Abstract: The invention describes a process for preparing peptides. More particularly, a process for preparing L-.alpha.-aspartyl-L-phenylalanine C.sub.1 -C.sub.4 lower alkyl ester is described and claimed by enzymatic hydrolysis of a suitable N-acyl-derivative.

Abstract: The invention discloses a method for extracting phenylalanine from the broths obtained by enzymatic processes; this method consists in flocculating and filtering the broth, concentrating the filtrate followed by filtering off the resulting cinnamic acid, decolorating and concentrating the filtrate to obtain phenylalanine crystals at a very pure degree.

Abstract: The present invention relates to new condensed benzopyrone derivatives having a 5-tetrazolyl substituent thereon, and to pharmaceutical compositions containing them. The compounds are useful in the treatment of allergic conditions.

Abstract: Described is a novel process for the preparation of penams and penems useful as antibacterial agents, which comprises the reaction of an appropriate 4-substituted-azetidin-2-one with a base, followed by reaction of the thereby formed penam compound with an oxidating agent and a organic or inorganic base.Also described are novel penam compounds useful as antibacterials which are prepared by the described process.

Abstract: There are provided ergoline compounds of the formula: ##STR1## wherein R.sub.1 is a hydrogen atom or a methyl group; R.sub.2 is a hydrogen or halogen atom, a methyl or thiomethyl group; R.sub.3 is a hydrogen atom or a methoxy group; R.sub.4 is a hydrocarbon group having from 1 to 4 carbon atoms; n is 1 or 2; each of R.sub.5 and R.sub.6 independently is a hydrogen atom, an alkyl group having from 1 to 3 carbon atoms, or a phenyl or hydroxy or alkoxy group having from 1 to 4 carbon atoms, and X is an oxygen atom or a group of the formula NR.sub.7 wherein R.sub.7 is selected from the group consisting of a hydrogen atom, an alkyl having from 1 to 4 carbon atoms and a phenyl group, or a group of the formula N.dbd.C--R.sub.8 wherein the carbon atom is positioned between the nitrogen atoms in the ring and R.sub.8 is an amino, substituted amino, methyl, phenyl, thiomethyl or mercapto group. The compounds have antihypertensive and antiprolactin activity.

Abstract: A process for the preparation of the N-L-.alpha.-aspartyl-L-phenylalanine 1-methyl ester (aspartame) which is characterized by adding phosphoric acid and a lower alkyl alcohol to the reaction mixture containing N-formyl .alpha.-L-aspartyl- and .beta.-L-aspartyl-L-phenyl-alanine methyl ester and only one of the resultant deformylated isomers, i.e. aspartame phosphate precipitates.The .alpha.-isomer phosphate is collected by filtration and converted to free aspartame by treatment with a base.

Abstract: A method for performing porosimetric analyses and apparatus therefor are disclosed. In particular, a method for performing porosimetric anaylses by the so-called mercury method is disclosed, wherein volumetric variations of mercury placed in a vessel are recorded. These variations are due to mercury penetration into the pores of a solid sample placed in the vessel under the mercury pressure variations. In the method disclosed, additional porosimetric information is obtained by reducing the pressure from a maximum value as a predetermined function of time. For example, the pressure reduction can be at a constant rate. Simultaneously, volume variations of the mercury exiting the sample pores are detected as the pressure decreases.

Abstract: A water-swellable, water-insoluble polymer is loaded with a biologically active substance or substance convertible into a biologically active substance in vivo by preparing and grinding a mixture of a said substance with a water-swellable, water-insoluble polymer in a weight ratio of the said substance:polymer of from 1:0.1 to 1:100. The thus-loaded polymer is useful as a pharmaceutical composition.

Abstract: A water-swellable, water-insoluble polymer is loaded with methylhydroxyprogesterone acetate (MAP) by:(a) preparing and grinding a mixture of a said polymer and MAP; or(b)(i) preparing a mixture of a said polymer which is stable under the heating to which the mixture is subjected in step (ii) and MAP and (ii) heating the mixture up to the melting temperature of MAP; or(c) swelling a said polymer with a MAP solution capable thereof and drying the resulting swollen polymer/MAP system.The MAP loaded polymer is useful as a pharmaceutical composition.

Abstract: There are provided ergoline derivatives of the formula: ##STR1## wherein R.sub.1 represents a hydrogen atom or a methyl group, R.sub.2 represents a hydrogen or halogen atom or a methyl group, R.sub.3 represents a hydrogen atom or a methoxy group, R.sub.4 represents a hydrocarbon group having from 1 to 4 carbon atoms; each of X and W independently represents a hydrogen atom, a methyl group, a chlorine atom or a methoxy group, and n is 0, 1 or 2. A method for their preparation is also provided. The compounds have strong antiprolactin activity.

Abstract: A process for preparing 2-methyl substituted penems useful as antibiotics agent and/or as intermediates thereof, by reacting an appropriate 1-imido-3,4-disubstituted azetidinone derivative with a trivalent organophosphorus compound in an inert solvent at a temperature of from 110.degree. to 150.degree. C. for a period of from 2 hours to a few days.

Abstract: 16-Fluoro-16,17-didehydro prostanoids, processes for their preparation, compositions containing them and methods of using them are disclosed. The compounds and compositions have pharmaceutical utility including, for example, luteolytic activity.

Abstract: A compound of formula I: ##STR1## wherein either (i) each of R.sub.1 and R.sub.2 independently represents a hydrogen atom or an organic group, or (ii) R.sub.1 and R.sub.2 linked together form a heterocyclic ring or (iii) R.sub.2 is hydrogen and R.sub.1 is ##STR2## wherein each of R.sub.6 and R.sub.7 independently represents hydrogen or an organic group, n is 0-3, X is O, S, NH, NR.sub.8, CHNO.sub.2 or CHSO.sub.2 R.sub.4, wherein R.sub.8 and R.sub.4 are organic groups and R.sub.3 represents an organic group. The compound of formula I is effective as an anti-ulcer agent and is highly effective as a histamine H.sub.2 -receptor antagonist.

Abstract: The invention relates to compounds having the general formula (I) ##STR1## wherein R.sub.1 is carboxy, esterified carboxy or an amide of formula ##STR2## in which R.sub.9 is hydrogen or C.sub.1 -C.sub.6 alkyl, A is C.sub.2 -C.sub.6 alkylene and R.sub.a and R.sub.b are hydrogen or C.sub.1 -C.sub.6 alkyl or R.sub.a and R.sub.b taken together with the nitrogen atom to which they are linked form a saturated, optionally substituted, heteromonocyclic ring;R.sub.2 is hydrogen or C.sub.1 -C.sub.6 alkyl;each of R.sub.3 to R.sub.8 is independently hydrogen, halogen, C.sub.1 -C.sub.6 -alkyl, C.sub.3 -C.sub.4 alkenyloxy or C.sub.1 -C.sub.6 alkoxy; and the pharmaceutically acceptable salts thereof, which are useful as immunomodulating and anti-viral agents.

Abstract: Penem derivatives are disclosed characterized by a substituted pyridiniomethyl group in the 2-position of the penem nucleus. The compounds of the present application exhibit better antibacterial activity than other known penem derivatives.

Abstract: The present invention relates to an automatic sampling apparatus for sample injection into a gas chromatographic column. In order to allow automatic injection with a non-vaporizing direct on-column injector, the apparatus includes a switch valve, an on-column injector, and a pre-column each having a passage with a diameter greater than 0.5 mm for receiving the injection syringe. The present invention also relates to a device provided with a series of small arms for driving the needle during injection, a switch valve constructed and arranged in a manner to prevent any contamination of the injector by the sample during the injection step, as well as an injection method which can be used with the apparatus and switch valve.

Abstract: Carboxy-thiazolo[3,2-a]pyrimidine derivatives, and pharmaceutical compositions containing them. The compounds and compositions possess anti-allergic activity.

Abstract: A new antitumor anthracycline glycoside, 4-demethoxy-13-dihydrodaunorubicin, is disclosed.The new compound is prepared by reduction of the side-chain ketone function of the known 4-demethoxydaunorubicin, with sodium borohydride in aqueous solution at room temperature.

Abstract: Compounds of the formula (I) ##STR1## wherein the symbol represents a single or a double bond;each of R.sub.1, R.sub.2, R.sub.3 and R.sub.4, which may be the same or different is(a) hydrogen; hydroxy; halogen; cyano; C.sub.1 -C.sub.6 alkyl; C.sub.1 -C.sub.6 alkoxy; a C.sub.2 -C.sub.4 acyl or C.sub.2 -C.sub.4 acylamino group; --SR', --N(R') (R"), --CH.sub.2 OR', --COR or --CH.sub.2 COR, wherein R is OR' or --N(R') (R") and each of R' and R", being the same or different, is hydrogen or C.sub.1 -C.sub.6 alkyl; or(b) one of R.sub.1, R.sub.2, R.sub.3 and R.sub.4 is 5-tetrazolyl or a group selected from --COCH.sub.2 OR', --CH.dbd.C(R')--COR and --X--C(R')(R")--COR, wherein R, R' and R" are as defined above, and X is --O--, --S--, or --NH--, and the others are as defined above under (a);R.sub.5 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl, or a phenyl or 3-pyridyl ring, wherein the phenyl or pyridyl ring is unsubstituted or substituted by one to three substituents chosen from hydroxy and C.sub.

Abstract: (.+-.)4-demethoxy-6(and-11-)-deoxydaunomycinone which are starting materials for anthracycline antitumor antibiotics are prepared by reacting 1,2,3,6-tetrahydrophthalic anhydride with an alcohol of the formula ROH, wherein R is lower alkyl, substituted lower alkyl or aryl to form a monoester, subjecting the monoester to a Friedel-Crafts reaction with acetyl chloride, followed by mild alkaline treatment, to give the corresponding .alpha.,.beta. unsaturated ketone, catalytically reducing same to form the corresponding 4-acetyl-perhydrophthalate reacting the latter with 1,4-dimethoxynaphthalone in the presence of tritluoroacetic anhydride and trifluoroacetic acid to form a mixture of two isomeric compounds, submitting said mixture of isomers to a catalytic reduction of the benzylic carbonyl function, followed by treatment thereof with sulphuric acid at room temperature to afford a mixture of tetracyclic isomers, treating the mixture of tetracyclic isomers with sulphuric acid at 80.degree. C.