogen or together with the carbons to which they are attached represent a benzene ring optionally substituted by defined substituents. Intermediates of formula ##STR2## are also disclosed wherein R.sup.1, R.sup.4, R.sup.5 are as defined above and B.sup.+ is a cation.